Use of substitute Nonidet P-40 nonionic detergents in intracellular tubulin polymerization assays for screening of microtubule targeting agents

2017 ◽  
Vol 95 (3) ◽  
pp. 379-384 ◽  
Author(s):  
S. Sinha ◽  
J.J. Field ◽  
J.H. Miller
Keyword(s):  
Anticancer Agent ◽  
Research Community ◽  
General Interest ◽  
Tubulin Polymerization ◽  
Chemical Company ◽  
Major Class ◽  
Biochemical Assays ◽  
Microtubule Targeting Agents ◽  
Shell Chemical ◽  
Nonionic Detergents

Shell Chemical Company Nonidet P-40 has been used for decades in many biochemical assays as a nonionic, nondenaturing detergent; however, Shell no longer manufactures this product. Four commercially available substitutes were investigated and their activities titrated in an intracellular tubulin polymerization assay. Although claimed by the supply companies to be identical to the Shell Nonidet P-40, all four substitutes were about 10-fold more potent and needed to be diluted accordingly. As microtubule targeting drugs are a major class of anticancer agent, and many researchers use the intracellular tubulin polymerization assay, this information is important to help troubleshoot assay development with the new substitutes. As the Shell Nonidet P-40 has been used in many biochemical buffers, these results will be of general interest to the biochemical, cell, and molecular research community.

scholarly journals Simple Thalidomide Analogs in Melanoma: Synthesis and Biological Activity

2021 ◽  
Vol 11 (13) ◽  
pp. 5823
Author(s):  
Alexia Barbarossa ◽  
Alessia Catalano ◽  
Jessica Ceramella ◽  
Alessia Carocci ◽  
Domenico Iacopetta ◽  
...  
Keyword(s):  
Anticancer Agent ◽  
Ring System ◽  
In Vitro Assays ◽  
Tubulin Polymerization ◽  
Cytotoxic Effects ◽  
Ongoing Research ◽  
Drug Candidates ◽  
Small Series ◽  
Clinical Interest

Thalidomide is an old well-known drug that is still of clinical interest, despite its teratogenic activities, due to its antiangiogenic and immunomodulatory properties. Therefore, efforts to design safer and effective thalidomide analogs are continually ongoing. Research studies on thalidomide analogs have revealed that the phthalimide ring system is an essential pharmacophoric fragment; thus, many phthalimidic compounds have been synthesized and evaluated as anticancer drug candidates. In this study, a panel of selected in vitro assays, performed on a small series of phthalimide derivatives, allowed us to characterize compound 2k as a good anticancer agent, acting on A2058 melanoma cell line, which causes cell death by apoptosis due to its capability to inhibit tubulin polymerization. The obtained data were confirmed by in silico assays. No cytotoxic effects on normal cells have been detected for this compound that proves to be a valid candidate for further investigations to achieve new insights on possible mechanism of action of this class of compounds as anticancer drugs.

Semi-synthesis and anti-lung cancer activity evaluation of aryl dihydrothiazol acyl podophyllotoxin ester derivatives

RSC Advances ◽  
2015 ◽  
Vol 5 (35) ◽  
pp. 27775-27784 ◽  
Author(s):  
Hong-Yan Lin ◽  
Li-Fei Bai ◽  
Fang Wang ◽  
Xun Wu ◽  
Lu-Jing Han ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Anticancer Agent ◽  
Tubulin Polymerization ◽  
Inhibition Effect ◽  
Activity Evaluation ◽  
Podophyllotoxin Derivatives ◽  
Cancer Activity

S12, the best anticancer agent among the 17 podophyllotoxin derivatives, showed a proliferative inhibition effect via inhibiting tubulin polymerization.

scholarly journals Exploring Diverse-Ring Analogues on Combretastatin A4 (CA-4) Olefin as Microtubule-Targeting Agents

2020 ◽  
Vol 21 (5) ◽  
pp. 1817 ◽  
Author(s):  
Ming-Yu Song ◽  
Qiu-Rui He ◽  
Yi-Lin Wang ◽  
Hao-Ran Wang ◽  
Tian-Cheng Jiang ◽  
...  
Keyword(s):  
Hepg2 Cells ◽  
Annexin V ◽  
Docking Studies ◽  
Cytotoxic Agents ◽  
Tubulin Polymerization ◽  
Microtubule Network ◽  
Microtubule Targeting Agents ◽  
Ic50 Values ◽  
Tubulin Polymerization Inhibitor

Combretastatin-4 (CA-4) as a tubulin polymerization inhibitor draws extensive attentions. However, due to its weak stability of cis-olefin and poor metabolic stability, structure modifications on cis-configuration are being performed. In this work, we constructed a series of novel CA-4 analogues with linkers on olefin containing diphenylethanone, cis-locked dihydrofuran, α-substituted diphenylethanone, cyclobutane and cyclohexane on its cis-olefin. Cytotoxic activity of all analogues was measured by an SRB assay. Among them, compound 6b, a by-product in the preparation of diphenylethanone analogues, was found to be the most potent cytotoxic agents against HepG2 cells with IC50 values of less than 0.5 μM. The two isomers of 6b induced cellular apoptosis tested by Annexin V-FITC and propidium iodide (PI) double staining, arrested cells in the G2/M phase by PI staining analysis, and disrupted microtubule network by immunohistochemistry study in HepG2 cells. Moreover, 6b-(E) displayed a dose-dependent inhibition effect for tubulin assembly in in vitro tubulin polymerization assay. In addition, molecular docking studies showed that two isomers of 6b could bind efficiently at colchicine binding site of tubulin similar to CA-4.

Design and Synthesis of New Tubulin Polymerization Inhibitors Inspired from Combretastatin A‐4: An Anticancer Agent

2020 ◽  
Vol 5 (37) ◽  
pp. 11560-11572
Author(s):  
Akanksha Sharma ◽  
Doddabasappa Talimarada ◽  
Umesh Prasad Yadav ◽  
Nidhi Singh ◽  
A. Sudharshan Reddy ◽  
...  
Keyword(s):  
Anticancer Agent ◽  
Tubulin Polymerization ◽  
Design And Synthesis ◽  
Tubulin Polymerization Inhibitors

Eponate 12, a new epoxy resin: Comparisons with EPON 812 and observations on its use for general biological electron microscopy

1987 ◽  
Vol 45 ◽  
pp. 628-629
Author(s):  
J.A. Mascorro ◽  
G.S. Kirby
Keyword(s):  
Electron Microscopy ◽  
Epoxy Resin ◽  
Flow Rate ◽  
Epoxy Resins ◽  
Physical Characteristics ◽  
Past Study ◽  
Chemical Company ◽  
Shell Chemical

Many epoxy resins have been introduced during the last several years as replacements for Epon 812 since the Shell Chemical Company discontinued production of this popular embedding resin. In a past study, the present investigators examined several of the “replacement” resins for physical characteristics such as viscosity, flow rate, density, mass weight, and hardness of the polymerized medium. In addition, other equally important parameters including sectioning and infiltrating character as well as stain-ability and section strength subsequent to beam and vacuum conditions also were evaluated. The present work follows a similar rationale and seeks to determine this same information for Eponate 12, an epoxy resin designated as a true generic replacement for the formerly available Epon 812 product.For purposes of physical comparisons, Eponate 12 was tested against a sample of original Shell Epon 812 still maintained in our laboratory.

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