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苦参抗氧化活性及其强效提取物的脂质体开发。

Antioxidant activity of Sophora exigua and liposome development of its powerful extract.

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand.

National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency (NSTDA), Pathum Thani, Thailand.

出版信息

Drug Discov Ther. 2024 Jul 9;18(3):150-159. doi: 10.5582/ddt.2024.01018. Epub 2024 May 22.

Abstract

Sophora exigua (SE) was sequentially extracted using hexane, ethyl acetate, and ethanol. The obtained extracts were tested for antioxidant activity. Among them, the fractionated ethyl acetate extract (SE-EA) showed the highest potential in free radical scavenging and ferric-reducing properties. The chemical analysis identified sophoraflavanone G as one of the active ingredients in SE-EA. According to SE-EA solubility, SE-EA liposomes were developed using a sonication-assisted thin film method. Cholesterol and phospholipids were used as the main compositions of the liposomes. The obtained liposomes were spherical with different nano-size ranges, size distribution, and zeta potential depending on SE-EA and total lipid concentrations. SE-EA liposomes were slightly bigger than their empty liposomes. All liposomes exhibited a phospholipid crystalline structure. Cholesterol and SE-EA existed in the liposomes as an amorphous state. SE-EA liposomes with high total lipid content exhibited high entrapment efficiency and sustained release behavior. Whereas liposomes with low total lipid content showed low entrapment efficiency and fast-release behavior. All SE-EA liposomes showed stronger antioxidant activity than the non-entrapped SE-EA. In conclusion, SE-EA is a natural source of potent antioxidants. The developed SE-EA liposomes are a promising pharmaceutical formulation to efficiently deliver the active ingredients of SE-EA and are suitable for further study in vivo.

摘要

苦参(SE)依次用正己烷、乙酸乙酯和乙醇进行提取。测试了得到的提取物的抗氧化活性。其中,分馏得到的乙酸乙酯提取物(SE-EA)在自由基清除和铁还原能力方面表现出最高的潜力。化学分析鉴定出 SE-EA 中的苦参黄酮 G 是其活性成分之一。根据 SE-EA 的溶解度,采用超声辅助薄膜法开发了 SE-EA 脂质体。胆固醇和磷脂是脂质体的主要组成部分。所得到的脂质体为球形,具有不同的纳米尺寸范围、粒径分布和zeta 电位,这取决于 SE-EA 和总脂质浓度。SE-EA 脂质体比空脂质体稍大。所有脂质体均表现出磷脂的结晶结构。胆固醇和 SE-EA 以无定形状态存在于脂质体中。高总脂质含量的 SE-EA 脂质体表现出高包封效率和持续释放行为。而总脂质含量低的脂质体表现出低包封效率和快速释放行为。所有 SE-EA 脂质体均表现出比非包封 SE-EA 更强的抗氧化活性。总之,SE-EA 是一种潜在的强效抗氧化剂的天然来源。开发的 SE-EA 脂质体是一种有前途的药物制剂,可有效传递 SE-EA 的活性成分,适合进一步进行体内研究。

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