Fabad Journal of Pharmaceutical Sciences最新文献_第3页

Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates 新型扑热息痛-三唑缀合物的合成及生物学评价

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-08-24 DOI: 10.55262/fabadeczacilik.1336831

Necla KULABAŞ, Merve GÜRBOĞA, Özlem BİNGÖL ÖZAKPINAR, Jianyang LİU, Per-johan JAKOBSSON, Özkan DANIŞ, Ayşe OGAN, İlkay KÜÇÜKGÜZEL

{"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}

引用次数: 0

Development and Characterization of Nanofiber Strip Containing Sertraline for Buccal Application 口腔用舍曲林纳米纤维带的研制与表征

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-08-23 DOI: 10.55262/fabadeczacilik.1313014

Kutsal ÖZCAN, Sibel İLBASMIŞ TAMER, Eylül Su SARAL ACARCA

{"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}

引用次数: 0

Topotekan, karvakrol, epigallokateşin gallat ve kombinasyonlarının nöroblastom ve astrosit hücrelerinde apoptotik süreç üzerine etkisinin değerlendirilmesi 评估托泊替康、香芹酚、表没食子儿茶素没食子酸酯及其组合对神经母细胞瘤和星形胶质细胞凋亡过程的影响

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-08-11 DOI: 10.55262/fabadeczacilik.1301973

Çağatay OLTULU, Melek AKINCI, Elvan BAKAR

{"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}

引用次数: 0

Parasite-Derived MicroRNAs: Potential Alternative Targets for Laboratory Diagnosis of Cystic Echinococcosis 寄生虫衍生的MicroRNAs:囊性棘球蚴病实验室诊断的潜在替代靶点

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-07-21 DOI: 10.55262/fabadeczacilik.1324184

Serra Örsten, İ. Baysal, S. Maçin

{"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}

引用次数: 0

Validation of RP-HPLC UV method for determination ketoconazole in rabbit plasma: An application to the pharmacokinetic study RP-HPLC - UV法测定兔血浆中酮康唑的验证:在药动学研究中的应用

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-07-20 DOI: 10.55262/fabadeczacilik.1259636

Viviane Annisa, Teuku Nanda Syaifullah Sulai̇man, A. Nugroho, A. Nugroho

引用次数: 2

Phytochemical And Antimicrobial Study of Glycosmis mauritiana (Lam.) Tanaka 毛缕糖(Glycosmis mauritiana)的植物化学和抗菌研究田中

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-07-10 DOI: 10.55262/fabadeczacilik.1192521

S. Kamal, A. Mehreen, Sevinc Musayeva, Abdur Rahman Siddique, Rida Jabbar, Sumia Urai̇nab

引用次数: 0

Toxicological Evaluations of Smilax Myosotiflora Methanol Extract and its Effect to Testosterone Level of Male in Subacute Study 菝葜甲醇提取物亚急性期毒性评价及其对男性睾酮水平的影响

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-07-05 DOI: 10.55262/fabadeczacilik.1263949

Rasmaizatul Akma Rosdi, M. D. Sul'ain, D. Darni̇s, Nur Bazlını Baharun, Nur Fatıhah Ahmad, Wan Rosli Wan Ishak

{"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}

引用次数: 0

Determination of Biological Activities of Salvia sclarea L. 鼠尾草生物活性的测定。

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-06-12 DOI: 10.55262/fabadeczacilik.1293118

Y. Yücel, Ebru Özdemi̇r

{"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}

引用次数: 0

Interaction of Statins with Grapefruit Juice 他汀类药物与葡萄柚汁的相互作用

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-05-17 DOI: 10.55262/fabadeczacilik.1187441

M. Ates, S. Sahin

引用次数: 0

Kemik Metastazlarının Tedavisinde Radyofarmasötiklerin Rolü

Fabad Journal of Pharmaceutical Sciences Pub Date : 2023-05-02 DOI: 10.55262/fabadeczacilik.1191048

Hümeyra Battal, Suna Erdoğan

{"title":"Kemik Metastazlarının Tedavisinde Radyofarmasötiklerin Rolü","authors":"Hümeyra Battal, Suna Erdoğan","doi":"10.55262/fabadeczacilik.1191048","DOIUrl":"https://doi.org/10.55262/fabadeczacilik.1191048","url":null,"abstract":"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. \u0000 \u0000In 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. \u0000 \u0000This 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.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84021762","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}

引用次数: 0