Pub Date : 2019-06-01DOI: 10.21608/aps.2019.13058.1005
M. Ghany, O. Abdel-Aziz, N. Fares, Eman Wafik Eskander
The present study describes accurate and sensitive stability-indicating spectrophotometric methods for the determination of Milnacipran HCl in presence of its acid, base degradates, and Duloxetine HCl in presence of its base degradates; including Dual-wavelength, Ratio difference, and Ratio derivative techniques. The developed methods were validated according to the International Conference on Harmonisation (ICH) guidelines. The recovery percentage of Milnacipran HCl and Duloxetine HCl were found to be in the ranges 99.42-100.42% and 100.17-100.3%, respectively. The low relative standard deviation of precision results confirms the suitability of the proposed methods for the estimation of the studied drugs in pure form, laboratory-prepared mixtures, and pharmaceutical formulations. Statistical comparison of the proposed methods with the reported methods revealed that there were no significant differences concerning the accuracy and precision of the adopted techniques. Validation studies demonstrated that the proposed methods are easy, specific, and rapid for the determination of Milnacipran HCl and Duloxetine HCl.
{"title":"Stability-Indicating Spectrophotometric Methods for Determination of Milnacipran HCl and Duloxetine HCl in Bulk Drug and Pharmaceutical Formulations","authors":"M. Ghany, O. Abdel-Aziz, N. Fares, Eman Wafik Eskander","doi":"10.21608/aps.2019.13058.1005","DOIUrl":"https://doi.org/10.21608/aps.2019.13058.1005","url":null,"abstract":"The present study describes accurate and sensitive stability-indicating spectrophotometric methods for the determination of Milnacipran HCl in presence of its acid, base degradates, and Duloxetine HCl in presence of its base degradates; including Dual-wavelength, Ratio difference, and Ratio derivative techniques. The developed methods were validated according to the International Conference on Harmonisation (ICH) guidelines. The recovery percentage of Milnacipran HCl and Duloxetine HCl were found to be in the ranges 99.42-100.42% and 100.17-100.3%, respectively. The low relative standard deviation of precision results confirms the suitability of the proposed methods for the estimation of the studied drugs in pure form, laboratory-prepared mixtures, and pharmaceutical formulations. Statistical comparison of the proposed methods with the reported methods revealed that there were no significant differences concerning the accuracy and precision of the adopted techniques. Validation studies demonstrated that the proposed methods are easy, specific, and rapid for the determination of Milnacipran HCl and Duloxetine HCl.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83274876","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 : 2019-06-01DOI: 10.21608/aps.2019.14995.1006
H. Ibrahim, Deena S. Lasheen, Rabah A T Serya, D. Abu-ELElla
Apoptosis is a normal physiological process which is very crucial to maintain tissue homeostasis. Dysregulated apoptosis can lead to various diseases as cancer. Thus, evasion of apoptosis stands out as a key hallmark of cancer cells. Bcl-2 family of proteins is the key modulator of the mitochondrial apoptotic pathway. Therefore, the balance between the anti-apoptotic (BCL-2, BCL-XL and MCL-1) and pro-apoptotic (BAK, BAX, BAD, PUMA and NOXA) members of this family will govern cell fate. Overexpression of anti-apoptotic BCL-2 members including MCL-1 is implicated in the progression of many human cancers as well as the emerging resistance to various anti-cancer agents including targeted therapies. Indeed, inhibition of the anti-apoptotic BCL-2 members by small molecule BH3 mimetics may provide an excellent approach in cancer therapy. Unfortunately, it was reported that MCL-1 overexpression is linked to Venetoclax, first FDA approved BCL-2 selective inhibitor, resistance in AML. Thus, inhibition of MCL-1 with a selective small molecule inhibitor may provide an attractive strategy in cancer targeted therapy. Recently, several small molecule MCL-1 selective inhibitors have been developed and few are testing in clinical trials. Herein, we will discuss the recent advances in the development of selective small molecule MCL-1 inhibitors.
{"title":"Selective Small Molecule Myeloid Cell Leukemia-1 (MCL-1) Inhibitors: Novel Agents in Cancer Therapy","authors":"H. Ibrahim, Deena S. Lasheen, Rabah A T Serya, D. Abu-ELElla","doi":"10.21608/aps.2019.14995.1006","DOIUrl":"https://doi.org/10.21608/aps.2019.14995.1006","url":null,"abstract":"Apoptosis is a normal physiological process which is very crucial to maintain tissue homeostasis. Dysregulated apoptosis can lead to various diseases as cancer. Thus, evasion of apoptosis stands out as a key hallmark of cancer cells. Bcl-2 family of proteins is the key modulator of the mitochondrial apoptotic pathway. Therefore, the balance between the anti-apoptotic (BCL-2, BCL-XL and MCL-1) and pro-apoptotic (BAK, BAX, BAD, PUMA and NOXA) members of this family will govern cell fate. Overexpression of anti-apoptotic BCL-2 members including MCL-1 is implicated in the progression of many human cancers as well as the emerging resistance to various anti-cancer agents including targeted therapies. Indeed, inhibition of the anti-apoptotic BCL-2 members by small molecule BH3 mimetics may provide an excellent approach in cancer therapy. Unfortunately, it was reported that MCL-1 overexpression is linked to Venetoclax, first FDA approved BCL-2 selective inhibitor, resistance in AML. Thus, inhibition of MCL-1 with a selective small molecule inhibitor may provide an attractive strategy in cancer targeted therapy. Recently, several small molecule MCL-1 selective inhibitors have been developed and few are testing in clinical trials. Herein, we will discuss the recent advances in the development of selective small molecule MCL-1 inhibitors.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88236341","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 : 2019-06-01DOI: 10.21608/aps.2019.15746.1008
Safaa A Hafez, Samir Othman, H. Ibrahim, A. Seida, N. Ayoub
A review of chemical constituents and pharmacological activities of genus Cassia, Family Leguminosae has been presented. There are about 600 species of this genus distributed all around the world. Many of these species are still not investigated. Hence, an attempt is made to present a review on the phytochemical and biological studies of Cassia species that remain a potential source for new natural pharmacologically active components.
{"title":"Chemical Constituents and Biological Activities of Cassia Genus: Review","authors":"Safaa A Hafez, Samir Othman, H. Ibrahim, A. Seida, N. Ayoub","doi":"10.21608/aps.2019.15746.1008","DOIUrl":"https://doi.org/10.21608/aps.2019.15746.1008","url":null,"abstract":"A review of chemical constituents and pharmacological activities of genus Cassia, Family Leguminosae has been presented. There are about 600 species of this genus distributed all around the world. Many of these species are still not investigated. Hence, an attempt is made to present a review on the phytochemical and biological studies of Cassia species that remain a potential source for new natural pharmacologically active components.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87628559","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 : 2019-06-01DOI: 10.21608/aps.2019.16625.1010
M. A. Shalaby, Eman M. E. Dokla, Rabah A T Serya, K. Abouzid
The antibiotic resistance of methicillin-resistant Staphylococcus aureus (MRSA) is attributable to the expression of the high molecular mass transpeptidase enzyme, penicillin-binding protein 2a (PBP2a), an enzyme that catalyzes the cross-linking reaction step in the cell wall biosynthesis in the face of the challenge by β-lactam antibiotics. In the current study, ten pyrazole and benzimidazole based-compounds were designed, synthesized, and evaluated as anti-MRSA agents. These derivatives were screened for their antibacterial activity against two Staphylococcus (S.) aureus strains; methicillin-sensitive Staphylococcus aureus (MSSA) ATTC6538 and MRSA USA300 strains. Three of the tested compounds (XII, XIII, and XIV) exhibited moderate bactericidal activity against MSSA, MRSA, and vancomycin-resistant Staphylococcus aureus (VRSA) strains. Docking of these compounds into the allosteric site of PBP2a showed comparable binding modes to that of the lead quinazolinone PBP2a inhibitors suggesting a similar mode of action. The present study presents a promising candidate for further optimization as a potential PBP2a inhibitor targeting MRSA infection.
{"title":"Identification of novel pyrazole and benzimidazole based derivatives as PBP2a inhibitors: Design, synthesis, and biological evaluation","authors":"M. A. Shalaby, Eman M. E. Dokla, Rabah A T Serya, K. Abouzid","doi":"10.21608/aps.2019.16625.1010","DOIUrl":"https://doi.org/10.21608/aps.2019.16625.1010","url":null,"abstract":"The antibiotic resistance of methicillin-resistant Staphylococcus aureus (MRSA) is attributable to the expression of the high molecular mass transpeptidase enzyme, penicillin-binding protein 2a (PBP2a), an enzyme that catalyzes the cross-linking reaction step in the cell wall biosynthesis in the face of the challenge by β-lactam antibiotics. In the current study, ten pyrazole and benzimidazole based-compounds were designed, synthesized, and evaluated as anti-MRSA agents. These derivatives were screened for their antibacterial activity against two Staphylococcus (S.) aureus strains; methicillin-sensitive Staphylococcus aureus (MSSA) ATTC6538 and MRSA USA300 strains. Three of the tested compounds (XII, XIII, and XIV) exhibited moderate bactericidal activity against MSSA, MRSA, and vancomycin-resistant Staphylococcus aureus (VRSA) strains. Docking of these compounds into the allosteric site of PBP2a showed comparable binding modes to that of the lead quinazolinone PBP2a inhibitors suggesting a similar mode of action. The present study presents a promising candidate for further optimization as a potential PBP2a inhibitor targeting MRSA infection.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73549417","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 : 2019-06-01DOI: 10.21608/aps.2019.17391.1014
Salma M Abdelaziz, K. Aboshanab, M. Yassien, N. Hassouna
Resistance of Staphylococcus (S.) aureus to the currently used antimicrobials has risen dramatically in the past years creating a medical challenge as therapeutic options became very limited. This study aimed to screen and detect the prevalence of some antimicrobial-resistant genes of S. aureus clinical isolates recovered from patients suffering lower respiratory tract infections (LRTI) in Egypt. A total of 231 bacterial isolates were recovered from sputum and bronchoalveolar lavage specimens obtained from patients with LRTI. Thirty-seven isolates (16%) were identified as S. aureus where seventeen isolates (46%) showed resistance to ten or more antimicrobials. The antimicrobial susceptibility testing revealed that all the tested isolates were sensitive to vancomycin and linezolid (0%), however, the lowest resistance was observed to doxycycline (3%), and the highest resistance was observed to ciprofloxacin (51%). Sixteen isolates (43%) were found resistant to cefoxitin and harbored the mecA gene (100%). However, the mepA gene was detected in only 12 isolates (75%). Extended-spectrum β-lactamase (ESBL) including, ctx-m, shv and tem and the aac(6’)-Ib genes, were detected in 10 (62%) and 8 (50%) isolates, respectively. None of the carbapenem-resistant genes including kpc, imp, vim, ndm, and oxa, were detected in any isolate. Multiple drug resistance (MDR) is a major health concern limiting the use of common antimicrobials in therapy. Thus, new national guidelines, as well as infection control strategies including antibiotic stewardship, must be implemented in the Egyptian hospitals to limit further spread of antimicrobial resistance.
{"title":"Antimicrobial resistance patterns of MDR Staphylococcus aureus clinical isolates involved in the lower respiratory tract infections in Egypt","authors":"Salma M Abdelaziz, K. Aboshanab, M. Yassien, N. Hassouna","doi":"10.21608/aps.2019.17391.1014","DOIUrl":"https://doi.org/10.21608/aps.2019.17391.1014","url":null,"abstract":"Resistance of Staphylococcus (S.) aureus to the currently used antimicrobials has risen dramatically in the past years creating a medical challenge as therapeutic options became very limited. This study aimed to screen and detect the prevalence of some antimicrobial-resistant genes of S. aureus clinical isolates recovered from patients suffering lower respiratory tract infections (LRTI) in Egypt. A total of 231 bacterial isolates were recovered from sputum and bronchoalveolar lavage specimens obtained from patients with LRTI. Thirty-seven isolates (16%) were identified as S. aureus where seventeen isolates (46%) showed resistance to ten or more antimicrobials. The antimicrobial susceptibility testing revealed that all the tested isolates were sensitive to vancomycin and linezolid (0%), however, the lowest resistance was observed to doxycycline (3%), and the highest resistance was observed to ciprofloxacin (51%). Sixteen isolates (43%) were found resistant to cefoxitin and harbored the mecA gene (100%). However, the mepA gene was detected in only 12 isolates (75%). Extended-spectrum β-lactamase (ESBL) including, ctx-m, shv and tem and the aac(6’)-Ib genes, were detected in 10 (62%) and 8 (50%) isolates, respectively. None of the carbapenem-resistant genes including kpc, imp, vim, ndm, and oxa, were detected in any isolate. Multiple drug resistance (MDR) is a major health concern limiting the use of common antimicrobials in therapy. Thus, new national guidelines, as well as infection control strategies including antibiotic stewardship, must be implemented in the Egyptian hospitals to limit further spread of antimicrobial resistance.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84891616","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}
Yomna N. Elkholy, W. Elkhatib, K. Aboshanab, M. Aboulwafa, N. Hassouna
Streptomyces manipurensis isolate H21 was recovered from a soil sample in Cairo, Egypt. Cell-free culture supernatant of Streptomyces manipurensis isolate H21 previously showed antifungal and broad-spectrum antibacterial activity against some Gram-positive, Gram-negative, MDR, and ESBL producer pathogens as well as some reference strains. The present study aimed at investigating antimicrobial and cytotoxic activities of its crude methanolic extract. The antibacterial activity of the crude methanolic extract was determined using broth-dilution method against Staphylococcus aureus ATCC 43300, Klebsiella oxytoca ATCC 700324, Klebsiella pneumoniae ATCC 700603, Klebsiella pneumoniae ATCC BAA-1705 and 2 MDR uropathogens. The minimum inhibitory concentrations (MICs) and the minimum bactericidal concentrations (MBCs) of the crude extract against the tested bacteria were in the range of 5-10 mg/mL and 10 mg/mL, respectively. The results revealed that the CD50 value of the extract was 1.17 mg/mL, against Caco-2 cell line, indicating in vitro safety and low cytotoxicity. Accordingly, Streptomyces manipurensis isolate H21 would be an excellent source of relatively safe and potent antibacterial agent.
{"title":"Evaluation of antimicrobial activity and in vitro safety of the methanolic extract of Streptomyces manipurensis soil isolate H21 for potential industrial applications","authors":"Yomna N. Elkholy, W. Elkhatib, K. Aboshanab, M. Aboulwafa, N. Hassouna","doi":"10.21608/APS.2019.20201","DOIUrl":"https://doi.org/10.21608/APS.2019.20201","url":null,"abstract":"Streptomyces manipurensis isolate H21 was recovered from a soil sample in Cairo, Egypt. Cell-free culture supernatant of Streptomyces manipurensis isolate H21 previously showed antifungal and broad-spectrum antibacterial activity against some Gram-positive, Gram-negative, MDR, and ESBL producer pathogens as well as some reference strains. The present study aimed at investigating antimicrobial and cytotoxic activities of its crude methanolic extract. The antibacterial activity of the crude methanolic extract was determined using broth-dilution method against Staphylococcus aureus ATCC 43300, Klebsiella oxytoca ATCC 700324, Klebsiella pneumoniae ATCC 700603, Klebsiella pneumoniae ATCC BAA-1705 and 2 MDR uropathogens. The minimum inhibitory concentrations (MICs) and the minimum bactericidal concentrations (MBCs) of the crude extract against the tested bacteria were in the range of 5-10 mg/mL and 10 mg/mL, respectively. The results revealed that the CD50 value of the extract was 1.17 mg/mL, against Caco-2 cell line, indicating in vitro safety and low cytotoxicity. Accordingly, Streptomyces manipurensis isolate H21 would be an excellent source of relatively safe and potent antibacterial agent.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75280005","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}
Cancer is a genetic disease characterized by two features: unregulated cell growth and tissue invasion (metastasis). It can be viewed as the result of a succession of genetic changes during which a normal cell is transformed into a malignant one. Evasion of cell death, apoptosis, is one of the essential changes in a cell that cause this malignant transformation. Hence, reduced apoptosis or its resistance plays a vital role in carcinogenesis. The Bcl-2 family of proteins regulates the mitochondrial apoptotic pathway. Disease states arise upon deregulation of the Bcl-2 family of proteins, where cell death is either promoted or evaded; one of the most common tactic cancer cells utilize to promote survival is anti-apoptotic protein overexpression. Specifically, Bcl-2 overexpression has been shown to be a major chemoresistance factor in a number of human cancers, and for this reason, Bcl-2 targeting is a pharmacologic priority in the quest to reactivate cell death for therapeutic benefit in cancer.
{"title":"Apoptosis in cancer: from pathogenesis to discovery of advanced selective Bcl-2 family inhibitors","authors":"Samaa Abbas, N. Abdou, Deena S. Lasheen, D. Ella","doi":"10.21608/APS.2019.20225","DOIUrl":"https://doi.org/10.21608/APS.2019.20225","url":null,"abstract":"Cancer is a genetic disease characterized by two features: unregulated cell growth and tissue invasion (metastasis). It can be viewed as the result of a succession of genetic changes during which a normal cell is transformed into a malignant one. Evasion of cell death, apoptosis, is one of the essential changes in a cell that cause this malignant transformation. Hence, reduced apoptosis or its resistance plays a vital role in carcinogenesis. The Bcl-2 family of proteins regulates the mitochondrial apoptotic pathway. Disease states arise upon deregulation of the Bcl-2 family of proteins, where cell death is either promoted or evaded; one of the most common tactic cancer cells utilize to promote survival is anti-apoptotic protein overexpression. Specifically, Bcl-2 overexpression has been shown to be a major chemoresistance factor in a number of human cancers, and for this reason, Bcl-2 targeting is a pharmacologic priority in the quest to reactivate cell death for therapeutic benefit in cancer.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84594337","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}
Nada A. Abdelrazek, W. Elkhatib, M. Raafat, M. Aboulwafa
L-asparaginase, also known as amidohydrolase, catalyzes the breakdown of asparagine into aspartic acid and ammonia. Due to its ability to inhibit the biosynthesis of protein lymphoblasts, it is used to treat acute lymphoblastic leukemia (ALL). It also has other applications in the food industry by preventing the formation of acrylamide. Different organisms including bacteria, fungi, actinomycetes, and plants produce L-asparaginase. This review highlights different applications of L-asparaginase in the industrial fields, the major sources of L-asparaginase, its immunological reactions and production techniques through the solid state (SSF) and submerged (SmF) fermentation as well as optimization of the production process.
l -天冬酰胺酶，也被称为氨基水解酶，催化天冬酰胺分解成天冬氨酸和氨。由于其抑制蛋白淋巴母细胞生物合成的能力，它被用于治疗急性淋巴母细胞白血病(ALL)。它还通过防止丙烯酰胺的形成在食品工业中有其他应用。包括细菌、真菌、放线菌和植物在内的不同生物都会产生l -天冬酰胺酶。本文综述了l -天冬酰胺酶在工业领域的不同应用、l -天冬酰胺酶的主要来源、l -天冬酰胺酶的免疫反应、固态(SSF)和浸水(SmF)发酵生产技术以及生产工艺的优化。
{"title":"Diverse origins of microbial L-asparaginases and their current miscellaneous applications","authors":"Nada A. Abdelrazek, W. Elkhatib, M. Raafat, M. Aboulwafa","doi":"10.21608/APS.2019.20220","DOIUrl":"https://doi.org/10.21608/APS.2019.20220","url":null,"abstract":"L-asparaginase, also known as amidohydrolase, catalyzes the breakdown of asparagine into aspartic acid and ammonia. Due to its ability to inhibit the biosynthesis of protein lymphoblasts, it is used to treat acute lymphoblastic leukemia (ALL). It also has other applications in the food industry by preventing the formation of acrylamide. Different organisms including bacteria, fungi, actinomycetes, and plants produce L-asparaginase. This review highlights different applications of L-asparaginase in the industrial fields, the major sources of L-asparaginase, its immunological reactions and production techniques through the solid state (SSF) and submerged (SmF) fermentation as well as optimization of the production process.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75251951","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}
Houdaii H. El-Houssaini, W. Elkhatib, Omnia M. Elnabawy, H. Nasser
Candida albicans remains the most common cause of hospital-acquired fungal infections due to its virulence determinants. Resistance to antifungal therapy has increased dramatically, narrowing the few available therapeutic options due to their potential toxicity. However, the association between C. albicans virulence determinants and resistance profiles needs further investigation. C. albicans (n= 25) isolated from various clinical samples were identified. Antibiogram analysis of the tested isolates against different antifungal agents was performed and their minimum inhibitory concentrations (MICs) were verified. Virulence determinants including extracellular hydrolytic enzymes, biofilm formation, and cell surface hydrophobicity (CSH) were investigated. Correlations between virulence determinants and resistance profiles of the experimented isolates, in addition to their potential association with the source of clinical specimens, were analyzed. All isolates were amphotericin B, nystatin and micafungin sensitive, while 100% were clotrimazole, fluconazole and voriconazole resistant. Extracellular hydrolytic activities were detected in 52, 68 and 100% of the tested isolates for phospholipase, protease, and hemolysin, respectively, while CSH and biofilm production was shown in 24 and 20% of isolates, respectively. CSH had significant (p < 0.05) positive as well as negative associations with amphotericin B and fluconazole MICs, respectively. Source of clinical isolates showed significant (p < 0.05) influence on some resistance and virulence patterns.
{"title":"Antifungal resistance and predominance of virulence determinants among Candida albicans isolated from various clinical specimens","authors":"Houdaii H. El-Houssaini, W. Elkhatib, Omnia M. Elnabawy, H. Nasser","doi":"10.21608/APS.2019.20210","DOIUrl":"https://doi.org/10.21608/APS.2019.20210","url":null,"abstract":"Candida albicans remains the most common cause of hospital-acquired fungal infections due to its virulence determinants. Resistance to antifungal therapy has increased dramatically, narrowing the few available therapeutic options due to their potential toxicity. However, the association between C. albicans virulence determinants and resistance profiles needs further investigation. C. albicans (n= 25) isolated from various clinical samples were identified. Antibiogram analysis of the tested isolates against different antifungal agents was performed and their minimum inhibitory concentrations (MICs) were verified. Virulence determinants including extracellular hydrolytic enzymes, biofilm formation, and cell surface hydrophobicity (CSH) were investigated. Correlations between virulence determinants and resistance profiles of the experimented isolates, in addition to their potential association with the source of clinical specimens, were analyzed. All isolates were amphotericin B, nystatin and micafungin sensitive, while 100% were clotrimazole, fluconazole and voriconazole resistant. Extracellular hydrolytic activities were detected in 52, 68 and 100% of the tested isolates for phospholipase, protease, and hemolysin, respectively, while CSH and biofilm production was shown in 24 and 20% of isolates, respectively. CSH had significant (p < 0.05) positive as well as negative associations with amphotericin B and fluconazole MICs, respectively. Source of clinical isolates showed significant (p < 0.05) influence on some resistance and virulence patterns.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83980780","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}
Akram ahmad Bashir, Sameh M. Abdel-Hamid, A. Badawi, A. Geneidi
Artesunate is a poorly soluble drug and liable to aqueous hydrolysis. This study aims to formulate Artesunate as an immediate release tablet through optimization of the melt granulation technique to improve the dissolution of the drug. Three different meltable binders were used (Polyethylene Glycol PEG 6000, Poloxamer 188 and Gelucire 50/13) for granulation step in high shear mixer prior tablets compression step applying Box-Behnken experimental design to determine the significant variables and their interactions that impact dissolution of Artesunate. Optimization mathematical models showed that by increasing binder concentration, D50 was increased, and narrow particle size distribution with minimum fines percentage was produced. Higher binder concentration and impeller speed resulted in retarding tablets dissolution. PEG 6000 and Poloxamer 188 based tablets showed faster disintegration and dissolution than Gelucire 50/13 based tablets, as well as tablets prepared by wet granulation due to hydrophilic pore forming. Melt granulation technique using a low level of PEG 6000 and Poloxamer 188 not only enhanced the dissolution of Artesunate from their immediate release tablets in comparison to traditional wet granulation technique but also maintained the stability of the product under accelerated conditions of heat and moisture.
{"title":"Enhancing dissolution of artesunate from immediate release tablets using a green granulation technique","authors":"Akram ahmad Bashir, Sameh M. Abdel-Hamid, A. Badawi, A. Geneidi","doi":"10.21608/APS.2019.20230","DOIUrl":"https://doi.org/10.21608/APS.2019.20230","url":null,"abstract":"Artesunate is a poorly soluble drug and liable to aqueous hydrolysis. This study aims to formulate Artesunate as an immediate release tablet through optimization of the melt granulation technique to improve the dissolution of the drug. Three different meltable binders were used (Polyethylene Glycol PEG 6000, Poloxamer 188 and Gelucire 50/13) for granulation step in high shear mixer prior tablets compression step applying Box-Behnken experimental design to determine the significant variables and their interactions that impact dissolution of Artesunate. Optimization mathematical models showed that by increasing binder concentration, D50 was increased, and narrow particle size distribution with minimum fines percentage was produced. Higher binder concentration and impeller speed resulted in retarding tablets dissolution. PEG 6000 and Poloxamer 188 based tablets showed faster disintegration and dissolution than Gelucire 50/13 based tablets, as well as tablets prepared by wet granulation due to hydrophilic pore forming. Melt granulation technique using a low level of PEG 6000 and Poloxamer 188 not only enhanced the dissolution of Artesunate from their immediate release tablets in comparison to traditional wet granulation technique but also maintained the stability of the product under accelerated conditions of heat and moisture.","PeriodicalId":8314,"journal":{"name":"Archives of Pharmaceutical Sciences Ain Shams University","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87789610","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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