Pub Date : 2020-07-01DOI: 10.4103/jrptps.JRPTPS_3_20
F. Hassanzadeh, E. Jafari, M. Saeedi, S. Saberi
Background and Objectives: The 1, 3, 4-thiadiazole scaffold is one of the principal structural components, in a variety of drug categories such as antimicrobial, anti-inflammatory, antineoplastic, and antileishmanial agents. Considering the reported antileishmanial effects of thiadiazole derivatives and the importance of this disease, some of the thiadiazole derivatives with modifications at sulfur atom or amine group attached to the 2-position were synthesized and evaluated for antileishmanial activity. Materials and Methods: Derivatives of 1,3,4-thiadiazole including 2-substituted-thio-1,3,4-thiadiazoles bearing (5-(4-nitrobenzylideneamino) or 5-amino (II, IV, V) and one derivative of 2-substituted-amino-1,3,4-thiadiazole bearing (5- (4-nitrophenyl) (VII) were synthesized and evaluated for their in vitro antileishmanial activity against promastigote and amastigote forms of the Leishmania major. Results: The most active compound was found to be compound II after 24-h incubation against promastigotes and amastigotes with the half maximal inhibitory concentration (IC50) values of 44.4 µM and 64.7 µM, respectively. Conclusion: All of the synthesized compounds showed good antileishmanial activity against both forms of L. major after 48 and 72h incubation.
{"title":"Synthesis and evaluation of thiadiazole-based antileishmanial agents","authors":"F. Hassanzadeh, E. Jafari, M. Saeedi, S. Saberi","doi":"10.4103/jrptps.JRPTPS_3_20","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_3_20","url":null,"abstract":"Background and Objectives: The 1, 3, 4-thiadiazole scaffold is one of the principal structural components, in a variety of drug categories such as antimicrobial, anti-inflammatory, antineoplastic, and antileishmanial agents. Considering the reported antileishmanial effects of thiadiazole derivatives and the importance of this disease, some of the thiadiazole derivatives with modifications at sulfur atom or amine group attached to the 2-position were synthesized and evaluated for antileishmanial activity. Materials and Methods: Derivatives of 1,3,4-thiadiazole including 2-substituted-thio-1,3,4-thiadiazoles bearing (5-(4-nitrobenzylideneamino) or 5-amino (II, IV, V) and one derivative of 2-substituted-amino-1,3,4-thiadiazole bearing (5- (4-nitrophenyl) (VII) were synthesized and evaluated for their in vitro antileishmanial activity against promastigote and amastigote forms of the Leishmania major. Results: The most active compound was found to be compound II after 24-h incubation against promastigotes and amastigotes with the half maximal inhibitory concentration (IC50) values of 44.4 µM and 64.7 µM, respectively. Conclusion: All of the synthesized compounds showed good antileishmanial activity against both forms of L. major after 48 and 72h incubation.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"189 - 195"},"PeriodicalIF":0.6,"publicationDate":"2020-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49664362","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 : 2020-07-01DOI: 10.4103/jrptps.JRPTPS_69_19
U. Rangaswamy, M. Ganachari
Introduction: Tuberculosis (TB) is an important global health problem, which is aimed to be eradicated by 2025 from India. Community pharmacists play a significant role in treating and eradication of TB. This study aimed to understand the contribution of community pharmacy and their potential role in RNTCP (Revised National TB Control Programme) functioning. Materials and Methods: The study was conducted at Belagavi, Karnataka, India on 312 community pharmacies. A structured interview form was used to assess several factors such as education, knowledge, anti-TB drug dispensing patterns, willingness to be trained, and become a DOTS (Directly Observed Treatment Short course) provider. Results: On an overall scale, we found that the majority of licensed community pharmacy was managed by D. Pharm holders with a limited knowledge of TB. It was also noted that there was a lack of willingness to be rigorously trained for updating their knowledge, although they were interested in being trained for being recognized as a DOTS center. Conclusion: There is a strong need for strengthening community pharmacy services in tune with RNTCP to achieve better efficiency in treating and eradication of TB.
{"title":"Contribution of community pharmacy in treating tuberculosis: A pharmacy centric study from Belagavi district","authors":"U. Rangaswamy, M. Ganachari","doi":"10.4103/jrptps.JRPTPS_69_19","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_69_19","url":null,"abstract":"Introduction: Tuberculosis (TB) is an important global health problem, which is aimed to be eradicated by 2025 from India. Community pharmacists play a significant role in treating and eradication of TB. This study aimed to understand the contribution of community pharmacy and their potential role in RNTCP (Revised National TB Control Programme) functioning. Materials and Methods: The study was conducted at Belagavi, Karnataka, India on 312 community pharmacies. A structured interview form was used to assess several factors such as education, knowledge, anti-TB drug dispensing patterns, willingness to be trained, and become a DOTS (Directly Observed Treatment Short course) provider. Results: On an overall scale, we found that the majority of licensed community pharmacy was managed by D. Pharm holders with a limited knowledge of TB. It was also noted that there was a lack of willingness to be rigorously trained for updating their knowledge, although they were interested in being trained for being recognized as a DOTS center. Conclusion: There is a strong need for strengthening community pharmacy services in tune with RNTCP to achieve better efficiency in treating and eradication of TB.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"246 - 250"},"PeriodicalIF":0.6,"publicationDate":"2020-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43230218","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 : 2020-07-01DOI: 10.4103/jrptps.jrptps_88_19
S. El-hawary, O. Mousa, R. El-Fitiany, Rania A El Gedaily
Background: Phytoconstituents of Prunus persica Linn. (Peach) and Malpighia glabra Linn. (Acerola) leaves were not thoroughly studied, although they are commonly incorporated in the food industry. Aim: Our aim is to explore metabolites and vitamins in three peach cultivars leaves; Desert red, Florida prince, Swelling and acerola. Material and Methods: Analysis was done using GC/MS (gas chromatography–mass spectrometry), HPLC (high-performance liquid chromatography), and spectrophotometry. Cytotoxicity was performed using MTT assay. Results: Total phenolic and flavonoid content varied from 79.54 to 121.51 μg gallic acid equivalent/mg dry weight and 31.05 to 39.77 μg quercetin equivalent/mg dry weight, respectively. Twenty-four flavonoids were identified; hesperidin was the major flavonoid in peach cultivars (3863.4 mg/100 g in Desert red, 2971 mg/100 g in Swelling, and 2624 mg/100g in Florida prince). Glucuronic acid (33.04%) and vitamin C (34 mg/100 g) were major in acerola. Thirty-four metabolites including supraene and sitosterol as well as 24 fatty-acid esters including linoleic and oleic acids were detected in the unsaponifiable and saponifiable matter, respectively. Antimicrobial activity against bacterial and fungal strains was screened in comparison with ampicillin and amphotericin B. All tested extracts significantly decreased cell viability against breast (MCF-7) and colon cell lines (HCT-116). M. glabra showed no significant difference from standard doxorubicin (0.1 μg/mL) which may suggest a strong anticancer activity against colon cell line. Conclusion: This study may highlight the magnitude of the leaves of these plants as rich sources of important metabolites and vitamin C.
{"title":"Cytotoxic, antimicrobial activities, and phytochemical investigation of three peach cultivars and acerola leaves","authors":"S. El-hawary, O. Mousa, R. El-Fitiany, Rania A El Gedaily","doi":"10.4103/jrptps.jrptps_88_19","DOIUrl":"https://doi.org/10.4103/jrptps.jrptps_88_19","url":null,"abstract":"Background: Phytoconstituents of Prunus persica Linn. (Peach) and Malpighia glabra Linn. (Acerola) leaves were not thoroughly studied, although they are commonly incorporated in the food industry. Aim: Our aim is to explore metabolites and vitamins in three peach cultivars leaves; Desert red, Florida prince, Swelling and acerola. Material and Methods: Analysis was done using GC/MS (gas chromatography–mass spectrometry), HPLC (high-performance liquid chromatography), and spectrophotometry. Cytotoxicity was performed using MTT assay. Results: Total phenolic and flavonoid content varied from 79.54 to 121.51 μg gallic acid equivalent/mg dry weight and 31.05 to 39.77 μg quercetin equivalent/mg dry weight, respectively. Twenty-four flavonoids were identified; hesperidin was the major flavonoid in peach cultivars (3863.4 mg/100 g in Desert red, 2971 mg/100 g in Swelling, and 2624 mg/100g in Florida prince). Glucuronic acid (33.04%) and vitamin C (34 mg/100 g) were major in acerola. Thirty-four metabolites including supraene and sitosterol as well as 24 fatty-acid esters including linoleic and oleic acids were detected in the unsaponifiable and saponifiable matter, respectively. Antimicrobial activity against bacterial and fungal strains was screened in comparison with ampicillin and amphotericin B. All tested extracts significantly decreased cell viability against breast (MCF-7) and colon cell lines (HCT-116). M. glabra showed no significant difference from standard doxorubicin (0.1 μg/mL) which may suggest a strong anticancer activity against colon cell line. Conclusion: This study may highlight the magnitude of the leaves of these plants as rich sources of important metabolites and vitamin C.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"221 - 236"},"PeriodicalIF":0.6,"publicationDate":"2020-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44694765","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 : 2020-07-01DOI: 10.4103/jrptps.JRPTPS_103_19
Braham Dutt, M. Choudhary, Vikaas Budhwar
Nowadays, poor solubility, lower bioavailability, and hindered physical, chemical, and biopharmaceutical properties of active pharmaceutical ingredients (APIs) become a very important matter of discussion for pharmaceutical scientists. It is a challenging task for pharmaceutical researchers and industry to develop a suitable formulation with improved physicochemical properties. The process of cocrystallization is long known; however, in the recent times, this approach has gained enormous importance in pharmaceuticals as a relatively new method for enhancement of solubility, bioavailability, stability, thermal properties, permeability, tablet ability, and other related physicochemical properties. Cocrystals are multicomponent systems in which two components, an API and a coformer, were present in stoichiometric ratio and bonded together with non-covalent interactions in the crystal lattice. Cocrystallization offers better optimization of not only physicochemical properties but also therapeutic response and pharmacological properties of APIs. The design of a cocrystallization experiment is based on robustness, hydrogen bonding rules, and potential intermolecular interactions. Various theoretical and experimental approaches increase the chances for selection of a suitable coformer, the most challenging step during the design of cocrystal formation. The present review covers classification of cocrystals, drug selection criteria for cocrystals, chemistry involved in cocrystal formation, methods of preparation, their characterizations, and various applications in pharmaceutical and biomedical fields.
{"title":"Cocrystallization: An innovative route toward better medication","authors":"Braham Dutt, M. Choudhary, Vikaas Budhwar","doi":"10.4103/jrptps.JRPTPS_103_19","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_103_19","url":null,"abstract":"Nowadays, poor solubility, lower bioavailability, and hindered physical, chemical, and biopharmaceutical properties of active pharmaceutical ingredients (APIs) become a very important matter of discussion for pharmaceutical scientists. It is a challenging task for pharmaceutical researchers and industry to develop a suitable formulation with improved physicochemical properties. The process of cocrystallization is long known; however, in the recent times, this approach has gained enormous importance in pharmaceuticals as a relatively new method for enhancement of solubility, bioavailability, stability, thermal properties, permeability, tablet ability, and other related physicochemical properties. Cocrystals are multicomponent systems in which two components, an API and a coformer, were present in stoichiometric ratio and bonded together with non-covalent interactions in the crystal lattice. Cocrystallization offers better optimization of not only physicochemical properties but also therapeutic response and pharmacological properties of APIs. The design of a cocrystallization experiment is based on robustness, hydrogen bonding rules, and potential intermolecular interactions. Various theoretical and experimental approaches increase the chances for selection of a suitable coformer, the most challenging step during the design of cocrystal formation. The present review covers classification of cocrystals, drug selection criteria for cocrystals, chemistry involved in cocrystal formation, methods of preparation, their characterizations, and various applications in pharmaceutical and biomedical fields.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"256 - 270"},"PeriodicalIF":0.6,"publicationDate":"2020-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41789962","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 : 2020-07-01DOI: 10.4103/jrptps.JRPTPS_89_19
O. Tavallaei, Marzieh Marzbany, M. Rasekhian
Heterogenicity is an indispensable element of breast cancer, which manifests itself on clinical, histopathological, and molecular levels. This heterogenicity could be a determinant factor of disease progression and drug resistance in the patients. Common therapies for metastatic breast cancer include surgery, radiotherapy, chemotherapy, and immunotherapy. On the introduction of biologic medicine, target therapy, and gene therapy, a potential has been reached to lower the rate of morbidity and mortality and also to improve the quality of life among patients with breast cancer. Although these treatments have been frequently proved by yielding promising results, a very few number of them have found their way into clinic settings due to progressive nature of these tumors, diversity of cancer populations and their microenvironments, genetic instability, and heterogenicity of breast cancers. As only minor advancements have been made in the case of recurrent metastatic breast cancer, handling this condition is now considered a medical necessity. According to genetic instability and heterogenicity of breast tumors, it is implausible to assume a single-targeted therapy could help treating most solid tumors. So, this review aimed to put together studies focused on combinational treatments targeting growth inhibition and apoptosis induction in breast cancer cells and comparing the results with monotherapies.
{"title":"Combinational treatments for breast cancer","authors":"O. Tavallaei, Marzieh Marzbany, M. Rasekhian","doi":"10.4103/jrptps.JRPTPS_89_19","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_89_19","url":null,"abstract":"Heterogenicity is an indispensable element of breast cancer, which manifests itself on clinical, histopathological, and molecular levels. This heterogenicity could be a determinant factor of disease progression and drug resistance in the patients. Common therapies for metastatic breast cancer include surgery, radiotherapy, chemotherapy, and immunotherapy. On the introduction of biologic medicine, target therapy, and gene therapy, a potential has been reached to lower the rate of morbidity and mortality and also to improve the quality of life among patients with breast cancer. Although these treatments have been frequently proved by yielding promising results, a very few number of them have found their way into clinic settings due to progressive nature of these tumors, diversity of cancer populations and their microenvironments, genetic instability, and heterogenicity of breast cancers. As only minor advancements have been made in the case of recurrent metastatic breast cancer, handling this condition is now considered a medical necessity. According to genetic instability and heterogenicity of breast tumors, it is implausible to assume a single-targeted therapy could help treating most solid tumors. So, this review aimed to put together studies focused on combinational treatments targeting growth inhibition and apoptosis induction in breast cancer cells and comparing the results with monotherapies.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"279 - 287"},"PeriodicalIF":0.6,"publicationDate":"2020-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42039242","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 : 2020-07-01DOI: 10.4103/jrptps.JRPTPS_87_19
A. Parvizpur, K. Fekri, L. Fekri, P. Ghadimi, M. Charkhpour
Introduction: Among various neurological systems involved in the development of morphine tolerance, serotonergic and adrenergic systems are very significant. In this study, we used duloxetine to further investigate the association between serotonergic and noradrenergic systems and the occurrence of opioid tolerance. Materials and Methods: Six groups of male Wistar rats were studied including saline, morphine, morphine + duloxetine (15, 30, and 60 mg.kg–1.day–1), and duloxetine-treated groups. Base latency time (BL) was determined using hot plate test (50 ± 0.5ºC). The latency times were reported as MPE% (maximum possible effect) and AUC (area under the curve) was calculated for each MPE%-Time curve (to evaluate global analgesic effect). Results: Morphine-treated group showed tolerance on the 9th day. As the same way, the groups treated with morphine and duloxetine (15, 30, 60 mg/kg) showed tolerance on the 13th, 17th, and 23rd days, respectively. Duloxetine-treated group was tolerated on the 11th day. There was a significant difference between the mean AUC in morphine + duloxetine (60 mg/kg-1/day–1) and morphine-treated groups. Conclusion: Previous studies revealed that chronic administration of morphine would reduce serotonin release in the central nervous system (CNS). This study showed the effective role of duloxetine and the serotonergic system in postponing the tolerance to analgesic effects of morphine.
{"title":"The role of duloxetine in changing the process of tolerance to morphine analgesic effects in male rats","authors":"A. Parvizpur, K. Fekri, L. Fekri, P. Ghadimi, M. Charkhpour","doi":"10.4103/jrptps.JRPTPS_87_19","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_87_19","url":null,"abstract":"Introduction: Among various neurological systems involved in the development of morphine tolerance, serotonergic and adrenergic systems are very significant. In this study, we used duloxetine to further investigate the association between serotonergic and noradrenergic systems and the occurrence of opioid tolerance. Materials and Methods: Six groups of male Wistar rats were studied including saline, morphine, morphine + duloxetine (15, 30, and 60 mg.kg–1.day–1), and duloxetine-treated groups. Base latency time (BL) was determined using hot plate test (50 ± 0.5ºC). The latency times were reported as MPE% (maximum possible effect) and AUC (area under the curve) was calculated for each MPE%-Time curve (to evaluate global analgesic effect). Results: Morphine-treated group showed tolerance on the 9th day. As the same way, the groups treated with morphine and duloxetine (15, 30, 60 mg/kg) showed tolerance on the 13th, 17th, and 23rd days, respectively. Duloxetine-treated group was tolerated on the 11th day. There was a significant difference between the mean AUC in morphine + duloxetine (60 mg/kg-1/day–1) and morphine-treated groups. Conclusion: Previous studies revealed that chronic administration of morphine would reduce serotonin release in the central nervous system (CNS). This study showed the effective role of duloxetine and the serotonergic system in postponing the tolerance to analgesic effects of morphine.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"215 - 220"},"PeriodicalIF":0.6,"publicationDate":"2020-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42880086","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 : 2020-07-01DOI: 10.4103/jrptps.JRPTPS_124_19
D. P. Pérez Gaudio, J. Mozo, G. Martínez, M. F. Fernández Paggi, J. Decundo, A. Romanelli, S. Diéguez, A. Soraci
Background: Fosfomycin (FOS) is a broad-spectrum antibiotic that inhibits cell wall synthesis. It has bactericidal activity against both gram-positive and gram-negative bacteria. FOS also promotes phagocytosis, has immunomodulatory effects, and protects against the toxicity caused by other drugs. On the contrary, deoxynivalenol (DON) causes cytotoxicity on tissues of rapid growth and fast turnover. Objectives: The aim of this study was to determine the percentage of nuclear changes indicative of DON-induced apoptosis on intestinal cell cultures (Caco-2) and to evaluate the protective effect of FOS on mycotoxin-exposed cells. Materials and Methods: Cell cultures were treated as follows: (1) DON: 2.8 µg/mL, (2) calcium FOS: 580 µg/mL, (3) DON 2.8 µg/mL + calcium FOS 580 µg/mL, and (4) negative control. Nuclear morphology was evaluated in fixed cells stained with 4′,6-diamino-2-phenylindol and then visualized under an immunofluorescence microscope. Results: Percentages of cells with nuclear changes were significantly higher in cells treated with DON (31.53% ± 4.17%) compared to those incubated with the antibiotic in conjunction with the mycotoxin (5.63% ± 4.23%). On the contrary, there were no significant differences between cells incubated with DON + FOS and cells incubated only with the antibiotic (1.10% ± 1.55%) when compared to the negative control (3.50% ± 0.09%). Conclusion: The results from this study showed that DON induces nuclear changes suggestive of apoptosis in intestinal cells and that FOS can protect cells from DNA damage. Further studies are needed to determine whether DON induces apoptosis only on cells of epithelial origin and to understand the implications of FOS protective effect under in vivo conditions.
{"title":"Fosfomycin protects intestinal cells from nuclear changes suggestive of deoxynivalenol-induced apoptosis","authors":"D. P. Pérez Gaudio, J. Mozo, G. Martínez, M. F. Fernández Paggi, J. Decundo, A. Romanelli, S. Diéguez, A. Soraci","doi":"10.4103/jrptps.JRPTPS_124_19","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_124_19","url":null,"abstract":"Background: Fosfomycin (FOS) is a broad-spectrum antibiotic that inhibits cell wall synthesis. It has bactericidal activity against both gram-positive and gram-negative bacteria. FOS also promotes phagocytosis, has immunomodulatory effects, and protects against the toxicity caused by other drugs. On the contrary, deoxynivalenol (DON) causes cytotoxicity on tissues of rapid growth and fast turnover. Objectives: The aim of this study was to determine the percentage of nuclear changes indicative of DON-induced apoptosis on intestinal cell cultures (Caco-2) and to evaluate the protective effect of FOS on mycotoxin-exposed cells. Materials and Methods: Cell cultures were treated as follows: (1) DON: 2.8 µg/mL, (2) calcium FOS: 580 µg/mL, (3) DON 2.8 µg/mL + calcium FOS 580 µg/mL, and (4) negative control. Nuclear morphology was evaluated in fixed cells stained with 4′,6-diamino-2-phenylindol and then visualized under an immunofluorescence microscope. Results: Percentages of cells with nuclear changes were significantly higher in cells treated with DON (31.53% ± 4.17%) compared to those incubated with the antibiotic in conjunction with the mycotoxin (5.63% ± 4.23%). On the contrary, there were no significant differences between cells incubated with DON + FOS and cells incubated only with the antibiotic (1.10% ± 1.55%) when compared to the negative control (3.50% ± 0.09%). Conclusion: The results from this study showed that DON induces nuclear changes suggestive of apoptosis in intestinal cells and that FOS can protect cells from DNA damage. Further studies are needed to determine whether DON induces apoptosis only on cells of epithelial origin and to understand the implications of FOS protective effect under in vivo conditions.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"209 - 214"},"PeriodicalIF":0.6,"publicationDate":"2020-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47411448","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 : 2020-01-01DOI: 10.4103/jrptps.JRPTPS_32_19
R. Kachave, P. Mandlik, S. Wakchaure
The aim of this study was to provide information of the development in analytical perspective of impurity profiling, force degradation, and bioanalysis of pharmaceutical drug substance and drug products used for the treatment of gout. This information was discussed on the basis of year of publication, matrix (active pharmaceutical ingredient, dosage form, and biological fluid), sample preparation technique, column and types of elution in chromatography (isocratic or gradient), detector, and therapeutic categories of drug, which were used for analysis. It focuses mainly on analytical methods including hyphenated techniques for the identification and quantification of impurity, degradants, and metabolites in different pharmaceutical and biological matrices.
{"title":"A review on analytical methods of antigout agents","authors":"R. Kachave, P. Mandlik, S. Wakchaure","doi":"10.4103/jrptps.JRPTPS_32_19","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_32_19","url":null,"abstract":"The aim of this study was to provide information of the development in analytical perspective of impurity profiling, force degradation, and bioanalysis of pharmaceutical drug substance and drug products used for the treatment of gout. This information was discussed on the basis of year of publication, matrix (active pharmaceutical ingredient, dosage form, and biological fluid), sample preparation technique, column and types of elution in chromatography (isocratic or gradient), detector, and therapeutic categories of drug, which were used for analysis. It focuses mainly on analytical methods including hyphenated techniques for the identification and quantification of impurity, degradants, and metabolites in different pharmaceutical and biological matrices.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"136 - 167"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46782311","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 : 2020-01-01DOI: 10.4103/jrptps.JRPTPS_15_19
F. Shafiee, M. Rabbani, A. Jahanian-Najafabadi
Purpose: In the previous studies, we designed an anticancer immunotoxin containing the catalytic and translocation domains of diphtheria toxin fused to BR2, a buforin II-derived antimicrobial peptide as a cancer-specific cell penetrating peptide, in order to target various cancer cells. The aim of this study was to evaluate the in vitro cytotoxicity of DT386–BR2 against K-562 cells as the most famous cell line for leukemia. Materials and Methods: MTT and flow-cytometry assays were used for determining the cytotoxic effects and cell death mechanism of DT386–BR2, respectively, against K-562 cell line. The recombinant DT386 and synthetic BR2 were used as the negative control in cytotoxicity assay. Results: The results of this study showed a significant reduction in survival of K-562 cells caused by DT386–BR2 as compared with BR2 and DT386 fragments. On the contrary, the flow-cytometry results showed apoptosis induction by DT386–BR2 after 12h in a dose- and time-dependent manner. Conclusion: DT386–BR2 fusion protein can be used for further preclinical studies for determining its pharmacokinetic/pharmacodynamic profiles and evaluating its anticancer efficacy in suitable animal models.
{"title":"Evaluation of cytotoxic and apoptotic effects of DT386–BR2: A promising anticancer fusion protein","authors":"F. Shafiee, M. Rabbani, A. Jahanian-Najafabadi","doi":"10.4103/jrptps.JRPTPS_15_19","DOIUrl":"https://doi.org/10.4103/jrptps.JRPTPS_15_19","url":null,"abstract":"Purpose: In the previous studies, we designed an anticancer immunotoxin containing the catalytic and translocation domains of diphtheria toxin fused to BR2, a buforin II-derived antimicrobial peptide as a cancer-specific cell penetrating peptide, in order to target various cancer cells. The aim of this study was to evaluate the in vitro cytotoxicity of DT386–BR2 against K-562 cells as the most famous cell line for leukemia. Materials and Methods: MTT and flow-cytometry assays were used for determining the cytotoxic effects and cell death mechanism of DT386–BR2, respectively, against K-562 cell line. The recombinant DT386 and synthetic BR2 were used as the negative control in cytotoxicity assay. Results: The results of this study showed a significant reduction in survival of K-562 cells caused by DT386–BR2 as compared with BR2 and DT386 fragments. On the contrary, the flow-cytometry results showed apoptosis induction by DT386–BR2 after 12h in a dose- and time-dependent manner. Conclusion: DT386–BR2 fusion protein can be used for further preclinical studies for determining its pharmacokinetic/pharmacodynamic profiles and evaluating its anticancer efficacy in suitable animal models.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"9 1","pages":"68 - 72"},"PeriodicalIF":0.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41356610","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 : 2020-01-01DOI: 10.4103/jrptps.JRPTPS_57_18
A. Mohammadi-Farani, Hosna Mousavi, A. Hosseini, A. Aliabadi
Background: Discovery of new anticancer drugs is one of the urgent issues in the medicinal chemistry researches. Incidence of severe side effects and acquired resistance to the current medications are the logical reasons for the development of novel antineoplastic agents. Methods: Herein, a new series of 4H-1,2,4-triazole derivatives was synthesized and subsequently their cytotoxicity was assessed using dimethylthiazol diphenyltetrazolium bromide assay. Furthermore, activity of caspase 3, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were investigated. All synthesized derivatives (3a–3o) were tested against Hela (cervical cancer), A549 (lung carcinoma), and U87 (glioblastoma), and the obtained data were compared with doxorubicin. Results: Among the chlorinated derivatives, compound 3c with para positioning of the chlorine on the phenyl residue possessed higher cytotoxicity (IC50 = s3.2 ± 0.6 μM) than compounds 3a and 3b, which positioned chlorine at ortho and meta position, respectively. Chlorine as electron-withdrawing moiety caused enhancement in cytotoxicity. Conclusion: Fortunately, most of the tested compounds showed remarkable cytotoxic activity toward applied cells, especially Hela. Activation of caspase 3, MMP reduction, and ROS generation were also observed for the studied compounds.
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