Abstract:
Phytotherapeutic studies on some extracts have revealed promising anti-prostatic
growth or anticancer activities. In this study, the pharmacological and toxicological
activities of the aqueous stem (CMASE) and sequential stem fractions (SECM) of
Croton membranaceus were evaluated in; testosterone-induced benign prostatic
hyperplasia (BPH) Sprague-Dawley (S-D) male rats and prostate cancer lines (PC3
and LNCaP). Phytochemical screening of CMASE revealed presence of phenols,
alkaloids, saponins, terpenoids and tannins. Gas chromatography-mass spectrometry
analysis of CMASE showed the presence of n-hexadeconoic acid and 6-octadecanoic
acid, known for their anti-androgenic, antioxidant, and 5-alpha reductase inhibitory
properties. All extracts (SECM and CMASE) exhibited mild antioxidant potentials,
and antiproliferative activities against PC3 and LNCaP cells. Sequential aqueous
fraction and CMASE exhibited selective indices for PC3 (SI=75.41, 85.11) and
LNCaP (SI=2.2, 2.07) cells, respectively. CMASE induced key apoptotic hallmarks
in PC3 cells. Acute (1000, 2500, 5000 mg/kg) and sub-chronic (30, 150 and 300
mg/kg for 90 days) toxicity studies of CMASE in male S-D rats revealed, it was
relatively safe, possessed nephroprotective, mild hepatotoxic activity, and had LD50
value greater than 5 g/kg. CMASE caused significant (p<0.001) reduction in prostatic
prostate specific antigens levels, significant (p<0.01 and p<0.05) reductions in 5-
alpha reductase activity, marked reduction in prostatic androgens levels, and size of
prostates (between 48.1-70.4%) in BPH-induced rats. Also, CMASE caused marked
elevation of prostatic and liver antioxidant enzymes. In conclusion, CMASE was
relatively safe, had apoptotic, mild antioxidant potential, anti-prostate growth and
anti-cancer activity, and is a 5-alpha reductase inhibitor.
