ABSTRACT
Byrsocarpus coccineus is a shrub belonging to the family Connaraceae. It is used in the management and treatment of benign prostatic hyperplasia, diabetes, cancer, inflammation, and hypertension. Benign prostatic hyperplasia (BPH) is described as a proliferation of the cellular elements of the prostate, leading to an enlarged prostate condition. This study evaluated the phytochemical profile, biosafety, anti-benign prostatic hyperplasia and possible mechanisms of action of B. coccineus. The preliminary phytochemical profiling was evaluated using GC-MS. Acute, sub-chronic and reproductive toxicological study were experimented to determine the lethal dose (LD50), regular body weight, hematological, serum biochemistry and hormonal parameters. The visceral organs weight was determined with the histopathological study on male Wistar rats using standard procedures. The effect of B. coccineus on inflammatory and BPH markers such as prostanglandinE2, Cytochrome P450 2D6, IL-1, TNF-, testosterone, TGF1, Estradiol, Dihydrogen-testosterone and prostate specific antigen in serum were determined using ELISA kit. Mechanisms of action of the extract was investigated using molecular docking of the compounds to the binding sites of different receptors implicated in BPH. The results showed the presence of some vital compound such as quercetin and its derivatives. Acute toxicity of B. coccineus aqueous extracts showed no mortality rate at 5000 mg/kg after fourteen days of observations with less or no adverse effect. The aqueous leaf extract maintains the body weight gained. The hematological results showed no significant difference in the treatment groups compared with the control. The kidney function and liver function test, and lipid profile results of B. coccineus leaf extract had no significant difference when compared with the control group (p < 0.05). B coccineus aqueous leaf extract on the testosterone, follicle stimulating hormone, luteinizing hormone and progesterone showed no significant difference when compared 8 with the control. The results for the aqueous leaf extract on the histopathological tissues showed a mild effect on the various organs when compared with the control group. The results of the BPH study, revealed that testosterone-treated animals, had an increase TNF-α and IL-1 expression with marked inflamed cells that degenerated to prostate-specific antigen. The extract and the positive control (finasteride) led to a significant reduction in the inflammatory cells with reduced PSA levels when compared with untreated control. B. coccineus leaf extract and finasteride also displayed immunoprotected effect on the prostate glands. Quercetin and its glycoside derivatives were observed to be the bioactive principle using in silico mode. The mechanisms of action of the active principle was suggested to be via antagonistic inhibition of 5apha reductase 2 receptor and down regulation of the gene expressing the protein. In conclusion, the experimental findings justify the ethnomedicinal claim of usage of the plant in the management of BPH among locals.
