Steroids with inhibitory activity against the prostate cancer cells and chemical diversity of marine alga Tydemania expeditionis

doi:10.1016/j.fitote.2012.04.019

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	Steroids with inhibitory activity against the prostate cancer cells and chemical diversity of marine alga Tydemania expeditionis
	Zhang, Jian-Long 2; Tian, Hai-Yan 2; Li, Juan 2; Jin, Lu 1,2; Luo, Cheng1 ; Ye, Wen-Cai 2; Jiang, Ren-Wang 2
刊名	FITOTERAPIA
	2012-07
卷号	83 期号:5 页码:973-978
关键词	Tydemania expeditionis Steroid Prostate cancer Androgen receptor Docking
ISSN号	0367-326X
DOI	10.1016/j.fitote.2012.04.019
文献子类	Article
英文摘要	A new diketosteroid, (E)-stigmasta-24(28)-en-3,6-dione (1), along with three known steroids (2-4) was isolated from marine alga Tydemania expeditionis collected in China Sea. Their structures were elucidated by extensive spectroscopic methods. Comparison of the chemical constituents revealed significant diversity among different locations. The biological activities of 1, 3 and 4 were evaluated on the prostate cancer cell lines and androgen receptor. Compound 1 exhibited moderate inhibitory activities against the prostate cancer cells DU145, PC3 and LNCaP with IC50 values of 31.27 +/- 1.50. 40.59 +/- 3.10 and 19.80 +/- 3.84 mu M, respectively. Compound 3 showed more potent activities with IC50 values of 12.38 +/- 2.47, 2.14 +/- 0.33 and 1.38 +/- 0.07 mu M, respectively. However, compound 4 showed only weak inhibitory activities on LNCaP cells and was inactive on DU 145 and PC3 cells. A competitive binding assay showed that compound 1 exhibited significant affinity to the androgen receptor with an IC50 value of 7.19 +/- 0.45 mu M, while 3 and 4 were inactive. The fact that the inhibitory properties of 1 and 3 against the prostate cancer cells were inconsistent with their affinities to the androgen receptor suggested that there might be other mechanism of action involved in the cytotoxic activity. (C) 2012 Elsevier B.V. All rights reserved.
资助项目	National Natural Science Foundation of China[30801433] ; National Natural Science Foundation of China[91029704] ; New Century Excellent Talents Scheme of the Ministry of Education[NCET-08-0612] ; Fundamental Research Funds for the Central Universities[21609202] ; Hi-Tech Research and Development Program of China[SS2012AA021103] ; Chinese Academy of Sciences[XDA01040305]
WOS关键词	ANDROGEN-RECEPTOR ; FATTY-ACIDS ; TRITERPENOIDS ; CHLOROPHYTA ; SULFATES
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000305657900025
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278029]
专题	药物发现与设计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
通讯作者	Jiang, Ren-Wang
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Jinan Univ, Coll Pharm, Guangdong Prov Key Lab Pharmacodynam Constituents, Guangzhou 510632, Guangdong, Peoples R China;
推荐引用方式 GB/T 7714	Zhang, Jian-Long,Tian, Hai-Yan,Li, Juan,et al. Steroids with inhibitory activity against the prostate cancer cells and chemical diversity of marine alga Tydemania expeditionis[J]. FITOTERAPIA,2012,83(5):973-978.
APA	Zhang, Jian-Long.,Tian, Hai-Yan.,Li, Juan.,Jin, Lu.,Luo, Cheng.,...&Jiang, Ren-Wang.(2012).Steroids with inhibitory activity against the prostate cancer cells and chemical diversity of marine alga Tydemania expeditionis.FITOTERAPIA,83(5),973-978.
MLA	Zhang, Jian-Long,et al."Steroids with inhibitory activity against the prostate cancer cells and chemical diversity of marine alga Tydemania expeditionis".FITOTERAPIA 83.5(2012):973-978.