Quercetin, a major flavonol, present abundantly in apples and onions, is widely studied for ameliorating metabolic syndrome abnormalities. However, quercetin is mainly present in plant food in the form of quercetin glycosides and has been reported for poor gastrointestinal absorption. The present study was designed with the purpose of imparting a lipophilic property to quercetin-3-O-glucoside (QG) by its acylation with eicosapentaenoic acid (EPA) and to study the influence of eicosapentaenoic acid ester of quercetin-3-O-glucoside (QE) on hyperlipidemia and inflammation in vivo and in vitro. QE was more effective in reducing the production of tumor necrosis factor-alpha (TNF-α), prostaglandin 2 (PGE2), cyclo-oxygenase (COX)-2 levels and nuclear expression of nuclear factor-kappa B (NF-кB) compared to the parent compounds (QG and EPA) and commercial drugs, after lipopolysaccharides (LPS) induced inflammation in THP-1 derived macrophages. Serum high-density lipoprotein (HDL)-cholesterol was significantly higher and hepatic total cholesterol concentration was lower in the rats fed high-fat diet supplemented with QE, compared to the high-fat diet with inflammation (HFL). The serum concentrations of C-reactive protein (CRP), interleukin (IL)-6, and interferon-gamma (IFN-γ) were significantly lower in QE treatment group than HFL group. EPA conjugated flavonol, QE, had significant anti-inflammatory and hypolipidemic properties and may be effective for the treatment of obesity-related disorders.
Background: Hypertension is a crucial risk factor for development of cardiovascular and neurological diseases. Flavonoids exhibit a wide range of biological effects and have had increased interest as a dietary approach for the prevention or possible treatment of hypertension. However, continuous efforts have been made to structurally modify natural flavonoids with the hope of improving their biological activities. One of the methods used for the possible enhancement of flavonoid efficacy is enzymatic esterification of flavonoids with fatty acids. Objective: The current study is designed to investigate the antihypertensive activity of isoquercitrin (quercetin-3-O-glucoside, Q3G) and phloridzin (PZ) in comparison to their twelve long chain fatty acid derivatives via enzymatic inhibition of renin angiotensin aldosterone system (RAAS) enzymes.Methods: The novel flavonoid esters were synthesized by the acylation of isoquercitrin and phloridzin with long chain unsaturated and saturated fatty acids (C18–C22). These acylated products were then tested for their in vitro angiotensin converting enzyme (ACE), renin and aldosterone synthase activities.Results: The linoleic and α-linolenic acid esters of PZ were the strongest (IC50 69.9-70.9 µM) while Q3G and PZ (IC50 >200 µM) were the weakest renin inhibitors in vitro (p≤0.05). The eicosapentaenoic acid ester of PZ (IC50 16.0 µM) was the strongest inhibitor of ACE, while PZ (IC50 124.0 µM) was the weakest inhibitor (p≤0.05) among all tested compounds. However, all investigated compounds had low (5.0-11.9%) or no effect on aldosterone synthase inhibition (p≤0.05). The parent compound Q3G and the eicosapentaenoic acid ester of PZ emerged as the strongest ACE inhibitors.Conclusions: The structural modification of Q3G and PZ significantly improved their antihypertensive activities. The potential use of PZ derivatives as natural health products to treat hypertension needs to be further evaluated.Keywords: hypertension, phloridzin, isoquercitrin, flavonoids, ACE, renin, RAAS, acylation, fatty acids
Scabies is a Contiguous skin disease characterized by generalized itching of skin. It is caused by skin infestation with Sarcoptesscabiei Vor hominis. Patients present with itching and many other cutaneous complications. Objective: - Objective of this study was to find epidemiology and clinical profile of scabies patients presenting to skin OPD, Hayat Abad Medical Complex (HMC), and Peshawar. Methods - This non-interventional, cross-sectionalStudy was carried out in Dermatology OPD of HM, Peshawar from 15 Oct 2022 to 15 January 2023.Permission was taken from Hospital Ethical Committee, HMC, Peshawar.867 patients of scabies wereenrolled. Diagnosis was done on basis of history and clinical examination. Their age, gender, economic class, personal hygiene, family history of scabies, address, area of body involvement and type of cutaneous presentation were recorded in predesigned performa. Results: - Out of 867 patients 472(54%) were males and 395 (46%) were female.Most cases were in age groups 5-19 years i.e. 338 (39%) with highest ratio of patients from poor socio-economic group 511(59%) and majority 643 (74.2%) having poor personal hygiene. Family history was positive in 737(85%) and we received maximum cases from 15 Dec - 15 January.
Phloridzin Fatty Acid Esters Induce Apoptosis and Alters Gene Expression in Human Liver Cancer Cells Sandhya VG Nair, Ziaullah, HP Vasantha Rupasinghe*Department of Environmental Sciences, Faculty of Agriculture, Dalhousie University, Truro, NS B2N 5E3, Canada Abstract Phloridzin (phloretin 2‐O‐glucoside) is a dihydrochalcone, which is specifically found in apple and well known for its beneficial biological effects. To date, there is no report of antiproliferative effect of phloridzin on human cancer cell lines. We have synthesized novel acylated derivatives of phloridzin with six different long chain saturated, mono‐, and poly‐unsaturated fatty acids by regioselective enzymatic acylation. We investigated the effect of these six phloridzin fatty acid esters and their parent compounds on cell proliferation of hepatocellular carcinoma cells (HepG2) and its potential molecular mechanisms. Phloridzin fatty acid esters inhibited HepG2 cells growth in a concentration‐dependent manner by inducing apoptosis, as evidenced by decreased cell viability, formation of apoptotic bodies, decreased mitochondrial membrane potential, activation of caspase 3 and inhibition of DNA topoisomerases IIα activity that might induce G0/G1 phase arrest. However, phloridzin fatty acid esters did not significantly affect the growth of normal hepatocytes. Antiproliferative effect of phloridzin docosahexaenoic acid (DHA) ester was also associated with the down regulation of anti‐apoptotic genes, growth factor receptors, PI3k/AKT/mTOR as well as epigenetics regulators. Results reveal that phloridzin fatty acid esters possess potential as therapeutic agents for treating hepatocellular carcinoma.
Present study was carried out to assess different parameters (physiochemical) of water for public health safety. 25 samples from majority of areas of Khyber-Pakhtunkhwa (KP) along with Rawalpindi and Islamabad were chosen. Total twelve parameter which include color, odour, pH, TSS (total suspended solids), TDS (total dissolved solids), Na (Sodium), K (Potassium), hardness, alkalinity, EC (Electric Conductivity), Cl (Chloride) and SO4 (Sulphate) were assessed for each sample and were compared with WHO and other limits. Results showed that very few samples 3 out of 14 in Mardan, 5/12 in Bannu, 2/11 in Buner, 3/4 in Batkhela, 1/6 in Malakand, 2/4 in Shangla, 3/18 in Mansehra, 2/7 in Karak, 1/17 in Kohat, 2/5 in Upper Dir, 3/12 in Islamabad, 3/11 in Abbottabad and 2 out of 17 samples were found to have objectionable color and odour. None of the samples exceeded the permissible limit of WHO for pH, TDS, alkalinity, Cl and SO4. While, other parameters like TSS was higher in 9 samples, Na in 2, K in 6, hardness in 1 and EC in 7 as compare to permissible limit. It was recommended that proper water treatment especially effective chlorination with residual chlorine be rendered at all sources in order to achieve safe water quality up to the consumer’s end. However, it is also important to investigate other potential water contaminations such as chemicals and microbial and radiological materials for a longer period of time, including human body fluids, in order to assess the overall water quality of Pakistan.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
customersupport@researchsolutions.com
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.
Copyright © 2025 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.