Inhibitory effects of genistein and resveratrol on guinea pig gallbladder contractility in vitro
AIM： To observe and compare the effects of phytoestrogen genistein, resveratrol and 17β-estradiol on the tonic contraction and the phasic contraction of isolated gallbladder muscle strips and to study the underlying mechanisms. METHODS： Isolated strips of gallbladder muscle from guinea pigs were sus...
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| Veröffentlicht in: | World journal of gastroenterology : WJG 2008-08, Vol.14 (31), p.4955-4960 |
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| creator | Wang, Long-De Qiu, Xiao-Qing Tian, Zhi-Feng Zhang, Ying-Fu Li, Hong-Fang |
| description | AIM： To observe and compare the effects of phytoestrogen genistein, resveratrol and 17β-estradiol on the tonic contraction and the phasic contraction of isolated gallbladder muscle strips and to study the underlying mechanisms. METHODS： Isolated strips of gallbladder muscle from guinea pigs were suspended in organ baths containing Kreb＇s solution, and the contractilities of strips were measured before and after incubation with genistein, resveratrol and 17β-estradiol respectively. RESULTS： Similar to 17β-estradiol, genistein and resveratrol could dose-dependently inhibit the phasic contractile activities, they decreased the mean contractile amplitude and the contractile frequencies of gallbladder muscle strips, and also produced a marked reduction in resting tone. The blocker of estrogen receptor ICI 182780 failed to alter the inhibitory effects induced by genistein and resveratrol, but potassium bisperoxo （1, 10 phenanthroline） oxovanadate bpV （phen）, a potent protein tyrosine phosphatase inhibitor, markedly attenuated the inhibitory effects induced by genistein and resveratrol. In calcium-free Kreb＇s solution containing 0.01 mmol/L egtazic acid （EGTA）, genistein and resveratrol inhibited the first phasic contraction induced by acetylcholine （ACh）, but did not affect the second contraction induced by CaCl2. In addition, genistein, resveratrol and 17β-estradiol also could reduce the contractile responses of ACh and KCl, and shift their cumulative concentration-response curves rightward. CONCLUSION： Phytoestrogen genistein and resveratrol can directly inhibit the contractile activity of isolated gallbladder muscle both at rest and in response to stimulation. The mechanisms responsible for the inhibitory effects probably due mainly to inhibition of tyrosine kinase, Ca^2＋ influx through potential-dependent calcium channels （PDCs） and Ca^2＋ release from sarcoplasmic reticulum （SR）, but were not related to the estrogen receptors. |
| doi_str_mv | 10.3748/wjg.14.4955 |
| format | Article |
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METHODS： Isolated strips of gallbladder muscle from guinea pigs were suspended in organ baths containing Kreb＇s solution, and the contractilities of strips were measured before and after incubation with genistein, resveratrol and 17β-estradiol respectively. RESULTS： Similar to 17β-estradiol, genistein and resveratrol could dose-dependently inhibit the phasic contractile activities, they decreased the mean contractile amplitude and the contractile frequencies of gallbladder muscle strips, and also produced a marked reduction in resting tone. The blocker of estrogen receptor ICI 182780 failed to alter the inhibitory effects induced by genistein and resveratrol, but potassium bisperoxo （1, 10 phenanthroline） oxovanadate bpV （phen）, a potent protein tyrosine phosphatase inhibitor, markedly attenuated the inhibitory effects induced by genistein and resveratrol. In calcium-free Kreb＇s solution containing 0.01 mmol/L egtazic acid （EGTA）, genistein and resveratrol inhibited the first phasic contraction induced by acetylcholine （ACh）, but did not affect the second contraction induced by CaCl2. In addition, genistein, resveratrol and 17β-estradiol also could reduce the contractile responses of ACh and KCl, and shift their cumulative concentration-response curves rightward. CONCLUSION： Phytoestrogen genistein and resveratrol can directly inhibit the contractile activity of isolated gallbladder muscle both at rest and in response to stimulation. The mechanisms responsible for the inhibitory effects probably due mainly to inhibition of tyrosine kinase, Ca^2＋ influx through potential-dependent calcium channels （PDCs） and Ca^2＋ release from sarcoplasmic reticulum （SR）, but were not related to the estrogen receptors.</description><identifier>ISSN: 1007-9327</identifier><identifier>EISSN: 2219-2840</identifier><identifier>DOI: 10.3748/wjg.14.4955</identifier><identifier>PMID: 18756606</identifier><language>eng</language><publisher>United States: Affiliated Hospital,Gansu Chinese Medical College,Lanzhou 730020,Gansu Province,China%Functional Lab of Medicine,Lanzhou University,Lanzhou 730000,Gansu Province,China%Department of Physiology,College of Basic Medicine,Lanzhou University,Key Laboratory of Pre-clinical Study for New Drugs of Gansu Province,Lanzhou 730000,Gansu Province,China</publisher><subject>Acetylcholine - pharmacology ; Animals ; Calcium Chloride - pharmacology ; Dose-Response Relationship, Drug ; Enzyme Inhibitors - pharmacology ; Estradiol - analogs & derivatives ; Estradiol - pharmacology ; Estrogen Antagonists - pharmacology ; Female ; Fulvestrant ; Gallbladder - drug effects ; Gallbladder - enzymology ; Genistein - pharmacology ; Guinea Pigs ; In Vitro Techniques ; Male ; Muscle Contraction - drug effects ; Muscle, Smooth - drug effects ; Muscle, Smooth - enzymology ; Organometallic Compounds - pharmacology ; Phenanthrolines - pharmacology ; Phytoestrogens - pharmacology ; Potassium Chloride - pharmacology ; Protein Tyrosine Phosphatases - antagonists & inhibitors ; Protein Tyrosine Phosphatases - metabolism ; Rapid Communication ; Resveratrol ; Stilbenes - pharmacology ; 平滑肌 ; 收缩性 ; 胆囊疾病 ; 雌二醇</subject><ispartof>World journal of gastroenterology : WJG, 2008-08, Vol.14 (31), p.4955-4960</ispartof><rights>Copyright © Wanfang Data Co. Ltd. All Rights Reserved.</rights><rights>2008 The WJG Press and Baishideng. All rights reserved. 2008</rights><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c435t-f11354d2713b584c4882222bb4f6bf9962ccaa8e67ebf33bb42301ae77a0e8953</citedby><cites>FETCH-LOGICAL-c435t-f11354d2713b584c4882222bb4f6bf9962ccaa8e67ebf33bb42301ae77a0e8953</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Uhttp://image.cqvip.com/vip1000/qk/84123X/84123X.jpg</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2739951/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2739951/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18756606$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Wang, Long-De</creatorcontrib><creatorcontrib>Qiu, Xiao-Qing</creatorcontrib><creatorcontrib>Tian, Zhi-Feng</creatorcontrib><creatorcontrib>Zhang, Ying-Fu</creatorcontrib><creatorcontrib>Li, Hong-Fang</creatorcontrib><title>Inhibitory effects of genistein and resveratrol on guinea pig gallbladder contractility in vitro</title><title>World journal of gastroenterology : WJG</title><addtitle>World Journal of Gastroenterology</addtitle><description>AIM： To observe and compare the effects of phytoestrogen genistein, resveratrol and 17β-estradiol on the tonic contraction and the phasic contraction of isolated gallbladder muscle strips and to study the underlying mechanisms. METHODS： Isolated strips of gallbladder muscle from guinea pigs were suspended in organ baths containing Kreb＇s solution, and the contractilities of strips were measured before and after incubation with genistein, resveratrol and 17β-estradiol respectively. RESULTS： Similar to 17β-estradiol, genistein and resveratrol could dose-dependently inhibit the phasic contractile activities, they decreased the mean contractile amplitude and the contractile frequencies of gallbladder muscle strips, and also produced a marked reduction in resting tone. The blocker of estrogen receptor ICI 182780 failed to alter the inhibitory effects induced by genistein and resveratrol, but potassium bisperoxo （1, 10 phenanthroline） oxovanadate bpV （phen）, a potent protein tyrosine phosphatase inhibitor, markedly attenuated the inhibitory effects induced by genistein and resveratrol. In calcium-free Kreb＇s solution containing 0.01 mmol/L egtazic acid （EGTA）, genistein and resveratrol inhibited the first phasic contraction induced by acetylcholine （ACh）, but did not affect the second contraction induced by CaCl2. In addition, genistein, resveratrol and 17β-estradiol also could reduce the contractile responses of ACh and KCl, and shift their cumulative concentration-response curves rightward. CONCLUSION： Phytoestrogen genistein and resveratrol can directly inhibit the contractile activity of isolated gallbladder muscle both at rest and in response to stimulation. The mechanisms responsible for the inhibitory effects probably due mainly to inhibition of tyrosine kinase, Ca^2＋ influx through potential-dependent calcium channels （PDCs） and Ca^2＋ release from sarcoplasmic reticulum （SR）, but were not related to the estrogen receptors.</description><subject>Acetylcholine - pharmacology</subject><subject>Animals</subject><subject>Calcium Chloride - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Estradiol - analogs & derivatives</subject><subject>Estradiol - pharmacology</subject><subject>Estrogen Antagonists - pharmacology</subject><subject>Female</subject><subject>Fulvestrant</subject><subject>Gallbladder - drug effects</subject><subject>Gallbladder - enzymology</subject><subject>Genistein - pharmacology</subject><subject>Guinea Pigs</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Muscle Contraction - drug effects</subject><subject>Muscle, Smooth - drug effects</subject><subject>Muscle, Smooth - enzymology</subject><subject>Organometallic Compounds - pharmacology</subject><subject>Phenanthrolines - pharmacology</subject><subject>Phytoestrogens - pharmacology</subject><subject>Potassium Chloride - pharmacology</subject><subject>Protein Tyrosine Phosphatases - antagonists & inhibitors</subject><subject>Protein Tyrosine Phosphatases - metabolism</subject><subject>Rapid Communication</subject><subject>Resveratrol</subject><subject>Stilbenes - pharmacology</subject><subject>平滑肌</subject><subject>收缩性</subject><subject>胆囊疾病</subject><subject>雌二醇</subject><issn>1007-9327</issn><issn>2219-2840</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpVkc1vEzEQxS0EoqH0xB1ZiBva1J9r7wUJVVAqVeqlnF3bO944bO3g3aTKf19HiSj4MpLnN2-e5iH0gZIlV0JfPq2HJRVL0Un5Ci0Yo13DtCCv0YISopqOM3WG3k3TmhDGuWRv0RnVSrYtaRfo4SatootzLnsMIYCfJ5wDHiDFaYaYsE09LjDtoNi55BHnhIdtTGDxJg54sOPoRtv3ULDPaS7Wz3GM8x7X0V2sE-_Rm2DHCS5O9Rz9-vH9_upnc3t3fXP17bbxgsu5CZRyKXqmKHdSCy-0ZvU5J0LrQte1zHtrNbQKXOC8_jNOqAWlLAHdSX6Ovh51N1v3CL2Hg5nRbEp8tGVvso3m_06KKzPknWGKd52kVeDzUeDJpmDTYNZ5W1K1bOqBGSGaU0Lbin05Yr7kaSoQ_q6gxBzyOOCGCnPIo9If_3X1wp4CqMCnk9wqp-FPrHud9b9DHMEwzbkQVPJncbeUEg</recordid><startdate>20080821</startdate><enddate>20080821</enddate><creator>Wang, Long-De</creator><creator>Qiu, Xiao-Qing</creator><creator>Tian, Zhi-Feng</creator><creator>Zhang, Ying-Fu</creator><creator>Li, Hong-Fang</creator><general>Affiliated Hospital,Gansu Chinese Medical College,Lanzhou 730020,Gansu Province,China%Functional Lab of Medicine,Lanzhou University,Lanzhou 730000,Gansu Province,China%Department of Physiology,College of Basic Medicine,Lanzhou University,Key Laboratory of Pre-clinical Study for New Drugs of Gansu Province,Lanzhou 730000,Gansu Province,China</general><general>The WJG Press and Baishideng</general><scope>2RA</scope><scope>92L</scope><scope>CQIGP</scope><scope>W91</scope><scope>~WA</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>2B.</scope><scope>4A8</scope><scope>92I</scope><scope>93N</scope><scope>PSX</scope><scope>TCJ</scope><scope>5PM</scope></search><sort><creationdate>20080821</creationdate><title>Inhibitory effects of genistein and resveratrol on guinea pig gallbladder contractility in vitro</title><author>Wang, Long-De ; 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METHODS： Isolated strips of gallbladder muscle from guinea pigs were suspended in organ baths containing Kreb＇s solution, and the contractilities of strips were measured before and after incubation with genistein, resveratrol and 17β-estradiol respectively. RESULTS： Similar to 17β-estradiol, genistein and resveratrol could dose-dependently inhibit the phasic contractile activities, they decreased the mean contractile amplitude and the contractile frequencies of gallbladder muscle strips, and also produced a marked reduction in resting tone. The blocker of estrogen receptor ICI 182780 failed to alter the inhibitory effects induced by genistein and resveratrol, but potassium bisperoxo （1, 10 phenanthroline） oxovanadate bpV （phen）, a potent protein tyrosine phosphatase inhibitor, markedly attenuated the inhibitory effects induced by genistein and resveratrol. In calcium-free Kreb＇s solution containing 0.01 mmol/L egtazic acid （EGTA）, genistein and resveratrol inhibited the first phasic contraction induced by acetylcholine （ACh）, but did not affect the second contraction induced by CaCl2. In addition, genistein, resveratrol and 17β-estradiol also could reduce the contractile responses of ACh and KCl, and shift their cumulative concentration-response curves rightward. CONCLUSION： Phytoestrogen genistein and resveratrol can directly inhibit the contractile activity of isolated gallbladder muscle both at rest and in response to stimulation. The mechanisms responsible for the inhibitory effects probably due mainly to inhibition of tyrosine kinase, Ca^2＋ influx through potential-dependent calcium channels （PDCs） and Ca^2＋ release from sarcoplasmic reticulum （SR）, but were not related to the estrogen receptors.</abstract><cop>United States</cop><pub>Affiliated Hospital,Gansu Chinese Medical College,Lanzhou 730020,Gansu Province,China%Functional Lab of Medicine,Lanzhou University,Lanzhou 730000,Gansu Province,China%Department of Physiology,College of Basic Medicine,Lanzhou University,Key Laboratory of Pre-clinical Study for New Drugs of Gansu Province,Lanzhou 730000,Gansu Province,China</pub><pmid>18756606</pmid><doi>10.3748/wjg.14.4955</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| identifier | ISSN: 1007-9327 |
| ispartof | World journal of gastroenterology : WJG, 2008-08, Vol.14 (31), p.4955-4960 |
| issn | 1007-9327 2219-2840 |
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| source | MEDLINE; Baishideng "World Journal of" online journals; PubMed Central; Alma/SFX Local Collection; EZB Electronic Journals Library |
| subjects | Acetylcholine - pharmacology Animals Calcium Chloride - pharmacology Dose-Response Relationship, Drug Enzyme Inhibitors - pharmacology Estradiol - analogs & derivatives Estradiol - pharmacology Estrogen Antagonists - pharmacology Female Fulvestrant Gallbladder - drug effects Gallbladder - enzymology Genistein - pharmacology Guinea Pigs In Vitro Techniques Male Muscle Contraction - drug effects Muscle, Smooth - drug effects Muscle, Smooth - enzymology Organometallic Compounds - pharmacology Phenanthrolines - pharmacology Phytoestrogens - pharmacology Potassium Chloride - pharmacology Protein Tyrosine Phosphatases - antagonists & inhibitors Protein Tyrosine Phosphatases - metabolism Rapid Communication Resveratrol Stilbenes - pharmacology 平滑肌 收缩性 胆囊疾病 雌二醇 |
| title | Inhibitory effects of genistein and resveratrol on guinea pig gallbladder contractility in vitro |
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