PPAR alpha

Publication Title: 
Journal of Ethnopharmacology

ETHNOPHARMACOLOGICAL RELEVANCE: The fruits of Terminalia bellerica Roxb. (Combretaceae) and T. chebula Retz. (Combretaceae) are important components of triphala, a popular Ayurvedic formulation, for treating diabetes in Indian traditional medicine. AIM OF THE STUDY: The aim of this study was to evaluate the effects of the constituents of T. bellerica and T. chebula fruit extracts on PPAR? and PPAR? signaling/expression, cellular glucose uptake and adipogenesis. MATERIALS AND METHODS: PPAR? and PPAR?

Author(s): 
Yang, Min Hye
Vasquez, Yelkaira
Ali, Zulfiqar
Khan, Ikhlas A.
Khan, Shabana I.
Publication Title: 
Planta Medica

Medicinal plants are a rich source of ligands for nuclear receptors. The present study was aimed to screen a collection of plant extracts for PPAR?/?-activating properties and identify the active extract that can stimulate cellular glucose uptake without enhancing the adipogenesis. A reporter gene assay was performed to screen ethanolic extracts of 263 plant species, belonging to 94 families, for activation of PPAR? and PPAR?. Eight extracts showed activation of PPAR?, while 22 extracts showed activation of PPAR?.

Author(s): 
Yang, Min Hye
Avula, Bharathi
Smillie, Troy
Khan, Ikhlas A.
Khan, Shabana I.
Publication Title: 
Nature

Adiponectin secreted from adipocytes binds to adiponectin receptors AdipoR1 and AdipoR2, and exerts antidiabetic effects via activation of AMPK and PPAR-? pathways, respectively. Levels of adiponectin in plasma are reduced in obesity, which causes insulin resistance and type 2 diabetes. Thus, orally active small molecules that bind to and activate AdipoR1 and AdipoR2 could ameliorate obesity-related diseases such as type 2 diabetes. Here we report the identification of orally active synthetic small-molecule AdipoR agonists.

Author(s): 
Okada-Iwabu, Miki
Yamauchi, Toshimasa
Iwabu, Masato
Honma, Teruki
Hamagami, Ken-ichi
Matsuda, Koichi
Yamaguchi, Mamiko
Tanabe, Hiroaki
Kimura-Someya, Tomomi
Shirouzu, Mikako
Ogata, Hitomi
Tokuyama, Kumpei
Ueki, Kohjiro
Nagano, Tetsuo
Tanaka, Akiko
Yokoyama, Shigeyuki
Kadowaki, Takashi
Publication Title: 
Toxicology and Applied Pharmacology

Salacia oblonga (SO) root is an Ayurvedic medicine with anti-diabetic and anti-obese properties. Peroxisome proliferator-activated receptor (PPAR)-alpha, a nuclear receptor, plays an important role in maintaining the homeostasis of lipid metabolism.

Author(s): 
Huang, Tom Hsun-Wei
Peng, Gang
Li, George Qian
Yamahara, Johji
Roufogalis, Basil D.
Li, Yuhao
Publication Title: 
Toxicology and Applied Pharmacology

Excess cardiac triglyceride accumulation in diabetes and obesity induces lipotoxicity, which predisposes the myocytes to death. On the other hand, increased cardiac fatty acid (FA) oxidation plays a role in the development of myocardial dysfunction in diabetes. PPAR-alpha plays an important role in maintaining homeostasis of lipid metabolism.

Author(s): 
Huang, Tom Hsun-Wei
Yang, Qinglin
Harada, Masaki
Uberai, Jasna
Radford, Jane
Li, George Q.
Yamahara, Johji
Roufogalis, Basil D.
Li, Yuhao
Publication Title: 
Diabetes, Obesity & Metabolism

PPARs are transcription factors belonging to the superfamily of nuclear receptors. PPAR-alpha is involved in the regulation of fatty acid (FA) uptake and oxidation, inflammation and vascular function, while PPAR-gamma participates in FA uptake and storage, glucose homeostasis and inflammation. The PPARs are thus major regulators of lipid and glucose metabolism. Synthetic PPAR-alpha or PPAR-gamma agonists have been widely used in the treatment of dyslipidaemia, hyperglycaemia and their complications. However, they are associated with an incidence of adverse events.

Author(s): 
Li, Yuhao
Qi, Yanfei
Huang, Tom H. W.
Yamahara, Johji
Roufogalis, Basil D.
Publication Title: 
Food and Chemical Toxicology: An International Journal Published for the British Industrial Biological Research Association

Activation of peroxisome proliferator-activated receptor (PPAR)-alpha by natural and synthetic chemicals induces hepatic hypertrophy. An aqueous extract of Salacia oblonga root (SOW) is an Ayurvedic medicine with anti-diabetic and anti-obesity properties. In the present study, it was found that SOW (100, 300 and 900mg/kg, once daily by oral gavage over a 28 day period) elicited dose-related increases in liver weight (LW) by 1.6%, 13.4% and 42.5%, respectively, and in the ratio of LW to body weight by 8.8%, 16.7% and 40.2%, respectively, in male rats.

Author(s): 
Rong, Xianglu
Kim, Moon Sun
Su, Ning
Wen, Suping
Matsuo, Yukimi
Yamahara, Johji
Murray, Michael
Li, Yuhao
Publication Title: 
Life Sciences

In many traditional schools of medicine it is claimed that a balanced modulation of several targets can provide a superior therapeutic effect and decrease in side effect profile compared to a single action from a single selective ligand, especially in the treatment of certain chronic and complex diseases, such as diabetes and obesity. Diabetes and obesity have a multi-factorial basis involving both genetic and environmental risk factors. A wide array of medicinal plants and their active constituents play a role in the prevention and treatment of diabetes.

Author(s): 
Li, Yuhao
Huang, Tom Hsun-Wei
Yamahara, Johji
Publication Title: 
Journal of Ethnopharmacology

ETHNOPHARMACOLOGICAL RELEVANCE: The fruits of Terminalia bellerica Roxb. (Combretaceae) and T. chebula Retz. (Combretaceae) are important components of triphala, a popular Ayurvedic formulation, for treating diabetes in Indian traditional medicine. AIM OF THE STUDY: The aim of this study was to evaluate the effects of the constituents of T. bellerica and T. chebula fruit extracts on PPARα and PPARγ signaling/expression, cellular glucose uptake and adipogenesis.

Author(s): 
Yang, Min Hye
Vasquez, Yelkaira
Ali, Zulfiqar
Khan, Ikhlas A.
Khan, Shabana I.
Publication Title: 
Physiological Genomics

Intake of soy protein has been associated with improvements in lipid metabolism, with much attention being focused on the serum cholesterol-lowering property of soy. The component or components of soy that are responsible for improvements in lipid metabolism have been investigated and their specific actions debated. One component, the isoflavones, has been shown to have weak estrogenic activity, and recently, several research groups have suggested that isoflavones are activating peroxisome proliferator-activated receptors (PPARs).

Author(s): 
Mezei, Orsolya
Li, Yilan
Mullen, Eimear
Ross-Viola, Jennifer S.
Shay, Neil F.

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