2. Academic Validation
  3. Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A

Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A

  • J Med Chem. 2012 Jan 26;55(2):971-5. doi: 10.1021/jm2015292.
Weiguo Liu 1,  Jinming Zhou,  Guoyan Geng,  Qingwen Shi,  Francoise Sauriol,  Jian Hui Wu
Affiliations

Affiliation

  • 1 Segal Cancer Center and Lady Davis Institute for Medical Research, Sir Mortimer B. Davis-Jewish General Hospital, McGill University, 3755 Cote-Ste-Catherine, Road, Montreal, Quebec H3T 1E2, Canada.
PMID: 22175694 DOI: 10.1021/jm2015292
Abstract

Expression of metastatic suppressor maspin is lost in advanced prostate Cancer. Clinically relevant mutations in Androgen Receptor (AR) convert antiandrogens into AR agonists, promoting prostate tumor growth. We discovered tanshinone IIA (TS-IIA) is a potent antagonist of mutated ARs and induces maspin expression through AR. TS-IIA suppressed AR expression and induced Apoptosis in LNCaP cells. Syntheses of TS-IIA derivatives (1-9) revealed that the 4,4-dimethyl group at ring A is important for TS-IIA's antiandrogenic and maspin induction activities.

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