Cited by 913Insect Pest Control StrategiesInsect Resistance and GeneticsInsect-Plant Interactions and Control

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NEW INSECTICIDES WITH ECDYSTEROIDAL AND JUVENILE HORMONE ACTIVITY

Dhadialla, Tarlochan S., Carlson, Glenn R., Le, Dat P.·1998·Annual Review of Entomology

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Abstract

Agrochemical research over the last two decades has resulted in the discovery of chemically novel insecticides that mimic the action of the two insect growth and developmental hormones, the steroidal 20-hydroxyecdysone (20E) and the sesquiterpenoid juvenile hormone (JH). Bisacylhydrazines are non-steroidal agonists of 20E and exhibit their insecticidal activity via interaction with the ecdysteroid receptor proteins. Interestingly, two of the bisacylhydrazine (tebufenozide and RH-2485) insecticides are very selectively toxic to lepidopteran pests. These insecticides are safe to beneficial insects and have a benign ecotoxicological profile. Aromatic non-terpenoidal insecticides (fenoxycarb and pyriproxyfen) mimic the action of JHs. However, like the JHs, their exact mode of action is not well understood. These insecticides are toxic to a broad spectrum of insects during their embryonic, last larval, or reproductive stages. The insecticidal, ecotoxicological properties and the mode of action of the two groups of insecticides are reviewed in this article.

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Impact of low lethal concentrations of buprofezin on biological traits and expression profile of chitin synthase 1 gene (CHS1) in melon aphid, Aphis gossypii
Ullah, F., Gul, H., Yousaf, H. K., Xiu, W., Qian, D., Gao, X., Tariq, K., Han, P., Desneux, N., & Song, D. (2019) · Scientific Reports · doi:10.1038/s41598-019-48199-w · Cited by 52
Biorational Pest Control – An Overview
Horowitz, A., Ellsworth, P. C., & Ishaaya, I. (2009) · Springer eBooks · doi:10.1007/978-90-481-2316-2_1 · Cited by 45
“(reviewed by Dhadialla et al. 1998 ) such as ecdysone agonists, JH analogs (JHAs) and JH mimics, e.g., methoprene, fenoxycarb and pyriproxyfen.”
Background
Low Exposure Concentration Effects of Methoprene on Endocrine-Regulated Processes in the Crustacean Daphnia magna
Olmstead, A. W. (2001) · Toxicological Sciences · doi:10.1093/toxsci/62.2.268 · Cited by 52
“These insecticides typically perturb enzymatic and hormonally regulated processes that are relatively specific to insect physiology (Dhadialla et al., 1998; Retnakaran et al., 1985).”
Background
Studies on two ecdysone receptor isoforms of the spruce budworm, Choristoneura fumiferana
Perera, S. C., Ladd, T. R., Dhadialla, T. S., Krell, P. J., Sohi, S. S., Retnakaran, A., & Palli, S. R. (1999) · Molecular and Cellular Endocrinology · doi:10.1016/s0303-7207(99)00058-1 · Cited by 52
Phytocompounds for mosquito larvicidal activity and their modes of action: A review
Ganesan, P., Samuel, R., Mutheeswaran, S., Pandikumar, P., Reegan, A. D., Aremu, A. O., & Savarimuthu Ignacimuthu, S. J. (2022) · South African Journal of Botany · doi:10.1016/j.sajb.2022.11.028 · Cited by 51
Ligand‐Binding Pocket of the Ecdysone Receptor
Billas, I. M. L., & Moras, D. (2005) · Vitamins and hormones · doi:10.1016/s0083-6729(05)73004-1 · Cited by 51
Ligand specificity and developmental expression of RXR and ecdysone receptor in the migratory locust
Hayward, D. C., Dhadialla, T. S., Zhou, S., Kuiper, M. J., Ball, E. E., Wyatt, G. R., & Walker, V. K. (2003) · Journal of Insect Physiology · doi:10.1016/j.jinsphys.2003.08.007 · Cited by 51
Comparison of dose responses and resistance ratios in four populations of the rice stem borer, Chilo suppressalis (Lepidoptera: Pyralidae), to 20 insecticides
He, Y. P., Gao, C. F., Chen, W. M., Huang, L. Q., Zhou, W. J., Liu, X. G., Shen, J. L., & Zhu, Y. C. (2008) · Pest Management Science · doi:10.1002/ps.1522 · Cited by 50
Insect Midgut as a Site for Insecticide Detoxification and Resistance
Smagghe, G. J., & Tirry, L. (2001) · Springer eBooks · doi:10.1007/978-3-642-59549-3_14 · Cited by 50
Methoprene Interferes with Mosquito Midgut Remodeling During Metamorphosis
Nishiura, J. T., Ho, P., & Ray, K. (2003) · Journal of Medical Entomology · doi:10.1603/0022-2585-40.4.498 · Cited by 50
Cross-resistance and Fitness Cost Analysis of Resistance to Thiamethoxam in Melon and Cotton Aphid (Hemiptera: Aphididae)
Zhang, H., Chen, A., Shan, T., Dong, W., Shi, X., & Gao, X. (2020) · Journal of Economic Entomology · doi:10.1093/jee/toaa090 · Cited by 50
Baseline Susceptibility of Bemisia tabaci B Biotype (Hemiptera: Aleyrodidae) Populations From California and Arizona to Spirotetramat
Prabhaker, N., Castle, S. J., & Perring, T. M. (2014) · Journal of Economic Entomology · doi:10.1603/ec13429 · Cited by 50
“Most IGRs are active against the immature stages of a number of insect species (Dhadialla et al. 1998) by disrupting the molting process or cuticle formation (Tasei 2001).”
Background
Ecdysteroids
Lafont, R., Balducci, C., & Dinan, L. (2021) · Encyclopedia · doi:10.3390/encyclopedia1040096 · Cited by 49
Ligand binding by recombinant domains from insect ecdysone receptors
Graham, L. D., Johnson, W. M. P., Pawlak-Skrzecz, A., Eaton, R. E., Bliese, M., Howell, L., Hannan, G. N., & Hill, R. J. (2007) · Insect Biochemistry and Molecular Biology · doi:10.1016/j.ibmb.2007.03.006 · Cited by 49
Comparative toxicity and ecdysone receptor affinity of non-steroidal ecdysone agonists and 20-hydroxyecdysone in Chironomus tentans
Smagghe, G. J., Dhadialla, T. S., & Lezzi, M. (2002) · Insect Biochemistry and Molecular Biology · doi:10.1016/s0965-1748(01)00109-6 · Cited by 49
“This indeed has been the basis for the development of new, target pest selective insecticides with an ecdysone mode of action (Dhadialla et al., 1998; Carlson, 2000).”
BackgroundInfluential
Basis for selective action of a synthetic molting hormone agonist, RH-5992 on lepidopteran insects
Sundaram, M., Palli, S. R., Krell, P. J., Sohi, S. S., Dhadialla, T. S., & Retnakaran, A. (1998) · Insect Biochemistry and Molecular Biology · doi:10.1016/s0965-1748(98)00035-6 · Cited by 49
The Ecdysteroid Receptor
Henrich, V. C. (2005) · Elsevier eBooks · doi:10.1016/b0-44-451924-6/00037-5 · Cited by 49
Selectivity of novel and traditional insecticides used for management of whiteflies on the parasitoid Encarsia formosa
Wang, Z., Dai, P., Yang, X., Ruan, C., Biondi, A., Desneux, N., & Zang, L. (2019) · Pest Management Science · doi:10.1002/ps.5380 · Cited by 48
Environmental risk assessment (ERA) of pyriproxyfen in non-target aquatic organisms
Moura, J. A. D. S., & de Souza-Santos, L. P. (2020) · Aquatic Toxicology · doi:10.1016/j.aquatox.2020.105448 · Cited by 50
The ecdysone agonist tebufenozide (RH-5992) blocks the progression into the ecdysteroid-induced regulatory cascade and arrests silkmoth oogenesis at mid-vitellogenesis
Swevers, L. (1999) · Insect Biochemistry and Molecular Biology · doi:10.1016/s0965-1748(99)00059-4 · Cited by 48
Synergism of Tebufenozide in Resistant and Susceptible Strains of Obliquebanded Leafroller (Lepidoptera: Tortricidae) and Resistance to New Insecticides
Waldstein, D. E., & Reissig, W. H. (2000) · Journal of Economic Entomology · doi:10.1603/0022-0493-93.6.1768 · Cited by 48
Toxic effects of hexaflumuron on the development of Coccinella septempunctata
Yu, C., Fu, M., Lin, R., Zhang, Y., Liu, Y., Jiang, H., & Brock, T. C. M. (2013) · Environmental Science and Pollution Research · doi:10.1007/s11356-013-2036-8 · Cited by 47
“Exposure to hexaflumuron is likely to perturb the development of the beneficial arthropod C. septempunctata, since it is an IGR that disrupts molting and cuticle formation and more generally acts on the insect's endocrine system (Dhadialla et al. 1998).”
Background
Arthropod venoms: A vast arsenal of insecticidal neuropeptides
Schwartz, E. F., Mourão, C. B. F., Moreira, K. G., Camargos, T. S., & Mortari, M. R. (2012) · Biopolymers · doi:10.1002/bip.22100 · Cited by 47
Susceptibility of Ceraeochrysa cubana larvae and adults to six insect growth-regulator insecticides
Ono, É. K., Zanardi, O. Z., Santos, K. F. A., & Yamamoto, P. T. (2016) · Chemosphere · doi:10.1016/j.chemosphere.2016.10.061 · Cited by 47
Recent Progress in Juvenile Hormone Analogs (JHA) Research
Ramaseshadri, P., Farkas, R., & Palli, S. R. (2012) · Advances in insect physiology · doi:10.1016/b978-0-12-391500-9.00005-x · Cited by 49
Optimization of α-acylaminoketone ecdysone agonists for control of gene expression
Tice, C. M., Hormann, R. E., Thompson, C. S., Friz, J. L., Cavanaugh, C. K., & Saggers, J. A. (2003) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(03)00315-9 · Cited by 46
Exploiting semiochemicals in insect control
Agelopoulos, N. G., Birkett, M. A., Hick, A. J., Hooper, A. M., Pickett, J. A., Pow, E. M., Smart, L. E., Smiley, D. W. M., Wadhams, L. J., & Woodcock, C. M. (1999) · Pesticide Science · doi:10.1002/(sici)1096-9063(199903)55:3 · Cited by 161
Juvenile hormone esterase activity in the pupating and diapausing larvae of Sesamia nonagrioides
Schafellner, C., Eizaguirre, M., López, C., & Sehnal, F. (2008) · Journal of Insect Physiology · doi:10.1016/j.jinsphys.2008.04.015 · Cited by 45
Rapid direct analysis in real time (DART) mass spectrometric detection of juvenile hormone III and its terpene precursors
Navare, A., Mayoral, J. G., Nouzová, M., Noriega, F. G., & Fernández, F. M. (2010) · Analytical and Bioanalytical Chemistry · doi:10.1007/s00216-010-4269-4 · Cited by 45
Short and Long-Term Effects of Endosulfan, Cypermethrin, Spinosad, and Methoxyfenozide on Adults of Chrysoperla externa (Neuroptera: Chrysopidae)
Rimoldi, F., Schneider, M. I., & Ronco, A. E. (2012) · Journal of Economic Entomology · doi:10.1603/ec12189 · Cited by 45
“MACs directly stimulate the molting hormone receptor by binding to the same natural hormone receptors, causing an anticipated lethal molt (Dhadialla et al. 1998).”
Background
Lethal and Sublethal Effects of an Insect Growth Regulator, Pyriproxyfen, on Obliquebanded Leafroller (Lepidoptera: Tortricidae)
Sial, A. A., & Brunner, J. F. (2010) · Journal of Economic Entomology · doi:10.1603/ec09295 · Cited by 45
The Effect of Insecticides Considered Harmless to Honey Bees (Apis mellifera): Proboscis Conditioning Studies by Using the Insect Growth Regulators Tebufenozide and Diflubenzuron
Abramson, C. I., Squire, J., Sheridan, A. B., & Mulder, P. G. (2004) · Environmental Entomology · doi:10.1603/0046-225x-33.2.378 · Cited by 45
“The active ingredient is tebufenozide, which is described as “being safe for pollinators such as the honey bee” ( Dhadialla et al. 1998 ).”
Background
A review of research on Sunn Pest {Eurygaster integriceps Puton (Hemiptera: Scutelleridae)} management published 2004–2016
Davari, A., & Parker, B. L. (2018) · Journal of Asia-Pacific Entomology · doi:10.1016/j.aspen.2018.01.016 · Cited by 45
A Chimeric Ecdysone Receptor Facilitates Methoxyfenozide-Dependent Restoration of Male Fertility in ms45 Maize
Unger‐Wallace, E., Cigan, A. M., Trimnell, M. R., Xu, R., Kendall, T., Roth, B., & Albertsen, M. C. (2002) · Transgenic Research · doi:10.1023/a:1020350208095 · Cited by 45
“Ligands that do have excellent field application potential include the commercially available non-steroidal ecdysone agonists tebufenozide and methoxyfenozide (Dhadialla et al., 1998; Martinez & Jepson, 1999).”
Background
Efficacy of Olyset ® Duo, a permethrin and pyriproxyfen mixture net against wild pyrethroid-resistant Anopheles gambiae s.s. from Côte d’Ivoire: an experimental hut trial
Koffi, A. A., Ahoua Alou, L. P., Djenontin, A., Kabran, J.-P. K., Dosso, Y., Kone, A., Moiroux, N., & Pennetier, C. (2015) · Parasite · doi:10.1051/parasite/2015028 · Cited by 45
“PPF is a juvenile hormone analogue (JHA) which inhibits metamorphosis and embryogenesis in several mosquitoes [5] and is already widely used as a larvicide [4].”
Background
Comparison of the activity of non‐steroidal ecdysone agonists between dipteran and lepidopteran insects, using cell‐based EcR reporter assays
Soin, T., Swevers, L., Kotzia, G. A., Iatrou, K., Janssen, C., Rougé, P., Harada, T., Nakagawa, Y., & Smagghe, G. J. (2010) · Pest Management Science · doi:10.1002/ps.1998 · Cited by 43
Dual ecdysteroid action on the epitracheal glands and central nervous system preceding ecdysis ofManduca sexta
Žitňanová, I., Adams, M. E., & Žitňan, D. (2001) · Journal of Experimental Biology · doi:10.1242/jeb.204.20.3483 · Cited by 44
Differential responses of germinating Venturia inaequalis conidia to kresoxim-methyl
Olaya, G., Zheng, D., & Köller, W. (1998) · Pesticide Science · doi:10.1002/(sici)1096-9063(1998110)54:3 · Cited by 103
A Possible Link Between Pyriproxyfen and Microcephaly
Evans, D., Nijhout, F., Parens, R., Morales, A. J., & Bar‐Yam, Y. (2017) · PLoS Currents · doi:10.1371/currents.outbreaks.5afb0bfb8cf31d9a4baba7b19b4edbac · Cited by 41
Peptide Hormones in the Insect Midgut
Wu, K. C., Li, S., Wang, J., Ni, Y., Huang, W., Liu, Q., & Ling, E. (2020) · Frontiers in Physiology · doi:10.3389/fphys.2020.00191 · Cited by 45
“Studies have increasingly shown that ecdysone, JH, and their analogs can be used for biological control of pests (Dhadialla et al., 1998; Retnakaran et al., 2003; Wilson, 2004).”
Background
Comparative impacts of white grub (Coleoptera: Scarabaeidae) control products on the abundance of non-target soil-active arthropods in turfgrass
Peck, D. C. (2008) · Pedobiologia · doi:10.1016/j.pedobi.2008.10.003 · Cited by 43
“The insect growth regulator halofenozide is an ecdysteroid mimic that induces premature and lethal molt in scarab larvae (Dhadialla et al., 1998).”
Background
Characterization of the Ligand-Binding Domain of the Ecdysteroid Receptor from Drosophila Melanogaster
Grebe, M., Przibilla, S., Henrich, V. C., & Spindler‐Barth, M. (2003) · Biological Chemistry · doi:10.1515/bc.2003.011 · Cited by 43
“This leads us to assume that this region contributes to the species-specific differences in ligand binding and sensitivity to ecysteroids and diacylhdrazines (Dhadialla et al., 1998; Wurtz et al., 2000).”
Background
Molecular cloning, expression analysis and functional confirmation of two ecdysone receptor isoforms from the rice stem borer Chilo suppressalis
Minakuchi, C., Nakagawa, Y., Kiuchi, M., Tomita, S., & Kamimura, M. (2002) · Insect Biochemistry and Molecular Biology · doi:10.1016/s0965-1748(02)00036-x · Cited by 43
Sublethal effects of hexaflumuron on development and reproduction of the diamondback moth, Plutella xylostella (Lepidoptera: Yponomeutidae)
Mahmoudvand, M., Abbasipour, H., Garjan, A. S., & Bandani, A. R. (2011) · Insect Science · doi:10.1111/j.1744-7917.2011.01411.x · Cited by 42
“Insect growth regulators (IGRs) interrupt molting (juvenile hormone or ecdysone mimics) and cuticle formation (chitin synthesis inhibitors) and affect endocrine systems (Dhadialla et al., 1998).”
Background
Chemically inducible expression of the PHB biosynthetic pathway in Arabidopsis
Kourtz, L., Dillon, K., Daughtry, S., Peoples, O. P., & Snell, K. D. (2007) · Transgenic Research · doi:10.1007/s11248-007-9067-1 · Cited by 43
“These promoters can be activated by nonsteroidal ecdysone analogs that act specifically on receptors from lepidopteran insects and are not toxic to non-lepidopteran organisms ( Dhadialla et al. 1998; Retnakaran et al. 2003).”

Authors: Dhadialla, T. S., Carlson, G. R., & Le, D. P.
Affiliations: Insecticide Research Laboratories, Rohm and Haas Company, 727 Norristown Road, Spring House, Pennsylvania 19477;
Venue: Annual Review of Entomology
Publisher: Annual Reviews
Published: 1998-01
Volume: 43
Issue: 1
Pages: 545-569
ISSN: 0066-4170 (ISSN-L)
1545-4487
DOI: 10.1146/annurev.ento.43.1.545
OpenAlex: W2149662691
Cited by: 912
References: 131
Citations by year: 2026: 12 · 2025: 29 · 2024: 29 · 2023: 22 · 2022: 23 · 2021: 44 · 2020: 22 · 2019: 30 · 2018: 23 · 2017: 34 · 2016: 32 · 2015: 28 · 2014: 21 · 2013: 32 · 2012: 49
FWCI: 3.70
Type: journal article
Language: en
Open access: closed
Locations: Annual Review of Entomology (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Agricultural and Biological Sciences › Plant Science › Insect Pest Control Strategies
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Insect Resistance and Genetics
Life Sciences › Agricultural and Biological Sciences › Insect Science › Insect-Plant Interactions and Control
Keywords: insect growth regulators, ecdysteroid agonists, juvenile hormone agonists, tebufenozide, fenoxycarb, pyriproxyfen, 20-hydroxyecdysone, ecdysteroid receptor, insecticide mode of action, ecotoxicology, lepidopteran pests
MeSH terms: Animals, Forecasting, Hydrazines, Insecticides, Insecta, Juvenile Hormones, Steroids, Molecular Structure, Molecular Mimicry, Ecdysteroids

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NEW INSECTICIDES WITH ECDYSTEROIDAL AND JUVENILE HORMONE ACTIVITY

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