Growth inhibitory activity of lemnabourside on human prostate cancer cells
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AbstractInduction of apoptosis and androgen ablation are two major approaches for treating human prostate carcinoma. In a study of the bioactive components of the soft coral Nephthea chabroli, we found that lemnabourside is a 5alpha-reductase inhibitor, as shown by its ability to inhibit the conversion of testosterone into the more potent dihydrotestosterone in rat prostate homogenate. The compound also inhibited the incorporation of tritiated thymidine into human prostate androgen-dependent carcinoma LNCaP cells, and thus blocking the cell proliferation IC50 = 37.5 muM). The expression of prostate marker genes, including 5a-reductase, prostate-specific antigen, prostatic acid phosphatase and androgen receptor, and the anti-apoptotic bcl-2 gene were markedly reduced, but the transcription of apoptosis-related caspase 3 gene showed a dose-dependent increase in lemnabourside-treated LNCaP cells. Immunofluorescent microscopy and flow cytometric analysis further demonstrated apoptotic changes in these cells. Taken all results together, a relatively weak 5(x-reductase inhibitory activity on LNCaP cells (EC50 > 250 muM), and a similar growth inhibitory activity on both androgen dependent- and independent-prostate cells (IC50 approximate to 37.5 muM) indicated that caspase-3 apoptosis pathway is one of the possible antiproliferative activities mediated by lemnabourside. (C) 2002 Elsevier Science Inc. All rights reserved.
All Author(s) ListLiu WK, Wong NLY, Huang HM, Ho JKC, Zhang WH, Che CT
Journal nameLife Sciences
Year2002
Month1
Day4
Volume Number70
Issue Number7
PublisherPERGAMON-ELSEVIER SCIENCE LTD
Pages843 - 853
ISSN0024-3205
eISSN1879-0631
LanguagesEnglish-United Kingdom
Keywords5 alpha-reductase; apoptosis; human prostate carcinoma cell lines; Lemnabourside
Web of Science Subject CategoriesMedicine, Research & Experimental; MEDICINE, RESEARCH & EXPERIMENTAL; Pharmacology & Pharmacy; PHARMACOLOGY & PHARMACY; Research & Experimental Medicine

Last updated on 2020-20-10 at 02:33