Design, Synthesis, and Antifungal Evaluation of Cryptolepine Derivatives against Phytopathogenic Fungi
Design, Synthesis, and Antifungal Evaluation of Cryptolepine Derivatives against Phytopathogenic Fungi
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隐磷脂衍生物的设计、合成和抗植物病原真菌的抗真菌评价
DOI：
10.1021/acs.jafc.0c06480
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发表时间：
2021-01-26
影响因子：
6.1
通讯作者：
Tang, Chen
中科院分区：
文献类型：
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作者：
Chen, Yong-Jia;Liu, Hua;Tang, Chen
受天然衍生物广泛抗植物病原应用的启发，设计、合成并评价了Cryptolepine及其衍生物对4种重要的农业真菌Rhizoctonia solani、Botrytis cinerea、Fusarium graminearum和Sclerotinia sclerotiorum的抗真菌活性。体外杀菌试验结果表明，化合物a1-a24对B具有较好的杀菌活性。其中α 3的抑制活性最强，EC_（50）为0.027 μ g/mL。为了进一步扩大cryptolepine的抗真菌谱，开环化合物f1对R. solani，EC_（50）为5.599 μ g/mL。禾谷早熟禾此外，还对a3的抗B作用机制进行了初步研究。结果表明，该菌株不仅孢子萌发受到有效抑制，菌丝正常生理结构受到严重破坏，而且有害活性氧明显积累，细胞核的正常功能受到严重破坏。此外，还进行了抗B. Cinerea发现A3的治疗作用与阳性对照嘧菌酯相当。这些结果表明，化合物a3是一种很有前途的新型抗B药物。cinerea其宝贵的潜力。
Inspired by the widely antiphytopathogenic application of diversified derivatives from natural sources, cryptolepine and its derivatives were subsequently designed, synthesized, and evaluated for their antifungal activities against four agriculturally important fungi Rhizoctonia solani, Botrytis cinerea, Fusarium graminearum, and Sclerotinia sclerotiorum. The results obtained from in vitro assay indicated that compounds a1-a24 showed great fungicidal property against B. cinerea (EC50 < 4 mu g/mL); especially, a3 presented significantly prominent inhibitory activity with an EC50 of 0.027 mu g/mL. In the pursuit of further expanding the antifungal spectrum of cryptolepine, ring-opened compound f1 produced better activity with an EC50 of 3.632 mu g/mL against R. solani and an EC50 of 5.599 mu g/mL against F. graminearum. Furthermore, a3 was selected to be a candidate to investigate its preliminary antifungal mechanism to B. cinerea, revealing that not only spore germination was effectively inhibited and the normal physiological structure of mycelium was severely undermined but also detrimental reactive oxygen was obviously accumulated and the normal function of the nucleus was fairly disordered. Besides, in vivo curative experiment against B. cinerea found that the therapeutic action of a3 was comparable to that of the positive control azoxystrobin. These results suggested that compound a3 could be regarded as a novel and promising agent against B. cinerea for its valuable potency.