School of Medical and Allied Sciences, G.D. Goenka University, Sohna-Gurgaon Road, Sohna, 122103, Gurugram, Haryana, India.
Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research, Delhi Pharmaceutical Sciences and Research University, New Delhi, 110017, India.
Mini Rev Med Chem. 2022;22(12):1607-1618. doi: 10.2174/1389557521666211124143117.
Among all the parasitic diseases in humans, malaria is the most significant and malicious one. The widespread species are Plasmodium falciparum and Plasmodium vivax, but the infection caused by the former is the deadliest. According to the November 2018 report of the World Health Organization (WHO), a total of 219 million cases of malaria were reported globally in 2017, which led to an estimated 435,000 deaths. Mortality due to malaria is estimated at 1.5 - 2.7 million deaths each year. Among all the complications associated with Plasmodium falciparum infection, cerebral malaria (CM) is the most fretful, accounting for almost 13% of all malaria-related deaths. CM is a medical emergency that requires immediate clinical testing and treatment. A compromised microcirculation, with sequestration of parasitized erythrocytes, is central in the disease pathology. No effective therapeutic agents are available yet for the treatment of CM, and therefore, potential interventions are needed to be developed urgently. The currently available anti-malarial drugs lack lipophilicity and are thus not able to reach the brain tissues. Therefore, safe, cost-effective agents with improved lipophilicity possessing the potential to target brain tissues are needed to be searched in order to fight CM worldwide. The aim of present review is to systematically revise the published research work available concerning the development and evaluation of some potential drug targets in the management of CM.
在人类所有寄生虫病中，疟疾是最严重和最具危害性的一种。广泛存在的疟原虫物种包括恶性疟原虫和间日疟原虫，但前者引起的感染最为致命。根据世界卫生组织（WHO）2018 年 11 月的报告，2017 年全球共报告了 2.19 亿例疟疾病例，导致约 43.5 万人死亡。疟疾导致的死亡率估计每年为 150 万至 270 万人。在与恶性疟原虫感染相关的所有并发症中，脑型疟疾（CM）最为令人担忧，占所有与疟疾相关死亡的近 13%。CM 是一种医疗紧急情况，需要立即进行临床检测和治疗。微循环受损，寄生红细胞被隔离，是疾病病理的核心。目前尚无有效的治疗 CM 的药物，因此需要紧急开发潜在的干预措施。目前可用的抗疟药物缺乏亲脂性，因此无法到达脑组织。因此，需要寻找具有亲脂性、安全性和成本效益的潜在靶向脑组织的药物，以在全球范围内对抗 CM。本综述的目的是系统地回顾已发表的研究工作，探讨一些潜在药物靶点在 CM 管理中的开发和评估。
