Molecular analysis of the mode of action of RH-5992, a lepidopteran-specific, non-steroidal ecdysteroid agonist

Retnakaran, Arthur; Hiruma, Kiyoshi; Palli, Subba Reddy; Riddiford, Lynn M.

doi:10.1016/0965-1748(94)00037-i

Cited by 106 publications

(77 citation statements)

References 23 publications

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“…The mechanism by which RH-2485 cause the arrest of oocyte maturation is not fully known, it is presumed that the longer persistence of the mimic would have caused the arrest, by sustaining the receptor-complex. This may be analogous to what was explained by Retnakaran et al (1995Retnakaran et al ( , 1997 for lethal moulting in C. fumiferana and homologus to the observation made by Swevers & Iatrou (1999) on oogenesis and choriogenis arrest in B. mori by RH-5992.…”

mentioning

confidence: 82%

“…Continuous building up of this compound in the haemolymph and the persistence of tebufenozide in the body of the treated larva prevented successful shedding of the cuticle in S. exempta and S. exigua and (Smagghe & Degheele, 1994). Retnakaran et al (1995) had reported the persistence of tebufenozide in the body tissues of C. fumiferana which permitted the expression of cuticular protein genes (LCP14) that were upregulated by the presence of 20E, but did not permit the expression of those genes that were turned on in the absence of the hormone. Similarly, Carlson et al (2001) suggested that the longer persistence/slow removal of RH-2485 resulted in death of the larvae due to failure in moulting process.…”

Section: Discussionmentioning

confidence: 99%

“…Structure of non-steroidal ecdysteroid agonists (Retnakaran et al 1995) Formula 2. Structure of 20-hydroxyecdysone the computation of median lethal dose.…”

Section: Experimental Animal: Bombyx Morimentioning

confidence: 99%

“…The longer persistence of methoxyfenozide also prevented the expression of down regulated genes by 20E. Retnakaran et al (1995) have reported that the persistence of tebufenozide in the body tissues of C. fumiferana permitted the expression of cuticular protein genes (LCP14) that were upregulated by the presence of 20E, but did not permit the expression of those genes that were turned on in the absence of this hormone. Carlson et al (2001) suggested that the longer persistence/slow removal of RH-2485 resulted in disruption of moulting process leading to the death of the larvae.…”

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confidence: 99%

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Effect of RH-2485 on development, metamorphosis and synthesis of major proteins in female silkworm Bombyx mori

2010

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Toxicological data on silkworm Bombyx mori are quite comparable to those of other lepidopteran pest insects, therefore, it is considered as a suitable model for exploring effects of any new synthetic formulations. In this study, female V instar larvae of silk moth B. mori were chosen to evaluate the lethal and sublethal toxicity effects of RH-2485 (methoxyfenozide), a non-steroidal ecdysteroid agonist and to substantiate the ecdysteroid mimicking action of RH-2485 on ovary development, vitellogenin incorporation and egg production in isolated pupal abdomen (IPA). Probit analysis was carried out to find the median lethal dose (LD50) from 96 h cumulative mortality percent. Protein profile of haemolymph, fat body, ovary and eggs were separated in SDS-PAGE. Western blot analysis was carried out to confirm vitellogenin in the ovary. Sublethal effects on feeding, cocoon spinning, pupation, adult emergence and egg production were studied at doses of 1/5 th , 1/10 th and 1/20 th of LD50. Significant changes were observed in all these parameters at all three sublethal doses. The morphological effects were related to underlying biochemical changes by finding the changes in haemolymph, fat body, ovary and egg protein profile. Marked changes were observed in storage proteins (80 kDa) and 30 kDa proteins in the haemolymph at all three sublethal doses. The larvae that escaped the sublethal effects at a dose of 1/20 of LD50 and emerged as adults with malformed wings produced significantly lower number of eggs. The isolated pupal abdomen (IPA) treated with RH-2485 did not metamorphose into adult but the oocyte development and vitellogenesis were normal but the egg precursor processing was incomplete leading to failure in choriogenesis.

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mentioning

confidence: 82%

Section: Discussionmentioning

confidence: 99%

“…Structure of non-steroidal ecdysteroid agonists (Retnakaran et al 1995) Formula 2. Structure of 20-hydroxyecdysone the computation of median lethal dose.…”

Section: Experimental Animal: Bombyx Morimentioning

confidence: 99%

mentioning

confidence: 99%

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Effect of RH-2485 on development, metamorphosis and synthesis of major proteins in female silkworm Bombyx mori

2010

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“…Lack of lamellated procuticle in treated larvae agrees with the current electromicroscopic observations in L. decemlineata integument and those of Binnington & Retnakaran (i 991) in caterpillars of the spruce budworm, Choristoneurafumiferana Clemens. Retnakaran et al (1995) also demonstrated that RH-5849 and tebufenozide suppressed the expression of genes for endocuticular proteins and for DOPA-decarboxylase, which is required for sclerotization. It is striking that they observed a similar inhibition in the presence of high doses of 20E.…”

Section: Discussionmentioning

confidence: 99%

Nonsteroidal moulting hormone agonists: effects on protein synthesis and cuticle formation in Colorado potato beetle larvae

Smagghe¹,

Viñuela

Limbergen³

et al. 1999

Entomologia Exp Applicata

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Larvae of the Colorado potato beetle, Leptinotarsa decemlineata (Say), that were orally treated with RH-0345 a 0.1 mg r 1 , RH-5849 at 10 and 50 mg l _l , tebufenozide at 2 g I -1 , and 20-hydroxyecdysone at 2 g l -1 , showec symptoms of premature moulting, followed by inhibition of ecdysis. In addition, fresh weight gain and total proteir content were blocked. The effects on haemolymphal and cuticular polypeptides after PAGE were linked with premature, new epicuticle deposition as was observed under the electron microscope. These observations suppor the concept that the ecdysteroid-mimicking action of the three nonsteroidal molecules is specific.

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Deposition of aerially applied tebufenozide (RH5992) on balsam fir (Abies balsamea) and its control of spruce budworm (Choristoneura fumiferana[Clem.])

et al. 1998

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: A Ðeld trial was conducted in 1994 to determine the foliar deposit of tebufenozide (RH5992), applied aerially, and its efficacy against spruce budworm, Choristoneura fumiferana (Clem.). A commercial 240 g litre~1 formulation of the insecticide (Mimic 240LV) was mixed with water, dyed with a tracer dye (Rhodamine WT) and sprayed with a light Ðxed-wing aircraft. Six application strategies were tested. Five used 70 g AI ha~1 in a spray volume of 1 or 2 litre~1 ha~1 with single or double applications ; the sixth was an unsprayed control.Results show that the spectra of the spray applications were, with one exception, fairly uniform. Volume and number median diameters ranged from 100 to 130 km and 27 to 72 km, respectively. Mean number of drops cm~2 on Kromekote cards were \2É0 for strategies where either 1 or 2 litre ha~1 were sprayed. Nevertheless no one strategy produced droplet densities that were signiÐcantly di †erent (P \ 0É05) from the other strategies. Tebufenozide recovered from foliage averaged 2É5 to 5É9 kg g foliage~1 when 1 litre ha~1 was sprayed and 5É8 to 6É8 kg g foliage~1 after 2 litre ha~1 were sprayed. When a single application was the strategy used, the mean number of droplets cm~2 and kg tebufenozide g foliage~1 ranged from 1É2 to 1É4 and 2É5 to 5É9, respectively. With double applications, the same response parameters ranged from 0É3 to 1É9 and 2É5 to 6É8, respectively. Budworm population reductions (%) and the number of larvae that survived tebufenozide treatments were signiÐcantly di †erent (P \ 0É05) from the controls. After strategies that used 1 litre spray ha~1, mean percentage population reductions ranged from 61É4 to 93É6 whereas populations were reduced by 85É6 to 98É3% when 2 litre ha~1 were sprayed. After double applications the mean percentage population reductions ranged from 93É6 to 98É3, but single application strategies resulted in mean reductions of 61 to 86%. Mean population reductions in the controls were 61%. The mean number of larvae per branch that survived spray strategies of 1 litre ha~1 ranged from 1É3 to 7É4, and from 0É4 to 1É3 when 2 litre ha~1 was the spray volume. In the controls an average of 10É2 larvae survived. With one exception, mean percentage defoliation in the treated areas was also signiÐcantly less (P \ 0É05) than that in the control. Mean defoliation in trees sprayed at 1 litre spray ha~1 ranged from 40 to 62É8% whereas those treated at 2 litre ha~1 had mean defoliation levels from 31É5 to 62É8%. In contrast, average defoliation in the controls was 92É1%. When a single application was the spray strategy, mean defoliation ranged from 31É5 to 62É8%. These data imply that a double application of tebufenozide at 70 g in 2 litre ha~1 was the most efficacious strategy. However, analyses of the data also show that the primary inÑuence on deposits and defoliation was interactions between number of applications and spray. Nevertheless the two independent variables acted without signiÐcant interactions when inÑuencing percentage reductions of spruce budw...

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Molecular analysis of the mode of action of RH-5992, a lepidopteran-specific, non-steroidal ecdysteroid agonist

Cited by 106 publications

References 23 publications

Effect of RH-2485 on development, metamorphosis and synthesis of major proteins in female silkworm Bombyx mori

Effect of RH-2485 on development, metamorphosis and synthesis of major proteins in female silkworm Bombyx mori

Nonsteroidal moulting hormone agonists: effects on protein synthesis and cuticle formation in Colorado potato beetle larvae

Deposition of aerially applied tebufenozide (RH5992) on balsam fir (Abies balsamea) and its control of spruce budworm (Choristoneura fumiferana[Clem.])

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