Some new triazole containing acetamide derivatives 9-20 using paracetamol as starting material were synthesized and their structure were characterized by FTIR, 1H-NMR, 13C-NMR and MS data. In vitro cytotoxic activities of all synthesized molecules against five cancer cell lines (human lung cancer A549, human chronic myelogenous leukemia K562, human breast cancer MCF-7, human prostate cancer PC-3, human neuroblastoma SH-SY5Y cell lines) were examined and were also tested their cytotoxic effect on mouse embryonic fibroblast cells (NIH/3T3) to define selectivity. MTT assay were used these in vitro activity studies. Additionally, twelve target compounds 9-20 were screened for their mPGES-1 and COX-1/2 inhibitory activities. While none of the synthesized compounds showed a significant inhibition against both cancer cells and mPGES-1 as well as COX-1/2, it was determined that they were not cytotoxic against healthy cells, too. Finally, ADMET data were presented by predicting the drug-like properties of newly synthesized compounds using computational methods.
{"title":"Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates","authors":"Necla KULABAŞ, Merve GÜRBOĞA, Özlem BİNGÖL ÖZAKPINAR, Jianyang LİU, Per-johan JAKOBSSON, Özkan DANIŞ, Ayşe OGAN, İlkay KÜÇÜKGÜZEL","doi":"10.55262/fabadeczacilik.1336831","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1336831","url":null,"abstract":"Some new triazole containing acetamide derivatives 9-20 using paracetamol as starting material were synthesized and their structure were characterized by FTIR, 1H-NMR, 13C-NMR and MS data. In vitro cytotoxic activities of all synthesized molecules against five cancer cell lines (human lung cancer A549, human chronic myelogenous leukemia K562, human breast cancer MCF-7, human prostate cancer PC-3, human neuroblastoma SH-SY5Y cell lines) were examined and were also tested their cytotoxic effect on mouse embryonic fibroblast cells (NIH/3T3) to define selectivity. MTT assay were used these in vitro activity studies. Additionally, twelve target compounds 9-20 were screened for their mPGES-1 and COX-1/2 inhibitory activities. While none of the synthesized compounds showed a significant inhibition against both cancer cells and mPGES-1 as well as COX-1/2, it was determined that they were not cytotoxic against healthy cells, too. Finally, ADMET data were presented by predicting the drug-like properties of newly synthesized compounds using computational methods.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135471035","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 : 2023-08-23DOI: 10.55262/fabadeczacilik.1313014
Kutsal ÖZCAN, Sibel İLBASMIŞ TAMER, Eylül Su SARAL ACARCA
Sertraline is one of the selective serotonin reuptake inhibitors indicated in major depressive disorder. Schizophrenia is a mental disorder with frequent depressive symptoms. Sertraline is thought to be useful for the treatment of depressive symptoms in schizophrenia. The objective of this study is to formulate sertraline-containing nanofiber strips produced by the electrospinning process, which can be easily dispersed by the buccal route, suitable for the use of schizophrenia patients. Here, various ratios (%5, %7.5 and %10) of polyvinyl pyrrolidone (PVP) polymer solutions were prepared, and electrical conductivity, viscosity and surface tension characterization studies were performed on polymer solutions. After characterization studies, a polymer solution containing 5% PVP was selected to prepare nanofibers. Nanofibers were obtained by using the electrospinning method, each strip containing 5 mg sertraline. It was observed that the optimum formulation selected nanofiber had an average particle diameter of 371-439 nm in the SEM image. Tensile strength and elongation at break percentage values of 5% PVP-sertraline nanofibers values were 0.449±0.284 (Mpa) and 22.6±3.66 (%), respectively. The loading capacity and encapsulation efficiency of the formulation are 4.53%±0.31 and 79.61±10.56 respectively. In vitro drug dissolution studies showed that sertraline-containing buccal nanofibers conformed to the Hixson-Crowell kinetic model.
{"title":"Development and Characterization of Nanofiber Strip Containing Sertraline for Buccal Application","authors":"Kutsal ÖZCAN, Sibel İLBASMIŞ TAMER, Eylül Su SARAL ACARCA","doi":"10.55262/fabadeczacilik.1313014","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1313014","url":null,"abstract":"Sertraline is one of the selective serotonin reuptake inhibitors indicated in major depressive disorder. Schizophrenia is a mental disorder with frequent depressive symptoms. Sertraline is thought to be useful for the treatment of depressive symptoms in schizophrenia. The objective of this study is to formulate sertraline-containing nanofiber strips produced by the electrospinning process, which can be easily dispersed by the buccal route, suitable for the use of schizophrenia patients. Here, various ratios (%5, %7.5 and %10) of polyvinyl pyrrolidone (PVP) polymer solutions were prepared, and electrical conductivity, viscosity and surface tension characterization studies were performed on polymer solutions. After characterization studies, a polymer solution containing 5% PVP was selected to prepare nanofibers. Nanofibers were obtained by using the electrospinning method, each strip containing 5 mg sertraline. It was observed that the optimum formulation selected nanofiber had an average particle diameter of 371-439 nm in the SEM image. Tensile strength and elongation at break percentage values of 5% PVP-sertraline nanofibers values were 0.449±0.284 (Mpa) and 22.6±3.66 (%), respectively. The loading capacity and encapsulation efficiency of the formulation are 4.53%±0.31 and 79.61±10.56 respectively. In vitro drug dissolution studies showed that sertraline-containing buccal nanofibers conformed to the Hixson-Crowell kinetic model.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135621557","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 : 2023-08-11DOI: 10.55262/fabadeczacilik.1301973
Çağatay OLTULU, Melek AKINCI, Elvan BAKAR
Neuroblastoma is the sympathetic nervous system cancer. It most commonly affects children under 5 years of age and is the most common solid tumor in childhood. Topotecan is a topoisomerase 1 inhibitor. Carvacrol and Epigallocatechin gallate are naturally derived substances with anticancer, antioxidant, and apoptotic properties. The aim of our study was to evaluate the effects of topotecan, carvacrol, EGCG, topotecan+carvacrol, and topotecan+ epigallocatechin gallate combinations on the apoptotic signaling pathway. IC50 values were determined in neuroblastoma and healthy astrocyte cells using the MTT assay. Apoptotic mRNA expressions (topoisomerase 1 and 2, p53, BCL2, BAX, caspase 9, caspase 3, IL1, TNFα) in astrocytes and neuroblastoma cells at the neuroblastoma IC50 dose were analyzed using quantitative real-time PCR. We found that topotecan and carvacrol did not exhibit selective cytotoxic effects between healthy astrocytes and neuroblastoma cells. However, we found that the combination of topotecan+ epigallocatechin gallate and topotecan+carvacrol with epigallocatechin gallate showed selective cytotoxic effects on the neuroblastoma cell line compared to astrocyte cells. The obtained mRNA results can be interpreted as the initiation of apoptosis in neuroblastoma cells in the topotecan, carvacrol, epigallocatechin gallate, and topotecan+epigallocatechin gallate groups. Further studies are needed to investigate this matter in more detail.
{"title":"Topotekan, karvakrol, epigallokateşin gallat ve kombinasyonlarının nöroblastom ve astrosit hücrelerinde apoptotik süreç üzerine etkisinin değerlendirilmesi","authors":"Çağatay OLTULU, Melek AKINCI, Elvan BAKAR","doi":"10.55262/fabadeczacilik.1301973","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1301973","url":null,"abstract":"Neuroblastoma is the sympathetic nervous system cancer. It most commonly affects children under 5 years of age and is the most common solid tumor in childhood. Topotecan is a topoisomerase 1 inhibitor. Carvacrol and Epigallocatechin gallate are naturally derived substances with anticancer, antioxidant, and apoptotic properties. The aim of our study was to evaluate the effects of topotecan, carvacrol, EGCG, topotecan+carvacrol, and topotecan+ epigallocatechin gallate combinations on the apoptotic signaling pathway. IC50 values were determined in neuroblastoma and healthy astrocyte cells using the MTT assay. Apoptotic mRNA expressions (topoisomerase 1 and 2, p53, BCL2, BAX, caspase 9, caspase 3, IL1, TNFα) in astrocytes and neuroblastoma cells at the neuroblastoma IC50 dose were analyzed using quantitative real-time PCR. We found that topotecan and carvacrol did not exhibit selective cytotoxic effects between healthy astrocytes and neuroblastoma cells. However, we found that the combination of topotecan+ epigallocatechin gallate and topotecan+carvacrol with epigallocatechin gallate showed selective cytotoxic effects on the neuroblastoma cell line compared to astrocyte cells. The obtained mRNA results can be interpreted as the initiation of apoptosis in neuroblastoma cells in the topotecan, carvacrol, epigallocatechin gallate, and topotecan+epigallocatechin gallate groups. Further studies are needed to investigate this matter in more detail.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135492923","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 : 2023-07-21DOI: 10.55262/fabadeczacilik.1324184
Serra Örsten, İ. Baysal, S. Maçin
Cystic Echinococcosis (CE) is a type of zoonotic infection that can be caused by a specific form of a parasite called Echinococcus granulosus sensu lato. Mostly, imaging techniques are utilized to diagnose CE. Serological tests are used only when imaging findings are atypical. Additionally, laboratory assays including direct microscopy and PCR are used in the confirmation of diagnosis after treatment though obtained negative results with these tests cannot be ruled out the diagnosis. Specific miRNAs produced by the parasite could be used as markers to diagnose and monitor CE. This research focuses on investigating the diagnostic potential of parasite-derived miRNAs compared to the presence of protoscolex in animal-derived hydatid cyst samples. Accordingly, egr-let-7-5p, egr-miR71-5p and egr-miR-9-5p were found to be positive in 26, 25 and 11 out of 30 samples (86.6%, 83.3% and (36.6%), respectively. There was no relationship between protoscolex presence and detection of either egr-let-7-5p or egr-miR-9-5p (p>0.05). On the other hand, egr-miR71-5p positivity was found statistically significant compared with protoscolex presence (p=0.04). As a result, egr-miR-71 are a promising potential target for the diagnosis of CE. Additional research is necessary to assess the diagnostic value of miRNAs in CE using a larger group of samples.
{"title":"Parasite-Derived MicroRNAs: Potential Alternative Targets for Laboratory Diagnosis of Cystic Echinococcosis","authors":"Serra Örsten, İ. Baysal, S. Maçin","doi":"10.55262/fabadeczacilik.1324184","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1324184","url":null,"abstract":"Cystic Echinococcosis (CE) is a type of zoonotic infection that can be caused by a specific form of a parasite called Echinococcus granulosus sensu lato. Mostly, imaging techniques are utilized to diagnose CE. Serological tests are used only when imaging findings are atypical. Additionally, laboratory assays including direct microscopy and PCR are used in the confirmation of diagnosis after treatment though obtained negative results with these tests cannot be ruled out the diagnosis. Specific miRNAs produced by the parasite could be used as markers to diagnose and monitor CE. This research focuses on investigating the diagnostic potential of parasite-derived miRNAs compared to the presence of protoscolex in animal-derived hydatid cyst samples. Accordingly, egr-let-7-5p, egr-miR71-5p and egr-miR-9-5p were found to be positive in 26, 25 and 11 out of 30 samples (86.6%, 83.3% and (36.6%), respectively. There was no relationship between protoscolex presence and detection of either egr-let-7-5p or egr-miR-9-5p (p>0.05). On the other hand, egr-miR71-5p positivity was found statistically significant compared with protoscolex presence (p=0.04). As a result, egr-miR-71 are a promising potential target for the diagnosis of CE. Additional research is necessary to assess the diagnostic value of miRNAs in CE using a larger group of samples.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82233317","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 : 2023-07-20DOI: 10.55262/fabadeczacilik.1259636
Viviane Annisa, Teuku Nanda Syaifullah Sulai̇man, A. Nugroho, A. Nugroho
Ketoconazole is an imidazole broad-spectrum antifungal agent used for systemic and local infections. The pharmacokinetic information for ketoconazole is relatively limited. The validated method for determining ketoconazole in plasma rabbit is not yet reported. The HPLC-UV method is simple, rapid, cost-effective, sensitive, and only requires a small blood sampling. The chromatographic system consisted of a reversed-phase C18 column (250 x 4.6 mm, 5 µm) at a flow rate of 1 ml/min and detection wavelength of 240 nm, and the retention time of about 5 minutes for ketoconazole and 11 min for itraconazole as internal standard. The calibration curve presented linearity in the 0.05-8 µg/ml with R2=0.9969, which indicated good linearity. The method's precision was obtained by intra-day and inter-day repeatability studies, and accuracy was examined by %diff. The result is
{"title":"Validation of RP-HPLC UV method for determination ketoconazole in rabbit plasma: An application to the pharmacokinetic study","authors":"Viviane Annisa, Teuku Nanda Syaifullah Sulai̇man, A. Nugroho, A. Nugroho","doi":"10.55262/fabadeczacilik.1259636","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1259636","url":null,"abstract":"Ketoconazole is an imidazole broad-spectrum antifungal agent used for systemic and local infections. The pharmacokinetic information for ketoconazole is relatively limited. The validated method for determining ketoconazole in plasma rabbit is not yet reported. The HPLC-UV method is simple, rapid, cost-effective, sensitive, and only requires a small blood sampling. The chromatographic system consisted of a reversed-phase C18 column (250 x 4.6 mm, 5 µm) at a flow rate of 1 ml/min and detection wavelength of 240 nm, and the retention time of about 5 minutes for ketoconazole and 11 min for itraconazole as internal standard. The calibration curve presented linearity in the 0.05-8 µg/ml with R2=0.9969, which indicated good linearity. The method's precision was obtained by intra-day and inter-day repeatability studies, and accuracy was examined by %diff. The result is","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86967697","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 : 2023-07-10DOI: 10.55262/fabadeczacilik.1192521
S. Kamal, A. Mehreen, Sevinc Musayeva, Abdur Rahman Siddique, Rida Jabbar, Sumia Urai̇nab
We have successfully extracted a novel geranyl flavanone from the root barks of Glycosmis mauritiana. The structucture was eleducated as 6-geranyl-5-hydroxy-3′ -methoxy-7, 8- (2", 2"-dimethyl pyrano) flavanone- 4'-O-D-glucopyranoside (GM-1), along with 3 known compounds (GM-2, GM-3, GM-4), was separated and identified by a variety of spectroscopic techniques. The range of inhibition against four bacteria examined was shown to be 4-25 mm; the GM-1 revealed a significant inhibition zone.
从毛里亚糖的根皮中提取了一种新的香叶黄酮。结构鉴定为6-香叶基-5-羟基-3′-甲氧基- 7,8 -(2′，2′-二甲基吡喃)黄烷酮-4′- o -d -葡萄糖吡喃苷(GM-1)，并与3个已知化合物GM-2、GM-3、GM-4进行了分离鉴定。对4种细菌的抑制范围为4 ~ 25mm;GM-1表现出明显的抑制带。
{"title":"Phytochemical And Antimicrobial Study of Glycosmis mauritiana (Lam.) Tanaka","authors":"S. Kamal, A. Mehreen, Sevinc Musayeva, Abdur Rahman Siddique, Rida Jabbar, Sumia Urai̇nab","doi":"10.55262/fabadeczacilik.1192521","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1192521","url":null,"abstract":"We have successfully extracted a novel geranyl flavanone from the root barks of Glycosmis mauritiana. The structucture was eleducated as 6-geranyl-5-hydroxy-3′ -methoxy-7, 8- (2\", 2\"-dimethyl pyrano) flavanone- 4'-O-D-glucopyranoside (GM-1), along with 3 known compounds (GM-2, GM-3, GM-4), was separated and identified by a variety of spectroscopic techniques. The range of inhibition against four bacteria examined was shown to be 4-25 mm; the GM-1 revealed a significant inhibition zone.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91145736","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 : 2023-07-05DOI: 10.55262/fabadeczacilik.1263949
Rasmaizatul Akma Rosdi, M. D. Sul'ain, D. Darni̇s, Nur Bazlını Baharun, Nur Fatıhah Ahmad, Wan Rosli Wan Ishak
Smilax myosotiflora A. DC., the horny little devil, is a tropical creeping plant which popularly consumed as a male aphrodisiac, energy booster and lumbago reliever in the old traditional medicinal. The scientific studies showed that the plant able to increase sexual behaviors and testosterone level in male rats. However, its toxicity effect is still remained unknown. Therefore, this study aimed to investigate the toxicity effects of S. myosotiflora methanol extract (SMME) through in vitro and in vivo studies. The SMME was subjected to the brine shrimp lethality test (BSLT) to determine the LC50. Acute and subacute toxicity studies according to the Limit Test of OECD guidelines no. 425 and 407 was carried out through oral gavage accordingly. It was found that the LC50 of SMME was 674.4ppm while its LD50 via acute test was more than 5000mg/kg. Neither sign of toxicity nor significant difference in food intake, weight gain, gross necropsy, the hematological and biochemical analyses and histological evaluations were recorded between the control and treated groups except for the level of AST and testosterone in male and sodium and triglycerides in female rats. The increase of testosterone in male might occur through specific pathway as the SMME did not increase the hormone level in the female. According to GHS classification, SMME in this study can be classified as Category 5 (Safe) and non-toxic. Data from this study can be served as a primary predictive guide for future research in assessing the efficiency and safety of S. myosotiflora consumption for human trial.
{"title":"Toxicological Evaluations of Smilax Myosotiflora Methanol Extract and its Effect to Testosterone Level of Male in Subacute Study","authors":"Rasmaizatul Akma Rosdi, M. D. Sul'ain, D. Darni̇s, Nur Bazlını Baharun, Nur Fatıhah Ahmad, Wan Rosli Wan Ishak","doi":"10.55262/fabadeczacilik.1263949","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1263949","url":null,"abstract":"Smilax myosotiflora A. DC., the horny little devil, is a tropical creeping plant which popularly consumed as a male aphrodisiac, energy booster and lumbago reliever in the old traditional medicinal. The scientific studies showed that the plant able to increase sexual behaviors and testosterone level in male rats. However, its toxicity effect is still remained unknown. Therefore, this study aimed to investigate the toxicity effects of S. myosotiflora methanol extract (SMME) through in vitro and in vivo studies. The SMME was subjected to the brine shrimp lethality test (BSLT) to determine the LC50. Acute and subacute toxicity studies according to the Limit Test of OECD guidelines no. 425 and 407 was carried out through oral gavage accordingly. It was found that the LC50 of SMME was 674.4ppm while its LD50 via acute test was more than 5000mg/kg. Neither sign of toxicity nor significant difference in food intake, weight gain, gross necropsy, the hematological and biochemical analyses and histological evaluations were recorded between the control and treated groups except for the level of AST and testosterone in male and sodium and triglycerides in female rats. The increase of testosterone in male might occur through specific pathway as the SMME did not increase the hormone level in the female. According to GHS classification, SMME in this study can be classified as Category 5 (Safe) and non-toxic. Data from this study can be served as a primary predictive guide for future research in assessing the efficiency and safety of S. myosotiflora consumption for human trial.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89370818","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 : 2023-06-12DOI: 10.55262/fabadeczacilik.1293118
Y. Yücel, Ebru Özdemi̇r
Within the last two or three decades the treatment of the neurodegenerative disorders became became the main focus of the researches. In this, our aim was to determine some biological activities of the ethanolic and methanolic extracts of Salvia sclarea L. After obtaining the extracts, first they have been tested for their DPPH radical scavenging activity and then the total phenolic contents of the extracts have been identified. Afterwords, the extracts were evaluated for both their effects on acetylcholinesterase (AChE) and monoamine oxidase-A. These two enzymes are very important enyzmes for their importance in the treatment of neurodegenerative disorders. AChE plays a very crucial role especially in Alzheimer’s Disease. Monoamine oxidases and their inhibitors have also critical value in Alzheimer type dementia and in other neurologic diseases. It has been found that DPPH activity of the methanolic extract was higher than that of ethanolic extracts; while TPC was higher for the ethanolic extract. IC50 values were found for both AChE and MAO-A. For AChE the IC50 values for ethanolic extract and methanolic extract were, 0,27±0,005 mg/mL and 1,19±0,037 mg/mL; respectively. And for MAO-A the IC50 values for ethanolic extract and methanolic extract were 6,53±0,72 microgramg/mL and 3,03±0,05 microgram/mL; respectively.
{"title":"Determination of Biological Activities of Salvia sclarea L.","authors":"Y. Yücel, Ebru Özdemi̇r","doi":"10.55262/fabadeczacilik.1293118","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1293118","url":null,"abstract":"Within the last two or three decades the treatment of the neurodegenerative disorders became became the main focus of the researches. In this, our aim was to determine some biological activities of the ethanolic and methanolic extracts of Salvia sclarea L. After obtaining the extracts, first they have been tested for their DPPH radical scavenging activity and then the total phenolic contents of the extracts have been identified. Afterwords, the extracts were evaluated for both their effects on acetylcholinesterase (AChE) and monoamine oxidase-A. These two enzymes are very important enyzmes for their importance in the treatment of neurodegenerative disorders. AChE plays a very crucial role especially in Alzheimer’s Disease. Monoamine oxidases and their inhibitors have also critical value in Alzheimer type dementia and in other neurologic diseases. It has been found that DPPH activity of the methanolic extract was higher than that of ethanolic extracts; while TPC was higher for the ethanolic extract. IC50 values were found for both AChE and MAO-A. For AChE the IC50 values for ethanolic extract and methanolic extract were, 0,27±0,005 mg/mL and 1,19±0,037 mg/mL; respectively. And for MAO-A the IC50 values for ethanolic extract and methanolic extract were 6,53±0,72 microgramg/mL and 3,03±0,05 microgram/mL; respectively.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89617365","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 : 2023-05-17DOI: 10.55262/fabadeczacilik.1187441
M. Ates, S. Sahin
Grapefruit juice, which discovered to interact with felodipine for the first time, is now known to interact with more that 80 drugs. Statins are among the drugs that interact with grapefruit juice. Grapefruit juice-statin interactions were first investigated in 1998 in human pharmacokinetic studies with lovastatin and simvastatin. The pharmacokinetic and pharmacodynamic basis of the interaction has been extensively investigated in studies. Flavonoids and furanocoumarins, the main components of grapefruit juice, have been reported to cause drug interactions. Furthermore, statin-grapefruit juice interactions occur mostly through inhibition of cytochrome-3A4 (CYP3A4), to a lesser extent through inhibition of P-glycoprotein (P-gp) and organic anion transporting polypeptides (OATPs). Changes in plasma drug levels as a result of interaction may increase the side-effect of statins or reduce their therapeutic efficacy. Therefore, patients using statins are generally advised to avoid grapefruit juice consumption.
{"title":"Interaction of Statins with Grapefruit Juice","authors":"M. Ates, S. Sahin","doi":"10.55262/fabadeczacilik.1187441","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1187441","url":null,"abstract":"Grapefruit juice, which discovered to interact with felodipine for the first time, is now known to interact with more that 80 drugs. Statins are among the drugs that interact with grapefruit juice. Grapefruit juice-statin interactions were first investigated in 1998 in human pharmacokinetic studies with lovastatin and simvastatin. The pharmacokinetic and pharmacodynamic basis of the interaction has been extensively investigated in studies. Flavonoids and furanocoumarins, the main components of grapefruit juice, have been reported to cause drug interactions. Furthermore, statin-grapefruit juice interactions occur mostly through inhibition of cytochrome-3A4 (CYP3A4), to a lesser extent through inhibition of P-glycoprotein (P-gp) and organic anion transporting polypeptides (OATPs). Changes in plasma drug levels as a result of interaction may increase the side-effect of statins or reduce their therapeutic efficacy. Therefore, patients using statins are generally advised to avoid grapefruit juice consumption.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78316468","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 : 2023-05-02DOI: 10.55262/fabadeczacilik.1191048
Hümeyra Battal, Suna Erdoğan
Cancer, having quite high morbidity and mortality rates, has become a significant public health problem in recent years, and it is the second leading cause of death after heart disease in the world. Metastases are one of the most serious complications of cancer, and bone metastases are detected in 2/3 of metastatic cancer cases. General therapy approaches in bone metastases can be classified as surgery, bisphosphonates therapy, radiotherapy, and radionuclide therapy. Radionuclide therapy using alpha and beta emitting radionuclides is more selective and effective than other local and systemic treatment methods, and this feature provide several advantages over existing therapeutic methods. Radionuclide therapy used in bone metastasis for reducing the pain, killing tumor cells, prolonging life span, and improving quality of life. In recent years, alpha-emitting radiopharmaceuticals [such as Radium-223 (Ra-223) chloride] and beta-emitting radiopharmaceuticals [such as Strontium-89 (Sr-89) chloride, Lutetium-177 (Lu-177) labeled Ethylenediamine Tetra Methylene Phosphonic Acid (EDTMP), Samarium-153 (Sm-153) labeled EDTMP] are introduced in the clinic for especially the treatment of painful bone metastases and on the other hand new radiopharmaceutical development studies also continue intensively, like Actinium-225 labeled prostate-specific membrane antigen-617 (Ac-225-PSMA). Many studies have proven that using radiopharmaceuticals in the therapy of bone metastases improves the patient's general health, reduces pain and the risk of pathological fractures, and increases survival. This review presents an overview of radionuclide therapy used in bone metastases. In this context, general information about the radiopharmaceuticals is given, and the importance of the use of radiopharmaceuticals in bone metastases therapy is explained with experimental and clinical studies examples.
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