Tautomerism of Some 5-Arylazo-2-thiohydantoin Derivatives as a Criterion of Their Acidity

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Botanical and genetic characterization of Hydrocotyle umbellata L. cultivated in Egypt

Hydrocotyle umbellata L. is a creeping aquatic herb belonging to family Araliaceae. The plant has been used in folk medicine as an anti-inflammatory, anxiolytic and memory stimulant herb. This study targets the botanical features of the leaf, rhizome and roots, in addition to DNA fingerprinting using rapid amplified (RAPD) and inter simple sequence repeat (ISSR) based polymerase chain reaction (PCR) techniques. Microscopically, leaves and rhizomes are characterized by numerous brown schizogenous ducts containing volatile oils. On the other hand, a total of 34 random amplified polymorphic DNA (RAPD) markers were identified using seven random decamer primers and a total of 15 inter simple sequence repeat (ISSR) markers were identified using five decamer random primers. Both the botanical study and DNA fingerprinting could be useful in identification and authentication of the plant

Electrochemical behaviour of some 1,3,4-thiadiazole derivatives: Part 2 - Effect of acid and base on electro-oxidation mechanism of 2-benzoylamino- 5-( 1-cyanoarylhydrazono )-1,3,4-thiadiazoles at a platinum anode

864-867The oxidation of the title compounds in acetonitrile containing LiClO4 as supporting electrolyte, in both acidic and basic media, has been studied by cyclic voltammetry, coulometry and preparative electrolysis. In the presence of HClO4, the compounds are oxidized in the protonated forms and the main products are the corresponding perchlorate salts, whereas in media containing γ-collidine, the anion is the oxidizable moiety and the 4-aminocinnoline derivative is the main product. Mechanism of electrochemical oxidation is proposed and discussed

MS/MS-based molecular networking for mapping the chemical diversity of the pulp and peel extracts from Citrus japonica Thunb.; in vivo evaluation of their anti-inflammatory and anti-ulcer potential

Although inflammation is a beneficial response to harmful triggers, the associated diseases develop the potential for death-threatening conditions. Citrus species are valuable sources of chemical compounds with diverse structural properties that could alleviate damaging inflammation and reduce serious side effects of synthetic drugs. Kumquats are the smallest trees among the citrus family widely distributed in Asia, Europe, and North America, with little cultivation in Africa. The current study aims to conduct comprehensive chemical, anti-inflammatory and anti-ulcer studies of Citrus japonica, thus focusing attention on extensive cultivation of these species in Africa to enhance their beneficial uses. A comparative chemical profiling of peel and pulp extracts was performed via HPLC-MS/MS analysis, 164 metabolites were annotated aided by the spectral similarity networks. Around 148 of which were visualized as a species-first documentation. Phenolics were the predominant classes including methoxylated flavonoids, O/C-glycosylated flavones, and flavanones with the less common O- or C-O-triglycosyl methoxylated flavones among the genus Citrus. Moreover, the anti-inflammatory study demonstrated the significant activity of the pulp and peel extracts (200 and 400 mg/kg, p.o.) via reducing paw swelling induced by carrageenan at all-time points and decreasing the formation of TNF-α and IL-1β. Moreover, in ethanol-induced gastric ulcer rat model, the high doses of both extracts significantly improved ulcer indexes and suppressed gastric inflammation by inhibiting myeloperoxidase activity and possessed an antioxidant effect via increasing reduced glutathione, decreasing malondialdehyde, and nitric oxide. Additionally, histopathological investigations confirmed the anti-inflammatory and anti-ulcer effects. Considering the two fruit tissues, peels markedly improved inflammatory and gastroprotective properties associated with the high diversity of their flavonoid structures

Discovery of 4-benzyloxy and 4-(2-phenylethoxy) chalcone fibrate hybrids as novel PPAR\u3b1 agonists with anti-hyperlipidemic and antioxidant activities: Design, synthesis and in vitro/in vivo biological evaluation

In the current work, a series of novel 4-benzyloxy and 4-(2-phenylethoxy) chalcone fibrate hybrids (10a-o) and (11a-e) were synthesized and evaluated as new PPAR\u3b1 agonists in order to find new agents with higher activity and fewer side effects. The 2-propanoic acid derivative 10a and the 2-butanoic acid congener 10i showed the best overall PPAR\u3b1 agonistic activity showing Emax% values of 50.80 and 90.55%, respectively, and EC50 values of 8.9 and 25.0 \u3bcM, respectively, compared to fenofibric acid with Emax = 100% and EC50 = 23.22 \u3bcM, respectively. These two compounds also stimulated carnitine palmitoyltransferase 1A gene transcription in HepG2 cells and PPAR\u3b1 protein expression. Molecular docking simulations were performed for the newly synthesized compounds to study their predicted binding pattern and energies in PPAR\u3b1 active site to rationalize their promising activity. In vivo, compounds 10a and 10i elicited a significant hypolipidemic activity improving the lipid profile in triton WR-1339-induced hyperlipidemic rats, including serum triglycerides, total cholesterol, LDL, HDL and VLDL levels. Compound 10i possessed better anti-hyperlipidemic activity than 10a. At a dose of 200 mg/kg, it demonstrated significantly lower TC, TG, LDL and VLDL levels than that of fenofibrate at the same dose with similar HDL levels. Compounds 10i and 10a possessed atherogenic indices (CRR, AC, AI, CRI-II) like that of fenofibrate. Additionally, a promising antioxidant activity indicated by the increased tissue reduced glutathione and plasma total antioxidant capacity with decreased plasma malondialdehyde levels was demonstrated by compounds 10a and 10i. No histopathological alterations were recorded in the hepatic tissue of compound 10i (200 mg/kg)

INVESTIGATION OF THE LIPID AND CARBOHYDRATE CONTENTS OF GREWIA TENAX FORSSK. FRUITS & EVALUATION OF HEPATOPROTECTION ACTIVITY

Objective: Grewia tenax Forssk. is represented in Egypt and known for its edible fruits which are nutritionally balanced and rich in iron and calcium. This work was to investigate the Lipid and Carbohydrate Contents of Grewia tenax Forssk. fruits and evaluation of Hepatoprotection activity.Methods: Investigation of carbohydrate contents of Grewia tenax Forssk. fruits were carried out using HPLC. The lipids content of Grewia tenax Forssk. fruits were analyzed by GLC. Also, the hepatoprotective activity on rat hepatocytes monolayer culture was studied.Results: The HPLC analysis of free sugars of Grewia tenax Forssk. fruits revealed the presence of stachyose, sucrose, glucose and fructose. While the HPLC analysis of the polysaccharide hydrolysate from Grewia tenax Forssk. fruits showed the presence of glucuronic acid, glucose, galactose and arabinose.GLC of the unsaponifiable matter of hexane extract of Grewia tenax Forssk. fruits revealed the presence of a mixture of a series of n-alkanes (63%) and a series of sterols (9.9%). A series of hydrocarbons ranging from C10-C26 in addition to cholesterol, campasterol, stigmasterol and β-Sitosterol and six fatty acids among which Linoleic acid (C18:2) was the major one (55.5 %) was identified. Also, the hepatoprotective activity study of the extracts of Grewia tenax Forssk. fruits (80% MeOH extract of defatted powder) and water extract indicated that they exhibited hepatoprotection at (25 μg/ml and 50 μg/ml) and (12.5 μg/ml to 100 μg/ml); respectively.Conclusion: Our study was the first record of carbohydrate and lipid fraction contents of Grewia tenax Forssk. fruits. From the obtained results, the highly nutritive and medicinal values of Grewia tenax Forssk. fruits should be considered. Furthermore, and due to the high hepatoprotection effects of the plant extracts, further investigation and studies should be done to isolate the bioactive compounds. Â