Table 1.
Disk diffusion assay zone of inhibition data for the parent Oceanapia sp. C011027 extract, synthetic 2a, various indole analogs of 2, and therapeutic standards compared across five solid tumor cell lines, a leukemia line (CEM), and bone marrow progenitor cells (CFU-GM). Bold numbers indicate selectivity, defined as a differential zone of inhibition greater than 7 mm between solid tumor cell line and at least one normal cell proxy (CEM/CFU-GM).
| nmol/disk | Zone of Inhibition (mm)
|
||||||||
|---|---|---|---|---|---|---|---|---|---|
| H125 | MCF-7 | OVC-5 | U251N | PANC-1 | CEM | CFU-GM
|
|||
| mouse | human | ||||||||
| gemcitabine | 0.02 | 33 | 13 | 33 | 33 | 13 | 20 | 0 | 33 |
| 5-fluorouracil | 46 | 33 | 33 | 29 | 7 | 18 | 21 | 33 | 33 |
|
| |||||||||
| Oceanapia sp. C011027 crude extract | – | 11 | 8 | 15 | 20 | 23 | 13 | 16 | |
| 6-Br-8-keto-conicamin A (2a) | 112 | 7 | 33 | 10 | 15 | 28 | 7 | 7 | 5 |
| “ | 28 | 16 | 12 | 2.5 | 2 | 0 | |||
| 5-Br-8-keto-conicamin A (3) | 112 | 7 | 33 | 13 | 10 | 20 | 5 | 8 | 5 |
| “ | 28 | 10 | 7 | 20 | 5 | 3 | 0 | ||
| 1H-indole-3-carbonyl cyanide (8) | 352 | 7 | 10 | 7 | 7 | 7 | 10 | ||
| 8-keto-tryptamine (10) | 172 | 7 | 11 | 5 | 5 | 3 | |||
| 6-Br-8-keto-tryptamine (11) | 130 | 2 | 3 | 3 | 2 | 0 | |||
| 5-Br-8-keto-tryptamine (12) | 71 | 0 | 3 | 2 | 2 | 0 | |||
| N,N,N-trimethyl 8-keto-tryptamine (13) | 207 | 2 | 10 | 3 | 2 | 7 | 3 | ||
| 6-Br-N,N-dimethyl-8-keto-tryptamine (14) | 53 | 0 | 3 | 0 | 0 | 2 | |||
| 5-Br-N,N-dimethyl-8-keto-tryptamine (15) | 32 | 0 | 2 | 0 | 0 | 0 | |||
| N,N-dimethyl-8-keto-tryptamine (16) | 59 | 0 | 2 | 0 | 0 | 0 | |||
Cell lines: H-125 = lung adenocarcinoma; MCF-7 = breast adenocarcinoma; OVCAR-5 = ovarian carcinoma; U251N = glioblastoma cells; PANC-1 = prostrate adenocarcinoma; CEM = leukemic lymphoid; CFU-GM = granulocyte-macrophage progenitor cells.