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Acta Pharmacol Sin ; 31(5): 609-15, 2010 May.
Article in English | MEDLINE | ID: mdl-20418896

ABSTRACT

AIM: To investigate the cytotoxic effects of four cyclic bisbibenzyls, Riccardin C (Ric), Pakyonol (Pak), Marchantin M (Mar), and Plagiochin E (Pla) against chemoresistant prostate cancer PC3 cells. METHODS: Cell growth was assayed by MTT method, and apoptotic related protein Bcl-2 and Bax, poly(ADP-ribose) polymerase (PARP) were examined by Western blotting. Cell cycle and apoptosis of PC3 cells were evaluated with flow cytometry and morphologic examinations. RESULTS: The four compounds inhibited proliferation and elicited cell death in a dose- and time-dependent manner with IC(50) values of 3.22 micromol/L for Ric, 7.98 micromol/L for Pak, 5.45 micromol/L for Mar, and 5.99 micromol/L for Pla, respectively. Furthermore, exposed to these chemicals caused a decrease in the antiapoptotic protein Bcl-2 and an increase in proapoptotic Bax expression. PARP cleavage and caspase-3 activity were also observed. CONCLUSION: The results suggest that cyclic bisbibenzyls could be used for the development of novel therapeutic chemicals against prostate cancer.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Bibenzyls/pharmacology , Cell Proliferation/drug effects , Prostatic Neoplasms/drug therapy , Antineoplastic Agents, Phytogenic/isolation & purification , Bibenzyls/isolation & purification , Caspase 3/metabolism , Gene Expression Regulation, Neoplastic/drug effects , Humans , Male , Plant Extracts/isolation & purification , Plant Extracts/pharmacology
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