MXPA99011311A - Non-hazardous pest control - Google Patents
Non-hazardous pest controlInfo
- Publication number
- MXPA99011311A MXPA99011311A MXPA/A/1999/011311A MX9911311A MXPA99011311A MX PA99011311 A MXPA99011311 A MX PA99011311A MX 9911311 A MX9911311 A MX 9911311A MX PA99011311 A MXPA99011311 A MX PA99011311A
- Authority
- MX
- Mexico
- Prior art keywords
- larvae
- afflicting
- mixture
- invertebrates
- alcohol
- Prior art date
Links
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Abstract
Se presentan un plaguicida y un método para utilizar al plaguicida para matar invertebrados, especialmente, insectos, arácnidos y larvas. El método consiste en:preparar una mezcla de un vehículo o portador con el plaguicida y aplicar la mezcla a los insectos, arácnidos y larvas y a su hábitat. El plaguicida es un agente afectador de neurotransmisores que utiliza los sitios receptores de octopamina en insectos, arácnidos y larvas. El agente afectador es un compuesto químico que tiene un anillo de carbonos de seis miembros que en el mismo tiene sustituido al menos un grupo funcional oxigenado. El agente afectador es un componente químico de un aceite esencial vegetal de origen natural. La deposición de los compuestos químicos de la presente invención sobre una superficie proporciona una toxicidad residual de hasta 30 días. Se revelan diversos portadores para el agente afectador. Los compuestos químicos de la presente invención impiden la alimentación de los insectos, arácnidos y larvas y también retardan el crecimiento de las larvas de los insectos y los arácnidos.
Description
CONTROL OF PESTS INOCUO
FIELD OF THE INVENTION The present invention relates to a method for controlling pests and, more particularly, to a method for preparing and applying a pesticide that affects the octopamine receptor sites of insects, arachnids and larvae.
BACKGROUND OF THE INVENTION For many years, the pesticidal activity of many chemical compounds and mixtures has been studied in order to obtain a product that is selective for invertebrates, such as insects, arachnids and larvae thereof, and which has little or no toxicity to the invertebrates. vertebrates such as mammals, fish, poultry and other species and that in no other way persists or subsists in the environment and damages it. Most of the products that applicants are aware of and that have sufficient pesticide activity to be of commercial importance also have toxic or perceptive effects on mammals, fish, poultry and other non-target species of the product. For example, organophosphorus compounds and carbamates inhibit the activity of acetylcholinesterase in insects as well as in all classes of animals. It's known
P1721 / 99MX that the chlordimeform and the related formamidines act on the receptors of the octopamine of the insects but have been withdrawn from the market, due to the cardiotoxic potential in the vertebrates and to the carcinogenicity in animals and a variable effect on different insects. Also, very high doses are required to be toxic to certain insect species. It was postulated that amidine compounds affect the octopamine sensitive adenylate cyclase present in insects [Nathanson et al, Mol. Parmacol 20: 68-75 (1981) and Nathanson, Mol. Parmacol 28: 254-268 (1985)]. Another study was conducted with respect to the absorption of octopamine and metabolism in the insect's nervous system [Wierenga et al, Neurochem 54, 479-489 (1990)]. These studies focused on compounds that contain nitrogen and that mimic the structure of octopamine. Insecticides such as trioxabicyclooctans, dithians, silatrans, lindane, toxafem, cyclodienes and picrotoxin act on the GABA receptor (gamma aminobutyric acid). However, these products also affect mammals, birds, fish and other species. There is a need for a pesticide that focuses only on insects, arachnids and their larvae and that does not produce undesirable effects and
P1721 / 99MX pe judicial in other species.
BRIEF SUMMARY OF THE INVENTION It is a primary objective of the present invention to provide a method for preparing and applying a pesticide that kills invertebrates, especially insects, arachnids and their larvae and that has no detrimental effects on other species, including mammals, fish and birds. of corral. It is a further object of the present invention to provide a method for preparing and applying a pesticide, which exerts its pesticidal properties via the octopamine receptor site on insects, arachnids and on their larvae and on other invertebrates. Still another object of the present invention is to provide a method for preparing and applying a pesticide in relatively low concentrations, which will be effective over a comparatively long period of time, such as at least 24 hours. In accordance with the teachings of the present invention, a method for killing insects and arachnids and larvae thereof is disclosed. Cases include preparing a mixture of a vehicle or carrier with an affecting agent that interferes with the neurotransmitters of the octopamine receptor site in insects, arachnids and their larvae and
P1721 / 99MX apply the mixture to insects, arachnids, larvae and their habitat. The affected agent interacts with the octopamine receptor sites in insects, arachnids and larvae and interferes with neurotransmission in invertebrates but does not affect mammals, fish and poultry .. The agent is a chemical compound that has the structure of a six-membered carbon ring the carbon ring has substituted at least one oxygenated functional group in it. It also reveals a method to kill insects and arachnids and larvae thereof. A mixture of cinnamic alcohol, eugenol and alpha terpineol is prepared. The mixture is mixed with a carrier to produce a uniform mixture. The mixture is applied to insects and arachnids and their larvae and their habitat. The mixture interacts with the octopamine receptor sites in invertebrates and interferes with neurotransmission in invertebrates but does not affect mammals, fish and poultry. In another aspect, a pesticide is disclosed having an afflicting agent having a six-membered carbon ring. The carbon ring or carbon ring has substituted at least one oxygenated functional group therein. The affecting agent affects the receptor site of octopamine in invertebrates that include insects,
P1721 / 99MX arachnids and their larvae. The afflicting agent is intimately mixed with a carrier. The exposure of insects, arachnids and their larvae to the afflicting agent produces a disturbance or alteration in the octopamine receptor sites in the invertebrates to interfere with the neurotransmission in invertebrates and the death of the exposed invertebrate. It also reveals a method to kill insects, arachnids and their larvae. A mixture of a chemical compound derived from a plant essential oil with a carrier is prepared. The chemical compound has therein at least one oxygenated functional group with inhibitory activity of the receptor site. The chemical compound has octopamine. The mixture is applied to insects, arachnids, larvae and their habitat. The chemical compound interacts with an octopamine receptor site in insects, arachnids and larvae and interferes with neurotransmission in insects, arachnids and larvae of these but does not affect mammals, fish and poultry. In another aspect, a method for controlling insects, arachnids and their larvae is revealed. An emulsion of an affecting agent is prepared that disturbs neurotransmission in the octopamine receptor site in insects, arachnids and their larvae. The mixture is applied to insects, arachnids, larvae and their habitat. The agent interacts with the sites
P1721 / 99MX receptors of octopamine in insects, arachnids and larvae and prevents the feeding of insects, arachnids and larvae but does not affect mammals, fish and poultry. In a further aspect, a method for controlling insects, arachnids and their larvae is disclosed. An afflicting agent mixed with a vehicle is applied to the larvae of insects and arachnids and their habitat. The affected agent retards the growth of the larvae. The affected agent interacts with the octopamine receptor sites in the larvae of insects and arachnids and interferes with neurotransmission in larvae but does not affect mammals, fish and poultry. The afflicting agent is an organic chemical compound present in nature which has at least six (6) carbon atoms. In addition, a method for killing insects, arachnids and larvae thereof is disclosed. A mixture of a carrier and an organic chemical compound present in nature, which has at least six carbon atoms, is prepared. The chemical compound has inhibitory activity on the octopamine receptor site. The mixture is applied to insects and arachnids and their larvae and their habitat. The chemical compound interacts with an octopamine receptor site in insects and arachnids and larvae thereof.
P1721 / 99MX interferes with neurotransmission in insects, arachnids and larvae but does not affect mammals, fish and poultry. These and other objects of the present invention will be apparent from the reading of the following specification, considered together with the accompanying drawings.
BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 is a graph showing the effect of the 3-B mixture of the present invention on the intracellular concentration of [Ca + 2] in neuronal cells. Figure 2 is a diagram showing the contraction of cockroach leg muscles induced by electrical stimulation when the 3-B mixture of the present invention is injected into the thorax of a live cockroach. Figure 3 is a diagram showing the contraction of the leg muscles of a cockroach in an isolated leg, induced by electrical stimulation when the 3-B mixture of the present invention is applied to the isolated leg. Figure 4 is a diagram showing the test of Figure 2 using acetone as a control without the 3-B mixture. Figure 5 is a diagram showing the test of Figure 3 using acetone as control
P1721 / 99MX without the 3-B mixture. Figure 6 is a series of diagrams showing the transmission of signals from the mechano-receivers of the fences after the application of the 3-B mixture and the control to the abdominal nerve of the cockroach. Figure 7 is a diagram showing the damage to the feed in leaf discs of the cabbage plant with the mixture 3-B compared to a control.
DETAILED DESCRIPTION OF THE PREFERRED MODALITIES The physiological activity in insect invertebrates, arachnids and their larvae is produced by the chemical compounds of the present invention and by mixtures of these chemical compounds. The following chemical compounds have a six-membered carbon ring and having at least one oxygenated functional group substituted therein are representative of the chemical compounds of the present invention but these are not considered to be all chemical compounds and are not an limiting
trans-anetole
benzyl acetate
P1721 / 99MX benzyl alcohol HOCH. -O CH3 carvacrol /
HOCH2 0CH3 cinnamic alcohol eugenol / CH2 = CH-CH2
alcohol HOCH2CH2 -o - OH
phenylethyl
Or pulegona \\
to f-terpineol
OH timol \
The materials listed above are all components of plant essential oils. An additional plant essential oil that is a
P1721 / 99MX chemical compound of the present invention is
citronellal CH, CH, CH2C = C CH CH3 / CH, HC CH2 O Anetole, carvacrol, citronellal, eugenol, D-pulegone, alpha-terpineol and thymol are all monoterpenes each having ten (10) carbon atoms. The present invention is not limited to the chemical compounds listed herein. All the chemical compounds of the present invention are organic chemical compounds present in nature, which are devoid of halogens. In addition, several of the chemical compounds of the present invention are considered, by the Environmental Protection Agency (EPA) as safe for humans and exempt from registration. Thus, these chemical compounds do not require prior approval or registration in the EPA, some of these chemical compounds have been added to the prior art insecticides as attractants and repellents. However, there are no reports that these chemicals have toxic pesticidal activity at the concentrations disclosed in the present invention. All chemical compounds of the present invention act as agonists or antagonists in the
P1721 / 99MX octopamine receptor sites in insects, arachnids and their larvae and, consequently, produce physiological effects in exposed invertebrates. The chemical compounds of the present invention are considered as affectating agents. Exposure to reduced concentrations of chemical compounds or exposure for short periods of time affects the eating habits of exposed insects, arachnids and larvae. This is important in those invertebrates that feed on vegetation, since there is reduced damage to plants by invertebrates that have received sublethal concentrations of the chemical compounds of the present invention. Also, the insects, arachnids or larvae that survive the exposure to the chemicals of the present invention show that they have a hindered growth. The alpha-terpineol, the eugenol and the cinnamic alcohol were dissolved in acetone and designated as sample 3B. The range of percentages by weight of the components of the mixture is alpha-terpineol 10% -50%, eugenol 10% -50% and cinnamic alcohol 20% -35%. The preferred mixture has equal parts by weight of each of the components. The male and female American cockroaches were injected with sample 3B in the abdomen. Significant signs of toxicity were observed at 1 mg cockroach in 2 μl of acetone. At lower doses, no symptoms were observed. With this
P1721 / 99MX approach, 2 out of 6 died in less than 30 minutes. For the survivors, some showed locomotor difficulties. Hyperactivity was not observed even in those who died quickly. In some cases, the treated insects (21) died after 2 or 3 days. None of the American cockroaches died when they were treated by topical application before 24 hours. A mortality of 40% (4/10) was observed 24 hours after treatment and this effect is time dependent. After 72 hours, 100% died. Control insects that received 2 μl of acetone alone by injection did not show any disease effects (Table 1) •
Table 1: Effect of time course of 3-B (1 mg / insect) on American cockroaches treated by topical application. Time (hour) Mortality- 3B Mortality-Control 24 4/10 0 48 6/10 0 72 10 // 10 0
The data from the previous study suggest that the action of 3B depends on the site of application, that is, abdominal injection against topical application for the whole body.
P1721 / 99MX The 3B was applied in different areas of the insect. When supplied to the ventral sternum region (at the base of the hind legs) of the American cockroach, 3B was the most toxic at 125 μg / insects. In this case, toxic signs were observed in less than 10 minutes. A lethal dose of 250-500 μg / insect was injected and the insects died within 30 minutes (Table 2).
Table 2: Time course and response to the dose of 3B on American cockroaches treated by injection through the sternum or ventral plate. Dose for Time Test for (hrs.) Mortality - μg / insect 50 100 125 250 500
0. 5 0 2/10 6/10 10/10 1.0 2/10 3/10 7/10 1.5 5/10 7/10 9/10 2.0 5/10 9/10 10/10 3.0 6/10 9/10 5.0 8 / 10 10/10 24.0 10/10 _.
* No mortality was found in insects treated in exactly the same way with an equal volume of acetone alone (vehicle) as control.
P1721 / 99MX In the last case of injection of a lethal dose, it seemed that the hind legs were paralyzed and that the middle front legs moved quickly, although there was no overt hyperexcitation. This phenomenon of rapid death was also observed in German cockroaches that were treated by means of topical application (3B is more toxic to German cockroaches than to American cockroaches). At 125 μg / insect, they were knocked down to 80% (8/10) of the German cockroaches in 2 to 3 hours and died in less than 24 hours (the dose was 125 mg of 3B per insect with 0.4 μl of acetone) . The above data supports the observation that the application site provides varying degrees of toxicity. For further confirmation, 1 mg of 3B in 20 ml of acetone was applied to small jars covering all surfaces. One hour after the acetone had completely evaporated, 5 American cockroaches were introduced into each jar. The control jars were treated exactly like the previous ones but, with 20 ml of acetone alone. All cockroaches died from 10 to 30 minutes in jars containing 3B. None died in the control jars. Some insects
(3/5) showed hyperactivity within 1 to 3 minutes after exposure. At 8 minutes, paralysis was observed in the hind legs. These
P1721 / 99MX data "in passing" are consistent with the previous study in which a rapid death was observed when 3B was delivered to the sternum or ventral plate region instead of the abdomen. The fact that toxins can penetrate faster through the legs (there is no chitin layer as in the body) supports the notion that the permeability / penetration of 3B plays a key role in its toxicity (Table 3).
Table 3: Effect of time course of 3B (1 mg / jar) on American cockroaches exposed to a pretreated surface one hour after the application of 3-B. * Time (min.) Mortality 10 3/5 15 3 / 5 20 4/5 30 5/5 * There are no deaths in insects exposed to the surface treated with pure acetone.
Based on these data, the same treated jars were used for a residual study. In this experiment, the American cockroaches were transferred to the treated and control jars at different times from the time the acetone was evaporated, i.e., 24, 48, 96, 72 hours and
P1721 / 99MX 7 days It is very interesting that all insects died after being exposed to the treated jars, even 7 days after the application of 3B. However, it required more time for the cockroaches to die in proportion to the time span from the initial application of 3B to the jar. Some toxic signs were observed in all cases after exposure. In addition, when the same experiment was repeated with German cockroaches, greater and more rapid toxic effects were observed. It seems that there is some degradation in the toxic effects with the passage of time (Table 4).
Table 4: Effect of 3-B (1 mg / jar) when it was applied to surfaces on American cockroaches exposed to these surfaces at different times after surface treatment. Time elapsed from Time required to kill the application of 3B to 100% of insects (days) (days) 1 1 2 3 3 6 5 8 10 (6/10 died)
* Only 6 insects died when 10 roaches were exposed to jars pretreated 7 days after the application of 3-B.
P1721 / 99MX The toxic effects shown in Table 4 could be prolonged by combining them with oils having different characteristics. Eugenol, one of the ingredients of 3-B, was dissolved in galoxolide, a perfume oil that imparted longer lasting properties related to evaporation and oxidation of the pesticide properties of eugenol. Mixtures having 30% -60% galaxolide and 40% -70% eugenol, by weight, have been effective. As an example, eugenol and galoxolide, 1 mg of each, were mixed in equal portions in 10 ml of acetone and stirred vigorously for two minutes and then applied (1 mg of the mixture / jar) as before, to small jars and all surfaces were covered. The data in this example (Table 5) show that the lethal effect of the mixture was extended and improved.
Table 5 Time elapsed Time required to kill after 100% application of eugenol / galoxolide * insects (days) (weeks)
2 1 3 1 4 1
* 1, 3, 4, 6, 7, 8-hexahydro-4, 6,6,7,8, 8-hexamethyl-cyclopenta-gamma-2-benzopyran.
P1721 / 99MX The abdominal nerve cord of the cockroaches showed the second highest absorption of octopamine from all the tissues studied [J. Neurochem 5_4 479-489 (1990)]. The high efficiency of the chemical compounds of the present invention in the "run-through" study was attributed to the high concentration of optopamine receptors in the ventral nerve cord in close proximity to the hind paws. Since the toxic signs produced by the
3B did not indicate patterns of cholinergic action, other main possibilities were considered, such as GABA receptor, optopamine receptor binding / biogenic amine, [Ca2 +], or venom for mitochondrial respiration: 1. Study of chloride-receptor channel of GABA: It is known that this site of action is one of the main sites of action of several insecticides. When the action of 3B was tested, 3H-EBOB ([3H] n-propyl bicyclo orthobenzoate) and 35S-TBPS were used.
(Phosphorous bicycle esters). The first ligand was used based on the findings that EBOB has shown to be very toxic and with high affinity for radioligand for the receptor-GABA convulsant binding site in insects. It also shows identical or overlapping binding sites with seven classes of insecticides: trioxabicyclooctans, dithians, silatrans, lindane, toxafiene, cyclodienes and
P1721 / 99 X picrotoxinin. TBPS has been obstructed by poor toxicological relevance and binding affinity in insects. In this study both radioligands were used for a comparison. As shown in Table 6, 3B did not induce antagonistic action on the binding affinity of 3H-EB0B or 35S-TBPS at concentrations of 3B ranging from 10 μM to 10 NM. Only at 100 BM a significant effect was observed. However, at this high concentration (100 μM), specificity at the site of action is unlikely. In contrast, the heptaclorepoxide alone and a mixture of Endosulfan I
(60%) and Endosulfan II (40%) as a positive pattern, were very active even at 10 Nm. These data indicate that this test system works poorly with 3B and that the lack of its action is due to its inaccessibility to the GABA receptor site. The fact that the London strain resistant to cyclodiene showed a cross resistance to 3B supports the above data and discards the GABA receptor as the target or site of action for e 3B.
P1721 / 99MX Table 6: Effect of 3B on receptor-GABA binding. dpm per 200 μg of synaptosomal membrane protein (X ± SD)
Evaluated Concentration? -EBOB 35 S -TBPS μM 3 -B 0 2558 ± 159 3361 ± 297 0.01 2069 + 98 2991 + 101 0.10 2069 ± 198 29391111 1.0 2088 + 76 2917 ± 85 10 2111 + 151 3001 + 173 100 2109 + 88 2985 ± 203
Endosu mixture .lf, an μM 0 2558 ± 71 3361 + 297 0.01 1886 ± 71 2477 ± 162 0.1 1009 + 83 1358 + 101 1.0 350 ± 35 552 ± 43 10 255 + 29 360115 100 241118 285 ± 11
Heptaclorepoxide μM 0.001 2010 ± 91 2470 ± 188 0.01 1583 ± 77 2000 75 0.10 1221 + 63 1699 ± 109 1.0 1142 ± 85 1493 ± 99 10 591 ± 41 685 ± 66
P1721 / 99MX Table 6: Effect of 3B on receptor-GABA binding. dpm per 200 μg of synaptosomal membrane protein (X ± SD)
Ligand without Marker μM 0.001 499 ± 34 533 ± 25 0.01 346 ± 29 381 + 17 0.10 206 ± 15 211 ± 19
The control value (pure solvent) was respectively 2558 ± 159 X3361 ± 297 for EBOB X TBPS. 2. Octopamine / biogenic amine receptor binding site: It is known that biogenic amines perform various physiological functions through their specific receptors on insects. The octopamine receptor is the biogenic amine receptor with the highest predominance in insects. It is known that certain acaricides, such as chlordemeform, act on octopamine receptors, causing a variety of symptoms, including behavioral changes. When 3B was incubated directly with a homogenate of the nervous cord of American cockroaches, a significant increase in cyclic AMP (camp) was found at a dose of 1 μM. Chemical octopamine was used as a positive control and induced a significant increase in the 1 μM field. Additional evidence that the
P1721 / 99MX octopamine is the main site of action of 3B is that in co-treatment of 3B and octopamine, 3B ftr abolished the increase induced by octopamine in the camp. 5 To confirm that 3B is a toxic octopamine receptor, two important biomarkers were measured: the heartbeat / 30 seconds and the activity of the protein kinase (PKA) dependent on the camp. It is considered that these two are
Particularly important for identifying the octopamine receptor activity, since it has been shown that the heart of the cockroach has a higher concentration of octopamine receptors. When to the region of the sternum or ventral plate of
a live and intact American cockroach was applied a concentration of 3B of 200 μg / insect, a significant increase in heart beats / 30 seconds was observed and this was accompanied by an increase in camp. As before, older
concentrations of 3B resulted in a reduction in heart beats (Table 7).
P1721 / 99MX Table 7: Effect of_ 3-B on _ the heartbeat / 30 seconds of the American cockroach. Tested doses, μg Before 30 Min. After Treatment Control treatment 55 ± 1.9 55 ± 3.2
200 55 ± 2.1 71 ± 4.5
300 58 ± 0.81 67 ± 1.63
600 57 ± 0.47 41 ± 2.4
900 53 + 1.9 38 + 2.8 octopamine (20 μ) 5412.1 75 ± 3.6
clordimeformo (20 μ) 51 ± 1.4 69 ± 2.5
(positive control)
In addition, when 3B was incubated with a synaptosomal preparation from American cockroach heads, a significant increase in PKA activity was found, which is consistent with the previous conclusion (Table 7).
Table 8: In Vivo effect of 3-B (220 μg / cockroach) on the activity of PKA in the synaptosomal membrane of American cockroaches. dpm / 1 nmol Kemptide / 5 min. X ± SD Control 1753 ± 57 3B 4008 ± 201
Possible role of [Ca]: Due to the
P1721 / 99MX locomotor difficulties observed among cockroaches treated with 3B in the region of the sternum or ventral plate, it was postulated that increases in intramuscular Ca2 + levels could be involved in contractions of the hind legs. For this purpose, adrenal cells of rat chromaffin PC12 of the mammalian cell line were used. It is known that this cell line mimics neuronal cells, particularly to catecholaminergic neurons and has been used as a model of the phenomenon of release of the presynaptic transmitter induced by Ca2 +. As shown in Figure 1, when 3B was added to these cells (in A) at 100 μM, there was no change in free intracellular Ca2 + The concentration of [Ca2 +] in the interior of PC12 cells was found using spectrofluorometric measurements with Fura 2 / AM (a cell penetrating fluorescence probe for free Ca2 +). A positive control pattern, tapsigargin clearly increased the [Ca2 +] + (in B) even to 500 Nm. Also, 10 μM of ionomycin and a Ca2 + ionophore (in C) produced the expected increase in Ca2 + entry. These results show that 3B shows no ability to regulate any type of calcium homeostasis in mammalian cells. The effect of the chemical compounds of the present invention on rat brain tissue cells was as follows, wherein the generation of
P1721 / 99MX cyclic AMP was measured as dpm / mg of control protein 5395143 3-B 54111391 terpineol 5399.1219 eugenol 54611488 phenyl ethyl alcohol 54991415
Thus, there was no change in the neurotransmission system of a mammal. These data confirm the lack of neurotoxicity of these essential oils in mammals. 4. Mitochondrial / respiratory poison: Another possible form of action is that of mitochondrial or respiratory poisoning. It has been observed that all mitochondrial poisons induce hyperactivity at some point of their action. However, when American cockroaches were treated with a topical application of 3B, hyperactivity or hyper-excitation was not observed at any stage of poisoning at all concentrations used. On the other hand, when the American cockroaches were exposed to jars coated with 1 mg of a 60% 3B solution, the insects showed hyperexcitation. These data suggest that the input form is a determining factor in the mode of action of these essential oils. These observations support the idea that 3B is not a type of poison that attacks the Na + channel as a target
P1721 / 99MX main. The fact that the strain resistant to Kdr (with a mutated Na + channel that makes it insensitive to DDT and pyrethroids) did not show cross resistance to 3B also supports this diagnosis. In accordance with the above circumstances, where it was found that all the main known sites of action of the insecticides were insensitive to 3B, with the exception of the antagonistic effect on the octopamine receptor, the possibility was considered that the mode of action of this group of chemical compounds is completely new. It was noted that the toxicity of 3B varies according to the site of application, at least in the case of the American cockroach. This observation indicates that 3B is probably not as systemic and if a site produces a high toxicity, its target will probably be located very close to that site of application. In view of the locomotor difficulty observed in the American cockroaches treated in the central sternum, the reasoning was made that the thoracic ganglia could be affected. When 3B (250 mg in 0.4 μl of acetone) was injected into the thorax of a live cockroach and contractions were induced in the hind paw by means of external electrical stimuli applied to the outside of the body, the ability of the paw muscles to respond to the stimuli
P1721 / 99MX disappeared completely in less than one minute (Figure 2). When 3-B was applied to the paw in isolation when directly providing electrical stimuli, no effect of 3B was found (Figure 3). These data suggest that the effect of 3B is on the nervous system and not on the muscles. The control tests using acetone (0.4 μl) without any 3-B showed no effects (Figures 4 and 5). This possibility was further tested using the 6th. abdominal ganglion and studying the transmission of signals from the mechanoreceptors of the fences generated by inflation with air. To this end, the abdominal cavity was opened, exposing the entire abdominal nervous cord. A suspension solution of 3B in 20 μl of insect saline was applied directly to the entire abdominal nerve cord. The results were dramatic, producing the complete blockage of transmission at 250-500 PPM in less than 5 minutes from the time of application (Figure 6). The blocking effect of 3B was evident even at 10 PPM, producing visible effects in 15 minutes. These results clearly indicate that 3B is a non-systemic nerve blocker. An additional study was conducted on the cockroaches to determine the effect of other chemical compounds of the present invention on the heart rate of the insects. The experimental conditions were as previously described
P1721 / 99MX in the application of 300 μg of the respective chemical compound to the entire abdominal nervous cord. Each group of insects was comprised of three individuals. All heart rates were observed and the counts were recorded three times for each individual, that is, nine accounts before the introduction of the chemical compound and nine accounts 30 minutes after the application of approximately 300 μg of the chemical compound. The data from these heartbeat tests are in accordance with the "in passing" test previously described. The following chemical compounds showed a measurable change in heart rate thirty (30) minutes after the application of the chemical compound: terpineol, eugenol, phenyl ethyl alcohol, benzyl acetate and benzyl alcohol. The following mixtures also showed a measurable change in heart rate: terpineol with eugenol, terpineol with phenyl ethyl alcohol and eugenol with phenyl ethyl alcohol. The toxicity of individual chemical compounds was also determined by topical application to Asian worm worms 4a. Early chrysalis (Spodopter litura) (15-20 mg live by weight) and measurement after 24 hours (Table 9).
Table 9: Toxicity of chemical compounds of the
P1721 / 99MX present invention. 95% confidence interval interval confidence LD90 confidence
Compues o (μg / larva) 95% (μg / larva) 95% α-terpineol 156.0 148.7-163.7 206.4 190.4-249.9
Eugenol 157.7 149.9-165.8 213.0 194.8-263.3
Alcohol LD50 > 250 cinnamic (+) -terpinen- 130.4 121.8-139.5 205.8 180.2-283.8
4-ol (-) -terpinen- 122.9 108.1-139.7 276.0 202.4-583.9
4-ol-carvacrol 42.7 37.7-48.3 73.8 55.7-142.0
D-pulegone 51.6 49.0-54.4 69.7 62.3-91.3 t-anetole 65.5 61.7-69.6 98.8 88.4-129.1 thymol 25.5 22.9-28.3 46.8 38.5-74.5 citronella 111.3 103.9-119.1 153.4 130.8-223.5
During the establishment of the LD50 dose, it was observed that all larvae treated with pulegone, even at the lowest doses tested, were paralyzed almost immediately. However, at lower doses, many or most of these larvae exceeded this effect, while at higher doses the larvae succumbed. To determine if the observed sublethal toxicity resulted in some long-term effect, the subsequent growth of the larvae treated at the three lowest doses (20.31 and 49 μg per larva) was monitored and compared with the control growth (larva no. treated) at 72 and 100 hours after treatment, (Table 10).
P1721 / 99MX Table 10: Growth of the larvae exposed to the chemical compounds of the present invention. Control 20 μg / larva 31 μg / larva 40 μg / larva
Mortality 0 0 2 52 (5) Live weight- 148 mg 109 81 52 72 hr. Live weight- 363 mg 289 248 163 110 hr.
The results indicate that the subsequent larval growth of the survivors of the highest dose was drastically delayed. More importantly, the effect is also observed (and so significantly) at the two lowest doses, which almost did not produce mortality. Therefore, exposure to uniform sublethal doses can have significant consequences for larvae. Dry powder formulations were prepared using the chemical compounds of the present invention. The examples listed below are for mixture 3B as previously described
(cinnamic alcohol, eugenol, and alpha terpineol). However, these examples are for illustrative purposes only and do not limit the range of active chemical compounds. Other mixtures and individual chemical compounds can also be used. The suggested mixtures are phenyl ethyl alcohol, benzyl alcohol, eugenol and alpha terpineol (3C) and acetate
P1721 / 99MX benzyl, benzyl alcohol, phenyl ethyl alcohol, cinnamic alcohol and alpha terpineol (2D). The mixtures listed herein are not limiting but are typical and the present invention is not limited to these mixtures. The procedure was to place the powder components in a 500 ml capsule and apply the chemical compound (usually a liquid) to the powder. The powder and chemical compound mixed in the vessel were placed in an electric drum for drying for about 30 minutes. Approximately 1 cc of the resulting dry powder was applied to a Whatman No. 1 filter paper in a 9 cm Petri dish. The powder dispersed evenly with a brush of camel hair. A control consisting only of the powdered components without the chemical compound of the present invention was used. The following compositions were prepared: (Tables 12a-12c) Table 12a% by weight components amount 40 20 gr diatomaceous earth 20 10 gr calcium carbonate 20 10 g sodium bicarbonate 10 5 gr Hi-Sil 233 10 5 gr active ingredient *
P1721 / 99MX Table 12b% by weight number of components 40 20 gr diatomaceous earth 23 11.5 gr calcium carbonate 20 10 g sodium bicarbonate 10 5 gr Hi-Sil 233 17 3.5 gr active ingredient * Table 12c% by weight number of components 40 20 diatomite earth 25 12.5 gr calcium carbonate 20 10 g sodium bicarbonate 10 5 gr Hi-Sil 233 5 2.5 gr active ingredient * * the active ingredient was a mixture of the chemical compounds of the present invention.
The mixtures were tested by placing ten (10) common arrieras ants inside respective petri dishes, which were then covered. The time for irreversible knockdown (KD) to occur was determined from periodic irregular observations. KD were considered to be insects when they were on their back or could roll over on their backs and could not straighten themselves within a period of at least two (2) minutes. The KT-50 and the KT-90 (respectively the time for a KD of 50%
P1721 / 99MX and 90%) were calculated by interpolation of the KD between the times when data was collected. The 10% mixture (Table 12) had a 50% KT of 5 minutes 50 seconds and a 90% KT of 6 minutes 40 seconds. For the 7% mixture (Table 12b) the 50% KT was 3 minutes 40 seconds and the 90% KT was 4 minutes 40 seconds. The 5% mixture (Table 12c) had a 50% KT of 2 minutes 33 seconds and a 90% KT of 3 minutes 45 seconds. The above data are examples that clearly demonstrate the effectiveness of the mixture of chemical compounds above concentrations ranging from 5 to 10% by weight of the active ingredients. These are typical but not limiting examples. It has also been shown that concentrations as low as 0.1% by weight are effective for some individual chemical compounds and for various mixtures of chemical compounds. Much higher concentrations can also be used. As an example of a high concentration, an emulsifiable concentrate has the following formulation:
P1721 / 99MX Ingredient Purpose% by weight 3B ingredient 90.0 active Dodecyl benzene sulfonate emulsifier 6.6 sodium Pareth-3 C12-15 emulsifier sulfonate 2.0 Sodium POE 20 Sorbitan emulsifier Monooleate 1.4
Another emulsifiable concentrate is: Ingredient Purpose% by weight
3B active ingredient 90.0
Castor oil (40 emulsifier 10.0 mol EO)
The concentrate was diluted with up to 50-70 parts of water per 1 part of concentrate to provide an effective aqueous medium. Although these examples are for mixtures 3B and 3C, the formulation is not limited in this way and an emulsifiable concentrate can be prepared from any of the individual chemical compounds of the present invention or from any combination of mixtures of the individual chemical compounds. The mixture of emulsifiable concentrate 3B was diluted in tap water and sprayed on cabbage and bean plants to evaluate its effectiveness against Asian worm worms and spider mites Tetranychus urti falls respectively. Everybody
P1721 / 99MX values are based on a minimum of four doses with five replicates and ten worms or thirty adults and / or deutonymph mites per replicate. The reported values represent the proportions of water to formulation (ie, dilution rate) (for example, LD50 of 46.8 means a water to emulsifiable concentrate ratio of 46.8: 1). Mortality was assessed at 24 hours (Table 13).
Table 13 Mortality of the emulsifiable mixture of the 3-B Asian worm worm mix LDS50 (95% CI) = 46.8 (44.0-49.8) with age 3 days LDS50 (95% CI) = 30.6 (27.2-40.7) Asian worm worm LDS50 (95% CI) = 53.0 (49.6-56.7) with age 5 days LDS50 (95% CI) = 33.7 (29.7-45.6) spider mite of two LDS50 (95% CI) = 82.3 (76.5-88.5) spots LDS50 (95% CI) = 55.9 (49.3-75.5)
The formulation of the diluted 3B emulsifiable concentrate shows good efficacy against both ages of worms and even better efficacy against spider mites. The worms with age of 5 days are of approximately the same size as the larva of the nocturnal butterfly with back of mature diamond (last chrysalis), a potential white species. Also of importance, it was observed that the sublethal concentrations clearly prevented the feeding and, therefore, the damage to the plant. At a dilution of 50: 1, 60: 1 and 70: 1, mortality
Larval P1721 / 99MX is only 64%, 42% and 12% respectively. However, there is minimal damage by feeding the surviving larva. As shown in Figure 7, discs of cabbage leaf with 3-B emulsifiable concentrate diluted 50: 1, 60: 1 and 70: 1 have areas consumed (ac) after 24 hours, less than 5% -30 % compared to a control (without 3-B) of more than 80% of the area consumed. Another example of a high concentration is a wettable powder having the following formulation:
Ingredient Purpose% by weight
3B active ingredient 50.0
Silica, hydrated and amorphous absorbent 41.5
Alkyl naphthalene sulfonate dispersant 3.0 sodium Dioctyl sufosuccinate wetting agent 0.5 sodium Dodecyl benzene sulfonate emulsifier 5.0 sodium
A part of this powder is mixed with up to 30-50 parts of water to provide an effective pesticide. This example is for mixture 3B but is not limited and can be prepared with any of the individual chemical compounds of the present invention or with any combination of mixtures of the individual chemical compounds. A waterproof powder can be prepared
P1721 / 99MX using any of the individual chemical compounds or a mixture of any of the chemical compounds of the present invention. The following formulation is representative in which the 3C mixture is equal parts by weight of benzyl alcohol, phenyl ethyl alcohol and terpineol:
Ingredient Purpose% by weight
3C active ingredient 5.0
Land of diatomite loading ingredient 75.0
Hydrophobic absorbent silica 20.0
The following formulations represent two easy to use sprays, representative of mixtures 3B and 3C but can be used for other mixtures and for individual chemical compounds of the present invention:
Ingredient Purpose% by weight
3B active ingredient 5.0
Castor oil (40 moles emulsifier 2.7 of EO) POE 20 Sorbitan emulsifier Monooleate 0. 6
Alkyl benzene sulfonate emulsifier 1. 7 isopropyl amine Water di luyente 9 0. 0
P1721 / 99MX Ingredient Purpose% by weight
3C active ingredient 5.0
Castor oil (40 moles emulsifier 2.7 of EO) POE 20 Sorbitan Monooleate emulsifier 0.6
Emulsifier alkyl benzene sulfonate 1.7 isopropyl amine Water diluent 90.0
The individual chemical compounds of the present invention and the mixtures can also be used as an aerosol spray. Insofar as it is not limited to them, the following formulation is typical:
Ingredient Purpose% by weight
3C active ingredient 5. 0
Propanol solubilization agent 1. 5
Propellant carbon dioxide 3. 5
Hydrocarbon solvent 90. 0 isoparaffinic
A pesticidal shampoo has the following composition, wherein the active ingredient is an individual chemical compound of the present invention or mixture of chemical compounds:
P1721 / 99MX Ingredient% by weight Active ingredient 0.5 - 10.0 Sequestrant for hard water 0.5 - 3.0 Emulsifier (s) 1.0 - 5.0 Thickener (s) 0.5 - 5.0 Foam stabilizer 0.5 - 2.0 Detergent 5.0 - 20.0 pH regulator 0.1 - 2.0 ( for the required pH) Dye / dye 0.01 -Conservator 0.01 - 1.0 Deionized water up to 100%
The gel formulations have been prepared as follows: Color Blue 3.00% Active ingredient 15.00% Ethanol 0.42% Carbopol 934 0.42% -10% Sodium hydroxide in water 81.16% Water Color Yellow 3.00% Active ingredient 30.00% Ethanol 0.42% Carbopol 934 0.42 % -10% Sodium hydroxide in water 66.16% Water The active ingredient is an individual chemical compound of the present invention or a
P1721 / 99MX mix thereof. A dry powder formulation consists of mixing an alkaline earth metal carbonate, such as, calcium carbonate, an alkali metal bicarbonate, such as, sodium bicarbonate, the active ingredient, an absorbent material, such as to be diatomaceous earth and a filler ingredient, such as HiSil 233. The relative concentrations of the mixture are preferably about 20% -30% alkaline earth metal carbonate, 15% -25%, alkali metal bicarbonate, 0.1 % -5% active ingredient, 30% -50% absorbent material and 5% -15% loading ingredient (all by weight). The powder granules are preferably ground to a size of less than 100 microns. The active ingredients can be individual chemical compounds of the present invention or mixtures thereof. In all the aforementioned examples, it may be desirable to add a trace amount (less than 2%) of a material to provide a pleasant smell, not only for aesthetic reasons but also to identify the areas of a building that have received the treatment. The pleasant smell can be vanilla, cinnamon, floral and other scents that are acceptable to consumers. Pleasant smells are not limited to examples
P1721 / 99MX provided herein. Obviously, many modifications can be made without deviating from the basic spirit of the present invention. In accordance with the foregoing, those skilled in the art will appreciate that within the scope of the appended claims, the invention may be practiced in a manner different from that specifically described herein.
P1721 / 99MX
Claims (22)
- NOVELTY OF THE INVENTION Having described the present invention, it is considered as a novelty and, therefore, what is claimed as property is contained in the following CLAIMS I 1. A method for interacting with the neurotransmitters of the octopamine receptor sites in invertebrates and / or in the larvae thereof, in order to kill and / or affect the feeding habits and the growth of the invertebrates and / or the larvae thereof without affecting in a similar way to mammals, fish or poultry, the method comprises: selecting an afflicting agent based on the ability of the afflicting agent to interact as an agonist or an antagonist on the neurotransmitters of the octopamine receptor sites in the invertebrates and / or larvae thereof, the afflicting agent comprises a compound naturally present having a six-membered carbon ring structure wherein the carbon ring is replaced by at least one group fu oxygenated oxygen and the structure of the afflicting agent is devoid of nitrogen; apply to the invertebrates, their larvae and / or their habitat, a pesticide composition of a vehicle with the afflicting agent. where the afflicting agent is present
- P1721 / 99MX in the pesticidal composition in an amount effective to interact as an agonist or an antagonist on the octopamine receptor sites to kill or affect the feeding and growth of invertebrates and / or their larvae and is not detrimental to mammals, fish or poultry. The method according to claim 1, comprising applying the mixture to insects, worms, arachnids, larvae thereof and / or their habitat.
- 3. The method according to claim 2, wherein the afflicting agent is selected from the group consisting of anetole, benzyl acetate, benzyl alcohol, carvacrol, cinnamic alcohol, augen, ethyl phenyl alcohol, pulegone, alpha terpineol and mixtures thereof. same.
- 4. A method according to claim 3, wherein the mixture is selected from a group consisting of cinnamic alcohol, eugenol with alpha terpineol; benzyl alcohol, phenyl ethyl alcohol, eugenol with alpha terpineol and benzyl acetate, benzyl alcohol, phenyl ethyl alcohol, cinnamic alcohol with alpha terpineol.
- A method according to claim 4, wherein the weight percent range of the mixture is cinnamic alcohol 20% -35%, eugenol 10% -50% and alpha terpineol 10% -50%.
- 6. A method according to claim 1, further comprising adding to the mixture a material thatP1721 / 99MX has a pleasant smell.
- 7. A method according to claim 1, wherein the carrier is water having at least one emulsifier therein.
- 8. A method according to claim 1, wherein the carrier is a wettable powder.
- 9. A method according to claim 1, wherein the carrier is an impermeable powder.
- 10. A method according to claim 1, wherein the carrier is an aerosol.
- 11. A method according to claim 1, wherein the carrier is a dry powder.
- 12. A method according to claim 1, wherein the mixture is in the form of an emulsion.
- 13. A method according to claim 1, wherein the mixture comprises an oil.
- 14. A method according to claim 13, wherein the oil is galoxolide and the affectating agent is eugenol.
- 15. A method according to claim 14, wherein the mixture comprises about 30% -60% by weight of galoxolide and about 40% -70% by weight of eugenol.
- 16. A method according to claim 13, comprising dispersing about 1 mg of the mixture over an area of about 10 cm2.
- 17. A method according to claim 1, wherein the action as an agonist or antagonistP1721 / 99MX on the receptor sites is produced by external contact of the invertebrates and / or their larvae with the afflicting agent.
- 18. A method to kill and / or affect the eating habits of invertebrates and / or their larvae, the method comprises: selecting the afflicting agents based on the agonist or antagonist activity of the afflicting agents with the neurotransmitters of the sites Octopamine receptors in invertebrates. apply to invertebrates, to the larvae of the same and / or to their habitat the afflicting agents as a mixture of cinnamic alcohol, eugenol and alpha terpineol. the mixture will be mixed with a carrier to produce a practically uniform pesticidal composition, wherein the mixture of the afflicting agents is present in the pesticidal composition in an amount effective to interact as an agonist or an antagonist on the octopamine receptor sites to kill or affect the eating habits and growth of invertebrates and / or their larvae and is not harmful to mammals, fish and poultry. The method according to claim 18, wherein the range of percent by weight of the mixture is cinnamic alcohol 20% -35%, eugenol 10% -50% and alpha terpineol 10% -50%.
- P1721 / 99MX
- 20. A method according to claim 18, comprising applying the pesticidal composition to insects, worms, arachnids, larvae thereof and / or their habitat wherein the afflicting agents make external contact with insects, worms, arachnids and the larvae of them.
- 21. A method to kill and / or affect the feeding habits and growth of invertebrates and / or larvae thereof, the method comprises: selecting the afflicting agents based on the selected afflicting agents that interact as an agonist or a antagonist with the neurotransmitters of the octopamine receptor sites in invertebrates; apply to the invertebrates, their larvae and / or their habitat, a pesticidal composition comprising a carrier and the afflicting agents as a mixture selected from the group consisting of: (1) cinnamic alcohol, eugenol and alpha terpineol; (2) benzyl alcohol, phenyl ethyl alcohol, eugenol and alpha terpineol; (3) ethyl phenyl alcohol, eugenol and alpha terpineol; and (4) benzyl acetate, benzyl alcohol, phenyl ethyl alcohol, cinnamic alcohol and alpha terpineol; wherein the mixture of afflicting agents is present in the pesticidal composition in an amount effective to interact as an agonist orP1721 / 99MX antagonist on octopamine receptor sites to kill or affect the eating habits and growth of invertebrates and / or their larvae and is not harmful to mammals, fish or poultry.
- 22. The method according to claim 21, which comprises applying the pesticidal composition to insects, worms, arachnids, larvae thereof and / or their habitat, wherein the afflicting agents make external contact with insects, worms, arachnids and larvae. thereof.P1721 / 99MX
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US08870560 | 1997-06-06 |
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MXPA99011311A true MXPA99011311A (en) | 2001-05-17 |
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