Differential toxicity of vincristine and vinblastine against cells of a cloned subline of human promyelocytic leukemia (HL-60/Cl) was dependent on exposure conditions. During continuous exposures of 48 h, vincristine and vinblastine were equitoxic with drug concentrations that inhibited proliferation rates by 50% of 7.6 and 8.1 nM, respectively. When cells were subjected to 4-h exposures and tr...

background: tubulin protein being the fundamental unit of microtubules is actively involved in cell division thus making them a potential anti-cancer drug target. in spite of many reported drugs against tubulin, few of them have started developing resistance in human β-tubulin due to amino acid substitutions. methods: in this study we generated three mutants (f270v, a364t and q292e) using model...

Disorazoles comprise a family of 29 macrocyclic polyketides isolated from the fermentation broth of the myxobacterium Sorangium cellulosum. The major fermentation product, disorazole A1, was found previously to irreversibly bind to tubulin and to have potent cytotoxic activity against tumor cells, possibly because of its highly electrophilic epoxide moiety. To test this hypothesis, we synthesiz...

TAKANO, S. Difference in Effects o f Vinblastine and V incristine on the Dog Platelet Aggregation. Tohoku J. exp. Med., 1981, 135 (1), 79-85 The present study was attempted to determine difference in effects of vinblastine and vincristine on ADP-induced aggregation of dog platelets. Vinblastine manifested biphasic influence depending upon concentrations, i.e., in low concentrations (0.2-20 ,ug/...

in this study, monte carlo statistical mechanical simulations for vinblastine and vincristine werecarried out in standard manner using the metropolis sampling technique in canonical (t, v, n)ensemble., geometrical optimizations of vinblastine and vincristine were carried out with the hfmethod coupled to 6-31g(d) basis sets for all atoms. simulation was done by four force fields ofmm+, bio+, amb...

Vinca alkaloids used in anticancer therapy are the well-known vinblastine and vincristine as classical antitumor agents. These dimeric molecules consist of two monomers, vindoline catharanthine, which have no particular activity on their own. The goal our research work was to obtain derivatives one these, vindoline, resulted with important antiproliferative effect. This type were hybrids; conju...

Background: Chemotherapy is expected to remain an important part of invasive urothelial carcinoma (UC) treatment. Strategies to enhance chemotherapy efficacy are needed. Objective: To determine the chemotherapy-enhancing effects of a nonselective cyclooxygenase (COX) inhibitor on vinblastine in a naturally-occurring canine model of invasive UC. Methods: With IACUC approval, privately-owned dogs...

Tubulin plays essential roles in vital cellular activities and is the target of a wide range proteins ligands. Here, using combined computational crystallographic fragment screening approach, we addressed question how many binding sites exist tubulin. We identified 27 distinct sites, which 11 have not been described previously, analyzed their relationship to known tubulin–protein tubulin–ligand...

The objective of the study was to prepare vinblastine microparticles by supercritical antisolvent process using N-methyl-2-pyrrolidone as solvent and carbon dioxide as antisolvent and evaluate its physicochemical properties. The effects of four process variables, pressure, temperature, drug concentration and drug solution flow rate, on drug particle formation during the supercritical antisolven...

microtubules are unique cytoskeletal structures that have structural subunits of αβ tubulin. taxol is a typical microtubule stabilizing drug. the epothilones are other natural products with similar mechanism of action totaxol. despite the highly conserved nature of β-tubulin, some organism like saccharomyces cerevesia is resistance to taxol, but sensitive to epothilones. in order to find differ...