Abstract
Based on the broad-spectrum biological activities of echinopsine and acylhydrazones, a series of echinopsine derivatives containing acylhydrazone moieties have been designed, synthesized and their biological activities were evaluated for the first time. The bioassay results indicated that most of the compounds showed moderate to good antiviral activities against tobacco mosaic virus (TMV), among which echinopsine (I) (inactivation activity, 49.5 ± 4.4%; curative activity, 46.1 ± 1.5%; protection activity, 42.6 ± 2.3%) and its derivatives 1 (inactivation activity, 44.9 ± 4.6%; curative activity, 39.8 ± 2.6%; protection activity, 47.3 ± 4.3%), 3 (inactivation activity, 47.9 ± 0.9%; curative activity, 43.7 ± 3.1%; protection activity, 44.6 ± 3.3%), 7 (inactivation activity, 46.2 ± 1.6%; curative activity, 45.0 ± 3.7%; protection activity, 41.7 ± 0.9%) showed higher anti-TMV activity in vivo at 500 mg/L than commercial ribavirin (inactivation activity, 38.9 ± 1.4%; curative activity, 39.2 ± 1.8%; protection activity, 36.4 ± 3.4%). Some compounds exhibited insecticidal activities against Plutella xylostella, Mythimna separate and Spodoptera frugiperda. Especially, compounds 7 and 27 displayed excellent insecticidal activities against Plutella xylostell (mortality 67 ± 6% and 53 ± 6%) even at 0.1 mg/L. Additionally, most echinopsine derivatives exhibited high fungicidal activities against Physalospora piricola and Sclerotinia sclerotiorum.
Highlights
Plant virus diseases can be caused by more than 900 viruses, which reduce grain production and lead to huge economic losses all over the world1–3
Song et al reported that the EC50 value of purine nucleoside derivative for the inactivating activity against tobacco mosaic virus (TMV) was 48 mg/L, which was better than that of ningnanmycin (88 mg/L)11
The anti-TMV activity of echinopsine was investigated by our group and the result shows that the inactivation, curative and protection activities of echinopsine (49.5 ± 4.4%, 46.1 ± 1.5% and 42.6 ± 2.3% at 500 mg/L, in Table 1) were higher than that of ribavirin (38.9 ± 1.4%, 39.2 ± 1.8%, 36.4 ± 3.4%, at 500 mg/L)
Summary
Plant virus diseases can be caused by more than 900 viruses, which reduce grain production and lead to huge economic losses all over the world1–3. The anti-TMV activity of echinopsine was investigated by our group and the result shows that the inactivation, curative and protection activities of echinopsine (49.5 ± 4.4%, 46.1 ± 1.5% and 42.6 ± 2.3% at 500 mg/L, in Table 1) were higher than that of ribavirin (38.9 ± 1.4%, 39.2 ± 1.8%, 36.4 ± 3.4%, at 500 mg/L).
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