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INFLUENCE OF A LOW-LEVEL SEMICONDUCTOR GALLIUM ARSENATE LASER IN EXPERIMENTAL ENVENOMATION INDUCED BY BOTHROPS ATROX SNAKE VENOM 低能级半导体砷酸镓激光对蝮蛇毒液实验中毒的影响
Pub Date : 2012-12-29 DOI: 10.3844/AJPTSP.2012.141.148
Elziliam Aranha de Sousa, J. A. H. M. Bittencourt, Nayana Keyla Seabra de Oliveira, S. V. C. Henriques, Leide C. S. Picanço, Camila Pena Lobato, J. R. Ribeiro, W. L. Pereira, J. Carvalho, J. Silva
Bothrops atrox is responsible for the majority of snakebite accidents in Brazilian Amazon and its venom can cause prominent local tissue damage. Experimental groups consisted of five male mice, each administered either B. atrox Venom (VB), B. atrox Venom + Antivenom (VAV), B. atrox Venom + Laser (VL), B. atrox Venom + Antivenom + Laser (VAVL), or Sterile Saline Solution (SSS) alone. Paw oedema was induced by intradermal administration of 0.05 mg kg-1 of B. atrox venom and was expressed in mm of directly induced oedema. Mice were subcutaneously injected with 0.10 mg kg-1 of venom for evaluation nociceptive activity and the time (in seconds) spent in licking and biting responses of the injected paw were taken as an indicator of pain response. Inflammatory infiltration was determined by counting the number of leukocytes present in the gastrocnemius muscle after venom injection (0.10 mg kg-1). Myotoxicity was studied by determining the plasmatic rise of creatine kinase activity after venom injection (0.20 mg kg-1). For histological examination of myonecrosis, venom (0.10 mg kg-1) was administered intramuscularly. The site of venom injection was irradiated by GaAs laser and some animals received antivenom intraperitoneally. GaAs laser irradiation administered in conjunction with antivenom, reduced pain, oedema, inflammation and myonecrosis induced by B. atrox venom in mice. The combined antivenom and GaAs laser treatment was more effective than separately treatments. The results suggest that laser therapy may reduce the local effects induced by B. atrox venom when associated with antivenom.
在巴西亚马逊地区,大多数蛇咬伤事故都是由Bothrops atrox造成的,它的毒液会造成明显的局部组织损伤。试验组为5只雄性小鼠,分别给药B. atrox毒液(VB)、B. atrox毒液+抗蛇毒血清(VAV)、B. atrox毒液+激光(VL)、B. atrox毒液+抗蛇毒血清+激光(VAVL)或单独给药无菌生理盐水(SSS)。经皮内给药0.05 mg kg-1的牛头蛇毒诱导足跖水肿,以mm为单位表达。小鼠皮下注射0.10 mg kg-1毒液,评价其痛觉活性,并以注射后爪的舔和咬反应时间(秒)作为疼痛反应的指标。注射毒液(0.10 mg kg-1)后,通过计数腓肠肌中存在的白细胞数量来确定炎症浸润。通过测定注射毒液(0.20 mg kg-1)后血浆肌酸激酶活性的升高来研究肌肉毒性。肌肉注射毒液0.10 mg kg-1进行肌坏死组织学检查。用砷化镓激光照射毒液注射部位,部分动物腹腔注射抗蛇毒血清。GaAs激光照射联合抗蛇毒血清对小鼠的疼痛、水肿、炎症和肌坏死有明显的缓解作用。抗蛇毒血清和砷化镓激光联合治疗比单独治疗更有效。提示激光治疗与抗蛇毒血清联合使用,可明显减轻蛇毒所致的局部损伤。
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引用次数: 4
EVALUATION OF SELF-MEDICATION AMONG PHARMACY STUDENTS 药学专业学生自我药疗的评价
Pub Date : 2012-12-15 DOI: 10.3844/AJPTSP.2012.135.140
S. Sharif, O. M. Ibrahim, Laila Mouslli, Riham Waisi
To determine the incidence of self-medication among Sharjah university students and the impact of medical knowledge on such practice. A pre-validated questionnaire was distributed to 200 pharmacy students during May, 2012. Data were analyzed using SPSS and results expressed as counts and percentages. The overall response rate was 85% with 98% of respondents being Arabs. Females comprised about 91% of students and the mean age (SD) was 19.5(2.4). Practicing self-medication in the past year was high as145 (86%) used drugs without medical consultation. Most respondents (128, 76%) obtained their medication from pharmacies and used the medication for one week (106, 63%). Antibiotics were used by 54(32%) of students despite the fact that slightly more than 50% of students were aware of the possibility of emergence of bacterial resistance and were also aware of the concept of rational drug use in general. Main reasons for self-medication were non-serious health problem, illness is minor, seeking quick relief and to avoid long waiting hours at clinics. Reasons against self-medication include risks of adverse effects, using the wrong medication, drug interaction, misdiagnosis and drug abuse and dependence. Medical consultation is mainly sought in case of presence of severe pain, worsening of symptoms, or persistence of the latter for more than a week. Headache or mild pain, eye and ear symptoms, gastric problems, cold, fever and allergy were the commonest symptoms for self-medication. Knowledge of responsible self medication is inadequate but the practice is high and common among pharmacy students. Interventions to promote responsible self-medication among university students are required.
确定沙迦大学生自我药疗的发生率以及医学知识对这种做法的影响。于2012年5月向200名药学专业学生发放预验证问卷。数据采用SPSS统计软件进行分析,结果以计数和百分比表示。总体回复率为85%,98%的受访者是阿拉伯人。女生约占91%,平均年龄(SD)为19.5(2.4)岁。在过去一年中进行自我药疗的比例很高,有145人(86%)未经医疗咨询就使用了药物。大多数受访者(128.76%)从药店获得药物并使用一周(106.63%)。54名(32%)学生使用了抗生素,尽管略多于50%的学生知道细菌耐药性可能出现,也知道合理用药的概念。自我药疗的主要原因是健康问题不严重、病情轻微、寻求快速缓解和避免在诊所长时间等待。反对自我药疗的原因包括不良反应的风险、使用错误的药物、药物相互作用、误诊和药物滥用和依赖。主要是在出现剧烈疼痛、症状恶化或症状持续一周以上的情况下求诊。头痛或轻微疼痛、眼耳症状、胃病、感冒、发烧和过敏是自我药物治疗最常见的症状。负责任的自我药疗知识不足,但实践是高和普遍的药学学生。需要采取干预措施,在大学生中促进负责任的自我药疗。
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引用次数: 71
Neuropharmacological Assessment of an Aqueous Bark Extract of Antiaris toxicaria (Pers.) Lesch. (Moraceae) in Rodents 抗蛇皮水提物的神经药理学研究Lesch。啮齿类动物中的桑科动物
Pub Date : 2012-11-27 DOI: 10.3844/AJPTSP.2012.123.134
P. Mante, D. W. Adongo, K. E. Kukuia, E. Ameyaw, E. Woode
Antiaris toxicaria is a plant traditionally used in Ghana for the treatment of various neurological conditions such as epilepsy and pain. This present study therefore seeks to screen for the neuropharmacological activities of the aqueous extract of Antiaris toxicaria (AAE) stem bark. The effect of Antiaris extract on pentobarbital-induced sleeping time, tail immersion test, spontaneous locomotor activity, motor coordination, PTZ-induced convulsions as well as the Irwin test was investigated. The extract produced analgesia and Straub tail at (300-3000 mg kg-1) in the Irwin test suggestive of a morphine-like action. These effects were absent after 24 h. No deaths were recorded in the test estimating the LD50 to be above 3000 mg kg-1. Spontaneous locomotor activity of the mice in the activity meter test was decreased significantly (p
抗毒草是加纳传统上用于治疗癫痫和疼痛等各种神经系统疾病的植物。因此,本研究旨在筛选抗炎草(AAE)茎皮水提物的神经药理活性。观察抗炎参提取物对戊巴比妥致大鼠睡眠时间、尾浸试验、自主运动活动、运动协调、ptz致惊厥及Irwin试验的影响。在欧文试验中,该提取物在(300-3000 mg kg-1)时产生镇痛和斯特劳布尾,提示有吗啡样作用。这些影响在24小时后消失。在估计LD50高于3000 mg kg-1的试验中,没有记录到死亡。活动计试验小鼠自发运动活性显著降低(p
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引用次数: 5
PROTECTION OF TERMINALIA BELERICA ROXB. AGAINST IRON OVERLOAD INDUCED LIVER TOXICITY: AN ACCOUNT OF ITS REDUCING AND IRON CHELATING CAPACITY 终端机的保护。抗铁超载引起的肝毒性:其还原和铁螯合能力的说明
Pub Date : 2012-11-20 DOI: 10.3844/AJPTSP.2012.109.122
B. Hazra, Rhitajit Sarkar, N. Mandal
Excess iron deposition in the liver catalyses the production of Reactive Oxygen Species (ROS) which in turn initiate oxidative damage of protein and nucleic acids leading to several human diseases. The fruits of Terminalia Belerica Roxb. (TB) has been most commonly used not only in stimulating gastrointestinal health, but also in treatment of various hepatic disorders. The present study was aimed to evaluate the ameliorating effect of 70% methanol extract of TB (TBME) on iron overload induced liver injury, along with its in vitro iron chelating and DNA protection studies. Iron overload was induced by intraperitoneal administration of iron-dextran into mice. The biochemical markers of hepatic damage, liver iron, protein carbonyl and hydroxyproline content were measured in response to the oral administration of TBME. The reductive release of ferritin iron by TBME was further studied. The extract exhibited significant iron chelation with IC50 of 27.70 ± 2.27 µg mL-1 and considerable DNA protection with [P]50 of 1.30 ± 0.01 µg mL-1. Treatment with different doses (50, 100 and 200 kg body weight) of TBME showed dose dependent reduction in liver iron, lipid peroxidation, protein oxidation, liver fibrosis, serum enzymes and ferritin. The antioxidant enzymes levels were enhanced and the reductive release of ferritin iron increased significantly with gradually increasing concentrations of TBME. From the present results, it appears possible to support that TBME represents beneficial effects on iron overload mediated liver toxicity and hence possibly useful as iron chelating drug for iron overload diseases.
肝脏中过量的铁沉积催化活性氧(ROS)的产生,进而引发蛋白质和核酸的氧化损伤,导致几种人类疾病。秋葵的果实。(TB)不仅用于刺激胃肠道健康,而且还用于治疗各种肝脏疾病。本研究旨在评价TB 70%甲醇提取物(TBME)对铁超载诱导的肝损伤的改善作用,并进行体外铁螯合和DNA保护研究。通过腹腔注射右旋糖酐铁诱导小鼠铁超载。测定大鼠口服TBME后肝损伤生化指标、肝铁、蛋白羰基和羟脯氨酸含量。进一步研究了TBME对铁蛋白铁的还原释放。提取物具有显著的铁螯合作用,IC50为27.70±2.27µg mL-1,具有较好的DNA保护作用,[P]50为1.30±0.01µg mL-1。不同剂量(50、100和200 kg体重)TBME治疗肝铁、脂质过氧化、蛋白质氧化、肝纤维化、血清酶和铁蛋白均呈剂量依赖性降低。随着TBME浓度的逐渐升高,抗氧化酶水平增强,铁蛋白铁的还原释放显著增加。从目前的结果来看,似乎有可能支持TBME对铁超载介导的肝毒性具有有益作用,因此可能作为铁螯合药物用于铁超载疾病。
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引用次数: 11
Possible Mechanism of Plumbago zeylanica in Prevention of Hepatic Dammage in Wistar Rat 白花苜蓿预防Wistar大鼠肝损伤的可能机制
Pub Date : 2012-11-20 DOI: 10.3844/AJPTSP.2012.101.108
R. Goyal, P. Sharma
Plumbago zeylanica root has been used traditionally to treat various body ailments including liver diseases. The present study was designed to investigate the hepatoprotective effects of standardized methanolic extract of Plumbago zeylanica root on paracetamol, CCl4 and alcohol induced hepatic injuries in rats and its possible mechanism(s) of hepatoprotection. Administration of hepatotoxicants like paracetamol (3 g kg-1, p.o.) or CCl4 (1 mL kg-1, s.c.) or alcohol (15 g kg-1, p.o.) to Wistar albino rats (180-240 g of either sex, n = 8) caused significant increase in serum ALT, AST, ALP and bilirubin; tissue lipid peroxidation, nitrite/nitrate, collagen; and decrease in tissue GSH and SOD levels. The liver histopathology revealed central vein dilation, infiltration and fatty degeneration in hepatotoxicant control groups. Pretreatment with methanolic extract of Plumbago zeylanica (100, 200 and 400 mg kg-1) and silymarin (50 mg kg-1) as standard significantly reversed these toxic changes dose dependently, as compared to hepatotoxicant control. The results in present study suggested that Plumbago zeylanica root possesses marked hepatoprotective potential through its oxidative, inflammatory and fibrotic effects against experimentally induced liver toxicity. These findings support and extend the rational basis for the use of this plant as hepatoprotective in traditional and folk-lore medicine.
传统上,白芷根被用来治疗各种身体疾病,包括肝脏疾病。本研究旨在探讨白花苜蓿根标准化甲醇提取物对扑热息痛、CCl4和酒精致大鼠肝损伤的保护作用及其可能的机制。给Wistar白化大鼠(雌雄各180-240 g, n = 8)服用肝毒物如扑热息痛(3 g kg-1, p.o.)或CCl4 (1 mL kg-1, p.o.)或酒精(15 g kg-1, p.o.)引起血清ALT、AST、ALP和胆红素显著升高;组织脂质过氧化,亚硝酸盐,胶原蛋白;组织GSH和SOD水平降低。肝毒性对照组肝组织病理显示中心静脉扩张、浸润及脂肪变性。与肝毒性对照相比,以白花苜蓿甲醇提取物(100、200和400 mg kg-1)和水飞蓟素(50 mg kg-1)为标准进行预处理可显著逆转这些毒性变化。本研究结果表明,白花苜蓿根对实验性肝毒性具有氧化、炎症和纤维化作用,具有明显的肝保护作用。这些发现支持和扩展了传统和民间医学中使用该植物作为保护肝脏的合理依据。
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引用次数: 4
CIPROFLOXACIN INDUCED CHONDROTOXICITY AND TENDINOPATHY 环丙沙星诱导软骨毒性和肌腱病变
Pub Date : 2012-10-19 DOI: 10.3844/AJPTSP.2012.94.100
Elias Adikwu, N. Brambaifa
Ciprofloxacin is one of the fluoroquinolones with a wide clinical acceptability. Rescently there are increasing reports on Ciprofloxacin induce Chondrotoxicity and Tendinopathy in Animal experiment and clinical experience which is of great clinical concern. A comprehensive survey and review of literaure on reported ciprofloxacin induced Chondrotoxicity and Tendinopathy in Humans and Animals was performed. It was observd that ciprofloxacin is a potential inducer of Chrondrotoxicity and Tendinopathy which could be potentiated by coadministration with corticosteroids.This conditions were reported to be characterised by cartilage lesion, matrix swelling, inhibition of chondrocytes proliferation, secretion of soluble proteoglycan, modification of the metabolism and integrity of extracellular proteins, decrease in epiphyseal growth plate, humerus and femur.The mechanism behind this phenomenon is said to be multifactoral. Ciprofloxacin induced Chrondrotoxicity and Tendinopathy in growing animals is attributed to oxidative stress (lipid peroxidation, Deoxyribonucleic Acid (DNA) oxidative stress). Ciprofloxacin induced cartilage damage may also be attributed to formation of Ciprofloxacin chelates and complexes which possesses the potential to induce a deficiency of functionally available divalent ions resulting in cytoskeletal changes. Animal studies showed that oxidative damage or metabolism of tissues was also found suggesting the involvement of a reactive oxygen species. Administration of magnesium, zinc chloride and vitamin E (α tocopherol) were found to prevent or reverse ciprofloxacin induced Chrondrotoxicity and Tendinopathy. Through excess formation of collagen, increase osteoblastic activity, increase bone growth, inhibition of free oxidation radicals’ formation thereby preventing DNA oxidation and oxidative stress. Zinc also directly stimulates DNA synthesis either by enzyme stimulation or altering, the binding of f1 and f3 histones to DNA so as to affect RNA synthesis. Patient medical history should be considered before Ciprofloxacin recommendation. Coadministration with corticosteroid should be done with caution. Further evaluation of antioxidants effect in Ciprofloxacin induce Chonrotoxicity, Tendinopathy in humans could be of clinical importance as observed in Animal studies.
环丙沙星是临床广泛接受的氟喹诺酮类药物之一。近年来,环丙沙星在动物实验和临床经验中引起软骨毒性和肌腱病变的报道越来越多,引起了临床的高度关注。本文对环丙沙星在人类和动物中引起的软骨毒性和肌腱病变的文献进行了全面的调查和回顾。观察到环丙沙星是一种潜在的慢性毒性和肌腱病变的诱导剂,与皮质类固醇共给药可增强。据报道,这种情况的特征是软骨病变、基质肿胀、软骨细胞增殖抑制、可溶性蛋白聚糖分泌、代谢和细胞外蛋白完整性改变、骨骺生长板、肱骨和股骨减少。这种现象背后的机制据说是多因素的。环丙沙星对生长动物的慢性毒性和肌腱病变可归因于氧化应激(脂质过氧化、脱氧核糖核酸(DNA)氧化应激)。环丙沙星诱导的软骨损伤也可归因于环丙沙星螯合物和复合物的形成,其具有诱导功能可用二价离子缺乏导致细胞骨架变化的潜力。动物研究表明,组织的氧化损伤或代谢也被发现,表明活性氧的参与。镁、氯化锌和维生素E (α生育酚)可预防或逆转环丙沙星引起的慢性毒性和肌腱病变。通过过量形成胶原蛋白,增加成骨细胞活性,促进骨骼生长,抑制自由基的形成,从而防止DNA氧化和氧化应激。锌也通过酶刺激或改变f1和f3组蛋白与DNA的结合直接刺激DNA合成,从而影响RNA合成。在推荐使用环丙沙星之前应考虑患者的病史。与皮质类固醇合用应谨慎。进一步评估环丙沙星抗氧化剂对人体软骨毒性和肌腱病变的影响,在动物实验中可以观察到具有临床意义。
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引用次数: 8
FORMULATION AND CLINICAL TESTING OF GLYCERYL TRINITRATE OINTMENT FOR TREATMENT OF ANAL FISSURES 三硝酸甘油软膏治疗肛裂的配方及临床试验
Pub Date : 2012-09-01 DOI: 10.3844/AJPTSP.2012.89.93
A. Khaleel, H. Mahdi, E. Yousif, Shathel K. Noaman
Until know surgical intervention considered to be the cornerstone for treatment of anal fissure condition. Regarding all the circumstances that hinder the possibility of accomplishment of surgical operation and the possible post-urgical complications; all that motivates the necessity for a non-surgical procedure for treatment of anal fissure. This study was designed to establish a pharmaceutically active and chemically and physically stable formula of 0.4% (w/w) glyceryl trinitrate ointment. High Performance Liquid Chromatography (HPLC) was used to assay the active ingredient and to determine the rate of release of glyceryl trinitrate from the prepared ointment base. After establishing the formula, the prepared ointment was clinically tested on selected patients under supervision of specialized surgeons. After 3 months monitoring of a small scale pilot batch of 0.4% glyceryl trinitrate ointment and depending on Accelerated stability method, a physically and chemically stable formula was achieved with an unaltered pH and with a release rate value range between 83.4-85.1%. Up to 6 months of clinical follow up shows a variation in responses from complete healing to moderate relief of symptoms. Glyceryl trinitrate shows a high rate of healing for both acute and chronic anal fissures with tolerable side effect. A significant rate of pain relief and a high rate of complete healing lead to a conclusion of effectiveness of glyceryl trinitrate as a non-surgical treatment of both chronic and acute anal fissure.
直到知道手术干预被认为是治疗肛裂状况的基石。对一切妨碍手术顺利进行的情况和可能发生的术后并发症;所有这些都促使了非手术治疗肛裂的必要性。本研究旨在建立一种具有药理活性、化学和物理稳定性的0.4% (w/w)三硝酸甘油软膏配方。采用高效液相色谱法测定其有效成分,并测定三硝酸甘油的释放率。建立配方后,在专科医生的监督下,对选定的患者进行临床试验。经过对小规模中试批次0.4%三硝酸甘油软膏3个月的监测,并根据加速稳定法,获得了物理化学稳定的配方,pH不变,释放率范围在83.4-85.1%之间。长达6个月的临床随访显示,从完全愈合到症状中度缓解的反应各不相同。三硝酸甘油对急性和慢性肛裂均有很高的治愈率,副作用可容忍。显著的疼痛缓解率和高的完全愈合率使得三硝酸甘油作为一种非手术治疗慢性和急性肛裂的有效结论。
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引用次数: 0
COSCINIUM FENESTRATUM PROTECTS AGAINST ETHANOL- INDUCED NEURODEGENERATION IN ADULT RAT BRAIN 麝香草对乙醇诱导的成年大鼠脑神经变性有保护作用
Pub Date : 2012-08-16 DOI: 10.3844/AJPTSP.2012.81.88
W. Phachonpai, J. Wattanathorn, P. Wannanon, Chonlatip Thipkaew, B. Sripanidkulchai, S. Muchimapura
Alcoholism is a serious problem throughout the world. Despite intensive efforts to develop novel therapeutics for strategy efficacy against neuronal loss leading to memory impairment in alcoholism is still limited. In view of the pitfalls of psychological dependence and adverse behavioral effects of synthetic drugs, the development of low toxicity and high efficiency medicines derived from natural herbal antioxidants exhibits expansive market prospects. In this respect, Coscinium Fenestratum (C. Fenestratum; CF) could be an attractive candidate as a diet supplement for neuroprotactant against ethanol-induced neurodegeneration. Herein, we determined the neuroprotective effects of CF against ethanol-induced neuronal damage in both hippocampus and cerebral cortex. The stems of CF extract (No. HHP-2-462) were dried, refluxed with ethanoland evaporated with lyophilizer. Extract was gave a yield of 8.53%. The rats were pretreated with the extract at various doses ranging from 5, 10 and 20 mg kg-1 once daily per os, 30 min prior to ethanol administration at a dose of 1.8 g kg-1 via i.p for 14 consecutive days and were evaluated the densities of survival and cholinergic neurons in all areas as mention above by immune histological techniques. CF extract at a dose of 5 mg kg-1 showed the attenuation of the neurotoxicity in all brain areas just mentioned except in the temporal cortex. In addition, it also mitigated the degeneration of cholinergic neurons in all areas of hippocampus except in CA3 region. This study indicated that CF extract consumption may be served as a diet supplement protect against neuronal degeneration resulting from excessive continuous consumption of alcohol. However, further researches about possible active ingredients and pharmacokinetic of the extract are still required before moving forward to clinical trial study.
酗酒是全世界的一个严重问题。尽管大力开发新的策略治疗方法,但针对酒精中毒导致记忆障碍的神经元丧失的疗效仍然有限。鉴于合成药物存在心理依赖和不良行为效应的隐患,天然草药抗氧化剂衍生的低毒高效药物的开发具有广阔的市场前景。在这方面,Coscinium Fenestratum (C. Fenestratum;CF)可能是一种有吸引力的候选,作为一种饮食补充,以防止乙醇诱导的神经变性。在此,我们确定了CF对乙醇诱导的海马和大脑皮层神经元损伤的神经保护作用。CF提取液茎部(编号;HHP-2-462)干燥,用乙醇回流,用冻干机蒸发。提取液得率为8.53%。在以1.8 g kg-1的剂量通过腹腔灌胃给药前30分钟,以5、10和20 mg kg-1的不同剂量的提取物预处理大鼠,连续14天,通过免疫组织学技术评估上述各区域的存活率和胆碱能神经元密度。在剂量为5mg kg-1时,除颞叶皮质外,上述所有脑区神经毒性均有所减弱。此外,它还能减轻除CA3区外海马各区域胆碱能神经元的变性。本研究表明,食用CF提取物可作为一种饮食补充,防止过度连续饮酒导致的神经元变性。然而,在进入临床试验研究之前,还需要进一步研究其可能的有效成分和药代动力学。
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引用次数: 3
Gastroprotective Effect and Safety Assessment of Zanthoxylum Zanthoxyloides (Lam) Waterm Root Bark Extract 花椒水皮提取物的胃保护作用及安全性评价
Pub Date : 2012-08-07 DOI: 10.3844/AJPTSP.2012.73.80
A. Boye, G. Koffuor, J. N. Boampong, Patrick Amoateng, E. Ameyaw, E. Ansah, Gabriel Manu Addai, Cecilia Konama Adjei, J. Addo, D. Penu
Problem statement: Gastrointestinal ulcers account significantly for morbidity and mortality in Ghana. The study therefore investigate d the gastroprotective effect of an ethanolic root bark extract of Zanthoxylum zanthxyloides and its safety for us. Approach: Gastric ulceration was induced in Sprague-Dawley rats with Indomethacin (25 mg kg -1 , p.o) and was treated with 150, 250, or 500 mg kg -1 of the extract, or 20 mg kg -1 Esomeprazole. The number of ulcers per stomach, Ulcerative Index and Curative Ratio were determined. A histolo gical study of the gastric mucosa was also performed. The extract's effect on an isolated guin ea-pig ileum preparation was investigated to elucidate its possible mechanism of action. Safety assessments involving, organ weight to body weight ratio determination, hematological analysis and liv er function tests were performed. Results: The extract significantly decreased (p ≤0.001) the number of ulcers per stomach and the Ulc erative Index (similar to Esomeprazole) and significantly increas ed (p ≤0.001) the Curative Ratio in a dose-dependent manner. It completely corrected the architectural d istortions caused by gastric ulceration and inhibit ed significantly (p ≤0.001) the contractile responses of the isolated gu inea-pig ileum to Acetylcholine, Nicotine and Histamine in a manner comparable to reference antagonists. The extract had no significant effect (p>0.05) on organ weight to body ratio and hematological profile. Plasma levels of Alanine transaminase and Alkaline phosphatase decreased significantly (p ≤0.001) in extract and Esomeprazole-treated ulcerated rats. Levels of Gamma-glutamyl transferase , Total bilirubin (direct and indirect) however increased significantly (p≤0.01-0.001). Conclusion/Recommendations: Per the findings, the ethanolic root bark extract of Zanthoxylum zanthoxyloides has gastroprotective effect in Sprague-Dawley rats working possibly via antimuscarinic or antihistaminic mechanism. It however has a potential of causing cholestasis hence liver func tion should be monitored.
问题说明:胃肠道溃疡在加纳的发病率和死亡率中占有重要地位。研究了花椒乙醇根皮提取物的胃保护作用及其对人体的安全性。方法:用吲哚美辛(25 mg kg -1, p.o)诱导sd大鼠胃溃疡,分别用吲哚美辛提取物150、250、500 mg kg -1或埃索美拉唑提取物20 mg kg -1处理。测定每胃溃疡数、溃疡指数和治愈率。同时对胃粘膜进行组织学检查。研究了该提取物对离体豚鼠-猪回肠制剂的作用,以阐明其可能的作用机制。安全性评估包括器官重量与体重比测定、血液学分析和肝功能测试。结果:该提取物显著降低(p≤0.001)每胃溃疡数和溃疡指数(与埃索美拉唑相似),显著提高治愈率(p≤0.001),且呈剂量依赖性。它完全纠正了胃溃疡引起的结构扭曲,并显著抑制离体猪回肠对乙酰胆碱、尼古丁和组胺的收缩反应(p≤0.001),其效果与对照拮抗剂相当。对脏器体重比和血液学指标无显著影响(p>0.05)。溃疡大鼠血浆丙氨酸转氨酶和碱性磷酸酶水平显著降低(p≤0.001)。然而,γ -谷氨酰转移酶、总胆红素(直接和间接)水平显著升高(p≤0.01-0.001)。结论/建议:花椒乙醇根皮提取物对sd - dawley大鼠具有胃保护作用,可能是通过抗毒蕈碱或抗组胺作用机制。然而,它有可能引起胆汁淤积,因此应监测肝功能。
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引用次数: 21
Quercetin in Dimethyl Benzanthracene Induced Breast Cancer in Rats 槲皮素对二甲基苯并蒽致大鼠乳腺癌的影响
Pub Date : 2012-07-30 DOI: 10.3844/AJPTSP.2012.68.72
N. S. Reddy, P. Nirmala, N. Chidambaram, Patidar Ashok Kumar
Problem statement: Vincristine a commonly used anticancer agent in th e treatment of breast cancer results in serious adverse effects li ke teratogenicity, neurotoxicity and carcinogenicit y on long term use. Drug resistance is also a common pro blem encountered with vincristine. Hence the effect of flavonol quercetin, a known antioxidant w ith no known documented adverse effect was tried in treatment of DMBA induced breast cancer in female rats and its effect was compared with vincristine. Approach: Quercetin at the dose of 50, 100-200 mg kg -1 body weight was administered in DMBA induced breast cancer in female wistar rats and its effects were compared with Vincristine. The anti oxidant enzymes, catalase, glutathione peroxid ase and superoxide dismutase and Thiobarbituric Acid Reactive Substances (TBARS) level in cancerous breast tissue, TBARS and catalase in plasma and superoxide dismutase and glutathione peroxidase in erythrocyte lysate were estimated. Results: Quercetin supplementation at the dose of 100 mg kg -1 body weight was most effective in alleviating cancer symptoms and was comparable to vincristine. The plasma TBARS were reduced and breast tissue TBARS were elevated. The antioxidant enzymes were rejuvenated by quercetin supplementation at all three dose levels. Conclusion: Quercetin is found to be an effective chemotherape utic agent in the treatment of breast cancer on par with vincrist ine. Being a plant product, quercetin can also be u sed in chemoprophylaxis in high risk individuals with g enetic predisposition towards breast cancer. Besides, it can be given orally and has a wide marg in of safety.
问题陈述:长春新碱是治疗乳腺癌常用的抗癌药物,长期使用会产生致畸、神经毒性、致癌性等严重不良反应。耐药性也是长春新碱遇到的一个常见问题。因此,黄酮醇槲皮素,一种已知的抗氧化剂,没有已知的不良反应,被用于治疗雌性大鼠DMBA诱导的乳腺癌,并与长春新碱进行了比较。方法:采用槲皮素50、100 ~ 200 mg kg -1体重剂量对DMBA诱导的雌性wistar大鼠乳腺癌进行治疗,并与长春新碱进行比较。测定癌性乳腺组织中抗氧化酶、过氧化氢酶、谷胱甘肽过氧化物酶、超氧化物歧化酶和硫代巴比妥酸活性物质(TBARS)水平,血浆中TBARS和过氧化氢酶水平,红细胞裂解液中超氧化物歧化酶和谷胱甘肽过氧化物酶水平。结果:槲皮素补充剂量为100 mg kg -1体重对缓解癌症症状最有效,与长春新碱相当。血浆TBARS降低,乳腺组织TBARS升高。槲皮素在三种剂量水平下均能使抗氧化酶恢复活力。结论:槲皮素是一种与长春素相当的治疗乳腺癌的有效化疗药物。作为一种植物产品,槲皮素也可用于具有乳腺癌遗传易感性的高危人群的化学预防。此外,它可以口服,有很大的安全范围。
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引用次数: 13
期刊
American Journal of Pharmacology and Toxicology
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