Bioactivities of six sterols isolated from marine invertebrates

CORC > 南海海洋研究所 > 中国科学院南海海洋研究所 > 广东省海洋药物重点实验室

	Bioactivities of six sterols isolated from marine invertebrates
	Zhou, XF ; Sun, JF ; Ma, WL ; Fang, W ; Chen, ZF ; Yang, B ; Liu, YH
刊名	PHARMACEUTICAL BIOLOGY
	2014
卷号	52 期号:2 页码:187-190
关键词	Dichotella gemmacea Glyptocidaris crenularis high-throughput screening marine sterols Mycale sp. Xestospongia testudinaria
ISSN号	1388-0209
通讯作者	yonghongliu@scsio.ac.cn
中文摘要	Context: Epidioxy sterols and sterols with special side chains, such as hydroperoxyl sterols, usually obtained from marine natural products, are attractive for bioactivities. Objective: To isolate and screen bioactive and special sterols from China Sea invertebrates. Materials and methods: Two hydroperoxyl sterols (1 and 2) from the sponge Xestospongia testudinaria Lamarck (Petrosiidae), three epidioxy sterols (3-5) from the sea urchin Glyptocidaris crenularis A. Agassiz (Glyptocidaridae), sponge Mycale sp. (Mycalidae) and gorgonian Dichotella gemmacea Milne Edwards and Haime (Ellisellidae) and an unusual sterol with 25-acetoxy-19-oate (6) also from D. gemmacea were obtained and identified. Using high-throughput screening, their bioactivities were tested toward Forkhead box O 3a (Foxo3a), 3-hydroxy-3-methylglutaryl CoA reductase gene fluorescent protein (HMGCR-GFP), nuclear factor kappa B (NF-kappa B) luciferase, peroxisome proliferator-activated receptor-gamma co-activator 1 alpha (PGC-1 alpha), protein-tyrosine phosphatase 1B (PTP1B), mitochondrial membrane permeabilization (MMP) and adenosine monophosphate-activated protein kinase. Results: Their structures were determined by comparing their nuclear magnetic resonance data with those reported in the literature. Three epidioxy sterols (3-5) showed inhibitory activities toward Foxo3a, HMGCR-GFP and NF-kappa B-luciferase with the IC50 values 4.9-6.8 mu g/mL. The hydroperoxyl sterol 29-hydroperoxystigmasta-5,24(28)-dien-3-ol (2) had diverse inhibitory activities against Foxo3a, HMGCR-GFP, NF-kappa B-luciferase, PGC-1 alpha, PTP1B and MMP, with IC50 values of 3.8-19.1 mu g/mL. Discussion and conclusion: The bioactivities of 3-5 showed that 5 alpha,8 alpha-epidioxy is the active group. Otherwise, the most plausible biosynthesis pathway for 1 and 2 in sponge involves the abstraction of an allylic proton by an activated oxygen, such as O-2, along with migration of carbon-carbon double bond. Therefore, the bioactive and unstable steroid should be biosynthesized in sponge under a special ecological environment to act as a defensive strategy against invaders.
学科主题	Plant Sciences ; Medical Laboratory Technology ; Pharmacology & Pharmacy
收录类别	SCI
资助信息	National Key Basic Research Program of China (973)'s Project [2010CB833800, 2011CB915503]; National High Technology Research and Development Program of China (863 Program) [2012AA0 92104]; National Natural Science Foundation of China [31270402, 20902094, 30973679, 21172230]; Knowledge Innovation Program of Chinese Academy of Sciences [SQ201019]
原文出处	INFORMA HEALTHCARE
WOS记录号	WOS:000329301800009
公开日期	2014-12-11
内容类型	期刊论文
源URL	[http://ir.scsio.ac.cn/handle/344004/10666]
专题	南海海洋研究所_广东省海洋药物重点实验室
推荐引用方式 GB/T 7714	Zhou, XF,Sun, JF,Ma, WL,et al. Bioactivities of six sterols isolated from marine invertebrates[J]. PHARMACEUTICAL BIOLOGY,2014,52(2):187-190.
APA	Zhou, XF.,Sun, JF.,Ma, WL.,Fang, W.,Chen, ZF.,...&Liu, YH.(2014).Bioactivities of six sterols isolated from marine invertebrates.PHARMACEUTICAL BIOLOGY,52(2),187-190.
MLA	Zhou, XF,et al."Bioactivities of six sterols isolated from marine invertebrates".PHARMACEUTICAL BIOLOGY 52.2(2014):187-190.