Bioactive Natural Products 2018

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The global phenomenon of antibioresistance, resistance genes pool (clinical and environmental reservoirs), and environmental pollution, especially by xenobiotics, including antibiotics which are considered water micropollutants, are acknowledged as some of the most important problems the world is facing today [1]。因此，具有新的，有效，无毒，并且没有选择性压力活性的抗微生物剂的必要性是显而易见的。

尽管vaccinatio巨大的科学进步n and chemotherapy, infectious diseases remain a serious health issue. Under the selective pressure of therapeutical antibiotics, used excessively during the last decades, some bacterial species/strains harboring resistance genes (pre-existent to antibiotherapy) were selected and disseminated, developing other mechanisms of resistance. As a consequence, infectious diseases remain among the leading causes of morbidity worldwide and a top priority for the public health. However, little progress has been made in the development of new antimicrobial drugs. Moreover, the wide use of antibiotics has evolutionary and ecological effects, leading to the recruitment of more genes into the抵抗和手机组合，对人类福利和环境的不利后果[2那3.]。还存在许多生物膜相关的感染，生物膜嵌入细胞显示出不同的抗性形式，称为耐受性。生物膜会导致良好的医疗问题，因为它们可以在医疗器械，组织和器官（正常或损坏）上开发，而且还可以在任何设备和工业设备上形成。附着于底层并在生物膜中组织的微生物表现出对目前抗生素，防腐剂和杀生物剂的高耐受性，以及主体防御机制。此外，由于它们的接近，通过水平转移在生物膜的嵌入式细胞之间容易实现抗性和毒力基因[4.]。

In the industrial environment, current anti-fouling agents are also far from being efficient. Hence, the adherent microorganisms on surfaces produce great economical losses caused by the uncontrolled development of biofilms on pharmaceutical or food industrial equipment. Therefore, numerous industrial technologies have to make a difficult choice: either to utilize a high amount of an efficient anti-fouling agent with the risk of developing side effects and impurifications on the final product or not to be able to control the microbial contamination and biofilm development within the technological processes. In these conditions, new, safe for health (without cytotoxicity), and eco-friendly biocides are necessary, because the consumers are currently informed, show great interest, and demand healthy food. In the coming years, it is estimated that the EU regulations will be changed and certain biocides will be banned, due to their biohazard effects.

Considering the high frequency of genetic antibioresistance in the most common pathogens, the huge public health burden of severe biofilm-associated infections (60–80% of all infections), and the great economical loses caused by the uncontrolled development of biofilms on industrial equipment, alternative strategies are urgently needed to efficiently control their formation and their negative effects. Thus, the researchers are in a continuous quest for new antibacterial agents for resistant/multiresistant strains, able to penetrate the biofilms and with activity on adherent cells. Innovative approaches include the following: (1) the development of prophylactic antimicrobial peptides, able to interfere with the intercellular communication by quorum-sensing (QS) mechanism, involved in regulation of a series of genes, including virulence genes; such QS inhibitors (QSIs) belong to the antipathogenic strategies [5.]; (2) enzymes able to degrade biofilm’s matrix (dispersins) or the signal molecules (quenching enzymes). To date, none of the envisaged antibiofilm solutions has an absolute outcome, but only their combinations seem to be effective.

The use and abuse of antibiotics, especially those with large spectrum of activity, are the cause of the frequent condition of disbiosis or alteration of the intestinal microbiota’s interspecific equilibrium. Such conditions are leading to opportunistic infections, metabolic disturbances, increased intestinal permeability, and chronic inflammation. Evidence obtained by animal models and clinical studies confirm the association of an altered gut microbiota with all corollary consequences, such as metabolic diseases from obesity to type-2 diabetes, tooth decay, cardiovascular diseases, and cancer [6.]。

所有这些最近的高度增加的问题都催化了研究努力寻找对抗病原体的新方法，对宿主没有副作用及其正常的微生物群，也没有对环境进行副作用。现在重点研究了许多研究，研究了生物活性天然产物（Bionps），主要是从植物中获得的生物活性范围的植物：抗微生物，抗炎，抗氧化剂，免疫调节，抗抑郁药，抗血糖血糖（淀粉酶活性），抗高血压，抗癌等。这些生物分子用作植物提取物或级分，偶联或不用载体（纳米颗粒）。现已在分子水平上进行研究，以识别动作，效率和缺乏细胞毒性的机制，因为它们的使用必须与疗法相比，它们的使用必须以明确的量和特定的目标进行科学依据。药物。还应探讨具有抗生素的潜在协同活动[7.那8.]。

因此，植物是Bi原的重要来源;所有植物都有由抗传染性植物化合物介导的免疫防御机制，例如植物法素和植物植物素，并且最近描述的QSIS。QSIS表现出，当即使在产水位浓度下使用时，通过抑制QS机制的细菌细胞间通信和根据细胞密度来诱导毒力基因的协调表达，表现出间接抗菌效果。QSIS的使用可以代表一种有效且智能的策略来控制抗性/耐受，毒力和殖民化/生物膜形成，没有选择性压力和其他副作用[5.那9.-13.]。

然而，由于它们的低可用性和稳定性，高波动性和不建议他们在目前的医疗实践中实施的巨大扩散能力，因此使用Bi原的使用具有一些局限性。这些特征导致促进升值的效率和递送剂的必要性，以及适用于其特定性质的优化测定方法。然而，研究努力通过巨大的潜力充分合理。

Yiannis Kourkoutas
Nikos Chorianopoulos.
Veronica拉扎尔
皮尔卢格迪·迪卡西奥

参考资料

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版权所有©2018 Yiannis Kourkoutas等。这是分布下的开放式访问文章创意公共归因许可证如果正确引用了原始工作，则允许在任何媒体中的不受限制使用，分发和再现。