Triterpenoids and Sterols from the Leaves and Twigs of Melia azedarach.
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ABSTRACT:
SUBMITTER: Zhang WM
PROVIDER: S-EPMC4050312 | biostudies-literature |
REPOSITORIES: biostudies-literature
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Project description:Four new limonoids, dysohainanins A–D (1–4), and two new triterpenoids, dysohainanins E and F (5 and 6), together with seven known ones were isolated from the twigs and leaves of Dysoxylum hainanense Merr. The structures of the new compounds were determined by a variety of spectroscopic methods. The cytotoxic activities of these compounds were evaluated, and the known compound ent-19-nor-4,16,18-trihydroxy-8(14)-pomaren-15-one (13) showed in vitro cytotoxicity against HL-60, A-549, MCF-7, and SW480 cells, with IC50 values of 24.3, 28.1, 30.7, and 22.5 µM, respectively. Compounds 2 and 3 were tested their insecticidal activities using brine shrimp and both of them were inactive. Electronic Supplementary Material Supplementary material is available for this article at 10.1007/s13659-011-0030-8 and is accessible for authorized users.
| S-EPMC4131571 | biostudies-literature
Project description:Melia azedarach L. is used widely in traditional medicine for local or systemic ailments. Although studies exist on phytochemicals and potencies of Chinese and Indian cultivars of Melia, the present study investigated in vitro antioxidant properties of Melia wild type and its cytotoxicity against T47D cell. The ethanolic extract of the Melia leaves was fractionated with n-hexane, ethyl acetate and water, and the secondary metabolites were obtained. The antioxidant properties were determined with IC50 DPPH (2,2-diphenyl-1-pycrylhydrazyl) radical and FRAP (ferric reducing antioxidant power), while the cytotoxicity was determined with the MTT method. The total phenolic (TPC) and ?-sitosterol (SC) contents were also measured. The results showed that the ethyl acetate fraction had higher antioxidant and cytotoxic activities (IC50 211.89?±?10.86 and 147.90?±?8.49 ?g/mL, respectively) than others. Significant (p?<?0.05) correlations were observed between TPC, IC50DPPH, FRAP and IC50T47D. LC-EI MS analysis of the ethyl acetate fraction revealed the steroid and triterpenoid saponins, limonoids and quercetin glycosides, which influenced the medicinal properties of the Melia leaves. Melia azedarach L. wild type leaf extracts are a promising natural resource for managing breast cancer.
| S-EPMC7044715 | biostudies-literature
Project description:The leaves of Azadirachta indica L. and Melia azedarach L., belonging to Meliaceae family, have been shown to have medicinal benefits and are extensively employed in traditional folk medicine. Herein, HPLC analysis of the ethyl acetate fraction of the total methanolic extract emphasized the enrichment of both A. indica L., and M. azedarach L. leaves extracts with phenolic and flavonoids composites, respectively. Besides, 4 limonoids and 2 flavonoids were isolated using column chromatography. By assessing the in vitro antiviral activities of both total leaves extracts against Severe Acute Respiratory Syndrome Corona virus 2 (SARS-CoV-2), it was found that A. indica L. and M. azedarach L. have robust anti-SARS-CoV-2 activities at low half-maximal inhibitory concentrations (IC50) of 8.451 and 6.922 μg/mL, respectively. Due to the high safety of A. indica L. and M. azedarach L. extracts with half-maximal cytotoxic concentrations (CC50) of 446.2 and 351.4 μg/ml, respectively, both displayed extraordinary selectivity indices (SI>50). A. indica L. and M. azedarach L. leaves extracts could induce antibacterial activities against both Gram-negative and positive bacterial strains. The minimal inhibitory concentrations of A. indica L. and M. azedarach L. leaves extracts varied from 25 to 100 mg/mL within 30 min contact time towards the tested bacteria. Our findings confirm the broad-spectrum medicinal value of A. indica L. and M. azedarach L. leaves extracts. Finally, additional in vivo investigations are highly recommended to confirm the anti-COVID-19 and antimicrobial activities of both plant extracts.
| S-EPMC9994683 | biostudies-literature
Project description:Melia azedarach cultivar:JPN11 Genome sequencing and assembly
| PRJNA906622 | ENA
Project description:The estrogen hormone dependent accounts for a major cause in the incidence of women breast cancer. Thus, their receptor, especially the estrogen receptor α (ER-α), is becoming a target in endocrine treatment. These ligand-inducible nuclear functions are regulated by an array of phytochemical and synthetic compounds, such as 17 β-estradiol and tamoxifen (4-hydroxytamoxifen [4OHT]). The Chinaberry (Melia azedarach) leaves are known naturally for relieving internal and external diseases. Previous studies revealed the potency of Melia's ethanolic extract and ethyl acetate fractions as anticancer; furthermore, this study aimed to resolve possible ER-α antagonist's mechanism and safety from M. azedarach leaves ethyl acetate fraction contents. Melia's phytochemical content was analyzed with electrospray ionization liquid chromatography-mass spectrometry, while its ER-α antagonist's potency was investigated by in silico. The computational docking was used to 3ERT (a human ER-α-4OHT binding domain complex) with Autodock Vina and related programs. The results presented Energy binding (ΔG) of Melia's quercetin 3-O-(2'',6''-digalloyl)-β-D-galactopyranoside was similar to 4OHT, and lower than its agonist 17 β-estradiol. Furthermore, the toxicity prediction of these compounds were revealed safer than 4OHT. The Melia's leaves ethyl acetate fraction, therefore, is a potential pharmacological material for further studies.
| S-EPMC8300330 | biostudies-literature
Project description:Melia azedarach L. is an important economic tree widely distributed in tropical and subtropical regions of China and some other countries. However, it is unclear how the species' suitable habitat will respond to future climate changes. We aimed to select the most accurate one among seven data mining models to predict the current and future suitable habitats for M. azedarach in China. These models include: maximum entropy (MaxEnt), support vector machine (SVM), generalized linear model (GLM), random forest (RF), naive bayesian model (NBM), extreme gradient boosting (XGBoost), and gradient boosting machine (GBM). A total of 906 M. azedarach locations were identified, and sixteen climate predictors were used for model building. The models' validity was assessed using three measures (Area Under the Curves (AUC), kappa, and overall accuracy (OA)). We found that the RF provided the most outstanding performance in prediction power and generalization capacity. The top climate factors affecting the species' suitable habitats were mean coldest month temperature (MCMT), followed by the number of frost-free days (NFFD), degree-days above 18 °C (DD > 18), temperature difference between MWMT and MCMT, or continentality (TD), mean annual precipitation (MAP), and degree-days below 18 °C (DD < 18). We projected that future suitable habitat of this species would increase under both the RCP4.5 and RCP8.5 scenarios for the 2011-2040 (2020s), 2041-2070 (2050s), and 2071-2100 (2080s). Our findings are expected to assist in better understanding the impact of climate change on the species and provide scientific basis for its planting and conservation.
| S-EPMC9308798 | biostudies-literature
Project description:BACKGROUND:MAPK/ERK kinases transmit signals from many growth factors/kinase receptors during normal cell growth/differentiation, and their dysregulation is a hallmark of diverse types of cancers. A plethora of drugs were developed to block this kinase pathway for clinical application. With the exception of a recently identified agent, EQW, most of these inhibitors target upstream factors but not ERK1/2; no activator of ERK1/2 is currently available. METHOD:A library of compounds isolated from medicinal plants of China was screened for anti-cancer activities. Three limonoid compounds, termed A1541-43, originally isolated from the plant Melia azedarach, exhibiting strong anti-leukemic activity. The anti-neoplastic activity and the biological target of these compounds were explored using various methods, including western blotting, flow cytometry, molecular docking and animal model for leukemia. RESULTS:Compounds A1541-43, exhibiting potent anti-leukemic activity, was shown to induce ERK1/2 phosphorylation. In contrast, the natural product Cedrelone, which shares structural similarities with A1541-43, functions as a potent inhibitor of ERK1/2. We provided evidence that A1541-43 and Cedrelone specifically target ERK1/2, but not the upstream MAPK/ERK pathway. Computational docking analysis predicts that compounds A1541-43 bind a region in ERK1/2 that is distinct from that to which Cedrelone and EQW bind. Interestingly, both A1541-43, which act as ERK1/2 agonists, and Cedrelone, which inhibit these kinases, exerted strong anti-proliferative activity against multiple leukemic cell lines, and induced robust apoptosis as well as erythroid and megakaryocytic differentiation in erythroleukemic cell lines. These compounds also suppressed tumor progression in a mouse model of erythroleukemia. CONCLUSIONS:This study identifies for the first time activators of ERK1/2 with therapeutic potential for the treatment of cancers driven by dysregulation of the MAPK/ERK pathway and possibly for other disorders.
| S-EPMC6679490 | biostudies-literature