Table 2. . Structure of caffeic acid (3,4-dihydroxycinnamic acid) phenethyl ester derivatives and selected physiochemical and biological properties.
Compound | Structure | Nematode survival (μg/ml) | NF-κB inhibition† | MIC (μg/ml) | Solubility in PBS (μM) | Plasma stability (% remaining) | ||
---|---|---|---|---|---|---|---|---|
Human | Mouse | Rat | ||||||
CAPE | 4–8 | 66 | 32–64 | 18 | 97 | 2 | ND | |
Caffeic acid | >32 | ND | >256 | |||||
1 | None | 86 | >256 | |||||
2 | 4–16 | 44 | >256 | 2 | 93 | 1 | ND | |
3 | None | ND | 128–256 | |||||
4 | None | ND | >256 | |||||
5 | 32 | 75 | >256 | |||||
6 | >256 | 143 | >256 | |||||
7 | 4–8 | 49 | 16 | 246 | 100 | 95 | ND | |
8 | 64 | 68 | 32 | |||||
9 | 64 | 99 | >256 | |||||
10 | 4–16 | 113 | >256 | |||||
11 | >256 | 42 | 32–64 | |||||
12 | >256 | 94 | 32–64 | |||||
13 | 4–32 | 50 | 32–64 | 78 | 93 | 91 | ND | |
14 | 2–16 | 92 | >256 | 236 | 97 | 99 | 102 |
†Percent of NF-κB activity was calculated by normalizing to treatment with TNF-α and solvent alone (DMSO) as 100%.
CAPE: Caffeic acid (3,4-dihydroxycinnamic acid) phenethyl ester; MIC: Minimum inhibitory concentration; PBS: Phosphate-buffered saline.