Molecules

Editorial

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6 pages, 221 KiB

Open AccessEditorial

Special Issue “Plant Extracts: Biological and Pharmacological Activity”

by Raffaele Capasso and Lorenzo Di Cesare Mannelli

Molecules 2020, 25(21), 5131; https://doi.org/10.3390/molecules25215131 - 4 Nov 2020

Cited by 3 | Viewed by 2448

Abstract

The use of plant extracts for therapeutic purposes knows a wide diffusion [...] Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

Research

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21 pages, 4413 KiB

Open AccessArticle

Ulva intestinalis Protein Extracts Promote In Vitro Collagen and Hyaluronic Acid Production by Human Dermal Fibroblasts

by Justine Bodin, Amandine Adrien, Pierre-Edouard Bodet, Delphine Dufour, Stanislas Baudouin, Thierry Maugard and Nicolas Bridiau

Molecules 2020, 25(9), 2091; https://doi.org/10.3390/molecules25092091 - 30 Apr 2020

Cited by 18 | Viewed by 5573

Abstract

With the increase in life expectancy, reducing the visible signs of skin aging has become a major issue. A reduction in collagen and hyaluronic acid synthesis by fibroblasts is a feature of skin aging. The green seaweed, Ulva intestinalis, is an abundant [...] Read more.

With the increase in life expectancy, reducing the visible signs of skin aging has become a major issue. A reduction in collagen and hyaluronic acid synthesis by fibroblasts is a feature of skin aging. The green seaweed, Ulva intestinalis, is an abundant and rich source of nutrients, especially proteins and peptides. The aim of this study was to assess the potential cosmetic properties of a protein fraction from Ulva intestinalis (PROT-1) containing 51% of proteins and 22% of polysaccharides, and its enzymatic peptide hydrolysates on human dermal fibroblasts. PROT-1 was extracted using a patented acid- and solvent-free process (FR2998894 (B1)). The biochemical characterization and chromatographic analysis showed a main set of proteins (25 kDa). To demonstrate the anti-aging potential of PROT-1, fibroblast proliferation and collagen and hyaluronic acid production were assessed on fibroblast cell lines from donors aged 20 years (CCD-1059Sk) and 46 years (CCD-1090Sk). PROT-1 induced a significant increase in collagen and hyaluronic acid production per cell, and a reduction in cell proliferation without increasing cell mortality. These effects were reversed after protein hydrolysis of PROT-1, showing the central role of proteins in this promising anti-aging property. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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14 pages, 937 KiB

Open AccessArticle

Mulberry Fruit Cultivar ‘Chiang Mai’ Prevents Beta-Amyloid Toxicity in PC12 Neuronal Cells and in a Drosophila Model of Alzheimer’s Disease

by Uthaiwan Suttisansanee, Somsri Charoenkiatkul, Butsara Jongruaysup, Somying Tabtimsri, Dalad Siriwan and Piya Temviriyanukul

Molecules 2020, 25(8), 1837; https://doi.org/10.3390/molecules25081837 - 16 Apr 2020

Cited by 34 | Viewed by 4951

Abstract

Alzheimer’s disease (AD) is the most common form of dementia, characterized by chronic neuron loss and cognitive problems. Aggregated amyloid beta (Aβ) peptides, a product of cleaved amyloid precursor protein (APP) by beta-secretase 1 (BACE-1), have been indicated for the progressive pathogenesis of [...] Read more.

Alzheimer’s disease (AD) is the most common form of dementia, characterized by chronic neuron loss and cognitive problems. Aggregated amyloid beta (Aβ) peptides, a product of cleaved amyloid precursor protein (APP) by beta-secretase 1 (BACE-1), have been indicated for the progressive pathogenesis of AD. Currently, screening for anti-AD compounds in foodstuffs is increasing, with promising results. Hence, the purpose of this study was to investigate the extraction conditions, phytochemical contents, and anti-AD properties, targeting Aβ peptides of Morus cf. nigra ‘Chiang Mai’ (MNCM) both in vitro and in vivo. Data showed that the aqueous extract of MNCM contained high amounts of cyanidin, keracyanin, and kuromanin as anthocyanidin and anthocyanins. The extract also strongly inhibited cholinesterases and BACE-1 in vitro. Moreover, MNCM extract prevented Aβ-induced neurotoxicity and promoted neurite outgrowth in neuronal cells. Interestingly, MNCM extract reduced Aβ_1–42 peptides and improved locomotory coordination of Drosophila co-expressing human APP and BACE-1, specifically in the brain. These findings suggest that MNCM may be useful as an AD preventive agent by targeting Aβ formation. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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14 pages, 2809 KiB

Open AccessArticle

Inhibitory Effects of Aucklandia lappa Decne. Extract on Inflammatory and Oxidative Responses in LPS-Treated Macrophages

by Jae Sung Lim, Sung Ho Lee, Sang Rok Lee, Hyung-Ju Lim, Yoon-Seok Roh, Eun Jeong Won, Namki Cho, Changju Chun and Young-Chang Cho

Molecules 2020, 25(6), 1336; https://doi.org/10.3390/molecules25061336 - 15 Mar 2020

Cited by 14 | Viewed by 4589

Abstract

Aucklandia lappa Decne., known as “Mok-hyang” in Korea, has been used for the alleviation of abdominal pain, vomiting, diarrhea, and stress gastric ulcers in traditional oriental medicine. We investigated the anti-inflammatory and antioxidative effects of the ethanol extract of Aucklandia lappa Decne. (ALDE) [...] Read more.

Aucklandia lappa Decne., known as “Mok-hyang” in Korea, has been used for the alleviation of abdominal pain, vomiting, diarrhea, and stress gastric ulcers in traditional oriental medicine. We investigated the anti-inflammatory and antioxidative effects of the ethanol extract of Aucklandia lappa Decne. (ALDE) in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. ALDE significantly inhibited the LPS-induced nitric oxide (NO) production and reduced inducible nitric oxide synthase (iNOS) expression in RAW 264.7 cells. The production of other proinflammatory mediators, including COX-2, interleukin (IL)-6, IL-1β, and tumor necrosis factor (TNF)-α, was reduced by ALDE in LPS-stimulated RAW 264.7 cells. The mechanism underlying the anti-inflammatory effects of ALDE was elucidated to be the suppression of LPS-induced nuclear translocation of p65, followed by the degradation of IκB and the inhibition of the phosphorylation of mitogen-activated protein kinases (MAPK). In addition, ALDE showed enhanced radical scavenging activity. The antioxidant effect of ALDE was caused by the enhanced expression of heme oxygenase (HO-1) via stabilization of the expression of the nuclear transcription factor E2-related factor 2 (Nrf2) pathway. Collectively, these results indicated that ALDE not only exerts anti-inflammatory effects via the suppression of the NF-κB and MAPK pathways but also has an antioxidative effect through the activation of the Nrf2/HO-1 pathway. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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18 pages, 3696 KiB

Open AccessArticle

Bioadhesive Polymeric Films Based on Red Onion Skins Extract for Wound Treatment: An Innovative and Eco-Friendly Formulation

by Cinzia Pagano, Maura Marinozzi, Claudio Baiocchi, Tommaso Beccari, Paola Calarco, Maria Rachele Ceccarini, Michela Chielli, Ciriana Orabona, Elena Orecchini, Roberta Ortenzi, Maurizio Ricci, Stefania Scuota, Maria Cristina Tiralti and Luana Perioli

Molecules 2020, 25(2), 318; https://doi.org/10.3390/molecules25020318 - 13 Jan 2020

Cited by 34 | Viewed by 6916

Abstract

The onion non-edible outside layers represent a widely available waste material deriving from its processing and consumption. As onion is a vegetable showing many beneficial properties for human health, a study aiming to evaluate the use of extract deriving from the non-edible outside [...] Read more.

The onion non-edible outside layers represent a widely available waste material deriving from its processing and consumption. As onion is a vegetable showing many beneficial properties for human health, a study aiming to evaluate the use of extract deriving from the non-edible outside layers was planned. An eco-friendly extraction method was optimized using a hydroalcoholic solution as solvent. The obtained extract was deeply characterized by in vitro methods and then formulated in autoadhesive, biocompatible and pain-free hydrogel polymeric films. The extract, very soluble in water, showed antioxidant, radical scavenging, antibacterial and anti-inflammatory activities, suggesting a potential dermal application for wounds treatment. In vitro studies showed a sustained release of the extract from the hydrogel polymeric film suitable to reach concentrations necessary for both antibacterial and anti-inflammatory activities. Test performed on human keratinocytes showed that the formulation is safe suggesting that the projected formulation could be a valuable tool for wound treatment. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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12 pages, 669 KiB

Open AccessArticle

Chemical Composition, Antimicrobial, Antioxidant, and Antiproliferative Properties of Grapefruit Essential Oil Prepared by Molecular Distillation

by Weihui Deng, Ke Liu, Shan Cao, Jingyu Sun, Balian Zhong and Jiong Chun

Molecules 2020, 25(1), 217; https://doi.org/10.3390/molecules25010217 - 5 Jan 2020

Cited by 110 | Viewed by 9930

Abstract

Grapefruit essential oil has been proven to have wide range of bioactivities. However, bioactivity of its molecular distillate has not been well studied. In this study, a light phase oil was obtained by molecular distillation from cold-pressed grapefruit essential oil and GC-MS was [...] Read more.

Grapefruit essential oil has been proven to have wide range of bioactivities. However, bioactivity of its molecular distillate has not been well studied. In this study, a light phase oil was obtained by molecular distillation from cold-pressed grapefruit essential oil and GC-MS was used to identify its chemical composition. The antimicrobial activity of the light phase oil was tested by filter paper diffusion method, and the anticancer activity was determined by the Cell Counting Kit-8 (CCK-8) assay. Twenty-four components were detected with a total relative content of 99.74%, including 97.48% of terpenes and 1.66% of oxygenated terpenes. The light phase oil had the best antimicrobial effect on Bacillus subtilis, followed by Escherichia coli, Staphylococcus aureus and Salmonellaty phimurium. DPPH and ABTS assays demonstrated that the light phase oil had good antioxidant activity. The CCK-8 assay of cell proliferation showed that the light phase oil had a good inhibitory effect on the proliferation of HepG2 liver cancer cells and HCT116 colon cancer cells. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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9 pages, 3190 KiB

Open AccessArticle

Inhibitory Effect of Osthole from Cnidium monnieri on Tobacco Mosaic Virus (TMV) Infection in Nicotiana glutinosa

by Ya-Han Chen, Dong-Sheng Guo, Mei-Huan Lu, Jian-Ying Yue, Yan Liu, Chun-Ming Shang, De-Rong An and Ming-Min Zhao

Molecules 2020, 25(1), 65; https://doi.org/10.3390/molecules25010065 - 24 Dec 2019

Cited by 28 | Viewed by 4215

Abstract

The coumarin compound of osthole was extracted from Cnidium monnieri and identified by LC-MS and ¹H- and ¹³C-NMR. Osthole was tested for anti-virus activity against tobacco mosaic virus (TMV) using the half-leaf method. The results showed that stronger antiviral activity on [...] Read more.

The coumarin compound of osthole was extracted from Cnidium monnieri and identified by LC-MS and ¹H- and ¹³C-NMR. Osthole was tested for anti-virus activity against tobacco mosaic virus (TMV) using the half-leaf method. The results showed that stronger antiviral activity on TMV infection appeared in Nicotiana glutinosa than that of eugenol and ningnanmycin, with inhibitory, protective, and curative effects of 72.57%, 70.26%, and 61.97%, respectively. Through observation of the TMV particles, we found that osthole could directly affect the viral particles. Correspondingly, the level of coat protein detected by Western blot was significantly reduced when the concentrations of osthole increased in tested plants compared to that of the control. These results suggest that osthole has anti-TMV activity and may be used as a biological reagent to control the plant virus in the half-leaf method. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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12 pages, 2329 KiB

Open AccessArticle

Study on the Antinociceptive Activity and Mechanism of Action of Isolated Saponins from Siolmatra brasiliensis (Cogn.) Baill

by Thais Biondino Sardella Giorno, Carlos Henrique Corrêa dos Santos, Mario Geraldo de Carvalho, Virgínia Cláudia da Silva, Paulo Teixeira de Sousa, Jr., Patricia Dias Fernandes and Fabio Boylan

Molecules 2019, 24(24), 4584; https://doi.org/10.3390/molecules24244584 - 14 Dec 2019

Cited by 7 | Viewed by 2996

Abstract

Infusions of roots of Siolmatra brasiliensis (Cogn.) Baill, (“taiuiá”, “cipó-tauá”) are used for toothache pain and ulcers. We aimed to study the antinociceptive effects and identify the possible mechanism of action of this plant and its isolated substances (cayaponoside A1, cayaponoside B4, cayaponoside [...] Read more.

Infusions of roots of Siolmatra brasiliensis (Cogn.) Baill, (“taiuiá”, “cipó-tauá”) are used for toothache pain and ulcers. We aimed to study the antinociceptive effects and identify the possible mechanism of action of this plant and its isolated substances (cayaponoside A1, cayaponoside B4, cayaponoside D, and siolmatroside I). Hydroethanol extract (HE), ethyl acetate fraction (EtOAc), and isolated saponins were evaluated in chemical and thermal models of pain in mice. Animals were orally pretreated and evaluated in the capsaicin- or glutamate-induced licking and in the hot plate tests. The antinociceptive mechanism of action was evaluated using the hot plate test with the following pretreatments: Atropine (cholinergic antagonist), naloxone (opioid antagonist), or L-NAME (nitric oxide synthase inhibitor). All extracts and isolated saponins increased the area under the curve in the hot plate test. Tested substances induced a higher effect than the morphine-treated group. Our data suggest that stems of S. brasiliensis and their isolated substances present antinociceptive effects. Cholinergic and opioidergic pathways seem to be involved in their mechanism of action. Taken together our data corroborate the traditional use of the plant and expands the information regarding its use. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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17 pages, 8406 KiB

Open AccessArticle

Antimicrobial Activity and Chemical Constitution of the Crude, Phenolic-Rich Extracts of Hibiscus sabdariffa, Brassica oleracea and Beta vulgaris

by Seham Abdel-Shafi, Abdul-Raouf Al-Mohammadi, Mahmoud Sitohy, Basma Mosa, Ahmed Ismaiel, Gamal Enan and Ali Osman

Molecules 2019, 24(23), 4280; https://doi.org/10.3390/molecules24234280 - 24 Nov 2019

Cited by 61 | Viewed by 6796

Abstract

Crude, phenolic-rich extracts (CPREs) were isolated from different sources, such as Hibiscus sabdariffa (H. sabdariffa), Brassica oleracea var. capitata f. rubra (B. oleracea) and Beta vulgaris (B. vulgaris) and characterized. These CPREs showed potential antibacterial and antifungal activities. H. sabdariffa CPRE (HCPRE) [...] Read more.

Crude, phenolic-rich extracts (CPREs) were isolated from different sources, such as Hibiscus sabdariffa (H. sabdariffa), Brassica oleracea var. capitata f. rubra (B. oleracea) and Beta vulgaris (B. vulgaris) and characterized. These CPREs showed potential antibacterial and antifungal activities. H. sabdariffa CPRE (HCPRE) is the most potent, as it inhibited all tested bacteria and fungi. Total anthocyanins content (TAC), total phenolic content (TPC) and total flavonoid content (TFC) were estimated in all three CPREs. H. sabdariffa contained 4.2 mg/100 g TAC, 2000 mg/100 g of TPC and 430 mg/100 g of TFC in a dry weight sample. GC–MS analysis of HCPRE showed 10 different active compounds that have antimicrobial effects against pathogenic bacteria and fungi, especially alcoholic compounds, triazine derivatives and esters. Scanning and transmission electron microscopy images of Staphylococcus aureus DSM 1104 and Klebsiella pneumonia ATCC 43816 treated with HCPRE (50 μg/mL) exhibited signs of asymmetric, wrinkled exterior surfaces, cell deformations and loss of cell shapes; and adherence of lysed cell content led to cell clumping, malformations, blisters, cell depressions and diminished cell numbers. This indicates death of bacterial cells and loss of cell contents. Aspergillus ochraceus EMCC516 (A. ochraceus, when treated with 100 μg/mL of HCPRE showed irregular cell organelles and cell vacuolation. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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12 pages, 1767 KiB

Open AccessCommunication

Anti-Amyloidogenic and Cyclooxygenase Inhibitory Activity of Guettarda speciosa

by Mario A. Tan, Mark Wilson D. Lagamayo, Grecebio Jonathan D. Alejandro and Seong Soo A. An

Molecules 2019, 24(22), 4112; https://doi.org/10.3390/molecules24224112 - 14 Nov 2019

Cited by 13 | Viewed by 4341

Abstract

Guettarda speciosa is known in traditional folk medicine for treating cough, cold, sore throat, fever, wounds, epilepsy, and headaches. To discover the scientific pharmacological potential of G. speciosa, we explore its anti-inflammatory, cytotoxicity, and inhibition of amyloid-beta (Aβ) aggregation effects. Cyclooxygenase [...] Read more.

Guettarda speciosa is known in traditional folk medicine for treating cough, cold, sore throat, fever, wounds, epilepsy, and headaches. To discover the scientific pharmacological potential of G. speciosa, we explore its anti-inflammatory, cytotoxicity, and inhibition of amyloid-beta (Aβ) aggregation effects. Cyclooxygenase assay of the G. speciosa CHCl₃ (GSC) extract and G. speciosa MeOH (GSM) extract are more selective to COX-1 inhibition with a 50% inhibitory concentration (IC₅₀) of 3.56 μg/mL for the GSC extract and 4.98 μg/mL for the GSM extract. Neuroblastoma SH-SY5Y inhibition and thioflavin T assay amyloid-beta (Aβ) aggregate inhibition of the GSM and GSC extracts showed their potential therapeutic effects against Alzheimer’s disease. The putative compounds from the LC-MS analysis could be responsible for the observed activities. The results suggest that G. speciosa possesses anti-inflammatory and anti-neurodegenerative properties and a promising lead as a source of pharmacologically active compounds. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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12 pages, 1369 KiB

Open AccessArticle

Antioxidant, Xanthine Oxidase, α-Amylase and α-Glucosidase Inhibitory Activities of Bioactive Compounds from Rumex crispus L. Root

by Truong Ngoc Minh, Truong Mai Van, Yusuf Andriana, Le The Vinh, Dang Viet Hau, Dang Hong Duyen and Chona de Guzman-Gelani

Molecules 2019, 24(21), 3899; https://doi.org/10.3390/molecules24213899 - 29 Oct 2019

Cited by 28 | Viewed by 4458

Abstract

The root of Rumex crispus L. has been shown to possess anti-gout and anti-diabetic properties, but the compounds responsible for these pharmaceutical effects have not yet been reported. In this study, we aimed to isolate and purify active components from the root of [...] Read more.

The root of Rumex crispus L. has been shown to possess anti-gout and anti-diabetic properties, but the compounds responsible for these pharmaceutical effects have not yet been reported. In this study, we aimed to isolate and purify active components from the root of R. crispus, and to evaluate their anti-radical, anti-gout and anti-diabetic capacities. From the ethyl acetate (EtOAc) extract, two compounds, chrysophanol (1) and physcion (2), were isolated by column chromatography with an elution of hexane and EtOAc at a 9:1 ratio. Their structures were identified by spectrometric techniques including gas chromatography-mass spectrometry (GC-MS), electrospray ionization-mass spectrometry (ESI-MS), X-ray diffraction analyses and nuclear magnetic resonance (NMR). The results of bioassays indicated that (1) showed stronger activities than (2). For antioxidant activity, (1) and (2) exhibited remarkable DPPH radical scavenging capacity (IC₅₀ = 9.8 and 12.1 µg/mL), which was about two times stronger than BHT (IC₅₀ = 19.4 µg/mL). The anti-gout property of (1) and (2) were comparable to the positive control allopurinol, these compounds exerted strong inhibition against the activity of xanthine oxidase (IC₅₀ = 36.4 and 45.0 µg/mL, respectively). In the anti-diabetic assay, (1) and (2) displayed considerable inhibitory ability on α-glucosidase, their IC₅₀ values (IC₅₀ = 20.1 and 18.9 µg/mL, respectively) were higher than that of standard acarbose (IC₅₀ = 143.4 µg/mL). Findings of this study highlight that (1) and (2) may be promising agents to treat gout and diabetes, which may greatly contribute to the medicinal properties of Rumex crispus root. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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17 pages, 1828 KiB

Open AccessArticle

In-Vitro Antioxidant, Hypoglycemic Activity, and Identification of Bioactive Compounds in Phenol-Rich Extract from the Marine Red Algae Gracilaria edulis (Gmelin) Silva

by Thilina L. Gunathilaka, Kalpa W. Samarakoon, P. Ranasinghe and L. Dinithi C. Peiris

Molecules 2019, 24(20), 3708; https://doi.org/10.3390/molecules24203708 - 15 Oct 2019

Cited by 49 | Viewed by 5977

Abstract

Obesity and diabetes are major metabolic disorders which are prevalent worldwide. Algae has played an important role in managing these disorders. In this study, Gracilaria edulis, a marine red algae, was investigated for antioxidant and hypoglycemic potential using in vitro models. De-polysaccharide [...] Read more.

Obesity and diabetes are major metabolic disorders which are prevalent worldwide. Algae has played an important role in managing these disorders. In this study, Gracilaria edulis, a marine red algae, was investigated for antioxidant and hypoglycemic potential using in vitro models. De-polysaccharide methanol extract of G. edulis was sequentially partitioned with hexane, chloroform, ethyl acetate, and antioxidants, and hypoglycemic potentials were evaluated using multiple methods. High antioxidant potential was observed in the ethyl acetate fraction in terms of ferric reducing antioxidant power, iron chelating, and DPPH and ABTS radical scavenging activities, while the crude methanol extract exhibited potent oxygen radical-absorbance capacity. Potent α-amylase inhibitory activity was observed in the ethyl acetate fraction, while the ethyl acetate fraction was effective against α-glucosidase inhibition. Glucose diffusion was inhibited by the ethyl acetate fraction at 180 min, and the highest antiglycation activity was observed in both chloroform and ethyl acetate fractions. Additionally, gas chromatography-mass spectrometry analysis of the ethyl acetate fraction revealed the presence of several potent anti-diabetic compounds. In conclusion, G. edulis exhibited promising antidiabetic potential via multiple mechanisms. The ethyl acetate fraction exhibited the strongest hypoglycemic and antiglycation potential among the four fractions, and hence the isolation of active compounds is required to develop leads for new drugs to treat diabetes. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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11 pages, 2935 KiB

Open AccessArticle

Anticancer Activity of Smallanthus sonchifolius Methanol Extract against Human Hepatocellular Carcinoma Cells

by Phyu Phyu Myint, Thien T. P. Dao and Yeong Shik Kim

Molecules 2019, 24(17), 3054; https://doi.org/10.3390/molecules24173054 - 22 Aug 2019

Cited by 16 | Viewed by 4913

Abstract

Background: This research aimed to investigate the cytotoxicity of methanol extract of Smallanthus sonchifolius leaf (YLE) against a human hepatocellular carcinoma cell line (HepG2). This plant is currently used as a traditional herbal remedy in the treatment of liver diseases in some rural [...] Read more.

Background: This research aimed to investigate the cytotoxicity of methanol extract of Smallanthus sonchifolius leaf (YLE) against a human hepatocellular carcinoma cell line (HepG2). This plant is currently used as a traditional herbal remedy in the treatment of liver diseases in some rural parts of Myanmar. Methods: The cytotoxic activity of the plant extract against the cancerous cell line was assessed using an MTT assay. YLE demonstrated a significant effect (IC50 = 58.2 ± 1.9 μg/mL) on anti-cancer activity, which was further investigated using various assays including an in vitro cell migration assay, a colony formation assay, cell cycle analysis, western blot analysis, and a ROS assay. The significance of the phytochemical constituents of YLE could be identified using LC/Q-TOF-MS techniques. Results: We putatively identified the active components in YLE, which were possibly melampolide-type sesquiterpenoids. YLE showed an inhibitory effect on HepG2 cell proliferation and cell migration. YLE also induced cell cycle arrest and necrosis in a dose-dependent manner. Additionally, YLE significantly suppressed ROS formation in HepG2 cells. Conclusions: These findings suggest that YLE is sufficient for application as a promising anti-liver drug in herbal medicine. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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14 pages, 2333 KiB

Open AccessFeature PaperArticle

Protective Effects Induced by Two Polyphenolic Liquid Complexes from Olive (Olea europaea, mainly Cultivar Coratina) Pressing Juice in Rat Isolated Tissues Challenged with LPS

by Lucia Recinella, Annalisa Chiavaroli, Giustino Orlando, Luigi Menghini, Claudio Ferrante, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Luigi Brunetti and Sheila Leone

Molecules 2019, 24(16), 3002; https://doi.org/10.3390/molecules24163002 - 19 Aug 2019

Cited by 24 | Viewed by 3731

Abstract

MOMAST^(®) HY100 and MOMAST^(®) HP30 are polyphenolic liquid complexes from olive pressing juice with a total polyphenolic content of 100 g/kg (at least 50% as hydroxytyrosol) and 36 g/kg (at least 30% as hydroxytyrosol), respectively. We investigated the potential protective role [...] Read more.

MOMAST^(®) HY100 and MOMAST^(®) HP30 are polyphenolic liquid complexes from olive pressing juice with a total polyphenolic content of 100 g/kg (at least 50% as hydroxytyrosol) and 36 g/kg (at least 30% as hydroxytyrosol), respectively. We investigated the potential protective role of MOMAST^(®) HY100 and MOMAST^(®) HP30 on isolated rat colon, liver, heart, and prefrontal cortex specimens treated with Escherichia coli lipopolysaccharide (LPS), a validated ex vivo model of inflammation, by measuring the production of prostaglandin (PG)E₂, 8-iso-PGF_2α, lactate dehydrogenase (LDH), as well as cyclooxygenase (COX)-2, tumor necrosis factor α (TNFα), and inducible nitric oxide synthase (iNOS) mRNA levels. MOMAST^(®) HY100 decreased LPS-stimulated PGE₂ and LDH levels in all tested tissues. Following treatment with MOMAST^(®) HY100, we found a significant reduction in iNOS levels in prefrontal cortex and heart specimens, COX-2 and TNFα mRNA levels in heart specimens, and 8-iso-PGF_2α levels in liver specimens. On the other hand, MOMAST^(®) HP30 was found to blunt COX-2, TNFα, and iNOS mRNA levels, as well as 8-iso-PGF_2α in cortex, liver, and colon specimens. MOMAST^(®) HP30 was also found to decrease PGE₂ levels in liver specimens, while it decreased iNOS mRNA, LDH, and 8-iso-PGF_2α levels in heart specimens. Both MOMAST^(®) HY100 and MOMAST^(®) HP30 exhibited protective effects on multiple inflammatory and oxidative stress pathways. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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21 pages, 4608 KiB

Open AccessArticle

Potential Photoprotective Effect of Dietary Corn Silk Extract on Ultraviolet B-Induced Skin Damage

by Yeon-hee Kim, Amy Cho, Sang-Ah Kwon, Minju Kim, Mina Song, Hye won Han, Eun-Ji Shin, Eunju Park and Seung-Min Lee

Molecules 2019, 24(14), 2587; https://doi.org/10.3390/molecules24142587 - 16 Jul 2019

Cited by 21 | Viewed by 5996

Abstract

Ultraviolet B (UVB) irradiation causes adverse effects on the skin. Corn silk contains flavonoids and other bioactive compounds and antioxidants, which may prevent skin photoaging through antioxidant and anti-inflammatory effects. We aimed to investigate the potential photoprotective effects of dietary corn silk on [...] Read more.

Ultraviolet B (UVB) irradiation causes adverse effects on the skin. Corn silk contains flavonoids and other bioactive compounds and antioxidants, which may prevent skin photoaging through antioxidant and anti-inflammatory effects. We aimed to investigate the potential photoprotective effects of dietary corn silk on UVB-induced skin damage in mice and the mechanisms behind these effects on human skin cells. Oral administration of corn silk water extract (CS) (2 or 4 g/kg/day) for 19 weeks decreased epidermal thickness, wrinkle formation, and positive staining for PCNA, Ki67, and 8-OHdG, and increased collagen staining in UVB-irradiated SKH-1 hairless mice compared with controls. The pro-inflammatory NF-κB target genes (IL-1β, iNOS, and COX-2) and MMP-9 expressions were lower in the CS groups, and TGF-β/Smad signaling increased. Low skin lipid peroxidation and blood DNA oxidation levels and high blood glutathione were detected. Antioxidant transcription factor Nrf2-related catalase and SOD1 proteins and glutaredoxin mRNA levels increased. The results of CS extract treatment and UVB irradiation in HaCaT cells showed the same results in Nrf2 and NF-κB target genes. An LC-MS/MS analysis showed that the CS extract contained potential antioxidants, which might have contributed to its anti-photoaging effects in tissues and cells. CS extract may reduce UVB-induced skin damage through antioxidant and anti-inflammatory mechanisms. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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25 pages, 3265 KiB

Open AccessArticle

Comprehensive Chemical Profiling and Multidirectional Biological Investigation of Two Wild Anthemis Species (Anthemis tinctoria var. Pallida and A. cretica subsp. tenuiloba): Focus on Neuroprotective Effects

by Giustino Orlando, Gokhan Zengin, Claudio Ferrante, Maurizio Ronci, Lucia Recinella, Ismail Senkardes, Reneta Gevrenova, Dimitrina Zheleva-Dimitrova, Annalisa Chiavaroli, Sheila Leone, Simonetta Di Simone, Luigi Brunetti, Carene Marie Nancy Picot-Allain, Mohamad Fawzi Mahomoodally, Kouadio Ibrahime Sinan and Luigi Menghini

Molecules 2019, 24(14), 2582; https://doi.org/10.3390/molecules24142582 - 16 Jul 2019

Cited by 26 | Viewed by 4156

Abstract

Ethyl acetate (EA), methanol (MeOH), and aqueous extracts of aerial parts of Anthemis tinctoria var. pallida (ATP) and A. cretica subsp. tenuiloba (ACT) were investigated for their phenol and flavonoid content, antioxidant, and key enzyme inhibitory potentials. All extracts displayed antiradical effects, with [...] Read more.

Ethyl acetate (EA), methanol (MeOH), and aqueous extracts of aerial parts of Anthemis tinctoria var. pallida (ATP) and A. cretica subsp. tenuiloba (ACT) were investigated for their phenol and flavonoid content, antioxidant, and key enzyme inhibitory potentials. All extracts displayed antiradical effects, with MeOH and aqueous extracts being a superior source of antioxidants. On the other hand, EA and MeOH extracts were potent against AChE and BChE. Enzyme inhibitory effects against tyrosinase and α-glucosidase were observed, as well. We also studied Anthemis extracts in an ex vivo experimental neurotoxicity paradigm. We assayed extract influence on oxidative stress and neurotransmission biomarkers, including lactate dehydrogenase (LDH) and serotonin (5-HT), in isolated rat cortex challenged with K⁺ 60 mM Krebs-Ringer buffer (excitotoxicity stimulus). An untargeted proteomic analysis was finally performed in order to explore the putative mechanism in the brain. The pharmacological study highlighted the capability of ACT water extract to blunt K⁺ 60 mM increase in LDH level and 5-HT turnover, and restore physiological activity of specific proteins involved in neuron morphology and neurotransmission, including NEFMs, VAMP-2, and PKCγ, thus further supporting the neuroprotective role of ACT water extract. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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17 pages, 1882 KiB

Open AccessArticle

Antioxidant and Hepatoprotective Effects of Croton hypoleucus Extract in an Induced-Necrosis Model in Rats

by Thania Alejandra Urrutia-Hernández, Jorge Arturo Santos-López, Juana Benedí, Francisco Jose Sánchez-Muniz, Claudia Velázquez-González, Minarda De la O-Arciniega, Osmar Antonio Jaramillo-Morales and Mirandeli Bautista

Molecules 2019, 24(14), 2533; https://doi.org/10.3390/molecules24142533 - 11 Jul 2019

Cited by 13 | Viewed by 3680

Abstract

The aim of this study was to evaluate the antioxidant and hepatoprotective activity of Croton hypoleucus (EC). The present work reports the first pharmacological, toxicological, and antioxidant studies of EC extract on liver injury. Liver necrosis was induced by thioacetamide (TAA). Five groups [...] Read more.

The aim of this study was to evaluate the antioxidant and hepatoprotective activity of Croton hypoleucus (EC). The present work reports the first pharmacological, toxicological, and antioxidant studies of EC extract on liver injury. Liver necrosis was induced by thioacetamide (TAA). Five groups were established: Croton Extract (EC), thioacetamide (TAA), Croton extract with thioacetamide (EC + TAA), vitamin E with thioacetamide (VE + TAA) and the positive control and vehicle (CT). For EC and EC + TAA, Wistar rats (n = 8) were intragastrically pre-administered for 4 days with EC (300 mg/kg.day) and on the last day, EC + TAA received a single dose of TAA (400 mg/kg). At 24 h after damage induction, animals were sacrificed. In vitro activity and gene expression of superoxide dismutase (SOD), catalase (Cat), and Nrf2 nuclear factor were measured. The results show that EC has medium antioxidant properties, with an IC₅₀ of 0.63 mg/mL and a ferric-reducing power of 279.8 µM/mg. Additionally, EC reduced hepatic damage markers at 24 h after TAA intoxication; also, it increased SOD and Cat gene expression against TAA by controlling antioxidant defense levels. Our findings demonstrated the hepatoprotective effect of EC by reducing hepatic damage markers and controlling antioxidant defense levels. Further studies are necessary to identify the mechanism of this protection. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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17 pages, 5638 KiB

Open AccessArticle

Hepatotoxicity of a Cannabidiol-Rich Cannabis Extract in the Mouse Model

by Laura E. Ewing, Charles M. Skinner, Charles M. Quick, Stefanie Kennon-McGill, Mitchell R. McGill, Larry A. Walker, Mahmoud A. ElSohly, Bill J. Gurley and Igor Koturbash

Molecules 2019, 24(9), 1694; https://doi.org/10.3390/molecules24091694 - 30 Apr 2019

Cited by 105 | Viewed by 137977

Abstract

The goal of this study was to investigate Cannabidiol (CBD) hepatotoxicity in 8-week-old male B6C3F₁ mice. Animals were gavaged with either 0, 246, 738, or 2460 mg/kg of CBD (acute toxicity, 24 h) or with daily doses of 0, 61.5, 184.5, or [...] Read more.

The goal of this study was to investigate Cannabidiol (CBD) hepatotoxicity in 8-week-old male B6C3F₁ mice. Animals were gavaged with either 0, 246, 738, or 2460 mg/kg of CBD (acute toxicity, 24 h) or with daily doses of 0, 61.5, 184.5, or 615 mg/kg for 10 days (sub-acute toxicity). These doses were the allometrically scaled mouse equivalent doses (MED) of the maximum recommended human maintenance dose of CBD in EPIDIOLEX^® (20 mg/kg). In the acute study, significant increases in liver-to-body weight (LBW) ratios, plasma ALT, AST, and total bilirubin were observed for the 2460 mg/kg dose. In the sub-acute study, 75% of mice gavaged with 615 mg/kg developed a moribund condition between days three and four. As in the acute phase, 615 mg/kg CBD increased LBW ratios, ALT, AST, and total bilirubin. Hepatotoxicity gene expression arrays revealed that CBD differentially regulated more than 50 genes, many of which were linked to oxidative stress responses, lipid metabolism pathways and drug metabolizing enzymes. In conclusion, CBD exhibited clear signs of hepatotoxicity, possibly of a cholestatic nature. The involvement of numerous pathways associated with lipid and xenobiotic metabolism raises serious concerns about potential drug interactions as well as the safety of CBD. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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14 pages, 7893 KiB

Open AccessArticle

Ameliorative Effect and Mechanism of the Purified Anthraquinone-Glycoside Preparation from Rheum Palmatum L. on Type 2 Diabetes Mellitus

by Fang-Rong Cheng, Hong-Xin Cui, Ji-Li Fang, Ke Yuan and Ying Guo

Molecules 2019, 24(8), 1454; https://doi.org/10.3390/molecules24081454 - 12 Apr 2019

Cited by 37 | Viewed by 5154

Abstract

Rheum palmatum L. is a traditional Chinese medicine with various pharmacological properties, including anti-inflammatory, antibacterial, and detoxification effects. In this study, the mechanism of the hypoglycemic effect of purified anthraquinone-Glycoside from Rheum palmatum L. (PAGR) in streptozotocin (STZ) and high-fat diet induced type [...] Read more.

Rheum palmatum L. is a traditional Chinese medicine with various pharmacological properties, including anti-inflammatory, antibacterial, and detoxification effects. In this study, the mechanism of the hypoglycemic effect of purified anthraquinone-Glycoside from Rheum palmatum L. (PAGR) in streptozotocin (STZ) and high-fat diet induced type 2 diabetes mellitus (T2DM) in rats was investigated. The rats were randomly divided into normal (NC), T2DM, metformin (Met), low, middle (Mid), and high (Hig) does of PAGR groups. After six weeks of continuous administration of PAGR, the serum indices and tissue protein expression were determined, and the pathological changes in liver, kidney, and pancreas tissues were observed. The results showed that compared with the type 2 diabetes mellitus group, the fasting blood glucose (FBG), total cholesterol (TC), and triglyceride (TG) levels in the serum of rats in the PAGR treatment groups were significantly decreased, while superoxide dismutase (SOD) and glutathione peroxidase (GSH-PX) levels were noticeably increased. The expression of Fas ligand (FasL), cytochrome C (Cyt-c), and caspase-3 in pancreatic tissue was obviously decreased, and the pathological damage to the liver, kidney, and pancreas was improved. These indicate that PAGR can reduce oxidative stress in rats with diabetes mellitus by improving blood lipid metabolism and enhancing their antioxidant capacity, thereby regulating the mitochondrial apoptotic pathway to inhibitβ-cell apoptosis and improve β-cell function. Furthermore, it can regulate Fas/FasL-mediated apoptosis signaling pathway to inhibit β-cell apoptosis, thereby lowering blood glucose levels and improving T2DM. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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10 pages, 2513 KiB

Open AccessArticle

Solvent Fractionation and Acetone Precipitation for Crude Saponins from Eurycoma longifolia Extract

by Lee Suan Chua, Cher Haan Lau, Chee Yung Chew and Dawood Ali Salim Dawood

Molecules 2019, 24(7), 1416; https://doi.org/10.3390/molecules24071416 - 10 Apr 2019

Cited by 26 | Viewed by 6139

Abstract

Eurycoma longifolia is a popular folk medicine in South East Asia. This study was focused on saccharide-containing compounds including saponins, mainly because of their medical potentials. Different organic solvents such as ethyl acetate, butanol, and chloroform were used to fractionate the phytochemical groups, [...] Read more.

Eurycoma longifolia is a popular folk medicine in South East Asia. This study was focused on saccharide-containing compounds including saponins, mainly because of their medical potentials. Different organic solvents such as ethyl acetate, butanol, and chloroform were used to fractionate the phytochemical groups, which were consequently precipitated in cold acetone. Solvent fractionation was found to increase the total saponin content based on colorimetric assay using vanillin and sulfuric acid. Ethyl acetate fraction and its precipitate were showed to have the highest crude saponins after acetone precipitation. The samples were shown to have anti-proliferative activity comparable with tamoxifen (IC₅₀ = 110.6 µg/mL) against human breast cancer cells. The anti-proliferative activities of the samples were significantly improved from crude extract (IC₅₀ = 616.3 µg/mL) to ethyl acetate fraction (IC₅₀ = 185.4 µg/mL) and its precipitate (IC₅₀ = 153.4 µg/mL). LC-DAD-MS/MS analysis revealed that the saccharide-containing compounds such as m/z 497, 610, 723, 836, and 949 were abundant in the samples, and they could be ionized in negative ion mode. The compounds consisted of 226 amu monomers with UV-absorbing property at 254 nm, and were tentatively identified as formylated hexoses. To conclude, solvent fractionation and acetone precipitation could produce saccharide-containing compounds including saponins with higher anti-proliferative activity than crude extract against MCF-7 cells. This is the first study to use non-toxic solvents for fractionation of bioactive compounds from highly complex plant extract of E. longifolia. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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24 pages, 879 KiB

Open AccessArticle

Investigation of the Biological Activities and Characterization of Bioactive Constituents of Ophiorrhiza rugosa var. prostrata (D.Don) & Mondal Leaves through In Vivo, In Vitro, and In Silico Approaches

by Md. Adnan, Md. Nazim Uddin Chy, A.T.M. Mostafa Kamal, Md Obyedul Kalam Azad, Arkajyoti Paul, Shaikh Bokhtear Uddin, James W. Barlow, Mohammad Omar Faruque, Cheol Ho Park and Dong Ha Cho

Molecules 2019, 24(7), 1367; https://doi.org/10.3390/molecules24071367 - 8 Apr 2019

Cited by 108 | Viewed by 7541

Abstract

Ophiorrhiza rugosa var. prostrata is one of the most frequently used ethnomedicinal plants by the indigenous communities of Bangladesh. This study was designed to investigate the antidiarrheal, anti-inflammatory, anthelmintic and antibacterial activities of the ethanol extract of O. rugosa leaves (EEOR). The leaves [...] Read more.

Ophiorrhiza rugosa var. prostrata is one of the most frequently used ethnomedicinal plants by the indigenous communities of Bangladesh. This study was designed to investigate the antidiarrheal, anti-inflammatory, anthelmintic and antibacterial activities of the ethanol extract of O. rugosa leaves (EEOR). The leaves were extracted with ethanol and subjected to in vivo antidiarrheal screening using the castor oil-induced diarrhea, enteropooling, and gastrointestinal transit models. Anti-inflammatory efficacy was evaluated using the histamine-induced paw edema test. In parallel, in vitro anthelmintic and antibacterial activities were evaluated using the aquatic worm and disc diffusion assays respectively. In all three diarrheal models, EEOR (100, 200 and 400 mg/kg) showed obvious inhibition of diarrheal stool frequency, reduction of the volume and weight of the intestinal contents, and significant inhibition of intestinal motility. Also, EEOR manifested dose-dependent anti-inflammatory activity. Anthelmintic action was deemed significant (P < 0.001) with respect to the onset of paralysis and helminth death. EEOR also resulted in strong zones of inhibition when tested against both Gram-positive and Gram-negative bacteria. GC-MS analysis identified 30 compounds within EEOR, and of these, 13 compounds documented as bioactive showed good binding affinities to M3 muscarinic acetylcholine, 5-HT3, tubulin and GlcN-6-P synthase protein targets in molecular docking experiments. Additionally, ADME/T and PASS analyses revealed their drug-likeness, likely safety upon consumption and possible pharmacological activities. In conclusion, our findings scientifically support the ethnomedicinal use and value of this plant, which may provide a potential source for future development of medicines. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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14 pages, 1964 KiB

Open AccessArticle

In Vitro and In Situ Characterization of the Intestinal Absorption of Capilliposide B and Capilliposide C from Lysimachia capillipes Hemsl

by Xu Zhang, Xiao Cheng, Yali Wu, Di Feng, Yifan Qian, Liping Chen, Bo Yang and Mancang Gu

Molecules 2019, 24(7), 1227; https://doi.org/10.3390/molecules24071227 - 28 Mar 2019

Cited by 12 | Viewed by 3250

Abstract

The goal of this investigation was to determine the processes and mechanism of intestinal absorption for capilliposide B (CAPB) and capilliposide C (CAPC) from the Chinese herb, Lysimachia capillipes Hemsl. An analysis of basic parameters, such as drug concentrations, time, and behavior in [...] Read more.

The goal of this investigation was to determine the processes and mechanism of intestinal absorption for capilliposide B (CAPB) and capilliposide C (CAPC) from the Chinese herb, Lysimachia capillipes Hemsl. An analysis of basic parameters, such as drug concentrations, time, and behavior in different intestinal segments was analyzed by liquid chromatography-tandem mass spectrometry (LC-MS). The susceptibility of CAPB and CAPC to various inhibitors such as P-glycoprotein (P-gp) inhibitor (verapamil); multidrug resistance-associated protein 2 (MRP2) inhibitor (indomethacin); cytochrome P450 protein 3A4 (CYP3A4) inhibitor (ketoconazole); and the co-inhibitor of P-gp, MRP2 and CYP3A4 (cyclosporine A) were assessed using both caco-2 cell monolayer and single-pass intestinal perfusion (SPIP) models. As a result, CAPB and CAPC are both poorly absorbed in the intestines and exhibited segment-dependent permeability. The intestinal permeability of CAPB and CAPC were significantly increased by the co-treatment of verapamil, indomethacin. In addition, the intestinal permeability of CAPB was also enhanced by ketoconazole and cyclosporine A. It can be concluded that the intestinal absorption mechanisms of CAPB and CAPC involve processes such as facilitated passive diffusion, efflux transporters, and enzyme-mediated metabolism. Both CAPB and CAPC are suggested to be substrates of P-gp and MRP2. However, CAPB may interact with the CYP3A4 system. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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13 pages, 1948 KiB

Open AccessArticle

3′-O-β-d-glucopyranosyl-α,4,2′,4′,6′-pentahydroxy-dihydrochalcone, from Bark of Eysenhardtia polystachya Prevents Diabetic Nephropathy via Inhibiting Protein Glycation in STZ-Nicotinamide Induced Diabetic Mice

by Rosa Martha Pérez Gutierrez, Abraham Heriberto García Campoy, Silvia Patricia Paredes Carrera, Alethia Muñiz Ramirez, José Maria Mota Flores and Sergio Odin Flores Valle

Molecules 2019, 24(7), 1214; https://doi.org/10.3390/molecules24071214 - 28 Mar 2019

Cited by 15 | Viewed by 4297

Abstract

Previous studies have shown that accumulation of advanced glycation end products (AGEs) can be the cause of diabetic nephropathy (DN) in diabetic patients. Dihydrochalcone 3′-O-β-d-glucopyranosyl α,4,2′,4′,6′-pentahydroxy–dihydrochalcone (1) is a powerful antiglycation compound previously isolated from Eysenhardtia polystachya [...] Read more.

Previous studies have shown that accumulation of advanced glycation end products (AGEs) can be the cause of diabetic nephropathy (DN) in diabetic patients. Dihydrochalcone 3′-O-β-d-glucopyranosyl α,4,2′,4′,6′-pentahydroxy–dihydrochalcone (1) is a powerful antiglycation compound previously isolated from Eysenhardtia polystachya. The aim was to investigate whether (1) was able to protect against diabetic nephropathy in streptozotocin (STZ)-induced diabetic mice, which displayed renal dysfunction markers such as body weight, creatinine, uric acid, serum urea, total urinary protein, and urea nitrogen in the blood (BUN). In addition, pathological changes were evaluated including glycated hemoglobin (HbA1c), advanced glycation end products (AGEs) in the kidney, as well as in circulation level and pro-inflammatory markers ICAM-1 levels in diabetic mice. After 5 weeks, these elevated markers of dihydrochalcone treatment (25, 50 and 100 mg/kg) were significantly (p < 0.05) attenuated. In addition, they ameliorate the indices of renal inflammation as indicated by ICAM-1 markers. The kidney and circulatory AGEs levels in diabetic mice were significantly (p < 0.05) attenuated by (1) treatment. Histological analysis of kidney tissues showed an important recovery in its structure compared with the diabetic group. It was found that the compound (1) attenuated the renal damage in diabetic mice by inhibiting AGEs formation. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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14 pages, 322 KiB

Open AccessArticle

Antioxidant, α-Amylase and α-Glucosidase Inhibitory Activities and Potential Constituents of Canarium tramdenum Bark

by Nguyen Van Quan, Tran Dang Xuan, Hoang-Dung Tran, Nguyen Thi Dieu Thuy, Le Thu Trang, Can Thu Huong, Yusuf Andriana and Phung Thi Tuyen

Molecules 2019, 24(3), 605; https://doi.org/10.3390/molecules24030605 - 9 Feb 2019

Cited by 88 | Viewed by 8587

Abstract

The fruits of Canarium tramdenum are commonly used as foods and cooking ingredients in Vietnam, Laos, and the southeast region of China, whilst the leaves are traditionally used for treating diarrhea and rheumatism. This study was conducted to investigate the potential use of [...] Read more.

The fruits of Canarium tramdenum are commonly used as foods and cooking ingredients in Vietnam, Laos, and the southeast region of China, whilst the leaves are traditionally used for treating diarrhea and rheumatism. This study was conducted to investigate the potential use of this plant bark as antioxidants, and α-amylase and α-glucosidase inhibitors. Five different extracts of C. tramdenum bark (TDB) consisting of the extract (TDBS) and factional extracts hexane (TDBH), ethyl acetate (TDBE), butanol (TDBB), and water (TDBW) were evaluated. The TDBS extract contained the highest amount of total phenolic (112.14 mg gallic acid equivalent per g dry weight), while the TDBB extract had the most effective antioxidant capacity compared to other extracts. Its IC₅₀ values were 12.33, 47.87, 33.25, and 103.74 µg/mL in 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis (ABTS), reducing power (RP), and nitric oxide (NO) assays, respectively. Meanwhile, the lipid peroxidation inhibition of the four above extracts was proximate to that of butylated hydroxytoluene (BHT) as a standard antioxidant. The result of porcine pancreatic α-amylase inhibition showed that TDB extracts have promising effects which are in line with the commercial diabetic inhibitor acarbose. Interestingly, the inhibitory ability on α-glucosidase of all the extracts was higher than that of acarbose. Among the extracts, the TDBB extract expressed the strongest activity on the enzymatic reaction (IC₅₀ = 18.93 µg/mL) followed by the TDBW extract (IC₅₀ = 25.27 µg/mL), TDBS (IC₅₀ = 28.17 µg/mL), and TDBE extract (IC₅₀ = 141.37 µg/mL). The phytochemical constituents of the TDB extract were identified by gas chromatography–mass spectrometry (GC-MS). The principal constituents included nine phenolics, eight terpenoids, two steroids, and five compounds belonging to other chemical classes, which were the first reported in this plant. Among them, the presence of α- and β-amyrins were identified by GC-MS and appeared as the most dominant constituents in TDB extracts (1.52 mg/g). The results of this study revealed that C. tramdenum bark possessed rich phenolics and terpenoids, which might confer on reducing risks from diabetes. A high quantity of α- and β-amyrins highlighted the potentials of anti-inflammatory, anti-ulcer, anti-hyperlipidemic, anti-tumor, and hepatoprotective properties of C. tramdenum bark. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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16 pages, 2214 KiB

Open AccessArticle

Metabolomics Profiling Reveals Rehmanniae Radix Preparata Extract Protects against Glucocorticoid-Induced Osteoporosis Mainly via Intervening Steroid Hormone Biosynthesis

by Tianshuang Xia, Xin Dong, Yiping Jiang, Liuyue Lin, Zhimin Dong, Yi Shen, Hailiang Xin, Qiaoyan Zhang and Luping Qin

Molecules 2019, 24(2), 253; https://doi.org/10.3390/molecules24020253 - 11 Jan 2019

Cited by 33 | Viewed by 5498

Abstract

Rehmanniae Radix Preparata (RR), the dry rhizome of Rehmannia glutinosa Libosch., is a traditional herbal medicine for improving the liver and kidney function. Ample clinical and pharmacological experiments show that RR can prevent post-menopausal osteoporosis and senile osteoporosis. In the present study, in [...] Read more.

Rehmanniae Radix Preparata (RR), the dry rhizome of Rehmannia glutinosa Libosch., is a traditional herbal medicine for improving the liver and kidney function. Ample clinical and pharmacological experiments show that RR can prevent post-menopausal osteoporosis and senile osteoporosis. In the present study, in vivo and in vitro experiments, as well as a UHPLC-Q/TOF-MS-based metabolomics study, were used to explore the preventing effect of RR on glucocorticoid-induced osteoporosis (GIOP) and its underlying mechanisms. As a result, RR significantly enhanced bone mineral density (BMD), improved the micro-architecture of trabecular bone, and intervened in biochemical markers of bone metabolism in dexamethasone (DEX)-treated rats. For the in vitro experiment, RR increased the cell proliferation and alkaline phosphatase (ALP) activity, enhanced the extracellular matrix mineralization level, and improved the expression of runt-related transcription factor 2 (RUNX2) and osteopontin (OPN) in DEX-injured osteoblasts. For the metabolomics study, a total of 27 differential metabolites were detected in the DEX group vs. the control group, of which 10 were significantly reversed after RR treatment. These metabolites were majorly involved in steroid hormone biosynthesis, sex steroids regulation, and amino acid metabolism. By metabolic pathway and Western blotting analysis, it was further ascertained that RR protected against DEX-induced bone loss, mainly via interfering steroid hormone biosynthesis, as evidenced by the up-regulation of cytochrome P450 17A1 (CYP17A1) and aromatase (CYP19A1), and the down-regulation of 11β-hydroxysteroid dehydrogenase (HSD11B1). Collectively, these results indicated that RR had a notable preventing effect on GIOP, and the action mechanism might be related to steroid hormone biosynthesis. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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14 pages, 4383 KiB

Open AccessArticle

Modulatory Effect of Guinep (Melicoccus bijugatus Jacq) Fruit Pulp Extract on Isoproterenol-Induced Myocardial Damage in Rats. Identification of Major Metabolites Using High Resolution UHPLC Q-Orbitrap Mass Spectrometry

by Chukwuemeka R. Nwokocha, Isheba Warren, Javier Palacios, Mario Simirgiotis, Magdalene Nwokocha, Sharon Harrison, Rory Thompson, Adrian Paredes, Jorge Bórquez, Astrid Lavado and Fredi Cifuentes

Molecules 2019, 24(2), 235; https://doi.org/10.3390/molecules24020235 - 10 Jan 2019

Cited by 6 | Viewed by 4263

Abstract

Guinep is traditionally used in the management of cardiovascular ailments. This study aims to evaluate its medicinal constituents and effects in the management of myocardial injury in an experimental isoproterenol (ISO) rat model. Sprague-Dawley rats were randomly assigned to four groups: Group 1 [...] Read more.

Guinep is traditionally used in the management of cardiovascular ailments. This study aims to evaluate its medicinal constituents and effects in the management of myocardial injury in an experimental isoproterenol (ISO) rat model. Sprague-Dawley rats were randomly assigned to four groups: Group 1 was the control group; Group 2 received M. bijugatus extract (100 mg/Kg; MB) for six weeks; Group 3 was given ISO (85 mg/Kg) i.p. twice during a 24-hour period; and Group 4 was given ISO (85 mg/Kg) i.p. and MB extract (100 mg/Kg) for six weeks. The MB was administered orally by gavage, daily. The blood pressure of conscious animals was measured, while ECG was performed under anesthesia. Blood and serum were collected for biochemical and hematological analysis. The ISO group treated with MB showed a significant decrease (p < 0.001) in (SBP), diastolic (DBP), mean arterial (MAP) and heart rate (HR) compared to the ISO only group. Conversely, MB treated rats that were not induced with ISO displayed a significant decreases (p < 0.001) in SBP, DBP, MAP, and HR. ISO significantly elevated the ST segment (p < 0.001) and shortened the QTc interval (p < 0.05), which were recovered after treatment with 100 mg/Kg of MB. In addition, the results showed a significant decrease (p < 0.001) in the heart to body weight ratio of the ISO group treated with MB compared to the ISO only group. Furthermore, the extract normalized the hematological values depressed by the ISO while significantly elevating the platelet count. UHPLC high-resolution orbitrap mass spectrometry analysis results revealed the presence of several antioxidants like vitamin C and related compounds, phenolic acids, flavonoid, fatty acids (oxylipins), and terpene derivatives. The results of this study indicated that Melicoccus bijugatus did display some cardio-protective effects in relation to myocardial injury. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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Jump to: Editorial, Research

28 pages, 3140 KiB

Open AccessReview

Genus Ophiorrhiza: A Review of Its Distribution, Traditional Uses, Phytochemistry, Biological Activities and Propagation

by Muhammad Taher, Siti Syazwani Shaari, Deny Susanti, Dayar Arbain and Zainul Amiruddin Zakaria

Molecules 2020, 25(11), 2611; https://doi.org/10.3390/molecules25112611 - 4 Jun 2020

Cited by 26 | Viewed by 5689

Abstract

Almost 50 species of Ophiorrhiza plants were reviewed in this work and the main objective is to critically analyse their distribution, phytochemical content, biological activity, and propagation. Moreover, the information would be useful in promoting the relevant uses of the plant, especially in [...] Read more.

Almost 50 species of Ophiorrhiza plants were reviewed in this work and the main objective is to critically analyse their distribution, phytochemical content, biological activity, and propagation. Moreover, the information would be useful in promoting the relevant uses of the plant, especially in the medicinal fields based on in vitro and in vivo studies. To this end, scientific sources, including theses, PubMed, Google Scholar, International Islamic University Malaysia IIUM EBSCO, PubChem, and Elsevier, were accessed for publications regarding the Ophiorrhiza genus in this review. Scientific literature regarding the Ophiorrhiza plants revealed their wide distribution across Asia and the neighbouring countries, whereby they were utilised as traditional medicine to treat various diseases. In particular, various active compounds, such as alkaloids, flavonoids, and terpenoids, were reported in the plant. Furthermore, the Ophiorrhiza species showed highly diverse biological activities, such as anti-cancer, antiviral, antimicrobial, and more. The genus propagation reported could produce a high quality and quantity of potent anticancer compound, namely camptothecin (CPT). Hence, it is believed that the relevant uses of natural compounds present in the plants can replace the existing crop of synthetic anticancer drugs associated with a multitude of unbearable side effects. Additionally, more future studies on the Ophiorrhiza species should be undertaken to establish the links between its traditional uses, active compounds, and pharmacological activities reported. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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17 pages, 2201 KiB

Open AccessReview

Bee Products in Dermatology and Skin Care

by Anna Kurek-Górecka, Michał Górecki, Anna Rzepecka-Stojko, Radosław Balwierz and Jerzy Stojko

Molecules 2020, 25(3), 556; https://doi.org/10.3390/molecules25030556 - 28 Jan 2020

Cited by 152 | Viewed by 27988

Abstract

Honey, propolis, bee pollen, bee bread, royal jelly, beeswax and bee venom are natural products which have been used in medicine since ancient times. Nowadays, studies indicate that natural bee products can be used for skin treatment and care. Biological properties of these [...] Read more.

Honey, propolis, bee pollen, bee bread, royal jelly, beeswax and bee venom are natural products which have been used in medicine since ancient times. Nowadays, studies indicate that natural bee products can be used for skin treatment and care. Biological properties of these products are related to flavonoids they contain like: chrysin, apigenin, kaempferol, quercetin, galangin, pinocembrin or naringenin. Several pharmacological activities of phenolic acids and flavonoids, and also 10-hydroxy-trans-2-decenoic acid, which is present in royal jelly, have been reported. Royal jelly has multitude of pharmacological activities: antibiotic, antiinflammatory, antiallergenic, tonic and antiaging. Honey, propolis and pollen are used to heal burn wounds, and they possess numerous functional properties such as: antibacterial, anti-inflammatory, antioxidant, disinfectant, antifungal and antiviral. Beeswax is used for production of cosmetics and ointments in pharmacy. Due to a large number of biological activities, bee products could be considered as important ingredients in medicines and cosmetics applied to skin. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

22 pages, 4804 KiB

Open AccessReview

Fragaria Genus: Chemical Composition and Biological Activities

by Radu Claudiu Fierascu, Georgeta Temocico, Irina Fierascu, Alina Ortan and Narcisa Elena Babeanu

Molecules 2020, 25(3), 498; https://doi.org/10.3390/molecules25030498 - 23 Jan 2020

Cited by 38 | Viewed by 8056

Abstract

The strawberries represent in our days one of the main fresh fruits consumed globally, inevitably leading to large amounts of by-products and wastes. Usually appreciated because of their specific flavor, the strawberries also possess biological properties, including antioxidant, antimicrobial, or anti-inflammatory effects. In [...] Read more.

The strawberries represent in our days one of the main fresh fruits consumed globally, inevitably leading to large amounts of by-products and wastes. Usually appreciated because of their specific flavor, the strawberries also possess biological properties, including antioxidant, antimicrobial, or anti-inflammatory effects. In spite of the wide spread of the Fragaria genus, few species represent the subject of the last decade scientific research. The main components identified in the Fragaria species are presented, as well as several biological properties, as emerging from the scientific papers published in the last decade. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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23 pages, 905 KiB

Open AccessReview

Lamium Plants—A Comprehensive Review on Health Benefits and Biological Activities

by Bahare Salehi, Lorene Armstrong, Antonio Rescigno, Balakyz Yeskaliyeva, Gulnaz Seitimova, Ahmet Beyatli, Jugreet Sharmeen, Mohamad Fawzi Mahomoodally, Farukh Sharopov, Alessandra Durazzo, Massimo Lucarini, Antonello Santini, Ludovico Abenavoli, Raffaele Capasso and Javad Sharifi-Rad

Molecules 2019, 24(10), 1913; https://doi.org/10.3390/molecules24101913 - 17 May 2019

Cited by 29 | Viewed by 8019

Abstract

This work is an updated snapshot of Lamium plants and their biological activities. The main features of the plant are described and the components of its essential oils are summarized. The traditional medicinal uses of Lamium plants has been reported. The presence of [...] Read more.

This work is an updated snapshot of Lamium plants and their biological activities. The main features of the plant are described and the components of its essential oils are summarized. The traditional medicinal uses of Lamium plants has been reported. The presence of these chemicals i.e., hydroxycinnamic acids, iridoids, secoiridoids, flavonoids, anthocyanins, phenylpropanoids, phytoecdysteroids, benzoxazinoids, betaine can provide biological activities. After the discussion of antioxidant properties documented for Lamium plants, the biological activities, studied using in vitro models, antimicrobial, antiviral, anti-inflammatory, anti-nociceptive activity, and pain therapy and cytotoxicity and cytoprotective activity are here described and discussed. Finally, targeted examples of in vivo studies are reported. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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23 pages, 2845 KiB

Open AccessReview

Cucurbits Plants: A Key Emphasis to Its Pharmacological Potential

by Bahare Salehi, Esra Capanoglu, Nabil Adrar, Gizem Catalkaya, Shabnum Shaheen, Mehwish Jaffer, Lalit Giri, Renu Suyal, Arun K Jugran, Daniela Calina, Anca Oana Docea, Senem Kamiloglu, Dorota Kregiel, Hubert Antolak, Ewelina Pawlikowska, Surjit Sen, Krishnendu Acharya, Zeliha Selamoglu, Javad Sharifi-Rad, Miquel Martorell, Célia F. Rodrigues, Farukh Sharopov, Natália Martins and Raffaele Capasso Show full author list Hide full author list

Molecules 2019, 24(10), 1854; https://doi.org/10.3390/molecules24101854 - 14 May 2019

Cited by 112 | Viewed by 12086

Abstract

Cucurbita genus has received a renowned interest in the last years. This plant species, native to the Americas, has served worldwide folk medicine for treating gastrointestinal diseases and intestinal parasites, among other clinical conditions. These pharmacological effects have been increasingly correlated with their [...] Read more.

Cucurbita genus has received a renowned interest in the last years. This plant species, native to the Americas, has served worldwide folk medicine for treating gastrointestinal diseases and intestinal parasites, among other clinical conditions. These pharmacological effects have been increasingly correlated with their nutritional and phytochemical composition. Among those chemical constituents, carotenoids, tocopherols, phenols, terpenoids, saponins, sterols, fatty acids, and functional carbohydrates and polysaccharides are those occurring in higher abundance. However, more recently, a huge interest in a class of triterpenoids, cucurbitacins, has been stated, given its renowned biological attributes. In this sense, the present review aims to provide a detailed overview to the folk medicinal uses of Cucurbita plants, and even an in-depth insight on the latest advances with regards to its antimicrobial, antioxidant and anticancer effects. A special emphasis was also given to its clinical effectiveness in humans, specifically in blood glucose levels control in diabetic patients and pharmacotherapeutic effects in low urinary tract diseases. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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25 pages, 545 KiB

Open AccessFeature PaperReview

Use of Cannabidiol in the Treatment of Epilepsy: Efficacy and Security in Clinical Trials

by Serena Silvestro, Santa Mammana, Eugenio Cavalli, Placido Bramanti and Emanuela Mazzon

Molecules 2019, 24(8), 1459; https://doi.org/10.3390/molecules24081459 - 12 Apr 2019

Cited by 133 | Viewed by 22967

Abstract

Cannabidiol (CBD) is one of the cannabinoids with non-psychotropic action, extracted from Cannabis sativa. CBD is a terpenophenol and it has received a great scientific interest thanks to its medical applications. This compound showed efficacy as anti-seizure, antipsychotic, neuroprotective, antidepressant and anxiolytic. [...] Read more.

Cannabidiol (CBD) is one of the cannabinoids with non-psychotropic action, extracted from Cannabis sativa. CBD is a terpenophenol and it has received a great scientific interest thanks to its medical applications. This compound showed efficacy as anti-seizure, antipsychotic, neuroprotective, antidepressant and anxiolytic. The neuroprotective activity appears linked to its excellent anti-inflammatory and antioxidant properties. The purpose of this paper is to evaluate the use of CBD, in addition to common anti-epileptic drugs, in the severe treatment-resistant epilepsy through an overview of recent literature and clinical trials aimed to study the effects of the CBD treatment in different forms of epilepsy. The results of scientific studies obtained so far the use of CBD in clinical applications could represent hope for patients who are resistant to all conventional anti-epileptic drugs. Full article

(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)

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