Mukherjee Avinaba, Sadhukhan Gobinda Chandra
Department of Pharmaceutical Technology, Natural Science Laboratory, Jadavpur University, Kolkata, India.
UGC-Human Resource Development Sector, Jadavpur University, Kolkata, West Bengal, India.
J Pharmacopuncture. 2016 Mar;19(1):7-15. doi: 10.3831/KPI.2016.19.001.
Malaria has been a major global health problem in recent times with increasing mortality. Current treatment methods include parasiticidal drugs and vaccinations. However, resistance among malarial parasites to the existing drugs has emerged as a significant area of concern in anti-malarial drug design. Researchers are now desperately looking for new targets to develop anti-malarials drug which is more target specific. Malarial parasites harbor a plastid-like organelle known as the 'apicoplast', which is thought to provide an exciting new outlook for the development of drugs to be used against the parasite. This review elaborates on the current state of development of novel compounds targeted againstemerging malaria parasites.
The apicoplast, originates by an endosymbiotic process, contains a range of metabolic pathways and housekeeping processes that differ from the host body and thereby presents ideal strategies for anti-malarial drug therapy. Drugs are designed by targeting the unique mechanism of the apicoplasts genetic machinery. Several anabolic and catabolic processes, like fatty acid, isopenetyl diphosphate and heme synthess in this organelle, have also been targeted by drugs.
Apicoplasts offer exciting opportunities for the development of malarial treatment specific drugs have been found to act by disrupting this organelle's function, which wouldimpede the survival of the parasite.
Recent advanced drugs, their modes of action, and their advantages in the treatment of malaria by using apicoplasts as a target are discussed in this review which thought to be very useful in desigining anti-malarial drugs. Targetting the genetic machinery of apicoplast shows a great advantange regarding anti-malarial drug design. Critical knowledge of these new drugs would give a healthier understanding for deciphering the mechanism of action of anti-malarial drugs when targeting apicoplasts to overcome drug resistance.
近年来，疟疾一直是一个重大的全球健康问题，死亡率不断上升。目前的治疗方法包括杀寄生虫药物和疫苗接种。然而，疟原虫对现有药物的耐药性已成为抗疟疾药物设计中一个重要的关注领域。研究人员目前正迫切寻找新的靶点来开发更具靶点特异性的抗疟疾药物。疟原虫含有一种称为“顶质体”的类质体细胞器，被认为为开发针对该寄生虫的药物提供了令人兴奋的新前景。本综述阐述了针对新兴疟原虫的新型化合物的当前开发状况。
顶质体起源于内共生过程，包含一系列与宿主体内不同的代谢途径和管家过程，从而为抗疟疾药物治疗提供了理想的策略。通过针对顶质体遗传机制的独特作用机制来设计药物。该细胞器中的一些合成代谢和分解代谢过程，如脂肪酸、异戊烯基二磷酸和血红素合成，也已成为药物的作用靶点。
顶质体为开发疟疾特异性治疗药物提供了令人兴奋的机会，已发现这些药物通过破坏该细胞器的功能来发挥作用，这将阻碍寄生虫的生存。
本综述讨论了最近的先进药物、它们的作用方式以及以顶质体为靶点治疗疟疾的优势，认为这对设计抗疟疾药物非常有用。针对顶质体的遗传机制在抗疟疾药物设计方面显示出巨大优势。对这些新药的关键了解将有助于更深入地理解以顶质体为靶点克服耐药性的抗疟疾药物的作用机制。
