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Optimized and validated stability indicating RP-UPLC method for the determination of famotidine in pharmaceutical formulations 优化并验证了RP-UPLC法莫替丁含量测定方法的稳定性
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.003
Tummala Vijaya Bhaskara Reddy, Nallagari Sowjanya Reddy, Sanivarapu Ravi Prakash Reddy, Golkonda Ramu, Chintala Rambabu

Background

Famotidine (FMD) is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease and gastro esophageal reflux disease. The main objective of the present investigation is to develop a rapid, precise and accurate stability indicating ultra performance liquid chromatographic method for the analysis of pharmaceutical formulations.

Methods

Waters-Alliance Ultra Performance Liquid Chromatographic system equipped with Auto Sampler, PDA detector, detection at a wavelength of 297 nm, Symmetry C18 (2.1 × 50 mm, 1.7 μm, Make: BEH) column and mobile phase of potassium dihydrogen phosphate buffer of pH = 7.0 and acetonitrile in the ratio 40:60 v/v at a flow rate of 0.2 per minute was used for the assay of famotidine in tablets by a reverse phase ultra performance liquid chromatographic method (RP-UPLC).

Results and discussion

The system suitable parameters such as tailing factor and theoretical plate count were found to 1.48 and 8896 respectively under the optimized experimental conditions. The retention time of the compound was observed to be 0.595 min. The developed method was proved to be precise and accurate by calculating percent of relative standard deviation (% RSD is equal to 0.900%) for six replicate injections and mean recovery (99.8%) of famotidine at three different concentration levels. Linearity between peak area and concentration was found to be 5.0–20.0 μg/mL. The limit of detection (LOD) and limit of quantitation (LOQ) values were found to be 0.006 μg/mL and 0.02 μg/mL respectively. The drug was found to be stable (81.37%–93.44%) under different degradation conditions like acid (0.1 N HCl), alkali (0.1 N NaOH), peroxide (3% H2O2), photolytic and thermal.

Conclusions

The developed method was found to be simple, rapid, repeatable, reproducible, robust, rugged and economic hence it can be used as a new analytical method for the analysis of pharmaceutical formulations in any pharmaceutical industries.

法莫替丁(FMD)是一种抑制胃酸产生的组胺h2受体拮抗剂,常用于治疗消化性溃疡病和胃食管反流病。本研究的主要目的是建立一种快速、精确、准确、稳定性指示的超高效液相色谱分析方法。MethodsWaters-Alliance超高液相色谱系统配备自动取样器,PDA检测器,检测波长297 nm,对称C18(2.1×50毫米,1.7μm,:本·)列和磷酸二氢钾缓冲液的流动相pH = 7.0和乙腈比例40:6 0 v / v 0.2每分钟的流量是用于测定法莫替丁在平板电脑市场的反向阶段超高效液相色谱测定方法(RP-UPLC)。结果与讨论在优化的试验条件下,系统的适宜参数尾矿系数和理论板数分别为1.48和8896。法莫替丁在3种不同浓度下的平均回收率(99.8%)和6次重复注射的相对标准偏差(% RSD = 0.900%)证明了该方法的精密度和准确性。峰面积与浓度呈5.0 ~ 20.0 μg/mL的线性关系。检测限和定量限分别为0.006 μg/mL和0.02 μg/mL。在酸(0.1 N HCl)、碱(0.1 N NaOH)、过氧化物(3% H2O2)、光解和热降解条件下,该药物的稳定性为81.37% ~ 93.44%。结论该方法简便、快速、重复性好、可重复性好、稳健性好、经济可靠,可作为一种新的分析方法,应用于各医药行业的制剂分析。
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引用次数: 7
Physiochemical analysis and HPLC-PDA method for quantification of stigmasterol in Dipteracanthus patulus (Jacq.) Nees 双棘豆中豆甾醇的理化分析及HPLC-PDA定量方法需要雇
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.014
Kannikaparameswari Nachimuthu , Chinnaswamy Palaniswamy

Background

Plant-based foods provide, not only essential nutrients needed for life, but also other bioactive compounds for health promotion and disease prevention. Standardization is an essential measure of quality, purity and authenticity. The present study focuses on the investigation of physiochemical parameters and to identify and quantify Stigmasterol from the leaves of Dipteracanthus patulus (Jacq.) Nees.

Methods

Physiochemical analyses like total ash, acid insoluble ash, water soluble ash, moisture content (Loss on Drying) and extractive values were calculated by standard procedures. High performance liquid chromatography with photo diode array detector (HPLC-PDA) was used to quantify Stigmasterol in the methanolic leaves extract of D. patulus.

Results

The percentage of the total ash, acid insoluble ash, water soluble ash and moisture content (Loss on Drying) were 9.1%, 1.3%, 6.2% and 4.1% respectively. The methanolic extractive value was found to be higher (13.4%). HPLC analysis revealed that the methanolic leaves extract showed the presence of Stigmasterol and the content was 0.22 mg/g dry weight which supports the biological potency of the plant.

Conclusion

Physiochemical analyses have shown the purity and quality of crude drug. Quantitative estimation by HPLC-PDA revealed the presence of good percentage of stigmasterol in D. patulus. This study has grasped the importance since stigmasterol possesses lipid peroxidation inhibitory action and anticancer activity. These features make this plant a promising candidate for the further studies on isolation and pharmacological studies of this compound from D. patulus.

植物性食物不仅提供生命所需的必需营养素,还提供促进健康和预防疾病的其他生物活性化合物。标准化是质量、纯度和真实性的重要衡量标准。本文主要研究了双翅蕨叶中豆甾醇的理化参数,并对其进行了鉴定和定量。需要雇。方法按标准程序计算总灰分、酸不溶灰分、水溶性灰分、水分含量(干燥损失)和萃取物等理化指标。采用高效液相色谱-光电二极管阵列检测器(HPLC-PDA)定量分析了苍蝇子甲醇叶提取物中豆甾醇的含量。结果总灰分、酸不溶灰分、水溶性灰分和干燥损失率分别为9.1%、1.3%、6.2%和4.1%。甲醇提取值较高(13.4%)。高效液相色谱分析表明,甲醇叶提取物中含有豆甾醇,含量为0.22 mg/g干重,支持该植物的生物效力。结论理化分析表明该药材纯度高,质量可靠。高效液相色谱- pda定量分析表明,苍蝇拍中含有较高比例的豆甾醇。由于豆甾醇具有抑制脂质过氧化作用和抗癌活性,因此这项研究具有重要意义。这些特征使该植物成为进一步研究该化合物分离和药理研究的有希望的候选植物。
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引用次数: 1
Antioxidant property of Grewia serrulata DC and its hypoglycemic effect on normal and hyperglycemic rats 山参的抗氧化性能及其对正常和高血糖大鼠的降血糖作用
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.004
Irisappan Sarath Chandiran , Korlakunta Narasimha Jayaveera , Karimulla Shaik

Aim

The present study was aimed to evaluate the antioxidant property and hypoglycemic activity of aqueous and ethanolic extracts of aerial parts of Grewia serrulata DC (AEGS & EEGS) in normal and hyperglycemic male Wistar Albino rats.

Methods

The antioxidant property was evaluated both in vitro and in vivo model using standard procedures. The hypoglycemic activity was evaluated by normal glucose and oral glucose tolerance test (NG-OGTT) method and by acute administration of AEGS and EEGS extracts at doses 200 and 400 mg/kg body wt p.o in Streptozotocin (STZ) induced hyperglycemic rats.

Results

The ethanolic extract of Grewia serrulata DC exhibited strong free radical scavenging activity as evidenced by their low IC50 values in DPPH (1,1-diphenyl-2-picryl-hydrazyl) (9.16 ± 1.05 μg/ml), Superoxide (35.59 ± 1.6805 μg/ml) and nitric oxide (151.80 ± 1.79 μg/ml) methods. In in vivo study, treatment with ethanolic extract at both doses shows a significant dose dependent increase (p < 0.05 to p < 0.001) in the levels of superoxide dismutase (SOD) and Catalase (CAT) and a significant decrease (p < 0.05 to p < 0.001) in the levels of Thiobarbituric acid reactive substances (TBARS), when compared to CCl4 treated control in both liver and kidney. In NG-OGTT method EEGS shows reduction in glucose levels in normal rats and glucose loaded hyperglycemic rats and in STZ-induced hyperglycemic rats.

Conclusion

EEGS was found to possess strong antioxidant activity and good hypoglycemic activity compared to that of AEGS.

目的研究山黧豆(Grewia serrulata DC, aags &正常和高血糖雄性Wistar白化大鼠的脑电图。方法采用标准方法对其体外和体内模型的抗氧化性能进行评价。采用正常血糖和口服糖耐量试验(NG-OGTT)法,并分别以200和400 mg/kg体wt p.o剂量急性给予链脲佐菌素(STZ)诱导的高血糖大鼠,观察其降血糖活性。结果木参醇提物对DPPH(1,1-二苯基-2-苦味酰肼)(9.16±1.05 μg/ml)、超氧化物(35.59±1.6805 μg/ml)和一氧化氮(151.80±1.79 μg/ml)的IC50值较低,具有较强的自由基清除活性。在体内研究中,两种剂量的乙醇提取物均显示出显著的剂量依赖性增加(p <0.05至p <0.001),超氧化物歧化酶(SOD)和过氧化氢酶(CAT)水平显著降低(p <0.05至p <0.001)硫代巴比妥酸反应性物质(TBARS)的水平,与CCl4处理的肝脏和肾脏对照组相比。在NG-OGTT方法中,脑电图显示正常大鼠、葡萄糖负荷高血糖大鼠和stz诱导的高血糖大鼠的葡萄糖水平降低。结论eegs具有较强的抗氧化活性和较好的降糖活性。
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引用次数: 3
Development and evaluation of Nanostructured Lipid Carrier (NLC) based topical delivery of an anti-inflammatory drug 基于纳米结构脂质载体(NLC)的抗炎药物局部递送的开发和评价
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.020
Atul Anand Phatak , Praveen Digambar Chaudhari

Aims

The work is aimed to formulate aqueous nanodispersion of aceclofenac Nanostructured Lipid Carriers (NLC) by using modified hot sonication method and to prepare NLC based gel for topical delivery of aceclofenac.

Methods

The lipids incorporated in the study were Compritol 888 ATO and Miglyol and the emulsifier/stabilizer used was Polysorbate 80. The formulations were optimized by using 3 factor, 3 levels, Box–Behenken design. The independent variables were combination of lipids (% w/w), concentration of emulsifier (% w/v), lipid drug ratio and the response variables were particle size, percentage entrapment and drug release after 12 h. The formulations were also characterized for particle size, entrapment efficiency, drug loading and depression in melting point.

Results

The DSC, FTIR analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by SEM which showed spherical shape of the formulations. Further the formulations were evaluated for in vitro drug permeability study, rheological properties, skin irritation, pharmacodynamic and stability studies.

Conclusion

The pharmacodynamic characteristics of aceclofenac NLC gel with reference to the conventional gel were compared by using Carrageenan induced rat paw edema method. The study showed the promising and stable alternative form for the aceclofenac for topical application.

目的采用改进的热超声方法制备乙酰氯芬酸纳米结构脂质载体(NLC)的水相分散体,并制备以NLC为基础的醋酸氯芬酸外用凝胶。方法本研究采用的脂类为Compritol 888 ATO和Miglyol,乳化剂/稳定剂为聚山梨酯80。采用3因素3水平Box-Behenken设计对配方进行优化。自变量为脂质组合(% w/w)、乳化剂浓度(% w/v)、脂质药物比,响应变量为粒径、包封率和12 h后药物释放量,并对其粒径、包封效率、载药量和熔点降低进行表征。结果DSC、FTIR分析表征了药物和脂质修饰的状态。通过扫描电镜对配方的形状和表面形貌进行了测定,结果表明配方为球形。进一步对制剂进行了体外药物渗透性研究、流变学特性、皮肤刺激、药效学和稳定性研究。结论采用卡拉胶诱导大鼠足部水肿法,比较了乙酰氯芬酸NLC凝胶与常规凝胶的药效学特性。研究结果表明,乙酰氯芬酸外用的替代剂型具有良好的应用前景和稳定性。
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引用次数: 32
α-Glucosidase enzyme inhibitory and free radical scavenging constituents from Premna tomentosa Linn. 毛蕊花α-葡萄糖苷酶抑制及自由基清除成分研究。
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.013
Sridhar Rao Ayinampudi

A bioassay-guided fractionation and chemical investigation of the whole plant of Premna tomentosa resulted in the isolation and characterization of premnalin (1), along with the known compounds coniferaldehyde (2), syrangaldehyde (3), acetoxy syrangaldehyde (4), lupeol (5), betulin (6), 2-(4-methoxyphenyl)-2-butanone (7), icetexatriene-1 (8), icetexatriene-2 (9). Their structures were established on the basis of extensive spectroscopic such as (IR, MS, 2D NMR) data analysis and by comparison with the spectroscopic data reported in the literature, premnalin (IC50: 12.11 μg/mL) & (SC50: 20.58 μg/mL), acetoxy syrangaldehyde (IC50: 18.41 μg/mL) & (SC50: 20.83 μg/mL) displayed potent α-glucosidase inhibition and free radical scavengers (DPPH).

对毛蕊花全株进行生物测定和化学分析,分离鉴定了毛蕊花苷(1),并鉴定了已知化合物松柏醛(2)、丁香醛(3)、乙氧基丁香醛(4)、芦皮醇(5)、白桦醛(6)、2-(4-甲氧基苯基)-2-丁酮(7)、冰四萜烯-1(8)、冰四萜烯-2(9)。二维核磁共振)数据分析,并与文献报道的光谱数据比较,premnalin (IC50: 12.11 μg/mL) &(SC50: 20.58 μg/mL),乙氧基丁香醛(IC50: 18.41 μg/mL);(SC50: 20.83 μg/mL)具有较强的α-葡萄糖苷酶抑制作用和自由基清除作用。
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引用次数: 2
Development of SOP's and pharmacopoeial standards for Jawarish-e-Jalinoos Jawarish-e-Jalinoos标准操作规程和药典标准的制定
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.022
Rampratap Meena , S. Mageswari , D. Ramasamy , P. Meera Devi Sri , Jameeluddin Ahmed , Shamsul Arfin , Syed Shakir Jamil

Background

Jawarish-e-Jalinoos is a Unani poly herbal compound formulations listed under the Majooniath category in National Formulary of Unani Medicine (NFUM), Part-I. It is used in various ailments such as Zof-e-Aza-Raeesa (weakness of the principle organs like brain, heart and liver), Zof-e-Meda (weakness of the stomach), Nafkh-e-Shikam (flatulence in the stomach) and Khafqan (palpitation).

Aim

Present study was undertaken to develop the Standard Operating Procedure for the preparation of drug Jawarish-e-Jalinoos and to evaluate its pharmacopoeial standards.

Methods

To prepare the drug in different batches at laboratory scale using 18 single drugs were used. The drug was prepared as per the method prescribed in NFUM. To evaluate the pharmacopoeial standards and quality control parameters pharmacognostical, physico-chemical and WHO methods were followed.

Results

Microscopical studies show the presence of various characteristic features of single drugs used in the preparation viz., vessels elements with reticulate, scalariform, pitted; perisperm cells with angular and bulbous projections; pollen grains; fibre like sclereids; septate fibres; starch grains of various shapes and sizes; stone cells with horse shoe shaped thickening; druses of calcium oxalate crystals. The physico-chemical study shows presence of moisture content 19.87%, ash content 0.8% and acid insoluble ash 0.20%. Alcohol and water soluble extractive value of the drug obtained were 40.80% and 62.78% respectively. Other parameters such as heavy metals, microbial load, aflatoxins and pesticidal residues were found within the permissible limit.

Conclusion

The evaluated data from this study will be helpful in laying down the SOP's and pharmacopoeial standards for the drug Jawarish-e-Jalinoos.

jawarish -e- jalinoos是一种乌纳尼多草药复方制剂,列在乌纳尼国家药物处方(NFUM)第一部分的马洛尼亚类下。它被用于各种疾病,如Zof-e-Aza-Raeesa(主要器官如大脑、心脏和肝脏的虚弱)、Zof-e-Meda(胃虚弱)、Nafkh-e-Shikam(胃胀气)和Khafqan(心悸)。本研究旨在制定Jawarish-e-Jalinoos制剂的标准操作程序,并对其药典标准进行评价。方法采用18种单药,在实验室规模下分批次制备该药。本品按《全国药典》规定的方法配制。采用生药学、理化和WHO方法对其药典标准和质量控制参数进行评价。结果显微研究表明,该制剂具有单一药物的多种特征,即血管元件呈网状、鳞片状、凹陷状;外胚乳细胞具角状和球茎状突起;花粉粒;纤维状硬核;有隔膜的纤维;各种形状和大小的淀粉粒;石细胞呈马蹄形增厚;草酸钙晶体的颗粒。理化研究结果表明,其水分含量为19.87%,灰分含量为0.8%,酸不溶性灰分含量为0.20%。所得药物的醇溶萃取值为40.80%,水溶性萃取值为62.78%。其他参数如重金属、微生物负荷、黄曲霉毒素和农药残留均在允许范围内。结论本研究的评价数据可为制定中药制剂标准操作规程和药典标准提供依据。
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引用次数: 0
Pilot study: Hypoglycemic and antiglycation activities of bitter melon (Momordica charantia L.) in type 2 diabetic patients 初步研究:苦瓜(Momordica charantia L.)对2型糖尿病患者的降糖和抗糖化活性
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.007
Wilai Trakoon-osot , Uthai Sotanaphun , Pariya Phanachet , Supatra Porasuphatana , Umaporn Udomsubpayakul , Surat Komindr

Background/Objectives

Bitter melon (Momordica charantia L., MC) has been used as a traditional remedy in diabetics due to its hypoglycemic activity. However, its anti-hyperglycemic effect and antiglycation activity have been demonstrated in vitro and in animal experiments, but not in a long-term clinical study. The aim of this study was to investigate the effect of bitter melon on long-term glycemic control and glycation status in type 2 diabetic patients.

Methods

This study was a two-arm, parallel, randomized, double-blinded, placebo-controlled trial in which type 2 diabetic patients were randomized to continuously take either 6 g/day of MC dried-fruit pulp containing 6.26 ± 0.28 mg of charantin (N = 19) or placebo (N = 19) for 16 weeks.

Results

After 8 and 16 weeks of the treatment, the reduction of A1C from baseline in the MC group was greater than that of the placebo group (0.25 ± 0.12%, P = 0.042 and 0.31 ± 0.15%, P = 0.044, respectively). In addition, the MC group showed a significant decline of total advanced glycation endproducts (AGEs) in serum after 16 weeks of the intervention. The mean difference between both groups was 8.22 ± 3.58 × 103 AU/g protein (P = 0.028). The levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and serum creatinine (Cr) did not change from baseline in each group and were not different between the two groups. None of participants experienced serious adverse events.

Conclusions

It is possible that this herb is beneficial not only on glycemic control, but also on potential systemic complications of type 2 diabetes mellitus.

背景/目的苦瓜(Momordica charantia L., MC)因具有降血糖作用而被用作治疗糖尿病的传统药物。然而,其抗高血糖作用和抗糖化活性已在体外和动物实验中得到证实,但尚未在长期临床研究中得到证实。本研究的目的是探讨苦瓜对2型糖尿病患者长期血糖控制和糖化状态的影响。方法本研究是一项双组、平行、随机、双盲、安慰剂对照试验,2型糖尿病患者随机分为两组,分别服用6 g/d(含6.26±0.28 mg charantin)的MC干果肉(N = 19)和安慰剂(N = 19),持续16周。结果治疗8周和16周后,MC组A1C较基线下降幅度大于安慰剂组(分别为0.25±0.12%,P = 0.042和0.31±0.15%,P = 0.044)。此外,MC组在干预16周后血清中总晚期糖基化终产物(AGEs)显著下降。两组平均差异为8.22±3.58 × 103 AU/g蛋白(P = 0.028)。各组血清丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)和肌酐(Cr)水平与基线相比无显著变化,两组间无显著差异。没有参与者出现严重的不良事件。结论黄芪不仅对2型糖尿病的血糖控制有益,而且对2型糖尿病潜在的全身并发症也有一定的治疗作用。
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引用次数: 35
A case study – Regulation and functional mechanisms of cancer cells and control its activity using plants and their derivatives 一个案例研究-利用植物及其衍生物对癌细胞的调控和功能机制及其活性的控制
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.08.002
Palaniselvam Kuppusamy, Mashitah M. Yusoff, Gaanty Pragas Maniam, Natanamurugaraj Govindan

Novel exploiting to the understanding of conventional medicine was followed by the findings of many unique secondary metabolites and its biological property and is highly required for treating of many endemic diseases. The plants have been a long background in ethno pharmacological knowledge for treatment of endemic and non-endemic diseases. Such plants are traditionally used in different form of paste, extraction and powder to treat seasonal diseases. Nowadays main uses of some medicinal plants have been a great deal with cure and control various chronic diseases such as cancer, AIDS, hepatitis, neurogenic disorders and acute kidney diseases. Cancer is molecular dysfunction and disarrangement in DNA base pairs it leads to change the human physiological and biochemical behavior of the system. Apoptotic mechanisms are regulating by two distinct pathways in which basic creeds perform in common to all eukaryotes. The key components in apoptosis especially mitochondrial intracellular organelles are identified (DNA, protein and ATP, Ca2+). These components control the next cellular binder step and participate in effecting cell suicide mechanisms. The diverse aspects of mitochondria involved in apoptosis include dealing with other proceedings such as release of protein or enzymes to effective for cell death. In these mechanism plants and related natural products using alternative therapeutic management, very less toxicity and cost benefits. Plant extracts and its biomass has revealed the existing of various pharmacologically active compounds like steroids, polyphenols, polysaccharides, saponins, alkaloids, tannins and terpenoids. The reliable natural products are acting as high sources for anticancer drugs. The natural derived compounds are the prolongation of life span of the zeolites and decrease of malignancy cell formation in the cellular system.

许多独特的次生代谢产物及其生物学特性的发现是对传统医学认识的新开拓,是许多地方病的治疗所迫切需要的。这些植物在治疗地方病和非地方病方面具有悠久的民族药理学知识背景。传统上,这些植物以不同形式的膏状、提取物和粉末用于治疗季节性疾病。目前,一些药用植物的主要用途是治疗和控制各种慢性疾病,如癌症、艾滋病、肝炎、神经源性疾病和急性肾病。癌症是分子功能障碍和DNA碱基对的紊乱,导致人体生理生化行为的系统改变。凋亡机制是通过两种不同的途径调节的,这些途径的基本原理对所有真核生物都是一样的。细胞凋亡的关键成分,特别是线粒体胞内细胞器(DNA,蛋白质和ATP, Ca2+)被确定。这些成分控制下一个细胞结合步骤,并参与影响细胞自杀机制。线粒体参与细胞凋亡的不同方面包括处理其他过程,如释放蛋白质或酶以有效地导致细胞死亡。在这些机制中,植物及相关天然产物采用替代治疗管理,毒性非常小,成本效益高。植物提取物及其生物量揭示了类固醇、多酚、多糖、皂苷、生物碱、单宁和萜类化合物等多种药理活性物质的存在。这些可靠的天然产品是抗癌药物的高来源。天然衍生化合物是延长沸石寿命,减少细胞系统恶性细胞的形成。
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引用次数: 20
Inhibition of growth of Helicobacter pylori and its urease by coumarin derivatives: Molecular docking analysis 香豆素衍生物对幽门螺杆菌及其脲酶生长的抑制:分子对接分析
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.09.002
Sharad G. Jadhav, Rohan J. Meshram, Dhanaji S. Gond, Rajesh N. Gacche

Objective

In the present study series of selected coumarin derivatives (CDs) were assessed for their inhibition of growth of Helicobacter pylori (H. pylori) and its related urease. The selected CDs were docked in-silico onto the ligand binding site of H. pylori urease.

Methods

The anti-H. pylori studies were carried out using agar diffusion assay and minimum inhibitory concentrations (MICs) were calculated by microbroth dilution method. Urease inhibitory activity of H. pylori using selected CDs was determined by Berthelot reaction and their IC50 values were calculated using GraphPad Prism version 6.00 while, docking studies were performed by ArgusLab 4.0.1.

Result

The results obtained indicate that, most of the CDs showed considerable anti-H. pylori activity (MIC range of 10–40 μg/ml) as well as significant inhibition of H. pylori urease (IC50 of 48.90–72.56 μM). To a greater extent, the in-silico results were in agreement with in-vitro results of inhibition of H. pylori urease.

Conclusion

The present investigation may find applications in designing and developing a novel, safe and effective anti-H. pylori agents using coumarin scaffold.

目的评价香豆素衍生物对幽门螺杆菌及其相关脲酶生长的抑制作用。选择的CDs通过硅对接到幽门螺杆菌脲酶的配体结合位点上。MethodsThe anti-H。用琼脂扩散法对幽门螺杆菌进行研究,用微肉汤稀释法计算最低抑菌浓度(mic)。选择的CDs通过Berthelot反应测定幽门螺杆菌的脲酶抑制活性,使用GraphPad Prism version 6.00计算其IC50值,使用ArgusLab 4.0.1进行对接研究。结果结果表明,大多数CDs具有较强的抗h活性。抑制幽门螺杆菌脲酶(IC50为48.90 ~ 72.56 μM)。在很大程度上,计算机模拟结果与体外幽门螺杆菌脲酶抑制结果一致。结论本研究为设计和开发一种新型、安全、有效的抗h。利用香豆素支架治疗幽门螺杆菌。
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引用次数: 18
A detail study of phytochemical screening, antioxidant potential and acute toxicity of Agaricus bisporus extract and its chitosan loaded nanoparticles 双孢蘑菇提取物及其壳聚糖纳米颗粒的植物化学筛选、抗氧化潜力和急性毒性研究
Pub Date : 2013-08-01 DOI: 10.1016/j.jopr.2013.07.025
Ganesan Dhamodharan, Sankaran Mirunalini

Aim

Scrutinize the phytochemical, antioxidant and acute toxicity of Agaricus bisporus extract (ABE) and A. bisporus loaded chitosan nanoparticles (ABCNPs).

Methods

Phytochemical such as total phenol and flavonoid, and terpenoid, alkaloid, steroid, carbohydrate, tannins and proteins where determined. The antioxidant activity such as DPPH, ABTS and reducing power of ABE and ABCNPs where estimated by spectrophotometry assay. The estimation of total phenolic content was determined by Folin–Ciocalteu method. The acute toxicity studies of ABE and ABCNPs were investigated in male Sprague Dawley rats. Results: In the DPPH, ABTS•+ and reducing power scavenging assays, of ABE displayed significant antioxidant activities with the inhibition values of 27.78, 27.62 and 81.97% and ABCNPs inhibition values 27.78, 27.62 and 78.13% respectively. The reducing power of the extract increased dose-dependently, and the ABE and ABCNPs reduced the most Fe3+ ions. The amount of total phenolics was reported 1 g of sample contains 8.19±1 mg of gallic acid and total flavonoid analysis by the assay of aluminum chloride spectrophotometric reported 1 g of sample contains 10.3 ± 1 mg of quercetin in ABE and ABCNPs. The acute toxicity was found bellow 2747.25 mg/kg b.w. in ABE and 3178.86 mg/kg b.w. of ABCNPs.

Conclusion

The white button mushroom A. bisporus could be considered as a dietary natural food products with antioxidant activity. Thus our results provide evidence that AB and ABCNPs proves to have a potent antioxidant and intermittent therapy against cancer.

目的研究双孢蘑菇提取物(ABE)和双孢蘑菇壳聚糖纳米颗粒(ABCNPs)的植物化学、抗氧化和急性毒性。方法测定植物化学成分,如总酚、类黄酮、萜类、生物碱、类固醇、碳水化合物、单宁、蛋白质等。用分光光度法测定ABE和ABCNPs的抗氧化活性,如DPPH、ABTS和还原能力。用Folin-Ciocalteu法测定总酚含量。研究了ABE和ABCNPs对雄性大鼠的急性毒性。结果:在DPPH、ABTS•+和还原力清除实验中,ABE表现出显著的抗氧化活性,其抑制值分别为27.78、27.62和81.97%,ABCNPs的抑制值分别为27.78、27.62和78.13%。提取物的还原能力呈剂量依赖性增加,ABE和ABCNPs还原Fe3+离子最多。总酚类物质的含量被报道为1g样品中含有8.19±1mg没食子酸和总黄酮,通过氯化铝分光光度法分析报道1g样品中含有10.3±1mg槲皮素的ABE和ABCNPs。ABE的急性毒性低于2747.25 mg/kg b.w., ABCNPs的急性毒性低于3178.86 mg/kg b.w.。结论双孢白针菇是一种具有抗氧化活性的天然膳食食品。因此,我们的研究结果为AB和ABCNPs证明具有有效的抗氧化剂和间歇性治疗癌症提供了证据。
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引用次数: 23
期刊
Journal of Pharmacy Research
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