Pub Date : 2019-12-01DOI: 10.26650/istanbuljpharm.2019.19022
Gökçe Cihan-Üstündağ, Emel Mataracı-Kara, G. Çapan
DOI : 10.26650/IstanbulJPharm.2019.19022 A novel series of benzoyl hydrazones (2a-j) have been synthesized and evaluated, in vitro, for antimicrobial activity against selected bacteria and fungi. The structures of the compounds were established by IR, 1H-NMR, 13C-NMR (APT), electrospray ionization mass spectrometry (ESI-MS) and microanalysis (C, H, N). All of the tested compounds, except for compound 2h, displayed weak antibacterial properties against Staphylococcus epidermidis ATCC 12228 and Staphylococcus aureus ATCC 29213. Compounds 2a, 2b, 2e, 2f and 2i further exhibited marginal antifungal activity against Candida parapsilosis. You may cite this article as : Cihan-Ustundag G, Mataraci-Kara E, Capan G (2019). Synthesis, Characterization, Antibacterial and Antifungal Evaluation of Novel Cyclohexanone Benzoylhydrazones. Istanbul J Pharm 10.26650/IstanbulJPharm.2019.19022.
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Pub Date : 2019-12-01DOI: 10.26650/istanbuljpharm.2019.19012
Turgay Kolaç, P. Gürbüz, Gülsüm Yetiş, Z. Çirak
DOI : 10.26650/IstanbulJPharm.2019.19012 Magistral drugs are preferred when present preparations are not sufficient. Even though , the tendency of their usage ha d been decreased , it is predicted that magistral applications will be used more often in the future. In this study pharmacists and pharmacy emplo yees, who work in 95 pharmacies in Malatya city center and accepted to join the study (n=203 ), filled a questionnaire which was prepared by using the literature. In the analysis of the obtained data, frequency and percentages were calculated by using SPSS 24.0 program. It was observed that 11.1 of the pharmacies were close to a health center and 88.0 of the participants were preparing magistral drugs. It was stated that 55.2 of the participants prepared magistral medications 1 2 times a week According to the results, although the frequency varied with the localization of pharmacies, magistral drug preparation ratios w ere generally similar with the literature. Preferred magistral drug forms were; cream (74.7 %%), pomade (69.8 and solution (54.7 in order. Of the participants who stated themselves to be insufficient in magistral drug preparation 19.5 said that the p rescriptions were insufficient and 33.3 reported that the doctors' prescriptions were incomplete or unreadable. You may cite this article as : Kolac T, Gurbuz P, Yetis G, Cirak ZD (2019). Determination of Pharmacy Pharmacists and Pharmacy Employees' Knowledge and Attitudes about Magistral Drug Preparation in Malatya/Turkey. Istanbul J Pharm 10.26650/IstanbulJPharm.2019.19012.
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Pub Date : 2019-12-01DOI: 10.26650/istanbuljpharm.2019.19034
B. Sen-Utsukarci, N. Tabanca, A. Estep, Ozlem Akbal-Dagistan, S. Kessler, Z. Ozturk, J. Becnel, A. Kiemer, A. Mat
DOI : 10.26650/IstanbulJPharm.2019.19034 Delphinium species are well-known toxic plants with their diterpenoid alkaloid contents. There has been no previous investigation on the cytotoxicity of Delphinium formosum Boiss. & Huet. The extracts of the different parts of D. formosum, an endemic species in Turkey, were investigated for their cytotoxic activity against the human liver carcinoma cell line (HepG2) and primary human umbilical vein endothelial cells (HUVEC). The cytotoxic effects of twelve extracts and subfractions were determined against HepG2 cells using MTT assay. The only active extract was applied to the HUVEC as a model for healthy cells. Only one of the alkaloid-containing extracts from the aerial parts was toxic (IC50 = 244,9 μg/mL against HepG2 and 144,4 μg/mL against HUVEC), while the root extracts were inactive. The results were improbable although it’s predicted secondary metabolites, such as diterpene alkaloids (methyllycaconitine, browniine, lycoctonine, avardharidine, antranoyllycoctonine, delsemine A/B and lycoctonine). Based on previous studies in literature, the cytotoxic plants were also expected to exhibit insecticidal activity. Therefore, the cytotoxic extract of D. formosum was examined for its adulticidal and larvicidal activity against the yellow fever, dengue fevers and Zika virus vector Aedes aegypti L. You may cite this article as : Sen-Utsukarci B, Tabanca N, Estep AS, Akbal-Dagistan O, Kessler SM, Ozturk Z, Becnel J, Kiemer AK, Mat A (2019). The Cytotoxicity and Insecticidal Activity of Extracts from Delphinium formosum Boiss. & Huet. Istanbul J Pharm 10.26650/IstanbulJPharm.2019.19034.
飞燕草是众所周知的有毒植物,含有二萜生物碱。对台湾飞燕草的细胞毒性研究尚未见报道。和休伊特。研究了土耳其特有植物D. formosum不同部位提取物对人肝癌细胞株HepG2和人脐静脉内皮细胞(HUVEC)的细胞毒活性。采用MTT法测定了12种提取物和亚组分对HepG2细胞的细胞毒作用。唯一的活性提取物应用于HUVEC作为健康细胞的模型。对HepG2和HUVEC的IC50分别为244,9 μg/mL和144,4 μg/mL,根部提取物对HepG2和HUVEC均无活性。结果是不可能的,尽管它预测了次生代谢产物,如二萜生物碱(甲基茄头碱,棕色碱,番茄碱,阿瓦达定,antranoyllycoctonine, delsemine A/B和番茄碱)。根据以往的文献研究,细胞毒性植物也有望表现出杀虫活性。为此,我们检测了台湾金丝梅细胞毒提取物对黄热病、登革热和寨卡病毒载体埃及伊蚊的杀虫活性。本文可引为:Sen-Utsukarci B, Tabanca N, Estep as, Akbal-Dagistan O, Kessler SM, Ozturk Z, Becnel J, Kiemer AK, Mat A(2019)。台湾飞燕草提取物的细胞毒性和杀虫活性。和休伊特。IstanbulJPharm 10.26650/ istanbuljpharma .2019.19034。
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Pub Date : 2019-12-01DOI: 10.26650/istanbuljpharm.2019.19036
A. Sahin, Secil Caban-Toktas, H. Tonbul, F. Yerlikaya, Y. Aktaş, Y. Capan
DOI : 10.26650/IstanbulJPharm.2019.19036 Nano drug co-delivery system is a popular strategy for combined application of two or more anticancer and/or synergistic drugs. Synergistic effects of nonsteroidal anti-inflammatory drugs and anti-cancer drugs in cancer treatment are shown in the literature. In this study, it was aimed to screen and understand critical formulation and process parameters inthe preparationflurbiprofen and paclitaxel co-loaded nanoparticles for developing an anti-cancer nano co-delivery system. With this aim, critical parameters were determined using Plackett–Burman experimental design (DoE). Flurbiprofen and paclitaxel drug loading amounts were considered as critical quality attributes to controleffective drug loading ratio. Furthermore, average particle size and zeta potential were also defined as critical quality attributes in order to optimize passive drug targeting and colloidal stability. Surfactant type was determined as the most significant factors for the average particle size and zeta potential. For flurbiprofen and paclitaxel drug loading into the nanoparticles, amounts of both flurbiprofen and paclitaxel were determined as critical factors. Consequently, paclitaxel and flurbiprofen were efficiently loaded into nanoparticles and the impact of the formulation variables were successfully screened by a DoE. By controlling the determined parameters, therapeutic efficacy of co-loaded drug nanoparticles could be maximized in further studies. You may cite this article as : Şahin A, Caban-Toktas S, Tonbul H, Yerlikaya F, Aktas Y, Capan Y (2019). Development of Paclitaxel and Flurbiprofen Co-Loaded PLGA Nanoparticles: Understanding Critical Formulation and Process Parameters Using Plackett–Burman Design. Istanbul J Pharm 10.26650/IstanbulJPharm.2019.19036.
纳米药物共递送系统是两种或多种抗癌和/或协同药物联合应用的流行策略。文献显示非甾体抗炎药和抗癌药物在癌症治疗中的协同作用。本研究旨在筛选和了解制备氟比洛芬和紫杉醇共载纳米颗粒的关键配方和工艺参数,以开发抗癌纳米共递送系统。为此,采用Plackett-Burman实验设计(DoE)确定了关键参数。氟比洛芬和紫杉醇载药量被认为是控制有效载药率的关键质量属性。此外,平均粒径和zeta电位也被定义为关键的质量属性,以优化被动药物靶向性和胶体稳定性。表面活性剂类型是影响平均粒径和zeta电位的最重要因素。对于氟比洛芬和紫杉醇类药物在纳米颗粒中的装载,氟比洛芬和紫杉醇的量被确定为关键因素。结果表明,紫杉醇和氟比洛芬被有效地装载到纳米颗粒中,并通过DoE成功地筛选了配方变量的影响。通过控制所确定的参数,可以在进一步的研究中最大限度地提高共载药物纳米颗粒的治疗效果。您可以将本文引用为:Şahin A, Caban-Toktas S, Tonbul H, Yerlikaya F, Aktas Y, Capan Y(2019)。紫杉醇和氟比洛芬共载PLGA纳米颗粒的研制:利用Plackett-Burman设计了解关键配方和工艺参数。IstanbulJPharm 10.26650/ istanbuljpharma .2019.19036。
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Pub Date : 2019-12-01DOI: 10.26650/istanbuljpharm.2019.19021
Mahmoud Abudayyak
Rheum ribes is a perennial herbaceous plant belonging to the Polygonaceae family that grows more in rocky and gravelly slopes in high altitude areas of Levant and Turkey. Rheum ribes is consumed as food and widely used in folk medicine against nausea, constipation and for different diseases including diabetesand hypertension. Unfortunately, the researches on Rheum ribes toxicity are insufficient. In our study, human hepatocellular carcinoma (HepG2) cell line was used in cytotoxicity evaluation of Rheum ribes water, methanol and chloroform extracts by MTT and NRU test. Comet assay was used to investigate the genotoxicity potentials of the plant extracts. Our results show that all extracts cause cell death in a concentration dependent manner at 5-50 mg/mL concentrations. The IC50 values are 14.29- 31.94 mg/mL by MTT and 21.15 - 27.66 mg/mL by NRU assay. The highest concentration (25 mg/mL) of methanol extract causes a significant DNA damage (8.7-folds). In conclusion, similar to a lot of plants used in the folk medicine the risk of Rheum ribes is still unknown. The uncontrolled use of this plant could harm to the patients. Our results indicate possible cyto- and gentoxicity effects of Rheum ribes, these results should rise the concerns about the safety of Rheum ribes and other folk herbs. Cite this article as : Abudayyak M (2019). In vitro evaluation of Rheum ribes induced genotoxicity in HepG2 cell lines. Istanbul J Pharm 10.26650/IstanbulJPharm.2019.19021.
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Pub Date : 2019-12-01DOI: 10.26650/istanbuljpharm.2019.19020
E. Oztas, Mahmoud Abudayyak, Beyza Aykanat, Zubeyde Can, E. Baram, G. Özhan
DOI : 10.26650/IstanbulJPharm.2019.19020 Bismuth (III) oxide nanoparticles’ (Bi2O3-NPs) unique physicochemical properties attracted the attention in biological, industrial, technological and medical fields. Concurrently, increasing numbers of studies revealing their potential toxic effects and possible toxicity mechanisms are ongoing. In this study, we assessed the toxic potentials of Bi2O3-NPs in human SH-SY5Y neuroblastoma cell line. After Bi2O3-NPs characterization using TEM, the cytotoxic potentials were evaluated by MTT and LDH assays. The induction of reactive oxygen species production was evaluated by H2DCFDA. In order to evaluate the oxidative damages, the changes in antioxidant catalase and superoxide dismutase and glutathione levels were determined. The cellular death pathway and the role of immune response were studied by measuring the mRNA expression levels of related genes. Our results showed that Bi2O3-NPs decreased the cell viability through disruption on mitochondrial activity (IC50:77.57 μg/mL) and membrane integrity (LDH%50:16.97 μg/mL). At 50 μg/mL Bi2O3-NPs, the production of reactive oxygen species (ROS) was induced significantly as well as the catalase and superoxide dismutase levels. In immune response, the mRNA expression levels of interleukin (IL)-6 were increased more than 1.5-fold in all doses; whereas, TNF-α, NF-ĸB and MAPK8 expressions were remained unchanged. Consequently, Bi2O3-NPs induced oxidative stress-related inflammation via activation of pro-inflammatory cytokine, IL-6. You may cite this article as : Oztas E, Abudayyak M, Aykanat B, Can Z, Baram E, Ozhan G (2019). Bismuth Oxide Nanoparticles Induced Oxidative Stress-Related Inflammation in SH-SY5Y Cell Line. Istanbul J Pharm 10.26650/IstanbulJPharm.2019.19020.
铋(III)氧化物纳米粒子(Bi2O3-NPs)独特的物理化学性质引起了生物、工业、技术和医疗领域的关注。同时,越来越多的研究正在揭示其潜在的毒性作用和可能的毒性机制。在这项研究中,我们评估了Bi2O3-NPs对人SH-SY5Y神经母细胞瘤细胞系的毒性潜能。在用TEM表征Bi2O3-NPs后,用MTT和LDH测定细胞毒性电位。用H2DCFDA评价其对活性氧生成的诱导作用。为了评价氧化损伤,测定了抗氧化过氧化氢酶、超氧化物歧化酶和谷胱甘肽水平的变化。通过检测相关基因mRNA表达水平,研究细胞死亡途径及其在免疫应答中的作用。结果表明,Bi2O3-NPs通过破坏线粒体活性(IC50:77.57 μg/mL)和膜完整性(LDH%50:16.97 μg/mL)来降低细胞活力。50 μg/mL Bi2O3-NPs显著诱导活性氧(ROS)生成,过氧化氢酶和超氧化物歧化酶水平显著升高。在免疫应答中,各剂量组白细胞介素(IL)-6 mRNA表达水平均升高1.5倍以上;而TNF-α、NF-ĸB和MAPK8的表达则保持不变。因此,Bi2O3-NPs通过激活促炎细胞因子IL-6诱导氧化应激相关炎症。你可以将这篇文章引用为:Oztas E, Abudayyak M, Aykanat B, Can Z, Baram E, Ozhan G(2019)。氧化铋纳米颗粒诱导SH-SY5Y细胞氧化应激相关炎症IstanbulJPharm 10.26650/ istanbuljpharma .2019.19020。
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Pub Date : 2019-10-11DOI: 10.5152/ISTANBULJPHARM.2018.396764
S. Uysal, R. Ceylan, A. Aktumsek, G. Guler, C. M. N. Picot, G. Zengin, M. Mahomoodally
DOI : 10.5152/IstanbulJPharm.2018.396764 Prevention and treatment of noncommunicable diseases such as neurodegenerative diseases, diabetes, and hyperpigmentation using medicinal plants has attracted increasing attention during the past few decades. In this study, Colutea cilicica Boiss. & Balansa extracts (ethyl acetate, methanol, and water) were evaluated against key enzymes involved in neurodegenerative diseases, diabetes, and hyperpigmentation. The antioxidant (free radical scavenging, reducing power, β-carotene/linoleic acid, and phosphomolybdenum) and metal chelation properties were also investigated. The methanol extracts of C. cilicica vigorously inhibited the activities of acetylcholinesterase and butyrylcholinesterase (1.33 and 0.68 mg galantamine equivalents (GALAE)/g extract, respectively). It was observed that C. cilicica extracts possessed a higher inhibitory potential for α-glucosidase (2.71–1.23 mmol acarbose equivalents (ACAE)/g extract) than that for α-amylase (0.57–0.12 mmol ACAE/g extract). The water extract of C. cilicica showed potent radical scavenging capacity against DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ABTS (2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (42.46 and 57.70 mg trolox equivalents (TE)/g extract, respectively). Phytochemical determination showed that C. cilicica water extract (17.26 mg rutin equivalents (RE)/g extract) was rich in flavonoids compared with ethyl acetate and methanol extracts (2.78 and 2.83 mg RE/g extract, for the respective extracts). These findings reveal the interesting potential of C. cilicica as a valuable source of phytochemicals that can be used against common noncommunicable diseases, particularly against enzymes involved in neurodegenerative diseases.
{"title":"In vitro multiple pharmacological targets of Colutea cilicica Boiss. & Balansa\u0000 against key enzymes linked to neurodegenerative diseases, diabetes, and\u0000 hyperpigmentation","authors":"S. Uysal, R. Ceylan, A. Aktumsek, G. Guler, C. M. N. Picot, G. Zengin, M. Mahomoodally","doi":"10.5152/ISTANBULJPHARM.2018.396764","DOIUrl":"https://doi.org/10.5152/ISTANBULJPHARM.2018.396764","url":null,"abstract":"DOI : 10.5152/IstanbulJPharm.2018.396764 Prevention and treatment of noncommunicable diseases such as neurodegenerative diseases, diabetes, and hyperpigmentation using medicinal plants has attracted increasing attention during the past few decades. In this study, Colutea cilicica Boiss. & Balansa extracts (ethyl acetate, methanol, and water) were evaluated against key enzymes involved in neurodegenerative diseases, diabetes, and hyperpigmentation. The antioxidant (free radical scavenging, reducing power, β-carotene/linoleic acid, and phosphomolybdenum) and metal chelation properties were also investigated. The methanol extracts of C. cilicica vigorously inhibited the activities of acetylcholinesterase and butyrylcholinesterase (1.33 and 0.68 mg galantamine equivalents (GALAE)/g extract, respectively). It was observed that C. cilicica extracts possessed a higher inhibitory potential for α-glucosidase (2.71–1.23 mmol acarbose equivalents (ACAE)/g extract) than that for α-amylase (0.57–0.12 mmol ACAE/g extract). The water extract of C. cilicica showed potent radical scavenging capacity against DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ABTS (2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (42.46 and 57.70 mg trolox equivalents (TE)/g extract, respectively). Phytochemical determination showed that C. cilicica water extract (17.26 mg rutin equivalents (RE)/g extract) was rich in flavonoids compared with ethyl acetate and methanol extracts (2.78 and 2.83 mg RE/g extract, for the respective extracts). These findings reveal the interesting potential of C. cilicica as a valuable source of phytochemicals that can be used against common noncommunicable diseases, particularly against enzymes involved in neurodegenerative diseases.","PeriodicalId":14484,"journal":{"name":"İstanbul Journal of Pharmacy","volume":"57 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72608473","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}