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22 pages, 3984 KiB

Open AccessArticle

Synergistic Roles of Curcumin in Sensitising the Cisplatin Effect on a Cancer Stem Cell-Like Population Derived from Non-Small Cell Lung Cancer Cell Lines

by Nazilah Abdul Satar, Mohd Nazri Ismail and Badrul Hisham Yahaya

Molecules 2021, 26(4), 1056; https://doi.org/10.3390/molecules26041056 - 18 Feb 2021

Cited by 23 | Viewed by 4044

Abstract

Cancer stem cells (CSCs) represent a small subpopulation within a tumour. These cells possess stem cell-like properties but also initiate resistance to cytotoxic agents, which contributes to cancer relapse. Natural compounds such as curcumin that contain high amounts of polyphenols can have a [...] Read more.

Cancer stem cells (CSCs) represent a small subpopulation within a tumour. These cells possess stem cell-like properties but also initiate resistance to cytotoxic agents, which contributes to cancer relapse. Natural compounds such as curcumin that contain high amounts of polyphenols can have a chemosensitivity effect that sensitises CSCs to cytotoxic agents such as cisplatin. This study was designed to investigate the efficacy of curcumin as a chemo-sensitiser in CSCs subpopulation of non-small cell lung cancer (NSCLC) using the lung cancer adenocarcinoma human alveolar basal epithelial cells A549 and H2170. The ability of curcumin to sensitise lung CSCs to cisplatin was determined by evaluating stemness characteristics, including proliferation activity, colony formation, and spheroid formation of cells treated with curcumin alone, cisplatin alone, or the combination of both at 24, 48, and 72 h. The mRNA level of genes involved in stemness was analysed using quantitative real-time polymerase chain reaction. Liquid chromatography-mass spectrometry was used to evaluate the effect of curcumin on the CSC niche. A combined treatment of A549 subpopulations with curcumin reduced cellular proliferation activity at all time points. Curcumin significantly (p < 0.001) suppressed colonies formation by 50% and shrank the spheroids in CSC subpopulations, indicating inhibition of their self-renewal capability. This effect also was manifested by the down-regulation of SOX2, NANOG, and KLF4. Curcumin also regulated the niche of CSCs by inhibiting chemoresistance proteins, aldehyde dehydrogenase, metastasis, angiogenesis, and proliferation of cancer-related proteins. These results show the potential of using curcumin as a therapeutic approach for targeting CSC subpopulations in non-small cell lung cancer. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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12 pages, 1512 KiB

Open AccessArticle

Microfluidic Chip-Based Induced Phase Separation Extraction as a Fast and Efficient Miniaturized Sample Preparation Method

by Yao Shen, Bo Chen, Han Zuilhof and Teris A. van Beek

Molecules 2021, 26(1), 38; https://doi.org/10.3390/molecules26010038 - 23 Dec 2020

Cited by 13 | Viewed by 3343

Abstract

Induced phase separation extraction (IPSE) is an efficient sample clean-up technique that can replace liquid-liquid extraction (LLE). The purpose of this study was to miniaturize IPSE by carrying it out in a microfluidic chip. An IPSE chip was designed and evaluated for its [...] Read more.

Induced phase separation extraction (IPSE) is an efficient sample clean-up technique that can replace liquid-liquid extraction (LLE). The purpose of this study was to miniaturize IPSE by carrying it out in a microfluidic chip. An IPSE chip was designed and evaluated for its ability to separate and purify samples on a microscale. The 5 × 2 cm chip was fed with a solution of polar to non-polar model compounds in acetonitrile-water (1:1). In the 100 µm wide and 40 µm deep microchannels, the sample solution was efficiently separated into two immiscible phases by adding a hydrophobic solvent as inducer. Analytes present in the sample solution each migrated to their own favorable phase upon phase separation. After optimization, extraction and fractionation were easily and efficiently achieved. The behavior of analytes with a pH-dependent partitioning could be influenced by adjusting the pH of the sample solution. Scutellaria baicalensis extract, used in Traditional Chinese Medicine (TCM), was successfully separated in aglycones and glycosides. In this microscale system, the sample and solvent consumption is reduced to microliters, while the time needed for the sample pretreatment is less than one minute. Additionally, the extraction efficiency can reach up to 98.8%, and emulsion formation is avoided. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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18 pages, 2432 KiB

Open AccessArticle

Biotechnological Approaches on Two High CBD and CBG Cannabis sativa L. (Cannabaceae) Varieties: In Vitro Regeneration and Phytochemical Consistency Evaluation of Micropropagated Plants Using Quantitative ¹H-NMR

by Kostas Ioannidis, Evangelos Dadiotis, Vangelis Mitsis, Eleni Melliou and Prokopios Magiatis

Molecules 2020, 25(24), 5928; https://doi.org/10.3390/molecules25245928 - 15 Dec 2020

Cited by 22 | Viewed by 4006

Abstract

High cannabidiol (CBD) and cannabigerol (CBG) varieties of Cannabis sativa L., a species with medicinal properties, were regenerated in vitro. Explants of nodal segments including healthy axillary bud, after sterilization, were placed in Murashige-Skoog (MS) culture medium. The shoots formed after 30 days [...] Read more.

High cannabidiol (CBD) and cannabigerol (CBG) varieties of Cannabis sativa L., a species with medicinal properties, were regenerated in vitro. Explants of nodal segments including healthy axillary bud, after sterilization, were placed in Murashige-Skoog (MS) culture medium. The shoots formed after 30 days were subcultured in full- or half-strength MS medium supplemented with several concentrations of 6-benzyl-amino-purine (BA) or thidiazuron (TDZ). The highest average number and length of shoots was achieved when both full and half-strength MS media were supplemented with 4.0 μM BA. The presence of 4.0 μM TDZ showed also comparable results. BA and TDZ at concentrations of 4.0, 8.0 μM and 2.0, 4.0 μM respectively, displayed the maximum shooting frequency. The new shoots were transferred on the same media and were either self-rooted or after being enhanced with different concentrations of indole-3-butyric acid (IBA) or α-naphthalene acetic acid (NAA). Presence of 2.0 or 4.0 μM IBA or 4.0 μM NAA resulted to the optimum rooting rates. The maximum average number and length of roots per shoot was observed when the culture media was supplemented with 4.0 μM IBA or NAA. Approximately 92% of the plantlets were successfully established and acclimatized in field. The consistency of the chemical profile of the acclimatized in vitro propagated clones was assessed using quantitative ¹H-NMR high throughput screening. In each variety, analysis of the micropropagated plant in comparison with the mother plant showed no statistically significant differences (p ≤ 0.05) in CBD+ cannabidiolic acid (CBDA) and CBG+ cannabigerolic acid (CBGA) content respectively, thus indicating stability of their chemical profile. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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14 pages, 4100 KiB

Open AccessArticle

Natural Approaches for Neurological Disorders—The Neuroprotective Potential of Codium tomentosum

by Joana Silva, Alice Martins, Celso Alves, Susete Pinteus, Helena Gaspar, Amparo Alfonso and Rui Pedrosa

Molecules 2020, 25(22), 5478; https://doi.org/10.3390/molecules25225478 - 23 Nov 2020

Cited by 11 | Viewed by 3590

Abstract

Parkinson’s disease (PD) is the second most common neurodegenerative disorder, and is characterized by a progressive degeneration of the dopaminergic neurons in the substantianigra. Although not completely understood, several abnormal cellular events are known to be related with PD progression, such [...] Read more.

Parkinson’s disease (PD) is the second most common neurodegenerative disorder, and is characterized by a progressive degeneration of the dopaminergic neurons in the substantianigra. Although not completely understood, several abnormal cellular events are known to be related with PD progression, such as oxidative stress, mitochondrial dysfunction and apoptosis. Accordingly, the aim of this study was to evaluate the neuroprotective effects of Codium tomentosum enriched fractions in a neurotoxicity model mediated by 6-hydroxydopamine (6-OHDA) on SH-SY5Y human cells, and the disclosure of their mechanisms of action. Additionally, a preliminary chemical screening of the most promising bioactive fractions of C. tomentosum was carried out by GC-MS analysis. Among the tested fractions, four samples exhibited the capacity to revert the neurotoxicity induced by 6-OHDA to values higher or similar to the vitamin E (90.11 ± 3.74% of viable cells). The neuroprotective effects were mediated by the mitigation of reactive oxygen species (ROS) generation, mitochondrial dysfunctions and DNA damage, together with the reduction of Caspase-3 activity. Compounds belonging to different chemical classes, such as terpenes, alcohols, carboxylic acids, aldehydes, esters, ketones, saturated and unsaturated hydrocarbons were tentatively identified by GC-MS. The results show that C. tomentosum is a relevant source of neuroprotective agents, with particular interest for preventive therapeutics. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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16 pages, 1311 KiB

Open AccessArticle

Comparison of Maceration and Ultrasonication for Green Extraction of Phenolic Acids from Echinacea purpurea Aerial Parts

by Plamen Momchev, Petar Ciganović, Mario Jug, Eva Marguí, Jasna Jablan and Marijana Zovko Končić

Molecules 2020, 25(21), 5142; https://doi.org/10.3390/molecules25215142 - 5 Nov 2020

Cited by 18 | Viewed by 4272

Abstract

Echinacea purpurea is used in herbal medicinal products for the prevention and treatment of the common cold, as well as for skin disorders and minor wounds. In this study, the efficiency of traditional maceration using water and ethanol was compared with the maceration [...] Read more.

Echinacea purpurea is used in herbal medicinal products for the prevention and treatment of the common cold, as well as for skin disorders and minor wounds. In this study, the efficiency of traditional maceration using water and ethanol was compared with the maceration using mixtures of water and glycerol, a non-toxic, biodegradable solvent from renewable sources. It was found that the glycerol–water mixtures were as effective as ethanol/water mixtures for the extraction of caffeic acid derivatives. All the prepared extracts demonstrated notable antiradical properties. Furthermore, an efficient ultrasound-assisted extraction using glycerol–water mixtures was developed using six independent variables. Their levels needed for the maximum extraction of caffeic acid derivatives were as follows: glycerol 90% (m/m), temperature 70 °C, ultrasound power 72 W, time 40 min, and ascorbic acid 0 mg/mL. Under the optimized conditions, ultrasound-assisted extraction was superior to maceration. It achieved significantly higher yields of phenolic acids in shorter extraction time. The presence of zinc in plant material may contribute to the beneficial effects of E. purpurea preparations. Since glycerol is a non-toxic solvent with humectant properties, the prepared extracts can be directly used for the preparation of cosmetics or oral pharmaceutical formulations without the need for solvent removal. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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22 pages, 4330 KiB

Open AccessArticle

Advances in Azorella glabra Wedd. Extract Research: In Vitro Antioxidant Activity, Antiproliferative Effects on Acute Myeloid Leukemia Cells and Bioactive Compound Characterization

by Daniela Lamorte, Immacolata Faraone, Ilaria Laurenzana, Stefania Trino, Daniela Russo, Dilip K. Rai, Maria Francesca Armentano, Pellegrino Musto, Alessandro Sgambato, Luciana De Luca, Luigi Milella and Antonella Caivano

Molecules 2020, 25(21), 4890; https://doi.org/10.3390/molecules25214890 - 22 Oct 2020

Cited by 4 | Viewed by 2564

Abstract

Azorella glabra Wedd. (AG) is traditionally used to treat gonorrhea or kidney’s problems. The antioxidant, antidiabetic, anticholinesterase and in vitro antitumor activities of AG extracts were recently reported. The aim of this work was to investigate anti-leukemic properties of AG chloroform fraction (AG [...] Read more.

Azorella glabra Wedd. (AG) is traditionally used to treat gonorrhea or kidney’s problems. The antioxidant, antidiabetic, anticholinesterase and in vitro antitumor activities of AG extracts were recently reported. The aim of this work was to investigate anti-leukemic properties of AG chloroform fraction (AG CHCl₃) and of its ten sub-fractions (I-X) and to identify their possible bioactive compounds. We determined their in vitro antioxidant activity using 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), nitric oxide (NO) and superoxide anion (SO) assays, and their phytochemical profile by spectrophotometric and LC-MS/MS techniques. I-X action on two acute myeloid leukemia (AML) cell lines viability, apoptosis and cell cycle were evaluated by MTS, western blotting and cytofluorimetric assays. Different polyphenol, flavonoid and terpenoid amount, and antioxidant activity were found among all samples. Most of I-X induced a dose/time dependent reduction of cell viability higher than parent extract. IV and VI sub-fractions showed highest cytotoxic activity and, of note, a negligible reduction of healthy cell viability. They activated intrinsic apoptotic pathway, induced a G₀/G₁ block in leukemic cells and, interestingly, led to apoptosis in patient AML cells. These activities could be due to mulinic acid or azorellane terpenoids and their derivatives, tentatively identified in both IV and VI. In conclusion, our data suggest AG plant as a source of potential anti-AML agents. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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13 pages, 2663 KiB

Open AccessArticle

Anti-Inflammatory Property of the Essential Oil from Cinnamomum camphora (Linn.) Presl Leaves and the Evaluation of Its Underlying Mechanism by Using Metabolomics Analysis

by Jiali Chen, Cailin Tang, Yang Zhou, Rongfei Zhang, Shaoxia Ye, Zhimin Zhao, Ligen Lin and Depo Yang

Molecules 2020, 25(20), 4796; https://doi.org/10.3390/molecules25204796 - 19 Oct 2020

Cited by 13 | Viewed by 3083

Abstract

Cinnamomum camphora (Linn.) Presl has been widely used in traditional Chinese medicine for a variety of purposes. Our previous study indicated the antibacterial mechanism of the essential oil (EO) from C. camphora leaves; however, its anti-inflammatory activity and the underlying mechanism have not [...] Read more.

Cinnamomum camphora (Linn.) Presl has been widely used in traditional Chinese medicine for a variety of purposes. Our previous study indicated the antibacterial mechanism of the essential oil (EO) from C. camphora leaves; however, its anti-inflammatory activity and the underlying mechanism have not been clearly demonstrated. Thus, the present study investigated its anti-inflammatory property. Our data revealed that EO significantly decreased the release of nitric oxide (NO) and the mRNA expression of inducible NO synthase (iNOS) in lipopolysaccharide (LPS)-induced BV2 microglial cells. EO also attenuated LPS-induced increase in the mRNA expression and secretion of inflammatory cytokines including interleukin-6 (IL-6), IL-18, IL-1β and tumor necrosis factor-α (TNF-α). Furthermore, the metabolic profiles of LPS-induced BV2 microglial cells treated with or without EO were explored. Thirty-nine metabolites were identified with significantly different contents, including 21 upregulated and 18 downregulated ones. Five pathways were enriched by shared differential metabolites. Compared with the control cells, the glucose level was decreased, while the lactate level was increased, in the culture supernatant from LPS-stimulated cells, which were reversed by EO treatment. Moreover, compared to the LPS-treated group, the activities of phosphofructokinase (PFK) and pyruvate kinase (PK) in EO group were decreased. In summary, the current study demonstrated that EO from C. camphora leaves acts as an anti-inflammatory agent, which might be mediated through attenuating the glycolysis capacity of microglial cells. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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9 pages, 1181 KiB

Open AccessArticle

Pimarane Diterpenoids from the Seeds of Caesalpinia minax as PTP1B Inhibitors and Insulin Sensitizers

by Yunshao Xu, Zheling Feng, Tian Zhang, Peng Lv, Jun Cao, Dan Li, Cheng Peng and Ligen Lin

Molecules 2020, 25(20), 4674; https://doi.org/10.3390/molecules25204674 - 13 Oct 2020

Cited by 7 | Viewed by 2434

Abstract

Protein-tyrosine phosphatase 1B (PTP1B) has been considered as a promising target for treating insulin resistance. In searching for naturally occurring PTB1B antagonists, two new pimarane diterpenoids, named 2α-hydroxy-7-oxo-pimara-8(9),15-diene (1) and 19-hydroxy-2α-acetoxy-7-oxo-pimara-8(9),15-diene (2), were isolated from the seeds of Caesalpinia [...] Read more.

Protein-tyrosine phosphatase 1B (PTP1B) has been considered as a promising target for treating insulin resistance. In searching for naturally occurring PTB1B antagonists, two new pimarane diterpenoids, named 2α-hydroxy-7-oxo-pimara-8(9),15-diene (1) and 19-hydroxy-2α-acetoxy-7-oxo-pimara-8(9),15-diene (2), were isolated from the seeds of Caesalpinia minax. Their structures were determined by extensive analysis of NMR and HR-ESIMS data, and their absolute configurations were determined by electronic circular dichroism (ECD) spectra. Compound 1 was disclosed as a competitive inhibitor of PTP1B with an IC₅₀ (the half-maximal inhibitory concentration) value of 19.44 ± 2.39 µM and a Ki (inhibition constant) value of 13.69 ± 2.72 μM. Moreover, compound 1 dose-dependently promoted insulin-stimulated glucose uptake in C2C12 myotubes through activating insulin signaling pathway. Compound 1 might be further developed as an insulin sensitizer. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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15 pages, 2873 KiB

Open AccessArticle

Antiulcer Activity of Steamed Ginger Extract against Ethanol/HCl-Induced Gastric Mucosal Injury in Rats

by Jun-Kyu Shin, Jae Hyeon Park, Kyeong Seok Kim, Tong Ho Kang and Hyung Sik Kim

Molecules 2020, 25(20), 4663; https://doi.org/10.3390/molecules25204663 - 13 Oct 2020

Cited by 25 | Viewed by 4718

Abstract

Ginger (Zingiber officianale), the most widely consumed species, is traditionally used as a folk medicine to treat some inflammatory diseases in China and Korea. However, the functional activity of steamed ginger extract on gastric ulcers has not been previously explored. The [...] Read more.

Ginger (Zingiber officianale), the most widely consumed species, is traditionally used as a folk medicine to treat some inflammatory diseases in China and Korea. However, the functional activity of steamed ginger extract on gastric ulcers has not been previously explored. The present study aimed to investigate antiulcer activity of steamed ginger extract (GGE03) against ethanol (EtOH)/HCl-induced gastric ulcers in a rat model. GGE03 (100 mg/kg) was orally administered for 14 days to rats before oral intubation of an EtOH/HCl mixture to induce gastric damage. Pretreatment with GGE03 markedly protected the formation of microscopic pathological damage in the gastric mucosa. Further, administration of GGE03 significantly increased mucosal total nitrate/nitrite production in gastric tissues, and elevated total GSH content, catalase activity and superoxide dismutase (SOD) expression as well as decreasing lipid peroxidation and myeloperoxidase (MPO) activity. Underlying protective mechanisms were examined by assessing inflammation-related genes, including nuclear factor-κB (NF-κB), prostaglandin E2 (PGE₂), and pro-inflammatory cytokines levels. GGE03 administration significantly reduced the expression of NF-κB and pro-inflammatory cytokines. Our findings suggest that GGE03 possesses antiulcer activity by attenuating oxidative stress and inflammatory responses. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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14 pages, 1534 KiB

Open AccessArticle

Effects of Ultrasonic-Assisted Extraction on the Yield and the Antioxidative Potential of Bergenia emeiensis Triterpenes

by Siyuan Luo, Chen Zeng, Jiajia Li, Shiling Feng, Lijun Zhou, Tao Chen, Ming Yuan, Yan Huang, Hongyu Yang and Chunbang Ding

Molecules 2020, 25(18), 4159; https://doi.org/10.3390/molecules25184159 - 11 Sep 2020

Cited by 6 | Viewed by 2655

Abstract

This study was the first designed to evaluate the extraction and antioxidant ability of triterpenes from Bergenia emeiensis rhizomes. The yield of triterpenes from B. emeiensis was mainly affected by the concentration of ethanol, followed by the extraction time, solvent to sample ratio, [...] Read more.

This study was the first designed to evaluate the extraction and antioxidant ability of triterpenes from Bergenia emeiensis rhizomes. The yield of triterpenes from B. emeiensis was mainly affected by the concentration of ethanol, followed by the extraction time, solvent to sample ratio, and the power of ultrasound. Thus, the response surface method was applied to investigate the interaction between the two factors and to optimize the extraction process. The optimal extraction conditions were 210 W, 75% ethanol, 40 min and 25 mL/g with a maximum yield of 229.37 ± 7.16 mg UAE/g. Moreover, the antioxidant ability of triterpenes from B. emeiensis (TBE) was evaluated by determining the scavenging capacity on free radicals and the protection on CHO cells and Caenorhabditis elegans against oxidative stress. The results showed the triterpenes could clear 2,2-Diphenyl-1-picryl-hydrazyl (DPPH) radicals well and had a strong reducing power. In addition, the survival of CHO cells was higher than that of the control group as a result of reducing the reactive oxygen species (ROS) level and promoting the activities of antioxidant enzymes. In addition, TBE could also enhance the survival of C. elegans under H₂O₂ conditions. Therefore, triterpenes from B. emeiensis could be developed into a beneficial potential for antioxidants. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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11 pages, 2794 KiB

Open AccessArticle

Deletion of the Histone Deacetylase HdaA in Endophytic Fungus Penicillium chrysogenum Fes1701 Induces the Complex Response of Multiple Bioactive Secondary Metabolite Production and Relevant Gene Cluster Expression

by Zhuang Ding, Haibo Zhou, Xiao Wang, Huiming Huang, Haotian Wang, Ruiyan Zhang, Zhengping Wang and Jun Han

Molecules 2020, 25(16), 3657; https://doi.org/10.3390/molecules25163657 - 11 Aug 2020

Cited by 16 | Viewed by 3103

Abstract

Epigenetic regulation plays a critical role in controlling fungal secondary metabolism. Here, we report the pleiotropic effects of the epigenetic regulator HdaA (histone deacetylase) on secondary metabolite production and the associated biosynthetic gene clusters (BGCs) expression in the plant endophytic fungus Penicillium chrysogenum [...] Read more.

Epigenetic regulation plays a critical role in controlling fungal secondary metabolism. Here, we report the pleiotropic effects of the epigenetic regulator HdaA (histone deacetylase) on secondary metabolite production and the associated biosynthetic gene clusters (BGCs) expression in the plant endophytic fungus Penicillium chrysogenum Fes1701. Deletion of the hdaA gene in strain Fes1701 induced a significant change of the secondary metabolite profile with the emergence of the bioactive indole alkaloid meleagrin. Simultaneously, more meleagrin/roquefortine-related compounds and less chrysogine were synthesized in the ΔhdaA strain. Transcriptional analysis of relevant gene clusters in ΔhdaA and wild strains indicated that disruption of hdaA had different effects on the expression levels of two BGCs: the meleagrin/roquefortine BGC was upregulated, while the chrysogine BGC was downregulated. Interestingly, transcriptional analysis demonstrated that different functional genes in the same BGC had different responses to the disruption of hdaA. Thereinto, the roqO gene, which encodes a key catalyzing enzyme in meleagrin biosynthesis, showed the highest upregulation in the ΔhdaA strain (84.8-fold). To our knowledge, this is the first report of the upregulation of HdaA inactivation on meleagrin/roquefortine alkaloid production in the endophytic fungus P. chrysogenum. Our results suggest that genetic manipulation based on the epigenetic regulator HdaA is an important strategy for regulating the productions of secondary metabolites and expanding bioactive natural product resources in endophytic fungi. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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8 pages, 1289 KiB

Open AccessCommunication

Phenolic Composition, Antioxidant and Anticancer Potentials of Extracts from Rosa banksiae Ait. Flowers

by Chen Zeng, Siyuan Luo, Shiling Feng, Tao Chen, Lijun Zhou, Ming Yuan, Yan Huang, Jinqiu Liao and Chunbang Ding

Molecules 2020, 25(13), 3068; https://doi.org/10.3390/molecules25133068 - 6 Jul 2020

Cited by 15 | Viewed by 3077

Abstract

Rosa banksiae Ait. (R. banksiae) is a traditional Chinese folk medicine and an ornamental plant. Most previous studies have focused on cultivation and utilization while there are few research papers on the pharmacological activity of R. banksiae. This study aimed [...] Read more.

Rosa banksiae Ait. (R. banksiae) is a traditional Chinese folk medicine and an ornamental plant. Most previous studies have focused on cultivation and utilization while there are few research papers on the pharmacological activity of R. banksiae. This study aimed to get a better understanding of R. banksiae by extracting polyphenols with fractionated extraction technology. The results showed that ethyl acetate phase (EAP) contained the most polyphenols, while water phase (WP) had the least. HPLC analysis indicated that rutin and luteolin-4′-O-glucoside existed in the EAP and butanol phase (BP), but quercetin was only detected in the EAP. Six phenolic compositions were not detected in WB. The antioxidant and anti-tumor abilities of the EAP and BP were excellent. The results revealed that R. banksiae possessed a great antioxidant capacity and was rich in polyphenols, thus indicating R. banksiae was suitable for being a natural antioxidant and an abundant source of polyphenols. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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14 pages, 4130 KiB

Open AccessArticle

Anti-Hepatocellular-Cancer Activity Exerted by β-Sitosterol and β-Sitosterol-Glucoside from Indigofera zollingeriana Miq

by Tuong Kha Vo, Qui Thanh Hoai Ta, Quang Truyen Chu, Thuy Trang Nguyen and Van Giau Vo

Molecules 2020, 25(13), 3021; https://doi.org/10.3390/molecules25133021 - 2 Jul 2020

Cited by 48 | Viewed by 4780

Abstract

Indigofera zollingeriana Miq (I. zollingeriana) is a widely grown tree in Vietnam. It is used to cure various illnesses. The purpose of this study was to investigate the chemical constituents of an I. zollingeriana extract and test its anticancer activity on [...] Read more.

Indigofera zollingeriana Miq (I. zollingeriana) is a widely grown tree in Vietnam. It is used to cure various illnesses. The purpose of this study was to investigate the chemical constituents of an I. zollingeriana extract and test its anticancer activity on hepatocellular cells (Huh7 and HepG2). The experimental results of the analysis of the bioactive compounds revealed that β-sitosterol (β-S) and β-sitosterol-glucoside (β-SG) were the main ingredients of the I. zollingeriana extract. Regarding anticancer activity, the β-S and β-SG of I. zollingeriana were found to exhibit cytotoxic effects against HepG2 and Huh7 cells, but not against normal human primary fibroblasts. The β-S was able to inhibit the proliferation of HepG2 and Huh7 cells in a dose-dependent manner with half-maximal inhibitory concentration (IC₅₀) values of 6.85 ± 0.61 µg/mL and 8.71 ± 0.21 µg/mL, respectively (p < 0.01), whereas the β-SG IC₅₀ values were 4.64 ± 0.48 µg/mL for HepG2 and 5.25 ± 0.14 µg/mL for Huh7 cells (p < 0.01). Remarkably, our study also indicated that β-S and β-SG exhibited cytotoxic activities via inducing apoptosis and activating caspase-3 and -9 in these cells. These findings demonstrated that β-S and β-SG from I. zollingeriana could potentially be developed into promising therapeutic agents to treat liver cancer. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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12 pages, 620 KiB

Open AccessArticle

Anti-Inflammatory Principles from Tamarix aphylla L.: A Bioassay-Guided Fractionation Study

by Adel S. Gadallah, Mujeeb-ur-Rehman, Atta-ur-Rahman, Sammer Yousuf, Atia-tul-Wahab, Almas Jabeen, Mahmoud M. Swilam, Shaden A. M. Khalifa, Hesham R. El-Seedi and M. Iqbal Choudhary

Molecules 2020, 25(13), 2994; https://doi.org/10.3390/molecules25132994 - 30 Jun 2020

Cited by 22 | Viewed by 4386

Abstract

Natural products have served as primary remedies since ancient times due to their cultural acceptance and outstanding biodiversity. To investigate whether Tamarix aphylla L. modulates an inflammatory process, we carried out bioassay-guided isolation where the extracts and isolated compounds were tested for their [...] Read more.

Natural products have served as primary remedies since ancient times due to their cultural acceptance and outstanding biodiversity. To investigate whether Tamarix aphylla L. modulates an inflammatory process, we carried out bioassay-guided isolation where the extracts and isolated compounds were tested for their modulatory effects on several inflammatory indicators, such as nitric oxide (NO), reactive oxygen species (ROS), proinflammatory cytokine; tumour necrosis factor (TNF-α), as well as the proliferation of the lymphocyte T-cells. The aqueous ethanolic extract of the plant inhibited the intracellular ROS production, NO generation, and T-cell proliferation. The aqueous ethanolic crude extract was partitioned by liquid-liquid fractionation using n-hexane (n-C₆H₆), dichloromethane (DCM), ethyl acetate (EtOAc), n-butanol (n-BuOH), and water (H₂O). The DCM and n-BuOH extracts showed the highest activity against most inflammatory indicators and were further purified to obtain compounds 1–4. The structures of 3,5-dihydroxy-4’,7-dimethoxyflavone (1) and 3,5-dihydroxy-4-methoxybenzoic acid methyl ester (2) from the DCM extracts; and kaempferol (3), and 3-hydroxy-4-methoxy-(E)-cinnamic acid (4) from the n-BuOH extract were elucidated by different spectroscopic tools, including MS, NMR, UV, and IR. Compound 2 inhibited the production of ROS and TNF-α, whereas compound 3 showed inhibitory activity against all the tested mediators. A better understanding of the potential aspect of Tamarix aphylla L. derivatives as anti-inflammatory agents could open the door for the development of advanced anti-inflammatory entities. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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12 pages, 3535 KiB

Open AccessArticle

Discovery of a Natural Product That Binds to the Mycobacterium tuberculosis Protein Rv1466 Using Native Mass Spectrometry

by Ali R. Elnaas, Darren Grice, Jianying Han, Yunjiang Feng, Angela Di Capua, Tin Mak, Joseph A. Laureanti, Garry W. Buchko, Peter J. Myler, Gregory Cook, Ronald J. Quinn and Miaomiao Liu

Molecules 2020, 25(10), 2384; https://doi.org/10.3390/molecules25102384 - 21 May 2020

Cited by 19 | Viewed by 4767

Abstract

Elucidation of the mechanism of action of compounds with cellular bioactivity is important for progressing compounds into future drug development. In recent years, phenotype-based drug discovery has become the dominant approach to drug discovery over target-based drug discovery, which relies on the knowledge [...] Read more.

Elucidation of the mechanism of action of compounds with cellular bioactivity is important for progressing compounds into future drug development. In recent years, phenotype-based drug discovery has become the dominant approach to drug discovery over target-based drug discovery, which relies on the knowledge of a specific drug target of a disease. Still, when targeting an infectious disease via a high throughput phenotypic assay it is highly advantageous to identifying the compound’s cellular activity. A fraction derived from the plant Polyalthia sp. showed activity against Mycobacterium tuberculosis at 62.5 μge/μL. A known compound, altholactone, was identified from this fraction that showed activity towards M. tuberculosis at an minimum inhibitory concentration (MIC) of 64 μM. Retrospective analysis of a target-based screen against a TB proteome panel using native mass spectrometry established that the active fraction was bound to the mycobacterial protein Rv1466 with an estimated pseudo-K_d of 42.0 ± 6.1 µM. Our findings established Rv1466 as the potential molecular target of altholactone, which is responsible for the observed in vivo toxicity towards M. tuberculosis. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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Polyphenols’ Cardioprotective Potential: Review of Rat Fibroblasts as Well as Rat and Human Cardiomyocyte Cell Lines Research

by Michał Otręba, Leon Kośmider and Anna Rzepecka-Stojko

Molecules 2021, 26(4), 774; https://doi.org/10.3390/molecules26040774 - 3 Feb 2021

Cited by 15 | Viewed by 3117

Abstract

According to the World Health Organization, cardiovascular diseases are responsible for 31% of global deaths. A reduction in mortality can be achieved by promoting a healthy lifestyle, developing prevention strategies, and developing new therapies. Polyphenols are present in food and drinks such as [...] Read more.

According to the World Health Organization, cardiovascular diseases are responsible for 31% of global deaths. A reduction in mortality can be achieved by promoting a healthy lifestyle, developing prevention strategies, and developing new therapies. Polyphenols are present in food and drinks such as tea, cocoa, fruits, berries, and vegetables. These compounds have strong antioxidative properties, which might have a cardioprotective effect. The aim of this paper is to examine the potential of polyphenols in cardioprotective use based on in vitro human and rat cardiomyocytes as well as fibroblast research. Based on the papers discussed in this review, polyphenols have the potential for cardioprotective use due to their multilevel points of action which include, among others, anti-inflammatory, antioxidant, antithrombotic, and vasodilatory. Polyphenols may have potential use in new and effective preventions or therapies for cardiovascular diseases, yet more clinical studies are needed. Full article

(This article belongs to the Special Issue Advances on Natural Compounds Research: Chemistry, Biology and Biotechnology)

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