Evaluation of Novel 3-Hydroxyflavone Analogues as HDAC Inhibitors against Colorectal Cancer.

Evaluation of Novel 3-Hydroxyflavone Analogues as HDAC Inhibitors against Colorectal Cancer. Adv Pharmacol Sci. 2018;2018:4751806 Authors: Biswas S, Reddy ND, Jayashree BS, Rao CM Abstract Alteration of epigenetic enzymes is associated with the pathophysiology of colon cancer with an overexpression of histone deacetylase 8 (HDAC8) enzyme in this tissue. Numerous reports suggest that targeting HDAC8 is a viable strategy for developing new anticancer drugs. Flavonols provide a rich source of molecules that are effective against cancer; however, their clinical use is limited. The present study investigated the potential of quercetin and synthetic 3-hydroxyflavone analogues to inhibit HDAC8 enzyme and evaluated their anticancer property. Synthesis of the analogues was carried out, and cytotoxicity was determined using MTT assay. Nonspecific and specific HDAC enzyme inhibition assays were performed followed by the expression studies of target proteins. Induction of apoptosis was studied through annexin V and caspase 3/7 activation assay. Furthermore, the analogues were assessed against in vivo colorectal cancer. Among the synthesized analogues, QMJ-2 and QMJ-5 were cytotoxic against HCT116 cells with an IC50 value of 68 ± 2.3 and 27.4 ± 1.8 µM, respectively. They inhibited HDAC enzyme in HCT116 cells at an IC50 value of 181.7 ± 22.04 and 70.2 ± 4.3 µM, respectively, and inhibited human HDAC8 and 1 en...
Source: Advances in Pharmacological Sciences - Category: Drugs & Pharmacology Tags: Adv Pharmacol Sci Source Type: research

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By STEVEN MERAHN, MD In 1807, in an effort to spite the British and French for shipping interference (and forced recruitment of American citizens into military service), the United States Congress passed an Embargo Act, effectively shutting down trade with these two countries. Britain and France quickly found other trading partners; the US, then limited in our capacity to sell products outside our borders, was left with a devastated economy and a gaping hole in our face. It took only weeks before Congress passed a loophole; they repealed the act within 15 months of its passing. It was a great lesson in unintended co...
Source: The Health Care Blog - Category: Consumer Health News Authors: Tags: Health Policy Politics Uncategorized Health care debate Health Care Reform Steven Merahn universal healthcare Source Type: blogs
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Source: Fight Aging! - Category: Research Authors: Tags: Daily News Source Type: blogs
Conditions:   Colon Adenocarcinoma;   Colon Cancer Intervention:   Other: Exercise assessment Sponsors:   Northumbria University;   York St John University;   Newcastle University Not yet recruiting
Source: ClinicalTrials.gov - Category: Research Source Type: clinical trials
Authors: Mansour-Ghanaei F, Varshi G, Joukar F, Ashoobi MT, Esmaeilpour J, Gharibpoor A, Daryakar A, Mansour-Ghanaei R, Balou HA, Saedi HS, Mavaddati S, Sepehrimanesh M Abstract Colon cancer is the most commonly diagnosed gastrointestinal cancers in developed countries with varied incidence and the onset age of disease worldwide. Overall, 161 participants who were under patronage of a local relief foundation and referred to the endoscopy ward of Razi Hospital affiliated to the Guilan University of Medical Sciences. These patients have been aged more than 50 or more than 40 years with history of colorectal cancer in...
Source: Journal of Medicine and Life - Category: General Medicine Tags: J Med Life Source Type: research
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Source: Medicine and Science in Sports and Exercise - Category: Sports Medicine Tags: EPIDEMIOLOGY Source Type: research
Source: Clinical Nutrition - Category: Nutrition Authors: Tags: Nutrition and cancer II Source Type: research
Source: Clinical Nutrition - Category: Nutrition Authors: Tags: Nutrition and cancer II Source Type: research
Conclusion Provoked venous thromboembolism is an entity that can be prevented. Malignancy and surgical treatment are the most common risk factors and these patients should be treated with special care. The creation of a register of patients with venous thromboembolism in Bosnia and Herzegovina would enable the development of a preventive strategy in the groups of patients at risk. PMID: 31402639 [PubMed - as supplied by publisher]
Source: Primary Care - Category: Primary Care Authors: Tags: Med Glas (Zenica) Source Type: research
e Min Yoo Betula platyphylla bark has been evaluated for the treatment of dermatitis, inflammatory conditions, and cancer. Diarylheptanoids are the major constituents of the B. platyphylla bark and possess various pharmacological effects. Our previous study confirmed the selective antiproliferative effect of platyphylloside (BPP) isolated from B. platyphylla on colon cancer and leukemic cells using 60 different cancer cell lines from thr National Cancer Institution (NCI). In line with previous reports, this study focuses on the apoptotic pathway of BPP, a phenolic glycoside composed of two aromatic rings joined by a se...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
As clinical testing for Mendelian causes of colorectal cancer (CRC) is largely driven by recognition of family history and early age of onset, the rates of such findings among individuals with prevalent CRC not recognized to have these features is largely unknown. We evaluated actionable genomic findings in community-based participants ascertained by three phenotypes: (1) CRC, (2) one or more adenomatous colon polyps, and (3) control participants over age 59 years without CRC or colon polyps. These participants underwent sequencing for a panel of genes that included colorectal cancer/polyp (CRC/P)-associated and actionable...
Source: The American Journal of Human Genetics - Category: Genetics & Stem Cells Authors: Tags: Article Source Type: research
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