title: 20(S)-Ginsenoside Rh2 as aldose reductase inhibitor from Panax ginseng.
abstract: The root of Panax ginseng C. A. Meyer (Araliaceae) is a well-known herbal medicine in East Asia. The major bioactive metabolites in this root are commonly identified as ginsenosides. A series of ginsenosides were determined for in vitro human recombinant aldose reductase. This Letter aims to clarify the structural requirement for aldose reductase inhibition. We discovered that only ginsenoside 20(S)-Rh2 showed potent against aldose reductase, with an IC50 of 147.3 μM. These results implied that the stereochemistry of the hydroxyl group at C-20 may play an important role in aldose reductase inhibition. An understanding of these requirements is considered necessary in order to develop a new type of aldose reductase inhibitor. Furthermore, P. ginseng might be an important herbal medicine in preventing diabetic complications.
authors.affiliation: Department of Agro-environmental Sciences, Faculty of Agriculture, Kyushu University, Fukuoka 812-8581, Japan; Department of Chemistry, Faculty of Mathematics and Natural Sciences, Institut Teknologi Sepuluh Nopember, Kampus ITS-Sukolilo, Surabaya 60111, Indonesia.
authors.forename: Sri
authors.initials: S
authors.lastname: Fatmawati
authors.affiliation: Department of Chemistry, Faculty of Mathematics and Natural Sciences, Institut Teknologi Sepuluh Nopember, Kampus ITS-Sukolilo, Surabaya 60111, Indonesia.
authors.forename: Taslim
authors.initials: T
authors.lastname: Ersam
authors.affiliation: College of Biotechnology, Dalian Polytechnic University, Dalian 116034, China.
authors.forename: Hongshan
authors.initials: H
authors.lastname: Yu
authors.affiliation: College of Biotechnology, Dalian Polytechnic University, Dalian 116034, China.
authors.forename: Chunzhi
authors.initials: C
authors.lastname: Zhang
authors.affiliation: College of Biotechnology, Dalian Polytechnic University, Dalian 116034, China.
authors.forename: Fengxie
authors.initials: F
authors.lastname: Jin
authors.affiliation: Department of Agro-environmental Sciences, Faculty of Agriculture, Kyushu University, Fukuoka 812-8581, Japan. Electronic address: shimizu@agr.kyushu-u.ac.jp.
authors.forename: Kuniyoshi
authors.initials: K
authors.lastname: Shimizu
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D036145:Ginsenosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D008968:Molecular Conformation; D005894:Panax / Q000737:chemistry*; D018517:Plant Roots / Q000737:chemistry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D036145:Ginsenosides; C055305:ginsenoside Rh2; D000449:Aldehyde Reductase
keywords: Aldose reductase inhibitor; Ginsenoside; Panax ginseng; Structure–activity relationships