Posts tagged Curcumin

Cytotoxicity of curcumin derivatives in ALK positive non-small cell lung cancer

Non-small cell lung cancer with ALK rearrangements can be targeted effectively with ALK inhibitors such as crizotinib. However, cancer progression typically occurs within a year as drug resistance develops. One strategy to overcome this drug resistance is to determine if novel cytotoxic agents retain the ability to kill lung cancer cells that have developed ALK inhibitor resistance. We therefore examined curcumin, a drug with anticancer properties, and 2 s-generation curcumin derivatives (1-methyl-3,5-bis[(E)-4-pyridyl) methylidene]-4-piperidone (RL66) and 1-isopropyl-3,5-bis[(pyridine-3-yl) methylene]piperidin-4-one (RL118)) in lung cancer cell lines. The cytotoxicity of curcumin, RL66, and RL118 were tested in both ALK+ lung cancer cells (H3122), crizotinib resistant ALK+ cells (CR-H3122) and ALK- lung cancer cells (A549), both alone and in combination with crizotinib. ALK+ cells were 2-3x more sensitive to RL66 and RL118 than ALK- cells, with the drugs' eliciting IC50 values in the ..... READ ARTICLE

European Journal of Pharmacology DOI:10.1016/j.ejphar.2019.172749

Authors: Abigail R Bland, Rebekah L Bower, Mhairi Nimick, Bill C Hawkins, Rhonda J Rosengren, John C Ashton

Pre-ClinicalKirk SmithDecember 15, 2019ALK, Curcumin, Derivatives, Non-small cell lung cancer (NSCLC)

Curcumin as tyrosine kinase inhibitor in cancer treatment

Curcumin is a natural substance known for ages, exhibiting a multidirectional effect in cancer prevention and adjuvant cancer therapies. The great advantage of using nutraceuticals of vegetable origin in comparison to popular cytostatic drugs is the minimized side effect and reduced toxicity. The targets in oncological therapy are, among others, tyrosine kinases, important mediators of signaling pathways whose impaired expression is observed in many types of cancer. Unfortunately, the hydrophobic nature of the curcumin molecule often limits its bioavailability, which is why many studies focus on the chemical modification of this compound. Current research is aimed at modifying structures that improve the pharmacokinetic parameters of curcumin, e.g. the formation of nanoparticles, complexes with metals or the synthesis of curcumin derivatives with functional substituents that allow tumor targeting. The article is a review and analysis of current literature on the properties of curcumin ..... READ ARTICLE

European Journal of Medicinal Chemistry DOI:10.1016/j.ejmech.2019.07.015

Authors: A. Golonko, H. Lewandowska, R. Świsłocka, U.T. Jasińska, W. Priebe, W. Lewandowski

Review PaperKirk SmithJuly 15, 2019Tyrosine kinases, Curcumin, Nanoparticles, Complexes, Growth factors, Cancer therapy