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Ethanolic Extract of Syzygium cumini Causes Toxic Effects on Ethanol-induced Liver and Kidney Damage in Albino Wistar Rats: A Biochemical and Histological Study 小茴香醇提物对乙醇致白化Wistar大鼠肝肾损伤的毒性作用:生化和组织学研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-01-01 DOI: 10.32598/ijt.16.1.879.1
Abba Aji Manu, Bello Muhammad Musa, Martha Orendu Oche Attah, H. Bedan
Background: The therapeutic value of Syzygium cumini (S. cumini) has been documented in traditional medicine for the treatment of many diseases and ailments. Various preparations of this plant have been made and used especially for liver inflammatory conditions in livestock. Further, many liver diseases in humans are inflammatory conditions, which are caused by alcohol intake. This study sought to examine the effect of S. cumini on ethanol-induced hepatotoxicity in Wistar albino rats. Methods: Twenty-five rats were divided into five groups of five rats each. The first group was control and the other four were administered ethanol at varying doses to induce liver and kidney damages. Two doses of the S. cumini extract were administered at a concentration of 200 mg/kg or 400 mg/kg. Silymarin was administered to the last group at 10 mg/kg. The liver and kidney tissue samples were collected and preserved for histological analyses and the rat sera were analyzed for the associated biochemical biomarkers. Results: Histopathological analyses revealed pyknotic nuclei and distortion in the arrangement of the hepatocytes in extract-treated groups. The kidney tissue samples showed signs of interstitial bleeding and aggregation of lymphocytes in the peri-glomerular areas. The analyses of the biochemical parameters revealed that there were significant increases in the aspartate aminotransferase (AST), alanine transaminase (ALT), Urea and creatinine in the sera of the groups treated with the extract compared to those of the controls (P<0.05). Conclusion: The S. cumini extract caused elevation of serum hepatic and renal biomarkers at 400 mg/kg and did not have a hepatoprotective effect.
背景:在传统医学中,对许多疾病和小病的治疗价值都有文献记载。这种植物的各种制剂已被制成,并特别用于家畜的肝脏炎症。此外,人类的许多肝脏疾病都是由酒精摄入引起的炎症性疾病。本研究旨在探讨鱼尾草对乙醇诱导的Wistar白化大鼠肝毒性的影响。方法:25只大鼠随机分为5组,每组5只。第一组为对照组,其余四组分别给予不同剂量的乙醇,以诱导肝脏和肾脏损伤。以200 mg/kg或400 mg/kg的浓度给药两剂。最后一组以10 mg/kg剂量给予水飞蓟素。收集并保存肝脏和肾脏组织样本用于组织学分析,并分析大鼠血清中相关的生化生物标志物。结果:组织病理学分析显示,提取物组肝细胞核固缩,排列扭曲。肾组织样本显示间质出血和肾小球周围淋巴细胞聚集的迹象。生化指标分析显示,各试验组血清中谷草转氨酶(AST)、谷丙转氨酶(ALT)、尿素和肌酐均显著高于对照组(P<0.05)。结论:400 mg/kg时,茴香提取物可引起血清肝脏和肾脏生物标志物升高,不具有保肝作用。
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引用次数: 0
Ameliorative Effect of Trevo Dietary Supplement Against Lead Acetate Nephrotoxicity Trevo膳食补充剂对醋酸铅肾毒性的改善作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-01-01 DOI: 10.32598/ijt.16.1.857.1
O. Ilesanmi, E. Agoro
Background: Trevo is a nutritional supplement with numerous bioactive natural products, with detoxifying and antioxidant properties. The purpose of this study was to investigate the ability of Trévo to protect against oxidative stress induced by lead in the kidneys of male Wistar rats. Methods: Thirty-five healthy male Wistar rats were divided into five groups of seven rats each, using a randomized design. I=control; II=15 mg/kg of lead acetate (PbA); III=2 ml/kg of trevo+PbA; IV=5 ml/kg of trevo+PbA; V=5 ml/kg of trevo. Animals were treated with trevo for five days before co-administration with lead intraperitoneally for 10 consecutive days. Animals were sacrificed 24hr after the last administration, blood samples were collected via cardiac puncture, and processed for assessment of urea, creatinine, and uric acid (UA), while the kidney samples were excised and processed for the following biochemical assays: Malondialdehyde (MDA), Glutathione-S-Transferase (GST), Catalase (CAT), Superoxide Dismutase (SOD), and Reduced Glutathione (GSH). Results: Injection of PbA caused a significant increase in the serum levels of urea, creatinine, and uric acid, and a significant increase (P<0.001) in the MDA concentration, and decreases in GSH concentration, CAT, SOD, and GST activities (P<0.05) as compared to the controls. Pretreatment with trevo prevented the oxidative stress induced by lead acetate in the kidney tissue samples and improve the renal function. The protective effect was evident at 5 ml/kg of trevo. Conclusion: The results showed that trevo was nephroprotective against lead toxicity and the activity might be linked to the presence of numerous antioxidant phytochemicals present in trevo.
背景:Trevo是一种营养补充剂,具有多种生物活性的天然产物,具有解毒和抗氧化特性。本研究的目的是研究trsamvo对雄性Wistar大鼠肾脏中铅引起的氧化应激的保护作用。方法:健康雄性Wistar大鼠35只,随机分为5组,每组7只。我=控制;II=15 mg/kg醋酸铅(PbA);III= 2ml /kg trevo+PbA;IV=5 ml/kg trevo+PbA;V= 5ml /kg的trevo。动物先用三氟唑啉治疗5天,然后与铅腹腔内共给药,连续10天。末次给药后24小时处死动物,穿刺取血检测尿素、肌酐、尿酸(UA),取肾检测丙二醛(MDA)、谷胱甘肽s转移酶(GST)、过氧化氢酶(CAT)、超氧化物歧化酶(SOD)、还原性谷胱甘肽(GSH)。结果:与对照组相比,注射PbA使血清尿素、肌酐、尿酸水平显著升高(P<0.001), MDA浓度显著升高(P<0.001), GSH浓度、CAT、SOD、GST活性显著降低(P<0.05)。trevo预处理可抑制醋酸铅引起的肾组织氧化应激,改善肾功能。在5 ml/kg的剂量下,保护作用明显。结论:三叶参具有抗铅肾保护作用,其作用机制可能与三叶参中含有多种抗氧化植物化学物质有关。
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引用次数: 2
The Extract of Viola odorata Flowers Improves the Biochemical, Pancreas Histological, and Insulin Resistance Parameters in an Animal Model of Diabetes 堇菜花提取物改善糖尿病动物模型的生化、胰腺组织学和胰岛素抵抗参数
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-01-01 DOI: 10.32598/ijt.16.1.869.1
R. Gazor, F. Niknezhad, Fatemeh Yousefbeyk, Monireh Aghajany-Nasab, F. Mohammadghasemi
Background: The antioxidant defense in the pancreas is low because they are exposed to toxic substances daily. This study aimed to evaluate the ameliorating effect of Viola odorata flowers Extract (VOE) on the pancreas histology and function in Streptozotocin (STZ)-induced diabetic rats. Methods: Forty male rats were divided into five groups, consisting of controls; STZ; and STZ plus various doses of VOE (100, 200 or 400 mg/kg). The amylase, lipase, insulin and total antioxidant capacity levels were measured in the sera. The homeostatic model assessment of insulin resistance was also measured. The histopathological alterations of the rats’ pancreases were examined microscopically. Results: The serum amylase and total antioxidant activities were reduced in diabetic rats (P=0.001). Varying doses of VOE reduced the serum amylase and glucose levels, and increased the total antioxidant activities compared to that of the diabetic rats (P<0.05). There were no significant differences in the serum lipase and insulin levels among the groups. Treatment with VOE at all doses significantly lowered the insulin resistance compared to that of the diabetic group (P=0.001). Significant reductions were observed in the areas of the pancreatic Langerhans islets and the number of beta cells in the STZ group (P=0.001). Conclusion: This study demonstrated that VOE ameliorated the adverse effects induced by STZ in the rat’s pancreas in the short-term. These effects are likely to be due to the reduced insulin resistance and amylase activity, and increased total antioxidant activity along with the histopathological alterations in the pancreas.
背景:胰腺的抗氧化防御能力较低,因为它们每天都暴露在有毒物质中。本研究旨在探讨堇菜花提取物(VOE)对链脲佐菌素(STZ)诱导的糖尿病大鼠胰腺组织和功能的改善作用。方法:40只雄性大鼠分为5组,对照组;STZ;和STZ加上不同剂量的VOE(100、200或400 mg/kg)。测定血清中淀粉酶、脂肪酶、胰岛素和总抗氧化能力水平。还测量了胰岛素抵抗的稳态模型评估。显微镜下观察大鼠胰腺组织病理学改变。结果:糖尿病大鼠血清淀粉酶和总抗氧化活性降低(P=0.001)。与糖尿病大鼠相比,不同剂量的VOE降低了血清淀粉酶和葡萄糖水平,提高了总抗氧化活性(P<0.05)。各组间血清脂肪酶和胰岛素水平无显著差异。与糖尿病组相比,所有剂量的VOE治疗均显著降低了胰岛素抵抗(P=0.001)。STZ组胰腺朗格汉斯胰岛面积和β细胞数量显著减少(P=0.001)。结论:本研究表明,VOE可在短期内改善STZ对大鼠胰腺的不良反应。这些影响可能是由于胰岛素抵抗和淀粉酶活性降低,总抗氧化活性增加以及胰腺的组织病理学改变。
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引用次数: 1
Septilin, A Polyherbal Formulation Against the Immunosuppression Induced by Cyclophosphamide and Cisplatin in Swiss Albino Mice 复方Septilin抗环磷酰胺和顺铂对瑞士白化病小鼠免疫抑制作用的研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-01-01 DOI: 10.32598/ijt.16.1.853.1
S. S., B. K. Shenoy
Background: Septilin (Spt) is an ayurvedic drug formulation from Himalaya Drug Company and is well-known for its antibacterial, anti-inflammatory and immunomodulatory activities. Interest in the use of medicinal plants and herbal medicine as immunomodulators has currently been the subject of scientific investigation worldwide. Cyclophosphamide (CP) and Cisplatin (Csp) are widely used chemotherapeutic drugs and are known for their immunosuppressive effects. Methods: The present study evaluated the immune-stimulating activity of Spt (125, 250 and 500 mg/kg; PO/7 days) against CP (50 mg/kg) and Csp (10 mg/kg) induced immunosuppression in mice sensitized with sheep Red Blood Cells (RBC) by measuring Hemagglutination Antibody (HA) titre values and by determining the haematological parameters, such as Haemoglobin (Hb) content, White Blood Cells (WBC), RBC and platelet counts. Thymus index and differential counts of leukocytes were also determined. Results: Upon HA assay, the titre was significantly decreased in CP (59.40%) and Csp (62.16%) in the treatment groups (P<0.001). An increase in the HA titre value in Spt-treated mice showed the stimulation of humoral immune response (P<0.001). The results of haematological study in Spt-treated mice indicated stimulation of total leukocytes, RBC and platelet counts. Moreover, Spt treatment prior to the administration of CP and Csp prevented the loss of body weight and minimized their adverse effect on the mice thymus. Conclusion: Our experimental evidence suggests the immunostimulatory potency of Spt against the immunosuppression induced by chemotherapeutic drugs in mice. The study results are comparable with the immune-potentiating effects of standard immunomodulatory drug Levamisole (Lev). Hence, Spt may be used as an adjuvant to obviate the immune suppression induced by chemotherapeutic medications.
背景:Septilin (Spt)是喜玛拉雅制药公司生产的一种印度草药制剂,具有抗菌、抗炎和免疫调节作用。对使用药用植物和草药作为免疫调节剂的兴趣目前已成为世界范围内科学研究的主题。环磷酰胺(CP)和顺铂(Csp)是广泛使用的化疗药物,以其免疫抑制作用而闻名。方法:观察Spt(125、250、500 mg/kg)的免疫刺激活性;通过测定血凝抗体(HA)滴度值和血液学参数,如血红蛋白(Hb)含量、白细胞(WBC)、红细胞和血小板计数,对绵羊红细胞(RBC)致敏小鼠进行免疫抑制。同时测定胸腺指数和白细胞的差异计数。结果:经血凝素测定,治疗组CP滴度(59.40%)和Csp滴度(62.16%)显著降低(P<0.001)。spt处理小鼠的HA滴度值升高,显示出体液免疫反应的刺激(P<0.001)。spt治疗小鼠的血液学研究结果显示,总白细胞、红细胞和血小板计数受到刺激。此外,在给予CP和Csp之前进行Spt治疗可以防止体重减轻,并将其对小鼠胸腺的不良影响降至最低。结论:Spt对化疗药物引起的小鼠免疫抑制具有免疫刺激作用。研究结果与标准免疫调节药物左旋咪唑(Lev)的免疫增强作用相当。因此,Spt可以作为一种佐剂来消除化疗药物引起的免疫抑制。
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引用次数: 1
A Five-year Report on Body Packing and Body Stuffing in Isfahan 伊斯法罕的尸体包装和尸体填充五年报告
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-10-01 DOI: 10.32598/ijt.15.4.120.3
F. Gheshlaghi, Mojgan Gomari, S. Greene, J. Rotella, Shayan Gheshlaghi
Background: Body packing and body stuffing of illicit drugs have increased in recent decades. The drug contents of the packages vary from region to region, and there are controversies surrounding the diagnostic and therapeutic methods. The aim of this study was to explore the clinical presentations, diagnostic and therapeutic measures, and the subsequent clinical outcomes of drug concealment by people. Methods: A retrospective analysis was performed on data for all cases of body packing and body stuffing that were referred to a university hospital, in Isfahan, Iran, from Mar. 2013 to Feb. 2018. Results: Sixty-eight body stuffers and 18 body packers (n=86) were included in this study. Seventy-eight patients (90.7%) were male, mostly aged between 20 to 40 years. There was no significant difference between the two groups with respect to the signs and symptom, hospital stay, treatment and clinical outcomes. Heroin and crystal methamphetamine, n=52 (60%) and n=22 (25%), respectively, were the most substances detected, irrespective of the concealment method. Abdominal X-ray and CT scan tests were positive for the detection of at least one packet in each of the 94.4% of the patients. Conclusion: Heroin and crystal methamphetamine were the most common substances concealed in the bodies of the patients. Based on our findings, CT scan was more sensitive than abdominal X-ray test in the detection of illicit drug packets concealed in the patients. Close observation and whole bowel irrigation were effective therapeutic modalities in most cases. All cases were fully recovered and discharged from the hospital.
背景:近几十年来,非法药物的尸体包装和尸体填塞有所增加。不同地区包装的药物成分不同,围绕诊断和治疗方法存在争议。本研究旨在探讨人藏药的临床表现、诊疗措施及后续临床结局。方法:回顾性分析2013年3月至2018年2月在伊朗伊斯法罕某大学医院转诊的所有尸体包装和尸体填充物病例的数据。结果:共纳入68例填充物和18例填充物(n=86)。男性78例(90.7%),年龄多在20 ~ 40岁之间。两组在症状体征、住院时间、治疗和临床结果方面无显著差异。无论采用何种隐蔽方式,检出最多的是海洛因和冰毒,分别为52(60%)和22(25%)。在94.4%的患者中,腹部x线和CT扫描检查至少检测到一个包。结论:海洛因和甲基苯丙胺晶体是患者体内最常见的隐藏物质。结果表明,CT扫描比腹部x线检查对隐藏在患者体内的非法药物包更敏感。密切观察和全肠冲洗是大多数病例有效的治疗方法。所有病例均已完全康复出院。
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引用次数: 0
Effect of Nano-eugenol and Aerobic Exercise Against the Streptozotocin Toxicity and Inflammatory Mediators P38-MAPK, NPY, and A-Rα2A in the Dorsal Root Ganglia of Diabetic Rats 纳米丁香酚和有氧运动对糖尿病大鼠背根神经节中链脲佐菌素毒性及炎症介质P38-MAPK、NPY和a - r - α 2a的影响
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-10 DOI: 10.32598/IJT.15.3.822.1
Abbas Shareghi boroujeni, K. J. Dehkordi, G. Sharifi, F. Taghian, Z. Mazaheri
Background: The aim of this study was to investigate the effects of nano-eugenol combined with aerobic exercise against the streptozotocin toxicity and inflammatory mediators P38-MAPK, NPY and A-Rα2A in the dorsal root ganglia of diabetic rats. Methods: Twenty-five, 8-week-old Wistar male rats were divided into 5 groups: 1) normal control group (normal model); 2) diabetic control group (diabetic model); 3), diabetic + exercise group (diabetic+exercise model); 4) diabetic group + nano-eugenol (diabetic+nano model); and 5) diabetic + exercise + nano-eugenol (diabetic+exercise+nano model). Diabetes was induced in the experimental groups 2 through 5 by the intraperitoneal injection of streptozotocin at 4mg/100 grams of the rats’ body weight. The nano-eugenol supplement was also gavaged into the supplement groups 4 and 5 only. Groups 3 and 5 exercised progressively at a speed of 8 to 20 meter/min for 5 to 30 min, five days a week over the 8-week study duration. Results: The diabetic rats that exercised and were treated with the nano-eugenol, showed a significant decrease in P38-MAPK gene expression compared to the normal model group (P=0.001). The study of the therapeutic modalities also showed that only the diabetic + exercise + nano-eugenol group showed a significant increase in NPY and A-Rα2A genes compared to the normal model (P=0.001). Conclusion: Based on the results, the use of nano-eugenol supplementation combined with aerobic exercise is likely to be effective in controlling the neurological damages due to diabetes by negatively regulating the P38-MAPK gene while positively regulating the NPY and A-Rα2A genes in the DRG region.
背景:本研究旨在探讨纳米丁香酚联合有氧运动对糖尿病大鼠背根神经节链脲佐菌素毒性和炎症介质P38-MAPK、NPY和A-Rα2A的影响。方法:25只8周龄Wistar雄性大鼠分为5组:1)正常对照组(正常模型);2) 糖尿病对照组(糖尿病模型);3) 糖尿病+运动组(糖尿病+运动模型);4) 糖尿病组+纳米丁香酚(糖尿病+纳米模型);5)糖尿病+运动+纳米丁香酚(糖尿病+运动+nano模型)。实验组2-5通过腹膜内注射4mg/100g大鼠体重的链脲佐菌素诱导糖尿病。纳米丁香酚补充剂也仅被灌胃到补充剂组4和5中。第3组和第5组在8周的研究期间每周5天,以8至20米/分钟的速度进行5至30分钟的渐进式运动。结果:运动和纳米丁香酚治疗的糖尿病大鼠,与正常模型组相比,P38-MAPK基因表达显著降低(P=0.001)。治疗模式的研究还表明,只有糖尿病+运动+纳米丁香酚组的NPY和a-Rα2A基因与正常模型相比显著增加(P=0.001,纳米丁香酚补充与有氧运动相结合的使用可能通过负调控P38-MAPK基因而正调控DRG区域的NPY和A-Rα。
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引用次数: 3
Evaluation of Methadone Consumption Rate Based on Post-mortem Toxicology Examinations in Cases of Drug-related Deaths in Iran: 2015-2017 2015-2017年伊朗药物相关死亡病例中基于尸检的美沙酮消耗率评估
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-10 DOI: 10.32598/IJT.15.3.786.1
Jalil Hasani, Davood Mirtorabi, M. Ghadirzadeh, A. Mahdavi, S. H. Nazari
Background: Given the increasing prevalence of methadone overdose and the growing number of deaths in Iran, the present study was conducted to determine the mortality rate of methadone detected in the cadavers brought to the Forensic Medicine Organization between 2015 and 2017. Methods: This cross-sectional study was performed on 7,486 cases of substance abuse deaths registered in the Forensic Medicine Organization during 2015-2017. In order to investigate the drug abuse, samples collected from the cadavers were initially examined for their drug contents, such as methadone, by standard screening methods and then confirmed by Thin Layer Chromatography (TLC). Using two checklists, the information collected about each cadaver consisted of the identity, autopsy and laboratory data. After data collection, they were entered into the Stata software version 14 MP. Results: The cadavers’ mean age was 36.6±12.6 years. Over the 3-year duration of the study, the standardized mortality rate increased from 35 to 39 cases per million per year. Of these cases, 6066 were randomly assigned to toxicology, 50.1% had used methadone one month before their death. Approximately 75% of the methadone abusers had taken another drug simultaneously, mostly morphine or methamphetamine. Conclusion: Considering the relatively high prevalence of methadone detected post-mortem, monitoring for methadone entry into public market and identifying the death-related factors in the drug abusers are considered as significant measures to improve upon the current alarming situation in the Iranian society.
背景:鉴于美沙酮过量的流行和伊朗死亡人数的增加,本研究旨在确定2015年至2017年期间法医组织在尸体中检测到的美沙酮死亡率。方法:对2015-2017年法医学组织登记的7486例药物滥用死亡病例进行横断面研究。为了调查药物滥用,从尸体中收集的样本首先通过标准筛选方法检查其药物含量,如美沙酮,然后用薄层色谱法(TLC)进行确认。利用两份核对表,收集到的每具尸体的信息包括身份、尸检和实验室数据。数据收集后,将其输入Stata软件版本14mp。结果:平均年龄36.6±12.6岁。在为期3年的研究期间,标准化死亡率从每年每百万人35例增加到39例。在这些病例中,6066例被随机分配到毒理学组,50.1%的患者在死亡前一个月曾使用美沙酮。大约75%的美沙酮滥用者同时服用另一种药物,主要是吗啡或甲基苯丙胺。结论:鉴于死后美沙酮的检出率较高,监测美沙酮进入公共市场和确定药物滥用者的死亡相关因素被认为是改善伊朗社会目前令人震惊的状况的重要措施。
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引用次数: 0
Evaluation of the Extracts From Rhizomes of Polygonum bistorta for the Median Lethal Dosages in Swiss Albino Mice 白蓼根茎提取物对瑞士白化病小鼠中位致死剂量的评价
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-10 DOI: 10.32598/IJT.15.3.716.1
M. Pillai
Background: Polygonum bistorta has been used as a remedy for jaundice, smallpox, pimples, measles, cholera, diarrhoea, dysentery, expelling worms, insect stings and snakebites. In this study, the crude extract from P. bistorta and two fractions viz. hexane and chloroform obtained from the crude extract were studied for their median Lethal Dosages (LD50) in Swiss albino mice. Methods: Powdered rhizomes of P. bistorta was macerated with chloroform and the crude extract was dissolved in a solvent mixture of methanol/water (95:5). The mixture was then subjected to solvent-solvent partition, first with hexane followed by chloroform. The crude extract and the hexane and chloroform fractions were evaluated for their LD50 in Swiss albino mice of both sexes. Results: The LD50 of the crude extract and the hexane and chloroform fractions were determined to be 142.82, 200 and 200.17mg per kg of the mice body weight, respectively. Conclusion: The LD50 values of the crude extract and the hexane and chloroform fractions from P. bistorta were determined. The crude extract of P. bistorta had greater lethality than the hexane and chloroform fractions. This is the first report on the LD50 values of Swiss albino mice for P. bistorta.
背景:历史蓼已被用作治疗黄疸,天花,丘疹,麻疹,霍乱,腹泻,痢疾,驱虫,昆虫叮咬和蛇咬伤。本研究以白化病小鼠为研究对象,研究了白化病小鼠的中位致死剂量(LD50)。方法:用氯仿浸透根茎粉末,粗提物用甲醇/水(95:5)的混合溶剂溶解。然后将混合物进行溶剂-溶剂分割,首先是己烷,然后是氯仿。测定了粗提物和己烷、氯仿部分在瑞士白化病小鼠体内的LD50。结果:测定粗提物和己烷、氯仿部位的LD50分别为142.82、200和200.17mg / kg小鼠体重。结论:测定了历史藤粗提物和己烷、氯仿部分的LD50值。粗提物的致死率高于己烷和氯仿部分。这是首次报道瑞士白化小鼠对历史单胞菌的LD50值。
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引用次数: 0
A Comparative Study of the Cytotoxic Effects and Oxidative Stress of Gossypol on Bovine Kidney and HeLa Cell Lines 棉酚对牛肾脏和HeLa细胞系细胞毒性和氧化应激的比较研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-10 DOI: 10.32598/IJT.15.3.795.1
M. Daneshmand, J. Amoli, T. Esfahani
Background: Cotton seed is one of the main sources of protein in animal feeds, containing gossypol, which has been shown to have toxic effects. Results reported by various studies also indicate the anti-cancer effects of gossypol on various cell types. However, its toxic effects on human and animal cells have not been fully established. This study was planned to investigate, for the first time, the cytotoxic effects and oxidative stress induced by gossypol on normal Bovine Kidney (BK) and HeLa cell lines, representing typical healthy and cancer cells, respectively. Methods: The BK and HeLa cell lines were treated for 24, 48 or 72 hours with 5, 10 or 20 ppm of gossypol (+/-). The cellular bio-availability and cytotoxicity were measured by MTT assay. The catalase and Malondialdehyde (MDA) levels were also measured to represent the oxidative stress parameters. Results: The percentages of cytotoxicity in BK and HeLa cell lines were calculated at a gossypol concentration of 5, 10 and 20 ppm over 24, 48 or 72 hours of incubation, respectively. The Lethal Concentration 50 (lC50) values were also determined for the two cell lines. No changes in the catalase and lipid peroxidase activities were observed in either cell line. Conclusion: The percentage of the gossypol cytotoxicity was concentration-dependent. By comparing the IC50 in both cell lines using one-way Analysis of Variance (ANOVA) analysis, a significant difference was observed, suggesting that Hela cells were less sensitive to gossypol than the BK cells. Lack of changes in the oxidative stress, as tested by catalase and MDA assays, demonstrated that gossypol did not induce oxidative stress in either cell line.
背景:棉花种子是动物饲料中蛋白质的主要来源之一,含有棉酚,已被证明具有毒性作用。各种研究报告的结果也表明棉酚对各种细胞类型的抗癌作用。然而,它对人类和动物细胞的毒性作用尚未完全确定。本研究旨在首次研究棉酚对正常牛肾脏(BK)和HeLa细胞系(分别代表典型的健康和癌症细胞)的细胞毒性作用和氧化应激。方法:用5、10或20ppm棉酚(+/-)处理BK和HeLa细胞24、48或72小时。MTT法测定细胞生物利用率和细胞毒性。过氧化氢酶和丙二醛(MDA)水平也被测量以代表氧化应激参数。结果:在棉酚浓度为5、10和20ppm的条件下,分别培养24、48或72小时,计算BK和HeLa细胞系的细胞毒性百分比。还测定了两种细胞系的致死浓度50(lC50)值。在任一细胞系中均未观察到过氧化氢酶和脂质过氧化物酶活性的变化。结论:棉酚的细胞毒性百分比呈浓度依赖性。通过使用单因素方差分析(ANOVA)分析比较两种细胞系中的IC50,观察到显著差异,表明Hela细胞对棉酚的敏感性低于BK细胞。通过过氧化氢酶和MDA测定,氧化应激没有变化,这表明棉酚在两种细胞系中都没有诱导氧化应激。
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引用次数: 0
Synthesis, Characterization of Pyrano-[2,3-c]-Pyrazoles Derivatives and Determination of Their Antioxidant Activities 吡喃-[2,3-c]-吡唑衍生物的合成、表征及抗氧化活性测定
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-07-01 DOI: 10.32598/IJT.15.3.798.1
Boutaina Addoum, B. E. Khalfi, Mohamed Idiken, Souraya Sakoui, Reda Derdak, O. Filali, A. Elmakssoudi, A. Soukri
Background: Antioxidants are developed to assist the immune system and overcome oxidative stress, the aggression of cellular constituents due to imbalance between reactive oxygen species and the inner antioxidant system. The main objective of this study was to search for new and potent antioxidants to protect humans against diseases associated with oxidative stress. Methods: In this study, three pyrano-[2,3-c]-pyrazole derivatives were synthesized via Multicomponent Reaction (MCR) approach and were characterized, using a melting point, High-Performance Liquid Chromatography (HPLC), and spectroscopic analyses (IR; 1H-NMR; 13C-NMR). All of the generated compounds were screened for their antioxidant properties in vivo, using ciliate “Tetrahymena” as a model organism exposed to oxidative and nitrative stress. They were then studied in vitro by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays. Results: The results demonstrated that the three compounds (5a, b, c) are biologically active and possess potent antioxidant activities, especially the 5a and 5b derivatives. On the other hand, the in vitro bioassays revealed that the 5a derivative possessed a significant antioxidant activity much greater than ascorbic acid. Accordingly, the in silico data are consistent with the experimental data. Conclusion: These findings confirmed the potent antioxidant property of the synthesized compounds, providing us with new inspiration and challenges to design a library of pharmaceutical compounds with strong activity and low toxicity in the future.
背景:抗氧化剂是为了帮助免疫系统和克服氧化应激而开发的,氧化应激是由于活性氧和内部抗氧化系统之间的不平衡而引起的细胞成分的攻击。这项研究的主要目的是寻找新的强效抗氧化剂,以保护人类免受与氧化应激相关的疾病。方法:本研究采用多组分反应(MCR)方法合成了三种吡喃并[2,3-c]-吡唑衍生物,并用熔点、高效液相色谱(HPLC)和光谱分析(IR、1H-NMR和13C-NMR)对其进行了表征。使用纤毛虫“四膜虫”作为暴露于氧化和硝化应激的模型生物,在体内筛选所有产生的化合物的抗氧化特性。然后使用1,1-二苯基-2-苦基肼(DPPH)测定法对它们进行体外研究。结果:三个化合物(5a、b、c)均具有生物活性,并具有较强的抗氧化活性,特别是5a和5b衍生物。另一方面,体外生物测定显示,5a衍生物具有比抗坏血酸高得多的显著抗氧化活性。因此,计算机模拟数据与实验数据一致。结论:这些发现证实了合成化合物的强大抗氧化性能,为我们设计一个具有强活性和低毒性的药物化合物库提供了新的灵感和挑战。
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引用次数: 3
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Iranian Journal of Toxicology
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