The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists

Azadeh Matin; Munikumar Reddy Doddareddy; Navnath Gavande; Srinivas Nammi; Paul W. Groundwater; Rebecca H. Roubin; David E. Hibbs

doi:10.1016/j.bmc.2012.11.040

The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists

Azadeh Matin, Munikumar Reddy Doddareddy, Navnath Gavande, Srinivas Nammi, Paul W. Groundwater, Rebecca H. Roubin, David E. Hibbs

School of Science

Research output: Contribution to journal › Article › peer-review

27 Citations (Scopus)

Abstract

Twenty three dual PPAR alpha and gamma molecules of natural product origin, previously reported by our group, were further investigated for pan PPAR transactivation against PPAR delta. The in vitro cell toxicity profile, as well as, in silico study of the most active molecules within this new class of pan PPAR agonists are also described. 3',5' Dimethoxy-7 hydroxyisoflavone 6, Psi-baptigenin 7, 4' fluoro-7 hydroxyisoflavone 8, and 3' methoxy-7 hydroxyisoflavone 9 were identified as the most potent molecules studied within the set compared to the commercially available pan PPAR agonist, bezafibrate 1. These novel active molecules may thus be useful as future leads in PPAR-related disorders, including type II diabetes mellitus and metabolic syndrome.

Original language	English
Pages (from-to)	766-778
Number of pages	13
Journal	Bioorganic & Medicinal Chemistry
Volume	21
Issue number	3
DOIs	https://doi.org/10.1016/j.bmc.2012.11.040
Publication status	Published - 2013

Keywords

cells
ligand
metabolism
non-insulin-dependent diabetes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmc.2012.11.040

Cite this

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abstract = "Twenty three dual PPAR alpha and gamma molecules of natural product origin, previously reported by our group, were further investigated for pan PPAR transactivation against PPAR delta. The in vitro cell toxicity profile, as well as, in silico study of the most active molecules within this new class of pan PPAR agonists are also described. 3',5' Dimethoxy-7 hydroxyisoflavone 6, Psi-baptigenin 7, 4' fluoro-7 hydroxyisoflavone 8, and 3' methoxy-7 hydroxyisoflavone 9 were identified as the most potent molecules studied within the set compared to the commercially available pan PPAR agonist, bezafibrate 1. These novel active molecules may thus be useful as future leads in PPAR-related disorders, including type II diabetes mellitus and metabolic syndrome.",

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author = "Azadeh Matin and Doddareddy, {Munikumar Reddy} and Navnath Gavande and Srinivas Nammi and Groundwater, {Paul W.} and Roubin, {Rebecca H.} and Hibbs, {David E.}",

year = "2013",

doi = "10.1016/j.bmc.2012.11.040",

language = "English",

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T1 - The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists

AU - Matin, Azadeh

AU - Doddareddy, Munikumar Reddy

AU - Gavande, Navnath

AU - Nammi, Srinivas

AU - Groundwater, Paul W.

AU - Roubin, Rebecca H.

AU - Hibbs, David E.

PY - 2013

Y1 - 2013

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AB - Twenty three dual PPAR alpha and gamma molecules of natural product origin, previously reported by our group, were further investigated for pan PPAR transactivation against PPAR delta. The in vitro cell toxicity profile, as well as, in silico study of the most active molecules within this new class of pan PPAR agonists are also described. 3',5' Dimethoxy-7 hydroxyisoflavone 6, Psi-baptigenin 7, 4' fluoro-7 hydroxyisoflavone 8, and 3' methoxy-7 hydroxyisoflavone 9 were identified as the most potent molecules studied within the set compared to the commercially available pan PPAR agonist, bezafibrate 1. These novel active molecules may thus be useful as future leads in PPAR-related disorders, including type II diabetes mellitus and metabolic syndrome.

KW - cells

KW - ligand

KW - metabolism

KW - non-insulin-dependent diabetes

UR - http://handle.uws.edu.au:8081/1959.7/524332

U2 - 10.1016/j.bmc.2012.11.040

DO - 10.1016/j.bmc.2012.11.040

M3 - Article

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JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

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ER -

The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists

Abstract

Keywords

UN SDGs

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