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青蒿素为从黄花蒿(Artemisia annua L.)中分得的具有过氧键的新型倍半萜内酯,其结构证明为Ⅰ。大量的动物实验和临床观察证明为高效、速效、低毒的抗疟新药。搞清其体内代谢转化及转化物的生理活性是有意义的,为此我们进行了青蒿素人体内代谢转化的研究。所用方法为间日疟病人口服青蒿素胶囊二天总量3.52g,正常人一天服用青蒿素2g,常法收集尿液和大便,均作空白对照。收集的尿液以乙酸乙酯萃取,萃取物经硅胶柱层或制备性薄层分离,通过理化数据、光谱分析并与标准样品对照,证明尿液代谢转化物为Ⅱ、Ⅳ、Ⅴ,它们对小白鼠柏氏疟模型无效。正常人口服青蒿素后的大便用氯仿搅溶,提取物主要为青蒿素原形。提示人口服青蒿素后,部分以原
Artemisinin is a novel sesquiterpene lactone with a peroxy bond assigned from Artemisia annua L. Its structure is proved to be I. A large number of animal experiments and clinical observations have proved to be highly effective, quick-acting, and low-toxic antimalarial drugs. It is of interest to understand the metabolism and the physiological activities of the transformants in vivo. For this reason, we have conducted studies on the metabolism of artemisinin in vivo. The method used was oral administration of artemisinin capsules for patients with vivax malaria in a total of 3.52 g for two days. Normal individuals were given 2 g of artemisinin for one day, and urine and stool were collected in a routine manner. All were used as blank controls. The collected urine was extracted with ethyl acetate. The extracts were separated on silica gel column or preparative thin layer. Through physicochemical data, spectral analysis and comparison with standard samples, it was proved that the urine metabolic converters were II, IV, V. The P. berghei mouse model was ineffective. After the oral administration of artemisinin to normal people, the stool was dissolved with chloroform and the extract was mainly of artemisinin. Prompt that after oral administration of artemisinin, some