College of Chemistry and Pharmacy, Qingdao Agricultural University, Changcheng Road 700, Qingdao, Shandong 266109, PR China.
Analytical and Testing Center, Qingdao Agricultural University, Qingdao, Shandong 266109, PR China.
Pestic Biochem Physiol. 2018 Sep;150:59-65. doi: 10.1016/j.pestbp.2018.07.001. Epub 2018 Jul 6.
In the search for antifungal lead compounds from natural resources, Notopterygium incisum, a medicine plant only distributed in China, showed antifungal potential against apple fruit pathogens. Based on the bioassay-guided isolation, chromatography fraction 6 of the ethyl acetate partition exhibited significant in vitro and in vivo antifungal activities against apple fruit pathogens. Furthermore, nine antifungal secondary metabolites, including five linear furocoumarins (1-5), two phenylethyl esters (6-7), one falcarindiol (8), and one sesquiterpenoid (9), were isolated and elucidated from fraction 6. Compound 5 is a new metabolite, and 9 isolated from the genus Notopterygium for the first time. The purified compounds (1-9) were firstly reported to exhibit antifungal activities against apple fruit pathogens of Colletotrichum gloeosporioides and Botryosphaeria dothidea with the MIC values ranging from 8 to 250 mg L, especially 8 of 16 and 8 mg L, respectively. Moreover, 8 could inhibit the spore germination and new sporulation of B. dothidea, as well as enhance the membrane permeabilization of B. dothidea spores. This was the first investigation for the antifungal components against apple fruit pathogens from Notopterygium incisum, which has great potential to be developed into bio-fungicides.
在从天然资源中寻找抗真菌先导化合物的过程中，羌活，一种仅分布在中国的药用植物，表现出对苹果果实病原菌的抗真菌潜力。基于生物测定指导的分离，乙酸乙酯部分的色谱馏分 6 显示出对苹果果实病原菌具有显著的体外和体内抗真菌活性。此外，从馏分 6 中分离并阐明了 9 种抗真菌次生代谢物，包括 5 种线性呋喃香豆素（1-5）、2 种苯乙基酯（6-7）、1 种法卡林二醇（8）和 1 种倍半萜（9）。化合物 5 是一种新的代谢物，而 9 则是首次从羌活属中分离得到。所纯化的化合物（1-9）首先被报道具有抗苹果果实病原菌炭疽菌和大茎点霉的活性，其 MIC 值范围为 8 至 250mg/L，特别是 8 的 MIC 值分别为 16 和 8mg/L。此外，8 可以抑制大茎点霉孢子的萌发和新的产孢，以及增强大茎点霉孢子的膜通透性。这是首次对羌活抗苹果果实病原菌的成分进行研究，具有很大的开发为生物杀菌剂的潜力。
