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New Utilities for Cancer Treatment to Inhibit Tubulin Assembly and Suppressing Microtubule Formation: Research Hypothesis 抑制微管蛋白组装和抑制微管形成在癌症治疗中的新应用:研究假设
Pub Date : 2018-09-27 DOI: 10.19080/omcij.2018.08.555727
V. Raj
The main objective of present research hypothesis was to give the idea and taking the attention of researcher for tubulin as an anticancer drug target. Inhibiting tubulin by novel lead scaffold may be helpful to treat the cancer with reduced side effect and higher selectivity toward the cancer cells. The present problems with cancer drug have cancer cell resistant and adverse effects. Assisting the solution of this problem, we hypothesized; Pharmacophore based selection for new scaffold may exhibit better binding affinity and selectivity towards the tubulin assembly and suppressing microtubule formation and attenuating the adverse effects and resistant of drug molecules.
本研究假设的主要目的是为微管蛋白作为抗癌药物靶点提供思路和引起研究者的重视。新型铅支架抑制微管蛋白可能有助于治疗癌症,减少副作用,提高对癌细胞的选择性。目前抗癌药物存在的问题是癌细胞耐药和不良反应。为了帮助解决这个问题,我们假设;基于药效团的新支架选择可能对微管蛋白的组装具有更好的结合亲和力和选择性,可以抑制微管的形成,减轻药物分子的不良反应和耐药性。
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引用次数: 0
Potentiometric Determination of Asenapine Maleate Using PVC Membrane and Carbon Paste Ion-selective Electrodes PVC膜-碳糊离子选择电极电位法测定马来酸阿西那平
Pub Date : 2018-09-20 DOI: 10.19080/omcij.2018.08.555726
Rowayda M Fouad
Asenapine maleate is a white to off-white non hygroscopic powder, slightly soluble in water (5.80 mg/mL) [1], sparingly soluble in 0.1 M HCl, soluble in methanol. The pH of a saturated asenapine solution in water is 4.2 at 23.5 0C, its pKa is 8.6. AS is atypical antipsychotic drug developed for the treatment of schizophrenia and acute mania associated with bipolar disorder [2]. It shows high affinity for numerous receptors like serotonin, adrenergic, dopamine, histamine [3]. Many methods have been mentioned in the literature for the determination of AS in pure form, in pharmaceutical formulation, as well as in biological fluids as, Titrimetric method [4], Spectrophotometric methods [5-8]. Gas chromatography [9], Liquid chromatography [10,11] and Thin layer chromatography [12]. Different HPLC methods using different mobile phases and detectors [13-24]. There were 5 stability indicating HPLC methods [25-29]. No electrochemical method was introduced for determination of asenapine. Ionselective electrodes have been used recently for quantitative determination of drugs as it has many advantages comparing to other sophisticated methods [30,31]. ISEs have low detection limit, good accuracy, wide concentration range and good applicability to turbid and coloured solutions. ISEs give high selectivity towards the drugs in the presence of different excipients. The proposed work introduces three different electrodes for the determination of asenapine maleate according to ICH guidelines [32]. The electrochemical sensitivity of the electrode is based on the incorporation of ion pair (AS-AR and AS–PTA) using PVC membrane and carbon paste (Figure 1). Figure 1: Chemical Structure of Asenapine Maleate.
马来酸阿塞那平为白色至灰白色不吸湿性粉末,微溶于水(5.80 mg/mL)[1],微溶于0.1 M盐酸,溶于甲醇。在23.5℃时,阿塞那平在水中的饱和溶液pH值为4.2,pKa为8.6。AS是一种非典型抗精神病药物,用于治疗精神分裂症和双相情感障碍相关的急性躁狂症[2]。它对血清素、肾上腺素、多巴胺、组胺等多种受体具有高亲和力[3]。文献中提到了许多测定纯形式、药物制剂以及生物液体中砷的方法,如滴定法[4]、分光光度法[5-8]。气相色谱法[9]、液相色谱法[10,11]、薄层色谱法[12]。不同的HPLC方法使用不同的流动相和检测器[13-24]。有5种稳定性指示HPLC方法[25-29]。未建立测定阿塞那平的电化学方法。离子选择电极最近被用于药物的定量测定,因为与其他复杂的方法相比,它具有许多优点[30,31]。检测限低,准确度好,浓度范围宽,适用于浑浊和有色溶液。在不同赋形剂的存在下,ise对药物具有很高的选择性。根据ICH指南[32],本文介绍了三种不同的电极用于测定马来酸阿塞那平。电极的电化学灵敏度是基于离子对(AS-AR和AS-PTA)在PVC膜和碳糊中的掺入(图1)。图1:马来酸阿西那平的化学结构。
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引用次数: 4
HPLC Detectors, Their Types and Use: A Review 高效液相色谱检测器的类型及应用综述
Pub Date : 2018-05-29 DOI: 10.19080/OMCIJ.2018.06.555700
A. Sunil
The most powerful technique to determine quantitatively and separate the mixture of composition in today’s modern chemistry is Chromatography especially High Performance Liquid Chromatography or High Pressure Liquid Chromatography [1]. HPLC works on the principle of Affinity chromatography. The solution of the sample is injected into a column of a porous material (stationary phase) and a liquid (mobile phase) is pumped at high pressure through the column. The mixture on travelling through the stationary phase splits into its constituents and the component with high affinity for stationary phase travels late whereas one with less affinity elutes fast. This is also based partition coefficient of the material [2]. Abstract
在当今的现代化学中,定量测定和分离混合物的最有力的技术是色谱法,特别是高效液相色谱法或高压液相色谱法。HPLC的工作原理是亲和色谱法。将样品的溶液注入多孔材料(固定相)柱中,并在高压下泵送液体(流动相)通过该柱。混合物在通过固定相时分裂成不同的组分,对固定相亲和度高的组分移动较晚,而对固定相亲和度低的组分洗脱较快。这也是基于材料的分割系数[2]。摘要
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引用次数: 5
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Organic & Medicinal Chemistry International Journal
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