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Selective Anti-proliferative Activity of Indole Alkaloids from Rhazya stricta Decne Leaves

机译:来自Rhazya Stricta Decne叶片的吲哚生物碱的选择性抗增殖活性

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Rhazya stricta is a rich indole alkaloid medicinal plant species, that is used in traditional medicine particularly in Middle East countries to treat inflammations, diabetes, rheumatism, and skin disorders. The alkaloid plant extract of R. stricta was fractionated on aluminum oxide column and further purified by different chromatographic methods. The chemical structures of the isolated compounds were elucidated by interpretation of their 1D and 2D NMR, IR, UV and MS spectral data. The potential antitumor effect was examined against three cancer cell lines; HCT-116-colon cancer, PC-3-prostate cancer and HepG2-liver cancer as well as a control cell line (Vero) using MTT assay. Two new indole alkaloids, identified as 16-epi-stemmadenine-N-oxide (1) and stemmadenine-N-methyl (2), along with the known indole alkaloid 20-epi-antirhine (3) were isolated from the leaves of Rhazya stricta. Compound 2, stemmadenine-N-methyl exhibited a reasonable selectivity index and a broad anticancer effect against the examined cell lines with IC50 35.0 +/- 0.7, 35.0 +/- 0.6, 40.0 +/- 07and 79.0 +/- 1.0 mu M, respectively. Furthermore, the effect of stemmadenine-N-methyl was evaluated on cell migration using wound-healing assay. It significantly hindered cell migration and delayed-wound healing. 16-epistemmadenine-N-oxide and stemmadenine-N-methyl are new indole alkaloids isolated from the leaves of Rhazya stricta, of which stemmadenine-N-methyl selectively inhibited the proliferation of three different cancer cell lines. In addition, it prevented cell migration and delayed wound-healing. Further studies are required to confirm the mechanism by which this promising alkaloid exhibits its antitumor activity.
机译:Rhazya Stricta是一种丰富的吲哚生物碱药用植物物种,用于传统医学,特别是在中东国家,治疗炎症,糖尿病,风湿病和皮肤病。 R. Strica的生物碱植物提取物在氧化铝柱上分离并通过不同的色谱方法进一步纯化。通过解释其1D和2D NMR,IR,UV和MS光谱数据来阐明分离的化合物的化学结构。检查潜在的抗肿瘤效果是否对三种癌细胞系进行检查; HCT-116-结肠癌,PC-3-前列腺癌和HepG2-肝癌以及使用MTT测定的对照细胞系(Vero)。从Rhazya的叶子中分离出两种新的吲哚生物碱(1)和Sypmadenine-N-甲基(2),与已知的吲哚生物碱20-Epi-intirhine(3)分离出来stricta。化合物2,STEMMADENINE-N-甲基表现出合理的选择性指数和针对IC50 35.0 +/- 0.7,35.0 +/- 0.6,49.0 +/- 07和79.0 +/- 1.0 mu m,分别。此外,使用伤口愈合测定对细胞迁移评价苯胺丁烯-N-甲基的影响。它显着阻碍细胞迁移和延迟伤口愈合。 16-EpiSemmadenine-N-氧化物和STEMMADENINE-N-甲基是从Rhazya Stricka的叶子中分离的新吲哚生物碱,其中STEMMADENINE-N-甲基选择性地抑制了三种不同癌细胞系的增殖。此外,它防止了细胞迁移和延迟伤口愈合。需要进一步的研究来确认该有前途的生物碱表现出其抗肿瘤活性的机制。

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