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Novel (p-tolyl)-3(2H)-pyridazinone derivatives containing substituted-1,2,3-triazole moiety as new anti-Alzheimer agents: Synthesis, in vitro and in silico assays 新型含取代1,2,3-三唑的(对甲基)-3(2H)-吡嗪酮衍生物抗阿尔茨海默病新药物:合成、体外和硅检测
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-08-04 DOI: 10.55262/fabadeczacilik.1128446
İrem Bozbey, Gülce Taşkor Önel, B. Türkmenoğlu, S. Gürsoy, Esra Dilek
Alzheimer hastalığı (AH), demansın en yaygın nedeni olan kronik nörodejeneratif bir hastalıktır. Hastalığa yakalanma riski yaşla birlikte artar. Hastalığın histopatolojisi incelendiğinde senil amiloid plakları, nörofibriler yumak oluşumu, sinaps-nöron kaybı ve beyinde belirgin atrofi saptanır. Alzheimer hastalığında asetilkolin sentezinden sorumlu olan kolin asetil transferaz düzeyindeki azalma %58-90'dır. Mevcut ilaçlar hastalığın ilerlemesini durduramadığından, hastalığın temel nedenini hedef alan yeni ilaçlara büyük ihtiyaç vardır. Bu çalışmada asetilkolinesteraz inhibisyonu gösteren triazol-piridazinon türevi bileşikler sentezlenmiştir ve enzim inhibisyonları araştırılmıştır. Bileşik 6e, 0.049 ± 0.014 µM Ki değeri ile en güçlü inhibitör etkiyi göstermiştir (Takrin Ki= 0.226 ± 0.025 µM). Ayrıca sentezlenen tüm bileşikler için in-silico çalışmalar yapıldı.
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引用次数: 2
Glycosides Isolated from Leaf Extract of Phyllanthus muellerianus (Kuntze) Excell (Phyllanthaceae) Upregulated Cell-mediated Innate Immunity 江蓠叶提取物中分离的糖苷上调细胞介导的先天免疫
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-08-01 DOI: 10.55262/fabadeczacilik.1083066
Martha N. Ofokansi, O. Isiogugu, I. E. Peter, Matthas Agbo, F. C. Okoye, P. Akah
Intracellular pathogens are mainly eliminated by cell-mediated immunity offered by phagocytic cells like neutrophils, macrophages and monocytes. Two tannin glycosides, 1-O-galloyl-6-O-luteoyl-α-D-glucopyranoside (1) and 3-O-methylellagic acid 3'-O-α-rhamnopyranoside (2) were isolated from the ethyl acetate fraction (EF) of the methanol leaf extract of Phyllanthus muellerianus. The structures of the isolated compounds were elucidated by 1H-NMR and by mass spectroscopy. The effects of the isolated compounds on phagocytic competence of macrophages and neutrophils using in vitro models were evaluated. Compounds 1 and 2 significantly (p
细胞内病原体主要通过吞噬细胞如中性粒细胞、巨噬细胞和单核细胞提供的细胞介导免疫来消除。从余叶甲醇提取物的乙酸乙酯部分(EF)中分离得到1-O没食子酰基-6-O木犀油基-α- d -葡萄糖吡喃苷(1)和3-O甲基鞣花酸3′-O-α-鼠李糖苷(2)两个单宁苷类化合物。分离得到的化合物的结构经1H-NMR和质谱鉴定。用体外模型评价分离化合物对巨噬细胞和中性粒细胞吞噬能力的影响。化合物1和2显著(p
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引用次数: 0
The Role of Carbon Monoxide and Their Donor (CORM-2) in Skin Wound Healing in Mice 一氧化碳及其供体(CORM-2)在小鼠皮肤伤口愈合中的作用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-07-10 DOI: 10.55262/fabadeczacilik.1095369
S. Beschasnyi, Olena Hasiuk
Carbon monoxide, which is a toxic gas, has a beneficial effect on cells in low doses. It is known that low concentrations of this gas are produced in the body during the decay of heme-containing proteins and have pro-apoptotic, anti-inflammatory, anti-allergic, vasodilator effects, stimulating angiogenesis. The danger of using this gas is the difficulty of its dosage. CO donors are used to controlling the amount and gradual release of carbon monoxide. This study studied the effect of treatment with CO and donor CORM-2 on wound healing processes in laboratory mice. Treatment with CO and CORM-2 reduced the healing rate of skin wounds in laboratory mice. The greatest delay in healing was observed in animals whose wounds were treated with CO. In this group, aquaporin-3 mRNA expression was decreased to the smallest degree among all other animals. This most likely caused the appearance of crusts. CORM-2 treatment also led to a decrease in AQP3 mRNA expression, but no crusts were formed. This can be explained by the fact that CO is released slowly. Having a dry crust on the wound increases the healing time. But, the formation of a dry crust is useful in the healing of burns, because with a dry scab, pus cannot appear; with some degrees of burns, it prevents suppuration and creates a protective barrier. The study confirmed the hypothesis that CO and CORM-2 reduce AQP3 expression after treatment of damaged skin.
一氧化碳是一种有毒气体,低剂量对细胞有益。众所周知,在体内含血红素蛋白的衰变过程中会产生低浓度的这种气体,并具有促凋亡、抗炎、抗过敏、血管扩张作用,刺激血管生成。使用这种气体的危险在于它的剂量。一氧化碳供体用于控制一氧化碳的数量和逐渐释放。本研究研究了CO和供体CORM-2对实验小鼠伤口愈合过程的影响。用CO和CORM-2治疗可降低实验小鼠皮肤伤口的愈合速度。在伤口用一氧化碳处理的动物中,观察到愈合延迟最大。在这一组中,水通道蛋白-3 mRNA表达的下降程度是所有动物中最小的。这很可能导致了地壳的出现。CORM-2处理也导致AQP3 mRNA表达降低,但未形成结皮。这可以用CO释放缓慢的事实来解释。伤口上有一层干皮可以延长愈合时间。但是,干燥结痂的形成对烧伤的愈合是有用的,因为干燥的痂不会出现脓液;对于某种程度的烧伤,它可以防止化脓并形成保护屏障。本研究证实了CO和CORM-2在损伤皮肤处理后降低AQP3表达的假设。
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引用次数: 0
Synthesis of 2-Substitutedbenzimidazolium Tetrachloroplatinate(II) Compounds and Their Cytotoxic Activities on Different Cell Lines 2-取代苯并咪唑四氯铂酸酯类化合物的合成及其对不同细胞系的细胞毒活性
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-07-01 DOI: 10.55262/fabadeczacilik.1134520
Mahmut Gözelle, A. Kılıç Süloğlu
The aim of the study was the synthesis of novel platinum compoundshaving benzimidazole ligands and screening for their in vitro cytotoxicactivity on human cervical carcinoma HeLa, human lung carcinomaA549, and human lung epithelial Beas-2B cell lines. 2-Substitutedbenzimidazole ligands were synthesized by using appropriatealdehydes and o-phenylenediamine. Subsequently, 2-substitutedbenzimidazole ligands and potassium tetrachloroplatinate(II)(K2PtCl4) were used to synthesize 2-isopropylbenzimidazoletetrachloroplatinate(II) (K1) and 2-(1-methylpropyl)benzimidazoletetrachloroplatinate(II) monohydrate (K2). HRMS, IR, elementalanalysis, 1H-NMR, and melting point were used to characterizethe synthesized compounds. Cytotoxic activities against HeLa,A549, and Beas-2B cells after 48 h and 72 h incubation of theplatinum compounds were investigated via MTT assay. Cisplatinand carboplatin were used as reference drugs. The cytotoxic activityresults showed that K2 platinum compound displayed 53.42%±2.21(at 160 μM) on HeLa, 88.16%±0.22 (at 160 μM) on A549 and92.09%±0.57 (at 160 μM) on Beas-2B after 48 h incubation, K2displayed 27.42%±2.03 (at 160 μM) on HeLa, 93.95%±0.53(at 160 μM) on A549 and 91.99±0.22 (at 160 μM) on Beas-2Bafter 72 h incubation. Both of the platinum compounds have highercell inhibitory effects than reference drug carboplatin after 48 h incubation for tested cells.
本研究旨在合成新型含苯并咪唑配体铂类化合物,并筛选其对人宫颈癌HeLa、人肺癌aa549和人肺上皮Beas-2B细胞系的体外细胞毒活性。采用适当的醛和邻苯二胺合成了2-取代苯并咪唑配体。随后,用2-取代苯并咪唑配体和四氯铂酸钾(II)(K2PtCl4)合成2-异丙基苯并咪唑烯四氯铂酸盐(II)(K1)和2-(1-甲基丙基)苯并咪唑烯四氯铂酸盐(II)一水合物(K2)。利用HRMS、IR、元素分析、1H-NMR和熔点对合成的化合物进行表征。MTT法观察铂类化合物对HeLa、A549和Beas-2B细胞的细胞毒活性。以顺铂和卡铂为对照药。结果表明,K2铂化合物对HeLa的细胞毒活性为53.42%±2.21(160 μM),对A549的细胞毒活性为88.16%±0.22 (160 μM),对Beas-2B的细胞毒活性为92.09%±0.57 (160 μM),对HeLa的细胞毒活性为27.42%±2.03 (160 μM),对A549的细胞毒活性为93.95%±0.53(160 μM),对Beas-2B的细胞毒活性为91.99±0.22 (160 μM)。这两种铂化合物在被试细胞孵育48小时后都比对照药物卡铂具有更高的细胞抑制作用。
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引用次数: 0
Hastaların İlaç Uyumunun Arttırılmasında Toplum Eczacılarının Rolü
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-22 DOI: 10.55262/fabadeczacilik.1092310
Felat Çelebi̇, Muammer Çalikuşu, Gülbin Özçeli̇kay
In this study, the importance of compliance to treatment for the patient to benefit from the treatment, and the effects of patient compliance were determined. The study is a decisive type of research. The forms with 5-point Likert-type questions created by the researchers were asked to community pharmacists via the Internet. 110 pharmacists from different parts of Turkey participated in the survey. The data obtained in the research were analyzed with the SPSS ver. 25.0 program. The significance level (α) was determined as 0.05 in the analyzes made in the study. The Cronbach-alpha reliability coefficient for the developed scale was found to be 0.847. In this study, it is found that community pharmacists make an effort to increase the drug compliance of patients. There was no significant difference between the age and professional experience of the pharmacist in improving patient compliance. Pharmacists need to work more systematically to improve patients' drug compliance. It is thought that the concept of drug compliance is frequently included in the education curriculum of Pharmacy Schools. Still, the necessary educational content and learning opportunities are not sufficient to increase it.
在本研究中,依从性对于患者从治疗中获益的重要性,以及患者依从性的影响被确定。这是一种决定性的研究。研究人员通过互联网向社区药剂师询问了5分李克特式问题,来自土耳其不同地区的110名药剂师参与了调查。使用SPSS软件对研究中获得的数据进行分析。25.0项目。在本研究的分析中,显著性水平(α)为0.05。编制的量表的Cronbach-alpha信度系数为0.847。本研究发现,社区药师努力提高患者的用药依从性。在提高患者依从性方面,药师年龄和从业经验差异无统计学意义。药剂师需要更系统地工作,以提高患者的药物依从性。人们认为,药物依从性的概念经常被纳入药学学校的教育课程。然而,必要的教育内容和学习机会不足以增加它。
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引用次数: 0
Leukotriene D4 Levels in Patıents With Breast Cancer Patıents乳腺癌患者体内白三烯D4水平
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-16 DOI: 10.55262/fabadeczacilik.1086291
S. Akaydin, Sümeyye Ramazanoğlu, Ece MİSER SALİHOĞLU, H. Karanlık, S. Demokan
Leukotriene D4 (LTD4) is an inflammatory mediator synthesized in the arachidonic acid pathway and has been reported to induce cell proliferation and survival in cancer. LTD4 is synthesized from LTC4 by the enzyme gamma-glutamyltransferase (GGT). Here, we examined serum LTD4 levels and the relationship of LTD4 with GGT in patients with breast cancer. For that purpose, serum samples were taken from 43 patients diagnosed with breast cancer and 8 healthy controls. The patients were divided into five subgroups, as Luminal A, Luminal B, Luminal B-HER2(+), HER2(+) and triple negative. LTD4 levels were measured by ELISA method. Mean levels of LTD4 in the patients were significantly higher than in healthy controls [3,43 (2,21) ng/mL vs 1,47 (0,46) ng/mL; p < 0.05]. According to the molecular subtypes, serum LTD4 levels were found to be significantly higher in the Luminal A, Luminal B and Triple (-) subgroups than in the controls (p
白三烯D4 (LTD4)是花生四烯酸途径合成的一种炎症介质,据报道可诱导肿瘤细胞增殖和存活。LTD4是由LTC4通过谷氨酰转移酶(GGT)合成的。在这里,我们检测了乳腺癌患者血清LTD4水平以及LTD4与GGT的关系。为此,研究人员采集了43名乳腺癌患者和8名健康对照者的血清样本。将患者分为Luminal A、Luminal B、Luminal B-HER2(+)、HER2(+)和三阴性5个亚组。ELISA法检测LTD4水平。患者LTD4的平均水平显著高于健康对照组[3,43 (2,21)ng/mL vs 1,47 (0,46) ng/mL;P < 0.05]。根据分子亚型,Luminal A、Luminal B和Triple(-)亚组的血清LTD4水平明显高于对照组(p
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引用次数: 0
Development of Innovative Cosmetic Formulations to Help Fungal Treatment and Testing the Efficiency of Formulations 创新化妆品配方的开发,以帮助真菌治疗和测试配方的效率
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-16 DOI: 10.55262/fabadeczacilik.1100973
G. Yener, Caner Acar
In the fungus of hands and toenails, the thickening of the nail and its yellow color are the first signs of attention. Fungus on the nails of the hands and feet is often caused by Trichophyton rubrum dermatophyte. They have antifungal properties due to the components found in lavender oil, geranium oil and tea tree oil structures. Oral antifungal agents used for treatment of nail fungi have serious side effects especially on liver. Therefore, topical applications have been given importance in recent years. However, in topical applications antifungal agents have difficulties in sending to the target area. For this reason, nanoemulsion technology was preferred in the study. Nanoemulsion formulations of essential oils were prepared using ultrasonication method. Centrifugal and thermal test were applied as preliminary stability to the formulations and the pH value, viscosity, droplet size and polidispersity index of the formulations passing this step were measured and organoleptic controls were performed. Antifungal efficacy and release studies were performed on the formulations F4P3-I (pelargonium), F4P3-L (lavender), F4P3-C (tea tree) and F4P3-K (mixture) which were successful as a result of all the tests. According to the study, it was concluded that F4P3-I, F4P3-L, F4P3-Ç, F4P3-K formulations may help in the treatment of fungi.
在手和脚趾甲的真菌中,指甲的增厚和黄色是引起注意的第一个迹象。手脚指甲上的真菌通常是由红毛癣菌引起的。由于薰衣草油、天竺葵油和茶树油结构中的成分,它们具有抗真菌的特性。用于治疗指甲真菌的口服抗真菌药物有严重的副作用,特别是对肝脏。因此,近年来,局部应用受到重视。然而,在局部应用中,抗真菌药物很难到达目标区域。因此,纳米乳技术是研究的首选技术。采用超声法制备了精油纳米乳液配方。采用离心和热试验对配方进行初步稳定性测试,并对通过该步骤的配方进行pH值、粘度、液滴大小和多元指数的测定,并进行感官控制。对配方F4P3-I(天竺葵)、F4P3-L(薰衣草)、F4P3-C(茶树)和F4P3-K(混合物)进行了抑菌效果和释放研究,所有试验均成功。研究结果表明,F4P3- i、F4P3- l、F4P3-Ç、F4P3- k等配方对真菌有一定的治疗作用。
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引用次数: 0
Quercetin Based Standardization Of Polyherbal Anti-Gout Remedy And İts Molecular Docking Study Against Anti-Gout And Anti-İnflammatory Protein Targets 基于槲皮素的多药抗痛风药物标准化及抗痛风与抗-İnflammatory蛋白靶点的İts分子对接研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-08 DOI: 10.55262/fabadeczacilik.1085825
Ayisha Shaukat, K. Hussain
A five-herb containing traditional homemade medicine is extensively used to treat gout but has not been standardized for quercetin content. Therefore, the current study describes a reversed-phase liquid chromatographic method for quercetin determination in traditional herbal remedy. The elution was carried out using aqueous 2.0% acetic acid, acetonitrile and tetrahydrofuran (55:40:5, V/V/V) as mobile phase at flow rate of 0.8 mL/min and detection was performed using diode array detector operated at 370 nm. The response of the detector was linear in the range investigated (2.5-160.0 µg/mL) with R2 = 0.996. Results of recovery (98.26-103.22%, SD
一种含有传统自制药物的五种草药被广泛用于治疗痛风,但槲皮素含量尚未标准化。因此,本研究建立了一种反相液相色谱法测定传统中药中槲皮素的方法。以2.0%醋酸、乙腈和四氢呋喃(55:40:5,V/V/V)为流动相,流速为0.8 mL/min,检测采用二极管阵列检测器,工作波长为370 nm。在2.5 ~ 160.0µg/mL范围内呈线性关系,R2 = 0.996。回收率为98.26 ~ 103.22%,SD
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引用次数: 2
Conductor of the Astrocyte-Neuron Metabolic Orchestra 星形细胞-神经元代谢乐团指挥
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-03-01 DOI: 10.55262/fabadeczacilik.1078905
M. Welcome
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引用次数: 0
Recent Advancements in Antipsoriatic Therapy: An Update 抗银屑病治疗的最新进展
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-03-01 DOI: 10.55262/fabadeczacilik.1078882
Shaik Shafiulla, S. Dhaneshwar
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引用次数: 1
期刊
Fabad Journal of Pharmaceutical Sciences
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