School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China; Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences, Lanzhou 730000, People's Republic of China.
Pestic Biochem Physiol. 2019 Sep;159:51-58. doi: 10.1016/j.pestbp.2019.05.015. Epub 2019 May 25.
Isoquinoline alkaloids possess broad pharmacological activities. In this study, the antifungal activity of twelve isoquinoline alkaloids, including berberine (1), jatrorrhizine (2), coptisine (3), corydaline (4), tetrahydroberberine (5), chelidonine (6), dihydrosanguinarine (7), chelerythrine (8), sanguinarine (9), palmatine (10), tetrahydropalmatine (11) and columbamine (12) were evaluated against eight plant pathogenic fungi in vitro. All the tested compounds showed varying degrees of inhibition against the eight tested plant fungi. Among them, sanguinarine exhibited high antifungal activity (EC ranging from 6.96-59.36 μg/mL). It displayed the best inhibitory activity against Magnaporthe oryzae (EC = 6.96 μg/mL), compared with azoxystrobin (EC = 12.04 μg/mL), and significantly suppressed spore germination of M. oryzae with the inhibition rate reaching 100% (50 μg/mL). The optical microscopy and scanning electron microscopy observations revealed that after treating M. oryzae mycelia with sanguinarine at 10 μg/mL, the mycelia appeared curved, collapsed and the cell membrane integrity was eventually damaged. Furthermore, the reactive oxygen species production, mitochondrial membrane potential and nuclear morphometry of mycelia had been changed, and the membrane function and cell proliferation of mycelia were destroyed. These results will enrich our insights into action mechanisms of antifungal activity of sanguinarine against M. oryzae.
异喹啉生物碱具有广泛的药理活性。在这项研究中,评估了 12 种异喹啉生物碱,包括小檗碱(1)、黄连碱(2)、小檗碱(3)、紫堇碱(4)、四氢小檗碱(5)、白屈菜红碱(6)、二氢血根碱(7)、白屈菜红碱(8)、血根碱(9)、巴马汀(10)、四氢巴马汀(11)和刻叶紫堇碱(12)对 8 种植物病原真菌的体外抗真菌活性。所有测试的化合物对 8 种测试的植物真菌都表现出不同程度的抑制作用。其中,血根碱表现出很高的抗真菌活性(EC 范围为 6.96-59.36μg/mL)。与肟菌酯(EC=12.04μg/mL)相比,它对稻瘟病菌(EC=6.96μg/mL)表现出最好的抑制活性,并且显著抑制稻瘟病菌孢子萌发,抑制率达到 100%(50μg/mL)。光学显微镜和扫描电子显微镜观察表明,用 10μg/mL 的血根碱处理稻瘟病菌菌丝后,菌丝出现弯曲、塌陷,细胞膜完整性最终受损。此外,菌丝的活性氧产生、线粒体膜电位和核形态计量学发生了变化,菌丝的膜功能和细胞增殖被破坏。这些结果将丰富我们对血根碱抗稻瘟病菌活性的作用机制的认识。