Dibenzocyclooctadiene Lignans from Fructus Schisandrae Chinensis Improve Glucose Uptake in vitro

Abstract

Glucose uptake assay-guided fractionations of the methanol extract of Schisandra chinensis led to the isolation of the dibenzocyclooctadiene lignans: gomisin J (1), gomisin N (2), wuweizisu B (3), wuweizisu C (4), gomisin C (5), gomisin D (6), (+)-schisandrin A (7), schisandrin C (8), schisandrol A (9), gomisin H (10), angeloylgomisin H (11), gomisin A (12), and schizandrin (13). Among these, 1, 2, 7, and 8 significantly improved basal glucose uptake in HepG2 cells. Their improving effects were concentration-dependent. Compound 2 exhibited a stronger effect than that of rosiglitazone, which has been used as an anti-diabetic drug. The results suggest that these lignans may partially contribute to the anti-diabetic activity of Fructus Schisandrae Chinensis in traditional use by stimulating the glucose uptake into peripheral tissue, which may be responsible for reducing the level of blood glucose in circulation. Thus, these findings show the potential of these lignans for development as hypoglycemic drugs.

The lignan-rich fractions of Fructus Schisandrae improve insulin sensitivity via the PPAR-γ pathways in in vitro and in vivo studies

“…That study is partially consistent with our results: in the present study FS-80 that contained gomisin N induced weaker PPAR-␥ activity than FS-60. However, since gomisin A, schizandrin and angeloylgomisin H were not studied by Zhang et al (2010), there is the possibility that they have a greater influence on PPAR-␥ agonistic activity. Thus, lignan-rich fractions, especially FS-60, have the potential to be developed as hypoglycemic agents.…”

“…FS-60 contains schizandrin, gomisin A and angeloylgomisin H, and FS-80 contains deoxyschizandrin, ␥-schizandrin, and gomisin N. Recently, Zhang et al (2010) reported that gomisin J, gomisin N, (+)-schisandrin A, and schisandrin C significantly improved basal glucose uptake in HepG2 cells and gomisin A exhibited a stronger PPAR-␥ agonistic action than rosiglitazone. That study is partially consistent with our results: in the present study FS-80 that contained gomisin N induced weaker PPAR-␥ activity than FS-60.…”

“…They are known to have several biological features that help prevent hyperglycemia, hepatotoxicity and inflammation (Pan et al, 2008;Stacchiotti et al, 2009;Zhang et al, 2010). Gomisin J, gomisin N, schizandrin A and schizandrin C among lignans isolated Schisandrae chinensis significantly increase basal glucose uptake in HepG2 cells, and gomisin N especially was found to have a stronger effect than RGZ (Zhang et al, 2010). Deoxyschisandrin inhibited H 2 O 2 -stimulated degradation of IB-␣ and activation of NF-B by blocking translocation of NF-B to the nucleus (Gu et al, 2010).…”

“…We previously showed that 60 and 80% methanol fractions from XAD column chromatography improved insulinstimulated glucose uptake and increased GLUT4 expression in 3T3-L1 adipocytes (Ko et al, 2004). The major components of Fructus Schisandrae are lignans such as schizandrins and gomisins and some of them, gomisin J, gomisin N, schizandrin A, have been revealed to increase basal glucose uptake in HepG2 cells (Zhang et al, 2010). In addition, several schizandrins in Schiandra chinensis (Turcz.)…”

Schisandra polysaccharide inhibits hepatic lipid accumulation by downregulating expression of SREBPs in NAFLD mice

“…Aqueous and ethanolic extracts of Schisandra were recently shown to have a significant lipid-lowering effect in mice models of fatty liver [6]. Its active components and synthetic derivatives such as, bifendate and bicyclol, also showed a similar effect [7, 8]. The effect may be mediated via downregulation of SREBP-1 expression.…”