啮齿动物疟疾的化学疗法，XL。青蒿素及相关倍半萜的作用。

The chemotherapy of rodent malaria, XL. The action of artemisinin and related sesquiterpenes.

作者信息

Peters W, Li Z L, Robinson B L, Warhurst D C

出版信息

Ann Trop Med Parasitol. 1986 Oct;80(5):483-9. doi: 10.1080/00034983.1986.11812054.

DOI:10.1080/00034983.1986.11812054

Abstract

Artemisinin (Qinghaosu), a poorly soluble sesquiterpene lactone derived from the plant Artemisia annua Linn., and a number of more soluble, semi-synthetic derivatives are rapidly-acting blood schizontocides against Plasmodium berghei and P. yoelii nigeriensis. An oily suspension of artemisinin given s.c. is more effective than aqueous suspensions. The activity is retained against lines resistant to primaquine, cycloguanil, pyrimethamine, sulphonamides, mefloquine and menoctone, but a highly chloroquine-resistant line is much less sensitive. Artemisinin has no causal prophylactic, gametocytocidal or sporontocidal action. Dihydroartemisinin causes the pigment of P. berghei to clump, but in a different fashion from the pigment changes induced by chloroquine or quinine, reflecting a different mode of action of the sesquiterpenes from that of these other antimalarials.

摘要

青蒿素（青蒿琥酯）是一种从植物黄花蒿中提取的难溶性倍半萜内酯，以及一些更易溶的半合成衍生物，是对伯氏疟原虫和约氏疟原虫尼日尔株有快速作用的血内裂殖体杀灭剂。皮下注射的青蒿素油悬液比水悬液更有效。其活性对耐伯氨喹、环氯胍、乙胺嘧啶、磺胺类、甲氟喹和甲萘醌的品系仍然有效，但对高度耐氯喹的品系敏感性要低得多。青蒿素没有病因性预防、杀配子体或杀孢子体作用。双氢青蒿素会使伯氏疟原虫的色素结块，但方式与氯喹或奎宁引起的色素变化不同，这反映了倍半萜与其他抗疟药的作用方式不同。