A novel compound has shown remarkable results in relieving symptoms of dyspepsia and reduction in Helicobacter pylori infection. [1-4]
Zinc Carnosine, also called Polaprezinc and Z-103, is a chelate of a zinc ion plus carnosine in a 1:1 ratio. It has been used in Japan for a variety of gastric complaints since 1994, the combination having been quoted as being 3 times more effective than the singular ingredients, and has greater ulcer healing effects than cimetidine - a first generation anti-ulcer drug with significant drug-drug interactions. [1-7]
Safety
75mg of zinc carnosine provides a dose of 17-18mg elemental zinc and 57-58mg L-carnosine, both of which are well below the Tolerable Upper Limit (USA).
The compound's safety has been evaluated by Ohio State University and accepted by the FDA.
The dose used in clinical trials in Japan, where zinc carnosine is an approved anti-ulcer drug, are between 36.5-75 mg twice daily (75-150mg/day). This provides a daily dose of up to 38mg elemental zinc and up to 120mg carnosine, which still falls well below designated safety limits. [1,2,7] The compound is therefore deemed safe at human doses under 150mg elemental zinc per day (equivalent to 8 x 75 mg zinc carnosine tablets), above which inhibition of copper absorption could potentially occur.[7,8]
Why zinc?
Zinc is an essential cofactor in over 300 biochemical reactions and plays a pivotal role in normal deoxyribonucleic acid (DNA), ribonucleic acid (RNA) synthesis and gene transcription which affects tissue repair, normal growth, gametogenesis, and immune function. Zinc has been used to treat numerous gastrointestinal diseases such as infections (bacterial, viral and parasitic), intestinal inflammation and delayed wound healing including peptic ulcers.[8,9]
Why carnosine?
Carnosine, a dipeptide of L-histidine and beta-alanine, is found in high amounts in the brain, muscle, kidney, stomach and skeletal muscle. L-carnosine appears to have less anti-ulcer effect in isolation, possibly because it is not retained at the inflamed mucosal site for a long enough time to enhance healing.[5] As a complex, zinc carnosine has a slowed dissociation in gastric juice due to its polymeric character. It is thought that the L-carnosine portion is preferentially bound to the oozing by-products of inflamed mucosal tissue like albumin resulting in the zinc carnosine complex being retained at the site of inflammation where both the L-carnosine and zinc portions can then exert their anti-inflammatory and healing effects directly on gastrointestinal tissue.[5,6,10]
The practical uses of zinc carnosine
Apart from healing gastric and duodenal tissue injury, zinc carnosine has also been successfully used to ameliorate NSAID-induced small intestinal injury.[10] For example, when given with indomethacin, zinc carnosine successfully prevented small bowel permeability issues, meaning that zinc carnosine may have potential utility in the treatment of increased zonulin and resultant intestinal permeability from coeliac disease and wheat intolerance, and may also show benefit alongside other therapies for Inflammatory Bowel Disease and Irritable Bowel Syndrome.[11]
Actions of zinc carnosine include:[1-17]
- Anti-acid effects
- Anti-inflammatory actions (NFkB, HIF-1)
- Gastric mucous membrane adhesion
- Stabilisation of gastric and intestinal mucous membrane
- Improvement of taste disorders
- Cellular protection
- Accelerated wound healing (including pressure sores from oral dosing, and ulcerative colitis from rectal administration)
- Prevention of chemotherapy-induced oral mucositis
- Enhances interferon therapy in Hepatitis C
The use of zinc carnosine in many oral, gastric, liver and lower intestinal disorders, as well as oral treatment of pressure sores, gives practitioners a safe and effective option for either stand-alone or a safe adjunct therapy to pharmacological treatment.
Practice points
- The most common doses used in clinical studies are 75 mg zinc carnosine (equivalent to 17-18mg elemental zinc and 57-58 mg L-carnosine), given twice daily [1-5,10]
- Practitioners should not exceed 8 x 75 mg dose without responsibly adjusting for copper inhibition.
- When used in combination with Triple Therapy for Helicobacter pylori infection, possible side-effect of diarrhoea is likely not from zinc carnosine but the antibiotic component of triple therapy.
- Zinc carnosine shows no deleterious effect on chemotherapy or radiotherapy when used to prevent mucositis which would otherwise prevent therapy.
References
- Takei M. [Development of polaprezinc research].[Article in Japanese]. Yakugaku Zasshi 2012;132(3):271-277. [Abstract in English]
- Hayakawa A, Inoue M, Kunizaki M, et al. Clinical evaluation of Z-103 on gastric ulcer (thesis). Japan Pharmacol Ther 1992;20(1):1-18. [Full Text]
- Miyoshi A, Matsuo H, Miwa T, et al. Clinical evaluation of Z-103 in the treatment of gastritis, Ref. 30. A multicenter double-blind dose finding study. Jpn Pharmacol Ther 1997;25(5):1403-1442. [Full Text]
- Mori K, Karino A, Murakami A, et al. Phase III clinical study of Z-103 tablet against gastric ulcers. [Full Text]
- Matsukura T, Tanaka H. Applicability of zinc complex of L-carnosine for medical use. Biochemistry (Mosc). 2000;65(7):817-823. [Full Text]
- Furuta S, Toyama S, Miwa M, et al. Residence time of polaprezinc (zinc L-carnosine complex) in the rat stomach and adhesiveness to ulcerous sites. Jpn J Pharmacol 1995;67(4):271-278. [Full Text]
- DiSilvestro R. Polaprezinc FDA evaluation. 2002 Sect 6, Att C, Vol 98. [Full Text]
- Lee SR, Noh SJ, Pronto JR, et al. The critical roles of zinc: beyond impact on myocardial signaling. Korean J Physiol Pharmacol 2015;19(5):389-399. [Full Text]
- Skrovanek S, DiGuilio K, Bailey R, et al. Zinc and gastrointestinal disease. World J Gastrointest Pathophys 2014;5(4):496-513. [Full Text]
- Mahmood A, FitzGerald AJ, Marchbank T, et al. Zinc carnosine, a health food supplement that stabilises small bowel integrity and stimulates gut repair processes. Gut 2007;56(2):168-175. [Full Text]
- Watari I, Oka S, Tanaka S, et al. Effectiveness of polaprezinc for low-dose aspirin-induced small-bowel mucosal injuries as evaluated by capsule endoscopy: a pilot randomized controlled study. BMC Gastroenterol. 2013;13:108. [Full Text]
- Watanabe T, Ishihara M, Matsuura K, et al. Polaprezinc prevents oral mucositis associated with radiochemotherapy in patients with head and neck cancer. Int J Cancer 2010;127(8):1984-1990. [Full Text]
- Hayashi H, Kobayashi R, Suzuki A, et al. Polaprezinc prevents oral mucositis in patients treated with high-dose chemotherapy followed by hematopoietic stem cell transplantation. Anticancer Res 2014;34(12):7271-7277. [Full Text]
- Sakae K, Yanagisawa H. Oral treatment of pressure ulcers with polaprezinc (zinc L-carnosine complex): 8-week open-label trial. Biol Trace Elem Res 2014;158(3):280-288. [Abstract]
- Itagaki M, Saruta M, Saijo H, et al. Efficacy of zinc-carnosine chelate compound, Polaprezinc, enemas in patients with ulcerative colitis. Scand J Gastroenterol 2014;49(2):164-172. [Abstract]
- Sakagami M, Ikeda M, Tomita H, et al. A zinc-containing compound, Polaprezinc, is effective for patients with taste disorders: randomized, double-blind, placebo-controlled, multi-center study. Acta Otolaryngol 2009;129(10):1115-1120. [Abstract]
- Takagi H, Nagamine T, Abe T, et al. Zinc supplementation enhances the response to interferon therapy in patients with chronic hepatitis C. J Viral Hepat 2001;8(5):367-371. [Abstract]
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