Qu Tingli, Suo Shasha, Yan Liqiu, Wang Liwei, Liang Taigang
School of Pharmaceutical Science, Shanxi Medical University, Taiyuan, P. R. China.
Chem Biodivers. 2025 Feb 1:e202402234. doi: 10.1002/cbdv.202402234.
Astragaloside IV (ATS) is an active component of Astragalus membranaceus, which has immune regulation and anti-inflammatory effects. However, owing to its large molecular weight and poor solubility in water, the therapeutic effects of ATS are limited. We aimed to prepare ATS-chitosan (ATS-CS) nanoparticles and determine their anti-inflammatory effect and mechanism of action on RAW264.7 cells using metabolomics. The size of the ATS-CS nanoparticles was 200.3 nm with a zeta potential of 30.5 mV, and the encapsulation rate and drug loading were 69% and 13%, respectively. ATS-CS nanoparticles not only significantly decreased the increase of nitric oxide, interleukin-6, and tumor necrosis factor-α levels induced by lipopolysaccharide, but also exerted an anti-inflammatory effect by acting on arginine and proline, glutathione, sphingolipid, glycerophospholipid, glycine, serine, and threonine metabolism. Our findings confirmed that ATS-CS nanoparticles had good anti-inflammatory activity and showed that the activity of high molecular weight could be increased by producing nanoparticles. Our study paves the way for exploring the mechanism of nanoparticles through metabolomics.
黄芪甲苷IV(ATS)是黄芪的一种活性成分,具有免疫调节和抗炎作用。然而,由于其分子量较大且在水中溶解度较差,ATS的治疗效果有限。我们旨在制备ATS-壳聚糖(ATS-CS)纳米颗粒,并利用代谢组学确定其对RAW264.7细胞的抗炎作用及作用机制。ATS-CS纳米颗粒的尺寸为200.3nm,zeta电位为30.5mV,包封率和载药量分别为69%和13%。ATS-CS纳米颗粒不仅显著降低了脂多糖诱导的一氧化氮、白细胞介素-6和肿瘤坏死因子-α水平的升高,还通过作用于精氨酸和脯氨酸、谷胱甘肽、鞘脂、甘油磷脂、甘氨酸、丝氨酸和苏氨酸代谢发挥抗炎作用。我们的研究结果证实,ATS-CS纳米颗粒具有良好的抗炎活性,并表明通过制备纳米颗粒可以提高高分子量物质的活性。我们的研究为通过代谢组学探索纳米颗粒的作用机制铺平了道路。