Table 1. In vitro effects of apoprotein mimetic peptides.
| Name | Cholesterol Efflux | Stabilize ABCA1 | Antioxidative in MCA | Lipid and Lipoprotein Effects | Reference |
|---|---|---|---|---|---|
| Peptides of Human ApoA-I Helices | |||||
| apoA-I helix 1 (44-65) | — | — | 41 | ||
| apoA-I helix 10 (220-241) | — | — | 41 | ||
| apoA-I helix 1/9 chimera | + | + | 41 | ||
| apoA-I helix 9/10 chimera | + | + | 41 | ||
| apoA-I helix 10/9 chimera | — | — | 41 | ||
| Monomeric ApoA-I Mimetic Peptides | |||||
| 2F (Ac-18-NH2) | + | + | Weak | binds VLDL and displaces apoE and apoCs | 10, 16, 26. 75 |
| 3F-1 | + | 16, 17 | |||
| 3F-2 | + | binds HDL>VLDL>IDL/LDL binds oxidized PL with > affinity than apoA-I |
17, 18, 23 | ||
| 3F-3 | — | 16, 17 | |||
| 3F-14 | — | binds VLDL/IDL/LDL>HDL binds oxidized PL with ≈ affinity as apoA-I |
16-18, 23 | ||
| 4F | + | + | + | reduces LDL oxidation binds oxidized PL with > affinity than apoA-I |
16, 17, 23, 25, 26, 33, 62 |
| 5F | + | activates LCAT | 16, 65 | ||
| 6F | + | activates LCAT | 16 | ||
| 7F | weak | 16 | |||
| Tandem ApoA-I Mimetic Peptides | |||||
| 37pA (18A-Pro-18A) | + | + | increases secretion of apoA-I and HDL from HepG2 cells binds VLDL and displaces apoE and apoCs detergent-like effects may account for increased cholesterol efflux |
10, 24, 26, 37, 39, 75 | |
| 5A (18A-Pro-18A with Ala substitutions) | + (>37pA) | no detergent-like effects | 38 | ||
| 37aA (18A-Ala-18A) | + | 37 | |||
| 4F-IHS-4F | + (>4F) | remodels HDL to >extent than 4F | 33 | ||
| 4F-Ala-4F | + (>4F) | remodels HDL to >extent than 4F increases LDL oxidation | 33 | ||
| 4F-Pro-4F | + (>4F) | binds HDL | 33 | ||
| Peptides mimicking other apoproteins | |||||
| [113-122]apoJ | ↑PON ↓ LOOH |
45 | |||
| apoE Y(141-155)2 | binds LDL receptor | 48 | |||
| apoE Y(141-p-155)2 | does not bind LDL receptor | 48 | |||
| apoE AcY(141-155)2 | binds LDL receptor binds VLDL, IDL/LDL, HDL |
48 | |||
| Ac-hE-18A-NH2 [(141-150)-18A] | + (ABCA1 independent) | binds VLDL and LDL ↑ VLDL and LDL uptake by cells displaces apoE from VLDL ↓ LPS induced inflammatory response of EC |
49, 50, 76 | ||
| ATI-5261 | + | 53 | |||
| mSAA1.1(1-20) | + | 56, 57 | |||
| mSAA2.1(1-20) | + (↓ ACAT activity) | 56, 57 | |||
| mSAA2.1(74-103) | + (↑ CEH activity) | 56, 57 | |||
| hSAA1.1/2.1(1-23) | + (↓ ACAT activity) | 56, 57 | |||
| Generically amphipathic Peptides | |||||
| KRES | + | 58 | |||
| KERS | — | 58 | |||
| FREL | + | ↓ LOOH ↑ PON activity |
58 | ||
+ = positive effect; — = no effect; blank cells = no information