<?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%">Kibrnesh Bezu</style></author><author><style face="normal" font="default" size="100%">Daniel Bisrat</style></author><author><style face="normal" font="default" size="100%">Kaleab Asres</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">In vivo Antimalarial Evaluation of Embelin and its Semi-Synthetic Aromatic Amine Derivatives</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%">Anti-malarial.</style></keyword><keyword><style  face="normal" font="default" size="100%">Aromatic substituted embelin</style></keyword><keyword><style  face="normal" font="default" size="100%">Embelia schimperi</style></keyword><keyword><style  face="normal" font="default" size="100%">Embelin</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">18 th June 2015</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">7</style></volume><pages><style face="normal" font="default" size="100%">7-7</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p style=&quot;text-align: justify;&quot;&gt;&lt;strong&gt;Background:&lt;/strong&gt; In less developed countries like Ethiopia, malaria is traditionally treated by remedies prepared from medicinal plants. One such plant that falls in this category is &lt;em&gt;Embelia schimperi&lt;/em&gt; Vatke whose fruits are employed for the treatment of a variety of ailments including taeniasis and malaria. &lt;strong&gt;Objective:&lt;/strong&gt; In the present study, the &lt;em&gt;in vivo &lt;/em&gt;antimalarial activity of embelin isolated from the fruits of &lt;em&gt;Embelia schimperi&lt;/em&gt; Vatke and its semi-synthetic aromatic amine derivatives was evaluated. &lt;strong&gt;Methods:&lt;/strong&gt; Silica gel column chromatography was used to isolate embelin from the ethyl acetate extract of the fruits of &lt;em&gt;E. schimperi&lt;/em&gt;. Aromatic substituted embelin derivatives were semi-synthesized by using a one-step condensation reaction of embelin with aromatic amines. The compounds were characterized based on their UV, IR, HR-ESIMS, &lt;sup&gt;1&lt;/sup&gt;H and &lt;sup&gt;13&lt;/sup&gt;C NMR and DEPT-135 spectral data. Anti-malarial activity was evaluated using a modified Peter&amp;rsquo;s 4-day suppressive test against chloroquine sensitive &lt;em&gt;Plasmodium berghei&lt;/em&gt; infection in mice. &lt;strong&gt;Results:&lt;/strong&gt; Embelin and the semi-synthetic derivatives showed significant (p&amp;lt;0.05) &lt;em&gt;in vivo &lt;/em&gt;anti-malarial activity in a dose-dependent manner with 47.8-74.7% parasite suppression at tested doses of 100-400 mg/kg. Among the compounds semi-synthesized, 5-(p-tolylamino)-2-hydroxy-3-undecylcyclohexa-2,5-diene-1,4-dione showed maximum anti-malarial activity (74.7% suppression) at a dose of 400 mg/kg. No major signs of toxicity were observed when either embelin or the semi-synthesized derivatives were administrated to mice at the highest tested dose (2 g/kg). &lt;strong&gt;Conclusion:&lt;/strong&gt; The results underline that the antimalarial activity of embelin can be improved by preparing its aromatic semi-synthetic amine derivatives without affecting the safety of the parent molecule.&lt;/p&gt;&lt;p style=&quot;text-align: justify;&quot;&gt;&lt;strong&gt;Key words:&lt;/strong&gt;&lt;em&gt;Embelia schimperi&lt;/em&gt;, Embelin, Aromatic substituted embelin, Anti-malarial.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">5</style></issue><work-type><style face="normal" font="default" size="100%">Original Article</style></work-type><section><style face="normal" font="default" size="100%">7</style></section><auth-address><style face="normal" font="default" size="100%">&lt;p style=&quot;text-align: justify;&quot;&gt;&lt;strong&gt;Kibrnesh Bezu&lt;sup&gt;1&lt;/sup&gt;, Daniel Bisrat&lt;sup&gt;1 &lt;/sup&gt;and Kaleab Asres&lt;sup&gt;1*&lt;/sup&gt;&lt;/strong&gt;&lt;/p&gt;&lt;p style=&quot;text-align: justify;&quot;&gt;&lt;sup&gt;1&lt;/sup&gt;Department of Pharmaceutical Chemistry and Pharmacognosy, School of Pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa, Ethiopia.&lt;/p&gt;</style></auth-address></record><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%">Kibrnesh Bezu</style></author><author><style face="normal" font="default" size="100%">Daniel Bisrat</style></author><author><style face="normal" font="default" size="100%">Kaleab Asres</style></author></authors></contributors><titles><title><style face="normal" font="default" size="100%">In vivo Antimalarial Evaluation of Embelin and its Semi-Synthetic Aromatic Amine Derivatives</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%">A 4-Day suppressive test</style></keyword><keyword><style  face="normal" font="default" size="100%">Antimalarial</style></keyword><keyword><style  face="normal" font="default" size="100%">Aromatic substituted embelin</style></keyword><keyword><style  face="normal" font="default" size="100%">Embelia schimperi</style></keyword><keyword><style  face="normal" font="default" size="100%">Embelin.</style></keyword></keywords><dates><year><style  face="normal" font="default" size="100%">2015</style></year><pub-dates><date><style  face="normal" font="default" size="100%">01/2015</style></date></pub-dates></dates><volume><style face="normal" font="default" size="100%">7</style></volume><pages><style face="normal" font="default" size="100%">305-310</style></pages><language><style face="normal" font="default" size="100%">eng</style></language><abstract><style face="normal" font="default" size="100%">&lt;p style=&quot;text-align: justify;&quot;&gt;&lt;strong&gt;Background: &lt;/strong&gt;In less developed countries like Ethiopia, malaria is traditionally treated by remedies prepared from medicinal plants. One such plant that falls in this category is &lt;em&gt;Embelia schimperi &lt;/em&gt;Vatke whose fruits are employed for the treatment of a variety of ailments including taeniasis and malaria. &lt;strong&gt;Objective:&lt;/strong&gt; In the present study, the &lt;em&gt;in vivo&lt;/em&gt; antimalarial activity of embelin isolated from the fruits of &lt;em&gt;Embelia schimperi&lt;/em&gt; Vatke and its semisynthetic aromatic amine derivatives was evaluated. &lt;strong&gt;Methods:&lt;/strong&gt; Silica gel column chromatography was used to isolate embelin from the ethyl acetate extract of the fruits of &lt;em&gt;E. schimperi&lt;/em&gt;. Aromatic substituted embelin derivatives were semi-synthesized by using a one-step condensation reaction of embelin with aromatic amines. The compounds were characterized based on their UV, IR, HR-ESIMS, &lt;sup&gt;1&lt;/sup&gt;H and &lt;sup&gt;13&lt;/sup&gt;C NMR and DEPT-135 spectral data. Antimalarial activity was evaluated using a modified Peter&amp;rsquo;s 4-day suppressive test against chloroquine sensitive Plasmodium berghei infection in mice. &lt;strong&gt;Results:&lt;/strong&gt; Embelin and the semi-synthetic derivatives showed significant (p&amp;lt;0.05)&lt;em&gt; in vivo&lt;/em&gt; antimalarial activity in a dose-dependent manner with 47.8-74.7% parasite suppression at tested doses of 100-400 mg/kg. Among the compounds semi-synthesized, 5-(p-tolylamino)-2-hydroxy-3-undecylcyclohexa- 2,5-diene-1,4-dione showed maximum antimalarial activity (74.7 % suppression) at a dose of 400 mg/kg. No major signs of toxicity were observed when either embelin or the semi-synthesized derivatives were administrated to mice at the highest tested dose (2 g/kg). &lt;strong&gt;Conclusion:&lt;/strong&gt; The results underline that the antimalarial activity of embelin can be improved by preparing its aromatic semi-synthetic amine derivatives without affecting the safety of the parent molecule.&lt;/p&gt;</style></abstract><issue><style face="normal" font="default" size="100%">5</style></issue><work-type><style face="normal" font="default" size="100%">Original Article</style></work-type><section><style face="normal" font="default" size="100%">305</style></section><auth-address><style face="normal" font="default" size="100%">&lt;p&gt;&lt;strong&gt;Kibrnesh Bezu, Daniel Bisrat and Kaleab Asres&lt;sup&gt;*&lt;/sup&gt; &lt;/strong&gt;&lt;/p&gt;

&lt;p&gt;Department of Pharmaceutical Chemistry and Pharmacognosy, School of Pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa, Ethiopia.&lt;/p&gt;</style></auth-address></record></records></xml>