Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources
Identifieur interne : 000B87 ( Ncbi/Merge ); précédent : 000B86; suivant : 000B88Use 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
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<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>
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<front><journal-meta><journal-id journal-id-type="nlm-ta">BMC Pharmacol</journal-id>
<journal-title-group><journal-title>BMC Pharmacology</journal-title>
</journal-title-group>
<issn pub-type="epub">1471-2210</issn>
<publisher><publisher-name>BioMed Central</publisher-name>
</publisher>
</journal-meta>
<article-meta><article-id pub-id-type="pmid">20537191</article-id>
<article-id pub-id-type="pmc">2898707</article-id>
<article-id pub-id-type="publisher-id">1471-2210-10-7</article-id>
<article-id pub-id-type="doi">10.1186/1471-2210-10-7</article-id>
<article-categories><subj-group subj-group-type="heading"><subject>Methodology article</subject>
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<title-group><article-title>Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources</article-title>
</title-group>
<contrib-group><contrib contrib-type="author" id="A1"><name><surname>Asami</surname>
<given-names>Yukihiro</given-names>
</name>
<xref ref-type="aff" rid="I1">1</xref>
<email>yasami@kribb.re.kr</email>
</contrib>
<contrib contrib-type="author" id="A2"><name><surname>Horie</surname>
<given-names>Ryo</given-names>
</name>
<xref ref-type="aff" rid="I1">1</xref>
<email>ff097116@mail.ecc.u-tokyo.ac.jp</email>
</contrib>
<contrib contrib-type="author" id="A3"><name><surname>Hamamoto</surname>
<given-names>Hiroshi</given-names>
</name>
<xref ref-type="aff" rid="I1">1</xref>
<email>hamamoto@mol.f.u-tokyo.ac.jp</email>
</contrib>
<contrib contrib-type="author" corresp="yes" id="A4"><name><surname>Sekimizu</surname>
<given-names>Kazuhisa</given-names>
</name>
<xref ref-type="aff" rid="I1">1</xref>
<email>sekimizu@mol.f.u-tokyo.ac.jp</email>
</contrib>
</contrib-group>
<aff id="I1"><label>1</label>
Department of Microbiology, Faculty of Pharmaceutical Sciences, Graduate of the University of Tokyo. 7-3-1, Hongo, Bunkyo-ku, Tokyo, Japan</aff>
<pub-date pub-type="collection"><year>2010</year>
</pub-date>
<pub-date pub-type="epub"><day>11</day>
<month>6</month>
<year>2010</year>
</pub-date>
<volume>10</volume>
<fpage>7</fpage>
<lpage>7</lpage>
<history><date date-type="received"><day>18</day>
<month>12</month>
<year>2009</year>
</date>
<date date-type="accepted"><day>11</day>
<month>6</month>
<year>2010</year>
</date>
</history>
<permissions><copyright-statement>Copyright ©2010 Asami et al; licensee BioMed Central Ltd.</copyright-statement>
<copyright-year>2010</copyright-year>
<copyright-holder>Asami et al; licensee BioMed Central Ltd.</copyright-holder>
<license license-type="open-access" xlink:href="http://creativecommons.org/licenses/by/2.0"><license-p>This is an Open Access article distributed under the terms of the Creative Commons Attribution License (<ext-link ext-link-type="uri" xlink:href="http://creativecommons.org/licenses/by/2.0">http://creativecommons.org/licenses/by/2.0</ext-link>
), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.</license-p>
</license>
</permissions>
<self-uri xlink:href="http://www.biomedcentral.com/1471-2210/10/7"></self-uri>
<abstract><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>
</abstract>
</article-meta>
</front>
</pmc>
<affiliations><list><country><li>Japon</li>
</country>
<settlement><li>Tokyo</li>
</settlement>
</list>
<tree><country name="Japon"><noRegion><name sortKey="Asami, Yukihiro" sort="Asami, Yukihiro" uniqKey="Asami Y" first="Yukihiro" last="Asami">Yukihiro Asami</name>
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<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>
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