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Repositioning an Old Anti-Alcoholism Drug: Disulfiram as a Selective,Effective and Economical Anticancer Agent 重新定位一种古老的抗酒精药物:双硫仑作为一种选择性、有效和经济的抗癌药物
Pub Date : 2016-05-31 DOI: 10.4172/2329-6631.1000E147
C. Soave, Maricela Viola-Rhenals, Y. Elghoul, Tao Peng, Q. Dou
Disulfiram (tetra ethyl thiuram disulfide, or DSF), is a disulfide derivative of N, N-diethyl dithiocarbamate (DEDTC). DSF is an FDA approved drug for the treatment of alcoholism, and at low doses continues to be a useful treatment option for those suffering from the disease. DSF is a member of the dithiocarbamate family, and is thus a metal chelator. Many cancer cells have elevated levels of copper, a metal to which DSF can bind. Thus, DSF is of great interest in cancer research as an antitumor agent, as studies suggest the DSF-copper complex may be cytotoxic to cancer cells. This could allow for targeting of some types of cancer cells with elevated copper levels by DSF.
二硫醚(四乙基硫脲二硫化,或DSF)是N, N-二乙基二硫氨基甲酸酯(DEDTC)的二硫衍生物。DSF是FDA批准的一种治疗酒精中毒的药物,低剂量仍然是那些患有这种疾病的人的有效治疗选择。DSF是二硫代氨基甲酸酯家族的成员,因此是一种金属螯合剂。许多癌细胞中铜的含量升高,而这种金属可以与DSF结合。因此,DSF作为一种抗肿瘤药物在癌症研究中引起了极大的兴趣,因为研究表明DSF-铜复合物可能对癌细胞具有细胞毒性。这可以使DSF靶向某些类型的铜水平升高的癌细胞。
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引用次数: 4
Antibacterial activity of raw honey versus simulated honey solution 原料蜂蜜与模拟蜂蜜溶液的抑菌活性比较
Pub Date : 2016-05-11 DOI: 10.4172/2329-6631.C1.014
Reham F. El-Kased
S relationship is a key to the understanding of functioning of bioactive molecules, as well as a prerequisite for predictive analysis and design of novel molecules with desirable bioactive properties. The authors group had analysed various in silico methodologies (Ganguli and Sharma, Computer Society of India Communication, January 2016, pp 26—28) and the use of open source software packages. Use of open source software and databases permit molecular modeling and predictive design of molecules and of the active site in the protein by homolgy. Stability of a protein molecule in vivo determines the effectiveness of its function under physilogical conditions. Pathological conditions can be traced to malfunctioning of the proteins due the alteration in primary structure by mutation or by alteration in the post-translational modifications affecting functioning of the molecule. This review catalogues few of the better studied protein structures and describe their characteristic peculiarities with the hope that one would be able to develop predictive heuristics.
S关系是理解生物活性分子功能的关键,也是预测分析和设计具有理想生物活性的新分子的先决条件。作者小组分析了各种计算机方法(Ganguli和Sharma,印度通信计算机协会,2016年1月,第26-28页)和开源软件包的使用。使用开源软件和数据库,可以通过同源性对分子和蛋白质活性位点进行分子建模和预测设计。蛋白质分子在体内的稳定性决定了其在生理条件下功能的有效性。病理条件可以追溯到由于突变或翻译后修饰改变影响分子功能的初级结构而导致的蛋白质功能失调。这篇综述列出了一些研究较好的蛋白质结构,并描述了它们的特性,希望人们能够开发预测启发式。
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引用次数: 13
Pharmaceutical biotechnology manufacturing the future of medicine 制药生物技术制造医药的未来
Pub Date : 2016-05-11 DOI: 10.4172/2329-6631.C1.013
Abdulaziz Saddique
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引用次数: 0
Green Synthesis of Silver Nanoparticles from Glycyrrhiza glabra Root Extract for the Treatment of Gastric Ulcer 绿色合成光甘草提取物纳米银治疗胃溃疡的研究
Pub Date : 2016-04-09 DOI: 10.4172/2329-6631.1000152
Sreelakshmy, Deepa Mk, P. Mridula
Glycyrrhiza glabra is a traditional herb which grows in various parts of the world, which have been used for the treatment of various diseases like gastric ulcer. Many reports have been published about the biogenesis of silver nanoparticles using Glycyrrhiza glabra, but green synthesized silver nanoparticles from Glycyrrhiza glabra has not yet been investigate the in-vitro anti-ulcer activity against H. pylori. In the present study was aimed to investigate the in-vitro anti-ulcer activity of green-synthesised silver nanoparticles (AgNPs) from Glycyrrhiza glabra root extract. The green synthesized of silver nanoparticles were characterized by UV-Visible Spectroscopy, X-ray diffraction (XRD), TEM, and FT-IR Analysis. UV-VIS Spectral analysis of the green synthesised nanoparticles was observed a sharp peak at 404 nm indicates the formation of silver nanoparticles. We successfully synthesized uniformly dispersed silver nanoparticles with a uniform size and shape in the range of 7 nm to 45 nm with an average size of 19 nm. The crystalline natures of Ag nanoparticles were confirmed from the XRD analysis. FTIR analysis was carried out to identify the possible biomolecules in Glycyrrhiza glabra root responsible for capping leading to efficient stabilization of the silver nanoparticles. The in-vitro antiulcer activities of synthesized silver nanoparticles were studied by Agar disc diffusion method and Micro broth dilution method. In Agar disc diffusion method showed the activity against H. pylori at the concentration of 500 μg/ml, which exhibit the most potent concentration of silver nanoparticles of gastric Cytoprotective anti-ulcer. In micro broth dilution method, The Minimum Inhibitory Concentration (MIC) of silver nanoparticles by visual examination was found to be 250 μg/ml.
甘草是一种生长在世界各地的传统草药,被用于治疗胃溃疡等各种疾病。关于光甘草合成银纳米粒子的生物发生机制已有许多报道,但从光甘草合成的绿色银纳米粒子对幽门螺杆菌的体外抗溃疡活性尚未得到研究。本研究旨在探讨绿色合成银纳米颗粒(AgNPs)的体外抗溃疡活性。采用紫外可见光谱、x射线衍射(XRD)、透射电镜(TEM)和傅里叶变换红外光谱(FT-IR)对合成的绿色纳米银进行了表征。对合成的绿色纳米粒子进行紫外可见光谱分析,在404 nm处出现尖峰,表明银纳米粒子的形成。我们成功地合成了均匀分散的银纳米颗粒,其尺寸和形状在7 ~ 45 nm之间,平均尺寸为19 nm。通过XRD分析证实了银纳米颗粒的结晶性质。利用傅里叶红外光谱(FTIR)分析确定了甘草根中可能的生物分子,这些分子对银纳米粒子的有效稳定起作用。采用琼脂盘扩散法和微肉汤稀释法研究了合成银纳米颗粒的体外抗溃疡活性。琼脂盘扩散法在浓度为500 μg/ml时显示出对幽门螺杆菌的抑制作用,表明银纳米颗粒对胃细胞保护抗溃疡的作用最强。在微肉汤稀释法中,目测银纳米颗粒的最小抑制浓度(MIC)为250 μg/ml。
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引用次数: 43
In-vivo Animal Models and In-vitro Techniques for Screening Antidiabetic Activity 筛选抗糖尿病活性的体内动物模型和体外技术
Pub Date : 2016-04-08 DOI: 10.4172/2329-6631.1000153
M. Karthikeyan, T. Balasubramanian, Pawan Kumar
Diabetes mellitus is a group of metabolic disorder, is characterized by absolute by lack of insulin and resulting in hyperglycemia. About 2.8% of global populations are affected by Diabetes mellitus. The search for new drug with new properties to treat the disease is still in progress. The current review have made an attempt to bring together all reported models and advanced techniques. Experimentally diabetes mellitus is generally induced in laboratory animals by several methods that include: chemical, surgical and genetic manipulations. The various in vitro techniques includes: In-vitro studies on insulin secretion, In-vitro studies on glucose uptake, Studies using isolated pancreatic islet cell lines, Assay of Amylase Inhibition and Inhibition of α-Glucosidase Activity. Experimental induction of diabetes mellitus in animal models and in vitro techniques are essentials for the advancement of our knowledge, clear understanding of pathogenesis and for finding new therapy. The animal models and in vitro techniques are essentials for developing a new drug for the treatment diabetes. More animal models, advanced techniques have to be developed for advances in diabetes research.
糖尿病是一种代谢性疾病,其特点是绝对缺乏胰岛素而导致高血糖。全球约有2.8%的人口患有糖尿病。寻找具有新特性的治疗这种疾病的新药仍在进行中。本综述试图将所有已报道的模型和先进技术结合起来。在实验动物中,糖尿病通常通过几种方法诱导,包括:化学、手术和基因操作。各种体外技术包括:胰岛素分泌的体外研究,葡萄糖摄取的体外研究,分离胰岛细胞系的研究,淀粉酶抑制试验和α-葡萄糖苷酶活性抑制试验。动物模型和体外技术的实验诱导是提高我们对糖尿病的认识,明确其发病机制和寻找新的治疗方法的必要条件。动物模型和体外实验技术是开发治疗糖尿病新药的必要条件。为了糖尿病研究的进展,必须开发更多的动物模型和先进的技术。
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引用次数: 16
Acute Pancreatitis after Therapy with GABARAN GABARAN治疗后急性胰腺炎
Pub Date : 2015-12-24 DOI: 10.4172/2329-6631.1000146
M. Stoicescu
The main objective of this clinical-case-presentation is to attract attention that the therapy with Gabaran in high dosage and per long period of time without a careful control of function of pancreas (common dosage of amilasemia and amilasuria level) can develop unexpected severe acute pancreatitis and may put the patient’s life in danger.
本临床病例报告的主要目的是引起人们的注意,在没有仔细控制胰腺功能的情况下,大剂量和长时间使用加巴兰治疗(常见剂量为贫血和无尿水平)可能会发生意想不到的严重急性胰腺炎,并可能危及患者的生命。
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引用次数: 1
Formulation of Improved Norfloxacin HCl Tablets: Quality Control Assessment and Comparison Study of Acidic and Basic Form of Norfloxacin in Tablet Formulation 改进盐酸诺氟沙星片的处方:诺氟沙星片中酸、碱剂型的质量控制评价及比较研究
Pub Date : 2015-12-17 DOI: 10.4172/2329-6631.1000145
Somia Gul, Sidra Sajid
Current study emphasis on development of an improved formulation of NFX HCl tablets that must be acceptable with reasonable limits of standards required for tablet. Central premise of research conducted was to evaluate and compare two available forms of Norfloxacin raw material, NFX base and another it’s acidic salt NFX HCl in tablet formulation and establish the effect of acidic and basic form of Norfloxacin. NFX base has been widely used in tablet formulation while Norfloxacin HCl is newly available form in market. After tablet preparation from each form, physical and chemical characterization was performed. Tablets formulated with Norfloxacin base complies with all specifications of physicochemical analysis whereas Norfloxacin HCl containing tablets exhibited twisted results in physical testing, increased hardness and disintegration. Thus an improved formulation was developed that could not interfere with physical as well as chemical characteristics. Result reveals that improved formulation with NFX HCl complies with standard of QC assessment.
目前的研究重点是开发一种改进的盐酸NFX片剂配方,该配方必须在片剂所需标准的合理限度内可接受。本研究的中心前提是对诺氟沙星原料NFX碱和另一种酸盐NFX HCl两种剂型在片剂配方中的可用性进行评价比较,确定诺氟沙星酸碱性剂型的效果。盐酸诺氟沙星是市场上新出现的剂型,而氟氧基已广泛用于片剂配方。从每种形式制备片剂后,进行了物理和化学表征。以诺氟沙星碱配制的片剂符合理化分析的各项指标,而盐酸诺氟沙星配制的片剂在理化检验中出现扭曲、硬度增加、崩解等现象。因此,一种改进的配方被开发出来,它不会干扰物理和化学特性。结果表明,加入NFX HCl的改进制剂符合质量评价标准。
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引用次数: 8
ñ-Glucosidase Inhibitory Activity of Common Traditional Medicinal PlantsUsed for Diabetes Mellitus ñ-糖尿病常用中药葡糖苷酶抑制活性研究
Pub Date : 2015-12-07 DOI: 10.4172/2329-6631.1000144
A. Hamza, T. Ksiksi, Obaid Ali Al Shamsi, Salem Abobakr Balfaqh
Inhibition of α-glucosiase and the associated reduction of glucose absorption is an attractive approach for decreasing postprandial hyperglycemia and for the discovery of potent antidiabetic agents. One of the most important sources of potential α-glucosiase inhibitors represents the class of polyphenols. This paper aims to evaluate previous herbal polyphenol-rich extracts plan on the management of diabetes mellitus, to address their α-glucosidase inhibitory activity. Polyphenol-rich extracts from thirteen widely used traditionally anti-diabetic plants in Asia and Mediterranean regions were evaluated for their potential α-glucosidaseinhibitory activity. Among these evaluated plants, 10 were much stronger than that of acarbose standard. Punica granatum manifested the highest inhibitory activity with IC50 at 3.59 ± 0.11 μg/mL, followed by Psidium guajava with IC50 at 8.08 ± 0.10 μg/mL and Cinnamomum zeylanicum with IC50 at 9.87.08 ± 0.14 μg/mLA. A high correlation (r=0.65, p<0.001) was observed between α-glucosidase inhibition and total phenolic content of all plants. Punica granatum, P. guajava, C. zeylanicum and Ziziphus spina-christi had also the highest total phenolic content. Extracts for the above studied plant species may potentially replace acarbose in its current clinical use in improving post-prandial glycaemic control in type 2 diabetics. As a result, these polyphenol-rich extracts potentially offer a complementary approach to develop functional food and potential antidiabetic agents.
抑制α-葡萄糖酶和相关的葡萄糖吸收减少是降低餐后高血糖和发现有效的抗糖尿病药物的一个有吸引力的方法。潜在α-葡萄糖酶抑制剂的最重要来源之一是多酚类。本文旨在评价以往富含多酚的中药提取物对糖尿病的治疗方案,探讨其α-葡萄糖苷酶抑制活性。从13种亚洲和地中海地区广泛使用的传统抗糖尿病植物中提取富含多酚的提取物,对其α-葡萄糖苷酶抑制活性进行了评价。其中10株比阿卡波糖标准株强得多。石榴的抑菌活性最高,IC50为3.59±0.11 μg/mL,其次是瓜石榴,IC50为8.08±0.10 μg/mL,肉桂的IC50为9.87.08±0.14 μg/mL。α-葡萄糖苷酶抑制率与总酚含量呈高度相关(r=0.65, p<0.001)。石榴、瓜石榴、泽兰和酸枣的总酚含量最高。上述植物提取物有可能取代阿卡波糖,改善2型糖尿病患者餐后血糖控制。因此,这些富含多酚的提取物可能为开发功能性食品和潜在的抗糖尿病药物提供补充途径。
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引用次数: 7
Mathematical Models of the Pharmacokinetic Behavior of Digoxin in FiveHealthy Subjects following Rapid Intravenous Injection of 1 mg of Digoxin 5名健康受试者快速静脉注射1 mg地高辛后地高辛药代动力学行为的数学模型
Pub Date : 2015-11-24 DOI: 10.4172/2329-6631.1000143
Mária Äurišová
Objectives: The main objective of the current study was to present a further example which showed that a nontraditional mathematical modeling method can be advantageously used for the development of mathematical models in pharmacokinetics. An additional objective was to motivate researchers working in the field of pharmacokinetics to use a modeling method based on the theory of dynamic systems in their research work. Method: The current study is a companion piece of the earlier study by Kramer et al. Therefore the data published in the study cited here were used. As stated above, an advanced modeling method based on the theory of dynamic systems was employed. Conclusions: All mathematical models developed, successfully described the data of all volunteers investigated in the previous study by Kramer et al. and in the current study. The modeling method used in the current study is universal, comprehensive, and flexible. Therefore, it can be used to developed mathematical models not only in pharmacokinetics but also in several other scientific and practical fields.
目的:本研究的主要目的是提出一个进一步的例子,表明非传统的数学建模方法可以很好地用于药代动力学数学模型的开发。另一个目的是激励在药代动力学领域工作的研究人员在他们的研究工作中使用基于动力学系统理论的建模方法。方法:目前的研究是Kramer等人早期研究的一个同伴。因此,这里引用的数据发表在研究中。如上所述,采用了基于动态系统理论的先进建模方法。结论:所有建立的数学模型都成功地描述了Kramer等人在之前的研究和本次研究中调查的所有志愿者的数据。本研究采用的建模方法具有通用性、综合性和灵活性。因此,它不仅可以用来建立药代动力学的数学模型,还可以用于其他一些科学和实用领域。
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引用次数: 3
HPLC method development and validation as per ICH guidelines 根据ICH指南开发和验证HPLC方法
Pub Date : 2015-11-20 DOI: 10.4172/2329-6631.C1.011
Khalid Khan, Mohi Durakshan
Q based DOE approach was explored to study the effect of various factors influencing the optimisation of HPLC method for the simultaneous estimation of the four drugs viz. Ofloxacin (OFX), Ornidazole (ORN), Terbinafine Hydrochloride (TBH) and Clobetasol Propionate (CBP) in bulk drug and cream formulation. A full factorial design was employed to study the factors such as pH of the mobile phase, initial percentage of organic content for gradient elution (%BI) and gradient time (tG). The optimal conditions obtained after applying the principles of QbD with good system suitability parameters for all four drugs were found to be at pH 2.6, %BI as 24% of acetonitrile and gradient time of 4 min. The optimal conditions were found to be in a good agreement with the experimental results. The HPLC method thus developed was validated using ICH guidelines and was applied for the assay of cream formulation. The percentage recoveries were found to be 99.74±0.39 for OFX, 98.72±0.71 for ORN, 98.19±0.23 for TBH and 99.05±0.76 for CBP. The HPLC method was successfully applied to study the in vitro permeability of cream formulation in rat skin using Franz diffusion cell.
采用基于Q的DOE法,研究了影响原料药和乳膏配方中氧氟沙星(OFX)、奥硝唑(ORN)、盐酸特比萘芬(TBH)和丙酸氯倍他索(CBP)四种药物同时测定的各因素对HPLC法优化的影响。采用全因子设计研究流动相pH、梯度洗脱的初始有机含量百分比(%BI)和梯度时间(tG)等因素。应用QbD原理得到的最佳条件为pH为2.6,BI为乙腈的24%,梯度时间为4 min,系统适宜性参数好,与实验结果吻合较好。所建立的高效液相色谱法根据ICH指南进行了验证,并应用于乳膏配方的测定。OFX的回收率为99.74±0.39,ORN的回收率为98.72±0.71,TBH的回收率为98.19±0.23,CBP的回收率为99.05±0.76。采用高效液相色谱法,采用Franz扩散池对乳膏制剂在大鼠皮肤中的透性进行了研究。
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引用次数: 62
期刊
Journal of Developing Drugs
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