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An antitumor promoter from Moringa oleifera Lam.

机译:来自辣木的抗肿瘤启动子。

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In the course of studies on the isolation of bioactive compounds from Philippine plants, the seeds of Moringa oleifera Lam. were examined and from the ethanol extract were isolated the new O-ethyl-4-(alpha-L-rhamnosyloxy)benzyl carbamate (1) together with seven known compounds, 4(alpha-L-rhamnosyloxy)-benzyl isothiocyanate (2), niazimicin (3), niazirin (4), beta-sitosterol (5), glycerol-1-(9-octadecanoate) (6), 3-O-(6'-O-oleoyl-beta-D-glucopyranosyl)-beta-sitosterol (7), and beta-sitosterol-3-O-beta-D-glucopyranoside (8). Four of the isolates (2, 3, 7, and 8), which were obtained in relatively good yields, were tested for their potential antitumor promoting activity using an in vitro assay which tested their inhibitory effects on Epstein-Barr virus-early antigen (EBV-EA) activation in Raji cells induced by the tumor promoter, 12-O-tetradecanoyl-phorbol-13-acetate (TPA). All the tested compounds showed inhibitory activity against EBV-EA activation, with compounds 2, 3 and 8 having shown very significant activities. Based on the in vitro results, niazimicin (3) was further subjected to in vivo test and found to have potent antitumor promoting activity in the two-stage carcinogenesis in mouse skin using 7,12-dimethylbenz(a)anthracene (DMBA) as initiator and TPA as tumor promoter. From these results, niazimicin (3) is proposed to be a potent chemo-preventive agent in chemical carcinogenesis. Copyright 1999 Elsevier Science B.V.
机译:在从菲律宾植物中分离生物活性化合物的研究过程中,辣木的种子。检查并从乙醇提取物中分离出新的O-乙基-4-(α-L-鼠李糖氧基)苄基氨基甲酸酯(1)和7种已知化合物,4(α-L-鼠李糖氧基)-异硫氰酸苄酯(2),烟酰胺(3),烟酰胺(4),β-谷甾醇(5),甘油-1-(9-十八烷酸酯)(6),3-O-(6'-O-油酰基-β-D-吡喃葡萄糖基)-β -谷甾醇(7)和β-谷甾醇-3-O-β-D-吡喃葡萄糖苷(8)。使用体外试验检测了以较高收率获得的四个分离株(2、3、7和8)的潜在抗肿瘤促进活性,该试验检测了它们对爱泼斯坦-巴尔病毒早期抗原( EBV-EA)由肿瘤启动子12-O-十四烷酰-phorbol-13-乙酸酯(TPA)诱导的Raji细胞激活。所有测试的化合物均显示出对EBV-EA活化的抑制活性,其中化合物2、3和8具有非常重要的活性。根据体外结果,进一步对烟酰胺(3)进行了体内测试,发现使用7,12-二甲基苯并(a)蒽(DMBA)作为引发剂在小鼠皮肤的两阶段癌变中具有有效的抗肿瘤促进活性。和TPA作为肿瘤促进剂。根据这些结果,提出了烟酰胺(3)是化学致癌作用中的有效化学预防剂。版权所有1999 Elsevier Science B.V.

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