Bonagiri Pavani, Malothu Narender, D. Prasanth, C. Guntupalli
Background and objective For the simultaneous determination of glecaprevir (GPR) and pibrentasvir (PTR) in human plasma, a novel, accurate, and selective reversed-phase high-performance liquid chromatography method was developed and validated. Materials and methods Owing to structural resemblance, bictegravir was selected as an internal standard. Anticoagulant used was K2-EDTA. The GPR-PTR was the first of its kind approved drug by FDA for the treatment of chronic hepatitis C. Precipitation technique with acetonitrile was employed for the extraction of analyte from human plasma. Kromasil C18 column (5 μ, 150×4.6 mm) with an isocratic mobile phase of 0.1% orthophosphoric acid buffer pH 4.3, adjusted with dilute hydrochloric acid: acetonitrile in the ratio of 70 : 30 v/v, was used for the resolution. At a flow rate of 1 ml/min, the mobile phase was pumped. Using a photodiode array detector, effluents were monitored at 250 nm. Results Over concentration ranges of 5–200 μg/ml and 6.650–266.000 μg/ml, the method was found to be linear for GPR and PTR, respectively, in human plasma, with the precision and accuracy ranging from 0.76 to 9.05% and 90.55 to 98.98% for GPR respectively, whereas for PTR ranged from 0.74 to 9.52% and 91.56 to 105.61%, respectively. Conclusion The stability of the analyte was evaluated in plasma under different stress conditions.
{"title":"Development and validation of a novel bioanalytical method for the simultaneous determination of glecaprevir and pibrentasvir in human plasma using reversed-phase high-performance liquid chromatography","authors":"Bonagiri Pavani, Malothu Narender, D. Prasanth, C. Guntupalli","doi":"10.4103/epj.epj_47_22","DOIUrl":"https://doi.org/10.4103/epj.epj_47_22","url":null,"abstract":"Background and objective For the simultaneous determination of glecaprevir (GPR) and pibrentasvir (PTR) in human plasma, a novel, accurate, and selective reversed-phase high-performance liquid chromatography method was developed and validated. Materials and methods Owing to structural resemblance, bictegravir was selected as an internal standard. Anticoagulant used was K2-EDTA. The GPR-PTR was the first of its kind approved drug by FDA for the treatment of chronic hepatitis C. Precipitation technique with acetonitrile was employed for the extraction of analyte from human plasma. Kromasil C18 column (5 μ, 150×4.6 mm) with an isocratic mobile phase of 0.1% orthophosphoric acid buffer pH 4.3, adjusted with dilute hydrochloric acid: acetonitrile in the ratio of 70 : 30 v/v, was used for the resolution. At a flow rate of 1 ml/min, the mobile phase was pumped. Using a photodiode array detector, effluents were monitored at 250 nm. Results Over concentration ranges of 5–200 μg/ml and 6.650–266.000 μg/ml, the method was found to be linear for GPR and PTR, respectively, in human plasma, with the precision and accuracy ranging from 0.76 to 9.05% and 90.55 to 98.98% for GPR respectively, whereas for PTR ranged from 0.74 to 9.52% and 91.56 to 105.61%, respectively. Conclusion The stability of the analyte was evaluated in plasma under different stress conditions.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"424 - 431"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43429148","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}
Amal Aboelmaaty, M. Sayed, Mahmoud A. I. Elgabry, Mohamed Kotp, G. Fouad, M. El-Shamarka, E. Fouad, A. Soror, S. Omara
Background Silver nanoparticles (AgO-NPs) have shown antimicrobial effects against a broad spectrum of microorganisms. Objectives To assess the antimicrobial effects of AgO-NPs prepared using an eco-friendly green method against multidrug-resistant Escherichia coli in vivo after inducing endometritis in rats. Materials and methods In female mice, LD50 of AgO-NPs was determined, followed by a chronic toxicity in female rats by oral administration of 0, 20, 30, and 40 mg of AgO-NPs daily for 4 weeks. The induced endometritis model in female rats was performed by inoculating two doses of E. coli (100 μl of 10×105 CFU) intravaginally. Seven days later, vaginal swabs were stained with Wright stain to confirm the development of endometritis and used to re-isolate the inoculated microorganism. Two doses of 100 μl containing 10 mg AgO-NPs were inoculated intravaginally. Estradiol, progesterone, liver and kidney functions, oxidants and antioxidants, and zinc were measured in collected blood samples of chronic toxicity and induced endometritis model. Results and conclusion LD50 of AgO-NPs was 800 mg/kg body weight (BW). The use of 40 (1 : 20 LD50), 30 (1 : 26.67 LD50), and 20 (1 : 40 LD50) mg/kg BW during the chronic toxicity experiment was safe as indicated by blood biochemical analyses. The chronic toxicity experiment resulted in normal liver and kidney functions, oxidant–antioxidant status, acute-phase proteins, and ovarian hormones. The green method-synthesized AgO-NPs showed efficacy against E. coli-induced endometritis, and rats responded to the treatment as indicated by the uterine cytology and the clinical analysis with mild adverse effects on both liver and kidney. In conclusion, AgO-NPs showed treatment of experimental uterine infections induced by E. coli in rats and were safe for longer administration in concentrations lower than 50 mg/kg BW.
{"title":"Therapeutic effects of silver nanoparticles on Escherichia coli-induced endometritis in rats","authors":"Amal Aboelmaaty, M. Sayed, Mahmoud A. I. Elgabry, Mohamed Kotp, G. Fouad, M. El-Shamarka, E. Fouad, A. Soror, S. Omara","doi":"10.4103/epj.epj_67_22","DOIUrl":"https://doi.org/10.4103/epj.epj_67_22","url":null,"abstract":"Background Silver nanoparticles (AgO-NPs) have shown antimicrobial effects against a broad spectrum of microorganisms. Objectives To assess the antimicrobial effects of AgO-NPs prepared using an eco-friendly green method against multidrug-resistant Escherichia coli in vivo after inducing endometritis in rats. Materials and methods In female mice, LD50 of AgO-NPs was determined, followed by a chronic toxicity in female rats by oral administration of 0, 20, 30, and 40 mg of AgO-NPs daily for 4 weeks. The induced endometritis model in female rats was performed by inoculating two doses of E. coli (100 μl of 10×105 CFU) intravaginally. Seven days later, vaginal swabs were stained with Wright stain to confirm the development of endometritis and used to re-isolate the inoculated microorganism. Two doses of 100 μl containing 10 mg AgO-NPs were inoculated intravaginally. Estradiol, progesterone, liver and kidney functions, oxidants and antioxidants, and zinc were measured in collected blood samples of chronic toxicity and induced endometritis model. Results and conclusion LD50 of AgO-NPs was 800 mg/kg body weight (BW). The use of 40 (1 : 20 LD50), 30 (1 : 26.67 LD50), and 20 (1 : 40 LD50) mg/kg BW during the chronic toxicity experiment was safe as indicated by blood biochemical analyses. The chronic toxicity experiment resulted in normal liver and kidney functions, oxidant–antioxidant status, acute-phase proteins, and ovarian hormones. The green method-synthesized AgO-NPs showed efficacy against E. coli-induced endometritis, and rats responded to the treatment as indicated by the uterine cytology and the clinical analysis with mild adverse effects on both liver and kidney. In conclusion, AgO-NPs showed treatment of experimental uterine infections induced by E. coli in rats and were safe for longer administration in concentrations lower than 50 mg/kg BW.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"456 - 471"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48791873","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}
M. Elnahas, Donia H. Sheir, O. Amer, Ali El Hagrassi
Background and objectives Fungal deterioration of cultural heritage is a major problem that causes physical and chemical damage as well as esthetic alteration. In the current research, fungal species that exist on a brick sample obtained from Egyptian historical places were isolated and identified. Moreover, various metabolic products produced by the isolated fungal species were detected, which may play an important role in the deterioration of many historical buildings. Materials and methods Various fungi existing on brick samples collected from an Egyptian historical place were identified phenotypically and then confirmed molecularly based on the 18 S rDNA technique. The metabolites found in the chloroform extract of the isolated fungi were detected by gas chromatography-mass spectrometry. Quantitative mineralogical analysis of the deteriorated brick was studied by radiograph diffraction. Moreover, scanning electron microscopy-energy-dispersive radiograph was employed to identify the mineral compositions and surface structural morphology of the collected brick sample. Results and conclusion Three fungi showed the highest occurrence and were identified as Aspergillus niger, Aspergillus terreus, and Aspergillus flavus. The metabolites found in the chloroform extract of the three fungi were detected by gas chromatography-mass spectrometry, which showed that 5octadecene, (E) was common among A. niger, A. terreus, and A. flavus; nonadecane and E15heptadecenal were common between A. niger and A. flavus; αcadinol, tetradecane, and hexadecane were common between A. niger and A. terreus; and transcaryophyllene, αhumulene, taumuurolol, and octadecane were common between A. terreus and A. flavus. In addition, there was a presence of other hydrocarbons and various organic acid esters that play a vital role in the brick deterioration. Moreover, radiograph diffraction and scanning electron microscopy-energy-dispersive radiograph results showed that the brick sample contains Si, Fe, Ca, and Al, with small amounts of Na, Mg, and Cl. The fungal hyphae penetrating the brick sample were also detected. Our results demonstrate that fungi existence could result in physical deterioration by extending their hyphae through the brick pores resulting in stress. Fungi could also lead to chemical deterioration due to the production of different acids and acid derivatives that cause the brick demineralization via chelation of various metal. In addition, the production of various aliphatic and aromatic hydrocarbons by the fungi could play an important role in the deterioration process.
{"title":"Gas chromatography-mass spectrometry and scanning electron microscopy with energy-dispersive radiograph analysis of biodeteriorative metabolites produced by Aspergillus species","authors":"M. Elnahas, Donia H. Sheir, O. Amer, Ali El Hagrassi","doi":"10.4103/epj.epj_86_22","DOIUrl":"https://doi.org/10.4103/epj.epj_86_22","url":null,"abstract":"Background and objectives Fungal deterioration of cultural heritage is a major problem that causes physical and chemical damage as well as esthetic alteration. In the current research, fungal species that exist on a brick sample obtained from Egyptian historical places were isolated and identified. Moreover, various metabolic products produced by the isolated fungal species were detected, which may play an important role in the deterioration of many historical buildings. Materials and methods Various fungi existing on brick samples collected from an Egyptian historical place were identified phenotypically and then confirmed molecularly based on the 18 S rDNA technique. The metabolites found in the chloroform extract of the isolated fungi were detected by gas chromatography-mass spectrometry. Quantitative mineralogical analysis of the deteriorated brick was studied by radiograph diffraction. Moreover, scanning electron microscopy-energy-dispersive radiograph was employed to identify the mineral compositions and surface structural morphology of the collected brick sample. Results and conclusion Three fungi showed the highest occurrence and were identified as Aspergillus niger, Aspergillus terreus, and Aspergillus flavus. The metabolites found in the chloroform extract of the three fungi were detected by gas chromatography-mass spectrometry, which showed that 5octadecene, (E) was common among A. niger, A. terreus, and A. flavus; nonadecane and E15heptadecenal were common between A. niger and A. flavus; αcadinol, tetradecane, and hexadecane were common between A. niger and A. terreus; and transcaryophyllene, αhumulene, taumuurolol, and octadecane were common between A. terreus and A. flavus. In addition, there was a presence of other hydrocarbons and various organic acid esters that play a vital role in the brick deterioration. Moreover, radiograph diffraction and scanning electron microscopy-energy-dispersive radiograph results showed that the brick sample contains Si, Fe, Ca, and Al, with small amounts of Na, Mg, and Cl. The fungal hyphae penetrating the brick sample were also detected. Our results demonstrate that fungi existence could result in physical deterioration by extending their hyphae through the brick pores resulting in stress. Fungi could also lead to chemical deterioration due to the production of different acids and acid derivatives that cause the brick demineralization via chelation of various metal. In addition, the production of various aliphatic and aromatic hydrocarbons by the fungi could play an important role in the deterioration process.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"482 - 495"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44276814","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}
A. Barakat, N. Hassanain, M. Salman, Sabry A. S. Sadek, Amal Aboelmaaty, N. Rabie, H. E. El Fadaly, R. Abdelhameed
Background Foodborne diseases pose serious threats to the health of people. Escherichia coli is the most important foodborne pathogen of public health interest. Objectives To assess metal organic framework (MOF) nanoparticles with antimicrobial activity and incorporating the antibiotics onto MOFs for controlled release of antibiotics and also to solve the problem of antibiotic resistance, which is one of the most pressing issues in global public health. Materials and methods A total of 615 samples of animal and human origins were collected. Samples of poultry and poultry products (215), of meat and meat products (240), and of milk products (120), as well as stool samples from contact persons and food handlers (40) were collected from different localities in Cairo, Giza, and Qaluobya governorates during the period from October 2020 to September 2021. All samples were bacteriologically examined and morphologically characterized. The suspected isolates that have characteristics of E. coli species were identified to the serotype level. Antibiotic susceptibility testing of identified E. coli serotypes to the commonly used antibiotics in Egypt was carried out. Results and conclusion The results showed that the total percentage of E. coli spp. was 31.16%. E. coli spp. of 28, 35.7, 30, and 30% were isolated from sausage, beef, luncheon, and minced meat, respectively. E. coli spp. isolated from poultry liver, breast muscle, and wings were 35.33, 35.33, and 10%, respectively. The Karish cheese (55%) and yoghurt (35%) contained E. coli spp. Only 20% of human stool had E. coli. The total percentages of E. coli spp. in Cairo, Giza, and Qaluobya were 28.5, 39.33, and 36.66%, respectively. Serotypes identified from E. coli spp. were mainly O157 and non −O157 (O164, O26, O27, O53, O71, O95, O103, O111, O124, O125, O127, and O145). The isolated E. coli serotypes expressed high resistance to most of the used antibiotics (10/13, 76.9%) before adding nanoparticles. Three antibiotics showed the lowest resistance [imipenem (34.4%), cefotaxime (65.6%), and ceftriaxone (68.8%)] and after adding nanoparticles to the antibiotic discs, antibiotic resistance decreased to 29.5, 62.3, and 62.9%, respectively. Conclusion Regular epidemiological surveillance should be undertaken in monitoring the occurrence and distribution of E coli spp. Nanotechnology techniques can solve the problem of antibiotic resistance crisis in targeted organisms. Nanoparticles can penetrate the cell membrane of pathogenic microorganisms and interfere with important molecular pathways, formulating unique antimicrobial mechanisms. In combination with optimal antibiotics, nanoparticless have demonstrated synergy and may aid in limiting the global crisis of emerging bacterial resistance. MOF nanoparticles have antimicrobial activity, and incorporating the antibiotics onto MOFs to control the release of antibiotics helps to decrease the problem of antibiotic resistance.
{"title":"Assessment of metal organic framework as a new formulation for the treatment of main zoonotic foodborne pathogens","authors":"A. Barakat, N. Hassanain, M. Salman, Sabry A. S. Sadek, Amal Aboelmaaty, N. Rabie, H. E. El Fadaly, R. Abdelhameed","doi":"10.4103/epj.epj_93_22","DOIUrl":"https://doi.org/10.4103/epj.epj_93_22","url":null,"abstract":"Background Foodborne diseases pose serious threats to the health of people. Escherichia coli is the most important foodborne pathogen of public health interest. Objectives To assess metal organic framework (MOF) nanoparticles with antimicrobial activity and incorporating the antibiotics onto MOFs for controlled release of antibiotics and also to solve the problem of antibiotic resistance, which is one of the most pressing issues in global public health. Materials and methods A total of 615 samples of animal and human origins were collected. Samples of poultry and poultry products (215), of meat and meat products (240), and of milk products (120), as well as stool samples from contact persons and food handlers (40) were collected from different localities in Cairo, Giza, and Qaluobya governorates during the period from October 2020 to September 2021. All samples were bacteriologically examined and morphologically characterized. The suspected isolates that have characteristics of E. coli species were identified to the serotype level. Antibiotic susceptibility testing of identified E. coli serotypes to the commonly used antibiotics in Egypt was carried out. Results and conclusion The results showed that the total percentage of E. coli spp. was 31.16%. E. coli spp. of 28, 35.7, 30, and 30% were isolated from sausage, beef, luncheon, and minced meat, respectively. E. coli spp. isolated from poultry liver, breast muscle, and wings were 35.33, 35.33, and 10%, respectively. The Karish cheese (55%) and yoghurt (35%) contained E. coli spp. Only 20% of human stool had E. coli. The total percentages of E. coli spp. in Cairo, Giza, and Qaluobya were 28.5, 39.33, and 36.66%, respectively. Serotypes identified from E. coli spp. were mainly O157 and non −O157 (O164, O26, O27, O53, O71, O95, O103, O111, O124, O125, O127, and O145). The isolated E. coli serotypes expressed high resistance to most of the used antibiotics (10/13, 76.9%) before adding nanoparticles. Three antibiotics showed the lowest resistance [imipenem (34.4%), cefotaxime (65.6%), and ceftriaxone (68.8%)] and after adding nanoparticles to the antibiotic discs, antibiotic resistance decreased to 29.5, 62.3, and 62.9%, respectively. Conclusion Regular epidemiological surveillance should be undertaken in monitoring the occurrence and distribution of E coli spp. Nanotechnology techniques can solve the problem of antibiotic resistance crisis in targeted organisms. Nanoparticles can penetrate the cell membrane of pathogenic microorganisms and interfere with important molecular pathways, formulating unique antimicrobial mechanisms. In combination with optimal antibiotics, nanoparticless have demonstrated synergy and may aid in limiting the global crisis of emerging bacterial resistance. MOF nanoparticles have antimicrobial activity, and incorporating the antibiotics onto MOFs to control the release of antibiotics helps to decrease the problem of antibiotic resistance.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"515 - 525"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46633439","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}
Shimaa Mousa, abdel-hamid Haggran, T. El-Kawokgy, Zakia A. Abo El-kheir, Shadia M. Sabry, Shimaa E. Rashad
Background Cadmium (Cd) is a heavy metal that contributes to pollution in the environment. Cd intoxication can lead to diseases in the liver, kidneys, and lungs, among other organs. The liver is the primary organ affected by Cd overdose. Objective To evaluate the cytotoxic and genotoxic responses of cadmium chloride (CdCl2) on three different human cell lines and four different genotypes of yeast knockout strains. Materials and methods The effects of different concentrations of CdCl2 on cell viability in hepatocellular carcinoma (HepG2), lung cancer (A549), and normal lung cell carcinoma (Wi38) were investigated systematically using the MTT method. Moreover, flow cytometry was used to assess cell cycle arrest using propidium iodide (PI) staining and to quantify apoptotic cell death using PI staining and Annexin V/PI staining, respectively. The gene expression of p53, casp3, and Bcl-2 was measured using qRT-PCR. The Comet methodology was used to indicate DNA damage of yeast knockout strains. Results and conclusion The MTT assay revealed that CdCl2 was highly potent against hepatocellular carcinoma (HepG2), lung cancer (A549), and normal lung cell lines (Wi38) (IC50=3.12, 28.81, 191.14 μg/ml). These findings showed that CdCl2 reduced therapeutic efficacy in malignant cells at relatively low concentrations compared with nonmalignant cells, as well as confirmed the antitumor effect of the metal. CdCl2-damaged A549 cells revealed a significant increase in arrest of cell cycle in ‘S’ phases, and then apoptosis increased. Subsequently, when A549 cells were treated with a higher dosage of CdCl2, the gene expression of p53 and casp3 genes was upregulated, whereas Bcl-2 was downregulated. CdCl2 revealed its genotoxic activity at different concentrations of 10, 25, 50 μg/ml. MRE11, CLN1 and ZRC1 genes exhibited marked genotoxic effects, while MMT1 gene generated modret genotoxicity of yeast knockout strains. The Comet assay revealed that yeast cells were more responsive, which was indisputably demonstrated.
{"title":"Impact assessment of cadmium chloride on human cell lines and yeast knockout strains","authors":"Shimaa Mousa, abdel-hamid Haggran, T. El-Kawokgy, Zakia A. Abo El-kheir, Shadia M. Sabry, Shimaa E. Rashad","doi":"10.4103/epj.epj_59_22","DOIUrl":"https://doi.org/10.4103/epj.epj_59_22","url":null,"abstract":"Background Cadmium (Cd) is a heavy metal that contributes to pollution in the environment. Cd intoxication can lead to diseases in the liver, kidneys, and lungs, among other organs. The liver is the primary organ affected by Cd overdose. Objective To evaluate the cytotoxic and genotoxic responses of cadmium chloride (CdCl2) on three different human cell lines and four different genotypes of yeast knockout strains. Materials and methods The effects of different concentrations of CdCl2 on cell viability in hepatocellular carcinoma (HepG2), lung cancer (A549), and normal lung cell carcinoma (Wi38) were investigated systematically using the MTT method. Moreover, flow cytometry was used to assess cell cycle arrest using propidium iodide (PI) staining and to quantify apoptotic cell death using PI staining and Annexin V/PI staining, respectively. The gene expression of p53, casp3, and Bcl-2 was measured using qRT-PCR. The Comet methodology was used to indicate DNA damage of yeast knockout strains. Results and conclusion The MTT assay revealed that CdCl2 was highly potent against hepatocellular carcinoma (HepG2), lung cancer (A549), and normal lung cell lines (Wi38) (IC50=3.12, 28.81, 191.14 μg/ml). These findings showed that CdCl2 reduced therapeutic efficacy in malignant cells at relatively low concentrations compared with nonmalignant cells, as well as confirmed the antitumor effect of the metal. CdCl2-damaged A549 cells revealed a significant increase in arrest of cell cycle in ‘S’ phases, and then apoptosis increased. Subsequently, when A549 cells were treated with a higher dosage of CdCl2, the gene expression of p53 and casp3 genes was upregulated, whereas Bcl-2 was downregulated. CdCl2 revealed its genotoxic activity at different concentrations of 10, 25, 50 μg/ml. MRE11, CLN1 and ZRC1 genes exhibited marked genotoxic effects, while MMT1 gene generated modret genotoxicity of yeast knockout strains. The Comet assay revealed that yeast cells were more responsive, which was indisputably demonstrated.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"447 - 455"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46404755","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}
Background Antibiotic resistance is a global problem that has aggravated recently to threaten humans, cattle, and crops. This has inspired scientists to examine various natural products, herbs, and plants that have been used since antiquity for their valuable medicinal potential. They have not only proven less likelihood to produce resistant strains but also exert a positive effect on beneficial probiotics boosting the general health status of the host. Objective To identify the major multiple-drug-resistant bacteria underlying diabetic foot ulcer infections and screen and select herbs and natural extracts, commonly available in local herbal stores, for their activity against the isolated bacteria. Material and methods Bacteria isolated from diabetic foot ulcers of hospitalized patients were identified according to their morphological and biochemical properties. The isolated strains were tested against extracts of bitter melon, honey, pomegranate peel, myrrh gum, and turmeric powder using the in vitro agar well-diffusion assay technique. Results and conclusion The bacterial isolates were resistant to all of the tested standard antibiotics and identified to belong to five different genera: Gram positive bacteria Staphylococcus aureus and Streptococcus pyogenes and Gram negative bacteria Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. All of the natural preparations exerted different levels of antibacterial activity except for bitter melon. These findings shed tremendous light on the up-till-now promising effect of the natural antibiotics arsenal and necessitate the importance of systemically studying their individual and synergistic mechanisms, interactions, and kinetics.
{"title":"Antibacterial efficiency of natural products against multiple-drug-resistant clinical isolates","authors":"Dina E El-Ghwas, H. Yehia","doi":"10.4103/epj.epj_48_22","DOIUrl":"https://doi.org/10.4103/epj.epj_48_22","url":null,"abstract":"Background Antibiotic resistance is a global problem that has aggravated recently to threaten humans, cattle, and crops. This has inspired scientists to examine various natural products, herbs, and plants that have been used since antiquity for their valuable medicinal potential. They have not only proven less likelihood to produce resistant strains but also exert a positive effect on beneficial probiotics boosting the general health status of the host. Objective To identify the major multiple-drug-resistant bacteria underlying diabetic foot ulcer infections and screen and select herbs and natural extracts, commonly available in local herbal stores, for their activity against the isolated bacteria. Material and methods Bacteria isolated from diabetic foot ulcers of hospitalized patients were identified according to their morphological and biochemical properties. The isolated strains were tested against extracts of bitter melon, honey, pomegranate peel, myrrh gum, and turmeric powder using the in vitro agar well-diffusion assay technique. Results and conclusion The bacterial isolates were resistant to all of the tested standard antibiotics and identified to belong to five different genera: Gram positive bacteria Staphylococcus aureus and Streptococcus pyogenes and Gram negative bacteria Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. All of the natural preparations exerted different levels of antibacterial activity except for bitter melon. These findings shed tremendous light on the up-till-now promising effect of the natural antibiotics arsenal and necessitate the importance of systemically studying their individual and synergistic mechanisms, interactions, and kinetics.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"432 - 439"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45750090","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}
Safaa Omran, E. Shoukry, Eman E. Mohamed, E. Khaled, R. El-Attar
Background and objectives A simple and sensitive enzymatic potentiometric biosensor has been developed for toxicological studies of anticholinesterase drugs based on their inhibitory effect on cholinesterase activity. To verify the applicability, eight pharmaceutical formulations for Alzheimer′s treatment were assayed, namely rivastigmine, pyridostigmine, cyclopentolate, memantine, meclofenoxate, carbamazepine, oxfendazole, and methotrexate. Materials and methods Disposable screen-printed potentiometric sensors were utilized for monitoring the cholinesterase activity. The reaction conditions including the optimal enzyme substrate, incubation periods, and the linearity range for each drug were optimized for each drug. Results and conclusion Different sensitivities within subnanogram levels were reported based on the inhibitory effect of the aforementioned pharmaceutical compounds and their LD50 value. The proposed method showed improved sensitivity for the investigated compounds compared with their reported electroanalytical approaches. The introduced analysis protocol was successfully utilized for assaying the cited drugs in their pharmaceutical and environmental samples using a portable measuring system. Moreover, the toxicity of the pharmaceutical compounds against in-vitro cholinesterase enzymes studies can be performed with simple instrumentation requirements.
{"title":"Novel simple enzymatic potentiometric approach for toxicological assessment of anticholinesterase and Alzheimer’s drugs Enzymatic approach toxicological assessment","authors":"Safaa Omran, E. Shoukry, Eman E. Mohamed, E. Khaled, R. El-Attar","doi":"10.4103/epj.epj_80_22","DOIUrl":"https://doi.org/10.4103/epj.epj_80_22","url":null,"abstract":"Background and objectives A simple and sensitive enzymatic potentiometric biosensor has been developed for toxicological studies of anticholinesterase drugs based on their inhibitory effect on cholinesterase activity. To verify the applicability, eight pharmaceutical formulations for Alzheimer′s treatment were assayed, namely rivastigmine, pyridostigmine, cyclopentolate, memantine, meclofenoxate, carbamazepine, oxfendazole, and methotrexate. Materials and methods Disposable screen-printed potentiometric sensors were utilized for monitoring the cholinesterase activity. The reaction conditions including the optimal enzyme substrate, incubation periods, and the linearity range for each drug were optimized for each drug. Results and conclusion Different sensitivities within subnanogram levels were reported based on the inhibitory effect of the aforementioned pharmaceutical compounds and their LD50 value. The proposed method showed improved sensitivity for the investigated compounds compared with their reported electroanalytical approaches. The introduced analysis protocol was successfully utilized for assaying the cited drugs in their pharmaceutical and environmental samples using a portable measuring system. Moreover, the toxicity of the pharmaceutical compounds against in-vitro cholinesterase enzymes studies can be performed with simple instrumentation requirements.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"472 - 481"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43073165","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}
A. Abdou, N. Taha, Ahmed A. El-Ashmawy, Ebtesam W. Elsayed, K. Mahmoud, L. Emara
Background Conventional dosage forms of oral hypoglycemic drugs, including gliclazide (GLZ), may have a number of limitations, reducing their bioavailability. Thus, efforts are directed to design novel modified-release (MR) dosage forms for these drugs. The possible role of orally administered GLZ-MR multiparticulates in the treatment of hyperglycemia as well as improvement of impaired wound healing associated with type 2 diabetes mellitus was investigated. Objective This study aimed to evaluate the pharmacodynamics (PD) of GLZ-MR multiparticulate system against Diamicron MR tablets in nondiabetic (healthy) and streptozotocin-induced diabetic rats, by measuring blood glucose levels. For the first time, the hypothetical wound-healing capabilities of multiple doses of both treatments in diabetic rats were also studied by evaluating the wound diameter and histology. Materials and methods Novel cross-linked freeze-dried GLZ-alginate-gelatin beads were prepared. Two GLZ treatments at 4 mg/kg [test (T, MR beads) and reference (R, Diamicron MR 30 mg)] were administered to rats. A single-dose PD study was carried out on both healthy and diabetic rats, whereas the multiple-dose study was evaluated in diabetic rats. A single-dose pharmacokinetics (PK) study was conducted for assessment of the PK-PD relationship in healthy rats. Results and conclusion The single-dose study on nondiabetic rats showed that T beads exhibited a greater magnitude of blood glucose level reduction, with 1.5-fold increase in Cmax, compared with R. A direct linear relationship with high correlation was detected between GLZ glucose-lowering effect and its PK parameters, only for T beads. Multiple dosing of T beads was more efficient than R in managing hyperglycemia of wounded diabetic rats. T beads allowed almost complete wound closure, after multiple dosing for 17 days. The proposed GLZ beads could provide a promising therapeutic prospect for managing hyperglycemia as well as resolving impairment of wound healing associated with diabetes.
{"title":"Pharmacodynamic assessment of gliclazide multiparticulate system: single-dose and multiple-dose studies","authors":"A. Abdou, N. Taha, Ahmed A. El-Ashmawy, Ebtesam W. Elsayed, K. Mahmoud, L. Emara","doi":"10.4103/epj.epj_46_22","DOIUrl":"https://doi.org/10.4103/epj.epj_46_22","url":null,"abstract":"Background Conventional dosage forms of oral hypoglycemic drugs, including gliclazide (GLZ), may have a number of limitations, reducing their bioavailability. Thus, efforts are directed to design novel modified-release (MR) dosage forms for these drugs. The possible role of orally administered GLZ-MR multiparticulates in the treatment of hyperglycemia as well as improvement of impaired wound healing associated with type 2 diabetes mellitus was investigated. Objective This study aimed to evaluate the pharmacodynamics (PD) of GLZ-MR multiparticulate system against Diamicron MR tablets in nondiabetic (healthy) and streptozotocin-induced diabetic rats, by measuring blood glucose levels. For the first time, the hypothetical wound-healing capabilities of multiple doses of both treatments in diabetic rats were also studied by evaluating the wound diameter and histology. Materials and methods Novel cross-linked freeze-dried GLZ-alginate-gelatin beads were prepared. Two GLZ treatments at 4 mg/kg [test (T, MR beads) and reference (R, Diamicron MR 30 mg)] were administered to rats. A single-dose PD study was carried out on both healthy and diabetic rats, whereas the multiple-dose study was evaluated in diabetic rats. A single-dose pharmacokinetics (PK) study was conducted for assessment of the PK-PD relationship in healthy rats. Results and conclusion The single-dose study on nondiabetic rats showed that T beads exhibited a greater magnitude of blood glucose level reduction, with 1.5-fold increase in Cmax, compared with R. A direct linear relationship with high correlation was detected between GLZ glucose-lowering effect and its PK parameters, only for T beads. Multiple dosing of T beads was more efficient than R in managing hyperglycemia of wounded diabetic rats. T beads allowed almost complete wound closure, after multiple dosing for 17 days. The proposed GLZ beads could provide a promising therapeutic prospect for managing hyperglycemia as well as resolving impairment of wound healing associated with diabetes.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"411 - 423"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43459080","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}
Karishma, Sonam Kohli, M. Rajeesh, Usha Balan, B. Choudhury, Henston DSouza
Background Managing difficult and uncooperative pediatric dental patients is a challenging task. Conscious sedation has been propagated as a pharmacological means for handling such situations. Objective To evaluate the effects of sedation using nitrous oxide-oxygen inhalation versus oral midazolam-promethazine in pediatric patients. Patients and methods A total of 100 pediatric patients were selected and divided into two equal categories: group 1 (midazolam-promethazine) and group 2 (N2O-O2). Ethical committee approval was obtained, and patients were assessed. Data collected were analyzed using an unpaired t test. Results Duration of sedation was found to be statistically significant, and a higher duration was found for group 1. No significant differences were noted in the behavior rating scale with either of the combinations and in pulse oximeter readings. Conclusion Midazolam/promethazine is better in inducing longer sedation than N2O/O2.
{"title":"Efficacy of nitrous oxide-oxygen inhalation versus oral midazolam-promethazine as sedative agents in pediatric patients: a comparative study","authors":"Karishma, Sonam Kohli, M. Rajeesh, Usha Balan, B. Choudhury, Henston DSouza","doi":"10.4103/epj.epj_78_22","DOIUrl":"https://doi.org/10.4103/epj.epj_78_22","url":null,"abstract":"Background Managing difficult and uncooperative pediatric dental patients is a challenging task. Conscious sedation has been propagated as a pharmacological means for handling such situations. Objective To evaluate the effects of sedation using nitrous oxide-oxygen inhalation versus oral midazolam-promethazine in pediatric patients. Patients and methods A total of 100 pediatric patients were selected and divided into two equal categories: group 1 (midazolam-promethazine) and group 2 (N2O-O2). Ethical committee approval was obtained, and patients were assessed. Data collected were analyzed using an unpaired t test. Results Duration of sedation was found to be statistically significant, and a higher duration was found for group 1. No significant differences were noted in the behavior rating scale with either of the combinations and in pulse oximeter readings. Conclusion Midazolam/promethazine is better in inducing longer sedation than N2O/O2.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"526 - 530"},"PeriodicalIF":0.0,"publicationDate":"2022-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47058306","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}
Objectives Chitosan is a natural biopolymer that possesses various biological activities. The aim of the current study was to evaluate the potentiality of chitosan and its enzymatically depolymerized products as anticonvulsants. Materials and methods In the current study, chitosan enzymatic depolymerization was carried out using Bacillus cereus chitosanase followed by fractionation of the produced chitooligosaccharides. Phase I anticonvulsant activity of chitosan as well as its enzymatically depolymerized products was evaluated using pentylenetetrazole-induced seizures, maximal electric shock, and neurotoxicity tests. In phase II, median effective dose, median toxic dose, and protective index were determined. In addition, γ-aminobutyric acid brain level and acute toxicity were evaluated. Results and conclusion The results indicated that the fraction with the lower degree of acetylation and longer chains of glucosamine (COSH) possessed rapid onset of action with the highest protection (75%) at 0.5 h and long-acting effect for 4 h. In addition, the median effective dose of COSH was 12.7-fold more potent than the reference ethosuximide, whereas in the maximal electric shock test, COSH showed lower potency than phenytoin. The median toxic dose was 1.4-fold and 7.9-fold higher than ethosuximide and phenytoin, respectively. The protective index was 18.1-fold and 3.98-fold higher than ethosuximide and phenytoin, respectively, with a significant increase in γ-aminobutyric acid neurotransmitter brain level. In an attempt to prolong the anticonvulsant effect of COSH, a nano-formulation was carried out in which the particle size was estimated as 188.7±0.26 nm. After that, an equivalent dose of a combined treatment of COSH and the nanoformula (each 15 mg/kg) was evaluated in which a prolonged effect was achieved up to 24 h.
{"title":"Investigation of chitosan, its depolymerized products, and nanoformulation as novel anticonvulsants","authors":"M. Aboutabl, Bahgat Fayed, S. Ismail","doi":"10.4103/epj.epj_58_22","DOIUrl":"https://doi.org/10.4103/epj.epj_58_22","url":null,"abstract":"Objectives Chitosan is a natural biopolymer that possesses various biological activities. The aim of the current study was to evaluate the potentiality of chitosan and its enzymatically depolymerized products as anticonvulsants. Materials and methods In the current study, chitosan enzymatic depolymerization was carried out using Bacillus cereus chitosanase followed by fractionation of the produced chitooligosaccharides. Phase I anticonvulsant activity of chitosan as well as its enzymatically depolymerized products was evaluated using pentylenetetrazole-induced seizures, maximal electric shock, and neurotoxicity tests. In phase II, median effective dose, median toxic dose, and protective index were determined. In addition, γ-aminobutyric acid brain level and acute toxicity were evaluated. Results and conclusion The results indicated that the fraction with the lower degree of acetylation and longer chains of glucosamine (COSH) possessed rapid onset of action with the highest protection (75%) at 0.5 h and long-acting effect for 4 h. In addition, the median effective dose of COSH was 12.7-fold more potent than the reference ethosuximide, whereas in the maximal electric shock test, COSH showed lower potency than phenytoin. The median toxic dose was 1.4-fold and 7.9-fold higher than ethosuximide and phenytoin, respectively. The protective index was 18.1-fold and 3.98-fold higher than ethosuximide and phenytoin, respectively, with a significant increase in γ-aminobutyric acid neurotransmitter brain level. In an attempt to prolong the anticonvulsant effect of COSH, a nano-formulation was carried out in which the particle size was estimated as 188.7±0.26 nm. After that, an equivalent dose of a combined treatment of COSH and the nanoformula (each 15 mg/kg) was evaluated in which a prolonged effect was achieved up to 24 h.","PeriodicalId":11568,"journal":{"name":"Egyptian Pharmaceutical Journal","volume":"21 1","pages":"385 - 394"},"PeriodicalIF":0.0,"publicationDate":"2022-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49043109","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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