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N-ASETİL SİSTEİNİN ACINETOBACTER BAUMANNII İZOLATLARINA KARŞI ANTİMİKROBİYAL ETKİSİ VE ANTİBİYOTİKLERLE ETKİLEŞİMİ 正乙酰半胱氨酸对鲍曼不动杆菌分离株的抗微生物活性以及与抗生素的相互作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-02-05 DOI: 10.33483/jfpau.1358483
Alparslan Semih Salan, Suzan Ökten
Objective: The objective of this study was to delve into the effect of N-acetylcysteine (NAC) molecule on the minimum inhibitory concentration (MIC) of meropenem, ciprofloxacin, and gentamicin in clinical isolates of Acinetobacter baumannii, aiming to find potential alternatives for the treatment of bacterial infections that are resistant to conventional antibiotics.Material and Method: The study included 25 A. baumannii isolates that were confirmed to be resistant to meropenem, ciprofloxacin, and gentamicin. The susceptibility of antibiotics was re-evaluated in the presence of NAC using the microdilution method. FIC indexes were calculated based on the checkerboard test results to determine the effect of the combination, defined as synergistic or additive.Result and Discussion: The study demonstrated that NAC molecule, when used alongside meropenem, ciprofloxacin, and gentamicin, effectively reduced the MIC values of these antibiotics against Acinetobacteria. Furthermore, NAC molecule exhibited a synergistic effect when combined with meropenem. Additive effects were observed in all isolates for the GEN-NAC and CIP-NAC combinations. In conclusion, the findings suggest that NAC molecule could serve as a new alternative for combined drug therapy, offering a promising approach to treatment.
研究目的本研究的目的是探讨 N-乙酰半胱氨酸(NAC)分子对美罗培南、环丙沙星和庆大霉素在鲍曼不动杆菌临床分离株中的最小抑菌浓度(MIC)的影响,旨在寻找治疗对传统抗生素耐药的细菌感染的潜在替代方案:研究包括 25 个已确认对美罗培南、环丙沙星和庆大霉素耐药的鲍曼不动杆菌分离株。在有 NAC 的情况下,使用微量稀释法对抗生素的敏感性进行了重新评估。根据棋盘试验结果计算 FIC 指数,以确定组合的效果,即协同作用或相加作用:研究表明,当 NAC 分子与美罗培南、环丙沙星和庆大霉素同时使用时,可有效降低这些抗生素对醋肽杆菌的 MIC 值。此外,当 NAC 分子与美罗培南联合使用时,还能产生协同效应。在 GEN-NAC 和 CIP-NAC 组合的所有分离物中都观察到了相加效应。总之,研究结果表明,NAC 分子可作为联合药物疗法的新替代品,为治疗提供了一种前景广阔的方法。
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引用次数: 0
N-ASETİL SİSTEİNİN ACINETOBACTER BAUMANNII İZOLATLARINA KARŞI ANTİMİKROBİYAL ETKİSİ VE ANTİBİYOTİKLERLE ETKİLEŞİMİ 正乙酰半胱氨酸对鲍曼不动杆菌分离株的抗微生物活性以及与抗生素的相互作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-02-05 DOI: 10.33483/jfpau.1358483
Alparslan Semih Salan, Suzan Ökten
Objective: The objective of this study was to delve into the effect of N-acetylcysteine (NAC) molecule on the minimum inhibitory concentration (MIC) of meropenem, ciprofloxacin, and gentamicin in clinical isolates of Acinetobacter baumannii, aiming to find potential alternatives for the treatment of bacterial infections that are resistant to conventional antibiotics.Material and Method: The study included 25 A. baumannii isolates that were confirmed to be resistant to meropenem, ciprofloxacin, and gentamicin. The susceptibility of antibiotics was re-evaluated in the presence of NAC using the microdilution method. FIC indexes were calculated based on the checkerboard test results to determine the effect of the combination, defined as synergistic or additive.Result and Discussion: The study demonstrated that NAC molecule, when used alongside meropenem, ciprofloxacin, and gentamicin, effectively reduced the MIC values of these antibiotics against Acinetobacteria. Furthermore, NAC molecule exhibited a synergistic effect when combined with meropenem. Additive effects were observed in all isolates for the GEN-NAC and CIP-NAC combinations. In conclusion, the findings suggest that NAC molecule could serve as a new alternative for combined drug therapy, offering a promising approach to treatment.
研究目的本研究的目的是探讨 N-乙酰半胱氨酸(NAC)分子对美罗培南、环丙沙星和庆大霉素在鲍曼不动杆菌临床分离株中的最小抑菌浓度(MIC)的影响,旨在寻找治疗对传统抗生素耐药的细菌感染的潜在替代方案:研究包括 25 个已确认对美罗培南、环丙沙星和庆大霉素耐药的鲍曼不动杆菌分离株。在有 NAC 的情况下,使用微量稀释法对抗生素的敏感性进行了重新评估。根据棋盘试验结果计算 FIC 指数,以确定组合的效果,即协同作用或相加作用:研究表明,当 NAC 分子与美罗培南、环丙沙星和庆大霉素同时使用时,可有效降低这些抗生素对醋肽杆菌的 MIC 值。此外,当 NAC 分子与美罗培南联合使用时,还能产生协同效应。在 GEN-NAC 和 CIP-NAC 组合的所有分离物中都观察到了相加效应。总之,研究结果表明,NAC 分子可作为联合药物疗法的新替代品,为治疗提供了一种前景广阔的方法。
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引用次数: 0
MICROMERIA MYRTIFOLIA BOISS. & HOHEN’İN BİYOLOJİK AKTİVİTELERİNİN BELİRLENMESİ 测定米克罗米瑞亚的生物活性
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-02-05 DOI: 10.33483/jfpau.1372535
Y. Yücel, Ebru ÖZDEMİR NATH
Objective: Lamiaceae family has a wide variety of well-known and lesser-known plants with strong medicinal qualities. The genus Micromeria Benth. is a member of this family consisting of herbaceous plants with a variety of significant biological, phytochemical, and ethnobotanical uses. In this study, the biological activities of methanol and ethanol extracts of Micromeria myrtifolia were evaluated.Material and Method: To demonstrate the antioxidant activity DPPH radical scavenging activity and total phenolic content assays were done. The effects of the extracts on acetylcholinesterase (AChE) and monoamine oxidase-A were then assessed. Result and Discussion: Methanol extract showed the highest DPPH scavenging activity, at the dose of 10 mg/ml with a value of 96.55%. For the highest concentration that can be applicable, AChE inhibitions for the methanol and ethanol extracts were 25% and 27%, respectively. On the other hand, the inhibitory effects of the ethanol and methanol extracts of the plant on MAO-A were determined; for the ethanol extract IC50 value was found as 32.5876 ± 0.89 g/ml, and for the methanol extract it was found as 34.6544 ± 0.76 g/ml. It can be told that M. myrtifolia can act as a potential antioxidant. With further research and investigation, it is thought that Micromeria myrtifolia could be used as a natural source for the treatment of various neurological diseases.
目的灯心草科(Lamiaceae)中有多种知名或不太知名的植物,具有很强的药用价值。本草纲目中的小叶紫檀属是该科中的一种草本植物,具有多种重要的生物学、植物化学和民族植物学用途。本研究评估了小叶紫檀甲醇和乙醇提取物的生物活性:为了证明其抗氧化活性,进行了 DPPH 自由基清除活性和总酚含量测定。然后评估了提取物对乙酰胆碱酯酶(AChE)和单胺氧化酶-A 的影响。结果与讨论甲醇提取物的 DPPH 清除活性最高,剂量为 10 mg/ml,清除率为 96.55%。在可适用的最高浓度下,甲醇和乙醇提取物对 AChE 的抑制率分别为 25% 和 27%。另一方面,测定了该植物的乙醇和甲醇提取物对 MAO-A 的抑制作用;乙醇提取物的 IC50 值为 32.5876 ± 0.89 g/ml,甲醇提取物的 IC50 值为 34.6544 ± 0.76 g/ml。由此可见,M. myrtifolia 可以作为一种潜在的抗氧化剂。随着进一步的研究和调查,人们认为桃金娘小叶可作为治疗各种神经系统疾病的天然药物。
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引用次数: 0
BAZI BENZOKSAZOL-2(3H)-ON/BENZOTİYAZOL-2(3H)-ON TÜREVLERİNİN SENTEZİ VE ALZHEİMER HASTALIĞINA KARŞI ETKİLERİNİN İNCELENMESİ 一些苯并恶唑-2(3H)-酮/苯并噻唑-2(3H)-酮衍生物的合成及其对老年痴呆症作用的研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-07 DOI: 10.33483/jfpau.1387244
Merve Bardakkaya, Burcu Kiliç, Deniz Doğruer
Amaç: Bu çalışmada benzoksazolon/benzotiyazolon halkası taşıyan asetamit türevi 28 yeni bileşik sentez edilmiş ve Alzheimer hastalığına karşı etkileri in vitro olarak test edilmiştir.Gereç ve Yöntem: Sonuç bileşiklerin sentezinde kullanılan amin türevleri (5 ve 6), öncelikle ticari olarak mevcut 1,3-benzoksazol-2(3H)-on ve 1,3-benzotiyazol-2(3H)-on halkalarının metillenmesi, nitrik asit ile nitrolanması ve ardından kalay klorürle indirgenmesi ile sentez edilmiştir. Daha sonra, amin türevi 5 ve 6’nın bromoasetil bromür ile açilasyonundan hazırlanan ara ürünlerin (7 ve 8) uygun amin türevleri ile tepkimesinden sonuç bileşikler (9a-n ve 10a-n) elde edilmiştir. Sentezlenen bileşiklerin kimyasal yapıları spektroskopik yöntemler, HRMS ve elementel analiz ile aydınlatılmıştır. Tüm sonuç bileşiklerin modifiye Ellman yöntemiyle kolinesteraz inhibitör aktiviteleri belirlendikten sonra DPPH ve ORAC yöntemiyle antioksidan aktiviteleri ölçülmüştür. Son olarak sonuç bileşiklerin metal şelatör özellikleri tayin edilmiştir. Sonuç ve Tartışma: Yeni 2-sübstitüe-N-(3-metil-2-okso-2,3-dihidro-1,3-benzoksazol/1,3-benzotiyazol-6-il)asetamit türevi bileşikler sentez edilmiştir. Kolinesteraz inhibitör etkileri ve yapı aktivite ilişkileri belirlenmiştir. Asetilkolinesteraz (AKE) inhibisyonu için bileşik 10g’nin (IC50: 52.90 µM), butirilkolinesteraz BKE inhibisyonu için bileşik 10h’nin (IC50: 51.03 µM ) en yüksek aktiviteye sahip olduğu bulunmuştur. ORAC testi ile yapılan antioksidan aktivite tayininde ise yan zincirinde fenilpiperazin türevleri taşıyan bileşiklerin referans trolokstan daha yüksek antioksidan aktivite gösterdikleri bulunmuştur. Ayrıca sonuç bileşiklerin metal şelatör etkileri incelendiğinde büyük çoğunluğunun metal şelatör özellik taşıdığı belirlenmiştir.
研究目的本研究合成了 28 种新的含苯并恶唑酮/苯并噻唑酮环的乙酰胺衍生化合物,并在体外测试了它们对阿尔茨海默病的作用:用于合成最终化合物的胺衍生物(5 和 6)首先是通过将市售的 1,3-苯并恶唑-2(3H)-酮和 1,3-苯并噻唑-2(3H)-酮环甲基化,然后用硝酸硝化,再用氯化锡还原而合成的。然后,胺衍生物 5 和 6 与溴乙酰溴酰化制备的中间体(7 和 8)与适当的胺衍生物反应,得到化合物(9a-n 和 10a-n)。合成化合物的化学结构通过光谱方法、HRMS 和元素分析得以阐明。在用改良埃尔曼法测定了所有合成化合物的胆碱酯酶抑制活性后,又用 DPPH 法和 ORAC 法测定了它们的抗氧化活性。最后,测定了所得化合物的金属螯合特性。结论与讨论:合成了新的 2-取代-N-(3-甲基-2-氧代-2,3-二氢-1,3-苯并恶唑/1,3-苯并噻唑-6-基)乙酰胺衍生物。对其胆碱酯酶抑制作用和结构活性关系进行了测定。结果发现,化合物 10g(IC50:52.90 µM)对乙酰胆碱酯酶(ACE)的抑制活性最高,化合物 10h(IC50:51.03 µM)对丁酰胆碱酯酶(BKE)的抑制活性最高。通过 ORAC 试验测定抗氧化活性时发现,侧链中含有苯基哌嗪衍生物的化合物的抗氧化活性高于参考特罗环。此外,在对所得化合物的金属螯合作用进行检测时,确定它们中的大多数都具有金属螯合作用。
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引用次数: 0
TOWARDS UNDERSTANDING NATURAL ALPHA-GLUCOSIDASE INHIBITORS: A COMPUTATIONAL STUDY 了解天然α-葡萄糖苷酶抑制剂:计算研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-01-05 DOI: 10.33483/jfpau.1356028
Muhammed Tilahun Muhammed, Nesli Aksoy, Aybüke Krilmaz, Enise Türkmen
Objective: Diabetes mellitus is a metabolic disorder affecting hundreds of millions of people around the world. It is characterized by hyperglycemia caused by impaired glucose homeostasis that results from insufficient insulin production or insulin resistance. There are clinically available α-glucosidase inhibitor drugs that are used to decrease postprandial blood glucose level. However, these drugs have side effects that necessitated the discovery of new α-glucosidase inhibitors with less side effects and high potency. The interest in the use of natural products to deal with diabetes has been increasing. Therefore, the potential of natural α-glucosidase inhibitors to inhibit the enzyme was investigated through computational methods. Material and Method: The binding potential of selected natural α-glucosidase inhibitors was investigated through molecular docking. Thereafter, the stability of the complexes with the highest binding potential were assessed through molecular dynamics (MD) simulation. Result and Discussion: The molecular docking demonstrated that compound 2 had better binding potential than the standard drug, acarbose. Compound 7 had comparable binding potential to the standard drug. Furthermore, all the tested compounds exhibited a reasonable binding potential towards the enzyme but were weaker than the standard drug. The MD simulation demonstrated that compounds 2 and 7 gave complexes with similar stability to the standard drug. The overall computational results revealed that the natural inhibitors investigated had the ability to bind to the enzyme and formed stable complexes. Therefore, these compounds could be potential α-glucosidase inhibitors for clinical use. For this reason, further in vitro investigations on compounds with the highest binding potential is recommended.
目的:糖尿病是一种代谢性疾病,影响着全球数亿人。其特点是由于胰岛素分泌不足或胰岛素抵抗导致葡萄糖稳态受损,从而引起高血糖。临床上有一些α-葡萄糖苷酶抑制剂药物可用于降低餐后血糖水平。然而,这些药物都有副作用,因此需要发现副作用小、效力高的α-葡萄糖苷酶抑制剂。人们对使用天然产品治疗糖尿病的兴趣与日俱增。因此,我们通过计算方法研究了天然α-葡萄糖苷酶抑制剂抑制该酶的潜力。材料与方法:通过分子对接研究了所选天然α-葡萄糖苷酶抑制剂的结合潜力。随后,通过分子动力学(MD)模拟评估了具有最高结合潜力的复合物的稳定性。结果与讨论:分子对接表明,化合物 2 比标准药物阿卡波糖具有更好的结合潜力。化合物 7 的结合潜力与标准药物相当。此外,所有测试化合物都表现出与酶的合理结合潜力,但弱于标准药物。MD 模拟结果表明,化合物 2 和 7 生成的复合物与标准药物具有相似的稳定性。总体计算结果显示,所研究的天然抑制剂能够与酶结合并形成稳定的复合物。因此,这些化合物有可能成为临床上使用的α-葡萄糖苷酶抑制剂。因此,建议对具有最高结合潜力的化合物进行进一步的体外研究。
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引用次数: 0
PİYASADAN TEMİN EDİLEN NİOLİ UÇUCU YAĞI ÖRNEKLERİNİN FARMAKOPE ANALİZİ 对从市场上获得的精油样本进行药典分析
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-31 DOI: 10.33483/jfpau.1406371
Burçin Ergene, Gizem Öztürk
Amaç: Halk arasında doğal kaynakların güvenli olarak kabul edilmesi ve sentetik içerikli ürünlerden uzaklaşma isteği, uçucu yağ kullanımını son zamanlarda arttırmıştır. Fakat uçucu yağlar, içerisinde çok sayıda bileşik barındırdığından standardizasyon konusunda sıkıntılar yaşanmaktadır. Bu sebeple uçucu yağların kalitesini ve terapötik amaçla kullanılabilirliğini değerlendirmek için monograflardan yararlanılmaktadır. Yapılan çeşitli çalışmalar sonucunda nioli uçucu yağının; üst solunum yolu ve üriner sistem enfeksiyonlarına, cilt rahatsızlıklarına karşı kullanılabileceği ve antioksidan, antienflamatuvar, antiseptik, antifungal, antibakteriyel, antihelmintik, insektisidal, larvisidal ve akarisidal etkinliği tespit edilmiştir. Halk arasında ise soğuk algınlığı, influenza, öksürük, sinüzit, farenjit, rinit, romatizmal rahatsızlıklarda ve üriner sistem enfeksiyonlarında kullanılmaktadır. Bu etkinlikleri ve halk arasındaki kullanımından yola çıkılarak, piyasada bulunan bazı nioli uçucu yağ örneklerinin Türk Farmakopesi 2017’ye uygunluğunun değerlendirilmesi hedeflenmiştir. Gereç ve Yöntem: Çalışma kapsamında; 5 farklı markadan temin edilen nioli uçucu yağı örneklerinin Türk Farmakopesi’nde (2017) yer alan monografa göre analiz edilmiştir. Analizde, bağıl yoğunluk, kırılım imleci, optik çevirme değerleri tespit edilmiş; organoleptik kontrol, ince tabaka kromatografisi ve gaz kromatografisi analizleri yürütülmüştür. Sonuç ve Tartışma: Çalışma kapsamında yapılan farmakope analizi sonucunda, temin edilen beş nioli uçucu yağ numunesinden sadece bir tanesi farmakope standardına uygun olduğu bulunmuştur. Diğer nioli uçucu yağ numuneleri, farmakopede istenilen şartları karşılamamıştır.
目的:公众认为天然资源是安全的,并希望摒弃合成产品,这使得精油的使用最近有所增加。然而,由于精油中含有多种化合物,因此在标准化方面存在问题。因此,人们使用各论来评估精油的质量及其治疗用途。多项研究结果表明,红景天精油可用于治疗上呼吸道和泌尿系统感染、皮肤疾病,并具有抗氧化、消炎、杀菌、抗真菌、抗菌、驱虫、杀幼虫剂和杀螨剂的活性。它常用于治疗感冒、流感、咳嗽、鼻窦炎、咽炎、鼻炎、风湿病和泌尿系统感染。基于这些活性及其在公众中的使用情况,本研究旨在评估市场上的一些尼奥里精油样本是否符合《2017 年土耳其药典》。 材料和方法:在研究范围内,根据《土耳其药典》(2017 年)中的专著分析了从 5 个不同品牌获得的牛至精油样本。在分析过程中,测定了相对密度、折光光标、光学转换值;进行了感官控制、薄层色谱法和气相色谱法分析。结论与讨论:在研究范围内进行的药典分析结果显示,获得的五个牛至精油样本中只有一个符合药典标准。其他牛至精油样本不符合药典要求。
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引用次数: 0
THE EFFECT OF ESCHERICHIA COLI BACTERIOPHAGE COCKTAIL ON BACTERIAL CONTAMINATION IN WATER 大肠杆菌噬菌体鸡尾酒对水中细菌污染的影响
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-29 DOI: 10.33483/jfpau.1390191
H. B. Erol, Aylin Keski̇n
Objective: Wastewater and environmental water resources are treated to eliminate pathogenic microorganisms but contamination is still a significant problem. In particular, the presence of contamination with Escherichia coli (E. coli) is an important indicator of fecal contamination. Due to increasing antimicrobial resistance and failures of new antimicrobial processes, interest in bacteriophages in pathogen control has increased. Therefore, in our study, phage-based bacteria control in environmental waters was investigated as a natural solution. Material and Method: In our study, E. coli and lytic bacteriophages specific to these E. coli were isolated from environmental water samples in Ankara. The lytic activities of the isolated phages were determined on environmental and clinical extended-spectrum β-lactamases E. coli isolates. Three phages with high lytic activity were selected, and the effectiveness of the single phage and their mixtures on E. coli contamination in water was tested. Result and Discussion: As a result of the study, 17 E. coli strains were isolated from 30 environmental water samples. Lytic bacteriophages in 30 different plaque structures were also isolated from water samples. The isolated phages were found to have lytic activity in the range of 32-70% on the tested bacteria. The effectiveness of three selected phages and their cocktail on E. coli contamination in water was measured at 6th and 24th. As a result, it was observed that the cocktail application reduced the number of host bacteria in the water below detectable limits, also provided a 5-log reduction in non-host test bacteria and maintained its effect for 24 hours. When the results are evaluated, it is thought that cocktail phage application will be an effective method against E. coli contamination in water.
目的:废水和环境水资源经过处理后可消除病原微生物,但污染仍是一个重大问题。特别是,大肠杆菌(E. coli)污染是粪便污染的一个重要指标。由于抗菌药耐药性的增加和新型抗菌工艺的失败,人们对噬菌体在病原体控制方面的作用越来越感兴趣。因此,在我们的研究中,研究了基于噬菌体的环境水体细菌控制作为一种自然解决方案。材料与方法在我们的研究中,从安卡拉的环境水样中分离出了大肠杆菌和针对这些大肠杆菌的特异性噬菌体。测定了分离出的噬菌体对环境和临床广谱β-内酰胺酶大肠杆菌分离物的溶菌活性。选出了三种具有高溶菌活性的噬菌体,并测试了单一噬菌体及其混合物对水中大肠杆菌污染的有效性。结果与讨论:研究结果显示,从 30 个环境水样中分离出 17 株大肠杆菌。还从水样中分离出 30 种不同斑块结构的致死噬菌体。研究发现,分离出的噬菌体对被测细菌的溶菌活性在 32-70% 之间。第 6 次和第 24 次测量了三种选定噬菌体及其鸡尾酒对水中大肠杆菌污染的有效性。结果表明,鸡尾酒应用可将水中宿主细菌的数量减少到可检测到的限度以下,还可将非宿主测试细菌的数量减少 5 个菌落,其效果可维持 24 小时。在对这些结果进行评估后,我们认为鸡尾酒噬菌体的应用将成为一种有效的方法,可有效防止水中的大肠杆菌污染。
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引用次数: 0
BAZI TIBBİ BİTKİLERDE ATOMOKSETİN TAYİNİ İÇİN YENİ BİR UHPLC-DAD YÖNTEMİNİN GELİŞTİRİLMESİ VE VALİDASYONU 建立和验证测定某些药用植物中阿托西汀含量的 uhplc-dad 新方法
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-28 DOI: 10.33483/jfpau.1345130
Burhan Ceylan
Objective: Atomoxetine (ATX) is a medication that is extensively used to treat attention deficit hyperactivity disorder in children, adolescents, and adults. The goal of this work was to create a speedy, easy, and sensitive ultra high performance liquid chromatographic method (UHPLC) for the measurement of atomoxetine in various medicinal plants. (Salvia officinalis L., Rosmarinus officinalis L., Melissa officinalis L., Ginkgo biloba L.). Material and Method: Prior to chromatographic separation, liquid-liquid extraction was applied, which is currently the preferred extraction technique due to its simple, fast and efficient procedure for sample preparation. The chromatographic separation was achieved by reversed phase C18 (5 μm × 4.6 mm × 150 mm) analytical column and a mobile phase consisting of monobasic potassium dihydrogen orthophosphate (pH=6.8) and acetonitrile (50:50 v/v) at flow rate of 0.8 ml/min and diode array detector (DAD) detecting at 215±2 nm. Result and Discussion: The envisioned method's linear behavior was tested in the 0.5-20 μg/ml range (r2=0.09990). In compliance with International Conference on Harmonisation (ICH) criteria, the method received validation by means of accuracy, precision, repeatability, specificity, robustness, and detection and quantification boundaries. LOD and LOQ values were determined as 0.16 and 0.5 μg/ml. RSD values for hourly and daily measurements are found to be below 2.5% for both assays. The proposed method can be used effectively for quantification of atomoxetine in medicinal and aromatic plants. The proposed analytical procedure represents an efficient method for the quantification and routinee analysis of atomoxetine in medicinal and aromatic plants.
目的:阿托莫西汀(ATX)是一种广泛用于治疗儿童、青少年和成人注意缺陷多动障碍的药物。这项工作的目的是建立一种快速、简便、灵敏的超高效液相色谱法(UHPLC),用于测定多种药用植物(丹参、麝香草、麝香草苷、麝香石竹)中的阿托莫西汀。(丹参、迷迭香、香薷、银杏)中的阿托西汀。材料与方法在进行色谱分离之前,先采用液液萃取技术,该技术因其简单、快速、高效的样品制备程序而成为目前首选的萃取技术。色谱分离采用反相 C18(5 μm × 4.6 mm × 150 mm)分析柱,流动相为单碱式磷酸二氢钾(pH=6.8)和乙腈(50:50 v/v),流速为 0.8 ml/min,二极管阵列检测器(DAD)的检测波长为 215±2 nm。 结果与讨论该方法在 0.5-20 μg/ml 范围内线性良好(r2=0.09990)。按照国际协调会议(ICH)的标准,该方法通过了准确度、精密度、重复性、特异性、稳健性以及检测和定量界限的验证。LOD 和 LOQ 值分别为 0.16 和 0.5 μg/ml。两种检测方法每小时和每天测量的 RSD 值均低于 2.5%。该方法可有效地用于药用植物和芳香植物中阿托西汀的定量分析。该分析程序是一种高效的药用植物和芳香植物中阿托西汀的定量和常规分析方法。
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引用次数: 0
KOENZİM Q10 YÜKLÜ MİSEL İÇEREN KONTAKT LENSLERİN HAZIRLANMASI VE İN-VİTRO KARAKTERİZASYONU 含有辅酶 Q10 胶束的隐形眼镜的制备和体外表征
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-25 DOI: 10.33483/jfpau.1400373
Ahmet Doğan Ergi̇n
Objective: Coenzyme Q10 (CoQ10) offers potential therapeutic benefits for ocular health, yet faces challenges of poor solubility and bioavailability when applied to the eye. This study aimed to enhance CoQ10 delivery using contact lenses by incorporating CoQ10-loaded polymeric micelles, using Pluronic F127 and solvent evaporation technique. Material and Method: Polymeric micelles encapsulating CoQ10 were produced via solvent evaporation with Pluronic F127. Commercial contact lenses were subsequently loaded with these micelles. Characterization of the loaded lenses included assessments of light transmittance, swelling behavior, and drug release profile under non-sink conditions, simulating the constraints of the ocular surface. Result and Discussion: The unloaded lenses exhibited a light transmittance of 91.78±3.29% and swelling percentage of 47.51±4.45% while micelle-loaded lenses demonstrated high light transmittance levels (95.31±0.80%), ensuring optical clarity. Swelling studies showed a slight increase in size to 48.1±4.4%. The lenses effectively encapsulated 403.6±21.8 µg of CoQ10. In vitro release profile exhibited controlled release over six hours, indicating potential for sustained drug delivery. These results highlight the feasibility of micelle-loaded contact lenses for efficient ocular drug delivery, warranting further exploration into their long-term effectiveness and safety.
目的:辅酶 Q10(CoQ10)对眼部健康具有潜在的治疗作用,但在眼部使用时面临着溶解度和生物利用度较低的挑战。本研究旨在通过使用 Pluronic F127 和溶剂蒸发技术,在隐形眼镜中加入含有 CoQ10 的聚合物胶束,从而加强 CoQ10 的输送。材料和方法:使用 Pluronic F127 通过溶剂蒸发技术生产出包裹 CoQ10 的聚合物胶束。随后在商用隐形眼镜中添加了这些胶束。对载入的镜片进行表征,包括透光率、膨胀行为和非沉降条件下的药物释放曲线评估,模拟眼球表面的限制条件。 结果与讨论:未负载镜片的透光率为 91.78±3.29%,膨胀率为 47.51±4.45%,而胶束负载镜片的透光率较高(95.31±0.80%),确保了光学清晰度。膨胀研究表明,镜片尺寸略有增加,达到 48.1±4.4%。镜片有效封装了 403.6±21.8 µg CoQ10。体外释放曲线显示,CoQ10 可在 6 小时内得到控制释放,这表明它具有持续给药的潜力。这些结果凸显了胶束载药隐形眼镜用于高效眼部给药的可行性,值得进一步探索其长期有效性和安全性。
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引用次数: 0
KOJİK ASİT İLE LAVANDULA ANGUSTIFOLIA L. UÇUCU YAĞININ ANTİMİKROBİYAL KOMBİNASYONU 曲酸和薰衣草精油的抗菌组合
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-12-25 DOI: 10.33483/jfpau.1399176
Damla Kirci, Özge ÖZŞEN BATUR, B. Demi̇rci̇
Objective: Lavandula angustifolia L. (Lavender) is one of the most plants essential oils used in the cosmetic, food and biological activities. Kojic acid has been used in cosmetics for its whitening effect and pharmaceutical activity. The aim of this study to determine the composition of the Pharmacopoeia quality L. angustifolia essential oil (EO). Moreover, antimicrobial activities against skin pathogens and synergistic antibacterial activity were also examined of EO and kojic acid. Material and Method: In this work, chemical composition of the EO was defined. Linalyl acetate (43.3%) and linalool (38.6%) were determined as the major components by GC-MS and GC-FID, simultaneously. The antimicrobial activity was evaluated against Candida albicans, C. glabrata, Staphylococcus aureus and Salmonella typhimurium. Result and Discussion: EO and kojic acid showed weak antimicrobial effects. MIC values were determined as the EO 10 mg/ml and kojic acid 1.25 mg/ml against S. typhimurium. To assess the synergistic activity was evaluated by the checkerboard microdilution assay, EO was combined with kojic acid against S. typhimurium. Among the tested skin pathogen microorganisms, S. typhimurium was more sensitive to kojic acid. Therefore, synergic activity was investigated against S. typhimurium and found indifferent effect.
目的:薰衣草(Lavandula angustifolia L.)是用于化妆品、食品和生物活动最多的植物精油之一。曲酸具有美白效果和药物活性,已被用于化妆品中。本研究的目的是确定药典级薰衣草精油(EO)的成分。此外,还研究了 EO 和曲酸对皮肤病原体的抗菌活性和协同抗菌活性。材料和方法:在这项工作中,确定了环氧乙烷的化学成分。通过 GC-MS 和 GC-FID 同时测定了乙酸芳樟酯(43.3%)和芳樟醇(38.6%)的主要成分。对白色念珠菌、光滑念珠菌、金黄色葡萄球菌和鼠伤寒沙门氏菌的抗菌活性进行了评估。结果与讨论:环氧乙烷和曲酸显示出微弱的抗菌效果。对伤寒沙门氏菌的 MIC 值分别为环氧乙烷 10 毫克/毫升和曲酸 1.25 毫克/毫升。为了评估协同活性,采用了棋盘式微量稀释试验,将环氧乙烷与曲酸结合起来,共同对抗伤寒杆菌。在测试的皮肤病原微生物中,鼠伤寒杆菌对曲酸更为敏感。因此,对伤寒杆菌的协同活性进行了研究,发现效果并不明显。
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引用次数: 0
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Ankara Universitesi Eczacilik Fakultesi Dergisi
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