Classifications

• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
  • A01N37/06—Unsaturated carboxylic acids or thio analogues thereof; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
  • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
  • A01N63/00—Biocides, pest repellants or attractants, or plant growth regulators containing microorganisms, viruses, microbial fungi, animals or substances produced by, or obtained from, microorganisms, viruses, microbial fungi or animals, e.g. enzymes or fermentates
  • A01N63/10—Animals; Substances produced thereby or obtained therefrom

Definitions

• TECHNICAL FIELD This invention is in the field of topical insect repellents. More particularly, effective, natural and safe biting fly repellents comprising oil from ratites, which include rheas, emus, ostriches, kiwis and cassowaries, active fractions of ratite oil and compositions comprising ratite oil or active fractions thereof and citronella or citronella and saponin are provided. Compositions comprising ratite oil or active fractions thereof and at least one other insect repellent are also provided. In addition, compositions for repelling biting insects comprising a mixture of fatty acids are provided. Methods for repelling insects comprising applying such compositions are also provided. BACKGROUND ART
• This invention relates to a compositions and methods for repelling insects, and more particularly to compositions and methods for repelling biting insects such as mosquitoes and biting flies, for example, ceratopogonid flies, using a natural ingredient, oil from ratites, which include rheas, emus, ostriches, kiwis and cassowaries, active fractions of such oils and compositions comprising ratite oil or active fractions thereof and at least one other insect repellent such as citronella or DEET, optionally, further comprising saponin. Also included are compositions for repelling insects comprising a mixture of certain fatty acids and methods for repelling insects comprising application of such compositions comprising certain fatty acids.
• Known natural oils that repel insects include rotundial (from the leaves of Vitex rotundifolia, Watanabe K et al. (1995) Biotech Biochem 59(10):1979-1980); citronella oil (e.g. U.S. Patent No. 5,346,922); eucalyptus oil (Watanabe et al. (1993) J. Agric. Food Chem. 41:2164-2166); neem oil (Sharma VP et al. (1993) J. American Mosquito Control Association 9(3):359-360); and oil of Hedeoma pulgioides, oil of anisum and oil of chrysanthemum (U.S. Patent No. 5,208,209).
• Another natural oil that has repellent activity is saponin (Croda from Sapindus). Saponin has been shown to repel lice and also serves to improve the spreading consistency of repellent compositions and reduce greasiness.
• DEET N,N-diethyl-m-toluamide
• the active fractions of the naturally-occurring insect repellents are also largely unknown.
• Methods of resolving heterogeneous compounds into chemical species are well- known in the art.
• silica gel flash chromatography provides for high speed resolution of organic compounds (see, e.g., U.S. Patent No. 4,293,422). After separation, the eluted fractions can be recovered and tested for the activity of interest.
• Bencsits U.S. Patent No. 5,589,181
• the Cl to C4 fatty acid alkyl esters can be obtained from C5 to C9 fatty acids present in rape-seed oil, sunflower oil, peanut oil, peanut butter, soy oil, safflower seed oil, cuphea oil, coconut oil, palm kernel oil, palm oil and fish oil.
• the fatty alcohols may be obtained from paraffin and/or ethene. Bencsits further discloses that in order to slow down the evaporation of the active substances, the
• a carrier can be provided consisting of natural or nature-identical vegetal and/or animal oils. Bencsits does not, however, teach or suggest the compositions of the instant invention.
• compositions comprising ratite oil or active fractions thereof and compositions comprising ratite oil or active fractions thereof in combination with at least one other insect repellent such as citronella, DEET or saponin.
• Compositions comprising mixtures of fatty acids that effectively repel insects are also needed.
• compositions for repelling insects comprising topically applying compositions comprising ratite oil, active fractions thereof or mixtures of fatty acids and at least one other insect repellent such as citronella or DEET to the skin of a subject are also provided.
• the invention further provides compositions for repelling biting insects comprising active fractions of ratite oil or a mixture of fatty acids or compositions comprising ratite oil, active fractions thereof or a mixture of fatty acids and at least one other insect repellent such as citronella, DEET or saponin.
• FIGURES show the number of mosquitoes present on filter paper treated with water, sucrose or sucrose and diluted emu oil (sample 776) at 2.5 minute intervals.
• the solid triangles show water-treated filter paper controls.
• the open squares show sucrose-treated filter paper.
• the solid squares show sucrose-treated paper overlaid with undiluted sample 776.
• the open triangles show sucrose-treated paper overlaid with a 50% dilution of sample 776.
• the open circles show sucrose-treated paper overlaid with sample 776 diluted to 25%.
• Figure 2 shows the number of mosquitoes present on filter paper treated with water, sucrose, or sucrose and fractions of sample 776 at 5 minute intervals.
• the solid squares show water-treated paper.
• the open squares show sucrose-treated paper overlaid.
• the solid triangles show sucrose-treated paper overlaid with a sample 776.
• the open triangles show sucrose-treated paper overlaid with fraction FI.
• the solid circles show sucrose- treated paper overlaid with fraction F2.
• Figure 3 shows the ⁇ NMR spectrum of the FI fraction of emu oil.
• Figure 4 shows the 'H NMR spectrum of the F2 fraction of emu oil.
• Figure 5 shows the average number of mosquitoes biting test limbs per ten minute intervals.
• the present invention provides methods of repelling insects, particularly biting insects, using oil from ratites, which include rheas, emus, ostriches, kiwis and cassowaries, and is a natural and safe substance.
• the invention also includes methods of repelling insects comprising applying active fractions of ratite oils.
• the present invention also provides compositions for repelling insects comprising fatty acids that have a repellent effect.
• the invention also provides for methods of repelling insects comprising applying such compositions comprising mixtures of fatty acids topically.
• pure ratite oil is applied to the skin.
• diluted ratite oil is topically applied.
• an active fraction of ratite oil is applied to the skin.
• a composition comprising ratite oil or an active fraction thereof and at least one other insect repellent is applied to the skin.
• suitable insect repellents that can be combined with ratite oil or an active fraction thereof include, but are not limited to, N,N-diethyl-m-toluamide (DEET) citronella oil, rotundial oil, eucalyptus oil, neem oil, oil of Hedeoma pulgioides, oil of anisum, oil of chrysanthemum and saponin.
• DEET N,N-diethyl-m-toluamide
• the present invention further provides compositions for repelling biting insects comprising ratite oil, active fractions of ratite oil or a mixture of fatty acids. Also included are compositions comprising ratite oil, an active fraction thereof or a mixture of fatty acids and at least one other insect repellent.
• Suitable insect repellents that can be combined with ratite oil, an active fraction thereof or a composition comprising a mixture of fatty acids include, but are not limited to, N,N-diethyl-m-toluamide (DEET), citronella oil, rotundial oil, eucalyptus oil, neem oil, oil of Hedeoma pulgioides, oil of anisum, oil of chrysanthemum and saponin.
• DEET N,N-diethyl-m-toluamide
• compositions comprising ratite oil, an active fraction thereof or a mixture of fatty acids and at least one other insect repellent were found to exhibit surprisingly unexpected synergistic results.
• the repellent activity of these compositions was much greater than either ratite oil, active fractions of ratite oil, a mixture of fatty acids or the other insect repellent alone. This synergistic effect was also observed with diluted preparations of ratite oil and another insect repellent.
• Example 1 The effect of emu oil on frequency of mosquito lands and bites
• emu oil effectively repel mosquitoes.
• emu oil reduces by one-half the number of mosquitoes which land.
• the number of mosquito lands drops to one-tenth of lands on an untreated hand.
• emu oil is an effective insect repellent at a concentration of 1% or higher.
• a mosquito repellent bioassay was performed by treating wedges of filter paper with sucrose overlaid with either an aliquot of the crude sample 776, FI or F2.
• Filter paper treated with water or sucrose served as controls.
• Samples of FI and F2 were tested at full- strength or diluted with corn oil to 50% or 25% of full-strength. At regular time intervals, the number of mosquitoes which landed and fed on the wedges of filter paper was recorded. Results are shown in Figures 1 and 2.
• Black-legged ticks were placed on the fingers of the hands and observed as they climbed toward the treated or untreated skin of the hand. Ticks crossing onto the treated skin were scored as "crossing.” Those not crossing were scored as “repelled.” Ticks were removed after a single score was recorded. Repellency is calculated as the proportion of all trials in which a tick is repelled. For example, 8 repels in 10 trials provides a repellency of 80%.
• Aedes taeniorhynchus accounted for >99% of mosquitoes that approached or attacked subjects.
• Test subjects counted and recorded bites in a series of 10 minute periods. Counts were recorded on data sheets. In the first study, the testing period was two hours, with 12 consecutive 10 minute recording periods. In the second study, the test was interrupted during two brief windy periods by the need to move to more productive locales (i. e. , places with higher biting rates) within the test sites. As a result, the total testing period including the interruption was two hours and twenty-five minutes.
• a composition comprising emu oil and oil of citronella was particularly effective as a repellent (see Figure 5).
• the repellent properties of emu oil alone reduced the number of bites to an average of 5.7 bites per ten minutes.
• the composition comprising emu oil and citronella approximated the positive control, Ultrathon, with 0.8 bites per ten minutes for the emu oil/citronella composition compared to 0.2 bites per ten minutes for Ultrathon.
• emu oil a composition comprising emu oil and citronella and Ultrathon substantially reduced biting rates from Aedes taeniorhynchus.
• a composition comprising emu oil and citronella was much more effective than emu oil alone and offers protection comparable to that offered by mosquito repellents registered by the U.S. Environmental Protection Agency (EPA). No pattern of diminishing repellency over time was observed for emu oil and citronella.
• emu oil Two preparations of emu oil were prepared for testing: a) 100%) emu oil alone; and b) 20 mL emu oil plus 30 drops of oil of citronella and 2 mL saponin (Croda, from Sapindus).
• the two commercially available repellents used as comparative controls were: a) UltrathonTM (3M®, Minneapolis, MN, a United States Environmental Protection Agency (EPA)-registered DEET-based product, approximately 32%) DEET); and b) TreoTM (Primavera Laboratories, Inc.®, SPF 15 lotion with 0.05% citronella).
• the negative control was untreated skin.
• test materials were applied either to the lower arm or lower leg skin of the study subjects.
• the areas of treated skin surfaces were calculated for each subject in advance of the application.
• Applications of the test materials, except Ultrathon were made at a dosage of 3.0 mL/650 cm 2 , a dosage comparable to that used in studies of herbal repellents for EPA registration. Ultrathon was applied at the manufacturer's recommended dosage of 1 mL/650 cm 2 .
• Biting rates were much lower on each of the test materials than with the control. Biting rates with emu oil and with the emu oil, citronella and saponin composition were much lower than with the control and lower than the EPA-registered herbal repellent, Treo.
• emu oil, citronella and saponin composition prevented biting altogether in many of the sampling periods, with confirmed bites (a bite followed by another bite within 30 minutes) recorded only on subject 1 in the first sampling period and subject 3 in the third sampling period.
• emu oil has a pronounced synergistic effect when combined with a herbal repellent, such as citronella.
• Example 8 The synergistic repellent effects of emu oil
• a preparation of emu oil was prepared wherein the emu oil was diluted to a final concentration of 0.02% with ethanol.
• SkintasticTM S.C. Johnson
• a 1 : 1 solution (by volume) of the diluted OFF! and the diluted emu oil was prepared.
• a 1 :1 :1 solution consisting of 10 mL of the diluted 0.01%) OFF!, 10 mL of the diluted 0.02% emu oil, and 10 mL of ethanol was prepared.
• compositions comprising various percentages of certain fatty acids known to be present in emu oil were prepared and tested for repellent activity.
• Table 6 shows the chemical composition of one such composition and comparative information vis-a-vis corn oil, which has been previously shown to be non-repellent, and soybean oil, which is a component of an insect repellent recently introduced to the market as BiteBlockerTM (Consep, Inc., Bend, OR).
• the percentages of fatty acids in corn and soybean oil listed in Table 6 are from deMan, John M, PRINCIPLES OF FOOD CHEMISTRY (Avi Publishing Co., 1980).
• Test 2 was conducted as in previous experiments reported in the foregoing examples. Tests were conducted in the outdoors in a wildlife area in New Mexico in which the predominant species of mosquito is Aedes vexans, an aggressive biting insect. Tests were performed in the summer months in the early afternoon (1430-1630 hours, Test 1) and in the late afternoon/early evening (1515-1915 hours, Test 2) near a stream at an elevation of approximately 2500 meters. In two separate tests, four subjects in total applied approximately 2.5 mL of the fatty acid composition shown in Table 6 to one lower arm. The other lower arm of each subject was untreated and served as a control. Test l In Test 1, three subjects were exposed for a period of two hours. Ambient biting was estimated at three (3) bites per minute on each untreated lower arm.
• Test 2 In Test 2, one subject was exposed for a period of four hours. The ambient biting rate per lower arm was measured in each of twenty-four (24) ten (10) minute periods. The ambient biting rate average 0.5 bites per minute and ranged from 0 to 1.5 bites per minute. The test subject received one bite on the treated lower arm surface at approximately 225 minutes after application of the composition. In contrast, the test subject received a total of 116 bites on the untreated control lower arm surface during the 240 minute test period.
• compositions comprising mixtures of fatty acids present in ratite oil are effective as insect repellents.

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• 1998
  • 1998-05-07 WO PCT/US1998/009026 patent/WO1998057542A1/en not_active Application Discontinuation
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  • 1998-05-07 CN CN98807358A patent/CN1283959A/zh active Pending
  • 1998-05-07 JP JP50440099A patent/JP2002504141A/ja active Pending
  • 1998-05-07 AU AU73672/98A patent/AU756465B2/en not_active Expired
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