Inhibitory Effects of Herbal Extracts on Breast Cancer Resistance Protein (BCRP) and Structure-Inhibitory Potency Relationship of Isoflavonoids
The inhibition of intestinal breast cancer resistance protein (BCRP), which restricts the absorption of xenobiotics, may increase the systemic availability of its substrates. The aim of this study was to evaluate the inhibitory effects of herbal extracts and their constituents on BCRP-mediated trans...
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| Veröffentlicht in: | DRUG METABOLISM AND PHARMACOKINETICS 2010-01, Vol.25 (2), p.170-179 |
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| creator | Tamaki, Hirofumi Satoh, Hiroki Hori, Satoko Ohtani, Hisakazu Sawada, Yasufumi |
| description | The inhibition of intestinal breast cancer resistance protein (BCRP), which restricts the absorption of xenobiotics, may increase the systemic availability of its substrates. The aim of this study was to evaluate the inhibitory effects of herbal extracts and their constituents on BCRP-mediated transport. The inhibitory effects of 9 herbal extracts and 23 isoflavonoids, including soybean-derived isoflavones, on BCRP-mediated methotrexate (MTX) transport were evaluated using BCRP-expressing membrane vesicles. The structure-inhibitory potency relationship was investigated by multiple factor analysis. Extracts of soybean, Gymnema sylvestre, black cohosh and passion flower and rutin strongly inhibited BCRP-mediated transport of MTX at 1mg/ml, while inhibition by chlorella, milk thistle and Siberian ginseng extracts was weak. Among the 23 isoflavonoids examined, all of which inhibited BCRP-mediated transport, coumestrol showed the most potent inhibition (IC50=63 nM). The inhibitory potencies of 6 isoflavonoid glucosides were 10- to 100-fold lower than those of the corresponding aglycones. The addition of a 5-hydroxyl or 6-methoxyl moiety tended to potentiate the inhibition. The inhibitory potency of daidzein was decreased 100-fold by 7-glucuronidation, but was virtually unaffected by 4'-sulfation. Thus, some herbal and dietary supplements and isoflavonoids may increase the systemic availability of BCRP substrates when concomitantly given orally. |
| doi_str_mv | 10.2133/dmpk.25.170 |
| format | Article |
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The aim of this study was to evaluate the inhibitory effects of herbal extracts and their constituents on BCRP-mediated transport. The inhibitory effects of 9 herbal extracts and 23 isoflavonoids, including soybean-derived isoflavones, on BCRP-mediated methotrexate (MTX) transport were evaluated using BCRP-expressing membrane vesicles. The structure-inhibitory potency relationship was investigated by multiple factor analysis. Extracts of soybean, Gymnema sylvestre, black cohosh and passion flower and rutin strongly inhibited BCRP-mediated transport of MTX at 1mg/ml, while inhibition by chlorella, milk thistle and Siberian ginseng extracts was weak. Among the 23 isoflavonoids examined, all of which inhibited BCRP-mediated transport, coumestrol showed the most potent inhibition (IC50=63 nM). The inhibitory potencies of 6 isoflavonoid glucosides were 10- to 100-fold lower than those of the corresponding aglycones. The addition of a 5-hydroxyl or 6-methoxyl moiety tended to potentiate the inhibition. The inhibitory potency of daidzein was decreased 100-fold by 7-glucuronidation, but was virtually unaffected by 4'-sulfation. Thus, some herbal and dietary supplements and isoflavonoids may increase the systemic availability of BCRP substrates when concomitantly given orally.</description><identifier>ISSN: 1347-4367</identifier><identifier>EISSN: 1880-0920</identifier><identifier>DOI: 10.2133/dmpk.25.170</identifier><identifier>PMID: 20460823</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>ATP Binding Cassette Transporter, Sub-Family G, Member 2 ; ATP-binding cassette transporter G2 (ABCG2) ; ATP-Binding Cassette Transporters - antagonists & inhibitors ; ATP-Binding Cassette Transporters - pharmacology ; Biological Transport ; breast cancer resistance protein (BCRP) ; Breast Neoplasms ; Cell Line, Tumor ; dietary supplement ; drug interactions ; Drug Resistance, Neoplasm ; Humans ; Isoflavones - pharmacology ; isoflavonoids ; Multidrug Resistance-Associated Proteins ; Neoplasm Proteins - antagonists & inhibitors ; Neoplasm Proteins - pharmacology ; Plant Extracts - pharmacology ; Polyglutamic Acid - pharmacology ; Structure-Activity Relationship</subject><ispartof>DRUG METABOLISM AND PHARMACOKINETICS, 2010-01, Vol.25 (2), p.170-179</ispartof><rights>2010 The Japanese Society for the Study of Xenobiotics</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c588t-48371e3d7f417632d39265eca6222db31af2c12fb1e078b3818d0d1c3a7ed8d53</citedby><cites>FETCH-LOGICAL-c588t-48371e3d7f417632d39265eca6222db31af2c12fb1e078b3818d0d1c3a7ed8d53</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20460823$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tamaki, Hirofumi</creatorcontrib><creatorcontrib>Satoh, Hiroki</creatorcontrib><creatorcontrib>Hori, Satoko</creatorcontrib><creatorcontrib>Ohtani, Hisakazu</creatorcontrib><creatorcontrib>Sawada, Yasufumi</creatorcontrib><creatorcontrib>Laboratory of Drug Informatics</creatorcontrib><creatorcontrib>The University of Tokyo</creatorcontrib><creatorcontrib>Graduate School of Interdisciplinary Information Studies</creatorcontrib><creatorcontrib>Graduate School of Pharmaceutical Sciences</creatorcontrib><title>Inhibitory Effects of Herbal Extracts on Breast Cancer Resistance Protein (BCRP) and Structure-Inhibitory Potency Relationship of Isoflavonoids</title><title>DRUG METABOLISM AND PHARMACOKINETICS</title><addtitle>Drug Metab Pharmacokinet</addtitle><description>The inhibition of intestinal breast cancer resistance protein (BCRP), which restricts the absorption of xenobiotics, may increase the systemic availability of its substrates. The aim of this study was to evaluate the inhibitory effects of herbal extracts and their constituents on BCRP-mediated transport. The inhibitory effects of 9 herbal extracts and 23 isoflavonoids, including soybean-derived isoflavones, on BCRP-mediated methotrexate (MTX) transport were evaluated using BCRP-expressing membrane vesicles. The structure-inhibitory potency relationship was investigated by multiple factor analysis. Extracts of soybean, Gymnema sylvestre, black cohosh and passion flower and rutin strongly inhibited BCRP-mediated transport of MTX at 1mg/ml, while inhibition by chlorella, milk thistle and Siberian ginseng extracts was weak. Among the 23 isoflavonoids examined, all of which inhibited BCRP-mediated transport, coumestrol showed the most potent inhibition (IC50=63 nM). The inhibitory potencies of 6 isoflavonoid glucosides were 10- to 100-fold lower than those of the corresponding aglycones. The addition of a 5-hydroxyl or 6-methoxyl moiety tended to potentiate the inhibition. The inhibitory potency of daidzein was decreased 100-fold by 7-glucuronidation, but was virtually unaffected by 4'-sulfation. Thus, some herbal and dietary supplements and isoflavonoids may increase the systemic availability of BCRP substrates when concomitantly given orally.</description><subject>ATP Binding Cassette Transporter, Sub-Family G, Member 2</subject><subject>ATP-binding cassette transporter G2 (ABCG2)</subject><subject>ATP-Binding Cassette Transporters - antagonists & inhibitors</subject><subject>ATP-Binding Cassette Transporters - pharmacology</subject><subject>Biological Transport</subject><subject>breast cancer resistance protein (BCRP)</subject><subject>Breast Neoplasms</subject><subject>Cell Line, Tumor</subject><subject>dietary supplement</subject><subject>drug interactions</subject><subject>Drug Resistance, Neoplasm</subject><subject>Humans</subject><subject>Isoflavones - pharmacology</subject><subject>isoflavonoids</subject><subject>Multidrug Resistance-Associated Proteins</subject><subject>Neoplasm Proteins - antagonists & inhibitors</subject><subject>Neoplasm Proteins - pharmacology</subject><subject>Plant Extracts - pharmacology</subject><subject>Polyglutamic Acid - pharmacology</subject><subject>Structure-Activity Relationship</subject><issn>1347-4367</issn><issn>1880-0920</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkUtv1DAUhSMEog9YsUfeQYUy-BHHniUdTelIlRiVdm059o3qktiD7VSdX9G_jMMUxIKNr2Wf-_n6nKp6R_CCEsY-23H3Y0H5ggj8ojomUuIaLyl-WfasEXXDWnFUnaR0jzFjvKGvqyOKmxZLyo6rp42_c53LIe7Ruu_B5IRCjy4hdnpA68cc9e8jj84j6JTRSnsDEV1DcinPe7SNIYPz6OP56np7hrS36HuOk8lThPof_LbIvNmX1kFnF3y6c7v5rU0K_aAfgg_OpjfVq14PCd4-19Pq9mJ9s7qsr7593ay-XNWGS5nrRjJBgFnRN0S0jFq2pC0Ho1tKqe0Y0T01hPYdASxkxySRFltimBZgpeXstPpw4O5i-DlBymp0ycAwaA9hSkoUqwgmdFZ-OihNDClF6NUuulHHvSJYzQGoOQBFuSoBFPX7Z-7UjWD_av84XgQXB0G5dUYPwQ_Og7oPU_Tlw8oEMkLWXekofIwpx7QUoXDBz8uSC8r5PBc_gKDY9OAgqmRcMbhgY4lR2eD-O-Ev-7CrdQ</recordid><startdate>20100101</startdate><enddate>20100101</enddate><creator>Tamaki, Hirofumi</creator><creator>Satoh, Hiroki</creator><creator>Hori, Satoko</creator><creator>Ohtani, Hisakazu</creator><creator>Sawada, Yasufumi</creator><general>Elsevier Ltd</general><general>Japanese Society for the Study of Xenobiotics</general><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>20100101</creationdate><title>Inhibitory Effects of Herbal Extracts on Breast Cancer Resistance Protein (BCRP) and Structure-Inhibitory Potency Relationship of Isoflavonoids</title><author>Tamaki, Hirofumi ; Satoh, Hiroki ; Hori, Satoko ; Ohtani, Hisakazu ; Sawada, Yasufumi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c588t-48371e3d7f417632d39265eca6222db31af2c12fb1e078b3818d0d1c3a7ed8d53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>ATP Binding Cassette Transporter, Sub-Family G, Member 2</topic><topic>ATP-binding cassette transporter G2 (ABCG2)</topic><topic>ATP-Binding Cassette Transporters - antagonists & inhibitors</topic><topic>ATP-Binding Cassette Transporters - pharmacology</topic><topic>Biological Transport</topic><topic>breast cancer resistance protein (BCRP)</topic><topic>Breast Neoplasms</topic><topic>Cell Line, Tumor</topic><topic>dietary supplement</topic><topic>drug interactions</topic><topic>Drug Resistance, Neoplasm</topic><topic>Humans</topic><topic>Isoflavones - pharmacology</topic><topic>isoflavonoids</topic><topic>Multidrug Resistance-Associated Proteins</topic><topic>Neoplasm Proteins - antagonists & inhibitors</topic><topic>Neoplasm Proteins - pharmacology</topic><topic>Plant Extracts - pharmacology</topic><topic>Polyglutamic Acid - pharmacology</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tamaki, Hirofumi</creatorcontrib><creatorcontrib>Satoh, Hiroki</creatorcontrib><creatorcontrib>Hori, Satoko</creatorcontrib><creatorcontrib>Ohtani, Hisakazu</creatorcontrib><creatorcontrib>Sawada, Yasufumi</creatorcontrib><creatorcontrib>Laboratory of Drug Informatics</creatorcontrib><creatorcontrib>The University of Tokyo</creatorcontrib><creatorcontrib>Graduate School of Interdisciplinary Information Studies</creatorcontrib><creatorcontrib>Graduate School of Pharmaceutical Sciences</creatorcontrib><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>DRUG METABOLISM AND PHARMACOKINETICS</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tamaki, Hirofumi</au><au>Satoh, Hiroki</au><au>Hori, Satoko</au><au>Ohtani, Hisakazu</au><au>Sawada, Yasufumi</au><aucorp>Laboratory of Drug Informatics</aucorp><aucorp>The University of Tokyo</aucorp><aucorp>Graduate School of Interdisciplinary Information Studies</aucorp><aucorp>Graduate School of Pharmaceutical Sciences</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibitory Effects of Herbal Extracts on Breast Cancer Resistance Protein (BCRP) and Structure-Inhibitory Potency Relationship of Isoflavonoids</atitle><jtitle>DRUG METABOLISM AND PHARMACOKINETICS</jtitle><addtitle>Drug Metab Pharmacokinet</addtitle><date>2010-01-01</date><risdate>2010</risdate><volume>25</volume><issue>2</issue><spage>170</spage><epage>179</epage><pages>170-179</pages><issn>1347-4367</issn><eissn>1880-0920</eissn><abstract>The inhibition of intestinal breast cancer resistance protein (BCRP), which restricts the absorption of xenobiotics, may increase the systemic availability of its substrates. The aim of this study was to evaluate the inhibitory effects of herbal extracts and their constituents on BCRP-mediated transport. The inhibitory effects of 9 herbal extracts and 23 isoflavonoids, including soybean-derived isoflavones, on BCRP-mediated methotrexate (MTX) transport were evaluated using BCRP-expressing membrane vesicles. The structure-inhibitory potency relationship was investigated by multiple factor analysis. Extracts of soybean, Gymnema sylvestre, black cohosh and passion flower and rutin strongly inhibited BCRP-mediated transport of MTX at 1mg/ml, while inhibition by chlorella, milk thistle and Siberian ginseng extracts was weak. Among the 23 isoflavonoids examined, all of which inhibited BCRP-mediated transport, coumestrol showed the most potent inhibition (IC50=63 nM). The inhibitory potencies of 6 isoflavonoid glucosides were 10- to 100-fold lower than those of the corresponding aglycones. The addition of a 5-hydroxyl or 6-methoxyl moiety tended to potentiate the inhibition. The inhibitory potency of daidzein was decreased 100-fold by 7-glucuronidation, but was virtually unaffected by 4'-sulfation. Thus, some herbal and dietary supplements and isoflavonoids may increase the systemic availability of BCRP substrates when concomitantly given orally.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>20460823</pmid><doi>10.2133/dmpk.25.170</doi><tpages>10</tpages></addata></record> |
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| subjects | ATP Binding Cassette Transporter, Sub-Family G, Member 2 ATP-binding cassette transporter G2 (ABCG2) ATP-Binding Cassette Transporters - antagonists & inhibitors ATP-Binding Cassette Transporters - pharmacology Biological Transport breast cancer resistance protein (BCRP) Breast Neoplasms Cell Line, Tumor dietary supplement drug interactions Drug Resistance, Neoplasm Humans Isoflavones - pharmacology isoflavonoids Multidrug Resistance-Associated Proteins Neoplasm Proteins - antagonists & inhibitors Neoplasm Proteins - pharmacology Plant Extracts - pharmacology Polyglutamic Acid - pharmacology Structure-Activity Relationship |
| title | Inhibitory Effects of Herbal Extracts on Breast Cancer Resistance Protein (BCRP) and Structure-Inhibitory Potency Relationship of Isoflavonoids |
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