Abstract
BackgroundCyanidin-3-rutinoside (C3R), a naturally occurring anthocyanin, possesses anti-oxidant, anti-hyperglycemic, anti-glycation and cardioprotective properties. However, its mechanisms responsible for anti-hyperlipidemic activity have not been fully identified. The aim of the study was to investigate the lipid-lowering mechanisms of C3R through inhibition of lipid digestion and absorption in vitro.MethodsThe inhibitory activity of C3R against pancreatic lipase and cholesterol esterase was evaluated using enzymatic fluorometric and enzymatic colorimetric assays, respectively. An enzyme kinetic study using Michaelis-Menten and the derived Lineweaver-Burk plot was performed to understand the possible types of inhibition. The formation of cholesterol micelles was determined using the cholesterol assay kit. The bile acid binding was measured using the colorimetric assay. The NBD cholesterol uptake in Caco-2 cells was determined using fluorometric assay. The mRNA expression of cholesterol transporter (Niemann-Pick C1-like 1) was determined by RT-PCR.ResultsThe results showed that C3R was a mixed-type competitive inhibitor of pancreatic lipase with the IC50 value of 59.4 ± 1.41 μM. Furthermore, C3R (0.125–1 mM) inhibited pancreatic cholesterol esterase about 5–18%. In addition, C3R inhibited the formation of cholesterol micelles and bound to primary and secondary bile acid. In Caco-2 cells, C3R (12.5–100 μM) exhibited a significant reduction in cholesterol uptake in both free cholesterol (17–41%) and mixed micelles (20–30%). Finally, C3R (100 μM) was able to suppress mRNA expression of NPC1L1 in Caco-2 cells after 24 h incubation.ConclusionsThe present findings suggest that C3R acts as a lipid-lowering agent through inhibition of lipid digestion and absorption.
Highlights
Cyanidin-3-rutinoside (C3R), a naturally occurring anthocyanin, possesses anti-oxidant, antihyperglycemic, anti-glycation and cardioprotective properties
Clinical evidence revealed that supplementation of anthocyanin reduced total cholesterol, triglyceride and the level of low-density lipoprotein cholesterol (LDL-C) and increased the level of high-density lipoprotein cholesterol (HDL-C) in patients with dyslipidemia [28, 29]
The results from the pancreatic lipase inhibitory activity of C3R are in agreement with previous reports suggesting that pure anthocyanins, cyanidin-3-glucoside (C3G) and peonidin-3-glucoside, and anthocyanins extracted from dietary sources demonstrated inhibitory action against pancreatic lipase [31, 32]
Summary
Cyanidin-3-rutinoside (C3R), a naturally occurring anthocyanin, possesses anti-oxidant, antihyperglycemic, anti-glycation and cardioprotective properties. The risk of developing cardiovascular diseases in subjects with hyperlipidemia was twice as high as in effective phytochemical compounds from dietary fruits, vegetables and herbal medicines as lipid-lowering agents [9, 10]. Anthocyanins are one of the largest groups of natural pigments responsible for red, purple and blue colors in fruits and vegetables They have been proven to possess favorable antioxidant, anti-inflammatory and anti-diabetic properties under both in vitro and in vivo study [13]. Cyanidin-3-rutinoside (C3R), a naturally occurring anthocyanin, is widely distributed in a high number of dietary sources, such as blackberry, mulberry and black raspberry [15, 16] This compound has demonstrated promising benefits for reduction of postprandial glucose through inhibition of pancreatic α-amylase and intestinal α-glucosidase [17, 18]. Since the blood cholesterol level is influenced by absorption of cholesterol in the small intestine, the effect of C3R on cholesterol uptake in the enterocytes was determined
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