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Piperidine containing Murrayanine-Chalcones as Emerging Bactericidal and Fungicidal Agents 新出现的杀菌剂及杀菌剂——含摩拉亚胺-查尔酮哌啶
Pub Date : 2018-11-11 DOI: 10.15436/2377-1313.18.2008
Debarshi Kar Mahapatra, Ruchi S. Shivhare, Ajmal R. Bhat
Among the 20 other alkaloid molecules, murrayanine is the highest explored alkaloidal component present in the curry plant (Murraya koenigii L.). In the current research, a piperidine containing chalcone [(E)-1-(1-methoxy-9H-carbazol3-yl)-3-(4-(piperidin-1-yl)phenyl)prop-2-en-1-one] was rationally developed by incorporating the natural portion (murrayanine) in the A-ring and a synthetic component (1-(4-(piperidin-1-yl)phenyl)ethanone, a piperidine containing acetophenone) in the B-ring and screened against two bacterial species (Escherichia coli and Staphylococcus aureus) and two fungal species (Candida albicans and Aspergillus niger). The chalcone (1, 3-diphenyl-2E-propene-1-one) candidate expressed a better anti-bacterial activity than that of anti-fungal activity. The chalcone displayed the highest activity against E. coli followed by S. aureus, and lowest against C. albicans. Although, were found to have less activity and potency than that of the standard compounds (ciprofloxacin and fluconazole). The current study will open new avenues of research on hybrid heterocyclic chalcones and will motivate researchers to further developing highly active compounds based on benzylideneacetophenone scaffold.
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引用次数: 0
Evaluation of the Physicochemical and Thermal Properties of the Biofield Energy Healing Treated Ofloxacin 生物场能量愈合处理氧氟沙星的理化热性能评价
Pub Date : 2018-10-05 DOI: 10.15436/2377-1313.18.1965
A. Branton, M. Trivedi, Dahryn Trivedi, G. Nayak, S. Jana
Ofloxacin is a broad-spectrum antibiotic useful for the treatment of many Gram-positive and Gram-negative bacterial infections. The objective of this research work was to evaluate the impact of the Trivedi Effect® on the physicochemical and thermal properties of ofloxacin using modern analytical techniques. The sample was divided into two parts. One part of ofloxacin was considered as the control sample (no biofield energy treatment was provided), whereas the second part was received the Biofield Treatment remotely by a famous Biofield Energy Healer, Alice Branton and was termed as the treated sample. The PXRD peak intensities and crystallite sizes were significantly altered ranging from 7.45% to 73.06% and -44.1% to 77.95%, respectively in the treated sample compared to the control sample. The particle size values were significantly altered at d10 (-19.47%), d50 (1.14%), d90 (-8.70%), and D (4, 3) (-10.20%); whereas, the specific surface area was significantly increased by 15.66% in the treated sample compared to the control sample. The latent heat of fusion and latent heat of decomposition of the treated ofloxacin were significantly increased by 16.24% and 88.03%, respectively compared with the control sample. The total weight loss was significantly decreased by 6.21 %; additionally, the residue amount was significantly increased by 47.16% in the treated ofloxacin compared with the control sample. Thus, the Trivedi Effect® might generate a new polymorphic form of ofloxacin which would be more soluble, bioavailable, and be thermally more stable compared with the untreated sample. The Biofield Treated ofloxacin would be more efficacious against urinary tract infections, infections of the urethra and cervix, infectious diarrhoea, pneumonia, cellulitis, chronic bronchitis, prostatitis, plague, etc.
氧氟沙星是一种广谱抗生素,可用于治疗许多革兰氏阳性和革兰氏阴性细菌感染。本研究的目的是利用现代分析技术评估Trivedi效应®对氧氟沙星理化和热性能的影响。样品分为两部分。其中一部分氧氟沙星作为对照样本(未进行生物场能量处理),另一部分氧氟沙星由著名生物场能量治疗师Alice Branton远程接受生物场治疗,称为处理样本。与对照样品相比,处理后样品的PXRD峰强度和晶粒尺寸分别发生了7.45% ~ 73.06%和-44.1% ~ 77.95%的显著变化。d10(-19.47%)、d50(1.14%)、d90(-8.70%)和D(4,3)(-10.20%)的粒径值变化显著;而处理后的样品比表面积较对照样品显著提高了15.66%。处理后的氧氟沙星溶合潜热和分解潜热较对照分别显著提高16.24%和88.03%。总减重显著降低6.21%;处理后的氧氟沙星的残留量较对照提高了47.16%。因此,Trivedi效应®可能产生一种新的多形性氧氟沙星,与未经处理的样品相比,这种多形性氧氟沙星更具可溶性、生物利用度和热稳定性。经生物场治疗的氧氟沙星对尿路感染、尿道和宫颈感染、感染性腹泻、肺炎、蜂窝组织炎、慢性支气管炎、前列腺炎、鼠疫等更有效。
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引用次数: 9
Some Aspects of Medicine Distribution in Sudan 苏丹药品分配的一些方面
Pub Date : 2018-09-10 DOI: 10.15436/2377-1313.18.1953
Abdeen Mustafa Omer
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引用次数: 0
Nanorobots a future Device for Diagnosis and Treatment 纳米机器人是未来的诊断和治疗设备
Pub Date : 2018-08-05 DOI: 10.15436/2377-1313.18.1815
Sarath Kumar S
This article focusses on the application of the nanorobots in diagnosis and treatment of some of the diseases like cancer, heart diseases, diabetes, gout etc. Nanorobots are controllable machines at the nanometer or molecular scale that are composed of nano scale components. With the modern scientific capabilities, it has become possible to attempt the creation of nanorobotic devices and interface them with the macro world for control. These devices are also a helpful tool in the drug delivery, which is a very important aspect of medical treatment. Nanorobots are capable of performing task like actuating, sensing, signalling, information processing and intelligence at the nanoscale. The most recent application of these devices are, the brain targeted delivery of drugs, glucose monitoring in diabetes patients, bone reconstruction, cancer treatment, removal of blood clots, nerve regeneration and protein and peptide drug delivery system. Thus they play a vital role in the field of biomedicine especially in the treatment of cancer, cerebral aneurysm, kidney stones removal and some other treatments that have greatest aid to save human lives. This review guides to the recent research on nanorobots in the bio medical applications.
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引用次数: 2
Evaluation of arterial-venous blood alcohol concentration gradients of ethanol administered by an infusion to dogs 犬注射乙醇后动静脉血酒精浓度梯度的评价
Pub Date : 2018-08-03 DOI: 10.15436/2377-1313.18.1549
M. Ďurišová, Ommega Internationals
Numerous workers investigated ethanol pharmacokinetic. Therefore, the goal of the present study was not an investigation of ethanol pharmacokinetics; instead, the goal of the present study was to prepare further illustrative examples of a successful use of computational and modeling tools from system engineering in pharmacokinetic investigations. The previous study by Wilkinson and Rheingold published in October 1977 issue of the Journal of Pharmacokinetics, described an investigation of arterial-venous blood concentration gradients of ethanol administration by a constant rate intravenous infusion through indwelling venous catheters to dogs. The present study is a free continuation of the study by Wilkinson and Rheingold; therefore, the data available in the study by Wilkinson and Rheingold were used. An advanced modeling method, implemented in the computer program named CTDB, and described in the study by Dedik et al[1] was used for modeling purposes.
许多工作者研究了乙醇的药代动力学。因此,本研究的目的不是研究乙醇的药代动力学;相反,本研究的目的是准备进一步的说明性例子,说明在药代动力学研究中成功地使用了系统工程中的计算和建模工具。Wilkinson和Rheingold先前的研究发表在1977年10月的《药代动力学杂志》(Journal of Pharmacokinetics)上,描述了通过留置静脉导管等速静脉输注乙醇给狗的动静脉血浓度梯度的研究。本研究是Wilkinson和Rheingold研究的自由延续;因此,我们使用了Wilkinson和Rheingold的研究数据。采用了一种先进的建模方法,该方法在计算机程序CTDB中实现,并在Dedik等[1]的研究中描述。
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引用次数: 0
Entecavir patent evaluation, method for diastereomeric Impurities 恩替卡韦专利评价,非对映异构体杂质的方法
Pub Date : 2018-07-16 DOI: 10.15436/2377-1313.18.1899
krishna sarma Pathy
Entecavir is an oral antiviral drug used in the treatment of hepatitis B infection. Entecavir is a guanosine nucleoside analogue with selective activity against hepatitis B virus (HBV), which inhibits reverse transcription, Hepatitis B virus (HBV) is highly endemic in South Africa and across sub-Saharan Africa, where around 8% of people are chronically infected, and rates of HBV-related liver cancer are some of the highest in the world. Globally, viral hepatitis causes approximately 1.3 million deaths every year more than either malaria or tuberculosis with around 240 million people chronically infected with HBV1. The currently available anti-HBV drugs show potent antiviral activity in patients with chronic hepatitis B; however, the resistance and cross-resistance to the drugs is a major obstacle in long-term treatment. Many studies have been conducted to understand the molecular basis of drug resistance, and the mechanistic characterization and molecular modeling of anti-HBV drugs complexed with HBV RT have been reported. Although the three-dimensional X-ray structure of HBV polymerase is not available, its homology model has been reported using the X-ray structure of HIV RT as a template[1-13]. Even though the homology models may not be accurate due to the low sequence homology between the overall HIV and HBV polymerase, the sequence conservation between the RT domains of HIV and HBV polymerase enables molecular modeling of HBV RT[14]. In particular, the residues around the active site that are responsible for recognizing the template-primer or an incoming nucleoside triphosphate are highly conserved. Nucleoside analogue HBV polymerase inhibitors cause chain termination after incorporation into the growing chain in the active site of HBV polymerase and consequently inhibit viral reverse transcriptase. Thus, the HBV homology model structure based on the crystal structure of HIV polymerase serves as a useful guide for understanding the molecular basis of HBV resistance to drugs.. Department of Chemistry, IPL research center, Lucknow, India *Corresponding author: KrishnaSarmaPathy, Department of Chemistry, IPL research center, Lucknow, India, Email: drkrishnasarmapathy@yahoo.in Citation: Krishna, S .P. Process and Molecular Modelling Study of Entecavir Drug-Resistant HBV. (2018) J Pharm Pharmaceutics 5(1): 3139. Received date: May 21 2018 Accepted date: July 09 2018 Publish date: July 16 2018 Introduction The initial patent on entecavir expired in South Africa in 2011 ZA 1991/07894. Current status available on: http://patentsearch.cipc.co.za/, which should have permitted lower-cost generic competitors to enter the market. However, South Africa granted BMS three additional patents on entecavir that only expire between 2022 and 2026. Two of these patents have lapsed meaning BMS has not paid the renewal fees, and they cannot be enforced while one patent covering a lower dosage form of entecavir remains in force. This patent is currently under litigat
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引用次数: 1
Counterfeit Drugs Set Alarm Bells Ringing: Comparative Analysis of Drug Policies 假药敲响警钟:药物政策的比较分析
Pub Date : 2018-06-23 DOI: 10.15436/2377-1313.18.1907
Abdeen Mustafa Omer
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引用次数: 4
In Vitro Antibacterial Activity and Phytochemical Screening of Garcinia Kola Extracts Against Methicillin Resistant Staphylococcus Aureus (MRSA) Garcinia Kola提取物对耐甲氧西林金黄色葡萄球菌(MRSA)的体外抗菌活性及植物化学筛选
Pub Date : 2018-06-01 DOI: 10.15436/2377-1313.18.1884
Muhammad Asghar Ali, A. U. Zage, I. Ahmed, L. Fagwalawa, Ommega Internationals
Modern medicines have always depended on herbal extracts from plants as fundamental source of therapeutic ingredients. The aim of the study was to determine the phytochemical constituents and antibacterial activity of Garcinia kola seed extracts against clinical isolates of Methicillin Resistant Staphylococcus Aureus (MRSA). Total of 107 Staphylococcus isolates from infected wound and urine and were collected from Abubakar Imam Urology Center in Kano State, Nigeria over a period of eight months (October 2015 to May 2016). A disc diffusion method was used for characterization of MRSA. The phytochemical screening of the plant materials was done using conventional laboratory method while the antibacterial activity of the plant extracts was determined using agar well diffusion method. The result of bacterial characterization showed that eight isolates found were to be Methicillin Resistant Staphylococcus aureus (MRSA). Phytochemical screening of the seeds, leaves and stem bark extracts indicated the presence of Alkaloid, Tannin, Saponin, and Cardiac glycoside, Flavonoid, Terpenoid, Phenols Anthraquinone and Steroid. However, reducing sugar is absent. The antibacterial activity of the plant showed that the plant part extracts demonstrated antimicrobial effect against the test isolates with higher activity in seeds compared to leaves and stem. Statistical analysis of the result revealed that the overall average zone of inhibition shown by the extracts is 11.68 mm with methanolic seeds extract exerting the highest antibacterial effects on the test isolates with average zone of inhibition of 12.78 mm, followed by methanolic leaf extract 12.37 mm then aqueous seed extract with zone of inhibition of 11.87 mm. Least zones of inhibition were recorded in aqueous leaf extract and methanolic stem back extract with zones of inhibition of 11.28 and 10.43 mm respectively. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of the extracts range from 12.5 – 100 mg/ml of the extracts. Findings from this work support the use of seed extracts from G. kola as medicinal plant.
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引用次数: 3
Structural-Parametric Model of Electroelastic Actuator for Nanotechnology and Biotechnology 纳米技术与生物技术电弹性致动器的结构参数模型
Pub Date : 2018-05-28 DOI: 10.15436/2377-1313.18.1881
Afonin Sm, Ommega Internationals
The generalized parametric structural schematic diagram, the generalized matrix equation for the electro elastic actuator for the nanotechnology and the biotechnology are obtained. The deformations of the electro elastic actuator are described by the matrix equation. The structural-parametric model and the parametric structural sсhematic diagram of the electro elastic actuator or the piezoactuator are determined in contrast the electrical equivalent circuit types Cady or Mason for the calculation of the piezoelectric transmitter and receiver, the vibration piezomotor with the mechanical parameters in form the velocity and the pressure. The parametric structural schematic diagram of electro elastic actuator is obtained with the mechanical parameters the displacement and the force. The transfer functions of the electro elastic actuator are determined. The method of mathematical physics is used.
得到了纳米技术和生物技术电弹性作动器的广义参数结构原理图和广义矩阵方程。电弹性作动器的变形用矩阵方程来描述。对比电弹性作动器和压电作动器的等效电路类型Cady和Mason,建立了电弹性作动器的结构参数模型和参数结构原理图,计算了压电式收发器和振动式压电马达的速度和压力等机械参数。得到了电弹性作动器的力学参数、位移和力的参数化结构原理图。确定了电弹性作动器的传递函数。运用了数学物理的方法。
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引用次数: 18
The Obstacles to Current Extracellular Vesicle-Mediated Drug Delivery Research. 当前细胞外囊泡介导的药物递送研究的障碍。
Pub Date : 2017-01-01 Epub Date: 2017-10-27 DOI: 10.15436/2377-1313.17.1331
Heedoo Lee, Duo Zhang, Ashish Rai, Yang Jin

Extracellular Vesicles (EVs) are nanometer-sized cell-derived membrane vesicles that are released by donor cells and play an important role in intercellular communication. In this short communication, we discuss the obstacles currently faced in EV-mediated drug delivery research. The commonly used vehicle for drug delivery in prevalent practice are liposome's which are synthetic vesicles, these vesicles commonly interact with serum proteins, macrophages and other innate immune response molecules and may be destroyed before they can deliver the drug. EVs however have the same membrane compositions and similar cell surface markers as the cells from which they are derived which thus prevents interactions or provocations of an immune response. In addition, EVs have been used to deliver molecules across tight cellular junctions such as the blood brain barrier. This has led to an interest in using EVs as a novel method for drug delivery. We hereby discuss the potential pitfalls and difficulties that need to be addressed before EVs can be used as drug delivery vehicles in pharmacological research.

细胞外囊泡(Extracellular Vesicles, EVs)是由供细胞释放的纳米级细胞源性膜囊泡,在细胞间通讯中起重要作用。在这篇简短的文章中,我们讨论了目前在ev介导的药物递送研究中面临的障碍。目前普遍使用的药物递送载体是脂质体,脂质体是一种合成囊泡,这些囊泡通常与血清蛋白、巨噬细胞和其他先天免疫反应分子相互作用,可能在它们递送药物之前就被破坏了。然而,电动汽车具有与衍生它们的细胞相同的膜组成和相似的细胞表面标记,从而防止相互作用或引发免疫反应。此外,电动汽车已被用于传递分子通过紧密的细胞连接,如血脑屏障。这引起了人们对使用电动汽车作为一种新的药物输送方法的兴趣。在此,我们讨论了电动汽车在药理学研究中用作药物传递载体之前需要解决的潜在缺陷和困难。
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引用次数: 6
期刊
Journal of pharmacy and pharmaceutics
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