Purification, biochemical characterization, and DPP‐IV and α‐amylase inhibitory activity of Berberine from Cardiospermum halicacabum

Abstract

Diabetes mellitus (DM) has spread across the globe, increasing the risk of obesity, cardiovascular disease, and other comorbidities. Despite substantial research into the development of diabetic treatments that are effective in lowering blood glucose levels, their efficiency is short‐lived due to unpleasant side effects such as weight gain and hypoglycemia. The discovery of secondary metabolites in the prevention and treatment of diabetes and its complications has an incentive to take interest in plant‐based medications, and enzyme inhibitors have the potential to aid in the treatment and management of DM. This study aims to isolate, characterize, and analyse the influence of berberine‐like alkaloids from alcoholic Cardiospermum halicacabum extract in vitro and in silico, as a possible inhibitor of Dipeptidyl peptidase‐IV (DPP‐IV) and α‐amylase, two essential enzymes involved in diabetes. The alkaloid from C. halicacabum was identified as berberine, with an m/z of 336.1263. Purified berberine inhibits DPP‐IV with an IC50 of 16.328 ± 1.344 μM and inhibits α‐amylase by 72% at 10 μg/mL. In‐silico studies demonstrated that berberine was found to bind to the active site of both DPP‐IV and α‐amylase. The precise mechanism underlying the observation has to be researched further in order to investigate C. halicacabum's anti‐diabetic effects and argue for its possible application as alternative medicine.

Edible freshwater snail (Paludomas conica) attenuates STZ‐induced diabetic complications by regulating PFK‐1 and PON‐1 gene expression

“…α‐Amylase and α‐Glucosidase are crucial enzymes that break down starch into simpler sugars in the human body. α‐Amylase s hydrolyses complex polysaccharides into oligosaccharides and disaccharides, which are then hydrolysed by α‐Glucosidase into monosaccharides absorbed into the hepatic portal vein to increase postprandial glucose levels (Naik et al ., 2022). Inhibiting carbohydrate‐digesting enzymes such as α‐Amylase and α‐Glucosidase in gastrointestinal glucose absorption, which lower postprandial glucose levels, is used to manage diabetes mellitus.…”

Computational Screening for the Dipeptidyl Peptidase-IV Inhibitory Peptides from Putative Hemp Seed Hydrolyzed Peptidome as a Potential Antidiabetic Agent

“…The Rg level of ADP 3 fluctuated between 26.8 and 27.2 Å, while csADP2 showed a fluctuation between 26.9 and 27.3 Å. These fluctuations were slightly lower compared to several previous studies [55,56]. Moreover, the number of hydrogen bonds was also considered to examine the dynamic equilibration of the complex system.…”

New Insights into the Latest Advancement in α-Amylase Inhibitors of Plant Origin with Anti-Diabetic Effects

“…Similarly, another known alkaloid, berberine (Figure 9b), was isolated from the Cardiospermum halicacabum plant and found to retard the activity of α-amylase by 72% at 10 μg/mL. In addition, in silico investigations indicated that berberine adheres to the enzyme's active site [156]. Another class of bioactive molecules, xanthones named garcixanthone D and garcinone E (Figure 9c), were purified from the pericarp of Garcinia mangostana and showed 93.8 and 85.6% inhibition against α-amylase, respectively.…”

“…Similarly, another known alkaloid, berberine ( Figure 9 b), was isolated from the Cardiospermum halicacabum plant and found to retard the activity of α-amylase by 72% at 10 μg/mL. In addition, in silico investigations indicated that berberine adheres to the enzyme’s active site [ 156 ].…”