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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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BACKGROUND Induced apoptosis mechanism is an intriguing and effective manner that can reprogram cellular physiological and pathological processes to eradicate the undesired cells by their innate systems. Inspired by this… Click to show full abstract

BACKGROUND Induced apoptosis mechanism is an intriguing and effective manner that can reprogram cellular physiological and pathological processes to eradicate the undesired cells by their innate systems. Inspired by this opinion, numerous apoptosis inducers have been developed to treat animal diseases, especially in anticancer field. However, few studies reported to develop that kind of inductive agents for attacking plant pathogens by activation of apoptosis. With the aim of exploring and discovering abovementioned apoptosis inducers targeting phytopathogens, herein, a cluster of piperazine-tailored ursolic acid (UA) hybrids was systematically fabricated. RESULTS In vitro testing announced that title molecules could inhibit the growth of two intractable bacterial strains, defined as Xanthomonas oryzae pv. oryzae and X. axonopodis pv. citri. The corresponding lowest EC50 values were 0.37 and 1.08 μg/mL, which exceeded those of UA (> 400 μg/mL) and positive controls. Moreover, compounds 5u and 5v could manage bacterial blight in vivo using pot experiments. Flow cytometer analysis indicted that 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, and subsequently leading to the accumulation of reactive oxygen species. CONCLUSION This study can promote the development of apoptosis initiators for managing bacterial infections in agriculture by an innovative mode of action. This article is protected by copyright. All rights reserved.

Keywords: piperazine tailored; activation apoptosis; tailored ursolic; apoptosis; targeting phytopathogens; oryzae

Journal Title: Pest management science
Year Published: 2020

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