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Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells
Summary In the present investigation the antiproliferative activity of thirteen derivatives of betulinic acid and betulin was tested against five different tumor cell lines. The toxicity against normal human fibroblasts (WWO70327) and the mode of cell death on HT-29 (colon cancer) as well as caspase...
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| Published in: | Investigational new drugs 2011-04, Vol.29 (2), p.266-272 |
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| cited_by | cdi_FETCH-LOGICAL-c371t-13b9937a282d01426bede2a959b74380ba9d12f5924100d406f06dac7cfb70c13 |
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| cites | cdi_FETCH-LOGICAL-c371t-13b9937a282d01426bede2a959b74380ba9d12f5924100d406f06dac7cfb70c13 |
| container_end_page | 272 |
| container_issue | 2 |
| container_start_page | 266 |
| container_title | Investigational new drugs |
| container_volume | 29 |
| creator | Kommera, Harish Kaluđerović, Goran N. Kalbitz, Jutta Paschke, Reinhard |
| description | Summary
In the present investigation the antiproliferative activity of thirteen derivatives of betulinic acid and betulin was tested against five different tumor cell lines. The toxicity against normal human fibroblasts (WWO70327) and the mode of cell death on HT-29 (colon cancer) as well as caspase activity induced by the most active compounds,
9
(3-O-chloroacetylbetulinic acid) and
15
(28-O-chloroacetylbetulin) were determined. Investigated derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. Treatment of HT-29 cells for 24 h with
9
and
15
induced apoptosis, as observed by dye exclusion test (trypan blue) and confirmed by the appearance of a typical ladder pattern in the DNA fragmentation assay. |
| doi_str_mv | 10.1007/s10637-009-9358-x |
| format | article |
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In the present investigation the antiproliferative activity of thirteen derivatives of betulinic acid and betulin was tested against five different tumor cell lines. The toxicity against normal human fibroblasts (WWO70327) and the mode of cell death on HT-29 (colon cancer) as well as caspase activity induced by the most active compounds,
9
(3-O-chloroacetylbetulinic acid) and
15
(28-O-chloroacetylbetulin) were determined. Investigated derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. Treatment of HT-29 cells for 24 h with
9
and
15
induced apoptosis, as observed by dye exclusion test (trypan blue) and confirmed by the appearance of a typical ladder pattern in the DNA fragmentation assay.</description><identifier>ISSN: 0167-6997</identifier><identifier>EISSN: 1573-0646</identifier><identifier>DOI: 10.1007/s10637-009-9358-x</identifier><identifier>PMID: 19957199</identifier><identifier>CODEN: INNDDK</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Acids ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Apoptosis ; Apoptosis - drug effects ; Cancer ; Caspases - metabolism ; Cell culture ; Cell death ; Cell Line, Tumor ; Cell Survival - drug effects ; Chemistry ; Colorectal cancer ; Cytotoxicity ; DNA Fragmentation - drug effects ; Drug dosages ; Drug Screening Assays, Antitumor ; Enzymes ; Fibroblasts ; Humans ; Inhibitory Concentration 50 ; Investigations ; Kinetics ; Laboratories ; Medicine ; Medicine & Public Health ; Natural products ; Oncology ; Penicillin ; Pharmaceuticals ; Pharmacology/Toxicology ; Preclinical Studies ; R&D ; Research & development ; Toxicity ; Triterpenes - chemistry ; Triterpenes - pharmacology</subject><ispartof>Investigational new drugs, 2011-04, Vol.29 (2), p.266-272</ispartof><rights>Springer Science+Business Media, LLC 2009</rights><rights>Springer Science+Business Media, LLC 2011</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c371t-13b9937a282d01426bede2a959b74380ba9d12f5924100d406f06dac7cfb70c13</citedby><cites>FETCH-LOGICAL-c371t-13b9937a282d01426bede2a959b74380ba9d12f5924100d406f06dac7cfb70c13</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.proquest.com/docview/1112130581/fulltextPDF?pq-origsite=primo$$EPDF$$P50$$Gproquest$$H</linktopdf><linktohtml>$$Uhttps://www.proquest.com/docview/1112130581?pq-origsite=primo$$EHTML$$P50$$Gproquest$$H</linktohtml><link.rule.ids>314,780,784,11688,27924,27925,36060,44363,74895</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19957199$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kommera, Harish</creatorcontrib><creatorcontrib>Kaluđerović, Goran N.</creatorcontrib><creatorcontrib>Kalbitz, Jutta</creatorcontrib><creatorcontrib>Paschke, Reinhard</creatorcontrib><title>Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells</title><title>Investigational new drugs</title><addtitle>Invest New Drugs</addtitle><addtitle>Invest New Drugs</addtitle><description>Summary
In the present investigation the antiproliferative activity of thirteen derivatives of betulinic acid and betulin was tested against five different tumor cell lines. The toxicity against normal human fibroblasts (WWO70327) and the mode of cell death on HT-29 (colon cancer) as well as caspase activity induced by the most active compounds,
9
(3-O-chloroacetylbetulinic acid) and
15
(28-O-chloroacetylbetulin) were determined. Investigated derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. Treatment of HT-29 cells for 24 h with
9
and
15
induced apoptosis, as observed by dye exclusion test (trypan blue) and confirmed by the appearance of a typical ladder pattern in the DNA fragmentation assay.</description><subject>Acids</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Apoptosis</subject><subject>Apoptosis - drug effects</subject><subject>Cancer</subject><subject>Caspases - metabolism</subject><subject>Cell culture</subject><subject>Cell death</subject><subject>Cell Line, Tumor</subject><subject>Cell Survival - drug effects</subject><subject>Chemistry</subject><subject>Colorectal cancer</subject><subject>Cytotoxicity</subject><subject>DNA Fragmentation - drug effects</subject><subject>Drug dosages</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Enzymes</subject><subject>Fibroblasts</subject><subject>Humans</subject><subject>Inhibitory Concentration 50</subject><subject>Investigations</subject><subject>Kinetics</subject><subject>Laboratories</subject><subject>Medicine</subject><subject>Medicine & Public Health</subject><subject>Natural products</subject><subject>Oncology</subject><subject>Penicillin</subject><subject>Pharmaceuticals</subject><subject>Pharmacology/Toxicology</subject><subject>Preclinical Studies</subject><subject>R&D</subject><subject>Research & development</subject><subject>Toxicity</subject><subject>Triterpenes - chemistry</subject><subject>Triterpenes - pharmacology</subject><issn>0167-6997</issn><issn>1573-0646</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>M0C</sourceid><recordid>eNp1kM9OwzAMxiMEYmPwAFxQJM4Fu2mb5QgT_6RJXMYRRWmSokxbW5J2GjcegifkSWjVSnDhYlv258_yj5BzhCsE4NcBIWM8AhCRYOk82h-QKaacRZAl2SGZAmY8yoTgE3ISwhoAmODJMZmgECnvwpS8LttalZauvGusr21ZORO-P79ubdNuXElVaehYO02VdoYa691ONW5nA3WlabWlqq7qpgqub9Cm3VaearvZhFNyVKhNsGdjnpGX-7vV4jFaPj88LW6WkWYcmwhZLgTjKp7HBjCJs9waGyuRipwnbA65EgbjIhVx0v1tEsgKyIzSXBc5B41sRi4H39pX760NjVxXrS-7kxIRY2SQznsVDirtqxC8LWTt3Vb5D4kge6ByACo7oLIHKvfdzsXo3OZba343RoKdIB4EoRuVb9b_Of2v6w8bOoLd</recordid><startdate>20110401</startdate><enddate>20110401</enddate><creator>Kommera, Harish</creator><creator>Kaluđerović, Goran N.</creator><creator>Kalbitz, Jutta</creator><creator>Paschke, Reinhard</creator><general>Springer US</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><scope>3V.</scope><scope>7QO</scope><scope>7RV</scope><scope>7WY</scope><scope>7WZ</scope><scope>7X7</scope><scope>7XB</scope><scope>87Z</scope><scope>88E</scope><scope>8AO</scope><scope>8FD</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>8FL</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>BEZIV</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FRNLG</scope><scope>FYUFA</scope><scope>F~G</scope><scope>GHDGH</scope><scope>K60</scope><scope>K6~</scope><scope>K9-</scope><scope>K9.</scope><scope>KB0</scope><scope>L.-</scope><scope>M0C</scope><scope>M0R</scope><scope>M0S</scope><scope>M1P</scope><scope>NAPCQ</scope><scope>P64</scope><scope>PQBIZ</scope><scope>PQBZA</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>Q9U</scope></search><sort><creationdate>20110401</creationdate><title>Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells</title><author>Kommera, Harish ; Kaluđerović, Goran N. ; Kalbitz, Jutta ; Paschke, Reinhard</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c371t-13b9937a282d01426bede2a959b74380ba9d12f5924100d406f06dac7cfb70c13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Acids</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Apoptosis</topic><topic>Apoptosis - drug effects</topic><topic>Cancer</topic><topic>Caspases - metabolism</topic><topic>Cell culture</topic><topic>Cell death</topic><topic>Cell Line, Tumor</topic><topic>Cell Survival - drug effects</topic><topic>Chemistry</topic><topic>Colorectal cancer</topic><topic>Cytotoxicity</topic><topic>DNA Fragmentation - drug effects</topic><topic>Drug dosages</topic><topic>Drug Screening Assays, Antitumor</topic><topic>Enzymes</topic><topic>Fibroblasts</topic><topic>Humans</topic><topic>Inhibitory Concentration 50</topic><topic>Investigations</topic><topic>Kinetics</topic><topic>Laboratories</topic><topic>Medicine</topic><topic>Medicine & Public Health</topic><topic>Natural products</topic><topic>Oncology</topic><topic>Penicillin</topic><topic>Pharmaceuticals</topic><topic>Pharmacology/Toxicology</topic><topic>Preclinical Studies</topic><topic>R&D</topic><topic>Research & development</topic><topic>Toxicity</topic><topic>Triterpenes - chemistry</topic><topic>Triterpenes - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kommera, Harish</creatorcontrib><creatorcontrib>Kaluđerović, Goran N.</creatorcontrib><creatorcontrib>Kalbitz, Jutta</creatorcontrib><creatorcontrib>Paschke, Reinhard</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Biotechnology Research Abstracts</collection><collection>Proquest Nursing & Allied Health Source</collection><collection>ABI/INFORM Collection</collection><collection>ABI/INFORM Global (PDF only)</collection><collection>ProQuest Health and Medical</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>ABI/INFORM Collection</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Technology Research Database</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ABI/INFORM Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni)</collection><collection>ProQuest Central</collection><collection>ProQuest Central Essentials</collection><collection>AUTh Library subscriptions: ProQuest Central</collection><collection>Business Premium Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central</collection><collection>Engineering Research Database</collection><collection>Business Premium Collection (Alumni)</collection><collection>Health Research Premium Collection</collection><collection>ABI/INFORM Global (Corporate)</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Business Collection (Alumni Edition)</collection><collection>ProQuest Business Collection</collection><collection>Consumer Health Database (Alumni Edition)</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>ABI/INFORM Professional Advanced</collection><collection>ABI/INFORM Collection</collection><collection>ProQuest Family Health</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Nursing & Allied Health Premium</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>One Business (ProQuest)</collection><collection>ProQuest One Business (Alumni)</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central Basic</collection><jtitle>Investigational new drugs</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kommera, Harish</au><au>Kaluđerović, Goran N.</au><au>Kalbitz, Jutta</au><au>Paschke, Reinhard</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells</atitle><jtitle>Investigational new drugs</jtitle><stitle>Invest New Drugs</stitle><addtitle>Invest New Drugs</addtitle><date>2011-04-01</date><risdate>2011</risdate><volume>29</volume><issue>2</issue><spage>266</spage><epage>272</epage><pages>266-272</pages><issn>0167-6997</issn><eissn>1573-0646</eissn><coden>INNDDK</coden><abstract>Summary
In the present investigation the antiproliferative activity of thirteen derivatives of betulinic acid and betulin was tested against five different tumor cell lines. The toxicity against normal human fibroblasts (WWO70327) and the mode of cell death on HT-29 (colon cancer) as well as caspase activity induced by the most active compounds,
9
(3-O-chloroacetylbetulinic acid) and
15
(28-O-chloroacetylbetulin) were determined. Investigated derivatives exerted a dose dependent antiproliferative action at micromolar concentrations toward target tumor cell lines. Treatment of HT-29 cells for 24 h with
9
and
15
induced apoptosis, as observed by dye exclusion test (trypan blue) and confirmed by the appearance of a typical ladder pattern in the DNA fragmentation assay.</abstract><cop>Boston</cop><pub>Springer US</pub><pmid>19957199</pmid><doi>10.1007/s10637-009-9358-x</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0167-6997 |
| ispartof | Investigational new drugs, 2011-04, Vol.29 (2), p.266-272 |
| issn | 0167-6997 1573-0646 |
| language | eng |
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| source | ABI/INFORM Collection; Springer Nature |
| subjects | Acids Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis Apoptosis - drug effects Cancer Caspases - metabolism Cell culture Cell death Cell Line, Tumor Cell Survival - drug effects Chemistry Colorectal cancer Cytotoxicity DNA Fragmentation - drug effects Drug dosages Drug Screening Assays, Antitumor Enzymes Fibroblasts Humans Inhibitory Concentration 50 Investigations Kinetics Laboratories Medicine Medicine & Public Health Natural products Oncology Penicillin Pharmaceuticals Pharmacology/Toxicology Preclinical Studies R&D Research & development Toxicity Triterpenes - chemistry Triterpenes - pharmacology |
| title | Lupane Triterpenoids—Betulin and Betulinic acid derivatives induce apoptosis in tumor cells |
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