Antioxidant properties of benzylchroman derivatives from Caesalpinia sappan L. against oxidative stress evaluated in vitro.

abstract：:The present study shows the chemical profile and the in vitro properties (antioxidant and inhibition of nitric oxide production) of the Origanum heracleoticum L. (Lamiaceae). The ethanolic extract of the aerial parts is characterized by terpenes and fatty acids. The extract, with high total phenol and flavonoid conten...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Conforti F,Marrelli M,Menichini F,Tundis R,Statti GA,Solimene U,Menichini F

更新日期：2011-06-01 00:00:00

abstract：CONTEXT:Hypotension causes histologic changes in the hippocampal CA1 area, while behavior remains unchanged. We believe that an even stronger insult may also cause behavioral changes. OBJECTIVE:We used a rat hemorrhagic shock model plus temporary hypoxia to assess functional outcome at different time points post-injur...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chaparro E,Quiroga C,Erasso D,Bosco G,Rubini A,Mangar D,Camporesi E

更新日期：2014-12-01 00:00:00

abstract：:The ability of a novel bispyridinium oxime K203 to reactivate VX agent-inhibited acetylcholinesterase was compared with the reactivating efficacy of four commonly used oximes (obidoxime, trimedoxime, methoxime, HI-6) using in vivo model. Our results showed that the reactivating efficacy of the oxime HI-6 is higher tha...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kassa J,Zdarova Karasova J,Sepsova V

更新日期：2013-08-01 00:00:00

abstract：:Initial velocity enzyme kinetics was used to study the inhibition mechanism of guanidine hydrochloride (Gdm.Cl) on catalytic activity of recombinant human protein disulfide isomerase (rhPDI) in protein folding. Reduced C125A recombinant human interleukin 2 (C125A rhIL-2), the substrate, was dissolved in 8 M Gdm.Cl bef...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Du C,Wolfe JL

更新日期：2003-02-01 00:00:00

abstract：:New anticancer agents are highly needed to overcome cancer cell resistance. A novel series of pyrimidine pyrazoline-anthracene derivatives (PPADs) (4a-t) were designed and synthesised. The anti-liver cancer activity of all compounds was screened in vitro against two hepatocellular carcinoma (HCC) cell lines (HepG2 and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ahmed NM,Youns M,Soltan MK,Said AM

更新日期：2019-12-01 00:00:00

abstract：:The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and new antimycobacterial compound development. For this purpose, new triazoles were synthesized and evaluated for antituberculosis activity. A series of 4-arylidenamino-4H-1,2,4-triazol...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozdemir A,Turan-Zitouni G,Kaplancikli ZA,Chevallet P

更新日期：2007-08-01 00:00:00

abstract：:Matricaria chamomilla L. contains antioxidant flavonoids that can have their bioactivity enhanced by enzymatic hydrolysis of specific glycosyl groups. This study implements an untargeted metabolomics approach based on ultra-performance liquid chromatography coupled with electrospray ionisation quadrupole time-of-fligh...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Franco EPD,Contesini FJ,Lima da Silva B,Alves de Piloto Fernandes AM,Wielewski Leme C,Gonçalves Cirino JP,Bueno Campos PR,de Oliveira Carvalho P

更新日期：2020-12-01 00:00:00

abstract：:The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters ofN-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact e...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Aguirre-Alvarado C,Zaragoza-Martínez F,Rodríguez-Páez L,Nogueda B,Baeza I,Wong C

更新日期：2007-04-01 00:00:00

abstract：:In this work, we reported the synthesis and evaluation of antibacterial and antifungal activities of three new compound series obtained from 6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazole-3-acetic acid hydrazide: 2-{[6-(phenyl/4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl}-N-alkyl/arylhydrazinecarbothioamides (2a-...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güzeldemirci NU,Satana D,Küçükbasmacı O

更新日期：2013-10-01 00:00:00

abstract：:Human inosine 5'-monophosphate dehydrogenase 2 (hIMPDH2), being an age-old target, has attracted attention recently for anticancer drug development. Mycophenolic acid (MPA), a well-known immunosuppressant drug, was used a lead structure to design and develop modestly potent and selective analogues. The steep structure...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shah CP,Kharkar PS

更新日期：2018-12-01 00:00:00

abstract：:17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as potential 17β-HSD1 inhibitors have been synthesized. In addition, in...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Herman BE,Kiss A,Wölfling J,Mernyák E,Szécsi M,Schneider G

更新日期：2019-12-01 00:00:00

abstract：:Pig kidney diamine oxidase (DAO) and other semicarbazide-sensitive amine oxidases (SSAO) show clear substrate-inhibition kinetics and a reaction-scheme mechanism based on two substrate binding sites. We evaluated several reaction scheme mechanisms with a non-linear regression program (NCSS), estimating R2, the constan...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ignesti G

更新日期：2003-12-01 00:00:00

abstract：:In mammalian skin, melanocyte proliferation and melanogenesis can be stimulated by keratinocytes, fibroblasts and other regulatory factors. To determine whether hydroxybenzyl alcohols (HBAs) show more inhibitory in melanocytes cultured alone or in melanocytes co-cultured with keratinocytes, we developed a murine melan...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Liu SH,Chu IM,Pan IH

更新日期：2008-08-01 00:00:00

abstract：:The synthesis of new 4-[2-(alkylamino)ethylthio]pyrrolo[1,2-a]quinoxaline derivatives la-1 is described in five or six steps starting from various substituted nitroanilines 2a-e. The bioisostere 5-[2-(alkylamino)ethylthio]pyrrolo[1,2- a]thieno[3,2-e]pyrazine 1m was also prepared. The new derivatives were evaluated as ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vidaillac C,Guillon J,Moreau S,Arpin C,Lagardère A,Larrouture S,Dallemagne P,Caignard DH,Quentin C,Jarry C

更新日期：2007-10-01 00:00:00

abstract：:This article describes the photodynamic inactivation of mosquito iridescent virus (MIV) Aedes flavescens in the presence of water-soluble C(60) fullerenes. It has been observed that the photodynamic inactivation of MIV for about 1 h reduces the infectious titre of the virus in large wax-moth larvae Galleria mellonella...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rud Y,Buchatskyy L,Prylutskyy Y,Marchenko O,Senenko A,Schütze Ch,Ritter U

更新日期：2012-08-01 00:00:00

abstract：:We investigated the antioxidant and enzyme inhibitory activities and chemical composition of the hydro-distilled essential oil (0.35% yield) from aerial parts of Thymus spathulifolius. Antioxidant capacity of the oil was assessed by different methods including free radical scavenging (DPPH and ABTS), reducing power (F...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ceylan R,Zengin G,Uysal S,Ilhan V,Aktumsek A,Kandemir A,Anwar F

更新日期：2016-12-01 00:00:00

abstract：:Telomeres length and telomerase activity are currently considered aging molecular stigmata. Water is a major requirement for our body and water should be alkaline. Recent reports have shown that aging is related to a reduced water intake. We wanted to investigate the effect of the daily intake of alkaline water on the...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Logozzi M,Mizzoni D,Di Raimo R,Andreotti M,Macchia D,Spada M,Fais S

更新日期：2020-12-01 00:00:00

abstract：:A new series of 6, 7-dihydroxy-3-(methylphenyl) chromenones, including three new derivatives, i.e. 6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one (OPC); 6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one (MPC); 6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one (PPC) and one previously described, namely 6,7-dihydroxy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Basaran I,Sinan S,Cakir U,Bulut M,Arslan O,Ozensoy O

更新日期：2008-02-01 00:00:00

abstract：:The synthesis and biological evaluation of some novel thiazolofluorenones, thiazolofluorenes and thiazoloanthraquinones, substituted with amino side-chains are described. These polyheterocyclic compounds have been synthesized via the corresponding imino-1,2,3-dithiazoles. Their cytotoxic activity and their eventual se...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chabane H,Pierre A,Leonce S,Pfeiffer B,Renard P,Thiery V,Guillaumet G,Besson T

更新日期：2004-12-01 00:00:00

abstract：:This study reports on a preliminary structure-activity relationship exploration of 4-aryliden-2-methyloxazol-5(4H)-one-based compounds as MAGL/FAAH inhibitors. Our results highlight that this scaffold may serve for the development of selective MAGL inhibitors. A 69-fold selectivity against MAGL over FAAH was achieved ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Granchi C,Rizzolio F,Bordoni V,Caligiuri I,Manera C,Macchia M,Minutolo F,Martinelli A,Giordano A,Tuccinardi T

更新日期：2016-01-01 00:00:00

abstract：:The reaction mechanism of glycoside hydrolases belonging to family 1 (GH1) of carbohydrate-active enzymes classification, hydrolysing β-O-glycosidic bonds, is well characterised. This family includes several thousands of enzymes with more than 20 different EC numbers depending on the sugar glycone recognised as substr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Strazzulli A,Perugino G,Mazzone M,Rossi M,Withers SG,Moracci M

更新日期：2019-12-01 00:00:00

abstract：:A new series of fluorine containing 1,3,5-triazinyl sulfonamide derivatives obtained from cyanuric fluoride, sulfanilamide/4-aminoethylbenzenesulfonamide followed and incorporating also amin0, amino alcohol and amino acid moieties have been investigated as inhibitors of three β-carbonic anhydrases (CAs, EC 4.2.1.1) fr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ceruso M,Vullo D,Scozzafava A,Supuran CT

更新日期：2014-10-01 00:00:00

abstract：:A novel series of substituted pyrimidine compounds bearing N-phenylpyrazole and terminating with aryl and cyclic sulfonamido moiety were designed, synthesized, and evaluated in vitro as antiproliferative agents against a panel of 53 cell lines of different tissues at the NCI. Among them, compound 1d with p-chlorobenze...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gamal El-Din MM,El-Gamal MI,Abdel-Maksoud MS,Yoo KH,Baek D,Choi J,Lee H,Oh CH

更新日期：2016-01-01 00:00:00

abstract：:Previously, a glycoglycerolipid isolated from marine algae was reported to be a potent and selective inhibitor of the human Myt1 kinase, an enzyme involved in cell cycle regulation with great potential as an anti-cancer target. Based on that report, a lot of research effort has been invested by several working groups ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rohe A,Göllner C,Erdmann F,Sippl W,Schmidt M

更新日期：2015-06-01 00:00:00

abstract：:Ligand-protein docking is one of the most common techniques used in virtual screening campaigns. Despite the large number of docking software available, there is still the need of improving the efficacy of docking-based virtual screenings. To date, only very few studies evaluated the possibility of combining the resul...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Poli G,Martinelli A,Tuccinardi T

更新日期：2016-01-01 00:00:00

abstract：:Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites an...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Brito CCB,Silva HVCD,Brondani DJ,Faria AR,Ximenes RM,Silva IMD,Albuquerque JFC,Castilho MS

更新日期：2019-12-01 00:00:00

abstract：:Protein phosphatases are signalling molecules that regulate a variety of fundamental cellular processes including cell growth, metabolism and apoptosis. The aim of this work was to correlate the cytotoxicity of pervanadate and okadaic acid on HL60 cells and their effect on the phosphatase obtained from these cells. Th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Freire AC,Aoyama H,Haun M,Ferreira CV

更新日期：2003-10-01 00:00:00

abstract：CONTEXT:Endocrinological factors have been recently described to affect respiratory mechanics. OBJECTIVE:To review recent literature data, most of all obtained by the end-inflation occlusion method, describing the effects of molecules of endocrinological interest such as endothelin, erythropoietin and renin-angiotensi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rubini A,Frigo A,Carniel EL

更新日期：2016-12-01 00:00:00

abstract：:Starting from a simple general reaction mechanism of activation of aspartic proteinases zymogens involving a uni- and a bimolecular simultaneous activation route and a reversible inhibition step, the time course equation of the zymogen, inhibitor and activated enzyme concentrations have been derived. Likewise, express...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Muñoz-López A,Sotos-Lomas A,Arribas E,Masia-Perez J,Garcia-Molina F,García-Moreno M,Varon R

更新日期：2007-04-01 00:00:00

abstract：:The synthesis, in vitro antimicrobial activities of some novel hydroxy pyridines supported with various pharmacophores is described. Twenty-six out of the tested 58 compounds exhibited variable inhibitory effects on the growth of the tested Gram positive and Gram negative bacteria. The tested compounds revealed better...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Faidallah HM,Rostom SA,Khan KA,Basaif SA

更新日期：2013-10-01 00:00:00