title: Anticancer activity of chamaejasmine: effect on tubulin protein.
abstract: 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 (E(inter)) 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.
authors.affiliation: Department of Rheumatology, The Second Hospital Affiliated Harbin Medical University, Harbin 150086, China.
authors.forename: Wenlong
authors.initials: W
authors.lastname: Fang
authors.forename: Songtao
authors.initials: S
authors.lastname: Liu
authors.forename: Yingkun
authors.initials: Y
authors.lastname: Nie
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology* / Q000627:therapeutic use; D044946:Biflavonoids / Q000494:pharmacology* / Q000627:therapeutic use; D015153:Blotting, Western; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D002522:Chlorocebus aethiops; D004285:Dogs; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D017239:Paclitaxel / Q000494:pharmacology; D011485:Protein Binding; D013816:Thermodynamics; D014404:Tubulin / Q000096:biosynthesis* / Q000737:chemistry / Q000378:metabolism; D014709:Vero Cells
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D044946:Biflavonoids; D014404:Tubulin; C511440:chamaejasmine; D017239:Paclitaxel