Synthesis and Characterization of Novel Rutin Derivatives with Potential Antioxidant Properties

Rutin, a flavonol glycoside isolated from the fruit peels of Malus domestica family Rosaceae, is well known to possess antioxidant activity. This research was conducted in order to synthesize and characterize rutin derivatives and evaluate their antioxidant activities. Four derivatives were synthesized namely, Rutin-oxy-5, 7, 4' acetic acid (2), Rutin -oxy- 5,7, 4' methyl benzoate amide (3), 2'', 2''', 2''''-rutinoxymethyl-3-amino-1 -benzo[5,6-a] pyrimidine-4-one (4) and 5'', 5''', 5''''-tri-p-methoxybenzylideneamino-6-rutinoxy-benzo[5,6-a]-pyrimidin-4(5H)-one (5). Their structures were elucidated using different spectral data (Mass, IR and 1H, 13C NMR). The antioxidant activities of rutin and its derivatives were evaluated by reducing power, Fe+2 chelating, DPPH* and ferric thiocyanate FTC assays. In addition, the results were compared with natural and synthetic antioxidants, such as α- tocopherol, butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA) and trolox. Rutin and its derivatives were exhibited a strong reducing power, chelating activity on Fe2+ and free radical-scavenging.  Antioxidant activity of rutin and its derivatives increased with increased concentrations. Total antioxidant activity of rutin, its derivatives and both standards decreased in the order of rutin > compound (5) > trolox > compound (2) > BHA > compound (4) > compound (3). This study showed that Rutin and its derivatives exhibited antioxidant activity in all tests and could be considered as a source of natural and synthetic antioxidants.

Consuming Fat Supplemented Diet with Different Vegetable Oils Impacts the Serum Lipid Profiles and Body Weights of Male Rats

This research was conducted in order to evaluate the influence of consuming diet supplemented with different types of fixed oils (Olive oil, Soybean oil and Coconut oil) on the lipid profiles and body weights of healthy albino rats and linking these effects to their chemical compositions thus reaching out to recommendation about the healthiest type of fats among the studied oils to be used in healthy nutrition programs. The lipid contents of the fixed oils were determined by Gas Chromatography (GC) method, the vitamin contents were determined by High Performance Liquid Chromatography (HPLC) and the proximate analyses of the oils were also evaluated by different assays. Twenty-four healthy male albino rats were divided into four groups as follows: Olive oil supplemented diet, Soybean oil supplemented diet, Coconut oil supplemented diet and oil-free supplemented diet control group. The dieting continued for 28 days, at the end of which, the serum levels of total cholesterol, Low Density Lipoproteins (LDL), High Density Lipoproteins (HDL), Triglycerides (TG) and Free Fatty Acid (FFA) were measured spectrophotometrically and the rats body weights were monitored on daily basis. The results showed that olive oil, the richest studied oil in unsaturated fatty acids (84.16 %), had favorable effect on the rats’ lipid profiles, serum free fatty acid levels and rats body weights. In conclusion, olive oil supplemented diets are considered healthy diets and beneficial to decrease the risk of cardiovascular diseases

Profile of bioactive compounds of Capparis spinosa var. aegyptiaca growing in Egypt

The present study was designed to investigate polyphenolic and sulphur contents of the aerial parts of Capparis spinosa var. aegyptia (Lam.) Boiss., Capparaceae, wildly growing in Egypt. The chemical compositions of the water distilled essential oil were investigated by GC/MS analysis where the major constituent of the oil was methyl isothiocyanate (24.66%). Hydroethanolic extract was evaluated by LC-HRESI-MS⿿MS in both positive and negative modes. Forty-two compounds were identified including quercetin, kaempferol and isorhamnetin derivatives in addition to myricetin, eriodictyol, cirsimaritin and gallocatechin derivatives. Quercetin tetrahexoside dirhamnoside as well as kaempferol dihexoside dirhamnoside have not been identified before in genus Capparis. Phenolic acids, such as quinic acid, p-coumaroyl quinic acid and chlorogenic acid were also identified. Evaluation of cytotoxic activity of hydroethanolic extract against three human cancer cell lines (MCF-7; breast adenocarcinoma cells, Hep-G2; hepatocellular carcinoma cells and HCT-116; colon carcinoma) using 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay showed significant effect with IC50 values 24.5, 24.4 and 11 μg/ml, compared to Doxorubicin as a standard cytotoxic drug. C. spinosa revealed itself as a promising candidate for nutraceutical researches. Keywords: Capparis spinosa, LC-HRESI-MS⿿MS, Flavonoids, Isothiocyanate, Cytotoxicit

The impact of transformational leadership style on employee satisfaction

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A putative Chondroprotective role for IL-1β and MPO in herbal treatment of experimental osteoarthritis

Abstract Background Herbal treatment may have a chondroprotective and therapeutic effect on Osteoarthritis (OA). We investigated the mechanism of action of ginger and curcumin rhizomes cultivated in Egypt in treatment of OA in rat model. Methods Thirty-five albino rats were intra-articularly injected with Monosodium Iodoacetate in the knee joint. Ginger and curcumin was orally administered at doses of 200 and 400 mg/kg (F200 and F400). Serum levels of cartilage oligomeric matrix protein (COMP), hyaluronic acid (HA), malondialdehyde (MDA), myeloperoxidase (MPO), Interleukin-1 beta (IL-1β) and superoxide dismutase activity (SOD) were measured using ELISA. The composition of the herbal formula hydro-ethanolic extract was characterized using UPLC-ESI-MS. Histopathological changes in injected joints was examined using routine histopathology. Statistical analysis was performed using one-way ANOVA. Results Serum levels of COMP, HA, MPO, MDA, and IL-1β were significantly decreased in F 200, F 400 and V groups when compared to OA group (P value <0.0001). On the other hand SOD levels were significantly elevated in treated groups compared to OA groups (P value <0.0001). Conclusions The ginger/curcumin at 1:1 had chondroprotective effect via anti-inflammatory and antioxidant effect in rat OA model. Further pharmacological and clinical studies are needed to evaluate this effect

Additional file 1: of Resistin mediates tomato and broccoli extract effects on glucose homeostasis in high fat diet-induced obesity in rats

Individual data for serum resistin, leptin, and adiponectin. (DOCX 18 kb

Looking at marine-derived bioactive molecules as upcoming anti-diabetic agents: A special emphasis on PTP1B inhibitors

Diabetes mellitus (DM) is a chronic metabolic disease with high morbimortality rates. DM has two types: type 1, which is often associated with a total destruction of pancreatic beta cells, and non-insulin-dependent or type 2 diabetes mellitus (T2DM), more closely associated with obesity and old age. The main causes of T2DM are insulin resistance and/or inadequate insulin secretion. Protein-tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling pathways and plays an important role in T2DM, as its overexpression may induce insulin resistance. Thus, since PTP1B may be a therapeutic target for both T2DM and obesity, the search for novel and promising natural inhibitors has gained much attention. Hence, several marine organisms, including macro and microalgae, sponges, marine invertebrates, sea urchins, seaweeds, soft corals, lichens, and sea grasses, have been recently evaluated as potential drug sources. This review provides an overview of the role of PTP1B in T2DM insulin signaling and treatment, and highlights the recent findings of several compounds and extracts derived from marine organisms and their relevance as upcoming PTP1B inhibitors. In this systematic literature review, more than 60 marine-derived metabolites exhibiting PTP1B inhibitory activity are listed. Their chemical classes, structural features, relative PTP1B inhibitory potency (assessed by IC 50 values), and structure–activity relationships (SARs) that could be drawn from the available data are discussed. The upcoming challenge in the field of marine research—metabolomics—is also addressed.N. Martins would like to thank the Portuguese Foundation for Science and Technology (FCT–Portugal) for the Strategic project, reference numbers UID/BIM/04293/2013 and “NORTE2020-Programa Operacional Regional do Norte” (NORTE-01-0145-FEDER-000012)

Looking at Marine-Derived Bioactive Molecules as Upcoming Anti-Diabetic Agents: A Special Emphasis on PTP1B Inhibitors

Diabetes mellitus (DM) is a chronic metabolic disease with high morbimortality rates. DM has two types: type 1, which is often associated with a total destruction of pancreatic beta cells, and non-insulin-dependent or type 2 diabetes mellitus (T2DM), more closely associated with obesity and old age. The main causes of T2DM are insulin resistance and/or inadequate insulin secretion. Protein-tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling pathways and plays an important role in T2DM, as its overexpression may induce insulin resistance. Thus, since PTP1B may be a therapeutic target for both T2DM and obesity, the search for novel and promising natural inhibitors has gained much attention. Hence, several marine organisms, including macro and microalgae, sponges, marine invertebrates, sea urchins, seaweeds, soft corals, lichens, and sea grasses, have been recently evaluated as potential drug sources. This review provides an overview of the role of PTP1B in T2DM insulin signaling and treatment, and highlights the recent findings of several compounds and extracts derived from marine organisms and their relevance as upcoming PTP1B inhibitors. In this systematic literature review, more than 60 marine-derived metabolites exhibiting PTP1B inhibitory activity are listed. Their chemical classes, structural features, relative PTP1B inhibitory potency (assessed by IC50 values), and structure&#8315;activity relationships (SARs) that could be drawn from the available data are discussed. The upcoming challenge in the field of marine research&#8212;metabolomics&#8212;is also addressed