QUINOLINE ANTIMALARIAL-DRUGS INHIBIT SPONTANEOUS FORMATION OF BETA-HEMATIN (MALARIA PIGMENT)
QUINOLINE ANTIMALARIAL-DRUGS INHIBIT SPONTANEOUS FORMATION OF BETA-HEMATIN (MALARIA PIGMENT)
复制标题
DOI：
10.1016/0014-5793(94)00921-x
复制
发表时间：
1994-09-19
期刊：
影响因子：
3.5
通讯作者：
ADAMS, PA
中科院分区：
文献类型：
--
作者：
EGAN, TJ;ROSS, DC;ADAMS, PA
用红外光谱法研究了血红素在酸性醋酸溶液中聚合成β -血红素（血色素或疟疾色素）。该反应在6 ~ 65℃，0.1 ~ 4.5 M醋酸盐，pH 4.2 ~ 5.0之间自发发生。抗疟疾药物奎宁、氯喹和阿莫地喹被发现可以阻断自发的-血红素形成，而抗疟疾无效的9-epiquinine和8-羟基喹啉对该反应没有影响，伯氨喹也没有影响，这种药物仅对红细胞外感染阶段有效。有人认为，红细胞内活性抗疟疾药物的作用是通过与血红素结合，阻断-血红素的形成，并将有毒的血红素留在寄生虫的食物液泡中。
Polymerisation of haematin to beta-haematin (haemozoin or malaria pigment) in acidic acetate solutions was studied using infrared spectroscopy. The reaction was found to occur spontaneously between 6 and 65 degrees C, in 0.1-4.5 M acetate and pH 4.2-5.0. The anti-malarial drugs quinine, chloroquine and amodiaquin were found to block spontaneous beta-haematin formation, while the anti-malarially inactive 9-epiquinine and 8-hydroxyquinoline had no effect on the reaction, as did primaquine, a drug which is active only against exo-erythrocytic stages of infection. It is argued that the intra-erythrocytically active anti-malarial agents act by binding to haematin, blocking beta-haematin formation and leaving toxic haematin in the parasite food vacuoles.