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Action of a novel nonsteroidal ecdysteroid mimic ... - Insects.ugent.be

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90 Guy Smagghe, Danny Degheele<br />

P<br />

‘3<br />

350<br />

-m-<br />

5 150<br />

5<br />

0 100<br />

04 I<br />

0 5 10 15 20<br />

Time (days after first oviposition)<br />

Fig. 4. Effect <strong>of</strong> tebufenozide on the cumulative fecundity per<br />

female <strong>of</strong> L. decemlineata adults, at 20 pg per adult by topical<br />

treatment and at 30 or 100 mg litre-’ by continuous feeding<br />

on treated potato leaves. The arrow indicates the moment when<br />

topical treatment took place or oral application started. The<br />

symbol * indicates that all adults were dead.<br />

73( k 8) and 69( k 8)% for the groups treated topically<br />

with 0 and 20 pg per adult, respectively.<br />

3.3 Toxicity and effect <strong>of</strong> tebufenozide on Heteroptera<br />

No effect on growth, weight gain or ecdysis was observed<br />

on third- (N,) and last- (N5) instar nymphs <strong>of</strong> P. sagitta<br />

at doses ranging from 1 to 40 pg per nymph, topically<br />

applied either on the dorsal or on the ventral side.<br />

Likewise, no toxicity and no effects on the development<br />

<strong>of</strong> N, and N, bugs were noted when last-instar S. exigua<br />

larvae previously treated with 20 pg per larva were<br />

provided as prey.<br />

In a preliminary assay with 0. insidiosus, no effects on<br />

the development <strong>of</strong> any nymphal stage (N,-N,) or adult<br />

formation were noted when fresh eggs <strong>of</strong> S. exigua<br />

previously dipped in 1 g litre-’ tebufenozide were<br />

supplied ad libitum.<br />

3.4 Toxicity and effects <strong>of</strong> tebufenozide on Orthoptera<br />

First- and second-instar L. migratoria migratorioides<br />

larvae showed a pattern <strong>of</strong> growth and ecdysis into the<br />

following instar after a continuous treatment with 30 or<br />

100 mg litre-’ tebufenozide which was the same as that<br />

<strong>of</strong> the control insects.<br />

4 DISCUSSION<br />

Tebufenozide acts primarily by inducing a premature and<br />

lethal larval moult, especially in larval Lepidoptera. Our<br />

results strengthen the concept that the compound<br />

stimulates epidermal cells to undergo apolysis prematurely<br />

and to synthesize a new larval cuticle by imitating the<br />

activity <strong>of</strong> <strong>ecdysteroid</strong>s. In addition, LC50 values <strong>of</strong><br />

tebufenozide against the different stages <strong>of</strong> S. exempta<br />

and S. exigua illustrate the uniformity <strong>of</strong> response with<br />

respect to the larval stage, which is consistent with the<br />

pattern <strong>of</strong> RH-5849 against the different stages <strong>of</strong> several<br />

Lepidoptera obtained under comparable conditions.2*’2<br />

The minimum concentration <strong>of</strong> tebufenozide (by means<br />

<strong>of</strong> a continuous oral application) needed to induce a<br />

premature moult in the different larval instars was similar<br />

for each species: in third- to sixth-instar larvae (L3-Ls)<br />

<strong>of</strong> S. exempta at a concentration <strong>of</strong> 20.02 mg litre-’, and<br />

in L1-L5 <strong>of</strong> S. exigua at 21 mg litre-’. LC50 values for<br />

last instars reached lower levels, since abnormal and<br />

lethal pupation are included in the mortality percentages<br />

for last-intar larvae.<br />

The inability <strong>of</strong> treated larvae to ecdyse out <strong>of</strong> the old<br />

cuticle might <strong>be</strong> provoked by an interference with<br />

eclosion hormone (EH) production/release, since it is<br />

known that this hormone is released by a drop in<br />

<strong>ecdysteroid</strong> titre prior to ecyd~is.~~ Residual amounts <strong>of</strong><br />

<strong>ecdysteroid</strong> agonist in the insect body may cause an<br />

inhibition <strong>of</strong> EH-release. Similar results <strong>of</strong> death during<br />

a prematurely promoted moult have <strong>be</strong>en reported<br />

previously, following application <strong>of</strong> natural <strong>ecdysteroid</strong>s<br />

to different insect species.31<br />

The decrease in weight gain and feeding in larval<br />

Lepidoptera treated with tebufenozide may result from<br />

an ecdysonergic activity <strong>of</strong> the compound. It is well<br />

known that cessation <strong>of</strong> feeding and weight gain occurs<br />

prior to ecdysis as a result <strong>of</strong> <strong>ecdysteroid</strong> ~ecretion.~’ In<br />

contrast, no such effects were observed in larvae <strong>of</strong> L.<br />

decemlineata, D. virggera, P. sagitta and L. migratoria at<br />

similar doses/concentrations <strong>of</strong> te<strong>be</strong>nufenozide.<br />

The different toxicities <strong>of</strong> <strong>ecdysteroid</strong> agonists on<br />

last-instar larvae <strong>of</strong> S. exempta, S. exigua and L.<br />

decemlineata applied orally cannot <strong>be</strong> explained by<br />

differences in retention, distribution and metabolic<br />

detoxification <strong>of</strong> the compound in the insect body.”,33<br />

Consequently, we consider that the wide range <strong>of</strong><br />

susceptibilities to the <strong>ecdysteroid</strong>-<strong>mimic</strong>king compounds<br />

in the different insect species may <strong>be</strong> explained by<br />

differences in the structure <strong>of</strong> the EcR and their binding<br />

affinity for the <strong>ecdysteroid</strong> agonist ligand molecules. The<br />

latter hypothesis is consistent with the concept that<br />

structure and biochemical properties <strong>of</strong> EcR may differ<br />

among insect species.34 In general, although the hypothesis<br />

seems reasonable that the different toxicities <strong>of</strong><br />

<strong>ecdysteroid</strong> agonists are induced by differences in<br />

EcR-binding affinity, further research is required.<br />

In this study, it was noted that tebufenozide possessed<br />

little or no insecticidal activity against larvae <strong>of</strong> two<br />

coleopterans, L. decemlineata and D. virgqera virgqera,<br />

against various nymphal stages <strong>of</strong> the predatory heteropterans,<br />

P. sagitta and 0. insidiosus, or against larvae<br />

<strong>of</strong> the orthopteran, L. migratoria migratorioides, as

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