Central Institute of Medicinal and Aromatic Plants, CSIR, P.O.CIMAP, 226015 Lucknow, India.
Parasitol Res. 2011 Oct;109(4):1003-8. doi: 10.1007/s00436-011-2344-1. Epub 2011 May 4.
In an effort to evaluate novel derivatives from artemisinin, possessing potential antimalarial activity, a new derivative artecyclopentyl mether (CPM-1) was derivatized and evaluated for its dose-dependent efficacy in Plasmodium yoelii nigeriensis infected mice. The survivability of mice at 7.5 mg/kg was >28 days with negligible parasitaemia and recovered anemia (66.16-72.62%). Artecyclopentyl mether was also found to modulate the pro- and anti-inflammatory cytokines (IFN-γ, 39.64-56.92%; TNF, 49.10-74.31%; IL-4, 11.53-43.22%; IL-10, 37.60-53.52%) favourably besides optimizing the oxidative stress to the infected subjects as evident by the nitric oxide (88.76-95.43%), lipid peroxidation (59.30-76.05%) and glycaemic data (62.70-76.66%). The results indicate the potentiality of the new derivative as an antimalarial against asexual stages of the parasite.
为了评估具有抗疟活性的青蒿素新衍生物，合成了一种新的衍生物 artecyclopentyl mether（CPM-1），并对其在感染 Plasmodium yoelii nigeriensis 的小鼠中的剂量依赖性疗效进行了评估。在 7.5mg/kg 剂量下，小鼠的存活率>28 天，寄生虫血症可忽略不计，贫血得到恢复（66.16-72.62%）。artecyclopentyl mether 还被发现可以调节促炎和抗炎细胞因子（IFN-γ，39.64-56.92%；TNF，49.10-74.31%；IL-4，11.53-43.22%；IL-10，37.60-53.52%），同时使感染宿主的氧化应激得到优化，如一氧化氮（88.76-95.43%）、脂质过氧化（59.30-76.05%）和血糖数据（62.70-76.66%）所示。这些结果表明，这种新的衍生物具有作为抗疟药物对抗寄生虫无性阶段的潜力。
