Potential AMPK activators of cucurbitane triterpenoids from Siraitia grosvenorii Swingle

Chen, Xu-bing; Zhuang, Jingjing; Liu, Junhua; Lei, Min; Ma, Lei; Chen, Jing; Shen, Xu; Hu, Lihong

doi:10.1016/j.bmc.2011.08.030

Cited by 63 publications

(43 citation statements)

References 13 publications

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“…In this study, we showed that mogrol also phosphorylated AMPK in 3T3-L1 cells, similar to its role in hepatocytes [25]. Forskolin (an activator of adenylate cyclase) and cAMP analogs activate AMPK in 3T3-L1 cells during late-stage differentiation [11].…”

Section: Discussionmentioning

confidence: 90%

“…Several phytochemicals such as catechins [20], flavonoids [21], and carotenoids [22] produce beneficial effects by inhibiting lipid accumulation in adipocytes. Mogrosides possess anti-diabetic activities [23, 24] and mogrol was shown to increase AMPK activity in hepatocytes [25]. However, its effect on adipocytes has not yet been established.…”

Section: Introductionmentioning

confidence: 99%

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Mogrol Derived from Siraitia grosvenorii Mogrosides Suppresses 3T3-L1 Adipocyte Differentiation by Reducing cAMP-Response Element-Binding Protein Phosphorylation and Increasing AMP-Activated Protein Kinase Phosphorylation

Harada¹,

Ishihara²,

Horiuchi³

et al. 2016

PLoS ONE

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This study investigated the effects of mogrol, an aglycone of mogrosides from Siraitia grosvenorii, on adipogenesis in 3T3-L1 preadipocytes. Mogrol, but not mogrosides, suppressed triglyceride accumulation by affecting early (days 0–2) and late (days 4–8), but not middle (days 2–4), differentiation stages. At the late stage, mogrol increased AMP-activated protein kinase (AMPK) phosphorylation and reduced glycerol-3-phosphate dehydrogenase activity. At the early stage, mogrol promoted AMPK phosphorylation, inhibited the induction of CCAAT/enhancer-binding protein β (C/EBPβ; a master regulator of adipogenesis), and reduced 3T3-L1 cell contents (e.g., clonal expansion). In addition, mogrol, but not the AMPK activator AICAR, suppressed the phosphorylation and activity of the cAMP response element-binding protein (CREB), which regulates C/EBPβ expression. These results indicated that mogrol suppressed adipogenesis by reducing CREB activation in the initial stage of cell differentiation and by activating AMPK signaling in both the early and late stages of this process.

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Section: Discussionmentioning

confidence: 90%

Section: Introductionmentioning

confidence: 99%

Mogrol Derived from Siraitia grosvenorii Mogrosides Suppresses 3T3-L1 Adipocyte Differentiation by Reducing cAMP-Response Element-Binding Protein Phosphorylation and Increasing AMP-Activated Protein Kinase Phosphorylation

Harada¹,

Ishihara²,

Horiuchi³

et al. 2016

PLoS ONE

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“…Recently, hydrolyzed mogrosides were reported to activate AMPK (24). The process might contribute to upregulation of genes related to glucose metabolism and restore normal insulin secretion function in pancreatic β cells.…”

Section: Discussionmentioning

confidence: 99%

Antioxidant effect of mogrosides against oxidative stress induced by palmitic acid in mouse insulinoma NIT-1 cells

Chen

Deng

et al. 2013

Braz J Med Biol Res

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Excessive oxidative stress in pancreatic β cells, caused by glucose and fatty acids, is associated with the pathogenesis of type 2 diabetes. Mogrosides have shown antioxidant and antidiabetic activities in animal models of diabetes, but the underlying mechanisms remain unclear. This study evaluated the antioxidant effect of mogrosides on insulinoma cells under oxidative stress caused by palmitic acid, and investigated the underlying molecular mechanisms. Mouse insulinoma NIT-1 cells were cultured in medium containing 0.75 mM palmitic acid, mimicking oxidative stress. The effects of 1 mM mogrosides were determined with the dichlorodihydrofluorescein diacetate assay for intracellular reactive oxygen species (ROS) and FITC-Annexin V/PI assay for cell apoptosis. Expression of glucose transporter-2 (GLUT2) and pyruvate kinase was determined by semi-quantitative reverse-transcription polymerase chain reaction. Palmitic acid significantly increased intracellular ROS concentration 2-fold (P<0.05), and decreased expression of GLUT2 (by 60%, P<0.05) and pyruvate kinase (by 80%, P<0.05) mRNAs in NIT-1 cells. Compared with palmitic acid, co-treatment with 1 mM mogrosides for 48 h significantly reduced intracellular ROS concentration and restored mRNA expression levels of GLUT2 and pyruvate kinase. However, mogrosides did not reverse palmitic acid-induced apoptosis in NIT-1 cells. Our results indicate that mogrosides might exert their antioxidant effect by reducing intracellular ROS and regulating expression of genes involved in glucose metabolism. Further research is needed to achieve a better understanding of the signaling pathway involved in the antioxidant effect of mogrosides.

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“…Kainic acid [74] D-xylose [75] Phenformin [55] Inhibits mitochondria respiratory chain A-769662 [42] Direct AMPK activator Cucurbitane triterpenoids [73] D942 [74] O O F CO 2 H…”

Section: Ampk Activator and Diabetic Ulcer Animal Studymentioning

confidence: 99%

AMP-activated protein kinase activators in diabetic ulcers: from animal studies to Phase II drugs under investigation

Lin¹,

Chen

Chiu

et al. 2014

Expert Opinion on Investigational Drugs

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Animal studies have demonstrated that AMPK activators are a potential treatment for diabetic ulcers. AMPK activators alleviate tissue inflammation and promote re-epithelialization in diabetic wounds. However, due to the complicated pathological mechanism of diabetic foot ulcers, AMPK activators should be combined with other approaches. The new strategies for combination therapy with AMPK activator may provide a therapeutic advantage for patients with diabetic ulcers.

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Potential AMPK activators of cucurbitane triterpenoids from Siraitia grosvenorii Swingle

Cited by 63 publications

References 13 publications

Mogrol Derived from Siraitia grosvenorii Mogrosides Suppresses 3T3-L1 Adipocyte Differentiation by Reducing cAMP-Response Element-Binding Protein Phosphorylation and Increasing AMP-Activated Protein Kinase Phosphorylation

Mogrol Derived from Siraitia grosvenorii Mogrosides Suppresses 3T3-L1 Adipocyte Differentiation by Reducing cAMP-Response Element-Binding Protein Phosphorylation and Increasing AMP-Activated Protein Kinase Phosphorylation

Antioxidant effect of mogrosides against oxidative stress induced by palmitic acid in mouse insulinoma NIT-1 cells

AMP-activated protein kinase activators in diabetic ulcers: from animal studies to Phase II drugs under investigation

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