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Highly Sensitive, Selective and Validated Spectrofluorimetric Assay for Novel Oxazolidinone Antibiotic: Tedizolid Phosphate in Pharmaceutical Dosage Form and Human Plasma 药物剂型和人血浆中新型恶唑烷酮类抗生素磷酸二唑脂的高灵敏度、选择性和有效的荧光光谱分析
Pub Date : 2021-01-01 DOI: 10.21608/aprh.2021.77133.1132
Basma M. Tawfik, M. Rizk, M. Sultan, R. El-Eryan
Objectives: In this work we presented a highly sensitive, selective and validated method for determination of tedizolid phosphate (TEDP) antibiotic, based on its native fluorescence in aqueous solution. Methods: The maximum fluorescence intensity was measured at 408 nm after excitation at 298 nm after optimization of all experimental conditions. Results: The measured fluorescence was directly proportional to the concentration of the drug over the range of 2-30 ng/mL with a limit of detection of 0.13 and limit of quantification of 0.44 ng/mL The method succeeded to determine TEDP in its pharmaceutical dosage form and in human plasma with mean % recovery of 100.49 ±1.32 and 99.40 ± 2.18 respectively. Conclusion: The developed data was found to be with a good agreement with a valid method. The method was validated according to ICH guidelines for determination of the drug in its pure form and dosage form and according to FDA Guidance for Industry, Bioanalytical Method Validation for determination of TEDP in human plasma.
目的:建立了一种高灵敏度、高选择性、高可靠性的方法,利用磷酸盐二唑脂(tedizolid phosphate, TEDP)在水溶液中的天然荧光测定其含量。方法:优化所有实验条件后,在298 nm处激发后,在408 nm处测量最大荧光强度。结果:在2 ~ 30 ng/mL范围内,荧光值与药物浓度成正比,检测限为0.13,定量限为0.44 ng/mL,成功测定了TEDP在药物剂型和人血浆中的含量,平均%回收率分别为100.49±1.32和99.40±2.18。结论:所建立的数据与有效的方法吻合较好。该方法根据ICH指南进行了纯度和剂型测定,并根据FDA工业指南,生物分析方法验证用于测定人血浆中TEDP。
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引用次数: 0
Mangifera indica Leaves Extracts Mitigate Experimentally Induced Oxidative Stress and Iron-Overload via Iron Chelation and Modulation of HO-1, Nrf2, and MMP-9 芒果叶提取物通过铁螯合和调控HO-1、Nrf2和MMP-9减轻实验性诱导的氧化应激和铁超载
Pub Date : 2020-12-28 DOI: 10.21608/aprh.2020.42333.1115
Ahmed G. Abd Elhameed, Sara N. Suliman, Marwa Elsbaey, Mai M. Elnaggar, F. Badria
Objective: The current study aimed to investigate and compare the efficiency of the total extract and ethyl acetate (EtOAc) extract of Mangifera indica leaves to attenuate iron overload-induced hepatic and splenic dysfunctions, using an in-vivo iron-overload rat model. Methods: Rats received water supplemented with iron for 2 months, followed by treatment with either total extract or EtOAc extract of M. indica leaves for an extra 2 months. Results: Rats treated with EtOAc fraction of M. indica leaves, and the total extract, had significantly diminished iron accumulation within hepatic and splenic tissues. Both extracts normalized the hepatic enzymatic and non-enzymatic biomarkers like alkaline phosphatase (ALP), alanine aminotransferase (AST), and total bilirubin. Moreover, they restored the oxidants/antioxidants balance within the liver and spleen tissues. Additionally, they suppressed HO-1 levels, increased Nrf2 expression, and downregulated MMP-9 expression. Conclusion: Briefly, M. indica extracts showed iron-chelation, antioxidant, and antifibrotic potentials. These findings pointed out the usefulness of the mango leaves as a natural, affordable by-product in managing iron overload complications. However, the results also demonstrated that EtOAc extract is more accountable for such activities.
目的:采用体内铁超载大鼠模型,研究芒果叶总提取物和乙酸乙酯(EtOAc)提取物对铁超载诱导的肝脏和脾脏功能障碍的缓解作用,并进行比较。方法:大鼠先饮水加铁2个月,然后再用籼稻叶总提取物或乙酸乙酯提取物治疗2个月。结果:大鼠给予籼米叶乙酸乙酯提取物和总提取物后,肝脏和脾脏组织内铁积累明显减少。两种提取物均使肝脏酶和非酶生物标志物如碱性磷酸酶(ALP)、丙氨酸转氨酶(AST)和总胆红素正常化。此外,他们还恢复了肝脏和脾脏组织中氧化剂/抗氧化剂的平衡。此外,它们抑制HO-1水平,增加Nrf2表达,下调MMP-9表达。结论:籼稻提取物具有铁螯合、抗氧化和抗纤维化的作用。这些发现指出,芒果叶作为一种天然的、负担得起的副产品,在处理铁超载并发症方面是有用的。然而,结果也表明,EtOAc提取物更负责这些活动。
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引用次数: 1
Development of a Method for the Determination of Miconazole in Water Samples Using Gas Chromatography Mass Spectrometry 气相色谱-质谱法测定水样中咪康唑的方法研究
Pub Date : 2019-10-01 DOI: 10.21608/aprh.2019.15686.1089
M. Ibrahim, A. Y. Mohamed, A. A. Ahmed
This paper describes an enhanced gas chromatography mass spectrometry (GC-MS) strategy for the analysis of Miconazole in water samples. In this study, determination of Miconazole has been carried out according to standard method for water and waste water analysis. Samples of collected water were agriculture stream water, River Nile water and Hospital waste water samples from El-Gharbia governorate in Egypt. Miconazole was extracted by solid - liquid extraction and analyzed by GC-MS. The chromatographic separation was performed using a ZB5 column (30 m ×0.53 mm, 1.50 µm), and helium as a carrier gas. The limit of detection and limit of quantification for Miconazole were 0.75and 2.50 ng/mL respectively. The intra- and inter-day precisions were lower than 0.85% while the accuracy ranged from 98.55% to 101.53. Finally, solid phase extraction (SPE) in combination with GC-MS is a sensitive and effective method for the determination of Miconazole in water samples.
本文介绍了水样中咪康唑的气相色谱-质谱分析方法。本研究按照水、废水分析标准方法进行了咪康唑的测定。收集的水样本是来自埃及加尔比亚省的农业溪流、尼罗河水和医院废水样本。采用固液萃取法提取咪康唑,GC-MS分析。采用ZB5色谱柱(30 m ×0.53 mm, 1.50µm),氦气为载气进行色谱分离。咪康唑的检出限为0.75 ng/mL,定量限为2.50 ng/mL。日内、日间精密度均低于0.85%,准确度在98.55% ~ 101.53之间。最后,固相萃取-气相色谱-质谱联用是测定水样中咪康唑的一种灵敏、有效的方法。
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引用次数: 0
Pharmacokinetics of Tacrolimus in Egyptian Liver Transplant Recipients: Role of the Classic Co-variables 他克莫司在埃及肝移植受者体内的药代动力学:经典协变量的作用
Pub Date : 2019-10-01 DOI: 10.21608/aprh.2019.14237.1087
Abdel-hamid Ebid, S. Mohamed, A. Mira, A. Saleh
Objectives: This work was performed to study the pharmacokinetics of tacrolimus in adult liver transplant recipients after optimization of all the known classic factors contributing to inter-patient variability in whole blood tacrolimus levels. Also, to detect if any variability in whole blood tacrolimus levels still exists or this variability is only a function of the classic co-variables so that their optimization will diminish or eliminate it. Methods: Twenty-Six male patients with end-stage liver disease undergoing living donor liver transplantation were selected from the Gastroenterology Department of the International Medical Center, Cairo, Egypt, were enrolled in the study. A patient is initially considered to be a candidate for this study when tacrolimus was indicated as a part of a triple immune suppressive regimen with mycophenolate mofetil and prednisolone. Patients were selected to have non-significant variations in their demographics and pretreatment clinical data. Blood samples were drawn from each patient before the morning dose at specified intervals and the whole blood was assayed for tacrolimus, using Chemiluminescent Microparticle Immunoassay method (CMIA). Six months after liver transplantation, patients were classified into 3 groups based on their tacrolimus trough levels; normalized by its daily dose (C/D ratio), into fast, intermediate and slow metabolizers. Results: The results revealed unpredictable variability in whole blood tacrolimus levels among patients at each sampling time and a marked inter-patient variability in mean whole blood tacrolimus levels among individuals throughout the six months post transplantation period, (P value: <0.0001). Considerable inter-patient variability was also evident in tacrolimus pharmacokinetics. During 1st month post-transplant, tacrolimus C/D ratio varied from 0.53 to 12.2 (ng/ml*1/mg) and tacrolimus oral clearance (CL/F) varied from 3.4 to 79.4 L/hr. At 3rd month post-transplant, tacrolimus C/D ratio varied from 0.78 to 8.50 (ng/ml*1/mg) and tacrolimus CL/F varied from 4.9 to 53.2 L/hr. At 6th month post-transplant, tacrolimus C/D ratio varied from 0.73 to 7.10 (ng/ml*1/mg) and tacrolimus CL/F varied from 5.9 to 56.8 L/hr. The overall mean C/D ratio and oral clearance also showed a great variability among patients with a mean of 2.80±1.89 (CV: 67.5%) and 21.3±12.9 (CV:60.7%), respectively. Conclusion: The variability in whole blood tacrolimus concentrations and tacrolimus pharmacokinetics existed in spite of careful patient selection and optimization of all the classic co-variables known to affect tacrolimus concentrations, suggesting the presence of other unstudied factors; the recently evolving genetic factors might contribute to this variability. It is recommended to still considering therapeutic drug monitoring as an integral part of tacrolimus therapy to control variations in response until the discovery of a model that considers all the expected covariates to predict the respo
目的:在优化所有已知的影响他克莫司全血水平差异性的经典因素后,研究他克莫司在成人肝移植受者体内的药代动力学。同时,检测全血他克莫司水平的变异性是否仍然存在或者这种变异性仅仅是经典协变量的一个函数因此它们的优化将减少或消除它。方法:选取埃及开罗国际医学中心消化科26例接受活体供肝移植的男性终末期肝病患者。当他克莫司与霉酚酸酯和强的松龙联合使用三重免疫抑制方案时,患者最初被认为是本研究的候选者。选择的患者在人口统计学和预处理临床数据方面没有显著差异。在给药前每隔一段时间抽取患者血样,采用化学发光微粒免疫分析法(CMIA)检测全血中他克莫司的含量。肝移植后6个月,根据患者的他克莫司谷值将患者分为3组;按日剂量(C/D比)归一化,分为快、中、慢代谢产物。结果:结果显示,在每个采样时间,患者的全血他克莫司水平存在不可预测的变异性,在移植后6个月内,个体的平均全血他克莫司水平存在显著的患者间变异性(P值:<0.0001)。他克莫司的药代动力学也有明显的患者间差异。移植后1个月,他克莫司C/D比值为0.53 ~ 12.2 (ng/ml*1/mg),他克莫司口服清除率(CL/F)为3.4 ~ 79.4 L/hr。移植后3个月,他克莫司C/D比值为0.78 ~ 8.50 (ng/ml*1/mg),他克莫司CL/F为4.9 ~ 53.2 L/hr。移植后6个月,他克莫司C/D比值为0.73 ~ 7.10 (ng/ml*1/mg),他克莫司CL/F为5.9 ~ 56.8 L/hr。患者的总体平均C/D比和口服清除率也表现出很大的差异,分别为2.80±1.89 (CV: 67.5%)和21.3±12.9 (CV:60.7%)。结论:尽管对已知影响他克莫司浓度的所有经典协变量进行了仔细的患者选择和优化,但全血他克莫司浓度和他克莫司药代动力学仍存在变异性,提示存在其他未研究的因素;最近进化的遗传因素可能有助于这种变异性。建议仍将治疗药物监测作为他克莫司治疗的一个组成部分,以控制反应的变化,直到发现一个考虑所有预期协变量的模型来预测反应。
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引用次数: 3
Phytochemical Investigation and Assessment of Antioxidant, Antimicrobial and Cytotoxic Activities of the Root Bark Chrozophora oblongifolia (Delile) Spreng. (Euphorbiaceae) 根皮抗氧化、抗菌和细胞毒活性的植物化学研究与评价。(大戟科)
Pub Date : 2019-10-01 DOI: 10.21608/aprh.2019.17219.1090
M. R. Kamel, A. M. Nafady, A. Hassanein, R. Ragaey, E. Haggag
antioxidant, antimicrobial and cytotoxic activities of the total methanolic extract and different fractions of Chrozophora oblongifolia root bark. Methods: Phytochemical screening of Chrozophora oblongifolia was performed using specific test for each class of compounds. Different chromatographic techniques were used to isolate and purify compounds and their structures were elucidated by using different 1D-NMR spectroscopy (1H NMR and 13C NMR). The antioxidant activity was evaluated using DPPH radical scavenging assay, antimicrobial activity was done by standard agar well diffusion assay and cytotoxic activity was performed by using MTT colorimetric assay method. Results: Phytochemical investigation of chrozophora oblongifolia revealed the presence ofcarbohydrates and / or glycosides, sterols and or triterpene, alkaloids, tannins and saponins and the absence of flavonoids and anthraquinones. After fractionation,   methyl gallate (1), gallic acid (2) and β-sitosterol-3-O-β-D- glucopyranoside (3) were isolated from ethyl acetate fractions. The result of the antioxidant activity showed that, the ethyl acetate fraction showed highest antioxidant activity followed by n-butanol and total methanolic extract. The result of the antimicrobial activity showed that, the total methanolic extract and ethyl acetate fraction showed moderate activity against Staphylococcus aureus, Vancomycin resistant Staphylococcus aureus and Candida albicans. The result of the cytotoxic activity showed that, the methylene chloride fraction followed by the total methanolic extract showed the highest cytotoxic activity against (MCF-7 and Huh-7) cancer cell lines. Conclusion: The root bark of Chrozophora oblongifolia is a rich source of different classes of active constituents as phenolics. The total extract and some fractions of Chrozophora oblongifolia showing antioxidant and antimicrobial and cytotoxic activities.
黄皮总甲醇提取物及不同部位抗氧化、抑菌和细胞毒活性的研究。方法:采用对每一类化合物进行特异性试验的方法,对黄参进行植物化学筛选。采用不同的色谱技术对化合物进行分离纯化,并利用不同的1D-NMR (1H NMR和13C NMR)对化合物结构进行了鉴定。用DPPH自由基清除法测定其抗氧化活性,用标准琼脂孔扩散法测定其抗菌活性,用MTT比色法测定其细胞毒活性。结果:经植物化学鉴定,黄花参中含有碳水化合物和/或糖苷、甾醇和/或三萜、生物碱、单宁和皂苷,不含黄酮类和蒽醌类化合物。从乙酸乙酯中分离得到没食子酸甲酯(1)、没食子酸(2)和β-谷甾醇-3- 0 -β- d -葡萄糖吡喃苷(3)。抗氧化活性结果表明,乙酸乙酯部位抗氧化活性最高,其次为正丁醇部位和总甲醇部位。抑菌活性结果表明,总甲醇提取物和乙酸乙酯部位对金黄色葡萄球菌、耐万古霉素金黄色葡萄球菌和白色念珠菌具有中等抑菌活性。细胞毒活性结果表明,二氯甲烷部位对MCF-7和Huh-7癌细胞的细胞毒活性最高,其次是总甲醇提取物。结论:桔梗根皮中含有丰富的酚类活性成分。黄花总提取物及部分部位具有抗氧化、抑菌和细胞毒活性。
{"title":"Phytochemical Investigation and Assessment of Antioxidant, Antimicrobial and Cytotoxic Activities of the Root Bark Chrozophora oblongifolia (Delile) Spreng. (Euphorbiaceae)","authors":"M. R. Kamel, A. M. Nafady, A. Hassanein, R. Ragaey, E. Haggag","doi":"10.21608/aprh.2019.17219.1090","DOIUrl":"https://doi.org/10.21608/aprh.2019.17219.1090","url":null,"abstract":"antioxidant, antimicrobial and cytotoxic activities of the total methanolic extract and different fractions of Chrozophora oblongifolia root bark. Methods: Phytochemical screening of Chrozophora oblongifolia was performed using specific test for each class of compounds. Different chromatographic techniques were used to isolate and purify compounds and their structures were elucidated by using different 1D-NMR spectroscopy (1H NMR and 13C NMR). The antioxidant activity was evaluated using DPPH radical scavenging assay, antimicrobial activity was done by standard agar well diffusion assay and cytotoxic activity was performed by using MTT colorimetric assay method. Results: Phytochemical investigation of chrozophora oblongifolia revealed the presence ofcarbohydrates and / or glycosides, sterols and or triterpene, alkaloids, tannins and saponins and the absence of flavonoids and anthraquinones. After fractionation,   methyl gallate (1), gallic acid (2) and β-sitosterol-3-O-β-D- glucopyranoside (3) were isolated from ethyl acetate fractions. The result of the antioxidant activity showed that, the ethyl acetate fraction showed highest antioxidant activity followed by n-butanol and total methanolic extract. The result of the antimicrobial activity showed that, the total methanolic extract and ethyl acetate fraction showed moderate activity against Staphylococcus aureus, Vancomycin resistant Staphylococcus aureus and Candida albicans. The result of the cytotoxic activity showed that, the methylene chloride fraction followed by the total methanolic extract showed the highest cytotoxic activity against (MCF-7 and Huh-7) cancer cell lines. Conclusion: The root bark of Chrozophora oblongifolia is a rich source of different classes of active constituents as phenolics. The total extract and some fractions of Chrozophora oblongifolia showing antioxidant and antimicrobial and cytotoxic activities.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85148087","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
A Phytochemical and Biological Review on Plants of The family Aizoaceae 菊科植物的植物化学和生物学研究进展
Pub Date : 2019-10-01 DOI: 10.21608/aprh.2019.12303.1083
Khayrya A. Youssif, Ali M Elshamy, M. Rabeh, Nagwan M. Gabr, E. Haggag
Objectives: This study is aimed to be a comprehensive review of the phytochemical constituents and biological activities of Aizoaceae family plants (Mesembryanthemaceae). Methods: This study is covering articles between 1969 and 2018, reviewed from internationally accepted databases and scientific data from scientific Journals. Results: Phytochemically studied plants of family Aizoaceae have shown the presence of various classes of compounds including; alkaloids, triterpenes, sterols, lignans, phenolic compounds, betacyanins, and essential oils. Biological studies on plants of family Aizoaceae have indicated various bioactive potentials including antioxidant, antidiabetic, antimicrobial, antitumor, hepatoprotective, anti-inflammatory and other effects. The reported medicinal plants of family Aizoaceae were selected and summarized on the basis of their; phytochemical constituents and biological activities. Conclusion: The results of this study may inspire further ethno-botanical and ethno-pharmacological research and investigations toward drug discovery.
前言:目的:本文对菊科植物的化学成分和生物活性进行了综述。方法:本研究涵盖了1969年至2018年之间的文章,从国际公认的数据库和科学期刊的科学数据中进行了审查。结果:经植物化学研究,菊科植物中含有多种化合物,包括;生物碱、三萜、甾醇、木脂素、酚类化合物、甜菜花青素和精油。生物学研究表明,菊科植物具有抗氧化、抗糖尿病、抗菌、抗肿瘤、保肝、抗炎等多种生物活性。对已报道的菖蒲科药用植物进行了分类和总结;植物化学成分和生物活性。结论:本研究结果可为进一步开展民族植物学和民族药理学研究及药物开发提供参考。
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引用次数: 3
Phytochemical Investigation and Assessment of Antioxidant and Antimicrobial Activities of Phagnalon barbeyanum Aerial Parts barbeyanphagnalon barbeyanairparts植物化学研究及抗氧化、抗菌活性评价
Pub Date : 2019-07-10 DOI: 10.21608/APRH.2019.13691.1084
M. R. Kamel, A. M. Nafady, A. Hassanein, R. Ragaey, E. Haggag
Objectives: The present study aimed to investigate and isolate different phytochemical constituents and assess the antioxidant and antimicrobial activities of the total methanol extract and different fractions of Phagnalon barbeyanum aerial parts. Methods: Phytochemical screening of Phagnalon barbeyanum aerial parts was performed using specific test for each class of compounds. Different chromatographic techniques were used to isolate and purify compounds and their structures were elucidated by using different spectral techniques (1H NMR and 13C NMR). The antioxidant activity was evaluated by DPPH radical scavenging assay and antimicrobial activity was done by standard agar well diffusion assay. Results: Phytochemical investigation of Phagnalon barbeyanum aerial partswas done forthe presence ofcarbohydrates and or glycosides, sterols and or triterpene, flavonoids, tannins and saponins and revealed the absence of alkaloids and anthraquinones. Compounds; β-sitosterol (1), apigenin (2) and β-sitosterol-3-O-β-D- glucopyranoside (3) were isolated from methylene chloride and ethyl acetate fractions. The ethyl acetate fraction showed highest antioxidant activity followed by n-butanol and methylene chloride fractions. The total methanol extract and n-hexane fractions showed lowest antioxidant activity. The ethyl acetate fraction and total methanol extract showed moderate activity against Staphylococcus aureus and Vancomycin resistant Staphylococcus aureus. Conclusion: The aerial parts of Phagnalon barbeyanum is a rich source of different classes of active constituents as phenolics. The total methanol extract of Phagnalon barbeyanum aerial parts and some of its fractionated concentrates could be considered as antioxidant and antimicrobial agents.
目的:研究和分离巴贝飞天部位总甲醇提取物和不同部位的不同化学成分,并评价其抗氧化和抗菌活性。方法:采用对每一类化合物进行特异性试验的方法,对巴贝飞天部位进行植物化学筛选。采用不同的色谱技术分离纯化化合物,并采用不同的光谱技术(1H NMR和13C NMR)对化合物结构进行了鉴定。用DPPH自由基清除法测定其抗氧化活性,用标准琼脂孔扩散法测定其抑菌活性。结果:对barbeyanum气相部分进行了植物化学分析,主要成分为碳水化合物和苷类、甾醇和三萜、黄酮类、单宁类和皂苷类,不含生物碱和蒽醌类。化合物;从二氯甲烷和乙酸乙酯中分离得到β-谷甾醇(1)、芹菜素(2)和β-谷甾醇-3- 0 -β- d -葡萄糖吡喃苷(3)。乙酸乙酯部位抗氧化活性最高,其次是正丁醇部位和二氯甲烷部位。总甲醇提取物和正己烷提取物的抗氧化活性最低。乙酸乙酯部分和总甲醇提取物对金黄色葡萄球菌和耐万古霉素金黄色葡萄球菌具有中等活性。结论:barbeyanphagnalon barbeyanum的地上部分含有丰富的酚类活性成分。barbeyanum地上部分总甲醇提取物及其部分分馏浓缩液可作为抗氧化和抗菌药物。
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引用次数: 1
Validated HPLC Determination of the Potential Anti-Helicobacter pylori, Lepidine, in Lepidium sativum Seeds Assessed by Molecular Docking Study 高效液相色谱法测定枸杞种子中潜在的抗幽门螺杆菌碱的分子对接研究
Pub Date : 2019-07-01 DOI: 10.21608/APRH.2019.14036.1085
A. Haddad, W. Al-Shareef, S. Eid
Background: Nearly 50 % of the world residents are known to be infected with Helicobacter pylori which is the main cause of peptic ulcer and gastric cancer. Since resistance to the currently used treatments, other alternative approaches such as combination with natural products should be tried. Objectives: In this work, validated HPLC-UV method was developed for quantification of lepidine content in various extracts and crude oil of Lepidium sativum seeds. Furthermore, antibacterial activity of lepidine against H. pylori was compared with standard antibiotics supported by molecular docking study. Methods: Different solvents were used to extract lepidine as well as the contents were determined using HPLC-UV method. Anti-Helicobacter pylori activity was examined using agar diffusion and dilution methods. Molecular docking study was done on H. pylori phosphoribosyltransferase enzyme. Results: The highest content of lepidine (316.91 µg mL-1) was found in n-hexane extract. Lepidine exhibit antibacterialeffect (MIC = 6.25 µg mL-1) against H. pylori clinical isolates. The ability of lepidine to interact with amino acids in the phosphoribosyl transferase binding site might rationalize its observed activity. Conclusion: Our results demonstrate for the first time the anti-Helicobacter pylori activity of lepidine, which could therefore be developed as viable nutraceutical agent. Further investigations are required to formulate suitable pharmaceuticals to combat with the H. pylori infections on clinical grounds.
背景:已知世界上近50%的居民感染幽门螺杆菌,幽门螺杆菌是导致消化性溃疡和胃癌的主要原因。由于目前使用的治疗方法存在耐药性,因此应尝试其他替代方法,如与天然产品结合使用。目的:建立高效液相色谱-紫外分光光度法定量测定枸杞种子各种提取物和粗提物中枸杞碱的含量。通过分子对接研究,比较了韭素对幽门螺杆菌的抑菌活性。方法:采用不同溶剂提取麻风碱,采用高效液相色谱-紫外分光光度法测定其含量。用琼脂扩散法和稀释法检测抗幽门螺杆菌活性。对幽门螺杆菌磷酸核糖基转移酶进行了分子对接研究。结果:正己烷提取物中麻风碱含量最高,为316.91µg mL-1;Lepidine对幽门螺杆菌临床分离株具有抗菌作用(MIC = 6.25µg mL-1)。lepidine与磷酸核糖基转移酶结合位点的氨基酸相互作用的能力可能使其观察到的活性合理化。结论:本研究首次证实了槲皮素具有抗幽门螺杆菌的活性,可作为一种可行的营养保健剂开发。需要进一步的研究,以制定合适的药物,以对抗幽门螺杆菌感染的临床理由。
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引用次数: 4
In Vitro Anticlastogenic and Antioxidant properties of extracted and Pure form of Curcumin against Mitomycin C in Human Peripheral Leukocytes 姜黄素提取物和纯物对人外周血白细胞丝裂霉素C的体外抗裂和抗氧化作用
Pub Date : 2019-07-01 DOI: 10.21608/APRH.2019.10241.1080
Puspal De, M. Mukhopadhyay
Objectives: Turmeric is native to India and is widely used in Indian cuisine. Curcumin, the active principle of turmeric used primarily as a coloring agent in food, drug and cosmetics. The medicinal properties of curcumin are well known in ancient Indian Ayurvedic Medicine. Mitomycin C (MMC) is an antineoplastic agent used to fight a number of different cancers including cancer of the stomach, colon, rectum, pancreas, breast, lung, uterus, cervix, bladder, head, neck, eye and esophagus. It is a potent DNA cross-linker. But it has severe side effect, the prolonged use of the drug may result in permanent bone marrow damage and other various types of secondary tumors in normal cells. The present study was conducted to examine the anticlastogenic action of extracted curcumin from dry turmeric and pure curcumin against the MMC-induced chromosomal aberrations. For this purpose, in the present study, clastogenic parameter like chromosomal aberration test was conducted in peripheral human leukocytes. Methods: The antioxidant property of both extracted and pure curcumin was also evaluated by phosphomolybdenum method. Results: Our results demonstrated that, extracted as well as pure Curcumin, a strong antioxidant phyto-molecule is effective in counteracting the clastogenicity in human leukocyte in vitro. Conclusion: These results suggest that the use of turmeric in diet may be an effective protection against the health crisis generated by harmful agents.
目的:姜黄原产于印度,在印度菜中被广泛使用。姜黄素是姜黄的活性成分,主要用作食品、药品和化妆品的着色剂。姜黄素的药用特性在古印度阿育吠陀医学中是众所周知的。丝裂霉素C (MMC)是一种抗肿瘤药物,用于对抗多种不同的癌症,包括胃癌、结肠癌、直肠癌、胰腺癌、乳腺癌、肺癌、子宫癌、子宫颈癌、膀胱癌、头颈癌、眼癌和食道癌。它是一种有效的DNA交联剂。但它有严重的副作用,长期使用该药可能导致永久性骨髓损伤和正常细胞中其他各种类型的继发性肿瘤。研究了干姜黄提取物和纯姜黄素对mmc诱导的染色体畸变的抗裂作用。为此,本研究在人外周血白细胞中进行了染色体畸变等致裂参数试验。方法:采用磷钼法对姜黄素提取液和纯姜黄素的抗氧化性能进行评价。结果:我们的研究结果表明,姜黄素提取物和纯姜黄素是一种强抗氧化植物分子,可以有效地对抗体外人白细胞的致裂性。结论:在饮食中添加姜黄可有效预防有害物质对人体健康的危害。
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引用次数: 1
Synthesis and Biological Evaluation of Certain α,β-Unsaturated Ketones and their Corresponding Fused Pyridines 某些α,β-不饱和酮及其融合吡啶的合成与生物学评价
Pub Date : 2019-07-01 DOI: 10.21608/aprh.2019.10458.1081
A. Hassan, H. el-Hifnawi, W. Ahmed
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引用次数: 1
期刊
Journal of Advanced Pharmacy Research
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