Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents
A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds 7a, 7c, 8a, 8b, 8c, 8e and 8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged s...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2009-11, Vol.19 (22), p.6447-6451 |
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container_title | Bioorganic & medicinal chemistry letters |
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creator | Kumar, Atul Maurya, Ram Awatar Sharma, Siddharth Ahmad, Pervez Singh, A.B. Bhatia, Gitika Srivastava, Arvind K. |
description | A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds
7a,
7c,
8a,
8b,
8c,
8e and
8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged streptozotocin induced diabetic rat model (STZ). Compounds
8a and
8b were showing 38.0% and 42.0% blood glucose lowering activity in db/db mice model. In vitro anti-hyperglycemic activity evaluation exhibited that compounds
8a (IC
50
=
24.5
μM) and
8b (IC
50
=
36.2
μM) are potential PTP-1B inhibitors thereby revealing their possible mechanism of anti-diabetic action. Compounds
7a,
7b,
8a,
8b,
8d,
8e and
8f have shown significant anti-dyslipidemic activity in triton induced dyslipidemia in rats. |
doi_str_mv | 10.1016/j.bmcl.2009.09.031 |
format | Article |
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7a,
7c,
8a,
8b,
8c,
8e and
8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged streptozotocin induced diabetic rat model (STZ). Compounds
8a and
8b were showing 38.0% and 42.0% blood glucose lowering activity in db/db mice model. In vitro anti-hyperglycemic activity evaluation exhibited that compounds
8a (IC
50
=
24.5
μM) and
8b (IC
50
=
36.2
μM) are potential PTP-1B inhibitors thereby revealing their possible mechanism of anti-diabetic action. Compounds
7a,
7b,
8a,
8b,
8d,
8e and
8f have shown significant anti-dyslipidemic activity in triton induced dyslipidemia in rats.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2009.09.031</identifier><identifier>PMID: 19811915</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Animals ; Anti-dyslipidemic ; Anti-hyperglycemic ; Biological and medical sciences ; Blood Glucose ; Diabetes Mellitus, Experimental - blood ; Diabetes Mellitus, Experimental - drug therapy ; Dyslipidemias - blood ; Dyslipidemias - drug therapy ; General and cellular metabolism. Vitamins ; Hypoglycemic Agents - classification ; Hypoglycemic Agents - therapeutic use ; Lipid Metabolism - drug effects ; Medical sciences ; Mice ; Mice, Inbred C57BL ; Pharmacology. Drug treatments ; PPAR gamma - metabolism ; PTP 1B ; Pyranocoumarins ; Pyranocoumarins - metabolism ; Pyranocoumarins - therapeutic use ; Rats ; Rats, Wistar ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (22), p.6447-6451</ispartof><rights>2009 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c416t-52c50046b43929018b6d701d288410aac539b9fe2df75e62b8ee994930744ef53</citedby><cites>FETCH-LOGICAL-c416t-52c50046b43929018b6d701d288410aac539b9fe2df75e62b8ee994930744ef53</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2009.09.031$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,777,781,3537,27905,27906,45976</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22092243$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19811915$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kumar, Atul</creatorcontrib><creatorcontrib>Maurya, Ram Awatar</creatorcontrib><creatorcontrib>Sharma, Siddharth</creatorcontrib><creatorcontrib>Ahmad, Pervez</creatorcontrib><creatorcontrib>Singh, A.B.</creatorcontrib><creatorcontrib>Bhatia, Gitika</creatorcontrib><creatorcontrib>Srivastava, Arvind K.</creatorcontrib><title>Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds
7a,
7c,
8a,
8b,
8c,
8e and
8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged streptozotocin induced diabetic rat model (STZ). Compounds
8a and
8b were showing 38.0% and 42.0% blood glucose lowering activity in db/db mice model. In vitro anti-hyperglycemic activity evaluation exhibited that compounds
8a (IC
50
=
24.5
μM) and
8b (IC
50
=
36.2
μM) are potential PTP-1B inhibitors thereby revealing their possible mechanism of anti-diabetic action. Compounds
7a,
7b,
8a,
8b,
8d,
8e and
8f have shown significant anti-dyslipidemic activity in triton induced dyslipidemia in rats.</description><subject>Animals</subject><subject>Anti-dyslipidemic</subject><subject>Anti-hyperglycemic</subject><subject>Biological and medical sciences</subject><subject>Blood Glucose</subject><subject>Diabetes Mellitus, Experimental - blood</subject><subject>Diabetes Mellitus, Experimental - drug therapy</subject><subject>Dyslipidemias - blood</subject><subject>Dyslipidemias - drug therapy</subject><subject>General and cellular metabolism. Vitamins</subject><subject>Hypoglycemic Agents - classification</subject><subject>Hypoglycemic Agents - therapeutic use</subject><subject>Lipid Metabolism - drug effects</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred C57BL</subject><subject>Pharmacology. Drug treatments</subject><subject>PPAR gamma - metabolism</subject><subject>PTP 1B</subject><subject>Pyranocoumarins</subject><subject>Pyranocoumarins - metabolism</subject><subject>Pyranocoumarins - therapeutic use</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1r3DAQhkVpaDZp_0APwZc2J29mZPlDJZewtEkgkBwayE3I0jjR4o-t5G3xv4-Ml-YWGBh4eeaDh7GvCGsELC6267oz7ZoDyPVcGX5gKxSFSDMB-Ue2AllAWknxdMxOQtgCoAAhPrFjlBWixHzF7h8mr_vBDPtOe9eHH8lV0tO_xLQ6hGRoEt2PLn2ZduSf28lQ50yM7BLbKbRu5-ySPlM_hs_sqNFtoC-Hfsoef_38vblJ7-6vbzdXd6kRWIxpzk0OIIpaZJJLwKoubAloeVUJBK1NnslaNsRtU-ZU8LoiklLIDEohqMmzU3a-7N354c-ewqg6Fwy1re5p2AdVRgWyKiWP5Pd3SY5YlvFoBPkCGj-E4KlRO--ilUkhqFm42qpZuJqFq7kyjENnh-37uiP7NnIwHIFvB0AHo9sm2jYu_Oc4B8m5yCJ3uXAUrf115FUwjnpD1nkyo7KDe--PVxaXnX8</recordid><startdate>20091115</startdate><enddate>20091115</enddate><creator>Kumar, Atul</creator><creator>Maurya, Ram Awatar</creator><creator>Sharma, Siddharth</creator><creator>Ahmad, Pervez</creator><creator>Singh, A.B.</creator><creator>Bhatia, Gitika</creator><creator>Srivastava, Arvind K.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20091115</creationdate><title>Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents</title><author>Kumar, Atul ; Maurya, Ram Awatar ; Sharma, Siddharth ; Ahmad, Pervez ; Singh, A.B. ; Bhatia, Gitika ; Srivastava, Arvind K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c416t-52c50046b43929018b6d701d288410aac539b9fe2df75e62b8ee994930744ef53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Animals</topic><topic>Anti-dyslipidemic</topic><topic>Anti-hyperglycemic</topic><topic>Biological and medical sciences</topic><topic>Blood Glucose</topic><topic>Diabetes Mellitus, Experimental - blood</topic><topic>Diabetes Mellitus, Experimental - drug therapy</topic><topic>Dyslipidemias - blood</topic><topic>Dyslipidemias - drug therapy</topic><topic>General and cellular metabolism. Vitamins</topic><topic>Hypoglycemic Agents - classification</topic><topic>Hypoglycemic Agents - therapeutic use</topic><topic>Lipid Metabolism - drug effects</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred C57BL</topic><topic>Pharmacology. Drug treatments</topic><topic>PPAR gamma - metabolism</topic><topic>PTP 1B</topic><topic>Pyranocoumarins</topic><topic>Pyranocoumarins - metabolism</topic><topic>Pyranocoumarins - therapeutic use</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kumar, Atul</creatorcontrib><creatorcontrib>Maurya, Ram Awatar</creatorcontrib><creatorcontrib>Sharma, Siddharth</creatorcontrib><creatorcontrib>Ahmad, Pervez</creatorcontrib><creatorcontrib>Singh, A.B.</creatorcontrib><creatorcontrib>Bhatia, Gitika</creatorcontrib><creatorcontrib>Srivastava, Arvind K.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kumar, Atul</au><au>Maurya, Ram Awatar</au><au>Sharma, Siddharth</au><au>Ahmad, Pervez</au><au>Singh, A.B.</au><au>Bhatia, Gitika</au><au>Srivastava, Arvind K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2009-11-15</date><risdate>2009</risdate><volume>19</volume><issue>22</issue><spage>6447</spage><epage>6451</epage><pages>6447-6451</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds
7a,
7c,
8a,
8b,
8c,
8e and
8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged streptozotocin induced diabetic rat model (STZ). Compounds
8a and
8b were showing 38.0% and 42.0% blood glucose lowering activity in db/db mice model. In vitro anti-hyperglycemic activity evaluation exhibited that compounds
8a (IC
50
=
24.5
μM) and
8b (IC
50
=
36.2
μM) are potential PTP-1B inhibitors thereby revealing their possible mechanism of anti-diabetic action. Compounds
7a,
7b,
8a,
8b,
8d,
8e and
8f have shown significant anti-dyslipidemic activity in triton induced dyslipidemia in rats.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19811915</pmid><doi>10.1016/j.bmcl.2009.09.031</doi><tpages>5</tpages></addata></record> |
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source | MEDLINE; Elsevier ScienceDirect Journals |
subjects | Animals Anti-dyslipidemic Anti-hyperglycemic Biological and medical sciences Blood Glucose Diabetes Mellitus, Experimental - blood Diabetes Mellitus, Experimental - drug therapy Dyslipidemias - blood Dyslipidemias - drug therapy General and cellular metabolism. Vitamins Hypoglycemic Agents - classification Hypoglycemic Agents - therapeutic use Lipid Metabolism - drug effects Medical sciences Mice Mice, Inbred C57BL Pharmacology. Drug treatments PPAR gamma - metabolism PTP 1B Pyranocoumarins Pyranocoumarins - metabolism Pyranocoumarins - therapeutic use Rats Rats, Wistar Structure-Activity Relationship |
title | Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents |
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