Lyu Yuanfeng, Lin Lin, Xie Yuning, Li Dan, Xiao Min, Zhang Yufeng, Cheung Stanley Chun Kai, Shaw Pang Chui, Yang Xiao, Chan Paul Kay Sheung, Kong Alice Pik Shan, Zuo Zhong
School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, China.
Department of Microbiology, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, China.
Front Pharmacol. 2021 Jun 15;12:684358. doi: 10.3389/fphar.2021.684358. eCollection 2021.
extracts (CREs) have been used widely for their anti-diabetic and anti-microbial activities, and berberine/jatrorrhizine/coptisine/palmatine are the primary bioactive components. Although guidelines have adopted content analyses of these components as a quality control method for CREs, it is difficult to differentiate the CREs from different sources using this method because of the lack of indications for their related pharmacological activities. To explore the effect of CREs (CREA/CREB/CREC) with different compositions of major components on the gut microbiota and blood glucose levels in d mice. Degradation of berberine/jatrorrhizine/coptisine/palmatine from CREA/CREB/CREC in rat/mouse intestinal contents and their impact on nine common gastrointestinal bacteria were investigated. In addition, the effects of oral administration of CREA/CREB/CREC for 2 weeks on the gut microbiota and blood glucose levels in d mice were monitored insulin/glucose tolerance test (ITT/GTT), insulin concentration, homeostatic model assessment of insulin resistance and fecal 16S rRNA sequencing. The total amount of berberine/jatrorrhizine/coptisine/palmatine was highest in CREA. was strongly inhibited by all three CREs, with CREA demonstrating the most significant inhibitory effects on minimum inhibitory concentration, time-kill kinetics, and ATP production. In d mice, CREA resulted in the most significant decrease in ITT/GTT and depicted different changes in the microbiota from CREB/CREC. Thus, CREs with different compositions of berberine/jatrorrhizine/coptisine/palmatine differed in terms of time-kill kinetics and ATP production assays on . CREA revealed the potent bacterial inhibitory effects and glucose-lowering activity.
提取物（CREs）因其抗糖尿病和抗菌活性而被广泛使用，小檗碱/药根碱/黄连碱/巴马汀是主要的生物活性成分。尽管指南已采用对这些成分的含量分析作为CREs的质量控制方法，但由于缺乏其相关药理活性的指标，使用该方法难以区分不同来源的CREs。为了探究主要成分组成不同的CREs（CREA/CREB/CREC）对糖尿病小鼠肠道微生物群和血糖水平的影响。研究了CREA/CREB/CREC中的小檗碱/药根碱/黄连碱/巴马汀在大鼠/小鼠肠道内容物中的降解情况及其对九种常见胃肠道细菌的影响。此外，通过胰岛素/葡萄糖耐量试验（ITT/GTT）、胰岛素浓度、胰岛素抵抗的稳态模型评估和粪便16S rRNA测序，监测了连续2周口服CREA/CREB/CREC对糖尿病小鼠肠道微生物群和血糖水平的影响。CREA中小檗碱/药根碱/黄连碱/巴马汀的总量最高。所有三种CREs均强烈抑制其生长，其中CREA在最低抑菌浓度、时间杀菌动力学和ATP产生方面表现出最显著的抑制作用。在糖尿病小鼠中，CREA导致ITT/GTT的下降最为显著，并且与CREB/CREC相比，其微生物群呈现出不同的变化。因此，小檗碱/药根碱/黄连碱/巴马汀组成不同的CREs在对……的时间杀菌动力学和ATP产生试验方面存在差异。CREA显示出强大的细菌抑制作用和降血糖活性。
