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6-Gingerol is the most Potent Anticancerous Compound in Ginger (Zingiber officinale Rosc.) 6-姜辣素是生姜中最有效的抗癌化合物。
Pub Date : 2017-01-26 DOI: 10.4172/2329-6631.1000167
K. M., Shylajab Mr, Nazeemc Pa, Babu T
Cancer is one of the most deadly diseases in the world, which is caused due to uncontrolled growth of cells or malfunction of genes that control normal cell growth and division. Because of high death rate associated with cancer and because of serious side effects of chemotherapy and radiation therapy, many cancer patients seek alternative complementary methods of treatment. Ginger (Zingiber officinale Rosc.) is an important spice crop with immense medicinal properties and health beneficial effects. All the ginger ligands showed good interaction with the selected targets but based on ADME/Toxicity analysis 6-gingerol was superior with respect to absorption, solubility, and less neurotoxic effect as compared to other ginger ligands. 6-gingerol was also found cytotoxic to all the three cancer cells lines were studied. The cytotoxicity increased with increase in concentration of 6-gingerol. The IC50 values recorded for different cancer cell lines, 24 h. after treatment (100 µM for HCT15, 102 µM for L929 and 102 µM for Raw 264.7) showed uniform cytotoxicity in the three cell lines studied. The study highlights the potential of 6-gingerol for drug development against cancer.
癌症是世界上最致命的疾病之一,它是由于细胞不受控制的生长或控制正常细胞生长和分裂的基因发生故障而引起的。由于与癌症相关的高死亡率以及化疗和放射治疗的严重副作用,许多癌症患者寻求替代补充治疗方法。生姜(Zingiber officinale Rosc.)是一种重要的香料作物,具有巨大的药用价值和保健作用。所有生姜配体与选定靶点均表现出良好的相互作用,但基于ADME/毒性分析,与其他生姜配体相比,6-姜辣素在吸收、溶解度和神经毒性作用方面优于6-姜辣素。研究还发现6-姜辣素对三种癌细胞系均有细胞毒性。细胞毒性随6-姜辣素浓度的增加而增强。不同的癌细胞系在处理24 h后的IC50值(HCT15为100µM, L929为102µM, Raw 264.7为102µM)显示,所研究的三种细胞系的细胞毒性一致。这项研究强调了6-姜辣素在抗癌药物开发方面的潜力。
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引用次数: 32
Prevalence and Clinical Significance of Potential Drug-Drug Interactions at Ayder Referral Hospital, Northern Ethiopia 埃塞俄比亚北部艾德尔转诊医院潜在药物相互作用的患病率及临床意义
Pub Date : 2017-01-01 DOI: 10.4172/2329-6631.1000179
Teshager Aklilu Yesuf, A. Belay, Eskinder Ayalew Sisay, Zigbey Brhane Gebreamlak
Introduction: Clinically significant drug-drug interactions reduce effectiveness of drugs or cause fatal adverse events. Although harmful drug interactions are preventable, clinicians’ recognition and detection of drug interactions is not optimal. Objective: To assess prevalence, clinical significance and factors associated with potential drug-drug interactions at medical ward of Ayder Referral Hospital, Ethiopia. Methods: A cross-sectional study was conducted to determine potential drug-drug interactions. A total of 204 patients’ medical records were analyzed for drug-drug interaction using Micromedex drug interaction software. Data were analyzed using SPSS version 16. Results: We identified 135 interacting-combinations in a total of 266 potential drug-drug interactions (pDDIs) with a mean of 1.3 pDDIs per patient. Of these, 30.1% and 53.7% of patients had at least one major and one moderate pDDIs respectively. The most common pDDIs involved were concurrent use of clarithromycin with simvastatin, aspirin with heparin and dexamethasone with rifampin which have contraindication, major and moderate severity respectively. There was significant association of occurrence of pDDIs with polypharmacy (p<0.01). Conclusion: Potential drug-drug interactions were common at the medical ward of our hospital.
临床显著的药物-药物相互作用会降低药物的有效性或引起致命的不良事件。虽然有害的药物相互作用是可以预防的,但临床医生对药物相互作用的识别和检测并不理想。目的:评估埃塞俄比亚艾德尔转诊医院内科病房的患病率、临床意义和潜在药物-药物相互作用相关因素。方法:采用横断面研究确定潜在的药物-药物相互作用。采用Micromedex药物相互作用软件对204例患者病历进行药物相互作用分析。数据分析使用SPSS version 16。结果:我们在266个潜在的药物-药物相互作用(pddi)中确定了135个相互作用组合,平均每个患者1.3个pddi。其中,30.1%和53.7%的患者分别至少有一次重度和中度pddi。最常见的pddi是克拉霉素与辛伐他汀同时使用,阿司匹林与肝素同时使用,地塞米松与利福平同时使用,它们分别有禁忌症、重度和中度。pddi的发生与多药相关(p<0.01)。结论:在我院内科病房,潜在的药物相互作用较为普遍。
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引用次数: 3
Does the Boson Peaks Exist in Small Neutral Gold Clusters 小中性金团簇中存在玻色子峰吗
Pub Date : 2017-01-01 DOI: 10.4172/2329-6631.1000178
K. Vishwanathan, M. Springborg
The Boson peaks are typically ascribed to an excess density of vibrational states for the small clusters. A well resolved boson peak is observed in the low-frequency portion of the spectrum. A starting point for our discussion is the behaviour of the boson peak, derived from the vibrational density of states and the temperature dependencies of the vibrational heat capacities of the re-optimized neutral gold clusters. This Boson peak is associated with the existence of intermediate range order (IRO) in the arrangements of atoms. The low frequency (Far Infrared FIR, IR-C 200-10 cm−1) containing this dominant spectral line (Boson peak) is interpreted in terms of its relationship to the amplitude and extent of the density fluctuations in atoms and is, thereby, considered a measure of the intermediate range order in these atoms. We found a systematic relation among the boson peak energy, the boson peak intensity per atom, and the zigzag-bond density; the peak energy decreases and the peak intensity increases as zigzag-bond density decreases.
玻色子峰通常归因于小星团的振动态密度过大。在光谱的低频部分观察到一个分辨良好的玻色子峰。我们讨论的起点是玻色子峰的行为,该行为来源于状态的振动密度和重新优化的中性金团簇的振动热容的温度依赖性。这种玻色子峰与原子排列中存在中程序(IRO)有关。包含这条主要谱线(玻色子峰)的低频(远红外FIR, IR-C 200-10 cm−1)根据其与原子密度波动的幅度和程度的关系进行解释,因此被认为是这些原子中程顺序的量度。我们发现了玻色子峰值能量、每个原子的玻色子峰值强度与之字形键密度之间的系统关系;随着之字形键密度的减小,峰值能量减小,峰值强度增大。
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引用次数: 1
Design and Development of Fast Dissolving Tablet of Gliclazide 格列齐特速溶片的设计与研制
Pub Date : 2017-01-01 DOI: 10.4172/2329-6631.1000177
sharad Kondiba Kamble, S. ShindeSunita
In the present study, Gliclazide is a second-generation sulfonyl urea derivative used to treat non-insulin dependent diabetes mellitus. The drug has been classified as class-II drug according to biopharmaceutical classification system having low solubility and high permeability. So, an attempt was made to enhance the solubility of gliclazide by solvent evaporation technique. A significant enhancement of gliclazide dissolution rate will be obtained using by using suitable techniques. In this PVP-k30, polyethylene glycol and soluplus were mixed with the drug in different ratios (1:1, 1:3) and prepare P1, P2, PE1, PE2, S1 and S2 solid dispersion batches. The optimized solid dispersions P1 were further kneaded with suitable proportions of super disintegrants such as; Cross carmellose and Sodium starch glycolate. Dissolution profile will show decrease amount of drug release at specified time. DSC as well as X-ray diffraction showed reduced drug crystallinity in SDs. Scanning electron microscopy and particle size analysis revealed significant decreased particle size of the drug in SDs. FT-IR spectroscopy demonstrated no detectable interactions between the drug and excipients. On that the P1 batch will be consider for eight different fast dissolving tablets Preparation. The prepared FDT’s were evaluated for various parameters like disintegration time, wetting time, drug content, in vitro drug release study etc. and shows the satisfactory result. The formulation of F-4 containing cross carmellose sodium (5%) showed better result in disintegration time 11 sec. and maximum in vitro drug release of 99.89% at the end of 40 minutes.
在本研究中,格列齐特是第二代磺酰脲衍生物,用于治疗非胰岛素依赖型糖尿病。根据生物制药分类系统,该药物具有低溶解度和高渗透性,被归类为ii类药物。为此,尝试采用溶剂蒸发技术提高格列齐特的溶解度。采用合适的工艺可显著提高格列齐特的溶出率。在PVP-k30中,将聚乙二醇和溶液按不同比例(1:1,1:3)与药物混合,制备P1, P2, PE1, PE2, S1和S2固体分散批。将优化后的固体分散体P1与合适比例的强力崩解剂(如;交叉carmellose和Sodium starch glycolate。溶出曲线显示在一定时间内药物释放量减少。DSC和x射线衍射显示SDs中的药物结晶度降低。扫描电镜和粒径分析显示SDs中药物粒径明显减小。傅里叶变换红外光谱显示没有检测到药物和辅料之间的相互作用。在此基础上,P1批将被考虑用于八种不同的快速溶解片剂制备。对制备的FDT进行了崩解时间、润湿时间、药物含量、体外释药研究等参数的评价,取得了满意的结果。以5%交叉卡梅糖钠为主要成分的F-4为最佳处方,崩解时间为11秒,崩解40 min时体外最大释药率为99.89%。
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引用次数: 6
The Relationship of Polymorphism of RFC-I Gene on Methotrexate Serum Level and Related Toxicity in Pediatric Acute Lymphoblastic Leukemia 小儿急性淋巴细胞白血病rfc - 1基因多态性与甲氨蝶呤血清水平及相关毒性的关系
Pub Date : 2017-01-01 DOI: 10.4172/2329-6631.1000180
F. Zaker, S. Ansari, B. Toosi, M. Sayadi, H. Sharafi
Introduction: Methotrexate is one of the most effective agents in chemotherapy regimens for childhood ALL. However, methotrexate has remarkable side effects, which causes complications in various tissues and organs of some patients under treatment of this drug. It is proved that genetic factors can determine methotrexate toxicity. The aim of this study is to evaluate the effect of RFC-I A80G polymorphism on toxicity and serum level of methotrexate in children affected by acute lymphoblastic leukemia. Methods: A80G polymorphism of RFC-I was genotyped with PCR-RFLP method in 69 ALL patients treated with methotrexate. The relation between RFC-I genotypes and serum level of methotrexate and toxicity were evaluated using HPLC method and common terminology criteria for adverse events (CTCAE) respectively. Results: In this study, frequency of allele A for A80G polymorphism was 42.8% in patients who were studied. In consolidation phase, allele A frequency in patients with hepatotoxicity was higher than patients with no hepatic event (P=0.03, OR=2.32, 95% CI=1.10-4.98). Nevertheless, there were not any association between the other types of toxicity and RFC-I genotypes. Also, there was no association between A80G genotypes and the serum level of methotrexate. Conclusion: Based on the obtained results, we concluded that allele A of A80G polymorphism of RFC-I gene is a risk factor for methotrexate hepatotoxicity in consolidation phase and the A80G polymorphism can be utilized for prediction of methotrexate toxicity and dose adjustment.
简介:甲氨蝶呤是儿童ALL化疗方案中最有效的药物之一。然而,甲氨蝶呤有明显的副作用,一些患者在使用该药时会出现多种组织和器官的并发症。证明遗传因素可决定甲氨蝶呤的毒性。本研究旨在探讨RFC-I A80G多态性对急性淋巴细胞白血病患儿甲氨蝶呤毒性及血清水平的影响。方法:采用聚合酶链反应- rflp法对69例接受甲氨蝶呤治疗的ALL患者进行RFC-I A80G多态性基因分型。分别采用高效液相色谱法和不良事件通用术语标准(CTCAE)评价RFC-I基因型与甲氨蝶呤血清水平及毒性的关系。结果:本研究中A80G多态性等位基因A的频率为42.8%。在巩固期,肝毒性患者的等位基因A频率高于无肝事件患者(P=0.03, OR=2.32, 95% CI=1.10-4.98)。然而,其他类型的毒性与rfc - 1基因型之间没有任何关联。A80G基因型与血清甲氨蝶呤水平无相关性。结论:基于上述结果,我们认为RFC-I基因A80G多态性等位基因A是甲氨蝶呤巩固期肝毒性的危险因素,A80G多态性可用于甲氨蝶呤毒性和剂量调整的预测。
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引用次数: 2
Ternary Amorphous Solid Dispersions 三元非晶固体分散体
Pub Date : 2017-01-01 DOI: 10.4172/2329-6631.1000181
Dev Prasad, J. Lande, H. Chauhan, Harsh Chauhan
Dev Prasad1*, Jagdish Lande2, Hari Chauhan3 and Harsh Chauhan4 1Massachusetts College of Pharmacy and Health Sciences, MCPHS University, Boston, MA, USA 2Department of Analytical Innovation and Development, Fresenius Kabi, USA 3Analogue Devices, Cambridge, MA, USA 4Creighton University, Omaha, NE, USA *Corresponding author: Dev Prasad, Massachusetts College of Pharmacy and Health Sciences, MCPHS University, Boston, MA, USA, Tel: +1 617-732-2800; E-mail: dp1611@gmail.com
Dev Prasad1*, Jagdish Lande2, Hari Chauhan3和Harsh Chauhan4 1美国波士顿MCPHS大学马萨诸塞州药学与健康科学学院2美国Fresenius Kabi分析创新与发展部3美国剑桥模拟器件4美国奥马哈克雷顿大学通讯作者:Dev Prasad,马萨诸塞州波士顿MCPHS大学马萨诸塞州药学与健康科学学院,电话:+1 617-732-2800;电子邮件:dp1611@gmail.com
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引用次数: 1
A Review of Plant Sulfated Polysaccharides and their Relations with Anticoagulant Activities 植物硫酸多糖及其与抗凝血活性的关系研究进展
Pub Date : 2016-12-12 DOI: 10.4172/2329-6631.1000166
Oliveira Rcr, Almeida Rr, Gonçalves Ta
Heparin is an important therapeutic agent for the prophylaxis and treatment of thrombosis. Although effective, heparin can cause, among other adverse effects, bleeding and thrombocytopenia, being obtained from bovine lungs and porcine intestines, causing concern about contamination with pathogenic animal agents. This study aimed at reviewing the literature on the relationship between the sulfated polysaccharides isolated from plants and anticoagulant activity. Based on articles published between 2009 and 2016 was found that sulfation of polysaccharides can potentiate its biological activity, which is, in turn, influenced by the degree of substitution obtained, in the reaction, of the position of the sulfate group in the molecule or the final molecular weight. Thus, it is evident that the interest in the use of plant sulfated polysaccharides in the therapeutic field has increased, demonstrating the relevance of research in the field of drugs and materials.
肝素是预防和治疗血栓形成的重要药物。肝素虽然有效,但从牛肺和猪肠中提取的肝素可引起出血和血小板减少症等不良反应,引起人们对动物致病性病原体污染的担忧。本文对植物硫酸酸化多糖与抗凝血活性的关系进行了综述。根据2009年至2016年间发表的文章,我们发现多糖的磺化可以增强其生物活性,而这反过来又受到反应中获得的取代度的影响,硫酸盐基团在分子中的位置或最终分子量。因此,很明显,在治疗领域使用植物硫酸多糖的兴趣已经增加,表明在药物和材料领域的研究的相关性。
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引用次数: 15
Effect of AF-Anti Fungal Cream on Stratum Corneum and its Importance in Treating Cutaneous Mycoses af -抗真菌乳膏对角质层的作用及其在皮肤真菌病治疗中的意义
Pub Date : 2016-11-22 DOI: 10.4172/2329-6631.1000163
Aruna., Amrurthavalli Gv, G. Rajagopal
We have targeted the adhesion mechanism of fungal colonization to develop an effective siddha proprietary medicine-AF cream. The time tested siddha herbs like Cassia alata and Azadirachta indica were used to achieve total freedom from fungal infection. The findings show the uniqueness and the likely therapeutic value of AF cream in treating cutaneous fungal infection.
我们针对真菌定植的粘附机制,开发了一种有效的悉达专有药物- af霜。经过时间考验的siddha草药,如决明子和印楝,被用来实现完全免于真菌感染。结果显示AF乳膏治疗皮肤真菌感染的独特性和可能的治疗价值。
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引用次数: 1
Ivabradine for the Management of Chronic Stable Angina: Should it beconsidered? 伊伐布雷定治疗慢性稳定型心绞痛:应该考虑吗?
Pub Date : 2016-11-14 DOI: 10.4172/2329-6631.1000e149
Amy Wang
Angina, or chest pain, often occurs when oxygen demand of the heart exceeds oxygen supply. The imbalance between oxygen supply and demand may be due to blockage in the coronary arteries, arterial vasospasm, or myocardial dysfunction [1]. Chronic stable angina (CSA) is described as having chest pain due to exertion (such as exercise or stress), or chest pain that is relieved by rest or administration of nitroglycerin [2]. Conventional therapies for CSA includes negative inotropes, such as beta blockers (BB) and calcium channel blockers (CCB), or vasodilators, such as nitroglycerin (NTG). Unfortunately, BBs and CCBs have been associated with adverse effects such as fatigue and severe bradycardia, while use of NTG may lead to severe hypotension and headache [1]. Ivabradine is a new class of medication, and works by blocking the If current in the sinoatrial node to slow down heart rate. By lowering the heart rate, it decreases workload and oxygen demand for the heart [3]. In the European Union, ivabradine was approved for the management of symptoms on CSA in patients with history of coronary artery disease (CAD), or for the management of heart failure (HF). Prior to initiating ivabradine for the management of CSA, patients must have heart rates of at least 70 beats per minute, and either cannot tolerate beta blocker therapy, or whose symptoms are not adequately controlled by beta blocker therapy alone [4]. In the United States, ivabradine is only approved for the management of HF, but not for CSA [3].
心绞痛或胸痛通常发生在心脏需氧量超过供氧量时。冠状动脉阻塞、动脉血管痉挛、心肌功能障碍等可能导致血氧供需失衡[1]。慢性稳定型心绞痛(CSA)被描述为由于用力(如运动或压力)引起胸痛,或通过休息或给予硝酸甘油缓解胸痛[2]。CSA的常规治疗包括负性肌力药物,如-受体阻滞剂(BB)和钙通道阻滞剂(CCB),或血管扩张剂,如硝酸甘油(NTG)。不幸的是,BBs和CCBs与疲劳和严重心动过缓等不良反应有关,而使用NTG可能导致严重的低血压和头痛[1]。伊伐布雷定是一种新型药物,通过阻断窦房结的If电流来降低心率。通过降低心率,它减少了心脏的工作量和需氧量[3]。在欧盟,伊伐布雷定被批准用于治疗有冠状动脉疾病(CAD)病史的CSA患者的症状,或用于治疗心力衰竭(HF)。在开始使用伊伐布雷定治疗CSA之前,患者的心率必须至少为每分钟70次,并且不能耐受受体阻滞剂治疗,或者仅使用受体阻滞剂治疗不能充分控制症状[4]。在美国,伊伐布雷定仅被批准用于治疗心衰,未被批准用于CSA[3]。
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引用次数: 0
Pharmacological Options Beyond Proton Pump Inhibitors in Children with Gastroesophageal Reflux Disease 儿童胃食管反流病质子泵抑制剂以外的药物选择
Pub Date : 2016-10-18 DOI: 10.4172/2329-6631.1000161
C. Armano, L. Fumagalli, A. Ripepi, A. Moretti, F. Macchi, A. Scolari, S. Salvatore
Pharmacological treatment of gastroesophageal reflux (GER) disease is mostly based on acid control. However, different molecules have been proposed both for patients with persisting symptoms and to limit adverse effects of proton pump inhibitors (PPI). This paper focuses on other acid inhibitors, alginate, prokinetics, drug acting on lower esophageal sphincter and esophageal hypersensitivity. Mechanism of action, indications, efficacy, limits and recent advances are reported. Pediatric data and possible adverse effects are also considered.
胃食管反流(GER)疾病的药物治疗主要基于胃酸控制。然而,对于持续症状的患者和限制质子泵抑制剂(PPI)的不良反应,已经提出了不同的分子。本文重点介绍了其他酸抑制剂,海藻酸盐,前动力学,作用于食管下括约肌的药物和食管超敏反应。现报道其作用机制、适应症、疗效、局限性及最新进展。儿童数据和可能的不良反应也被考虑。
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引用次数: 0
期刊
Journal of Developing Drugs
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