In Vitro Antifungal Activity of Sanguinarine and Chelerythrine Derivatives against Phytopathogenic Fungi

Molecules

Xin-Juan Yang¹  Fang Miao²  Yao Yao¹  Fang-Jun Cao¹  Rui Yang¹  Yan-Ni Ma¹  Bao-Fu Qin² 

[1] College of Science, Northwest A&F University, Yangling 712100, Shaanxi, China;College of Life Science, Northwest A&F University, Yangling 712100, Shaanxi, China;

关键词: sanguinarine;    chelerythrine;    quaternary benzo[c]phenanthridine alkaloids;    antifungal activity;    phytopathogenic fungi;   

DOI  :  10.3390/molecules171113026

来源: mdpi

【 摘 要 】

In order to understand the antifungal activity of some derivatives of sanguinarine (S) and chelerythrine (C) and their structure-activity relationships, sixteen derivatives of S and C were prepared and evaluated for in vitro antifungal activity against seven phytopathogenic fungi by the mycelial growth rate method. The results showed that S, C and their 6-alkoxy dihydro derivatives S₁–S₄, C₁–C₄ and 6-cyanodihydro derivatives S₅, C₅ showed significant antifungal activity at 100 µg/mL against all the tested fungi. For most tested fungi, the median effective concentrations of S, S₁, C and C₁ were in a range of 14–50 µg/mL. The structure-activity relationship showed that the C=N⁺ moiety was the determinant for the antifungal activity of S and C. S₁–S₅ and C₁–C₅ could be considered as the precursors of S and C, respectively. Thus, the present results strongly suggested that S and C or their derivatives S₁–S₅ and C₁–C₅ should be considered as good lead compounds or model molecules to develop new anti-phytopathogenic fungal agents.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.