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Objective: To compare the safety and efficacy of valsartan/sacubitril (angiotensin receptor neprilysin inhibitor [ARNI]) against enalapril (angiotensin-converting enzyme inhibitor [ACEI]) in patients with acute heart failure at 6-month follow-up. Methods: In this prospective, single centre, and observational study conducted between September 2017 and February 2020 in India, patients with acute decompensated heart failure with reduced ejection fraction (<40%) were included. Patients were divided in two groups: valsartan/sacubitril (ARNI) group and enalapril (ACEI). Patients were followed up for at least 6 months after administration of first dose and were evaluated for safety, efficacy, and tolerability of target drug. Student's independent t-test was employed for comparing continuous variables. Chi-square test or Fisher's exact test, whichever appropriate, was applied for comparing categorical variables. Results: A total of 200 patients were included in the present study, 100 each in ARNI and ACEI group. The mean age of the population was 61.2 ± 8.4 years and 62.6 ± 8.6 years in ARNI group and ACEI group, respectively. The mean maximum tolerated dose by population in ARNI group was 203.6 mg and 8.9 mg in ACEI group. Readmission for heart failure were seen significantly higher in ACEI group than ARNI group (p value ¼ 0.001). Parameters like ejection fraction, left ventricular end diastolic and systolic dimensions, 6 min walk test and Kansas City Cardiomyopathy Questionnaires (KCCQ) showed p values < 0.05 between the groups. Conclusion: The ARNI study group showed better safety and efficacy outcomes at the end of 6 months follow-up compared to ACEI group
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Objective To evaluate the effects of antihypertensive drugs on renal function after percutaneous transluminal coronary angioplasty. Methods A retrospective analysis was performed on 193 patients who underwent percutaneous transluminal coronary angioplasty and took antihypertensive drugs regularly. Those patients were admitted to Nanjing Drum Tower Hospital during January 2020 to December 2020. The patients were divided into ACEI/ARB group, β-blockers, calcium channel blockers and hydration control group. All patients received routine hydration during the perioperative period. The changes of serum creatinine (Scr), blood urea nitrogen (BUN), estimated glomerular filtration rate(eGFR) and endogenous creatinine clearance rate (Ccr) before and after operation were compared. Results The incidence of CIN was 0% in four groups. Compared with the preoperative, there was no significant change in Scr and Ccr in every group. Except for the hydration control group, the BUN levels in three treated groups were reduced after postoperative. Specifically, the BUN reduction in β-blockers group has statistically significant difference compared to the hydration control group and CCB group. In addition, eGFR levels were significantly reduced in the β-blockers group. Preoperative Scr and Ccr levels in patients with high blood pressure (SBP≥140 or DBP≥90) were significantly different from the patients with normal blood pressure (SBP<140 and DBP<90). Conclusion The use of ACEI/ARB and CCB before percutaneous transluminal coronary angioplasty had no effect on renal function in the short term. β-blockers can slightly reduce renal function, especially in patients with high blood pressure, who should receive special attention.
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Objective:We compared the clinical outcomes between β-blocker with angiotensin converting enzyme inhibitor (ACEI) or angiotensin receptor blocker (ARB) in patients with acute myocardial infarction (AMI) without left ventricular systolic dysfunction.Methods:A total of 750 patients who were diagnosed as AMI without left ventricular systolic dysfunction and successfully received percutaneous coronary intervention (PCI) in TEDA International Cardiovascular Hospital from October 2016 to September 2017 were collected retrospectively. We divided the patients into two groups: β-blocker + ACEI group (BB+ ACEI group, n=666) and β-blocker + ARB group (BB+ ARB group, n=84) according to discharge medications. The clinical datas were gathered and the end-point events were followed up. K-M curve was used to describe cumulative survival rate of the two groups. We used Cox regression analysis to compare the clinical outcomes of the two groups. Results:The occurrence of major adverse cardiovascular and cerebrovascular events (MACCE) (8.3% vs 3.4%, HR=2.377, 95% CI: 1.006-5.616, P=0.048), all-cause death (3.6% vs 0.4%, HR=12.951, 95% CI: 1.947-86.159, P=0.008) and non-fatal myocardial infarction (3.6% vs 0.8%, HR=5.231, 95% CI: 1.193-22.934, P=0.028) in the BB+ ARB group was significantly higher than those in the BB+ ACEI group followed up for 13 months. However, there was no difference between the two groups in the incidence of stroke (1.2% vs 1.4%, HR=0.922, 95% CI: 0.117-7.276, P=0.516) and target vessel revascularization (3.6% vs 1.6%, HR=1.607, 95% CI: 0.384-6.729, P=0.516). The cumulative survival rate of BB+ ACEI group was higher than that of BB+ ARB group, with statistically significant difference ( P<0.05). Conclusions:Compared with β-blocker combined with ARB, β-blocker combined with ACEI are more beneficial to reduce the incidence of MACCE, all-cause death and non-fatal myocardial infarction in AMI patients without left ventricular systolic dysfunction after PCI.
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INTRODUCTION@#There are concerns that angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) may worsen the outcomes of patients with COVID-19. This systematic review and meta-analysis aimed to study the in-hospital mortality among COVID-19 patients who were on ACEIs/ARBs as compared to those not on ACEIs/ARBs.@*METHODS@#We searched PubMed, EMBASE, clinicaltrials.gov and Google Scholar between 1 January 2020 and 30 May 2020 to identify all studies that evaluated the use of ACEIs/ARBs and reported the in-hospital mortality outcomes of COVID-19 patients. Nine non-randomised studies were eligible for inclusion in the analysis. The primary outcome studied was the in-hospital mortality of COVID-19 patients who were on ACEIs/ARBs compared with those not on ACEIs/ARBs.@*RESULTS@#Of the 8,313 patients in the nine studies, 7,622 (91.7%) were from studies with all-comers, while 691 (8.3%) were from studies involving only patients with hypertension. 577 (14.6%) in-hospital deaths were observed out of a total of 3,949 patients with an outcome in the nine studies. Overall, no significant difference was observed in the in-hospital mortality between patients on ACEIs/ARBs and those not on ACEIs/ARBs (odds ratio [OR] 1.06, 95% confidence interval [CI] 0.75-1.50; p = 0.73). Further sensitivity analysis in the hypertension group and the all-comers group showed similar results (OR 0.88, 95% CI 0.58-1.32; p = 0.53 and OR 1.85, 95% CI 1.00-3.43; p = 0.05, respectively).@*CONCLUSION@#We observed that ACEIs/ARBs had no significant impact on the in-hospital mortality of COVID-19 patients and can be used safely in patients with indications.
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Humans , Angiotensin Receptor Antagonists/therapeutic use , Angiotensin-Converting Enzyme Inhibitors/therapeutic use , COVID-19 , Hospital Mortality , Hypertension/drug therapy , SARS-CoV-2ABSTRACT
Objective To investigate the influence of angiotensinreceptor neprilysin inhibitor (ARNI) and angiotensin converting enzyme inhibitor (ACEI) on clinical efficacy and safety of elderly patients with ischemic cardiomyopathy.Methods From January 2017 to December 2018,120 elderly patients with ischemic cardiomyopathy in the Third People's Hospital of Cixi were divided into 2 groups according to treatment methods,59 patients treated with ACEI (control group) and 61 patients treated with ARNI (observation group) on the basis of conventional intervention.The levels of blood lipid index,blood pressure index,B-type brain natriuretic peptide (BNP),6-minute walking test (6MWT) and echocardiographic index,endothelium-dependent diastolic function of brachial artery (FMD) and carotid intima-media thickness (CIMT) before and after treatment were compared.The adverse reactions incidence of 2 groups were compared.Results The levels of blood lipid index and blood pressure index after treatment of 2 groups were significantly lower than those before treatment,and the differences had statistical significant (P ＜ 0.05).There were no significant differences in the levels of blood lipid index and blood pressure index after treatment between 2 groups (P ＞ 0.05).After treatment of 12 weeks,the levels of BNP,6MWT,left ventricular ejection fraction (LVEF),left ventricular end-diastolic dimension (LVEDD) of observation group were significantly better than those of control group [(103.50 ± 23.95) ng/L vs.(175.20 ± 37.24) ng/L,(493.47 ± 92.54) m vs.(411.42 ± 61.09) m,(44.95 ± 5.89)％ vs.(41.54 ± 4.21)％,(149.59 ± 33.26) mm vs.(143.24 ± 34.25) mm](P ＜ 0.05).The level of brachial artery FMD after treatment of observation group was significantly higher than that of control group [(15.14 ± 2.52)％ vs.(9.25 ± 1.12)％](P ＜ 0.05).The level of CIMT after treatment of observation group was significantly lower than that of control group [(1.01 ± 0.28) mm vs.(1.32 ± 0.25) mm] (P＜ 0.05).There was no significant difference in the adverse reactions incidence between 2 groups (P＞ 0.05).Conclusions ARNI in assisted treatment of elderly patients with ischemic cardiomyopathy can efficiently improve cardiac function,increase exercise endurance,enhance vasodilation function and dose not aggravate adverse drug reactions.
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Aim To investigate the inhibitory effect of small molecule inhibitors of ornithine decarboxylase inhibitor 1 (AZIN-1) on non-small cell lung cancer and its mechanism. Methods Cell proliferation was detected by Cell Counting Kit-8 (CCK-8). Apoptosis was analyzed by flow cytometry (PI/Annexin V-FITC double staining). The expression of ornithine decarboxylase (ODC), ornithine decarboxylase anti-enzyme-1 (AZ-1) and AZIN-1 was detected by Western blot. Cell cycle was analyzed by flow cytometry (PI single staining). The total polyamine content in cellswas measured by high performance liquid chromatography (HPLC). Results Small molecule inhibitor of AZIN-1 could significantly inhibit the proliferation of A549 cells, cause G0/G, cycle arrest, induce apoptosis of A549 cells, inhibit the expression of AZIN-1 and ODC, interfere with intracellular polyamine metabolism, and reduce total polyamine content in cells. Conclusions Small molecule inhibitor of AZIN-1 has significant growth inhibitory effect on A549 cells, and its mechanism may be related to the induction of apoptosis and interference with polyamine metabolism.
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Objective@#To investigate the influence of angiotensinreceptor neprilysin inhibitor(ARNI) and angiotensin converting enzyme inhibitor (ACEI) on clinical efficacy and safety of elderly patients with ischemic cardiomyopathy.@*Methods@#From January 2017 to December 2018, 120 elderly patients with ischemic cardiomyopathy in the Third People′s Hospital of Cixi were divided into 2 groups according to treatment methods, 59 patients treated with ACEI (control group) and 61 patients treated with ARNI (observation group) on the basis of conventional intervention. The levels of blood lipid index, blood pressure index, B-type brain natriuretic peptide (BNP), 6- minute walking test (6MWT) and echocardiographic index, endothelium-dependent diastolic function of brachial artery (FMD) and carotid intima-media thickness (CIMT) before and after treatment were compared. The adverse reactions incidence of 2 groups were compared.@*Results@#The levels of blood lipid index and blood pressure index after treatment of 2 groups were significantly lower than those before treatment, and the differences had statistical significant (P<0.05). There were no significant differences in the levels of blood lipid index and blood pressure index after treatment between 2 groups (P>0.05). After treatment of 12 weeks, the levels of BNP, 6MWT, left ventricular ejection fraction (LVEF), left ventricular end-diastolic dimension(LVEDD) of observation group were significantly better than those of control group [(103.50 ± 23.95) ng/L vs. (175.20 ± 37.24) ng/L, (493.47 ± 92.54) m vs. (411.42 ± 61.09) m, (44.95 ± 5.89)% vs. (41.54 ± 4.21)%, (149.59 ± 33.26) mm vs. (143.24 ± 34.25) mm](P<0.05). The level of brachial artery FMD after treatment of observation group was significantly higher than that of control group [(15.14 ± 2.52)% vs. (9.25 ± 1.12)%](P<0.05). The level of CIMT after treatment of observation group was significantly lower than that of control group [(1.01 ± 0.28) mm vs. (1.32 ± 0.25) mm](P<0.05). There was no significant difference in the adverse reactions incidence between 2 groups (P>0.05).@*Conclusions@#ARNI in assisted treatment of elderly patients with ischemic cardiomyopathy can efficiently improve cardiac function, increase exercise endurance, enhance vasodilation function and dose not aggravate adverse drug reactions.
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Background: Nephropathy is responsible for an End Stage Renal Disease (ESRD) in type 2 diabetics if uncontrolled. The monotherapy/combination of Angiotensin Converting Enzyme inhibitor (ACEi) and Angiotensin II Receptor Blockers (ARBs) can retard the progression of urine albumin to creatinine ratio in diabetic nephropathy but, the data shows an inconsistency in the efficacy of these drugs. So, the present study was aimed at comparing the reno-protective effect of ACEi/ARBs in type 2 diabetics.Methods: A prospective, randomized study is conducted at Maharaja’s Institute of Medical Sciences, Nellimarla, Vizianagaram, Andhra Pradesh, India with 100 patients, who are randomly categorised and equally distributed among the two groups and treated with Enalapril (ACEi) and Losartan (ARBs) for 6 months. 24-hour urine albumin to creatinine ratio and HbA1c are recorded before and after the treatment.Results: Enalapril and losartan showed a non-significant reduction in urine albumin to creatinine ratio from 196.2±17.5 to 185.9±15.2 (p=0.66) and 236.8±16.3 to 193.7±20.6 (p=0.11) respectively. A strict glycemic control has shown a reduction in HbA1c in both the groups.Conclusions: Present findings suggested that losartan is relatively more effective than enalapril in reducing the 24-hour urine albumin to creatinine ratio of diabetic nephropathy patients. Along with these drugs, regulation of blood glucose will assist in retarding the progression of nephropathy in type 2 diabetics.
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This study aims to evaluate the potential of endophytic fungi isolated from Gandaria (Bouea macrophylla Griffith) as sources of enzyme inhibitor, antibacterial, and antioxidant and identify the chemical compounds of active extract. The endophytic fungi were identified as fungi closely related to the genus Neofusicoccum ribis based on sequence analysis of the 28S rDNA and internal transcribed spacer region. N. ribis was cultured on potato dextrose broth and extracted with hexane, ethyl acetate, and partition between methanol and ethyl acetate, respectively. Bioactivity screenings as enzyme inhibitor (acetylcholinesterase/acetylcholinesterase inhibitor (AChE) and β-glucosidase), antibacterial, and antioxidant were conducted by thin-layer chromatography-bioautography method. The chemical compounds were analyzed by gas chromatography-mass spectrometry (GC-MS). The results showed that the ethyl acetate extract of N. ribis had the activity as enzyme inhibitor for AChE and β-glucosidase. The minimum inhibitory concentration values of N. ribis extract against Staphylococcus aureus and Escherichia coli were in the range of 512–>512 µg/mL. Hexane extract had better antioxidant activity (IC50 = 479.66 µg/mL) than ethyl acetate extract (IC50 = 928.09–1102.60 µ g/mL). The GC-MS analysis showed that 12 identified chemical compounds were found in the ethyl acetate extract of N. ribis.
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Objective@#To observe the effect of panobinostat (LBH589) on the early brain injury (EBI) in the model of subarachnoid hemorrhage(SAH) in SD rats.@*Methods@#SD rats were randomly divided into 4 groups: sham(10 rats) and SAH(10 rats), SAH+ vehicle(20 rats) and SAH+ Panobinostat(20 rats). Drug or vehicle was given by lateral-ventricular stereotaxic injection 24h before the SAH model was introduced.Water contents and the neurological scores were determined at 24h post-SAH.The levels of Ac-H3K27 in frontal and lateral lobe were detected by Western blot.@*Results@#The mean neurological score of the SAH group was higher than that of the sham group(F=13.000, P=0.007). The water content of the SAH group was higher than that of the sham group (F=8.229, P=0.019). The level of Ac-H3K27 was higher in the SAH+ Panobinostat group than that in the SAH+ vehicle group(F=41.250, P=0.000). The mean neurological score of the SAH+ Panobinostat group was lower than that of the SAH+ vehicle group(F=9.560, P=0.011). The water content of the SAH+ Panobinostat group was lower than that of the SAH+ vehicle group(F=8.211, P=0.020). The correlation analysis indicated that the level of acetylation of H3 was negatively correlated with the neurological score(r=-0.585, P=0.046).@*Conclusion@#Panobinostat can improve the neurological behavior and alleviate early brain injury in the SAH model.
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Objective To observe the effect of panobinostat (LBH589) on the early brain injury (EBI) in the model of subarachnoid hemorrhage(SAH) in SD rats.Methods SD rats were randomly divided into 4 groups:sham(10 rats) and SAH(10 rats),SAH + vehicle(20 rats) and SAH + Panobinostat (20 rats).Drug or vehicle was given by lateral-ventricular stereotaxic injection 24h before the SAH model was introduced.Water contents and the neurological scores were determined at 24h post-SAH.The levels of Ac-H3K27 in frontal and lateral lobe were detected by Western blot.Results The mean neurological score of the SAH group was higher than that of the sham group(F =13.000,P =0.007).The water content of the SAH group was higher than that of the sham group (F =8.229,P =0.019).The level of Ac-H3K27 was higher in the SAH + Panobinostat group than that in the SAH +vehicle group(F =41.250,P =0.000).The mean neurological score of the SAH + Panobinostat group was lower than that of the SAH + vehicle group(F =9.560,P =0.011).The water content of the SAH + Panobinostat group was lower than that of the SAH + vehicle group (F =8.211,P =0.020).The correlation analysis indicated that the level of acetylation of H3 was negatively correlated with the neurological score (r =-0.585,P =0.046).Conclusion Panobinostat can improve the neurological behavior and alleviate early brain injury in the SAH model.
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Objective: To isolate, identify, and evaluate a new angiotensin-converting enzyme inhibitor from Peperomia pellucida (L.) Kunth herbs. Methods: A dried sample of Peperomia pellucida herb was successively macerated with n-hexane and ethyl acetate. The ethyl acetate extract solution was evaporated to obtain the crude extract. Vacuum liquid column chromatography and thin layer chromatography were performed to obtain two pure compounds. Then, both compounds were elucidated and identified using the spectroscopic method. Angiotensin-converting enzyme inhibitory activity studies of both compounds were determined using angiotensin-converting enzyme kit WST-1 with spectrophotometer microplate reader 96-well at 450 nm wavelength. Results: Two bioactive compounds were successfully isolated from Peperomia pellucida herb, including a new compound of 2,3,5-trimethoxy-9-(12,14,15-trimethoxybenzyl)-1H-indene and pellucidin A. Both compounds demonstrated angiotensin-converting enzyme inhibitory activity, with IC50 values of 72 μM (27.95 μg/mL) and 11 μM (4.4 μg/mL), respectively. Conclusions: In the present study, two active angiotensin-converting enzyme inhibitors were successfully isolated and purified from Peperomia pellucida which is used as an antihypertensive in traditional medicine, and support its use as an angiotensin-converting enzyme-inhibiting drug.
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BACKGROUND: Angiotensin-converting enzyme inhibitors (ACEIs) are the first choice for the treatment of acute myocardial infarction (AMI), and angiotensin receptor blockers (ARBs) should be considered in patients intolerant to ACEIs. Although previous studies support the use of ARBs as an alternative to ACEIs, these studies showed inconsistent results. The objective of this study was to demonstrate the clinical impact of ARBs as an alternative to ACEIs in patients with AMI undergoing percutaneous coronary intervention (PCI). METHODS: The CardiOvascular Risk and idEntificAtion of potential high-risk population in AMI (COREA-AMI) registry enrolled all consecutive patients with AMI undergoing PCI. The primary endpoint was the composite of cardiovascular death, myocardial infarction, stroke, or hospitalization due to heart failure. RESULTS: Of the 3,328 eligible patients, ARBs replaced ACEIs in 816 patients, while 824 patients continued to use ACEIs and 826 patients continued to use ARBs. The remaining 862 patients did not receive ACEIs/ARBs. After the adjustment with inverse probability weighting, the primary endpoints in the first groups were similar (7.5% vs. 8.0%, hazard ratio [HR], 0.89; 95% confidence interval [CI], 0.75–1.05; P = 0.164). Composite events were less frequent in the ACEI to ARB group than no ACEI/ARB group (7.5% vs. 11.8%, HR, 0.76; 95% CI, 0.64–0.90; P = 0.002). CONCLUSION: The alternative use of ARBs following initial treatment with ACEIs demonstrates comparable clinical outcomes to those with continued use of ACEIs and is associated with an improved rate of composite events compared to no ACEI/ARB use in patients with AMI undergoing PCI. TRIAL REGISTRATION: ClinicalTrials.gov Identifier: NCT02385682
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Humans , Angiotensin Receptor Antagonists , Angiotensin-Converting Enzyme Inhibitors , Angiotensins , Heart Failure , Hospitalization , Myocardial Infarction , Percutaneous Coronary Intervention , StrokeABSTRACT
Objective: To isolate, identify, and evaluate a new angiotensin-converting enzyme inhibitor from Peperomia pellucida (L.) Kunth herbs. Methods: A dried sample of Peperomia pellucida herb was successively macerated with n-hexane and ethyl acetate. The ethyl acetate extract solution was evaporated to obtain the crude extract. Vacuum liquid column chromatography and thin layer chromatography were performed to obtain two pure compounds. Then, both compounds were elucidated and identified using the spectroscopic method. Angiotensin-converting enzyme inhibitory activity studies of both compounds were determined using angiotensin-converting enzyme kit WST-1 with spectrophotometer microplate reader 96-well at 450 nm wavelength. Results: Two bioactive compounds were successfully isolated from Peperomia pellucida herb, including a new compound of 2,3,5-trimethoxy-9-(12,14,15-trimethoxybenzyl)-1H-indene and pellucidin A. Both compounds demonstrated angiotensin-converting enzyme inhibitory activity, with IC
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Objective To investigate the clinical efficacy and safety of angiotensin-converting enzyme inhibitor (ACEI) and angiotensin receptor blocker (ARB) in treatment of children with Alport syndrome (AS).Methods A total of 22 children with AS in Department of Pediatrics,Guangzhou First People's Hospital and Department of Pediatrics,Shenzhen People's Hospital between January 2013 and December 2017 were selected.But four children were not included in this study since they did not take medication regularly,and the other 18 cases were included in this study.All the 18 children were initially treated with ACEI.The observation time was from 1 to 5 years.If the symptoms were not effectively controlled,treatment plan would be changed to ACEI combined with ARB treatment.The observation time was from 1 to 3 years.The clinical data and laboratory examination results [including 24-hour urine protein (mg/24 h),urine red blood cell count,plasma albumin (Alb),urea nitrogen (BUN),serum creatinine (Scr),total cholesterol (TC)] were collected for retrospective analysis.Results Eighteen patients started their treatment with ACEI inhibitors (Fosinopril).Within 2 years of treatment,the urinary protein and urinary red blood cells in the children decreased to 47.7％ and 41.3％,respectively,and the differences were all statistically significant (all P ＜ 0.05),and the renal function was stable within the normal range.Two years later,7 patients had elevation of urinary protein and urinary erythrocyte elevations and decrease of renal function,and they were treated with ACEI and ARB (Losartan).The other children had no significant change in urine protein and urine red blood cells in the 3 rd,4th,and 5th year,and their renal function was stable.After ACEI treatment alone for 5 years,urinary protein was 47.8％ lower than before treatment,and the difference was statistically significant (P ＜ 0.05);urinary red blood cells decreased to 32.0％ compared with before treatment,and the difference was statistically significant (P ＜ 0.05).Seven patients with ACEI alone had poor efficacy,after the treatment with ACEI combined with ARB,the urinary protein and urine red blood cells were lower in the first year and the renal function improved.There was no significant change in urinary protein and urine red blood cells in the 2nd and 3rd year,and renal function was stable.After ACEI combined with ARB treatment for 3 years,urinary protein decreased to 42.3％ before treatment,and the difference was statistically significant (P ＜ 0.05),and urinary red blood cells decreased to 46.9％ compared with before treatment,and the difference was statistically significant(P ＜ 0.05).Conclusions ACEI treatment of children with AS can reduce urine protein and help delay renal failure.For children with poor efficacy of ACEI treatment,ACEI combined with ARB may have a certain effect.ARB can be used as an adjunctive treatment for patients with AS who have a poor response to ACEI alone.
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OBJECTIVE: To observe the improvement effects of angiotensin converting enzyme inhibitor (ACEI) fosinopril, perindopril and benazepril on ventricular remodeling in patients with acute myocardial infarction (AMI), and to evaluate its safety. METHODS: A total of 96 AMI patients selected from our hospital during Jan. 2014-Oct. 2016 were divided into group A, B, C according to random number table, with 32 cases in each group. All patients received symptomatic treatment, underwent percutaneous coronary intervention, and then given ACEI after blood vessels recanalization and keeping blood pressure stable. Group A was given Fosinopril sodium tablets 10 mg, qd; group B was given Perindopril tert-butylamine tablets 4 mg, qd; group C was given Benazepril hydrochloride tablets 10 mg, qd. All groups were treated for consecutive 6 months. Cardiac structure and function indexes (LVESD, LVEDD, IVSD, LVPWD, LVEF, CO), hemodynamic indexes (SBP, DBP, HR) and related lab indexes (FPG, TG, TC, HDL-C, LDL-C, AST, ALT, Scr, BUN) of 3 groups were observed before and after treatment. The occurrence of ADR was recorded. RESULTS: Before treatment, there was no statistical significance in cardiac structure and function indexes, hemodynamic indexes or related lab indexes among 3 groups (P＞0. 05). After treatment, the levels of LVESD, LVEDD, LVPWD, CO, HR, FPG, TG, TC and LDL-C in 3 groups were decreased significantly, while the levels of LVEF and SBP were increased significantly, with statistical significance (尸＜0. 05). There was no statistical significance in above indexes among 3 groups after treatment (P＞0. 05). After treatment, the level of Scr in group B was significantly increased and higher than group A and C, with statistical significance (P＜0. 05). There was no statistical significance in the levels of IVSD, DBP, HDL-C, AST, ALT or BUN among 3 groups before and after treatment as well as the level of Scr between group A and C (P＞ 0. 05). There was no statistical significance in the incidence of ADR among 3 groups(P＞0. 05). CONCLUSIONS: Fosinopril, perindopril and benazepril can significantly improve ventricular remodeling in AMI patients, narrowing the heart cavity, increasing systolic pressure, lowering heart rate, reducing the oxygen consumption of the ventricle, with similar effects. Perindopril may increase the level of Scr, so fosinopril and benazepril are safe and suitable for AMI patients with renal function disorder.
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Capillary electrophoresis with many advantages plays an important role in pharmaceutical analysis and drug screening. This review gives an overview on the recent advances in the developments and applications of capillary electrophoresis in the field of enzyme inhibitor screening. The period covers 2013 to 2017. Both the pre-capillary enzyme assays and in-capillary enzyme assays which include electrophoretically mediated microanalysis (EMMA) and immobilized enzyme microreactor (IMER) are summarized in this article.
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In recent years, owing to the abuse of antibiotics, the widespread of resistant bacterial strains became a serious threat to public health. This status demands development of new antibacterial agents with novel mechanisms of action. The reason for the limited new antibacterials is the small number of effective therapeutic targets, which cannot meet the current needs for the multiple drug-resistant treatment. Screening for new targets is the key step in the development of novel antibacterial agents. Peptidoglycan is the main component of the cell wall of bacteria, which is essential for survival of pathogenic bacteria. Within the biochemical pathway for peptidoglycan biosynthes is the Murligases, described in this review as highly potential targets for the development of new classes of antibacterial agents. This review provides an in-depth insight into the recent developments in the field of inhibitors of the Mur enzymes (MurA-F). Moreover, the reasons for the lack of candidate inhibitors and the challenges to overcome the hurdles are also discussed.
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Objective To evaluate the efficacy of angiotensin converting enzyme inhibitor (ACEI) and angiotensin receptor blocker (ARB) in the treatment of idiopathic pulmonary fibrosis through the method of system evaluation. Methods A computer-based online search of Pubmed, Embase, Cochrane Library, CNKI, CBM and Wanfang were used for database retrieval. Revman 5.0 was used to assess the bias of the included studies. The Stata 14.0 was used to evaluate the extraction indexes of efficacy, p (O2), p (CO2), DLco, FEV1 and VC. GRADE score was used to evaluate the level of evidence. Results A total of 17 articles (related with 1381 patients) were included in this study, including 14 studies using ARB and 3 studies using ACEI. Compared with the control group ACEI and ARB drugs showed advantages in the treatment of pulmonary fibrosis (RR=1.34, 95%CI:1.24-1.44, Z=7.81, P<0.001). Auxiliary index analysis showed that the test groups were treated with enalapril (SMD=0.72, 95%CI:0.21-1.22, Z=2.77, P=0.006), telmisartan (SMD=3.86, 95%CI:2.44-5.27, Z=5.35, P<0.001), valsartan (SMD=1.94, 95%CI:1.33-2.55, Z=6.27, P<0.001) and captopril (SMD=0.60, 95%CI:0.11-1.09, Z=2.41, P=0.016), the p(O2) levels were significantly improved in patients ≥65 years old (SMD=0.76, 95%CI:0.52-1.00, Z=6.18, P<0.001) and patients < 65 years old (SMD=3.97, 95%CI:2.61-5.32, Z=5.73, P<0.001), and disease duration≥5 years (SMD=1.39, 95%CI:0.45-2.33, Z=2.89, P=0.004) and disease duration<5 years (SMD=3.26, 95%CI:2.06-4.46, Z=5.34, P<0.001) compared with those of control group (SMD=2.95, 95%CI:1.95-3.94, Z=5.82, P<0.001). The curative effect of telmisartan was better than that of other drug groups (P < 0.001), and which was much better for patients under 65 years old (P<0.001). There was no significant difference in the disease duration between two groups (P=0.307). The p (CO2) levels were significantly improved in patients treated with telmisartan [SMD=-12.94,95%CI:(-14.01)-(-11.86),Z=23.51,P<0.001), valsartan [SMD=-1.95,95%CI:(-2.56)-(-1.34),Z=6.29,P<0.001] compared with those of control group [SMD=-11.13,95%CI:(-17.03)-(-5.24),Z=3.70,P<0.001]. The effect of telmisartan was better than that of valsartan (P<0.001). In addition, values of DLco (SMD=0.64, 95%CI:0.45-0.83, Z=6.72, P<0.001), FEV1 (SMD=1.19, 95%CI:0.52-1.86, Z=3.47, P<0.001) and VC (SMD=0.51, 95%CI:0.16-0.85, Z=2.85, P=0.004) were improved in test group compare with those of control group. And the GRADE scores of relevant indexes were low quality to moderate quality. Conclusion ACEI and ARB can improve the efficacy, the p (O2) and p (CO2) in the treatment of pulmonary fibrosis. Patients with age<65 years old and treated with telmisartan have the best curative effect, and which is not related to the disease duration.
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OBJECTIVE:To observe the clinical efficacy and safety of amlodipine besylate combined with lisinopril and hydro-chlorothiazide,atorvastatin in the treatment of severe primary hypertension complicating with carotid atherosclerosis. METHODS:90 patients with severe primary hypertension complicating with carotid atherosclerosis were divided into control group (45 cases) and observation group(45 cases)according to random lottery form. Both groups were given Atorvastatin calcium tablet 20 mg/time orally,qd;control group was additionally given Amlodipine besylate tablet 5 mg/time orally,qd;observation group was additional-ly given Lisinopril and hydrochlorothiazide tablet 10 mg/time orally,qd,on the basis of control group. Both groups were treated for 8 weeks. Clinical efficacies of 2 groups were compared as well as blood pressure level,IMT,PV of carotid atherosclerosis, hs-CRP,TNF-α before and after treatment. The occurrence of ADR was recorded. RESULTS:Total response rate of observation group was significantly higher than that of control group,with statistical significance (P0.05). After treatment,the levels of SBP,DBP, IMT,PV,hs-CRP and TNF-α level in 2 groups were significantly lower than before;the observation group was significantly lower than the control group,with statistical significance (P0.05). CONCLUSIONS:Amlodipine besylate combined with lisinopril and hydrochlorothiazide,atorvastatin in the treatment of primary hypertension complicating with carotid atherosclerosis can effectively control the blood pressure level, delay the progression process of carotid atherosclerosis,reduce the inflammatory reaction degree,but dose not increase the occur-rence of ADR with good safety.