大黄蒽醌类化学成分和药理作用研究进展

大黄的药用历史悠久、资源丰富,最早记载于《神农本草经》,药用大黄为掌叶大黄(Rheum palmatum),唐古特大黄(R.tanguticum)和药用大黄(R.officinale)3种,为临床常用药之一,具有清热泻火、凉血解毒、逐瘀通经、利湿退黄之功效。大黄中的蒽醌类化合物为9,10-蒽醌,羟基分布于两侧苯环上。蒽醌按母核结构可分为单蒽核类蒽醌与双蒽核类蒽醌,单蒽核类蒽醌含有游离型蒽醌和结合型蒽醌两类,目前已经报道的大黄蒽醌类化合物约有50个,其中单蒽核类型蒽醌类化合物34种,双蒽核类型蒽醌类化合物16种。蒽醌类化合物是大黄中一类重要的活性成分,具有抗炎、抗肿瘤、保护心血管、保肝、护肺、改善脑损伤、治疗肾纤维化等广泛的生物活性。通过查阅、整理国内外有关大黄蒽醌类化合物的文献资料,对其化学成分和近十年国内外药理研究进行归纳总结,分析其研究和开发前景,以期为大黄蒽醌类成分的深入研究和开发利用提供科学依据。未来,可继续深入对大黄蒽醌类化合物及其衍生产物的研究,为其合理应用及开发具有良好临床治疗效果的新药奠定基础。

Research Progress on Chemical Constituents and Pharmacological Action of Anthraquinone in Rhei Radix et Rhizoma

Rhei Radix et Rhizoma is one of the most common traditional Chinese medicines. It has rich resources in China and was earliest recorded in Shennong''s Herbal Classic. Among Rhei Radix et Rhizoma,only Rheum palmatum,R. tanguticum and R. officinale are used as medical materials and are commonly used in clinical application. It is recorded to possess the efficacy of eliminating heat and purging internal heat,cooling blood and detoxifying, dissipating blood stasis and promoting blood circulation, as well as removing dampness and relieving jaundice. The anthraquinone components in Rhei Radix et Rhizoma are 9,10-anthraquinone and the hydroxyls are distributed on two-sided benzene rings. Anthraquinones can be divided into anthraquinone and bianthraquinone according to the structure of the mother nucleus. There are about 50 reported anthraquinone components,consisting of 34 anthraquinones and 16 bianthraquinones. Anthraquinones,as an important component in Rhei Radix et Rhizoma, have broad effects of anti-inflammatory,anti-tumor,protecting cardiovascular system,liver and lung,improving brain injury and treating renal fibrosis. By referring to relevant papers at home and abroad,the researches on chemical and pharmacological effects of anthraquinones from Rhei Radix et Rhizoma in the last decade were summarized and the prospects of research and development were also analyzed for further study and comprehensive utilization of these anthraquinones. In the future, the further researches on anthraquinones and their derivatives should be done to lay a foundation for the rational application and development of new drugs with good clinical curative effect.