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SUB-CHRONIC TOXICITY STUDY OF T-AYU-HMTM PREMIUM: A HERBO-MINERAL FORMULATION 一种草药-矿物质制剂- t-ayu-hmtm premium的亚慢性毒性研究
Pub Date : 2022-01-30 DOI: 10.25004/ijpsdr.2022.140101
Atul Desai, Hemshree Desai, R. Desai, A. Merai, Maitri Kalan, Chirag V Desai, A. Paul
To perform a sub-chronic toxicity study and to generate scientific data regarding the safety profile of T-AYUHMTM Premium, a herbo-mineral formulation used for sickle cell disease. Experimental animals (Mice) were divided into six groups and were acclimatized and treated with 125 mg T-AYU-HMTM Premium/kg body weight (T1 LD), 625 mg T-AYU-HMTM Premium/kg body weight (T2 MD), and 1250 mg T-AYU-HMTM Premium/kg body weight (T3 HD) and two group of satellite daily for 90 days. 0.5% CMC was administered to the control group as a vehicle. The satellite groups were treated with 125 mg T-AYU-HMTM Premium/kg body weight (S1 LD) and 1250 mg T-AYU-HMTM Premium/kg body weight (S2 HD, 1250 mg/kg) receiving low and high dose respectively. The mice were closely observed for a clinical sign of toxicity, stereotypical behavior and alteration in autonomic activity during the entire study period. Hematological and blood biochemical parameters were observed on days 0, 60, 90. Motor coordination activity and sensory stimuli assessment were performed after the 11th week. At the termination of the study, all animals were sacrificed, and organs such as the heart, brain, kidney, liver, etc., were collected and observed for histopathology. There was no change in the normal gross behavior of animals in the sensory and motor assessment activity in the treatment group compared to the control group. Evaluation of hematological parameters shows a significant increase in red blood corpuscles. Histopathological examination of various organs shows a normal architecture in all the treated groups. T-AYU-HMTM Premium was found to be safe on repeat dose oral administration in NOAEL, dose up to 1250 mg/kg body weight when administered orally for 90 days in both the sexes of Swiss Albino mice.
开展亚慢性毒性研究并生成关于T-AYUHMTM Premium安全性的科学数据,T-AYUHMTM Premium是一种用于镰状细胞病的草药矿物配方。实验动物(小鼠)分为6组,分别以125 mg T-AYU-HMTM Premium/kg体重(T1 LD)、625 mg T-AYU-HMTM Premium/kg体重(T2 MD)、1250 mg T-AYU-HMTM Premium/kg体重(T3 HD)和2组卫星饲料进行驯化,共90 d。对照组给予0.5% CMC作为载体。卫星组按低、高剂量分别给予125 mg T-AYU-HMTM优品/kg体重(S1 LD)和1250 mg T-AYU-HMTM优品/kg体重(S2 HD, 1250 mg/kg)。在整个研究期间,密切观察小鼠的临床毒性症状、刻板行为和自主神经活动的改变。观察第0、60、90天的血液学和血液生化指标。第11周后进行运动协调活动和感觉刺激评估。实验结束时,处死所有动物,取心、脑、肾、肝等脏器进行组织病理学观察。与对照组相比,治疗组动物在感觉和运动评估活动中的正常大体行为没有变化。血液学参数评估显示红细胞显著增加。各脏器组织病理学检查均显示各治疗组结构正常。发现T-AYU-HMTM Premium在NOAEL中重复口服剂量是安全的,在瑞士白化病小鼠两性中口服90天,剂量高达1250 mg/kg体重。
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引用次数: 0
Design Development and Characterisation of Mupirocin Loaded Emulsion Based Gel 含莫匹罗星乳液凝胶的设计、研制与表征
Pub Date : 2021-09-30 DOI: 10.25004/ijpsdr.2021.130512
Hardik A. Lakkad, V. Patel
The objective of the present study was to develop more retentive and effective drug delivery system for mupirocin. The research was going on in achieving effective formulation. Mupirocin is an anti-microbial agent that is used in wounds healing treatment. First Screening of oil, surfactant and co-surfactant for SEDDS carried out. Solubility of drug was investigated in different oils, surfactant and co-surfactants by UV method. A drug was dissolved in available oil in which it exhibited maximum solubility, then surfactant and co-surfactant were added in which drug showed maximum solubility, mixed well on a magnetic stirrer. Transparent SEDDS were formed. Carbopol 940 and Polyacrylate sodium gelling agent was suspended in water and hydrated for overnight separately. For preparation of Emulgel, various ratios of gel and SEDDS were set. Emulgel was evaluated for %drug release, pH, and drug content. The results indicated that Emulgel gave better controlled release. The formulation F11 showed 99.27 percent drug release, pH 6.7 ± 0.1 and drug content 99.4 ± 0.11%. Formulation F11 was selected as an optimized formulation. The formulations of Emulgel delivered very good therapeutic efficacy for topical application.
本研究的目的是开发更有效的莫匹罗星给药系统。为取得有效的配方,正在进行研究。莫匹罗星是一种抗微生物剂,用于伤口愈合治疗。首先对SEDDS的油、表面活性剂和助表面活性剂进行了筛选。用紫外分光光度法考察了药物在不同油脂、表面活性剂和助表面活性剂中的溶解度。将药物溶解在溶解度最大的油中,然后加入溶解度最大的表面活性剂和助表面活性剂,在磁力搅拌器上搅拌均匀。形成透明的SEDDS。卡波波尔940和聚丙烯酸钠胶凝剂分别悬浮在水中,水合过夜。在制备乳凝胶时,设定了不同的凝胶与sedds的比例。测定凝胶的药物释放率、pH值和药物含量。结果表明,乳凝胶具有较好的控释效果。处方F11释药率为99.27%,ph值为6.7±0.1,药物含量为99.4±0.11%。优选配方F11为最佳配方。乳凝胶的配方对局部应用具有很好的治疗效果。
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引用次数: 1
Anticonvulsant Activity of Helianthus tuberosus Against MaximalElectroshock Induced Convulsions in Rats 桔梗对大鼠最大电休克惊厥的抗惊厥作用
Pub Date : 2021-09-30 DOI: 10.25004/ijpsdr.2021.130513
Nagnath R. Kadam, P. Mohanty, A. Jain
Epilepsy is an episodic brain dysfunction featured by recurring erratic spontaneous seizures followed by cognitive, social, neurobiological, and psychological consequences. Conventional anti-epileptic drugs are associated with several untoward effects, and hence long-term treatment compliance is a major problem in the management of epilepsy. Herbal drugs have shown promising efficacy as potent anticonvulsants in the past few years. In light of this, the anticonvulsant effect of alcoholic extract of leaves of Helianthus tuberosus (AHT) against maximal electroshock (MES) induced convulsions was investigated. In the present investigation, an indigenous plant, H. tuberosus was studied for its protective effect against maximalelectroshock (MES) induced convulsions in Wistar albino rats. The rats were pre-treated with differentdoses (100, 200, 400 mg/kg) of alcoholic extract of leaves of H. tuberosus for 14 days, and then, they weresubjected to maximal electroshock seizures (40 mA for 0.2 seconds) treatment. Alcoholic extract of leavesof H. tuberosus at the dose of 400 mg/kg significantly reduced the duration of hind limb extension andthe protection of rats against maximal electroshock-induced seizures. The reference standards phenytoin(20 mg/kg) provided complete protection. Thus, the present study revealed an anticonvulsant effect ofH. tuberosus against maximal electroshock-induced convulsions in rats.
癫痫是一种发作性脑功能障碍,其特征是反复无常的自发发作,随后出现认知、社会、神经生物学和心理后果。传统的抗癫痫药物与一些不良反应有关,因此长期治疗依从性是癫痫管理中的一个主要问题。在过去的几年里,草药作为有效的抗惊厥药已经显示出很好的疗效。有鉴于此,本文研究了菊芋叶醇提物(AHT)对最大电休克(MES)致惊厥的抗惊厥作用。本研究研究了一种本土植物,H. tuberosus对Wistar白化大鼠最大电休克(MES)引起的惊厥的保护作用。采用不同剂量(100、200、400 mg/kg)的荷叶醇提物预处理大鼠14 d,然后给予最大电刺激(40 mA, 0.2秒)。荷叶醇提物400mg /kg可显著缩短大鼠后肢伸展时间,并对最大电致癫痫发作有保护作用。参考标准苯妥英(20mg /kg)提供了完全的保护。因此,本研究揭示了黄芪的抗惊厥作用。结节对大鼠最大电休克惊厥的影响。
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引用次数: 0
Development of Candesartan Loaded Solid Lipid Nanoparticles by Box-Behnken Design Box-Behnken设计制备坎地沙坦固体脂质纳米颗粒
Pub Date : 2020-11-30 DOI: 10.25004/ijpsdr.2021.130604
Yelugudhari Ramulu, D. Bhikshapathi
The primary motive behind this the present investigation was to develop and optimize the solid lipid nanoparticles formulation of candesartan to enhance solubility and dissolution rate. The prepared SLNs composed of precirol, poloxamer 188, soy lecithin, tween 80, were fabricated employing hot emulsification/ ultrasonication technique. Box-Behnken design was employed for 17 formulation batches in which 3 factors namely lipid, surfactant, and co-surfactant (precirol, poloxamer 188 and soy lecithin) tween 80 weretested at 3 levels of their concentration, i.e., low, medium and high. The effect of different levels of factorswas evaluated for the particle size, entrapment efficiency and % cumulative drug release. Kinetic modelfitting for candesartan solid lipid nanoparticles (SLN) formulation was done to interpret the release ratefrom the SLN. Optimized formulation was subjected for fourier transform infrared spectroscopy (FTIR),scanning electron microscope (SEM) and stability studies. The mean particle size, PDI, zeta potential,entrapment efficiency, content uniformity and in-vitro drug release of optimized candesartan-loaded SLNs(CD10) were found to be 135.38 ± 3.41 nm, 0.125 ± 0.04, -18.16 ± 2.89 mV, 86.4 ± 2.35%, 99.78 ± 2.54%and 98.91 ± 0.85% respectively. The release kinetics suggested that drug release followed zero-order andrelease was anomalous non-fickian diffusion super case II transport. FTIR studies revealed no incompatibilitybetween drug and excipients, SEM images exhibited nanoparticles to be more porous and in a sphericalshape. Stability studies indicated good stability of the formulation. The proposed way of SLN preparationcould be considered a proper method for producing a candesartan-loaded colloidal carrier system.
本研究的主要目的是开发和优化坎地沙坦的固体脂质纳米颗粒配方,以提高其溶解度和溶解速度。采用热乳化-超声法制备了由苯醇、波洛沙姆188、大豆卵磷脂、tween 80组成的单链纳米粒子。采用Box-Behnken设计对17个剂型批次进行试验,在低、中、高3个浓度水平下对80个剂型批次的脂质、表面活性剂和助表面活性剂(普瑞罗尔、波洛沙姆188和大豆卵磷脂)进行检测。考察了不同水平因素对其粒径、包封效率和药物累积释放率的影响。采用动力学模型拟合坎地沙坦固体脂质纳米颗粒(SLN)的释放速率。对优化后的配方进行了傅里叶变换红外光谱(FTIR)、扫描电镜(SEM)和稳定性研究。优化后的坎地沙坦sln (CD10)平均粒径为135.38±3.41 nm, PDI为0.125±0.04,zeta电位为-18.16±2.89 mV,含量均匀度为86.4±2.35%,99.78±2.54%,体外释放度为98.91±0.85%。释放动力学表明,药物的释放服从零级,为异常非粘性扩散转运。FTIR研究显示药物和辅料之间没有不相容性,SEM图像显示纳米颗粒更多孔,呈球形。稳定性研究表明该制剂具有良好的稳定性。所提出的SLN制备方法可以被认为是制备坎地沙坦负载胶体载体体系的合适方法。
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引用次数: 0
GC-MS Profiling, Invitro Antidiabetic, Antioxidant and Antimicrobial Activities of a Novel Polyherbal Formulation 一种新型复方药的GC-MS分析、体外抗糖尿病、抗氧化和抗菌活性
Pub Date : 2020-11-30 DOI: 10.25004/ijpsdr.2020.120602
C. M. Shanmugavadivelu, N. Jain, A. Thirupathi, P. Murugesan
In the present study the methanol extract of a novel polyherbal formulation (PHF) was studied for alpha (α)- amylase and alpha (α)-glucosidase inhibition using an in vitro antidiabetic model. The polyherbal extract were also examined for its antioxidant activity by using free radical 1,1-diphenyl-2-picryl hydrazyl (DPPH) scavenging method. The study revealed that the polyherbal formulation exhibit potent radical scavenging activity using DPPH as substrate. The methanol extract exhibited significant α-amylase and α-glucosidase inhibitory activities with an IC50 value 31.52±0.74µg and 53.13±0.97µg respectively and well compared with standard acarbose drug. Further, antibacterial activity of methanol extract of PHF valuated against standard strains, the tested extract showed more potent inhibitory effects on both Gram (+) bacteria and  Gram (-) bacteria. Thus, it could be concluded that due the presence of antioxidant components the plant extract have well prospective for the management of diabetes and the related condition of oxidative stress. This knowledge will be useful in finding more potent antidiabetic principle from the natural resources for the clinical development of antidiabetic therapeutics.
本研究采用体外抗糖尿病模型,研究了一种新型复方中药(PHF)甲醇提取物对α (α)-淀粉酶和α (α)-葡萄糖苷酶的抑制作用。采用清除自由基1,1-二苯基-2-苦味基肼(DPPH)的方法考察了其抗氧化活性。研究表明,以DPPH为底物的复方具有较强的自由基清除活性。甲醇提取物具有显著的α-淀粉酶和α-葡萄糖苷酶抑制活性,IC50值分别为31.52±0.74µg和53.13±0.97µg,与标准阿卡波糖药物相比效果良好。此外,对PHF甲醇提取物对标准菌株的抑菌活性进行了评价,结果表明,PHF甲醇提取物对革兰氏(+)菌和革兰氏(-)菌均有较强的抑菌作用。因此,由于抗氧化成分的存在,该植物提取物在糖尿病和氧化应激相关疾病的治疗中具有良好的前景。这些知识将有助于从自然资源中发现更有效的抗糖尿病原理,为临床开发抗糖尿病治疗药物提供帮助。
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引用次数: 0
Production of value added Oyster mushrooms 生产具有附加值的平菇
Pub Date : 2020-11-30 DOI: 10.25004/ijpsdr.2020.120608
B. Sailaja, B. Radhika
Mushrooms are ironic in nutrimental resources and have converted into one of the common foods in the previous twenty years globally. The types of edible mushrooms are button, milky and oyster mushrooms. The research aimed at value addition of Oyster mushrooms by rising on paddy substrate complemented with two concentrations of four different medicinal plants. The plant parts selected were flowers of Butea monosperma, leaves of Moringa olifera, bark of Cinnamonom zeylianicum, fruits of Corindraum sativum at 5% and 10% concentration.  Different species of oyster mushrooms are available. In the present study Pleurotus florida was selected for value addition. Maximum mycelium running rate was detected in Cinnamon bark (5%) and paddy straw (95%) accompanied group and lowermost running rate of mycelium was observed in Moringa leaf (5%) and paddy straw (95%). The primordial arrival was fast with Cinnamon bark (5%) supplemented group and slowest in Moringa leaf (5%) supplemented group. The mushrooms grownup on Coriander fruit (5%) produced more but the growth was slow. Mushrooms supplemented with Butea flower (5%) exhibited slow growth and yield was next to coriander fruit supplemented mushrooms. The produced mushrooms were subjected to physical evaluation, preliminary phytochemical testing and also tested for estimation of total flavonoids, total phenols, total tannins and total cinnamaldehyde contents. Value addition of Oyster mushrooms was successful with cinnamon bark as cinnamaldehyde was noticed in the Cinnamon bark supplemented group, and also with Moringa leaves as flavonoids was observed in more concentration in Moringa leaf supplemented mushroom group.
蘑菇的营养资源具有讽刺意味,在过去的二十年里,蘑菇已经成为全球常见的食物之一。食用蘑菇的种类有钮扣菇、乳菇和平菇。本研究的目的是通过在水稻基质上生长,辅以四种不同药用植物的两种浓度来增加平菇的附加值。选取的植物部位分别为布茶(Butea monosperma)花、辣木(Moringa olifera)叶、肉桂(Cinnamonom zeylianicum)皮、哥林多(Corindraum sativum)果,浓度分别为5%和10%。有不同种类的平菇可供选择。本研究选择佛罗里达侧耳菇进行增值。伴随组菌丝体跑动率最高的是桂皮组(5%)和稻秆组(95%),最低的是辣木叶组(5%)和稻秆组(95%)。肉桂皮(5%)添加组的原始到达速度最快,辣木叶(5%)添加组的原始到达速度最慢。香菜果实(5%)成菇产量较高,但生长缓慢。添加Butea花(5%)的蘑菇生长缓慢,产量仅次于添加香菜果的蘑菇。对生产的香菇进行了物理评价、初步的植物化学试验以及总黄酮、总酚、总单宁和总肉桂醛的含量测定。肉桂皮对平菇的添加效果较好,肉桂皮添加组的肉桂醛含量较高;辣木叶添加组的黄酮含量较高。
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引用次数: 0
Determination of Spray Pattern and Plume Geometry of Combined Budesonide and Formoterol Fumarate pressurized Metered Dose Inhalation Aerosol 布地奈德与富马酸福莫特罗联合加压计量吸入气雾剂的喷雾模式和羽状结构的测定
Pub Date : 2020-11-30 DOI: 10.25004/ijpsdr.2020.120605
R. Kotak, C. Pandya, A. C. Pandya, Avnish Rajput, B. Thakur
Budesonide and formoterol fumarate pressurized metered-dose inhaler (pMDI) is combined aerosol dosage form. The label claim of this combined dosage form is 100 mcg of Budesonide and 6 mcg of Formoterol Fumarate per actuation. It is prescribed for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Formoterol fumarate is an anti-asthmatic drug (Bronchodilator), and Budesonide is Anti Inflammatory drug (Glucocortico steroid).The objective of plume geometry and spray pattern study is to monitor the consistency and quality of a device when actuated. The plume and pattern study aims to develop a formulation with robust device which can deliver an accurate amount of drug directly to the lungs of a patient. The chemistry manufacturing and controls (CMC) guideline outlined the basic data required for spray pattern and plume geometry measurement for different pMDI devices. In 2013, draft guidance on bioavailability and bioequivalence (BABE) of pMDI published, which provides details on plume geometry and spray pattern, image collection and evaluation.In the present study, the spray patterns were collected at 2 distances 3 and 6 cm from the actuator device's exit. The spray pattern Ovality results at 3 cm show 2.52% variation and at 6 cm results show 4.31% variation. Method precision, ruggedness and robustness study for Spray pattern also performed at 6 cm distance from actuator orifice. The plume geometry was collected at 6 cm distance from the exit of an actuator device. Plume geometry results show that Plume height is found in the range 16.20 cm to 18.98 cm, Plume angle is found from 17.7–24.9°, and Plume width is found between 3.68 to 4.57 cm.
布地奈德富马酸福莫特罗加压计量吸入器(pMDI)是复合气溶胶剂型。这种组合剂型的标签声明是每次服用100微克布地奈德和6微克富马酸福莫特罗。它是治疗哮喘和慢性阻塞性肺疾病(COPD)的处方。富马酸福莫特罗是一种抗哮喘药(支气管扩张剂),布地奈德是抗炎药(糖皮质激素)。羽状几何和喷雾模式研究的目的是监测装置在启动时的一致性和质量。羽状和模式研究旨在开发一种具有强大装置的配方,可以将准确数量的药物直接输送到患者的肺部。化学制造和控制(CMC)指南概述了不同pMDI设备的喷雾模式和羽流几何测量所需的基本数据。2013年,pMDI的生物利用度和生物等效性(BABE)指南草案发布,其中提供了羽流几何形状和喷雾模式、图像收集和评估的详细信息。在本研究中,在距离致动器出口3 cm和6 cm处收集了喷雾模式。椭圆度在3 cm处变化2.52%,在6 cm处变化4.31%。方法的精度、坚固性和鲁棒性也在距离执行器孔6cm处进行了研究。羽流几何形状是在距离执行器装置出口6厘米处收集的。羽流几何结果表明,羽高在16.20 ~ 18.98 cm之间,羽角在17.7 ~ 24.9°之间,羽宽在3.68 ~ 4.57 cm之间。
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引用次数: 0
Effects of Pterostilbene isolated from Pterocarpus marsupium on High Fat Diet induced Diabetic Rats 有袋蕨紫檀芪提取物对高脂饮食诱导的糖尿病大鼠的影响
Pub Date : 2020-11-30 DOI: 10.25004/ijpsdr.2021.130614
Bhavna Grover, P. Roy
Diabetes mellitus is a group of metabolic diseases characterized by hyperglycemia resulting from defectsin insulin secretion, insulin action or both. The present study tested the anti-diabetic and hypolipidemicpotential of pterostilbene isolated from Pterocarpus marsupium plants on high fat diet-induced diabeticrats. The high-fat diet-fed rats showed increased serum glucose, cholesterol, triglycerides and insulinresistance (p is less than  0.05). However, treating the animals with pterostilbene different biochemical parameterslike glucose tolerance, glycogen content, glucose homeostatic enzymes like glucose-6-phosphataseand hexokinase, adipocytes differentiation, and the expression profiles of different genes regulatingcarbohydrate and lipid metabolism were improved significantly (p is less than  0.05). Further, pterostilbene wasfound to demonstrate dual regulation activities for peroxisome proliferators-activated receptors (PPAR)(both PPARα and PPARγ). In conclusion, these results show that pterostilbene acts as a potent antidiabetic molecule. Hence further in-depth mechanistic studies are warranted to use this phytochemicalas a medicine.
糖尿病是一组以胰岛素分泌缺陷、胰岛素作用缺陷或两者兼而有之引起的高血糖为特征的代谢性疾病。本文研究了从有袋蕨植物中提取的紫檀芪对高脂饮食诱导的糖尿病患者的抗糖尿病和降血脂作用。高脂饮食大鼠血清葡萄糖、胆固醇、甘油三酯和胰岛素抵抗升高(p < 0.05)。然而,紫檀芪处理动物的糖耐量、糖原含量、葡萄糖-6-磷酸酶和己糖激酶等葡萄糖稳态酶、脂肪细胞分化以及调节碳水化合物和脂质代谢的不同基因的表达谱等生化指标均有显著改善(p < 0.05)。此外,还发现紫檀芪对过氧化物酶体增殖物激活受体(PPAR)(PPARα和PPARγ)具有双重调节活性。综上所述,这些结果表明紫檀芪是一种有效的抗糖尿病分子。因此,有必要进一步深入研究这种植物化学物质作为药物的机理。
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引用次数: 0
Effect of Ethanolic extract of Boerhvia diffusa against doxorubicin induced Nephrotoxicity in Albino Rats 白花菊醇提物对阿霉素致白化大鼠肾毒性的影响
Pub Date : 2020-11-30 DOI: 10.25004/ijpsdr.2021.130602
S. K. Nimbal, B. Koti
Anthracycline derivative i.e. doxorubicin (Dox) has proven efficacy in several malignancies suchas breast cancer, Hodgkin and non-Hodgkin lymphoma, acute leukemia, lung, thyroid and ovariancancer. The clinical usefulness is restricted due to its cardiotoxicity and nephrotoxicity. Boerhaaviadiffusa belongs to family Nyctaginaceae and in Ayurveda, it is claimed for use in renal disorders.The main phytoconstituents of the plant are alkaloids, terpenoids, tannins, glycosides, flavonoids, phenoliccompounds. To investigate the ameliorative role of ethanolic extract of petals of B. diffusa in doxorubicin-induced nephrotoxicity in rats. Nephrotoxicity was produced by administering doxorubicin (2.5 mg/kg b.w., i.p. alternate day) in six equal injections for two weeks to become cumulatively 15 mg/kg. Low (LEBD–100 mg/kg p.o.) and high (HEBD–200 mg/kg p.o.) dose of ethanolic extract of Boerhhvia diffusa was administered as a pretreatment before doxorubicin administration. The general parameters such as body weight, food, and water intake were measured throughout the study period. Serum markers such as blood urea nitrogen (BUN), serum creatinine and albumin were measured. Antioxidant enzymes such as glutathione (GSH),malondialdehyde (MDA), catalase (CAT), and superoxide dismutase (SOD) were monitored after thelast dose. Histopathological studies were also carried out to evaluate nephrotoxicity. The repeatedadministration of doxorubicin produces several morphological changes, decreased body weight, food, andwater consumption. Serum markers such as BUN and serum creatinine were increased and albumin levelsdecreased. The GSH, SOD, and CAT were decreased, whereas the MDA level was increased, and deterioratingchanges in the histological architecture of kidney tissue were observed. The HEBD pretreated groups dosedependently increased body weight and food and water intake (p is less than  0.01 and p is less than 0.05), whereas LEBD doesnot show any significant changes. The LEBD and HEBD pretreated groups decreased the BUN (p is less than 0.05and p is less than 0.01) and serum creatinine (p is less than 0.05 and p is less than 0.05) and increased in the albumin (p is less than 0.05 andp is less than 0.05) levels, respectively. The pretreatment with LEBD and HEBD increased the level of the antioxidantenzyme i.e., GSH (p is less than 0.05 and p is less than 0.01), SOD (p is less than 0.05 and p is less than 0.01), CAT (p is less than 0.05 and p is less than 0.01) anddecreased the MDA level (p is less than 0.05 and p is less than 0.01) respectively. Histopathological studies showed that thepretreatment with LEBD and HEBD groups minimized the tubular damage and reduced the inflammationas compared to doxorubicin-treated group. The biochemical and histopathological results data support thenephroprotective effect of ethanolic extract of B. diffusa, which might be credited to its antioxidant property.
蒽环类衍生物,即阿霉素(Dox)已被证明对几种恶性肿瘤有效,如乳腺癌、霍奇金淋巴瘤和非霍奇金淋巴瘤、急性白血病、肺癌、甲状腺癌和卵巢癌。由于其心脏毒性和肾毒性,其临床应用受到限制。Boerhaaviadiffusa属于Nyctaginaceae家族,在阿育吠陀中,它被声称用于肾脏疾病。该植物的主要成分有生物碱、萜类、单宁、苷类、黄酮类、酚类化合物等。探讨白花花花瓣乙醇提取物对阿霉素所致大鼠肾毒性的改善作用。给予阿霉素(2.5 mg/kg体重,隔天1次,每次1次)6次等量注射,连续2周达到累计15 mg/kg,产生肾毒性。低剂量(LEBD-100 mg/kg p.o)和高剂量(HEBD-200 mg/kg p.o)白花菊乙醇提取物作为阿霉素给药前的预处理。在整个研究期间测量了一般参数,如体重、食物和水的摄入量。测定血清指标如尿素氮(BUN)、血清肌酐、白蛋白。最后一次给药后监测抗氧化酶如谷胱甘肽(GSH)、丙二醛(MDA)、过氧化氢酶(CAT)和超氧化物歧化酶(SOD)。还进行了组织病理学研究以评估肾毒性。反复给予阿霉素可产生多种形态学改变,体重、食物和水的消耗减少。血清指标如BUN和肌酐升高,白蛋白水平降低。GSH、SOD、CAT水平降低,MDA水平升高,肾组织组织结构发生恶化变化。HEBD预处理组大鼠体重和摄食量呈剂量依赖性增加(p < 0.01和p < 0.05), LEBD预处理组大鼠无显著变化。LEBD和HEBD预处理组分别降低了BUN (p < 0.05和p < 0.01)和血清肌酐(p < 0.05和p < 0.05),升高了白蛋白(p < 0.05和p < 0.05)水平。LEBD和HEBD预处理分别提高了抗氧化酶GSH (p < 0.05和p < 0.01)、SOD (p < 0.05和p < 0.01)、CAT (p < 0.05和p < 0.01)和MDA (p < 0.05和p < 0.01)水平。组织病理学研究表明,与阿霉素治疗组相比,LEBD和HEBD预处理组使小管损伤最小化,炎症减轻。生物化学和组织病理学结果支持白花草乙醇提取物的肾保护作用,这可能与白花草乙醇提取物的抗氧化作用有关。
{"title":"Effect of Ethanolic extract of Boerhvia diffusa against doxorubicin induced Nephrotoxicity in Albino Rats","authors":"S. K. Nimbal, B. Koti","doi":"10.25004/ijpsdr.2021.130602","DOIUrl":"https://doi.org/10.25004/ijpsdr.2021.130602","url":null,"abstract":"Anthracycline derivative i.e. doxorubicin (Dox) has proven efficacy in several malignancies such\u0000as breast cancer, Hodgkin and non-Hodgkin lymphoma, acute leukemia, lung, thyroid and ovarian\u0000cancer. The clinical usefulness is restricted due to its cardiotoxicity and nephrotoxicity. Boerhaavia\u0000diffusa belongs to family Nyctaginaceae and in Ayurveda, it is claimed for use in renal disorders.\u0000The main phytoconstituents of the plant are alkaloids, terpenoids, tannins, glycosides, flavonoids, phenolic\u0000compounds. To investigate the ameliorative role of ethanolic extract of petals of B. diffusa in doxorubicin-induced nephrotoxicity in rats. Nephrotoxicity was produced by administering doxorubicin (2.5 mg/kg b.w., i.p. alternate day) in six equal injections for two weeks to become cumulatively 15 mg/kg. Low (LEBD–100 mg/kg p.o.) and high (HEBD–200 mg/kg p.o.) dose of ethanolic extract of Boerhhvia diffusa was administered as a pretreatment before doxorubicin administration. The general parameters such as body weight, food, and water intake were measured throughout the study period. Serum markers such as blood urea nitrogen (BUN), serum creatinine and albumin were measured. Antioxidant enzymes such as glutathione (GSH),\u0000malondialdehyde (MDA), catalase (CAT), and superoxide dismutase (SOD) were monitored after the\u0000last dose. Histopathological studies were also carried out to evaluate nephrotoxicity. The repeated\u0000administration of doxorubicin produces several morphological changes, decreased body weight, food, and\u0000water consumption. Serum markers such as BUN and serum creatinine were increased and albumin levels\u0000decreased. The GSH, SOD, and CAT were decreased, whereas the MDA level was increased, and deteriorating\u0000changes in the histological architecture of kidney tissue were observed. The HEBD pretreated groups dosedependently increased body weight and food and water intake (p is less than  0.01 and p is less than 0.05), whereas LEBD does\u0000not show any significant changes. The LEBD and HEBD pretreated groups decreased the BUN (p is less than 0.05\u0000and p is less than 0.01) and serum creatinine (p is less than 0.05 and p is less than 0.05) and increased in the albumin (p is less than 0.05 and\u0000p is less than 0.05) levels, respectively. The pretreatment with LEBD and HEBD increased the level of the antioxidant\u0000enzyme i.e., GSH (p is less than 0.05 and p is less than 0.01), SOD (p is less than 0.05 and p is less than 0.01), CAT (p is less than 0.05 and p is less than 0.01) and\u0000decreased the MDA level (p is less than 0.05 and p is less than 0.01) respectively. Histopathological studies showed that the\u0000pretreatment with LEBD and HEBD groups minimized the tubular damage and reduced the inflammation\u0000as compared to doxorubicin-treated group. The biochemical and histopathological results data support the\u0000nephroprotective effect of ethanolic extract of B. diffusa, which might be credited to its antioxidant property.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"50 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90279290","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
Synthesis and Oral Hypoglycemic Activity of Some New Sulphonyl Linkage Thiazolidine-2,4-diones 新型磺酰基噻唑烷-2,4-二酮的合成及口服降糖活性研究
Pub Date : 2020-11-30 DOI: 10.25004/ijpsdr.2020.120603
L. Kawale, V. Nade, R. Deshmukh, M. Dumbare
Type 2 diabetes mellitus and its complications, decreases the quality of life in diabetic patients. Thiazolidine-2,4-diones are found to be better insulin sensitizing agents, acting on peroxisome proliferator activated receptor-γ (PPAR-γ) and decrease blood glucose level in diabetic patient. Therefore, in the present work, we synthesized 5-[4-(substituted) sulphonylbenzylidene]thiazolidine-2,4-diones and evaluated for their oral hypoglycemic activity. The synthesized compounds were further studied for their find out interactions with 2PRG protein with the help of docking score and also find out their predicated ED25 values. The results of synthesized compounds were showed significant decrease in blood glucose level as compared to positive control group. All synthesized compounds have shown good hydrogen bond interactions with 2PRG protein, docking score and predicted ED25 value as compared with reference drug, pioglitazone and rosiglitazone, respectively. Thus, sulphonyl linked thiazolidine-2,4-diones may be used as promising oral hypoglycemic agent.
2型糖尿病及其并发症降低了糖尿病患者的生活质量。噻唑烷-2,4-二酮是较好的胰岛素增敏剂,可作用于过氧化物酶体增殖物激活受体-γ (PPAR-γ),降低糖尿病患者的血糖水平。因此,本文合成了5-[4-(取代)磺基苄基]噻唑烷-2,4-二酮类化合物,并对其口服降糖活性进行了评价。通过对接评分进一步研究合成的化合物与2PRG蛋白的相互作用,并确定其预测的ED25值。结果表明,与阳性对照组相比,合成的化合物显著降低了血糖水平。与对照药物吡格列酮和罗格列酮相比,所有合成的化合物均与2PRG蛋白表现出良好的氢键相互作用,对接评分和ED25预测值均较好。因此,磺酰基连接噻唑烷-2,4-二酮可能是一种有前景的口服降糖药。
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International Journal of Pharmaceutical Sciences and Drug Research
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