COX, a.k.a cyclooxygenase, and 5-LOX, a.k.a. 5-lypooxygenase, are the key enzymes involved in the development of inflammatory response.

COX-2 Inhibitors

COX-2 (cyclooxygenase-2, also known as Prostaglandin-endoperoxide synthase 2) is an enzyme responsible for inflammation. Cyclooxygenase-2 or simply COX-2 converts arachidonic acid (AA) to prostaglandin endoperoxide H2. Arachidonic acid (AA, sometimes ARA) is a polyunsaturated omega-6 fatty acid. Cyclooxygenase-2 (COX-2, prostaglandin H synthase-2, PGHS-2) is unexpressed under normal conditions in most cells, but elevated levels are found during inflammation. COX-1 (prostaglandin H2 synthase 1) is constitutively expressed in many tissues. COX 1 maintains normal lining of the stomach while COX-2 level increases in response to inflammation.

The main COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs). NSAID is a form of COX-2 selective inhibitors known as non-steroidal anti-inflammatory drug that directly targets COX-2.  Is is desired to turn off COX-2 without turning off COX 1. NSAIDs such as aspirin,ibuprofen,etc. turn off COX 1 and COX 2. The COX 2 inhibitors were supposed to turn off COX 2 but not interfere with COX-1, thus will cause less ulcers. Many skin care ingredients are found to have COX inhibitory activities in addition to their other anti-aging skin care properties.

Idebenone is a synthetic analog similar to the potent anti-wrinkle antioxidant ingredient -the Co-enzyme Q-10. Idebenone counteracts aging at its source as a super antioxidant and an anti-inflammatory and was found to have COX-2 inhibitory activities.

Essential fatty acids such as DGLA and EPA are competitive inhibitors with AA for the COX pathways. Dihomo-γ-linolenic acid (DGLA) is a 20-carbon ω−6 fatty acid and Eicosapentaenoic acid (EPA or also icosapentaenoic acid) is an omega-3 fatty acid. This inhibition is a major mode of action in the way that dietary sources of DGLA and EPA (e.g., borage, fish oil) reduce inflammation. DGLA and EPA directly compete with AA (Arachidonic acid, an omega-6 fatty acid which is a pro inflammatory molecule derived from red meat, dairy products higher than 1% milk fat, cheese higher than3% milk fat, prawns, peanuts, etc.) for conversion to less harmful prostanoids. AA, DGLA and EPA, all compete with each other as substrates of COX-2 enzymes. EPA provides the most important competing cascade against AA. DGLA provides a less prominent cascade. These two parallel cascades reduce the inflammatory effects of AA.

Many botanical extracts exhibits anti-inflammatory activities via inhibition of COX pathways. Centipeda Cunninghamii Extract has been for thousands of years cultivated in the wetlands of Australia for its remarkable anti- inflammatory, antibacterial and healing properties. The anti-inflammatory properties of this herb is 4000 times more than that of asprin. This extraordinary botanical extract from the Daisy family demonstrates outstanding results for its distinct ability to minimize inflammation by 4,000 times compared to that of asprin and promotes cell regeneration, and minimizes the appearance of fine lines and wrinkles.

Flavonoids is a groups of molecules widely distributed in plants fulfilling many functions A variety of flavonoids have been found to inhibit COX-2. Inhibition of arachidonic acid (AA) metabolism is one of the mechanisms by which flavonoids exert their anti-inflammatory effects. Numerous studies have proposed that flavonoids act through a variety mechanisms to prevent and attenuate inflammatory responses

Culinary mushrooms, like Maitake, may be able to partially inhibit COX-1 and COX-2

5-LOX Inhibitors

Arachidonate 5-lipoxygenase also known as 5-lipoxygenase or 5-LO is an enzyme belong to the lipoxygenase family. It transforms essential fatty acids (EFAs) into leukotrienes. Leukotrienes are fatty signaling molecules that were first found in leukocytes. One of the main 5-LOX substrate is Arachidonic acid (AA) which yields 4-series leukotrienes (LTB4, LTC4, LTD4, LTE4 that are proinflammatory.

5-lipoxygenase (5-LOX) is an enzyme that’s linked to degenerative effects in aging adults. Foods often found in our diets can cause the body to increase production of this enzyme. Life Extension has an anti-aging supplements which contain 5-LOX Inhibitor known as ApresFlex. ApresFlex is a potent daily supplement that can help neutralize this potentially harmful enzyme. It’s formulated with ApresFlex, a patent-pending standardized form of boswellia that can help the body absorb the plant extract and reduce potential damage from inflammation.

Boswellia serrata is Indian frankincense or Salai in Ayurvedic medicine. This Indian frankincense (Boswellia serrata) has been used for hundreds of years for treating arthritis.Common Boswellia serrata gum extracts contain the so called Boswellic acids which are able to inhibit leukotrienes synthesis by inhibiting the enzyme 5-lipoxygenase (5-LOX) that causes inflammation of the immune system. Wokvel is an anti-inflammatory cream that contains the Boswellia Serrata Gum Extract.

Boswellia serrata has been used in the manufacture of the so called anti-wrinkle ingredient “Boswelox” brought by L’Oréal Paris. Boswelox is, apparently, a breakthrough phyto-complex that combines a power dose of boswellia serrata extract and manganese, which help reduce the appearance of lines.