C.U. Shah College of Pharmacy, SNDT Women's University, Santacruz (West), Mumbai 400049, India.
Cipla Limited, Mumbai 400013, India.
Molecules. 2023 Jul 17;28(14):5472. doi: 10.3390/molecules28145472.
Malaria remains a life-threatening health problem and is responsible for the high rates of mortality and morbidity in the tropical and subtropical regions of the world. The increasing threat of drug resistance to available artemisinin-based therapy warrants an urgent need to develop new antimalarial drugs that are safer, more effective, and have a novel mode of action. Natural plants are an excellent source of inspiration in searching for a new antimalarial agent. This research reports a systematic investigation for determining the antimalarial potential of the seeds of . The study shows that the crude seed extract (CSE), protein, saponin, and the oily fractions of the seeds were nontoxic at a 2000 mg/kg body weight dose when tested in Wistar rats, thus revealing high safety is classified as class 5. The oily fraction, Annomaal, demonstrated pronounced antimalarial activity with low IC (1.25 ± 0.183 μg/mL) against in vitro. The CSE and Annomaal significantly inhibited the growth of parasites in vivo with 58.47% and 61.11% chemo suppression, respectively, while the standard drug artemether showed chemo suppression of 66.75%. Furthermore, the study demonstrated that oral administration of Annomaal at a daily dose of 250 mg/kg/day for 3 days was adequate to provide a complete cure to the -infected mice. Annomaal thus holds promise as being patient-compliant due to the shorter treatment schedule, eliminating the need for frequent dosing for extended time periods as required by several synthetic antimalarial drugs. Further studies are needed to determine the active compounds in the oily fraction responsible for antimalarial activity.
疟疾仍然是一个威胁生命的健康问题,是世界上热带和亚热带地区高死亡率和发病率的主要原因。现有青蒿素类疗法的耐药性威胁日益严重,因此迫切需要开发更安全、更有效、具有新作用模式的抗疟新药。天然植物是寻找新的抗疟药物的极好来源。本研究报告了一项系统的研究,旨在确定 的种子的抗疟潜力。研究表明,在 Wistar 大鼠中,当剂量为 2000mg/kg 体重时,粗提物(CSE)、蛋白质、皂苷和油性部分均无毒性,因此显示出高安全性,被归类为 5 级。油性部分 Annomaal 对 具有明显的抗疟活性,IC (1.25 ± 0.183 μg/mL)值较低。CSE 和 Annomaal 体内显著抑制 寄生虫的生长,化学抑制率分别为 58.47%和 61.11%,而标准药物青蒿素的化学抑制率为 66.75%。此外,研究表明,每天口服 250mg/kg 剂量的 Annomaal 连续 3 天足以完全治愈感染的小鼠。由于治疗方案较短,Annomaal 有望成为符合患者要求的药物,消除了对几种合成抗疟药物所需的长时间内频繁给药的需求。需要进一步研究以确定油性部分中负责抗疟活性的活性化合物。