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Microbial and mammalian metabolism studies on the semisynthetic antimalarial, deoxoartemisinin
Deoxoartemisinin is a semisynthetic antimalarial with potential for treatment of multiple drug resistant malaria. Metabolism studies were conducted to aid in future drug development. Microbial model systems were employed which have been shown to be good predictors of mammalian drug metabolites. Meta...
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| Published in: | Pharmaceutical research 1995-10, Vol.12 (10), p.1493-1498 |
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| Main Authors: | , , , , |
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| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c327t-b4129095ee1acccc7c1112267c1fea7cd3c289174cc107c1a97ad598f41b05d13 |
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| container_end_page | 1498 |
| container_issue | 10 |
| container_start_page | 1493 |
| container_title | Pharmaceutical research |
| container_volume | 12 |
| creator | KHALIFA, S. I BAKER, J. K MANKIL JUNG MCCHESNEY, J. D HUFFORD, C. D |
| description | Deoxoartemisinin is a semisynthetic antimalarial with potential for treatment of multiple drug resistant malaria. Metabolism studies were conducted to aid in future drug development.
Microbial model systems were employed which have been shown to be good predictors of mammalian drug metabolites. Metabolism studies using rats were also performed.
Three microbial metabolites of deoxoartemisinin were identified (2, 3, and 4). Metabolite 3 was also found in rat plasma. HPLC/MS analyses were performed on the rat plasma using 2, 3, and 4 as standards. All metabolites were thoroughly characterized by 1H and 13C-NMR. An additional rat plasma metabolite was revealed and it was shown not to be 9 alpha-hydroxyartemisinin.
Deoxoartemisinin was metabolized to three microbial metabolites. Metabolism by rats showed the presence of two metabolites in the plasma, one of which was the same as the microbial metabolite. |
| doi_str_mv | 10.1023/A:1016239505506 |
| format | article |
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Microbial model systems were employed which have been shown to be good predictors of mammalian drug metabolites. Metabolism studies using rats were also performed.
Three microbial metabolites of deoxoartemisinin were identified (2, 3, and 4). Metabolite 3 was also found in rat plasma. HPLC/MS analyses were performed on the rat plasma using 2, 3, and 4 as standards. All metabolites were thoroughly characterized by 1H and 13C-NMR. An additional rat plasma metabolite was revealed and it was shown not to be 9 alpha-hydroxyartemisinin.
Deoxoartemisinin was metabolized to three microbial metabolites. Metabolism by rats showed the presence of two metabolites in the plasma, one of which was the same as the microbial metabolite.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1023/A:1016239505506</identifier><identifier>PMID: 8584488</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>New York, NY: Springer</publisher><subject>Animals ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antimalarials - blood ; Antimalarials - chemistry ; Antimalarials - metabolism ; Antiparasitic agents ; Artemisinins ; Aspergillus - metabolism ; Biological and medical sciences ; Magnetic Resonance Spectroscopy ; Male ; Medical sciences ; Mucorales - metabolism ; Pharmacology. Drug treatments ; Rats ; Rats, Wistar ; Saccharomyces - metabolism ; Sesquiterpenes - blood ; Sesquiterpenes - chemistry ; Sesquiterpenes - metabolism ; Streptomyces - metabolism</subject><ispartof>Pharmaceutical research, 1995-10, Vol.12 (10), p.1493-1498</ispartof><rights>1995 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c327t-b4129095ee1acccc7c1112267c1fea7cd3c289174cc107c1a97ad598f41b05d13</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3701227$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8584488$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>KHALIFA, S. I</creatorcontrib><creatorcontrib>BAKER, J. K</creatorcontrib><creatorcontrib>MANKIL JUNG</creatorcontrib><creatorcontrib>MCCHESNEY, J. D</creatorcontrib><creatorcontrib>HUFFORD, C. D</creatorcontrib><title>Microbial and mammalian metabolism studies on the semisynthetic antimalarial, deoxoartemisinin</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><description>Deoxoartemisinin is a semisynthetic antimalarial with potential for treatment of multiple drug resistant malaria. Metabolism studies were conducted to aid in future drug development.
Microbial model systems were employed which have been shown to be good predictors of mammalian drug metabolites. Metabolism studies using rats were also performed.
Three microbial metabolites of deoxoartemisinin were identified (2, 3, and 4). Metabolite 3 was also found in rat plasma. HPLC/MS analyses were performed on the rat plasma using 2, 3, and 4 as standards. All metabolites were thoroughly characterized by 1H and 13C-NMR. An additional rat plasma metabolite was revealed and it was shown not to be 9 alpha-hydroxyartemisinin.
Deoxoartemisinin was metabolized to three microbial metabolites. Metabolism by rats showed the presence of two metabolites in the plasma, one of which was the same as the microbial metabolite.</description><subject>Animals</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antimalarials - blood</subject><subject>Antimalarials - chemistry</subject><subject>Antimalarials - metabolism</subject><subject>Antiparasitic agents</subject><subject>Artemisinins</subject><subject>Aspergillus - metabolism</subject><subject>Biological and medical sciences</subject><subject>Magnetic Resonance Spectroscopy</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mucorales - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Saccharomyces - metabolism</subject><subject>Sesquiterpenes - blood</subject><subject>Sesquiterpenes - chemistry</subject><subject>Sesquiterpenes - metabolism</subject><subject>Streptomyces - metabolism</subject><issn>0724-8741</issn><issn>1573-904X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><recordid>eNo9UEtLxDAQDqKs6-rZk5CDeLKaZ5N4WxZfsOJFwZNlmqYYadO1ScH990ZcnMs3zPfgYxA6peSKEsavlzeU0JJxI4mUpNxDcyoVLwwRb_toThQThVaCHqKjGD8JIZoaMUMzLbUQWs_R-5O341B76DCEBvfQ99B5CLh3Ceqh87HHMU2NdxEPAacPh6PrfdyGvCZvsyv5bIExR1zixg3fA4zpV-KDD8fooIUuupMdLtDr3e3L6qFYP98_rpbrwnKmUlELygwx0jkKNo-ylFLGyoytA2Ubbpk2VAlrKclHMAoaaXQraE1kQ_kCXfzlbsbha3IxVbmAdV0HwQ1TrJRSQpZcZuHZTjjVvWuqzZjbj9tq95DMn-94iBa6doRgffyXcUVyL8V_ANsMcNY</recordid><startdate>19951001</startdate><enddate>19951001</enddate><creator>KHALIFA, S. I</creator><creator>BAKER, J. K</creator><creator>MANKIL JUNG</creator><creator>MCCHESNEY, J. D</creator><creator>HUFFORD, C. D</creator><general>Springer</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>19951001</creationdate><title>Microbial and mammalian metabolism studies on the semisynthetic antimalarial, deoxoartemisinin</title><author>KHALIFA, S. I ; BAKER, J. K ; MANKIL JUNG ; MCCHESNEY, J. D ; HUFFORD, C. D</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c327t-b4129095ee1acccc7c1112267c1fea7cd3c289174cc107c1a97ad598f41b05d13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>Animals</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antimalarials - blood</topic><topic>Antimalarials - chemistry</topic><topic>Antimalarials - metabolism</topic><topic>Antiparasitic agents</topic><topic>Artemisinins</topic><topic>Aspergillus - metabolism</topic><topic>Biological and medical sciences</topic><topic>Magnetic Resonance Spectroscopy</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Mucorales - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Saccharomyces - metabolism</topic><topic>Sesquiterpenes - blood</topic><topic>Sesquiterpenes - chemistry</topic><topic>Sesquiterpenes - metabolism</topic><topic>Streptomyces - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>KHALIFA, S. I</creatorcontrib><creatorcontrib>BAKER, J. K</creatorcontrib><creatorcontrib>MANKIL JUNG</creatorcontrib><creatorcontrib>MCCHESNEY, J. D</creatorcontrib><creatorcontrib>HUFFORD, C. D</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>MEDLINE - Academic</collection><jtitle>Pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>KHALIFA, S. I</au><au>BAKER, J. K</au><au>MANKIL JUNG</au><au>MCCHESNEY, J. D</au><au>HUFFORD, C. D</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Microbial and mammalian metabolism studies on the semisynthetic antimalarial, deoxoartemisinin</atitle><jtitle>Pharmaceutical research</jtitle><addtitle>Pharm Res</addtitle><date>1995-10-01</date><risdate>1995</risdate><volume>12</volume><issue>10</issue><spage>1493</spage><epage>1498</epage><pages>1493-1498</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>Deoxoartemisinin is a semisynthetic antimalarial with potential for treatment of multiple drug resistant malaria. Metabolism studies were conducted to aid in future drug development.
Microbial model systems were employed which have been shown to be good predictors of mammalian drug metabolites. Metabolism studies using rats were also performed.
Three microbial metabolites of deoxoartemisinin were identified (2, 3, and 4). Metabolite 3 was also found in rat plasma. HPLC/MS analyses were performed on the rat plasma using 2, 3, and 4 as standards. All metabolites were thoroughly characterized by 1H and 13C-NMR. An additional rat plasma metabolite was revealed and it was shown not to be 9 alpha-hydroxyartemisinin.
Deoxoartemisinin was metabolized to three microbial metabolites. Metabolism by rats showed the presence of two metabolites in the plasma, one of which was the same as the microbial metabolite.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>8584488</pmid><doi>10.1023/A:1016239505506</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0724-8741 |
| ispartof | Pharmaceutical research, 1995-10, Vol.12 (10), p.1493-1498 |
| issn | 0724-8741 1573-904X |
| language | eng |
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| source | Springer LINK Archives |
| subjects | Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarials - blood Antimalarials - chemistry Antimalarials - metabolism Antiparasitic agents Artemisinins Aspergillus - metabolism Biological and medical sciences Magnetic Resonance Spectroscopy Male Medical sciences Mucorales - metabolism Pharmacology. Drug treatments Rats Rats, Wistar Saccharomyces - metabolism Sesquiterpenes - blood Sesquiterpenes - chemistry Sesquiterpenes - metabolism Streptomyces - metabolism |
| title | Microbial and mammalian metabolism studies on the semisynthetic antimalarial, deoxoartemisinin |
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