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Protective role of Ascidia sydneiensis Stimpson, 1855 on cardiac enzyme biochemistry and histopathology in isoproterenol - induced myocardial ischemia 悉尼海鞘1855对异丙肾上腺素诱导心肌缺血心肌酶生化和组织病理学的保护作用
Pub Date : 2017-02-02 DOI: 10.7439/IJPC.V7I1.3857
C. Packiam, R. Margret, V. Meenakshi
Myocardial ischemia refers to the condition in which a portion of a heart is starved of oxygen and nutrients as a result of sudden block i the coronary arteries. It may be caused by chemotherapy, complications from anorexia nervosa , adverse effects of heavy metals intake and an incorrectly administered drug.The aim of the study is to investigate the protective role of Ascidia sydneiensis in isoproterenol - induced myocardial ischemia in rats. The extract was administered at a dose of 50, 100 and 150 mg/kg bw i.g.c for 28 days. The animals of ISO control and Ascidia sydneiensis pretreated groups were given isoproterenol (150 mg/kg bw) at an interval of 24 hours on 29 th and 30 th day of the experiment. Biochemical parameters like LDH, AST, ALT in serum and lipid peroxidation marker enzyme - MDA in both serum and tissue; enzymatic and non-enzymatic myocardial antioxidant enzymes - SOD, CAT, GPx in heart tissue and GSH in both serum and tissue were analysed following standard procedures. Histopathological architecture of cardiac muscle was also studied. A significant increase in the level of LDH, AST, ALT in the serum and lipid peroxidation marker enzyme - MDA in serum and heart tissue and decrease in the enzymatic and non-enzymatic antioxidant enzymes - SOD, CAT, GPx in heart tissue and GSH in both serum and tissue were noted in ISO treated groups. In the pretreated groups all the above parameters were normal. Restoration of enzyme level observed in the co-treated groups indicate that the extract has protective role in ISO - induced myocardial ischemia. Histopathological studies also confirmed the protective nature of the extract on heart tissue. Based on present findings, it is concluded that Ascidia sydneiensis may be a potential and therapeutic agent against the oxidative stress associated ischemic heart disease owing to antioxidant and antiperoxidative activity.
心肌缺血是指心脏的一部分由于冠状动脉突然阻塞而缺氧和缺乏营养的情况。它可能是由化疗、神经性厌食症并发症、重金属摄入的不良影响和用药不当引起的。本研究旨在探讨悉尼海鞘对异丙肾上腺素所致大鼠心肌缺血的保护作用。以50、100和150 mg/kg bw .g.c的剂量给药28天。ISO对照组和悉尼海鞘预处理组在试验第29天和第30天每隔24小时给予异丙肾上腺素150 mg/kg bw。血清中LDH、AST、ALT等生化指标,血清和组织中脂质过氧化标记酶- MDA等生化指标;按照标准程序分析心肌酶和非酶抗氧化酶——心脏组织中SOD、CAT、GPx和血清和组织中GSH。并对心肌组织病理结构进行了研究。异黄酮处理组大鼠血清中LDH、AST、ALT水平显著升高,血清和心脏组织中脂质过氧化标记酶- MDA水平显著升高,心脏组织中酶和非酶抗氧化酶- SOD、CAT、GPx和血清和组织中GSH水平显著降低。预处理组以上各项指标均正常。共处理组酶水平的恢复表明提取物对异源性心肌缺血有保护作用。组织病理学研究也证实了提取物对心脏组织的保护作用。综上所述,悉尼海鞘具有抗氧化和抗过氧化活性,可能是抗氧化应激相关缺血性心脏病的潜在治疗药物。
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引用次数: 0
Design, synthesis and in vivo antitumor activity of novel 3, 4 di-substituted quinazoline derivatives 新型3,4二取代喹唑啉衍生物的设计、合成及体内抗肿瘤活性研究
Pub Date : 2017-02-01 DOI: 10.7439/ijpc.v7i1.3928
B. Dash, S. Dash, Damiki Laloo, Jashabir Chakraborty
Objective: The present investigation is designed to synthesize some new isomeric series of quinazoline-4-one/4-thione derivatives, depending upon on the pharmacophoric model of in-vivo anticancer activity by modifying the structures retaining the fundamental structural features for the activity and screened for their antitumor properties. Methods: A new series of 7-chloro-3-[substituted (amino/phenyl amino)]-2-phenyl quinazolin-4 (3H)-one/thione derivatives and 1-(7-chloro-4-oxo/-2-phenylquinazoline-3 (4H-yl)) substituted urea derivatives were synthesized. The reaction scheme proceeds through 7-chloro-2-phenyl-4H-benzo [d] [1, 3] oxazin-4-one which is the intermediate one. The structures of the newly synthesized compounds were characterised from infrared (IR), H 1 nuclear magnetic resonance (NMR) and mass spectra (m/z) and elemental analysis. The in-vivo antitumor activity was evaluated by body weight analysis, mean survival time and percentage increase in life span methods in Swiss albino mice bearing Ehrilich ascites carcinoma (EAC). Result: The physico-chemical and spectroscopic data established the synthesis of quinazoline derivatives with a common pharmacophore. The synthesized compounds were evaluated for their antitumor properties. Among the newly quinazoline derivatives screened, six compounds (IIh, IIi, IIj, IIIh, IIIi, IIIj)) have shown significant antitumor activity. Conclusion: The quinazoline derivatives obtained from the present study indicates that the amino group at 3 rd position and urea/thiourea group in phenyl hydrazine ring at 3 rd position of quinzoline skeleton are essential for antitumor activity. Compounds IIh, IIi, IIj, IIIh, IIIi and IIIj were found to be biologically active which may be useful as potential resource for the discovery of anti-tumor compound having common quinazoline pharmacophore with lesser toxic effects.
目的:本研究旨在根据体内抗癌活性的药理模型,通过修饰结构,保留活性的基本结构特征,并对其抗肿瘤特性进行筛选,合成一些新的喹唑啉-4- 1 /4-硫酮衍生物异构体系列。方法:合成了一系列新的7-氯-3-[取代(氨基/苯基氨基)]-2-苯基喹唑啉-4 (3H)酮/硫酮衍生物和1-(7-氯-4-氧/-2-苯基喹唑啉-3 (4h -基))取代尿素衍生物。反应方案通过中间产物7-氯-2-苯基- 4h -苯并[d][1,3]恶嗪-4- 1进行。通过红外(IR)、核磁共振(NMR)、质谱(m/z)和元素分析对新合成化合物的结构进行了表征。采用体重分析、平均生存时间和寿命增加百分率等方法评价瑞士白化小鼠ehlich腹水癌(EAC)体内抗肿瘤活性。结果:通过理化和光谱学数据确定了具有常见药效团的喹唑啉衍生物的合成方法。对合成的化合物进行了抗肿瘤性能评价。在筛选到的新喹唑啉衍生物中,有6个化合物(IIh, IIi, IIj, IIIh, IIIi, IIIj))具有显著的抗肿瘤活性。结论:本研究得到的喹唑啉类衍生物表明,喹唑啉骨架第3位氨基和苯基肼环第3位脲/硫脲基对其抗肿瘤活性至关重要。化合物IIh、IIi、IIj、IIIh、IIIi和IIIj具有生物活性,为发现具有常见喹唑啉药效团且毒性较小的抗肿瘤化合物提供了潜在资源。
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引用次数: 0
Analgesic and antiinflammatory evaluation of newer 2-amino nicotinate derivatives synthesized by baylis hillman reaction 贝利斯-希尔曼反应合成的新型2-氨基烟酸衍生物的镇痛和抗炎评价
Pub Date : 2017-02-01 DOI: 10.7439/ijpc.v7i1.3875
K. Ch., G. Raju, R. Nadendla
Nicotine is an important class of heterocyclic compound, has been shown to exhibit diverse biological and pharmacological activities. In this study, a series of newer 2-amino nicotinate derivativeshave been synthesized by Baylis Hillman reaction. All the synthesized compounds have been characterized by using elemental analysis, FT-IR, 1 H NMR, 13 C NMR spectroscopy and further supported by mass spectroscopy. Purity of all the compounds has been checked on thin layer chromatographic plate and HPLC technique. All the synthesized compounds were tested for their analgesic and anti-inflammatory activities. The compounds exhibited significant analgesic and anti-inflammatory activities. These compounds can be further exploited to get the potent lead compounds. The detailed synthesis and the pharmacological screening of 2-amino nicotinate derivatives are reported.
尼古丁是一类重要的杂环化合物,具有多种生物学和药理活性。本研究通过Baylis - Hillman反应合成了一系列较新的2-氨基烟酸衍生物。所有合成的化合物都通过元素分析、FT-IR、1h NMR、13c NMR以及质谱分析进行了表征。用薄层色谱板和高效液相色谱技术对所有化合物的纯度进行了检测。所有合成的化合物都进行了镇痛和抗炎活性测试。化合物具有明显的镇痛和抗炎活性。这些化合物可以进一步开发得到有效的先导化合物。本文报道了2-氨基烟酸衍生物的合成及药理筛选。
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引用次数: 1
Synthesis, hypoglycemic and aldose reductase inhibition activity of novel ferulic acid derivatives 新型阿魏酸衍生物的合成、降糖及醛糖还原酶抑制活性
Pub Date : 2017-01-30 DOI: 10.7439/IJPC.V7I1.3798
Xianfeng Huang, Yuanyuan Liu, Cheng Zhang, Guoqiang Song
A novel class of ferulic acid derivatives with urea groups were synthesized and evaluated for hypoglycemic and aldose reductase inhibition activities. Several compounds showed comparable in vivo hypoglycemic agents to the commercial drug glibenclamide. Furthermore, of the tested compounds, 7a and 7 b displayed the most potent aldose reductase inhibitory activity in vitro , with an IC 50 of 0.55 and 3.88 M, respectively. Docking simulation was performed to insert compound 7a and 12a into the crystal structure of aldose reductase at active site to determine the probable binding model.
合成了一类具有尿素基团的新型阿魏酸衍生物,并对其降糖和醛糖还原酶抑制活性进行了评价。几种化合物显示出与商业药物格列本脲相当的体内降糖药。其中,7a和7b的醛糖还原酶抑制活性最强,ic50分别为0.55和3.88 M。通过对接模拟,将化合物7a和12a插入醛糖还原酶活性位点的晶体结构中,确定可能的结合模式。
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引用次数: 0
Synthesis and Biological Evaluation of Pyrazolyl Isoxazolines as Antimicrobial Agents 吡唑基异恶唑啉类抗菌药物的合成及生物学评价
Pub Date : 2016-12-31 DOI: 10.7439/IJPC.V6I12.3610
Rajesh Kumar, Manoj Kumar, C. Sharma, K. R. Aneja, O. Prakash
Pyrazolyl isoxazolines were synthesized by 1,3-dipolar cycloaddition of pyrazolyl nitrile oxide with various activated alkene such as acrylonitrile, methyl acrylate and vinyl acetate in the presence of iodobenzene diacetate in methanol containing a catalytic amount of TFA at room temperature with an aim to explore their effect on in vitro growth of microorganism causing microbial infection. Eleven compounds were tested in vitro for their antibacterial activity against two Gram-positive bacteria namely, Staphylococcus aureus , Bacillus subtilis and two Gram-negative bacteria namely, Escherichia coli and Pseudomonas aeruginosa . All the synthesized compounds were also tested for their inhibitory action against two strains of fungus.
在含催化量TFA的甲醇中,在二醋酸碘苯的存在下,吡唑基腈氧化物与各种活性烯烃(丙烯腈、丙烯酸甲酯、醋酸乙烯酯)在室温下以1,3-偶极环加成法合成吡唑基异恶唑啉,探讨其对微生物体外生长引起微生物感染的影响。研究了11种化合物对两种革兰氏阳性菌(金黄色葡萄球菌、枯草芽孢杆菌)和两种革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)的抑菌活性。并对合成的化合物进行了抑菌试验。
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引用次数: 0
Antimicrobial Analysis and Structural Elucidation Of Active Compounds Of Dialium Indum Leaves Extract (Valvet Tarmarind) 杜仲叶提取物抑菌活性成分分析及结构解析
Pub Date : 2016-12-31 DOI: 10.7439/IJPC.V6I12.3658
K. I. Ijoma, V. Ajiwe, C. I. Awuzie
Antimicrobial analysis and structural elucidation were carried out on the purified leaves of Dialium indum. The Harbone method was used for the extraction. The extracts were separated using a combination of column chromatography and thin layer chromatography, which gave rise to the isolation of two fractions, these fractions were further purified using recrystallization. The melting point of each pure fraction was determined. The purified extracts were subjected to structural elucidation using various spectroscopic techniques which includes; FTIR, UV, H1 NMR, C13 NMR, DEPT 1350, COSY, TOCSY, HMBC and HSQC . The spectral analysis suggested the presence of Stigmasterol, and Lauric acid. The antimicrobial analysis (anti fungal and anti bacterial analysis) using the punched agar diffusion method was carried out on the isolated fractions comparatively with a standard drug Funbact-A cream (a broad spectrum antibiotic). A total of thirteen test organisms were used for this analysis amongst which were ten bacteria test organism and three fungi test organisms. The results from the average diameter zones of inhibition, minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and fungicidal concentrations (MFC) showed that all the fractions were all active on the entire test organism with zones of inhibition ranging from 14mm-36mm comparatively. None of these fractions showed similar antimicrobial effect as the standard drug Funbact-A cream but individually could serve as anti microbial to diseases caused by these test organisms from their MIC, MBC and MFC.
对纯化的杜仲叶片进行了抗菌分析和结构鉴定。采用Harbone法提取。采用柱层析和薄层析相结合的方法对提取物进行分离,分离出两个馏分,再用重结晶法对这两个馏分进行纯化。测定了各纯馏分的熔点。纯化的提取物使用各种光谱技术进行结构解析,其中包括;FTIR, UV, H1 NMR, C13 NMR, DEPT 1350, COSY, TOCSY, HMBC和HSQC。光谱分析表明含有豆甾醇和月桂酸。用穿孔琼脂扩散法与标准药物Funbact-A乳膏(广谱抗生素)进行了抗菌分析(抗真菌和抗菌分析)。共使用了13种试验生物进行分析,其中10种是细菌试验生物,3种是真菌试验生物。抑菌平均直径区、最小抑菌浓度(MIC)、最小杀菌浓度(MBC)和杀真菌浓度(MFC)的结果表明,各组分对整个被试生物均有活性,抑菌区范围为14mm ~ 36mm。这些组分的抑菌效果与标准药物Funbact-A乳膏的抑菌效果都不相似,但从这些试验微生物的MIC、MBC和MFC来看,它们单独可以对这些试验微生物引起的疾病起到抑菌作用。
{"title":"Antimicrobial Analysis and Structural Elucidation Of Active Compounds Of Dialium Indum Leaves Extract (Valvet Tarmarind)","authors":"K. I. Ijoma, V. Ajiwe, C. I. Awuzie","doi":"10.7439/IJPC.V6I12.3658","DOIUrl":"https://doi.org/10.7439/IJPC.V6I12.3658","url":null,"abstract":"Antimicrobial analysis and structural elucidation were carried out on the purified leaves of Dialium indum. The Harbone method was used for the extraction. The extracts were separated using a combination of column chromatography and thin layer chromatography, which gave rise to the isolation of two fractions, these fractions were further purified using recrystallization. The melting point of each pure fraction was determined. The purified extracts were subjected to structural elucidation using various spectroscopic techniques which includes; FTIR, UV, H1 NMR, C13 NMR, DEPT 1350, COSY, TOCSY, HMBC and HSQC . The spectral analysis suggested the presence of Stigmasterol, and Lauric acid. The antimicrobial analysis (anti fungal and anti bacterial analysis) using the punched agar diffusion method was carried out on the isolated fractions comparatively with a standard drug Funbact-A cream (a broad spectrum antibiotic). A total of thirteen test organisms were used for this analysis amongst which were ten bacteria test organism and three fungi test organisms. The results from the average diameter zones of inhibition, minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and fungicidal concentrations (MFC) showed that all the fractions were all active on the entire test organism with zones of inhibition ranging from 14mm-36mm comparatively. None of these fractions showed similar antimicrobial effect as the standard drug Funbact-A cream but individually could serve as anti microbial to diseases caused by these test organisms from their MIC, MBC and MFC.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"23 1","pages":"237-244"},"PeriodicalIF":0.0,"publicationDate":"2016-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77854324","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: 3
Phytochemical Screening, Spectroscpic Characterisation and Cardiotonic Activity of Aqueous Extract from Arieal Parts of Carmona Retusa (Vahl) Masam on Isolated Frogs Heart 水提物对离体青蛙心脏的植物化学筛选、光谱表征及强心活性研究
Pub Date : 2016-12-31 DOI: 10.7439/IJPC.V6I12.3804
G. Kumar, A. Rani, B. Pooja, Y. Kumar
The present study was undertaken to evaluate cardiotonic activity of aqueous extract of whole plant of carmona retusa (vahl) masam. Phytochemical screening of whole plant material revealed that the major constituent of Carmon retusa (Vahl.) Masam plant is an intractable mixture of alkaloids,triterpenes, flavanoids and cardiac gylcosides. Cardiotonic effect of aqueous extract of whole plant of carmona retusa was studied by using isolated frog heart perfusion technique (IFHP). Calcium free Ringer solution was used as vehicle for administration of aqueous extract of carmona retusa as a test extract and digoxin as a standard. A significant increase in height of force of contraction (positive inotropic effect) and decrease in heart rate (negative chronotropic effect) at a very low concentration (10g/ml) was observed with test extract as compared to the same dose of a standard digoxin. The present results indicated that a significant increase in height of force of contraction with decrease in heart rate was observed as the dose of test extract increased. The test extract does not produced cardiac arrest at 80g/ml, a higher concentration, as compared to standard, digoxin, a drug with narrow therapeutic window, carmona retusa showed wide therapeutic window.
本研究评价了山核桃全株水提物的强心活性。全株材料的植物化学筛选表明,香豆属植物的主要成分为:马萨姆是一种难处理的生物碱、三萜、黄酮类化合物和心脏苷的混合物。采用离体青蛙心脏灌注技术(IFHP)研究了金牛桃全株水提物的强心作用。以无钙林格氏液为对照品,以地高辛为对照品,以牛蒡水提物为对照品。与相同剂量的标准地高辛相比,试验提取物在极低浓度(10g/ml)下显著增加收缩力高度(正性肌力效应)和降低心率(负性变时效应)。本研究结果表明,随着试验提取物剂量的增加,收缩力的高度显著增加,心率降低。试验提取物在80g/ml浓度下不产生心脏骤停,与标准药物地高辛相比,治疗窗较窄,卡莫纳图沙的治疗窗较宽。
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引用次数: 1
UV-Visible Spectrophotometric Method Development and Validation of Itraconazole in Bulk and Capsule Formulation 紫外可见分光光度法测定伊曲康唑原料药和胶囊的含量及验证
Pub Date : 2016-12-30 DOI: 10.7439/IJAPA.V6I4.3833
P. Salunke, K. Ingale, Pooja Gondhankhede, Kanchan Ghate, S. S. Patil, S. Barhate
A simple, rapid, accurate and precise UV method was developed and validated for the estimation of Itraconazole in pharmaceutical dosage form. Spectroscopic method was carried out by using acidic ethanol as solvent. Itraconazole detection wavelength was set at 262nm for validation purpose linearity, accuracy, repeatability, precision, LOD, LOQ, and ruggedness parameters were studied. The linearity was found to be in the range of 2-12 g/ml.
建立了一种简便、快速、准确、精密度高的紫外分光光度法测定伊曲康唑制剂的含量。以酸性乙醇为溶剂进行光谱分析。伊曲康唑的检测波长为262nm,考察其线性度、准确度、重复性、精密度、定量限、定量定量限和坚固性等参数。在2 ~ 12 g/ml范围内呈线性关系。
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引用次数: 5
A validated stability-indicating HPLC assay method for Meclizine HCl in bulk drug 一种稳定性指示的高效液相色谱法测定原料药盐酸美甲嗪的方法
Pub Date : 2016-12-30 DOI: 10.7439/IJAPA.V6I3.3855
M. Ubale, M. Shioorkar, V. Choudhari
An isocratic reversed phase stability-indicating high-performance liquid chromatographic (HPLC) assay method was developed and validated for quantitative determination of Meclizine HCl in bulk drugs. An isocratic, reversed phase HPLC method was developed to separate the drug from the degradation products, using a Water Nova Pack C18 (250 x 4.6) mm, 5? column and the mobile phase containing 1.0 gm Sodium dihydrogen phosphate and 1.0 gm 1-octaneSulfonic acid salt in 1000ml water filter and mixed. Prepare a homogenous mixture of buffer, methanol and acetonitile. The detection was carried out at wavelength 264 nm. The developed method was validated with respect to linearity, accuracy (recovery), precision, system suitability, selectivity, robustness prove the stability indicating ability of the method.
建立了等容反相稳定高效液相色谱(HPLC)测定原料药中盐酸美甲嗪的方法。采用水Nova Pack C18 (250 × 4.6) mm, 5?流动相中含有1.0 gm磷酸二氢钠和1.0 gm 1-辛烷磺酸盐,于1000ml水中过滤混合。制备缓冲液、甲醇和乙腈的均匀混合物。检测波长为264 nm。对该方法进行了线性度、准确度(回收率)、精密度、系统适用性、选择性、鲁棒性等方面的验证,证明了该方法的稳定性。
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引用次数: 0
Synthesis and physico-chemical characterization of some novel oxazepine derivatives 一些新型恶西平衍生物的合成及理化性质
Pub Date : 2016-11-30 DOI: 10.7439/IJPC.V6I11.3713
L. Joseph, M. George, Surekha
Series of oxazepine derivatives were synthesized from Schiffs base as aldehyde derivatives by using semicarbazide as starting material.Then equimolar quantities of prepared Schiffs base reacts with pthallic anhydride or succinic anhydride undergo cycloaddition reaction in the presence of organic solvent benzene give an oxazepine ring system. Chemical structures of the synthesized compounds were confirmed on the basis of their spectral data
以氨基脲为原料,以希夫斯碱为醛类衍生物合成了一系列恶氮平衍生物。然后等量的希夫斯碱与邻苯二酸酐或丁二酸酐在有机溶剂苯的存在下进行环加成反应,得到恶氮平环体系。根据光谱数据确定了合成化合物的化学结构
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引用次数: 0
期刊
International Journal of Pharmaceutical Chemistry
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