Synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease
Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient r...
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| Veröffentlicht in: | International journal of molecular sciences 2011-11, Vol.12 (11), p.8208-8216 |
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| container_title | International journal of molecular sciences |
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| creator | Qian, Li-Hua Li, Nian-Guang Tang, Yu-Ping Zhang, Li Tang, Hao Wang, Zhen-Jiang Liu, Li Song, Shu-Lin Guo, Jian-Ming Ding, An-Wei |
| description | Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+•), (•)OH free radicals and its protective effect on H(2)O(2)-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H(2)SO(4) in 90% ethanol in N(2) atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease. |
| doi_str_mv | 10.3390/ijms12118208 |
| format | Article |
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However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+•), (•)OH free radicals and its protective effect on H(2)O(2)-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H(2)SO(4) in 90% ethanol in N(2) atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease.</description><identifier>ISSN: 1422-0067</identifier><identifier>ISSN: 1661-6596</identifier><identifier>EISSN: 1422-0067</identifier><identifier>DOI: 10.3390/ijms12118208</identifier><identifier>PMID: 22174659</identifier><language>eng</language><publisher>Switzerland: MDPI AG</publisher><subject>Animals ; Antioxidants ; Apigenin - pharmacology ; Atmosphere ; Benzothiazoles - metabolism ; Bioavailability ; Biphenyl Compounds - metabolism ; Cell Survival - drug effects ; Cerebrovascular disease ; Cerebrovascular diseases ; Cerebrovascular Disorders - drug therapy ; Chromatography ; Cytotoxicity ; Ethanol ; Free Radical Scavengers - pharmacology ; Free radicals ; Glucuronates - pharmacology ; Hydrogen Peroxide - adverse effects ; Ischemia ; Ischemia - drug therapy ; Metabolites ; Oral administration ; PC12 Cells ; Pheochromocytoma cells ; Picrates - metabolism ; Rats ; Solubility ; Sulfonic Acids - metabolism</subject><ispartof>International journal of molecular sciences, 2011-11, Vol.12 (11), p.8208-8216</ispartof><rights>Copyright MDPI AG 2011</rights><rights>2011 by the authors; licensee MDPI, Basel, Switzerland. 2011</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c444t-228a4f161f77ffaa70db1e5248b19978b6be3fb9b5f48be979e045e544926c0d3</citedby><cites>FETCH-LOGICAL-c444t-228a4f161f77ffaa70db1e5248b19978b6be3fb9b5f48be979e045e544926c0d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC3233465/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC3233465/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,727,780,784,885,27915,27916,53782,53784</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22174659$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Qian, Li-Hua</creatorcontrib><creatorcontrib>Li, Nian-Guang</creatorcontrib><creatorcontrib>Tang, Yu-Ping</creatorcontrib><creatorcontrib>Zhang, Li</creatorcontrib><creatorcontrib>Tang, Hao</creatorcontrib><creatorcontrib>Wang, Zhen-Jiang</creatorcontrib><creatorcontrib>Liu, Li</creatorcontrib><creatorcontrib>Song, Shu-Lin</creatorcontrib><creatorcontrib>Guo, Jian-Ming</creatorcontrib><creatorcontrib>Ding, An-Wei</creatorcontrib><title>Synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease</title><title>International journal of molecular sciences</title><addtitle>Int J Mol Sci</addtitle><description>Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+•), (•)OH free radicals and its protective effect on H(2)O(2)-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H(2)SO(4) in 90% ethanol in N(2) atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease.</description><subject>Animals</subject><subject>Antioxidants</subject><subject>Apigenin - pharmacology</subject><subject>Atmosphere</subject><subject>Benzothiazoles - metabolism</subject><subject>Bioavailability</subject><subject>Biphenyl Compounds - metabolism</subject><subject>Cell Survival - drug effects</subject><subject>Cerebrovascular disease</subject><subject>Cerebrovascular diseases</subject><subject>Cerebrovascular Disorders - drug therapy</subject><subject>Chromatography</subject><subject>Cytotoxicity</subject><subject>Ethanol</subject><subject>Free Radical Scavengers - pharmacology</subject><subject>Free radicals</subject><subject>Glucuronates - pharmacology</subject><subject>Hydrogen Peroxide - adverse effects</subject><subject>Ischemia</subject><subject>Ischemia - drug therapy</subject><subject>Metabolites</subject><subject>Oral administration</subject><subject>PC12 Cells</subject><subject>Pheochromocytoma cells</subject><subject>Picrates - metabolism</subject><subject>Rats</subject><subject>Solubility</subject><subject>Sulfonic Acids - metabolism</subject><issn>1422-0067</issn><issn>1661-6596</issn><issn>1422-0067</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>8G5</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><sourceid>GUQSH</sourceid><sourceid>M2O</sourceid><recordid>eNpdkUtr3DAUhU1paR7trusi6KaLONHTsjaFEPqCQBdp10KSrzIabGsqyQND_3xkkoZpF3ogffdwzz1N847gS8YUvgrbKRNKSE9x_6I5JZzSFuNOvjy6nzRnOW8xpowK9bo5oZRI3gl12vy5O8xlAzlkZOYB2RBb40rYh3JAsDfjYkqIM4oeZbcUGEeTIMzIVBztYoG5IHO_7j4mVIXWlczusFaE7DYwBYccJLAp7k3VqAJoCBlMhjfNK2_GDG-fzvPm15fPP2--tbc_vn6_ub5tHee8tJT2hnvSES-l98ZIPFgCgvLeEqVkbzsLzFtlha9PoKQCzAUIzhXtHB7YefPpUXe32AkGV9tNZtS7FCaTDjqaoP_9mcNG38e9ZpSxOqYq8PFJIMXfC-Sip-ptHcYMccma0F7gvuMdq-iH_9BtXNJc7WkiaIexlEJW6uKRcinmnMA_N0OwXlPVx6lW_P2xgWf4b4zsAezOoMg</recordid><startdate>20111101</startdate><enddate>20111101</enddate><creator>Qian, Li-Hua</creator><creator>Li, Nian-Guang</creator><creator>Tang, Yu-Ping</creator><creator>Zhang, Li</creator><creator>Tang, Hao</creator><creator>Wang, Zhen-Jiang</creator><creator>Liu, Li</creator><creator>Song, Shu-Lin</creator><creator>Guo, Jian-Ming</creator><creator>Ding, An-Wei</creator><general>MDPI AG</general><general>Molecular Diversity Preservation International (MDPI)</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>3V.</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>8G5</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>GUQSH</scope><scope>K9.</scope><scope>M0S</scope><scope>M1P</scope><scope>M2O</scope><scope>MBDVC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope><scope>7TK</scope><scope>5PM</scope></search><sort><creationdate>20111101</creationdate><title>Synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease</title><author>Qian, Li-Hua ; 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However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+•), (•)OH free radicals and its protective effect on H(2)O(2)-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H(2)SO(4) in 90% ethanol in N(2) atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease.</abstract><cop>Switzerland</cop><pub>MDPI AG</pub><pmid>22174659</pmid><doi>10.3390/ijms12118208</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Animals Antioxidants Apigenin - pharmacology Atmosphere Benzothiazoles - metabolism Bioavailability Biphenyl Compounds - metabolism Cell Survival - drug effects Cerebrovascular disease Cerebrovascular diseases Cerebrovascular Disorders - drug therapy Chromatography Cytotoxicity Ethanol Free Radical Scavengers - pharmacology Free radicals Glucuronates - pharmacology Hydrogen Peroxide - adverse effects Ischemia Ischemia - drug therapy Metabolites Oral administration PC12 Cells Pheochromocytoma cells Picrates - metabolism Rats Solubility Sulfonic Acids - metabolism |
| title | Synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease |
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