This study attempts to compare the pharmaceutical potential (antioxidant and key enzyme inhibition of clinical relevance) of organic and aqueous extracts of Parentucellia latifolia (L.) Caruel subsp. latifolia (L.) Caruel as well as phytochemical composition. The phytochemical compounds were eva...
Atherosclerosis is a chronic inflammatory disease of the vascular walls. ApoCIII is an independent factor which promotes atherosclerotic processes. This study aimed to investigate whether Loganin administration inhibits the inflammatory response in vitro and in vivo. In the apoCIII-induced mouse...
Inhibitors of protein synthesis such as chloramphenicol, streptomycin and pyromycin, have no effect on mycobacillin synthesis in a cell-free system. K+, NH4+ and non-mycobacillin amino acids appear to be neither stimulatory nor inhibitory whereas mercaptoethanol stimulates synthesis. Enzyme syst...
Mycobacillin has been purified and isolated as fine needle-shaped crystals from culture filtrates of Bacillus subtilis. Various purity tests show that the compound is homogeneous. Various physicochemical studies indicate that the pure compound is a polypeptide, somewhat different in chemical com...
The isotherms, π-A curves at air-water interface for mycobacillin, cholesterol, ergosterol, ergocalciferol, stigmasterol and cholesterol benzoate show that the antibiotic is compressible and collapses at 11.5 dyn/cm whereas the sterols are generally incompressible and do not show collapse withi...
Publisher SummaryThis chapter discusses carbonic acid and its derivatives, a large and diverse group of compounds. Metacarbonic acid and its esters, such as carbon dioxide, esters of carbonic acid, anhydrides of primary esters of carbonic acid, mixed anhydrides of primary carbonates, and mono-ca...
Application of the Bucherer reaction between 1-naphthol and alky lamines gave a satisfactory synthesis of N-substituted 1-naphthylamines. A method avoiding the use of pressurised reaction vessels, i.e. reaction of 1-naphthol with alkylamines in the presence of zinc chloride and hydrochloric acid...
The methyl and 1-octyl β-glycosides of the P-antigen tetrasaccharide [globotetraose, β-d-GalpNAc-(1→3)-α-d-Galp-(1→4)-β-d-Galp-(1→4)-d-Glc] were synthesised from a tetrasaccharide precursor, prepared using methyl disaccharide 1-thioglycosides as intermediates. In the key glycosidation wit...
Publisher SummaryThis chapter focuses on the low-molecular weight carbohydrates that can be formally considered as the oxidation products of mono- or oligo-saccharides in which an aldehyde group and/or one or more hydroxyl groups have been oxidized to carbonyl and/or carboxyl groups. Some acids ...
The interaction of the azidoacetic acid, N3CH2COOH, with an Ag (1 1 1) crystal modified by surface carbon has been observed. XPS measurements of C (1 s), O (1 s), N (1 s) and Ag 3d3/2,5/2 as a function of the exposure have been used to follow the predominant species rising with the azide adsorpt...
(R)-2-Azidoesters and their derived (R)-2-azido acids are readily prepared from common amino acids by an inversion methodology that employs (S)-2-nosyloxyesters as key intermediates. The (R)-2- azidoesters can be used as protected amino acid equivalents in peptide synthesis. Basic hydrolysis fre...
Under very mild conditions, biotransformations of racemic azido nitriles using Rhodococcus erythropolis AJ270, a nitrile hydratase/amidase-containing microbial whole-cell catalyst, afforded highly enantiopure, (R)-α-arylmethyl- and (+)-α-cyclohexylmethyl-β-azidopropanoic acids and their (S)- ...
We examined the ability of wedelolactone, heparin and para-bromophenacyl bromide to antagonize the myotoxic activity in mice of venoms from Crotalus viridis viridis and Agkistrodon contortrix laticinctus and two phospholipase A2 myotoxins, CVV myotoxin and ACL myotoxin, isolated from them. Myoto...
The influence of p-bromophenacyl bromide (pBPAB) and structural analogues on the assembly and Ca2+ sensitivity of porcine brain microtubules (MTs) was studied by spectrophotometric measurements in vitro. MT assembly was inhibited by 36 μM pBPAB but not by the structural analogues p-chlorophenac...
For the first time, the structure of a catalytic inactive phospholipase A2 homolog (Lys49-PLA2s) complexed with p-bromophenacyl bromide (BPB) has been solved by X-ray crystallography. Lys49-PLA2s are among the main components of Viperidae snake venoms, causing myonecrosis and other actions despi...
An acidic phospholipase A2 (PLA2) isolated from Bothrops jararacussu snake venom was crystallized with two inhibitors: α-tocopherol (vitamin E) and p-bromophenacyl bromide (BPB). The crystals diffracted at 1.45- and 1.85-Å resolution, respectively, for the complexes with α-tocopherol and p-bro...
We previously demonstrated that potassium (KCl)-induced depolarization of synaptoneurosomes prepared from rat telencephalon increased [3Hamino-3-hydroxy-5-methylisoxazole-4-propionate ([3HAMPA) binding to the AMPA receptor. In the present study, we determined the effects of inhibitors of various...
A series of novel 1-((indol-3-yl)methyl)–1H-imidazolium salts were prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 5,6-dimethyl-benzimidazole ring, and substitution of the imidazolyl-3-position with a naphthylacyl or 4-bromophenacyl group,...
C. Díaz, J. M. Gutiérrez, B. Lomonte and J. Núñez. p-Bromophenacyl bromide modification of Bothrops asper myotoxin II, a lysine-49 phospholipase A2, affects its pharmacological activities. Toxicon31, 1202–1206, 1993.—Modification of Bothrops asper myotoxin II, a lysine-49 phospholipase A2 v...
4-Bromophenacyl bromide (BPB) is generally used as a phospholipase A2 (PLA2) inhibitor. In the present study, we demonstrate that BPB induces Ca2+ influx in human gingival fibroblasts. In fura-2-loaded human gingival fibroblasts, BPB evoked a transient increase in intracellular Ca2+ concentratio...
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