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Biological Activity of Plant Compounds and Extracts, 2nd Edition

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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (28 February 2023) | Viewed by 33798

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Special Issue Editors

Prof. Dr. Gianluca Paventi

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Department of Agricultural, Environmental and Food Sciences, University of Molise, 86100 Campobasso, Italy
Interests: polyphenols; plant antioxidants; ROS; bioenergetics; lactate metabolism; mitochondrial transport; mitochondrial shuttles; cell redox balance; sperm energy metabolism, microbial metabolism
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Prof. Dr. Giuseppe Rotundo

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Department of Agricultural, Environmental and Food Sciences, University of Molise, via de Sanctis, 86100 Campobasso, Italy
Interests: semiochemicals; insect-plant and insect-plant-parasitoid interactions; essential oil; extraction purification and identification of active compounds; insect behavioural and electrophysiological assays; insect rearing; pest control
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Giacinto S. Germinara

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Department of Agricultural Sciences, Food, Natural Resources and Engineering (DAFNE), University of Foggia, Foggia, Italy
Interests: chemical ecology; insect pheromones; allelochemicals; extraction methods; electrophysiology; chemical analysis (GC-EAD, GC-MS-EAD); behavioral bioassays; insect–plant interactions; essential oil and plant extracts; stored-product insect pests; agricultural and forest pests; insect monitoring; mating disruption; attract and kill; mass trapping; integrated pest management; invasive alien species
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Special Issue Information

Dear Colleagues,

The use of plants for their beneficial effects dates back to the first steps in human history, as shown by Ebers Papyrus (1500 BC). Thus, the identification and classification of plant extracts and their compounds showing biological activity has attracted a huge number of ancient and modern researchers. However, after centuries of active research in this field and in spite of the remarkable recent advances in chemical synthesis, plants remain the most powerful and somewhat under-investigated source of bioactive molecules. In addition, in the last decades, the search for novel and more ecofriendly compounds has been strictly emphasised, thus further increasing the interest in plant metabolites. This is particularly true especially in some fields, such as pest control, in which botanical pesticides represent a valuable alternative to traditional chemicals since their use reduces the risk to non-target organisms and the probability of developing pest resistance.

The aim of this Special Issue is to collect original research articles, as well as review articles, addressing recent advances in the extraction, purification, identification, and biochemical characterization of bioactive plant compounds. The in vitro and in vivo biological activities shown by plant extracts will be also considered. Besides the discovery of new potential drugs and healthy compounds, special interest will also be given to papers dealing with non-medical purposes. In this regard, studies on the use of plant extracts/compounds in pest management and food preservation are strongly encouraged.

Prof. Dr. Gianluca Paventi
Prof. Dr. Giuseppe Rotundo
Prof. Dr. Giacinto S. Germinara
Guest Editors

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Keywords

antimicrobial activity
antiproliferative activity
anti-insect activity
insect repellence and attraction
enzyme inhibition
food deterrence
contact, ingestion, and inhalation toxicity
cytotoxicity
chemical identification of plant compounds
insect nutritional parameters
plant antioxidants
electroantennography
behavioural assays
pest control
food storage

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Biological Activity of Plant Compounds and Extracts in Molecules (23 articles)
Biological Activity of Plant Compounds and Extract, 3rd Edition in Molecules (1 article)

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20 pages, 10439 KiB

Open AccessArticle

Metabolomic Analysis of Phytochemical Compounds from Ethanolic Extract of Lime (Citrus aurantifolia) Peel and Its Anti-Cancer Effects against Human Hepatocellular Carcinoma Cells

by Pakkapong Phucharoenrak, Chawanphat Muangnoi and Dunyaporn Trachootham

Molecules 2023, 28(7), 2965; https://doi.org/10.3390/molecules28072965 - 26 Mar 2023

Cited by 9 | Viewed by 4381

Abstract

Lime peels are food waste from lime product manufacturing. We previously developed and optimized a green extraction method for hesperidin-limonin-rich lime peel extract. This study aimed to identify the metabolomics profile of phytochemicals and the anti-cancer effects of ethanolic extract of lime (Citrus aurantifolia) peel against liver cancer cells PLC/PRF/5. The extract’s metabolomics profile was analyzed by using LC-qTOF/MS and GC-HRMS. The anti-cancer effects were studied by using MTT assay, Annexin-PI assay, and Transwell-invasion assay. Results show that the average IC₅₀(s) of hesperidin, limonin, and the extract on cancer cells’ viability were 165.615, 188.073, and 503.004 µg/mL, respectively. At the IC₅₀ levels, the extract induced more apoptosis than those of pure compounds when incubating for 24 and 48 h (p < 0.0001). A combination of limonin and hesperidin showed a synergistic effect on apoptosis induction (p < 0.001), but the effect of the combination was still less than that of the extract at 48 h. Furthermore, the extract significantly inhibited cancer cell invasion better than limonin but equal to hesperidin. At the IC₅₀ level, the extract contains many folds lower amounts of hesperidin and limonin than the IC₅₀ doses of the pure compounds. Besides limonin and hesperidin, there were another 60 and 22 compounds detected from the LCMS and GCMS analyses, respectively. Taken altogether, the superior effect of the ethanolic extract against liver cancer cells compared to pure compound likely results from the combinatorial effects of limonin, hesperidin, and other phytochemical components in the extract. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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15 pages, 1097 KiB

Open AccessArticle

Rotenoids and Isoflavones from Xeroderris stuhlmannii (Taub.) Mendonça & E.P. Souza and Their Biological Activities

by Livie Blondèle Kenou Mekuete, Willifred Dongmo Tékapi Tsopgni, Augustine Kuinze Nkojap, Jacquy Joyce Wanche Kojom, Timo D. Stark, Yannick Fouokeng, Alain Bertrand Dongmo, Léon Tapondjou Azeufack and Anatole Guy Blaise Azebaze

Molecules 2023, 28(6), 2846; https://doi.org/10.3390/molecules28062846 - 21 Mar 2023

Cited by 2 | Viewed by 1782

Abstract

The phytochemical study of the ethanolic extract of the leaf of Xeroderris stuhlmannii led to the isolation of five hitherto unreported compounds including two isoflavones (1–2), and three rotenoids (3–5), along with eight known isoflavonoid derivatives (6–13) and one pterocarpan derivative (14). The structures of the new compounds and those of the known ones were established by the spectroscopic (1D and 2D NMR) and spectrometric (HRESIMS) techniques as well as a comparison of their spectroscopic data with those reported in the literature. The leaf extract, fractions, and isolated compounds were tested for their antibacterial effects against nine bacterial strains. Compounds 3, 8, 11, and 12 showed a significant antibacterial effect, with a minimum inhibitory concentration (MIC) value of 62.5 µg/mL each, against Salmonella typhi, Staphylococcus aureus, Klessiella pneumonae, and Escherichia coli, respectively. In addition, the leaf extract, fractions, and isolated compounds were tested for their antifungal effects against four fungal strains. The hexane fraction showed a significant antifungal effect with an MIC value of 125 µg/mL against Candida parasilosis, whereas compounds 3, 8, and 12 showed significant antifungal activity with an MIC value of 62.5 µg/mL, each against Candida parasilosis, Candida albicans, and Candida krusei, respectively. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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16 pages, 10692 KiB

Open AccessArticle

Effects of Thymus vulgaris Oil on Sodium Hypochlorite-Induced Damage in Rats

by Güneş Bolatli, Fatih Taş and Naci Ömer Alayunt

Molecules 2023, 28(5), 2164; https://doi.org/10.3390/molecules28052164 - 25 Feb 2023

Cited by 2 | Viewed by 1620

Abstract

We aimed to determine the potential damage mechanisms of exposure to widely used sodium hypochlorite (NaOCl) and the effects of Thymus vulgaris on this exposure. Rats were divided into six groups: control, T. vulgaris, 4% NaOCl, 4% NaOCl + T. vulgaris, 15% NaOCl, and 15% NaOCl + T. vulgaris. Serum and lung tissue samples were taken after applying NaOCl and T. vulgaris by inhalation twice a day for 30 min for four weeks. The samples were examined biochemically (TAS/TOS), histopathologically, and immunohistochemically (TNF-α). In serum TOS values, the mean of 15% NaOCl was significantly higher than in 15% NaOCl + T. vulgaris. This was the opposite in terms of serum TAS values. Histopathologically, there was a significant increase in lung injury in 15% NaOCl; significant improvement was observed in 15% NaOCl + T. vulgaris. Immunohistochemically, there was a significant increase in TNF-α expression in both 4% NaOCl and 15% NaOCl; significant decreases were observed in both 4% NaOCl + T. vulgaris and 15% NaOCl + T. vulgaris. The use of sodium hypochlorite, which is harmful to the lungs and is widely used in homes and industries, should be limited. In addition, using T. vulgaris essential oil by inhalation may protect against the harmful effects of sodium hypochlorite. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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14 pages, 4842 KiB

Open AccessArticle

Anti-Struvite, Antimicrobial, and Anti-Inflammatory Activities of Aqueous and Ethanolic Extracts of Saussurea costus (Falc) Lipsch Asteraceae

by Naima Mammate, Fatima Ezzahra El oumari, Hamada Imtara, Salim Belchkar, Ghita Benjelloun Touimi, Mohammed Al-Zharani, Hassan A. Rudayni, Ashraf Ahmed Qurtam, Mohammed S. Aleissa, Fahd A. Nasr, Omar M. Noman and Tarik Sqalli Houssaini

Molecules 2023, 28(2), 667; https://doi.org/10.3390/molecules28020667 - 9 Jan 2023

Cited by 6 | Viewed by 2604

Abstract

Saussurea costus (Falc) Lipsch is a traditional herb used to treat kidney stone problems because it contains several molecules used to treat this health problem, such as quercitrin. Infectious stones are the most painful of all urinary tract disorders, with ammonium phosphate (struvite) and carbapatite stones being the most common, caused by a bacterial infection with urease activity. These stones are treated with antibiotics, but antibiotic resistance is on the rise. The current study investigated the anti-urolithic activities of S. costus aqueous and ethanolic extracts of against struvite crystals synthesized using microscopic crystallization and turbidimetric methods, respectively. The utilized methods indicated that the ethanolic extract of this plant has a significant inhibitory effect on struvite crystallization, with a percentage inhibition of (87.45 ± 1.107) (p < 0.001) for a concentration of 1 mg mL⁻¹ and a decrease in the number of struvite crystals, reaching values less than 100/mm³. For the number of struvite crystals inhibited by cystone, we found a value of 400/mm³ and with the aqueous extract we found 700/mm³. The antibacterial activity of the plant extracts studied was examined against several urease-producing bacteria, and this activity was evaluated by qualitative and quantitative evaluation methods; the highest minimum inhibitory concentration was seen in the ethanolic extract, with an MIC of 50 mg mL⁻¹ for Staphylococcus aureus followed by an MIC of 200 mg mL⁻¹ for Klebsiella pneumoniae. It showed a minimal bactericidal concentration (MBC) against S. aureus and K. pneumoniae (>50 mg mL⁻¹ and >200 mg mL⁻¹, respectively). Furthermore, to determine the extract’s anti-inflammatory activity, in vivo anti-inflammatory activity was investigated in rats. The results show that at a dose of 400 mg kg⁻¹, the ethanolic extract has a maximum edema inhibition of 66%. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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23 pages, 1842 KiB

Open AccessArticle

Determination of Chemical Composition and Investigation of Biological Activities of Ocimum basilicum L.

by Ahmed Qasem, Hamza Assaggaf, Hanae Naceiri Mrabti, Faisal Minshawi, Bodour S. Rajab, Ammar A. Attar, Reema A. Alyamani, Munerah Hamed, Nidal Naceiri Mrabti, Aicha El Baaboua, Nasreddine El Omari, Mohammed Merae Alshahrani, Ahmed Abdullah Al Awadh, Ryan Adnan Sheikh, Long Chiau Ming, Khang Wen Goh and Abdelhakim Bouyahya

Molecules 2023, 28(2), 614; https://doi.org/10.3390/molecules28020614 - 6 Jan 2023

Cited by 11 | Viewed by 3661

Abstract

This study aimed to determine the chemical composition of the essential oils (EOs) of Ocimum basilicum L., as well as to evaluate the antibacterial, antidiabetic, dermatoprotective, and anti-inflammatory properties, and the EOs and aqueous extracts of O. basilicum. The antibacterial activity was evaluated against bacterial strains, Gram-positive and Gram-negative, using the well diffusion and microdilution methods, whereas the antidiabetic activity was assessed in vitro using two enzymes involved in carbohydrate digestion, α-amylase and α-glucosidase. On the other hand, the dermatoprotective and anti-inflammatory activities were studied by testing tyrosinase and lipoxygenase inhibition activity, respectively. The results showed that the chemical composition of O. basilicum EO (OBEO) is dominated by methyl chavicol (86%) and trans-anethol (8%). OBEO exhibited significant antibacterial effects against Gram-negative and Gram-positive strains, demonstrated by considerable diameters of the inhibition zones and lower MIC and MBC values. In addition, OBEO exhibited significant inhibition of α-amylase (IC₅₀ = 50.51 ± 0.32 μg/mL) and α-glucosidase (IC₅₀ = 39.84 ± 1.2 μg/mL). Concerning the anti-inflammatory activity, OBEO significantly inhibited lipoxygenase activity (IC₅₀ = 18.28 ± 0.03 μg/mL) compared to the aqueous extract (IC₅₀ = 24.8 ± 0.01 μg/mL). Moreover, tyrosinase was considerably inhibited by OBEO (IC₅₀ = 68.58 ± 0.03 μg/mL) compared to the aqueous extract (IC₅₀ = 118.37 ± 0.05 μg/mL). The toxicological investigations revealed the safety of O. basilicum in acute and chronic toxicity. The finding of in silico analysis showed that methyl chavicol and trans-anethole (main compounds of OBEO) validate the pharmacokinetics of these compounds and decipher some antibacterial targets. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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18 pages, 2259 KiB

Open AccessArticle

Cardioprotective Effect of Centaurea castriferrei Borbás & Waisb Extract against Doxorubicin-Induced Cardiotoxicity in H9c2 Cells

by Ewelina Humeniuk, Grzegorz Adamczuk, Joanna Kubik, Kamila Adamczuk, Aleksandra Józefczyk and Agnieszka Korga-Plewko

Molecules 2023, 28(1), 420; https://doi.org/10.3390/molecules28010420 - 3 Jan 2023

Cited by 1 | Viewed by 2521

Abstract

Doxorubicin (DOX) is one of the most used chemotherapeutic agents in the treatment of various types of cancer. However, a continual problem that is associated with its application in therapeutic regimens is the development of dose-dependent cardiotoxicity. The progression of this process is associated with a range of different mechanisms, but especially with the high level of oxidative stress. The aim of the study was to evaluate the effects of the water and methanol–water extracts from the plant Centaurea castriferrei (CAS) obtained by the ultrasound-assisted extraction method on the DOX-induced cardiotoxicity in the rat embryonic cardiomyocyte cell line H9c2. The H9c2 cells were treated for 48 h with the DOX and water or methanol–water extracts, or a combination (DOX + CAS H₂O/CAS MeOH). The MTT assay, cell cycle analysis, and apoptosis detection revealed that both the tested extracts significantly abolished the cytotoxic effect caused by DOX. Moreover, the detection of oxidative stress by the CellROX reagent, the evaluation of the number of AP sites, and the expressions of the genes related to the oxidative stress defense showed substantial reductions in the oxidative stress levels in the H9c2 cells treated with the combination of DOX and CAS H₂O/CAS MeOH compared with the DOX administered alone. The tested extracts did not affect the cytotoxic effect of DOX on the MCF-7 breast cancer cell line. The obtained results constitute the basis for further research in the context of the application of C. castriferrei extracts as adjuvants in the therapy regiments of cancer patients treated with DOX. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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17 pages, 3013 KiB

Open AccessArticle

Quercetin and Resveratrol Differentially Decrease Expression of the High-Affinity IgE Receptor (FcεRI) by Human and Mouse Mast Cells

by Syed Benazir Alam, Ashley Wagner, Steven Willows and Marianna Kulka

Molecules 2022, 27(19), 6704; https://doi.org/10.3390/molecules27196704 - 8 Oct 2022

Cited by 12 | Viewed by 2861

Abstract

Mast cells (MC) synthesize and store proinflammatory mediators and are centrally important in atopic diseases such as asthma and atopic dermatitis. Quercetin a and resveratrol are plant derived polyphenolic compounds with anti-inflammatory properties that inhibit MC degranulation and mediator release. However, the underlying mechanism of these inhibitory effects on MC is poorly understood and it is unclear whether this is a general effect on all MC phenotypes. We have characterized and compared the effects of quercetin with resveratrol on human (LAD2) and mouse (MC/9 and BMMC) MC mediator release, receptor expression and FcεRI signaling to better understand the mechanisms involved in quercetin and resveratrol-mediated inhibition of MC activation. Quercetin significantly decreased the expression of FcεRI by BMMC and MC/9, although the effects on MC/9 were associated with a significant reduction in cell viability. Quercetin also inhibited antigen-stimulated TNF release by BMMC. Although neither quercetin nor resveratrol significantly altered antigen-stimulated BMMC degranulation or downstream signaling events such as phosphorylation of spleen tyrosine kinase (SYK) or extracellular signal-regulated kinase 1/2 (ERK), resveratrol inhibited ERK phosphorylation and FcεRI- stimulated degranulation in LAD2. Our data suggests that quercetin and resveratrol inhibit human and mouse MC differentially and that these effects are associated with modification of FcεRI expression, signaling (phosphorylation of SYK and ERK) and mediator release. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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14 pages, 2909 KiB

Open AccessArticle

LC-MS Metabolite Profiling and the Hypoglycemic Activity of Morus alba L. Extracts

by Qing Yi-Jun Zhou, Xin Liao, Hao-Ming Kuang, Jia-Yu Li and Shui-Han Zhang

Molecules 2022, 27(17), 5360; https://doi.org/10.3390/molecules27175360 - 23 Aug 2022

Cited by 12 | Viewed by 2664

Abstract

Morus alba L. is used in traditional Chinese medicine for its anti-diabetic activity; however, the part of the hypoglycemic activity and related active metabolites are still not fully clarified. In this study, the metabolites in the M. alba roots, leaves, twigs, and fruits extracts (70% ethanol extracts) were systematically identified, and their hypoglycemic activity was evaluated by the high-fat diet/streptozotocin-induced 2 diabetes mellitus (T2D) mouse model. A total of 60 high-level compounds, including 16 polyphenols, 43 flavonoids, and one quinic acid, were identified by high-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (HPLC-Q-TOF-MS) combined with the fragmentation pathways of standards and the self-established database. Among them, 23 metabolites were reported for the first time from this plant. In contrast to the extracts of M. alba leaves and fruits, the extracts of roots and twigs displayed significant hypoglycemic activity The glycemia was significantly reduced from 32.08 ± 1.27 to 20.88 ± 1.82 mmol/L and from 33.32 ± 1.98 to 24.74 ± 1.02 mmol/L, respectively, after 4 weeks of treatment with roots and twigs extracts. Compound 46 (morusin), which is a high-level component identified from the extracts of M. alba roots, also displayed significant activity in decreasing the blood glucose level of T2D mice reduced from 31.45 ± 1.23 to 23.45 ± 2.13 mmol/L. In addition, the extracts of roots and twigs displayed significant activity in reducing postprandial glycemia. This work marks the first comparison of the metabolites and hypoglycemic activity of M. alba roots, leaves, twigs, and fruits extracts, and provides a foundation for further development of M. alba extracts as anti-diabetic drugs. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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13 pages, 1484 KiB

Open AccessArticle

Vasodilatory Effect of Alpinia officinarum Extract in Rat Mesenteric Arteries

by Chae Eun Haam, Seonhee Byeon, Soo Jung Choi, Soyeon Lim, Soo-Kyoung Choi and Young-Ho Lee

Molecules 2022, 27(9), 2711; https://doi.org/10.3390/molecules27092711 - 22 Apr 2022

Cited by 1 | Viewed by 2585

Abstract

Background: Alpinia officinarum (A. officinarum) is known to exhibit a beneficial effect for anti-inflammatory, anti-oxidant, and anti-hyperlipidemic effects. However, no sufficient research data are available on the cardiovascular effect of A. officinarum. Thus, in this study, we investigate whether A. officinarum extract has direct effects on vascular reactivity. Methods: To examine whether A. officinarum extract affects vascular functionality, we measured isometric tension in rat mesenteric resistance arteries using a wire myograph. After arteries were pre-contracted with high-K⁺ (70 mM), phenylephrine (5 µM), or U46619 (1 µM), A. officinarum extract was treated. Results: A. officinarum extract induced vasodilation in a concentration-dependent manner, and this effect was endothelium independent. To further investigate the mechanism, we incubated arteries in a Ca²⁺-free and high-K⁺ solution, followed by the cumulative addition of CaCl₂ (0.01–2.5 mM) with or without A. officinarum extract (30 µg/mL). Pre-treatment of A. officinarum extract reduced the contractile responses induced by cumulative administration of Ca²⁺, which suggests that extracellular Ca²⁺ influx was inhibited by the treatment of A. officinarum extract. These results were associated with a reduction in phosphorylated MLC₂₀ in VSMCs treated with A. officinarum extract. Furthermore, eucalyptol, an active compound of A. officinarum extract, had a similar effect as A. officinarum extract, which causes vasodilation in mesenteric resistance arteries. Conclusion: A. officinarum extract and its active compound eucalyptol induce concentration-dependent vasodilation in mesenteric resistance arteries. These results suggest that administration of A. officinarum extract could exert beneficial effects to treat high blood pressure. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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21 pages, 950 KiB

Open AccessFeature PaperArticle

Production and Structural Diversification of Withanolides by Aeroponic Cultivation of Plants of Solanaceae: Cytotoxic and Other Withanolides from Aeroponically Grown Physalis coztomatl

by Ya-Ming Xu, E. M. Kithsiri Wijeratne, Manping X. Liu, Lijiang Xuan, Wenqiong Wang and A. A. Leslie Gunatilaka

Molecules 2022, 27(3), 909; https://doi.org/10.3390/molecules27030909 - 28 Jan 2022

Viewed by 2435

Abstract

Withanolides constitute one of the most interesting classes of natural products due to their diversity of structures and biological activities. Our recent studies on withanolides obtained from plants of Solanaceae including Withania somnifera and a number of Physalis species grown under environmentally controlled aeroponic conditions suggested that this technique is a convenient, reproducible, and superior method for their production and structural diversification. Investigation of aeroponically grown Physalis coztomatl afforded 29 withanolides compared to a total of 13 obtained previously from the wild-crafted plant and included 12 new withanolides, physacoztolides I−M (9–13), 15α-acetoxy-28-hydroxyphysachenolide C (14), 28-oxophysachenolide C (15), and 28-hydroxyphysachenolide C (16), 5α-chloro-6β-hydroxy-5,6-dihydrophysachenolide D (17), 15α-acetoxy-5α-chloro-6β-hydroxy-5,6-dihydrophysachenolide D (18), 28-hydroxy-5α-chloro-6β-hydroxy-5,6-dihydrophysachenolide D (19), physachenolide A-5-methyl ether (20), and 17 known withanolides 3–5, 8, and 21–33. The structures of 9–20 were elucidated by the analysis of their spectroscopic data and the known withanolides 3–5, 8, and 21–33 were identified by comparison of their spectroscopic data with those reported. Evaluation against a panel of prostate cancer (LNCaP, VCaP, DU-145, and PC-3) and renal carcinoma (ACHN) cell lines, and normal human foreskin fibroblast (WI-38) cells revealed that 8, 13, 15, and 17–19 had potent and selective activity for prostate cancer cell lines. Facile conversion of the 5,6-chlorohydrin 17 to its 5,6-epoxide 8 in cell culture medium used for the bioassay suggested that the cytotoxic activities observed for 17–19 may be due to in situ formation of their corresponding 5β,6β-epoxides, 8, 27, and 28. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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16 pages, 3221 KiB

Open AccessArticle

Phytochemical Diversity and Antioxidant Potential of Natural Populations of Nelumbo nucifera Gaertn. throughout the Floristic Regions in Thailand

by Duangjai Tungmunnithum, Samantha Drouet and Christophe Hano

Molecules 2022, 27(3), 681; https://doi.org/10.3390/molecules27030681 - 20 Jan 2022

Cited by 6 | Viewed by 2370

Abstract

Asian lotus has long been consumed as a food and herbal drug that provides several health benefits. The number of studies on its biological activity is significant, but research at the population level to investigate the variation in phytochemicals and biological activity of each population which is useful for a more efficient phytopharmaceutical application strategy remains needed. This present study provided the frontier results to fill-in this necessary gap to investigating the phytopharmaceutical potential of perianth and stamen, which represent an important part for Asian traditional medicines, from 18 natural populations throughout Thailand by (1) determining their phytochemical profiles, such as total contents of phenolic, flavonoid, and anthocyanin, and (2) determining the antioxidant activity of these natural populations using various antioxidant assays to examine different mechanisms. The result showed that Central is the most abundant floristic region. The stamen was higher in total phenolic and flavonoid contents, whereas perianth was higher in monomeric anthocyanin content. This study provided the first description of the significant correlation between phytochemical contents in perianth compared with stamen extracts, and indicated that flavonoids are the main phytochemical class. This analysis indicated that the stamen is a richer source of flavonoids than perianth, and provided the first report to quantify different flavonoids accumulated in stamen and perianth extracts under their native glycosidic forms at the population level. Various antioxidant assays revealed that major flavonoids from N. nucifera prefer the hydrogen atom transfer mechanism when quenching free radicals. The significant correlations between various phytochemical classes and the different antioxidant tests were noted by Pearson correlation coefficients and emphasized that the antioxidant capability of an extract is generally the result of complex phytochemical combinations as opposed to a single molecule. These current findings offer the alternative starting materials to assess the phytochemical diversity and antioxidant potential of N. nucifera for phytopharmaceutical sectors. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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29 pages, 2547 KiB

Open AccessReview

Advances on Natural Abietane, Labdane and Clerodane Diterpenes as Anti-Cancer Agents: Sources and Mechanisms of Action

by Rosaria Acquaviva, Giuseppe A. Malfa, Monica R. Loizzo, Jianbo Xiao, Simone Bianchi and Rosa Tundis

Molecules 2022, 27(15), 4791; https://doi.org/10.3390/molecules27154791 - 26 Jul 2022

Cited by 20 | Viewed by 3175

Abstract

Extensive research over the past decades has identified numerous phytochemicals that could represent an important source of anti-cancer compounds. There is an immediate need for less toxic and more effective preventive and therapeutic strategies for the treatment of cancer. Natural compounds are considered suitable candidates for the development of new anti-cancer drugs due to their pleiotropic actions on target events with multiple manners. This comprehensive review highlighted the most relevant findings achieved in the screening of phytochemicals for anticancer drug development, particularly focused on a promising class of phytochemicals such as diterpenes with abietane, clerodane, and labdane skeleton. The chemical structure of these compounds, their main natural sources, and mechanisms of action were critically discussed. Full article

(This article belongs to the Special Issue Biological Activity of Plant Compounds and Extracts, 2nd Edition)

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