Oleanolic acid derivative NPLC441 potently stimulates glucose transport in 3T3-L1 adipocytes via a multi-target mechanism

Lin, Zhonghui; Zhang, Yinan; Shen, Hong; Hu, Lihong; Jiang, Hualiang; Shen, Xu

doi:10.1016/j.bcp.2008.08.016

Cited by 35 publications

(20 citation statements)

References 55 publications

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“…Recent evidence suggests that OA, UA, and a number of their derivatives can improve insulin signaling by enhancing insulin receptor (IR) β subunit phosphorylation and Akt in vitro . Insulin regulates glucose homeostasis through binding of its receptor to initiate a signaling cascade; activation and phosphorylation of the insulin receptor substrate (IRS) proteins, and mediation of the phosphatidylinositol 3‐kinase‐dependent/the protein kinase Akt (phosphoinositide 3 kinase/Protein kinase B [PI3K/Akt]) pathway (Fig.…”

Section: Oa and Ua Lower Blood Glucose Levels By Improving Insulin Akmentioning

confidence: 99%

The molecular mechanisms underpinning the therapeutic properties of oleanolic acid, its isomer and derivatives for type 2 diabetes and associated complications

Camer

Szabo

et al. 2014

Molecular Nutrition Food Res

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X. (2014). The molecular mechanisms underpinning the therapeutic properties of oleanolic acid, its isomer and derivatives for type 2 diabetes and associated complications. Molecular Nutrition and Food Research, 58 (8), 1750-1759. The molecular mechanisms underpinning the therapeutic properties of oleanolic acid, its isomer and derivatives for type 2 diabetes and associated complications AbstractRecent research has uncovered the molecular mechanisms responsible for the therapeutic properties of oleanolic acid (OA), its isomer ursolic acid (UA), and derivatives. In particular, recent reports have highlighted the benefits of these compounds in the prevention and treatment of type 2 diabetes and associated life-threatening complications, such as nonalcoholic fatty liver disease, nephropathy, retinopathy, and atherosclerosis. The prevalence of type 2 diabetes is of major concern since it is reaching global epidemic levels. Treatments targeting the signaling pathways altered in type 2 diabetes are being actively investigated, and OA and UA in natural and derivative forms are potential candidates to modulate these pathways. We will explore the findings from in vitro and in vivo studies showing that these compounds: (i) improve insulin signaling and reduce hyperglycemia; (ii) reduce oxidative stress by upregulating anti-oxidants and; (iii) reduce inflammation by inhibiting proinflammatory signaling. We will discuss the molecular mechanisms underpinning these therapeutic properties in this review in order to provide a rationale for the future use of OA, UA, and their derivatives for the prevention and treatment of type 2 diabetes and associated comorbidities. Abstract: Recent research has uncovered the molecular mechanisms responsible for the therapeutic properties of oleanolic acid (OA), its isomer ursolic acid (UA) and derivatives. In particular, recent reports have highlighted the benefits of these compounds in the prevention and treatment of type 2 diabetes and associated life-threatening complications, such as nonalcoholic fatty liver disease, nephropathy, retinopathy and atherosclerosis. The prevalence of type 2 diabetes is of major concern since it is reaching global epidemic levels. Treatments targeting the signalling pathways altered in type 2 diabetes are being actively investigated, and OA and UA in natural and derivative forms are potential candidates to modulate these pathways. We will explore the findings from in vitro and in vivo studies showing that these compounds: 1) Improve insulin signalling and reduce hyperglycaemia; 2) Reduce oxidative stress by upregulating anti-oxidants and; 3) Reduce inflammation by inhibiting proinflammatory signalling. We will discuss the molecular mechanisms underpinning these therapeutic properties in this review in order to provide a rationale for the future use of OA, UA and their derivatives for the prevention and treatment of type 2 diabetes and associated comorbidities.

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Section: Oa and Ua Lower Blood Glucose Levels By Improving Insulin Akmentioning

confidence: 99%

The molecular mechanisms underpinning the therapeutic properties of oleanolic acid, its isomer and derivatives for type 2 diabetes and associated complications

Camer

Szabo

et al. 2014

Molecular Nutrition Food Res

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“…Derivatization of oleanolic acid provided compound 95 (NPLC441) with improved selectivity over Tc-PTP although with decreased potency. 134 It enhanced insulin-stimulated phosphorylation of IR and AKT in HepG2 cell, indicating good cell permeability. Compound 96 was also originated from oleanolic acid but without any increase in potency.…”

Section: Natural Products and Derivativesmentioning

confidence: 98%

“…135 Several derivatives of maslinic acid have been synthesized and evaluated for PTP1B inhibition. 134 The best compound, 97, showed an IC 50 of 0.64 mM with selectivity of 6.9-fold over Tc-PTP. In addition, compound 98 was developed from another triterpenoid saponin.…”

Section: Natural Products and Derivativesmentioning

confidence: 99%

Chapter 6. Recent Advances in PTP1B Inhibitor Development for the Treatment of Type 2 Diabetes and Obesity

He¹,

Zeng²,

He³

et al. 2012

Drug Discovery

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“…Likewise, the natural product oleanolic acid has an antidiabetes action; its derivative (3-beta-(2-carboxybenzoyloxy)-oleanolic acid) upregulated the expression of GLUT4 in 3T3-L1 adipocytes [41]. Cryptolepine analogs based on Cryptolepis sanguinolenta have antihyperglycemic activities [42,43] Cephalotaxus sinensis…”

Section: Antidiabetic Drugsmentioning

confidence: 99%

Natural Product-Based Drug Discovery

Ahmad

2015

Reviews in Cell Biology and Molecular Medicine

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Oleanolic acid derivative NPLC441 potently stimulates glucose transport in 3T3-L1 adipocytes via a multi-target mechanism

Cited by 35 publications

References 55 publications

The molecular mechanisms underpinning the therapeutic properties of oleanolic acid, its isomer and derivatives for type 2 diabetes and associated complications

The molecular mechanisms underpinning the therapeutic properties of oleanolic acid, its isomer and derivatives for type 2 diabetes and associated complications

Chapter 6. Recent Advances in PTP1B Inhibitor Development for the Treatment of Type 2 Diabetes and Obesity

Natural Product-Based Drug Discovery

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