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Rhubarb decreased the systemic exposure of cyclosporine, a probe substrate of P-glycoprotein and CYP 3A
1. Rhubarb, rhizome of Rheum palmatum L. (RP), is an important herb in clinical Chinese medicine. 2. Cyclosporine (CSP) is an immunosuppressant with narrow therapeutic window. The oral bioavailability of CSP was associated with P-glycoprotein (P-gp) and CYP 3A4. CSP was used as a probe substrate to...
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| Published in: | Xenobiotica 2016-08, Vol.46 (8), p.677-682 |
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| Main Authors: | , , , , , , |
| Format: | Article |
| Language: | English |
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| cites | cdi_FETCH-LOGICAL-c366t-b3205110948768e9d8f6cd2fec6f9b8d6ff1fd0c9350792dd58dd4ab2df5b2753 |
| container_end_page | 682 |
| container_issue | 8 |
| container_start_page | 677 |
| container_title | Xenobiotica |
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| creator | Yu, Chung-Ping Lin, Hui-Ju Lin, Shiuan-Pey Shia, Chi-Sheng Chang, Pei-Hua Hou, Yu-Chi Hsieh, Yo-Wen |
| description | 1. Rhubarb, rhizome of Rheum palmatum L. (RP), is an important herb in clinical Chinese medicine.
2. Cyclosporine (CSP) is an immunosuppressant with narrow therapeutic window. The oral bioavailability of CSP was associated with P-glycoprotein (P-gp) and CYP 3A4. CSP was used as a probe substrate to investigate the in vivo modulation effects of RP on P-gp and CYP 3A.
3. Rats were orally administered 2.5 mg/kg of CSP with and without 0.25 and 1.0 g/kg of RP. The blood CSP concentration was determined by a specific monoclonal fluorescence polarization immunoassay.
4. Both dosages of RP significantly decreased the C
max
and AUC
0-t
of CSP in rats. Mechanism studies indicated that RP activated the functions of P-gp and CYP 3A.
5. RP ingestion reduced the systemic exposure of CSP through activating P-gp and CYP 3A. |
| doi_str_mv | 10.3109/00498254.2015.1117159 |
| format | article |
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2. Cyclosporine (CSP) is an immunosuppressant with narrow therapeutic window. The oral bioavailability of CSP was associated with P-glycoprotein (P-gp) and CYP 3A4. CSP was used as a probe substrate to investigate the in vivo modulation effects of RP on P-gp and CYP 3A.
3. Rats were orally administered 2.5 mg/kg of CSP with and without 0.25 and 1.0 g/kg of RP. The blood CSP concentration was determined by a specific monoclonal fluorescence polarization immunoassay.
4. Both dosages of RP significantly decreased the C
max
and AUC
0-t
of CSP in rats. Mechanism studies indicated that RP activated the functions of P-gp and CYP 3A.
5. RP ingestion reduced the systemic exposure of CSP through activating P-gp and CYP 3A.</description><identifier>ISSN: 0049-8254</identifier><identifier>EISSN: 1366-5928</identifier><identifier>DOI: 10.3109/00498254.2015.1117159</identifier><identifier>PMID: 26634287</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>Animals ; ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism ; Cyclosporine ; Cyclosporine - pharmacology ; CYP 3A ; Cytochrome P-450 CYP3A - metabolism ; Drugs, Chinese Herbal - pharmacology ; herb-drug interaction ; Immunosuppressive Agents - pharmacology ; P-glycoprotein ; Rats ; Rheum - chemistry ; rhubarb</subject><ispartof>Xenobiotica, 2016-08, Vol.46 (8), p.677-682</ispartof><rights>2015 Taylor & Francis. 2015</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c366t-b3205110948768e9d8f6cd2fec6f9b8d6ff1fd0c9350792dd58dd4ab2df5b2753</citedby><cites>FETCH-LOGICAL-c366t-b3205110948768e9d8f6cd2fec6f9b8d6ff1fd0c9350792dd58dd4ab2df5b2753</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/26634287$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yu, Chung-Ping</creatorcontrib><creatorcontrib>Lin, Hui-Ju</creatorcontrib><creatorcontrib>Lin, Shiuan-Pey</creatorcontrib><creatorcontrib>Shia, Chi-Sheng</creatorcontrib><creatorcontrib>Chang, Pei-Hua</creatorcontrib><creatorcontrib>Hou, Yu-Chi</creatorcontrib><creatorcontrib>Hsieh, Yo-Wen</creatorcontrib><title>Rhubarb decreased the systemic exposure of cyclosporine, a probe substrate of P-glycoprotein and CYP 3A</title><title>Xenobiotica</title><addtitle>Xenobiotica</addtitle><description>1. Rhubarb, rhizome of Rheum palmatum L. (RP), is an important herb in clinical Chinese medicine.
2. Cyclosporine (CSP) is an immunosuppressant with narrow therapeutic window. The oral bioavailability of CSP was associated with P-glycoprotein (P-gp) and CYP 3A4. CSP was used as a probe substrate to investigate the in vivo modulation effects of RP on P-gp and CYP 3A.
3. Rats were orally administered 2.5 mg/kg of CSP with and without 0.25 and 1.0 g/kg of RP. The blood CSP concentration was determined by a specific monoclonal fluorescence polarization immunoassay.
4. Both dosages of RP significantly decreased the C
max
and AUC
0-t
of CSP in rats. Mechanism studies indicated that RP activated the functions of P-gp and CYP 3A.
5. RP ingestion reduced the systemic exposure of CSP through activating P-gp and CYP 3A.</description><subject>Animals</subject><subject>ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism</subject><subject>Cyclosporine</subject><subject>Cyclosporine - pharmacology</subject><subject>CYP 3A</subject><subject>Cytochrome P-450 CYP3A - metabolism</subject><subject>Drugs, Chinese Herbal - pharmacology</subject><subject>herb-drug interaction</subject><subject>Immunosuppressive Agents - pharmacology</subject><subject>P-glycoprotein</subject><subject>Rats</subject><subject>Rheum - chemistry</subject><subject>rhubarb</subject><issn>0049-8254</issn><issn>1366-5928</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><recordid>eNp9kEtP3DAURi1UBMPjJ7TysotmsJ3YsXdFI0orIYEQLFhZflxDqiSe2olK_j0JM3TZ1V3c893HQegzJeuSEnVBSKUk49WaEcrXlNKacnWAVrQUouCKyU9otTDFAh2jk5x_E0IEZewIHTMhyorJeoWe719Ga5LFHlwCk8Hj4QVwnvIAXeMwvG5jHhPgGLCbXBvzNqamh2_Y4G2KdkZHm4dkhnfkrnhuJxfnzgBNj03v8ebpDpeXZ-gwmDbD-b6eoscfVw-bn8XN7fWvzeVN4ea7h8KWjHA6_1fJWkhQXgbhPAvgRFBWehECDZ44VXJSK-Y9l95XxjIfuGU1L0_R193c-YQ_I-RBd0120LamhzhmTWvJ65IzoWaU71CXYs4Jgt6mpjNp0pToxbH-cKwXx3rveM592a8YbQf-X-pD6gx83wFNH2LqzN-YWq8HM7UxhWR61-Rl_v92vAEMOovL</recordid><startdate>20160802</startdate><enddate>20160802</enddate><creator>Yu, Chung-Ping</creator><creator>Lin, Hui-Ju</creator><creator>Lin, Shiuan-Pey</creator><creator>Shia, Chi-Sheng</creator><creator>Chang, Pei-Hua</creator><creator>Hou, Yu-Chi</creator><creator>Hsieh, Yo-Wen</creator><general>Taylor & Francis</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>20160802</creationdate><title>Rhubarb decreased the systemic exposure of cyclosporine, a probe substrate of P-glycoprotein and CYP 3A</title><author>Yu, Chung-Ping ; Lin, Hui-Ju ; Lin, Shiuan-Pey ; Shia, Chi-Sheng ; Chang, Pei-Hua ; Hou, Yu-Chi ; Hsieh, Yo-Wen</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c366t-b3205110948768e9d8f6cd2fec6f9b8d6ff1fd0c9350792dd58dd4ab2df5b2753</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Animals</topic><topic>ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism</topic><topic>Cyclosporine</topic><topic>Cyclosporine - pharmacology</topic><topic>CYP 3A</topic><topic>Cytochrome P-450 CYP3A - metabolism</topic><topic>Drugs, Chinese Herbal - pharmacology</topic><topic>herb-drug interaction</topic><topic>Immunosuppressive Agents - pharmacology</topic><topic>P-glycoprotein</topic><topic>Rats</topic><topic>Rheum - chemistry</topic><topic>rhubarb</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yu, Chung-Ping</creatorcontrib><creatorcontrib>Lin, Hui-Ju</creatorcontrib><creatorcontrib>Lin, Shiuan-Pey</creatorcontrib><creatorcontrib>Shia, Chi-Sheng</creatorcontrib><creatorcontrib>Chang, Pei-Hua</creatorcontrib><creatorcontrib>Hou, Yu-Chi</creatorcontrib><creatorcontrib>Hsieh, Yo-Wen</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>Xenobiotica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yu, Chung-Ping</au><au>Lin, Hui-Ju</au><au>Lin, Shiuan-Pey</au><au>Shia, Chi-Sheng</au><au>Chang, Pei-Hua</au><au>Hou, Yu-Chi</au><au>Hsieh, Yo-Wen</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Rhubarb decreased the systemic exposure of cyclosporine, a probe substrate of P-glycoprotein and CYP 3A</atitle><jtitle>Xenobiotica</jtitle><addtitle>Xenobiotica</addtitle><date>2016-08-02</date><risdate>2016</risdate><volume>46</volume><issue>8</issue><spage>677</spage><epage>682</epage><pages>677-682</pages><issn>0049-8254</issn><eissn>1366-5928</eissn><abstract>1. Rhubarb, rhizome of Rheum palmatum L. (RP), is an important herb in clinical Chinese medicine.
2. Cyclosporine (CSP) is an immunosuppressant with narrow therapeutic window. The oral bioavailability of CSP was associated with P-glycoprotein (P-gp) and CYP 3A4. CSP was used as a probe substrate to investigate the in vivo modulation effects of RP on P-gp and CYP 3A.
3. Rats were orally administered 2.5 mg/kg of CSP with and without 0.25 and 1.0 g/kg of RP. The blood CSP concentration was determined by a specific monoclonal fluorescence polarization immunoassay.
4. Both dosages of RP significantly decreased the C
max
and AUC
0-t
of CSP in rats. Mechanism studies indicated that RP activated the functions of P-gp and CYP 3A.
5. RP ingestion reduced the systemic exposure of CSP through activating P-gp and CYP 3A.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>26634287</pmid><doi>10.3109/00498254.2015.1117159</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Xenobiotica, 2016-08, Vol.46 (8), p.677-682 |
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| language | eng |
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| source | Taylor and Francis:Jisc Collections:Taylor and Francis Read and Publish Agreement 2024-2025:Medical Collection (Reading list) |
| subjects | Animals ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism Cyclosporine Cyclosporine - pharmacology CYP 3A Cytochrome P-450 CYP3A - metabolism Drugs, Chinese Herbal - pharmacology herb-drug interaction Immunosuppressive Agents - pharmacology P-glycoprotein Rats Rheum - chemistry rhubarb |
| title | Rhubarb decreased the systemic exposure of cyclosporine, a probe substrate of P-glycoprotein and CYP 3A |
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