Growth inhibition and induction of early apoptosis by arenicolsterol A, a novel cytotoxic enolic sulphated sterol from the marine annelid, Arenicola cristata.
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.
Wang
Liang
L
Department of Chemistry, Fudan University, Shanghai, China.
Chen
Bin
B
Shen
Xian-Rong
XR
Zhou
Yue-Yang
YY
Jiang
Ding-Wen
DW
Li
Jia
J
Kong
Ji-Lie
JL
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