In vitro leishmanicidal activity of aurones
Abstract: A series of aurones with drug-potential for LEISHMANIA infections was identified IN VITRO using both a direct cytotoxicity assay against extracellular promastigotes of LEISHMANIA DONOVANI, L. INFANTUM, L. ENRIETTII, and L. MAJOR , and a test against intracellular amastigote forms of L. DON...
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| Veröffentlicht in: | Planta medica 1999-05, Vol.65 (4), p.316-319 |
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| container_title | Planta medica |
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| creator | Kayser, O Kiderlen, A.F Folkens, U Kolodziej, H |
| description | Abstract:
A series of aurones with drug-potential for LEISHMANIA infections was identified IN VITRO using both
a direct cytotoxicity assay against extracellular promastigotes of
LEISHMANIA DONOVANI, L. INFANTUM, L. ENRIETTII, and L. MAJOR , and a test against intracellular amastigote forms of
L. DONOVANI residing within murine macrophages. The most active
aurone (6-hydroxy-2-[phenylmethylene]-3(2H)-benzofuranone)
had an EC
50
of 0.45 μg/ml in the extra-, and an EC
50
of 1.40 μg/ml in the intracellular assay. Other aurones
were active between 0.06 - 12.50 μg/ml and
0.04 - 7.81 μg/ml, respectively. When tested
against murine bone marrow-derived macrophages as a mammalian host cell control,
the compounds showed only moderate cytotoxicity (EC
50
2.32 to > 25.0 μg/ml).
This is the first report on aurones as a new class of natural products with
leishmanicidal activity. |
| doi_str_mv | 10.1055/s-1999-13993 |
| format | Article |
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A series of aurones with drug-potential for LEISHMANIA infections was identified IN VITRO using both
a direct cytotoxicity assay against extracellular promastigotes of
LEISHMANIA DONOVANI, L. INFANTUM, L. ENRIETTII, and L. MAJOR , and a test against intracellular amastigote forms of
L. DONOVANI residing within murine macrophages. The most active
aurone (6-hydroxy-2-[phenylmethylene]-3(2H)-benzofuranone)
had an EC
50
of 0.45 μg/ml in the extra-, and an EC
50
of 1.40 μg/ml in the intracellular assay. Other aurones
were active between 0.06 - 12.50 μg/ml and
0.04 - 7.81 μg/ml, respectively. When tested
against murine bone marrow-derived macrophages as a mammalian host cell control,
the compounds showed only moderate cytotoxicity (EC
50
2.32 to > 25.0 μg/ml).
This is the first report on aurones as a new class of natural products with
leishmanicidal activity.</description><identifier>ISSN: 0032-0943</identifier><identifier>EISSN: 1439-0221</identifier><identifier>DOI: 10.1055/s-1999-13993</identifier><identifier>PMID: 10364835</identifier><identifier>CODEN: PLMEAA</identifier><language>eng</language><publisher>Stuttgart: Thieme</publisher><subject>Animals ; antiprotozoal agents ; Antiprotozoal Agents - pharmacology ; Benzofurans - pharmacology ; Benzylidene Compounds - pharmacology ; bioassays ; Biological and medical sciences ; Bone Marrow Cells - drug effects ; Bone Marrow Cells - parasitology ; Cell Line ; Cell Survival - drug effects ; chemical structure ; cytotoxicity ; General pharmacology ; hosts ; in vitro ; Leishmania - drug effects ; Leishmania donovani ; Leishmania enriettii ; Leishmania infantum ; Leishmania major ; lethal dose ; macrophages ; Macrophages - drug effects ; Macrophages - parasitology ; Medical sciences ; Mice ; Mice, Inbred C57BL ; Original Paper ; Pharmacognosy. Homeopathy. Health food ; Pharmacology. Drug treatments</subject><ispartof>Planta medica, 1999-05, Vol.65 (4), p.316-319</ispartof><rights>Georg Thieme Verlag Stuttgart · New York</rights><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c376t-b721e11d8be40b9b5981108ba424c49d54b459ae8e7697d5e5f8e9556bed843e3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-1999-13993.pdf$$EPDF$$P50$$Gthieme$$H</linktopdf><link.rule.ids>315,781,785,3018,3019,27929,27930,54564</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1830523$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10364835$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kayser, O</creatorcontrib><creatorcontrib>Kiderlen, A.F</creatorcontrib><creatorcontrib>Folkens, U</creatorcontrib><creatorcontrib>Kolodziej, H</creatorcontrib><title>In vitro leishmanicidal activity of aurones</title><title>Planta medica</title><addtitle>Planta Med</addtitle><description>Abstract:
A series of aurones with drug-potential for LEISHMANIA infections was identified IN VITRO using both
a direct cytotoxicity assay against extracellular promastigotes of
LEISHMANIA DONOVANI, L. INFANTUM, L. ENRIETTII, and L. MAJOR , and a test against intracellular amastigote forms of
L. DONOVANI residing within murine macrophages. The most active
aurone (6-hydroxy-2-[phenylmethylene]-3(2H)-benzofuranone)
had an EC
50
of 0.45 μg/ml in the extra-, and an EC
50
of 1.40 μg/ml in the intracellular assay. Other aurones
were active between 0.06 - 12.50 μg/ml and
0.04 - 7.81 μg/ml, respectively. When tested
against murine bone marrow-derived macrophages as a mammalian host cell control,
the compounds showed only moderate cytotoxicity (EC
50
2.32 to > 25.0 μg/ml).
This is the first report on aurones as a new class of natural products with
leishmanicidal activity.</description><subject>Animals</subject><subject>antiprotozoal agents</subject><subject>Antiprotozoal Agents - pharmacology</subject><subject>Benzofurans - pharmacology</subject><subject>Benzylidene Compounds - pharmacology</subject><subject>bioassays</subject><subject>Biological and medical sciences</subject><subject>Bone Marrow Cells - drug effects</subject><subject>Bone Marrow Cells - parasitology</subject><subject>Cell Line</subject><subject>Cell Survival - drug effects</subject><subject>chemical structure</subject><subject>cytotoxicity</subject><subject>General pharmacology</subject><subject>hosts</subject><subject>in vitro</subject><subject>Leishmania - drug effects</subject><subject>Leishmania donovani</subject><subject>Leishmania enriettii</subject><subject>Leishmania infantum</subject><subject>Leishmania major</subject><subject>lethal dose</subject><subject>macrophages</subject><subject>Macrophages - drug effects</subject><subject>Macrophages - parasitology</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred C57BL</subject><subject>Original Paper</subject><subject>Pharmacognosy. Homeopathy. Health food</subject><subject>Pharmacology. Drug treatments</subject><issn>0032-0943</issn><issn>1439-0221</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp10DtPwzAUhmELgaBcNmbIgFhK4PiW2COquFSqxACdLSc5AVe5FDtB6r8nJZVgYfLgR--RPkLOKdxSkPIuxFRrHVOuNd8jEyq4joExuk8mAJzFoAU_IschrACo0ACH5IgCT4TickKm8yb6cp1vowpd-Kht43JX2CqyeeeGj03UlpHtfdtgOCUHpa0Cnu3eE7J8fHibPceLl6f57H4R5zxNujhLGUVKC5WhgExnUitKQWVWMJELXUiRCaktKkwTnRYSZalQS5lkWCjBkZ-Q67G79u1nj6EztQs5VpVtsO2DSYag4Ek6wJsR5r4NwWNp1t7V1m8MBbMdxwSzHcf8jDPwi123z2os_uBxjQFc7YANua1Kb5vchV-nOEi27UxH1n04rNGs2t43wyD_Xb0cdWlbY9_9EFy-MqAcmIYkVSn_BuhpgT0</recordid><startdate>19990501</startdate><enddate>19990501</enddate><creator>Kayser, O</creator><creator>Kiderlen, A.F</creator><creator>Folkens, U</creator><creator>Kolodziej, H</creator><general>Thieme</general><scope>FBQ</scope><scope>IQODW</scope><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></search><sort><creationdate>19990501</creationdate><title>In vitro leishmanicidal activity of aurones</title><author>Kayser, O ; Kiderlen, A.F ; Folkens, U ; Kolodziej, H</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c376t-b721e11d8be40b9b5981108ba424c49d54b459ae8e7697d5e5f8e9556bed843e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Animals</topic><topic>antiprotozoal agents</topic><topic>Antiprotozoal Agents - pharmacology</topic><topic>Benzofurans - pharmacology</topic><topic>Benzylidene Compounds - pharmacology</topic><topic>bioassays</topic><topic>Biological and medical sciences</topic><topic>Bone Marrow Cells - drug effects</topic><topic>Bone Marrow Cells - parasitology</topic><topic>Cell Line</topic><topic>Cell Survival - drug effects</topic><topic>chemical structure</topic><topic>cytotoxicity</topic><topic>General pharmacology</topic><topic>hosts</topic><topic>in vitro</topic><topic>Leishmania - drug effects</topic><topic>Leishmania donovani</topic><topic>Leishmania enriettii</topic><topic>Leishmania infantum</topic><topic>Leishmania major</topic><topic>lethal dose</topic><topic>macrophages</topic><topic>Macrophages - drug effects</topic><topic>Macrophages - parasitology</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred C57BL</topic><topic>Original Paper</topic><topic>Pharmacognosy. Homeopathy. Health food</topic><topic>Pharmacology. Drug treatments</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kayser, O</creatorcontrib><creatorcontrib>Kiderlen, A.F</creatorcontrib><creatorcontrib>Folkens, U</creatorcontrib><creatorcontrib>Kolodziej, H</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><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><jtitle>Planta medica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kayser, O</au><au>Kiderlen, A.F</au><au>Folkens, U</au><au>Kolodziej, H</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In vitro leishmanicidal activity of aurones</atitle><jtitle>Planta medica</jtitle><addtitle>Planta Med</addtitle><date>1999-05-01</date><risdate>1999</risdate><volume>65</volume><issue>4</issue><spage>316</spage><epage>319</epage><pages>316-319</pages><issn>0032-0943</issn><eissn>1439-0221</eissn><coden>PLMEAA</coden><abstract>Abstract:
A series of aurones with drug-potential for LEISHMANIA infections was identified IN VITRO using both
a direct cytotoxicity assay against extracellular promastigotes of
LEISHMANIA DONOVANI, L. INFANTUM, L. ENRIETTII, and L. MAJOR , and a test against intracellular amastigote forms of
L. DONOVANI residing within murine macrophages. The most active
aurone (6-hydroxy-2-[phenylmethylene]-3(2H)-benzofuranone)
had an EC
50
of 0.45 μg/ml in the extra-, and an EC
50
of 1.40 μg/ml in the intracellular assay. Other aurones
were active between 0.06 - 12.50 μg/ml and
0.04 - 7.81 μg/ml, respectively. When tested
against murine bone marrow-derived macrophages as a mammalian host cell control,
the compounds showed only moderate cytotoxicity (EC
50
2.32 to > 25.0 μg/ml).
This is the first report on aurones as a new class of natural products with
leishmanicidal activity.</abstract><cop>Stuttgart</cop><cop>New York, NY</cop><pub>Thieme</pub><pmid>10364835</pmid><doi>10.1055/s-1999-13993</doi><tpages>4</tpages></addata></record> |
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| ispartof | Planta medica, 1999-05, Vol.65 (4), p.316-319 |
| issn | 0032-0943 1439-0221 |
| language | eng |
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| source | MEDLINE; Thieme Connect Journals |
| subjects | Animals antiprotozoal agents Antiprotozoal Agents - pharmacology Benzofurans - pharmacology Benzylidene Compounds - pharmacology bioassays Biological and medical sciences Bone Marrow Cells - drug effects Bone Marrow Cells - parasitology Cell Line Cell Survival - drug effects chemical structure cytotoxicity General pharmacology hosts in vitro Leishmania - drug effects Leishmania donovani Leishmania enriettii Leishmania infantum Leishmania major lethal dose macrophages Macrophages - drug effects Macrophages - parasitology Medical sciences Mice Mice, Inbred C57BL Original Paper Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments |
| title | In vitro leishmanicidal activity of aurones |
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