Department of Chemical Engineering, University of Chemistry and Technology Prague, Prague, Czech Republic.
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Prague, Czech Republic.
PLoS One. 2021 Mar 19;16(3):e0248878. doi: 10.1371/journal.pone.0248878. eCollection 2021.
Garlic is a well-known example of natural self-defence system consisting of an inactive substrate (alliin) and enzyme (alliinase) which, when combined, produce highly antimicrobial allicin. Increase of alliinase stability and its activity are of paramount importance in various applications relying on its use for in-situ synthesis of allicin or its analogues, e.g., pulmonary drug delivery, treatment of superficial injuries, or urease inhibitors in fertilizers. Here, we discuss the effect of temperature, pH, buffers, salts, and additives, i.e. antioxidants, chelating agents, reducing agents and cosolvents, on the stability and the activity of alliinase extracted from garlic. The effects of the storage temperature and relative humidity on the stability of lyophilized alliinase was demonstrated. A combination of the short half-life, high reactivity and non-specificity to particular proteins are reasons most bacteria cannot deal with allicin's mode of action and develop effective defence mechanism, which could be the key to sustainable drug design addressing serious problems with escalating emergence of multidrug-resistant (MDR) bacterial strains.
大蒜是一种众所周知的天然自卫系统的例子，它由一种非活性基质（蒜氨酸）和一种酶（蒜氨酸酶）组成，当两者结合时，会产生具有高度抗菌作用的蒜素。在各种依赖于使用蒜氨酸或其类似物原位合成的应用中，增加蒜氨酸酶的稳定性和活性至关重要，例如肺部药物输送、治疗浅表损伤或肥料中的脲酶抑制剂。在这里，我们讨论了温度、pH 值、缓冲液、盐和添加剂（如抗氧化剂、螯合剂、还原剂和共溶剂）对从大蒜中提取的蒜氨酸酶的稳定性和活性的影响。还证明了储存温度和相对湿度对冻干蒜氨酸酶稳定性的影响。半衰期短、反应性高且对特定蛋白质无特异性是大多数细菌无法应对蒜素作用模式并形成有效防御机制的原因，这可能是解决严重问题的可持续药物设计的关键，这些问题与不断出现的多药耐药（MDR）细菌菌株有关。
