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耳叶水蓑衣萜类化合物组分对脂多糖诱导的大鼠脓毒症休克的抗内毒素作用

Anti-endotoxin effects of terpenoids fraction from Hygrophila auriculata in lipopolysaccharide-induced septic shock in rats.

作者信息

Hussain Md Sarfaraj, Azam Faizul, Ahamed K F H Nazeer, Ravichandiran V, Alkskas Ismail

机构信息

a Faculty of Pharmacy , Misurata University , Misurata , Libya .

b Department of Pharmacognosy , Vels College of Pharmacy , Chennai , India , and.

出版信息

Pharm Biol. 2016;54(4):628-36. doi: 10.3109/13880209.2015.1070877. Epub 2015 Oct 1.

DOI:10.3109/13880209.2015.1070877
PMID:26428681
Abstract

CONTEXT

Hygrophila auriculata (K. Schum) Heine (Acanthaceae) has been traditionally used for the treatment of various ailments such as inflammation, rheumatism, jaundice and malaria.

OBJECTIVE

The present study aims to separate terpenoid fraction (TF) from alcohol (70%) extract of the whole plant of Hygrophila auriculata and assess its anti-inflammatory activity.

MATERIALS AND METHODS

HPTLC analysis of TF was performed for the estimation of lupeol. Edema was induced in Wistar albino rats by subplanter injection of 0.1 ml of 1% (w/v) carrageenan into the right hind paw after 1 h of TF administration (100 and 200 mg/kg oral). Septic shock was induced by intraperitoneal administration of LPS (100 μg/kg) in rats and interleukins (IL-1β and IL-6), tumor necrosis factor (TNF-α), superoxide dismutase (SOD), lipid peroxidation (LPO), and nitric oxide (NO) were measured in serum. AutoDock 4.2 was used for molecular docking.

RESULTS

Administration of TF significantly (p < 0.005) restored the serum levels of cytokines, LPO (7.77 ± 0.034 versus 4.59 ± 0.059 nmole of TBARS), NO (9.72 ± 0.18 versus 4.15 ± 0.23 µmol nitrite/mg of wet tissue), and SOD (4.89 ± 0.036 versus 7.83 ± 0.033 Unit/mg protein) compared with the LPS-challenged rats. Analysis of in silico results revealed that TNF-α is the most appropriate target in eliciting anti-inflammatory activity.

CONCLUSION

The present findings suggest that TF of Hygrophila auriculata possesses great promise as an anti-inflammatory agent which may be due to its antioxidant effect. Molecular docking results could be exploited for lead optimization and development of suitable treatment of inflammatory disorders.

摘要

背景

耳叶水蓑衣(Hygrophila auriculata (K. Schum) Heine,爵床科)传统上用于治疗各种疾病,如炎症、风湿、黄疸和疟疾。

目的

本研究旨在从耳叶水蓑衣全草的70%乙醇提取物中分离出萜类组分(TF),并评估其抗炎活性。

材料与方法

采用高效薄层色谱(HPTLC)分析法对TF进行分析,以测定羽扇豆醇含量。在给予TF(100和200 mg/kg口服)1小时后,通过向Wistar白化大鼠右后爪皮下注射0.1 ml 1%(w/v)角叉菜胶诱导水肿。通过向大鼠腹腔注射脂多糖(LPS,100 μg/kg)诱导脓毒症休克,并测定血清中的白细胞介素(IL-1β和IL-6)、肿瘤坏死因子(TNF-α)、超氧化物歧化酶(SOD)、脂质过氧化(LPO)和一氧化氮(NO)。使用AutoDock 4.2进行分子对接。

结果

与LPS攻击的大鼠相比,给予TF后显著(p < 0.(此处原文有误,推测应为p < 0.005))恢复了细胞因子、LPO(7.77 ± 0.034对4.59 ± 0.059 nmol丙二醛)、NO(9.72 ± 0.18对4.15 ± 0.23 μmol亚硝酸盐/毫克湿组织)和SOD(4.89 ± 对7.83 ± 0.033单位/毫克蛋白质)的血清水平。计算机模拟结果分析表明,TNF-α是引发抗炎活性的最合适靶点。

结论

目前的研究结果表明,耳叶水蓑衣的TF作为一种抗炎剂具有很大的潜力,这可能归因于其抗氧化作用。分子对接结果可用于先导化合物优化和开发合适的炎症性疾病治疗方法。

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