Screening of Euphorbiaceae Plant Extracts for Anti-5α-reductase

Biol Pharm Bull. 2018;41(8):1307-1310. doi: 10.1248/bpb.b18-00283.

Abstract

In our research program to find novel agents for alopecia from natural plant resources, we screened Euphorbiaceae plant extracts using an anti-5α-reductase assay. Among the samples tested, the extract of Phyllanthus urinaria showed the most potent activity with 24.3 and 64.6% inhibition at 50 and 200 µg/mL against the enzyme, respectively. The extract also suppressed the androgen activity of dihydrotestosterone in LNCaP cell line. These results show that the extract of P. urinaria may be a multi-potent agent for androgen-derived alopecia. We tested for activity on a hair regrowth model using mice. The extract of P. urinaria showed hair regrowth activity at 5 mg/mouse/d administration. Furthermore, the active principle for anti-5α-reductase activity was determined as stigmasterol glucoside from activity-guided fractionation and the IC50 was 27.2 µM. These results suggest that extract of P. urinaria may be a promising candidate anti-alopecia agent.

Keywords: 5α-reductase; Euphorbiaceae; Phyllanthus urinaria; androgen receptor; stigmasterol glucoside.

MeSH terms

  • 5-alpha Reductase Inhibitors / pharmacology*
  • Alopecia / drug therapy
  • Androgens / metabolism
  • Animals
  • Cell Line
  • Cholestenone 5 alpha-Reductase
  • Dihydrotestosterone / metabolism
  • Euphorbiaceae*
  • Hair / drug effects*
  • Hair / growth & development
  • Male
  • Mice, Inbred C57BL
  • Plant Extracts / pharmacology*

Substances

  • 5-alpha Reductase Inhibitors
  • Androgens
  • Plant Extracts
  • Dihydrotestosterone
  • Cholestenone 5 alpha-Reductase