ABSTRACT
Objective: The present work was to investigate the protective effects of the aqueous extract of Gynura procumbens (GPAE) against nonalcoholic steatohepatitis (NASH) in mice and NCTC-1469 cells. Methods: C57BL/6J mice were fed with methionine and choline-deficient (MCD) diet and administered simultaneously with GPAE (500 and 1000 mg/kg/d, respectively) by gavage for six weeks. The biomarkers of NASH in serum and liver were determined. NCTC-1469 cells were pretreated with 0.25 mmol/L palmitic acid (PA) plus 0.5 mmol/L oleic acid (OA) for 24 h or treated with adenovirus expressing short-hairpin RNA against CFLAR (Ad-shCFLAR) for 24 h and then treated with GPAE (80 and 160 µg/mL, respectively) for 24 h, and the content of cellular biomarkers of NASH was detected. Results: In mice treated with MCD, GPAE could decrease the levels of serum ALT, AST, the content of hepatic TG, TC and MDA, repress the activities and protein expression of CYP2E1 and CYP4A and the phosphorylation of JNK, increase the activities of HO-1, CAT and GSH-Px, up-regulate the mRNA expression of PPARα, FABP5, CPT1α, ACOX, SCD-1, mGPAT, MTTP and the protein expression of CFLAR and NRF2. In NCTC-1469 cells treated with PA and OA, GPAE could decrease the content of cellular TG and ROS, promote the uptake of 2-NBDG, up-regulate the protein expression of CFLAR and NRF2. In NCTC-1469 cells treated with Ad-shCFLAR, GPAE up-regulated the mRNA and protein expression of CFLAR, down-regulated the phosphorylation of JNK, and increased the protein expression of NRF2 and pIRS1. Conclusion: These results indicated that the activation on CFLAR-JNK pathway might be the main anti-NASH mechanism of GPAE, which on the one hand promote the β-oxidation and efflux of fatty acids in liver, and finally reduce hepatic lipid accumulation, on the other hand increase the activities of anti-oxidant enzymes and inhibit the activities of ROS generation enzymes by activating NRF2, and therefore attenuates hepatic oxidative stress damage.
ABSTRACT
Objective To investigate the chemical constituents from the whole plants of Gynura procumbens. Methods The chemical constituents were isolated and purified by silica gel, Sephadex LH-20, and ODS. Their structures were determined by physicochemical properties and spectroscopic analysis. Results Twenty-seven compounds were identified as dibutyl phthalate (1), ursolic acid (2), kaempferol 3-O-β-D-glucopyranoside (3), 5-hydroxymaltol (4), 4-hydroxylbenzoic acid (5), 4-aminocinnamic acid (6), (E)-2-hexenyl β-D-glucoside (7), 1-(3-indolyl)-2,3-dihydroxy-propan-1-one (8), kaempferol-7-O-β-D-glucoside (9), quercetin-3-O-β-D- glucopyranoside (10), 3,4,5-tri-caffeoylquinic acid methyl ester (11), rutin (12), hesperidin (13), 3,4-dihydroxyphenylacetic acid methyl ester (14), euscophic acid (15), tormentic acid (16), 2-methoxy-4-(2-propenyl)-phenyl-O-β-D-glucopyranoside (17), negletein (18), 4,5-dihydroxy-3-methoxybenzoic acid (19), caesalpiniaphenol D (20), gentisic acid (21), 3,4-dihydroxybenzaldehyde (22), isohematinic acid (23), icariside B1 (24), dendranthemoside B (25), 4-methoxycinnamic acid (26), and baicalin (27). Conclusion Compounds 1, 2, 10, and 12 are obtained from the plants of G. procumbens for the first time, and compounds 4, 6-9, 11, 13-16, and 17-27 are obtained from Gynura genus for the first time.
ABSTRACT
Objective: To investigate the chemical constituents from the whole plants of Gynura procumbens. Methods: The chemical constituents were isolated and purified by repeated silica gel column chromatography, Sephadex LH-20 gel column chromatography, medium pressure column chromatography, and semi-preparative HPLC, and their structures were elucidated by chemical properties and spectroscopic analyses. Results: Sixteen compounds were identified to be quercetin (1), apigenin (2), luteolin (3), kaempferol (4), astragaline (5), kaempferol-5-O-(6″-O-acetyl)-β-D-glucopyranoside (6), negletein (7), 4-methoxycinnamic acid (8), benzyl-O-β-D-glucopyranoside (9), 2-phenylethyl-O-β-D-glucopyranoside (10), 3,5-dicaffeoylquinic acid methyl ester (11), 3,5-dicaffeoylquinic acid ethyl ester (12), 3,4-dicaffeoylquinic acid methyl ester (13), 4,5-dicaffeoylquinic acid methyl ester (14), protocatechuic acid (15), and eugenol glucoside (16). Conclusion: Compounds 7, 8, 12, 14, and 16 are obtained from the plants in Gynura Cass. for the first time, and compounds 3, 6, 9-11 and 13 are obtained from this plant for the first time.
ABSTRACT
Gynura procumbens (Lour.) Merr. has been used in some parts of Southeast Asia as a folk medicine to treat kidney diseases, diabetes mellitus, and hyperlipidemia. The present work was undertaken to prove the mechanisms of G. procumbens in the management of glomerular diseases. We investigated the effect of an aqueous extract of G. procumbens on cell proliferation, DNA synthesis, and the expressions of TGF-beta1, PDGF-BB, CDK1, CDK2, and CDK4 in fetal bovine serum-activated human mesangial cells (MCs). The G. procumbens extract inhibited proliferation, DNA synthesis, expressions of PDGF-BB, CDK1, and CDK2 mRNA, and expression of TGF-beta1 protein in MCs. The inhibitory effect of G. procumbens on MC proliferation may be mediated by suppression of PDGF-BB and TGF-beta1 expressions and the modulation of CDK1 and CDK2 expression. Therefore, G. procumbens shows promise as an adjunct therapy in preventing progressive renal diseases.