Abstract

Increasing antimicrobial resistance, together with the occurrence of side effects of NSAIDs or glucocorticoids represents certain motivation to search for new natural dual antimicrobial and anti-inflammatory drugs. We here present selected natural compounds, possessing both antimicrobial and anti-inflammatory activity. The review contains also the information about structure–activity relationships with respect to natural or semisynthetic origin of compounds and synergy effects between natural dual inhibitors and commercially available antibiotics. Data published from 2000 to 2018 were obtained using databases Google Scholar, Science Direct and Web of Science, and searching keywords such as alkaloids, anti-inflammatory activity, antimicrobial activity, chalcones, coumarins, flavonoids, IC₅₀, lignans, MIC, natural compounds, synergistic effect and terpenoids, alone or in a combination. The primary criteria for the selection of appropriate compounds were the MICs and IC₅₀s used for a quantification of effects. The natural compounds with activity close to the reference substances or showing MIC up to 32 µg ml⁻¹, and IC₅₀ of anti-inflammatory effect up to 15 µM were considered as promising. When available, information about in vivo testing was included. Reviewed dual inhibitors can represent modern therapeutic approach, especially when the process of inflammation is followed by a secondary bacterial infection. Benefits of dual inhibitors are based on better compliance of patients, decreased number of side effects and extended spectrum of action.

Graphic abstract

中文翻译：

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具有双重抗菌和消炎作用的天然化合物

摘要

越来越多的抗微生物药物耐药性以及非甾体抗炎药或糖皮质激素的副作用的出现，代表了寻找新的天然双重抗微生物和抗炎药物的动机。我们在这里提出了具有抗微生物和抗炎活性的天然化合物。该综述还包含有关化合物天然或半合成来源的结构-活性关系以及天然双重抑制剂与市售抗生素之间协同作用的信息。数据2000至2018年使用的数据库谷歌学术，科学的科学指导和网络，并作为搜索关键字，得到了出版生物碱，抗-抗炎活性，抗菌活性，查耳酮，香豆素，类黄酮，IC ₅₀，木脂素，MIC，天然化合物，协同作用和萜类化合物，可单独使用或组合使用。选择合适化合物的主要标准是用于量化效应的MIC和IC ₅₀。活性接近参考物质或MIC高达32 µg ml ^-1的天然化合物，IC ₅₀高达15 µM的抗炎作用被认为很有希望。如果可用，则包括有关体内测试的信息。审查过的双重抑制剂可以代表现代治疗方法，尤其是在炎症继发于继发性细菌感染之后。双重抑制剂的益处基于患者更好的依从性，减少的副作用数量和作用范围的扩大。

图形摘要