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Published on: January 26, 2016
Oral amphipathic peptides as therapeutic agents
Srinivasa T Reddy1, G M Anantharamaiah, Mohamad Navab
1Division of Cardiology, Department of Medicine, David Geffen School of Medicine, UCLA, Los Angeles, California 90095-1679, USA. SReddy@mednet.ucla.edu
Expert Opinion on Investigational Drugs
|December 24, 2005
Summary
Amphipathic peptides reduce inflammation by decreasing oxidised phospholipids and releasing antioxidant enzymes. These peptides, including D-4F, show therapeutic potential for atherosclerosis and may be administered orally.
Area of Science:
- Biochemistry
- Immunology
- Pharmacology
Background:
- Cholesterol oxidation generates pro-inflammatory oxidised phospholipids, contributing to inflammation.
- High-density lipoproteins (HDLs) play a role in innate immunity and can be pro- or anti-inflammatory.
- Systemic inflammation, such as in atherosclerosis, can alter Apolipoprotein A-I, impairing reverse cholesterol transport and promoting pro-inflammatory HDLs.
Purpose of the Study:
- To investigate the anti-inflammatory and anti-atherosclerosis effects of amphipathic peptides.
- To explore the mechanism by which these peptides interact with lipids and influence HDL function.
- To assess the therapeutic potential of these peptides as oral agents.
Main Methods:
- Studied amphipathic peptides with varying helical structures (D-4F, D-[113-122]apoJ, KRES, FREL).
- Assessed peptide interaction with lipids and its effect on lipoprotein-lipid hydroperoxides.
- Evaluated the impact on HDL-associated antioxidant enzymes and pre-beta HDL formation.
Main Results:
- Amphipathic peptides reduced lipoprotein-lipid hydroperoxides.
- This reduction released HDL-associated antioxidant enzymes, such as paraoxonase, conferring anti-inflammatory and anti-atherosclerosis activity.
- The peptide D-4F specifically stimulated the formation and cycling of pre-beta HDL.
Conclusions:
- Amphipathic peptides possess antiatherosclerosis and anti-inflammatory properties.
- These peptides counteract inflammation by reducing oxidised phospholipids and enhancing antioxidant enzyme activity.
- Amphipathic peptides, including D-4F, demonstrate therapeutic potential as oral agents for inflammatory conditions.
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