氯喹 二磷酸盐

一般描述

氯喹是喹诺酮家族的一员，是一种弱的嵌入剂。氯喹用于治疗阿米巴病、类风湿性关节炎、盘状和系统性红斑狼疮。

Chloroquine effectively eliminates the erythrocytic forms of malaria parasites at all developmental stages, although it does not impact the sporozoites. It also functions as an antibiotic. In addition, it can be utilized at a concentration of 200 mg/mL (PBS, pH 5.0) to dissociate antigen-antibody complexes without denaturing red blood cell antigens. Recent research indicates chloroquine′s potential as an antitumor medication for cancer treatment along with chemotherapy and radiation. Its antimalarial effects are achieved by inhibiting the polymerization of heme into hemozoin, which serves as a food source for the malarial parasite. Chloroquine forms a complex with the drug-hemozoin, capping the polymerizing chain and preventing further polymerization. As a result, free heme accumulates in the food vacuole, exerting toxic effects on the parasite. Additionally, chloroquine acts as an anti-autoimmune therapy by binding to transcriptional factors on T helper 17 cells and inhibiting their differentiation.Chloroquine diphosphate (CQ) is frequently employed as an inhibitor of the autophagic pathway. The combined use of chloroquine diphosphate and salidroside initiates apoptosis in human liver cells by modulating mitochondrial dysfunction and autophagy.

应用

DNA嵌入剂。还可用于提高转染效率。
氯喹二磷酸盐已用于：

· 体外抗疟原虫试验

· 转染及感染试验

· 自噬抑制

· 诱导多能干细胞（iPS）分化成心肌细胞

· 感染血液的流动治疗

生化/生理作用

标准的抗疟疾药物。在多药耐药细胞系中用作MRP的底物并通过基于*啉的光活性药物IAAQ（N-[4-[1-羟基-2-（二丁基氨基）乙基]*啉-8-基] -4-叠氮基水杨酰胺）抑制MRP的光亲和标记。