title: Antidiabetic Effect of Schisandrae Chinensis Fructus Involves Inhibition of the Sodium Glucose Cotransporter.
abstract: Preclinical Research Schisandrae Chinensis Fructus (SCF), the fruit of Schisandra chinensis (Turcz.) Baill. (family Schisandraceae) is traditionally used as a tonic and antidiabetic agent in Asia. In this study, SCF was investigated for its effects on sodium glucose cotransporters 1 and 2 (SGLT 1 and 2) expressed in a COS-7 cell line for its specificity in inhibiting SGLT2, which is a novel mechanism to screen for potential antidiabetic agents. Using a bioassay-guided fractionation, we then tried to isolate and identify the active fraction(s)/component(s). The ethanol extract of SCF at a concentration of 1 mg/mL significantly inhibited 89% of SGLT1 and 73% of SGLT2 activities in a [14C]-α-methyl-d-glucopyranoside ([14C]-AMG) uptake assay. Fractionation of the ethanol extract yielded nine fractions, of which F8, at a concentration of 1 mg/mL, was specific in inhibiting SGLT 2 (42% inhibition, P < 0.001), without inhibiting SGLT 1. Using LC/MS-MS, three compounds, deoxyschisandrin, schisandrin B (γ-schisandrin) and schisandrin were identified in F8 and their amounts quantified. However, subsequent evaluation in the [14C]-AMG uptake assay showed that these three compounds failed to inhibit SGLT 2 activity indicating that the SGLT active component(s) from SCF have yet to be identified. Drug Dev Res 76 : 1-8, 2015.
authors.affiliation: School of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong.
authors.forename: Yue
authors.initials: Y
authors.lastname: Qu
authors.affiliation: Institute of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong.|State Key Laboratory of Phytochemistry and Plant Resources in West China, The Chinese University of Hong Kong, Hong Kong.
authors.forename: Judy Yuet-Wa
authors.initials: JY
authors.lastname: Chan
authors.affiliation: Institute of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong.|State Key Laboratory of Phytochemistry and Plant Resources in West China, The Chinese University of Hong Kong, Hong Kong.
authors.forename: Chun-Wai
authors.initials: CW
authors.lastname: Wong
authors.affiliation: Institute of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong.|State Key Laboratory of Phytochemistry and Plant Resources in West China, The Chinese University of Hong Kong, Hong Kong.
authors.forename: Ling
authors.initials: L
authors.lastname: Cheng
authors.affiliation: School of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong.
authors.forename: Chuanshan
authors.initials: C
authors.lastname: Xu
authors.affiliation: School of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong.
authors.forename: Albert Wing-Nang
authors.initials: AW
authors.lastname: Leung
authors.affiliation: Institute of Chinese Medicine, The Chinese University of Hong Kong, Hong Kong.|State Key Laboratory of Phytochemistry and Plant Resources in West China, The Chinese University of Hong Kong, Hong Kong.
authors.forename: Clara Bik-San
authors.initials: CB
authors.lastname: Lau
keywords: SGLT; Schisandrae Chinensis Fructus; diabetes mellitus; traditional Chinese medicine