Comparative effects of a non-steroidal ecdysone agonist RH-5992 and 20-hydroxyecdysone in a lepidopteran cell line (IAL-PID2).
The non-steroidal ecdysone agonist, RH-5992, exhibits ecdysteroid activities in vivo as well as in vitro more effectively than 20-hydroxyecdysone (20E). Using the IAL-PID2 cells derived from imaginal wing discs of last larval instar of Plodia interpunctella, we investigated the action of RH-5992 in the control of cell growth. Its effects on the proliferative activity of IAL-PID2 cells, the induction level in G2/M arrest and on the expression rate of Plodia B cyclin (PcycB), ecdysone B1-isoform (PIEcR-B1) and Ultraspiracle-2 isoform (PIUSP-2) were examined. From these cellular and molecular assays, our results brought evidence that RH-5992, like 20E, induced an inhibition on cell proliferation by blocking IAL-PID2 cells in G2/M phase. Moreover, this G2/M arrest was preceded by a decrease in the expression level of PcycB and a high induction of PIEcR-B1, PIUSP-2 mRNAs. Dose-response experiments revealed that RH-5992 was even more potent than 20E. On these parameters, we therefore suggest that the differential observed in the expression level of USP and EcR by RH-5992 and 20E could contribute to the difference observed for the biological potency of these two compounds.
Auzoux-Bordenave
Stéphanie
S
UMR 1272 Physiologie de l'insecte: Signalisation et Communication, Université Pierre et Marie Curie, 12 rue Cuvier, 75005 Paris, France.
Solvar
Marthe
M
Queguiner
Isabelle
I
Bozzolan
Françoise
F
Mottier
Violaine
V
Siaussat
David
D
Porcheron
Patrick
P
Debernard
Stéphane
S
D000818:Animals; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004441:Ecdysterone / Q000494:pharmacology*; D015870:Gene Expression / Q000187:drug effects; D006834:Hydrazines / Q000494:pharmacology*; D019476:Insect Proteins / Q000378:metabolism; D007306:Insecticides / Q000494:pharmacology*; D007915:Lepidoptera / Q000166:cytology* / Q000378:metabolism
D006834:Hydrazines; D019476:Insect Proteins; D007306:Insecticides; D004441:Ecdysterone; C082026:tebufenozide