Abstract
Objective The present study investigated the effect of the leaves extracts and fractions of Plectranthus glandulosus on the inhibition of pancreatic lipase, cholesterol esterase, adipocytes lipid uptake, and antithrombotic activity which may be important in atherosclerosis development. Methods Aqueous, ethanolic, and hydroethanolic extracts of Plactranthus glandulosus were prepared by maceration. The hydroethanolic extract was fractionated into n-hexane, ethylacetate, and n-butanol fractions and their inhibition of pancreatic lipase, cholesterol esterase, adipocytes lipid uptake, and antithrombotic activities measured. Liquid chromatography-high resolution mass spectrometry (LC-HRMS) analysis was carried out to determine phytochemical constituents present in the extracts. Results The standard orlistat exhibited a higher inhibitory activity on pancreatic lipase and cholesterol esterase (16.31 μg/mL and 15.75 μg/mL, respectively) compared to ethyl acetate fraction (IC50, 17.70 μg/mL and IC50, 24.8 μg/mL, respectively). Among crude extract, hydroethanolic extract showed a better inhibition against pancreatic lipase (IC50, 21.06 μg/mL) and cholesterol esterase (IC50, 25.14 μg/mL) though not comparable to the effect of orlistat. The best lipid uptake inhibition was observed in the hydroethanolic extract (IC50, 45.42 μg/mL) followed by the ethyl acetate fraction (IC50, 47.77 μg/mL). A better antithrombolytic activity was exhibited by the ethyl acetate fraction at all concentrations (50-800 μ/mL), while hydroethanolic extract exhibited the best activity among crude extract. However, these were not comparable to the standard aspirin. The LC-HRMS analysis revealed the presence of 7-O-methyl luteolin 5-O-β-D-glucopyranoside, chrysoeriol 5-O-β-D-glucopyranoside, 5,7-dihydroxy-3,2′,4′-trimethoxyflavone, and plectranmicin as major compounds in both hydroethanolic extract and ethyl acetate fraction. Conclusion Thus, our finding supports the traditional use of this plant, which might provide a potential source for future antiatherosclerotic drug discovery.
Highlights
Atherosclerosis is the major cause of stroke and heart attack, which are the leading cause of morbidity and mortality worldwide [1]
The dysregulation of lipid metabolism and aberrant inflammatory responses in the arterial walls at predisposed sites plays a central role from initiation to the progression and eventually rupture of the atherosclerotic plaque [3, 4] which is associated with thrombotic vessel occlusion, the main cause of atherosclerosis complications [5]
Excess release of fatty acids in the plasma will lead to very low-density lipoprotein (VLDL) production by the liver which may be transformed by lipoprotein lipase into intermediate density lipoprotein (IDl) and converted into smaller atherogenic LDL [8]
Summary
Atherosclerosis is the major cause of stroke and heart attack, which are the leading cause of morbidity and mortality worldwide [1]. Among fats from the diet, triglycerides and cholesterol are the most important because they are involved in increasing level of atherogenic low-density lipoprotein (LDL). Triglycerides are subjected to the action of pancreatic lipases, which hydrolyze triglycerides into monoacylglycerols and free fatty acids [7]. Excess release of fatty acids in the plasma will lead to very low-density lipoprotein (VLDL) production by the liver which may be transformed by lipoprotein lipase into intermediate density lipoprotein (IDl) and converted into smaller atherogenic LDL [8]. Hyperlipidemia may increase endothelial dysfunction and oxidative stress, which can lead to endothelial damage [10], promoting the infiltration of LDL cholesterol in the arterial wall, their oxidation by reactive oxygen species, inflammation, and foam cell formation in the arterial intima, which is the initial step of atherosclerosis formation
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