Cinnamic Acid Bornyl Ester Derivatives from Valeriana wallichii Exhibit Antileishmanial In Vivo Activity in Leishmania major-Infected BALB/c Mice
Human leishmaniasis covers a broad spectrum of clinical manifestations ranging from self-healing cutaneous leishmaniasis to severe and lethal visceral leishmaniasis caused among other species by Leishmania major or Leishmania donovani, respectively. Some drug candidates are in clinical trials to sub...
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| description | Human leishmaniasis covers a broad spectrum of clinical manifestations ranging from self-healing cutaneous leishmaniasis to severe and lethal visceral leishmaniasis caused among other species by Leishmania major or Leishmania donovani, respectively. Some drug candidates are in clinical trials to substitute current therapies, which are facing emerging drug-resistance accompanied with serious side effects. Here, two cinnamic acid bornyl ester derivatives (1 and 2) were assessed for their antileishmanial activity. Good selectivity and antileishmanial activity of bornyl 3-phenylpropanoate (2) in vitro prompted the antileishmanial assessment in vivo. For this purpose, BALB/c mice were infected with Leishmania major promastigotes and treated with three doses of 50 mg/kg/day of compound 2. The treatment prevented the characteristic swelling at the site of infection and correlated with reduced parasite burden. Transmitted light microscopy and transmission electron microscopy of Leishmania major promastigotes revealed that compounds 1 and 2 induce mitochondrial swelling. Subsequent studies on Leishmania major promastigotes showed the loss of mitochondrial transmembrane potential (ΔΨm) as a putative mode of action. As the cinnamic acid bornyl ester derivatives 1 and 2 had exhibited antileishmanial activity in vitro, and compound 2 in Leishmania major-infected BALB/c mice in vivo, they can be regarded as possible lead structures for the development of new antileishmanial therapeutic approaches. |
| doi_str_mv | 10.1371/journal.pone.0142386 |
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Some drug candidates are in clinical trials to substitute current therapies, which are facing emerging drug-resistance accompanied with serious side effects. Here, two cinnamic acid bornyl ester derivatives (1 and 2) were assessed for their antileishmanial activity. Good selectivity and antileishmanial activity of bornyl 3-phenylpropanoate (2) in vitro prompted the antileishmanial assessment in vivo. For this purpose, BALB/c mice were infected with Leishmania major promastigotes and treated with three doses of 50 mg/kg/day of compound 2. The treatment prevented the characteristic swelling at the site of infection and correlated with reduced parasite burden. Transmitted light microscopy and transmission electron microscopy of Leishmania major promastigotes revealed that compounds 1 and 2 induce mitochondrial swelling. Subsequent studies on Leishmania major promastigotes showed the loss of mitochondrial transmembrane potential (ΔΨm) as a putative mode of action. As the cinnamic acid bornyl ester derivatives 1 and 2 had exhibited antileishmanial activity in vitro, and compound 2 in Leishmania major-infected BALB/c mice in vivo, they can be regarded as possible lead structures for the development of new antileishmanial therapeutic approaches.</description><identifier>ISSN: 1932-6203</identifier><identifier>EISSN: 1932-6203</identifier><identifier>DOI: 10.1371/journal.pone.0142386</identifier><identifier>PMID: 26554591</identifier><language>eng</language><publisher>United States: Public Library of Science</publisher><subject>Acids ; Animals ; Antiprotozoal Agents - pharmacology ; Antiprotozoal Agents - therapeutic use ; Apoptosis ; Biology ; Carboxylic acids ; Care and treatment ; Cinnamates - pharmacology ; Cinnamates - therapeutic use ; Cinnamic acid ; Clinical trials ; Cutaneous leishmaniasis ; Derivatives ; Drug development ; Drug resistance ; Electron microscopy ; Female ; Health aspects ; Leishmania ; Leishmaniasis ; Leishmaniasis - drug therapy ; Light microscopy ; Liver - drug effects ; Liver - parasitology ; Medical research ; Membrane potential ; Mice ; Mice, Inbred BALB C ; Mitochondria ; Mode of action ; Oils & fats ; Parasites ; Parasitic diseases ; Pharmaceutical sciences ; Pharmacy ; Phytotherapy ; Plant extracts ; Plant Extracts - pharmacology ; Plant Extracts - therapeutic use ; Plant resistance ; Promastigotes ; Side effects ; Staphylococcus infections ; Studies ; Swelling ; Transmission electron microscopy ; Tropical diseases ; Valerian ; Valeriana ; Vector-borne diseases ; Visceral leishmaniasis</subject><ispartof>PloS one, 2015-11, Vol.10 (11), p.e0142386</ispartof><rights>COPYRIGHT 2015 Public Library of Science</rights><rights>2015 Masic et al. This is an open access article distributed under the terms of the Creative Commons Attribution License: http://creativecommons.org/licenses/by/4.0/ (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2015 Masic et al 2015 Masic et al</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c692t-e80ca101621fc411e95793b8e2f1713177854cb58310100090f0ead5fe99b67f3</citedby><cites>FETCH-LOGICAL-c692t-e80ca101621fc411e95793b8e2f1713177854cb58310100090f0ead5fe99b67f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4640567/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4640567/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,315,728,781,785,865,886,2103,2929,23871,27929,27930,53796,53798</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26554591$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><contributor>Saha, Bhaskar</contributor><creatorcontrib>Masic, Anita</creatorcontrib><creatorcontrib>Valencia Hernandez, Ana Maria</creatorcontrib><creatorcontrib>Hazra, Sudipta</creatorcontrib><creatorcontrib>Glaser, Jan</creatorcontrib><creatorcontrib>Holzgrabe, Ulrike</creatorcontrib><creatorcontrib>Hazra, Banasri</creatorcontrib><creatorcontrib>Schurigt, Uta</creatorcontrib><title>Cinnamic Acid Bornyl Ester Derivatives from Valeriana wallichii Exhibit Antileishmanial In Vivo Activity in Leishmania major-Infected BALB/c Mice</title><title>PloS one</title><addtitle>PLoS One</addtitle><description>Human leishmaniasis covers a broad spectrum of clinical manifestations ranging from self-healing cutaneous leishmaniasis to severe and lethal visceral leishmaniasis caused among other species by Leishmania major or Leishmania donovani, respectively. 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As the cinnamic acid bornyl ester derivatives 1 and 2 had exhibited antileishmanial activity in vitro, and compound 2 in Leishmania major-infected BALB/c mice in vivo, they can be regarded as possible lead structures for the development of new antileishmanial therapeutic approaches.</description><subject>Acids</subject><subject>Animals</subject><subject>Antiprotozoal Agents - pharmacology</subject><subject>Antiprotozoal Agents - therapeutic use</subject><subject>Apoptosis</subject><subject>Biology</subject><subject>Carboxylic acids</subject><subject>Care and treatment</subject><subject>Cinnamates - pharmacology</subject><subject>Cinnamates - therapeutic use</subject><subject>Cinnamic acid</subject><subject>Clinical trials</subject><subject>Cutaneous leishmaniasis</subject><subject>Derivatives</subject><subject>Drug development</subject><subject>Drug resistance</subject><subject>Electron microscopy</subject><subject>Female</subject><subject>Health aspects</subject><subject>Leishmania</subject><subject>Leishmaniasis</subject><subject>Leishmaniasis - 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Some drug candidates are in clinical trials to substitute current therapies, which are facing emerging drug-resistance accompanied with serious side effects. Here, two cinnamic acid bornyl ester derivatives (1 and 2) were assessed for their antileishmanial activity. Good selectivity and antileishmanial activity of bornyl 3-phenylpropanoate (2) in vitro prompted the antileishmanial assessment in vivo. For this purpose, BALB/c mice were infected with Leishmania major promastigotes and treated with three doses of 50 mg/kg/day of compound 2. The treatment prevented the characteristic swelling at the site of infection and correlated with reduced parasite burden. Transmitted light microscopy and transmission electron microscopy of Leishmania major promastigotes revealed that compounds 1 and 2 induce mitochondrial swelling. Subsequent studies on Leishmania major promastigotes showed the loss of mitochondrial transmembrane potential (ΔΨm) as a putative mode of action. As the cinnamic acid bornyl ester derivatives 1 and 2 had exhibited antileishmanial activity in vitro, and compound 2 in Leishmania major-infected BALB/c mice in vivo, they can be regarded as possible lead structures for the development of new antileishmanial therapeutic approaches.</abstract><cop>United States</cop><pub>Public Library of Science</pub><pmid>26554591</pmid><doi>10.1371/journal.pone.0142386</doi><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1932-6203 |
| ispartof | PloS one, 2015-11, Vol.10 (11), p.e0142386 |
| issn | 1932-6203 1932-6203 |
| language | eng |
| recordid | cdi_plos_journals_1732311426 |
| source | MEDLINE; DOAJ Directory of Open Access Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Public Library of Science (PLoS) Journals Open Access; PubMed Central; Free Full-Text Journals in Chemistry |
| subjects | Acids Animals Antiprotozoal Agents - pharmacology Antiprotozoal Agents - therapeutic use Apoptosis Biology Carboxylic acids Care and treatment Cinnamates - pharmacology Cinnamates - therapeutic use Cinnamic acid Clinical trials Cutaneous leishmaniasis Derivatives Drug development Drug resistance Electron microscopy Female Health aspects Leishmania Leishmaniasis Leishmaniasis - drug therapy Light microscopy Liver - drug effects Liver - parasitology Medical research Membrane potential Mice Mice, Inbred BALB C Mitochondria Mode of action Oils & fats Parasites Parasitic diseases Pharmaceutical sciences Pharmacy Phytotherapy Plant extracts Plant Extracts - pharmacology Plant Extracts - therapeutic use Plant resistance Promastigotes Side effects Staphylococcus infections Studies Swelling Transmission electron microscopy Tropical diseases Valerian Valeriana Vector-borne diseases Visceral leishmaniasis |
| title | Cinnamic Acid Bornyl Ester Derivatives from Valeriana wallichii Exhibit Antileishmanial In Vivo Activity in Leishmania major-Infected BALB/c Mice |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-11T21%3A00%3A53IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-gale_plos_&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Cinnamic%20Acid%20Bornyl%20Ester%20Derivatives%20from%20Valeriana%20wallichii%20Exhibit%20Antileishmanial%20In%20Vivo%20Activity%20in%20Leishmania%20major-Infected%20BALB/c%20Mice&rft.jtitle=PloS%20one&rft.au=Masic,%20Anita&rft.date=2015-11-10&rft.volume=10&rft.issue=11&rft.spage=e0142386&rft.pages=e0142386-&rft.issn=1932-6203&rft.eissn=1932-6203&rft_id=info:doi/10.1371/journal.pone.0142386&rft_dat=%3Cgale_plos_%3EA434196737%3C/gale_plos_%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1732311426&rft_id=info:pmid/26554591&rft_galeid=A434196737&rft_doaj_id=oai_doaj_org_article_8e85e456b48646d296cee5ea926ae1ce&rfr_iscdi=true |