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藜芦中生物碱的抗肿瘤和抗血小板活性。

Antitumor and antiplatelet activity of alkaloids from veratrum dahuricum.

机构信息

School of Pharmacy, Shanghai Jiao Tong University, Shanghai, PR China.

出版信息

Phytother Res. 2010 Jun;24(6):821-6. doi: 10.1002/ptr.3022.

Abstract

Ten steroidal alkaloids - cyclopamine, veratramine, jervine, 3, 15-diangyloylgermine, 3-angyloylzygadenine, 3-veratroyl zygadenine, 15-veratroylgermine, germine, veratrosine and pseudojervine - from Veratrum dahuricum, together with the ethanol extract and total alkaloids, were evaluated for their antitumor and antiplatelet activities. Cyclopamine, veratramine and germine significantly inhibited the hedgehog pathway in NIH/3T3 cells. Cyclopamine exerted a potent inhibitory effect against the growth of PANC-1 tumors in mice, with inhibition rates of 40.64%, 44.37%, 46.77% at doses of 5.0, 15.0 and 50.0 mg kg-1, respectively. Veratroylgermine was found to produce the strongest inhibition against the platelet aggregation induced by arachidonic acid, with inhibition rate of 92.0% at 100 microM.

摘要

从唐松草属植物中分离得到了 10 种甾体生物碱 - 羊角拗次碱、藜芦胺、金刚烷、3,15-二当归酰基金雀花碱、3-当归酰基千金藤啶碱、3-藜芦酰基千金藤啶碱、金雀花碱、藜芦酰酪氨酸和伪金刚烷 - 以及乙醇提取物和总生物碱,评估它们的抗肿瘤和抗血小板活性。羊角拗次碱、藜芦胺和金雀花碱显著抑制了 NIH/3T3 细胞中的刺猬通路。羊角拗次碱对小鼠 PANC-1 肿瘤的生长具有很强的抑制作用,在 5.0、15.0 和 50.0 mg/kg 剂量下的抑制率分别为 40.64%、44.37%和 46.77%。藜芦酰基金雀花碱对花生四烯酸诱导的血小板聚集抑制作用最强,在 100 microM 时抑制率为 92.0%。

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