Ursolic acid, an antagonist for transforming growth factor (TGF)-beta1
Transforming growth factor-beta (TGF-beta), a multifunctional cytokine which is involved in extracellular matrix modulation, has a major role in the pathogenesis and progression of fibrotic diseases. We now report the effects of ursolic acid on TGF-beta1 receptor binding and TGF-beta1-induced cellul...
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| Veröffentlicht in: | FEBS letters 2004-05, Vol.566 (1-3), p.55 |
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| creator | Murakami, Shigeru Takashima, Hajime Sato-Watanabe, Mariko Chonan, Sumi Yamamoto, Koji Saitoh, Masako Saito, Shiuji Yoshimura, Hiromitsu Sugawara, Koko Yang, Junshan Gao, Nannan Zhang, Xinggao |
| description | Transforming growth factor-beta (TGF-beta), a multifunctional cytokine which is involved in extracellular matrix modulation, has a major role in the pathogenesis and progression of fibrotic diseases. We now report the effects of ursolic acid on TGF-beta1 receptor binding and TGF-beta1-induced cellular functions in vitro. Ursolic acid inhibited [(125)I]-TGF-beta1 receptor binding to Balb/c 3T3 mouse fibroblasts with an IC(50) value of 6.9+/-0.8 microM. Ursolic acid dose-dependently recovered reduced proliferation of Minc Mv1Lu cells in the presence of 5 nM of TGF-beta1 and attenuated TGF-beta1-induced collagen synthesis and production in human fibroblasts. Molecular dynamics simulations suggest that ursolic acid may interact with the hydrophobic region of the dimeric interface and thereby inhibit the binding of TGF-beta1 to its receptor. All these findings taken together show that ursolic acid functions as an antagonist for TGF-beta1. This is the first report to show that a small molecule can inhibit TGF-beta1 receptor binding and influence functions of TGF-beta1. |
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We now report the effects of ursolic acid on TGF-beta1 receptor binding and TGF-beta1-induced cellular functions in vitro. Ursolic acid inhibited [(125)I]-TGF-beta1 receptor binding to Balb/c 3T3 mouse fibroblasts with an IC(50) value of 6.9+/-0.8 microM. Ursolic acid dose-dependently recovered reduced proliferation of Minc Mv1Lu cells in the presence of 5 nM of TGF-beta1 and attenuated TGF-beta1-induced collagen synthesis and production in human fibroblasts. Molecular dynamics simulations suggest that ursolic acid may interact with the hydrophobic region of the dimeric interface and thereby inhibit the binding of TGF-beta1 to its receptor. All these findings taken together show that ursolic acid functions as an antagonist for TGF-beta1. This is the first report to show that a small molecule can inhibit TGF-beta1 receptor binding and influence functions of TGF-beta1.</description><identifier>ISSN: 0014-5793</identifier><identifier>PMID: 15147868</identifier><language>eng</language><publisher>England</publisher><subject>Animals ; BALB 3T3 Cells ; Cell Division - drug effects ; Cells, Cultured ; Collagen Type I - biosynthesis ; Dose-Response Relationship, Drug ; Epithelial Cells - cytology ; Epithelial Cells - metabolism ; Fibroblasts - metabolism ; Humans ; Lung - cytology ; Mice ; Mink ; Models, Molecular ; Proline - metabolism ; Radioligand Assay ; Recombinant Proteins - antagonists & inhibitors ; Recombinant Proteins - genetics ; Recombinant Proteins - metabolism ; Thymidine - metabolism ; Transforming Growth Factor beta - antagonists & inhibitors ; Transforming Growth Factor beta - genetics ; Transforming Growth Factor beta - metabolism ; Transforming Growth Factor beta - pharmacology ; Transforming Growth Factor beta1 ; Triterpenes - pharmacology ; Ursolic Acid</subject><ispartof>FEBS letters, 2004-05, Vol.566 (1-3), p.55</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15147868$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Murakami, Shigeru</creatorcontrib><creatorcontrib>Takashima, Hajime</creatorcontrib><creatorcontrib>Sato-Watanabe, Mariko</creatorcontrib><creatorcontrib>Chonan, Sumi</creatorcontrib><creatorcontrib>Yamamoto, Koji</creatorcontrib><creatorcontrib>Saitoh, Masako</creatorcontrib><creatorcontrib>Saito, Shiuji</creatorcontrib><creatorcontrib>Yoshimura, Hiromitsu</creatorcontrib><creatorcontrib>Sugawara, Koko</creatorcontrib><creatorcontrib>Yang, Junshan</creatorcontrib><creatorcontrib>Gao, Nannan</creatorcontrib><creatorcontrib>Zhang, Xinggao</creatorcontrib><title>Ursolic acid, an antagonist for transforming growth factor (TGF)-beta1</title><title>FEBS letters</title><addtitle>FEBS Lett</addtitle><description>Transforming growth factor-beta (TGF-beta), a multifunctional cytokine which is involved in extracellular matrix modulation, has a major role in the pathogenesis and progression of fibrotic diseases. We now report the effects of ursolic acid on TGF-beta1 receptor binding and TGF-beta1-induced cellular functions in vitro. Ursolic acid inhibited [(125)I]-TGF-beta1 receptor binding to Balb/c 3T3 mouse fibroblasts with an IC(50) value of 6.9+/-0.8 microM. Ursolic acid dose-dependently recovered reduced proliferation of Minc Mv1Lu cells in the presence of 5 nM of TGF-beta1 and attenuated TGF-beta1-induced collagen synthesis and production in human fibroblasts. Molecular dynamics simulations suggest that ursolic acid may interact with the hydrophobic region of the dimeric interface and thereby inhibit the binding of TGF-beta1 to its receptor. All these findings taken together show that ursolic acid functions as an antagonist for TGF-beta1. This is the first report to show that a small molecule can inhibit TGF-beta1 receptor binding and influence functions of TGF-beta1.</description><subject>Animals</subject><subject>BALB 3T3 Cells</subject><subject>Cell Division - drug effects</subject><subject>Cells, Cultured</subject><subject>Collagen Type I - biosynthesis</subject><subject>Dose-Response Relationship, Drug</subject><subject>Epithelial Cells - cytology</subject><subject>Epithelial Cells - metabolism</subject><subject>Fibroblasts - metabolism</subject><subject>Humans</subject><subject>Lung - cytology</subject><subject>Mice</subject><subject>Mink</subject><subject>Models, Molecular</subject><subject>Proline - metabolism</subject><subject>Radioligand Assay</subject><subject>Recombinant Proteins - antagonists & inhibitors</subject><subject>Recombinant Proteins - genetics</subject><subject>Recombinant Proteins - metabolism</subject><subject>Thymidine - metabolism</subject><subject>Transforming Growth Factor beta - antagonists & inhibitors</subject><subject>Transforming Growth Factor beta - genetics</subject><subject>Transforming Growth Factor beta - metabolism</subject><subject>Transforming Growth Factor beta - pharmacology</subject><subject>Transforming Growth Factor beta1</subject><subject>Triterpenes - pharmacology</subject><subject>Ursolic Acid</subject><issn>0014-5793</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo1j01LAzEYhHNQ2lr7FyRHBQPJJtkkRyluKxS8rOfybj7WSPeDJCL-exdUGJh5GBiYK7ShlAkileFrdJPzB11YM7NCayaZULrWG9S8pTxdosVgo3vEMC4q0E9jzAWHKeGSYMxLGOLY4z5NX-UdB7Blqe7bQ_NAOl-A3aLrAJfsd3--RW3z3O6P5PR6eNk_ncgshSYG6s4LW3ETPA9GcOpULYSjwdCgdMVFsI4bVwWtvJWu0mAttZRrLTopKN-iu9_Z-bMbvDvPKQ6Qvs__f_gPhYxFJg</recordid><startdate>20040521</startdate><enddate>20040521</enddate><creator>Murakami, Shigeru</creator><creator>Takashima, Hajime</creator><creator>Sato-Watanabe, Mariko</creator><creator>Chonan, Sumi</creator><creator>Yamamoto, Koji</creator><creator>Saitoh, Masako</creator><creator>Saito, Shiuji</creator><creator>Yoshimura, Hiromitsu</creator><creator>Sugawara, Koko</creator><creator>Yang, Junshan</creator><creator>Gao, Nannan</creator><creator>Zhang, Xinggao</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>20040521</creationdate><title>Ursolic acid, an antagonist for transforming growth factor (TGF)-beta1</title><author>Murakami, Shigeru ; Takashima, Hajime ; Sato-Watanabe, Mariko ; Chonan, Sumi ; Yamamoto, Koji ; Saitoh, Masako ; Saito, Shiuji ; Yoshimura, Hiromitsu ; Sugawara, Koko ; Yang, Junshan ; Gao, Nannan ; Zhang, Xinggao</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p548-9a6be4c239fe3f9430d7644d0f90f78234fcd39d2f87ec5d28acc0c03884b5403</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Animals</topic><topic>BALB 3T3 Cells</topic><topic>Cell Division - drug effects</topic><topic>Cells, Cultured</topic><topic>Collagen Type I - biosynthesis</topic><topic>Dose-Response Relationship, Drug</topic><topic>Epithelial Cells - cytology</topic><topic>Epithelial Cells - metabolism</topic><topic>Fibroblasts - metabolism</topic><topic>Humans</topic><topic>Lung - cytology</topic><topic>Mice</topic><topic>Mink</topic><topic>Models, Molecular</topic><topic>Proline - metabolism</topic><topic>Radioligand Assay</topic><topic>Recombinant Proteins - antagonists & inhibitors</topic><topic>Recombinant Proteins - genetics</topic><topic>Recombinant Proteins - metabolism</topic><topic>Thymidine - metabolism</topic><topic>Transforming Growth Factor beta - antagonists & inhibitors</topic><topic>Transforming Growth Factor beta - genetics</topic><topic>Transforming Growth Factor beta - metabolism</topic><topic>Transforming Growth Factor beta - pharmacology</topic><topic>Transforming Growth Factor beta1</topic><topic>Triterpenes - pharmacology</topic><topic>Ursolic Acid</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Murakami, Shigeru</creatorcontrib><creatorcontrib>Takashima, Hajime</creatorcontrib><creatorcontrib>Sato-Watanabe, Mariko</creatorcontrib><creatorcontrib>Chonan, Sumi</creatorcontrib><creatorcontrib>Yamamoto, Koji</creatorcontrib><creatorcontrib>Saitoh, Masako</creatorcontrib><creatorcontrib>Saito, Shiuji</creatorcontrib><creatorcontrib>Yoshimura, Hiromitsu</creatorcontrib><creatorcontrib>Sugawara, Koko</creatorcontrib><creatorcontrib>Yang, Junshan</creatorcontrib><creatorcontrib>Gao, Nannan</creatorcontrib><creatorcontrib>Zhang, Xinggao</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>FEBS letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Murakami, Shigeru</au><au>Takashima, Hajime</au><au>Sato-Watanabe, Mariko</au><au>Chonan, Sumi</au><au>Yamamoto, Koji</au><au>Saitoh, Masako</au><au>Saito, Shiuji</au><au>Yoshimura, Hiromitsu</au><au>Sugawara, Koko</au><au>Yang, Junshan</au><au>Gao, Nannan</au><au>Zhang, Xinggao</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Ursolic acid, an antagonist for transforming growth factor (TGF)-beta1</atitle><jtitle>FEBS letters</jtitle><addtitle>FEBS Lett</addtitle><date>2004-05-21</date><risdate>2004</risdate><volume>566</volume><issue>1-3</issue><spage>55</spage><pages>55-</pages><issn>0014-5793</issn><abstract>Transforming growth factor-beta (TGF-beta), a multifunctional cytokine which is involved in extracellular matrix modulation, has a major role in the pathogenesis and progression of fibrotic diseases. We now report the effects of ursolic acid on TGF-beta1 receptor binding and TGF-beta1-induced cellular functions in vitro. Ursolic acid inhibited [(125)I]-TGF-beta1 receptor binding to Balb/c 3T3 mouse fibroblasts with an IC(50) value of 6.9+/-0.8 microM. Ursolic acid dose-dependently recovered reduced proliferation of Minc Mv1Lu cells in the presence of 5 nM of TGF-beta1 and attenuated TGF-beta1-induced collagen synthesis and production in human fibroblasts. Molecular dynamics simulations suggest that ursolic acid may interact with the hydrophobic region of the dimeric interface and thereby inhibit the binding of TGF-beta1 to its receptor. All these findings taken together show that ursolic acid functions as an antagonist for TGF-beta1. This is the first report to show that a small molecule can inhibit TGF-beta1 receptor binding and influence functions of TGF-beta1.</abstract><cop>England</cop><pmid>15147868</pmid></addata></record> |
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| source | Wiley Free Content; MEDLINE; Wiley Online Library Journals Frontfile Complete; Elsevier ScienceDirect Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Alma/SFX Local Collection |
| subjects | Animals BALB 3T3 Cells Cell Division - drug effects Cells, Cultured Collagen Type I - biosynthesis Dose-Response Relationship, Drug Epithelial Cells - cytology Epithelial Cells - metabolism Fibroblasts - metabolism Humans Lung - cytology Mice Mink Models, Molecular Proline - metabolism Radioligand Assay Recombinant Proteins - antagonists & inhibitors Recombinant Proteins - genetics Recombinant Proteins - metabolism Thymidine - metabolism Transforming Growth Factor beta - antagonists & inhibitors Transforming Growth Factor beta - genetics Transforming Growth Factor beta - metabolism Transforming Growth Factor beta - pharmacology Transforming Growth Factor beta1 Triterpenes - pharmacology Ursolic Acid |
| title | Ursolic acid, an antagonist for transforming growth factor (TGF)-beta1 |
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