Strong inhibitory activities and action modes of lipopeptides on lipase.

abstract：:Cyanidin-3-galactoside, a natural anthocyanin, was investigated for its alpha-glucosidase inhibitory activity. The IC(50) value of cyanidin-3-galactoside was 0.50 +/- 0.05 mM against intestinal sucrase. A low dose of cyanidin-3-galactoside showed a synergistic inhibition on intestinal alpha-glucosidase (maltase and su...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Adisakwattana S,Charoenlertkul P,Yibchok-Anun S

更新日期：2009-02-01 00:00:00

abstract：:Numerous studies have highlighted the implications of the glycogen synthase kinase 3 (GSK-3) in several processes associated with Alzheimer's disease (AD). Therefore, GSK-3 has become a crucial therapeutic target for the treatment of this neurodegenerative disorder. Hereby, we report the design and multistep synthesis...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sciú ML,Sebastián-Pérez V,Martinez-Gonzalez L,Benitez R,Perez DI,Pérez C,Campillo NE,Martinez A,Moyano EL

更新日期：2019-12-01 00:00:00

abstract：:Usually, all newborns demonstrate high serum unconjugated bilirubin (UCB) level. UCB may induce adverse effects in the central nervous system. We aimed to evaluate the cytotoxic effects of UCB and the protective effects of docosahexaenoic acid (DHA) on astrocyte cell cultures. The viability of astrocyte cells decrease...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Becerir C,Kılıç İ,Sahin Ö,Özdemir Ö,Tokgün O,Özdemir B,Akca H

更新日期：2013-08-01 00:00:00

abstract：:Selective PDE3 inhibitors improve cardiac contractility and may be used in congestive heart failure. However, their proarrhythmic potential is the most important side effect. In this research we designed, synthesized and evaluated the potential cardiotonic activity of thirteen PDE3 inhibitors (4-[(4-methyl-2-oxo-1,2-d...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sadeghian H,Seyedi SM,Saberi MR,Nick RS,Hosseini A,Bakavoli M,Mansouri SM,Parsaee H

更新日期：2009-08-01 00:00:00

abstract：:Histamine H3 receptors (H3R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H3R antagonists/inverse agonists have been designed and synthesised via hybriding the H3R pharmacophore (aliphatic amine with propyloxy chain) with the 1,2,4-triazol...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Song M,Yan R,Zhang Y,Guo D,Zhou N,Deng X

更新日期：2020-12-01 00:00:00

abstract：:The mechanism of inhalation anesthesia remains to be fully elucidated. While certain neuronal membrane proteins are considered sites of action, cytosolic proteins may also be targets. We hypothesize that inhaled anesthetics may act via glyceraldehyde 3-phosphate dehydrogenase (GAPDH), which has recently been shown to ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Swearengin TA,Fibuch EE,Seidler NW

更新日期：2006-10-01 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：:In this study, the synthesis and potential enzyme interactions of new Pyrrolo[2,3-d]pyrimidine derivatives along with their inhibitory activity against SFK enzymes such as Fyn, Lyn, Hck, and c-Src were reported. The results indicated that compounds were slightly active of tested SFK enzymes in comparison with PP2 for ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Dincer S,Cetin KT,Onay-Besikci A,Ölgen S

更新日期：2013-10-01 00:00:00

abstract：:Melatonin (MLT) is a well-known free-radical scavenger, involving in the prevention of cellular damage that can lead to cancer, ageing and a variety of neurodegenerative diseases. Research on MLT-related compounds has been required to optimise the maximum pharmaceutical activity with the lowest side effects. In our on...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Shirinzadeh H,Ince E,Westwell AD,Gurer-Orhan H,Suzen S

更新日期：2016-12-01 00:00:00

abstract：:In an in vitro screening for human carbonic anhydrase (hCA) inhibiting agents from higher plants, the petroleum ether and ethyl acetate extracts of Magydaris pastinacea seeds selectively inhibited hCA IX and hCA XII isoforms. The phytochemical investigation of the extracts led to the isolation of ten linear furocoumar...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fois B,Distinto S,Meleddu R,Deplano S,Maccioni E,Floris C,Rosa A,Nieddu M,Caboni P,Sissi C,Angeli A,Supuran CT,Cottiglia F

更新日期：2020-12-01 00:00:00

abstract：:Nineteen 5-nitrothiazolylthiosemicarbazones were synthesized from 5-nitrothiazole by three-step synthesis and evaluated for in vitro activities against seven mycobacterial species. Among them, N-(5-nitro-1, 3-thiazol-2-yl)-2-((Z)-4-[(phenylmethyl)oxy]phenylmethylidene)hydrazine-1-carbothioamide (4m) was found to be th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Sriram D,Yogeeswari P,Senthilkumar P,Sangaraju D

更新日期：2010-02-01 00:00:00

abstract：:Melatonin (N-acetyl-5-methoxytryptamine) is the chief secretory product of the pineal gland and synthesized enzymatically from serotonin (5-hydroxytryptamine). These indoleamine derivatives play an important role in the prevention of oxidative damage. In the present study, DMPD radical scavenging and cupric ion (Cu(2+...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Gulçin I

更新日期：2008-12-01 00:00:00

abstract：:Synthesis and pharmacological evaluation of various 2-(4-isobutylphenyl)propanoic acid derivatives containing 1,3,4-thiadiazole and thiadiazolo[3,2-a][1,3,5]triazine-5-thione nucleus is reported here. The structures of new compounds are supported by IR, (1)H & (13)C NMR data. These compounds were tested in vivo for th...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Raval JP,Gandhi AN,Akhaja TN,Myangar KN,Patel NH

更新日期：2012-02-01 00:00:00

abstract：CONTEXT:Tumor acidity represents a major cause of chemoresistance. Proton pump inhibitors (PPIs) can neutralize tumor acidity, sensitizing cancer cells to chemotherapy. OBJECTIVE:To compare the anti-tumor efficacy of different PPIs in vitro and in vivo. MATERIALS AND METHODS:In vitro experiments PPIs anti-tumor effic...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Lugini L,Federici C,Borghi M,Azzarito T,Marino ML,Cesolini A,Spugnini EP,Fais S

更新日期：2016-08-01 00:00:00

abstract：:In the present study we have evaluated the antigenotoxic effects of Farnesol (FL) a 15-carbon isoprenoid alcohol against benzo (a) pyrene [B(a)P] (125 mg kg(- 1).b.wt oral) induced toxicity. B(a)P administration lead to significant induction in Cytochrome P450 (CYP) content and aryl hydrocarbon hydrolase (AHH) activit...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Jahangir T,Sultana S

更新日期：2008-12-01 00:00:00

abstract：:The two β-carbonic anhydrases (CAs, EC 4.2.1.1) recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 aromatic, heterocyclic, and aliphatic sulfonamides and one sulfamate, many of which are clinically used agents. CAS1 was ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Vullo D,Lehneck R,Pöggeler S,Supuran CT

更新日期：2018-12-01 00:00:00

abstract：:The aims of this study were to examine the antiproliferation of Humulus lupulus extracts on human hepatoma carcinoma (Hep3B) and human colon carcinoma (HT-29) cell lines along with enzyme inhibitory effects of the crude extracts. Potential cell cytotoxicity of six different H. lupulus extracts were assayed on various ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cömert Önder F,Ay M,Aydoğan Türkoğlu S,Tura Köçkar F,Çelik A

更新日期：2016-01-01 00:00:00

abstract：:Histidinol dehydrogenase (HDH, EC EC1.1.1.23) catalyses the final step in the biosynthesis of histidine and constitutes an attractive novel target for the development of new agents against the pathogenous, bacteria Brucella suis. A small library of new HDH inhibitors based on the L-histidinylphenylsulfonyl hydrazide s...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Abdo MR,Joseph P,Boigegrain RA,Montero JL,Köhler S,Winum JY

更新日期：2008-06-01 00:00:00

abstract：:The in vivo and in vitro antiandrogenic activity of four aromatic esters 10a-10d, one aliphatic ester 10e based on the pregna-4,16-diene-6, 20-dione structure and two aromatic 17c, 17d and two aliphatic valeroyloxy esters 17a, 17b based on the more saturated 4-pregnene-6,20-dione skeleton was examined. The biological ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Cabeza M,Heuze I,Sánchez M,Bratoeff E,Ramírez E,Rojas A,Orozco A,Mungía A,Agustín G,Cuatepotzo L,Gonzalez C,Palma S,Padilla D,Perez V,Jimenez G

更新日期：2005-08-01 00:00:00

abstract：:Fatty acid synthase (FAS) has been proposed to be a new drug target for the development of anticancer agents because of the significant difference in expression of FAS between normal and tumour cells. Since a n-hexane-soluble extract from Ginkgo biloba was demonstrated to inhibit FAS activity in our preliminary test, ...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Oh J,Hwang IH,Hong CE,Lyu SY,Na M

更新日期：2013-06-01 00:00:00

abstract：:This research investigates the synthesis and inhibitory potency of a series of novel dipeptidyl allyl sulfones as clan CA cysteine protease inhibitors. The structure of the inhibitors consists of a R(1)-Phe-R(2)-AS-Ph scaffold (AS = allyl sulfone). R(1) was varied with benzyloxycarbonyl, morpholinocarbonyl, or N-methy...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Fennell BD,Warren JM,Chung KK,Main HL,Arend AB,Tochowicz A,Götz MG

更新日期：2013-06-01 00:00:00

abstract：:Resveratrol is a natural polyphenol with plethora of biological activities. Resveratrol has previously shown to decrease DNA-methyltransferase (DNMT) enzymes expression and to reactivate silenced tumor suppressor genes. Currently, it seems that no resveratrol analogs have been developed as DNMT inhibitors. Recently, w...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Aldawsari FS,Aguayo-Ortiz R,Kapilashrami K,Yoo J,Luo M,Medina-Franco JL,Velázquez-Martínez CA

更新日期：2016-10-01 00:00:00

abstract：:Pyrogallol is found naturally in crops and fruits of many plants. It is also an active ingredient of many pharmaceuticals. For this reason, we employed different in vitro antioxidant assays such as cupric ion Cu(2+) reducing power, Fe(3+) reducing power, total antioxidant activity by ferric thiocyanate method, ABTS ra...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Ozturk Sarikaya SB

更新日期：2015-01-01 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：:Dithiocarbamates (DTC) are promising compounds with potential applications in antitumoral and glaucoma therapy. Our aim is to understand molecular features affecting DTC interaction with carbonic anhydrases (CAs), zinc-containing enzymes maintaining acid-base balance in blood and other tissues. To this end, we generat...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Avram S,Milac AL,Carta F,Supuran CT

更新日期：2013-04-01 00:00:00

abstract：:3,6-Diazaphenothiazines were obtained in cyclization of 3-amino-3'-nitro-2,4'-dipyridinyl sulfide and the reaction of sodium 3-amino-2-pyridinethiolate with 4-chloro-3-nitropyridine followed by alkylation and heteroarylation. The thiazine ring formation ran via the Smiles rearrangement. The structure elucidation was b...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Morak-Młodawska B,Pluta K,Latocha M,Suwińska K,Jeleń M,Kuśmierz D

更新日期：2016-12-01 00:00:00

abstract：:QSAR analysis of a series of previously synthesised 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols(TDFPP) as analogues of fluconazole were tested for growth inhibitory activity against Candida albicans using computer assisted multiple regression analysis. This was in order to explore the s...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Singla RK,Bhat G V

更新日期：2010-10-01 00:00:00

abstract：:In the present study, some thiazole derivatives were synthesized via the ring closure reaction of 1-[2-(2-oxobenzo[d]thiazol-3(2H)-yl)acetyl]thiosemicarbazide with various phenacyl bromides. The chemical structures of the compounds were elucidated by (1)H NMR, (13)C NMR and mass spectral data and elemental analyses. E...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Turan-Zitouni G,Ozdemir A,Kaplancikli ZA,Altintop MD,Temel HE,Çiftçi GA

更新日期：2013-06-01 00:00:00

abstract：:Poly(ADP-ribose) polymerase (PARP)-1 inhibitor has been suggested to attenuate the ischemia-reperfusion injury. We investigated the protective effect of the cardioplegia with a PARP-1 inhibitor, 4-hydoxyquinazoline (4-HQ), against myocardial ischemia-reperfusion injury. Isolated rat hearts were perfused on a Langendor...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Yamazaki K,Tanaka S,Sakata R,Miwa S,Oriyanhan W,Takaba K,Minakata K,Marui A,Ikeda T,Toyokuni S,Komeda M,Ueda K

更新日期：2013-02-01 00:00:00

abstract：:The tumor-associated transmembrane carbonic anhydrase (CA, EC 4.2.1.1) isozymes IX (CA IX) and XII (CA XII) are involved in acidification of hypoxic tumors, a process correlated with poor prognosis and clinical outcome of patients harboring such tumors. This process may be reversed by inhibiting these enzymes with pot...

journal_title：Journal of enzyme inhibition and medicinal chemistry

authors： Pastorekova S,Vullo D,Casini A,Scozzafava A,Pastorek J,Nishimori I,Supuran CT

更新日期：2005-06-01 00:00:00