Comparison between Chinese medical herb Pueraria lobata crude extract and its main isoflavone puerarin : Antioxidant properties and effects on rat liver CYP-catalysed drug metabolism
Ge-gen ( Radix Puerariae; RP) is used in traditional oriental medicine for various medicinal purposes. The drug is the root of a wild leguminous creeper, Pueraria lobata (Willd) Ohwi. It possesses a high content of flavonoid derivatives, the most abundant of which is puerarin (PU). Here, using the e...
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| Veröffentlicht in: | Life sciences (1973) 2000-11, Vol.67 (24), p.2997-3006 |
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| creator | Guerra, M.C. Speroni, E. Broccoli, M. Cangini, M. Pasini, P. Minghetti, A. Crespi-Perellino, N. Mirasoli, M. Cantelli-Forti, G. Paolini, M. |
| description | Ge-gen (
Radix Puerariae; RP) is used in traditional oriental medicine for various medicinal purposes. The drug is the root of a wild leguminous creeper,
Pueraria lobata (Willd) Ohwi. It possesses a high content of flavonoid derivatives, the most abundant of which is puerarin (PU). Here, using the enhanced chemiluminescence technique based on horseradish peroxidase and a luminol-oxidant-enhancer reagent, we evaluated
in vitro the antioxidant activity of PU and RP crude extract. Both biological samples inhibited the steady-state chemiluminescent reaction in a dose-dependent fashion. However, different inhibition mechanism were postulated, since only RP behaved like conventional antioxidants. This activity was supposed to be due the presence of compounds other than PU in the crude extract. Using each of the specific substrates to different cytochrome P450 (CYP) isoforms or the regio- and stereo-selective hydroxylation of testosterone as polyfunctional probe we found that when intragastrically administered in male Wistar rats, PU (100 or 200 mg/kg b.w.) and RP (700 or 1,400 mg/kg b.w.) significantly altered hepatic CYP-linked monooxygenases. While both CYP content and NADPH-(CYP)-c-reductase activity were significantly increased in all situations, a complex pattern of CYP modulation was observed, including both induction (PU: CYP2A1, 1A1/2, 3A1, 2C11; RP: CYP1A2, 3A1, 2B1) and inactivation (PU and RP: CYP3A, 2E1, 2B1), the latter being due to either parental agents or metabolites, as demonstrated by
in vitro studies. Overall, these findings indicate that RP contains compounds with potent antioxidant activity and that both PU and RP impairs CYP-catalysed drug metabolism. |
| doi_str_mv | 10.1016/S0024-3205(00)00885-7 |
| format | Article |
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Radix Puerariae; RP) is used in traditional oriental medicine for various medicinal purposes. The drug is the root of a wild leguminous creeper,
Pueraria lobata (Willd) Ohwi. It possesses a high content of flavonoid derivatives, the most abundant of which is puerarin (PU). Here, using the enhanced chemiluminescence technique based on horseradish peroxidase and a luminol-oxidant-enhancer reagent, we evaluated
in vitro the antioxidant activity of PU and RP crude extract. Both biological samples inhibited the steady-state chemiluminescent reaction in a dose-dependent fashion. However, different inhibition mechanism were postulated, since only RP behaved like conventional antioxidants. This activity was supposed to be due the presence of compounds other than PU in the crude extract. Using each of the specific substrates to different cytochrome P450 (CYP) isoforms or the regio- and stereo-selective hydroxylation of testosterone as polyfunctional probe we found that when intragastrically administered in male Wistar rats, PU (100 or 200 mg/kg b.w.) and RP (700 or 1,400 mg/kg b.w.) significantly altered hepatic CYP-linked monooxygenases. While both CYP content and NADPH-(CYP)-c-reductase activity were significantly increased in all situations, a complex pattern of CYP modulation was observed, including both induction (PU: CYP2A1, 1A1/2, 3A1, 2C11; RP: CYP1A2, 3A1, 2B1) and inactivation (PU and RP: CYP3A, 2E1, 2B1), the latter being due to either parental agents or metabolites, as demonstrated by
in vitro studies. Overall, these findings indicate that RP contains compounds with potent antioxidant activity and that both PU and RP impairs CYP-catalysed drug metabolism.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/S0024-3205(00)00885-7</identifier><identifier>PMID: 11133012</identifier><language>eng</language><publisher>Netherlands: Elsevier Inc</publisher><subject>Animals ; Antioxidant activity ; Antioxidants - pharmacology ; Chromatography, High Pressure Liquid ; Chromatography, Thin Layer ; Cytochrome P-450 Enzyme System - metabolism ; Cytochrome P450 ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal - analysis ; Drugs, Chinese Herbal - pharmacology ; Free radicals ; In Vitro Techniques ; Isoflavones - isolation & purification ; Isoflavones - pharmacology ; Luminescent Measurements ; Male ; Microsomes, Liver - drug effects ; Microsomes, Liver - enzymology ; Pueraria lobata ; Rats ; Rats, Sprague-Dawley</subject><ispartof>Life sciences (1973), 2000-11, Vol.67 (24), p.2997-3006</ispartof><rights>2000 Elsevier Science Inc.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c315t-ec9f68c98d8273a32a0aa54115a2bfb856bbb5accd6043059522688544cee8fa3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0024-3205(00)00885-7$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11133012$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Guerra, M.C.</creatorcontrib><creatorcontrib>Speroni, E.</creatorcontrib><creatorcontrib>Broccoli, M.</creatorcontrib><creatorcontrib>Cangini, M.</creatorcontrib><creatorcontrib>Pasini, P.</creatorcontrib><creatorcontrib>Minghetti, A.</creatorcontrib><creatorcontrib>Crespi-Perellino, N.</creatorcontrib><creatorcontrib>Mirasoli, M.</creatorcontrib><creatorcontrib>Cantelli-Forti, G.</creatorcontrib><creatorcontrib>Paolini, M.</creatorcontrib><title>Comparison between Chinese medical herb Pueraria lobata crude extract and its main isoflavone puerarin : Antioxidant properties and effects on rat liver CYP-catalysed drug metabolism</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>Ge-gen (
Radix Puerariae; RP) is used in traditional oriental medicine for various medicinal purposes. The drug is the root of a wild leguminous creeper,
Pueraria lobata (Willd) Ohwi. It possesses a high content of flavonoid derivatives, the most abundant of which is puerarin (PU). Here, using the enhanced chemiluminescence technique based on horseradish peroxidase and a luminol-oxidant-enhancer reagent, we evaluated
in vitro the antioxidant activity of PU and RP crude extract. Both biological samples inhibited the steady-state chemiluminescent reaction in a dose-dependent fashion. However, different inhibition mechanism were postulated, since only RP behaved like conventional antioxidants. This activity was supposed to be due the presence of compounds other than PU in the crude extract. Using each of the specific substrates to different cytochrome P450 (CYP) isoforms or the regio- and stereo-selective hydroxylation of testosterone as polyfunctional probe we found that when intragastrically administered in male Wistar rats, PU (100 or 200 mg/kg b.w.) and RP (700 or 1,400 mg/kg b.w.) significantly altered hepatic CYP-linked monooxygenases. While both CYP content and NADPH-(CYP)-c-reductase activity were significantly increased in all situations, a complex pattern of CYP modulation was observed, including both induction (PU: CYP2A1, 1A1/2, 3A1, 2C11; RP: CYP1A2, 3A1, 2B1) and inactivation (PU and RP: CYP3A, 2E1, 2B1), the latter being due to either parental agents or metabolites, as demonstrated by
in vitro studies. Overall, these findings indicate that RP contains compounds with potent antioxidant activity and that both PU and RP impairs CYP-catalysed drug metabolism.</description><subject>Animals</subject><subject>Antioxidant activity</subject><subject>Antioxidants - pharmacology</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Chromatography, Thin Layer</subject><subject>Cytochrome P-450 Enzyme System - metabolism</subject><subject>Cytochrome P450</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drugs, Chinese Herbal - analysis</subject><subject>Drugs, Chinese Herbal - pharmacology</subject><subject>Free radicals</subject><subject>In Vitro Techniques</subject><subject>Isoflavones - isolation & purification</subject><subject>Isoflavones - pharmacology</subject><subject>Luminescent Measurements</subject><subject>Male</subject><subject>Microsomes, Liver - drug effects</subject><subject>Microsomes, Liver - enzymology</subject><subject>Pueraria lobata</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kU9v1DAQxS0EotvCRwD5hOghMLbjJMsFVRH_pEpUAg6crLEzoUaJs9jO0n4xPh_ubuE0l9-befMeY88EvBIgmtdfAGRdKQn6JcA5QNfpqn3ANqJrtxU0Sjxkm__ICTtN6ScAaN2qx-xECKEUCLlhf_pl3mH0aQncUv5NFHh_7QMl4jMN3uHErylafrVSLBzyabGYkbu4DsTpJkd0mWMYuM-Jz-gDL8vGCfdLIL47qgJ_wy9C9suNHzBkvovLjmL2lA5KGkdyRV08RMx88nuKvP9-VblyabpNNPAhrj-KoYx2mXyan7BHI06Jnt7PM_bt_buv_cfq8vOHT_3FZeWU0Lkitx2bzm27oZOtQiUREHUthEZpR9vpxlqr0bmhgVqB3mopm5JkXTuibkR1xl4c9xbHv1ZK2cw-OZomDLSsybRSi1rJpoDP78HVltzMLvoZ4635l3QB3h4BKnb3nqJJzlNwJeNYnjfD4o0Ac9etOXRr7oozAObQrWnVX3LVmUQ</recordid><startdate>20001103</startdate><enddate>20001103</enddate><creator>Guerra, M.C.</creator><creator>Speroni, E.</creator><creator>Broccoli, M.</creator><creator>Cangini, M.</creator><creator>Pasini, P.</creator><creator>Minghetti, A.</creator><creator>Crespi-Perellino, N.</creator><creator>Mirasoli, M.</creator><creator>Cantelli-Forti, G.</creator><creator>Paolini, M.</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>20001103</creationdate><title>Comparison between Chinese medical herb Pueraria lobata crude extract and its main isoflavone puerarin : Antioxidant properties and effects on rat liver CYP-catalysed drug metabolism</title><author>Guerra, M.C. ; Speroni, E. ; Broccoli, M. ; Cangini, M. ; Pasini, P. ; Minghetti, A. ; Crespi-Perellino, N. ; Mirasoli, M. ; Cantelli-Forti, G. ; Paolini, M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c315t-ec9f68c98d8273a32a0aa54115a2bfb856bbb5accd6043059522688544cee8fa3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Animals</topic><topic>Antioxidant activity</topic><topic>Antioxidants - pharmacology</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Chromatography, Thin Layer</topic><topic>Cytochrome P-450 Enzyme System - metabolism</topic><topic>Cytochrome P450</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drugs, Chinese Herbal - analysis</topic><topic>Drugs, Chinese Herbal - pharmacology</topic><topic>Free radicals</topic><topic>In Vitro Techniques</topic><topic>Isoflavones - isolation & purification</topic><topic>Isoflavones - pharmacology</topic><topic>Luminescent Measurements</topic><topic>Male</topic><topic>Microsomes, Liver - drug effects</topic><topic>Microsomes, Liver - enzymology</topic><topic>Pueraria lobata</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Guerra, M.C.</creatorcontrib><creatorcontrib>Speroni, E.</creatorcontrib><creatorcontrib>Broccoli, M.</creatorcontrib><creatorcontrib>Cangini, M.</creatorcontrib><creatorcontrib>Pasini, P.</creatorcontrib><creatorcontrib>Minghetti, A.</creatorcontrib><creatorcontrib>Crespi-Perellino, N.</creatorcontrib><creatorcontrib>Mirasoli, M.</creatorcontrib><creatorcontrib>Cantelli-Forti, G.</creatorcontrib><creatorcontrib>Paolini, M.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Guerra, M.C.</au><au>Speroni, E.</au><au>Broccoli, M.</au><au>Cangini, M.</au><au>Pasini, P.</au><au>Minghetti, A.</au><au>Crespi-Perellino, N.</au><au>Mirasoli, M.</au><au>Cantelli-Forti, G.</au><au>Paolini, M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Comparison between Chinese medical herb Pueraria lobata crude extract and its main isoflavone puerarin : Antioxidant properties and effects on rat liver CYP-catalysed drug metabolism</atitle><jtitle>Life sciences (1973)</jtitle><addtitle>Life Sci</addtitle><date>2000-11-03</date><risdate>2000</risdate><volume>67</volume><issue>24</issue><spage>2997</spage><epage>3006</epage><pages>2997-3006</pages><issn>0024-3205</issn><eissn>1879-0631</eissn><abstract>Ge-gen (
Radix Puerariae; RP) is used in traditional oriental medicine for various medicinal purposes. The drug is the root of a wild leguminous creeper,
Pueraria lobata (Willd) Ohwi. It possesses a high content of flavonoid derivatives, the most abundant of which is puerarin (PU). Here, using the enhanced chemiluminescence technique based on horseradish peroxidase and a luminol-oxidant-enhancer reagent, we evaluated
in vitro the antioxidant activity of PU and RP crude extract. Both biological samples inhibited the steady-state chemiluminescent reaction in a dose-dependent fashion. However, different inhibition mechanism were postulated, since only RP behaved like conventional antioxidants. This activity was supposed to be due the presence of compounds other than PU in the crude extract. Using each of the specific substrates to different cytochrome P450 (CYP) isoforms or the regio- and stereo-selective hydroxylation of testosterone as polyfunctional probe we found that when intragastrically administered in male Wistar rats, PU (100 or 200 mg/kg b.w.) and RP (700 or 1,400 mg/kg b.w.) significantly altered hepatic CYP-linked monooxygenases. While both CYP content and NADPH-(CYP)-c-reductase activity were significantly increased in all situations, a complex pattern of CYP modulation was observed, including both induction (PU: CYP2A1, 1A1/2, 3A1, 2C11; RP: CYP1A2, 3A1, 2B1) and inactivation (PU and RP: CYP3A, 2E1, 2B1), the latter being due to either parental agents or metabolites, as demonstrated by
in vitro studies. Overall, these findings indicate that RP contains compounds with potent antioxidant activity and that both PU and RP impairs CYP-catalysed drug metabolism.</abstract><cop>Netherlands</cop><pub>Elsevier Inc</pub><pmid>11133012</pmid><doi>10.1016/S0024-3205(00)00885-7</doi><tpages>10</tpages></addata></record> |
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| subjects | Animals Antioxidant activity Antioxidants - pharmacology Chromatography, High Pressure Liquid Chromatography, Thin Layer Cytochrome P-450 Enzyme System - metabolism Cytochrome P450 Dose-Response Relationship, Drug Drugs, Chinese Herbal - analysis Drugs, Chinese Herbal - pharmacology Free radicals In Vitro Techniques Isoflavones - isolation & purification Isoflavones - pharmacology Luminescent Measurements Male Microsomes, Liver - drug effects Microsomes, Liver - enzymology Pueraria lobata Rats Rats, Sprague-Dawley |
| title | Comparison between Chinese medical herb Pueraria lobata crude extract and its main isoflavone puerarin : Antioxidant properties and effects on rat liver CYP-catalysed drug metabolism |
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