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An Update on Oral Anti-coagulants 口服抗凝血剂的最新进展
Pub Date : 2015-09-14 DOI: 10.4172/2329-6631.1000134
Deepak Gupta, Raman Sharma
Anti-thrombotic drugs generally refer to the group of drugs that prevent either occurrence or enlargement of a thrombus. They can be broadly divided into anti-coagulant (AC) and anti-platelet agents. Alternatively, some anti-thrombotics specifically referred to as thrombolytic, can act by dissolving already existing clots. ACs plays a very significant role in pharmacotherapy and oral ACs is major players in outpatient settings. Main focus of this article will be on oral ACs including application and comparison of newer agents with warfarin, which is still considered a gold standard in AC therapy.
抗血栓药物一般是指一组预防血栓发生或扩大的药物。它们大致可分为抗凝血剂(AC)和抗血小板剂。另外,一些抗血栓药物,特别是溶栓药物,可以通过溶解已经存在的血栓来起作用。ACs在药物治疗中起着非常重要的作用,口服ACs在门诊治疗中发挥着重要作用。本文的主要重点将是口服AC,包括与华法林的应用和比较,华法林仍然被认为是AC治疗的金标准。
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引用次数: 0
Characterization of Physical, Thermal and Spectral Properties of Biofield Treated 2, 6-Diaminopyridine 生物场处理2,6 -二氨基吡啶的物理、热及光谱特性表征
Pub Date : 2015-08-28 DOI: 10.4172/2329-6631.1000133
M. Trivedi, R. M. Tallapragada, A. Branton, Dahryn Trivedi, G. Nayak, R. Mishra, S. Jana
2, 6-Diaminopyridine (2, 6-DAP) has extensive use in synthesis of pharmaceutical compounds. The objective of present research was to investigate the influence of biofield treatment on physical, thermal and spectral properties of 2, 6-DAP. The study was performed in two groups, control and treated. The control group remained as untreated, and biofield treatment was given to treatment group. The control and treated 2, 6-DAP samples were characterized by X-ray diffraction (XRD), Differential scanning calorimetry (DSC), Thermo gravimetric analysis (TGA), Laser particle size analyzer, surface area analyzer, Fourier transform infrared (FT-IR) spectroscopy, and UV-visible spectroscopy. XRD analysis revealed decrease in intensity of the peaks of treated 2, 6-DAP with respect to control. Unit cell volume and molecular weight were decreased by 2.97% and 2.98% respectively in treated 2, 6-DAP as compared to control. Crystallite size was decreased by 24.70% in treated 2, 6-DAP with respect to control. DSC analysis showed no significant change in melting temperature of treated 2, 6-DAP with respect to control. Nevertheless, the treated 2, 6-DAP showed significant increase in latent heat of fusion by 35.52% as compared to control 2, 6-DAP. TGA analysis showed decrease in percent weight loss of the treated 2, 6-DAP in comparison with control. Additionally, substantial increase in maximum thermal decomposition temperature (Tmax) was observed in treated 2, 6-DAP (203.52°C) as compared with control 2, 6-DAP (186.84°C). Particle size analysis results showed a substantial decrease in d50 (average particle size) and d99 (size exhibited by 99% of the particles) of the treated 2, 6-DAP by 20.5 and 57.4%, respectively as compared to control. Additionally, the BET analysis showed substantial increase in surface area of treated 2, 6-DAP by 75.58% as compared to control. FT-IR spectrum of treated 2, 6-DAP showed alteration in O-H stretching (3390→3370 cm-1), C-H stretching (3132→3138 cm-1) and N-H bending (1637→1604 cm-1) vibration peaks with respect to control. However, UV-visible analysis of treated 2, 6-DAP showed no significant changes in absorption peaks (λ max) with respect to control. Overall, the results demonstrated that biofield has significant impact on the physical, thermal and spectral properties of the treated 2, 6-DAP.
2,6 -二氨基吡啶(2,6 - dap)在药物化合物的合成中有着广泛的用途。本研究的目的是研究生物场处理对2,6 - dap的物理、热和光谱性质的影响。研究分为两组,对照组和实验组。对照组不进行治疗,治疗组给予生物场治疗。采用x射线衍射(XRD)、差示扫描量热法(DSC)、热重分析(TGA)、激光粒度分析仪、表面积分析仪、傅里叶变换红外光谱(FT-IR)和紫外可见光谱对对照和处理后的2,6 - dap样品进行了表征。XRD分析表明,处理后的2,6 - dap的峰强度与对照相比有所降低。与对照相比,2,6 - dap处理的细胞体积和分子量分别降低了2.97%和2.98%。与对照相比,2,6 - dap处理的晶体尺寸减小了24.70%。DSC分析显示,与对照组相比,处理后的2,6 - dap的熔化温度没有显著变化。然而,与对照2,6 - dap相比,2,6 - dap处理组的融合潜热显著增加35.52%。TGA分析显示,与对照组相比,2,6 - dap处理组的体重损失率有所下降。此外,与对照2,6 - dap(186.84°C)相比,2,6 - dap处理的最高热分解温度(Tmax)显著增加(203.52°C)。粒径分析结果表明,处理后的2,6 - dap的d50(平均粒径)和d99(99%的颗粒显示的粒径)分别较对照显著降低20.5%和57.4%。此外,BET分析显示,与对照组相比,处理过的2,6 - dap的表面积大幅增加了75.58%。处理后的2,6 - dap的FT-IR光谱显示,与对照相比,O-H拉伸(3390→3370 cm-1)、C-H拉伸(3132→3138 cm-1)和N-H弯曲(1637→1604 cm-1)振动峰发生了变化。然而,处理后的2,6 - dap的紫外可见分析显示,与对照相比,吸收峰(λ max)没有显著变化。综上所述,生物场对处理后的2,6 - dap的物理、热和光谱特性有显著影响。
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引用次数: 25
Treatment Development of Chronic Myeloid Leukemia 慢性髓性白血病的治疗进展
Pub Date : 2015-08-22 DOI: 10.4172/2329-6631.1000E144
Gamal Abdul Hamid
Chronic Myeloid Leukemia (CML) is a hematologic stem cell disorder leading to myeloproliferation and its attendant consequences [1]. CML typically evolves in 3 distinct clinical phases; An indolent or chronic phase (CP) course easily controlled with therapy that can last for 3 to 5 years and accelerated phase (AP) that lasts for less than 12 months and blast phase (BP), characterized by rapid expansion of a population of myeloid or lymphoid blasts of at least 30% in the peripheral blood or bone marrow resulting in the patient’s death within 4 to 6 months [2]. Busulfan is the oral anti-CML alkylating agent in the 1950s and was convenient to administer and inexpensive but associated with severe and prolong myelosuppression. Busulfan was largely replaced by hydroxyurea in 1970s. Hydroxyurea was the available and effective anti-CML agents in the 1980s. These were able to control the clinical manifestations of the disease, but were rarely, if ever, capable of eliminating the malignant clone. In 1990s the interferon alpha has constituted first-line therapy for patients with CML resulted in major cytogenetic responses of 25% [3]. The combination of interferon alpha with hydroxyurea or with Ara-C was effective in clinical practice and induces cytogenetic remissions in some patients [4].
慢性髓系白血病(Chronic Myeloid Leukemia, CML)是一种导致骨髓增生及其相关后果的血液干细胞疾病[1]。CML通常分为3个不同的临床阶段;通过治疗易于控制的慢性期或慢性期(CP)病程,可持续3 ~ 5年;加速期(AP)持续不到12个月;母细胞期(BP),其特征是外周血或骨髓中髓细胞或淋巴细胞群迅速扩增至少30%,导致患者在4 ~ 6个月内死亡[2]。布磺胺是20世纪50年代的口服抗cml烷基化剂,使用方便,价格低廉,但与严重和延长的骨髓抑制有关。20世纪70年代,Busulfan在很大程度上被羟基脲取代。羟基脲是20世纪80年代可用且有效的抗cml药物。这些药物能够控制疾病的临床表现,但很少能够(如果有的话)消除恶性克隆。20世纪90年代,干扰素α作为CML患者的一线治疗药物,导致25%的主要细胞遗传学应答[3]。在临床实践中,干扰素α与羟基脲或与Ara-C联合使用是有效的,并在一些患者中引起细胞遗传学缓解[4]。
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引用次数: 3
Preliminary Identification of Lactate Dehydrogenase Inhibitors towards Anticancer Drug Development 乳酸脱氢酶抑制剂在抗癌药物开发中的初步鉴定
Pub Date : 2015-08-20 DOI: 10.4172/2329-6631.1000132
A. Emmanuel, J. Sanya, O. Olubiyi
In tumor cells undergoing rapid cellular division, significantly increased quantities of lactic acid are produced in an anaerobic respiration via the Cori cycle. While this produces a lower of the pH in the local environment, the hepatic conversion of the generated lactate into glucose places a huge energy demand on the body which makes the patient weaker and results in cancer cachexia. Thus, instead of producing acetyl CoA, the dividing tumorous cells synthesize lactic acid catalyzed by the enzyme lactate dehydrogenase (LDH). LDH’s involvement in tumor initiation and metabolism primarily involves a state of fermentative glycolysis catalyzed by the A form of the enzyme which allows tumorous cells convert the majority of their glucose stores into lactate even under anaerobic conditions which invariably shifts the utilization of glucose metabolites from simple energy production to an active promotion of accelerated cell growth and replication. This makes LDH a vital target for drug development. And in the present work a combination of virtual screening, database scouting and biophysical analysis of binding site properties have been employed in analysis the interaction of about 30,000 compounds with LDH. Using a synthetic NADH inhibitor, as a reference, only four compounds were found to demonstrate stronger binding features than the inhibitor. This preliminary in silicon screening represents the foundational effort in a cancer drug discovery project aimed at generating specific inhibitors of LDH for use in cancer therapeutics.
在经历快速细胞分裂的肿瘤细胞中,通过Cori循环在厌氧呼吸中产生的乳酸量显著增加。虽然这会降低局部环境的pH值,但肝脏将生成的乳酸转化为葡萄糖会对身体产生巨大的能量需求,从而使患者变得更虚弱,并导致癌症恶病质。因此,分裂的肿瘤细胞不产生乙酰辅酶a,而是合成乳酸脱氢酶(乳酸脱氢酶)催化的乳酸。LDH参与肿瘤起始和代谢主要涉及由酶的a形式催化的发酵性糖酵解状态,该状态允许肿瘤细胞将其大部分葡萄糖储存转化为乳酸盐,即使在厌氧条件下也不可避免地将葡萄糖代谢物的利用从简单的能量生产转变为积极促进加速细胞生长和复制。这使得LDH成为药物开发的重要靶点。在目前的工作中,结合虚拟筛选、数据库搜索和结合位点特性的生物物理分析,分析了大约30,000种化合物与LDH的相互作用。以合成的NADH抑制剂为对照,发现只有四种化合物比该抑制剂具有更强的结合特性。这项初步的硅筛选代表了癌症药物发现项目的基础工作,该项目旨在产生用于癌症治疗的LDH特异性抑制剂。
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引用次数: 3
In vivo anti-diabetic effects of aqueous leaf extracts of Rhoicissus tridentata in alloxan induced diabetic mice 三叉荆叶水提物对四氧嘧啶诱导的糖尿病小鼠的体内抗糖尿病作用
Pub Date : 2015-06-08 DOI: 10.4172/2329-6631.1000131
M. J. Mukundi, N. E. Mwaniki, N. M. Piero, Njagi J Murugi, Agyirifo S Daniel, Gathumbi K Peter, Muchugi N Alice
The drawbacks associated with conventional anti-diabetic agents have largely stimulated desire for alternative and complementary anti-diabetic agents, majority of which are plant-derived. The medicinal plant, Rhoicissus tridentata has been used extensively in traditional medical practice against various ailments. However, its ethno medicinal use against diabetes mellitus has not been scientifically evaluated and validated. This study was, therefore, designed to evaluate the anti-diabetic potential of aqueous leaf extracts of Rhoicissus tridentata in alloxan induced diabetic mice. As the results show, the aqueous leaf extracts of Rhoicissus tridentata showed anti-diabetic activity. The intraperitoneal route of herbal extract administration was found to be more effective than the oral route. Further, qualitative and quantitative phytochemical screening of aqueous leaf extracts of Rhoicissus tridentata indicated the presence of phenols, alkaloids, flavonoids, tannins and saponins. However, cardiac glycosides and phylobatanins were not detected.
传统抗糖尿病药物的缺点在很大程度上刺激了对替代和补充抗糖尿病药物的需求,其中大多数是植物来源的。药用植物三叉戟在传统医学实践中被广泛用于治疗各种疾病。然而,其对糖尿病的民族药用作用尚未得到科学的评价和验证。因此,本研究旨在评价三叉戟叶水提物对四氧嘧啶诱导的糖尿病小鼠的抗糖尿病作用。结果表明,三叉戟叶水提物具有抗糖尿病活性。研究发现,中药提取物腹腔给药比口服给药更有效。此外,对三叉红叶水提物进行了定性和定量的植物化学筛选,发现其中含有酚类、生物碱、黄酮类、单宁和皂苷。但未检测到心糖苷和藻蓝蛋白。
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引用次数: 21
The Role of Machine Learning in Drug Design and Delivery 机器学习在药物设计和交付中的作用
Pub Date : 2015-05-18 DOI: 10.4172/2329-6631.1000E143
Jonathan P. Bernick
The applications discussed in this article typically use learning machines to perform supervised classification; i.e., the construction of algorithms to determine of the presence or absence of an exemplar in a class based on the values of the data comprising said exemplar. For example, a pharmacologist who wished to predict whether potential drug compounds were neurotoxic or not might use machine learning to construct a decision function from a set of drugs of known neurotoxicity or lack-thereof, and the function thus created would classify other drug compounds as belonging to the mutually exclusive classes of “neurotoxic” or “non-neurotoxic.”
本文讨论的应用程序通常使用学习机来执行监督分类;即,基于包含所述示例的数据的值来确定类中示例的存在或不存在的算法的构造。例如,一位希望预测潜在药物化合物是否具有神经毒性的药理学家可能会使用机器学习从一组已知或缺乏神经毒性的药物中构建决策函数,从而创建的函数将其他药物化合物分类为属于相互排斥的“神经毒性”或“非神经毒性”类别。
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引用次数: 4
Protective Effects of Urtica dioica and Cimetidineî on Liver FunctionFollowing Acetaminophen Induced Hepatotoxicity in Mice 荨麻疹和Cimetidineî对对乙酰氨基酚肝毒性小鼠肝功能的保护作用
Pub Date : 2015-05-09 DOI: 10.4172/2329-6631.1000130
J. Kk, Maina Sg, Muriithi Jn, Mwangi Bm, Mworia Kj, M. M.J., J. Ngeranwa, Mburu Nd
Studies have demonstrated that Urtica dioica promotes regeneration of the liver cells following damage by carbon tetrachloride. This study investigated the effects of Urtica dioica on liver function following acetaminophen overdose. Mice were divided into eight groups of ten each. Acetaminophen at 250 mg/kg and 500 mg/kg significantly (p<0.05) reduced red blood cells, neutrophils and albumins while mean corpuscular hemoglobin, lymphocytes, alanine amino transferase, aspartate amino transferase, prothrombin time and liver pathology were increased. Lactate dehydrogenase was significantly reduced in acetaminophen 250 mg/kg while acetaminophen 500 mg/kg significantly increased alkaline phosphatase and total bilirubin. Even after exposure to acetaminophen toxicity, mice pre-treated with Urtica dioica retained the following parameters within normal range: neutrophils, lymphocytes, alanine amino transferase, and liver integrity. Mice co-treated with the drug cimetidine had all parameters within normal except for aspartate amino transferase at acetaminophen dose of 500 mg/kg. The result suggests that Urtica dioica and cimetidine are both hemoprotective and hepatoprotective. They have potential in the management of acetaminophen toxicity.
研究表明,荨麻能促进四氯化碳损伤后肝细胞的再生。本研究探讨了荨麻疹对对乙酰氨基酚过量后肝功能的影响。老鼠被分成8组,每组10只。250 mg/kg和500 mg/kg对乙酰氨基酚显著(p<0.05)降低了红细胞、中性粒细胞和白蛋白,平均红细胞血红蛋白、淋巴细胞、丙氨酸氨基转移酶、天冬氨酸氨基转移酶、凝血酶原时间和肝脏病理升高。对乙酰氨基酚250 mg/kg组乳酸脱氢酶显著降低,对乙酰氨基酚500 mg/kg组碱性磷酸酶和总胆红素显著升高。即使在暴露于对乙酰氨基酚毒性后,经荨荨痛预处理的小鼠仍将以下参数保持在正常范围内:中性粒细胞、淋巴细胞、丙氨酸氨基转移酶和肝脏完整性。对乙酰氨基酚剂量为500 mg/kg时,除天冬氨酸氨基转移酶外,其余指标均正常。结果表明,杜鹃花和西咪替丁均具有保护血液和肝脏的作用。它们在治疗对乙酰氨基酚毒性方面具有潜力。
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引用次数: 13
Methods Introduction of Transgenic Animal 方法转基因动物介绍
Pub Date : 2015-04-16 DOI: 10.4172/2329-6631.1000E142
Andrea Wang
At present, the most common used method for producing transgenic animal is known as DNA microinjection. It directly injects the exogenous gene into fertilized egg cells by using a syringe with micromanipulation instrument. With the exogenous gene integrated into DNA, a transgenic animal is produced. The founders of this method are Jaenisch, Mintz etc. Gordon and Palmiter [1] successively obtained transgenic animals by this method. This method is commonly used at present, and now the transgenic animal research is mostly going based on the Palmiter method, or the method on its improvement. Wang Minhua [2] reported he produced transgenic rabbits with microinjection method transferring anti plague virus nucleic acid enzyme gene. Application of Krimpenfort produced transgenic bovine using both embryos cultured in vitro and microinjection methods.
目前,生产转基因动物最常用的方法是DNA显微注射。它通过带微操作仪器的注射器将外源基因直接注射到受精卵细胞中。将外源基因整合到DNA中,就产生了转基因动物。这种方法的创始人是耶尼施、明茨等人。Gordon和Palmiter[1]先后用这种方法获得了转基因动物。该方法是目前常用的方法,目前的转基因动物研究大多是在帕尔米特方法或其改进方法的基础上进行的。王敏华b[2]报道了用微量注射法转移抗鼠疫病毒核酸酶基因制备转基因家兔。krmpenfort转基因牛体外培养和显微注射的应用。
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引用次数: 0
Triple-Negative Breast Cancer; Future Treatment in Limited Resource Centers 三阴性乳腺癌;在有限资源中心的未来治疗
Pub Date : 2015-04-16 DOI: 10.4172/2329-6631.1000E141
Gamal Abdul Hamid, S. Yassin, F. Al-Ahdel
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引用次数: 3
Recent Developments in Cancer 癌症的最新进展
Pub Date : 2015-04-14 DOI: 10.4172/2329-6631.1000R001
Sushma Bottu, Ravalli Remella
Cancer is one among the leading cause of deaths worldwide. In the present review I have mentioned recent statistics of cancer and mentioned few recent developments in cancer research especially on the most common cancers like lung cancer, breast cancer, prostate cancer, skin cancer and endometrial cancer which would give a brief idea on the ongoing research in cancer for the students, Research Scholars.
癌症是世界上导致死亡的主要原因之一。在目前的回顾中,我提到了最近的癌症统计数据并提到了癌症研究的一些最新进展特别是在最常见的癌症上,如肺癌,乳腺癌,前列腺癌,皮肤癌和子宫内膜癌这将给正在进行的癌症研究的学生,研究学者一个简要的想法。
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引用次数: 7
期刊
Journal of Developing Drugs
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