Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi
[Display omitted] Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicida...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2016-04, Vol.26 (7), p.1772-1775 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Sandjo, Louis P. de Moraes, Milene H. Kuete, Victor Kamdoum, Blaise C. Ngadjui, Bonaventure T. Steindel, Mario |
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Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2–4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70μg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14μg/mL. In addition, antiprotozoal effect of mixtures of 1–6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63μg/mL) was combined with 1 in ratios 1:1 (10.01μg/mL) and 3:1 (7.78μg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3). |
| doi_str_mv | 10.1016/j.bmcl.2016.02.044 |
| format | Article |
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Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2–4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70μg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14μg/mL. In addition, antiprotozoal effect of mixtures of 1–6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63μg/mL) was combined with 1 in ratios 1:1 (10.01μg/mL) and 3:1 (7.78μg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3).</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2016.02.044</identifier><identifier>PMID: 26906638</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Activity in combination ; Alkaloids - chemistry ; Alkaloids - pharmacology ; Anthraquinones - chemistry ; Anthraquinones - pharmacology ; Antiparasitic Agents - chemistry ; Antiparasitic Agents - pharmacology ; Antiparasitic effect ; Antiprotozoal Agents - chemistry ; Antiprotozoal Agents - pharmacology ; Chagas Disease - drug therapy ; Chalcones - chemistry ; Chalcones - pharmacology ; Flavanones - chemistry ; Flavanones - pharmacology ; Humans ; Leishmania amazonensis ; Leishmania mexicana - drug effects ; Leishmaniasis, Cutaneous - drug therapy ; Moraceae - chemistry ; Plant Extracts - chemistry ; Plant Extracts - pharmacology ; Plants - chemistry ; Rubiaceae - chemistry ; Secondary metabolites ; Structure-Activity Relationship ; Trypanocidal Agents - chemistry ; Trypanocidal Agents - pharmacology ; Trypanosoma cruzi ; Trypanosoma cruzi - drug effects ; Zanthoxylum - chemistry</subject><ispartof>Bioorganic & medicinal chemistry letters, 2016-04, Vol.26 (7), p.1772-1775</ispartof><rights>2016 Elsevier Ltd</rights><rights>Copyright © 2016 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c508t-43d3c79fd13231661451eb9e5b0dbace2361467c5847e427f72950775ed404183</citedby><cites>FETCH-LOGICAL-c508t-43d3c79fd13231661451eb9e5b0dbace2361467c5847e427f72950775ed404183</cites><orcidid>0000-0001-5840-7733</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2016.02.044$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27929,27930,46000</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26906638$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sandjo, Louis P.</creatorcontrib><creatorcontrib>de Moraes, Milene H.</creatorcontrib><creatorcontrib>Kuete, Victor</creatorcontrib><creatorcontrib>Kamdoum, Blaise C.</creatorcontrib><creatorcontrib>Ngadjui, Bonaventure T.</creatorcontrib><creatorcontrib>Steindel, Mario</creatorcontrib><title>Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2–4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70μg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14μg/mL. In addition, antiprotozoal effect of mixtures of 1–6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63μg/mL) was combined with 1 in ratios 1:1 (10.01μg/mL) and 3:1 (7.78μg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3).</description><subject>Activity in combination</subject><subject>Alkaloids - chemistry</subject><subject>Alkaloids - pharmacology</subject><subject>Anthraquinones - chemistry</subject><subject>Anthraquinones - pharmacology</subject><subject>Antiparasitic Agents - chemistry</subject><subject>Antiparasitic Agents - pharmacology</subject><subject>Antiparasitic effect</subject><subject>Antiprotozoal Agents - chemistry</subject><subject>Antiprotozoal Agents - pharmacology</subject><subject>Chagas Disease - drug therapy</subject><subject>Chalcones - chemistry</subject><subject>Chalcones - pharmacology</subject><subject>Flavanones - chemistry</subject><subject>Flavanones - pharmacology</subject><subject>Humans</subject><subject>Leishmania amazonensis</subject><subject>Leishmania mexicana - drug effects</subject><subject>Leishmaniasis, Cutaneous - drug therapy</subject><subject>Moraceae - chemistry</subject><subject>Plant Extracts - chemistry</subject><subject>Plant Extracts - pharmacology</subject><subject>Plants - chemistry</subject><subject>Rubiaceae - chemistry</subject><subject>Secondary metabolites</subject><subject>Structure-Activity Relationship</subject><subject>Trypanocidal Agents - chemistry</subject><subject>Trypanocidal Agents - pharmacology</subject><subject>Trypanosoma cruzi</subject><subject>Trypanosoma cruzi - drug effects</subject><subject>Zanthoxylum - chemistry</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkU1v1DAQhi0EotvCH-CAfOSSYDuOnUhcUAW00kpcisTNcuwJzCqOg51UdH89XrZwRJz89cxrzTyEvOKs5oyrt4d6CG6qRdnXTNRMyidkx6WSVSNZ-5TsWK9Y1fXy6wW5zPnAGJcFek4uhOqZUk23I8fb2eM9-s1O1M6euhgGnMGXw4qLTTbjio7COIJbaRxpxp90mcorDbDaIU64Qqb2m8U5r3QPmL8HO6OlNthjnGHOmH8n36WHxc4xx2CpS9sRX5Bno50yvHxcr8iXjx_urm-q_edPt9fv95VrWbdWsvGN0_3oeSMarhSXLYehh3ZgfrAORFOulHZtJzVIoUct-pZp3YIv3fKuuSJvzrlLij82yKsJmB1MpQmIWzZc96xvlWyb_0C1KP9L3RdUnFGXYs4JRrMkDDY9GM7MSY85mJMec9JjmDBl8qXo9WP-NgTwf0v--CjAuzMAZSD3CMlkhzA78JiKAOMj_iv_Fzd0ohM</recordid><startdate>20160401</startdate><enddate>20160401</enddate><creator>Sandjo, Louis P.</creator><creator>de Moraes, Milene H.</creator><creator>Kuete, Victor</creator><creator>Kamdoum, Blaise C.</creator><creator>Ngadjui, Bonaventure T.</creator><creator>Steindel, Mario</creator><general>Elsevier Ltd</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>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>M7N</scope><scope>P64</scope><orcidid>https://orcid.org/0000-0001-5840-7733</orcidid></search><sort><creationdate>20160401</creationdate><title>Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi</title><author>Sandjo, Louis P. ; de Moraes, Milene H. ; Kuete, Victor ; Kamdoum, Blaise C. ; Ngadjui, Bonaventure T. ; Steindel, Mario</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c508t-43d3c79fd13231661451eb9e5b0dbace2361467c5847e427f72950775ed404183</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Activity in combination</topic><topic>Alkaloids - chemistry</topic><topic>Alkaloids - pharmacology</topic><topic>Anthraquinones - chemistry</topic><topic>Anthraquinones - pharmacology</topic><topic>Antiparasitic Agents - chemistry</topic><topic>Antiparasitic Agents - pharmacology</topic><topic>Antiparasitic effect</topic><topic>Antiprotozoal Agents - chemistry</topic><topic>Antiprotozoal Agents - pharmacology</topic><topic>Chagas Disease - drug therapy</topic><topic>Chalcones - chemistry</topic><topic>Chalcones - pharmacology</topic><topic>Flavanones - chemistry</topic><topic>Flavanones - pharmacology</topic><topic>Humans</topic><topic>Leishmania amazonensis</topic><topic>Leishmania mexicana - drug effects</topic><topic>Leishmaniasis, Cutaneous - drug therapy</topic><topic>Moraceae - chemistry</topic><topic>Plant Extracts - chemistry</topic><topic>Plant Extracts - pharmacology</topic><topic>Plants - chemistry</topic><topic>Rubiaceae - chemistry</topic><topic>Secondary metabolites</topic><topic>Structure-Activity Relationship</topic><topic>Trypanocidal Agents - chemistry</topic><topic>Trypanocidal Agents - pharmacology</topic><topic>Trypanosoma cruzi</topic><topic>Trypanosoma cruzi - drug effects</topic><topic>Zanthoxylum - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sandjo, Louis P.</creatorcontrib><creatorcontrib>de Moraes, Milene H.</creatorcontrib><creatorcontrib>Kuete, Victor</creatorcontrib><creatorcontrib>Kamdoum, Blaise C.</creatorcontrib><creatorcontrib>Ngadjui, Bonaventure T.</creatorcontrib><creatorcontrib>Steindel, Mario</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sandjo, Louis P.</au><au>de Moraes, Milene H.</au><au>Kuete, Victor</au><au>Kamdoum, Blaise C.</au><au>Ngadjui, Bonaventure T.</au><au>Steindel, Mario</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2016-04-01</date><risdate>2016</risdate><volume>26</volume><issue>7</issue><spage>1772</spage><epage>1775</epage><pages>1772-1775</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2–4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70μg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14μg/mL. In addition, antiprotozoal effect of mixtures of 1–6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63μg/mL) was combined with 1 in ratios 1:1 (10.01μg/mL) and 3:1 (7.78μg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3).</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>26906638</pmid><doi>10.1016/j.bmcl.2016.02.044</doi><tpages>4</tpages><orcidid>https://orcid.org/0000-0001-5840-7733</orcidid></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2016-04, Vol.26 (7), p.1772-1775 |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Activity in combination Alkaloids - chemistry Alkaloids - pharmacology Anthraquinones - chemistry Anthraquinones - pharmacology Antiparasitic Agents - chemistry Antiparasitic Agents - pharmacology Antiparasitic effect Antiprotozoal Agents - chemistry Antiprotozoal Agents - pharmacology Chagas Disease - drug therapy Chalcones - chemistry Chalcones - pharmacology Flavanones - chemistry Flavanones - pharmacology Humans Leishmania amazonensis Leishmania mexicana - drug effects Leishmaniasis, Cutaneous - drug therapy Moraceae - chemistry Plant Extracts - chemistry Plant Extracts - pharmacology Plants - chemistry Rubiaceae - chemistry Secondary metabolites Structure-Activity Relationship Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma cruzi Trypanosoma cruzi - drug effects Zanthoxylum - chemistry |
| title | Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi |
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