scholarly journals Trans-Epithelial Transport, Metabolism, and Biological Activity Assessment of the Multi-Target Lupin Peptide LILPKHSDAD (P5) and Its Metabolite LPKHSDAD (P5-Met)

Nutrients ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 863
Author(s):  
Carmen Lammi ◽  
Gilda Aiello ◽  
Carlotta Bollati ◽  
Jianqiang Li ◽  
Martina Bartolomei ◽  
...  
Keyword(s):  
Bioactive Peptides ◽  
Epithelial Transport ◽  
Cholesterol Metabolism ◽  
Mechanisms Of Action ◽  
Dynamic Nature ◽  
Activity Assessment ◽  
Lupin Protein ◽  
Metabolic Transformation ◽  
Target Activity ◽  
Hypocholesterolemic Peptide

P5 (LILPKHSDAD) is a hypocholesterolemic peptide from lupin protein with a multi-target activity, since it inhibits both 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCoAR) and proprotein convertase subtilisin/kexin type-9 (PCSK9). This work shows that, during epithelial transport experiments, the metabolic transformation mediated by intestinal peptidases produces two main detected peptides, ILPKHSDAD (P5-frag) and LPKHSDAD (P5-met), and that both P5 and P5-met are linearly absorbed by differentiated human intestinal Caco-2 cells. Extensive comparative structural, biochemical, and cellular characterizations of P5-met and the parent peptide P5 demonstrate that both peptides have unique characteristics and share the same mechanisms of action. In fact, they exert an intrinsically multi-target behavior being able to regulate cholesterol metabolism by modulating different pathways. The results of this study also highlight the dynamic nature of bioactive peptides that may be modulated by the biological systems they get in contact with.

Bile acid sequestrants: mechanisms of action on bile acid and cholesterol metabolism

1991 ◽  
Vol 40 (S1) ◽  
pp. S53-S58 ◽  
Author(s):  
K. Einarsson ◽  
S. Ericsson ◽  
S. Ewerth ◽  
E. Reihnér ◽  
M. Rudling ◽  
...  
Keyword(s):  
Bile Acid ◽  
Cholesterol Metabolism ◽  
Mechanisms Of Action ◽  
Bile Acid Sequestrants

scholarly journals Lupin protein influences the expression of hepatic genes involved in fatty acid synthesis and triacylglycerol hydrolysis of adult rats

2008 ◽  
Vol 99 (5) ◽  
pp. 952-962 ◽  
Author(s):  
Anja Bettzieche ◽  
Corinna Brandsch ◽  
Kristin Weiße ◽  
Frank Hirche ◽  
Klaus Eder ◽  
...  
Keyword(s):  
Fatty Acid ◽  
Fatty Acid Synthesis ◽  
Cholesterol Metabolism ◽  
Acid Synthesis ◽  
Cholesterol Concentration ◽  
Liver Cholesterol ◽  
Bile Acid Metabolism ◽  
Adult Rats ◽  
Lupin Protein ◽  
Triacylglycerol Hydrolysis

To assess the effect of lupin protein on concentrations of lipids in plasma lipoproteins and liver and hepatic mRNA concentrations of genes involved in lipid metabolism, adult rats were fed egg albumin-based diets containing either lupin protein fromLupinus albusor casein (50 g/kg) supplemented (hypercholesterolaemic) or not (normolipaemic) with a cholesterol–cholate mixture for 20 d. Lupin protein compared with casein lowered the concentrations of TAG in liver (P < 0·01) and circulating VLDL + chylomicrons (P < 0·05) of hypercholesterolaemic rats, but not of normolipaemic rats. Hepatic mRNA concentrations of genes involved in fatty acid synthesis such as sterol regulatory element-binding protein-1c, glucose-6-phosphate dehydrogenase, fatty acid synthase, stearoyl-CoA desaturase-1 and acyl-CoA:glycerol-3-phosphate acyltransferase were lower and mRNA concentrations of lipoprotein lipase, hepatic lipase and apoA5 involved in TAG hydrolysis were higher in rats fed lupin protein than in rats fed casein. These effects were stronger in hypercholesterolaemic rats than in normolipaemic rats. Hypercholesterolaemic rats fed the lupin protein had higher liver cholesterol concentrations (P < 0·01) and lower levels of LDL-cholesterol (P < 0·05) than rats fed casein. No effect of lupin protein was observed on cholesterol concentration in VLDL + chylomicrons and HDL and hepatic mRNA concentrations of genes involved in cholesterol and bile acid metabolism. In conclusion, the present study shows that lupin protein has hypotriacylglycerolaemic action possibly via down regulation of fatty acid synthesis genes and up regulation of genes involved in TAG hydrolysis. Alterations in cholesterol metabolism could not be explained on the basis of mRNA data.

scholarly journals Mechanisms of action of clofibrate on cholesterol metabolism in patients with hyperlipidemia

1972 ◽  
Vol 13 (4) ◽  
pp. 531-551
Author(s):  
Scott M. Grundy ◽  
E.H. Ahrens ◽  
Gerald Salen ◽  
Paul H. Schreibman ◽  
Paul J. Nestel
Keyword(s):  
Cholesterol Metabolism ◽  
Mechanisms Of Action

Bile acid sequestrants: Mechanisms of action on bile acid and cholesterol metabolism

1991 ◽  
Vol 40 (1) ◽  
pp. S53-S58 ◽  
Author(s):  
K. Einarsson ◽  
S. Ericsson ◽  
S. Ewerth ◽  
E. Reihn�r ◽  
M. Rudling ◽  
...  
Keyword(s):  
Bile Acid ◽  
Cholesterol Metabolism ◽  
Mechanisms Of Action ◽  
Bile Acid Sequestrants

Case Formulation and Design of Behavioral Treatment Programs

2003 ◽  
Vol 19 (3) ◽  
pp. 164-174 ◽  
Author(s):  
Stephen N. Haynes ◽  
Andrew E. Williams
Keyword(s):  
Functional Analysis ◽  
Behavior Problems ◽  
Behavioral Treatment ◽  
Clinical Case ◽  
Relative Magnitude ◽  
Mechanisms Of Action ◽  
Treatment Programs ◽  
Case Formulation ◽  
Functional Relations ◽  
Causal Variables

Summary: We review the rationale for behavioral clinical case formulations and emphasize the role of the functional analysis in the design of individualized treatments. Standardized treatments may not be optimally effective for clients who have multiple behavior problems. These problems can affect each other in complex ways and each behavior problem can be influenced by multiple, interacting causal variables. The mechanisms of action of standardized treatments may not always address the most important causal variables for a client's behavior problems. The functional analysis integrates judgments about the client's behavior problems, important causal variables, and functional relations among variables. The functional analysis aids treatment decisions by helping the clinician estimate the relative magnitude of effect of each causal variable on the client's behavior problems, so that the most effective treatments can be selected. The parameters of, and issues associated with, a functional analysis and Functional Analytic Clinical Case Models (FACCM) are illustrated with a clinical case. The task of selecting the best treatment for a client is complicated because treatments differ in their level of specificity and have unequally weighted mechanisms of action. Further, a treatment's mechanism of action is often unknown.

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