Knockdown of Uridine Diphosphate Glucosyltransferase 86Dg Enhances Susceptibility of Tribolium castaneum (Coleoptera: Tenebrionidae) to Artemisia vulgaris (Asterales: Asteraceae) Essential Oil.

Uridine diphosphate glucosyltransferases (UGTs), which are phase II detoxification enzymes, are found in various organisms. These enzymes play an important role in the detoxification mechanisms of plant allelopathy and in insects. Artemisia vulgaris L. (Asterales: Asteraceae: Artemisia) essential oil has strong contact toxicity to Tribolium castaneum Herbst (Coleoptera: Tenebrionidae) larvae. However, the effect of A. vulgaris essential oil on UGTs is unclear. In this study, A. vulgaris essential oil was shown to significantly induce the expression of the TcUgt86Dg transcript. Furthermore, treatment of TcUgt86Dg-silenced individuals with A. vulgaris essential oil resulted in higher mortality than for the control individuals, indicating that TcUgt86Dg is involved in detoxification of A. vulgaris essential oil in T. castaneum. The developmental expression profile showed that the expression of TcUgt86Dg in late adults was higher than in other developmental stages. Furthermore, the expression profile in adult tissues revealed higher expression of TcUgt86Dg in the head, antenna, fat body, and accessory gland than in other tissues. These data show that TcUgt86Dg may be involved in the metabolism of exogenous toxins by T. castaneum; thus, our results have elucidated one possible mechanism of resistance to A. vulgaris essential oil and provide a theoretical basis for a control scheme for T. castaneum.

Odorant Binding Protein C17 Contributes to the Response to Artemisia vulgaris Oil in Tribolium castaneum.

The red flour beetle, Tribolium castaneum (T. castaneum), generates great financial losses to the grain storage and food processing industries. Previous studies have shown that essential oil (EO) from Artemisia vulgaris (A. vulgaris) has strong contact toxicity to larvae of the beetle, and odorant-binding proteins (OBPs) contribute to the defense of larvae against A. vulgaris. However, the functions of OBPs in insects defending against plant oil is still not clear. Here, expression of one OBP gene, TcOBPC17, was significantly induced 12-72 h after EO exposure. Furthermore, compared to the control group, RNA interference (RNAi) against TcOBPC17 resulted in a higher mortality rate after EO treatment, which suggests that TcOBPC17 involves in the defense against EO and induces a declining sensitivity to EO. In addition, the tissue expression profile analysis revealed that the expression of TcOBPC17 was more abundant in the metabolic detoxification organs of the head, fat body, epidermis, and hemolymph than in other larval tissue. The expression profile of developmental stages showed that TcOBPC17 had a higher level in early and late adult stages than in other developmental stages. Taken together, these results suggest that TcOBPC17 could participate in the sequestration process of exogenous toxicants in T. castaneum larvae.

Synthesis and potential anticonvulsant activity of new N-3-substituted 5,5-cyclopropanespirohydantoins.

Thirteen new 5-cyclopropanespirohydantoins with various N-3 substituents were synthesized and their pharmacological activity was determined with the objective to better understand their structure-activity relationship (SAR) for anticonvulsant activity. The anticonvulsant effects of these compounds were evaluated by maximal electroshock seizure (MES) test and subcutaneous pentylenetetrazole (scPTZ) test models in mice. All compounds substituted with cyclopropyl group at fifth position of hydantoin ring showed better protection against MES test. Compounds 5b, 5d, 5e, 5g and 5j were found to be the most potent compounds of this series and compared with the reference drug phenytoin sodium in MES test. Compound 5j also showed equipotent activity with the standard drug sodium valproate at the doses of 20 and 40 mg kg(-1) in scPTZ test.