High-throughput screening of lipase inhibitors as anti-obesity drugs on liquid crystal-infused porous surfaces

Abstract

High-throughput screening of lipase inhibitors is critical for developing anti-obesity drugs. Herein, a robust and versatile sensing platform based on the difference in the sliding time of droplets on liquid crystal-infused porous surfaces (LCIPS) is developed to detect lipase inhibitors. Lipase catalyzes glycerol trioleate (GT) to produce oleate that can adsorb at the solution/liquid crystal (LC) interface due to its high amphiphilicity, which impedes the sliding of droplets on LCIPS, resulting in an extended sliding time. However, in the presence of lipase inhibitors, the enzymatic hydrolysis of GT by lipase is inhibited, which shortens the sliding time. The screening of three lipase inhibitors, orlistat, cetilistat, and epigallocatechin gallate (EGCG), popular anti-obesity drugs, is demonstrated to have IC50 values of 17.45 ± 3.15 nM, 72.15 ± 6.32 nM, and 2.19 ± 0.24 μM, respectively. This study provides a simple, inexpensive, portable, user-friendly, and instrument-free method for rapid, accurate, and high-throughput screening of lipase inhibitors. The LCIPS-based sensing platform is up-and-coming in developing advanced bioanalytical sensors.