Ajayi F O, Salako L A, Kuye J O
Department of Pharmacology & Therapeutics, University of Ibadan, Nigeria.
Afr J Med Med Sci. 1989 Jun;18(2):95-100.
The partitioning of chloroquine and its two desethyl metabolites between red blood cells (RBCs) and plasma was studied in vitro, using blood from healthy adults and from children with Plasmodium falciparum parasitaemia. Blood from the volunteers was incubated with varying concentrations of chloroquine (CQ), desethylchloroquine (DCQ) and bisdesethyl-chloroquine (BDCQ) for 15 min and the RBC/plasma concentration ratio determined. Desethylchloroquine and BDCQ were concentrated in the red cells of uninfected blood to the same extent as chloroquine. On the other hand, DCQ and BDCQ were concentrated to a significantly lower extent than CQ in the red cells from malarial children. The reduced ability of infected RBCs to concentrate DCQ and BDCQ may have an important bearing on the development of resistance to chloroquine by P. falciparum.
利用健康成年人以及患有恶性疟原虫血症儿童的血液，在体外研究了氯喹及其两种去乙基代谢物在红细胞（RBC）与血浆之间的分配情况。将志愿者的血液与不同浓度的氯喹（CQ）、去乙基氯喹（DCQ）和双去乙基氯喹（BDCQ）孵育15分钟，然后测定红细胞/血浆浓度比。去乙基氯喹和双去乙基氯喹在未感染血液的红细胞中的浓缩程度与氯喹相同。另一方面，在疟疾患儿的红细胞中，DCQ和BDCQ的浓缩程度明显低于CQ。受感染红细胞浓缩DCQ和BDCQ能力的降低可能对恶性疟原虫对氯喹耐药性的产生具有重要影响。
