The pharmacokinetic characteristics of Hyperoside-2-hydroxypropyl-β-cyclodextrin inclusion complex in rats were evaluated. Compared with Hyperoside, the results showed that maximum plasma concentration and AUC0-t indexes of Hyperoside inclusion complex in rat plasma were increased, the value of half-life time was prolonged, and the value of apparent clearance was decreased, which proved that Hyperoside complexed with 2-hydroxypropyl-β-cyclodextrin could improve its bioavailability and increase its blood concentration. Secondly, the therapeutic effect of Hyperoside before and after complexing was further compared through the dextran sodium sulfate-induced colitis in mice. The experimental results showed that under the same dose, the Hyperoside inclusion complex had a better therapeutic effect, which could significantly increase the body weight of mice, improve the disease activity index, alleviate colon shortening, improve pathological colon changes, and have a better protective effect on colitis mice. According to 16S rDNA sequencing analyses, Hyperoside-2-hydroxypropyl-β-cyclodextrin may have an anti-inflammatory effect by increasing the abundance of beneficial bacteria (e.g. Firmicuria) and decreasing the proportion of harmful bacteria (e.g. Bacteroidetes) to balance the colon’s microbiota.
Jianqing Su, Xinyu Zhang, Shengliang Cao, Cheng Liu, Xiang Fu, Rui Zhang, Xiaoli Li, Jiaojiao Xue, Ying Li, Xueyan Wang, Yi Ding, Yubao Li, Xiuling Chu; Pharmacokinetic studies of hyperoside-2-hydroxypropyl-β-cyclodextrin inclusion complex and ameliorated DSS-induced colitis in mice. Biosci Rep 31 May 2023; 43 (5): BSR20230003. doi: https://doi.org/10.1042/BSR20230003