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Synthesis and antimicrobial activity of chalcones and pyrazolines 查尔酮和吡唑啉的合成及其抗菌活性
Pub Date : 2017-08-28 DOI: 10.7439/ijpc.v7i8.4348
R. Umadevi
Chalcones are 1,3-diphenyl-2-propene-1-one, in which two aromatic rings are linked by a three carbon ?,?-unsaturated carbonyl system. They have displayed a broad spectrum of biological activities. In this view it was proposed to synthesize some novel pyrazolines from chalcones. Chalcones are prepared by treating 2-acetyl-5-bromothiophene with different aromatic compounds. These chalcones on condensation with phenyl hydrazine HCl. pyridine as a catalyst gave 3-(5-bromothiphene-2yl)-1-phenyl-1H-pyrazole derivatives. The synthesized compounds have been characterized by their melting point, TLC, IR and 1H NMR spectral data. They have been screened for their antibacterial activity against Gram positive bacteria B.subtillis & B.pumilus and Gram negative bacteria E. coli & P.vulgaris and antifungal against A.niger & p.crysogenium .
查尔酮是1,3-二苯基-2-丙烯-1- 1,其中两个芳香环由三个碳?,?-不饱和羰基体系。它们显示出广泛的生物活性。在此基础上,提出了以查尔酮为原料合成新型吡唑啉的方法。用不同的芳香族化合物对2-乙酰基-5-溴噻吩进行处理制备查尔酮。这些查尔酮与盐酸苯基肼缩合。吡啶为催化剂得到3-(5-溴噻吩-2基)-1-苯基- 1h -吡唑衍生物。对合成的化合物进行了熔点、薄层色谱、红外光谱和核磁共振氢谱的表征。对革兰氏阳性菌枯草芽孢杆菌和矮芽孢杆菌、革兰氏阴性菌大肠杆菌和普通芽孢杆菌具有抑菌活性,对黑霉杆菌和低温芽孢杆菌具有抑菌活性。
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引用次数: 1
A comparative study of isolation, identification and grouping of streptococcal isolates from throat swabs of school going children applying different methods of extraction for antigen 不同抗原提取方法对学龄儿童咽拭子链球菌分离、鉴定和分型的比较研究
Pub Date : 2017-07-30 DOI: 10.7439/IJPC.V7I7.4249
S. Mohana, C. Sasikumar, S. Yasodha
Objective: The objective of this research was to collect the throat swabs from symptomatic and asymptomatic children and microbiologically positive sample were further taken up for grouping. Methods: Extraction of streptococcal group antigen by various methods namely enzyme extraction, fullers extraction, Lancefield extraction. Comparing the antigen extraction methods in identifying the sero groups of BHS.Comparative studies between conventional and enzymatic methods of extraction. Which one is ideal method of extraction and which one is common among the children. Results: Throat swabs were collected in the age group of 5-12 both symptomatic and asymptomatic children. Symptomatic such as rashes, throat pain, fever, cold, cough etc. Totally 361 throat swabs were collected of which 19 were BHS.18 isolates were typeable and 1 was non typeable. In enzyme extraction is not effective in the extraction of group D streptococci may be extracted with mutanolysin only after 4H incubation although effective for the extraction of some strains of group D streptococci.in fullers extraction it was seen to give an important clue to the structure of cell wall of gram positive bacteria in lance field extraction was easily performed specific and sensitive method. Conclusion: Group A streptococcal isolates were just 2 in no which shows that group A is not the predominant strain in our study. There by denoting the prevalence of rheumatic fever and RHD are becoming less. There was no cross reaction among groups were lancefield and fullers method were applied.in enzymatic method there was slight cross reaction noted between A and D in one isolate,F and G in one isolate and C and G in another isolate.
目的:收集有症状和无症状儿童的咽拭子,并进一步采集微生物阳性样本进行分组。方法:采用酶法、富勒法、兰斯菲尔德法提取链球菌群抗原。比较不同抗原提取方法鉴定BHS血清群。常规提取法与酶法的比较研究。哪一种是理想的提取方法,哪一种在儿童中是常见的。结果:收集了5-12岁有症状和无症状儿童的咽拭子。有皮疹、咽喉痛、发热、感冒、咳嗽等症状。共采集361份咽拭子,其中bhs阳性19株,可分型18株,不可分型1株。在酶提法中对D群链球菌的提取不有效,虽然对部分D群链球菌的提取有效,但只有在孵育4H后才能用变溶素提取。富勒提取是研究革兰氏阳性菌细胞壁结构的重要线索,lance field提取方法简便、特异、灵敏。结论:A群链球菌分离株仅2株,表明A群不是本研究的优势菌株。在那里,风湿热和RHD的患病率正在减少。采用lancefield法和fullers法,各组间无交叉反应。在酶促法中,一株分离物中的A和D、F和G以及C和G之间存在轻微的交叉反应。
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引用次数: 0
Extraction and characterization of Hydroxy Citric Acid from Garcinia combogia cultivated at two different locations of Malabar and Srilanka 马拉巴尔和斯里兰卡两地栽培藤黄中羟基柠檬酸的提取及特性研究
Pub Date : 2017-07-30 DOI: 10.7439/IJPC.V7I7.4298
R. Ravikumar, B. Ranganathan, S. Vinothkumar, S. Yamuna, P. Yasodha, P. Priyanka, R. V. Rasikaa, Y. Sownisha
Obesity is one of the major problems faced by many people all around the world. There are many ways to reduce it physically, but it needs some hardwork. Hydroxy citric acid (HCA) is the compound which is used to reduce weight. This compound is abundantly present in the fruits of Garcinia combogia . This is a type of tamarind which is cultivated in Srilanka and also in some parts of Malabar in India. The purity and yield of HCA varies between G. cambogia cultivated at different locations. It is very important to extract HCA with maximum purity and with higher yield to benefit the mankind. Hence, in the present research work, HCA was extracted from G. combogia cultivated at two different location of Malabar and Srilanka and compared their elements and purity using HPLC and FTIR. The purity of HCA extracted from G. combogia cultivated at Malabar was found to be higher of about 50.95% in comparison with HCA extracted from G. combogia cultivated at Srilanka which was 41.16%.
肥胖是全世界许多人面临的主要问题之一。有很多方法可以减少身体上的疲劳,但这需要一些努力。羟基柠檬酸(HCA)是一种用于减肥的化合物。这种化合物在藤黄果中大量存在。这是一种罗望子,在斯里兰卡和印度马拉巴尔的一些地区都有种植。不同产地栽培的黄藤,其HCA的纯度和产量各不相同。以最高的纯度和更高的收率提取HCA对造福人类具有重要意义。因此,在本研究中,我们从马拉巴尔和斯里兰卡两个不同地点种植的三叶草中提取了HCA,并使用HPLC和FTIR对其元素和纯度进行了比较。结果表明,马拉巴尔栽培的三叶草中提取的HCA纯度为50.95%,高于斯里兰卡栽培的三叶草中提取的41.16%。
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引用次数: 1
The effect of essential oil of Lavandula angustifolia on amyloid beta polymerization: An in vitro study 薰衣草精油对β -淀粉样蛋白聚合作用的体外研究
Pub Date : 2017-07-30 DOI: 10.7439/IJPC.V7I7.4085
Masoud Soheili, Farzaneh Khalaji, M. Mirhashemi, M. Salami
Alzheimer’s disease (AD) is a progressive neurological disorder associated with cognitive and memory deficits. Accumulation of amyloid beta (Aβ) plaques is one of the major causes of AD. Therefore, inhibition of the plaque formation has been aimed to play a preventive role in the disease.  Lavender, through some neuroprotective roles such as antioxidant effects, is known to be an effective candidate in treatment of neurodegenerative disorders. In this study using Thioflavin T Measurement and Atomic Force Microscope (AFM) Imaging we evaluated effect of essential oil of lavender on Aβ polymerization.Thioflavin T Method showed that the essential oil enhances the Aβ aggregation. The results of AFM method also confirmed it. Our data antagonizes previous results indicating clearing effect of aqueous extract of lavender on Aβ plaque. It seems that the different combination of essential oil and aqueous extract considerably determines if or not the aggregation occurs.
阿尔茨海默病(AD)是一种与认知和记忆缺陷相关的进行性神经系统疾病。淀粉样蛋白(Aβ)斑块的积累是AD的主要原因之一。因此,抑制斑块形成的目的是在疾病中发挥预防作用。薰衣草具有抗氧化等神经保护作用,是治疗神经退行性疾病的有效候选物质。本研究采用硫黄素T测定和原子力显微镜(AFM)成像技术研究了薰衣草精油对Aβ聚合的影响。硫黄素T法表明,香精油对Aβ聚集有增强作用。原子力显微镜的结果也证实了这一点。我们的数据与先前的结果相反,表明薰衣草水提物对Aβ斑块有清除作用。精油和水萃取物的不同组合似乎在很大程度上决定了聚合是否发生。
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引用次数: 7
Application of Validated HPLC Method for Degradation Study of Vildagliptin and Metformin HCl 高效液相色谱法在维格列汀和盐酸二甲双胍降解研究中的应用
Pub Date : 2017-06-28 DOI: 10.7439/IJAPA.V7I2.4375
I. Sheikh, M. Charde, R. Chakole
A novel and simple reverse phase liquid chromatographic method has been established for the determination of Sitagliptin and Metformin HCl and studies its degradation pattern in pharmaceutical dosage forms. Sitagliptin and Metformin HCl is used to control Type 2 Diabetes. The proposed work was performed on Younglin( S.K) isocratic System UV DetectorC18 column (150 mm 4.6 mm). A mixture of Potassium Phosphate buffer pH-3.2 with orthophosphoric acid and acetonitrile was used as mobile phase in this method with flow rate 0.7 ml/min (UV detection at 203 nm) and the method was validated as per ICH guidelines. Forced degradation studies were performed by exposing the drug Sitagliptin and Metformin HCl to acidic, alkaline, oxidation and thermal stress degradations. The proposed RP-HPLC method was found to be robust and specific and this method is suitable for the assay of pharmaceutical dosage forms as well as kinetic studies.
建立了一种新型、简便的反相液相色谱法测定西格列汀和盐酸二甲双胍,并研究了其在药物剂型中的降解规律。西格列汀和盐酸二甲双胍用于控制2型糖尿病。所提出的工作在Younglin(S.K)等温系统UV DetectorC18柱(150 mm 4.6 mm)上进行。以磷酸钾缓冲液pH-3.2与正磷酸和乙腈的混合物为流动相,流速0.7 ml/min (203nm紫外检测),按照ICH指南进行验证。通过将西格列汀和盐酸二甲双胍暴露于酸性、碱性、氧化和热应激降解中,进行了强制降解研究。所建立的反相高效液相色谱法具有较好的鲁棒性和特异性,适用于药物剂型的测定和动力学研究。
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引用次数: 2
Phytochemical investigation for the authentication of Indian traditional herbal drug Boerhavia diffusa and its differentiation from morphologically similar plant B. erecta 印度传统草药白花布草鉴别及与形态相近植物直叶布草鉴别的植物化学研究
Pub Date : 2017-06-28 DOI: 10.7439/IJPC.V7I6.4244
V. Vadivel, P. Brindha
Boerhavia diffusa is an important herbal ingredient of several Ayurvedic and Unani formulations and it is commonly called as Punarnava in Indian system of medicine. But, this plant is often confused with Boerhavia erecta due to morphological similarity and also being adulterated in Indian herbal market. In order to differentiate these plant drugs, in the present work we have developed chemical fingerprints through phytochemical analysis, UV-Visible, FT-IR & NMR spectroscopy, HPTLC and HPLC chromatography. Phytochemical analysis of methanolic extract of investigated materials showed that B. diffusa contained higher level of total phenolic compounds (339.40 mg GAE / 100 g) when compared to B. erecta (269.87 mg GAE / 100 g). Scanning in UV-Visible spectroscopy exhibited maximum absorption at 212, 362, 428 & 663 nm for B. diffusa while B. erecta showed peaks at 214, 308, 349, 532 & 663 nm. Similarly, FT-IR spectroscopy of raw materials indicated notable difference between the samples at 400 – 1000 cm -1 region. NMR spectroscopy illustrated remarkable difference between the chloroform extract of selected samples at 1-3 ppm region. HPTLC profile of methanolic extract of B. diffusa exhibited a total number of 9 peaks while B. erecta showed 12 number of peaks. Chemical profile investigated in the present study will be helpful to differentiate B. diffusa from B. erecta and also useful to prevent their adulteration in herbal industry.
白花布尔哈维亚是几种阿育吠陀和乌纳尼配方的重要草药成分,在印度医学系统中通常被称为Punarnava。但是,由于形态相似,这种植物经常与布尔哈维亚(Boerhavia erecta)混淆,并且在印度草药市场上也被掺假。为了鉴别这些植物药物,本研究通过植物化学分析、紫外可见光谱、傅里叶变换红外光谱和核磁共振光谱、HPTLC和HPLC色谱等方法建立了化学指纹图谱。植物化学分析表明,白花草的总酚类化合物含量为339.40 mg GAE / 100 g,高于白花草的269.87 mg GAE / 100 g。紫外可见光谱扫描显示,白花草的最大吸收波长为212、362、428和663nm,而白花草的最大吸收波长为214、308、3449、532和663nm。同样,原料的FT-IR光谱在400 - 1000 cm -1区域显示出样品之间的显著差异。核磁共振波谱显示,所选样品的氯仿提取物在1- 3ppm区域存在显著差异。白花草甲醇提取物的HPTLC谱图共有9个峰,而直立草有12个峰。本研究对白花芽孢杆菌和直立芽孢杆菌的化学特征进行了研究,有助于区分白花芽孢杆菌和直立芽孢杆菌,并有助于防止其在草药工业中的掺假。
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引用次数: 1
Synthesis and biological Evaluation of some new Amide Derivatives of Sulphonamide 磺胺类新酰胺类衍生物的合成及生物学评价
Pub Date : 2017-06-28 DOI: 10.7439/IJPC.V7I6.4196
H. Pal, Arvind Kumar, Sonu, B. Parveen, S. Praveen
A series of substituted amide derivatives of Sulphonamides were synthesized, and their anticonvulsant activity and antimicrobial activity were evaluated which include the MES model and by Cup-plate method. However, further studies need to be carried out to ascertain the precise mechanism of action of anticonvulsant activity of these molecules. The compounds.N-(4-Acetylsulfamoyl-phenyl)-4-(4-chloro-3-methyl-phenyl)-4-oxo-butyramide (HP-1) showed significant anticonvulsant activity. Some compounds show the good antibacterial activity against Escherichia coli. The Compound 4-(4-chloro-3-methyl-phenyl)-4-oxo-N-(4-sulfamoyl-phenyl)-butyramide (HP-2) and 4-(4-Methoxy-phenyl)-4-oxo-N-(4-Sulfomoyl-Phenyl-)butyramide(HP-3) showed significant inhibitory characteristics with stronger antimicrobial activity against MTCC-521 gram(-)ve bacteria.
合成了一系列磺胺类取代酰胺衍生物,并采用MES模型和杯盘法对其抗惊厥活性和抗菌活性进行了评价。然而,需要进一步的研究来确定这些分子抗惊厥活性的确切作用机制。化合物n -(4-乙酰氨基甲酰苯基)-4-(4-氯-3-甲基苯基)-4-氧-丁酰胺(HP-1)具有显著的抗惊厥活性。部分化合物对大肠杆菌具有良好的抑菌活性。化合物4-(4-氯-3-甲基苯基)-4-氧- n -(4-磺酰基苯基)-丁酰胺(HP-2)和4-(4-甲氧基苯基)-4-氧- n -(4-磺酰基苯基)丁酰胺(HP-3)对MTCC-521 g (-)ve细菌具有较强的抑菌活性。
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引用次数: 2
Synthesis And Biological Evaluation of Some New Schiff base 1,2,4-Triazole Derivatives 新型希夫碱1,2,4-三唑衍生物的合成及生物学评价
Pub Date : 2017-06-28 DOI: 10.7439/IJPC.V7I6.4213
S. Praveen, Arvind Kumar, B. Parveen, Sonu, H. Pal
A series of substituted 1,2,4-Triazole derivatives were synthesized, and their anticonvulsant activity and antimicrobial activity were evaluated which include the MES model and by Cup-plate method. However, further studies need to be carried out to ascertain the precise mechanism of action of anticonvulsant activity of these molecules. The compounds 4-[1-(2-Bromo-phenyl)-ethylideneamino]-5-pyridin-3-yl-2,4-dihydro[1, 2, 4] triazole-3-thione (SB-1) and 4-[1-(4-Fluoro-phenyl)-ethylideneamino]-5-pyridin-3-yl-2,4-dihydro[1, 2, 4] triazole-3-thione (SB-2) showed significant anticonvulsant activity and antibacterial activity against Escherichia coli.
合成了一系列取代的1,2,4-三唑衍生物,并采用MES模型和杯盘法对其抗惊厥活性和抗菌活性进行了评价。然而,需要进一步的研究来确定这些分子抗惊厥活性的确切作用机制。化合物4-[1-(2-溴苯基)-乙基氨基]-5-吡啶-3-基-2,4-二氢[1,2,4]三唑-3-硫酮(SB-1)和4-[1-(4-氟苯基)-乙基氨基]-5-吡啶-3-基-2,4-二氢[1,2,4]三唑-3-硫酮(SB-2)具有显著的抗惊抽搐活性和对大肠杆菌的抗菌活性。
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引用次数: 0
Multi-wavelength Spectrophotometric Determination of Chlorzoxazone and Paracetamol in Bulk and Capsules 多波长分光光度法测定散装和胶囊中氯唑恶酮和扑热息痛的含量
Pub Date : 2017-06-28 DOI: 10.7439/IJAPA.V7I2.4161
Imad Osman Abu Reid, Abdelrahman Mohamed Tageldin
A simple, cost effective spectrophotometric method has been developed for the simultaneous determination of paracetamol (PAR) and chlorzoxazone (CHL) in bulk and dosage forms. The method permits data to be taken at multiple wavelengths to generate linear plots, from which the concentrations can be determined. The absorbance values of the two analytes were linear with the concentration at the wavelengths taken at 10 nm interval over the range of 230 -300 nm. The accuracy and the precision of the developed method were very good (RSD ? 2%). The validity of the proposed method was confirmed through the statistical comparison of the obtained data with those obtained by a reference method utilizing H-point for the determination of the two actives.
建立了同时测定原料药和剂型对乙酰氨基酚(PAR)和氯唑唑酮(CHL)的简单、经济有效的分光光度法。该方法允许在多个波长采集数据,生成线性图,从中可以确定浓度。在230 ~ 300 nm范围内,两种分析物在10 nm波长处的吸光度值与浓度呈线性关系。该方法的准确度和精密度均较好(RSD ?2%)。将所得数据与采用h点测定两种活性物质的参考方法进行统计比较,证实了所提方法的有效性。
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引用次数: 1
Development and validation of a dissolution method for a BCS class IV drug tadalafil BCS IV类药物他达拉非溶出度方法的开发和验证
Pub Date : 2017-06-28 DOI: 10.7439/IJAPA.V7I2.4155
Francine Regina Zachow Philippsen, Brunna Ricci Falcao, L. Teixeira, T. R. Sausen
The present study describes the development and validation of a dissolution method for tadalafil, a Biopharmaceutical Classification System class II drug. 0.1 N hydrochloric acid (HCl)+0.5% sodium lauryl sulphate (SLS), pH 4.5-acetate buffer+0.5% SLS and pH 6.8phosphate buffer+0.5% SLS were tested as dissolution medium, and influences of apparatus, and rotation speed were evaluated. Samples were analyzed by UV spectrophotometric method at 225 nm. The results also shows a better dissolution profile using pH 6.8phosphate buffer + 0.5% SLS as medium and paddle as apparatus is a speed of 100 rpm. The conditions that allowed dissolution determination were USP type II apparatus at 100 rpm, containing 900 mL of pH 6.8phosphate buffer+0.5% SLS as dissolution medium, with analysis at wavelength of 225 nm. Samples were analyzed by UV spectrophotometric method and validated as per ICH guidelines, showing specificity, linearity, precision and accuracy.
本研究描述了他达拉非(生物制药分类系统II类药物)溶出度方法的开发和验证。以0.1 N盐酸(HCl)+0.5%十二烷基硫酸钠(SLS)、pH为4.5-乙酸缓冲液+0.5% SLS、pH为6.8磷酸盐缓冲液+0.5% SLS作为溶解介质,考察了仪器、转速对溶解介质的影响。采用225 nm紫外分光光度法对样品进行分析。以pH为6.8的磷酸盐缓冲液+ 0.5%的SLS为介质,转速为100 rpm的桨叶为装置,溶解效果较好。溶出度测定条件为USPⅱ型仪器,转速100 rpm,溶解介质为900 mL pH 6.8磷酸盐缓冲液+0.5% SLS,波长225 nm。采用紫外分光光度法对样品进行分析,并按照ICH指南进行验证,显示特异性、线性度、精密度和准确性。
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引用次数: 1
期刊
International Journal of Pharmaceutical Chemistry
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