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ANTIMICROBIAL ACTIVITY OF PIMPINELLA - AN OVERVIEW 茴芹的抗菌活性--综述
Pub Date : 2024-07-09 DOI: 10.54994/emujpharmsci.1508972
Mehmet İlktaç, Zeynep Pelin Kutlu, Yankı Çelebi, Gülden Çelik
Pimpinella species, belonging to Apiaceae (Lindl.) family, utilized in many fields of industry as spice, fruit, vegetable and beverage have especially been used in traditional medicine as a remedy in various countries. Essential oils (EO) of various species including Pimpinella cypria, Pimpinella kotshchyana, Pimpinella saxifraga, and Pimpinella anisum were reported to have antibacterial and antifungal activities. Furthermore, it was observed that P. anisum EO possessed antiviral properties. Along with its antimicrobial activity, Pimpinella species were found to have antioxidant, anti-inflammatory, anticonvulsant, antispasmodic, estrogenic, cytotoxic, insecticidal, and repellent properties. This review aims to provide an enhanced understanding on some Pimpinella species’ morphology, chemical constituent, industrial and medicinal usage, and antimicrobial activities against bacteria, fungi, and viruses.
茴芹(Pimpinella)属于伞形科(Apiaceae (Lindl.))茴芹属植物,在许多工业领域被用作香料、水果、蔬菜和饮料,特别是在许多国家被用作传统医药的补救措施。据报道,包括 Pimpinella cypria、Pimpinella kotshchyana、Pimpinella saxifraga 和 Pimpinella anisum 在内的多个物种的精油(EO)具有抗菌和抗真菌活性。此外,还观察到茴芹环氧乙烷具有抗病毒特性。除抗菌活性外,研究还发现茴芹还具有抗氧化、抗炎、抗惊厥、解痉、雌激素、细胞毒性、杀虫和驱虫特性。本综述旨在加深人们对一些皮蓬属植物的形态、化学成分、工业和药用用途以及对细菌、真菌和病毒的抗菌活性的了解。
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引用次数: 0
DEVELOPMENT OF ZINC-LOADED HYDROGEL INFUSED WITH ALOE BARBADENSIS MUCILAGE FOR WOUND HEALING 开发注入芦荟粘液的锌负载水凝胶,用于伤口愈合
Pub Date : 2024-07-09 DOI: 10.54994/emujpharmsci.1489024
Ibilola Cardoso-daodu, Emmanuel Agbarakwe, M. Ilomuanya, ChukwuemekaPaul Azubuike, Boladale Silva
This study aims to formulate and characterize zinc-loaded hydrogel infused with Aloe barbadensis mucilage for wound dressing. Five formulations containing varying proportions of carbopol, zinc, aloe and water (as vehicle) were developed via physical crosslinking using triethanolamine. All formulations had a translucent off-white colour while the control gave a transparent gel. The viscosity was highest in the control, 30000.00 ± 2.07 PaS. The pH of the formulations was between 5.7 and 5.8. Formulation 2 which is composed of 30 mg of Zinc and 1.4 mg of Aloe barbadensis incorporated into 1% w/v Carbopol Ultrez hydrogel polymer had the lowest swelling index of 79.2 ± 1.95% implying that it had the fastest drug release rate. The wounds treated with Formulation 2 had the most rapid wound healing with no sign of scars in the wound area. Histomorphometric evaluation reflected a high re-epithelisation rate of 70%, a significant percentage occupied by collagen in granulation tissue of 85%. The thickness of the tissue's central region was 10 mm. The inflammatory cells /mm2 tissue was 200 cells/mm2 while the number of microvessels in granulation tissue was 1.0 microvessels/mm2. Zinc-loaded hydrogel infused with Aloe barbadensis mucilage shows great potential as a modern wound dressing.
本研究旨在配制和表征注入芦荟粘液的锌负载水凝胶,用于伤口敷料。通过使用三乙醇胺进行物理交联,研制出了五种配方,分别含有不同比例的 carbopol、锌、芦荟和水(作为载体)。所有配方都呈半透明的米白色,而对照组则呈透明凝胶状。对照组的粘度最高,为 30000.00 ± 2.07 PaS。配方的 pH 值介于 5.7 和 5.8 之间。配方 2 由 30 毫克锌和 1.4 毫克芦荟与 1%(重量/体积)Carbopol Ultrez 水凝胶聚合物组成,其溶胀指数最低,为 79.2 ± 1.95%,这意味着其药物释放速度最快。使用配方 2 处理的伤口愈合最快,伤口区域没有疤痕。组织形态学评估显示,伤口的再上皮率高达 70%,肉芽组织中胶原蛋白的比例高达 85%。组织中心区域的厚度为 10 毫米。每平方毫米组织的炎症细胞数为 200 个,而肉芽组织中的微血管数为 1.0 个/平方毫米。注入芦荟粘液的含锌水凝胶显示出作为现代伤口敷料的巨大潜力。
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引用次数: 0
Screening cholinesterase inhibitory potential of selected amines 筛选某些胺类的胆碱酯酶抑制潜力
Pub Date : 2024-07-09 DOI: 10.54994/emujpharmsci.1503153
Açelya Mavideniz, Tuğba Erçetin, Aybike Yektaoglu, Zahra Nobavar, Jale Yuzugulen, Emine Dilek Özyılmaz, H. O. Gülcan
Cholinesterase inhibition has gained attention in the treatment of some disease states, covering cholinergic deficiency. Alzheimer’s disease (AD) can be counted as the most important one among them. Indeed, the current drugs used in the treatment of AD are cholinesterase inhibitor molecules, besides memantine, and biological new drugs. Many pharmacophores have been suggested so far for cholinesterase inhibition and many of them possess a basic center with an amine function. Within this work, we have selected some simple amines and investigated their potential to inhibit acetylcholinesterase and butyrylcholinesterase enzymes. The results indicated that simple amines by themselves don’t have strong potential unless they are used with other pharmacophores.
胆碱酯酶抑制剂在治疗某些胆碱能缺乏的疾病方面受到了关注。阿尔茨海默病(AD)可以说是其中最重要的一种。事实上,目前用于治疗阿尔茨海默病的药物除了美金刚外,还有胆碱酯酶抑制剂分子和生物新药。迄今为止,已有许多抑制胆碱酯酶的药理作用被提出,其中许多药理作用都具有带胺功能的碱性中心。在这项工作中,我们选择了一些简单的胺,并研究了它们抑制乙酰胆碱酯酶和丁酰胆碱酯酶的潜力。结果表明,除非与其他药剂一起使用,否则单胺本身并不具有很强的潜力。
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引用次数: 0
Antibacterial potency of Ibuprofen and its interaction with ciprofloxacin against Gram positive and Gram negative bacteria 布洛芬及其与环丙沙星的相互作用对革兰氏阳性菌和革兰氏阴性菌的抗菌效力
Pub Date : 2024-07-09 DOI: 10.54994/emujpharmsci.1506675
Ertuğrul Özbil, Sultan Öğmen Seven, Açelya Mavideniz, Mehmet İlktaç
Ibuprofen, a nonsteroidal anti-inflammatory drug (NSAID), works by reducing hormones for the treatment of fever, inflammation, and pain. Previously, it was only shown that the Ibuprofen inhibits the effect of various bacteria that are stimulated by bacterial infections and not directly on bacterial cells. In this study, we aimed to investigate antibacterial and synergistic activities of Ibuprofen against Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922 and Klebsiella pneumoniae ATCC 700603. The results revealed promising antibacterial activity against tested Gram-positive bacteria, but there was no effect on Gram-negative bacteria. Furthermore, checkerboard assays did not reveal any additive or synergistic activity when combined with ciprofloxacin against tested Gram-positive bacteria. Collectively, our data reveal the selective antibacterial activity of ibuprofen against Gram-positive bacteria which suggests that ibuprofen can be further investigated as a potential source for new therapeutic options.
布洛芬是一种非甾体抗炎药(NSAID),通过减少激素来治疗发烧、炎症和疼痛。以前,只有研究表明布洛芬能抑制细菌感染刺激的各种细菌,而不是直接抑制细菌细胞。在本研究中,我们旨在研究布洛芬对粪肠球菌 ATCC 29212、金黄色葡萄球菌 ATCC 25923、大肠埃希菌 ATCC 25922 和肺炎克雷伯菌 ATCC 700603 的抗菌和协同活性。结果表明,该物质对测试的革兰氏阳性菌具有良好的抗菌活性,但对革兰氏阴性菌没有作用。此外,在与环丙沙星联合使用时,棋盘格试验也没有发现其对测试的革兰氏阳性菌具有任何添加或协同活性。总之,我们的数据揭示了布洛芬对革兰氏阳性菌的选择性抗菌活性,这表明布洛芬可作为新治疗方案的潜在来源得到进一步研究。
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引用次数: 0
In vitro antibacterial acitivity of Naproxen and its combination with ciprofloxacin 萘普生及其与环丙沙星复方制剂的体外抗菌活性
Pub Date : 2024-07-09 DOI: 10.54994/emujpharmsci.1506693
Sultan Öğmen Seven, Ertuğrul Özbil, Açelya Mavideniz, Mehmet İlktaç
Naproxen, a nonsteroidal anti-inflammatory drug (NSAID), is commonly used to reduce fever, and to treat pain and inflammation caused by several conditions. Previously, naproxen was evaluated for its antimicrobial potency in various studies. In our study, we aimed to demonstrate the antibacterial and synergistic activities of naproxen and ciprofloxacin against various Gram-positive and Gram-negative bacteria including, Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922 and Klebsiella pneumoniae ATCC 700603. The results showed promising antibacterial activity against tested Gram-positive bacteria. However, there was no effect on Gram-negative bacteria. Additionally, checkerboard assays did not reveal any additive or synergistic activity when combined with Ciprofloxacin. Collectively, our study's data show naproxen's selectivity against Gram-positive bacteria. This result suggests that naproxen can be further used as a potential source of antibiotics against Gram-positive bacteria.
萘普生是一种非甾体抗炎药(NSAID),常用于退烧、治疗多种疾病引起的疼痛和炎症。此前,已有多项研究对萘普生的抗菌效力进行了评估。在我们的研究中,我们旨在证明萘普生和环丙沙星对各种革兰氏阳性和革兰氏阴性细菌的抗菌和协同活性,包括粪肠球菌 ATCC 29212、金黄色葡萄球菌 ATCC 25923、大肠埃希菌 ATCC 25922 和肺炎克雷伯菌 ATCC 700603。结果表明,它对测试的革兰氏阳性菌具有良好的抗菌活性。但是,对革兰氏阴性菌没有效果。此外,在与环丙沙星联用时,棋盘格试验并未显示出任何相加或协同活性。总之,我们的研究数据显示了萘普生对革兰氏阳性菌的选择性。这一结果表明,萘普生可进一步用作抗革兰氏阳性菌的潜在抗生素来源。
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引用次数: 0
Evaluation of Microbiological Cleanliness of Machines/Equipment through Rinse Technique Using Statistical Process Control 用统计过程控制技术评价机器/设备的微生物洁净度
Pub Date : 2023-06-21 DOI: 10.54994/emujpharmsci.1196909
M. Eissa
To guarantee that patients receive safe therapy with predictable and acceptable medicinal properties, monitoring the quality standards in the healthcare sector and the pharmaceutical business, in particular, is essential. Medicinal products are no exception from these crucial characteristics and hence mitigation of the sources of microbial contamination is a mandatory strategy to avoid harming already-ill populations. Machines, equipment and tools that are used in the industry must be appropriately cleaned to ensure that they will not contaminate the product under processing. The study herein aimed to establish an evaluation system for cleaning efficiency through the rinse technique using Statistical Process Control (SPC) methodologies. A database was established and created for the recorded cleaning process over 20 months of the monitoring period. The control charts were constructed and evaluated from processed data using SPC software. A rare event control chart was used to track the cleaning process intervals with event probability estimated to be 0.080. Concerning the monitoring of the bioburden of rinse samples, the most appropriate fitting attribute chart is U type with Laney modification of over-dispersion to correct for tight control limits that increase alarming false points. Understanding the inspection property is inevitable for the right interpretation of trends.
为了确保患者接受具有可预测和可接受的药性的安全治疗,监测医疗保健部门和制药业务的质量标准尤其重要。医药产品也不例外,具有这些关键特征,因此减少微生物污染源是一项强制性战略,以避免伤害已经患病的人群。工业中使用的机器、设备和工具必须进行适当的清洁,以确保它们不会污染正在加工的产品。本研究旨在利用统计过程控制(SPC)方法,建立一套通过冲洗技术进行清洗效率评估的系统。为监测期间20个月的清洁过程记录建立和建立了一个数据库。利用SPC软件对处理后的数据进行控制图的构建和评价。采用罕见事件控制图对清洗过程间隔进行跟踪,估计事件概率为0.080。对于漂洗样品的生物负荷监测,最合适的拟合属性图为U型,并对过度分散进行Laney修正,以纠正控制范围过紧导致报警虚点增加的情况。了解检验性质对于正确解释趋势是不可避免的。
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引用次数: 0
Formulation development and evaluation of controlled release matrix tablets of glibenclamide 格列本脲控释基质片的处方研制与评价
Pub Date : 2023-05-26 DOI: 10.54994/emujpharmsci.1215120
Biji Palatty, Praveena Raj, Daiay Pa, Boby JOHNS .G
Matrix tablets were prepared by three different polymers as sustained-release agents, using Glibenclamide as a model drug. The aim of the present study was to formulate and evaluate the controlled release matrix tablets of Glibenclamide which is an antidiabetic drug which belongs to the second generation oral hypoglycemics. Three polymers were selected for this study- HPMC K 15, HPMC K 100 and EC in different drug: polymer ratio. The drug was identified by FTIR spectroscopic method. The pre compression and post compression parameters of all formulations were found to be within acceptable limit. The release rate of Glibenclamide from matrix tablets was studied using USP Dissolution Testing Apparatus type-I (Basket method). The formulation F6 which contained EC 50mg showed a maximum release of 99.28% in 24 hrs and revealed that EC was more effective in sustaining the drug release and therefore the formulation F6 selected as the optimized formulation. The in-vitro release data of optimized formulation was fit into various kinetic models, among the different models data of in-vitro release of best fit into Zero order kinetic model. The formulation best fit to Higuchi model showed that drug release from the prepared matrix tablets occurs via diffusion process.
以三种不同的聚合物为缓释剂,以格列本脲为模型药物制备基质片。格列本脲是第二代口服降糖药,其控释基质片的研制与评价是本研究的目的。本研究选择了三种不同药高比的聚合物HPMC k15、HPMC k100和EC。用FTIR光谱法对该药物进行了鉴定。所有配方的预压缩和后压缩参数均在可接受范围内。采用美国药典i型溶出度测定仪(筐法)研究了格列本脲在基质片中的释放度。含EC 50mg的配方F6在24 h内的最大释放量为99.28%,表明EC具有较好的缓释效果,因此选择F6为最佳配方。优化制剂的体外释放数据可拟合到多个动力学模型中,不同模型中体外释放数据最适合于零级动力学模型。最符合Higuchi模型的处方表明,所制备的基质片通过扩散过程释放药物。
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引用次数: 0
Antimicrobial Activity Studies of 3-Substituted Indole-2-one and -thione derivatives and Molecular Docking and ADME Evaluations 3-取代吲哚-2- 1和-硫酮衍生物的抗菌活性研究、分子对接和ADME评价
Pub Date : 2023-05-26 DOI: 10.54994/emujpharmsci.1202754
Derya Doğanay, Şevval Maral ÖZCAN AYKOL, A. Şentürk, S. Ölgen
Objectives:Increasing antibiotic resistance is an important problem for public health therefore new antimicrobial compounds are needed. In this study, the antimicrobial effect of 3-Substituted Indole-2-one and -thione derivatives was investigated. Methods: Antimicrobial effects of previously synthesized 18 different 3-substituted indole-2-one and 2-thione derivatives against 5 different microorganisms were investigated and the structure-activity relationships and drug-like properties of compounds were analyzed by molecular docking and in silico prediction studies.The in vitro antimicrobial activities of compounds were tested by microdilution method. Results:The most active compounds 2, 3, 4, 5, 6, 7 and 8 showed antimicrobial activity at 125 μg/mL of MIC value comparable to reference compound ampicillin. Compounds 2 and 3 were found to be active against S. enterica and compounds 4, 5, 6, 7, and 8 were found to be active against methicillin-resistant S. aureus (MRSA). According to molecular docking studies, all compounds presented weaker binding properties than ciprofloxacin, ampicillin and gentamicin. The predicted values for molecular weight, log P, PSA, crossing the BBB, GI absorption properties and type of CYPP450 inhibition data of compounds were found promising for drug-like properties. Conclusions: 3-Substituted Indole-2-one and -thione derivatives can proivide an important contribution to develop alternative antimicrobial agents.
目的:抗生素耐药性的增加是公共卫生的一个重要问题,因此需要新的抗菌化合物。本研究考察了3-取代吲哚-2- 1和-硫酮衍生物的抗菌作用。方法:采用分子对接和计算机预测的方法,研究合成的18种不同的3-取代吲哚-2- 1和2-硫酮衍生物对5种不同微生物的抑菌效果,分析化合物的构效关系和类药物性质。采用微量稀释法测定化合物的体外抑菌活性。结果:活性最高的化合物2、3、4、5、6、7和8在MIC值为125 μg/mL时的抑菌活性与参比化合物氨苄西林相当。化合物2和3对肠球菌有活性,化合物4、5、6、7和8对耐甲氧西林金黄色葡萄球菌(MRSA)有活性。根据分子对接研究,所有化合物的结合性能均弱于环丙沙星、氨苄西林和庆大霉素。化合物的分子量、对数P、PSA、过血脑区、GI吸收特性和CYPP450抑制类型的预测值均具有较好的药物样性质。结论:3-取代吲哚-2- 1和-硫酮衍生物可为开发替代抗菌药物提供重要贡献。
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引用次数: 0
Common Treatment Formulation for Non-Scaring (Androgenetic) Alopecia 非瘢痕性(雄激素源性)脱发的常用治疗配方
Pub Date : 2023-01-24 DOI: 10.54994/emujpharmsci.1211611
Jannat AL-JUBOURİ, Leyla BEBA POJARANİ, M. Celi̇k
In spite of being a non-life-threatening condition, hair loss (alopecia) severely impacts the quality of life of individuals who experience it. Recent studies indicate that the number of patients suffering from alopecia globally is on the rise. Androgenic alopecia (AGA) affects both genders at all ages. Genetic factors and family history are found to greatly impact the likelihood of experiencing hair loss. Statistics reveal that during the course of their lives, 80% of men experience alopecia, while 40 to 50% of women are likely to face some form of hair shedding. AGA is characterized by frontal-temporal hair shedding in men and hair thinning of the midline part of the scalp for women. A variety of herbal formulations are available on the market to combat AGA, while only two FDA-approved medications exist at the moment: oral finasteride and topical minoxidil. Topical formulations of finasteride are still under clinical trials. Minoxidil and finasteride formulations provide effective AGA treatment for both genders. Recent concerns regarding potential side effects of these two medications have drawn interest in providing new innovative alternative formulations (nutrients, minerals and vitamins) to provide a safer treatment against AGA. This article provides a brief overview of the current and alternative AGA formulations.
尽管是一种不会危及生命的疾病,但脱发严重影响了有这种经历的人的生活质量。最近的研究表明,全球脱发患者的数量正在上升。雄激素性脱发(AGA)影响所有年龄段的男女。研究发现,遗传因素和家族史对脱发的可能性有很大影响。统计数据显示,在他们的一生中,80%的男性会经历脱发,而40%到50%的女性可能会面临某种形式的脱发。AGA的特点是男性额颞部脱发,女性头皮中线部分头发稀疏。市场上有多种草药配方可用于对抗AGA,而目前fda批准的药物只有两种:口服非那雄胺和外用米诺地尔。非那雄胺的局部配方仍在临床试验中。米诺地尔和非那雄胺制剂为两性提供有效的AGA治疗。最近对这两种药物潜在副作用的关注引起了人们对提供新的创新替代配方(营养素、矿物质和维生素)的兴趣,以提供更安全的治疗AGA。本文提供了当前和替代的AGA配方的简要概述。
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引用次数: 0
Synthesis and cholinesterase inhibitory potential of 2-phenoxy-N-substituted-acetamide derivatives 2-苯氧基n -取代乙酰胺衍生物的合成及其胆碱酯酶抑制潜力
Pub Date : 2022-12-16 DOI: 10.54994/emujpharmsci.1211796
H. O. Gülcan
The research studies worldwide on the identification of novel molecules having the potential to inhibit cholinesterase enzymes generated many compounds with promising results for some of them. With respect to the limited number of drugs corresponding to the central nervous system active cholinesterase inhibitory potential, these research studies continue. Within the scope of this study, four 2-phenoxy-N-substituted-acetamide derivatives were synthesized and their structures were identified employing spectroscopic techniques. The title molecules were further evaluated for their cholinesterase inhibitory potential in modified Ellman’s method. The results displayed that the compounds have moderate activity and the simple scaffold employed might be used in future studies for more promising compounds.
世界范围内对具有抑制胆碱酯酶潜力的新分子的研究产生了许多化合物,其中一些化合物的研究结果很有希望。针对数量有限的药物对应中枢神经系统活性胆碱酯酶的抑制潜能,这些研究仍在继续。在本研究范围内,合成了4个2-苯氧基n -取代乙酰胺衍生物,并利用光谱技术鉴定了它们的结构。用改进的Ellman方法进一步评价标题分子的胆碱酯酶抑制潜力。结果表明,这些化合物具有中等的活性,所采用的简单支架可用于未来研究更有前途的化合物。
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引用次数: 0
期刊
EMU Journal of Pharmaceutical Sciences
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