Isolation and characterization of antiplasmodial constituents from the marine sponge Coscinoderma sp.

Huijeong Jeong, A. Latif, C. Kong, Y. Seo, Yeon-Ju Lee, S. Dalal, M. Cassera, D. Kingston
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引用次数: 3

Abstract

Abstract Six known compounds, namely two halisulfates 1 and 2 and four epidioxy sterols 3–6, were isolated from the marine sponge Coscinoderma sp. The structures of these compounds were confirmed by nuclear magnetic resonance (1H and 13C NMR) spectroscopy, and their antiplasmodial activities were determined against the chloroquine-resistant Dd2 strain of Plasmodium falciparum. The epidioxy steroids 3–6 all showed moderate to weak antiplasmodial activity, with IC50 values of 2.7 μM for (24S)-5α,8α-epidioxy-24-methylcholesta-6-en-3β-ol (3), 11.6 μM for 5α,8α-epidioxycholesta-6,24(28)-dien-3β-o1 (4), 2.33 μM for 5α,8α-epidioxy-24-methylcholesta-6,9(11)-24(28)-trien-3β-ol (5), and between 12 and 24 μM for 5α,8α-epidioxycholesta-6-en-3β-ol (6). In contrast, halisulfate 2 (1) was inactive, and halisulfate 1 (2) had an of IC50 value of about 24 μM.
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海绵体Coscinoderma sp.抗疟原虫成分的分离与鉴定。
摘要从海绵Coscinoderma sp.中分离得到6个已知化合物,即2个盐酸盐1和2个和4个附睾甾醇3 ~ 6个,通过核磁共振(1H和13C NMR)鉴定了这些化合物的结构,并测定了它们对耐氯喹的恶性疟原虫Dd2菌株的抗疟原虫活性。epidioxy类固醇3 - 6所有显示中度到弱antiplasmodial活动,IC50值为2.7μM(24) 5α,α8 -epidioxy-24-methylcholesta-6-en-3βol(3), 11.6μM 5α,α8 -epidioxycholesta-6, 24 (28) -dien-3βo1群(4),2.33μM 5α,α8 -epidioxy-24-methylcholesta-6, 9 (11) -24 (28) -trien-3βol(5),和12到24μM 5α,α8 -epidioxycholesta-6-en-3βol(6)。相比之下,halisulfate 2(1)是不活跃的,halisulfate 1(2)有一个24的IC50值μM。
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