Design, synthesis and biological evaluation of novel betulinic acid derivatives
<p>Abstract</p> <p>Background</p> <p>Tumor, is one of the major reason for human death, due to its widespread occurrence. Betulinic acid derivatives have attracted considerable attention as cancer chemopreventive agents and also as cancer therapeutics. Many of its deriv...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
BMC
2012-11-01
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| Series: | Chemistry Central Journal |
| Online Access: | http://journal.chemistrycentral.com/content/6/1/141 |
| _version_ | 1819280025636044800 |
|---|---|
| author | Yang Shengjie Liang Na Li Hu Xue Wei Hu Deyu Jin Linhong Zhao Qi Yang Song |
| author_facet | Yang Shengjie Liang Na Li Hu Xue Wei Hu Deyu Jin Linhong Zhao Qi Yang Song |
| author_sort | Yang Shengjie |
| collection | DOAJ |
| description | <p>Abstract</p> <p>Background</p> <p>Tumor, is one of the major reason for human death, due to its widespread occurrence. Betulinic acid derivatives have attracted considerable attention as cancer chemopreventive agents and also as cancer therapeutics. Many of its derivatives inhibit the growth of human cancer cell lines by triggering apoptosis. With this background, we planned to synthesize a series of betulinic acid derivatives to assess their antiproliferation efficacy on human cancer cell lines.</p> <p>Results</p> <p>A series of novel betulinic acid derivatives were designed and synthesized as highlighted by the preliminary antitumor evaluation against MGC-803, PC3, A375, Bcap-37 and A431 human cancer cell lines <it>in vitro</it>. The pharmacological results showed that some of the compounds displayed moderate to high levels of antitumor activities with most of new exhibiting higher inhibitory activities compared to BA. The IC<sub>50</sub> values of compound 3c on the five cancer cell lines were 2.3, 4.6, 3.3, 3.6, and 4.3 μM, respectively. Subsequent fluorescence staining and flow cytometry analysis (FCM) indicated that compound 3c could induce apoptosis in MGC-803 and PC3 cell lines, and the apoptosis ratios reached the peak (37.38% and 33.74%) after 36 h of treatment at 10 μM.</p> <p>Conclusions</p> <p>This study suggests that most of betulinic acid derivatives could inhibit the growth of human cancer cell lines. Furthermore, compound 3c could induce apoptosis of cancer cells.</p> |
| first_indexed | 2024-12-24T00:37:14Z |
| format | Article |
| id | doaj.art-8270641c3bfa4686a7a365f770ba0a72 |
| institution | Directory Open Access Journal |
| issn | 1752-153X |
| language | English |
| last_indexed | 2024-12-24T00:37:14Z |
| publishDate | 2012-11-01 |
| publisher | BMC |
| record_format | Article |
| series | Chemistry Central Journal |
| spelling | doaj.art-8270641c3bfa4686a7a365f770ba0a722022-12-21T17:24:03ZengBMCChemistry Central Journal1752-153X2012-11-016114110.1186/1752-153X-6-141Design, synthesis and biological evaluation of novel betulinic acid derivativesYang ShengjieLiang NaLi HuXue WeiHu DeyuJin LinhongZhao QiYang Song<p>Abstract</p> <p>Background</p> <p>Tumor, is one of the major reason for human death, due to its widespread occurrence. Betulinic acid derivatives have attracted considerable attention as cancer chemopreventive agents and also as cancer therapeutics. Many of its derivatives inhibit the growth of human cancer cell lines by triggering apoptosis. With this background, we planned to synthesize a series of betulinic acid derivatives to assess their antiproliferation efficacy on human cancer cell lines.</p> <p>Results</p> <p>A series of novel betulinic acid derivatives were designed and synthesized as highlighted by the preliminary antitumor evaluation against MGC-803, PC3, A375, Bcap-37 and A431 human cancer cell lines <it>in vitro</it>. The pharmacological results showed that some of the compounds displayed moderate to high levels of antitumor activities with most of new exhibiting higher inhibitory activities compared to BA. The IC<sub>50</sub> values of compound 3c on the five cancer cell lines were 2.3, 4.6, 3.3, 3.6, and 4.3 μM, respectively. Subsequent fluorescence staining and flow cytometry analysis (FCM) indicated that compound 3c could induce apoptosis in MGC-803 and PC3 cell lines, and the apoptosis ratios reached the peak (37.38% and 33.74%) after 36 h of treatment at 10 μM.</p> <p>Conclusions</p> <p>This study suggests that most of betulinic acid derivatives could inhibit the growth of human cancer cell lines. Furthermore, compound 3c could induce apoptosis of cancer cells.</p>http://journal.chemistrycentral.com/content/6/1/141 |
| spellingShingle | Yang Shengjie Liang Na Li Hu Xue Wei Hu Deyu Jin Linhong Zhao Qi Yang Song Design, synthesis and biological evaluation of novel betulinic acid derivatives Chemistry Central Journal |
| title | Design, synthesis and biological evaluation of novel betulinic acid derivatives |
| title_full | Design, synthesis and biological evaluation of novel betulinic acid derivatives |
| title_fullStr | Design, synthesis and biological evaluation of novel betulinic acid derivatives |
| title_full_unstemmed | Design, synthesis and biological evaluation of novel betulinic acid derivatives |
| title_short | Design, synthesis and biological evaluation of novel betulinic acid derivatives |
| title_sort | design synthesis and biological evaluation of novel betulinic acid derivatives |
| url | http://journal.chemistrycentral.com/content/6/1/141 |
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