Procyanidin B-3, isolated from barley and identified as a hair-growth stimulant, has the potential to counteract inhibitory regulation by TGF-beta1.
With the aim of identifying natural products, which possess hair-growing activity, we examined more than 1000 plant extracts with respect to their growth-promoting effects on hair epithelial cells. We discovered intensive growth-promoting activity, about 140% relative to controls, in barley extract. Our strategy for identifying active compounds in barley extract involved subjecting it to column chromatography using HP-20 resin columns, an LH-20 resin column, and preparative high-performance liquid chromatography (HPLC) using an ODS column. The 60% (v/v) aqueous methanol eluted fraction from the HP-20 column and the 75% (v/v) aqueous methanol eluted fraction from the subsequent LH-20 column showed high hair-growing activity in vivo. We isolated two major substances from the LH-20 active fraction using preparative HPLC. By means of mass spectrometry, 1H-NMR, and 13C-NMR analyses, one substance was revealed to be procyanidin B-3 and the other substance was identified as (+)-catechin. Purified procyanidin B-3 showed high hair-growing activity in the form of in vitro hair epithelial cell growth-promoting activity and in vivo anagen-inducing activity; however (+)-catechin showed no hair-growing activity. For the purpose of examining the hair-growing mechanisms of procyanidin B-3, we examined its relationship to the TGF-beta signal pathway, which is known to be a regulator of catagen induction. Addition of TGF-beta1 to hair epithelial cell cultures dose-dependently decreased the cell growth, and addition of procyanidin B-3 to the culture neutralized the growth-inhibiting effect of TGF-beta1. From these results, it is concluded that procyanidin B-3 can directly promote hair epithelial cell growth in vitro, has the potential to counteract the growth-inhibiting effect caused by TGF-beta1 in vitro, and has potential to stimulate anagen induction in vivo.
Kamimura
Ayako
A
Tsukuba Research Laboratories, Kyowa Hakko Kogyo Co, Tsukuba, Ibaraki, Japan. ayako.kamimura@kyowa.co.jp
Takahashi
Tomoya
T
D000818:Animals; D044946:Biflavonoids; D002392:Catechin / Q000008:administration & dosage / Q000302:isolation & purification* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D000078404:Epidermal Cells; D006197:Hair / Q000166:cytology / Q000187:drug effects* / Q000254:growth & development*; D001467:Hordeum / Q000737:chemistry*; D051379:Mice; D008809:Mice, Inbred C3H; D010936:Plant Extracts / Q000494:pharmacology; D044945:Proanthocyanidins; D016212:Transforming Growth Factor beta / Q000008:administration & dosage / Q000037:antagonists & inhibitors*; D053773:Transforming Growth Factor beta1
D044946:Biflavonoids; D010936:Plant Extracts; D044945:Proanthocyanidins; C508961:Tgfb1 protein, mouse; D016212:Transforming Growth Factor beta; D053773:Transforming Growth Factor beta1; C479578:procyanidin B; C017674:procyanidin; D002392:Catechin