The study of a novel sorafenib derivative HLC-080 as an antitumor agent.
In this study, our objective is to evaluate the potential of a novel Sorafenib derivative, named HLC-080, as a new anticancer agent for colon cancer. We firstly carried out MTT assay, colony formation assay, flow cytometry analysis and transwell invasion assay to determine effect of our compound HLC...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Public Library of Science (PLoS)
2014-01-01
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| Series: | PLoS ONE |
| Online Access: | http://europepmc.org/articles/PMC4086976?pdf=render |
| _version_ | 1811270995185500160 |
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| author | Ke Tang Can Luo Yan Li Chenshu Lu Wanqi Zhou Haihong Huang Xiaoguang Chen |
| author_facet | Ke Tang Can Luo Yan Li Chenshu Lu Wanqi Zhou Haihong Huang Xiaoguang Chen |
| author_sort | Ke Tang |
| collection | DOAJ |
| description | In this study, our objective is to evaluate the potential of a novel Sorafenib derivative, named HLC-080, as a new anticancer agent for colon cancer. We firstly carried out MTT assay, colony formation assay, flow cytometry analysis and transwell invasion assay to determine effect of our compound HLC-080 on cell viability, anti-proliferation activity, cell cycle arrest and the intervention on cell invasion, respectively. On the other hand, in vivo antitumor activity of HLC-080 was also tested using H22 xenograft model and the angiogenesis effect of HLC-080 was measured by EA.hy926 tube formation assay. The expression levels of various proteins in HLC-080 treated with HT-29 cell lines were examined using Western blot and ELISA experiments. The results showed that HLC-080 could dramatically inhibit the growth and colony formation of various tumor cells, therefore exhibited remarkable antitumor activity. HLC-080 can induce cell cycle arrest at G1 phase in HT-29 cells and subsequently inhibit the invasive potential of colon cancer cells. HLC-080 also exhibits anti-angiogenesis effect in EA.hy926 model. Additionally, the in vivo study showed that HLC-080 was able to reduced the tumor weight with the rate of 35.81%. And at the concentration of 0.352±0.034 µM, HLC-080 is able to reduce half of the regular protein level of p-c-Raf (Ser259), consequently block Raf/MEK/ERK signaling in HT-29 cell lines. In conclusion, our study suggests that Sorafenib derivative HLC-080 has the potential to inhibit cell proliferation and angiogenesis, Since, HLC-080 is particularly active against human colon cancer cells, our study highlights that HLC-080 and its related analogues may serve as a new anti-cancer drug, particularly against colon cancer. |
| first_indexed | 2024-04-12T22:13:21Z |
| format | Article |
| id | doaj.art-aebb31a785d34243911cdd7d761ea070 |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-04-12T22:13:21Z |
| publishDate | 2014-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-aebb31a785d34243911cdd7d761ea0702022-12-22T03:14:40ZengPublic Library of Science (PLoS)PLoS ONE1932-62032014-01-0197e10188910.1371/journal.pone.0101889The study of a novel sorafenib derivative HLC-080 as an antitumor agent.Ke TangCan LuoYan LiChenshu LuWanqi ZhouHaihong HuangXiaoguang ChenIn this study, our objective is to evaluate the potential of a novel Sorafenib derivative, named HLC-080, as a new anticancer agent for colon cancer. We firstly carried out MTT assay, colony formation assay, flow cytometry analysis and transwell invasion assay to determine effect of our compound HLC-080 on cell viability, anti-proliferation activity, cell cycle arrest and the intervention on cell invasion, respectively. On the other hand, in vivo antitumor activity of HLC-080 was also tested using H22 xenograft model and the angiogenesis effect of HLC-080 was measured by EA.hy926 tube formation assay. The expression levels of various proteins in HLC-080 treated with HT-29 cell lines were examined using Western blot and ELISA experiments. The results showed that HLC-080 could dramatically inhibit the growth and colony formation of various tumor cells, therefore exhibited remarkable antitumor activity. HLC-080 can induce cell cycle arrest at G1 phase in HT-29 cells and subsequently inhibit the invasive potential of colon cancer cells. HLC-080 also exhibits anti-angiogenesis effect in EA.hy926 model. Additionally, the in vivo study showed that HLC-080 was able to reduced the tumor weight with the rate of 35.81%. And at the concentration of 0.352±0.034 µM, HLC-080 is able to reduce half of the regular protein level of p-c-Raf (Ser259), consequently block Raf/MEK/ERK signaling in HT-29 cell lines. In conclusion, our study suggests that Sorafenib derivative HLC-080 has the potential to inhibit cell proliferation and angiogenesis, Since, HLC-080 is particularly active against human colon cancer cells, our study highlights that HLC-080 and its related analogues may serve as a new anti-cancer drug, particularly against colon cancer.http://europepmc.org/articles/PMC4086976?pdf=render |
| spellingShingle | Ke Tang Can Luo Yan Li Chenshu Lu Wanqi Zhou Haihong Huang Xiaoguang Chen The study of a novel sorafenib derivative HLC-080 as an antitumor agent. PLoS ONE |
| title | The study of a novel sorafenib derivative HLC-080 as an antitumor agent. |
| title_full | The study of a novel sorafenib derivative HLC-080 as an antitumor agent. |
| title_fullStr | The study of a novel sorafenib derivative HLC-080 as an antitumor agent. |
| title_full_unstemmed | The study of a novel sorafenib derivative HLC-080 as an antitumor agent. |
| title_short | The study of a novel sorafenib derivative HLC-080 as an antitumor agent. |
| title_sort | study of a novel sorafenib derivative hlc 080 as an antitumor agent |
| url | http://europepmc.org/articles/PMC4086976?pdf=render |
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