Chemical profile of Roselle extract and its inhibitory activities on three digestive enzymes in vitro and in vivo

Roselle is rich in an extensive diversity of beneficial substances, including phenolic acids, amino acids, anthocyanins, vitamins, and flavonoids. Herein, the chemical constituents in Roselle extract (RE) were identified by UPLC-DAD-QTOF-MS. Besides, its inhibitory effects on three digestive enzymes, i.e. alpha-amylase, alpha-glucosidase, and pancreatic lipase, were investigated in both in vitro and in vivo. Thirty-three constituents including hibiscus acid, 18 phenolic acids, 2 anthocyanins and 12 flavonoids were identified. The anthocyanins content in RE was 21.44 +/- 0.68 %, while the contents of chlorogenic acids, rutin and quercetin were 17.76 +/- 2.28 %, 0.31 +/- 0.01 % and 0.32 +/- 0.01 %, respectively. RE inhibited pancreatic lipase in a non-competitive way with an IC50 value of 0.84 mg/mL. Besides, it demonstrated a mixed-type inhibition on both alpha-glucosidase and alpha-amylase with IC50 values of 0.59 mg/mL and 1.93 mg/mL, respectively. Fluorescence quenching assays confirmed the binding of RE to the enzyme proteins. Furthermore, rats pre-treated with RE at doses of 50 and 100 mg/kg body weight (bwt) exhibited significant reductions in fat absorption and improvements in fat excretion through feces. Additionally, the in vivo study revealed that RE was effective in suppressing the increase of blood glucose after starch consumption, while its effects on maltose and sucrose consumption were relatively weak.

Automated summary

Roselle extract contains various beneficial substances and has inhibitory effects on digestive enzymes. The extract inhibits pancreatic lipase in a non-competitive manner, and exhibits mixed-type inhibition on alpha-glucosidase and alpha-amylase. In vivo experiments show that the extract reduces fat absorption and improves fat excretion through feces. Additionally, it effectively suppresses the increase of blood glucose after starch consumption.