Ye Z, Van Dyke K
Department of Pharmacology, China Academy of Traditional Chinese Medicine, Beijing, China.
Parasite. 1994 Sep;1(3):211-8. doi: 10.1051/parasite/1994013211.
Antimalarial activities of tetracycline (TC) and erythromycin (EM), alone or in combination with artemisinin (Qinghaosu, QHS), were studied using chloroquine (CQ)-sensitive (D6) and -resistant (W2) strains of Plasmodium falciparum in vitro. The antimalarial potency of TC (IC50 = 9862 nM for the CQ-sensitive parasite, 32414 nM for the CQ-resistant one) or EM (IC50 = 45787 nM for the CQ-sensitive parasite, 33397 nM for the CQ-resistant one) was much less than that of QHS (IC50 ranging from 25 to 40 nM). The CQ-resistant falciparum parasite displayed a cross-resistance to TC, while both the drug-sensitive and -resistant parasites exhibited similar responses to EM. However, antimalarial potency of EM appeared to be less than that of TC against the drug-sensitive parasite. When TC was combined with QHS, an additive interaction was observed against the CQ-sensitive falciparum parasite, while synergism was found with the CQ-resistant parasite. When EM was tested in combination with QHS, a potentiating interaction occurred with both the CQ-sensitive and resistant falciparum parasite. The above results indicated that the QHS combination with either TC or EM may be a promising antimalarial preparation with low recrudescence compared to artemisinin used alone in clinical practice.
在体外，使用氯喹敏感（D6）和耐药（W2）的恶性疟原虫株，研究了四环素（TC）和红霉素（EM）单独或与青蒿素（青蒿素，QHS）联合使用时的抗疟活性。TC（对氯喹敏感寄生虫的IC50 = 9862 nM，对氯喹耐药寄生虫的IC50 = 32414 nM）或EM（对氯喹敏感寄生虫的IC50 = 45787 nM，对氯喹耐药寄生虫的IC50 = 33397 nM）的抗疟效力远低于QHS（IC50范围为25至40 nM）。氯喹耐药的恶性疟原虫对TC表现出交叉耐药性，而药物敏感和耐药的寄生虫对EM表现出相似的反应。然而，EM对药物敏感寄生虫的抗疟效力似乎低于TC。当TC与QHS联合使用时，对氯喹敏感的恶性疟原虫观察到相加作用，而对氯喹耐药的寄生虫则发现协同作用。当EM与QHS联合测试时，对氯喹敏感和耐药的恶性疟原虫均出现增效作用。上述结果表明，与临床实践中单独使用青蒿素相比，QHS与TC或EM联合使用可能是一种有前景的抗疟制剂，复发率较低。
