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In Vitro Anti-Acetylcholinesterase Activity of Crude Fruits Sap Extract of Solanum incanum in Green Peach Aphids 龙葵果液提取物对青桃蚜虫体外抗乙酰胆碱酯酶活性的研究
Pub Date : 2015-11-10 DOI: 10.4172/2329-6631.1000142
A. Umar, A. J. Mgutu, N. M. Piero, Njoroge W Ann, Gitahi S Maina, M. Maina, N. J. Muriithi, M. J. Kiambi, Ngure G Mutero, Mwonjoria K John
Acetylcholinesterase is a key enzyme that terminates nerve impulses by catalyzing the hydrolysis of neurotransmitter, acetylcholine, in the nervous system in various organisms. Irreversible inhibitors have been developed as insecticides such as organophosphates and carbamates. Aqueous crude fruit sap extract of S. incanum was evaluated for acetylcholinesterase activity in green peach aphids using Ellman’s method and is found active in inhibiting the ACHe of green peach aphids. All tested concentrations of crude fruits sap extract of S. incanum possessed the ability to inhibit acetylcholinesterase of green peach aphids at dose dependent manner and IC50 of 49.9 was calculated. This study suggest that aqueous crude fruit sap extract of S. incanum inhibit the acetylcholinesterase of the green peach aphids and it is possible the extract has compounds that increase both the level and duration of the neurotransmitter action.
乙酰胆碱酯酶是多种生物神经系统中通过催化神经递质乙酰胆碱水解而终止神经冲动的关键酶。不可逆抑制剂如有机磷酸酯和氨基甲酸酯已被开发为杀虫剂。用Ellman法测定了白杨水提液对青桃蚜虫乙酰胆碱酯酶活性的影响,发现白杨水提液对青桃蚜虫乙酰胆碱酯酶活性有抑制作用。各试验浓度对青桃蚜虫乙酰胆碱酯酶的抑制作用均呈剂量依赖性,IC50为49.9。本研究表明,白芷水提物对青桃蚜虫乙酰胆碱酯酶有抑制作用,可能含有增加神经递质作用水平和持续时间的化合物。
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引用次数: 4
Routes of Opioid Abuse and its Novel Deterrent Formulations 阿片类药物滥用途径及其新型威慑制剂
Pub Date : 2015-11-09 DOI: 10.4172/2329-6631.1000141
A. Omidian, D. Mastropietro, H. Omidian
This review aimed to investigate the abuse patterns of common prescription opioids currently on the market by collecting large-scale surveys of different abuser populations. Furthermore, we aimed to analyze the efficacy and properties of currently implemented abuse-deterrent formulations (ADF) for these compounds. Our investigation showed that while oxycodone and oxymorphone are primarily abused by oral ingestion and insufflations, respectively, their ADF products (reformulated OxyContin and Opana ER) show some encouraging results to deter their abuse. Tapentadol is not popular amongst abuser populations, its ADF are difficult to tamper with, and it does not produce significantly desirable effects in noncompliant patients when compared to other opioids. Hydromorphone is predominantly abused by injection, and any effective abuse-deterrent strategy must specifically prioritize and target this route. Current formulations have successfully conferred aversive properties onto the drug in the event of preparation for injection, yet overall rates of hydromorphone abuse remain high, suggesting that more innovative steps need to be taken. Despite novel deterrent technologies that collectively offer deterrence by insufflations, injection and co-ingestion with alcohol, more priority needs to be given to deterring the most common and accessible route of abuse, i.e., oral ingestion of multiple doses.
本综述旨在通过收集不同滥用人群的大规模调查,调查目前市场上常见处方阿片类药物的滥用模式。此外,我们旨在分析目前实施的滥用威慑制剂(ADF)对这些化合物的功效和性质。我们的调查显示,虽然羟考酮和羟吗啡酮主要通过口服摄入和注射滥用,但它们的ADF产品(重新配制的奥施康定和Opana ER)显示出一些令人鼓舞的结果,以阻止它们的滥用。他他多在滥用人群中不受欢迎,它的ADF难以篡改,与其他阿片类药物相比,它在不依从性患者中不会产生显着的理想效果。氢吗啡酮主要通过注射滥用,任何有效的滥用威慑策略都必须特别优先考虑和针对这一途径。目前的配方已经成功地赋予药物在制备注射时的厌恶特性,但氢吗啡酮的总体滥用率仍然很高,这表明需要采取更多的创新措施。尽管新的威慑技术通过注入、注射和与酒精一起摄入共同提供威慑,但需要更加优先考虑阻止最常见和最容易获得的滥用途径,即口服多次剂量。
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引用次数: 4
The Antioxidant Activities of C3, 6-Dibenzoylated Phenyl-Thiosemicarbazone-Chitosans C3, 6-二苯甲酰化苯基硫代氨基脲壳聚糖的抗氧化活性
Pub Date : 2015-11-03 DOI: 10.4172/2329-6631.1000140
Yunliang Dai, Zhimei Zhong
Ten new C3, 6-dibenzoylated thiosemicarbazone-chitosan derivatives (with two different molecular weights) were prepared. The purpose of this study was to further investigate the antioxidant activities of this series of derivatives and the relationship between the structure and their antioxidant behavior. In order to know how the structure influenced the antioxidant activities of the derivatives, their structures were characterized by FT-IR spectroscopy and elemental analysis in this paper. In addition, the antioxidant activities of these new derivatives were also researched employing various established systems, such as hydroxyl radical (•OH)/superoxide anion (O2 −)/DPPH scavenging and reducing power. Besides that, the cell toxicity of those derivatives was determined with MTT method. The results indicated that 3,6-DBZPTSCZLCS, 3,6-DBZ(p-NP)TSCZLCS, 3,6-DBZ(o-CP)TSCZHCS, and 3,6-DBZ(p-NP)TSCZHCS had the potential to be used as natural antioxidants because of their excellent activities in all these assays. O O O O NH2 C S NNH C NH C NNH C S NH 3,6-DBZPTSCZCS 3,6-DBZPTSCZHCS , Mw= 200 KDa ; 3,6-DBZPTSCZLCS , Mw= 3 KDa . n Ten new 3, 6-diacetylated phenyl-thiosemicarbazone-chitosans were synthesized and characterized. The antioxidant activities of the derivatives were investigated.
制备了10种不同分子量的C3, 6-二苯甲酰化硫代氨基脲壳聚糖衍生物。本研究的目的是进一步研究该系列衍生物的抗氧化活性及其结构与抗氧化行为的关系。为了了解其结构对衍生物抗氧化活性的影响,本文采用FT-IR光谱和元素分析对其结构进行了表征。此外,还研究了这些新衍生物的抗氧化活性,采用各种已建立的体系,如羟基自由基(•OH)/超氧阴离子(O2−)/DPPH的清除和还原能力。此外,用MTT法测定了这些衍生物的细胞毒性。结果表明,3,6- dbz (p-NP)TSCZLCS、3,6- dbz (o-CP)TSCZHCS和3,6- dbz (p-NP)TSCZHCS具有良好的抗氧化活性,具有作为天然抗氧化剂的潜力。O O O O O NH2 CS NNH C NNH C NNH CS NH 3,6- dbzptsczhcs 3,6- dbzptsczhcs, Mw= 200 KDa;3,6- dbzptsczlcs, Mw= 3kda。n合成了10个新的3,6 -二乙酰化苯基硫代氨基脲壳聚糖并进行了表征。研究了这些衍生物的抗氧化活性。
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引用次数: 4
Efficacy of Dobesilate in Allergic Rhinitis - Case Report 多贝酸酯治疗变应性鼻炎1例
Pub Date : 2015-11-02 DOI: 10.4172/2329-6631.1000139
P. Cuevas, M. Hinojosa, J. Angulo, G. Giménez-Gallego
Allergic rhinitis is a common condition that causes a negative effect on patient well-being. Antihistamines and glucocorticoids, the first line treatments usually administered for rhinitis, are normally associated to side effects. In addition, they may show limited efficiency in controlling nasal obstruction, edema and hyperemia occurring secondary to persistent inflammation. Dobesilate, an inhibitor of fibroblast growth factor and vascular endothelial growth factor, shows a markedly anti-inflammatory activity in several inflammation-dependent diseases and inflammation models. Our study shows that nostril spray application of dobesilate for one week is effective in reducing symptoms and signs in patients with seasonal allergic rhinitis.
过敏性鼻炎是一种常见的疾病,会对患者的健康产生负面影响。抗组胺药和糖皮质激素,通常是鼻炎的一线治疗方法,通常与副作用有关。此外,它们在控制继发于持续性炎症的鼻塞、水肿和充血方面的效果有限。多贝酸酯是一种成纤维细胞生长因子和血管内皮生长因子的抑制剂,在几种炎症依赖性疾病和炎症模型中显示出明显的抗炎活性。我们的研究表明,在季节性变应性鼻炎患者的鼻腔喷雾剂应用一个星期是有效的减轻症状和体征。
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引用次数: 2
ABCG2 Inhibitors: Will They Find Clinical Relevance? ABCG2抑制剂:它们会发现临床相关性吗?
Pub Date : 2015-10-18 DOI: 10.4172/2329-6631.1000138
Jerec Ricci, Debbie Lovato, R. Larson
Multiple drug resistance (MDR) is a prominent way by which cancer develops resistance to various chemotherapeutic agents and continues to be a hurdle in treating cancer patients. A few ATP binding cassette (ABC) transporters have been described as comprising the main mechanism behind MDR: ABCB1, ABCC1, and ABCG2. Of these three, ABCG2 is unique in that it seems to be mainly expressed in solid tumors. Despite the recent discovery of many compounds that inhibit its activity, it remains one of the least well-studied transporters in both animal models and in humans with regard to its contribution to MDR. Though the blockade of the ABCG2 efflux protein has great potential in reversing MDR in cancer, will it be enough to overcome chemoresistance in the clinic?
多重耐药(MDR)是癌症对各种化疗药物产生耐药性的重要途径,一直是癌症患者治疗的障碍。一些ATP结合盒(ABC)转运蛋白已被描述为构成MDR背后的主要机制:ABCB1, ABCC1和ABCG2。在这三者中,ABCG2的独特之处在于它似乎主要在实体肿瘤中表达。尽管最近发现了许多抑制其活性的化合物,但就其对耐多药的贡献而言,它仍然是动物模型和人类中研究最少的转运蛋白之一。虽然阻断ABCG2外排蛋白在逆转癌症耐多药方面具有很大的潜力,但在临床中是否足以克服化疗耐药?
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引用次数: 11
Evidence that Food Proteins in Vaccines Cause the Development of FoodAllergies and Its Implications for Vaccine Policy 疫苗中的食物蛋白导致食物过敏的证据及其对疫苗政策的影响
Pub Date : 2015-10-10 DOI: 10.4172/2329-6631.1000137
Vinu Arumugham
Nobel Laureate Charles Richet demonstrated over a hundred years ago that injecting a protein into animals or humans causes immune system sensitization to that protein. Subsequent exposure to the protein can result in allergic reactions or anaphylaxis. This fact has since been demonstrated over and over again in humans and animal models. The Institute of Medicine (IOM) confirmed that food proteins in vaccines cause food allergy, in its 2011 report on vaccine adverse events. The IOM’s confirmation is the latest and most authoritative since Dr. Richet’s discovery. Many vaccines and injections contain food proteins. Many studies since 1940 have demonstrated that food proteins in vaccines cause sensitization in humans. Allergens in vaccines are not fully disclosed. No safe dosage level for injected allergens has been established. As a result, allergen quantities in vaccines and injections are not regulated. Allergen quantities in vaccine excipients are also not regulated. It has been demonstrated that a smaller quantity of allergen is needed to cause sensitization than elicitation. It is well recognized that many currently approved vaccines have enough allergen to cause anaphylaxis. Therefore, they contain more than enough allergen to cause sensitization. Children today have fewer childhood infectious diseases. They have less exposure to helminths. C-section birth rates have increased in the last few decades by 50%. C-section births are known to result in sub-optimal gut micro biome in the newborn. All the above result in an immune imbalance biased towards atopy. Vaccine schedules today include 30-40 shots. Up to five shots may be simultaneously administered in one sitting. Vaccines contain adjuvants such as pertussis toxins and aluminum compounds that also bias towards allergy. Adjuvants also increase the immunogenicity of injected food proteins. This combination of atopic children and food protein injection along with adjuvants, contributes to millions developing lifethreatening food allergies. Given the scale and severity of the food allergy epidemic, urgent action is needed to change vaccine policy concerning vaccine specifications, manufacture, vaccine package insert documentation requirements, the Vaccine Adverse Event Reporting System (VAERS) and the National Vaccine Injury compensation program. Many researchers have called for the removal of food proteins from vaccines and re-evaluation of adjuvants such as aluminum compounds. In the interim, food allergy warnings can be included in vaccine package inserts. Simultaneous administration of multiple vaccines can be stopped to avoid the combined negative effects of multiple food proteins and adjuvants.
诺贝尔奖得主查尔斯·里歇(Charles Richet)在100多年前就证明,将一种蛋白质注射到动物或人类体内,会导致免疫系统对这种蛋白质产生过敏反应。随后暴露于这种蛋白质可导致过敏反应或过敏反应。这一事实已经在人类和动物模型中一次又一次地得到证实。医学研究所(IOM)在其2011年关于疫苗不良事件的报告中证实,疫苗中的食物蛋白质会导致食物过敏。国际医学研究所的确认是自里切特博士发现以来最新也是最权威的。许多疫苗和注射剂都含有食物蛋白质。自1940年以来的许多研究表明,疫苗中的食物蛋白质会导致人类致敏。疫苗中的过敏原并没有完全公开。注射过敏原的安全剂量尚未确定。因此,疫苗和注射剂中的过敏原数量不受管制。疫苗辅料中的过敏原数量也不受管制。已经证明,引起致敏所需的过敏原量比诱发量要少。众所周知,许多目前批准的疫苗含有足以引起过敏反应的过敏原。因此,它们含有足够多的过敏原导致致敏。今天的儿童患儿童传染病的人数减少了。他们很少接触到蠕虫。在过去的几十年里,剖腹产的出生率上升了50%。众所周知,剖腹产会导致新生儿的肠道微生物群不理想。所有这些导致免疫失衡偏向于特异反应。今天的疫苗接种计划包括30-40针。一次最多可同时注射五针。疫苗含有佐剂,如百日咳毒素和铝化合物,也倾向于过敏。佐剂也增加了注射食物蛋白质的免疫原性。这种特应性儿童和食物蛋白注射以及佐剂的结合,导致数百万人发生危及生命的食物过敏。鉴于食物过敏流行的规模和严重程度,需要采取紧急行动改变疫苗政策,包括疫苗规格、生产、疫苗包装说明书文件要求、疫苗不良事件报告系统(VAERS)和国家疫苗伤害赔偿计划。许多研究人员呼吁从疫苗中去除食物蛋白,并重新评估铝化合物等佐剂。在此期间,食物过敏警告可以包括在疫苗包装的说明书中。可以停止同时注射多种疫苗,以避免多种食物蛋白和佐剂的联合负面影响。
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引用次数: 11
Physical, Thermal and Spectral Properties of Biofield Treated 1,2,3-Trimethoxybenzene 生物场处理1,2,3-三甲氧基苯的物理、热及光谱特性
Pub Date : 2015-10-10 DOI: 10.4172/2329-6631.1000136
M. Trivedi, R. M. Tallapragada, A. Branton, Dahryn Trivedi, G. Nayak, R. Mishra, S. Jana
Study background: 1,2,3-Trimethoxybenzene is an important compound used for the synthesis of chemicals and pharmaceutical agents. The objective of this study was to investigate the influence of biofield energy treatment on the physical, thermal and spectral properties of 1,2,3-trimethoxybenzene. Methods: The study was performed by dividing the sample into two groups (control and treated). The control group remained as untreated, while the treated group received Mr Trivedi’s biofield energy treatment. The control and treated 1,2,3-trimethoxybenzene samples were then characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy, and ultra violetvisible spectroscopy (UV-Vis) analysis. Results: XRD studies revealed the significant increase in crystallite size of treated sample by 45.96% as compared to the control sample. DSC analysis showed a decrease in melting temperature of the treated sample (45.93oC) with respect to control (46.58oC). Additionally, the substantial change was evidenced in latent heat of fusion of treated sample by 64.18% as compared to the control. TGA analysis indicated a decrease in maximum thermal decomposition temperature (Tmax) of treated sample (151.92oC) as compared to the control sample (154.43oC). This indicated the decrease in thermal stability of the treated sample as compared to the control. FT-IR spectroscopic analysis showed an increase in the frequency of C-O bond in treated sample (1105→1174 cm-1) as compared to the control sample. However, UV analysis showed no changes in absorption peaks in treated sample as compared to the untreated sample. Conclusion: Overall, the result indicated that biofield energy treatment has altered the physical, thermal and spectral properties of the treated sample as compared to control. Hence, the treated sample could be used as an intermediate in the synthesis of organic compounds.
研究背景:1,2,3-三甲氧基苯是一种重要的化合物,用于合成化学品和药物制剂。研究了生物场能量处理对1,2,3-三甲氧基苯的物理、热及光谱性质的影响。方法:将样本分为两组(对照组和实验组)。对照组保持未治疗,而治疗组接受Trivedi先生的生物场能量治疗。采用x射线衍射(XRD)、差示扫描量热法(DSC)、热重分析(TGA)、傅里叶变换红外光谱(FT-IR)和紫外可见光谱(UV-Vis)对对照和处理后的1,2,3-三甲氧基苯样品进行了表征。结果:XRD研究表明,处理后样品的晶粒尺寸比对照样品增大了45.96%。DSC分析表明,处理后样品的熔化温度(45.93oC)较对照组(46.58oC)降低。此外,与对照组相比,处理后样品的融合潜热发生了64.18%的实质性变化。TGA分析表明,处理后样品的最高热分解温度(Tmax)为151.92oC,较对照样品(154.43oC)有所降低。这表明与对照相比,处理后样品的热稳定性有所下降。FT-IR光谱分析表明,与对照样品相比,处理后样品的C-O键频率(1105→1174 cm-1)增加。然而,紫外分析显示,与未处理的样品相比,处理后样品的吸收峰没有变化。结论:总的来说,结果表明,与对照相比,生物场能量处理改变了处理样品的物理、热和光谱性质。因此,处理后的样品可以用作有机化合物合成的中间体。
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引用次数: 6
It is Good to Be an Orphan 做个孤儿真好
Pub Date : 2015-09-29 DOI: 10.4172/2329-6631.1000e146
Rebecca Smith, R. Lodder
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引用次数: 0
Study on Blood Parameters of Tetrahydropyrimidine CarboxamideDerivatives on Breast Cancer 四氢嘧啶羧胺类衍生物对乳腺癌患者血液指标的影响
Pub Date : 2015-09-24 DOI: 10.4172/2329-6631.1000135
M. Jayanthi, P. Venkatesh, Sathiravada Veeraswamy Thirunavukkarasu
Pyrimidine is one of the most important heterocycles exhibiting remarkable pharmacological activities. Pyrimidine is a heterocyclic aromatic organic compound containing 1,2,3,4-Tetrahydropyrimidine carboxamide derivatives ring which shows wide range of biological activities. Numerous methods for the synthesis of pyrimidine and also their diverse reactions offer enormous scope in the field of medicinal chemistry. The potential antitumor activities of 1,2,3,4-Tetrahydropyrimidine carboxamide derivatives were prepared and used for the anti Cancer treatment. Inhibitory action of the tumor of this compound was shown significantly improved blood parameter includes hemoglobin (HB), RBC, platelets and WBC. In-vivo studies results showed substantial improved blood parameters in compared to untreated control rats. The newly synthesized compound exhibited significant effects on the treated animals as compared to DMBA induced animals.
嘧啶是一类重要的杂环化合物,具有显著的药理活性。嘧啶是一种含有1,2,3,4-四氢嘧啶羧胺衍生物环的杂环芳香族有机化合物,具有广泛的生物活性。嘧啶的合成方法众多,反应方式多样,为药物化学研究提供了广阔的空间。制备了具有潜在抗肿瘤活性的1,2,3,4-四氢嘧啶羧酰胺衍生物,并将其用于抗癌治疗。该化合物对肿瘤的抑制作用显示出明显改善血液参数,包括血红蛋白(HB)、红细胞、血小板和白细胞。体内研究结果显示,与未经治疗的对照大鼠相比,血液参数有了实质性改善。与DMBA诱导的动物相比,新合成的化合物对治疗动物有显著的影响。
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引用次数: 4
Why it is Important to Protect Intellectual Property and Data Confidentialityin Trade Agreements 为什么在贸易协定中保护知识产权和数据保密很重要
Pub Date : 2015-09-21 DOI: 10.4172/2329-6631.1000E145
R. Freeman
{"title":"Why it is Important to Protect Intellectual Property and Data Confidentialityin Trade Agreements","authors":"R. Freeman","doi":"10.4172/2329-6631.1000E145","DOIUrl":"https://doi.org/10.4172/2329-6631.1000E145","url":null,"abstract":"","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89559846","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
期刊
Journal of Developing Drugs
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