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目的研究虎杖Polygonum cuspidatum中的抗补体活性蒽醌类成分及其作用靶点。方法采用溶血试验法进行抗补体活性成分的导向分离,对所得化合物进行抗补体活性测定,并利用补体缺失血清鉴定主要活性化合物的作用靶点。结果从虎杖醋酸乙酯活性部位分离得到10个蒽醌类和3个其他类成分,分别鉴定为大黄素甲醚(1)、大黄酚(2)、大黄素-8-甲醚(3)、大黄素-8-O-β-D-葡萄糖苷(4)、大黄素(5)、大黄酸(6)、迷人醇(7)、6-羟基芦荟大黄素(8)、xanthorin(9)、isorhodoptilometrin(10)、2,5-二甲基-7-羟基-色原酮(11)、7-羟基-4-甲氧基-5-甲基-香豆素(12)和5,7-二羟基-异苯并呋喃酮(13)。化合物9、10为首次从蓼科中分离得到,化合物9是首次从虎杖中发现的茜草素型蒽醌;化合物3~9对补体系统的经典和旁路途径有不同程度的抑制活性,以化合物7的活性最显著[CH50=(6±2)μg/mL;AP50=(50±5)μg/mL]。靶点研究表明,化合物4作用于补体系统的C1q、C2及C9组分;化合物7作用于C1q、C2、C4及C9组分。结论蒽醌类化合物是虎杖的主要抗补体活性成分,迷人醇活性强、靶点明确,值得深入研究。
Objective To study the anti-complement active anthraquinones in Polygonum cuspidatum and its target. Methods Hemolysis was used to guide the separation of anti-complement active ingredients. Anti-complement activity was measured on the obtained compounds. The target of the active compounds was identified by serum-free complement. Results Ten anthraquinones and three other components were isolated from the active site of Polygonum cuspidatum and identified as physicochemical properties of physcion (1), chrysophanol (2), emodin-8-methyl ether (3) Emodin (8), xanthorin (9), emodin (8), emodin (9), emodin isorhodoptilometrin (10), 2,5-dimethyl-7-hydroxy-chromogen (11), 7-hydroxy-4-methoxy-5-methyl-coumarin (12) Dihydroxy-isobenzofuranone (13). Compounds 9 and 10 were isolated from Polygonaceae for the first time. Compound 9 was the first anthraquinone found in Polygonum cuspidatum. Compounds 3 and 9 showed inhibitory activities to classical and alternative pathway of complement. 7 was the most significant [CH50 = (6 ± 2) μg / mL; AP50 = (50 ± 5) μg / mL]. Targeting studies showed that compound 4 acted on the C1q, C2 and C9 components of the complement system; compound 7 acted on the C1q, C2, C4 and C9 components. CONCLUSION Anthraquinones are the main anti-complement active ingredients of Polygonum cuspidatum. Their attractive alcohol activity is strong and their targets are clear, which deserves further study.