Scutellaria baicalensis is a widely used Chinese herbal medicine historically used in antiinflammatory and anticancer
therapy. The goals of the study were to 1) determine its in vitro and in vivo anti-
prostate cancer activity, 2) investigate its molecular mechanism directed at cell proliferation control including
cyclooxygenase-2(COX-2)
prostaglandin E2 (
PGE2) and
cyclins/cdks pathways, and 3) compare it with those of
PC-SPES (PC stands for
prostate cancer and spes is Latin for hope), a former herbal mixture for
prostate cancer treatment of which S. baicalensis is a major constituent. Two human
prostate cancer cell lines (LNCaP,
androgen dependent, and PC-3,
androgen independent) were assessed for growth inhibition. S. baicalensis exerted dose- and time-dependent increased growth inhibition in both cell lines. However, the PC-3 cells IC50 (50% growth inhibition concentration) were slightly more sensitive than LNCaP cells (IC50=0.15 mg/ml), although the former is
androgen independent. S. baicalensis was more effective in inhibition of cell growth compared with
PC-SPES (IC50=0.38 mg/ml for PC-3 cells). Significant reduction of
PGE2 synthesis in both cells
after treatment with S. baicalensis resulted from direct inhibition of COX-2 activity rather than COX-2
protein suppression. S. baicalensis also inhibited
prostate-specific antigen production in LNCaP cells. Finally, S. baicalensis suppressed expression of
cyclin D1 in LNCaP cells, resulting in a G1 phase arrest, while inhibiting cdk1 expression and
kinase activity in PC-3 cells, ultimately leading to a G2/M cell cycle arrest. Animal studies showed a 50% reduction in
tumor volume after
a 7-wk treatment period. This study demonstrated that S. baicalensis may be a novel
anticancer agent for the treatment of
prostate cancer.