Quantitation Assay for Absorption and First-Pass Metabolism of Emodin in Isolated Rat Small Intestine Using Liquid Chromatography-Tandem Mass Spectrometry
Emodin has numerous biochemical and pharmacological activities, though information about its intestinal absorption and first-pass metabolism is scarce. The purpose of this study was to evaluate intestinal absorption and metabolism of luminally administered emodin in an isolated rat small intestine u...
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| Veröffentlicht in: | Biological & Pharmaceutical Bulletin 2007/09/01, Vol.30(9), pp.1628-1633 |
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| creator | Teng, Zeng-Hui Zhou, Si-Yuan Yang, Run-Tao Liu, Xin-You Liu, Ren-Wang Yang, Xi Zhang, Bang-Le Yang, Jing-Yue Cao, Da-Yong Mei, Qi-Bing |
| description | Emodin has numerous biochemical and pharmacological activities, though information about its intestinal absorption and first-pass metabolism is scarce. The purpose of this study was to evaluate intestinal absorption and metabolism of luminally administered emodin in an isolated rat small intestine using the method of LC/MS/MS. About 22.55% of the administered emodin appeared at the vascular side, chiefly as free emodin (12.01%), but some emodin glucuronide (8.69%) and sulfate (1.84%) were also detected. Free glucuronide (5.23%) and sulfate (1.08%) moieties were found in the luminal perfusate. This model serves as a valuable tool for understanding intestinal handling of emodin, and our results confirm absorption and first-pass metabolism of emodin in the rat small intestine. Phase II metabolic enzymes such as glucuronyl transferase or sulfate transferase may also play an important role in the first-pass metabolism of emodin in the small intestine, which may ultimately reduce the bioavailability (and thus the efficacy) of orally administered emodin. |
| doi_str_mv | 10.1248/bpb.30.1628 |
| format | Article |
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The purpose of this study was to evaluate intestinal absorption and metabolism of luminally administered emodin in an isolated rat small intestine using the method of LC/MS/MS. About 22.55% of the administered emodin appeared at the vascular side, chiefly as free emodin (12.01%), but some emodin glucuronide (8.69%) and sulfate (1.84%) were also detected. Free glucuronide (5.23%) and sulfate (1.08%) moieties were found in the luminal perfusate. This model serves as a valuable tool for understanding intestinal handling of emodin, and our results confirm absorption and first-pass metabolism of emodin in the rat small intestine. Phase II metabolic enzymes such as glucuronyl transferase or sulfate transferase may also play an important role in the first-pass metabolism of emodin in the small intestine, which may ultimately reduce the bioavailability (and thus the efficacy) of orally administered emodin.</description><identifier>ISSN: 0918-6158</identifier><identifier>EISSN: 1347-5215</identifier><identifier>DOI: 10.1248/bpb.30.1628</identifier><identifier>PMID: 17827711</identifier><language>eng</language><publisher>Japan: The Pharmaceutical Society of Japan</publisher><subject>absorption ; Animals ; Biological Availability ; Cathartics - metabolism ; Chromatography, Liquid ; emodin ; Emodin - metabolism ; first-pass metabolism ; Glucuronides - metabolism ; In Vitro Techniques ; Intestinal Absorption ; Intestine, Small - metabolism ; LC/MS/MS ; Male ; Perfusion ; Rats ; Rats, Sprague-Dawley ; small intestine ; Splanchnic Circulation - physiology ; Sulfates - metabolism ; Tandem Mass Spectrometry</subject><ispartof>Biological and Pharmaceutical Bulletin, 2007/09/01, Vol.30(9), pp.1628-1633</ispartof><rights>2007 The Pharmaceutical Society of Japan</rights><rights>Copyright Japan Science and Technology Agency 2007</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c687t-e734b9cd95ce3f0e33aa96c18c0861fa760e3c1a45c1b3aef2cdf0388d79a75c3</citedby><cites>FETCH-LOGICAL-c687t-e734b9cd95ce3f0e33aa96c18c0861fa760e3c1a45c1b3aef2cdf0388d79a75c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,1883,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17827711$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Teng, Zeng-Hui</creatorcontrib><creatorcontrib>Zhou, Si-Yuan</creatorcontrib><creatorcontrib>Yang, Run-Tao</creatorcontrib><creatorcontrib>Liu, Xin-You</creatorcontrib><creatorcontrib>Liu, Ren-Wang</creatorcontrib><creatorcontrib>Yang, Xi</creatorcontrib><creatorcontrib>Zhang, Bang-Le</creatorcontrib><creatorcontrib>Yang, Jing-Yue</creatorcontrib><creatorcontrib>Cao, Da-Yong</creatorcontrib><creatorcontrib>Mei, Qi-Bing</creatorcontrib><creatorcontrib>aDepartment of Pharmacology</creatorcontrib><creatorcontrib>cXijing Hospital</creatorcontrib><creatorcontrib>bDepartment of Pharmacy</creatorcontrib><creatorcontrib>School of Pharmacy</creatorcontrib><creatorcontrib>Tangdu Hospital</creatorcontrib><creatorcontrib>Fourth Military Medical University</creatorcontrib><title>Quantitation Assay for Absorption and First-Pass Metabolism of Emodin in Isolated Rat Small Intestine Using Liquid Chromatography-Tandem Mass Spectrometry</title><title>Biological & Pharmaceutical Bulletin</title><addtitle>Biol Pharm Bull</addtitle><description>Emodin has numerous biochemical and pharmacological activities, though information about its intestinal absorption and first-pass metabolism is scarce. The purpose of this study was to evaluate intestinal absorption and metabolism of luminally administered emodin in an isolated rat small intestine using the method of LC/MS/MS. About 22.55% of the administered emodin appeared at the vascular side, chiefly as free emodin (12.01%), but some emodin glucuronide (8.69%) and sulfate (1.84%) were also detected. Free glucuronide (5.23%) and sulfate (1.08%) moieties were found in the luminal perfusate. This model serves as a valuable tool for understanding intestinal handling of emodin, and our results confirm absorption and first-pass metabolism of emodin in the rat small intestine. Phase II metabolic enzymes such as glucuronyl transferase or sulfate transferase may also play an important role in the first-pass metabolism of emodin in the small intestine, which may ultimately reduce the bioavailability (and thus the efficacy) of orally administered emodin.</description><subject>absorption</subject><subject>Animals</subject><subject>Biological Availability</subject><subject>Cathartics - metabolism</subject><subject>Chromatography, Liquid</subject><subject>emodin</subject><subject>Emodin - metabolism</subject><subject>first-pass metabolism</subject><subject>Glucuronides - metabolism</subject><subject>In Vitro Techniques</subject><subject>Intestinal Absorption</subject><subject>Intestine, Small - metabolism</subject><subject>LC/MS/MS</subject><subject>Male</subject><subject>Perfusion</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>small intestine</subject><subject>Splanchnic Circulation - physiology</subject><subject>Sulfates - metabolism</subject><subject>Tandem Mass Spectrometry</subject><issn>0918-6158</issn><issn>1347-5215</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkU1r3DAQhk1pabZpT70XQaGX4lSybEu-dVk27cKGfiQ5i7Es72qRJUeSD_tX-murjTcNFMRomHn0zqA3y94TfEWKkn9px_aKprwu-ItsQWjJ8qog1ctsgRvC85pU_CJ7E8IBY8xwQV9nF4TxgjFCFtmfXxPYqCNE7SxahgBH1DuPlm1wfnwsgu3QtfYh5j8hBHSjIrTO6DAg16P14DptUTqb4AxE1aHfENHtAMagjY0qRG0Vug_a7tBWP0y6Q6u9dwNEt_Mw7o_5XRqgBnRzEr8dlYypq6I_vs1e9WCCene-L7P76_Xd6nu-_fFts1puc1lzFnPFaNk2smsqqWiPFaUATS0Jl5jXpAdWp5okUFaStBRUX8iux5TzjjXAKkkvs0-z7ujdw5QWFoMOUhkDVrkpiJoXFSaYJPDjf-DBTd6m3QQpy4bWFFc0UZ9nSnoXgle9GL0ewB8FweJkmEiGCZryZFiiP5w1p3ZQ3TN7digB6xlIXS3BOGvShz5PloG12hkniuSuwJhi3IhTepJPgdIyLVUmna-zziFE2Kl_g8BHLY16WqqZw-Pjp5bcgxfK0r8E1MC0</recordid><startdate>20070901</startdate><enddate>20070901</enddate><creator>Teng, Zeng-Hui</creator><creator>Zhou, Si-Yuan</creator><creator>Yang, Run-Tao</creator><creator>Liu, Xin-You</creator><creator>Liu, Ren-Wang</creator><creator>Yang, Xi</creator><creator>Zhang, Bang-Le</creator><creator>Yang, Jing-Yue</creator><creator>Cao, Da-Yong</creator><creator>Mei, Qi-Bing</creator><general>The Pharmaceutical Society of Japan</general><general>Pharmaceutical Society of Japan</general><general>Japan Science and Technology Agency</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>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U9</scope><scope>8FD</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20070901</creationdate><title>Quantitation Assay for Absorption and First-Pass Metabolism of Emodin in Isolated Rat Small Intestine Using Liquid Chromatography-Tandem Mass Spectrometry</title><author>Teng, Zeng-Hui ; 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The purpose of this study was to evaluate intestinal absorption and metabolism of luminally administered emodin in an isolated rat small intestine using the method of LC/MS/MS. About 22.55% of the administered emodin appeared at the vascular side, chiefly as free emodin (12.01%), but some emodin glucuronide (8.69%) and sulfate (1.84%) were also detected. Free glucuronide (5.23%) and sulfate (1.08%) moieties were found in the luminal perfusate. This model serves as a valuable tool for understanding intestinal handling of emodin, and our results confirm absorption and first-pass metabolism of emodin in the rat small intestine. Phase II metabolic enzymes such as glucuronyl transferase or sulfate transferase may also play an important role in the first-pass metabolism of emodin in the small intestine, which may ultimately reduce the bioavailability (and thus the efficacy) of orally administered emodin.</abstract><cop>Japan</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>17827711</pmid><doi>10.1248/bpb.30.1628</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | absorption Animals Biological Availability Cathartics - metabolism Chromatography, Liquid emodin Emodin - metabolism first-pass metabolism Glucuronides - metabolism In Vitro Techniques Intestinal Absorption Intestine, Small - metabolism LC/MS/MS Male Perfusion Rats Rats, Sprague-Dawley small intestine Splanchnic Circulation - physiology Sulfates - metabolism Tandem Mass Spectrometry |
| title | Quantitation Assay for Absorption and First-Pass Metabolism of Emodin in Isolated Rat Small Intestine Using Liquid Chromatography-Tandem Mass Spectrometry |
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