Denglang Zou,Yunbin Cui,Si Li,Duocheng Sang,Weimeng Liu,Tianshu Zhao,Xueli Gu,Tao Chen,Yulin Li
Biosynthesis is a promising way to manufacture desired products, however, the purification of its final products is a tough work due to the huge amount of reaction matrix. Liquid stationary phase of high-speed counter-current chromatography could easily avoid the commonly disadvantages that occurred in traditional column chromatography in the field of biosynthesized products purification. This characteristic makes high-speed counter-current chromatography particularly applicable for final products separation in biosynthesis. In this study, the glycosylation products of Silybin B by one-pot glycosylation were successfully purified by high-speed counter-current chromatography to show the applicability of high-speed counter-current chromatography for preparative separation of biosynthesis products. An optimized n -hexane/ethyl acetate/methanol/water (2:5:2:3, v/v/v/v ) system was applied in this study. As a result, four Silybin B glycosylation products, including 7 mg of Silybin B-5-O- β -D-glucoside ( SG-1 ), 12 mg of Silybin B-3-O- β -D-glucoside ( SG-2 ), 10 mg of Silybin B-7-O- β -D-glucoside ( SG-3 ), and 24 mg of Silybin B-20-O- β -D-glucoside ( SG-4 ), were simultaneously separated from 200 mg of glycosylation crude products, with the purity of 89.3, 95.2, 96.4, and 97.5%, respectively. Their structures were identified by spectroscopic analysis.
Tianlong Zhao,Zixin Rong,Demei Wang,Shiyu Liu,Zimei Chen,Yicheng Cai,Tingming Fu
Silybin is a clinically validated adjunct for liver disorders, yet poor absorption and rapid metabolism curtail its wider therapeutic use. Exploiting the distinctive hepatic distribution of glycyrrhetinic acid (GA) receptors, we augmented silybin B (SilB, an isomer of silybin) delivery by encapsulating it within GA-modified liposomes. We constructed a response-surface model to optimize liposome fabrication, identifying the optimal recipe: 5.89:1 lecithin/cholesterol, 100:2.13 lecithin/DSPE-PEG2000, and 12:5.05 lecithin/SilB. DSPE-PEG2000-GA was generated through amidation and substituted for DSPE-PEG2000 to yield GA-modified SilB liposomes (GSL). GSL exhibited 49.34 ± 0.25% encapsulation efficiency, 9.13 ± 0.04% drug loading, 148.881 ± 4.786 nm diameter, 0.269 ± 0.024 polydispersity index, and −23.433 ± 0.775 mV zeta potential. GSL remained stable for 7 days and sustained drug release for 24 h in PBS. GA-modified liposomes displayed accelerated HepG2 uptake and heightened murine hepatic retention, underpinning its superior therapeutic performance. GSL engaged non-alcoholic fatty liver disease on multiple aspects, suppressing lipid accretion, inflammation, and insulin resistance, and significantly surpassed free SilB in therapeutic magnitude. Download: Download high-res image (305KB) Download: Download full-size image
危险品化学品经营许可证（带存储）