| Description: |
Phillyrin is a novel AMPK activator, has anti-obesity effects in nutritive obesity mice,
it can prevent lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation. Phillyrin may be a new preventive agent of acute lung injury in the clinical setting, it potentially contributes to the suppression of the activation of MAPK and NF-κB pathways, it also has protective effects on H2O2-induced oxidative stress and apoptosis in PC12 cells. |
| Targets: |
Fatty Acid Synthase | AMPK | ROS | Bcl-2/Bax | TNF-α | IL Receptor | MAPK | NF-kB |
| In vitro: |
| Food Chem. 2013 Jan 15;136(2):415-25. | | Phillyrin attenuates high glucose-induced lipid accumulation in human HepG2 hepatocytes through the activation of LKB1/AMP-activated protein kinase-dependent signalling.[Pubmed: 23122079] | Phillyrin, an active constituent found in many medicinal plants and certain functional foods, has anti-obesity activity in vivo. The aim of our study was to provide new data on the molecular mechanism(s) underlying the role of phillyrin in the prevention of high glucose-induced lipid accumulation in human HepG2 hepatocytes.
METHODS AND RESULTS:
We found that phillyrin suppressed high glucose-induced lipid accumulation in HepG2 cells. Phillyrin strongly inhibited high glucose-induced fatty acid synthase (FAS) expression by modulating sterol regulatory element-binding protein-1c (SREBP-1c) activation. Moreover, use of the pharmacological AMP-activated protein kinase (AMPK) inhibitor compound C revealed that AMPK is essential for suppressing SREBP-1c expression in phillyrin-treated cells. Finally, we found that liver kinase B1 (LKB1) phosphorylation is required for the phillyrin-enhanced activation of AMPK in HepG2 hepatocytes.
CONCLUSIONS:
These results indicate that phillyrin prevents lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation, suggesting that phillyrin is a novel AMPK activator with a role in the prevention and treatment of obesity. | | Xenobiotica . 2017 Apr;47(4):297-303. | | Effects of phillyrin and forsythoside A on rat cytochrome P450 activities in vivo and in vitro[Pubmed: 27310729] | | Abstract
1. Phillyrin and forsythoside A are two important active ingredients in Forsythia suspensa. However, the effects of phillyrin and forsythoside A on the activities of cytochrome P450 (CYP450) remain unclear. 2. This study aimed to investigate the effects of phillyrin and forsythoside A on the activities of CYP1A2, CYP2C11, CYP2D1 and CYP3A1/2 by cocktail probe drugs in rats both in vivo and in vitro. 3. Many pharmacokinetic parameters of caffeine and metoprolol in phillyrin pretreatment group, caffeine and tolbutamide in forsythoside A pretreatment group were affected significantly. In rat liver microsomal incubation system, the concentrations of acetaminophen and dextrophan in the phillyrin pretreatment group are higher than blank control group by 207.69% and 125.00%, however, the concentrations of 4-hydroxytolbutamide and 6β-hydroxytestosterone were not significantly altered. The concentrations of acetaminophen and 4-hydroxytolbutamide in the forsythoside A pretreatment group are higher than blank control group by 223.07% and 154.16%, whereas the concentrations of dextrophan and 6β-hydroxytestosterone were not significantly altered. 4. These results indicated that Phillyrin had potential inductive effects on rat CYP1A2 and CYP2D1 activities, without affecting CYP2C11 and CYP3A1/2 activities. Moreover, forsythoside A had inductive effects on the activities of CYP1A2 and CYP2C11, without affecting CYP2D1 and CYP3A1/2 activities.
Keywords: CYP1A2; CYP2C11; CYP2D1; CYP3A1/2; cytochrome P450; forsythoside A; phillyrin. |
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| In vivo: |
| Zhong Yao Cai. 2005 Feb;28(2):123-4. | | [Effect of phillyrin on the anti-obesity in nutritive obesity mice].[Pubmed: 15981888] | To study on the anti-obesity effect of phillyrin in nutritive obesity mice.
METHODS AND RESULTS:
The alimentary obesity model was established by hyperalimentation. The wet weight of fat, fat index, number of fat cells per unit visual field, Lee's index, jejunum microvillus area, serum triglyceride and cholesterol were selected to observe the anti-obesity effect of phillyrin.
Phillyrin could lower wet weight of fat (P < 0.01), fat index (P < 0.05 or P < 0.01), diameter of fat cell and Lee's index (P < 0.05), decrease the jejunum microvillus area, lower the level of serum triglyceride and cholesterol.
CONCLUSIONS:
Phillyrin has anti-obesity effect in nutritive obesity mice. | | Arch Pharm Res . 2016 Jul;39(7):998-1005. | | Protective effects of phillyrin against influenza A virus in vivo[Pubmed: 27323762] | | Abstract
Influenza A virus infection represents a great threat to public health. However, owing to side effects and the emergence of resistant virus strains, the use of currently available anti-influenza drugs may be limited. In order to identify novel anti-influenza drugs, we investigated the antiviral effects of phillyrin against influenza A virus infection in vivo. The mean survival time, lung index, viral titers, influenza hemagglutinin (HA) protein and serum cytokines levels, and histopathological changes in lung tissue were examined. Administration of phillyrin at a dose of 20 mg/kg/day for 3 days significantly prolonged the mean survival time, reduced the lung index, decreased the virus titers and interleukin-6 levels, reduced the expression of HA, and attenuated lung tissue damage in mice infected with influenza A virus. Taken together, these data showed that phillyrin had potential protective effects against infection caused by influenza A virus.
Keywords: Influenza A virus; Mouse; Phillyrin. |
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