scholarly journals The colchicine derivative CT20126 shows a novel microtubule-modulating activity with apoptosis

2013 ◽  
Vol 45 (4) ◽  
pp. e19-e19 ◽  
Author(s):  
Sung-Kuk Kim ◽  
Sang-Min Cho ◽  
Ho Kim ◽  
Heon Seok ◽  
Soon-Ok Kim ◽  
...  
Keyword(s):  
Colchicine Derivative

Binding of a bicyclic colchicine derivative to tubulin

1985 ◽  
Vol 321 (7) ◽  
pp. 636-636
Author(s):  
Heinz Decker ◽  
James C. Lee
Keyword(s):  
Colchicine Derivative

scholarly journals Fluorescein colchicine. Synthesis, purification, and biological activity.

1978 ◽  
Vol 76 (3) ◽  
pp. 619-627 ◽  
Author(s):  
J I Clark ◽  
D Garland
Keyword(s):  
Spectral Analysis ◽  
Biological Activity ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Fluorescein Isothiocyanate ◽  
Significant Loss ◽  
Colchicine Derivative ◽  
Layer Chromatography ◽  
Kinetics Of ◽  
Brain Tubulin

The synthesis of a fluorescent colchicine derivative permits the localization of colchicine-binding receptors in cells. Fluorescein colchicine (FC) was prepared by the addition of fluorescein isothiocyanate to deacetyl colchicine. The product, FC, was separated from the reactants by thin-layer chromatography (TLC). The purity of FC was demonstrated by TLC, UV spectral analysis, and analysis of the kinetics of photodecomposition. FC inhibited [3H] colchicine binding to purified brain tubulin. The biological activity of FC was compared to the activity of unlabeled colchicine on mitosis, motility, secretion, and myogenesis. The effects of FC were identical to those of unlabeled colchicine in all biological systems tested. The results demonstrate that FC may be substituted for colchicine in biological experiments without significant loss in specificity or effectiveness.

Disposition and metabolism of the colchicine derivative [14C]-ZD6126 in rat and dog

Xenobiotica ◽  
2008 ◽  
Vol 38 (4) ◽  
pp. 399-421 ◽  
Author(s):  
E. A. Partridge ◽  
R. A. D'souza ◽  
E. M. Lenz ◽  
S. M. Smith ◽  
J. Clarkson-Jones ◽  
...  
Keyword(s):  
Colchicine Derivative

scholarly journals Size-Dependent Biodistribution of Fluorescent Furano-Allocolchicinoid-Chitosan Formulations in Mice

Polymers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 2045
Author(s):  
Iuliia Gracheva ◽  
Maria Konovalova ◽  
Dmitrii Aronov ◽  
Ekaterina Moiseeva ◽  
Alexey Fedorov ◽  
...  
Keyword(s):  
Chitosan Nanoparticles ◽  
Ionotropic Gelation ◽  
Size Dependent ◽  
Hydrophobic Substances ◽  
Tissue Homogenates ◽  
Colchicine Derivative ◽  
Kidney Liver ◽  
Colchicine Derivatives

The aim of this study was to compare the biodistribution in mice of functionalized rhodamine B (Rh) labeled colchicine derivative furano-allocolchicinoid (AC, 6) either conjugated to 40 kDa chitosan (AC-Chi, 8) or encapsulated into chitosan nanoparticles (AC-NPs). AC-NPs were formed by ionotropic gelation and were 400–450 nm in diameter as estimated in mice by dynamic light scattering and confocal microscopy. AC-Chi and AC-NPs preserved the specific colchicine activity in vitro. AC preparations were once IV injected into C75BL/6 mice; muscles, spleen, kidney, liver, lungs, blood cells and serum were collected at 30 min, 2, 5, 10, and 20 h post injection. To analyze the distribution of the furano-allocolchicinoid preparations in body liquids and tissues, Rh was measured directly in sera or extracted by acidic ethanol from tissue homogenates. Preliminary Rh extraction rate was estimated in vitro in tissue homogenates and was around 25–30% from total quantity added. After in vivo injection, AC-NPs were accumulated more in liver and spleen, while less in kidney and lungs in comparison with free AC and AC-Chi. Therefore, incorporation of colchicine derivatives as well as other hydrophobic substances into nano/micro sized carriers may help redistribute the drug to different organs and, possibly, improve antitumor accumulation.

Effect of Pretreatment with Colchicine or a Colchicine Derivative on Hemopoiesis in Irradiated Mice

1963 ◽  
Vol 19 (4) ◽  
pp. 621 ◽  
Author(s):  
Willie W. Smith ◽  
Ilo M. Alderman ◽  
Carol A. Schneider ◽  
Jerome Cornfield
Keyword(s):  
Colchicine Derivative

scholarly journals Novel colchicine conjugate with unusual effect on the microtubules of cancer cells

2020 ◽  
Vol 92 (8) ◽  
pp. 1217-1226
Author(s):  
Olga N. Zefirova ◽  
Evgenia V. Nurieva ◽  
Birgit Wobith ◽  
Svetlana Schulz ◽  
Nikolay A. Zefirov ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Anticancer Agents ◽  
Anticancer Agent ◽  
Research Data ◽  
Tubulin Polymerization ◽  
Structure Activity ◽  
Associated Proteins ◽  
Colchicine Derivative ◽  
Colchicine Derivatives

AbstractColchicine derivative bearing substituted bispidine moiety, namely N-{7-(3,7-Di-(tert-butoxycarbonyl)-1,5-dimethyl-3,7-diazabicyclo[3.3.1]nonan-9-yl)-oxy-7-oxoheptanoyl}-N-deacetylcolchicine, was synthesized and tested for its effect on the net of microtubules (MT) in lung cancer cells A549. The compound induced not only MT depolymerization but stimulated the formation of small tubulin aggregates and long tubulin fibrils localized mainly around nuclei. The assemblies were morphologically different from tubulin clusters induced by structurally related anticancer agent tubuloclustin. The biotests data demonstrate that the depolymerization takes place for both pure tubulin and tubulin in cellulo, while fibrils are formed only in the cells. The research data of structure–activity relationship for several similar colchicine derivatives synthesized in the work give evidence for the proposition that the initial conjugate may interact not only with tubulin and MT in the cells, but also with MT-associated proteins, involved in the process of tubulin polymerization. The ability to affect simultaneously MAP – tubulin interactions opens attractive prospects in the design of novel anticancer agents.

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