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Acute and Subchronic Oral Toxicities of Justicia pectoralis J. Extract in Wistar Rats 胸胸草提取物对Wistar大鼠的急性和亚慢性口服毒性
Pub Date : 2009-05-20 DOI: 10.2174/1874848100902010053
A. Lagarto, Viviana Bueno, I. Guerra, O. Valdés, Tatiana Gabilondo, Jorge Rodríguez
We have studied the acute and subchronic oral toxicities of Justicia pectoralis J hydroalcoholic extract in Wis- tar rats. In acute test, both sexes of adult Wistar rats were given single po dose of J. pectoralis extract at 2000 mg/kg. Fol- lowing euthanasia 14 days later, mortality and signs of toxicity were not observed. In subchronic test, J. pectoralis extract was po administered to both sexes of Wistar rats at 10, 100 and 1000 mg/kg/day, 5 days per week for 90 days. The major toxicological endpoints examined included animal body weight, food intake, selected tissue weights, and histopathologi- cal examinations. In addition, we examined blood elements and blood chemistry. Of the blood elements, the blood clotting time was significantly affected in males and females after 90 days. For blood chemistry parameters, cholesterol, ALT, bilirubin, and urea were affected. Organs and tissues abnormalities were not observed in histopathological examination. These results indicate that the effects observed are low and include slight variations in blood clotting time and biochemi- cal parameters.
研究了胸茱萸水酒精提取物对大鼠的急性和亚慢性口服毒性作用。急性试验中,雄性和雌性成年Wistar大鼠给予胸胸草提取物2000 mg/kg单次给药。在安乐死14天后,没有观察到死亡和毒性迹象。在亚慢性试验中,胸胸草提取物按10、100和1000 mg/kg/d给药Wistar大鼠,每周5天,连续90 d。检查的主要毒理学终点包括动物体重、食物摄入量、选定组织重量和组织病理学检查。此外,我们还检查了血液元素和血液化学。在血液元素中,90 d后男女的凝血时间受到显著影响。对于血液化学参数,胆固醇,ALT,胆红素和尿素受到影响。组织病理学检查未见脏器组织异常。这些结果表明,观察到的影响是低的,包括血液凝固时间和生化参数的轻微变化。
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引用次数: 1
Preclinical and clinical studies of Lapachol and beta-Lapachone. lapachhol和β - lapachone的临床前和临床研究。
Pub Date : 2009-04-14 DOI: 10.2174/1874848100902010042
E. R. Almeida
Lapachol whose isolation and study at the end of the century by Parterno, is one of the most brilliant chapters of Phytochemistry, especially in conjunction with the work of Max Siewert a communication on the wood of the Argen- tina Lapachol (Bignoniaceae) tree from Max Siewert, submitted along with Ricardo Napp in Exp. NAC. Philadelphia in 1876. The Lapachol has its origin in the Tabebuia avellanedae Lorentz ex. Griseb (Bignoniaceae) which in Brazil is known as Pau DArc, Ipe-purple, Ipe-Black, and Yellow-Ipe. It is a tree of huge size used in traditional medicine for cases of stomatitis, inflammatory processes in general and against cancer. � -Lapachone is an o-naphthoquinone from Lapachol used against, Trypanosome cruzi, cancer, viruses, bacteria, and leishmania is currently evaluated. This plant can also be found in other plant families such as, Verbenaceae Leguminosae, Sapotaceae, Scrophulariaceae, Malvaceae and Pro- teaceae. This paper aims at demonstrating the pharmacology and clinical activity of Lapachol and � -Lapachone, through their mechanism of action, and other actions which are not related to their anti neoplastic activity.
Parterno在本世纪末对Lapachol的分离和研究是植物化学最辉煌的篇章之一,特别是与Max Siewert关于Max Siewert的Argen- tina Lapachol (Bignoniaceae)树木材的通讯,与Ricardo Napp一起提交于Exp. NAC。1876年的费城。Lapachol起源于Tabebuia avellanedae Lorentz ex. Griseb (Bignoniaceae),在巴西被称为Pau DArc, Ipe-purple, Ipe-Black和Yellow-Ipe。这是一棵巨大的树,在传统医学中用于治疗口腔炎,一般的炎症过程和抗癌。-拉帕恰酮是从拉帕恰尔提取的一种o-萘醌,目前用于治疗克氏锥虫、癌症、病毒、细菌和利什曼原虫。这种植物也可以在其他植物科中发现,如马鞭草科、豆科、仙人掌科、玄参科、锦葵科和锦葵科。本文旨在通过拉帕康和-拉帕康的作用机制,以及其他与抗肿瘤活性无关的作用,论证拉帕康的药理学和临床活性。
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引用次数: 53
Anti-Tumor Activity of Oleanolic, Ursolic and Glycyrrhetinic Acid 齐墩果酸、熊果酸和甘草次酸的抗肿瘤活性
Pub Date : 2009-04-14 DOI: 10.2174/1874848100902010048
Ju Feng, Wei Chen, Yu Zhao, Xiu-lian Ju
Over last few years, there has been great interest on the anti-tumor properties of the triterpenoids, oleanolic, ur- solic and glycyrrhetinic acid in presence of many plants such as Olea europeae L., Actostaphylos uva-ursi and Glycyr- rhiza uralensis. The three acids and their derivatives show potential anti-tumor promoting and cytotoxic activities, inhibit- ing proliferation, inducing apotosis and preventing invasion, which suggested that they could be developed as anti-cancer and cancer chemopreventive agents. The mechanisms of the anti-tumor effects by triterpenoids need further investigation. A brief review is attempted here for their anti-tumor activities and chemical modification research.
近年来,人们对欧洲油橄榄、熊耳葡萄树和乌拉甘草等植物中含有的三萜、齐墩果酸、甘草酸和甘草次酸等抗肿瘤活性的研究引起了极大的兴趣。这三种酸及其衍生物具有潜在的促瘤和细胞毒活性、抑制细胞增殖、诱导细胞凋亡和防止细胞侵袭等作用,可作为抗癌和肿瘤化学预防药物开发。三萜抗肿瘤作用的机制有待进一步研究。现就其抗肿瘤活性及化学修饰研究作一综述。
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引用次数: 36
Fucoidan Protects Human Skin Fibroblast Cell Line HS68 Against γ -Radiation-Induced Damage 岩藻糖聚糖保护人皮肤成纤维细胞系HS68免受γ辐射引起的损伤
Pub Date : 2009-03-27 DOI: 10.2174/1874848100902010038
Keyong-Ho Lee, Sanggyu Bae, C. Cho, Ki-Hyeong Rhee
Fucoidan is a sulfated polysaccharide purified from brown algae including, Fucus vesiculosus and Fucus vesiculosus and Laminaria japonica. It has a variety of biological effects including antioxidant and antitumor activity. In this study, we investigated the radioprotective effects of fucoidan on normal human newborn foreskin fibroblast cell line HS68. To evaluate the effects of fucoidan, we assayed cell viability in vitro and change of blood cells such as thrombo- cytes, erythrocytes, leukocytes and hematocrit with radiation. In a viability assay, fucoidan increased dose-dependently the recovery of radiation-induced damage by 8Gy at all tested dose (10, 50 and 100 μg/ml). The survival rate of HS68 cells by pre-treatment with fucoidan was increased by 2 times more than it's compared with untreated cells. Furthermore, fucoidan protected the change of blood cells as follows; the thrombocyte of the irradiated controls had fallen to 35% com- pared with the initial values, the thrombocyte counts in fucoidan pre-treated group was recovered to 49% at the day 14. The Hematocrit level of fucoidan pre-treated group showed the recovery activity by 72% at the day 14, while hematocrit level of irradiated control without fucoidan fell to 61%. In case of erythrocyte level, the radiated controls was consistently maintained by the end of experiment at the range of 60~70%, on the other hand, the erythrocyte counts of fucoidan pre- treated group gently increased the level of erythrocyte at the range of 82~90%. These results may provide valuable and useful information in the field of radio-protection.
褐藻多糖是从褐藻中提纯出来的硫酸酸化多糖,褐藻包括褐藻、褐藻和海带。它具有多种生物效应,包括抗氧化和抗肿瘤活性。在本研究中,我们研究了岩藻聚糖对正常人新生包皮成纤维细胞HS68的辐射防护作用。为了评价岩藻糖聚糖的作用,我们在体外检测了细胞活力和放射线照射后血液细胞(血栓细胞、红细胞、白细胞和红细胞压积)的变化。在活力测定中,岩藻糖聚糖在所有测试剂量(10、50和100 μg/ml)下均以剂量依赖性增加8Gy的辐射损伤恢复。褐藻糖聚糖预处理后的HS68细胞存活率比未处理的细胞提高了2倍。岩藻聚糖对血细胞变化的保护作用如下:与初始值相比,照射组的血小板计数下降到35%,岩藻糖聚糖预处理组的血小板计数在第14天恢复到49%。褐藻糖聚糖预处理组红细胞压积在第14天恢复了72%,而未加褐藻糖聚糖的对照组红细胞压积下降到61%。在红细胞水平方面,辐射对照组在实验结束时保持在60~70%的范围内,而岩藻糖聚糖预处理组红细胞计数在82~90%的范围内缓慢增加。这些结果可为辐射防护领域提供有价值和有用的信息。
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引用次数: 5
Increase of Taxol Production in Taxus globosa Shoot Callus by Chlorocholine Chloride 氯胆碱对红豆杉芽愈伤组织中紫杉醇产量的影响
Pub Date : 2009-03-17 DOI: 10.2174/1874848100902010033
H. Barrios, Yuexin Zhang, C. Sandoval, Zun-an Xiao
Calluses from seasonal mature shoots of Taxus globosa Schltdl. were subcultured in new medium containing 1 mg l -1 NAA, 0.5 mg l -1 2, 4-D, 0.025 mg l -1 BA. Calluses growing for 30 and 40 days in a medium added with 0.1-5.0 mg l -1 of chlorocholine chloride (CCC) were harvested for determination of taxol, phenolic compounds, and for polyphenol oxidase (PPO) activity. The results showed that by increasing the CCC concentration, callus growth was decreased, phe- nolic level was raised up, but taxol content and PPO activity changed differently. The highest taxol production (0.0269 mg g -1 dry weight callus) and PPO activity (4.53 U g -1 fresh weight callus) were achieved at day 40 with a medium containing 0.5 mg l -1 CCC. Possible reason of higher taxol level stimulated by CCC is discussed in the text.
球形红豆杉季节性成熟芽的愈伤组织。在含有1 mg l -1 NAA, 0.5 mg l -1 2,4 - d, 0.025 mg l -1 BA的新培养基中传代。收集在添加0.1 ~ 5.0 mg l -1氯化氯胆碱(CCC)培养基中生长30和40天的愈伤组织,测定紫杉醇、酚类化合物和多酚氧化酶(PPO)活性。结果表明:随着CCC浓度的增加,愈伤组织生长减慢,酚类含量升高,但紫杉醇含量和PPO活性变化不同。在含有0.5 mg l -1 CCC的培养基中,第40天紫杉醇产量最高(干重0.0269 mg g -1), PPO活性最高(鲜重4.53 U g -1)。讨论了CCC刺激紫杉醇含量升高的可能原因。
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引用次数: 10
The Chemical Investigations of the Mangrove Plant Avicennia marina and its Endophytes 红树植物海棠及其内生植物的化学性质研究
Pub Date : 2009-03-11 DOI: 10.2174/1874848100902010024
Feng Zhu, Xin Chen, Yihua Yuan, M. Huang, Huili Sun, W. Xiang
A diverse array of bioactive compounds have been isolated and characterized from the mangrove plant Avicen- nia marina and its endophytes. Extensive chemical investigations of the different parts (barks, leaves, twigs, etc.) of the mangrove plant A. marina and its endophytes (mainly endophytic fungi) resulted in the reporting of the isolation of 123 compounds, and most of them are new or novel compounds. Most of compounds produced by the endophytes were differ- ent from the chemical components of the host A. marina, but it can still be found that some metabolites of the endophytes and some chemical components of the host possess the same structure unit. It suggested that there exist some biogenetic relationships between the endophytes and its host. Their biological activities, structural and stereochemical assignments are reported.
从红树植物海棠及其内生植物中分离和鉴定了多种生物活性化合物。对红树植物A. marina及其内生真菌(主要是内生真菌)的不同部位(树皮、叶子、树枝等)进行了广泛的化学研究,共分离到123个化合物,其中大部分为新化合物或新化合物。虽然大部分内生菌产生的化合物与寄主的化学成分不同,但仍可发现其代谢产物与寄主的某些化学成分具有相同的结构单元。说明内生菌与其寄主之间存在一定的生物发生关系。报道了它们的生物活性、结构和立体化学归属。
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引用次数: 47
Effect of Asparagus Racemosus Willd Root Extract on Ovariectomized Rats 野总状芦笋根提取物对去卵巢大鼠的影响
Pub Date : 2009-02-26 DOI: 10.2174/1874848100902010016
H. Chitme, I. Muchandi, S. Burli
Osteoporosis is a metabolic bone disease, characterized by increased porosity of the skeleton resulting from re- duced bone mass, the associated structural changes predispose the bone to fracture. The drug discovery process in this di- rection is very attractive, because of non-availability of suitable, safe and effective means for the management of this con- dition. The objective of the study was to evaluate antiosteoporotic activity of Asparagus racemosus. Ovariectomized rats model was used in this study for evaluation. Effects were evaluated by using biomechanical, bone mineral, serum and urine biochemical parameters. The effect on health status during the treatment was evaluated by regularly checking the overall body weight of the ovariectomized rats. In this study no significant change in body weight was observed. Metha- nolic and Aqueous extract obtained from Asparagus racemosus root has shown significant (p<0.05) effect on mineraliza- tion, ossification and osteoclastic activity suppression were observed in histopathological examination. Significant (p<0.05) increase in total ash weight, ash percent and ash calcium content were obtained. Treatments of ovariectomized rats by extract significantly reduced serum alkaline phosphatase activity, serum calcium and also inhibited the ovariec- tomized induced excessive loss of calcium in urine. Treatment of Aqueous and Methanolic extract of Asparagus racemo- sus also improved biomechanical parameters including hardness of 4 th lumbar vertebra, femoral length and its weight. We conclude from this study that phytosterols and other active constituents present in the root of Asparagus racemosus may effect on estrogen receptor similar to estrogen and produce antiosteoporotics effect. However, activity based fractionation and isolation of active constituents, is required to establish potency, safety and its clinical applicability in osteoporotic condition.
骨质疏松症是一种代谢性骨病,其特征是骨量减少导致骨骼孔隙度增加,相关的结构变化易使骨骼骨折。由于没有合适、安全、有效的治疗方法,这一方向的药物发现过程非常有吸引力。本研究的目的是评价总状芦笋的抗骨质疏松活性。本研究采用去卵巢大鼠模型进行评价。采用生物力学、骨矿物质、血清和尿液生化指标评价疗效。通过定期检查去卵巢大鼠的整体体重来评估治疗期间对健康状况的影响。在这项研究中,没有观察到体重的显著变化。组织病理学检查显示,总状芦笋根的甲基酚和水提物对矿化、骨化和破骨活性均有显著(p<0.05)的抑制作用。总灰分重、灰分率和灰分钙含量显著(p<0.05)提高。去卵巢大鼠经提取物处理后,血清碱性磷酸酶活性显著降低,血清钙含量显著降低,且能抑制去卵巢所致尿钙的过度流失。总状芦笋水提物和甲醇提物处理后,第4腰椎的硬度、股骨长度和重量等生物力学参数均有所改善。综上所述,总状芦笋根中的植物甾醇等活性成分可能对雌激素受体产生类似雌激素的作用,从而产生抗骨质疏松的作用。然而,需要基于活性的有效成分的分离和分离,以确定其效力,安全性及其在骨质疏松症中的临床适用性。
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引用次数: 27
Antiarthritis activity of Aristolochia bracteata extract in experimental animals. 马兜铃提取物抗关节炎实验动物活性研究。
Pub Date : 2009-02-19 DOI: 10.2174/1874848100902010006
H. Chitme, N. Patel
The Aristolochia bracteata is well known for its antiarthritis properties in Indian system of medicine and folk medicine. The objective of the present study was to evaluate its folk claim in rheumatoid arthritis (RA) and propose a probable mechanism of action. Anti arthritic activity was evaluated using Freund's complete adjuvant in rats, the course of treatment was followed for over and 4 weeks post inoculation period using health parameters, clinical and behavioral methods of study. Estimation of blood Hb, ESR and change in body weight were considered as health parameters and clinical observations included paw edema volume, thermal hyperalgesia, radiological and histomarphological analysis and exploratory behavior was studied in behavioral observations. The results indicates that, regular treatment of adjuvant in- duced arthritic rats with A. bracteata extracts improves ESR, Hb value and also restores body weight. Significant (P<0.01) inhibitory effect was observed with A. bracteata extract on Freund's complete adjuvant induced paw edema throughout the study (P<0.001). The latency to thermal stimuli and inhibitory effect on xylene induced ear edema was significantly (P<0.05) affected by oral treatment of A. bracteata, irrespective of solvent used for extraction. Treatment of FCA induced rats with A. bracteata extracts shown (P<0.05) increase in pain threshold, weight bearing ability, ambulation and also de- cline in scratching, defecation and urination, were observed as a sign of improvement in behavioral condition. The results obtained in this study showed promising effect on FCA modulated health status, clinical observations and behavioral changes.
马兜铃在印度医学和民间医学中以其抗关节炎的特性而闻名。本研究的目的是评价其在类风湿关节炎(RA)中的民间说法,并提出可能的作用机制。采用弗氏完全佐剂法对大鼠进行抗关节炎活性评价,接种期后用健康参数、临床和行为学方法随访治疗4周以上。以血Hb、ESR和体重变化为健康参数,临床观察包括足部水肿量、热痛觉、影像学和组织形态学分析,行为观察研究探索性行为。结果表明,定期用苞叶提取物治疗佐剂性关节炎大鼠,可改善ESR、Hb值,恢复体重。在整个研究过程中,苞叶提取物对Freund完全佐剂诱导的足跖水肿有显著(P<0.01)的抑制作用(P<0.001)。无论采用何种溶剂提取,口服小苞片对热刺激潜伏期和二甲苯诱导耳部水肿的抑制作用均有显著影响(P<0.05)。经FCA诱导的大鼠经花蒿提取物治疗后,疼痛阈值、负重能力、行走能力、抓伤、排便、排尿能力均有所改善(P<0.05)。本研究结果显示FCA在调节健康状况、临床观察和行为改变方面有良好的效果。
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引用次数: 42
A New Configurational Analysis of 1,6,7-triacetoxy-8,13-epoxy-14-labden- 11-one Isolated from Plectranthus ornatus Based on NMR and Theoretical Calculations 基于核磁共振和理论计算的红花中1,6,7-三乙酰氧基-8,13-环氧-14-labden- 11- 1的新构型分析
Pub Date : 2009-01-23 DOI: 10.2174/1874848100902010001
P. M. Oliveira, A. G. Pacheco, R. Pacheco, Alison G. Alves, D. Piló-Veloso, D. Raslan, A. Alcântara
This work describes the configurational and conformational analyses of 1,6,7-triacetoxy-8,13-epoxy-14-labden- 11-one, a labdane diterpenoid isolated from Plectranthus ornatus. Its relative stereochemistry was previously proposed by comparison with 1 H and 13 C NMR data of forskolin (2); however, the configurations of C-8 and C-13 have not been con- firmed. Correlations between 13 C NMR experimental data and HF/6-31G* calculated values of carbon chemical shifts were performed for configurational and conformational analyses. This procedure was formerly applied to the configura- tional analysis of 2. Among the seven different forskolin-type structures investigated, the 13 C NMR data of 2 correlated best with those with the same stereochemistry of 2 described in the literature. Thus, the same procedure was considered valid for configurational analysis of the labdane diterpenoid isolated from P. ornatus. The relative stereochemistry of this compound based on theoretical calculations was similar to the structure previously proposed, but the best results were ob- tained considering configurational inversion at C-13.
本文报道了一种从花楸中分离的唇丹二萜类化合物1,6,7-三乙酰氧基-8,13-环氧-14-labden- 11- 1的构型和构象分析。通过与福斯克林的1h和13c核磁共振数据的比较,提出了其相对立体化学(2);然而,C-8和C-13的配置尚未得到确认。将13c NMR实验数据与HF/6-31G*碳化学位移计算值进行相关性分析,进行构型和构象分析。这个程序以前应用于2的结构分析。在研究的7种不同的福斯克林型结构中,2的13c NMR数据与文献中描述的具有相同立体化学性质的2的13c NMR数据相关性最好。因此,同样的方法被认为是有效的构象分析从野樱草中分离的唇丹二萜。根据理论计算,该化合物的相对立体化学与先前提出的结构相似,但考虑到C-13的构型反转,获得了最好的结果。
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引用次数: 2
Beneficial Effect of Achyranthes apsera Linn. in Toluene-Di-Isocyanate Induced Occupational Asthma in Rats 牛膝草的有益作用。甲苯-二异氰酸酯诱发大鼠职业性哮喘的研究
Pub Date : 2008-12-05 DOI: 10.2174/1874848100801010044
Bhoomika R. Goyal, R. Goyal, A. Mehta
To study the bronchoprotective effect of ethanolic extract of Achyranthes aspera Linn. in toluene diisocyanate (TDI) induced occupational asthma in wistar rats. Wistar rats were divided into four different groups of eight animals each. All animals except control group were sensitized by the intranasal application of 10% TDI to induce airway hypersensitivity. At the end of the study, after provocation with 5%TDI the symptoms were observed in all animals. The total and differential leucocytes were counted in blood and bronchoalveolar (BAL) fluid. Liver homogenate was utilized for assessment of oxidative stress and lung histological examination was performed to investigate the inflammatory status in the airway. Our results suggest that, TDI sensitized rats exhibited asthmatic symptoms while A. aspera and dexamethasone treated rats did not show any airway abnormality. The neutrophils and eosinophils in blood were decreased significantly; the total cells and each different cell in particular eosinophils in BAL fluid were markedly decreased in treatment groups as compared to TDI sensitized rats. The antioxidant activity and histopathological observations also shows protective effect. From all above findings and observations, it can be concluded that A. aspera has beneficial role in occupational asthma in wistar rats.
目的:研究牛膝乙醇提取物的支气管保护作用。甲苯二异氰酸酯(TDI)致wistar大鼠职业性哮喘。Wistar大鼠被分成四组,每组8只。除对照组外,其余动物均采用10% TDI鼻内致敏诱导气道超敏反应。在研究结束时,用5%TDI刺激后,所有动物都观察到这些症状。计数血液和支气管肺泡(BAL)液中白细胞总数和分化数。肝脏匀浆用于评估氧化应激,肺组织学检查用于调查气道炎症状态。我们的研究结果表明,TDI致敏大鼠表现出哮喘症状,而曲霉和地塞米松治疗大鼠未表现出任何气道异常。血液中中性粒细胞和嗜酸性粒细胞明显减少;与TDI致敏大鼠相比,各治疗组BAL液中细胞总数及各细胞特别是嗜酸性粒细胞均明显减少。抗氧化活性和组织病理学观察也显示出保护作用。综上所述,曲霉对wistar大鼠职业性哮喘具有有益作用。
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引用次数: 26
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