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Antimicrobial Peptides for Plant Disease Control. From Discovery to Application

机译:植物疾病控制的抗菌肽肽。从发现到申请

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Sustainable protection of plant crops against diseases relies on a rational use of pesticides and to a reduction of the number of active ingredients to the more selective, less toxic and with a lower negative environmental impact. Antimicrobial peptides (AMPs) are envisaged as new plant disease control products because of the need for novel antifungals, antibacterials and plant strengtheners in Agriculture. Natural AMPs are produced in low amounts, some are toxic, or low active or unstable, and require generally complex and costly procedures for extraction and purification from the producing organism. Synthetic AMPs offer alternatives but require pharma approaches for development as plant protection products. We have developed linear undecapeptides (CECMEL11) and cyclic decapeptides (CYC 10) against plant pathogens following the classical hit-to-lead and lead optimization approaches, based on combinatorial chemistry of some critical positions in their amino acid sequence. The peptides were improved for activity against plant pathogenic bacteria and fungi, but minimizing hemolytic activity and protease susceptibility. The selected peptides covered a wide range of action spectrum. Peptide BP100 was strongly lytic against Gram negative bacteria including plant pathogenic bacteria and food-borne human bacterial pathogens, but poorly antifungal. Peptide BP21 displayed strong fungicidal and sporicidal activity but slight antibacterial activity. Acute oral toxicity in mice is slight or non-toxic. Proof-of-concept assays have been performed with success including whole plant tests against Erwinia amylovora and Pseudomonas syringae on pear, and Xanthomonas axonopodis pv. vesicatoria on pepper, as well as in postharvest against Penicillium-rot on apple. The main limitation of the implementation of the antimicrobial peptide technology in the field of plant protection is due to the production costs, but strong efforts are in progress to produce these peptides using microbial and plant biofactories.
机译:植物作物免受疾病的可持续保护依赖于合理使用农药,并减少活性成分的数量,以更具选择性,更毒性和较低的对抗环境影响。由于需要新的抗真菌,抗菌剂和农业增强剂,因此设想抗微生物肽(AMPs)被设想为新的植物疾病控制产品。天然AMPS以低量产生,有些是有毒的,或低活性或不稳定,并且需要大致复杂且昂贵的程序用于从生产的生物体中提取和纯化。合成放大器提供替代品,但需要制药方法作为植物保护产品的发展。在经典的袭击引线和铅优化方法基于在其氨基酸序列中的一些关键位置的组合化学,我们开发了针对植物病原体的线性未屠肽(CECMEL11)和环状疏皮肽(CYC 10)。肽的活性促进植物致病菌和真菌,但最小化溶血活性和蛋白酶敏感性。所选肽覆盖了各种动作光谱。肽BP100强烈含有针对革兰氏阴性细菌的含量,包括植物致病细菌和食品传播的人体细菌病原体,但抗真菌症差。肽BP21显示出强杀菌性和刺激性活性但轻微的抗菌活性。小鼠中的急性口腔毒性轻微或无毒。已经通过成功进行了概念证据,包括全植物测试对梨的艾尔维亚Amylovora和Pseudomonas incringae的全植物测试,以及Xanthomonas Axonopodis PV。胡椒的果酱,以及在苹果上的Penicillium-rot的波萨多。在植物保护领域实施抗微生物肽技术的主要限制是由于生产成本,但强劲的努力正在使用微生物和植物生物暗度生产这些肽。

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