Drug Design and Synthesis Research Group, Department of Pharmaceutical Chemistry, Kulliyyah of Pharmacy, International Islamic University Malaysia, Kuantan 25200, Pahang D. M., Malaysia.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Universiti Malaya, Kuala Lumpur 50603, Malaysia.
Molecules. 2022 Feb 9;27(4):1149. doi: 10.3390/molecules27041149.
According to the latest report released by the World Health Organization, bacterial resistance to well-known and widely available antibacterial drugs has become a significant and severe global health concern and a grim challenge to tackle in order to cure infections associated with multidrug-resistant pathogenic microorganisms efficiently. Consequently, various strategies have been orchestrated to cure the severe complications related to multidrug-resistant bacteria effectively. Some approaches involved the retardation of biofilm formation and multidrug-resistance pumps in bacteria as well as the discovery of new antimicrobial agents demonstrating different mechanisms of action. In this regard, natural products namely alkaloids, terpenoids, steroids, anthraquinone, flavonoids, saponins, tannins, etc., have been suggested to tackle the multidrug-resistant bacterial strains owing to their versatile pharmacological effects. Amongst these, flavonoids, also known as polyphenolic compounds, have been widely evaluated for their antibacterial property due to their tendency to retard the growth of a wide range of pathogenic microorganisms, including multidrug-resistant bacteria. The hydroxylation of C5, C7, C3', and C4'; and geranylation or prenylation at C6 have been extensively studied to increase bacterial inhibition of flavonoids. On the other hand, methoxylation at C3' and C5 has been reported to decrease flavonoids' antibacterial action. Hence, the latest information on the antibacterial activity of flavonoids is summarized in this review, with particular attention to the structure-activity relationship of this broad class of natural compounds to discover safe and potent antibacterial agents as natural products.
根据世界卫生组织发布的最新报告,细菌对知名且广泛使用的抗菌药物的耐药性已成为一个重大且严重的全球健康问题,也是一个严峻的挑战,需要有效地解决与多药耐药性病原微生物相关的感染。因此,已经制定了各种策略来有效地治疗与多药耐药菌相关的严重并发症。一些方法涉及抑制细菌生物膜的形成和多药耐药泵,以及发现具有不同作用机制的新抗菌剂。在这方面,由于其多样的药理作用,天然产物,如生物碱、萜类、类固醇、蒽醌、类黄酮、皂苷、单宁等,已被提议用于解决多药耐药菌菌株。在这些化合物中,类黄酮,也称为多酚化合物,由于其抑制多种病原微生物(包括多药耐药菌)生长的趋势,已被广泛评估其抗菌特性。C5、C7、C3'和 C4'的羟基化;以及 C6 位的香叶基化或 prenylation 已被广泛研究以增加黄酮类化合物对细菌的抑制作用。另一方面,据报道,C3'和 C5 的甲氧基化会降低类黄酮的抗菌作用。因此,本文综述了类黄酮的抗菌活性的最新信息,特别关注这一大类天然化合物的结构-活性关系,以发现安全有效的抗菌剂作为天然产物。