Design, Synthesis, Antibacterial Activity, Antiviral Activity, and Mechanism of Myricetin Derivatives Containing a Quinazolinone Moiety.
Design, Synthesis, Antibacterial Activity, Antiviral Activity, and Mechanism of Myricetin Derivatives Containing a Quinazolinone Moiety.
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DOI：
10.1021/acsomega.1c05256
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发表时间：
2021-11-16
期刊：
影响因子：
4.1
通讯作者：
Xue W
中科院分区：
文献类型：
--
作者：
Liu T;Peng F;Cao X;Liu F;Wang Q;Liu L;Xue W
植物细菌如Xanthomonasaxonopodispv. citri（Xac）、柑橘假单胞菌（Pseudomonasjetingaepv.）（Psa）、水稻黄单胞菌Xanthomonasoryzaepv.）烟草花叶病毒（Xoo）和烟草花叶病毒（TMV）对全球粮食和经济作物贸易造成了巨大障碍。然而，用于防治这些植物病害的传统化学药剂由于长期不规范使用，已逐渐变得不利。因此，寻找新的高效抗菌抗病毒药物势在必行。本研究设计并合成了一系列含喹唑啉酮结构的杨梅素衍生物，并对这些化合物的抗菌和抗病毒活性进行了评价。生物活性测定结果表明，部分目标化合物具有较好的体外抗菌活性和体内抗病毒活性。其中，化合物L18对Xac的半数有效浓度（EC 50）值为16.9 μg/mL，优于对照药物铋噻唑（BT）（62.2 μg/mL）和噻二唑铜（TC）（97.5 μg/mL）。扫描电子显微镜（SEM）结果证实化合物L18通过影响细胞形态抑制Xac生长。微量热电泳（MST）结果表明，化合物L11对TMV CP的解离常数（Kd）为0.012 μM，优于对照药剂宁南霉素（2.726 μM）。本研究揭示含有喹唑啉酮结构的杨梅素衍生物是潜在的抗菌和抗病毒剂。
Plant bacteria such as Xanthomonas axonopodispv. citri (Xac), Pseudomonas syringaepv. actinidiae (Psa), Xanthomonas oryzaepv. oryzae (Xoo), and tobacco mosaic virus (TMV) have created huge obstacles to the global trade of food and economic crops. However, traditional chemical agents used to control these plant diseases have gradually become disadvantageous due to long-term irregular use. Therefore, finding new and efficient antibacterial and antiviral agents is becoming imperative. In this study, a series of myricetin derivatives containing a quinazolinone moiety were designed and synthesized, and the antibacterial and antiviral activities of these compounds were evaluated. The bioassay results showed that some target compounds exhibited good antibacterial activities in vitro and antiviral activities in vivo. Among them, the median effective concentration (EC50) value of compound L18 against Xac was 16.9 μg/mL, which was better than those of the control drugs bismerthiazol (BT) (62.2 μg/mL) and thiodiazole copper (TC) (97.5 μg/mL). Scanning electron microscopy (SEM) results confirmed that compound L18 inhibited the growth of Xac by affecting the morphology of cells. Microscale thermophoresis (MST) test results indicated that the dissociation constant (Kd) value of compound L11 against TMV-CP was 0.012 μM, which was better than that of the control agent ningnanmycin (2.726 μM). This study reveals that myricetin derivatives containing a quinazolinone moiety are potential antibacterial and antiviral agents.
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