Inhibition of Naja Nigricolis Venom Acidic Phospholipase A 2 Catalysed Hydrolysis of Ghost Red Blood Cells by Columbin
The inhibitory effects of a naturally occurring diterpenoid furanolactone, columbin, on partially purified acidic phospholipase A 2 (PLA 2) from Naja nigricolis was investigated. Columbin inhibited the N. nigricolis PLA 2 in a dose related pattern with an IC 50 value of 2.5 μM. Double reciprocal plo...
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| Veröffentlicht in: | Journal of enzyme inhibition and medicinal chemistry 2002, Vol.17 (1), p.55-60 |
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| container_title | Journal of enzyme inhibition and medicinal chemistry |
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| creator | Nok, A.J. Balogun, E. Lori, J.A. Abubakar, M.S. |
| description | The inhibitory effects of a naturally occurring diterpenoid furanolactone, columbin, on partially purified acidic phospholipase A 2 (PLA 2) from Naja nigricolis was investigated. Columbin inhibited the N. nigricolis PLA 2 in a dose related pattern with an IC 50 value of 2.5 μM. Double reciprocal plots of initial velocity data of inhibition by columbin revealed a non-competitive pattern. The K M remained constant at 19 μM, while the V max changed from 54 μmoles/min/mg to 32 μmoles/min/mg and 20 μmoles/min/mg in the presence of 2 and 10 μM of columbin, respectively. Extrapolated K i values were 3 and 6.28 μM at 2 and 10 μM inhibitor, respectively. Columbin also inhibited PLA 2 hydrolysis of ghost RBC in a dose-dependent fashion. At least 70% suppression of PLA 2 -catalysed haemolysis of RBC was observed in the presence of 2 μM columbin. |
| doi_str_mv | 10.1080/14756360290011762 |
| format | Article |
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Columbin inhibited the N. nigricolis PLA 2 in a dose related pattern with an IC 50 value of 2.5 μM. Double reciprocal plots of initial velocity data of inhibition by columbin revealed a non-competitive pattern. The K M remained constant at 19 μM, while the V max changed from 54 μmoles/min/mg to 32 μmoles/min/mg and 20 μmoles/min/mg in the presence of 2 and 10 μM of columbin, respectively. Extrapolated K i values were 3 and 6.28 μM at 2 and 10 μM inhibitor, respectively. Columbin also inhibited PLA 2 hydrolysis of ghost RBC in a dose-dependent fashion. At least 70% suppression of PLA 2 -catalysed haemolysis of RBC was observed in the presence of 2 μM columbin.</description><identifier>ISSN: 1475-6366</identifier><identifier>EISSN: 1475-6374</identifier><identifier>DOI: 10.1080/14756360290011762</identifier><language>eng</language><publisher>Informa UK Ltd</publisher><subject>Columbin ; Inhibition ; Naja Nigricolis ; Pla 2</subject><ispartof>Journal of enzyme inhibition and medicinal chemistry, 2002, Vol.17 (1), p.55-60</ispartof><rights>2002 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 2002</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c1952-340464ca54c1c143080cf1b338b432473d0074b9190fede6a1c6195d5e3adcea3</citedby><cites>FETCH-LOGICAL-c1952-340464ca54c1c143080cf1b338b432473d0074b9190fede6a1c6195d5e3adcea3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.1080/14756360290011762$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.1080/14756360290011762$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,780,784,4024,27923,27924,27925,59647,60436,61221,61402</link.rule.ids></links><search><creatorcontrib>Nok, A.J.</creatorcontrib><creatorcontrib>Balogun, E.</creatorcontrib><creatorcontrib>Lori, J.A.</creatorcontrib><creatorcontrib>Abubakar, M.S.</creatorcontrib><title>Inhibition of Naja Nigricolis Venom Acidic Phospholipase A 2 Catalysed Hydrolysis of Ghost Red Blood Cells by Columbin</title><title>Journal of enzyme inhibition and medicinal chemistry</title><description>The inhibitory effects of a naturally occurring diterpenoid furanolactone, columbin, on partially purified acidic phospholipase A 2 (PLA 2) from Naja nigricolis was investigated. Columbin inhibited the N. nigricolis PLA 2 in a dose related pattern with an IC 50 value of 2.5 μM. Double reciprocal plots of initial velocity data of inhibition by columbin revealed a non-competitive pattern. The K M remained constant at 19 μM, while the V max changed from 54 μmoles/min/mg to 32 μmoles/min/mg and 20 μmoles/min/mg in the presence of 2 and 10 μM of columbin, respectively. Extrapolated K i values were 3 and 6.28 μM at 2 and 10 μM inhibitor, respectively. Columbin also inhibited PLA 2 hydrolysis of ghost RBC in a dose-dependent fashion. At least 70% suppression of PLA 2 -catalysed haemolysis of RBC was observed in the presence of 2 μM columbin.</description><subject>Columbin</subject><subject>Inhibition</subject><subject>Naja Nigricolis</subject><subject>Pla 2</subject><issn>1475-6366</issn><issn>1475-6374</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><recordid>eNp9kFFLwzAUhYMoOKc_wLf8gWnSpOmKvsyi22BMEfW13CapzUibkVSl_96MiSDCnu7hcL9zORehS0quKJmSa8qzVDBBkpwQSjORHKHRzpsIlvHjXy3EKToLYUNIQhPKR-hz2TWmMr1xHXY1XsMG8Nq8eyOdNQG_6c61eCaNMhI_NS5sm-hvIWg8wwkuoAc7BK3wYlDeRRmZGDOPmz1-jv6ddU7hQlsbcDXgwtmPtjLdOTqpwQZ98TPH6PXh_qVYTFaP82UxW00kzdNkwjjhgktIuaSSchabyppWjE0rzhKeMUVIxquc5qTWSgugUkRQpZqBkhrYGNF9rvQuBK_rcutNC34oKSl3jyv_PS4yt3vGdLXzLXw5b1XZw2Cdrz100oSSHcJv_uCNBts3ErwuN-7Dd7HugePfIcCFgg</recordid><startdate>2002</startdate><enddate>2002</enddate><creator>Nok, A.J.</creator><creator>Balogun, E.</creator><creator>Lori, J.A.</creator><creator>Abubakar, M.S.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>2002</creationdate><title>Inhibition of Naja Nigricolis Venom Acidic Phospholipase A 2 Catalysed Hydrolysis of Ghost Red Blood Cells by Columbin</title><author>Nok, A.J. ; Balogun, E. ; Lori, J.A. ; Abubakar, M.S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c1952-340464ca54c1c143080cf1b338b432473d0074b9190fede6a1c6195d5e3adcea3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Columbin</topic><topic>Inhibition</topic><topic>Naja Nigricolis</topic><topic>Pla 2</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nok, A.J.</creatorcontrib><creatorcontrib>Balogun, E.</creatorcontrib><creatorcontrib>Lori, J.A.</creatorcontrib><creatorcontrib>Abubakar, M.S.</creatorcontrib><collection>CrossRef</collection><jtitle>Journal of enzyme inhibition and medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nok, A.J.</au><au>Balogun, E.</au><au>Lori, J.A.</au><au>Abubakar, M.S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibition of Naja Nigricolis Venom Acidic Phospholipase A 2 Catalysed Hydrolysis of Ghost Red Blood Cells by Columbin</atitle><jtitle>Journal of enzyme inhibition and medicinal chemistry</jtitle><date>2002</date><risdate>2002</risdate><volume>17</volume><issue>1</issue><spage>55</spage><epage>60</epage><pages>55-60</pages><issn>1475-6366</issn><eissn>1475-6374</eissn><abstract>The inhibitory effects of a naturally occurring diterpenoid furanolactone, columbin, on partially purified acidic phospholipase A 2 (PLA 2) from Naja nigricolis was investigated. Columbin inhibited the N. nigricolis PLA 2 in a dose related pattern with an IC 50 value of 2.5 μM. Double reciprocal plots of initial velocity data of inhibition by columbin revealed a non-competitive pattern. The K M remained constant at 19 μM, while the V max changed from 54 μmoles/min/mg to 32 μmoles/min/mg and 20 μmoles/min/mg in the presence of 2 and 10 μM of columbin, respectively. Extrapolated K i values were 3 and 6.28 μM at 2 and 10 μM inhibitor, respectively. Columbin also inhibited PLA 2 hydrolysis of ghost RBC in a dose-dependent fashion. At least 70% suppression of PLA 2 -catalysed haemolysis of RBC was observed in the presence of 2 μM columbin.</abstract><pub>Informa UK Ltd</pub><doi>10.1080/14756360290011762</doi><tpages>6</tpages></addata></record> |
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| subjects | Columbin Inhibition Naja Nigricolis Pla 2 |
| title | Inhibition of Naja Nigricolis Venom Acidic Phospholipase A 2 Catalysed Hydrolysis of Ghost Red Blood Cells by Columbin |
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