Garcinielliptone FC: Antiparasitic activity without cytotoxicity to mammalian cells
[Display omitted] •Garcinielliptone FC is able to kill Schistosoma mansoni adult worms.•Garcinielliptone FC induced morphological changes on the tegument of the worms.•Garcinielliptone FC exhibited no in vitro activity toward Vero cells.•Garcinielliptone FC may be a promising antischistosomal compou...
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Veröffentlicht in: | Toxicology in vitro 2015-06, Vol.29 (4), p.681-687 |
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creator | Silva, Ana P. Silva, Marcos P. Oliveira, Cristiano G. Monteiro, Daniela C. Pinto, Pedro L. Mendonça, Ronaldo Z. Costa Júnior, Joaquim S. Freitas, Rivelilson M. de Moraes, Josué |
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•Garcinielliptone FC is able to kill Schistosoma mansoni adult worms.•Garcinielliptone FC induced morphological changes on the tegument of the worms.•Garcinielliptone FC exhibited no in vitro activity toward Vero cells.•Garcinielliptone FC may be a promising antischistosomal compound.
Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. In conclusion, these findings indicate the potential of GFC as an antiparasitic agent. |
doi_str_mv | 10.1016/j.tiv.2014.12.014 |
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•Garcinielliptone FC is able to kill Schistosoma mansoni adult worms.•Garcinielliptone FC induced morphological changes on the tegument of the worms.•Garcinielliptone FC exhibited no in vitro activity toward Vero cells.•Garcinielliptone FC may be a promising antischistosomal compound.
Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. In conclusion, these findings indicate the potential of GFC as an antiparasitic agent.</description><identifier>ISSN: 0887-2333</identifier><identifier>EISSN: 1879-3177</identifier><identifier>DOI: 10.1016/j.tiv.2014.12.014</identifier><identifier>PMID: 25553916</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Animals ; Antiparasitic activity ; Antiparasitic Agents - pharmacology ; Antiparasitic Agents - toxicity ; Antischistosomal drug ; Cell Survival - drug effects ; Cells, Cultured ; Cercopithecus aethiops ; Clusiaceae ; Clusiaceae - chemistry ; Confocal laser scanning microscopy ; Cytotoxicity ; Female ; Garcinielliptone FC ; Male ; Models, Molecular ; Motor Activity - drug effects ; Reproduction - drug effects ; Schistosoma ; Schistosoma mansoni ; Schistosoma mansoni - drug effects ; Schistosomicides - toxicity ; Seeds - chemistry ; Trematoda ; Triterpenes - isolation & purification ; Triterpenes - pharmacology ; Triterpenes - toxicity ; Vero Cells</subject><ispartof>Toxicology in vitro, 2015-06, Vol.29 (4), p.681-687</ispartof><rights>2014 Elsevier Ltd</rights><rights>Copyright © 2014 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-198419170713b66fb2ce3328b3b925deaf9fdd5be7e421728906051e6786970f3</citedby><cites>FETCH-LOGICAL-c386t-198419170713b66fb2ce3328b3b925deaf9fdd5be7e421728906051e6786970f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0887233314002549$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25553916$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Silva, Ana P.</creatorcontrib><creatorcontrib>Silva, Marcos P.</creatorcontrib><creatorcontrib>Oliveira, Cristiano G.</creatorcontrib><creatorcontrib>Monteiro, Daniela C.</creatorcontrib><creatorcontrib>Pinto, Pedro L.</creatorcontrib><creatorcontrib>Mendonça, Ronaldo Z.</creatorcontrib><creatorcontrib>Costa Júnior, Joaquim S.</creatorcontrib><creatorcontrib>Freitas, Rivelilson M.</creatorcontrib><creatorcontrib>de Moraes, Josué</creatorcontrib><title>Garcinielliptone FC: Antiparasitic activity without cytotoxicity to mammalian cells</title><title>Toxicology in vitro</title><addtitle>Toxicol In Vitro</addtitle><description>[Display omitted]
•Garcinielliptone FC is able to kill Schistosoma mansoni adult worms.•Garcinielliptone FC induced morphological changes on the tegument of the worms.•Garcinielliptone FC exhibited no in vitro activity toward Vero cells.•Garcinielliptone FC may be a promising antischistosomal compound.
Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. In conclusion, these findings indicate the potential of GFC as an antiparasitic agent.</description><subject>Animals</subject><subject>Antiparasitic activity</subject><subject>Antiparasitic Agents - pharmacology</subject><subject>Antiparasitic Agents - toxicity</subject><subject>Antischistosomal drug</subject><subject>Cell Survival - drug effects</subject><subject>Cells, Cultured</subject><subject>Cercopithecus aethiops</subject><subject>Clusiaceae</subject><subject>Clusiaceae - chemistry</subject><subject>Confocal laser scanning microscopy</subject><subject>Cytotoxicity</subject><subject>Female</subject><subject>Garcinielliptone FC</subject><subject>Male</subject><subject>Models, Molecular</subject><subject>Motor Activity - drug effects</subject><subject>Reproduction - drug effects</subject><subject>Schistosoma</subject><subject>Schistosoma mansoni</subject><subject>Schistosoma mansoni - drug effects</subject><subject>Schistosomicides - toxicity</subject><subject>Seeds - chemistry</subject><subject>Trematoda</subject><subject>Triterpenes - isolation & purification</subject><subject>Triterpenes - pharmacology</subject><subject>Triterpenes - toxicity</subject><subject>Vero Cells</subject><issn>0887-2333</issn><issn>1879-3177</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEFP3DAQha2KChbKD-ilypFLUo-9sR04oRXQSkg9tD1bjjNRZ7WJF9tLu_--Xi1w5PSk0Ztv5j3GPgNvgIP6um4yPTeCw7IB0RT5wBZgdFdL0PqELbgxuhZSyjN2ntKac94awU_ZmWjbVnagFuzng4ueZsLNhrY5zFjdr66r2znT1kWXKJOvnC9nKO-rv5T_hF2u_D6HHP6RPwxzqCY3TW5Dbq584aRP7OPoNgkvX_SC_b6_-7X6Vj_-ePi-un2svTQq19CZJXSguQbZKzX2wqOUwvSy70Q7oBu7cRjaHjUuBWhhOq54C6i0UZ3mo7xgV0fuNoanHaZsJ0qHD9yMYZcs6EIToFooVjhafQwpRRztNtLk4t4Ct4cu7dqWkPbQpQVhi5SdLy_4XT_h8LbxWl4x3BwNWEI-E0abPOHscaCIPtsh0Dv4_xuRhM0</recordid><startdate>201506</startdate><enddate>201506</enddate><creator>Silva, Ana P.</creator><creator>Silva, Marcos P.</creator><creator>Oliveira, Cristiano G.</creator><creator>Monteiro, Daniela C.</creator><creator>Pinto, Pedro L.</creator><creator>Mendonça, Ronaldo Z.</creator><creator>Costa Júnior, Joaquim S.</creator><creator>Freitas, Rivelilson M.</creator><creator>de Moraes, Josué</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>7U7</scope><scope>C1K</scope></search><sort><creationdate>201506</creationdate><title>Garcinielliptone FC: Antiparasitic activity without cytotoxicity to mammalian cells</title><author>Silva, Ana P. ; Silva, Marcos P. ; Oliveira, Cristiano G. ; Monteiro, Daniela C. ; Pinto, Pedro L. ; Mendonça, Ronaldo Z. ; Costa Júnior, Joaquim S. ; Freitas, Rivelilson M. ; de Moraes, Josué</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-198419170713b66fb2ce3328b3b925deaf9fdd5be7e421728906051e6786970f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Animals</topic><topic>Antiparasitic activity</topic><topic>Antiparasitic Agents - pharmacology</topic><topic>Antiparasitic Agents - toxicity</topic><topic>Antischistosomal drug</topic><topic>Cell Survival - drug effects</topic><topic>Cells, Cultured</topic><topic>Cercopithecus aethiops</topic><topic>Clusiaceae</topic><topic>Clusiaceae - chemistry</topic><topic>Confocal laser scanning microscopy</topic><topic>Cytotoxicity</topic><topic>Female</topic><topic>Garcinielliptone FC</topic><topic>Male</topic><topic>Models, Molecular</topic><topic>Motor Activity - drug effects</topic><topic>Reproduction - drug effects</topic><topic>Schistosoma</topic><topic>Schistosoma mansoni</topic><topic>Schistosoma mansoni - drug effects</topic><topic>Schistosomicides - toxicity</topic><topic>Seeds - chemistry</topic><topic>Trematoda</topic><topic>Triterpenes - isolation & purification</topic><topic>Triterpenes - pharmacology</topic><topic>Triterpenes - toxicity</topic><topic>Vero Cells</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Silva, Ana P.</creatorcontrib><creatorcontrib>Silva, Marcos P.</creatorcontrib><creatorcontrib>Oliveira, Cristiano G.</creatorcontrib><creatorcontrib>Monteiro, Daniela C.</creatorcontrib><creatorcontrib>Pinto, Pedro L.</creatorcontrib><creatorcontrib>Mendonça, Ronaldo Z.</creatorcontrib><creatorcontrib>Costa Júnior, Joaquim S.</creatorcontrib><creatorcontrib>Freitas, Rivelilson M.</creatorcontrib><creatorcontrib>de Moraes, Josué</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><jtitle>Toxicology in vitro</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Silva, Ana P.</au><au>Silva, Marcos P.</au><au>Oliveira, Cristiano G.</au><au>Monteiro, Daniela C.</au><au>Pinto, Pedro L.</au><au>Mendonça, Ronaldo Z.</au><au>Costa Júnior, Joaquim S.</au><au>Freitas, Rivelilson M.</au><au>de Moraes, Josué</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Garcinielliptone FC: Antiparasitic activity without cytotoxicity to mammalian cells</atitle><jtitle>Toxicology in vitro</jtitle><addtitle>Toxicol In Vitro</addtitle><date>2015-06</date><risdate>2015</risdate><volume>29</volume><issue>4</issue><spage>681</spage><epage>687</epage><pages>681-687</pages><issn>0887-2333</issn><eissn>1879-3177</eissn><abstract>[Display omitted]
•Garcinielliptone FC is able to kill Schistosoma mansoni adult worms.•Garcinielliptone FC induced morphological changes on the tegument of the worms.•Garcinielliptone FC exhibited no in vitro activity toward Vero cells.•Garcinielliptone FC may be a promising antischistosomal compound.
Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. In conclusion, these findings indicate the potential of GFC as an antiparasitic agent.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>25553916</pmid><doi>10.1016/j.tiv.2014.12.014</doi><tpages>7</tpages></addata></record> |
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subjects | Animals Antiparasitic activity Antiparasitic Agents - pharmacology Antiparasitic Agents - toxicity Antischistosomal drug Cell Survival - drug effects Cells, Cultured Cercopithecus aethiops Clusiaceae Clusiaceae - chemistry Confocal laser scanning microscopy Cytotoxicity Female Garcinielliptone FC Male Models, Molecular Motor Activity - drug effects Reproduction - drug effects Schistosoma Schistosoma mansoni Schistosoma mansoni - drug effects Schistosomicides - toxicity Seeds - chemistry Trematoda Triterpenes - isolation & purification Triterpenes - pharmacology Triterpenes - toxicity Vero Cells |
title | Garcinielliptone FC: Antiparasitic activity without cytotoxicity to mammalian cells |
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