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含肉桂醛制剂治疗口腔真菌感染的毒理学参数:一项研究。

Toxicological Parameters of a Formulation Containing Cinnamaldehyde for Use in Treatment of Oral Fungal Infections: An Study.

机构信息

Department of Clinical and Social Dentistry, Graduate Program in Natural and Synthetic Bioactive Products (PgPNSB), Center for Health Sciences, Federal University of Paraiba, João Pessoa PB, Brazil.

Graduate Program in Molecular and Cell Biology, Center for Health Sciences, Federal University of Paraiba, João Pessoa PB, Brazil.

出版信息

Biomed Res Int. 2021 Oct 22;2021:2305695. doi: 10.1155/2021/2305695. eCollection 2021.

DOI:10.1155/2021/2305695
PMID:34722758
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8556081/
Abstract

OBJECTIVE

We aimed to define the safety and toxicity of both isolated and embedded cinnamaldehyde using a pharmaceutical formulation for the treatment of oral fungal infections in an study.

MATERIALS AND METHODS

Acute toxicity was assessed in studies with larvae and embryos (zebrafish), and genotoxicity was assessed in a mouse model. The pharmaceutical formulation (orabase ointment) containing cinnamaldehyde was evaluated for verification of both antifungal activity and toxicity in keratinized oral rat mucosa.

RESULTS

In larvae, cinnamaldehyde was not toxic up to the highest dose tested (20 mg/kg) and presented no genotoxicity up to the dose of 4 mg/kg in the model using mice. However, it was found to be toxic in zebrafish embryos up to a concentration of 0.035 g/mL; LC 0.311; EC 0.097 (egg hatching delay); and 0.105 (Pericardial edema). In the orabase antifungal susceptibility test, cinnamaldehyde exhibited activity in concentrations greater than 200 g/mL. As for safety in the animal model with rats, the orabase ointment proved to be safe for use on keratinized mucosa up to the maximum concentration tested (700 g/mL).

CONCLUSIONS

At the concentrations tested, cinnamaldehyde was not toxic in vertebrate and invertebrate animal models and did not exhibit genotoxic activity. In addition, when used in the form of an ointment in orabase, having already recognized antifungal activity, it was shown to be safe up to the highest concentration tested.

摘要

目的

我们旨在使用一种用于治疗口腔真菌感染的药物制剂,定义孤立和嵌入肉桂醛的安全性和毒性。

材料和方法

在幼虫和胚胎(斑马鱼)研究中评估急性毒性,在小鼠模型中评估遗传毒性。含有肉桂醛的药物制剂(或abase 软膏)用于验证角质化口腔大鼠黏膜的抗真菌活性和毒性。

结果

在幼虫中,肉桂醛在最高测试剂量(20mg/kg)下没有毒性,在使用小鼠的模型中,最高剂量为 4mg/kg 时也没有遗传毒性。然而,它在斑马鱼胚胎中发现具有毒性,浓度达到 0.035g/ml;LC 0.311;EC 0.097(卵孵化延迟);和 0.105(心包水肿)。在 orabase 抗真菌药敏试验中,肉桂醛在浓度大于 200μg/ml 时表现出活性。至于在大鼠动物模型中的安全性,orabase 软膏在测试的最大浓度(700μg/ml)下证明对角化黏膜安全。

结论

在测试的浓度下,肉桂醛在脊椎动物和无脊椎动物动物模型中没有毒性,也没有表现出遗传毒性活性。此外,当以软膏形式在 orabase 中使用时,肉桂醛已经具有抗真菌活性,在测试的最高浓度下也表现出安全性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/5f8f92a0fdfe/BMRI2021-2305695.008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/cfc7ba257742/BMRI2021-2305695.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/5f8f92a0fdfe/BMRI2021-2305695.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/6ae1e5935f66/BMRI2021-2305695.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/640097a05152/BMRI2021-2305695.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/729207e161cc/BMRI2021-2305695.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/125a6a20577e/BMRI2021-2305695.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/08a8c2081f42/BMRI2021-2305695.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/a8b1a8cefbe0/BMRI2021-2305695.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/cfc7ba257742/BMRI2021-2305695.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d64b/8556081/5f8f92a0fdfe/BMRI2021-2305695.008.jpg

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