What drugs inhibit phospholipase A2?

Compounds that inhibit or block the activity of a PHOSPHOLIPASE A2 enzyme….Phospholipase A2 Inhibitors.

Drug Target Type
Varespladib methyl Phospholipase A2, membrane associated target
Varespladib methyl Group 10 secretory phospholipase A2 target
Darapladib Cytosolic phospholipase A2 target

What drugs inhibit phospholipase?

Phospholipase A2 Inhibitors

  • Agrylin.
  • anagrelide.
  • cilostazol.
  • Pletal.

What is cytosolic phospholipase?

Cytosolic phospholipase A2 (cPLA2) is a calcium-dependent enzyme that cleaves fatty acids, such as arachidonic acid, from phospholipids by hydrolyzing the SN-2 acyl bond (Leslie, 1997). Most cPLA2 pharmaceutical development has focused on treating asthma and other inflammatory diseases.

What is phospholipase A2 used for?

Phospholipase A2 (PLA2), which cleaves phospholipids producing lysophospholipids and free fatty acids, was originally identified as an intracellular protein involved in cell signaling and in the production of free fatty acids, such as arachidonic acid.

Does aspirin inhibit phospholipase A2?

We have shown previously that aspirin (ASA) ingestion by normal human volunteers inhibits peripheral blood monocyte phospholipase C (PLC) activities ex vivo. Cells preincubated with ASA were found to have decreased PLC activities. Phospholipase A2 activities were not affected by salicylates.

What is a phospholipase inhibitor?

Phospholipase A2 (PLA2) is a serine hydrolase that liberates arachidonic acid from membrane phospholipids. If increased leukotriene production is responsible for causing gastric distress,18 then a PLA2 inhibitor should block both pathways to offer the efficacy of an NSAID without the gastric ulcer risk.

What is an A2 inhibitor?

Phospholipase A2 (PLA2) inhibitors are drugs used to treat conditions associated with excessive platelet production and aggregation of platelets such as peripheral vascular disease.

What is arachidonic acid used for?

Arachidonic acid is actually the chemical messenger first released by your muscles during intense weight training, controlling the core physiological response to exercise and regulating the intensity of all growth signals to follow. Also, anytime you have tissue injury, inflammation is involved in healing the wound.

How does phospholipase A2 cause inflammation?

sPLA2 has been shown to promote inflammation in mammals by catalyzing the first step of the arachidonic acid pathway by breaking down phospholipids, resulting in the formation of fatty acids including arachidonic acid. This arachidonic acid is then metabolized to form several inflammatory and thrombogenic molecules.

What are side effects of boswellia?

Boswellia is a natural extract, but it can still have side effects. It may cause digestive side effects, such as nausea, acid reflux, and diarrhea. Some people may experience skin rashes when using boswellia, especially if they apply it directly to the skin.