Search for New Type of PPARγ Agonist-Like Anti-diabetic Compounds from Medicinal Plants

Matsuda, Hisashi; Nakamura, Seikou; Yoshikawa, Masayuki

doi:10.1248/bpb.b14-00037

Cited by 25 publications

(21 citation statements)

References 60 publications

(84 reference statements)

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“…Hydrangeic acid from the processed leaves of Hydrangea macrophylla var. thunbergii has been reported to have PPARγ agonistic activity . We further showed that SaR, ZR, EH and ScR were strongly bound to the PPARγ expressed in VAT of 20 week‐old male mice (Fig.…”

Section: Discussionsupporting

confidence: 59%

Anti‐obesity and anti‐inflammatory effects of peroxisome proliferator activated receptor‐γ induced by bofutsushosan powder versus extract

Kobayashi

Saito

Yumita

et al. 2017

Traditional & Kampo Medicine

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Aim: Bofutsushosan (BT) has been used to treat systemic inflammatory diseases, including obesity, according to an original Chinese prescription book written in 1172. The '-san' suffix of 'Bofutsushosan' means that BT is prescribed as a pulverized crude drug. Peroxisome proliferator-activated receptor (PPAR)γ is known to play a pivotal role in adipocyte differentiation and to downregulate the transcription of adipocytokine genes leading to an inflammatory response. Given that the 'san' formulation is important for the anti-inflammation effect, we compared the anti-obesity and anti-inflammatory effects of PPARγ induced by BT powder with those by BT extract. Methods: The PPARγ agonistic activity of the separate crude BT drug components was measured on enzyme-linked immunosorbent assay (ELISA). For in vivo studies, male mice of the C57BL/6 strain were fed a high-fat diet containing 6.4% BT extract or BT powder for 65 days. Results: Water extract prepared from the BT components Saposhnikoviae Radix, Zingiberis Rhizoma, Ephedra Herba, and Scutellariae Radix had strong PPARγ ligand activity on ELISA. BT powder produced a significant reduction in visceral fat weight in addition to increases in PPARγ mRNA expression and peroxidase activity in visceral fat. BT powder and BT extract considerably decreased fatty acid binding protein-4 (FABP4), although the difference was not statistically significant. Conclusion: Peroxidase catalyzes lipid peroxides. Oxidative stress and inflammation induce FABP4 expression. BT powder was a more effective anti-inflammatory agent than BT extract. Furthermore, FABP4 triggers the ubiquitination and subsequent proteasomal degradation of PPARγ. This suggests that decrease in PPARγ by FABP4 might be restored by treatment with BT powder.

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Section: Discussionsupporting

confidence: 59%

Anti‐obesity and anti‐inflammatory effects of peroxisome proliferator activated receptor‐γ induced by bofutsushosan powder versus extract

Kobayashi

Saito

Yumita

et al. 2017

Traditional & Kampo Medicine

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“…Thus, searching for drugs with a similar clinical function, but fewer side effects has become a new direction of effort. Natural products are rich sources of drug discovery; thus, natural products are a focus of research …”

Section: Pparγ Agonists From Natural Productsmentioning

confidence: 99%

Therapeutic potential of PPARγ natural agonists in liver diseases

Guo

2020

J Cellular Molecular Medi

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Peroxisome proliferator‐activated receptor gamma (PPARγ) is a vital subtype of the PPAR family. The biological functions are complex and diverse. PPARγ plays a significant role in protecting the liver from inflammation, oxidation, fibrosis, fatty liver and tumours. Natural products are a promising pool for drug discovery, and enormous research effort has been invested in exploring the PPARγ‐activating potential of natural products. In this manuscript, we will review the research progress of PPARγ agonists from natural products in recent years and probe into the application potential and prospects of PPARγ natural agonists in the therapy of various liver diseases, including inflammation, hepatic fibrosis, non‐alcoholic fatty liver and liver cancer.

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“…While there is no shortage of reviews on PPAR γ modulators12, 13, 14, including natural products, to the best of our knowledge, general reviews on natural PPAR α modulators are still lacking, although some papers have reported on the activity of certain classes of natural products 15 .…”

Section: Natural Products Modulating Pparαmentioning

confidence: 99%

The potential of natural products for targeting PPAR α

Rigano

Sirignano

Taglialatela‐Scafati

2017

Acta Pharmaceutica Sinica B

118

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Peroxisome proliferator activated receptors (PPARs) α, -γ and -β/δ are ligand-activated transcription factors and members of the superfamily of nuclear hormone receptor. These receptors play key roles in maintaining glucose and lipid homeostasis by modulating gene expression. PPARs constitute a recognized druggable target and indeed several classes of drugs used in the treatment of metabolic disease symptoms, such as dyslipidemia (fibrates, e.g. fenofibrate and gemfibrozil) and diabetes (thiazolidinediones, e.g. rosiglitazone and pioglitazone) are ligands for the various PPAR isoforms. More precisely, antidiabetic thiazolidinediones act on PPARγ, while PPARα is the main molecular target of antidyslipidemic fibrates. Over the past few years, our understanding of the mechanism underlying the PPAR modulation of gene expression has greatly increased. This review presents a survey on terrestrial and marine natural products modulating the PPARα system with the objective of highlighting how the incredible chemodiversity of natural products can provide innovative leads for this “hot” target.

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Search for New Type of PPARγ Agonist-Like Anti-diabetic Compounds from Medicinal Plants

Cited by 25 publications

References 60 publications

Anti‐obesity and anti‐inflammatory effects of peroxisome proliferator activated receptor‐γ induced by bofutsushosan powder versus extract

Anti‐obesity and anti‐inflammatory effects of peroxisome proliferator activated receptor‐γ induced by bofutsushosan powder versus extract

Therapeutic potential of PPARγ natural agonists in liver diseases

The potential of natural products for targeting PPAR α

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