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Biological, phytochemical, and physico-chemical properties of two commercial Nigella sativa seed oils: A comparative analysis 两种商业黑皮籽油的生物学、植物化学和物理化学性质:比较分析
Pub Date : 2019-10-11 DOI: 10.26650/ISTANBULJPHARM.2018.180003
M. Z. Aumeeruddy, Z. Aumeeruddy-Elalfi, H. Neetoo, G. Zengin, B. Fibrich, S. Rademan, A. B. V. Staden, K. Szuman, I. Lambrechts, N. Lall, M. Mahomoodally
This study was designed to evaluate and correlate the biological, phytochemical, and physicochemical properties of two NSS (Nigella sativa seed) oils (N1 and N2). The biological activity was evaluated in terms of antibacterial, antioxidant (nitric oxide scavenging), antielastase, antityrosinase, antimelanogenic, and anticancer activity. Physicochemical properties including colour, total soluble solids (TSS), and density were also investigated. N2 exhibited higher antibacterial, NO scavenging, extracellular antimelanogenic, and anticancer activity against the HeLa cell line compared to N1, which showed higher antityrosinase activity. TPC (total phenolic content) and TFC (total flavonoid content) of N1 were significantly higher than N2 while TTC (total tannin content) was higher in N2. In fact, TTC was strongly correlated (R=1.000) with the antioxidant, extracellular antimelanogenic, and HeLa cell inhibitory activity. To conclude, NSS oil may be considered as a complementary and alternative therapy in the management of infectious and chronic diseases but warrants further in vivo pharmacological validation and toxicological analysis.
本研究旨在评价和比较两种NSS (Nigella sativa seed)油(N1和N2)的生物学、植物化学和理化性质。从抗菌、抗氧化(清除一氧化氮)、抗弹性酶、抗酪氨酸酶、抗黑色素瘤和抗癌活性等方面对其生物活性进行了评价。理化性质包括颜色、总可溶性固形物(TSS)和密度也进行了研究。N2对HeLa细胞株具有较高的抗菌、NO清除、细胞外抗黑素生成和抗癌活性,而N1具有较高的抗酪氨酸酶活性。N1处理的总酚含量(TPC)和总黄酮含量(TFC)显著高于N2处理,总单宁含量(TTC)显著高于N2处理。事实上,TTC与抗氧化、细胞外抗黑素生成和HeLa细胞抑制活性密切相关(R=1.000)。综上所述,NSS油可能被认为是治疗感染性和慢性疾病的补充和替代疗法,但需要进一步的体内药理验证和毒理学分析。
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引用次数: 3
Ceragenins exhibiting promising antimicrobial activity against various multidrug resistant Gram negative bacteria 对多种多重耐药革兰氏阴性菌具有良好的抗菌活性
Pub Date : 2019-10-11 DOI: 10.26650/ISTANBULJPHARM.2018.400730
Ozlem Oyardi, P. Savage, Alper Akçalı, Z. Erturan, C. Bozkurt-Guzel
DOI : 10.26650/IstanbulJPharm.2018.400730 Ceragenins are novel promising agents for the treatment of infections caused by multi-drug resistant microorganisms. Since colistin resistance has become a worldwide problem, the need for new treatment agents has been increasing steadily. Therefore, this study aimed to investigate in vitro antimicrobial activities of ceragenins (Cationic Steroid Antibiotics) (CSA-8, CSA-13, CSA-142 and CSA-192) against multidrug resistant Gram negative isolates from Turkey. Experiments were performed by using broth microdilution method against Klebsiella pneumoniae, Morganella morganii, Pseudomonas aeruginosa and Stenotrophomonas maltophilia isolates. All microorganisms except for three isolates were identified as multidrug resistant. Among tested ceragenins, CSA-13 showed the best results (MIC: 8-64 µg/ml). Nevertheless, the antimicrobial activity of CSA-8 was not significant. In conclusion, ceragenins appear to be a good candidate as antimicrobial therapy in the presence of multidrug (including colistin) resistant microorganisms.
Ceragenins是治疗多重耐药微生物引起的感染的新型有希望的药物。由于粘菌素耐药性已成为一个世界性的问题,对新的治疗药物的需求一直在稳步增加。因此,本研究旨在研究阳离子类固醇抗生素cergenins (CSA-8、CSA-13、CSA-142和CSA-192)对土耳其革兰氏阴性多重耐药菌株的体外抗菌活性。采用微量肉汤稀释法对分离的肺炎克雷伯菌、莫氏摩根菌、铜绿假单胞菌和嗜麦芽窄养单胞菌进行了实验。除3株外,其余微生物均被鉴定为多重耐药。其中,CSA-13的MIC值为8 ~ 64µg/ml,效果最好。但CSA-8的抑菌活性不显著。总之,在存在多药(包括粘菌素)耐药微生物的情况下,皮草蛋白似乎是一个很好的抗微生物治疗候选者。
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引用次数: 2
The anatomical properties of Scabiosa atropurpurea L. (Caprifoliaceae) 杏叶卡皮草(capriaceae)的解剖性质
Pub Date : 2019-10-11 DOI: 10.5152/ISTANBULJPHARM.2018.376278
Y. Yeşil, Zeynep Büşra Erarslan
DOI : 10.5152/IstanbulJPharm.2018.376278 Scabiosa atropurpurea L. (Caprifoliaceae), a medicinal plant traditionally known as “Mor uyuzotu or Şeytanotu” in Turkey, has been used for treating acne, bronchitis, cold, and cough. Although phytochemical studies are available, there are no taxonomic studies related to this plant. The aim of this study was to investigate the anatomy of leaf, stem, and root of S. atropurpurea. Detailed photographs of plant parts were taken, and measurements of the leaf, stem, and root were carried out. The cross section of the stem revealed a single-layered epidermis containing one-celled simple eglandular trichomes and rarely one-celled hook-shaped eglandular trichomes. The cortex showed multilayered parenchymatous cells and a single-layered endodermis. The phloem was followed by the cambium, and the xylem was lignified. The pith was made up of parenchymatous cells. The leaves are bifacial and amphistomatic and stomata are mesomorphic in the cross section and also stomata are anomocytic in the surface section. The cross section of the root showed that the epidermis was replaced with the periderm. Under the phloem, which had few layers, the xylem was composed of tracheary elements surrounded with sclerenchymatous cells.
(Caprifoliaceae)是一种药用植物,在土耳其传统上被称为“Mor uyuzotu或Şeytanotu”,已被用于治疗痤疮,支气管炎,感冒和咳嗽。虽然植物化学研究是可用的,但没有与该植物相关的分类学研究。本研究的目的是研究紫荆的叶、茎和根的解剖结构。拍摄了植物各部分的详细照片,并对叶、茎和根进行了测量。茎的横切面为单层表皮,含有单细胞的简单腺毛,很少有单细胞的钩状腺毛。皮层可见多层薄壁细胞和单层内胚层。韧皮部之后是形成层,木质部木质化。髓由薄壁细胞组成。叶片为两面形和两口形,横截面气孔为中形,表面气孔为无形细胞。根的横切面显示表皮被周皮所取代。在韧皮部下面,木质部由被厚壁细胞包围的管状分子组成。
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引用次数: 6
Purification and partial characterization of thioredoxin reductase from the hepatopancreas of the mollusc Mytilus galloprovincialis Lam. 紫贻贝肝胰脏硫氧还蛋白还原酶的纯化及部分性质。
Pub Date : 2019-10-11 DOI: 10.5152/ISTANBULJPHARM.2018.382627
E. Acar, Gozde Hasbal, N. Ozsoy
DOI : 10.5152/IstanbulJPharm.2018.382627 Thioredoxin reductase (TrxR, EC 1.6.4.5) is a ubiquitous flavoenzyme that is present from Archaea to humans, and it is the only enzyme capable of catalyzing the reduction of thioredoxin (Trx) by nicotinamide adenine dinucleotide phosphate (NADPH). Although TrxR has been purified and characterized from different bacteria, plants, and mammalian organisms, a survey of the literature revealed no studies on the purification and characterization of TrxR from the mussel Mytilus galloprovincialis Lam. In this study, TrxR was purified to homogeneity from the hepatopancreatic tissue of M. galloprovincialis Lam. by extraction, ammonium sulfate precipitation, and DEAE-Sepharose CL-6B anion and 2’,5‘-ADP-agarose chromatographies, and some of its kinetic properties were examined. Molar mass determined by sodium dodecyl sulfate polyacrylamide gel electrophoresis revealed only a single protein band corresponding to a molecular weight of 35 kDa. Optimum pH and temperature were found to be 7.0 and 60°C, respectively. Km and Vmax values for NADPH were found to be 85 µmol and 4.82 µmol/min/mg, respectively. For 5,5ʹ-dithiobis (2-nitrobenzoic) acid (DTNB), the Km and Vmax values were 193 µmol and 1.32 µmol/min/mg, respectively. Increasing the knowledge on the kinetic properties of TrxR will significantly increase the prospects of enzyme application as an oxidative stress biomarker in mussels and fishes for monitoring contamination in coastal environments.
硫氧还蛋白还原酶(TrxR, EC 1.6.4.5)是一种普遍存在的黄酶,从古细菌到人类,它是唯一能够催化烟酰胺腺嘌呤二核苷酸磷酸(NADPH)还原硫氧还蛋白(Trx)的酶。虽然TrxR已经从不同的细菌、植物和哺乳动物生物中纯化和表征,但文献调查显示,没有关于贻贝Mytilus galloprovincialis Lam中TrxR的纯化和表征的研究。本研究从猪肝胰腺组织中纯化TrxR至均质性。通过萃取、硫酸铵沉淀、DEAE-Sepharose CL-6B阴离子层析和2′,5′- adp -琼脂糖层析,考察了其部分动力学性质。用十二烷基硫酸钠聚丙烯酰胺凝胶电泳测定其摩尔质量,结果显示只有一条分子量为35 kDa的蛋白质条带。最佳pH值为7.0℃,最佳温度为60℃。NADPH的Km和Vmax分别为85µmol和4.82µmol/min/mg。5,5′-二硫比斯(2-硝基苯甲酸)酸(DTNB)的Km和Vmax分别为193µmol和1.32µmol/min/mg。增加对TrxR动力学特性的了解将大大增加酶作为贻贝和鱼类氧化应激生物标志物在沿海环境污染监测中的应用前景。
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引用次数: 0
Synthesis, characterization and biological activity studies on amide derivatives 酰胺类衍生物的合成、表征及生物活性研究
Pub Date : 2019-10-11 DOI: 10.26650/ISTANBULJPHARM.2018.18007
S. Türk, K. Turan, S. Ulusoy, S. Karakuş, G. Boşgelmez-Tinaz
DOI : 10.26650/IstanbulJPharm.2018.18007 In this study, with intent to find out novel anti-biofilm and antiviral agents, a series of amide  derivatives were synthesized and their structures were elucidated by FT-IR and 1H-NMR and  13C-NMR and MS methods. And also, their purity were proven by TLC, HPLC and elemental  analyses. And finally, the synthesized compounds were examined for their biofilm formation  and swarming motility inhibitory activities in P. aeruginosa PA01. These compounds were  found to reduce biofilm formation by 8.7-25.6% and swarming motility by 18.3-33.8% in P.  aeruginosa PA01 at a concentration of 200 μM. Besides, all of the compounds were evaluated for their antiviral activity against influenza A viruses. The plaque inhibition assays indicated  that compound 6 (N-(4-{[5-(ethylamino)-1,3,4-thiadiazol-2-yl]methyl}phenyl)-4-  fluorobenzamide) has considerable inhibitory effect on influenza A virus plaque formation.
为了寻找新的抗生物膜和抗病毒药物,本研究合成了一系列酰胺衍生物,并通过FT-IR和1H-NMR以及13C-NMR和MS方法对其结构进行了鉴定。并通过薄层色谱、高效液相色谱和元素分析对其纯度进行了验证。最后,对合成的化合物在铜绿假单胞菌PA01中的生物膜形成和蜂群运动抑制活性进行了研究。在200 μM浓度下,这些化合物可使P. aeruginosa PA01的生物膜形成减少8.7-25.6%,使蜂群运动减少18.3-33.8%。此外,对所有化合物的抗病毒活性进行了评价。斑块抑制实验表明,化合物6 (N-(4-{[5-(乙胺)-1,3,4-噻二唑-2-基]甲基}苯基)-4-氟苯酰胺)对甲型流感病毒斑块形成具有显著的抑制作用。
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引用次数: 0
Alkaloid profiling in Galanthus gracilis Celak. from western Turkey by GC/MS 葛兰的生物碱谱分析。通过气相色谱/质谱分析
Pub Date : 2019-10-11 DOI: 10.26650/ISTANBULJPHARM.2018.422525
Ç. Karakoyun
DOI : 10.26650/IstanbulJPharm.2018.422525 Galanthus L. is generally acknowledged as a valuable biological source due to its Amaryllidaceae alkaloids with unusual chemical structures and a wide variety of biological activities. Among these alkaloids, galanthamine is the first example of their practical application in medicine as a potent and selective inhibitor of the enzyme acetylcholinesterase, and already present on the market as a therapeutic agent for Alzheimer’s disease. Lycorine is the main Amaryllidaceae alkaloid deeply investigated for its biological activity for many years. In this study the alkaloidal profile of G. gracilis collected from western Aegean (Alankiyi/Bayindir) will be illustrated for the first time. GC-MS profiling was carried out on the crude alkaloidal extract obtained from dried and powdered plant material. 11 alkaloids were detected by GC-MS, including graciline, demethylhomolycorine and tazettine as the major ones.
由于其具有不同寻常的化学结构和多种生物活性的Amaryllidaceae生物碱,Galanthus L.被普遍认为是一种有价值的生物来源。在这些生物碱中,加兰他敏是它们作为乙酰胆碱酯酶的有效和选择性抑制剂在医学上实际应用的第一个例子,并且已经作为阿尔茨海默病的治疗剂出现在市场上。石蒜碱是菊科生物碱的主要成分,其生物活性已被研究多年。本研究首次对在爱琴海西部地区(Alankiyi/Bayindir)采集的凤尾草生物碱谱进行了分析。采用气相色谱-质谱法对干燥和粉末状植物原料的生物碱粗提物进行了分析。GC-MS共检测到11种生物碱,其中以格西林、去甲基高氯碱和他泽汀为主要成分。
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引用次数: 0
Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring 一种新型含氮杂环苯并噻唑抗结核活性的设计、合成和评价
Pub Date : 2019-10-09 DOI: 10.5152/ISTANBULJPHARM.2018.320135
S. Sarkar
DOI: 10.5152/IstanbulJPharm.2018.320135 Recent studies have demonstrated that 2-amino-substituted benzothiazole derivatives exhibit significant antitubercular activity. In this study, new compounds of benzothiazole-containing azetidinone derivatives were designed and synthesized using substituted benzaldehydeN-(5fluoro-1,3-benzothiazol-2-yl) semicarbazone, chloroacetyl chloride, and  triethylamine in DMF. The structures of the synthesized compounds were characterized by TLC, IR, elemental analysis, and 1H NMR. In vitro screening data revealed that all the designed and synthesized compounds A6–A10 exhibited the ability to inhibit the growth of Mycobacterium tuberculosis in terms of MIC. Variable and modest activity was observed against the investigated strains of bacteria; however, the compound A6 exhibited significant antitubercular activity against M. tuberculosis H37Rv (MTCC 200) compared to that of the reference drugs isoniazid and rifampicin. These experimental data were consistent with our computational predictions in terms of the compound A6 that exhibited a satisfactory backbone for the antitubercular activity, perhaps due to an increase in hydrophobicity resulting in better penetration through the cell wall of M. tuberculosis.
最近的研究表明,2-氨基取代的苯并噻唑衍生物具有显著的抗结核活性。本研究以取代苯甲醛-(5氟-1,3-苯并噻唑-2-基)氨基脲、氯乙酰氯和三乙胺为原料,设计并合成了含苯并噻唑的氮杂二酮衍生物。通过薄层色谱(TLC)、红外光谱(IR)、元素分析和核磁共振氢谱(1H NMR)对合成的化合物进行了结构表征。体外筛选数据显示,设计和合成的化合物A6-A10在MIC方面均表现出抑制结核分枝杆菌生长的能力。对所调查的细菌菌株有不同的和适度的活性;与对照药异烟肼和利福平相比,化合物A6对结核分枝杆菌H37Rv (MTCC 200)具有显著的抗结核活性。这些实验数据与我们的计算预测一致,化合物A6表现出令人满意的抗结核活性,可能是由于疏水性的增加导致更好地穿透结核分枝杆菌的细胞壁。
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引用次数: 2
A validated method without derivatization for the determination of Letrozole by high performance liquid chromatography-fluorimetric method for pharmaceutical preparation 一种经验证的药物制剂用高效液相色谱-荧光法测定来曲唑的无衍生化方法
Pub Date : 2019-10-09 DOI: 10.5152/ISTANBULJPHARM.2018.397094
Cem Kaplan, D. Unal
DOI : 10.5152.IstanbulJPharm.2018.397094 A high performance liquid chromatography method has been developed for determination of letrozole in tablets. The method has developed in reverse phase column with acetonitrile-50.0 mM phosphoric acid solution, pH:7 (50:50, v/v) and 0.7 mL/min flow rate by using a fluorimetric detector. Letrozole has natural fluorescence properties, and there is no need for derivatization for this molecule. The detector was set at 256, 585 nm for excitation and emission wavelength respectively. The method was validated in accuracy, precision, specificity, linearity and system suitability parameters are studied.  The linear range was found 50-700 ng/mL. The limit of detection and quantification for letrozole was found to be 14-50 ng/mL respectively. The recovery of drug is found to be 98.8%. The developed method has been validated and successfully applied to tablet analysis of drug substance. This method is simple, reproducible and can be used safely for routine analysis of letrozole in tablets.
建立了高效液相色谱法测定来曲唑片剂含量的方法。方法采用反相色谱柱,以乙腈-50.0 mM磷酸溶液,pH:7 (50:50, v/v),流速0.7 mL/min为荧光检测器。来曲唑具有天然的荧光性质,该分子不需要衍生化。探测器的激发波长为256 nm,发射波长为585 nm。验证了该方法的准确性、精密度、专一性、线性度和系统适宜性参数。线性范围为50 ~ 700 ng/mL。来曲唑的检出限和定量限分别为14 ~ 50 ng/mL。药物回收率为98.8%。所建立的方法已被验证,并成功地应用于原料药的片剂分析。该方法操作简便,重现性好,可用于来曲唑片剂的常规分析。
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引用次数: 2
Plants used as painkillers in folk medicine in Turkey IV – TOOTHACHE 土耳其民间医药中用作止痛药的植物IV -牙痛
Pub Date : 2019-10-09 DOI: 10.5152/ISTANBULJPHARM.2018.412321
Meryem Seyda Erbay, S. Anıl, G. Melikoğlu
DOI : 10.5152/IstanbulJPharm.2018.412321 Turkey has a rich plant diversity due to its geography and many of these plants are used in the treatment of various diseases. The usage of these medicinal plants has been passed down from generation to generation. Ethnobotanical studies are used to record traditional treatment methods and this information is intended to contribute to drug development studies. This study (which is the fourth article in a series focusing on plants with painkilling properties) details the plants used to combat toothache. In this survey, which was prepared by screening ethnobotanical research, a total of 52 taxa were traditionally used in toothache treatment in Turkey. Scientific and local names, families, parts used, and treatment methods of these plants were recorded. According to the results of the research, the most common families are Lamiaceae, Asteraceae, Solanaceae, Euphorbiaceae, Liliaceae and Rosaceae. The most commonly used taxa in different regions of Turkey are Cornus mas, Dianthus zonatus var. zonatus and Hyocyamus niger. These plants contain analgesic and anti-inflammatory compounds. These plants are usually used externally as extracts (infusion/decoction) as well as are used directly. However, a few species are also used externally.
由于其地理位置,土耳其拥有丰富的植物多样性,其中许多植物被用于治疗各种疾病。这些药用植物的用法是代代相传的。民族植物学研究用于记录传统的治疗方法,这些信息旨在为药物开发研究做出贡献。这项研究(这是关注具有止痛特性的植物系列的第四篇文章)详细介绍了用于治疗牙痛的植物。在本次调查中,通过筛选民族植物学研究,土耳其共有52个分类群传统上用于牙痛治疗。记录了这些植物的学名和地名、科、使用部位和处理方法。根据研究结果,最常见的科是兰科、菊科、茄科、大戟科、百合科和蔷薇科。土耳其不同地区最常用的分类群是山茱萸(Cornus mas)、石竹(Dianthus zonatus var. zonatus)和黑山茱萸(Hyocyamus niger)。这些植物含有止痛和抗炎的化合物。这些植物通常作为提取物(输液/煎剂)外用,也可直接使用。然而,少数品种也用于外部。
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引用次数: 7
Overview on nanotechnology based cosmeceuticals to prevent skin aging 以纳米技术为基础的药妆预防皮肤老化概述
Pub Date : 2019-10-09 DOI: 10.5152/ISTANBULJPHARM.2018.424278
Gizem Otlatıcı, Gizem Yeğen, S. Güngör, B. Aksu
DOI : 10.5152/IstanbulJPharm.2018.424278 Skin aging is an inevitable process and the highest contributing factor to this process is the effect of ultraviolet rays. However, nutrients, dry skin, smoking, hormones and gravity are also other important factors. Skin aging is classified as intrinsic (chronological) and extrinsic (photo-aging). Generally, in aged skin, effects such as thinning, loss of elasticity, spotting, wrinkles and sagging are observed. There are various approaches to preventing skin aging. The most widely used age combating substances in cosmeceuticals are kinetin, retinoids, sun filters, herbal ingredients (such as resveratrol, turmeric, and green tea), and antioxidants (such as alpha-tocopherol, ascorbic acid, coenzyme Q10 and lipoic acid). In recent years, these molecules have been formulated as nanosized carriers such as vesicular systems, polymeric and lipid nanoparticles, nanoemulsions, dendrimers, and fullerenes. Novel carrier systems have a lot of advantages when compared to conventional formulations. In this review, an overview of cosmetic, product-oriented solutions for skin aging is given and different approaches to combat aging are summarized.
DOI: 10.5152/ istanbuljpharmacy .2018.424278皮肤老化是一个不可避免的过程,而这一过程的最高促成因素是紫外线的影响。然而,营养、皮肤干燥、吸烟、激素和重力也是其他重要因素。皮肤老化分为内在(时间)和外在(光老化)。通常,在老化的皮肤中,会观察到诸如变薄、失去弹性、斑点、皱纹和下垂等影响。预防皮肤老化的方法有很多。药妆中最广泛使用的抗衰老物质是动素、类维生素a、太阳过滤器、草药成分(如白藜芦醇、姜黄和绿茶)和抗氧化剂(如α -生育酚、抗坏血酸、辅酶Q10和硫辛酸)。近年来,这些分子已被配制成纳米级载体,如囊泡系统、聚合物和脂质纳米颗粒、纳米乳液、树状大分子和富勒烯。与传统配方相比,新型载体系统具有许多优点。在这篇综述中,概述了以化妆品为导向的皮肤衰老解决方案,并总结了对抗衰老的不同方法。
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引用次数: 9
期刊
İstanbul Journal of Pharmacy
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