Antispasmodic effects of the essential oil of Croton nepetaefolius on guinea-pig ileum: a myogenic activity

The effects of essential oil of Croton nepetaefolius (EOCN) on guinea‐pig‐isolated ileum were studied. We previously demonstrated that EOCN induced reversible relaxation of ileal tone artificially increased by high [K+] nutrient solution. This study aimed to elucidate whether these effects were caus...

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Veröffentlicht in:Fundamental & clinical pharmacology 2004-10, Vol.18 (5), p.539-546
Hauptverfasser: Magalhães, Pedro Jorge Caldas, Lahlou, Saad, Leal-Cardoso, José Henrique
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creator Magalhães, Pedro Jorge Caldas
Lahlou, Saad
Leal-Cardoso, José Henrique
description The effects of essential oil of Croton nepetaefolius (EOCN) on guinea‐pig‐isolated ileum were studied. We previously demonstrated that EOCN induced reversible relaxation of ileal tone artificially increased by high [K+] nutrient solution. This study aimed to elucidate whether these effects were caused by indirect, neural, or primarily by myogenic effect. EOCN (40 μg/mL) induced a relaxation of basal tone corresponding to approximately 38% of the reference contraction (K+ 60 mm), and was unaltered by 0.5 mm hexamethonium, 0.5 μm tetrodotoxin, 1 μm indomethacin, and 100 μml‐nitroarginine methyl ester (l‐NAME). Epinephrine‐ (100 μm) and EOCN‐induced maximal relaxation of ileum pre‐contracted with 60 mm KCl represented 16.8 ± 2.3% (n = 10) and 95.0 ± 6.4% (n = 6) of KCl‐induced contraction, respectively. EOCN (200 μg/mL) had no effect on the transmembrane resting potential (Em) of ileum in nutrient solutions with normal (5 mm) and high (80 mm) [K+]. EOCN similarly inhibited the contractions induced by KCl, acetylcholine (ACh) and histamine (IC50 values of approximately 18, 28 and 21 μg/mL, respectively). EOCN also inhibited both the nifedipine‐insensitive component of ACh‐induced contraction and the contraction induced by ACh in Ca2+‐free solution. EOCN accelerated the reversal of a KCl‐induced tonic contraction upon withdrawal of Ca2+ from the extracellular medium. Our results suggest that EOCN induces relaxation of guinea‐pig ileum by a direct action on smooth muscle via a mechanism largely independent of alterations of Em and Ca2+ influx, possibly at the level of the contractile apparatus.
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We previously demonstrated that EOCN induced reversible relaxation of ileal tone artificially increased by high [K+] nutrient solution. This study aimed to elucidate whether these effects were caused by indirect, neural, or primarily by myogenic effect. EOCN (40 μg/mL) induced a relaxation of basal tone corresponding to approximately 38% of the reference contraction (K+ 60 mm), and was unaltered by 0.5 mm hexamethonium, 0.5 μm tetrodotoxin, 1 μm indomethacin, and 100 μml‐nitroarginine methyl ester (l‐NAME). Epinephrine‐ (100 μm) and EOCN‐induced maximal relaxation of ileum pre‐contracted with 60 mm KCl represented 16.8 ± 2.3% (n = 10) and 95.0 ± 6.4% (n = 6) of KCl‐induced contraction, respectively. EOCN (200 μg/mL) had no effect on the transmembrane resting potential (Em) of ileum in nutrient solutions with normal (5 mm) and high (80 mm) [K+]. EOCN similarly inhibited the contractions induced by KCl, acetylcholine (ACh) and histamine (IC50 values of approximately 18, 28 and 21 μg/mL, respectively). EOCN also inhibited both the nifedipine‐insensitive component of ACh‐induced contraction and the contraction induced by ACh in Ca2+‐free solution. EOCN accelerated the reversal of a KCl‐induced tonic contraction upon withdrawal of Ca2+ from the extracellular medium. 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We previously demonstrated that EOCN induced reversible relaxation of ileal tone artificially increased by high [K+] nutrient solution. This study aimed to elucidate whether these effects were caused by indirect, neural, or primarily by myogenic effect. EOCN (40 μg/mL) induced a relaxation of basal tone corresponding to approximately 38% of the reference contraction (K+ 60 mm), and was unaltered by 0.5 mm hexamethonium, 0.5 μm tetrodotoxin, 1 μm indomethacin, and 100 μml‐nitroarginine methyl ester (l‐NAME). Epinephrine‐ (100 μm) and EOCN‐induced maximal relaxation of ileum pre‐contracted with 60 mm KCl represented 16.8 ± 2.3% (n = 10) and 95.0 ± 6.4% (n = 6) of KCl‐induced contraction, respectively. EOCN (200 μg/mL) had no effect on the transmembrane resting potential (Em) of ileum in nutrient solutions with normal (5 mm) and high (80 mm) [K+]. EOCN similarly inhibited the contractions induced by KCl, acetylcholine (ACh) and histamine (IC50 values of approximately 18, 28 and 21 μg/mL, respectively). EOCN also inhibited both the nifedipine‐insensitive component of ACh‐induced contraction and the contraction induced by ACh in Ca2+‐free solution. EOCN accelerated the reversal of a KCl‐induced tonic contraction upon withdrawal of Ca2+ from the extracellular medium. Our results suggest that EOCN induces relaxation of guinea‐pig ileum by a direct action on smooth muscle via a mechanism largely independent of alterations of Em and Ca2+ influx, possibly at the level of the contractile apparatus.</description><subject>Acetylcholine - pharmacology</subject><subject>Animals</subject><subject>antispasmodic</subject><subject>Biological and medical sciences</subject><subject>Calcium - metabolism</subject><subject>Croton - chemistry</subject><subject>Croton nepetaefolius</subject><subject>Epinephrine - pharmacology</subject><subject>essential oil</subject><subject>General pharmacology</subject><subject>Guinea Pigs</subject><subject>Histamine - pharmacology</subject><subject>ileum</subject><subject>Ileum - drug effects</subject><subject>Ileum - physiology</subject><subject>In Vitro Techniques</subject><subject>Isometric Contraction - drug effects</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Membrane Potentials - drug effects</subject><subject>Muscle, Smooth - drug effects</subject><subject>Muscle, Smooth - physiology</subject><subject>Oils, Volatile - pharmacology</subject><subject>Parasympatholytics - pharmacology</subject><subject>Pharmacognosy. Homeopathy. Health food</subject><subject>Pharmacology. Drug treatments</subject><subject>Potassium - metabolism</subject><subject>Potassium Chloride - pharmacology</subject><subject>relaxation</subject><subject>smooth muscle</subject><subject>Vasoconstrictor Agents - pharmacology</subject><subject>Vasodilator Agents - pharmacology</subject><issn>0767-3981</issn><issn>1472-8206</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkE2P0zAQhi0EYsvCX0C-wC3Bjh07QVxWFdtFlC8JBDdr4kyKu0kc4gTaf49Dq90rvtjyPO_M6CGEcpbyeF7tUy51lhQZU2nGmEwZy7RKDw_I6q7wkKyYVjoRZcEvyJMQ9oxxzbh6TC54LotM6HxFbq_6yYUBQudrZyk2DdopUN_Q6SdSDAFjHVrqXbt8rkc_-Z72OOAE2PjWzRHu6W52PUIyuB11Lc7dawq0O_od9rEp2Mn9dtPxKXnUQBvw2fm-JN-u335d3yTbT5t366ttYuNWKrEoeA1lUYEAVSi0gtVVZYtSIJOVbgrWyByYlEUprZA5y-o8YyJTDBTmFsQleXnqO4z-14xhMp0LFtsWevRzMEqVmktRRrA4gXb0IYzYmGF0HYxHw5lZRJu9WXyaxadZRJt_os0hRp-fZ8xVh_V98Gw2Ai_OAAQLbTNCb1245xQvFVcycm9O3J8o7vjfC5jr9ef4iPHkFHdhwsNdHMZbo3Tcw3z_uDH65oPY_ti8N1_EX_W_qQA</recordid><startdate>200410</startdate><enddate>200410</enddate><creator>Magalhães, Pedro Jorge Caldas</creator><creator>Lahlou, Saad</creator><creator>Leal-Cardoso, José Henrique</creator><general>Blackwell Science Ltd</general><general>Blackwell</general><scope>BSCLL</scope><scope>IQODW</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>7X8</scope></search><sort><creationdate>200410</creationdate><title>Antispasmodic effects of the essential oil of Croton nepetaefolius on guinea-pig ileum: a myogenic activity</title><author>Magalhães, Pedro Jorge Caldas ; Lahlou, Saad ; Leal-Cardoso, José Henrique</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4826-ce31da98ba3a686ec30dbbc893e04b7f80f45a044894c34502d5203260a6e5ca3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Acetylcholine - pharmacology</topic><topic>Animals</topic><topic>antispasmodic</topic><topic>Biological and medical sciences</topic><topic>Calcium - metabolism</topic><topic>Croton - chemistry</topic><topic>Croton nepetaefolius</topic><topic>Epinephrine - pharmacology</topic><topic>essential oil</topic><topic>General pharmacology</topic><topic>Guinea Pigs</topic><topic>Histamine - pharmacology</topic><topic>ileum</topic><topic>Ileum - drug effects</topic><topic>Ileum - physiology</topic><topic>In Vitro Techniques</topic><topic>Isometric Contraction - drug effects</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Membrane Potentials - drug effects</topic><topic>Muscle, Smooth - drug effects</topic><topic>Muscle, Smooth - physiology</topic><topic>Oils, Volatile - pharmacology</topic><topic>Parasympatholytics - pharmacology</topic><topic>Pharmacognosy. Homeopathy. Health food</topic><topic>Pharmacology. Drug treatments</topic><topic>Potassium - metabolism</topic><topic>Potassium Chloride - pharmacology</topic><topic>relaxation</topic><topic>smooth muscle</topic><topic>Vasoconstrictor Agents - pharmacology</topic><topic>Vasodilator Agents - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Magalhães, Pedro Jorge Caldas</creatorcontrib><creatorcontrib>Lahlou, Saad</creatorcontrib><creatorcontrib>Leal-Cardoso, José Henrique</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Fundamental &amp; clinical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Magalhães, Pedro Jorge Caldas</au><au>Lahlou, Saad</au><au>Leal-Cardoso, José Henrique</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antispasmodic effects of the essential oil of Croton nepetaefolius on guinea-pig ileum: a myogenic activity</atitle><jtitle>Fundamental &amp; clinical pharmacology</jtitle><addtitle>Fundam Clin Pharmacol</addtitle><date>2004-10</date><risdate>2004</risdate><volume>18</volume><issue>5</issue><spage>539</spage><epage>546</epage><pages>539-546</pages><issn>0767-3981</issn><eissn>1472-8206</eissn><coden>FCPHEZ</coden><abstract>The effects of essential oil of Croton nepetaefolius (EOCN) on guinea‐pig‐isolated ileum were studied. We previously demonstrated that EOCN induced reversible relaxation of ileal tone artificially increased by high [K+] nutrient solution. This study aimed to elucidate whether these effects were caused by indirect, neural, or primarily by myogenic effect. EOCN (40 μg/mL) induced a relaxation of basal tone corresponding to approximately 38% of the reference contraction (K+ 60 mm), and was unaltered by 0.5 mm hexamethonium, 0.5 μm tetrodotoxin, 1 μm indomethacin, and 100 μml‐nitroarginine methyl ester (l‐NAME). Epinephrine‐ (100 μm) and EOCN‐induced maximal relaxation of ileum pre‐contracted with 60 mm KCl represented 16.8 ± 2.3% (n = 10) and 95.0 ± 6.4% (n = 6) of KCl‐induced contraction, respectively. EOCN (200 μg/mL) had no effect on the transmembrane resting potential (Em) of ileum in nutrient solutions with normal (5 mm) and high (80 mm) [K+]. EOCN similarly inhibited the contractions induced by KCl, acetylcholine (ACh) and histamine (IC50 values of approximately 18, 28 and 21 μg/mL, respectively). EOCN also inhibited both the nifedipine‐insensitive component of ACh‐induced contraction and the contraction induced by ACh in Ca2+‐free solution. EOCN accelerated the reversal of a KCl‐induced tonic contraction upon withdrawal of Ca2+ from the extracellular medium. Our results suggest that EOCN induces relaxation of guinea‐pig ileum by a direct action on smooth muscle via a mechanism largely independent of alterations of Em and Ca2+ influx, possibly at the level of the contractile apparatus.</abstract><cop>Oxford, UK</cop><pub>Blackwell Science Ltd</pub><pmid>15482375</pmid><doi>10.1111/j.1472-8206.2004.00276.x</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record>
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subjects Acetylcholine - pharmacology
Animals
antispasmodic
Biological and medical sciences
Calcium - metabolism
Croton - chemistry
Croton nepetaefolius
Epinephrine - pharmacology
essential oil
General pharmacology
Guinea Pigs
Histamine - pharmacology
ileum
Ileum - drug effects
Ileum - physiology
In Vitro Techniques
Isometric Contraction - drug effects
Male
Medical sciences
Membrane Potentials - drug effects
Muscle, Smooth - drug effects
Muscle, Smooth - physiology
Oils, Volatile - pharmacology
Parasympatholytics - pharmacology
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Potassium - metabolism
Potassium Chloride - pharmacology
relaxation
smooth muscle
Vasoconstrictor Agents - pharmacology
Vasodilator Agents - pharmacology
title Antispasmodic effects of the essential oil of Croton nepetaefolius on guinea-pig ileum: a myogenic activity
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