Polaprezinc protects normal intestinal epithelium against exposure to ionizing radiation in mice

Odawara, Soichi; Doi, Hiroshi; Shikata, Toshiyuki; Kitajima, Kazuhiro; Suzuki, Hitomi; Niwa, Yasue; Kosaka, Kengo; Tarutani, K.; Tsujimura, Tohru; Kamikonya, Norihiko; Hirota, Shun

doi:10.3892/mco.2016.983

Cited by 17 publications

(6 citation statements)

References 14 publications

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“…Endoscopic and histological analyses demonstrated that mucosal inflammation is significantly reduced in theses rats compared with control group (44). Another study also reported that administration of 100 mg/kg polaprezinc 2 h before experiment can reduce the apoptosis of intestinal epithelial cells in the duodenum, jejunum and ileum during ion beam injury, protecting the normal epithelial cells in the intestine (45).…”

Section: Radioactive Esophagitis Hayashi Et Almentioning

confidence: 84%

Recent advances on polaprezinc for medical use (Review)

Sun

Zhang

2021

Exp Ther Med

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The present study described the chemical and biological properties of zinc complex of L-carnosine (L-CAZ; generic name, polaprezinc; chemical name, catena-molecular formula, C 9 H 14 N 4 O 3 Zn; molecular weight, 291.6404; CAS registry number, 107667-60-7). Characterized as a white or yellowish white crystalline powder, this drug is insoluble in glacial acetic acid and almost insoluble in water, methanol, ethanol and ether. It is soluble in dilute hydrochloric acid, dilute nitric acid and sodium hydroxide solution, and its melting point is 260-270˚C. Polaprezinc is an anti-ulcer drug that was jointly studied and developed by Hamari Chemicals Co., Ltd. and Zeria Pharmaceutical Co., Ltd., and was first approved in Japan in 1994. This review article summarizes the research advances of polaprezinc, including the patents, preparations, synthetic routes, pharmacokinetics, pharmacological effects and application in clinical research. Contents 1. Introduction 2. Patents and preparations 3. Synthetic route and pharmacokinetics of polaprezinc 4. Pharmacological study of polaprezinc 5. Clinical uses of polaprezinc 6. Other clinical applications 7. Safety 8. Conclusion

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Section: Radioactive Esophagitis Hayashi Et Almentioning

confidence: 84%

Recent advances on polaprezinc for medical use (Review)

Sun

Zhang

2021

Exp Ther Med

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“…Hepilor R has been used for the treatment of peptic ulcers in Japan since 1994, and many studies tested it in the gastrooesophageal and intestinal areas (4-11). In the anorectal field, this compound has proven to be very effective in treating radiation proctitis (12,13) and ulcerative colitis, where it induced a significant clinical and endoscopic remission (14). Zinc-L-Carnosine induces mucosal repair, stimulating mucus production, antioxidant activity, and membrane-stabilising activity.…”

Section: Discussionmentioning

confidence: 99%

“…This compound proved to be very effective in treating radiation proctitis, a difficult clinical condition, significantly improving endoscopic pictures and symptoms (12,13). Furthermore, the product has been effectively tested in ulcerative colitis, where it induced a significant clinical and endoscopic remission (14).…”

Section: Introductionmentioning

confidence: 99%

Efficacy and Tolerability of a New Formulation in Rectal Ointment Based on Zn-L-Carnosine (Proctilor®) in the Treatment of Haemorrhoidal Disease

Pietroletti

Giuliani

Buonanno³

et al. 2022

Front. Surg.

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Haemorrhoidal disease (HD) shows high prevalence in western countries, reaching 4.4% per year in the US. Topical preparations are the first-line treatments, which are readily available as “over-the-counter” (OTC) products, often containing a nonstandardised mixture of “natural” remedies, or anaesthetics or cortisol;those latter are not free from undesirable effects. The Zinc-L-Carnosine is a cytoprotective compound, promoting mucosal repair in the gastrointestinal tract and also in mucosal repair, following radiation injuries to the rectum as well as in ulcerative colitis. Our aim was to study the efficacy of Zinc-L-Carnosine in relieving acute symptoms of HD, testing a preparation in the rectal ointment, Proctilor®, in patients complaining of bleeding or thrombosed piles. In a multicentre open trial, 21 patients older than 18 years of age were enrolled. The symptoms of HD were graded according to the Haemorrhoidal Disease Symptoms Score (HDSS) in association with the Short Health Scale (SHS) to assess the influence of HD on quality of life. The pain was assessed with the VAS score, bowel habit by means of the Bristol scale. The patients were evaluated at enrolment (T0) and 2 (T1) and 4 (T2) weeks of treatment with Proctilor® rectal ointment. There were 10 men and 11 women; mean age, 49 years. Pain, bleeding, and thrombosis were all significantly reduced after treatment; the mean VAS score decreased from 4.71 ± 3.05 at T0 to.52 ± 0.87 and.05 ± 0.22 at T1 and T2, respectively; (mean ± SD; p < 0.001 in both cases). Similarly, the HDSS score showed to be significantly reduced between T0, T1 (8.05 ± 4.55 vs. 1.14 ± 1.01), and T2 (8.05 ± 4.55 vs. 24 ± 0.44) (mean ± SD; p < 0.001 in both cases). Quality of life showed to be improved as the SHS score decreased significantly with treatment (7.90 ± 4.17 at T0 vs. 4.24 ± 0.44 at T1 vs. 4.05 ± 0.22 at T2; mean ± SD; p < 0.001 in both cases). The Bristol score of defecation remained substantially unchanged. No side effects or discontinuation of treatment were reported. Results of our investigation suggest a role of Proctilor® rectal ointment in treating symptomatic HD with good results and an excellent safety profile. However, our preliminary results encourage further studies on a larger number of patients to confirm the role of Zinc-L-Carnosine in the rectal ointment for the topical treatment of HD.

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“…A research dealing with the long‐term use of low‐dose aspirin found that the aggregate median of small intestinal swelling, erosion and ulcer lesions was considerably decreased in Polaprezinc group . Animal studies have revealed that oral Polaprezinc prior to radiotherapy can effectively reduce the apoptosis of jejunal crypt cells in rats . According to the drug specification of Polaprezinc in the treatment of gastric ulcer, the recommended oral dosage amounts to be 75 mg, two times daily, and the instruction clearly suggests that the dose may be increased in accordance with the disease status as well as severity of symptoms.…”

Section: Discussionmentioning

confidence: 99%

Oral Administration of Polaprezinc Attenuates Fluorouracil‐induced Intestinal Mucositis in a Mouse Model

Xie

Teng

et al. 2017

Basic Clin Pharma Tox

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5-Fluorouracil (5-FU) has broadly been applied to treat colorectal cancer as one of the most effective chemotherapeutic agents. However, it frequently causes intestinal mucosal injury and related side effects, such as abdominal pain and diarrhoea, which limit the use of 5-FU in a clinic setting. Polaprezinc has gradually become known as a mucosal protective agent for the management of gastric ulcer. This study aimed to investigate the prophylactic efficacy of Polaprezinc administered orally against intestinal mucositis induced by 5-FU in mice on the condition that the antitumour effect could not be compromised. We induced intestinal mucositis in SPF-grade ICR mice with 5-FU, and evaluated intestinal damage in the absence or presence of Polaprezinc. We examined the score of diarrhoea and the loss of weight after the 5-FU treatment and assessed the integrity of villus and the proliferation of small intestine crypt cells by haematoxylin and eosin staining and PCNA immunohistochemical detection. The antitumour effect of 5-FU on colorectal cancer was assessed with or without Polaprezinc in a xenograft model. The result showed that Polaprezinc significantly reduced the elevated diarrhoea score and the body-weight loss caused by 5-FU abolished histological abnormality and crypt cell hypoproliferation in a dose-dependent manner, without affecting 5-FU efficacy on colon xenograft tumour in mice. We conclude that Polaprezinc could inhibit 5-FU-induced diarrhoea and alleviate the weight loss during 5-FU chemotherapy, as a possible candidate for treatment and prevention of intestinal mucositis, through protecting intestinal mucosa and improving the quality of life after chemotherapy.

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Polaprezinc protects normal intestinal epithelium against exposure to ionizing radiation in mice

Cited by 17 publications

References 14 publications

Recent advances on polaprezinc for medical use (Review)

Recent advances on polaprezinc for medical use (Review)

Efficacy and Tolerability of a New Formulation in Rectal Ointment Based on Zn-L-Carnosine (Proctilor®) in the Treatment of Haemorrhoidal Disease

Oral Administration of Polaprezinc Attenuates Fluorouracil‐induced Intestinal Mucositis in a Mouse Model

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