Chemical constituents from Sophora tonkinensis and their glucose transporter 4 translocation activities

Yang, Xinzhou; Deng, Shihao; Mi, Huang; Wang, Jialin; Chen, Li; Xiong, Mingrui; Yang, Jie; Zheng, Sijiang; Ma, Xiaochun; Zhao, Ping; Feng, Yunjiang

doi:10.1016/j.bmcl.2017.01.078

Cited by 21 publications

(11 citation statements)

References 19 publications

(14 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Many hypoglycemic agents from natural products have been approved for clinical use in China . Our previous studies have shown that many natural products have the potential to treat DM . Natural products are an important source for possible new drug development for the treatment of DM.…”

Section: Discussionmentioning

confidence: 99%

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐A^y Mice with Spontaneous Type 2 Diabetes Mellitus

Xiong

Huang

Liu

et al. 2018

Molecular Nutrition Food Res

Self Cite

View full text Add to dashboard Cite

show abstract

Section: Discussionmentioning

confidence: 99%

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐A^y Mice with Spontaneous Type 2 Diabetes Mellitus

Xiong

Huang

Liu

et al. 2018

Molecular Nutrition Food Res

Self Cite

View full text Add to dashboard Cite

show abstract

“…Then, all insoluble material was discarded and the BCA kit was used to measure the protein concentration. The proteins collected from tissues and cells were subjected to Western blot analysis according to the previously described methods (21).…”

Section: Protein Extracts and Western Blottingmentioning

confidence: 99%

Antidiabetic effects of a lipophilic extract obtained from flowers of Wisteria sinensis by activating Akt/GLUT4 and Akt/GSK3β

Ren

Zhang

et al. 2020

Food & Nutrition Research

Self Cite

View full text Add to dashboard Cite

Background: Type 2 diabetes mellitus is primarily caused by insulin resistance (IR) in insulin-sensitive tissues, including liver, white adipose tissues (WAT), and skeletal muscles. Discovering nutritious foods with antidiabetic effects is of great significance. Numerous published reports indicated that protein kinase B (Akt) and glucose transporter 4 (GLUT4) play crucial roles in ameliorating IR and diabetic symptoms. Objective: In the present study, antidiabetic effects and the potential mechanism of action of WS-PE (a lipophilic extract from edible flowers of Wisteria sinensis) were explored with L6 cells in vitro and in high-fat diet (HFD) + Streptozocin (STZ)-induced diabetic mice in vivo. Design: In vivo, HFD + STZ-induced diabetic mice were used as diabetic models to investigate the potential antidiabetic and antidyslipidemic activities. In vitro, a novel GLUT4 translocation assay system was established to evaluate the potential effects of WS-PE on GLUT4 translocation. Western blot analysis was adopted to investigate the molecular mechanisms of WS-PE both in vivo and in vitro. Results: In vitro, WS-PE increased glucose uptake by stimulating GLUT4 expression and translocation, which were regulated by Akt phosphorylation. In vivo, the WS-PE treatment ameliorated the hyperglycemia, IR, and dyslipidemia and reversed hepatic steatosis and pancreatic damage in diabetic mice. The WS-PE treatment increased GLUT4 expression by Akt activation in WAT and skeletal muscle. Akt activation stimulated GSK3β phosphorylation in liver and skeletal muscles, indicating that WS-PE showed regulatory effects on glycogen synthesis in liver and skeletal muscles. Conclusion: These in vitro and in vivo results indicated that the WS-PE treatment exerted antidiabetic effects by activating Akt/GLUT4 and Akt/GSK3β.

show abstract

“…It exhibits anti-inflammatory effects by inhibiting nitric oxide production in macrophages [4] and 5-lipoxygenase activity [3]. Several studies have also demonstrated its other biological activities, such as anti-cancer [5], anti-diabetic diabetic [6], and immunomodulatory [7] Figure 1. Chemical structure of (-)-sophoranone (SPN).…”

Section: Introductionmentioning

confidence: 99%

Lack of Correlation between In Vitro and In Vivo Studies on the Inhibitory Effects of (‒)-Sophoranone on CYP2C9 Is Attributable to Low Oral Absorption and Extensive Plasma Protein Binding of (‒)-Sophoranone

et al. 2020

View full text Add to dashboard Cite

(‒)-Sophoranone (SPN) is a bioactive component of Sophora tonkinensis with various pharmacological activities. This study aims to evaluate its in vitro and in vivo inhibitory potential against the nine major CYP enzymes. Of the nine tested CYPs, it exerted the strongest inhibitory effect on CYP2C9-mediated tolbutamide 4-hydroxylation with the lowest IC50 (Ki) value of 0.966 ± 0.149 μM (0.503 ± 0.0383 μM), in a competitive manner. Additionally, it strongly inhibited other CYP2C9-catalyzed diclofenac 4′-hydroxylation and losartan oxidation activities. Upon 30 min pre-incubation of human liver microsomes with SPN in the presence of NADPH, no obvious shift in IC50 was observed, suggesting that SPN is not a time-dependent inactivator of the nine CYPs. However, oral co-administration of SPN had no significant effect on the pharmacokinetics of diclofenac and 4′-hydroxydiclofenac in rats. Overall, SPN is a potent inhibitor of CYP2C9 in vitro but not in vivo. The very low permeability of SPN in Caco-2 cells (Papp value of 0.115 × 10−6 cm/s), which suggests poor absorption in vivo, and its high degree of plasma protein binding (>99.9%) may lead to the lack of in vitro–in vivo correlation. These findings will be helpful for the safe and effective clinical use of SPN.

show abstract

Chemical constituents from Sophora tonkinensis and their glucose transporter 4 translocation activities

Cited by 21 publications

References 19 publications

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐A^y Mice with Spontaneous Type 2 Diabetes Mellitus

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐A^y Mice with Spontaneous Type 2 Diabetes Mellitus

Antidiabetic effects of a lipophilic extract obtained from flowers of Wisteria sinensis by activating Akt/GLUT4 and Akt/GSK3β

Lack of Correlation between In Vitro and In Vivo Studies on the Inhibitory Effects of (‒)-Sophoranone on CYP2C9 Is Attributable to Low Oral Absorption and Extensive Plasma Protein Binding of (‒)-Sophoranone

Contact Info

Product

Resources

About

Chemical constituents from Sophora tonkinensis and their glucose transporter 4 translocation activities

Cited by 21 publications

References 19 publications

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐Ay Mice with Spontaneous Type 2 Diabetes Mellitus

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐Ay Mice with Spontaneous Type 2 Diabetes Mellitus

Antidiabetic effects of a lipophilic extract obtained from flowers of Wisteria sinensis by activating Akt/GLUT4 and Akt/GSK3β

Lack of Correlation between In Vitro and In Vivo Studies on the Inhibitory Effects of (‒)-Sophoranone on CYP2C9 Is Attributable to Low Oral Absorption and Extensive Plasma Protein Binding of (‒)-Sophoranone

Contact Info

Product

Resources

About

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐A^y Mice with Spontaneous Type 2 Diabetes Mellitus

Antidiabetic Activity of Ergosterol from Pleurotus Ostreatus in KK‐A^y Mice with Spontaneous Type 2 Diabetes Mellitus