Novel Piperazine-Tailored Ursolic Acid Hybrids as Significant Antibacterial Agents Targeting Phytopathogens Xanthomonas oryzae pv. oryzae and X. axonopodis pv. citri Probably Directed by Activation of Apoptosis
Novel Piperazine-Tailored Ursolic Acid Hybrids as Significant Antibacterial Agents Targeting Phytopathogens Xanthomonas oryzae pv. oryzae and X. axonopodis pv. citri Probably Directed by Activation of Apoptosis
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新型哌嗪定制熊果酸杂种作为针对植物病原体米黄单胞菌的重要抗菌剂。
DOI：
10.1002/ps.5822
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发表时间：
2020
影响因子：
4.1
通讯作者：
Yang Song
中科院分区：
文献类型：
--
作者：
Wang Pei-Yi;Xiang Meng;Luo Min;Liu Hong-Wu;Zhou Xiang;Wu Zhi-Bing;Liu Li-Wei;Li Zhong;Yang Song
背景诱导细胞凋亡是一种有效的技术，可以重新编程细胞的生理和病理过程，以利用其先天系统根除不需要的细胞。受此启发，许多细胞凋亡诱导剂被开发出来用于治疗动物疾病，特别是在抗癌领域。然而，很少有研究报道通过激活细胞凋亡来攻击植物病原体的诱导剂的开发。为了探索和发现针对植物病原体的细胞凋亡诱导剂，系统地构建了一簇哌嗪定制的熊果酸（UA）杂种。结果体外测试表明，标题分子可以抑制两种顽固菌株的生长，定义为Xanthomonas oryzaepv.oryzae和X。柑橘轴突变种。相应的最低EC50值为0.37和1.08 μg mL−1，超过了UA（>400 μg mL−1）和阳性对照。此外，化合物5u和5v可以通过盆栽实验控制体内白叶枯病。流式细胞仪分析表明标题化合物可以诱导测试细菌明显的细胞凋亡行为。深入研究表明，引入设计的化合物可以降低过氧化氢酶和超氧化物歧化酶的酶活性，从而导致活性氧的积累。结论本研究通过创新的作用方式促进了用于管理农业细菌感染的细胞凋亡引发剂的开发。 © 2020 中国化工学会
BACKGROUNDInduced apoptosis is an effective technique that can reprogram cellular physiological and pathological processes to eradicate undesirable cells using their innate systems. Inspired by this, numerous apoptosis inducers have been developed to treat animal diseases, especially in the anticancer field. However, few studies have reported on the development of inductive agents that attack plant pathogens by activation of apoptosis. With the aim of exploring and discovering apoptosis inducers that target phytopathogens, a cluster of piperazine‐tailored ursolic acid (UA) hybrids was systematically fabricated.RESULTSIn vitrotesting showed that the title molecules could inhibit the growth of two intractable bacterial strains, defined asXanthomonas oryzaepv.oryzaeandX. axonopodispv.citri. The corresponding lowest EC50values were 0.37 and 1.08 μg mL−1, which exceed those of UA (>400 μg mL−1) and positive controls. Moreover, compounds5uand5vcould manage bacterial blightin vivousing pot experiments. Flow cytometer analysis indicted that the title compounds could induce distinct apoptotic behaviors on tested bacteria. In‐depth study revealed that the introduction of designed compounds could reduce the enzyme activities of catalase and superoxide dismutase, subsequently leading to the accumulation of reactive oxygen species.CONCLUSIONThis study promoted the development of apoptosis initiators for managing bacterial infections in agriculture by an innovative mode of action. © 2020 Society of Chemical Industry