Anti-angiogenic effects of rhubarb and its anthraquinone derivatives
Anti-angiogenic effects of rhubarb and its anthraquinone derivatives
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DOI：
10.1016/j.jep.2008.11.008
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发表时间：
2009-01-21
影响因子：
5.4
通讯作者：
But, Paul Pui-Hay
中科院分区：
文献类型：
--
作者：
He, Zhi-Heng;He, Ming-Fang;But, Paul Pui-Hay
民族药理学相关性：大黄（大黄）经常作为一种成分被包括在治疗炎症性疾病的传统中药复方处方中。这种应用可能通过抗血管生成介导，从而揭示其在癌症治疗中的潜在价值。摘要目的：研究大黄不同部位及蒽醌衍生物对斑马鱼胚胎血管形成的抑制作用，探讨其抗血管生成的作用。材料与方法：采用定量内源性碱性磷酸酶法和染色法，对大黄根及5种蒽醌衍生物95%乙醇提取物及4个后续部位（正己烷、乙酸乙酯、正丁醇和水相）在斑马鱼模型上进行研究。结果：乙酸乙酯部位对血管形成的抑制作用最强，达到52%。三种蒽醌（芦荟大黄素）。大黄素和大黄素显示出较强的抗血管生成活性。结论：大黄根的血管生成特性可能是其治疗炎性疾病的部分原因。在C-6或C-3位置具有酸性或极性亲水性取代的蒽醌类化合物在抑制血管生成中起重要作用。这进一步支持了斑马鱼血管生成模型的价值。2008爱思唯尔爱尔兰有限公司版权所有。
Ethnopharmacological relevance: Rhubarb root (Dahuang) is often included as an ingredient in traditional Chinese compound prescriptions for the treatment of inflammatory diseases. This application may possibly be mediated through anti-angiogensis and thus would shed light on its potential value in cancer therapy.Aim of tire study: To elucidate the anti-angiogenic properties of rhubarb root, we tested the inhibitory effects of different fractions and a series of anthraquinone derivatives against vessel formation in zebrafish embryos.Materials and methods: The 95% ethanol extract and four subsequent fractions (n-hexane, ethyl acetate, n-butanol and aqueous fractions) of rhubarb root and five anthraquinone derivatives were investigated on zebrafish model by quantitative endogenous alkaline phosphatase assay and staining assay.Results: Ethyl acetate fraction showed the strongest inhibition of vessel formation by 52%. Three anthraquinones (aloe-emodin. emodin and rhein) displayed potent anti-angiogenic activities.Conclusions: The angiogenic properties of rhubarb root may partly account for its use in inflammatory diseases. The anthraquinones with acidic or polar, hydrophilic substitution at C-6 or C-3 positions played a substantial role in inhibiting angiogenesis. The value of the zebrafish angiogenic model is further supported. (C) 2008 Elsevier Ireland Ltd. All rights reserved.