Table 1.
Relative structure-function relationships of calcium antagonists (DHPs, verapamil, and diltiazem) and vitamin E. Effect on oxidative modification of isolated ex vivo human low-density lipoprotein using two various oxidation systems (copper (II) ions induced and monocyte induced). Compiled according to data presented by Rojstaczer and Triggle [119].
| Compound | Systems of LDL oxidation | |||
|---|---|---|---|---|
| Copper (II) ions induced system (comparison of three methods) | Monocyte induced cell oxidation system | |||
| Methods | ||||
| Reduction of TBARS level of LDL (relative efficacy) | Degradation of oxidized [125I] LDL by J774 macrophages | Relative electrophoretic mobility of LDL on agarose gel | TBARS content of LDL (in %%) |
|
| Relative efficacy (activity rank order (ARO); ARO = I for the most effective); effective inhibitor concentration [IC], in μM | ||||
| Amlodipine | + + (ARO = IV) |
+ + (ARO = II–V) |
25 μM 50 μM |
25 μM (ARO = III–V) |
| Felodipine | + + + + + (ARO = I) |
+ + + (ARO = I) 25 μM, 97 ± 2% |
50 μM | 25 μM, 65 ± 9% (ARO = II) |
| Nifedipine | + + + (ARO = III) |
+ + (ARO = II–V) |
10 μM; 50 μM | 25 μM, 96 ± 2% (ARO = I) |
| 2-Chloro analog of nifedipine | + + + + (ARO = II) |
— | — | — |
| 4-Nitro analog of nifedipine | — | + + (ARO = II–V) |
— | 25 μM (ARO = III–V) |
| Nitrendipine | + + (ARO = IV) |
— | No effect | — |
| Verapamil | + + (ARO = IV) |
+ + (ARO = II–V) |
— | 25 μM (ARO = III–V) |
| Diltiazem | + (ARO = V) |
— | No effect | — |
|
α-Tocopherol (vitamin E) |
+ + + + + + (ARO = I) |
— | 1 μM; 5 μM; 10 μM; 50 μM | — |