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Journal articles on the topic 'Colchicine Complexes'

Author: Grafiati

Published: 7 June 2025

Last updated: 2 August 2025

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1

Pang, Tao-Tao, and Xu-Yan Zhang. "Detection of Colchicine using p-Sulfonated Calix[4]arene Modified Electrode." Asian Journal of Chemistry 31, no. 11 (2019): 2663–68. http://dx.doi.org/10.14233/ajchem.2019.21695.

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Complex characteristics of p-sulfonated calix[4]arene (SC4A) and colchicine were examined using various techniques. Electrochemical impedance spectroscopy results enabled observation of the colchicine-SC4A interaction, and indicated that SC4A had high sensitivity to colchicine with a detection limit (S/N = 3) of 2 × 10-9 mol L-1. Cyclic voltammetry results indicated that the structural matching effect and the electrostatic interaction were the dominant stabilizing factors for the host-guest complexes of colchicine and SC4A. Molecular mechanics simulation showed that the benzene ring of colchic

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2

Vaishali, H. Gaikwad, R. Borude Kailash, Khade B.C. та B. Sabale Vaibhav. "Molecular Docking Study of Biologically Active Ligand and the Insights of Synthesis, Characterization and In Vitro Studies of Derivatives of β-tubulin Polymerization Inhibitor as Antigout Agent". Indian Journal of Science and Technology 13, № 7 (2020): 756–66. https://doi.org/10.17485/ijst/2020/v13i07/149615.

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Abstract <strong>Background/objective:</strong> The aim of the study is to synthesize derivatives of colchicine, which is an anti-gout drug, and to enhance the antimicrobial activity of it. As it is observed in case study of drug– drug interaction, i.e. Colchicine and clarithromycin, which is known as antimicrobial drug has given fatal results, in consequence to that we have tried to enhance the antimicrobial activity of the drug itself, as there is always a need of antimicrobial drugs in the treatment of gout. In addition, to study the binding of protein and colchicine through mole

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3

Skoufias, Dimitrios A., and Leslie Wilson. "Mechanism of inhibition of microtubule polymerization by colchicine: inhibitory potencies of unliganded colchicine and tubulin-colchicine complexes." Biochemistry 31, no. 3 (1992): 738–46. http://dx.doi.org/10.1021/bi00118a015.

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4

Barkovskiy, Mikhail, Elena Ilyukhina, Martin Dauner, Andreas Eichinger, and Arne Skerra. "An engineered lipocalin that tightly complexes the plant poison colchicine for use as antidote and in bioanalytical applications." Biological Chemistry 400, no. 3 (2019): 351–66. http://dx.doi.org/10.1515/hsz-2018-0342.

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Abstract Colchicine is a toxic alkaloid prevalent in autumn crocus (Colchicum autumnale) that binds to tubulin and inhibits polymerization of microtubules. Using combinatorial and rational protein design, we have developed an artificial binding protein based on the human lipocalin 2 that binds colchicine with a dissociation constant of 120 pm, i.e. 10000-fold stronger than tubulin. Crystallographic analysis of the engineered lipocalin, dubbed Colchicalin, revealed major structural changes in the flexible loop region that forms the ligand pocket at the open end of the eight-stranded β-barrel, r

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5

Sun, Kewei, Zhonghao Sun, Fenglan Zhao, Guangzhi Shan, and Qingguo Meng. "Recent advances in research of colchicine binding site inhibitors and their interaction modes with tubulin." Future Medicinal Chemistry 13, no. 9 (2021): 839–58. http://dx.doi.org/10.4155/fmc-2020-0376.

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Microtubules have been a concerning target of cancer chemotherapeutics for decades, and several tubulin-targeted agents, such as paclitaxel, vincristine and vinorelbine, have been approved. The colchicine binding site is one of the primary targets on microtubules and possesses advantages compared with other tubulin-targeted agents, such as inhibitors of tumor vessels and overcoming P-glycoprotein overexpression-mediated multidrug resistance. This study reviews and summarizes colchicine binding site inhibitors reported in recent years with structural studies via the crystal structures of comple

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6

Verma, R. C., P. Vyas, and S. N. Raina. "The effect of colchicine on meiosis in the Rhoeo discolor stabile complex translocation heterozygote." Genome 35, no. 4 (1992): 611–13. http://dx.doi.org/10.1139/g92-091.

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Rhoeo discolor (2n = 12) was used to study the effect of colchicine on chromosome pairing during meiosis. Pachytene pairing appeared unaffected, but only 17.5% of the PMCs formed a ring of 12 chromosomes at metaphase I of meiosis. While 27.5% of cells had a complete chain of 12, 49.0% had chain configurations of varying (2–11) number of chromosomes and 6.0% had complete univalence. Adjacent orientation was found in the majority of cells with chain complexes of 2–11 chromosomes. The result was highly disturbed anaphase I where 58.4% PMCs were abnormal. It is concluded that the presence of aberr

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7

VANDECANDELAERE, André, Stephen R. MARTIN, and Yves ENGELBORGHS. "Response of microtubules to the addition of colchicine and tubulin–colchicine: evaluation of models for the interaction of drugs with microtubules." Biochemical Journal 323, no. 1 (1997): 189–96. http://dx.doi.org/10.1042/bj3230189.

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The effects of free drug and tubulin-drug complexes on steady-state GTP/GDP-associated microtubules and on equilibrium guanosine 5´-[β,γ-imido]triphosphate-associated microtubules are compared. The addition of colchicine or the tubulin-colchicine complex (TuCol) to steady-state microtubules induces microtubule disassembly. Only limited disassembly of equilibrium microtubules is observed under similar conditions. Addition of colchicine or the bifunctional colchicine analogue 2-methoxy-5-(2´,3´,4´-trimethoxyphenyl)tropone to preassembled steady-state or equilibrium microtubules does induce disas

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8

Karpov, P. A., S. I. Spivak, O. V. Rayevsky, O. Yu Nyporko, S. P. Ozheredov та Ya B. Blume. "Assessment of structural peculiarities of glaziovianin A interaction with human α-, β and γ-tubulins". Faktori eksperimental'noi evolucii organizmiv 22 (9 вересня 2018): 340–44. http://dx.doi.org/10.7124/feeo.v22.972.

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Aim. To determine the features of the ligand-protein interaction of glaziovianin A and human α-, β- and γ-tubulin. Methods. Protein and ligand spatial structure modelling (I-Tasser, Grid), molecular docking (CCDC Gold), molecular dynamics simulation (GROMACS). Results. Using the method of molecular docking in CCDC Gold ligand-protein complexes of glaziovianin A and human α-, β- and γ-tubulin were reconstructed. Studied ligand interactions in GTP/GDP-exchange and colchicine binding sites of different tubulin isotypes. The built ligand-protein complexes were studied using molecular dynamics simu

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9

Kamel, Noha A., Nasser S. M. Ismail, Ibrahim S. Yahia, and Khaled M. Aboshanab. "Potential Role of Colchicine in Combating COVID-19 Cytokine Storm and Its Ability to Inhibit Protease Enzyme of SARS-CoV-2 as Conferred by Molecular Docking Analysis." Medicina 58, no. 1 (2021): 20. http://dx.doi.org/10.3390/medicina58010020.

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Despite the advance in the management of Coronavirus disease 2019 (COVID-19), the global pandemic is still ongoing with a massive health crisis. COVID-19 manifestations may range from mild symptoms to severe life threatening ones. The hallmark of the disease severity is related to the overproduction of pro-inflammatory cytokines manifested as a cytokine storm. Based on its anti-inflammatory activity through interfering with several pro and anti-inflammatory pathways, colchicine had been proposed to reduce the cytokine storm and subsequently improve clinical outcomes. Molecular docking analysis

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10

Gutmann, E. J., J. L. Niles, R. T. McCluskey, and D. Brown. "Colchicine-induced redistribution of an apical membrane glycoprotein (gp330) in proximal tubules." American Journal of Physiology-Cell Physiology 257, no. 2 (1989): C397—C407. http://dx.doi.org/10.1152/ajpcell.1989.257.2.c397.

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Factors governing the selective, polarized insertion of membrane proteins are poorly understood, but some studies have suggested that microtubules are involved in the generation and maintenance of cell polarity. We have examined by immunocytochemistry the effect of the microtubule-disrupting agent, colchicine, on the cellular distribution of an endogenous glycoprotein, gp330, which is normally inserted only into the apical plasma membrane of proximal tubule epithelial cells. In control rats, gp330 was localized in the brush border and in apical invaginations and vesicles. Six hours after injec

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11

Dykes, A. C., M. E. Fultz, M. L. Norton та G. L. Wright. "Microtubule-dependent PKC-α localization in A7r5 smooth muscle cells". American Journal of Physiology-Cell Physiology 285, № 1 (2003): C76—C87. http://dx.doi.org/10.1152/ajpcell.00515.2002.

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Using laser scanning confocal, fluorescence resonance energy transfer (FRET), and atomic force (AFM) microscopy, we investigated association of protein kinase C (PKC)-α with microtubules during stimulus-induced relocalization in A7r5 smooth muscle cells. Confocal microscopy with standard immunostaining techniques confirmed earlier observations that colchicine disruption of microtubules blocked PKC-α localization in the perinuclear region of the cell caused by phorbol 12,13-dibutyrate (PDBu; 10–6M). Dual immunostaining suggested colocalization of PKC-α and β-tubulin in both unstimulated and PDB

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12

Sardar, Pinki Saha, Shyam Sundar Maity, Lalita Das, and Sanjib Ghosh. "Luminescence Studies of Perturbation of Tryptophan Residues of Tubulin in the Complexes of Tubulin with Colchicine and Colchicine Analogues†." Biochemistry 46, no. 50 (2007): 14544–56. http://dx.doi.org/10.1021/bi701412k.

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13

Knossow, Marcel, Audrey Dorléans, Raimond Ravelli, and Benoît Gigant. "Complexes of tubulin with inhibitors that bind to the colchicine domain." Acta Crystallographica Section A Foundations of Crystallography 65, a1 (2009): s25—s26. http://dx.doi.org/10.1107/s0108767309099541.

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14

Castro, Mariana, Sílvia Castro, and João Loureiro. "Production of synthetic tetraploids as a tool for polyploid research." Web Ecology 18, no. 2 (2018): 129–41. http://dx.doi.org/10.5194/we-18-129-2018.

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Abstract. Polyploidization has been traditionally considered a phenomenon that mediates ecological differentiation; however, the adaptive value of genome duplications has been seldom explored. Natural or synthetic polyploids offer unique opportunities to experimentally quantify the immediate consequences of genome duplications in plant traits that may be involved with ecological differentiation. Jasione maritima is a diploid-tetraploid complex with cytotypes distributed allopatrically in an environmental gradient ideal for exploring the role of genome duplications in the success of polyploid l

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15

Yan, Wei, Tao Yang, Jianhong Yang, et al. "SKLB060 Reversibly Binds to Colchicine Site of Tubulin and Possesses Efficacy in Multidrug-Resistant Cell Lines." Cellular Physiology and Biochemistry 47, no. 2 (2018): 489–504. http://dx.doi.org/10.1159/000489983.

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Background/Aims: Many tubulin inhibitors are in clinical use as anti-cancer drugs. In our previous study, a novel series of 4-substituted coumarins derivatives were identified as novel tubulin inhibitors. Here, we report the anti-cancer activity and underlying mechanism of one of the 4-substituted coumarins derivatives (SKLB060). Methods: The anti-cancer activity of SKLB060 was tested on 13 different cancer cell lines and four xenograft cancer models. Immunofluorescence staining, cell cycle analysis, and tubulin polymerization assay were employed to study the inhibition of tubulin. N, N ′-Ethy

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16

Muhammad, Zahatu, Jamilu Yau, Abdulqadir U. Zezi, Mohammed G. Magaji, and Asmau N. Hamza. "Synthesis and anti-tumor activity of piperonal substituted chalcone." American Journal of Pharmacotherapy and Pharmaceutical Sciences 2 (July 25, 2023): 11. http://dx.doi.org/10.25259/ajpps_2023_011.

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Objectives: Chalcones have been identified as potential antitumor agents with a novel target, the tubulin. The aim of the study was to synthesize a piperonal substituted chalcone and evaluate its in vivo antitumor activity. Materials and Methods: Piperonal substituted chalcone was synthesized using Claisen-Schmidt condensation and characterized using various spectroscopic techniques. The lethal dose (LD50) of the synthesized compound was estimated using OECD-425 guidelines in rats. Antitumor activity of the synthesized compound was evaluated on 1-methyl nitrosourea (MNU)-induced mammary tumor

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17

Arslan, Mustafa, та Hulya Duymus. "Spectroscopic studies of charge transfer complexes between colchicine and some π acceptors". Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 67, № 3-4 (2007): 573–77. http://dx.doi.org/10.1016/j.saa.2006.06.045.

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18

Kurek, Joanna, Grażyna Bartkowiak, Wojciech Jankowski, et al. "Human Body Fluid Ions In colchicine complexes ESI MS, MADLI MS, Spectroscopic, DFT Studies and Fungicidal Activity of colchicine complexes With Sodium, Potassium, Magnesium and calcium carbonates and Sulphates." IOSR Journal of Pharmacy (IOSRPHR) 06, no. 08 (2016): 40–55. http://dx.doi.org/10.9790/3013-068024055.

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19

Li, Z., L. Wang, and D. Li. "42 ASSISTED ENUCLEATION IN GOLDEN HAMSTER OOCYTES TREATED WITH COLCHICINE AND DEMECOLCINE." Reproduction, Fertility and Development 21, no. 1 (2009): 120. http://dx.doi.org/10.1071/rdv21n1ab42.

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The golden hamster is an excellent experimental animal in many research fields. In an effort to establish experimental protocols necessary for cloning golden hamsters, optimized conditions for induced cytoplasmic protrusion and assisted enucleation of golden hamster oocytes with different concentrations of colchicine and demecolcine were examined in this study. The Golden hamsters (female, six weeks of age) were superovulated with eCG (30 IU, ip) followed by hCG (30 IU, ip) at intervals of 72 h. Hamsters were sacrificed at 13.5 h, 15 h and 18 h after hCG injection. The different ages of cumulu

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20

SINGH, Hardevinder Pal, Ashok Kumar TIWARY, and Subheet JAIN. "Preparation and in Vitro, in Vivo Characterization of Elastic Liposomes Encapsulating Cyclodextrin-Colchicine Complexes for Topical Delivery of Colchicine." YAKUGAKU ZASSHI 130, no. 3 (2010): 397–407. http://dx.doi.org/10.1248/yakushi.130.397.

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21

Antic, D., and J. D. Keene. "Messenger ribonucleoprotein complexes containing human ELAV proteins: interactions with cytoskeleton and translational apparatus." Journal of Cell Science 111, no. 2 (1998): 183–97. http://dx.doi.org/10.1242/jcs.111.2.183.

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Mammalian ELAV proteins bind to polyadenylated messenger RNAs and have specificity for AU-rich sequences. Preferred binding sites in vitro include the AUUUA pentamer and related sequences present in the 3′ untranslated regions of many growth regulatory mRNAs. Human ELAV (hELAV) proteins have been implicated in post-transcriptional regulation of gene expression by their effects on the stability and translatability of growth regulatory mRNAs. We have examined the intracellular localization of ELAV proteins in neurons and in tumor cells of neuronal origin using indirect immunofluorescence, confoc

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22

Hawash, Mohammed, Mohammed T. Qaoud, Nidal Jaradat, et al. "Anticancer Activity of Thiophene Carboxamide Derivatives as CA-4 Biomimetics: Synthesis, Biological Potency, 3D Spheroid Model, and Molecular Dynamics Simulation." Biomimetics 7, no. 4 (2022): 247. http://dx.doi.org/10.3390/biomimetics7040247.

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The present study aimed to synthesize thiophene carboxamide derivatives, which are considered biomimetics of the anticancer medication Combretastatin A-4 (CA-4), and compare the similarity in the polar surface area (PSA) between the novel series and CA-4. Our results showed that the PSA of the most synthesized structures was biomimetic to CA-4, and similar chemical and biological properties were observed against Hep3B cancer cell line. Among the synthesized series 2b and 2e compounds were the most active molecules on Hep3B (IC50 = 5.46 and 12.58 µM, respectively). The 3D results revealed that

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Reibman, J., K. A. Haines, D. Gude, and G. Weissmann. "Differences in signal transduction between Fc gamma receptors (Fc gamma RII, Fc gamma RIII) and FMLP receptors in neutrophils. Effects of colchicine on pertussis toxin sensitivity and diacylglycerol formation." Journal of Immunology 146, no. 3 (1991): 988–96. http://dx.doi.org/10.4049/jimmunol.146.3.988.

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Abstract Studies on the role of microtubule integrity in stimulus-response coupling in neutrophils have generated contradictory data. To determine the role of microtubule integrity in stimulus-response coupling elicited by two different mechanisms, i.e., engagement of the Fc receptors (FcR gamma II, FcR gamma III) or engagement of the receptor for FMLP, we utilized colchicine (10 microM), which reduces pericentriolar microtubules to 29% of control, and compared its effect with that of nocodazole (50 microM) and lumicolchicine (10 microM). We now demonstrate that treatment of neutrophils with c

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Yatribi,, Fatima Azzahraa, Abdelali Bentahila, and Bouchra Chkirate. "Infantile Periarteritis Nodosa (About 5 Cases and Review of the Literature)." SAS Journal of Medicine 8, no. 10 (2022): 770–73. http://dx.doi.org/10.36347/sasjm.2022.v08i10.020.

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PAN is an inflammatory and necrotizing vasculitis affecting small and medium caliber arteries of the body, rarely described in children. Its pathophysiology is complex and remains poorly elucidated, involving the deposition of circulating immune complexes in the vascular wall, neutrophil anti-cytoplasmic antibodies, the role of cytotoxic lymphocytes, cytokines, environmental factors (infections), as well as genetic susceptibility (mutations in ADA 2 and the MEFV gene). There are two main forms: a classic systemic form with visceral involvement (60% of cases) and a cutaneous form with lesions l

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Kurek, Joanna, Władysław Boczoń, Piotr Przybylski, and Bogumił Brzezinski. "ESI MS, spectroscopic and PM5 semiempirical studies of Colchicine complexes with lithium, sodium and potassium salts." Journal of Molecular Structure 846, no. 1-3 (2007): 13–22. http://dx.doi.org/10.1016/j.molstruc.2007.01.004.

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26

Ashrafuzzaman, Md, Zahid Khan, Ashwaq Alqarni, Mohammad Alanazi, and Mohammad Shahabul Alam. "Cell Surface Binding and Lipid Interactions behind Chemotherapy-Drug-Induced Ion Pore Formation in Membranes." Membranes 11, no. 7 (2021): 501. http://dx.doi.org/10.3390/membranes11070501.

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Chemotherapy drugs (CDs) disrupt the lipid membrane’s insulation properties by inducing stable ion pores across bilayer membranes. The underlying molecular mechanisms behind pore formation have been revealed in this study using several methods that confirm molecular interactions and detect associated energetics of drugs on the cell surface in general and in lipid bilayers in particular. Liposome adsorption and cell surface binding of CD colchicine has been demonstrated experimentally. Buffer dissolved CDs were considerably adsorbed in the incubated phospholipid liposomes, measured using the pa

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Johny, Dilip, Kodangala Subramanyam, Nandakishore Baikunje, and Giridhar Belur Hosmane. "Cardiac tamponade and massive pleural effusion in a young COVID-19-positive adult." BMJ Case Reports 14, no. 9 (2021): e244518. http://dx.doi.org/10.1136/bcr-2021-244518.

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COVID-19 has a broad spectrum of cardiac manifestations, and cardiac tamponade leading to cardiogenic shock is a rare presentation. A 30-year-old man with a history of COVID-19-positive, reverse transcription polymerase chain reaction (RT-PCR) done 1 week ago and who was home-quarantined, came to the emergency department with palpitations, breathlessness and orthopnoea. His ECG showed sinus tachycardia with low-voltage complexes, chest X-ray showed cardiomegaly and left pleural effusion and two-dimensional echocardiography showed large pericardial effusion with features suggestive of cardiac t

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Stitt, A. W., and I. Fairweather. "Fasciola hepatica: the effect of the microtubule inhibitors colchicine and tubulozole-C on the ultrastructure of the adult fluke." Parasitology 107, no. 3 (1993): 297–309. http://dx.doi.org/10.1017/s0031182000079270.

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SummaryThe effect of the microtubule inhibitors coichicine (1×10−3 M) and tubulozole-C(1×10−6 M) on the ultrastructure of adult Fasciola hepatica has been determined in vitro by transmission electron microscopy (TEM), using both intact flukes and tissue-slice material. With colchicine treatment, the apical membrane of the tegument became increasingly convoluted and blebbed, while accumulations of T1 secretory bodies occurred in the basal region of the syncytium, leading to progressively fewer secretory bodies in the syncytium. In the tegumental cells there were distinct accumulations of T1 sec

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Jenkins, G., and A. Okumus. "Indiscriminate synapsis in achiasmate Allium fistulosum L. (Liliaceae)." Journal of Cell Science 103, no. 2 (1992): 415–22. http://dx.doi.org/10.1242/jcs.103.2.415.

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Seedlings of Allium fistulosum (2n=2x=16) were treated with aqueous colchicine with the intention of inducing tetraploidy. One treated, but undoubled, diploid mutant is described which consistently fails to form any chiasmata at diakinesis and metaphase I of meiosis. Electron microscopy of whole-mount surface-spread synaptonemal complex complements of pollen mother cell nuclei revealed that the achiasmate condition is probably due not only to the failure to complete synapsis, but also to the indiscriminate way in which the chromosomes form synaptonemal complexes during meiotic prophase. Synaps

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Lai, Chao-Kuen, King-Song Jeng, Keigo Machida, and Michael M. C. Lai. "Association of Hepatitis C Virus Replication Complexes with Microtubules and Actin Filaments Is Dependent on the Interaction of NS3 and NS5A." Journal of Virology 82, no. 17 (2008): 8838–48. http://dx.doi.org/10.1128/jvi.00398-08.

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ABSTRACT The hepatitis C virus (HCV) RNA replication complex (RC), which is composed of viral nonstructural (NS) proteins and host cellular proteins, replicates the viral RNA genome in association with intracellular membranes. Two viral NS proteins, NS3 and NS5A, are essential elements of the RC. Here, by using immunoprecipitation and fluorescence resonance energy transfer assays, we demonstrated that NS3 and NS5A interact with tubulin and actin. Furthermore, immunofluorescence microscopy and electron microscopy revealed that HCV RCs were aligned along microtubules and actin filaments in both

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Thanh, Nguyen Ha, Le Quang Bao, Hai Pham-The, Dang Thi Tuyet Anh, and Phan Van Kiem. "Synthesis, Molecular Docking, and Cytotoxic Evaluation of Fluorinated Podophyllotoxin Derivatives." Natural Product Communications 18, no. 2 (2023): 1934578X2311537. http://dx.doi.org/10.1177/1934578x231153733.

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Objective: The study was conducted to evaluate the in vitro and in silico anticancer activity of fluorinated podophyllotoxin derivatives. Methods: Microwave-assisted multicomponent reactions were carried out in an Anton Paar Microwave Synthetic Reactor Monowave 400 in order to synthesize fluorinated podophyllotoxin derivatives. These products were identified by spectral analysis and evaluated for their cytotoxicity against 4 types of human cancer cell lines (KB, HepG2, A549, and MCF7), as well as human embryonic kidney (Hek) 293 cells using MTT protocol. Molecular docking was conducted using 2

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Karakasis, Paschalis, Konstantinos Pamporis, Panagiotis Theofilis, et al. "Inflammasome Signaling in Cardiac Arrhythmias: Linking Inflammation, Fibrosis, and Electrical Remodeling." International Journal of Molecular Sciences 26, no. 13 (2025): 5954. https://doi.org/10.3390/ijms26135954.

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Cardiac arrhythmias, including atrial fibrillation and ventricular arrhythmias, remain the leading causes of morbidity and mortality worldwide. While structural, electrical, and metabolic remodeling have long been recognized as drivers of arrhythmogenesis, emerging evidence identifies inflammation—particularly inflammasome signaling—as a central orchestrator of this pathological triad. Among the various inflammasome complexes, the NLRP3 inflammasome has garnered particular attention due to its activation in cardiomyocytes, fibroblasts, and immune cells in diverse clinical contexts. NLRP3 activ

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Suryono, Suryono, Muhammad I. Amien, Achmad I. Tohari, Antonius D. Saputra, Muhammad RF Hidayat та Hazbina F. Ramadhan. "In silico studies on quercetin, myricetin, and kaempferol in inhibiting TGF-β1 and galectin-3 for cardiac fibrosis management". Narra J 5, № 1 (2025): e1310. https://doi.org/10.52225/narra.v5i1.1310.

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Cardiac fibrosis remains as the leading cause of death worldwide and is often associated with elevated levels of transforming growth factor-β 1 (TGF-β1) and galectin-3, making them potential therapeutic targets. Recent studies revealed that quercetin, myricetin, and kaempferol have the biological effect for several cardiovascular diseases. However, the investigation into this topic through molecular models and analysis remain unexplored. The aim of this study was to evaluate the potential effect of quercetin, myricetin, and kaempferol which targeted TGF-β1 and galectin-3. In this study, querce

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Ding, Zhongpeng, Feifei Li, Lianghui Xie, et al. "Design and Synthesis of Novel Phenylahistin Derivatives Based on Co-Crystal Structures as Potent Microtubule Inhibitors for Anti-Cancer Therapy." Marine Drugs 20, no. 12 (2022): 752. http://dx.doi.org/10.3390/md20120752.

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Phenylahistin is a naturally occurring marine product with a diketopiperazine structure that can bind to the colchicine site of microtubulin as a possible anticancer agent. To develop more potent microtubule inhibitors, novel phenylahistin derivatives were designed and synthesized based on the co-crystal complexes of phenylahistin derivatives and microtubulin. We established a focused library of imidazole-type molecules for the introduction of different groups to the C-ring and A-ring of phenylahistin. Structure–activity relationship studies indicated that appropriate hydrocarbon substituents

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Camussi, G., J. R. Brentjens, B. Noble, et al. "Antibody-induced redistribution of Heymann antigen on the surface of cultured glomerular visceral epithelial cells: possible role in the pathogenesis of Heymann glomerulonephritis." Journal of Immunology 135, no. 4 (1985): 2409–16. http://dx.doi.org/10.4049/jimmunol.135.4.2409.

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Abstract In this study we analyze the ability of antibodies that produce passive Heymann glomerulonephritis to induce antigen redistribution on the surface of cultured glomerular visceral epithelial cells (GEC). Polyclonal antibodies produced by immunization with membrane vesicles prepared from proximal tubule brush borders (BB) and polyclonal (rabbit) and monoclonal (mouse) antibodies to a membrane glycoprotein (gp 330) purified from epithelial cells of rat proximal tubule were used. The study by immunofluorescence of GEC kept at 4 degrees C or fixed with paraformaldehyde showed that the thre

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Păunescu, Teodor G., Leileata M. Russo, Nicolas Da Silva, et al. "Compensatory membrane expression of the V-ATPase B2 subunit isoform in renal medullary intercalated cells of B1-deficient mice." American Journal of Physiology-Renal Physiology 293, no. 6 (2007): F1915—F1926. http://dx.doi.org/10.1152/ajprenal.00160.2007.

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Mice deficient in the ATP6V1B1 (“B1”) subunit of the vacuolar proton-pumping ATPase (V-ATPase) maintain body acid-base homeostasis under normal conditions, but not when exposed to an acid load. Here, compensatory mechanisms involving the alternate ATP6V1B2 (“B2”) isoform were examined to explain the persistence of baseline pH regulation in these animals. By immunocytochemistry, the mean pixel intensity of apical B2 immunostaining in medullary A intercalated cells (A-ICs) was twofold greater in B1−/− mice than in B1+/+ animals, and B2 was colocalized with other V-ATPase subunits. No significant

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Lei, Jia-Hong, Ling-Ling Ma, Jing-Hong Xian, et al. "Structural insights into targeting of the colchicine binding site by ELR510444 and parbendazole to achieve rational drug design." RSC Advances 11, no. 31 (2021): 18938–44. http://dx.doi.org/10.1039/d1ra01173a.

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Li, Zhongping, Lingling Ma, Chengyong Wu, et al. "The Structure of MT189-Tubulin Complex Provides Insights into Drug Design." Letters in Drug Design & Discovery 16, no. 9 (2019): 1069–73. http://dx.doi.org/10.2174/1570180816666181122122655.

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Background: Drugs that interfere with microtubule dynamics are used widely in cancer chemotherapy. Microtubules are composed of αβ-tubulin heterodimers, and the colchicine binding site of tubulin is an important pocket for designing tubulin polymerization inhibitors. We have previously designed and synthesized a series of colchicine binding site inhibitors (CBSIs). However, these compounds showed no anticancer activity in vivo. Then, we have used a deconstruction approach to obtain a new derivative MT189, which showed in vivo anticancer activity. Methods: We crystallized a protein complex incl

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Koutsioumpa, Marina, Herman Lelie, Pony Yu-Ling Lee, and Kun-Yuan Lin. "Implication of the novel microtubule targeting agent, AUS_001, in pancreatic cancer cellular signaling." Journal of Clinical Oncology 43, no. 4_suppl (2025): 748. https://doi.org/10.1200/jco.2025.43.4_suppl.748.

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748 Background: Pancreatic cancer (PanCa) is considered a major therapeutic challenge due to its poor prognosis, high mortality rate and resistance to most therapies, underlining the need for new treatment approaches. Our previous investigations revealed that the prenylated hydroxy-stilbene, AUS_001, inhibits β-tubulin polymerization via its unique binding to the colchicine site of tubulin. A cell-based profiling platform identified sensitivity of 12 out of 13 PanCa lines to AUS_001 with a median concentration causing 50% growth inhibition of 0.227µM. The goal of the current study was to eluci

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Kurek, Joanna, Patrycja Kwaśniewska‐Sip, Krzysztof Myszkowski, et al. "Antifungal, anticancer, and docking studies of colchiceine complexes with monovalent metal cation salts." Chemical Biology & Drug Design 94, no. 5 (2019): 1930–43. http://dx.doi.org/10.1111/cbdd.13583.

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Ulrichová, J., D. Walterová, F. Březina, and V. Šimánek. "Inhibition of the yeast alcoholdehydrogenase by Cu(II) - complexes of colchiceine and N-deacetylcolchiceine." Bioorganic & Medicinal Chemistry Letters 2, no. 9 (1992): 1097–100. http://dx.doi.org/10.1016/s0960-894x(00)80626-5.

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Canel, N. G., R. J. Bevacqua, M. I. Hiriart, and D. F. Salamone. "1 REPLICATION OF SOMATIC MICRONUCLEI IN BOVINE OOCYTES." Reproduction, Fertility and Development 24, no. 1 (2012): 112. http://dx.doi.org/10.1071/rdv24n1ab1.

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Microcell-mediated chromosome transfer was developed to introduce a low number of chromosomes into a host cell (Fournier and Ruddle 1977 PNAS 74, 319–323). As a first approach to individual chromosome manipulation, we designed a new technique that consists of injecting a micronucleus into an enucleated oocyte to replicate a low number of chromosomes. Additionally, we studied the capability of such micronuclei to be marked with a transgene. To this aim, micronuclei from adult bovine fibroblasts were produced by incubation in 0.05 μg mL–1 of demecolcine for 48 h followed by 2 mg mL–1 of mitomyci

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Sharma, R. K. "Stabilities of mixed metal complexes with biologically active colchiceine in dioxan-water and their relation to quantitative softness values: A new approach." Monatshefte f�r Chemie Chemical Monthly 125, no. 3 (1994): 267–74. http://dx.doi.org/10.1007/bf00811312.

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Ladyka, V. I., Yu I. Skliarenko, Yu M. Pavlenko, and L. F. Starodub. "KARYOTYPAL VARIABILITY OF UKRAINIAN BROWN DAIRY BREED COWS." Animal Breeding and Genetics 64 (December 26, 2022): 110–17. http://dx.doi.org/10.31073/abg.64.09.

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Cytogenetic analysis of breeding animals makes it possible to identify animals carrying cytogenetic abnormalities, the rate of spontaneous and induced somatic mutagenesis and the level of general genomic instability of animals. Scientists emphasize that in breeding work it is desirable to use animals whose offspring inherit high productivity and do not carry a genetic burden. The main factors that contribute to chromosomal instability are environmental factors, enzyme failure, changes in the system of repair or replication of chromosomes, suppression of immunity. It is important that the

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Gaikwad, Vaishali, Vaibhav Sabale, and Bhimrao Khade. "Synthesis, Characterization, in silico and in vitro Studies of Transition Metal Complexes with Biologically Active Ligand as Antigout Agent Colchicine." International Journal of Pharmaceutical Sciences and Drug Research, March 30, 2020, 107–14. http://dx.doi.org/10.25004/ijpsdr.2020.120203.

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Colchicine is essentially useful in the treatment of gout. In the present work Colchicine Complexes has been prepared with transition metals viz; Copper(II) [Cu(II)], Zinc (II) [Zn(II)], Cobalt (II) [Co(II)], Nickel (II) [Ni(II)] and those checked for molecular docking, it has been observed that Zn(II) and Ni(II) complex has revealed good binding energy than the parent ligand, the increased binding energy of colchicine metal complexes indicates that, the tubulin polymerization inhibitor tendency is enhanced, consequently antigout property is also increased. As transition metals have antimicrob

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Bhandari, Shashikant V., Sonali B. Anardi, Shrawani D. Nighot, et al. "Design of Colchicine‐Based Tubulin Inhibitors as Anticancer Agents by In Silico Analysis of Colchicine‐Based Tubulin Inhibitors: 3D‐QSAR, Molecular Docking, and Molecular Dynamics Simulations for Anticancer Drug Development." Chemistry & Biodiversity, July 29, 2025. https://doi.org/10.1002/cbdv.202500361.

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ABSTRACTThis study explores colchicine analogues as potential anticancer agents by analyzing their interactions with the tubulin–colchicine complex. A robust three‐dimensional quantitative structure–activity relationship (3D‐QSAR) model (r2 = 0.9438, q2 = 0.8915) identified key substituent regions influencing biological activity. Among 720 evaluated colchicine derivatives, 25 compounds exhibited superior binding affinities compared to colchicine. Compounds S3, S22, and a reference (Colchicine) were selected for molecular dynamics (MD) simulations, which confirmed stable binding interactions ov

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Talmor, Nina, Michael Pillinger, Ana Leonard, Fatmira Curovic, and Binita Shah. "Abstract 16734: Patterns of Inflammatory Activation in Cardiovascular Disease: Insights From the Randomized Colchicine PCI Trial." Circulation 148, Suppl_1 (2023). http://dx.doi.org/10.1161/circ.148.suppl_1.16734.

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INTRODUCTION: Recent studies demonstrate that neutrophils accumulate in atherosclerotic lesions and that neutrophil counts correlate with disease severity. The randomized double-blind Colchicine-PCI study demonstrated that colchicine attenuated systemic inflammation (IL-6, CRP) after percutaneous coronary intervention compared with placebo. GOALS/AIMS: We characterized neutrophil activity in patients across a spectrum of cardiovascular phenotypes, including severity of coronary artery disease (CAD) and presentation of acute myocardial infarct (AMI). METHODS: The Colchicine-PCI biomarker sub-st

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Arion, Vladimir, Iuliana Besleaga, Renata Raptova, et al. "Are the metal identity and stoichiometry of metal complexes important for colchicine site binding and inhibition of tubulin polymerization?" Dalton Transactions, 2024. http://dx.doi.org/10.1039/d4dt01469c.

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Quite recently we discovered that copper(II) complexes with isomeric morpholine-thiosemicarbazone (morph-TSCs) hybrid ligands show good cytotoxicity in cancer cells and that the molecular target responsible for this activity might be...

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Jankowski, Wojciech, Joanna Kurek, Piotr Barczyński, and Marcin Hoffmann. "Quantum-chemical, NMR, FT IR, and ESI MS studies of complexes of colchicine with Zn(II)." Journal of Molecular Modeling 23, no. 4 (2017). http://dx.doi.org/10.1007/s00894-017-3306-z.

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"Designing of Novel Quinolines Derivatives as Hepatocellular Carcinoma Inhibitors by Using In silico Approaches." Biointerface Research in Applied Chemistry 13, no. 3 (2022): 217. http://dx.doi.org/10.33263/briac133.217.

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Cancer is one of the very common diseases requiring long-term treatment, tubulin plays an important role in the development of cancer, and the use of colchicine binding site inhibitors against Hepatocellular Carcinoma has become the most common approach. A series of thirty quinoline derivatives have recently been identified as promising tubulin inhibitors with potent activity against human Hepatocellular Carcinoma. To design anti-cancer drugs, we applied the 3D-QSAR approach, this method is based on two contours (CoMFA and CoMSIA), the results obtained in two these contours are (R2 = 0.98, Q2

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