Phenolic compounds with pancreatic lipase inhibitory activity from Korean yam (Dioscorea opposita).

abstract：:The galangal (the rhizome of Alpinia officinarum, Hance) is popular in Asia as a traditional herbal medicine. The present study reports that the galangal extract (GE) can potently inhibit fatty-acid synthase (FAS, E.C.2.3.1.85). The inhibition consists of both reversible inhibition with an IC50 value of 1.73 microg dr...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Li BH,Tian WX

更新日期：2003-08-01 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

abstract：:The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio- and ester-derivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-3',4'-dithioglycol (1) and avarol-4'-(3)mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Tommonaro G,Pejin B,Iodice C,Tafuto A,De Rosa S

更新日期：2016-08-01 00:00:00

abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous enzymes that catalyze the hydration of CO(2) to bicarbonate and protons. Inhibition of CAs has been clinically exploited for the treatment of various classes of diseases for decades, but investigating new classes of inhibitors continues to be important. We have synt...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ayvaz S,Çankaya M,Atasever A,Altuntas A

更新日期：2013-04-01 00:00:00

abstract：:The present study investigated the ability of the arginine analog L-NAME (N(omega)-Nitro-L-arginine methyl ester) to modulate the activity of arginase. L-NAME inhibited the activity of arginase in lysates from rat colon cancer cells and liver. It also inhibited the arginase activity of tumor cells in culture. Furtherm...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Reisser D,Onier-Cherix N,Jeannin JF

更新日期：2002-08-01 00:00:00

abstract：:This paper reports the synthesis of O-methyl and O-ethyl NSAID hydroxamic acids, their antimicrobial activities, and their ability to inhibit urease and soybean lipoxygenase activities. Ibuprofen and fenoprofen hydroxamic acids with free hydroxy groups present the highest antimicrobial activity, while indomethacin and...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Rajić Z,Perković I,Butula I,Zorc B,Hadjipavlou-Litina D,Pontiki E,Pepeljnjak S,Kosalec I

更新日期：2009-10-01 00:00:00

abstract：:The flip regression procedure that we used earlier for handling the xanthones system has been applied to phenylaminoquinazoline analogues. It is known that the substituents at the 6- and 7- positions of the polycyclic system have been identified as the most important structural features. The steric as well as the elec...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Deeb O,Clare BW

更新日期：2008-12-01 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：:Nerve agents such as sarin, cyclosarin and tabun are organophosphorus substances able to inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators and anticholinergics are generally used as antidotes in the case of intoxication with these agents. None of the known AChE reactivators is able to react...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Hrabinova M,Musilek K,Jun D,Kuca K

更新日期：2006-10-01 00:00:00

abstract：:The antioxidant activity of extracts from Caesalpinia sappan L. (CSL) was studied in vitro by evaluating the total phenolics, measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) and on reactive nitrogen species (RNS), and measuring the inhibitory effect on Cu(2...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lee MJ,Lee HS,Kim H,Yi HS,Park SD,Moon HI,Park WH

更新日期：2010-10-01 00:00:00

abstract：:Histone demethylation is a vital process in epigenetic regulation of gene expression. A number of histone demethylases are present to control the methylated states of histone. Among these enzymes, KDM4s are one subfamily of JmjC KDMs and play important roles in both normal and cancer cells. The discovery of KDM4s inhi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lin H,Li Q,Li Q,Zhu J,Gu K,Jiang X,Hu Q,Feng F,Qu W,Chen Y,Sun H

更新日期：2018-12-01 00:00:00

abstract：:Isocitrate dehydrogenase (IDH) gene from Staphylococcus aureus ATCC12600 was cloned, sequenced and characterized (HM067707). PknB site was observed in the active site of IDH; thus, it was predicted as IDH may be regulated by phosphorylation. Therefore, in this study, PknB, alkaline phosphatase III (SAOV 2675) and IDH ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Prasad UV,Vasu D,Yeswanth S,Swarupa V,Sunitha MM,Choudhary A,Sarma PV

更新日期：2015-01-01 00:00:00

abstract：:Cytosine deaminase (CD) from Aspergillus parasiticus, which has half-life of 1.10 h at 37°C, was stabilized by immobilization on calcium alginate beads. The immobilized CD had pH and temperature optimum of 5 and 50°C respectively. The immobilized enzyme also stoichiometrically deaminated Cytosine and 5-fluorocytosine ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Zanna H,Nok AJ,Ibrahim S,Inuwa HM

更新日期：2013-12-01 00:00:00

abstract：:Structural modifications around 8-HETE (8-hydroxyeicosatetraenoic acid), a natural agonist of the PPAR (peroxisome proliferator-activated receptor) nuclear receptors have led previously to the identification of a promising analog, the quinoline S 70655. Series of novel quinoline or benzoquinoline derivatives were desi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Liutkus M,Caijo F,Girard AL,Ayral E,Audinot V,Boutin JA,Renard P,Caignard DH,Dacquet C,Ktorza A,Mosset P,Grée R

更新日期：2010-10-01 00:00:00

abstract：:In this study, firstly, antioxidant and polyphenol oxidase (PPO) properties of Yomra apple were investigated. Seventeen phenolic constituents were measured by reverse phase-high-performance liquid chromatography (RP-HPLC). Total phenolic compounds (TPCs), ferric reducing antioxidant power (FRAP) and 2, 2-diphenyl-1-pi...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Can Z,Dincer B,Sahin H,Baltas N,Yildiz O,Kolayli S

更新日期：2014-12-01 00:00:00

abstract：:A recombinant carbonic anhydrase (CA, EC 4.2.1.1) from the soil-dwelling bacterium Enterobacter sp. B13 was cloned and purified by Co(2+) affinity chromatography. Bioinformatic analysis showed that the new enzyme (denominated here B13-CA) belongs to the β-class CAs and to possess 95% homology with the ortholog enzyme ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Eminoğlu A,Vullo D,Aşık A,Çolak DN,Supuran CT,Çanakçı S,Osman Beldüz A

更新日期：2016-12-01 00:00:00

abstract：:Photodynamic molecules represent an alternative approach for cancer therapy for their property (i) to be photo-reactive; (ii) to be not-toxic for target cells in absence of light; (iii) to accumulate specifically into tumour tissues; (iv) to be activable by a light beam only at the tumour site and (v) to exert cytotox...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kusuzaki K,Matsubara T,Murata H,Logozzi M,Iessi E,Di Raimo R,Carta F,Supuran CT,Fais S

更新日期：2017-12-01 00:00:00

abstract：:Serum paraoxonase (PON1) is a high-density lipoprotein (HDL)-associated enzyme that protects lipoproteins, both low-density lipoprotein (LDL) and HDL, against oxidation, and is considered as an antioxidative/anti-inflammatory component of HDL. In this study, PON1 was purified from bovine serum by ammonium sulfate prec...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sayın M,Guler OO

更新日期：2015-02-01 00:00:00

abstract：:Novel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 µg/mL for all com...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Özdemir Z,Utku S,Mathew B,Carradori S,Orlando G,Di Simone S,Alagöz MA,Özçelik AB,Uysal M,Ferrante C

更新日期：2020-12-01 00:00:00

abstract：:Carbonic anhydrases (CAs) are widespread metalloenzymes in higher vertebrates including humans. A series of phenolic compounds, including guaiacol, 4-methylguaiacol, 4-propylguaiacol, eugenol, isoeugenol, vanillin, syringaldehyde, catechol, 3-methyl catechol, 4-methyl catechol and 3-methoxy catechol were investigated ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Scozzafava A,Passaponti M,Supuran CT,Gülçin İ

更新日期：2015-01-01 00:00:00

abstract：:Inflammatory bowel disease (IBD) is a chronic immuno-inflammation in gastrointestinal tract. We have evaluated the activity of the compounds to inhibit the adhesion of monocytes to colon epithelial cells is triggered by a pro-inflammatory cytokine, tumour necrosis factor (TNF)-α. The in vitro activity of the compounds...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Chaudhary CL,Gurung P,Jang S,Banskota S,Nam TG,Kim JA,Jeong BS

更新日期：2020-12-01 00:00:00

abstract：:The benzimidazole derivative Schiff bases and their copper(II) (Cu(II)) mixed-polypyridyl complexes (1-4) have been synthesized and characterized by the spectral and analytical techniques. DNA binding/cleavage studies indicate a stronger binding capability for the complex 4 which is confirmed by the absorbance, viscom...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Raman N,Selvan A

更新日期：2012-06-01 00:00:00

abstract：:Di(2-ethylhexyl) phthalate (DEHP) is the most widely plasticizer for polyvinyl chloride (PVC) that is used in plastic tubes, in medical and paramedical devices as well as in food storage packaging. The toxicological profile of DEHP has been evaluated in a number of experimental animal models and has been extensively d...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Kambia N,Renault N,Dilly S,Farce A,Dine T,Gressier B,Luyckx M,Brunet C,Chavatte P

更新日期：2008-10-01 00:00:00

abstract：:The synthesis of 1,2-dioxolane derivatives in two different acetophenone series, as simplified models of natural coumarins is described. 2-Acetyl-3-acetoxy-4-(3-hydroperoxy-3-methylbut-1-enyl)phenyl acetate and 2-acetyl-5-acetoxy4-(3-hydroperoxy-3-methylbut-1-enyl) phenyl acetate synthons are used as precursors to the...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Helesbeux JJ,Peyronnet D,Labaïed M,Grellier P,Frappier F,Seraphin D,Richomme P,Duval O

更新日期：2002-12-01 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：:Berberine was investigated as an inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B) in an attempt to explain its anti-hyperglycemic activitiy. The investigation included simulated docking experiments to fit berberine within the binding pocket of h-PTP 1B. Berberine was found to readily fit within the bindin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Bustanji Y,Taha MO,Yousef AM,Al-Bakri AG

更新日期：2006-04-01 00:00:00

abstract：:A series of eighteen pyrrolo[3,2-c]pyridine derivatives were tested for inhibitory effect against FMS kinase. Compounds 1e and 1r were the most potent among all the other tested analogues (IC50 = 60 nM and 30 nM, respectively). They were 1.6 and 3.2 times, respectively, more potent than our lead compound, KIST101029 (...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： El-Gamal MI,Oh CH

更新日期：2018-12-01 00:00:00

abstract：:In this study, di(2,6-dimethylphenol) (Di-DMP), di(2,6-diisopropylphenol) (Di-DIP, dipropofol) and di(2,6-di-t-butylphenol) (Di-DTP) were synthesized by the reaction of monomeric phenol derivatives with catalytic CuCl(OH). TMEDA and Na2S2O4. Their antioxidant capacity and radical scavenging activity were examined usin...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Güllçin I,Daştan A

更新日期：2007-12-01 00:00:00

abstract：:In a new group of 3-methyl-2-phenyl-1-substituted-indole derivatives (10a-f), the indomethacin analogs were prepared via the Fisher indole synthesis reaction of propiophenone with appropriately substituted phenylhydrazine hydrochloride. This is followed by the insertion of the appropriate benzyl or benzoyl fragment. A...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abdellatif KR,Lamie PF,Omar HA

更新日期：2016-01-01 00:00:00

abstract：:Two fractions of rat intestinal alkaline phosphatase (IAP) were detected by Western blot: 168 +/- 6 and 475 +/- 45 kDa. The low molecular weight fraction constitutes 43% of the isolated proteins exhibiting 82% of the enzymatic activity, and a heavier fraction constitutes 57% of the isolated proteins and has 18% of the...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Brun LR,Brance ML,Rigalli A,Puche RC

更新日期：2006-12-01 00:00:00