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Secochiliolide ester derivatives: Preparation and evaluation of their antitrypanosomal and antimalarial efficacy
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-10-31 , DOI: 10.1111/cbdd.13392 Romina J. Ronchi 1, 2 , Claire Beaufay 3 , Joanne Bero 3 , Juan B. Robirosa 1, 2 , Marcia Mazzuca 4 , Jorge A. Palermo 1, 2 , Joëlle Quetin-Leclercq 3 , Marianela Sánchez 1, 2
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-10-31 , DOI: 10.1111/cbdd.13392 Romina J. Ronchi 1, 2 , Claire Beaufay 3 , Joanne Bero 3 , Juan B. Robirosa 1, 2 , Marcia Mazzuca 4 , Jorge A. Palermo 1, 2 , Joëlle Quetin-Leclercq 3 , Marianela Sánchez 1, 2
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In the present study, a series of new esters of secochiliolide acid (SA), a diterpene isolated from Nardophyllum bryoides, were synthesized in good yield. All compounds were evaluated for their in vitro antiparasitic properties (on Plasmodium falciparum and Trypanosoma brucei brucei) and cytotoxicity (on WI38, normal mammalian cells). They displayed moderate antitrypanosomal activity with IC50 values between 2.55 and 18.14 μm, with selectivity indices >10, and low antiplasmodial effects with IC50 > 29 μm. The only exception was the n‐hexyl ester of SA, which showed a strong and selective antiplasmodial activity (IC50 = 1.99 μm and selectivity index = 117.0). The in vivo antimalarial efficacy of this compound was then assessed according to the 4‐day suppressive test of Peters in mice. An intraperitoneal treatment at 50 mg kg−1 day−1 induced a slight parasitaemia reduction by 56% which was statistically significant on day 4 post‐infection and an increase in the survival time.
中文翻译：
花生四烯酸内酯衍生物的制备及其抗胰锥虫和抗疟药功效的评估
在本研究中，以高收率合成了一系列新的癸二内酯酸酯（SA），一种从溴二苯甲烷小球藻中分离出的二萜。评价所有化合物的体外抗寄生虫特性（对恶性疟原虫和布鲁氏锥虫）和细胞毒性（对WI38，正常哺乳动物细胞）。它们显示中等抗锥体虫活性，IC 50 2.55 18.14和μ之间的值米，具有选择性指数> 10，并与IC低抗疟原虫影响50 > 29μ米。唯一的例外是SA的正己酯，其显示出强大的选择性抗血浆活性（IC 50 = 1.99μ米和选择性指数= 117.0）。然后根据Peters在小鼠中进行的4天抑制试验评估了该化合物的体内抗疟疾功效。以50mg公斤腹膜内治疗-1 天-1诱导这是第4天感染后统计学显著56％的轻微减少寄生虫血症和增加的存活时间。
更新日期：2018-10-31
中文翻译：
花生四烯酸内酯衍生物的制备及其抗胰锥虫和抗疟药功效的评估
在本研究中，以高收率合成了一系列新的癸二内酯酸酯（SA），一种从溴二苯甲烷小球藻中分离出的二萜。评价所有化合物的体外抗寄生虫特性（对恶性疟原虫和布鲁氏锥虫）和细胞毒性（对WI38，正常哺乳动物细胞）。它们显示中等抗锥体虫活性，IC 50 2.55 18.14和μ之间的值米，具有选择性指数> 10，并与IC低抗疟原虫影响50 > 29μ米。唯一的例外是SA的正己酯，其显示出强大的选择性抗血浆活性（IC 50 = 1.99μ米和选择性指数= 117.0）。然后根据Peters在小鼠中进行的4天抑制试验评估了该化合物的体内抗疟疾功效。以50mg公斤腹膜内治疗-1 天-1诱导这是第4天感染后统计学显著56％的轻微减少寄生虫血症和增加的存活时间。
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