Hyperoside inhibits pancreatic lipase activity <i>in vitro</i> and reduces fat accumulation <i>in vivo</i>

Abstract

Hyperoside, the main component of many anti-obesity plants, might exhibit a lipase inhibition effect to reduce fat accumulation. The anti-obesity effect of hyperoside was investigated by studying its inhibitory effect and mechanism on pancreatic lipase <i>in vitro</i> and evaluating its ability to reduce lipid accumulation <i>in vivo</i>. Hyperoside is a mixed-type inhibitor of lipase with an IC₅₀ of 0.67 ± 0.02 mmol L^-<i>in vitro</i>. Hyperoside changed the secondary conformation of lipase, increased the α-helix content, and changed the microenvironment of lipase through static quenching. The interaction between hyperoside and lipase results from a strong binding spontaneous exothermic reaction, mainly through hydrogen bonding, van der Waals force and electrostatic force. Hyperoside protected hepatic lipid accumulation and adipose tissue hypertrophy and reduced the expression of inflammatory factors in high-fat diet-induced rats. Moreover, hyperoside had a good inhibitory effect on lipase activity in serum and increased fecal fat excretion, thereby reducing lipid absorption <i>in vivo</i>. This study provides theoretical support for the research and development of hyperoside in fat-reducing functional foods.