Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism

Yaoyao Jia; Muhammad Javidul Haque Bhuiyan; Hee Jin Jun; Ji Hae Lee; Minh Hien Hoang; Hak Ju Lee; Nahyun Kim; Dongho Lee; Kwang Yeon Hwang; Bang Yeon Hwang; Dal Woong Choi; Sung Joon Lee

doi:10.1016/j.bmcl.2011.07.095

Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism

Yaoyao Jia, Muhammad Javidul Haque Bhuiyan, Hee Jin Jun, Ji Hae Lee, Minh Hien Hoang, Hak Ju Lee, Nahyun Kim, Dongho Lee, Kwang Yeon Hwang, Bang Yeon Hwang, Dal Woong Choi, Sung Joon Lee

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

79 Citations (Scopus)

Abstract

In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-α in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-α; however, ursolic acid enhances the binding of PPAR-α to the peroxisome proliferator response element in PPAR-α-responsive genes, alters the expression of key genes in lipid metabolism, significantly reducing intracellular triglyceride and cholesterol concentrations in hepatocytes. Thus, ursolic acid is a PPAR-α agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-α.

Original language	English
Pages (from-to)	5876-5880
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2011.07.095
Publication status	Published - 2011 Oct 1

Keywords

Agonist
Hepatocyte
Lipid metabolism
PPAR-α
Ursolic acid

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2011.07.095

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title = "Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism",

abstract = "In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-α in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-α; however, ursolic acid enhances the binding of PPAR-α to the peroxisome proliferator response element in PPAR-α-responsive genes, alters the expression of key genes in lipid metabolism, significantly reducing intracellular triglyceride and cholesterol concentrations in hepatocytes. Thus, ursolic acid is a PPAR-α agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-α.",

keywords = "Agonist, Hepatocyte, Lipid metabolism, PPAR-α, Ursolic acid",

author = "Yaoyao Jia and Bhuiyan, {Muhammad Javidul Haque} and Jun, {Hee Jin} and Lee, {Ji Hae} and Hoang, {Minh Hien} and Lee, {Hak Ju} and Nahyun Kim and Dongho Lee and Hwang, {Kwang Yeon} and Hwang, {Bang Yeon} and Choi, {Dal Woong} and Lee, {Sung Joon}",

note = "Funding Information: This study was supported by the Korean Forest Service (Forest Science & Technology Project No. S120909L130110) and by the Technology Development Program for Fisheries of the Ministry for Food, Agriculture, Forestry and Fisheries, Republic of Korea (iPET, F20926409H220000110). The SPR instrument was provided by Korea Basic Science Institute. ",

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doi = "10.1016/j.bmcl.2011.07.095",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism

AU - Jia, Yaoyao

AU - Bhuiyan, Muhammad Javidul Haque

AU - Jun, Hee Jin

AU - Lee, Ji Hae

AU - Hoang, Minh Hien

AU - Lee, Hak Ju

AU - Kim, Nahyun

AU - Lee, Dongho

AU - Hwang, Kwang Yeon

AU - Hwang, Bang Yeon

AU - Choi, Dal Woong

AU - Lee, Sung Joon

N1 - Funding Information: This study was supported by the Korean Forest Service (Forest Science & Technology Project No. S120909L130110) and by the Technology Development Program for Fisheries of the Ministry for Food, Agriculture, Forestry and Fisheries, Republic of Korea (iPET, F20926409H220000110). The SPR instrument was provided by Korea Basic Science Institute.

PY - 2011/10/1

Y1 - 2011/10/1

N2 - In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-α in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-α; however, ursolic acid enhances the binding of PPAR-α to the peroxisome proliferator response element in PPAR-α-responsive genes, alters the expression of key genes in lipid metabolism, significantly reducing intracellular triglyceride and cholesterol concentrations in hepatocytes. Thus, ursolic acid is a PPAR-α agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-α.

AB - In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-α in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-α; however, ursolic acid enhances the binding of PPAR-α to the peroxisome proliferator response element in PPAR-α-responsive genes, alters the expression of key genes in lipid metabolism, significantly reducing intracellular triglyceride and cholesterol concentrations in hepatocytes. Thus, ursolic acid is a PPAR-α agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-α.

KW - Agonist

KW - Hepatocyte

KW - Lipid metabolism

KW - PPAR-α

KW - Ursolic acid

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SN - 0960-894X

VL - 21

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EP - 5880

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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ER -

Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism

Abstract

Keywords

ASJC Scopus subject areas

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