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芒果苷药质体的抗氧化和肝保护作用评价及其对抗乙醇诱导的肝损伤的潜力。

Pharmacological evaluation of mangiferin herbosomes for antioxidant and hepatoprotection potential against ethanol induced hepatic damage.

机构信息

Department of Pharmaceutical Sciences, Dr Hari Singh Gour Central University , Sagar, Madhya Pradesh , India.

出版信息

Drug Dev Ind Pharm. 2013 Nov;39(11):1840-50. doi: 10.3109/03639045.2012.738685. Epub 2012 Nov 20.

Abstract

CONTEXT

Fatty liver is the first stage of alcoholic damage which is reversible with abstinence from alcohol. Mangiferin (MF) showed potent scavenging activity on diphenyl-1-picrylhydrazyl radicals which stimulate liver regeneration in various liver injuries.

OBJECTIVE

Although, MF shows hepatoprotection against various liver disorders but due to rapid clearance and limited solubility in lipoid environment, there is problem of its poor absorption from intestine hence poor bioavailability. Owing to which there is a need to develop MF herbosomes to resolve the problem of poor bioavailability to enhance the therapeutic potential.

METHODS

Successfully prepared MF herbosomes through complexation with phospholipids were characterized by physicochemical, chromatography, spectroscopy (differential scanning calorimetry (DSC), infrared (IR), and nuclear magnetic resonance (NMR)), ex vivo absorption using everted small intestine sac technique and in vivo studies using ethanol inducing hepatotoxicity in albino rats and comparing the results against plain MF.

RESULTS

Ex vivo study showed significant increased absorption of MF from prepared MF herbosomes as compared to plain MF. The hepatoprotective potential of MF herbosomes evaluated by in vivo study revealed significantly decreased levels of serum glutamate oxaloacetate transminase (SGOT), serum glutamate pyruvate transminase (SGPT), total bilirubin, and alkaline phosphatase (ALP) in MF herbosomes as compared to plain MF. MF herbosomes also showed significantly decreased level of malonyl dehydrogenase along with increased levels of reduced glutathione, superoxide dismutase (SOD) and catalase as compared to plain MF which was also comparable to the standard drug, silymarin (SL).

CONCLUSION

The above mentioned results showed that hepatoprotective and antioxidant potency of MF enhanced due to the preparation of its herbosomes.

摘要

背景

脂肪肝是酒精损害的第一阶段,通过戒酒可以逆转。芒果苷(MF)对二苯基-1-苦基肼自由基具有很强的清除活性,可刺激各种肝损伤中的肝再生。

目的

尽管 MF 显示出对各种肝脏疾病的保护作用,但由于其在肠道中的吸收不良,清除率高且在脂环境中的溶解度有限,因此存在其生物利用度差的问题。因此,需要开发 MF 类囊体来解决生物利用度差的问题,以提高治疗潜力。

方法

通过与磷脂络合成功制备 MF 类囊体,通过物理化学、色谱、光谱(差示扫描量热法(DSC)、红外(IR)和核磁共振(NMR))进行特征描述,使用外翻肠囊技术进行体外吸收研究,并在体内研究中使用乙醇诱导白化大鼠肝毒性,并将结果与普通 MF 进行比较。

结果

体外研究表明,与普通 MF 相比,MF 类囊体的 MF 吸收明显增加。体内研究评估的 MF 类囊体的保肝潜力表明,与普通 MF 相比,MF 类囊体的血清谷氨酸草酰乙酸转氨酶(SGOT)、血清谷氨酸丙酮酸转氨酶(SGPT)、总胆红素和碱性磷酸酶(ALP)水平显著降低。MF 类囊体还显示出比普通 MF 更低的丙二醛脱氢酶水平,同时增加了还原型谷胱甘肽、超氧化物歧化酶(SOD)和过氧化氢酶的水平,与标准药物水飞蓟素(SL)相当。

结论

上述结果表明,由于 MF 类囊体的制备,MF 的保肝和抗氧化作用增强。

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