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Polyphenols with anti-proliferative activities from Penthorum chinense Pursh.

ABSTRACT: Two new polyphenols, penthorumin C (1) and 2,6-dihydroxyacetophenone-4-O- [4',6'-(S)-hexahydroxydiphenoyl]-β-D-glucose (2), along with four known polyphenolic acids, pinocembrin-7-O-[4",6"-hexahydroxydiphenoyl]-β-D-glucose(3), pinocembrin-7-O-[3"-O- galloyl- 4",6"-hexahydroxydiphenoyl]-β-D-glucose (4), thonningianin A (5), and thonningianin B (6) were isolated from Penthourm chinense. All compounds were evaluated for their anti-proliferative activity in HSC-T6 cells, and 2 and 5 showed significant activity, with IC50 values of 12.7 and 19.2 μM, respectively.

SUBMITTER: Huang D

PROVIDER: S-EPMC6271895 | biostudies-literature | 2014 Jul

REPOSITORIES: biostudies-literature

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Polyphenols with anti-proliferative activities from Penthorum chinense Pursh.

Huang Doudou D Jiang Yun Y Chen Wansheng W Yao Fengyan F Sun Lianna L

Molecules (Basel, Switzerland) 20140729 8

Two new polyphenols, penthorumin C (1) and 2,6-dihydroxyacetophenone-4-O- [4',6'-(S)-hexahydroxydiphenoyl]-β-D-glucose (2), along with four known polyphenolic acids, pinocembrin-7-O-[4",6"-hexahydroxydiphenoyl]-β-D-glucose(3), pinocembrin-7-O-[3"-O- galloyl- 4",6"-hexahydroxydiphenoyl]-β-D-glucose (4), thonningianin A (5), and thonningianin B (6) were isolated from Penthourm chinense. All compounds were evaluated for their anti-proliferative activity in HSC-T6 cells, and 2 and 5 showed significa ...[more]

PMID: 25076141

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Project description:Introduction: Alcoholic liver disease (ALD) was the second leading cause of liver injury. Penthorum chinense Pursh (GHC) is an important Miao ethnic drug of traditional Chinese medicine for the treatment of liver disease, but the pathogenesis is not clear. Aim of the study: To analysis the intestinal microflora and metabolic pathway of GHC on ALD mice. Methods: An HPLC-QTOF-MS method was used to identified the components from GHC extract, firstly. 60 mice were divided into six groups including blank group, model group, positive group and GHC groups (0.29, 0.87 and 2.61 g/kg). ALD mice was treated with GHC for 12 days. ALT, AST, TC and TG in serum were determined, liver index and pathological analysis were achieved. 16S rRNA gene sequencing was used to detect the intestinal microbial diversity. Finally, UPLC-QTOF-MS was used to analysis the metabolic pathways. Results: 38 ingredients were identified in GHC extract. Compared with the model group, liver index of the positive group and GHC (2.61 g/kg) group was significantly reduced. Compared with the model group, contents of ALT, AST, TC and TG of GHC groups reduced in a dose-dependent manner. Intestinal microbial diversity analysis indicated that Chao1, Observed species, Pielou_e, and Shannon indexes in GHC group (2.61 g/kg) were lower than those in model group. Principal coordinate analysis indicated that the intestinal microbial composition between blank group and model group, the model group and GHC (2.61 g/kg) group changed significantly. Compared with the model group, proportion of Firmicutes decreased, and the proportion of Bacteroidetes increased significantly in GHC group, which were 50.84% and 40.15%. The more prominent bacteria in the GHC group were odoribacteraceae, turicibacter, deferribacteraceae, and the intestinal beneficial symbiotic bacteria mucispirillum. Metabolic analysis indicated that, compared with blank group, 90 metabolites in model group changed significantly, and 68 metabolites were significantly callback in GHC group. Discussion: GHC has a therapeutic effect on ALD by regulating intestinal flora imbalance and metabolic pathways including Glycine, serine and threonine metabolism, Glutathione metabolism, Arginine and proline metabolism, Alanine, aspartate and glutamate metabolism, Butanoate metabolism and primary bile acid biosynthesis.

Project description:BackgroundPenthorum chinense Pursh (PCP), a medicinal and edible plant, has been reported to protect against liver damage by suppressing oxidative stress. Type 2 diabetes mellitus (T2DM) is associated with liver dysfunction and oxidative stress. In the present study, we aim to investigate the hypoglycemic effect of PCP on db/db mice and further explore the underlying mechanisms.MethodsThirty-two db/db mice were randomized into four groups, including a diabetic model control group (MC) and three diabetic groups treated with low (LPCP, 300 mg/kg/d), medium (MPLP, 600 mg/kg/d), and high doses of PCP (HPCP, 1200 mg/kg/d), and the normal control group (NC) of eight db/m mice were included. Mice in the NC and MC groups received the ultrapure water. After four weeks of intervention, parameters of fasting blood glucose (FBG), insulin resistance (IR), blood lipid levels, hepatic oxidative stress, and enzymes related to hepatic glucose metabolism were compared in the groups.ResultsPCP administration significantly reduced FBG and IR in diabetic db/db mice, and improved hepatic glucose metabolism by increasing glucose transporter 2 (GLUT2) and glucokinase (GCK) protein expression. Meanwhile, PCP supplementation ameliorated hepatic oxidative stress by decreasing malonaldehyde content and increasing the activities of superoxide dismutase and glutathione peroxidase in db/db mice. Furthermore, PCP treatment reduced obesity and food intake in db/db mice, and improved dyslipidemia demonstrated by increasing high-density lipoprotein cholesterol (HDL-C) while decreasing total cholesterol (TC), triglyceride (TG), and low-density lipoprotein cholesterol (HDL-C). All doses of PCP treatment decreased the values of LDL-C/HDL-C in a dose-response relationship.ConclusionPCP significantly alleviated hyperglycemia, hyperinsulinemia, hyperlipidemia, and obesity, inhibited hepatic oxidative stress, and enhanced hepatic glucose transport in T2DM mice. Based on the above findings, the hypoglycemic effect of PCP may be attributed to the activation of the GLUT2/GCK expression in the liver and the reduction of hepatic oxidative stress.

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Polyphenols with anti-proliferative activities from Penthorum chinense Pursh.

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Polyphenols with anti-proliferative activities from Penthorum chinense Pursh.

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