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

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

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

Dioscorea Plants: A Genus Rich in Vital Nutrapharmaceuticals-A Review

Dioscorea species, known as “Yams,” belong to family Dioscoreaceae. This genus consists of more than 600 species distributed from Africa, Asia, the Caribbean’s South America, and the South Pacific islands. Their organoleptic properties make them the most widely used carbohydrate food and dietary supplements. The underground and/or aerial tubers represent valuable sources of proteins, fats, and vitamins for millions of people in West Africa. This review gives a shot of secondary metabolites of Dioscorea plants, including steroids, clerodane diterpenes, quinones, cyanidins, phenolics, diarylheptanoids, and nitrogen-containing compounds. This review collected the evidence on biological properties of description Dioscorea, including in-vitro and in-vivo studies. Dioscorea species contain promising bioactive molecules i.e. diosgenin that support their different biological properties, including antioxidant, hypoglycaemic, hypolipidemic, anti- antimicrobial, inflammatory, antiproliferative, androgenic, estrogenic, and contraceptive drugs. Indeed, besides its nutrient values, Dioscorea is a potential source of bioactive substances of interest in the prevention/ treatment of several diseases, and thus represents a great challenge in developing countries. However, ethnomedicinal potential should be validated and further researches on pharmacological properties and phytochemical composition should be carried out. Particularly, doing some studies to convert the preclinical results to clinical efficacy should be guaranteed