Table 1. Affinities for inhibiting different targets and phospholipolytic activities of PLA2s.
PLA2 | Inhibition (IC50, µM) of α-[125I]Bgt Binding to… | Current Blocking and Phospholipolytic Activities | ||||
T. californica nAChR | Human α7 nAChR | L. stagnalis AChBP | A. californica AChBP | Inhibition (IC50, µM) of ACh (Cyt)-induced current in L. stagnalis neurons | Phospholipolytic activity, mmol/min/µmol | |
CM-II | 1.2±0.1 | 3.2±0.3 | 1.00±0.03 | >100 | 0.37±0.07* | 2.3 [5] |
Vurtoxin | 0.26±0.02 | 14±5 | >30 | >30 | 10.5±2.6* | 0.7 |
Vur-PL2 | >100 | 29±2 | >30 | nd** | >30 | 25.1 [19] |
Bitanarin | 4.3±0.2 [7] | 20±1.5 [7] | 10.6±0.6 [7] | >50 [7] | 4.8±1.3 | 1.95 [7] |
* The data obtained for antagonizing action on currents induced by ACh in nAChR-Ls-1 neurons and by Cyt were combined
** Not determined