Research Progress of Natural Product Gentiopicroside - a Secoiridoid Compound

Wu, Shaoping; Ning, Yaoyao; Zhao, Ying-Yong; Sun, Wenjun; Thorimbert, Serge; Dechoux, Luc; Sollogoub, Matthieu; Zhang, Yongmin

doi:10.2174/1389557516666160624124127

Cited by 33 publications

(21 citation statements)

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“…Several previous studies have demonstrated that GL root extract contains various physiologically beneficial bioactive compounds [ 17 , 18 ]. To identify the bioactive constituent(s) that are responsible for the antiadipogenic effects of GL root extract, we performed fractionation of a 30% ethanol extract of GL root ( Figure 1 ).…”

Section: Resultsmentioning

confidence: 99%

Antiadipogenic Effects of Loganic Acid in 3T3-L1 Preadipocytes and Ovariectomized Mice

et al. 2018

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Obesity is caused by an excess storage of body fat, resulting from a chronic imbalance between energy intake and expenditure. Gentiana lutea L. (GL) root has been reported to reduce lipid accumulation in the aortic wall of diabetic rats. Here, we performed fractionation and isolation of the bioactive constituent(s) that may be responsible for the antiadipogenic effects of the GL root extract. A single compound, loganic acid, was identified as a candidate component in the 30% ethanol extract of GL. Loganic acid treatment significantly decreased the adipocyte differentiation of 3T3-L1 preadipocytes in a dose-dependent manner. The expression of key adipogenesis-related genes such as adiponectin (Adipoq), peroxisome proliferator-activated receptor gamma (Pparg), lipoprotein lipase (Lpl), perilipin1 (Plin1), fatty acid binding protein 4 (Fabp4), glucose transporter type 4 (Slc2a4), CCAAT/enhancer-binding protein alpha (Cebpa), and tumor necrosis factor-alpha (Tnf) were significantly reduced following treatment with loganic acid. In vivo experiments in an ovariectomy-induced obesity mouse model showed that loganic acid (oral administration with 10 and 50 mg/kg/day) significantly inhibited body weight gain, total fat increase, fatty hepatocyte deposition in the liver, and adipocyte enlargement in the abdominal visceral fat tissues. These results suggest that loganic acid in the GL root extract has antiadipogenic effects in vitro and in vivo. Loganic acid may be beneficial for the prevention and treatment of obesity, particularly in menopausal obese women.

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Section: Resultsmentioning

confidence: 99%

Antiadipogenic Effects of Loganic Acid in 3T3-L1 Preadipocytes and Ovariectomized Mice

et al. 2018

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“…been used from ancient times in China. GPS, a water-soluble ingredient in GM has anti-inflammatory and hepatoprotective effects (Mirzaee et al, 2017;Wu et al, 2017). Previously, we reported GPS could reverse ethanol-induced liver steatosis and drug-induced liver injury (Lian et al, 2010b;Wang et al, 2010).…”

Section: Discussionmentioning

confidence: 99%

Gentiopicroside Ameliorates the Progression from Hepatic Steatosis to Fibrosis Induced by Chronic Alcohol Intake

Yang

Shang

Jin

et al. 2020

Biomolecules & Therapeutics

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In current study, we aimed to investigate whether the gentiopicroside (GPS) derived from Gentiana manshurica Kitagawa could block the progression of alcoholic hepatic steatosis to fibrosis induced by chronic ethanol intake. C57BL/6 mice were fed an ethanol-containing Lieber-DeCarli diet for 4 weeks. LX-2 human hepatic stellate cells were treated with GPS 1 h prior to transforming growth factor-β (TGF-β) stimulation, and murine hepatocyte AML12 cells were pretreated by GPS 1 h prior to ethanol treatment. GPS inhibited the expression of type I collagen (collagen I), α-smooth muscle actin (α-SMA) and tissue inhibitor of metal protease 1 in ethanol-fed mouse livers with mild fibrosis. In addition, the imbalanced lipid metabolism induced by chronic ethanol-feeding was ameliorated by GPS pretreatment, characterized by the modulation of lipid accumulation. Consistently, GPS inhibited the expression of collagen I and α-SMA in LX-2 cells stimulated by TGF-β. Inhibition of lipid synthesis and promotion of oxidation by GPS were also confirmed in ethanol-treated AML12 cells. GPS could prevent hepatic steatosis advancing to the inception of a mild fibrosis caused by chronic alcohol exposure, suggesting GPS might be a promising therapy for targeting the early stage of alcoholic liver disease.

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“…As gentiopicroside is the major active compound of traditional Chinese oral decoction‐Longdan xiegan decoction, gentiopicroside was oral administration once a day in the present work. According to pharmacokinetic parameters of gentiopicroside (Liu, Liu, Dai, & Ma, 2018; Lu, Lin, & Tsai, 2014; Wu et al, 2017) and referring to published work, dose of gentiopicroside was set at 20 mg/kg, which equaled to 222 mg per day for 70 kg adults. Although as reported that gentiopicroside at oral 40 mg/kg for mice (equaled 28 mg/kg for rats) showed no toxicity in the liver (Li et al, 2018; Yang et al, 2020), however, there are few reports on the toxicity experiments, which limits the safety evaluation of gentiopicroside.…”

Section: Discussionmentioning

confidence: 99%

Gentiopicroside prevents alcoholic liver damage by improving mitochondrial dysfunction in the rat model

Yang

Wang

Song

et al. 2020

Phytotherapy Research

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Gentianae Radix et Rhizoma is a medical plant that is widely cultivated in China, North Korea, Japan, and Russia, and gentiopicroside is one of its major active compounds. In this study, the hepatoprotective activity of gentiopicroside on rats with alcoholic liver damage (ALD) was evaluated using the transaminase and blood lipid levels and antioxidant capacity. The potential mechanism of hepatoprotective effect of gentiopicroside was evaluated by mitochondrial function detection, gas chromatography–mass spectrometry (GC–MS) metabolomic analysis, and anti‐apoptosis analysis. Results showed that the gentiopicroside exhibited good hepatoprotective activity on rats with ALD by decreasing the transaminase levels, regulating the blood lipid levels, and increasing the antioxidant capacity. The potential mechanisms were related to regulating mitochondrial dysfunction by recovering mitochondrial membrane potential level, adenosine triphosphate concentration, activities of key enzymes in tricarboxylic acid cycle, and activities of complex I‐V, regulating micromolecular metabolism and anti‐apoptosis. These findings supported the further exploration of Gentianae Radix et Rhizoma as effective phytotherapy to prevent and treat ALD.

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Research Progress of Natural Product Gentiopicroside - a Secoiridoid Compound

Cited by 33 publications

References 0 publications

Antiadipogenic Effects of Loganic Acid in 3T3-L1 Preadipocytes and Ovariectomized Mice

Antiadipogenic Effects of Loganic Acid in 3T3-L1 Preadipocytes and Ovariectomized Mice

Gentiopicroside Ameliorates the Progression from Hepatic Steatosis to Fibrosis Induced by Chronic Alcohol Intake

Gentiopicroside prevents alcoholic liver damage by improving mitochondrial dysfunction in the rat model

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