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Anti-Trichomonas vaginalis activity of ursolic acid derivative: a promising alternative
Trichomonas vaginalis is an extracellular parasite that binds to the epithelium of the human urogenital tract and causes the sexually transmitted infection, trichomoniasis. In view of increased resistance to drugs belonging to the 5-nitroimidazole class, new treatment alternatives are urgently neede...
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| Published in: | Parasitology research (1987) 2018-05, Vol.117 (5), p.1573-1580 |
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| Main Authors: | , , , , , , |
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| container_end_page | 1580 |
| container_issue | 5 |
| container_start_page | 1573 |
| container_title | Parasitology research (1987) |
| container_volume | 117 |
| creator | Bitencourt, Fernanda Gobbi de Brum Vieira, Patrícia Meirelles, Lucia Collares Rigo, Graziela Vargas da Silva, Elenilson Figueiredo Gnoatto, Simone Cristina Baggio Tasca, Tiana |
| description | Trichomonas vaginalis
is an extracellular parasite that binds to the epithelium of the human urogenital tract and causes the sexually transmitted infection, trichomoniasis. In view of increased resistance to drugs belonging to the 5-nitroimidazole class, new treatment alternatives are urgently needed. In this study, eight semisynthetized triterpene derivatives were evaluated for in vitro anti-
T. vaginalis
activity. Ursolic acid and its derivative, 3-oxime-urs-12-en-28-oic-ursolic acid (
9
), presented the best anti-
T. vaginalis
activity when compared to other derivatives, with minimum inhibitory concentration (MIC) at 25 μM. Moreover,
9
was active against several
T. vaginalis
fresh clinical isolates. Hemolysis assay demonstrated that
9
presented a low hemolytic effect. Importantly, 25 μM
9
was not cytotoxic against the Vero cell lineage. Finally, we demonstrated that compound
9
acts synergistically with metronidazole against a
T. vaginalis
metronidazole-resistant isolate. This report reveals the high potential of the triterpenoid derivative
9
as trichomonicidal agent. |
| doi_str_mv | 10.1007/s00436-018-5839-1 |
| format | article |
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is an extracellular parasite that binds to the epithelium of the human urogenital tract and causes the sexually transmitted infection, trichomoniasis. In view of increased resistance to drugs belonging to the 5-nitroimidazole class, new treatment alternatives are urgently needed. In this study, eight semisynthetized triterpene derivatives were evaluated for in vitro anti-
T. vaginalis
activity. Ursolic acid and its derivative, 3-oxime-urs-12-en-28-oic-ursolic acid (
9
), presented the best anti-
T. vaginalis
activity when compared to other derivatives, with minimum inhibitory concentration (MIC) at 25 μM. Moreover,
9
was active against several
T. vaginalis
fresh clinical isolates. Hemolysis assay demonstrated that
9
presented a low hemolytic effect. Importantly, 25 μM
9
was not cytotoxic against the Vero cell lineage. Finally, we demonstrated that compound
9
acts synergistically with metronidazole against a
T. vaginalis
metronidazole-resistant isolate. This report reveals the high potential of the triterpenoid derivative
9
as trichomonicidal agent.</description><identifier>ISSN: 0932-0113</identifier><identifier>EISSN: 1432-1955</identifier><identifier>DOI: 10.1007/s00436-018-5839-1</identifier><identifier>PMID: 29572567</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer Berlin Heidelberg</publisher><subject>Animals ; Antitrichomonal Agents - pharmacology ; Biomedical and Life Sciences ; Biomedicine ; Cell Death - drug effects ; Cell Line, Tumor ; Cell lineage ; Chlorocebus aethiops ; Clinical isolates ; Condoms ; Cytotoxicity ; Drug Resistance ; Drug Synergism ; Drug Therapy, Combination ; Epithelium ; Female ; Health aspects ; HeLa Cells ; Hemolysis - drug effects ; Humans ; Immunology ; Medical Microbiology ; Metronidazole ; Metronidazole - pharmacology ; Microbial Sensitivity Tests ; Microbiology ; Minimum inhibitory concentration ; Nitroimidazole ; Original Paper ; Parasitic diseases ; Prevention ; Sexually transmitted diseases ; STD ; Terpenoids ; Trichomonas ; Trichomonas Infections - drug therapy ; Trichomonas Infections - parasitology ; Trichomonas vaginalis ; Trichomonas vaginalis - drug effects ; Trichomonas Vaginitis - drug therapy ; Trichomonas Vaginitis - parasitology ; Trichomoniasis ; Triterpenes - chemistry ; Triterpenes - pharmacology ; Ursolic Acid ; Vero Cells</subject><ispartof>Parasitology research (1987), 2018-05, Vol.117 (5), p.1573-1580</ispartof><rights>Springer-Verlag GmbH Germany, part of Springer Nature 2018</rights><rights>COPYRIGHT 2018 Springer</rights><rights>Copyright Springer Science & Business Media 2018</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c439t-d6fb169625eece368d69bc17b70b69fc2bfe60952e9fb52da5132b2ee1be59ed3</citedby><cites>FETCH-LOGICAL-c439t-d6fb169625eece368d69bc17b70b69fc2bfe60952e9fb52da5132b2ee1be59ed3</cites><orcidid>0000-0002-8334-5105</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27903,27904</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/29572567$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bitencourt, Fernanda Gobbi</creatorcontrib><creatorcontrib>de Brum Vieira, Patrícia</creatorcontrib><creatorcontrib>Meirelles, Lucia Collares</creatorcontrib><creatorcontrib>Rigo, Graziela Vargas</creatorcontrib><creatorcontrib>da Silva, Elenilson Figueiredo</creatorcontrib><creatorcontrib>Gnoatto, Simone Cristina Baggio</creatorcontrib><creatorcontrib>Tasca, Tiana</creatorcontrib><title>Anti-Trichomonas vaginalis activity of ursolic acid derivative: a promising alternative</title><title>Parasitology research (1987)</title><addtitle>Parasitol Res</addtitle><addtitle>Parasitol Res</addtitle><description>Trichomonas vaginalis
is an extracellular parasite that binds to the epithelium of the human urogenital tract and causes the sexually transmitted infection, trichomoniasis. In view of increased resistance to drugs belonging to the 5-nitroimidazole class, new treatment alternatives are urgently needed. In this study, eight semisynthetized triterpene derivatives were evaluated for in vitro anti-
T. vaginalis
activity. Ursolic acid and its derivative, 3-oxime-urs-12-en-28-oic-ursolic acid (
9
), presented the best anti-
T. vaginalis
activity when compared to other derivatives, with minimum inhibitory concentration (MIC) at 25 μM. Moreover,
9
was active against several
T. vaginalis
fresh clinical isolates. Hemolysis assay demonstrated that
9
presented a low hemolytic effect. Importantly, 25 μM
9
was not cytotoxic against the Vero cell lineage. Finally, we demonstrated that compound
9
acts synergistically with metronidazole against a
T. vaginalis
metronidazole-resistant isolate. This report reveals the high potential of the triterpenoid derivative
9
as trichomonicidal agent.</description><subject>Animals</subject><subject>Antitrichomonal Agents - pharmacology</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Cell Death - drug effects</subject><subject>Cell Line, Tumor</subject><subject>Cell lineage</subject><subject>Chlorocebus aethiops</subject><subject>Clinical isolates</subject><subject>Condoms</subject><subject>Cytotoxicity</subject><subject>Drug Resistance</subject><subject>Drug Synergism</subject><subject>Drug Therapy, Combination</subject><subject>Epithelium</subject><subject>Female</subject><subject>Health aspects</subject><subject>HeLa Cells</subject><subject>Hemolysis - drug effects</subject><subject>Humans</subject><subject>Immunology</subject><subject>Medical Microbiology</subject><subject>Metronidazole</subject><subject>Metronidazole - pharmacology</subject><subject>Microbial Sensitivity Tests</subject><subject>Microbiology</subject><subject>Minimum inhibitory concentration</subject><subject>Nitroimidazole</subject><subject>Original Paper</subject><subject>Parasitic diseases</subject><subject>Prevention</subject><subject>Sexually transmitted diseases</subject><subject>STD</subject><subject>Terpenoids</subject><subject>Trichomonas</subject><subject>Trichomonas Infections - drug therapy</subject><subject>Trichomonas Infections - parasitology</subject><subject>Trichomonas vaginalis</subject><subject>Trichomonas vaginalis - drug effects</subject><subject>Trichomonas Vaginitis - drug therapy</subject><subject>Trichomonas Vaginitis - parasitology</subject><subject>Trichomoniasis</subject><subject>Triterpenes - chemistry</subject><subject>Triterpenes - pharmacology</subject><subject>Ursolic Acid</subject><subject>Vero Cells</subject><issn>0932-0113</issn><issn>1432-1955</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><recordid>eNp1kV9LHDEUxYNU3K36AfpSBvo8NjeZZDZ9W8RWQfBF8TEkmZttlpmJTWYX_PaNjn8oWPKQcM_vXE44hHwBegaUtt8zpQ2XNYVVLVZc1XBAltBwVoMS4hNZUlXeFIAvyOect5RCK5vmiCyYEi0Tsl2S-_U4hfo2Bfc7DnE0udqbTRhNH3Jl3BT2YXqsoq92Kcc-uDILXdVhCntTRPxRmeohxSHkMG4q00-YxmfhhBx602c8fbmPyd3Pi9vzy_r65tfV-fq6dg1XU91Jb0EqyQSiQy5XnVTWQWtbaqXyjlmPkirBUHkrWGcEcGYZIlgUCjt-TL7Ne0uKPzvMk97GXcnQZ80op0w0ist3amN61GH0cUrGldROrwWXIICqVaHOPqDK6XAILo7oQ5n_Y4DZ4FLMOaHXDykMJj1qoPqpIT03pEtD-qkhDcXz9SXwzg7YvTleKykAm4FcpHGD6f1H_9_6F6Lfm2E</recordid><startdate>20180501</startdate><enddate>20180501</enddate><creator>Bitencourt, Fernanda Gobbi</creator><creator>de Brum Vieira, Patrícia</creator><creator>Meirelles, Lucia Collares</creator><creator>Rigo, Graziela Vargas</creator><creator>da Silva, Elenilson Figueiredo</creator><creator>Gnoatto, Simone Cristina Baggio</creator><creator>Tasca, Tiana</creator><general>Springer Berlin Heidelberg</general><general>Springer</general><general>Springer Nature B.V</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><orcidid>https://orcid.org/0000-0002-8334-5105</orcidid></search><sort><creationdate>20180501</creationdate><title>Anti-Trichomonas vaginalis activity of ursolic acid derivative: a promising alternative</title><author>Bitencourt, Fernanda Gobbi ; de Brum Vieira, Patrícia ; Meirelles, Lucia Collares ; Rigo, Graziela Vargas ; da Silva, Elenilson Figueiredo ; Gnoatto, Simone Cristina Baggio ; Tasca, Tiana</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c439t-d6fb169625eece368d69bc17b70b69fc2bfe60952e9fb52da5132b2ee1be59ed3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Animals</topic><topic>Antitrichomonal Agents - pharmacology</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Cell Death - drug effects</topic><topic>Cell Line, Tumor</topic><topic>Cell lineage</topic><topic>Chlorocebus aethiops</topic><topic>Clinical isolates</topic><topic>Condoms</topic><topic>Cytotoxicity</topic><topic>Drug Resistance</topic><topic>Drug Synergism</topic><topic>Drug Therapy, Combination</topic><topic>Epithelium</topic><topic>Female</topic><topic>Health aspects</topic><topic>HeLa Cells</topic><topic>Hemolysis - drug effects</topic><topic>Humans</topic><topic>Immunology</topic><topic>Medical Microbiology</topic><topic>Metronidazole</topic><topic>Metronidazole - pharmacology</topic><topic>Microbial Sensitivity Tests</topic><topic>Microbiology</topic><topic>Minimum inhibitory concentration</topic><topic>Nitroimidazole</topic><topic>Original Paper</topic><topic>Parasitic diseases</topic><topic>Prevention</topic><topic>Sexually transmitted diseases</topic><topic>STD</topic><topic>Terpenoids</topic><topic>Trichomonas</topic><topic>Trichomonas Infections - drug therapy</topic><topic>Trichomonas Infections - parasitology</topic><topic>Trichomonas vaginalis</topic><topic>Trichomonas vaginalis - drug effects</topic><topic>Trichomonas Vaginitis - drug therapy</topic><topic>Trichomonas Vaginitis - parasitology</topic><topic>Trichomoniasis</topic><topic>Triterpenes - chemistry</topic><topic>Triterpenes - pharmacology</topic><topic>Ursolic Acid</topic><topic>Vero Cells</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bitencourt, Fernanda Gobbi</creatorcontrib><creatorcontrib>de Brum Vieira, Patrícia</creatorcontrib><creatorcontrib>Meirelles, Lucia Collares</creatorcontrib><creatorcontrib>Rigo, Graziela Vargas</creatorcontrib><creatorcontrib>da Silva, Elenilson Figueiredo</creatorcontrib><creatorcontrib>Gnoatto, Simone Cristina Baggio</creatorcontrib><creatorcontrib>Tasca, Tiana</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Parasitology research (1987)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bitencourt, Fernanda Gobbi</au><au>de Brum Vieira, Patrícia</au><au>Meirelles, Lucia Collares</au><au>Rigo, Graziela Vargas</au><au>da Silva, Elenilson Figueiredo</au><au>Gnoatto, Simone Cristina Baggio</au><au>Tasca, Tiana</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Anti-Trichomonas vaginalis activity of ursolic acid derivative: a promising alternative</atitle><jtitle>Parasitology research (1987)</jtitle><stitle>Parasitol Res</stitle><addtitle>Parasitol Res</addtitle><date>2018-05-01</date><risdate>2018</risdate><volume>117</volume><issue>5</issue><spage>1573</spage><epage>1580</epage><pages>1573-1580</pages><issn>0932-0113</issn><eissn>1432-1955</eissn><abstract>Trichomonas vaginalis
is an extracellular parasite that binds to the epithelium of the human urogenital tract and causes the sexually transmitted infection, trichomoniasis. In view of increased resistance to drugs belonging to the 5-nitroimidazole class, new treatment alternatives are urgently needed. In this study, eight semisynthetized triterpene derivatives were evaluated for in vitro anti-
T. vaginalis
activity. Ursolic acid and its derivative, 3-oxime-urs-12-en-28-oic-ursolic acid (
9
), presented the best anti-
T. vaginalis
activity when compared to other derivatives, with minimum inhibitory concentration (MIC) at 25 μM. Moreover,
9
was active against several
T. vaginalis
fresh clinical isolates. Hemolysis assay demonstrated that
9
presented a low hemolytic effect. Importantly, 25 μM
9
was not cytotoxic against the Vero cell lineage. Finally, we demonstrated that compound
9
acts synergistically with metronidazole against a
T. vaginalis
metronidazole-resistant isolate. This report reveals the high potential of the triterpenoid derivative
9
as trichomonicidal agent.</abstract><cop>Berlin/Heidelberg</cop><pub>Springer Berlin Heidelberg</pub><pmid>29572567</pmid><doi>10.1007/s00436-018-5839-1</doi><tpages>8</tpages><orcidid>https://orcid.org/0000-0002-8334-5105</orcidid></addata></record> |
| fulltext | fulltext |
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| ispartof | Parasitology research (1987), 2018-05, Vol.117 (5), p.1573-1580 |
| issn | 0932-0113 1432-1955 |
| language | eng |
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| subjects | Animals Antitrichomonal Agents - pharmacology Biomedical and Life Sciences Biomedicine Cell Death - drug effects Cell Line, Tumor Cell lineage Chlorocebus aethiops Clinical isolates Condoms Cytotoxicity Drug Resistance Drug Synergism Drug Therapy, Combination Epithelium Female Health aspects HeLa Cells Hemolysis - drug effects Humans Immunology Medical Microbiology Metronidazole Metronidazole - pharmacology Microbial Sensitivity Tests Microbiology Minimum inhibitory concentration Nitroimidazole Original Paper Parasitic diseases Prevention Sexually transmitted diseases STD Terpenoids Trichomonas Trichomonas Infections - drug therapy Trichomonas Infections - parasitology Trichomonas vaginalis Trichomonas vaginalis - drug effects Trichomonas Vaginitis - drug therapy Trichomonas Vaginitis - parasitology Trichomoniasis Triterpenes - chemistry Triterpenes - pharmacology Ursolic Acid Vero Cells |
| title | Anti-Trichomonas vaginalis activity of ursolic acid derivative: a promising alternative |
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