Bioactive constituents from the green alga Caulerpa racemosa

doi:10.1016/j.bmc.2014.11.031

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	Bioactive constituents from the green alga Caulerpa racemosa
	Yang, Peng 1; Liu, Ding-Quan 1; Liang, Tong-Jun 2; Li, Jia3 ; Zhang, Hai-Yan3 ; Liu, Ai-Hong 4; Guo, Yue-Wei3 ; Mao, Shui-Chun 1
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2015
卷号	23 期号:1 页码:38-45
关键词	Caulerpa racemosa PTP1B inhibitory activity Neuroprotective activity Cytotoxic activity
ISSN号	0968-0896
DOI	10.1016/j.bmc.2014.11.031
文献子类	Article
英文摘要	Three diterpenoids, including a pair of epimers, racemobutenolids A and B (1 and 2), and 4',5'-dehydrodiodictyonema A (3), an alpha-tocopheroid, alpha-tocoxylenoxy (8), and an 28-oxostigmastane steroid, (23E)-3 beta-hydroxy-stigmasta-5,23-dien-28-one (11), together with 12 known compounds, were isolated from the green alga Caulerpa racemosa. The structures of the new compounds were elucidated by detailed analysis of spectroscopic data, and by comparison with data for related known compounds. The epimers (1 and 2) are two unusual diterpenoid lactones bearing a beta-methyl-gamma-substituted butenolide moiety, and 3 and 8 represent the first naturally occurring natural products with a hematinic acid ester group and 3,5-dimethylphenoxy functionality, respectively. The enzyme inhibitory activities of the isolated compounds were evaluated in vitro against PTP1B and related PTPs (TCPTP, CDC25B, LAR, SHP-1, and SHP-2). Compounds 3, 5, 6, and 9-14 exhibited different levels of PTP1B inhibitory activities with IC50 values ranging from 2.30 to 50.02 mu M. Of these compounds, 3, 9, and 11 showed the most potent inhibitory activities towards PTP1B with IC50 values of 2.30, 3.85, and 3.80 mu M, respectively. More importantly, the potent PTP1B inhibitors 3, 9, and 11 also displayed high selectivity over the highly homologous TCPTP and other PTPs. Also, the neuroprotective effects of the isolates against A beta(25-35)-induced cell damage in SH-SY5Y cells were investigated. Compounds 10, 11, and 14 exhibited significant neuroprotective effects against A beta(25-35)-induced SH-SY5Y cell damage with 11.31-15.98% increases in cell viability at 10 mu M. In addition, the cytotoxic activities of the isolated compounds were tested against the human cancer cell lines A-549 and HL-60. (C) 2014 Elsevier Ltd. All rights reserved.
资助项目	National Natural Science Foundation of China[81001397] ; National Natural Science Foundation of China[21162016] ; National Natural Science Foundation of China[21362024] ; Young Scientists Training Program of Jiangxi Province[20133BCB23004] ; Natural Science Foundation of Jiangxi Province[20114BAB205034] ; Foundation of Education Department of Jiangxi Province[GJJ12028]
WOS关键词	INHIBITOR ; TAXIFOLIA ; CELLS ; IDENTIFICATION ; CHLOROPHYTA ; METABOLITES ; REGULATOR ; STEROLS ; SPONGE ; CHAIN
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000346586400004
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276783]
专题	国家新药筛选中心中科院受体结构与功能重点实验室新药研究国家重点实验室天然药物化学研究室药理学第二研究室药物安全性评价中心
通讯作者	Mao, Shui-Chun
作者单位	1.Nanchang Univ, Sch Pharm, Nanchang 330006, Peoples R China; 2.Jiangxi Prov & Chinese Acad Sci, Lushan Bot Garden, Lushan 332900, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 4.Nanchang Univ, Ctr Anal & Testing, Nanchang 330047, Peoples R China
推荐引用方式 GB/T 7714	Yang, Peng,Liu, Ding-Quan,Liang, Tong-Jun,et al. Bioactive constituents from the green alga Caulerpa racemosa[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(1):38-45.
APA	Yang, Peng.,Liu, Ding-Quan.,Liang, Tong-Jun.,Li, Jia.,Zhang, Hai-Yan.,...&Mao, Shui-Chun.(2015).Bioactive constituents from the green alga Caulerpa racemosa.BIOORGANIC & MEDICINAL CHEMISTRY,23(1),38-45.
MLA	Yang, Peng,et al."Bioactive constituents from the green alga Caulerpa racemosa".BIOORGANIC & MEDICINAL CHEMISTRY 23.1(2015):38-45.