Powers K G, Jacobs R L
Antimicrob Agents Chemother. 1972 Jan;1(1):49-53. doi: 10.1128/AAC.1.1.49.
The chloroquine-resistant Oak Knoll strain of Plasmodium falciparum, recently adapted to the owl monkey (Aotus trivirgatus), was insusceptible to chloroquine therapy. Two chlorinated lincomycin analogues tested in this host-parasite system cured blood-induced infections. Acute infections were treated orally for 7 consecutive days with either 15 or 75 mg of clindamycin hydrochloride (U-21) per kg per day, 10 or 50 mg of N-demethyl-4'-pentyl clindamycin hydrochloride (U-24) per kg per day, or 20 mg of chloroquine base per kg per day. These lincomycin analogues cleared trophozoites from the peripheral blood by the end of the 7-day treatment period. The speed of clearance of parasites was not dose-related, but curative activity appeared dependent upon the amount of drug given as well as the number of daily treatments. The efficacy of U-21 and U-24 is of particular interest since they represent major structural departures from compounds commonly used in the treatment of malaria.
对氯喹耐药的恶性疟原虫奥克诺尔株最近适应了夜猴（三带犰狳），对氯喹治疗不敏感。在这个宿主-寄生虫系统中测试的两种氯化林可霉素类似物治愈了血液感染。急性感染连续7天口服治疗，每天每公斤体重给予15或75毫克盐酸克林霉素（U-21）、10或50毫克盐酸N-去甲基-4'-戊基克林霉素（U-24）或20毫克氯喹碱。这些林可霉素类似物在7天治疗期结束时清除了外周血中的滋养体。寄生虫清除速度与剂量无关，但治愈活性似乎取决于给药量以及每日治疗次数。U-21和U-24的疗效特别令人感兴趣，因为它们与常用于治疗疟疾的化合物在结构上有很大差异。
