title: Inhibitory effect of Rhus verniciflua Stokes extract on human aromatase activity; butin is its major bioactive component.
abstract: Rhus verniciflua Stokes has been used as a traditional herbal medicine in Asia. In this study, the effect of R. verniciflua extract on human aromatase (cytochrome P450 19, CYP19) activity was investigated to elucidate the mechanism for the effect of R. verniciflua extract on androgen hormone levels. Androstenedione was used as a substrate and incubated with R. verniciflua extract in cDNA-expressed CYP19 supersomes in the presence of NADPH, and estrone formation was measured using liquid chromatography-tandem mass spectrometry. R. verniciflua extract was assessed at concentrations of 10-1000 μg/mL. The resulting data showed that R. verniciflua extract inhibited CYP19-mediated estrone formation in a concentration-dependent manner with an IC50 value of 136 μg/mL. Subsequently, polyphenolic compounds from R. verniciflua extract were tested to identify the ingredients responsible for the aromatase inhibitory effects by R. verniciflua extract. As a result, butin showed aromatase inhibitory effect in a concentration-dependent manner with an IC50 value of 9.6 μM, whereas the inhibition by other compounds was negligible. These results suggest that R. verniciflua extract could modulate androgen hormone levels via the inhibition of CYP19 activity and butin is a major ingredient responsible for this activity.
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 426-791, Republic of Korea.
authors.forename: Myeong Hyeon
authors.initials: MH
authors.lastname: Park
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 426-791, Republic of Korea.
authors.forename: In Sook
authors.initials: IS
authors.lastname: Kim
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 426-791, Republic of Korea.
authors.forename: Sun-A
authors.initials: SA
authors.lastname: Kim
authors.affiliation: Lifetree Biotech Co., Ltd, Suwon, Gyeonggi-do 441-350, Republic of Korea.
authors.forename: Chun-Soo
authors.initials: CS
authors.lastname: Na
authors.affiliation: Lifetree Biotech Co., Ltd, Suwon, Gyeonggi-do 441-350, Republic of Korea.
authors.forename: Cheol Yi
authors.initials: CY
authors.lastname: Hong
authors.affiliation: School of Life Sciences and Biotechnology, Korea University, Seoul 136-713, Republic of Korea. Electronic address: msdong@korea.ac.kr.
authors.forename: Mi-Sook
authors.initials: MS
authors.lastname: Dong
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Gyeonggi-do 426-791, Republic of Korea. Electronic address: yoohh@hanyang.ac.kr.
authors.forename: Hye Hyun
authors.initials: HH
authors.lastname: Yoo
mesh_terms: D001141:Aromatase / Q000378:metabolism*; D047072:Aromatase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001578:Benzopyrans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008519:Medicine, Traditional; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D018514:Plant Structures / Q000737:chemistry*; D029045:Rhus / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D047072:Aromatase Inhibitors; D001578:Benzopyrans; D010936:Plant Extracts; C051437:butin; D001141:Aromatase; C561410:CYP19A1 protein, human
keywords: Butin; CYP19; Human aromatase; Rhus verniciflua Stokes