Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein
In this work, the anticancer activity of chamaejasmine was studied by evaluating its in vitro cytotoxicity against several human cancer cell lines (MCF-7, A549, SGC-7901, HCT-8, HO-4980, Hela, HepG2, PC-3, LNCap, Vero and MDCK) using the MTT assay. Results indicated chamaejasmine showed more notable...
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| Format: | Article |
| Language: | English |
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MDPI AG
2011-07-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/16/8/6243/ |
| _version_ | 1818290160396140544 |
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| author | Yingkun Nie Wenlong Fang Songtao Liu |
| author_facet | Yingkun Nie Wenlong Fang Songtao Liu |
| author_sort | Yingkun Nie |
| collection | DOAJ |
| description | In this work, the anticancer activity of chamaejasmine was studied by evaluating its in vitro cytotoxicity against several human cancer cell lines (MCF-7, A549, SGC-7901, HCT-8, HO-4980, Hela, HepG2, PC-3, LNCap, Vero and MDCK) using the MTT assay. Results indicated chamaejasmine showed more notable anticancer activity than taxol against PC-3 cells, with IC50 values of 2.28 and 3.98 µM, respectively. Furthermore, Western blot analysis showed that chamaejasmine was able to increase the expression of β-tubulin, but not α-tubulin. In silico simulations indicated that chamaejasmine specifically interacts with the active site which is located at the top of β-tubulin, thanks to the presence of strong hydrophobic effects between the core templates and the hydrophobic surface of the TB active site. The binding energy (Einter) was calculated to be −164.77 kcal·mol−1. Results presented here suggest that chamaejasmine possesses anti-cancer properties relating to β-tubulin depolymerization inhibition, and therefore is a potential source of anticancer leads for the pharmaceutical industry. |
| first_indexed | 2024-12-13T02:23:45Z |
| format | Article |
| id | doaj.art-187ddb06567943db8120628ae84f38ae |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-13T02:23:45Z |
| publishDate | 2011-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-187ddb06567943db8120628ae84f38ae2022-12-22T00:02:41ZengMDPI AGMolecules1420-30492011-07-011686243625410.3390/molecules16086243Anticancer Activity of Chamaejasmine: Effect on Tubulin ProteinYingkun NieWenlong FangSongtao LiuIn this work, the anticancer activity of chamaejasmine was studied by evaluating its in vitro cytotoxicity against several human cancer cell lines (MCF-7, A549, SGC-7901, HCT-8, HO-4980, Hela, HepG2, PC-3, LNCap, Vero and MDCK) using the MTT assay. Results indicated chamaejasmine showed more notable anticancer activity than taxol against PC-3 cells, with IC50 values of 2.28 and 3.98 µM, respectively. Furthermore, Western blot analysis showed that chamaejasmine was able to increase the expression of β-tubulin, but not α-tubulin. In silico simulations indicated that chamaejasmine specifically interacts with the active site which is located at the top of β-tubulin, thanks to the presence of strong hydrophobic effects between the core templates and the hydrophobic surface of the TB active site. The binding energy (Einter) was calculated to be −164.77 kcal·mol−1. Results presented here suggest that chamaejasmine possesses anti-cancer properties relating to β-tubulin depolymerization inhibition, and therefore is a potential source of anticancer leads for the pharmaceutical industry.http://www.mdpi.com/1420-3049/16/8/6243/chamaejasmineanti-cancer activityPC-3 cellstubulindocking |
| spellingShingle | Yingkun Nie Wenlong Fang Songtao Liu Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein Molecules chamaejasmine anti-cancer activity PC-3 cells tubulin docking |
| title | Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein |
| title_full | Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein |
| title_fullStr | Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein |
| title_full_unstemmed | Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein |
| title_short | Anticancer Activity of Chamaejasmine: Effect on Tubulin Protein |
| title_sort | anticancer activity of chamaejasmine effect on tubulin protein |
| topic | chamaejasmine anti-cancer activity PC-3 cells tubulin docking |
| url | http://www.mdpi.com/1420-3049/16/8/6243/ |
| work_keys_str_mv | AT yingkunnie anticanceractivityofchamaejasmineeffectontubulinprotein AT wenlongfang anticanceractivityofchamaejasmineeffectontubulinprotein AT songtaoliu anticanceractivityofchamaejasmineeffectontubulinprotein |