<?xml version="1.0" encoding="UTF-8"?><xml><records><record><source-app name="Biblio" version="7.x">Drupal-Biblio</source-app><ref-type>17</ref-type><contributors><authors><author><style face="normal" font="default" size="100%">Augustine A. Ahmadu</style></author><author><style face="normal" font="default" size="100%">Bilqis A. Lawal</style></author><author><style face="normal" font="default" size="100%">Anas Haruna</style></author><author><style face="normal" font="default" size="100%">Lukman Mustapha</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">Tetrahydroxy Flavone from Acacia auriculiformis A. Cunn Ex Benth. (Fabaceae) with Novel Kinase Activity</style></title><secondary-title><style face="normal" font="default" size="100%">Pharmacognosy Journal</style></secondary-title></titles><keywords><keyword><style  face="normal" font="default" size="100%">CDK9</style></keyword><keyword><style  face="normal" font="default" size="100%">DYRK1A</style></keyword><keyword><style  face="normal" font="default" size="100%">Protein kinases</style></keyword><keyword><style  face="normal" font="default" size="100%">Tetrahydroxyflavone</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2019</style></year><pub-dates><date><style  face="normal" font="default" size="100%">May 2019</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">11</style></volume><pages><style face="normal" font="default" size="100%">559-563</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p class=&quot;rtejustify&quot;&gt;&lt;strong&gt;Background:&lt;/strong&gt; The decoctions of the bark of &lt;em&gt;Acacia auriculiformis&lt;/em&gt; are used in folkloric medicine to relieve pain and inflammation and as remedy for cancer. &lt;strong&gt;Objective: &lt;/strong&gt;The aim of this work is to screen the extract and fractions of &lt;em&gt;Acacia auriculiformis&lt;/em&gt; for protein kinase inhibitory activity and also to isolate and characterize chemical entities from this plant and evaluate their protein kinase inhibitory activity. &lt;strong&gt;Materials and Methods: &lt;/strong&gt;Kinase inhibitory activity were assayed in appropriate buffer, with either protein or peptide as substrate in the presence of 15&lt;em&gt;μ&lt;/em&gt;M (33-P) ATP (3,000Ci/mmol; 10mCi/ml) in a final volume of 30&lt;em&gt;μ&lt;/em&gt;L. Controls were performed with appropriate dilutions of dimethyl sulphoxide. A portion of the Chloroform extract, ethylacetate and n-butanol soluble fractions of the stem bark of &lt;em&gt;Acacia auriculiformis&lt;/em&gt; were screened against a panel of disease-related protein kinases and the active fractions was tested over a wide range of concentrations from 0.016 to 50&lt;em&gt;μ&lt;/em&gt;g/ml and the IC&lt;sub&gt;50&lt;/sub&gt; values were determined from the dose response curve. The most active fraction was subjected to chromatographic separation using Silica gel G column chromatography and sephadex LH-20 to give compound I. The structure of the isolated compound was elucidated using NMR and LCMS. &lt;strong&gt;Results:&lt;/strong&gt; The Primary screening of the extract and fractions showed that the chloroform extract was inactive against all the protein kinases investigated, while the ethylacetate and n-butanol soluble fractions inhibited all the protein kinases tested. Compound I also inhibited all the kinases tested. The IC&lt;sub&gt;50&lt;/sub&gt; of the active fractions and compound were also evaluated. Ethylacetate fraction inhibited all the kinases tested with the highest activity against Haspine kinase with IC&lt;sub&gt;50&lt;/sub&gt; of 1.0 &lt;em&gt;μ&lt;/em&gt;g/ml, while n-butanol also gave the highest activity against Haspine kinase with 1C&lt;sub&gt;50 &lt;/sub&gt;of 1.3 &lt;em&gt;μ&lt;/em&gt;g/ml. From the active ethylacetate fractions 3, 4’, 7, 8- tetrahydroxy flavone was isolated. The Compound exhibited the maximal activity against DYRK1A kinase with an IC&lt;sub&gt;50&lt;/sub&gt; of 2.05 &lt;em&gt;μ&lt;/em&gt;g/ml followed by CDK9 with an IC&lt;sub&gt;50&lt;/sub&gt; of 2.28 &lt;em&gt;μ&lt;/em&gt;g/ml. &lt;strong&gt;Conclusion:&lt;/strong&gt; 3, 4’,7, 8- tetrahydroxy flavone was isolated was found to be a DYRK1A and CDK9 inhibitor which might justify the anticancer potential of this plant.&lt;/p&gt;
</style></abstract><issue><style face="normal" font="default" size="100%">3</style></issue><work-type><style face="normal" font="default" size="100%">Original Article</style></work-type><section><style face="normal" font="default" size="100%">559</style></section><auth-address><style face="normal" font="default" size="100%">&lt;p class=&quot;rtejustify&quot;&gt;&lt;strong&gt;Augustine A. Ahmadu&lt;sup&gt;1,*&lt;/sup&gt;, Bilqis A. Lawal&lt;sup&gt;2&lt;/sup&gt;, Anas Haruna&lt;sup&gt;1&lt;/sup&gt;, Lukman Mustapha&lt;sup&gt;1&lt;/sup&gt; &lt;/strong&gt;&lt;/p&gt;

&lt;p class=&quot;rtejustify&quot;&gt;&lt;sup&gt;1&lt;/sup&gt;Department of Pharm and Medicinal Chemistry, Kaduna State University, Tafawa Balewa Road, Kabala Costain, Kaduna, NIGERIA.&lt;/p&gt;

&lt;p class=&quot;rtejustify&quot;&gt;&lt;sup&gt;2&lt;/sup&gt;Department of Pharmacognosy and Drug Development, University of Ilorin, Ilorin, Kwara, NIGERIA.&lt;/p&gt;
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