Extracts from Pygeum africanum and Other Ethnobotanical Species with Antiandrogenic Activity

Abstract

Extracts from Pygeum africanum, Serenoa repens and Cucurbita pepo are used in the treatment of benign prostatic hyperplasia (BPH) and prostate cancer (PCa). The activity of the androgen receptor (AR) is known to control growth of the prostate. Here, we examined extracts of these plants for their antiandrogenic activity using an AR responsive reporter gene assay for drug discovery. A selective dichloromethane extract from the stem barks of Pygeum africanum revealed the highest antiandrogenic effect. Bioactivity-directed fractionation of this extract led to the isolation of N-butylbenzenesulfonamide (NBBS) indicating that extracts of the stem bark of P. africanum harbour androgen antagonistic activity. This compound may provide a novel approach for the prevention and treatment of BPH and human PCa.

Abbreviations

AR:human androgen receptor

BPH:benign prostate hyperplasia

C. pep:Cucurbita pepo

IPSS:international prostate symptom score

NBBS:N-butylbenzenesulfonamide

P. africanum:Pygeum africanum

PCa:prostate cancer

QoL:quality of life

R1881:methyltrienolone

RLU:relative light units

S. repens:Serenoa repens

Key words

Antiandrogenic activity - Pygeum africanum - Rosaceae - Serenoa repens - Arecaceae - Cucurbita pepo - Cucurbitaceae - N-butylbenzenesulfonamide - prostate hyperplasia

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