Basis for selective action of a synthetic molting hormone agonist, RH- 5992 on lepidopteran insects

M. Sundaram; S. R. Palli; P. J. Krell; S. S. Sohi; T. S. Dhadialla; A. Retnakaran

doi:10.1016/S0965-1748(98)00035-6

Basis for selective action of a synthetic molting hormone agonist, RH- 5992 on lepidopteran insects

M. Sundaram, S. R. Palli, P. J. Krell, S. S. Sohi, T. S. Dhadialla, A. Retnakaran

Research output: Contribution to journal › Article › peer-review

42 Scopus citations

Abstract

The non-steroidal ecdysone agonist, RH-5992, induces a precocious incomplete molt in lepidopteran insects but is refractory to insects of other orders. We used two lepidopteran cell lines, FPMI-CF-203 (CF-203) and IPRI- MD-66 (MD-66) and two dipteran cell lines, DM-2 and K(c), to investigate the lepidopteran specificity of RH-5992. The mRNAs for hormone receptor 3 homologues cloned from Drosophila (DHR3) and Choristoneura (CHR3) are directly induced by 20-hydroxyecdysone (20E)and serve as suitable markers for studying ecdysone action. Dose response experiments showed that 10^-7 M 20E induced CHR3 mRNA in CF-203 cells and DHR3 mRNA in DM-2 cells. Concentrations of RH-5992 as low as 10^-10 M induced CHR3 mRNA in CF-203 cells, whereas concentrations as high as 10^-0 M induced only very low levels of DHR3 mRNA in DM-2 cells. Studies using ¹⁴C- RH-5992 revealed that lepidopteran cell lines (CF-203 and MD-66) retained more of this compound within the cells than the dipteran cell lines (DM2 and K(c)). The clearance of RH-5992 from DM-2 cells was temperature dependent and was blocked by 10^-5 M ouabain, an inhibitor of Na⁺, K⁺-ATPase suggesting that the efflux was due to active transport.

Original language	English
Pages (from-to)	693-704
Number of pages	12
Journal	Insect Biochemistry and Molecular Biology
Volume	28
Issue number	9
DOIs	https://doi.org/10.1016/S0965-1748(98)00035-6
State	Published - Sep 1998

Bibliographical note

Funding Information:
This research was supported by a Canadian Forest Service/Natural Sciences and Engineering Research Council Research partnership program award CRD# 0192158, with Rohm and Haas Company. We thank Drs. M. Koelle and D. Hogness of Stanford University for the gift of Drosophila DHR3 cDNA clone.

Keywords

20-hydroxyecdysone
Choristoneura hormone receptor 3 (CHR3)
Drosophila hormone receptor 3 (DHR3)
Efflux
Influx
Ouabain
RH-5992

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Insect Science

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10.1016/S0965-1748(98)00035-6

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title = "Basis for selective action of a synthetic molting hormone agonist, RH- 5992 on lepidopteran insects",

abstract = "The non-steroidal ecdysone agonist, RH-5992, induces a precocious incomplete molt in lepidopteran insects but is refractory to insects of other orders. We used two lepidopteran cell lines, FPMI-CF-203 (CF-203) and IPRI- MD-66 (MD-66) and two dipteran cell lines, DM-2 and K(c), to investigate the lepidopteran specificity of RH-5992. The mRNAs for hormone receptor 3 homologues cloned from Drosophila (DHR3) and Choristoneura (CHR3) are directly induced by 20-hydroxyecdysone (20E)and serve as suitable markers for studying ecdysone action. Dose response experiments showed that 10-7 M 20E induced CHR3 mRNA in CF-203 cells and DHR3 mRNA in DM-2 cells. Concentrations of RH-5992 as low as 10-10 M induced CHR3 mRNA in CF-203 cells, whereas concentrations as high as 10-0 M induced only very low levels of DHR3 mRNA in DM-2 cells. Studies using 14C- RH-5992 revealed that lepidopteran cell lines (CF-203 and MD-66) retained more of this compound within the cells than the dipteran cell lines (DM2 and K(c)). The clearance of RH-5992 from DM-2 cells was temperature dependent and was blocked by 10-5 M ouabain, an inhibitor of Na+, K+-ATPase suggesting that the efflux was due to active transport.",

keywords = "20-hydroxyecdysone, Choristoneura hormone receptor 3 (CHR3), Drosophila hormone receptor 3 (DHR3), Efflux, Influx, Ouabain, RH-5992",

author = "M. Sundaram and Palli, {S. R.} and Krell, {P. J.} and Sohi, {S. S.} and Dhadialla, {T. S.} and A. Retnakaran",

note = "Funding Information: This research was supported by a Canadian Forest Service/Natural Sciences and Engineering Research Council Research partnership program award CRD# 0192158, with Rohm and Haas Company. We thank Drs. M. Koelle and D. Hogness of Stanford University for the gift of Drosophila DHR3 cDNA clone. ",

year = "1998",

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doi = "10.1016/S0965-1748(98)00035-6",

language = "English",

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T1 - Basis for selective action of a synthetic molting hormone agonist, RH- 5992 on lepidopteran insects

AU - Sundaram, M.

AU - Palli, S. R.

AU - Krell, P. J.

AU - Sohi, S. S.

AU - Dhadialla, T. S.

AU - Retnakaran, A.

N1 - Funding Information: This research was supported by a Canadian Forest Service/Natural Sciences and Engineering Research Council Research partnership program award CRD# 0192158, with Rohm and Haas Company. We thank Drs. M. Koelle and D. Hogness of Stanford University for the gift of Drosophila DHR3 cDNA clone.

PY - 1998/9

Y1 - 1998/9

N2 - The non-steroidal ecdysone agonist, RH-5992, induces a precocious incomplete molt in lepidopteran insects but is refractory to insects of other orders. We used two lepidopteran cell lines, FPMI-CF-203 (CF-203) and IPRI- MD-66 (MD-66) and two dipteran cell lines, DM-2 and K(c), to investigate the lepidopteran specificity of RH-5992. The mRNAs for hormone receptor 3 homologues cloned from Drosophila (DHR3) and Choristoneura (CHR3) are directly induced by 20-hydroxyecdysone (20E)and serve as suitable markers for studying ecdysone action. Dose response experiments showed that 10-7 M 20E induced CHR3 mRNA in CF-203 cells and DHR3 mRNA in DM-2 cells. Concentrations of RH-5992 as low as 10-10 M induced CHR3 mRNA in CF-203 cells, whereas concentrations as high as 10-0 M induced only very low levels of DHR3 mRNA in DM-2 cells. Studies using 14C- RH-5992 revealed that lepidopteran cell lines (CF-203 and MD-66) retained more of this compound within the cells than the dipteran cell lines (DM2 and K(c)). The clearance of RH-5992 from DM-2 cells was temperature dependent and was blocked by 10-5 M ouabain, an inhibitor of Na+, K+-ATPase suggesting that the efflux was due to active transport.

AB - The non-steroidal ecdysone agonist, RH-5992, induces a precocious incomplete molt in lepidopteran insects but is refractory to insects of other orders. We used two lepidopteran cell lines, FPMI-CF-203 (CF-203) and IPRI- MD-66 (MD-66) and two dipteran cell lines, DM-2 and K(c), to investigate the lepidopteran specificity of RH-5992. The mRNAs for hormone receptor 3 homologues cloned from Drosophila (DHR3) and Choristoneura (CHR3) are directly induced by 20-hydroxyecdysone (20E)and serve as suitable markers for studying ecdysone action. Dose response experiments showed that 10-7 M 20E induced CHR3 mRNA in CF-203 cells and DHR3 mRNA in DM-2 cells. Concentrations of RH-5992 as low as 10-10 M induced CHR3 mRNA in CF-203 cells, whereas concentrations as high as 10-0 M induced only very low levels of DHR3 mRNA in DM-2 cells. Studies using 14C- RH-5992 revealed that lepidopteran cell lines (CF-203 and MD-66) retained more of this compound within the cells than the dipteran cell lines (DM2 and K(c)). The clearance of RH-5992 from DM-2 cells was temperature dependent and was blocked by 10-5 M ouabain, an inhibitor of Na+, K+-ATPase suggesting that the efflux was due to active transport.

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KW - Choristoneura hormone receptor 3 (CHR3)

KW - Drosophila hormone receptor 3 (DHR3)

KW - Efflux

KW - Influx

KW - Ouabain

KW - RH-5992

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AN - SCOPUS:0032168146

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JO - Insect Biochemistry and Molecular Biology

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IS - 9

ER -

Basis for selective action of a synthetic molting hormone agonist, RH- 5992 on lepidopteran insects

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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