Zinc L-carnosine
Chelating agent containing zinc and carnosine From Wikipedia, the free encyclopedia
Zinc L-carnosine (beta-alanyl-L-histidinato zinc[1]) (N-(3-aminopropionyl)-L-histidinato zinc[2]), often simply called zinc carnosine, and also known as polaprezinc,[3] is a mucosal protective[4][5] chelate compound of zinc and L-carnosine invented by Hamari Chemicals, Ltd.[6][7] It is a quadridentate 1:1 complex of a polymeric nature.[6] Although it contains 23% zinc and 77% L-carnosine by mass,[8] zinc carnosine is a molecule and not a mixture of zinc and L-carnosine.
It is an approved drug requiring a medical prescription in Japan and South Korea where it is clinically used to treat gastric ulcers.[3][9] Clinical studies have also shown its efficacy for oral mucositis, esophagitis, proctitis, taste alteration and dermatitis during and after radiotherapy.[10][11] In the United States, zinc carnosine is regulated as a New Dietary Ingredient, where notification with the US-FDA is required.[12] In Australia, it is regulated as a complementary medicine.[13] In Canada, it is regulated as a Natural Health Product.[14]
Gastrointestinal
Its mechanism of action is oxygen radical scavenging, anti-oxidation, and acceleration of gastrointestinal wound healing.[3] It exhibits ROS-quenching activities.[4] It can remain in the stomach without rapid dissociation and adhere specifically to ulcerous lesions, after which L-carnosine and zinc are released to heal the ulcer.[6] It has been shown to stimulate mucus production and to maintain the integrity of the gastric mucosal barrier.[5] It maintains homeostasis of the gastric mucosa by prostaglandin-independent cytoprotective effects due to anti-oxidative membrane stabilizing actions, and it promotes the repair of damaged tissues by wound healing action.[6]
It exerts cytoprotection through regulating heat shock proteins and chemokines, and by stabilizing mast cells.[10] It does so without affecting the secretion of gastric acid.[10] It has a potential to stimulate Hsp70 expression, with overexpression of Hsp70 being found to prevent the development of inflammatory process in the large intestinal mucosa provoked by various damaging factors.[15] It decreases p53, p21 and Bax expression and apoptosis in the intestine after irradiation.[10] It possesses antioxidant, anti-inflammatory, and genomic stability enhancement effects, thereby having potential in preventing gastrointestinal cancer development.[9]
It exhibits an inhibitory effect on H. pylori.[6]
Comparisons
Its healing efficacy against ulceration is significantly greater than that of other zinc complexes, free L-carnosine, and zinc D-carnosine[6] (which is not sold as a supplement to consumers). The pharmacological activity of zinc L-carnosine seems attributable mainly to zinc ion, presumably transported effectively into the ulcer by means of L-carnosine together with the action of L-carnosine itself.[6] In contrast, a simple mixture of L-carnosine and zinc had a lesser effect, presumably due to rapid diffusion of L-carnosine and zinc ion in the entire stomach.[6] Per preclinical data, zinc L-carnosine is superior to zinc sulfide for mucositis.[10]
Other
It has a stimulatory effect on bone formation and a restorative effect on bone loss under various pathophysiologic conditions.[16]
Zinc L-carnosine has been used orally[8][17] or as an oral rinse, lozenge or suppository.[10] The typical clinical oral dose is 150 mg/day, containing 34 mg zinc and 116 mg L-carnosine.[8][17] (The Tolerable Upper Intake Level (UL) for total zinc intake from all sources in adults is 40 mg/day.[18])
As an oral rinse, it has been used three to four times a day, with or without swallowing, providing a total amount of 150 mg/day.[10] A solution of 5% sodium alginate has been used.[10] Alternatively, it has been used as a lozenge containing 18.75 mg, four times a day.[10] It has also been used as a suppository of 75 mg with Witepsol as a base.[10]
Good clinical compliance was observed at the typical clinical oral dose of 150 mg/day, with no symptomatic side effect reported.[6] The adverse event rate was higher at high dose zinc L-carnosine (300 mg/day) without additional benefits, and therefore high dose is not recommended.[19] Side-effects are associated with the amount of zinc intake.[19]
According to the Japanese product monograph, safety in children below the age of 12, pregnant women and lactating women are not established (no experience in use); and the level of use in the elderly population is suggested and recommended at 100 mg zinc L-carnosine per day because of reduced digestive system function in the general elderly population; and those with poor liver functions should be under medical supervision.[20]
Those with copper deficiency should also be under medical supervision.[21] Although zinc L-carnosine caused an increase in serum zinc level, the serum copper level and copper:zinc ratio decreased, and a case of preexisting copper deficiency deteriorated.[8] As a mitigative, supplementation of 2 mg/day copper as glycinate chelate safely increases Cu-Zn superoxide dismutase activity.[22]
There is no evidence of a reduced tumor response to radiotherapy.[10]
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