天然单萜吲哚生物碱作为强效杀菌剂的评价

IF 1.7 4区 化学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Zhuoyi Wang, Yanyan Chen, Hean Liu, Yueming Li, Mingjie Zhang, Yongyong Zhang, Junwei Sun
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引用次数: 0

摘要

目的:对86种植物源单萜吲哚生物碱(MIAs)的抑菌活性进行评价,以鉴定具有抑菌潜力的新型先导化合物。方法:采用体外和体内抗真菌试验对所选的MIAs进行抑菌效果评价。结果与讨论:在初步筛选的化合物中,rhazinilam(32)和rhazinal(33)对黑曲霉的抗真菌活性明显强于酮康唑。进一步的菌丝生长抑制实验证实,这两种化合物在体外对黑曲霉、白僵菌和玉米尖孢菌的抑制作用明显高于酮康唑。rhazinilam(32)的IC50值分别为5、10和17.89 μg/mL;对拉莫那(33),其值分别为<; 2.5、< 5、< 5 μg/mL。此外,在黄瓜叶片的体内实验表明,在浓度为40 μg/mL时,化合物(32)和(33)对黑曲霉的保护效果显著,分别为77.27%和100%,而酮康唑的保护效果为47.62%。结论:Rhazinilam(32)和rhazinal(33)在体外和体内实验中都显示出强大的抗真菌活性,这表明它们有望成为开发新型杀菌剂的主要候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Evaluation of Natural Monoterpene Indole Alkaloids as Potent Fungicide Candidates

Evaluation of Natural Monoterpene Indole Alkaloids as Potent Fungicide Candidates

Objective: The fungicidal activity of 86 monoterpene indole alkaloids (MIAs) derived from plants was evaluated to identify novel lead compounds with antifungal potential. Methods: In this study, both in vitro and in vivo antifungal assays were performed to assess the efficacy of the selected MIAs. Results and Discussion: Among the tested compounds, rhazinilam (32) and rhazinal (33) exhibited markedly stronger antifungal activity against Aspergillus niger than ketoconazole in preliminary screenings. Further evaluation using mycelial growth inhibition assays confirmed that both compounds were significantly more active than ketoconazole against A. niger, B. dothidea, and F. oxysporum f. sp. cubense in vitro. The IC50 values for rhazinilam (32) were < 5, < 10, and 17.89 μg/mL, respectively; for rhazinal (33), the values were < 2.5, < 5, and < 5 μg/mL, respectively. Moreover, in vivo tests on cucumber leaves demonstrated that at a concentration of 40 μg/mL, compounds (32) and (33) provided significant protection against A. niger, with protection rates of 77.27 and 100%, respectively, compared to 47.62% for ketoconazole. Conclusions: Rhazinilam (32) and rhazinal (33) demonstrated potent antifungal activity in both in vitro and in vivo experiments, highlighting their promise as lead candidates for the development of novel fungicidal agents.

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来源期刊
Russian Journal of Bioorganic Chemistry
Russian Journal of Bioorganic Chemistry 生物-生化与分子生物学
CiteScore
1.80
自引率
10.00%
发文量
118
审稿时长
3 months
期刊介绍: Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.
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