The invasion ofSpodoptera frugiperdahas imposed a serious impact on global food security. Matrine is a botanical pesticide with a broad spectrum of insecticidal activity which was recommended for controllingSpodoptera frugiperda. In order to discover effective insecticide forSpodoptera frugiperda, two matrine derivatives modified with carbon disulfide and nitrogen-containing groups were systhesized. And their inhibition activities onSf9cell were evaluated. The structural configuration of compounds were characterized by IR, HPLC, MS, NMR and XRD, with yields of 52% and 65%, respectively. The IC₅₀of the two newly synthesized compounds onSf9cell reduced to 0.648 mmol/L and 1.13 mmol/L, respectively, compared with that of matrine (5.330 mmol/L). In addition, microscopic observation ofSf9cell treated with the compounds showed that the number of adherent cells decreased, the cells shrunk, vacuolated and apoptotic bodies appeared. The two newly synthesized compounds exhibited better inhibitory effect onSf9cell than that of the parent matrine, suggesting that the positive effect of the introduction of 1-pyrrolidinecarbodithioate and diethylcarbamodithioate groups to matrine. The morphological observation ofSf9cell induced by derivatives indicated that apoptosis induction may be a mechanism that inhibits insect cell proliferation and exerts insecticidal effect.

Matrine is a traditional botanical pesticide with a broad-spectrum biological activity that is widely applied in agriculture. Halopyrazole groups are successfully introduced to the C13 of matrine to synthesize eight new derivatives with a yield of 78–87%. The insecticidal activity results show that the introduction of halopyrazole groups can significantly improve the insecticidal activity of matrine on Plutella xylostella, Mythimna separata and Spodoptera frugiperda with a corrected mortality rate of 100%, which is 25–65% higher than matrine. The fungicidal activity results indicate that derivatives have a high inhibitory effect on Ceratobasidium cornigerum, Cibberella sanbinetti, Gibberrlla zeae and Collectot tichum gloeosporioides. Thereinto, 4-Cl-Pyr-Mat has the best result, with an inhibition rate of 23–33% higher than that of matrine. Therefore, the introduction of halogenated pyrazole groups can improve the agricultural activity of matrine.

Many studies on intracellular calcium ([Ca²⁺]_i) and intracellular pH (pH_i) have been carried out due to their importance in regulation of different cellular functions. However, most of the previous studies are focused on human or mammalian cells. The purpose of the present study was to characterize the effect of Rhodojaponin-III (R-III) on [Ca²⁺]_i and pH_i and the proliferation of Sf9 cells. R-III strongly inhibited Sf9 cells proliferation with a time- and dose-dependent manner. Flow cytometry established that R-III interfered with Sf9 cells division and arrested them in G2/M. By using confocal scanning technique, effects of R-III on intracellular free calcium ([Ca²⁺]_i) and intracellular pH (pH_i) in Sf9 cells were determined. R-III induced a significant dose-dependent (1, 10, 100, 200 μg/mL) increase in [Ca²⁺]_i and pH_i of Sf9 cells in presence of Ca²⁺-containing solution (Hanks) and an irreversible decrease in the absence of extra cellular Ca²⁺. We also found that both extra cellular Ca²⁺ and intracellular Ca²⁺ stores contributed to the increase of [Ca²⁺]_i, because completely treating Sf9 cells with CdCl₂ (5 mM), a Ca²⁺ channels blocker, R-III (100 μg/mL) induced a transient elevation of [Ca²⁺]_i in case of cells either in presence of Ca²⁺ containing or Ca²⁺ free solution. In these conditions, pH_i showed similar changes with that of [Ca²⁺]_i on the whole. Accordingly, we supposed that there was a certain linkage for change of [Ca²⁺]_i, cell cycle arrest, proliferation inhibition in Sf9 cells induced by R-III.