Pub Date : 2020-09-01DOI: 10.21608/ajps.2020.118377
M. Elaasser
In the present investigation, a trial was done to find a new antimicrobial agent producing microbe from soil microbiota of local habitats to control the problem of multiple drug resistance. The term of Antimicrobial resistance (AMR) is used to describe microorganisms that can resist the effects of drugs and chemicals designed to kill them. Seventy six actinomycetes isolates were isolated from fifteen soil samples different localities in Egypt were primary screening for antimicrobial activity by agar plug diffusion method against test microorganisms. Sixteen isolates were selected for secondary screening in small scale submerged fermentation system and assayed against pathogenic tested microorganisms using agar well diffusion method. Among of these isolates tested, the isolate (S1SHA1) showed the highest antimicrobial activity against pathogenic test organisms. This isolate was identified as Streptomyces griseoplanus by morphological, physiological, biochemical characters and 16s rRNA gene sequence. Physical and nutritional factors affecting activity of antimicrobial agent were studied. The results showed that, optimum activity of antimicrobial agent achieved with pH 7, incubation temperature 28 C, for 7 days, at 150 rpm agitation, carbon and nitrogen source starch 1.5% and potassium nitrate 0.4%, as well as phosphorus 2 g/l and NaCl at concentration of 1 %. Antimicrobial agent from batch culture was subjected to extraction and purification processes using ethyle acetate and preparative TLC, respectively. Determination of minimum inhibitory concentrations (MIC) and Mode of action of antimicrobial agent produced by S. griseoplanus (S1SHA1) on the test microbial strains using Transmission Electron Microscopy (TEM). Cytotoxic studies showed that no cytotoxic effects were observed for the compound when tested even at high concentrations
{"title":"A NEW TRIAL FOR BIOFORMATION OF ANTIMICROBIAL AGENT CONTROLLING MULTI DRUG RESISTANT MICROORGANISM","authors":"M. Elaasser","doi":"10.21608/ajps.2020.118377","DOIUrl":"https://doi.org/10.21608/ajps.2020.118377","url":null,"abstract":"In the present investigation, a trial was done to find a new antimicrobial agent producing microbe from soil microbiota of local habitats to control the problem of multiple drug resistance. The term of Antimicrobial resistance (AMR) is used to describe microorganisms that can resist the effects of drugs and chemicals designed to kill them. Seventy six actinomycetes isolates were isolated from fifteen soil samples different localities in Egypt were primary screening for antimicrobial activity by agar plug diffusion method against test microorganisms. Sixteen isolates were selected for secondary screening in small scale submerged fermentation system and assayed against pathogenic tested microorganisms using agar well diffusion method. Among of these isolates tested, the isolate (S1SHA1) showed the highest antimicrobial activity against pathogenic test organisms. This isolate was identified as Streptomyces griseoplanus by morphological, physiological, biochemical characters and 16s rRNA gene sequence. Physical and nutritional factors affecting activity of antimicrobial agent were studied. The results showed that, optimum activity of antimicrobial agent achieved with pH 7, incubation temperature 28 C, for 7 days, at 150 rpm agitation, carbon and nitrogen source starch 1.5% and potassium nitrate 0.4%, as well as phosphorus 2 g/l and NaCl at concentration of 1 %. Antimicrobial agent from batch culture was subjected to extraction and purification processes using ethyle acetate and preparative TLC, respectively. Determination of minimum inhibitory concentrations (MIC) and Mode of action of antimicrobial agent produced by S. griseoplanus (S1SHA1) on the test microbial strains using Transmission Electron Microscopy (TEM). Cytotoxic studies showed that no cytotoxic effects were observed for the compound when tested even at high concentrations","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"04 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86110909","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-03-01DOI: 10.21608/ajps.2020.86023
E. El-Gebaly
Biosurfactant producing bacteria (28 isolates) were isolated from 30 oil contaminated soils and tested for production of biosurfactant by different screening methods. About 75% of the isolated bacteria showed no blood hemolysis and their emulsification index for hexane and xylene ranges from 28-35% and 30-45% respectively. Biosurfactant producing ability was confirmed by other tests where about 40% of isolates showed positive oil spreading activity, hydrocarbon overlay and 67% showed to be positive for drop collapsing test. 16s RNA sequencing of the most active isolates revealed one Stenotrophomonas maltophila, two Bacillus spp. and two Achromobacter spp. Biosurfactants extracted from these isolates showed variable antimicrobial activity against Staphylococcus aureus, E. coli and Pseudomonas aeruginosa. This study demonstrated that the biosurfactants produced by these bacteria could be used in combination with antibiotics for treating bacterial infections. Further study is required for enhancing biosurfactant production by bacterial isolates to be used environmentally for bioremediation of oil contaminated soils.
{"title":"SCREENING OF BIOSURFACTANT PRODUCTION BY BACTERIAL STRAINS ISOLATED FROM {SUDHANSHU SHEKHAR, 2015 #18}OIL CONTAMINATED SITES NEAR GAS STATIONS IN EGYPT.","authors":"E. El-Gebaly","doi":"10.21608/ajps.2020.86023","DOIUrl":"https://doi.org/10.21608/ajps.2020.86023","url":null,"abstract":"Biosurfactant producing bacteria (28 isolates) were isolated from 30 oil contaminated soils and tested for production of biosurfactant by different screening methods. About 75% of the isolated bacteria showed no blood hemolysis and their emulsification index for hexane and xylene ranges from 28-35% and 30-45% respectively. Biosurfactant producing ability was confirmed by other tests where about 40% of isolates showed positive oil spreading activity, hydrocarbon overlay and 67% showed to be positive for drop collapsing test. 16s RNA sequencing of the most active isolates revealed one Stenotrophomonas maltophila, two Bacillus spp. and two Achromobacter spp. Biosurfactants extracted from these isolates showed variable antimicrobial activity against Staphylococcus aureus, E. coli and Pseudomonas aeruginosa. This study demonstrated that the biosurfactants produced by these bacteria could be used in combination with antibiotics for treating bacterial infections. Further study is required for enhancing biosurfactant production by bacterial isolates to be used environmentally for bioremediation of oil contaminated soils.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"109 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79211174","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/ajps.2019.70234
A. Sami
Onychomycosis is a widely distributed fungal nail infection which can be caused by dermatophytes, yeasts or non-dermatophytic fungi. In our study a total of 7 species related to 4 genera were isolated from 50 patients suspected with the fungal nail infection (onychomycosis) these namely Aspergillus flavus (8 isolates), Aspergillus niger (13 isolates), Candida albicans (8 isolates), C. tropicalis (5 isolates), Epidermophyton floccosum (1 isolate), Trichophyton mentagrophytes (2 isolates) and Trichophyton rubrum (1 isolate). Nowadays the field of nanotechnology becomes one of the most topics of interest. The impact of gold nanoparticles on the isolated fungal species was evaluated by agar well diffusion method and micro-dilution method. Best antifungal activity of gold nanoparticles was observed by using 100 µl of AuNps containing 20 µg of gold nanoparticles with the greatest zone of inhibition (19 mm) against C. albicans. AuNps showed variable MIC (minimum inhibitory concentration). MIC50 and MIC90 values of AuNPs ranged from 3.125 to 25.0 μg/ml and from 12.5 to100 μg/ml respectively. All isolated fungi could grow on keratin agar medium but with variable degrees indicating their ability to hydrolyze keratin. Keratinase activity in presence and absence of AuNPs was determined for dermatophytes and Aspergillus species. AuNPs had an inhibitory effect causing reduction in keratinase enzyme activity reaching 52.17 %, 40 % and 37.5 % was attained in case of E. floccosum, A. flavus and A. niger (the most susceptible isolates) respectively, by application of 20 µg/ml of AuNPs.
{"title":"ANTIFUNGAL EFFECT OF GOLD NANOPARTICLES ON FUNGI ISOLATED FROM ONYCHOMYCOSIS PATIENTS","authors":"A. Sami","doi":"10.21608/ajps.2019.70234","DOIUrl":"https://doi.org/10.21608/ajps.2019.70234","url":null,"abstract":"Onychomycosis is a widely distributed fungal nail infection which can be caused by dermatophytes, yeasts or non-dermatophytic fungi. In our study a total of 7 species related to 4 genera were isolated from 50 patients suspected with the fungal nail infection (onychomycosis) these namely Aspergillus flavus (8 isolates), Aspergillus niger (13 isolates), Candida albicans (8 isolates), C. tropicalis (5 isolates), Epidermophyton floccosum (1 isolate), Trichophyton mentagrophytes (2 isolates) and Trichophyton rubrum (1 isolate). Nowadays the field of nanotechnology becomes one of the most topics of interest. The impact of gold nanoparticles on the isolated fungal species was evaluated by agar well diffusion method and micro-dilution method. Best antifungal activity of gold nanoparticles was observed by using 100 µl of AuNps containing 20 µg of gold nanoparticles with the greatest zone of inhibition (19 mm) against C. albicans. AuNps showed variable MIC (minimum inhibitory concentration). MIC50 and MIC90 values of AuNPs ranged from 3.125 to 25.0 μg/ml and from 12.5 to100 μg/ml respectively. All isolated fungi could grow on keratin agar medium but with variable degrees indicating their ability to hydrolyze keratin. Keratinase activity in presence and absence of AuNPs was determined for dermatophytes and Aspergillus species. AuNPs had an inhibitory effect causing reduction in keratinase enzyme activity reaching 52.17 %, 40 % and 37.5 % was attained in case of E. floccosum, A. flavus and A. niger (the most susceptible isolates) respectively, by application of 20 µg/ml of AuNPs.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84415240","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/AJPS.2019.70236
Ahmed Mancy
Antibiotics are a cornerstone of medical treatment for various bacterial infections and are prescribed at a rate that exceeds the limit of prescribing. Phenylthiazoles were reported previously as a new scaffold that possesses antibacterial activity against an array of clinically-relevant strains of multidrug-resistant staphylococci.The structure-activity-relationships (SAR) of phenylthiazoles revealed important structural features necessary for their antibacterial activity: a nitrogenous head and a lipophilic tail. Incorporating the acetylene part in analogues with a prolonged half-life, while the cyclic nitrogenous extention revealed the most potent analogue. In the current work, advantageous moieties have been tethered together to produce a new scaffold of phenylthiazole with the objective of promoting new scaffold enhancing both antimicrobial resistance activity and drug-like properties. Among the tested phenylthiazoles, compounds 14 and 16 were found to exert a bactericidal activity against MRSA. The pharmacokinetic profile of compound 15 was significantly enhanced against biofilm of the bacteria.
{"title":"SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF ARYLAZOLE DERIVATIVES","authors":"Ahmed Mancy","doi":"10.21608/AJPS.2019.70236","DOIUrl":"https://doi.org/10.21608/AJPS.2019.70236","url":null,"abstract":"Antibiotics are a cornerstone of medical treatment for various bacterial infections and are prescribed at a rate that exceeds the limit of prescribing. Phenylthiazoles were reported previously as a new scaffold that possesses antibacterial activity against an array of clinically-relevant strains of multidrug-resistant staphylococci.The structure-activity-relationships (SAR) of phenylthiazoles revealed important structural features necessary for their antibacterial activity: a nitrogenous head and a lipophilic tail. Incorporating the acetylene part in analogues with a prolonged half-life, while the cyclic nitrogenous extention revealed the most potent analogue. In the current work, advantageous moieties have been tethered together to produce a new scaffold of phenylthiazole with the objective of promoting new scaffold enhancing both antimicrobial resistance activity and drug-like properties. Among the tested phenylthiazoles, compounds 14 and 16 were found to exert a bactericidal activity against MRSA. The pharmacokinetic profile of compound 15 was significantly enhanced against biofilm of the bacteria.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88899328","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/AJPS.2019.70238
Ali Hammad
The narrow antibacterial spectrum of phenylthiazole antibiotics was expanded by replacing the central thiazole with a pyrazole ring while maintaining its other pharmacophoric features. The most promising derivative, compound 10, was moderate potent against MDR-Gram-positive clinical isolates, including vancomycin- and linezolid-resistant MRSA, with a minimum inhibitory concentration (MIC) value 8 g/mL. Moreover, compound 10 was promising against highly pathogenic carbapenem-resistant strains, such as Acinetobacter baumannii, Klebsiella pneumoniae and E. coli. In addition to the notable biofilm inhibition activity, compound 10 outperformed both vancomycin and kanamycin in reducing the intracellular burden of both Gram-positive and Gram-negative pathogenic bacteria. Compound 10 cleared 90% of intracellular MRSA and 98% of Salmonella enteritidis at 2× the MIC.
{"title":"SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF PHENYLPYRAZOLE DERIVATIVES","authors":"Ali Hammad","doi":"10.21608/AJPS.2019.70238","DOIUrl":"https://doi.org/10.21608/AJPS.2019.70238","url":null,"abstract":"The narrow antibacterial spectrum of phenylthiazole antibiotics was expanded by replacing the central thiazole with a pyrazole ring while maintaining its other pharmacophoric features. The most promising derivative, compound 10, was moderate potent against MDR-Gram-positive clinical isolates, including vancomycin- and linezolid-resistant MRSA, with a minimum inhibitory concentration (MIC) value 8 g/mL. Moreover, compound 10 was promising against highly pathogenic carbapenem-resistant strains, such as Acinetobacter baumannii, Klebsiella pneumoniae and E. coli. In addition to the notable biofilm inhibition activity, compound 10 outperformed both vancomycin and kanamycin in reducing the intracellular burden of both Gram-positive and Gram-negative pathogenic bacteria. Compound 10 cleared 90% of intracellular MRSA and 98% of Salmonella enteritidis at 2× the MIC.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78242433","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/ajps.2019.70243
M. Kamel
Racecadotril and ofloxacin are co-formulated for treatment of acute symptomatic diarrhea. In the present work RP-HPLC method was developed for simultaneous determination of racecadotril and ofloxacin in the combined dosage form. An isocratic separation was carried out on BDS Equisil C18 (150 X 4.6 mm, 5 μm particle size) reversed phase column with a mobile phase consists of water and acetonitrile in the ratio of (20:80 % v/v) and pH 3 maintained by 0.1% ortho phosphoric acid. The flow rate was 1 ml/min and UV detection at 230 nm. The linear regression analysis of the calibration graphs showed a good linear relationship over a concentration range of 5-25 μg/ml with main recovery percent 100.06±0.952 and 99.93±0.798 for racecadotril and ofloxacin, respectively. The proposed method was validated according to ICH guidelines, and has been successfully applied for simultaneous determination of both drugs in both bulk and commercial dosage form.
消旋卡多曲和氧氟沙星共同配制用于治疗急性症状性腹泻。建立了反相高效液相色谱法同时测定消旋卡多曲和氧氟沙星联合剂型的含量。在BDS Equisil C18 (150 X 4.6 mm, 5 μm粒径)反相柱上进行等密度分离，流动相为水和乙腈，流动相为(20:80 % v/v)， pH为0.1%邻位磷酸维持pH为3。流速为1 ml/min，紫外检测波长为230 nm。线性回归分析表明，在5 ~ 25 μg/ml范围内，盐酸替卡多曲和氧氟沙星的主回收率分别为100.06±0.952和99.93±0.798，线性关系良好。所提出的方法根据ICH指南进行了验证，并已成功应用于散装和商业剂型的两种药物的同时测定。
{"title":"APPLICATION OF HIGH-PERFORMANCE LIQUID CHROMATOGRAPHIC METHOD FOR SIMULTANEOUS DETERMINATION OF RACECADOTRIL AND OFLOXACIN IN THEIR PHARMACEUTICAL DOSAGE FORM","authors":"M. Kamel","doi":"10.21608/ajps.2019.70243","DOIUrl":"https://doi.org/10.21608/ajps.2019.70243","url":null,"abstract":"Racecadotril and ofloxacin are co-formulated for treatment of acute symptomatic diarrhea. In the present work RP-HPLC method was developed for simultaneous determination of racecadotril and ofloxacin in the combined dosage form. An isocratic separation was carried out on BDS Equisil C18 (150 X 4.6 mm, 5 μm particle size) reversed phase column with a mobile phase consists of water and acetonitrile in the ratio of (20:80 % v/v) and pH 3 maintained by 0.1% ortho phosphoric acid. The flow rate was 1 ml/min and UV detection at 230 nm. The linear regression analysis of the calibration graphs showed a good linear relationship over a concentration range of 5-25 μg/ml with main recovery percent 100.06±0.952 and 99.93±0.798 for racecadotril and ofloxacin, respectively. The proposed method was validated according to ICH guidelines, and has been successfully applied for simultaneous determination of both drugs in both bulk and commercial dosage form.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"55 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90097248","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/AJPS.2019.70241
F. Fawzy
The H19 gene is an oncofetal RNA expressed during embryo development and in several types of cancer. However, little is known about the role of the plasma H19 in liver cancer diagnosis. The current study aimed at measuring the plasma levels of long non-coding RNAs (H19) expression in chronic liver disease (CLD) due to HCV genotype 4 infections with/without cirrhosis and Hepatocellular carcinoma (HCC) patients in an attempt to evaluate the potential benefits of these new circulating, noninvasive, diagnostic, prognostic and epigenetic markers for liver cirrhosis and carcinogenesis of Egyptian patients. A hundred subjects were included in this study, divided into two groups; Group I (50 patients) were classified into subgroup Ia (CLD without cirrhosis, n=25) and subgroup Ib (CLD with cirrhosis, n=25), Group II (CLD patients with HCC, n=25), and control (Healthy volunteer, n=25). The expression of lncRNAs (H19) genes was analyzed by Real-Time PCR. LncRNAs (H19) showed upregulation in all diseased groups, which was in consistence with the progression of the disease toward the HCC stage. In addition, H19 showed a diagnostic ability to discriminate between cases of cirrhosis and HCC compared to healthy control (p< 0.001), while it did not show a discrimination significance differences between cirrhotic cases and non cirrhotic cases. By using receiver operating characteristic curve (ROC) analysis, it was found that H19 could diagnose HCC with AUC (81.4%). The increased H19 expression was associated with advanced tumor stages and higher grades. Plasma level of H19 marker might serve as a potential non-invasive biomarker for diagnosis of HCC.
{"title":"LONG NON-CODING RNA H19 AS POTENTIAL BIOMARKER FOR HCV GENOTYPE 4 INDUCED HEPATOCELLULAR CARCINOMA PATIENTS","authors":"F. Fawzy","doi":"10.21608/AJPS.2019.70241","DOIUrl":"https://doi.org/10.21608/AJPS.2019.70241","url":null,"abstract":"The H19 gene is an oncofetal RNA expressed during embryo development and in several types of cancer. However, little is known about the role of the plasma H19 in liver cancer diagnosis. \u0000The current study aimed at measuring the plasma levels of long non-coding RNAs (H19) expression in chronic liver disease (CLD) due to HCV genotype 4 infections with/without cirrhosis and Hepatocellular carcinoma (HCC) patients in an attempt to evaluate the potential benefits of these new circulating, noninvasive, diagnostic, prognostic and epigenetic markers for liver cirrhosis and carcinogenesis of Egyptian patients. \u0000A hundred subjects were included in this study, divided into two groups; Group I (50 patients) were classified into subgroup Ia (CLD without cirrhosis, n=25) and subgroup Ib (CLD with cirrhosis, n=25), Group II (CLD patients with HCC, n=25), and control (Healthy volunteer, n=25). The expression of lncRNAs (H19) genes was analyzed by Real-Time PCR. \u0000LncRNAs (H19) showed upregulation in all diseased groups, which was in consistence with the progression of the disease toward the HCC stage. In addition, H19 showed a diagnostic ability to discriminate between cases of cirrhosis and HCC compared to healthy control (p< 0.001), while it did not show a discrimination significance differences between cirrhotic cases and non cirrhotic cases. By using receiver operating characteristic curve (ROC) analysis, it was found that H19 could diagnose HCC with AUC (81.4%). The increased H19 expression was associated with advanced tumor stages and higher grades. \u0000Plasma level of H19 marker might serve as a potential non-invasive biomarker for diagnosis of HCC.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81092788","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/ajps.2019.70245
M. El-Derany
Chronic hepatitis C (CHC) treatment modalities dramatically evolve, however some patients still suffer treatment failure with sever aggressive side effects. Accordingly personalizing antiviral treatment becomes an urgent cornerstone in treatment path. Inflammation is one of the hallmarks of viral infection. Besides it is one of the main factors interfering with drug response. Accordingly, this study focused on studying some inflammatory markers interfering with antiviral response in different CHC patients. A cohort of 157 genotype 4 (G4) Egyptian CHC patients treated with sofosbuvir (SOF), pegylated interferon-alpha-2a (Peg-IFNα-2a) plus ribavirin (RBV) were enrolled. Single nucleotide polymorphism (SNP) within chemerin gene (rs17173608) was analyzed by quantitative real-time PCR (qRT-PCR). Serum chemerin, serum IL-6 and serum alpha-fetoprotein (AFP) were analyzed by enzyme-linked immunosorbent assay (ELISA). Fibrosis grade, serum AFP, serum IL-6 and serum chemerin levels were found to be significant univariant predictors of SOF, Peg- IFNα-2a and RBV response at (p<0.01). Moreover, G/G Chemerin (rs17173608) genotype was also proved to be associated with treatment failure (OR=17.067- 95% CI =6.684-43.575- p<0.001) in Egyptian CHC G4 patients. Combining all predictors in Multiple stepwise regression analysis concluded that higher serum chemerin levels and G/G Chemerin rs17173608 genotype formulated the strongest predictive model with a significant prediction capacity expressed by area under the receiving operating curve (AUROC) 0.881(95% CI = 0.832–0.931) with specificity of 77.1%, sensitivity of 80.2% and accuracy of 78.9%. Chemerin is a vital pretreatment predictor of anti-HCV drug response as it accurately predicts SOF, Peg- IFNα-2a and RBV different outcomes in naive Egyptian CHC G4 patients.
慢性丙型肝炎(CHC)的治疗方式发生了巨大的变化，然而一些患者仍然遭受治疗失败和严重的侵袭性副作用。因此，个性化抗病毒治疗成为治疗路径中一个紧迫的基石。炎症是病毒感染的标志之一。此外，它也是影响药物反应的主要因素之一。因此，本研究的重点是研究不同CHC患者中干扰抗病毒反应的炎症标志物。157名基因型4 (G4)埃及CHC患者接受索非布韦(SOF)、聚乙二醇化干扰素α-2a (Peg-IFNα-2a)加利巴韦林(RBV)治疗。采用实时荧光定量PCR (qRT-PCR)分析趋化素基因rs17173608的单核苷酸多态性(SNP)。采用酶联免疫吸附试验(ELISA)检测血清趋化素(chemerin)、血清白细胞介素(IL-6)和甲胎蛋白(AFP)。纤维化分级、血清AFP、血清IL-6、血清趋化素水平是soff、Peg- IFNα-2a、RBV反应的单变量预测因子(p<0.01)。此外，G/G Chemerin (rs17173608)基因型也被证明与埃及CHC G4患者的治疗失败相关(OR=17.067- 95% CI =6.684-43.575- p<0.001)。多元逐步回归分析结果表明，较高的血清趋化素水平和G/G趋化素rs17173608基因型构成最强的预测模型，其预测能力为接受工作曲线下面积(AUROC) 0.881(95% CI = 0.832 ~ 0.931)，特异性为77.1%，敏感性为80.2%，准确性为78.9%。Chemerin是抗hcv药物反应的重要预处理预测因子，因为它能准确预测埃及CHC G4患者SOF、Peg- IFNα-2a和RBV的不同结局。
{"title":"CHEMERIN IS AN INDISPENSABLE PRE-TREATMENT PREDICTOR OF SOFOSBUVIR, PEGYLATED INTERFERON-ALPHA AND RIBAVIRIN OUTCOMES IN CHRONIC HEPATITIS C EGYPTIAN PATIENTS","authors":"M. El-Derany","doi":"10.21608/ajps.2019.70245","DOIUrl":"https://doi.org/10.21608/ajps.2019.70245","url":null,"abstract":"Chronic hepatitis C (CHC) treatment modalities dramatically evolve, however some patients still suffer treatment failure with sever aggressive side effects. Accordingly personalizing antiviral treatment becomes an urgent cornerstone in treatment path. Inflammation is one of the hallmarks of viral infection. Besides it is one of the main factors interfering with drug response. Accordingly, this study focused on studying some inflammatory markers interfering with antiviral response in different CHC patients. A cohort of 157 genotype 4 (G4) Egyptian CHC patients treated with sofosbuvir (SOF), pegylated interferon-alpha-2a (Peg-IFNα-2a) plus ribavirin (RBV) were enrolled. Single nucleotide polymorphism (SNP) within chemerin gene (rs17173608) was analyzed by quantitative real-time PCR (qRT-PCR). Serum chemerin, serum IL-6 and serum alpha-fetoprotein (AFP) were analyzed by enzyme-linked immunosorbent assay (ELISA). Fibrosis grade, serum AFP, serum IL-6 and serum chemerin levels were found to be significant univariant predictors of SOF, Peg- IFNα-2a and RBV response at (p<0.01). Moreover, G/G Chemerin (rs17173608) genotype was also proved to be associated with treatment failure (OR=17.067- 95% CI =6.684-43.575- p<0.001) in Egyptian CHC G4 patients. Combining all predictors in Multiple stepwise regression analysis concluded that higher serum chemerin levels and G/G Chemerin rs17173608 genotype formulated the strongest predictive model with a significant prediction capacity expressed by area under the receiving operating curve (AUROC) 0.881(95% CI = 0.832–0.931) with specificity of 77.1%, sensitivity of 80.2% and accuracy of 78.9%. Chemerin is a vital pretreatment predictor of anti-HCV drug response as it accurately predicts SOF, Peg- IFNα-2a and RBV different outcomes in naive Egyptian CHC G4 patients.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"86 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85579243","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/AJPS.2019.70240
Hany G. Ezzat
The current arsenal of antimicrobials couldn't hold back the rapid and ferocious growth of the antimicrobial resistance phenomenon. Collectively the current situation points to the pressing need to develop other effective antimicrobial agents. In the search for novel antimicrobials, phenylthiazole derivatives have recently been found to possess antibacterial activity particularly against a range of several antibiotic-resistant staphylococcus aureus strains. Modification of the nitrogenous head by incorporation the hydrolysable -HC=N- linkage within a pyrimidine ring bearing one or more hydrogen bond-promoting group led to the discovery of the second generation of phenylthiazoles, with more potent activity and longer half-lives compared to the lead compound 1a. Based on the above rationale, the objective of this study was to create a new set of structures of n-butylphenylthiazole-5-pyrimidine that contains two or more heteroatoms in their side chain and to study the relationship between the structural form of these compounds and their antimicrobial activity and spectrum against certain multi-drug resistance (MDR) strains. The new set of derivatives is designed to cover all the possibilities of side chains carbon-units distance and spatial configurations.
目前的抗菌素武器库无法阻止抗菌素耐药性现象的迅速而凶猛的增长。总的来说，目前的情况表明迫切需要开发其他有效的抗微生物药物。在寻找新型抗菌剂方面，最近发现苯噻唑衍生物具有抗菌活性，特别是对一系列耐抗生素的金黄色葡萄球菌菌株。通过在含有一个或多个氢键促进基团的嘧啶环中加入可水解的- hc =N-键，对含氮头进行修饰，发现了第二代苯噻唑，与先导化合物1a相比，具有更强的活性和更长的半衰期。基于上述理论，本研究的目的是建立一组侧链上含有两个或两个以上杂原子的正丁基苯基噻唑-5-嘧啶的新结构，并研究这些化合物的结构形式与其抗菌活性和抗多药耐药(MDR)菌株的光谱之间的关系。新的衍生物集被设计为涵盖所有可能的侧链碳单元距离和空间构型。
{"title":"SYNTHESIS AND EVALUATION OF NEW PHENYLTHIAZOLE DERVATIVES AS ANTIMICROBIAL AGENTS","authors":"Hany G. Ezzat","doi":"10.21608/AJPS.2019.70240","DOIUrl":"https://doi.org/10.21608/AJPS.2019.70240","url":null,"abstract":"The current arsenal of antimicrobials couldn't hold back the rapid and ferocious growth of the antimicrobial resistance phenomenon. Collectively the current situation points to the pressing need to develop other effective antimicrobial agents. \u0000In the search for novel antimicrobials, phenylthiazole derivatives have recently been found to possess antibacterial activity particularly against a range of several antibiotic-resistant staphylococcus aureus strains. Modification of the nitrogenous head by incorporation the hydrolysable -HC=N- linkage within a pyrimidine ring bearing one or more hydrogen bond-promoting group led to the discovery of the second generation of phenylthiazoles, with more potent activity and longer half-lives compared to the lead compound 1a. \u0000Based on the above rationale, the objective of this study was to create a new set of structures of n-butylphenylthiazole-5-pyrimidine that contains two or more heteroatoms in their side chain and to study the relationship between the structural form of these compounds and their antimicrobial activity and spectrum against certain multi-drug resistance (MDR) strains. The new set of derivatives is designed to cover all the possibilities of side chains carbon-units distance and spatial configurations.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"30 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91277844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-09-01DOI: 10.21608/ajps.2019.70246
M. Sherif
A peptic ulcer is a chronic disease. Its main features are the incompetent defense of the mucosal and the existence of the gastric juice. The two most important factors that disrupt the balance between the acid and the mucus are the Helicobacter pylori infection (H. pylori) and Non-steroidal anti-inflammatory drugs (NSAIDs). The known treatments like proton pump inhibitors (PPIs) and histamine-2 (H2) receptor antagonists have demonstrated adverse effects and various drug interactions. So the desired approach nowadays is alternative therapies and the usage of herbal products. Boswellic acids provide a potential alternative to the treatment of non-steroidal anti-inflammatory drugs induced peptic ulcer.
{"title":"ROLE OF BOSWELLIC ACID IN THE TREATMENT OF PEPTIC ULCER DISEASE","authors":"M. Sherif","doi":"10.21608/ajps.2019.70246","DOIUrl":"https://doi.org/10.21608/ajps.2019.70246","url":null,"abstract":"A peptic ulcer is a chronic disease. Its main features are the incompetent defense of the mucosal and the existence of the gastric juice. The two most important factors that disrupt the balance between the acid and the mucus are the Helicobacter pylori infection (H. pylori) and Non-steroidal anti-inflammatory drugs (NSAIDs). The known treatments like proton pump inhibitors (PPIs) and histamine-2 (H2) receptor antagonists have demonstrated adverse effects and various drug interactions. So the desired approach nowadays is alternative therapies and the usage of herbal products. Boswellic acids provide a potential alternative to the treatment of non-steroidal anti-inflammatory drugs induced peptic ulcer.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"40 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90795453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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