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Naturally occurring mast cell stabilizers: Part 3

Coumarins are compounds that occur naturally in a number of plant species.  Several medications are derived from coumarins, including several anticoagulants, such as warfarin. They are notable for being fragrant.  Coumarin increases resorption of edema fluids.

Scopoletin is a coumarin present in the root structures of several species, including Urtica dioica (stinging nettle), Scopolia japonica (Japanese belladonna), chicory and passion flower.  In human mast cells, scopoletin interferes with production of TNF, IL-6 and IL-8.  It was found to inhibit NF-kB, which participates in the inflammatory response.

Artekeiskeanol A is a coumarin extracted from Artemisa keiskeana.  In traditional medicine systems, it is sometimes used to treat rheumatoid arthritis.  It suppressed degranulation, decreased production of TNF and IL-13.  Selinidin, a coumarin found in Angelica keiskei, suppresses IgE-initiated degranulation and decreases production of LTC4 and TNF. Rottlerin from the tree Mallotus philippensis attenuates IgE activation, degranulation of at least airway mast cells, and histamine release.

Cinnamic acid is a coumarin that decreased antigen stimulated degranulation in basophils, but similar action has not been recorded in mast cells.  It is most commonly extracted from cinnamon oil. A furanocoumarin found in Angelica dahurica inhibits action of COX-2 and 5-LO, decreasing production of PGD2 and LTC4, in addition to preventing degranulation.

Thunberginol A and B from Hydrangeae macrophylla inhibits histamine release from activated mast cells.  Thunberginol A prevents release of TNF and IL-4. In particular, thunberginol B is a potent mast cell stabilizer, suppressing degranulation from IgE or other causes.  It can also suppress production of IL-2, IL-3, IL-4, IL-13, TNF and GM-CSF when triggered by IgE.

Ellagic acid is found in nuts and fruit, such as strawberries, raspberries, pomegranate and walnuts. It interferes with IgE activation of mast cells and decreases release of histamine, TNF and IL-6.

Plant phenols have been reported to have medicinal effects for many years.  Magnolol and honokiol, two substance found in the bark of Magnolia obovata, can interfere with basophil degranulation as well as allergic response more generally.  Resveratrol is a phenol derivative present in berries, peanuts and grapes.  It is a potent supporessor of inflammatory mast cell products, including TNF, IL-6 and IL-8.  It also interferes with the structures required for degranulation and can also interfere with basophil degranulation.

Curcumin is another phenol derivative and is already quite popular in the mast cell community. (Disclaimer: I take turmeric, which contains curcumin.)  Curcumin has well described anti-inflammatory and anti-allergic benefits.  It inhibits mast cell and basophil degranulation and decreases release of IL-4 and TNF.  It also suppresses a popular lab model of allergy, passive cutaneous anaphylaxis.

References:

Zhang, T., et al. Mast cell stabilisers. Eur J Pharmacol (2015).

Finn, DF, Walsh, JJ. Twenty-first century mast cell stabilizers. J Pharmacol 2013 Sep; 170(1): 23-37.

Park HH, et al. Flavonoids inhibit histamine release and expression of proinflammatory cytokines in mast cells. Arch Pharm Res. 2008 Oct; 31(10): 1303-11.

Moon PD, et al. Use of scopoletin to inhibit the production of inflammatory cytokines through inhibition of the IkappaB/NF-kappaB signal cascade in the human mast cell line HMC-1. Eur J Pharmacol 2007 Jan 26; 555(2-3): 218-225.

Kishiro S, et al. Selinidin suppresses IgE-mediated mast cell activation by inhibiting multiple steps of Fc epsilonRI signaling. Biol Pharm Bull 2008 Mar; 31(3): 442-448.

Bheekha-Escura, Roy, et al. Pharmacologic regulation of histamine release by the human recombinant histamine-releasing factor. May 1999; 103(5): 937-943.

Hong J, et al. Suppression of the antigen-stimulated RBL-2H3 mast cell activation by Artekeiskeanol A. Planta Med 2009 Nov; 75(14): 1494-1498.