title: Growth inhibition and induction of early apoptosis by arenicolsterol A, a novel cytotoxic enolic sulphated sterol from the marine annelid, Arenicola cristata.
abstract: Arenicolsterol A (ASA), a novel cytotoxic enolic sulphated sterol, was isolated from the marine annelid, Arenicola cristata (AC). Growth inhibition of this compound on cancer cell lines was determined by MTT assay and suppression of tumour stem cells colony formation. The results showed that ASA was selectively cytotoxic on HeLa cell line (IC(50) = 6.00 +/- 1.16 micromol L(- 1) on HeLa cell line, IC(50) = 10.85 +/- 0.97 micromol L(- 1) on 929 cell line and 14.72 +/- 1.55 micromol L(- 1) on NCI-h6 cell line). In addition, the apoptosis induced by ASA was verified from monitoring the stainability with Annexin V and propidium iodine by a fluorescence-activated cell sorter. The experimental data confirmed that ASA could induce apoptosis in HeLa cells by arresting early stage in apoptosis. Meanwhile, the apoptosis was found to be correlative with the inhibition of the protein tyrosine phosphatases (cdc25A, cdc25B, JSP1, etc). Therefore, ASA might be a novel promising precursor of anticancer medicines.
authors.affiliation: Department of Chemistry, Fudan University, Shanghai, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Wang
authors.forename: Bin
authors.initials: B
authors.lastname: Chen
authors.forename: Xian-Rong
authors.initials: XR
authors.lastname: Shen
authors.forename: Yue-Yang
authors.initials: YY
authors.lastname: Zhou
authors.forename: Ding-Wen
authors.initials: DW
authors.lastname: Jiang
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.forename: Ji-Lie
authors.initials: JL
authors.lastname: Kong
mesh_terms: D000818:Animals; D000845:Annelida / Q000737:chemistry*; D017209:Apoptosis / Q000187:drug effects*; D002455:Cell Division / Q000187:drug effects*; D002460:Cell Line; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008386:Marine Biology; D051379:Mice; D015394:Molecular Structure