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学科主题: Plant Sciences ; Medical Laboratory Technology ; Pharmacology & Pharmacy
题名: Bioactivities of six sterols isolated from marine invertebrates
作者: Zhou, XF ; Sun, JF ; Ma, WL ; Fang, W ; Chen, ZF ; Yang, B ; Liu, YH
通讯作者: yonghongliu@scsio.ac.cn
关键词: Dichotella gemmacea ; Glyptocidaris crenularis ; high-throughput screening ; marine sterols ; Mycale sp. ; Xestospongia testudinaria
刊名: PHARMACEUTICAL BIOLOGY
发表日期: 2014
卷: 52, 期:2, 页:187-190
收录类别: sci
部门归属: [Zhou, Xuefeng ; Ma, Wanlei ; Chen, Zhefan ; Yang, Bin ; Liu, Yonghong] Chinese Acad Sci, South China Sea Inst Oceanol, Guangdong Key Lab Marine Mat Med, CAS Key Lab Trop Marine Bioresources & Ecol, Guangzhou 510301, Guangdong, Peoples R China ; [Sun, Jianfan] Jiangsu Univ, Sch Environm, Zhenjiang, Peoples R China ; [Fang, Wei] Hubei Acad Agr Sci, Ctr Biopesticide Engn Res, Wuhan, Peoples R China
项目归属: 广东省海洋药物重点实验室
资助者: 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]
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.
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WOS记录号: WOS:000329301800009
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内容类型: 期刊论文
URI标识: http://ir.scsio.ac.cn/handle/344004/10666
Appears in Collections:广东省海洋药物重点实验室_期刊论文

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Recommended Citation:
Zhou, XF; Sun, JF; Ma, WL; Fang, W; Chen, ZF; Yang, B; Liu, YH.Bioactivities of six sterols isolated from marine invertebrates,PHARMACEUTICAL BIOLOGY,2014,52(2):187-190
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