Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources
Identifieur interne : 001979 ( Main/Exploration ); précédent : 001978; suivant : 001980Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources
Auteurs : Yukihiro Asami [Japon] ; Ryo Horie [Japon] ; Hiroshi Hamamoto [Japon] ; Kazuhisa Sekimizu [Japon]Source :
- BMC Pharmacology [ 1471-2210 ] ; 2010.
Abstract
We use silkworms to evaluate therapeutic effects of drug candidates. Our previous reports have revealed that there are common mechanisms of pharmacokinetics of chemicals in silkworms and mammals. In this report, we attempt to establish a method by using silkworms to identify chemicals from plant extracts which are absorbed from intestine and also stably exist in body fluids.
Three compounds were detected in the silkworm hemolymph by HPLC analysis after midgut injection of acetone extracts of seihi, an herbal medicine obtained from orange peel. Analyses with MS and NMR revealed that the compounds were nobiletin, heptamethoxyflavone, and tangeretin. These compounds are reported to be stable in mammalian blood. The half-life of each of these compounds in the silkworm hemolymph was 18, 26 and 34 h, respectively.
These findings suggest that silkworms can be used as a model animal to easily identify compounds with appropriate pharmacokinetic behavior.
Url:
DOI: 10.1186/1471-2210-10-7
PubMed: 20537191
PubMed Central: 2898707
Affiliations:
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Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo</wicri:regionArea><placeName><settlement type="city">Tokyo</settlement></placeName></affiliation></author><author><name sortKey="Horie, Ryo" sort="Horie, Ryo" uniqKey="Horie R" first="Ryo" last="Horie">Ryo Horie</name><affiliation wicri:level="3"><nlm:aff id="I1">Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo</wicri:regionArea><placeName><settlement type="city">Tokyo</settlement></placeName></affiliation></author><author><name sortKey="Hamamoto, Hiroshi" sort="Hamamoto, Hiroshi" uniqKey="Hamamoto H" first="Hiroshi" last="Hamamoto">Hiroshi Hamamoto</name><affiliation wicri:level="3"><nlm:aff id="I1">Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo</wicri:regionArea><placeName><settlement type="city">Tokyo</settlement></placeName></affiliation></author><author><name sortKey="Sekimizu, Kazuhisa" sort="Sekimizu, Kazuhisa" uniqKey="Sekimizu K" first="Kazuhisa" last="Sekimizu">Kazuhisa Sekimizu</name><affiliation wicri:level="3"><nlm:aff id="I1">Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo</wicri:regionArea><placeName><settlement type="city">Tokyo</settlement></placeName></affiliation></author></analytic><series><title level="j">BMC Pharmacology</title><idno type="eISSN">1471-2210</idno><imprint><date when="2010">2010</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><sec><title>Background</title><p>We use silkworms to evaluate therapeutic effects of drug candidates. Our previous reports have revealed that there are common mechanisms of pharmacokinetics of chemicals in silkworms and mammals. In this report, we attempt to establish a method by using silkworms to identify chemicals from plant extracts which are absorbed from intestine and also stably exist in body fluids.</p></sec><sec><title>Results</title><p>Three compounds were detected in the silkworm hemolymph by HPLC analysis after midgut injection of acetone extracts of seihi, an herbal medicine obtained from orange peel. Analyses with MS and NMR revealed that the compounds were nobiletin, heptamethoxyflavone, and tangeretin. These compounds are reported to be stable in mammalian blood. The half-life of each of these compounds in the silkworm hemolymph was 18, 26 and 34 h, respectively.</p></sec><sec><title>Conclusions</title><p>These findings suggest that silkworms can be used as a model animal to easily identify compounds with appropriate pharmacokinetic behavior.</p></sec></div></front><back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Greaves, P" uniqKey="Greaves P">P Greaves</name></author><author><name sortKey="Williams, A" uniqKey="Williams A">A Williams</name></author><author><name sortKey="Eve, M" uniqKey="Eve M">M Eve</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Rostami Hodjegan, A" uniqKey="Rostami Hodjegan A">A Rostami-Hodjegan</name></author><author><name sortKey="Tucker, Gt" uniqKey="Tucker G">GT Tucker</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Berger, J" uniqKey="Berger J">J 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name="Japon"><noRegion><name sortKey="Asami, Yukihiro" sort="Asami, Yukihiro" uniqKey="Asami Y" first="Yukihiro" last="Asami">Yukihiro Asami</name></noRegion><name sortKey="Hamamoto, Hiroshi" sort="Hamamoto, Hiroshi" uniqKey="Hamamoto H" first="Hiroshi" last="Hamamoto">Hiroshi Hamamoto</name><name sortKey="Horie, Ryo" sort="Horie, Ryo" uniqKey="Horie R" first="Ryo" last="Horie">Ryo Horie</name><name sortKey="Sekimizu, Kazuhisa" sort="Sekimizu, Kazuhisa" uniqKey="Sekimizu K" first="Kazuhisa" last="Sekimizu">Kazuhisa Sekimizu</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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