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Cephalosporins: pharmacology and chemistry 头孢菌素:药理学和化学
Pub Date : 2017-12-03 DOI: 10.26510/2394-0859.PBE.2017.36
K. Shahbaz
Cephalosporins are the most important antibiotics having β-lactam ring and are obtained from a fungus Acremonium, also known as cephalosporium. The wide use of cephalosporins against bacteria in various severe infections such as respiratory tract infection (RTI), skin infection and urinary tract infection (UTI) has led the scientist dive into the detail of this antibacterial drug. The knowledge about structural activity relationship (SAR), spectrum of inhibition (SOI), chemical properties and pharmacology of cephalosporin has pivotal impact to device advanced therapeutic results. The treatment of a disease using cephalosporin has many pros and cons. If the pharmacology and chemical properties of this drug are known properly, many side effects can be diminished or minimized to a certain level. This article review some pharmacological and chemical properties of cephalosporins.
头孢菌素是最重要的具有β-内酰胺环的抗生素,从一种真菌Acremonium中提取,也称为头孢菌。头孢菌素广泛用于对抗各种严重感染的细菌,如呼吸道感染(RTI)、皮肤感染和尿路感染(UTI),这使得科学家们深入研究了这种抗菌药物的细节。了解头孢菌素的构效关系(SAR)、抑制谱(SOI)、化学性质和药理学对设备的先进治疗效果具有关键影响。使用头孢菌素治疗疾病有许多优点和缺点。如果正确了解这种药物的药理学和化学性质,许多副作用可以减少或最小化到一定程度。本文综述了头孢菌素的一些药理和化学性质。
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引用次数: 14
Green synthesis of silver nanoparticles from Morinda tinctoria Roxb and scrutiny of its multi facet on biomedical applications 巴戟达纳米银的绿色合成及其在生物医学上的应用
Pub Date : 2017-10-02 DOI: 10.26510/2394-0859.PBE.2017.35
G. Paramasivam, R. Kannan, S. Paulraj, J. Pandiarajan
Objective : This research work focus on synthesis of silver nanoparticles from Morinda tinctoria Roxb leaves. The synthesis of nanoparticles from biological processes is evolving a new era of research interests in nanotechnology. Silver nanoparticles are usually synthesized by chemicals. M. tinctoria Roxb leaves are reputed plant in traditional system of medicine and it is used for the treatment of illness such as arthritis, cancer, gastric ulcer and other heart disease etc. Methods : The present study the leaves were collected, air dried and extract silver nanoparticles. The extract was subjected to characterization, antimicrobial activity, antidiabetic and anticancer activity using M. tinctoria Roxb leaves following standard procedures. Results : Silver nanoparticles study showed the evaluation of antioxidant and anticancer activity of M. tinctoria Roxb. Antioxidant activities were done using DPPH antioxidant assay and hydrogen peroxide assay. The anticancer study was conducted to evaluate the in-vitro anticancer activity of green synthesized nanoparticles using human hepatic carcinoma cell lines (HepG2). Conclusions : The leaf extract of silver nanoparticle evaluation showed higher antioxidant activity and anticancer activity in M. tinctoria Roxb.
目的:研究从巴戟天叶中合成纳米银的工艺。从生物过程合成纳米粒子是纳米技术研究的一个新领域。银纳米颗粒通常是由化学物质合成的。黄芪叶是传统医学中享有盛誉的植物,用于治疗关节炎、癌症、胃溃疡和其他心脏病等疾病。方法:采用风干法提取银纳米粒子。采用标准方法,对提取液进行表征、抑菌活性、抗糖尿病活性和抗癌活性研究。结果:银纳米颗粒研究表明,银纳米颗粒具有抗氧化和抗癌活性。采用DPPH抗氧化法和过氧化氢法测定其抗氧化活性。以人肝癌细胞株HepG2为实验对象,研究了绿色合成纳米颗粒的体外抗癌活性。结论:银纳米颗粒叶提取物具有较高的抗氧化活性和抗癌活性。
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引用次数: 5
Synthesis, characterization and biological evaluation of Schiff’s bases derivatives as potent antibacterial agents 席夫碱衍生物高效抗菌的合成、表征及生物学评价
Pub Date : 2017-10-02 DOI: 10.26510/2394-0859.pbe.2017.34
V. Parcha, Ankith Kumar, B. Mahajan, J. Kaur
Objective : To design, synthesize and screen biologically newer Substituted Schiff bases by condensing substituted acid hydrazides with various benzaldehydes and explore their antimicrobial potential. Methods : Present study synthesis of various derivatives of Schiffs bases was carried out by: firstly converting substituted acids to acid hydrazides and then to Schiff's bases after condensation with substituted benzaldehyde. Synthesized compounds were characterised on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect against Salmonella typhimurium, Shigella sonnei, Staphylococcus aureus& Bacillus cereus. Results : From this study it could be observed that schiff’s bases 2-[( aminophenylhydrazinyldene o,m,dinitrobenzoyl] aniline (H) and compound 2-[( aminophenylzinyldene) p amino benzoyl] aniline (I) showed very good zone of inhibition against almost all strains tested for. Conclusions : So further attempts could be made to extend the series and explore their antibacterial potential to achieve hopeful goal.
目的:通过与各种苯甲醛缩合取代酸肼设计、合成和筛选生物学上较新的取代希夫碱,并探索其抗菌潜力。方法:本研究采用先将取代酸转化为酸酰肼,再与取代苯甲醛缩合为席夫碱的方法合成各种席夫碱衍生物。合成的化合物在光谱研究(如紫外、红外和核磁共振)的基础上进行了表征。进一步筛选合成的衍生物对鼠伤寒沙门菌、索尼氏志贺氏菌、金黄色葡萄球菌和蜡样芽孢杆菌的抑菌效果。结果:希夫碱2-[(氨基苯基肼基)o,m,二硝基苯甲酰]苯胺(H)和化合物2-[(氨基苯基肼基)对氨基苯甲酰]苯胺(I)对几乎所有被试菌株都有很好的抑制区。结论:可以进一步尝试扩展该系列,探索其抗菌潜力,以达到预期的目的。
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引用次数: 2
Assessment of bacterial contamination of toilets and bathroom doors handle/knobs at Daeyang Luke hospital 大阳路医院厕所和浴室门把手的细菌污染评估
Pub Date : 2017-08-01 DOI: 10.26510/2394-0859.PBE.2017.31
Frank Ngonda
Objective : The aim of the study was to determine the level of bacterial contamination of door handles/knobs of toilets and bathrooms at Daeyang Luke Hospital. Methods : Fomite can be described as a non-living object capable of carrying infectious organism and it is considered as one of the major source of spread of hospital acquired infection. In this study, door handles/knobs were swabbed with sterile swab stick moistened with sterile water. The content was evenly transferred to nutrient agar petric dish and then incubated for 24 hours at 37˚C. The study was done between the months of May to August 2016. Results : The results of the study showed that during the period of study there was 41.6% bacterial contamination with the female medical and surgical ward toilets being more contaminated as compared to staff toilets. Private room bathrooms were more contaminated during the period of study as compared to the staff room bathrooms that were less contaminated. Among the bacterial contaminant isolated and identified, Staphylococcus aureus had the highest prevalence followed by Escherichia coli , Pseudomonas aeruginosa , Citrobacter species and Klebsiella pneumoniae respectively. Conclusions : Therefore, from the study, it can be concluded that general public needs observe hand hygiene and use of quality disinfection procedures in order to reduce hospital acquired infection.
目的:本研究的目的是确定大阳路医院厕所和浴室门把手/把手的细菌污染水平。方法:螨虫是一种能够携带感染性微生物的无生命物体,是医院获得性感染的主要传染源之一。在本研究中,门把手/把手用无菌棉签蘸无菌水擦拭。将内容物均匀转移到营养琼脂培养皿中,在37℃条件下孵育24小时。这项研究是在2016年5月至8月期间进行的。结果:调查期间细菌污染率为41.6%,内科、外科女病区厕所污染程度高于工作人员厕所。在研究期间,与污染较少的员工浴室相比,私人浴室的污染更严重。在分离鉴定的细菌污染物中,金黄色葡萄球菌的患病率最高,其次是大肠杆菌、铜绿假单胞菌、柠檬酸杆菌和肺炎克雷伯菌。结论:从本研究中可以得出结论,一般公众需要遵守手卫生和使用优质消毒程序,以减少医院获得性感染。
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引用次数: 17
Melanin relieves oxidative stress in adipocytes culture in vitro 黑色素对体外脂肪细胞氧化应激的缓解作用
Pub Date : 2017-08-01 DOI: 10.26510/2394-0859.pbe.2017.33
M. Jarrar, A. E. Shafey, Rabia Essa, Ruksar Damji, A. Rauf, Ielaf Hindi
Obesity is one of major health disorders that has become epidemic worldwide. Studies have demonstrated that oxidative stress and inflammation in adipose tissue is involved in obesity linked complications. The ectopic synthesis of melanin in adipocytes of obese patients has been newly discovered. It is hypothesized that there is potential role of melanin and its intermediates to ameliorate oxidative stress in adipose which may prevent the secondary complications to obesity.  This study was done to determine whether melanin interferes with the level of oxidative stress produced in adipocyte cells in culture. Adipocyte cells were cultured in vitro and exposed to high concentration of glucose oxidase to induce oxidative stress, then cells were treated with melanin for different periods. Thereafter the levels of some oxidative stress and inflammatory biomarkers such as glutathione, TNF-alpha, Malondialdehyde (MDA), and protein carbonyl were measured. It was found that when cells were exposed to glucose oxidase the level of oxidative stress increased over time as reflected by the decrease of Glutathione.  Interestingly, when melanin was added the level of oxidative stress decreased over time as reflected by increase in glutathione concentrations. It was also found that TNF-alpha decreased upon treatment by melanin but after 72 hours but not on 24 and 48 hours treatments. However, protein carbonyl and MDA appeared to be less affected by melanin treatments. These results may indicate that melanin is capable of diminishing the effects of oxidative stress on the cells at early stages probably by interfering with lipids peroxidation and production of reactive oxygen species.
肥胖是一种主要的健康疾病,已成为世界性的流行病。研究表明,脂肪组织中的氧化应激和炎症与肥胖相关的并发症有关。肥胖患者脂肪细胞中黑色素异位合成已被新发现。我们推测黑色素及其中间体可能具有改善脂肪氧化应激的潜在作用,从而预防肥胖的继发性并发症。这项研究是为了确定黑色素是否会干扰培养脂肪细胞中产生的氧化应激水平。体外培养脂肪细胞,高浓度葡萄糖氧化酶诱导氧化应激,然后不同时期用黑色素处理。然后测量一些氧化应激和炎症生物标志物的水平,如谷胱甘肽、tnf - α、丙二醛(MDA)和蛋白质羰基。研究发现,当细胞暴露于葡萄糖氧化酶时,氧化应激水平随着时间的推移而增加,这反映在谷胱甘肽的减少上。有趣的是,当加入黑色素时,氧化应激水平随着时间的推移而下降,这反映在谷胱甘肽浓度的增加上。还发现tnf - α在黑色素治疗72小时后下降,但在24小时和48小时后没有下降。然而,蛋白质羰基和MDA似乎受黑色素治疗的影响较小。这些结果可能表明黑色素能够在早期阶段减少氧化应激对细胞的影响,可能是通过干扰脂质过氧化和活性氧的产生。
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引用次数: 1
Aldose reductase and advanced glycation end products formation inhibitory activity of standardized extracts of Picrorhiza kurroa (Royle ex benth) and Hibiscus rosa-sinensis (Linn.) 苦参和芙蓉标准化提取物醛糖还原酶和晚期糖基化终产物形成抑制活性的研究
Pub Date : 2017-08-01 DOI: 10.26510/2394-0859.pbe.2017.28
A. Santhosh, C. Veeresham, A. R. Rao
Objective: The objectives were to study the in-vitro and in-vivo aldose reductase and in-vitro advanced glycation end products formation inhibitory activities of the standardized extracts of Picrorhiza kurroa roots and Hibiscus rosa-sinensis flowers. Methods: In-vitro Aldose reductase inhibitory activity was studied by using isolated rat lens and kidney Aldose reductase by UV-Visible spectro photo metric method by using Quercetin as reference compound. In-vivo Aldose reductase inhibitory activity was evaluated by using experimental rat models of galactosemia and the final lens galactitol was evaluated by High performance liquid chromatography and Gas chromatography methods by using Quercetin as reference compound. In-vitro advanced glycation end products formation inhibitory activity was estimated by using laboratory test reaction with protein and sugars by spectro fluorimetric method by sung aminoguanidine as reference compound. Statistical analysis of the results was done by using Analysis of the variance method. Results: The plant extracts were found to possess significant aldose reductase and advanced glycation end products formation inhibitory activity. Conclusions: More study is required for isolation and characterization of the chief chemical constituents responsible for the biological activity of the plant extracts.
目的:研究芍药根和芙蓉花标准提取物体外和体内醛糖还原酶活性及体外晚期糖基化终产物形成抑制活性。方法:以槲皮素为对照物,采用紫外可见分光光度法,以离体大鼠晶状体和肾脏醛糖还原酶为对照物,研究醛糖还原酶的体外抑制活性。采用实验性半乳糖血症大鼠模型评价其体内醛糖还原酶抑制活性,以槲皮素为参比化合物,采用高效液相色谱法和气相色谱法评价最终晶状体半乳糖醇。以sung氨基胍为参比化合物,采用荧光光谱法与蛋白质和糖进行实验反应,评估了体外晚期糖基化终产物形成的抑制活性。采用方差分析法对结果进行统计分析。结果:该植物提取物具有显著的醛糖还原酶和晚期糖基化终产物形成抑制活性。结论:对该植物提取物生物活性的主要化学成分的分离和鉴定有待进一步研究。
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引用次数: 2
Phytochemical screening and in vivo antipyretic activity of the aqueous extracts of three Moroccan medicinal plants 三种摩洛哥药用植物水提物的植物化学筛选及体内解热活性
Pub Date : 2017-08-01 DOI: 10.26510/2394-0859.PBE.2017.30
Ghizlane Hajjaj, A. Bahlouli, K. Sayah, M. Tajani, Y. Cherrah, A. Zellou
Objective : In this study, the antipyretic effect of different extracts obtained from Matricaria chamomilla L. (MC), Ormenis mixta L. (OM) and Pistacia atlantica DESF. (PA) was investigated experimentally in rats. Methods : Antipyretic activity of aqueous extracts was evaluated by yeast induced pyrexia method. The antipyretic effect was retained in all extracts tested and was comparable to that of paracetamol used as the standard drug negative control group (distilled water). The extracts were also phytochemically screened for alkaloids, tannins, saponins, flavonoids, terpenoids, quinones and anthraquinones. Results : Treatment with aqueous extracts at dose of 400 mg/kg showed a significant (p≤0.05) reaction of pyrexia in rodents. The results suggest that this Moroccan medicinal plants possesses potent antipyretic activity. Phytochemical screening of the plants showed the presence of flavonoids, terpenoids, saponins, tannins, alkaloids and quinons which may responsible for this activity. However, anthraquinones were absent in all plants and alkaloids from PA. Conclusions : This study might be the first formal report on antipyretic effects of these three plants in Morocco.
目的:研究洋甘菊(MC)、酢浆草(OM)和黄连木(DESF)不同提取物的解热作用。(PA)在大鼠体内进行实验研究。方法:采用酵母解热法测定水提物的解热活性。所有测试提取物的解热作用都保持不变,并且与作为标准药物阴性对照组(蒸馏水)的扑热息痛相当。对提取液进行了生物碱、单宁、皂苷、黄酮类、萜类、醌类和蒽醌类的植物化学筛选。结果:400 mg/kg水提液处理小鼠发热反应显著(p≤0.05)。结果表明,这种摩洛哥药用植物具有很强的解热作用。植物化学筛选表明,黄酮类、萜类、皂苷类、单宁类、生物碱类和醌类物质可能与该活性有关。而蒽醌类化合物在所有植物和生物碱中均不存在。结论:本研究可能是摩洛哥首次正式报道这三种植物的解热作用。
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引用次数: 6
Study on the prescribing pattern of anti-diabetic drugs in community clinic in Uttar Pradesh state 北方邦社区诊所抗糖尿病药物处方模式研究
Pub Date : 2017-08-01 DOI: 10.26510/2394-0859.PBE.2017.32
S. Chandra, M. Khan, A. Mohan
Objective: The diabetes mellitus is most common diseases. Which are spread all over the world. At they  are change in modified in life style disease  in this study where the prescribe drugs while using in the diagnostic and treatment of diabetes mellitus .the most commonly use drugs Sitagliptin +Metfomin in the community clinic in U.P. In the survey which are found to be the prescription pattern in Jajmau (Kanpur, U.P.) areas the most common drug which are running Sitagliptin + Metformin the survey which are randomly collect the prescription there are many variation in prescribing pattern of diabetes mellitus .the prescribing pattern is most strong tools to role of drug use in the society which are treat the DM during medication follow the proscription pattern of the drugs. There is need for appropriate safe &effective treatment and economical study to find out the pattern of drug therapy among DM. Methods: In this study the method randomized and non randomized study design was conducted in October 2016 – November 2016 community clinic in U.P. this study found to the date which group gender in fasting blood sugar various classes of drugs analyzed them. Results: A total of 200 patients were included in this one month’s study. All the patients had Type 2 diabetes. Metformin is the drug of choice and Sitagliptin is the most preferred combination with Metformin. Conclusions: Insulin was not preferred as mono-therapy. Despite combination therapy, the postprandial glucose levels were not in range–suggesting either poor patient compliance or inadequate dosing/inappropriate therapy. In addition to drugs, the services of a clinical pharmacist might be helpful in these patients. Metformin is the drug of choice and Sitagliptin is the most preferred combination with Metformin.
目的:糖尿病是最常见的疾病。它们遍布世界各地。在本研究中,在糖尿病的诊断和治疗中使用的处方药物中,最常用的药物是西格列汀+二甲双胍,在北方邦的社区诊所中,在调查中发现,这是贾吉茂(坎普尔)的处方模式。(p)地区最常见的药物是西格列汀+二甲双胍,该调查是随机收集的处方,糖尿病的处方模式有很多变化,处方模式是社会上药物使用的最有力的工具,在治疗糖尿病期间遵循药物的禁止模式。方法:本研究采用随机和非随机研究设计的方法,于2016年10月- 2016年11月在upp社区诊所进行研究,研究发现到目前为止该组性别在空腹血糖中各类别药物的使用情况。结果:在为期一个月的研究中,共纳入200例患者。所有患者都患有2型糖尿病。二甲双胍是首选药物,西格列汀是最优选的二甲双胍联合用药。结论:胰岛素不适合作为单药治疗。尽管联合治疗,餐后血糖水平不在范围内-提示患者依从性差或剂量不足/治疗不当。除了药物,临床药师的服务可能对这些病人有帮助。二甲双胍是首选药物,西格列汀是最优选的二甲双胍联合用药。
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引用次数: 0
MUCOADHESIVE DRUG DELIVERY SYSTEM: A REVIEW 黏附给药系统研究进展
Pub Date : 2017-08-01 DOI: 10.26510/2394-0859.PBE.2017.29
P. Pandey, M. Saini, Neeta
The major objective of any dosage form is to deliver an optimum therapeutic amount of active agent to the proper site in the body to attain constant & maintenance of the desired drug concentration. Mucoadhesive drug delivery systems are effective delivery systems with various advantages as compared to other oral controlled release dosage forms in terms of drug delivery at specific sites with prolonged retention time of drugs at target sites. The main advantage of these systems includes avoiding first pass metabolism of the drugs and hence availability of high drug concentration at target site. Oral mucoadhesive systems have potential ability for controlled and extended release profile so as to get better performance and patient compliance. The present manuscript briefly reviews the benefits of mucoadhesive drug delivery systems, mechanisms involved in mucoadhesion, different factors affecting mucoadhesive drug delivery systems.
任何剂型的主要目标都是将最佳治疗量的活性剂输送到体内适当的部位,以达到和维持所需的药物浓度。黏附给药系统是一种有效的给药系统,与其他口服控释剂型相比,在特定部位给药,延长药物在靶部位的滞留时间方面具有各种优点。这些系统的主要优点包括避免药物的第一次代谢,从而在靶部位获得高浓度的药物。口腔黏附系统具有控制和延长释放的潜力,从而获得更好的性能和患者依从性。本文简要综述了黏附给药系统的优点、黏附机制、影响黏附给药系统的不同因素。
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引用次数: 13
Analytical method validation for estimation of avanafil and dapoxetine hydrochloride tablet dosage form by HPTLC method hplc法测定盐酸阿那非达泊西汀片剂剂型的分析方法验证
Pub Date : 2017-06-01 DOI: 10.26510/2394-0859.PBE.2017.26
Dhwani A. Shah, Kunjal L. Vegad, E. D. Patel, Hitesh K. Prajapati, Ronak N. Patel, Y. K. Patel
Objective: A simple, specific, accurate and precise RP-HPTLC method has been developed and validated for simultaneous estimation of Avanafil and Dapoxetine. Methods: The chromatographic separation was achieved on Aluminium plates precoated with Silica gel 60 F254 using chloroform: methanol: ethyl acetate: glacial acetic acid (5:2:3:0.2, v/v/v/v) as mobile phase detected at 279 nm. Results: The correlation coefficient for RP-HPLC method was found to be 0.9987 for Avanafil and 0.9991 Dapoxetine and the linearity range was found to be 1040-3640 ng*spot-1 for Avanafil and 80-280 ng*spot-1 for Dapoxetine. Conclusions: The developed method was successfully applied to marketed tablet dosage form and the results were found with higher confidence.
目的:建立一种简便、特异、准确、精密度高的RP-HPTLC方法,用于同时测定阿那非和达泊西汀的含量。方法:以氯仿:甲醇:乙酸乙酯:冰醋酸(5:2:3:2 .2,v/v/v/v)为流动相,在279 nm处进行色谱分离。结果:阿瓦那非和达泊西汀的RP-HPLC相关系数分别为0.9987和0.9991,线性范围分别为1040 ~ 3640 ng*spot-1和80 ~ 280 ng*spot-1。结论:所建立的方法可成功地应用于市售片剂剂型,结果具有较高的可信度。
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引用次数: 6
期刊
Pharmaceutical and Biological Evaluations
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