Inhibition of pancreatic lipase, α-glucosidase, α-amylase, and hypolipidemic effects of the total flavonoids from Nelumbo nucifera leaves

Abstract

Ethnopharmacological relevance: Nelumbo nucifera Gaertn. leaves have been used as medicinal herbs in the past 1300 years, specifically utilized to cure hyperlipidemia, hyperglycemia, and obesity. It has been recorded in the most famous medicinal book in China for more than 400 years. The present study aims to identify the potential therapeutic activities of the flavonoids isolated from Nelumbo nucifera leaves.

Materials and methods: Nelumbo nucifera leaf flavonoids (NLF) were tested for the inhibition of lipase, α-glucosidase, and α-amylase activities in vitro. A single dose of NLF was administered by oral gavage in mice for acute toxicity. Wistar rats with high-fat diet-induced hyperlipidemia and two other animal models were used to evaluate the hypolipidemic effects of NLF.

Results: Our in vitro biochemistry tests revealed that the NLF showed high inhibitory activity against porcine pancreatic lipase, α-amylase, and α-glucosidase with IC50 values of 0.38 ± 0.022, 2.20 ± 0.18, and 1.86 ± 0.018 mg/mL, respectively. Furthermore, the NLF significantly lowered the lipid components, such as the total cholesterol, triglycerides, low-density lipoprotein cholesterol, and malondialdehyde, in various established in vivo systems and raised the high-density lipoprotein cholesterol. Moreover, the NLF alleviated high-fat diet-induced lipid accumulation in the liver.

Conclusions: The results demonstrate that NLFs can effectively ameliorate hyperlipidemia and inhibit the key enzymes related to type 2 diabetes mellitus. Our findings may provide new pharmacological basis for the treatment of hyperlipidemia, hyperglycemia, and obesity using NLFs.

Keywords: 2,4-dinitrophenyl butyrate; A; AI; ALT; AS; AST; BW; C; CHDs; CPCSEA; CVD; Committee for the Purpose of Control and Supervision of Experiments on Animals; DNPB; Diabetes; Flavonoids; HDL-C; HFD; Hyperlipidemia; IAEC; Institutional Animal Ethical Committee; KM; Kun Ming; LDL-C; Lipids; MDA; NLF; Nelumbo nucifera; Nelumbo nucifera leaf flavonoids; OECD; Organization for Economic Cooperation and Development; PPB; PPL; T2DM; TC; TG; ZBT; Zhi-bi-tuo; absorbance; aspartate aminotransferase; atherogenic index; atherosclerosis; body weight; cardiovascular disease; concentration; coronary heart diseases; glutamate pyruvate transaminase; high fat diet; high-density lipoprotein-cholesterol; low-density lipoprotein-cholesterol; malondialdehyde; p-nitrophenyl-α-D-glucopyranoside; pNPG; porcine pancreatic lipase; potassium phosphate buffer; total cholesterol; triglyceride; type 2 diabetes mellitus.