CN114009443A - 截短侧耳素类化合物在抗植物病原细菌中的用途 - Google Patents
截短侧耳素类化合物在抗植物病原细菌中的用途 Download PDFInfo
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Abstract
本发明属于药物化学领域,公开了一种截短侧耳素类化合物在防治由水稻白叶枯病病原菌Xanthomonas oryzae ACCC 11602、柑橘溃疡病病原菌Xanthomonas axonopodis pv.Citri和马铃薯黑胫病病原菌Pectobacterium atrosepticaACCC 19901引起的植物病害中的用途。截短侧耳素类等上市化合物作为抗植物病原细菌剂具有广谱、高效等特点,具有进一步研究与开发的价值。
Description
技术领域
本发明属于天然药物化学领域,公开了截短侧耳素类化合物在防治由水稻白叶枯病病原菌Xanthomonas oryzae ACCC 11602、柑橘溃疡病病原菌Xanthomonas axonopodispv.Citri和马铃薯黑胫病病原菌Pectobacterium atroseptica ACCC 19901引起的农业细菌性病害中的用途。
背景技术
细菌性病害是农作物最难防治的一类病害,每年都对全世界农业造成巨大的损失。全世界细菌性作物病害约有500多种,而我国主要的细菌性作物病害有近70种。其中黄单胞菌属(Xanthomonas sp.)细菌,如水稻白叶枯病病原菌、柑橘溃疡病病原菌是生命力强、致病性高、造成重大经济损失的两种植物病原细菌。据估计,每年全世界的马铃薯产量因细菌性病害减少25%。然而现有防治植物细菌性病害的化学农药由于长期使用和滥用导致植物病害的抗性(resistance)、再增猖獗(resurgence)及农药残留超标(residue)等“3R”问题而一直是个世界性难题。因此,急需探索和开发新型高效的杀菌剂作为替代性杀菌剂,以应对农药领域目前面临的问题。
由于上市药物已经经过***的药效和生物学以及毒性研究,与全新药物的研发相比,老药新用的研发具有成功率相对较高、研发周期短且开发成本低等优点。截短侧耳素是由侧耳菌产生的一类广谱的二萜烯类抗生素,通过抑制细菌的蛋白质合成,从而达到抑制细菌生长的作用。目前截短侧耳素类抗生素主要用于由大部分革兰氏阳性菌、支原体以及部分革兰氏阴性菌引起的人或动物疾病的治疗。我们在大量筛选抗菌化合物的过程中,发现截短侧耳素类化合物对水稻白叶枯病病原菌Xanthomonas oryzae ACCC 11602、柑橘溃疡病病原菌Xanthomonas axonopodispv.Citri、马铃薯黑胫病病原菌PectobacteriumatrosepticaACCC 19901的表现出优异的抑制作用。然而尚未有其关于抗植物病原细菌活性的报道,因此可以作为先导进一步开发为新型抗植物病原细菌剂。
发明内容
本发明的目的是提供截短侧耳素类杀菌剂,用于防治由水稻白叶枯病病原菌、柑橘溃疡病病原菌、马铃薯黑胫病病原菌引起的植物病害中的用途。
为实现上述目的,本发明提供了如下技术方法:
通过二倍稀释法测定截短侧耳素、盐酸沃尼妙林化合物100、50、25、……μg/mL时对水稻白叶枯病病原菌Xanthomonas oryzae ACCC 11602、柑橘溃疡病病原菌Xanthomonasaxonopodis pv.Citri和马铃薯黑胫病病原菌Pectobacterium atrosepticaACCC 19901的抑制率,其中最低抑制浓度(MIC)定义为抑制率大于90%的最低浓度。
本发明提供的截短侧耳素类化合物作为新型抗植物病原细菌剂,具有以下优势:
1)杀菌谱广。本发明的截短侧耳素类化合物对水稻白叶枯病病原菌、柑橘溃疡病病原菌、马铃薯黑胫病病原菌等不同种属的细菌均具有抑制作用。
2)杀菌活性高。化合物盐酸沃尼妙林对水稻白叶枯病病原菌的MIC值低至0.78μg/mL,可作为新的杀植物病原细菌先导进行生物合理性设计与开发。
3)开发商业化药剂的抗植物病原细菌新作用属于“老药新用”策略,大大降低了药物的研发成本与周期。
具体实施方式
为了更好地理解本发明,通过以下具体实施例对本发明的上述内容做进一步的详细说明。但不应将此理解为对本发明的限制。下列实施例中所述实验方法,如无特殊说明,均为常规方法。
实施例1:化合物截短侧耳素、盐酸沃尼妙林为市场购买获得,截短侧耳素CAS:125-65-5,纯度>98%;盐酸沃尼妙林CAS:133868-46-9,纯度>98%。其结构式如下:
实施例2:截短侧耳素类化合物抗菌活性测定
本实验中所用的菌株为实验室-80℃含30%甘油冻存的菌株。将冻存菌株取出,分别在NB固体培养基(牛肉膏:3g,蛋白胨:5g,酵母粉:1g,蔗糖:10g,琼脂:15g,蒸馏水:1L,pH7.0;121℃灭菌20min)上面进行划线,在28℃下恒温培养直到长出单菌落。分别挑取固体培养基上单菌落至NB液体培养基(牛肉膏:3g,蛋白胨:5g,酵母粉:1g,蔗糖:10g,蒸馏水:1L;121℃灭菌20min)中,在恒温摇床上以28℃、180rpm振荡培养到对数生长期。将处于对数生长期的菌株用NB液体培养基稀释至约106CFU/mL备用。将化合物分别用DMSO溶解,加入液体培养基中,混合均匀,配制成浓度为200μg/mL的含药液体培养基。取50μL含药培养基和相同体积的含约106CFU/mL细菌培养物加入到96孔板的孔中,最终给药浓度为100μg/mL。含等量DMSO的相同浓度100μL菌液做对照。将96孔板在28℃恒温培养箱中培养24-48h直至对照组菌液长出,在酶标仪上测定孔中菌液的OD值(OD600)。并且另外测定100μL液体培养基和浓度为100μg/mL药剂的OD值,对培养基和药剂本身造成的OD值进行矫正。校正OD值和抑制率的计算公式如下:
校正OD值=含菌培养基OD值-无菌培养物OD值;
抑制率=(校正后对照培养基菌液OD值-校正后含药培养基OD值)/校正后对照培养基菌液OD值×100%
将化合物的含药液体培养基在96孔板中通过二倍稀释法稀释得到系列浓度的50μL含药培养基,然后根据上述相同的试验方法测定系列浓度对应的抑制率。所有实验设置三个重复,测定得到化合物的抑制率见表1,MIC值见表2。
表1.截短侧耳素类化合物对植物病原细菌的抑菌活性
注:“/”表示化合物的抗菌活性未测定
表2.截短侧耳素类化合物对植物病原细菌的MIC值
由表1、2生测结果可知,本发明涉及的截短侧耳素类化合物对植物病原细菌的活性明显强于商业化用药噻菌铜,表现出优异的抗菌活性。其中盐酸沃尼妙林对水稻白叶枯病病原菌的MIC值低至0.78μg/mL。
综上所述,本发明所述的截短侧耳素类化合物对植物病原细菌表现出优异的抑制作用,呈现出广谱、高活性等特点,具有进一步研究和开发的价值。
Claims (8)
1.本发明涉及截短侧耳素类化合物在抗植物病原细菌方向的用途。
3.根据权利要求1至2所述的用途,其中,截短侧耳素在防治水稻白叶枯病中的用途。
4.根据权利要求1至2所述的用途,其中,截短侧耳素在防治柑橘溃疡病中的用途。
5.根据权利要求1至2所述的用途,其中,截短侧耳素在防治马铃薯黑胫病中的用途。
6.根据权利要求1至2所述的用途,其中,盐酸沃尼妙林在防治水稻白叶枯病中的用途。
7.根据权利要求1至2所述的用途,其中,盐酸沃尼妙林在防治柑橘溃疡病中的用途。
8.根据权利要求1至2所述的用途,其中,盐酸沃尼妙林在防治马铃薯黑胫病中的用途。
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CN117223712A (zh) * | 2023-09-19 | 2023-12-15 | 贵州大学 | 一种截短侧耳素可湿性粉剂及其制备方法 |
CN117281117A (zh) * | 2023-09-19 | 2023-12-26 | 贵州大学 | 一种截短侧耳素悬浮剂及其制备方法 |
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孟丽丽等: "截短侧耳素对马铃薯幼苗生长的影响", 《中国农学通报》 * |
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CN117223712A (zh) * | 2023-09-19 | 2023-12-15 | 贵州大学 | 一种截短侧耳素可湿性粉剂及其制备方法 |
CN117281117A (zh) * | 2023-09-19 | 2023-12-26 | 贵州大学 | 一种截短侧耳素悬浮剂及其制备方法 |
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