Studies On Bioactivities And Chemical Constituents Of The Aerial Part Of Derris Elliptica

Botanical pesticides have drawn many people’s attention owing to its advantages of lower virulence, lower deposition and non-environmental pollutions. It was intended to find the active ingredients and discovery the lead compounds according to the systematic isolation of the aerial part of Derris elliptica and the corresponding bioassays on insecticidal, fungicidal and cytotoxic activities, which might provide theoretical basis for the development of new pesticides and the utilization of this plant.The PE-soluble and EtOAc-soluble fraction of90%ethanol extract of seeds of the aerial part of Derris elliptica exhibited potent contact activity against Aedes albopictus Skuse、Musca domestica Linaeus and Pomacea canaliculata. The two fractions were therefore applied separation using column chromatography (CC) over silica gel、Sephadex LH-20、MCI and TLC. A new compound,6,4’-dihydroxy-7,5’-dimethoxy-coumaronochromone (1), together with seventeen known ones,7,4’-dihydroxy-5’-methoxy-coumaronochromone (2),7-hydroxy-4’,5’-methylenedioxy-pterocarpan (3),3-hydroxy-8,9-methylenedioxypterocarp-6a-ene (4), flemichapparin-B (5), genistein (6), prunetin (7), formononetin (8), apigenin (9), luteolin (10), apigenin7-O-β-D-glucoside (11),5’R-6a,12a-dehydrorotenone (12),(22E,24R)-ergosta--5,7,22--trien-3β-ol (13), stigmast-4-en-3,6-dione (14), β-daucosterol (15),(23Z)-Cycloart-23-en-3/3,25-diol(16), Betulinic acid(17),3-hydroxy-4-methoxybenzoic acid(18) were isolated from the PE-soluble and EtOAc-soluble fraction. Their structures were elucidated on the basis of spectroscopic (IR, UV, EIMS, ESIMS,1D NMR and2D NMR).The preliminary assays of twelve isolated flavonoids compounds indicated that compounds3-hydroxy-8,9-methylenedioxypterocarp-6a-ene, formononetin and apigenin were active against larvae of A. albopictus, with corrected mortalities of96.67%,90.00%and93.33%, respectively, for24h after treatment, and all were100%for48h after treatment. On the same conditions after treatment for48h,7,4’-dihydroxy-5’-methoxy-coumaronochromone and prunetin the corrected mortalities also of93.33%�'�83.33%, respectively. The larvacidal activities of these five compounds were re-performed at different concentrations in order to determine LC50of them against larvae of A. albopictus.7,4’-dihydroxy-5’-methoxy-coumaronochromone showed the most potent activity with LC50value of5.85mg/L and3-hydroxy-8,9-methylenedioxypterocarp-6a-ene with LC50value of8.69mg/L.The cytotoxic activities of all compounds against SL and Hi-5cell lines were showed that flemichapparin-B showed highly cytotoxic activity against SL and Hi-5cell lines with inhibition rates of92.1%and82.7%at a concentration of20mg/L, compared to rotenone as a positive control (20.83%and21.53%, respectively). flemichapparin-B also showed highly cytotoxic activity against SL (81.10%) and Hi-5(86.96%) cell lines.In conclusion, some compounds from the aerial part of Derris elliptica by using the activity-guided fractionation. The present study obtained these compounds possessing obvious bioactivities, and therefore is significant to discovery of new pesticides.All of the above mentioned information suggested that the aerial part of this plant might be used as a source of insecticides, which are the potential inhibitors of SL and Hi-5cell lines. However, until now, the underground part of D. elliptica was used to preparation of insecticides in China and the aerial part was considered for useless and thrown away. And the study also provided a scientific basis for utilization of Derris elliptica in development of botanical pesticides.