Limitations of phosphatidylcholine/deoxycholate mixtures for the analysis of phospholipase A2 inhibition and activation: illustration with annexins

Biochim Biophys Acta. 1992 Aug 19;1127(3):270-6. doi: 10.1016/0005-2760(92)90231-j.

Abstract

The effects of human recombinant lipocortin I (annexin I) and bovine lung calpactin I (annexin II) on porcine pancreatic phospholipase A2 (PLA2) activity in phosphatidylcholine (PC)/deoxycholate (DOC) mixtures were investigated. Annexin-associated decreases in PLA2 activity were observed under some conditions, for example, at high DOC/PC molar ratios; however, activation was observed under other conditions. NaCl, which lowers the non-critical micellar concentration (NCMC) of deoxycholate, caused significant decreases in control PLA2 activity in the absence of annexins, and greater decreases in PLA2 activity in annexin-containing samples, resulting in an apparent increase in inhibition. The PC/DOC substrate mixtures themselves appeared unstable. Despite a large excess of detergent, precipitates were, at times, observed upon incubation of some PC/DOC mixtures at 37 degrees C. Such behavior is of interest in view of the numerous reports of PLA2 inhibition by annexins and annexin-derived peptides in the PC/DOC system. The influence of the annexins on activity in this system is consistent with effects on the phase behavior of the PC/DOC mixture and/or competition with the enzyme for available Ca2+. These results caution against use of the PC/DOC system for analysis of potential PLA2 inhibitors unless the phase behavior of the system is more fully delineated.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Annexins
  • Calcium-Binding Proteins / pharmacology*
  • Carbon Radioisotopes
  • Deoxycholic Acid
  • Enzyme Activation
  • Humans
  • Kinetics
  • Membrane Proteins / pharmacology
  • Oleic Acid
  • Oleic Acids / metabolism
  • Pancreas / enzymology
  • Phosphatidylcholines
  • Phospholipases A / antagonists & inhibitors
  • Phospholipases A / metabolism*
  • Phospholipases A2
  • Radioisotope Dilution Technique
  • Recombinant Proteins / pharmacology
  • Swine

Substances

  • Annexins
  • Calcium-Binding Proteins
  • Carbon Radioisotopes
  • Membrane Proteins
  • Oleic Acids
  • Phosphatidylcholines
  • Recombinant Proteins
  • Deoxycholic Acid
  • Oleic Acid
  • Phospholipases A
  • Phospholipases A2