Syntheses, Characterization and Biological Activity of Novel Thiazoylazo Dye and Its Coordination Compounds

The present work describes the synthesis of a novel heterocyclic azo dye by general diazonization of 2-amino-4,5-dimethylthiazole followed by the diazo- coupling of the resulting diazonium ion with 5-methyl-2-(propan-2-yl)phenol to obtain ligand L. This was characterized using Fourier-transformed infrared and electronic spectrophotometry. Ligand L was further coordinated with five metal ions, M:L, 1:2 [M = Cu(II), Mn(II), Zn(II), Ni(II) and Co(II)]. The coordination compounds obtained were characterized by electronic, IR spectrophotometry, magnetic susceptibility and percentage metal analyses. The results obtained suggested that a thiazoylazo dye was obtained as ligand L. It was proposed that two molecules of the solvent coordinated to the metal ion in addition with the ligands to give an octahedral geometry for copper(II), manganese(II) and nickel(II) complexes. On the other hand, square planar geometry was suggested for zinc(II) and cobalt(II) complexes. The anti-infla- mmatory activity of the ligand and coordination compounds was evaluated using four in vitro-based assays viz: xanthine oxidase and lipoxygenase inhibition assay, membrane stability and protein denaturation assay. The synthesized compounds generally exhibited good anti-inflammatory activity in all the assays carried out. However, the reference standards, in this instance, were more effective in the case of xanthine oxidase, lipoxygenase and protein denaturation inhibitory assays. For the membrane stability study, the coordination compounds and ligand L elicited more potent anti-inflammatory activity than the standard drug.

A systematic study on mycochemical profiles, antioxidant, and anti-inflammatory activities of 30 varieties of Jew’s ear(Auricularia auricula-judae)

The health-promoting properties and chemical profiles of 30 Jew’s ear mushroom varieties were investigated. The antioxidant properties were determined by ferric reducing antioxidant power(FRAP), 1,1-diphenyl-2-picrylhydrazyl(DPPH) free radical scavenging, 2,2’-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS) free radical scavenging, and metal chelating ability(MCA) assays, while phenolic profiles were determined by total phenol content(TPC) and total flavonoid content(TFC) colorimetric assays. Total carbohydrate, β-glucan, and melanin contents were determined by colorimetric methods. 5’-Nucleotides, vitamin D_(2), ergosterol, and ergothioneine contents were determined by high performance liquid chromatography(HPLC). Anti-inflammation activities of Jew’s ear were evaluated by the colorimetric protease inhibitory method. The results showed that Jew’s ear mushrooms possessed substantial phenolics and antioxidant properties. All the Jew’s ear varieties contain high amount of total carbohydrate, β-glucan, reducing sugar, melanin, pectin, vitamin D2, ergosterol, and ergothioneine. The current findings could provide scientific information for breeders to nurture desired varieties and for food industry to develop new health promoting products.

Synthesis and anti-HBV evaluation of mono L-amino acid ester, mono non-steroid anti-inflammation drug carboxylic ester derivatives of acyclonucleoside phosphonates

A series of mono L-amino acid ester, mono non-steroid anti-inflammation drug （NSAID）, carboxylic ester derivatives of acyclonucleoside phosphonates were prepared by using a ＂one pot synthesis＂ method and their in vitro anti-HBV activity were evaluated in HepG 2.2.15 cells. Compound 9a exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with IC50 and selective index （SI） values of 0.48μmol/L and 763.72, respectively.