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Title:
New Difluoro Knoevenagel Condensates of Curcumin, Their Schiff Bases and Copper Complexes as Proteasome Inhibitors and Apoptosis Inducers in Cancer Cells | Pharmaceutical Research
Description:
Purpose Emerging evidence clearly suggests the potential chemopreventive and anti-tumor activity of a well known “natural agent” curcumin. However, studies have shown that curcumin is not readily bioavailable, and thus the tissue bioavailability of curcumin is also poor except for gastrointestinal track. Because of the potential biological activity of curcumin, many studies have attempted for making a better analog of cucumin that is equally effective or better with increased bioavailability, which was the purpose of our current study. Methods We have designed and synthesized new difluoro Knoevenagel condensates of curcumin and Schiff bases along with their copper (II) complexes and evaluated their biological activities with respect to the inhibitory effects on purified rabbit 26S proteasome, and growth inhibition and induction of apoptosis in colon and pancreatic cancer cell lines. Results All copper complexes possess distorted square planar geometries with 1:1 metal to ligand stoichiometry with reversible copper redox couple. The difluoro compound CDF exhibited inhibitory effects on purified rabbit 20S proteasome or cellular 26S proteasome, and caused both growth inhibition of cancer cell lines and induced apoptotic cell death in our preliminary assessment. Conclusion Our results suggest that our newly synthesized classes of curcumin analogs could be useful as chemopreventive and/or therapeutic agents against cancers.
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article, curcumin, google, scholar, pubmed, cas, cancer, aggarwal, cell, res, kunnumakkara, research, cells, products, proteasome, copper, human, med, pharmacol, mol, privacy, cookies, content, difluoro, knoevenagel, condensates, complexes, apoptosis, yang, jamadar, sarkar, study, access, proliferation, doi, mice, gene, anand, biochem, chem, information, publish, search, schiff, padhye, dou, activity, biological, activities, effects,
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month download article/chapter transcription factor nf-kappa ]pyrene-induced forestomach cancer high-fat-fed hamsters [beta]-unsaturated carboxylate complexes plant natural products difluoro knoevenagel condensates cancer cell lines polymeric nanoparticle-encapsulated curcumin curcumin-casein micelle complexation metastatic gene products human cancer therapy full article pdf multiple gene expression privacy choices/manage cookies �natural agent” curcumin cellular 26s proteasome nano-metal chemistry 2007 related subjects multi-targeted therapy kunnumakkara ab knoevenagel condensates european economic area qiuzhi cindy cui labdane diterpene glucoside indian solid gold spectrochim acta part mono-carbonyl analogues anti-tumor activity conditions privacy policy article padhye cancer cells acta pharmacol toxicol landis-piwowar kr genetically diabetic mice anti-oxidant properties anti-bacterial properties abeda jamadar schiff base derivatives regulates chemokine expression accepting optional cookies ping dou & fazlul newly synthesized classes cancer therapy anti-inflammatory properties chem pharm bull article log main content log inhibitory effects selective fluorination
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headline:New Difluoro Knoevenagel Condensates of Curcumin, Their Schiff Bases and Copper Complexes as Proteasome Inhibitors and Apoptosis Inducers in Cancer Cells
description:Emerging evidence clearly suggests the potential chemopreventive and anti-tumor activity of a well known “natural agent” curcumin. However, studies have shown that curcumin is not readily bioavailable, and thus the tissue bioavailability of curcumin is also poor except for gastrointestinal track. Because of the potential biological activity of curcumin, many studies have attempted for making a better analog of cucumin that is equally effective or better with increased bioavailability, which was the purpose of our current study. We have designed and synthesized new difluoro Knoevenagel condensates of curcumin and Schiff bases along with their copper (II) complexes and evaluated their biological activities with respect to the inhibitory effects on purified rabbit 26S proteasome, and growth inhibition and induction of apoptosis in colon and pancreatic cancer cell lines. All copper complexes possess distorted square planar geometries with 1:1 metal to ligand stoichiometry with reversible copper redox couple. The difluoro compound CDF exhibited inhibitory effects on purified rabbit 20S proteasome or cellular 26S proteasome, and caused both growth inhibition of cancer cell lines and induced apoptotic cell death in our preliminary assessment. Our results suggest that our newly synthesized classes of curcumin analogs could be useful as chemopreventive and/or therapeutic agents against cancers.
datePublished:2009-05-07T00:00:00Z
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apoptosis
cancer cells
cell growth
curcumin
difluoro Knoevenagel condensates of curcumin
Pharmacology/Toxicology
Pharmacy
Biochemistry
general
Medical Law
Biomedical Engineering and Bioengineering
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description:Emerging evidence clearly suggests the potential chemopreventive and anti-tumor activity of a well known “natural agent” curcumin. However, studies have shown that curcumin is not readily bioavailable, and thus the tissue bioavailability of curcumin is also poor except for gastrointestinal track. Because of the potential biological activity of curcumin, many studies have attempted for making a better analog of cucumin that is equally effective or better with increased bioavailability, which was the purpose of our current study. We have designed and synthesized new difluoro Knoevenagel condensates of curcumin and Schiff bases along with their copper (II) complexes and evaluated their biological activities with respect to the inhibitory effects on purified rabbit 26S proteasome, and growth inhibition and induction of apoptosis in colon and pancreatic cancer cell lines. All copper complexes possess distorted square planar geometries with 1:1 metal to ligand stoichiometry with reversible copper redox couple. The difluoro compound CDF exhibited inhibitory effects on purified rabbit 20S proteasome or cellular 26S proteasome, and caused both growth inhibition of cancer cell lines and induced apoptotic cell death in our preliminary assessment. Our results suggest that our newly synthesized classes of curcumin analogs could be useful as chemopreventive and/or therapeutic agents against cancers.
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cancer cells
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difluoro Knoevenagel condensates of curcumin
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Biochemistry
general
Medical Law
Biomedical Engineering and Bioengineering
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