Synthesis and cholesterol-reducing potential of water-soluble phytosterol derivative

• Published in: Journal of functional foods Vol. 60; p. 103428
• Main Authors: He, Wen-Sen, Li, Lingling, Wang, Huihui, Rui, Jiaxin, Cui, Dandan
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 01.09.2019; Elsevier
• Subjects: Cholesterol-reducing potential; Ionic liquid; Polyethylene glycol; Water-soluble phytosterol derivative; [BSO3HMim]OTf; [BSO3HMIM]HSO4; LDL-C; SREBP-2; ALT; UA; CYP7A1; Ionic liquid; HDL-C; SD; LDL-C/HDL-C ratio; Water-soluble phytosterol derivative; CREA; Polyethylene glycol; LDL-R; [BSO3HMIM]TS; BUN; HPLC; AST; IL; PSHS; PPGS-1000; TC; LXR-α; PEG; TG; Cholesterol-reducing potential; HMG-CoR; NG; SD rats; HC; PEG-1000
• ISSN: 1756-4646; 2214-9414
• DOI: 10.1016/j.jff.2019.103428

[Display omitted] •PPGS-1000 was successfully synthesized using [BSO3HMim]OTf as catalyst.•The conversion of PPGS-1000 exceeded 94% after 60 min.•PPGS-1000 possessed cholesterol-reducing potential.•PPGS-1000 changed liver cholesterol-related gene expression. Phytosterols have recently received considerable attention. However, applications of these plant-derived lipids are greatly limited by water insolubility and poor oil solubility. Most previous studies have focused mainly on improving the oil solubility of phytosterols. The present study established an efficient method for synthesizing a water-soluble phytosterol derivative (PPGS-1000), employing [BSO3HMim]OTf as a catalyst. Here, the conversion of PPGS-1000 exceeded 94% over a short period (60 min). The cholesterol-reducing activity of PPGS-1000 was examined further in Sprague-Dawley rats fed a high cholesterol diet. Additionally, the effect of PPGS-1000 on the mRNA expression of hepatic genes involved in cholesterol metabolism was explored. In rats, PPGS-1000 significantly reduced the serum total cholesterol and low-density lipoprotein cholesterol (LDL-C) levels, serum LDL-C/high-density lipoprotein cholesterol ratio and liver cholesterol level by 10.3%, 33.7%, 35.9% and 25.9%, respectively. PPGS-1000 markedly promoted fecal cholesterol excretion. And the expression of HMG-CoR, LDL-R and SREBP-2 mRNA in the liver was up-regulated after PPGS-1000 treatment. In conclusion, PPGS-1000 possessed a cholesterol-reducing potential.