Leveraging botanical resources for crop protection: the isolation, bioactivity and structure-activity relationships of lycoris alkaloids

Background: Lycoris aurea (L' Herit.) Herb (Amaryllidaceae) is a native pesticide in China. The ethanolic extract of Lycoris aureate bulbs, the total alkaloids of L. aurea bulbs and the main alkaloids of L. aurea bulbs were systematically investigated as part of a novel project to study their antiviral, fungicidal (phytopathogenic) and insecticidal activities. We also prepared 18 lycorine derivatives and evaluated their bioactivities.

Results: Lycorine had excellent larvicidal activity against Plutella xylostella (LC₅₀ = 10.6 mg L^-1 ) and was also effective during a field trial. It also showed good inhibitory activity against tobacco mosaic virus (TMV) and good fungicidal activity against Phytophthora capsici (EC₅₀ = 7.76 mg L^-1 ). Compounds 13 and 15 exhibited good anti-TMV activity, excellent fungicidal activity against Rhizoctonia cerealis (EC₅₀ = 6.78 mg L^-1 ) and excellent larvicidal activity against Culex pipiens pallens (LC₅₀ at 0.1-0.25 mg L^-1 ).

Conclusion: Lycorine was identified as the main active component of L. aurea bulbs and showed potential for field application against P. xylostella. The activities of compounds 13 and 15 make them excellent candidates for new lead compounds in novel pesticide research. This study provides the basis for developing these alkaloids into potential agrochemicals. © 2018 Society of Chemical Industry.