ANTHELMINTIC ACTIVITY OF DIOXAPYRROLOMYCIN
Dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 produced by UC 11065 were evaluated as anthelmintics. Assays used to examine these compounds included effects on the free-living nematode Caenorhabditis elegans, ability to clear target nematodes (Haemonchus contortus and Trichostr...
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| Veröffentlicht in: | Journal of antibiotics 1992/06/25, Vol.45(6), pp.977-983 |
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| creator | CONDER, GEORGE A. ZIELINSKI, RAYMOND J. JOHNSON, SANDRA S. KUO, MING-SHANG T. COX, DEBBIE L. MARSHALL, VINCENT P. HABER, CHRISTOPHER L. DIROMA, PETER J. NELSON, STEPHEN J. CONKLIN, RICHARD D. LEE, B. LAMAR GEARY, TIMOTHY G. ROTHWELL, J. T. SANGSTER, N. C. |
| description | Dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 produced by UC 11065 were evaluated as anthelmintics. Assays used to examine these compounds included effects on the free-living nematode Caenorhabditis elegans, ability to clear target nematodes (Haemonchus contortus and Trichostrongylus colubriformis) from jirds, and clearance of Haemonchus contortus from lambs. A crude extract of UC 11065 containing dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 was active against C. elegans and against H. contortus in the jird. Purified and/or synthetic samples of dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 were tested in the jird model; only dioxapyrrolomycin exhibited appreciable activity against H. contortus ( ≥ 90.9% clearance at 0.33 mg/jird), while none of the compounds showed appreciable activity against T. colubriformis. Dioxapyrrolomycin cleared 99.9% of H. contortus from lambs at 12.5 mg/kg. An in vitro migration study using susceptible and closantel-resistant H. contortus showed there is cross-resistance between dioxapyrrolomycin and closantel. Dioxapyrrolomycin appears to be a narrow-spectrum anthelmintic which works through a closantel-like mode-of-action. |
| doi_str_mv | 10.7164/antibiotics.45.977 |
| format | Article |
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LAMAR ; GEARY, TIMOTHY G. ; ROTHWELL, J. T. ; SANGSTER, N. C.</creator><creatorcontrib>CONDER, GEORGE A. ; ZIELINSKI, RAYMOND J. ; JOHNSON, SANDRA S. ; KUO, MING-SHANG T. ; COX, DEBBIE L. ; MARSHALL, VINCENT P. ; HABER, CHRISTOPHER L. ; DIROMA, PETER J. ; NELSON, STEPHEN J. ; CONKLIN, RICHARD D. ; LEE, B. LAMAR ; GEARY, TIMOTHY G. ; ROTHWELL, J. T. ; SANGSTER, N. C.</creatorcontrib><description>Dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 produced by UC 11065 were evaluated as anthelmintics. Assays used to examine these compounds included effects on the free-living nematode Caenorhabditis elegans, ability to clear target nematodes (Haemonchus contortus and Trichostrongylus colubriformis) from jirds, and clearance of Haemonchus contortus from lambs. A crude extract of UC 11065 containing dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 was active against C. elegans and against H. contortus in the jird. Purified and/or synthetic samples of dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 were tested in the jird model; only dioxapyrrolomycin exhibited appreciable activity against H. contortus ( ≥ 90.9% clearance at 0.33 mg/jird), while none of the compounds showed appreciable activity against T. colubriformis. Dioxapyrrolomycin cleared 99.9% of H. contortus from lambs at 12.5 mg/kg. An in vitro migration study using susceptible and closantel-resistant H. contortus showed there is cross-resistance between dioxapyrrolomycin and closantel. Dioxapyrrolomycin appears to be a narrow-spectrum anthelmintic which works through a closantel-like mode-of-action.</description><identifier>ISSN: 0021-8820</identifier><identifier>EISSN: 1881-1469</identifier><identifier>DOI: 10.7164/antibiotics.45.977</identifier><identifier>PMID: 1500366</identifier><identifier>CODEN: JANTAJ</identifier><language>eng</language><publisher>Tokyo: JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</publisher><subject>Actinomycetales - metabolism ; Animals ; Anthelmintics - isolation & purification ; Anthelmintics - pharmacology ; Anti-Bacterial Agents - isolation & purification ; Anti-Bacterial Agents - pharmacology ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiparasitic agents ; Biological and medical sciences ; Medical sciences ; Pharmacology. Drug treatments ; Pyrroles - isolation & purification ; Pyrroles - pharmacology ; Sheep</subject><ispartof>The Journal of Antibiotics, 1992/06/25, Vol.45(6), pp.977-983</ispartof><rights>Japan Antibiotics Research Association</rights><rights>1992 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c606t-adf95bb347b06b2ee74ea9b5b36386f1fa6b20888bf4c59fab754fc51be7f8993</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1883,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=5517298$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1500366$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>CONDER, GEORGE A.</creatorcontrib><creatorcontrib>ZIELINSKI, RAYMOND J.</creatorcontrib><creatorcontrib>JOHNSON, SANDRA S.</creatorcontrib><creatorcontrib>KUO, MING-SHANG T.</creatorcontrib><creatorcontrib>COX, DEBBIE L.</creatorcontrib><creatorcontrib>MARSHALL, VINCENT P.</creatorcontrib><creatorcontrib>HABER, CHRISTOPHER L.</creatorcontrib><creatorcontrib>DIROMA, PETER J.</creatorcontrib><creatorcontrib>NELSON, STEPHEN J.</creatorcontrib><creatorcontrib>CONKLIN, RICHARD D.</creatorcontrib><creatorcontrib>LEE, B. LAMAR</creatorcontrib><creatorcontrib>GEARY, TIMOTHY G.</creatorcontrib><creatorcontrib>ROTHWELL, J. T.</creatorcontrib><creatorcontrib>SANGSTER, N. C.</creatorcontrib><title>ANTHELMINTIC ACTIVITY OF DIOXAPYRROLOMYCIN</title><title>Journal of antibiotics</title><addtitle>J. Antibiot.</addtitle><description>Dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 produced by UC 11065 were evaluated as anthelmintics. Assays used to examine these compounds included effects on the free-living nematode Caenorhabditis elegans, ability to clear target nematodes (Haemonchus contortus and Trichostrongylus colubriformis) from jirds, and clearance of Haemonchus contortus from lambs. A crude extract of UC 11065 containing dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 was active against C. elegans and against H. contortus in the jird. Purified and/or synthetic samples of dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 were tested in the jird model; only dioxapyrrolomycin exhibited appreciable activity against H. contortus ( ≥ 90.9% clearance at 0.33 mg/jird), while none of the compounds showed appreciable activity against T. colubriformis. Dioxapyrrolomycin cleared 99.9% of H. contortus from lambs at 12.5 mg/kg. An in vitro migration study using susceptible and closantel-resistant H. contortus showed there is cross-resistance between dioxapyrrolomycin and closantel. Dioxapyrrolomycin appears to be a narrow-spectrum anthelmintic which works through a closantel-like mode-of-action.</description><subject>Actinomycetales - metabolism</subject><subject>Animals</subject><subject>Anthelmintics - isolation & purification</subject><subject>Anthelmintics - pharmacology</subject><subject>Anti-Bacterial Agents - isolation & purification</subject><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiparasitic agents</subject><subject>Biological and medical sciences</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyrroles - isolation & purification</subject><subject>Pyrroles - pharmacology</subject><subject>Sheep</subject><issn>0021-8820</issn><issn>1881-1469</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpNkF1PwjAUhhujQUT_gIkJF8YLk2G7rl-XZIIsAjNkGrlq2tLqyPhwHRf-e0dGkJue5rzPOe_JC8Atgj2GaPSk1lWu802VG9-LSE8wdgbaiHMUoIiKc9CGMEQB5yG8BFfeLyHEDDPeAi1E6j-lbfDYn2ajwXiSTLMk7vbjLPlIsnk3HXafk_Sz_zafzdJxOpnHyfQaXDhVeHtzqB3wPhxk8SgYpy9J3B8HhkJaBWrhBNEaR0xDqkNrWWSV0ERjijl1yKm6Cznn2kWGCKc0I5EzBGnLHBcCd8BDs3dbbn521ldylXtji0Kt7WbnJcMICo55DYYNaMqN96V1clvmK1X-SgTlPiB5EpCMiKwDqofuDtt3emUX_yNNIrV-f9CVN6pwpVqb3B8xQhALxd77tcGWvlJf9qirsjYr7KkzEpTv3Wnz1EccKfOtSmnX-A9zu4iw</recordid><startdate>1992</startdate><enddate>1992</enddate><creator>CONDER, GEORGE A.</creator><creator>ZIELINSKI, RAYMOND J.</creator><creator>JOHNSON, SANDRA S.</creator><creator>KUO, MING-SHANG T.</creator><creator>COX, DEBBIE L.</creator><creator>MARSHALL, VINCENT P.</creator><creator>HABER, CHRISTOPHER L.</creator><creator>DIROMA, PETER J.</creator><creator>NELSON, STEPHEN J.</creator><creator>CONKLIN, RICHARD D.</creator><creator>LEE, B. LAMAR</creator><creator>GEARY, TIMOTHY G.</creator><creator>ROTHWELL, J. T.</creator><creator>SANGSTER, N. C.</creator><general>JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</general><general>Japan Antibiotics Research Association</general><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>1992</creationdate><title>ANTHELMINTIC ACTIVITY OF DIOXAPYRROLOMYCIN</title><author>CONDER, GEORGE A. ; ZIELINSKI, RAYMOND J. ; JOHNSON, SANDRA S. ; KUO, MING-SHANG T. ; COX, DEBBIE L. ; MARSHALL, VINCENT P. ; HABER, CHRISTOPHER L. ; DIROMA, PETER J. ; NELSON, STEPHEN J. ; CONKLIN, RICHARD D. ; LEE, B. LAMAR ; GEARY, TIMOTHY G. ; ROTHWELL, J. T. ; SANGSTER, N. 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C.</creatorcontrib><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>Journal of antibiotics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>CONDER, GEORGE A.</au><au>ZIELINSKI, RAYMOND J.</au><au>JOHNSON, SANDRA S.</au><au>KUO, MING-SHANG T.</au><au>COX, DEBBIE L.</au><au>MARSHALL, VINCENT P.</au><au>HABER, CHRISTOPHER L.</au><au>DIROMA, PETER J.</au><au>NELSON, STEPHEN J.</au><au>CONKLIN, RICHARD D.</au><au>LEE, B. LAMAR</au><au>GEARY, TIMOTHY G.</au><au>ROTHWELL, J. T.</au><au>SANGSTER, N. C.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>ANTHELMINTIC ACTIVITY OF DIOXAPYRROLOMYCIN</atitle><jtitle>Journal of antibiotics</jtitle><addtitle>J. Antibiot.</addtitle><date>1992</date><risdate>1992</risdate><volume>45</volume><issue>6</issue><spage>977</spage><epage>983</epage><pages>977-983</pages><issn>0021-8820</issn><eissn>1881-1469</eissn><coden>JANTAJ</coden><abstract>Dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 produced by UC 11065 were evaluated as anthelmintics. Assays used to examine these compounds included effects on the free-living nematode Caenorhabditis elegans, ability to clear target nematodes (Haemonchus contortus and Trichostrongylus colubriformis) from jirds, and clearance of Haemonchus contortus from lambs. A crude extract of UC 11065 containing dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 was active against C. elegans and against H. contortus in the jird. Purified and/or synthetic samples of dioxapyrrolomycin, pyrrolomycin C, pyrrolomycin D, and piericidin C2 were tested in the jird model; only dioxapyrrolomycin exhibited appreciable activity against H. contortus ( ≥ 90.9% clearance at 0.33 mg/jird), while none of the compounds showed appreciable activity against T. colubriformis. Dioxapyrrolomycin cleared 99.9% of H. contortus from lambs at 12.5 mg/kg. An in vitro migration study using susceptible and closantel-resistant H. contortus showed there is cross-resistance between dioxapyrrolomycin and closantel. Dioxapyrrolomycin appears to be a narrow-spectrum anthelmintic which works through a closantel-like mode-of-action.</abstract><cop>Tokyo</cop><pub>JAPAN ANTIBIOTICS RESEARCH ASSOCIATION</pub><pmid>1500366</pmid><doi>10.7164/antibiotics.45.977</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0021-8820 |
| ispartof | The Journal of Antibiotics, 1992/06/25, Vol.45(6), pp.977-983 |
| issn | 0021-8820 1881-1469 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_73109838 |
| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese |
| subjects | Actinomycetales - metabolism Animals Anthelmintics - isolation & purification Anthelmintics - pharmacology Anti-Bacterial Agents - isolation & purification Anti-Bacterial Agents - pharmacology Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Biological and medical sciences Medical sciences Pharmacology. Drug treatments Pyrroles - isolation & purification Pyrroles - pharmacology Sheep |
| title | ANTHELMINTIC ACTIVITY OF DIOXAPYRROLOMYCIN |
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