CN101176447A - Application of aubepine as liveness composition for driving and avoiding arthropod - Google Patents

Abstract

The invention discloses the application of the anisaldehyde as the active ingredient for repelling the arthropods. The test result indicates that the anisaldehyde has the obvious repelling activeness with an effective protection time of 4.3 plus or minus 0.5h for the human skin application, which is superior to the previously reported fragrant phytol, the citronellal, the linalool and the citral with repelling activeness. The repelling activeness of cockroaches and ticks both is superior to DEET.

Description

Anisaldehyde is as the application of repellent arthropods active ingredient

Technical field

The present invention relates to the new purposes of anisaldehyde.

Background technology

Anisaldehyde, English name is: p-Anisaldehyde or 4-Methoxy benzaldehyde, 4-methoxy-Benzaldehyde 4-anisaldehyde), has another name called P-methoxybenzal-dehyde, 4-methoxybenzaldehyde, p-anisaldehyde.CAS:123-11-5, molecular formula: C ₈H ₈O ₂, molecular mass: 136.15, boiling point: 248-249 ℃, relative density 1.1191 (15/4 ℃), refractive index refractive index 1.5730.Be soluble in organic solvents such as ethanol, ether, acetone, chloroform for colourless to light yellow transparent oily liquid, water insoluble, structural formula is as follows:

This compound extensively is present in oecoeclades falcata and belongs in Angraecum, Cypripedium Cypripedium, Fragaria Fragaria, angle Foeniculum Hypecoum, Nymphaea Nymphaea, eyebrow Cymbidium Ophrys and the Genus Syringa Syringa plant, has the fragrance of crab apple.

In research and application in the past, these product are temporary transient in China GB2760-86 regulation to be allowed to use to be flavorant; As the good brightener of non-cyanogen galvanization DE additive, it can improve anode polarization in the current range of broad, obtains bright coating; Being used to make antimicrobial medicine oxyammonia benzylpenicillin etc. at medical industry, is the intermediate of antihistamine drug.

In the repellant research field, (N, N-diethyl-3-methylbenzamide DEET) since the tool repellent activity, were widely used as the most effective repellant always from report Metadelphene in 1954.Yet the problem of relevant for many years its toxicity and safety aspect is subjected to people's attention always, as document: N.Engl.J.Med., 264:289,1961; N.Engl.J.Med., 307 (21): 1341,1982; Int.J.Dev.Neurosci, 2004 contents of being reported.

Therefore, the scientist of countries in the world is strengthening seeking safer, effective repellent material.From documents and materials in recent years, research to the plant resource repellant is more paid attention to, resemble states such as the U.S., India, Japan, Thailand, Singapore, South Africa, Kenya, Malaysia and all actively developing research, attempt from plant, to find more efficiently repellent thing.

Summary of the invention

The purpose of this invention is to provide the application of anisaldehyde, to satisfy people's needs as repellent arthropods active ingredient.

The present inventor discovers, therefore the repellent activity that anisaldehyde is good to the arthropods tool can be used for the repellent arthropods;

Described arthropods comprises Insecta or arachnids etc., the species that the Arthropoda on the animal classification meaning (Arthropoda) is contained.

For the ease of using, anisaldehyde can be mixed with one or more carriers, adopt conventional method preparation to become preparation;

Said preparation comprises the anisaldehyde and the carrier of repellent arthropods effective dose, and preferred, in the preparation, the weight concentration of anisaldehyde is 0.5-99%;

Said carrier comprises more than one in organic solvent, excipients, filler, adhesive, wetting agent, disintegrant, surfactant, absorption carrier, lubricant, stabilizing agent or the blowing agent etc. of agricultural chemicals and hygienic insecticide field routine;

Said organic solvent such as ethanol, acetone, ethyl acetate or hexane;

Excipients such as polyethylene glycol, agar, sodium alginate or sodium carboxymethylcellulose;

Filler such as calcium carbonate, calcinated argil, starch or dextrin;

Adhesive such as carboxymethyl cellulose, shellac, vinyl acetate resin or rosin;

Wetting agent such as sodium alkyl sulfonate, dialkyl succinylsuccinate ester sodium sulfonate, quaternary amine or aromatic sulphonate;

Disintegrant such as Ac-Di-Sol, hydroxypropul starch, crospolyvinylpyrrolidone or dried starch;

Surfactant such as DDAO, alkyl diphenyl ether disulfonate, lauryl sodium sulfate or stearine;

Absorption carrier such as diatomite, white carbon, talcum or bentonite;

Lubricant such as dolomol, talcum powder, stearic acid or month pure magnesium sulfate of extension;

Stabilizing agent such as epoxidized cyclohexene, isoamyl alcohol, dialkyl group succinate sodium sulfonate or turpentine oil;

Blowing agent such as Celogen Az, unifor, dinitrosopentamethylene tetramine or azodiisobutyronitrile;

The formulation of said preparation comprises liquor, emulsion, paste, creme, gel, spray, finish, tablet, pulvis, soap wax stone, shampoo, coating, fiber or fabric etc.

The using method of preparation of the present invention can be according to user's requirement and formulation, adopts to smear, burn or be positioned over space method such as volatilize naturally.

Following experimental data is in order to understand the present invention better, but and does not mean that any limitation of the invention.

1. the repellent compound is measured the repellent activity of mosquito

Laboratory sample:

DEET (95.4%), Jiangsu Province Huasheng Chemical Co Ltd, Danyang produces; Linalool (99%) is available from Sigma company; Geraniol (96%), citronellal (92%), citral (97%) is provided by Aipu Flavouring Co., Ltd., Shanghai; Anisaldehyde (99%) is available from Shanghai chemical reagent Co., Ltd.

Experimental animal:

Aedes albopictus (Aedes albopictus Skuse) Shanghai strain system, the female worm of not sucking blood in 5-8 days is selected in test for use.

Experiment condition:

25 ± 1 ℃; Humidity 70 ± 5%RH.

Experimental technique:

Individuality is coated with skin effective protecting time test to carry out with reference to the indoor harmacological effect evaluation method GB/T 17322.10-1998 of agriculture chemical registration hygienic insecticide.

Experimental result:

As shown in table 1, the result represents with mean value ± standard error.

Table 1. repellent thing human body is coated with the skin effective protecting time

Compound	Test number (TN) (inferior)	Effective protecting time (h) ± SE
			Anisaldehyde anisaldehyde geraniol geraniol citronellal citronellal linalool linalool citral citral	6 6 6 6 6	4.3±0.5 4.0±0.4 2.2±0.2 1.5±0.4 0.75±0.5

Originally studies show that, with the compound of reporting the tool repellent activity (geraniol, citronellic acid, J.Med.Entomol.41 (4): 726,2004; Linalool, Application No.: 20050090536; Citral, Phytomedicine 9 (3): 259,2002) compare, the tangible repellent activity of anisaldehyde tool, human body are coated with the skin effective protecting time and reach 4.3 ± 0.5h, are better than geraniol, citronellal, linalool and citral.

2. the repellent compound is measured the repellent activity of cockroach

Laboratory sample and experiment condition: as above 1 is described.

Experimental animal: Groton bug (Blattella germanica) male insect, age in days 7-14d.

Experimental technique: by 1,10,100,1000 μ g/cm ²The laboratory sample that dosage will be dissolved in methyl alcohol drips in diameter 15cm ²Half of filter paper, second half is the methyl alcohol blank, after waiting to dry, this filter paper is placed the hollow staving bottom of a diameter 16cm, high 8cm, the staving inwall is smeared vaseline, in case the examination worm escapes.During test, introduce an examination of staving worm, the time that the interior Groton bug of 300s avoids test paper is calculated in observation at every turn, and anti-repelling properties is calculated as follows:

Experimental result:

As shown in table 2, the result represents with mean value ± standard error.

Table 2. repellent compound is to the scattering ratio result of cockroach

Compound	Dosage (μ g/cm 2)
						0	1	10	100	1000
	DEET anisaldehyde anisaldehyde	46.0±5.4 46.0±5.4	53.7±1.4 69.6±4.4	59.5±7.8 73.9±5.8	63.9±3.8 75.8±4.2						88.4±8.6 96.4±5.3

As shown in table 2, anisaldehyde shows as tangible repellent activity to Groton bug, and in each concentration group, its repellent effect all is better than DEET, along with the increase of effective dose, at 1000 μ g/cm ²The time, scattering ratio can be up to 96.4%.

3. the repellent compound is measured the repellent activity of tick

Laboratory sample and experiment condition: as above 1 is described.

Experimental technique: examination person's forearm top and bottom (10cm at interval), smear respectively that the 10cm place is not coated with medicine between the trial drug, two ends of the wide 2cm of a circle, the tick alive (each 5) that to from thick grass, catch with cloth flag method, be placed on and do not smear the medicine place, observe the creep situation of tick on arm in the 5min, counting is crossed the tick sum of smearing the medicine position, observes once every 1h.

Experimental result:

As shown in table 3, the result represents with mean value ± standard error.

Table 3 repellent compound is to the repellent result of tick

Group	Test number (TN)	Repellent effect (only)
							1h	2h	3h	4h	5h
		Blank DEET anisaldehyde anisaldehyde	3 3 3	4.6±1.0 0 0	5±0 0 0	4.3±0.5 0 0						5.0±0 0 0	4.6±0.2 1.6±0.5 1.3±0.3

As shown in table 3, anisaldehyde has tangible repellent activity to tick, and the repellent time is up to 5h, and behind dispenser 5h, 1.6 ± 0.5 examination worms are crossed DEET and handle band, and only 1.3 ± 0.3 of anisaldehyde processed group are better than DEET.

From existing documents and materials, different types of insect only is the difference of sensitivity to the difference of repellant susceptibility, do not find that sense of smell experiences the fundamental difference on the respond style, even to the member in the annelids evolution chain repellent thing all had essentially identical physiological reaction (Cell.96:725,1999 arthropods; J Med.Entoml.14 (5): 536,1978).From applicant's research, anisaldehyde is to mosquito, the cockroach of Arthropoda Insecta, and the tick class of arachnids all has repellent activity preferably, also shows as certain broad spectrum activity.

Embodiment

Embodiment 1

A kind of preparation of solid mosquito repellent

Below all be weight percentage.

35% anisaldehyde, 2% menthol, 13% polyethylene glycol are mixed at normal temperatures, add 50% paraffin then, put and heat in the container, stir, mix to 55 ℃, till solids dissolves fully, add colorant again and stir evenly, warming up is poured into mould molding, naturally cooling, after treating to solidify fully, taking-up can obtain solid mosquito repellent.

Embodiment 2

A kind of preparation of shampoo for pets:

Below all be weight percentage.

With sodium sulfate of polyethenoxy ether of fatty alcohol 12%, fatty alcohol diethanol thiamines 3%, imidazoline 3%, sodium lauryl sulfate 1%, betain 3%, distilled water 64%, sodium chloride 4%; Behind the stirring and evenly mixing, be heated with stirring to 90 ℃ of constant temperature 30 minutes; Add preservative sodium benzoate 2%, stir when temperature drops to 45 ℃, add anisaldehyde 8% at last, stir, stop to stir and left standstill 12 hours, filter bottling.

Embodiment 3

A kind of preparation of culicifuge

Below all be weight percentage.

With anisaldehyde 8%, algin 7%, pigment 3%, dodecyl sodium sulfate 10%, water 62% are put into vessel in heating to 80 ℃ stirring 50 minutes, reduce the temperature to 40 ℃ then, add alcohol 10%, be warmed up to 75 ℃ again, stir and cool to 40 ℃ of packing after 60 minutes and get product.

Claims (8)

1. anisaldehyde is as the application of repellent arthropods active ingredient.

2. application according to claim 1 is characterized in that, described arthropods comprises Insecta or arachnids, species that the Arthropoda on the animal classification meaning (Arthropoda) is contained.

3. the application of anisaldehyde in preparation repellent arthropods preparation.

4. application according to claim 3 is characterized in that, said preparation comprises the anisaldehyde and the carrier of repellent arthropods effective dose.

5. application according to claim 4 is characterized in that, in the preparation, the weight concentration of anisaldehyde is 0.5-99%.

6. application according to claim 3, it is characterized in that said carrier comprises more than one in organic solvent, excipients, filler, adhesive, wetting agent, disintegrant, surfactant, absorption carrier, lubricant, stabilizing agent or the blowing agent of agricultural chemicals and hygienic insecticide field routine.

7. application according to claim 3 is characterized in that, the formulation of said application comprises liquor, emulsion, paste, creme, gel, spray, finish, tablet, pulvis, soap wax stone, shampoo, coating, fiber or fabric.

8. application according to claim 3 is characterized in that, described arthropods comprises Insecta or arachnids, species that the Arthropoda on the animal classification meaning (Arthropoda) is contained.