Displaying publications 61 - 80 of 374 in total

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  1. Chan YY, Kim KH, Cheah SH
    J Ethnopharmacol, 2011 Oct 11;137(3):1183-8.
    PMID: 21810462 DOI: 10.1016/j.jep.2011.07.050
    ETHNOPHARMACOLOGICAL RELEVANCE: Sargassum polycystum, a type of brown seaweed, has been used for the treatment of skin-related disorders in traditional medicine.

    AIM OF THE STUDY: The aim of the present study is to investigate the antimelanogenesis effect of Sargassum polycystum extracts by cell-free mushroom tyrosinase assay followed by cell viability assay, cellular tyrosinase assay and melanin content assay using B16F10 murine melanoma cells.

    MATERIALS AND METHODS: Sargassum polycystum was extracted with 95% ethanol and further fractionated with hexane, ethyl acetate and water. The ethanolic crude extract and its fractionated extracts were tested for their potential to act as antimelanogenesis or skin-whitening agents by their abilities to inhibit tyrosinase activity in the cell-free mushroom tyrosinase assay and cellular tyrosinase derived from melanin-forming B16F10 murine melanoma cells. The tyrosinase inhibitory activity was correlated to the inhibition of melanin production in α-MSH-stimulated and unstimulated B16F10 cells.

    RESULTS: Sargassum polycystum ethanolic extract and its fractions had little or no inhibitory effect on mushroom tyrosinase activity. However, when tested on cellular tyrosinase, the ethanolic extract and its non-polar fraction, hexane fraction (SPHF), showed significant inhibition of cellular tyrosinase activity. In parallel to its cellular tyrosinase inhibitory activity, SPHF was also able to inhibit basal and α-MSH-stimulated melanin production in B16F10 cells.

    CONCLUSIONS: Our findings showed that (i) cellular tyrosinase assay is more reliable than mushroom tyrosinase assay in the initial testing of potential antimelanogenesis agents and, (ii) SPHF inhibited melanogenesis by inhibiting cellular tyrosinase activity. SPHF may be useful for treating hyperpigmentation and as a skin-whitening agent in cosmetics industry.

    Matched MeSH terms: Enzyme Inhibitors/isolation & purification; Enzyme Inhibitors/pharmacology*
  2. Chandran G, Sirajudeen KN, Yusoff NS, Swamy M, Samarendra MS
    Oxid Med Cell Longev, 2014;2014:608512.
    PMID: 25254079 DOI: 10.1155/2014/608512
    Oxidative stress has been suggested to play a role in hypertension and hypertension induced organ damage. This study examined the effect of enalapril, an antihypertensive drug, on oxidative stress markers and antioxidant enzymes in kidney of spontaneously hypertensive rat (SHR) and Nω -nitro-L-arginine methyl ester (L-NAME) administered SHR. Male rats were divided into four groups (SHR, SHR+enalapril, SHR+L-NAME, and SHR+enalapril+L-NAME). Enalapril (30 mg kg(-1) day(-1)) was administered from week 4 to week 28 and L-NAME (25 mg kg(-1) day(-1)) was administered from week 16 to week 28 in drinking water. Systolic blood pressure (SBP) was measured during the experimental period. At the end of experimental periods, rats were sacrificed; urine, blood, and kidneys were collected for the assessment of creatinine clearance, total protein, total antioxidant status (TAS), thiobarbituric acid reactive substances (TBARS), superoxide dismutase (SOD), and catalase (CAT), as well as histopathological examination. Enalapril treatment significantly enhanced the renal TAS level (P < 0.001) and SOD activity (P < 0.001), reduced the TBARS levels (P < 0.001), and also prevented the renal dysfunction and histopathological changes. The results indicate that, besides its hypotensive and renoprotective effects, enalapril treatment also diminishes oxidative stress in the kidneys of both the SHR and SHR+L-NAME groups.
    Matched MeSH terms: Enzyme Inhibitors/pharmacology
  3. Chatsumpun N, Sritularak B, Likhitwitayawuid K
    Molecules, 2017 Oct 30;22(11).
    PMID: 29084164 DOI: 10.3390/molecules22111862
    Roots of Boesenbergia rotunda (L.) Mansf. are prominent ingredients in the cuisine of several Asian countries, including Thailand, Malaysia, Indonesia, India, and China. An extract prepared from the roots of this plant showed strong inhibitory activity against enzymes α-glucosidase and pancreatic lipase and was subjected to chromatographic separation to identify the active components. Three new biflavonoids of the flavanone-chalcone type (9, 12, and 13) were isolated, along with 12 known compounds. Among the 15 isolates, the three new compounds showed stronger inhibitory activity against α-glucosidase than the drug acarbose but displayed lower pancreatic lipase inhibitory effect than the drug orlistat. The results indicated the potential of B. rotunda roots as a functional food for controlling after-meal blood glucose levels.
    Matched MeSH terms: Enzyme Inhibitors/pharmacology*; Enzyme Inhibitors/chemistry
  4. Chay SY, Salleh A, Sulaiman NF, Zainal Abidin N, Hanafi MA, Zarei M, et al.
    Food Funct, 2018 Mar 01;9(3):1657-1671.
    PMID: 29469915 DOI: 10.1039/c7fo01769c
    Winged bean seed (WBS) is an underutilized tropical crop. The current study evaluates its potential to reduce blood pressure (BP) in spontaneously hypertensive rats and finds that it reduces BP significantly, in a dose-dependent manner. Five peptides with the sequences, RGVFPCLK, TQLDLPTQ, EPALVP, MRSVVT and DMKP, have been characterized in terms of their stability against ACE via in vitro and in silico modelling. All peptides exhibited IC50 values between 0.019 and 6.885 mM and various inhibitory modes, including substrate, prodrug and true inhibitor modes. The toxicity status of non-Current Good Manufacturing Practice (non-CGMP) peptides is evaluated and the results show that such peptides are toxic, and thus are not suitable to be tested in animals, particularly in repeated-dose studies. In short, WBS hydrolysate demonstrated in vitro ACE inhibitory properties and in vivo blood pressure lowering efficacy in rat models, fostering its potential as a functional food ingredient. Non-CGMP grade peptides are toxic and unfit for testing in animal models.
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/administration & dosage; Angiotensin-Converting Enzyme Inhibitors/adverse effects; Angiotensin-Converting Enzyme Inhibitors/chemistry
  5. Cheah HL, Lim V, Sandai D
    PLoS One, 2014;9(4):e95951.
    PMID: 24781056 DOI: 10.1371/journal.pone.0095951
    Candida albicans is an opportunistic pathogen that causes candidiasis in humans. In recent years, metabolic pathways in C. albicans have been explored as potential antifungal targets to treat candidiasis. The glyoxylate cycle, which enables C. albicans to survive in nutrient-limited host niches and its. Key enzymes (e.g., isocitrate lyase (ICL1), are particularly attractive antifungal targets for C. albicans. In this study, we used a new screening approach that better reflects the physiological environment that C. albicans cells experience during infection to identify potential inhibitors of ICL. Three compounds (caffeic acid (CAFF), rosmarinic acid (ROS), and apigenin (API)) were found to have antifungal activity against C. albicans when tested under glucose-depleted conditions. We further confirmed the inhibitory potential of these compounds against ICL using the ICL enzyme assay. Lastly, we assessed the bioavailability and toxicity of these compounds using Lipinski's rule-of-five and ADMET analysis.
    Matched MeSH terms: Enzyme Inhibitors/pharmacology*
  6. Chee KH, Amudha K, Hussain NA, Haizal HK, Choy AM, Lang CC
    PMID: 14608517
    Conventional diuretic agents are very effective agents in relieving volume overload and congestive symptoms in chronic heart failure (CHF). However, they are associated with activation of the renin-angiotensin system (RAS) and the sympathetic nervous system and a reduction in glomerular filtration rate, all of which have been associated with adverse outcomes in CHF. Therefore, there is an increasing interest in drugs that target the natriuretic system without neurohormonal activation and deterioration of renal function. In this review, we will discuss the underlying rationale and evidence behind currently pursued strategies that target the natriuretic system. This includes the administration of natriuretic peptides (NPs) and strategies that potentiate the NP system, such as neutral endopeptidase inhibition. We will also highlight some potentially important interactions of these strategies with drugs that target the RAS.
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/therapeutic use*
  7. Chia TY, Murugaiyah V, Khan NA, Sattar MA, Abdulla MH, Johns EJ, et al.
    Physiol Res, 2021 03 17;70(1):13-26.
    PMID: 33728924
    Reactive oxygen species (ROS) such as superoxide (O2-) generated by NAD(P)H oxidases have emerged as important molecules in blood pressure regulation. This study investigated the effect of apocynin and catalase on blood pressure and renal haemodynamic and excretory function in an L-NAME induced hypertension model. Forty Male Wistar-Kyoto (WKY) rats (n=8 per group) were treated with either: vehicle (WKY-C); L-NAME (WKY-L, 15 mg/kg/day in drinking fluid); WKY-L given apocynin to block NAD(P)H oxidase (WKY-LApo, 73 mg/kg/day in drinking water.); WKY-L given catalase to enhance ROS scavenging (WKY-LCat, 10000 U/kg/day i.p.); and WKY-L receiving apocynin plus catalase (WKY-LApoCat) daily for 14 days. L-NAME elevated systolic blood pressure (SBP), 116+/-1 to 181±4 mmHg, reduced creatinine clearance, 1.69+/-0.26 to 0.97+/-0.05 ml/min/kg and fractional sodium excretion, 0.84+/-0.09 to 0.55+/-0.09 % at day 14. Concomitantly, plasma malondialdehyde (MDA) increased six fold, while plasma total superoxide dismutase (T-SOD), plasma nitric oxide (NO) and plasma total antioxidant capacity (T-AOC) were decreased by 60-70 % and Nox 4 mRNA expression was increased 2-fold. Treatment with apocynin and catalase attenuated the increase in SBP and improved renal function, enhanced antioxidative stress capacity and reduced the magnitude of Nox4 mRNAs expression in the L-NAME treated rats. This study demonstrated that apocynin and catalase offset the development of L-NAME induced hypertension, renal dysfunction and reduced oxidative stress status, possibly contributed by a reduction in Nox4 expression during NOS inhibition. These findings would suggest that antioxidant compounds such as apocynin and catalase have potential in treating cardiovascular diseases.
    Matched MeSH terms: Enzyme Inhibitors/toxicity
  8. Chia YC, Ching SM
    BMC Fam Pract, 2014;15:131.
    PMID: 24997591 DOI: 10.1186/1471-2296-15-131
    Patients with resistant hypertension are subjected to a higher risk of getting stroke, myocardial infarction, congestive heart failure and renal failure. However, the exact prevalence of resistant hypertension in treated hypertensive patients in Malaysia is not known. This paper examines the prevalence and determinants of resistant hypertension in a sample of hypertensive patients.

    Study site: Primary care clinic, Universiti Malaya Medical Centre
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/therapeutic use
  9. Chin LC, Achike FI, Mustafa MR
    Vascul. Pharmacol., 2007 Mar;46(3):223-8.
    PMID: 17126611 DOI: 10.1016/j.vph.2006.10.005
    Hydrogen peroxide (H(2)O(2)) contributes in the regulation of vascular tone, especially in pathological states. The role of H(2)O(2) and superoxide anion free radicals in angiotensin II (Ang II)-induced contraction of diabetic tissues was examined with the aim of elucidating the underlying mechanisms. Isometric tension in response to various drug treatments was measured in isolated superior mesenteric arteries of streptozotocin (STZ)-induced diabetic WKY rats using the Mulvany wire myograph. Compared to the normal (euglycaemic) arteries, the Ang II-induced contraction was significantly reduced in diabetic arteries. Superoxide dismutase (SOD; converts superoxide to H(2)O(2)) significantly reduced the contraction in both types of arteries -- an effect abolished by catalase (H(2)O(2) scavenger), suggesting that the SOD effect was mediated by H(2)O(2). Treatment with catalase had no effect on the Ang II contraction in euglycaemic arteries, but it raised the contraction in diabetic arteries to euglycaemic levels. This increase was similar to that observed with diabetic arteries incubated with L-NAME. Combined catalase and L-NAME treatment further enhanced the contraction in diabetic arteries, suggesting that the catalase effect was not mediated by nitric oxide (NO). The catalase effect was abolished by indomethacin treatment. These results suggest that attenuation of Ang II-induced contraction in diabetic tissues is modulated by endogenous H(2)O(2), the scavenging of which unmasks an indomethacin-sensitive (and therefore cyclooxygenase product-mediated) Ang II-induced contraction.
    Matched MeSH terms: Enzyme Inhibitors/pharmacology
  10. Chin SP, Sapari S, How SH, Sim KH
    Med J Malaysia, 2006 Aug;61(3):278-83.
    PMID: 17240575 MyJurnal
    Evidence-based heart failure management now includes beta-blockers and spironolactone in addition to diuretics and angiotensin-converting enzyme inhibitors. We aim to determine if these recommendations had been applied in practice for acute and chronic stable heart failure, and what difficulties there might be. Data from 80 consecutive patients hospitalized for decompensated heart failure ('acute') between May and July 2003 were analyzed at admission, upon discharge and at 12 weeks follow-up; along with 74 cardiology clinic out-patients with stable congestive heart failure ('chronic'- no decompensation or admission in previous six months). Less than half of study patients with prior left ventricular dysfunction were on ACE-inhibitors (47%), diuretics (39%), ATII antagonists, spironolactone or digoxin (5% each). All 'acute' patients were commenced on diuretics and ACE-inhibitors in hospital. Six patients died or transferred to another center. Compliance with clinic appointment at 12 weeks was 85% despite telephone reminders. Drug prescription at 12 weeks was significantly lower for diuretics and ACE-inhibitors compared to prescription at discharge (all p < 0.05) but higher compared to patients with chronic HF. Diuretics and ACE inhibitors remain under-utilized for patients with recurrent heart failure. Use of spironolactone and beta-blocker is slow due to limited medical experience and funding. Clinic non-attendance is significant and due to patient factors.
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/therapeutic use
  11. Choi WC, Parr T, Lim YS
    J Food Sci Technol, 2019 Jan;56(1):281-289.
    PMID: 30728570 DOI: 10.1007/s13197-018-3488-0
    The global trend in increasing plant-based protein diets due to health and ideological reasons, has created an increased demand for food legumes that exceeds current production. To meet this demand, it is timely to reduce relying solely on soybean, and explore the potential of the underutilised legumes that are cultivated regionally. Underutilised legumes are rich in protein, carbohydrates and other nutrients that are essential for consumer. However, relatively little is known about their anti-nutritional properties and processing methods. Anti-nutritional factors (ANFs) such as enzyme inhibitors are prevalent in legumes and may interfere with digestibility and nutrient absorption. Nevertheless, an optimised food processing method will overcome this challenge and warrant a safe inclusion of legume in plant-based protein diets. Hence current study aimed to optimise the food processing methods (soaking, wet heating, autoclaving and freezing) and evaluate their efficiency in eliminating the enzyme inhibitors [trypsin, chymotrypsin (CIA) and α-amylase (AIA) inhibitors] present in seven underutilised legumes. Current study showed that autoclaving at 121 °C for 15 min reduced the AIA in all underutilised legumes tested. The AIA and CIA of bambara groundnut were successfully inactivated by wet heating at 50 °C for 60 min, and by autoclaving at 121 °C for 15 min. While the CIA of chickpea was successfully inactivated by freezing at - 80 °C for 24 h.
    Matched MeSH terms: Enzyme Inhibitors
  12. Chong AY, Rajaratnam R, Hussein NR, Lip GY
    Eur J Heart Fail, 2003 Aug;5(4):569-74.
    PMID: 12921820
    BACKGROUND: There are established differences in cardiovascular disease in different racial groups. Worldwide, the literature regarding the clinical epidemiology of congestive heart failure (CHF) in non-white populations is scarce.

    OBJECTIVES: To document the prevalence of CHF in the multiracial population of Malaysia, and to describe the clinical features and management of these patients.

    SETTING: Busy city centre general hospital in Kuala Lumpur, Malaysia.

    RESULTS: Of 1435 acute medical admissions to Kuala Lumpur General Hospital over the 4-week study period, 97 patients (6.7%) were admitted with the primary diagnosis of CHF. Coronary artery disease was the main aetiology of CHF, accounting for almost half (49.5%) the patients, followed by hypertension (18.6%). However, there were variations in associated aetiological factors between ethnic groups, with diabetes mellitus affecting the majority of Indians-as well as underutilisation of standard drugs for CHF, such as the angiotensin converting enzyme (ACE) inhibitors, which were only used in 43.3%.

    CONCLUSION: Amongst acute medical admissions to a single centre in Malaysia the prevalence of CHF was 6.7%. Coronary artery disease was the major aetiological factor in heart failure accounting for almost half the admissions. The under-prescription of ACE inhibitors was similar to other clinical surveys carried out amongst Caucasian populations in the West.

    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/therapeutic use
  13. Choo CY, Sulong NY, Man F, Wong TW
    J Ethnopharmacol, 2012 Aug 1;142(3):776-81.
    PMID: 22683902 DOI: 10.1016/j.jep.2012.05.062
    The leaves of Ficus deltoidea are used as a traditional medicine by diabetes patients in Malaysia.
    Matched MeSH terms: Enzyme Inhibitors/analysis; Enzyme Inhibitors/therapeutic use
  14. Choy YW, Cheong I
    Family Physician, 1989;1:19-22.
    This study was carried out on 30 patients to: i) determine the efficacy of low dose captopril as monotherapy (with or without a diuretic) in the treatment of various grades of hypertension. ii) assess the quality of life of these patients 12 weeks after commencement of therapy. Our results showed that there was a sustained and significant fall in both mean systolic and diastolic blood pressure from 171.9 ± 24 to 150.5 ± 25 mm Hg and 109.0 ± 14 to 93.6 ± 15mmHg respectively (p<0.001). Improvement in quality of life was however not statistically significant (p<0.05). We concluded that low dose captopril used alone or in combination with a diuretic can be considered for the initial therapy of mild to moderate hypertension. The optimal dosage and the longterm benefits on quality of life need further evaluation in a larger series.
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors
  15. Dehghan M, Mente A, Rangarajan S, Mohan V, Lear S, Swaminathan S, et al.
    Am J Clin Nutr, 2020 04 01;111(4):795-803.
    PMID: 31965140 DOI: 10.1093/ajcn/nqz348
    BACKGROUND: Eggs are a rich source of essential nutrients, but they are also a source of dietary cholesterol. Therefore, some guidelines recommend limiting egg consumption. However, there is contradictory evidence on the impact of eggs on diseases, largely based on studies conducted in high-income countries.

    OBJECTIVES: Our aim was to assess the association of egg consumption with blood lipids, cardiovascular disease (CVD), and mortality in large global studies involving populations from low-, middle-, and high-income countries.

    METHODS: We studied 146,011 individuals from 21 countries in the Prospective Urban Rural Epidemiology (PURE) study. Egg consumption was recorded using country-specific validated FFQs. We also studied 31,544 patients with vascular disease in 2 multinational prospective studies: ONTARGET (Ongoing Telmisartan Alone and in Combination with Ramipril Global End Point Trial) and TRANSCEND (Telmisartan Randomized Assessment Study in ACEI Intolerant Subjects with Cardiovascular Disease). We calculated HRs using multivariable Cox frailty models with random intercepts to account for clustering by study center separately within each study.

    RESULTS: In the PURE study, we recorded 14,700 composite events (8932 deaths and 8477 CVD events). In the PURE study, after excluding those with history of CVD, higher intake of egg (≥7 egg/wk compared with <1 egg/wk intake) was not significantly associated with blood lipids, composite outcome (HR: 0.96; 95% CI: 0.89, 1.04; P-trend = 0.74), total mortality (HR: 1.04; 95% CI: 0.94, 1.15; P-trend = 0.38), or major CVD (HR: 0.92; 95% CI: 0.83, 1.01; P-trend = 0.20). Similar results were observed in ONTARGET/TRANSCEND studies for composite outcome (HR 0.97; 95% CI: 0.76, 1.25; P-trend = 0.09), total mortality (HR: 0.88; 95% CI: 0.62, 1.24; P-trend = 0.55), and major CVD (HR: 0.97; 95% CI: 0.73, 1.29; P-trend = 0.12).

    CONCLUSIONS: In 3 large international prospective studies including ∼177,000 individuals, 12,701 deaths, and 13,658 CVD events from 50 countries in 6 continents, we did not find significant associations between egg intake and blood lipids, mortality, or major CVD events. The ONTARGET and TRANSCEND trials were registered at clinicaltrials.gov as NCT00153101. The PURE trial was registered at clinicaltrials.gov as NCT03225586.

    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/administration & dosage
  16. Dige NC, Mahajan PG, Raza H, Hassan M, Vanjare BD, Hong H, et al.
    Bioorg Chem, 2019 11;92:103201.
    PMID: 31445195 DOI: 10.1016/j.bioorg.2019.103201
    We have carried out the synthesis of new 4-oxoquinazolin-3(4H)-yl)furan-2-carboxamide derivatives by the reaction between isatoic anhydride, 2-furoic hydrazide and substituted salicylaldehydes in ethanol: water (5:5 v/v) solvent system using p-TSA as a catalyst under ultrasound irradiation at room temperature. The structures of newly synthesized compounds were confirmed through spectral techniques such as IR, 1H NMR, 13C NMR, and LCMS. The important features of this protocol include simple and easy workup procedure, reaction carried out at ambient temperature, use of ultrasound and high yield of oxoquinazolin-3(4H)-yl)furan-2-carboxamides in short reaction time. The synthesized compounds 4a-4j were screened against tyrosinase enzyme and all these compounds found to be potent inhibitors with much lower IC50 value of 0.028 ± 0.016 to 1.775 ± 0.947 µM than the standard kojic acid (16.832 ± 1.162 µM). The kinetics mechanism for compound 4e was analyzed by Lineweaver-Burk plots which revealed that compound inhibited tyrosinase non-competitively by forming an enzyme-inhibitor complex. Along with this all the synthesized compounds (4a-4j) were scanned for their DPPH free radical scavenging ability. The outputs received through in vitro and in silico analysis are coherent to the each other with good binding energy values (kcal/mol) posed by synthesized ligands.
    Matched MeSH terms: Enzyme Inhibitors/chemical synthesis*; Enzyme Inhibitors/metabolism
  17. Dige NC, Mahajan PG, Raza H, Hassan M, Vanjare BD, Hong H, et al.
    Bioorg Chem, 2020 07;100:103906.
    PMID: 32422387 DOI: 10.1016/j.bioorg.2020.103906
    A new series of 4H-chromene-3-carboxylate derivatives were synthesized using multicomponent reaction of salicylaldehyde, ethyl acetoacetate and dimedone in ethanol with K3PO4 as a catalyst at 80 °C. The structures of all newly synthesized compounds were confirmed by spectral techniques viz. IR, 1H NMR, 13C NMR, and LCMS analysis. The newly synthesized compounds 4a to 4j were screened against elastase enzyme. Interestingly, all these compounds found to be potent elastase inhibitors with much lower IC50 value. The compound 4b was found to be most potent elastase inhibitor (IC50 = 0.41 ± 0.01 µM) amongst the synthesized series against standard Oleanolic Acid (IC50 value = 13.45 ± 0.0 µM). The Kinetics mechanism for compound 4b was analyzed by Lineweaver-Burk plots which revealed that compound inhibited elastase competitively by forming an enzyme-inhibitor complex. Along with this, all the synthesized compounds (4a - 4j) exhibits excellent DPPH free radical scavenging ability. The inhibition constant Ki for compound 4b was found to be 0.6 µM. The computational study was comprehensible with the experimental results with good docking energy values (Kcal/mol). Therefore, these molecules can be considered as promising medicinal scaffolds for the treatment of skin-related maladies.
    Matched MeSH terms: Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/pharmacology*; Enzyme Inhibitors/chemistry*
  18. Ebrahimpour A, Rahman RN, Basri M, Salleh AB
    Bioresour Technol, 2011 Jul;102(13):6972-81.
    PMID: 21531550 DOI: 10.1016/j.biortech.2011.03.083
    The mature ARM lipase gene was cloned into the pTrcHis expression vector and over-expressed in Escherichia coli TOP10 host. The optimum lipase expression was obtained after 18 h post induction incubation with 1.0mM IPTG, where the lipase activity was approximately 1623-fold higher than wild type. A rapid, high efficient, one-step purification of the His-tagged recombinant lipase was achieved using immobilized metal affinity chromatography with 63.2% recovery and purification factor of 14.6. The purified lipase was characterized as a high active (7092 U mg(-1)), serine-hydrolase, thermostable, organic solvent tolerant, 1,3-specific lipase with a molecular weight of about 44 kDa. The enzyme was a monomer with disulfide bond(s) in its structure, but was not a metalloenzyme. ARM lipase was active in a broad range of temperature and pH with optimum lipolytic activity at pH 8.0 and 65°C. The enzyme retained 50% residual activity at pH 6.0-7.0, 50°C for more than 150 min.
    Matched MeSH terms: Enzyme Inhibitors/pharmacology
  19. Ee YS, Sow AJ, Goh BS
    J Laryngol Otol, 2010 Dec;124(12):1337-9.
    PMID: 20529395 DOI: 10.1017/S002221511000143X
    We report a case of an elderly man receiving treatment with perindopril, who presented with angioedema of the left side of the tongue, floor of the mouth and upper neck. This affected his speech and swallowing, and occurred one day after a burr hole and evacuation procedure undertaken to treat a subdural haematoma. The patient was kept under close observation and treated with intravenous hydrocortisone. The angioedema resolved completely in two days. This is the third reported case of unilateral tongue angioedema occurring secondary to angiotensin-converting enzyme inhibitor use.
    Matched MeSH terms: Angiotensin-Converting Enzyme Inhibitors/adverse effects*
  20. El-Sayed NNE, Almaneai NM, Ben Bacha A, Al-Obeed O, Ahmad R, Abdulla M, et al.
    J Enzyme Inhib Med Chem, 2019 Dec;34(1):672-683.
    PMID: 30821525 DOI: 10.1080/14756366.2019.1574780
    Some new 3H-quinazolin-4-one derivatives were synthesised and screened for anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities. Compound 15d was more potent in reducing the cell viabilities of HT-29 and SW620 cells lines to 38%, 36.7%, compared to 5-FU which demonstrated cell viabilities of 65.9 and 42.7% respectively. The IC50 values of 15d were ∼20 µg/ml. Assessment of apoptotic activity revealed that 15d decreased the cell viability by down regulating Bcl2 and BclxL. Moreover, compounds, 8j, 8d/15a/15e, 5b, and 8f displayed lowered IC50 values than oleanolic acid against proinflammatory isoforms of hGV, hG-X, NmPLA2, and AmPLA2. In addition, 8d, 8h, 8j, 15a, 15b, 15e, and 15f showed better anti-α-amylase than quercetin, whereas 8g, 8h, and 8i showed higher anti-α-glucosidase activity than allopurinol. Thus, these compounds can be considered as potential antidiabetic agents. Finally, none of the compounds showed higher antiproteases or xanthine oxidase activities than the used reference drugs.
    Matched MeSH terms: Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/pharmacology*; Enzyme Inhibitors/chemistry
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