Composition for repelling vector pests and application thereof

Abstract

The invention discloses a composition for repelling vector pests and application thereof, belongs to the field of agricultural chemistry, and particularly belongs to the field of prevention and control of biological pests. The composition comprises a compound of general formula (I), such as (E)-8-decene-5-lactone or (Z)-7-decene-5-lactone, and a carrier. The mosquito repellent has a remarkable repelling effect on mosquitoes, bed lice, ticks and blood sucking midges, and has durability and safety.

Description

Technical Field

[0001] The invention belongs to the field of agricultural chemistry, in particular to the field of controlling biological pests, and relates to a composition for repelling disease-carrying pests such as mosquitoes, bed bugs, ticks and blood-sucking midges, and a method for repelling disease-carrying pests using the composition. Background Art

[0002] Disease-carrying pests mainly include two major groups, one is some species of the class Insecta, such as mosquitoes, bed bugs and blood-sucking midges; the other is some species of the class Arachnida, such as ticks, chiggers, etc. They usually ingest disease-causing microorganisms when sucking blood from infected hosts (humans or animals), and then transmit the pathogens to new hosts after replication. In the documents of the World Health Organization, disease-carrying pests are also called vectors. Once disease-carrying pests become infectious, they can transmit pathogens in each subsequent bite / blood-sucking process. Every year, human diseases caused by disease-carrying pests, such as malaria, dengue fever, human African trypanosomiasis, leishmaniasis, Chagas disease, yellow fever, Japanese encephalitis and onchocerciasis, can cause more than 700,000 deaths.

[0003] N,N-Diethyl-3-methylbenzamide (DEET) is an effective repellent for mosquitoes and biting flies developed after World War II and used by more than 200 million people worldwide each year. Due to its widespread and long-term use, some disease-carrying pests have been reported to have developed resistance to DEET. DEET also has an unpleasant odor, a relatively short duration of action, and dissolves plastics. In addition, DEET can cause skin irritation or allergic reactions in some adults and children. When used in children, especially those who lack ornithine carboxylase, there may be a possibility of brain toxicity and epileptic seizures. For adults, excessive use can also cause mild neurotoxicity, such as insomnia, mood swings, and impaired cognitive function.

[0004] Due to the above disadvantages of DEET, researchers are constantly developing or looking for new pest repellents, such as Citronella Oil, PMD, Picaridin, IR3535, Nootkatone, etc. Although these compounds have been approved for use as repellents, they are not ideal repellent compounds. For example, Citronella Oil, Picaridin and Nootkatone are toxic to aquatic organisms. For another example, PMD, Picaridin, IR3535 and Nootkatone are irritating to the skin or eyes. Such adverse properties can be found in the registration information of the competent authorities of various countries, such as the public data of the US Environmental Protection Agency. Therefore, when preparing repellents with these compounds as active ingredients, it is necessary to pay attention to the safety of the final formula and insert usage instructions in the instructions. In addition to the repellent compounds already in use, some candidate compounds under development, such as those discussed only in patent applications and scientific papers, usually focus on discussing their repellent effects without fully evaluating their safety. Some are even prohibited from being used in products that come into contact with the skin (such as cosmetics, perfumes, etc.) because they can cause significant irritation or allergy. Therefore, the safety of suitable candidate compounds must be evaluated, and it is necessary to find safer compounds as repellents for disease vectors and pests.

[0005] In addition, the durability of the repellent effect of the candidate compounds needs to be examined. For example, according to the requirements of the Chinese national standard GB / T39513-2020 "On-site efficacy determination and evaluation of sanitary insecticides repellents", the outdoor complete protection time of the repellent is greater than or equal to 2 hours to be qualified. According to the requirements of the national standard GB / T 13917.9-2009 "Indoor efficacy test and evaluation of sanitary insecticides for pesticide registration Part 9: Repellents", the effective protection time in the laboratory is divided into two levels, A and B, and those that do not meet the B-level standard are unqualified products. Among them, the effective protection time of Class B is ≥4.0 hours. For another example, the "Guidelines for the Evaluation of the Efficacy of Mosquito Repellents" (August 2015) issued by the Ministry of Food and Drug Safety (MFDS) of South Korea requires that whether it is a laboratory or outdoor test method, the complete protection time of the tested substance is required to be 2 hours or longer. Therefore, as a candidate compound for repellents of disease-prone insects, it is necessary not only to have a strong repellent effect, but also to have a certain degree of repellent persistence. Testing repellency only for a short period of time after application (e.g., testing after spraying and drying, where data usually only represent effects within 15 to 30 minutes) does not prove that the compound is a suitable repellent compound. Some compounds have an initial repellent effect, but the persistence is poor. For example, when freshly applied to human skin, citronella oil has a repellent effect on some biting insects that is roughly equivalent to chemical repellents, but only lasts for about 1 hour (Vector Control, prepared by Jan A. Rozendaal, World Health Organization; ISBN 92-4-154494-5). Therefore, it is necessary to find compounds that are more persistent, that is, have a longer protection time, as repellents.

[0006] The candidate compounds disclosed herein fully demonstrate their safety, effectiveness and durability as repellents for disease-prone insects. Summary of the invention

[0007] The present invention provides a composition for repelling disease-causing insect pests, which composition is essentially composed of one or more compounds conforming to the general formula (I), one or more carriers, and optionally one or more excipients: (I) Among them, R 1 It is a C5 alkenyl group.

[0008] The compounds of general formula (I) have a strong repellent effect on disease-carrying pests, especially mosquitoes, bed bugs, blood-sucking midges and ticks. Specifically, the researchers found that the compositions containing 0.1% (v / v) to 5% (v / v) (E)-8-decene-5-lactone (CAS: 32764-98-0) had a repellent effect on mosquitoes, bed bugs and ticks that was comparable to or stronger than that containing 0.1% (v / v) to 5% (v / v) DEET under indoor experimental conditions. The repellent effect of the composition containing (E)-8-decene-5-lactone also has excellent persistence. Another configuration, a composition of (Z)-7-decene-5-lactone (CAS: 25524-95-2) was also found to have a repellent effect comparable to that of the composition containing (E)-8-decene-5-lactone. The repellent effect of a 10% (v / v) (E)-8-decene-5-lactone composition on blood-sucking midges was also verified in a tropical outdoor environment, and its complete protection time was shown to be superior to that of DEET at the same concentration. A method for repelling pests from vectors is also provided herein, comprising exposing the pests to the composition provided herein.

[0009] Optionally, preferred features are listed in the dependent claims. More details and embodiments of the compositions and methods described herein can be reflected through the following description, drawings and clauses. It should be noted that, under the premise of not contradicting each other, each feature described herein, and any combination of two or more features, are included in the scope of the invention described herein. In addition, any specific feature or feature combination can also be excluded from a certain embodiment. BRIEF DESCRIPTION OF THE DRAWINGS

[0010] Figure 1 Schematic diagram of the hand experiment setup.

[0011] Figure 2 Schematic diagram of the double-terminal experimental setup.

[0012] Figure 3 Schematic diagram of the blood-sucking experimental device.

[0013] Figure 4 Schematic diagram of the culture dish experimental setup.

[0014] Figure 5 The repellent effects of (E)-8-decene-5-lactone and DEET against Aedes aegypti in a hand test were demonstrated.

[0015] Figure 6 The repellent effects of (E)-8-decene-5-lactone and DEET against Aedes aegypti in a double-end assay were demonstrated.

[0016] Figure 7The figure shows the durability of the repellent effect of 5% (v / v) (E)-8-decene-5-lactone on Aedes aegypti. To avoid too long annotations in the figure, 5% compound refers to 5% (v / v) (E)-8-decene-5-lactone; ethanol solvent refers to 100% ethanol as solvent; mixed solvent refers to solvent composed of ethanol, propylene glycol and water.

[0017] Figure 8 The repellent effects of (E)-8-decene-5-lactone, (Z)-7-decene-5-lactone, and DEET against Aedes aegypti in a hand test were demonstrated.

[0018] Fig. 9 The repellent effect of (E)-8-decene-5-lactone on female Culex pipiens quinquefasciatus in a blood-sucking experiment was demonstrated, using 100% ethanol as a control.

[0019] Fig.10 The repellent effects of (E)-8-decene-5-lactone and DEET on bed bugs in a petri dish experiment were demonstrated.

[0020] Fig.11 The repellent effects of (E)-8-decene-5-olide and DEET on bed bugs in a field experiment were shown at three time points: 1 hour, 2 hours, and 4 hours. The negative control was 100% ethanol.

[0021] Fig.12 The repellent effects of (E)-8-decene-5-olide and DEET on ticks in a petri dish experiment are shown, with 100% ethanol as the control. DETAILED DESCRIPTION

[0022] Prior published documents may be listed or discussed in this article, but this does not mean that the applicant agrees that they belong to the prior art or common knowledge.

[0023] The compounds according to the general formula (I) show unexpected effects in repelling pests. Therefore, the present invention provides a composition for repelling pests, which mainly consists of one or more compounds according to the general formula (I), one or more carriers, and optionally one or more excipients: (I) Among them, R 1 It is a C5 alkenyl group.

[0024] In certain embodiments, the one or more compounds conforming to formula (I) are each independently selected from compounds corresponding to formula (Ia) or formula (Ib): , (Ia) (Ib)

[0025] In certain embodiments, the composition is mainly composed of two or more compounds conforming to the general formula (I), one or more carriers, and optionally one or more excipients. Typically, the two or more compounds conforming to the general formula (I) include compounds conforming to the general formula (Ia) and compounds conforming to the general formula (Ib).

[0026] For the avoidance of doubt, in this document, Formula (I), Formula (Ia) and Formula (Ib) are intended to encompass both E and Z isomers of compounds within the scope of these formulas. For example, Formula (Ia) encompasses compounds conforming to Formula (Ic) and Formula (Id): , (Ic) (Id)

[0027] Likewise, Formula (Ib) encompasses compounds conforming to Formula (Ie) and Formula (If): , (Ie) (If)

[0028] Therefore, when the one or more compounds conforming to the general formula (I) are compounds conforming to the general formula (Ia), the compound may be (E)-7-decene-5-lactone, (Z)-7-decene-5-lactone or a mixture thereof.

[0029] When one or more compounds conforming to the general formula (I) are compounds conforming to the general formula (Ib), these compounds may be (Z)-8-decene-5-lactone, (E)-8-decene-5-lactone or a mixture thereof.

[0030] Also for the avoidance of doubt, the compounds conforming to the general formula (I) (including compounds conforming to the general formula (Ia), (Ib), (Ic), (Id), (Ie) and (If)) referred to herein are intended to include all enantiomers thereof, unless otherwise specified. In general, the composition described herein may comprise a racemic mixture of the compound conforming to the general formula (I). However, the composition described herein may also be a composition comprising only one enantiomer of the compound conforming to the general formula (I), or a composition having different proportions of each enantiomer. If the specific compound name cited herein causes confusion due to descriptive differences such as nomenclature, the compound should be identified in conjunction with other information such as the CAS number given herein.

[0031] The compounds of general formula (I) can be synthesized by methods known in the field of organic chemistry. These compounds of general formula (I) can also be extracted from plants, for example, from jasmine plants and parts thereof, or plant species such as peach (Prunuspersica L.), passionflower (Passiflora) and mango (Mangifera).

[0032] The compositions provided herein may include one or more carriers. As used herein, "carrier" refers to a material that can dissolve or suspend one or more compounds of formula (I). When the composition is applied to the skin or hair of a subject, the carrier is preferably a dermatologically acceptable carrier.

[0033] Typically, the carrier is an aqueous solvent, an organic solvent or a mixture thereof. Suitable carriers for use in the compositions herein include, but are not limited to, water; hydrocarbons such as liquid paraffin, paraffin; siloxanes such as dimethyl siloxane, colloidal silica, and bentonite; monoalcohols such as ethanol, propanol, isopropanol, stearyl alcohol, lauryl alcohol, and cetyl alcohol; polyols such as polyethylene glycol, ethylene glycol, propylene glycol, and glycerol; carboxylic acids such as lauric acid and stearic acid; and esters such as beeswax and lanolin. The compositions herein may include a mixture of two or more of the above carriers. In certain exemplary embodiments, the carrier is a monoalcohol such as ethanol, propanol, or isopropanol. For example, the carrier may be ethanol.

[0034] The compositions herein may also include one or more excipients. As used herein, "excipients" refer to those components of the composition that are inactive (e.g., components that have no repellent activity) and are not considered to be carriers. For example, the composition may include the following excipients, such as emulsifiers or dispersants, extenders, wetting agents, suspending agents, preservatives, propellants, fragrances, and film formers. Examples of emulsifiers or dispersants suitable for use in the compositions herein include soaps, polyoxyethylene fatty acids; alcohol ethers, such as polyoxyethylene oleyl ether; polyoxyethylene alkyl aryl ethers, such as polyoxyethylene nonylphenol ethers, polyoxyethylene fatty acid esters, fatty acid glycerides, sorbitan fatty acid esters, sulfates of long-chain alcohols, and alkyl aromatic sulfonates, such as sodium dodecylbenzene sulfonate; examples of extenders and wetting agents include glycerol and polyethylene glycol; examples of suspending agents include casein, gelatin, alginic acid, carboxymethyl cellulose, gum arabic, hydroxypropyl cellulose and bentonite; examples of preservatives include methylparaben, ethylparaben, propylparaben and butylparaben; examples of propellants include dimethyl ether, chlorofluorocarbons and carbon dioxide; examples of film formers include nitrocellulose, cellulose acetate, cellulose acetate butyrate, methylcellulose derivatives, polyethylene resins (such as vinyl acetate resins) and polyvinyl alcohol. When the compositions of the present invention are to be applied to the skin or hair of a subject, the excipient, if any, is preferably a dermatologically acceptable excipient.

[0035] As used herein, the term "dermatologically acceptable" refers to a compound or ingredient that is approved for use on the skin or hair of humans or domesticated animals and / or is considered in the art to be suitable for dermatological use.

[0036] The composition herein can be in any physical form suitable for exposing the composition to the pest vectors. For example, the composition herein can be in a foam, gel, cream, lotion, oil, liquid suitable for aerosol spray or surface spray, suspension, emulsion, emulsifiable concentrate or other appropriate physical form.

[0037] In certain embodiments, when the carrier is an aqueous solvent, an organic solvent, or a mixture of the two, the concentration of one or more compounds according to formula (I) in the composition can be expressed as the volume percentage of the compound relative to the total volume of the composition. In this case, the unit used herein is "% (v / v)". For example, the composition herein contains 5% (v / v) of one or more compounds according to formula (I), which should be understood as 5 ml of one or more compounds according to formula (I) per 100 ml of the composition herein.

[0038] Therefore, in certain embodiments, when the carrier is an aqueous solvent, an organic solvent or a mixture thereof, the concentration of one or more compounds according to general formula (I) in the composition may be between about 0.01% (v / v) to about 20% (v / v), for example, from 0.1% (v / v) to 10% (v / v). In certain exemplary embodiments, when the carrier is an aqueous solvent, an organic solvent or a mixture thereof, the concentration of one or more compounds according to general formula (I) in the composition may be between 0.1% (v / v) to 10% (v / v), for example, 1% (v / v), 2% (v / v), 5% (v / v) and 10% (v / v).

[0039] In certain exemplary embodiments, the composition herein consists essentially of (Z)-7-decene-5-lactone, one or more carriers, and optionally one or more excipients. For example, the composition herein may consist essentially of (Z)-7-decene-5-lactone and a monoalcohol (e.g., ethanol). For example, the composition herein may consist essentially of (Z)-7-decene-5-lactone and a monoalcohol (e.g., ethanol), wherein the concentration of (Z)-7-decene-5-lactone in the composition is about 0.01% (v / v) to about 20% (v / v) (e.g., from 0.1% (v / v) to 10% (v / v), e.g., 1% (v / v), 2% (v / v), 5% (v / v) or 10% (v / v)).

[0040] In certain other exemplary embodiments, the composition herein is substantially composed of (E)-8-decene-5-lactone, one or more carriers, and optionally one or more excipients. For example, the composition herein may be substantially composed of (E)-8-decene-5-lactone and a monoalcohol (e.g., ethanol). For example, the composition herein may be substantially composed of (E)-8-decene-5-lactone and a monoalcohol (e.g., ethanol), wherein the concentration of (E)-8-decene-5-lactone in the composition is about 0.01% (v / v) to about 20% (v / v) (e.g., from 0.1% (v / v) to 10% (v / v), e.g., 1% (v / v), 2% (v / v), 5% (v / v) or 10% (v / v)).

[0041] In certain other embodiments, the composition herein consists essentially of (Z)-7-decene-5-lactone, (E)-8-decene-5-lactone, one or more carriers, and optionally one or more excipients. For example, the composition herein may consist essentially of (Z)-7-decene-5-lactone, (E)-8-decene-5-lactone and a monoalcohol (e.g., ethanol). For example, the composition herein may consist essentially of (Z)-7-decene-5-lactone, (E)-8-decene-5-lactone and a monoalcohol (e.g., ethanol), wherein (Z)-7-decene-5-lactone and (E)-8-decene-5-lactone are present together in the composition at a concentration of about 0.01% (v / v) to about 20% (v / v) (e.g., from 0.1% (v / v) to 10% (v / v), e.g., 1% (v / v), 2% (v / v), 5% (v / v) or 10% (v / v)).

[0042] Alternatively, the composition herein may be substantially composed of one or more compounds according to general formula (I), one or more carriers, one or more optional excipients, and one or more optional other substances having the activity of repelling disease-vectoring pests. Other substances having the activity of repelling disease-vectoring pests include, but are not limited to, those sold on the market and those cited herein, such as DEET, Citronella Oil, p-menene-3,8-diol (PMD), etc.

[0043] As shown in the embodiments herein, researchers herein have found that the compounds of general formula (I) have a significant repellent effect on disease-causing pests, especially mosquitoes, bed bugs, blood-sucking midges and ticks. Therefore, the present invention also provides a method for repelling disease-causing pests, which comprises exposing the disease-causing pests to the composition herein.

[0044] In this document, the word "include" may be interpreted as requiring the inclusion of the mentioned features, but not limiting the existence of other features. Alternatively, the word "include" may also refer to the situation where only the listed components / features are included (for example, the word "include" may be replaced by "consisting of" or "consisting essentially of"). Both broad and narrow interpretations apply to all aspects and embodiments of this document. That is, the word "include" and its synonyms may be replaced by "consisting of" or "consisting essentially of" or their synonyms, and vice versa.

[0045] The pest vectors described herein belong to the order Hemiptera, Hymenoptera, Siphonaptera, Diptera, Arachnids, Acarina or Blattagia. For example, the pest vectors can be mosquitoes, bed bugs, blood-sucking midges, ticks, ants, cockroaches, fleas, mites, spiders, termites or wasps.

[0046] In certain exemplary embodiments, the pest vector may be a mosquito, a bed bug, a blood-sucking midge, or a tick. When the pest vector is a mosquito, it may belong to the genus Aedes, Culex, or Anopheles. For example, the mosquito may be Aedes aegypti, Culex quinquefasciatus, Anopheles sinensis, or Anopheles gambiae. When the pest vector is a bed bug, it may be a tropical bed bug or a tropical bed bug (Cimex hemipterus). When the pest vector is a blood-sucking midge, it may belong to the genus Culicoides, Lasiohelea, or Forcipomyia, etc. When the pest vector is a tick, it may belong to Haemaphysalis longicornis. The researchers in this article found that compared with the same concentration of DEET, the composition in this article showed better repellent activity against these disease-carrying pests, especially mosquitoes and blood-sucking midges.

[0047] "Repellent" in the terms "pest repellent", "repellent composition", "repellent compound", "repellent effect" or similar terms refers to the ability of a composition or compound to reduce, decrease, deter or prevent pests from approaching or existing at a repellent source (e.g., in the air, on the surface of an object or on a surface of an object, such as a body part). "Repellent activity", "repellent effect" and "repellent effect" are terms that refer to this ability in different contexts.

[0048] In certain embodiments, the method of exposing the vector pest to the composition described herein includes applying the composition to an object or an article. The term "object" as used herein refers primarily to individual animals and parts of their bodies. Examples of individual animals include humans and domesticated animals. Generally, objects are considered to be food sources or habitats for vector pests. For example, humans can be bitten by mosquitoes and are susceptible to mosquito-borne diseases such as malaria, dengue virus, and Zika virus. Domesticated animals include, but are not limited to, mammals, including household pets and livestock animals, especially canines and felines, such as dogs and cats. These domesticated animals are susceptible to diseases spread by vector pests, or are susceptible to their invasion. Therefore, the compositions herein may help reduce disease transmission and / or invasion by vector pests. The compositions herein can be topically applied to an object, such as sprayed and / or applied to the skin or hair of the object.

[0049] In addition to contacting the composition directly with the object, the composition of the present invention can also be applied to the surface of the article, or penetrate into the article. The term "article" as used herein refers to objects, such as artificial products composed of fabrics or solid substrates, which may come into contact with or be close to pest vectors. The articles may include furniture, clothing, candles, air diffusers, tablets, cosmetics, nets, building materials, and aromatherapy products, etc.

[0050] The invention is described herein in a broad and general manner. A person of ordinary skill in the art will readily appreciate that all parameters, dimensions, materials, and configurations described herein are exemplary, and that the specific parameters, dimensions, materials, and / or configurations will depend on the specific application or applications for which the inventive technology is used. A person of ordinary skill in the art will be able to identify or determine by no more than routine experimentation many equivalents to the specific embodiments described in the invention. Therefore, it should be understood that the above embodiments are provided only as examples, and within the scope of the appended claims and their equivalents, the present invention may be implemented in a form different from that specifically described herein.

[0051] The present invention covers each independent feature, system, article, material, kit and / or method described herein. At the same time, if there is no conflict between these features, systems, articles, materials, kits and / or methods, any two or more combinations thereof are also included in the scope of the present invention. In addition, subsets and specific examples within the scope of the disclosure also constitute a part of the present invention. This includes general descriptions with qualifiers or negative limitations, even if the excluded content is not specifically mentioned in this article, it is also within the scope of the present invention. The following examples are used to illustrate the present invention.

[0052] Example

[0053] Materials and Methods

[0054] (Z)-7-Decen-5-olide (purity 97%, CAS: 25524-95-2) was purchased from Precision Technologies, Singapore. (E)-8-Decen-5-olide (purity ≥ 95%, CAS: 32764-98-0) was purchased from Lluch Essence. DEET (purity 97%, CAS: 134-62-3) was purchased from Sigma-Aldrich. Unless otherwise stated, the compounds described in each example were dissolved in 100% ethanol at the specified concentration.

[0055] Hand test (for Aedes aegypti): Dissolve the compound in 100% ethanol to make a 1 mL solution at the concentration described in the test. Add the solution dropwise onto a 10 cm diameter fabric. Dry the fabric in a fume hood for 5 minutes before use (in persistence experiments, the drying time may be longer). After drying, the fabric is fixed outside the cage opening and located between the cage wall and the ring cover.

[0056] Blood-feeding test (for Culex quinquefasciatus): The compound was dissolved in 100% ethanol and a 200 µL solution was prepared according to the concentration described in the experiment. The solution was applied dropwise to the surface of the mouse skin wrapped with a blood reservoir (blood feeding probe) and dried in a fume hood for 5 minutes before use.

[0057] Mosquito repellent experiment

[0058] Aedes aegypti and Culex pipiens used in the experiment were raised in an environmental chamber at 28 ± 1 °C, 75-80% relative humidity, and a photoperiod of 12 h light / 12 h dark. Larvae were fed a diet consisting of a mixture of ground fish food flakes (TetraMin) and dry yeast granules (ratio 2:1), while adults were provided with a 10% sugar solution. Blood sucking experiments were conducted using a membrane feeding system (provided by Orinno Technology) using rabbit blood and mouse skin as membrane materials.

[0059] a. Aedes aegypti hand experiment

[0060] Each experiment was repeated at least three times using 20 5- to 7-day-old female Aedes aegypti mosquitoes. Mosquitoes were fasted for 12 h before the experiment, with access to water only, and were placed in a 30 cm × 30 cm × 30 cm test cage, where they were allowed to acclimate for 10 min before the start of the experiment. Only female Aedes aegypti mosquitoes that exhibited host-seeking behavior were used in the experiment. The cage had a sleeved opening for transferring mosquitoes and a 9 cm diameter opening on each side of the test cage, with a mesh ( Figure 1In the experiment, the mesh with one opening was replaced by plastic wrap for better observation, and the mesh with the other opening was replaced by a piece of fabric (10 cm in diameter) soaked with the test compound.

[0061] To induce a host-seeking response in mosquitoes, a mixture of 10% CO2 and 90% air was introduced into the test cage at a flow rate of 3 NL / min through a fly pad placed on the top of the test cage ( Figure 1 ). Mosquitoes were acclimated for 10 minutes before the experiment. The palm was placed on the ring cover covering the outside of the fabric-covered opening of the test cage, forming a gap between the fabric and the palm. The timer was started and a picture was taken every minute for a total of 5 minutes for quantitative analysis. Fabric soaked in diluent (100% ethanol) was used in the control experiment. Each set of experiments consisted of 3 control experiments and 3 treatment experiments using the same test cage. For different compounds or different concentrations of the same compound, new test cages and mosquitoes were used.

[0062] The test cages used in this experiment are shown in Figure 1 The figure shows: 1. Openings for air exchange and observation (with screens); 2. A mixture of 10% CO2 and 90% air was introduced into the test cage at a flow rate of 3 NL / min through a fly pad placed on the top of the test cage. 3. The screen with one side opening was replaced with plastic wrap for better observation. 4. The rear end of the test cage contains an opening covered by a sleeve, which has been removed for ease of illustration. 5. The screen opening on the other side of the test cage is replaced with a piece of fabric soaked with the compound to be tested. 6. A petri dish lid with a central hollow (lid diameter 9 cm, hollow diameter 7 cm), the "ring lid", is buckled on the outside of the opening covered by the fabric soaked with the test compound to form a gap between the fabric and the palm. 7. Place your palm on the ring cover.

[0063] b. Double-end test for Aedes aegypti

[0064] The double-ended experimental device was modified from the Y-type olfactometer ( Figure 2). The cylindrical mosquito trap is separated from the holding cage by a sliding door, which is opened at the beginning of the experiment. At the other end of the holding cage, there is a square opening with a 20 cm diameter fan to generate airflow. The opening is covered with nylon mesh, and the airflow rate is 81-84 feet per minute when the fan is on. At the other end of the cylindrical mosquito trap, there is a round cover with fabric, which is soaked in either the test compound or the solvent, which serves as a barrier between the attraction source (hand) and the mosquitoes entering the mosquito trap.

[0065] Before the experiment, 50 female Aedes aegypti mosquitoes aged 5-7 days were placed in the holding cage and allowed to acclimate for 20 minutes. During the acclimatization period, fabrics soaked with solvent or test compound were prepared, dried and placed at the end of a cylindrical mosquito trap ( Figure 2 6). Then fix the cylindrical mosquito trap on the holding cage.

[0066] Two air delivery tubes are inserted through the diaphragm at the top of the cylindrical mosquito trap ( Figure 2 7 in the figure) and opened at the end of the adaptation period to deliver a mixture of 10% CO2 and 90% air at a flow rate of 3 NL / min. Figure 2 2), generating an airflow of 81-84 ft / min, and then opening the sliding door ( Figure 2 3). Place your palm at the end of the cylindrical mosquito trap as a source of attraction for female mosquitoes. Allow mosquitoes to freely enter any mosquito trap, and the experiment lasts for 8 minutes. After the time is up, close the sliding door, turn off the fan and CO2 supply, and count the number of mosquitoes caught in the mosquito trap. Mosquitoes that do not enter the mosquito trap and remain in the holding cage are removed. Before the next round of experiments, turn on the fan and raise the sliding door for ventilation for 15 minutes.

[0067] The holding cage used in the experiment is shown in Figure 2 The diagram shows the following: 1. A main holding cage for holding mosquitoes. One side of the holding cage can be opened to facilitate the removal of unattracted mosquitoes and cleaning. 2. Mesh-filtered fan. Use a 20 cm diameter fan to direct airflow at 81-84 ft / min. 3. Sliding door to cover the opening connected to the cylindrical mosquito trap. It can be opened at the beginning of the experiment. 4. Cylindrical mosquito trap, used to catch mosquitoes. 5. The funnel-shaped design between the holding cage and the cylindrical mosquito trap facilitates the entry of mosquitoes and reduces the possibility of mosquitoes escaping during the experiment. 6. A circular lid containing fabric soaked with the test compound is fixed to the end of the cylindrical mosquito trap. 7. An air supply tube that delivers a mixture of 10% CO2 and 90% air at a flow rate of 3 NL / min is delivered through the diaphragm at the top of the cylindrical mosquito trap.

[0068] c. Culex mosquito blood-sucking experiment

[0069] The test cages for this experiment were custom made and measured 10 cm × 10 cm × 10 cm. The cages had a cannulated opening for transferring mosquitoes and an 8 cm diameter mesh opening on the adjacent face for blood feeding (see Figure 3 ).

[0070] Twenty female Culex mosquitoes, 4 to 6 days old and showing blood-seeking behavior, were transferred to the test cage and placed in a dark environment to adapt for 10 minutes before the start of the experiment.

[0071] The blood reservoir (feeding probe) of the membrane feeding system was wrapped with depilated mouse skin. 1 mL of fresh rabbit blood was added to the reservoir. The test compound was dissolved in 100% ethanol, prepared into a 200 µL solution, and dripped onto the mouse skin. The blood reservoir was air-dried in a fume hood for 5 minutes before use. In each experiment, 20 mosquitoes were allowed to freely feed on blood for 15 minutes. After 15 minutes, the mosquitoes were removed and the number of blood-feeding mosquitoes was counted.

[0072] d. Statistical methods

[0073] Hand test: Count the number of mosquitoes landing on the fabric within 5 minutes (i.e., one photo per minute, 5 photos in total), and then divide the sum by 5 to get the average landing number. Repellency = (CT) / C × 100%, where C is the average landing number of the control group and T is the average landing number of the experimental group.

[0074] Two-ended experiment: The number of mosquitoes trapped in the cylindrical mosquito traps at the end of 8 minutes was recorded. Mosquito preference was calculated by dividing the number of mosquitoes in each cylindrical mosquito trap by the total number of mosquitoes released in the holding cage. The percentage of the experimental group was directly compared with the percentage of the control group.

[0075] Blood sucking experiment: Divide the number of blood-sucking mosquitoes by the total number of mosquitoes in the cage (20) to get the percentage of blood-sucking mosquitoes. The percentage of blood-sucking mosquitoes in the experimental group is directly compared with the percentage of blood-sucking mosquitoes in the control group.

[0076] Bed bug repellent experiment

[0077] The bed bugs (Cimex hemipterus) used in the experiment were kept in an incubator, maintained at a temperature of 26±1°C, a relative humidity of 40±10%, and a photoperiod of 12 hours of light / 12 hours of darkness. Only adult male bed bugs were used in the experiment to prevent egg laying in the experimental field.

[0078] a. Petri dish experiment

[0079] A glass culture dish (without cover) with a diameter of 15 cm and a height of 2 cm was used as the experimental site ( Figure 4 ). To prevent bed bugs from escaping, the inner wall of the culture dish was coated with polytetrafluoroethylene (PTFE). A filter paper with a diameter of 15 cm was cut into two halves; one half was treated with about 1.4 mL of 100% ethanol, and the other half was treated with about 1.4 mL of DEET or (E)-8-decene-5-lactone solution. Two different concentrations were tested in the experiment: 2% (v / v) and 5% (v / v). After the filter paper was dried under laboratory conditions for 30 minutes, it was fixed to the bottom of the culture dish. Next, 10 male bed bugs were placed in the center of the culture dish, and the number of bed bugs on each filter paper was recorded at 2 h and 6 h. Each treatment was repeated 6 times.

[0080] b. Arena Assay

[0081] The experimental arena was set up with a piece of brown kraft paper covering the bottom of a blue plastic tray (length: 95 cm, width: 75 cm, height: 10 cm), and the inner wall of the tray was coated with PTFE to prevent bed bugs from escaping. 12 to 14 hours before the experiment, 100 male bed bugs were placed in the center of the arena for acclimatization. The bed bugs were confined in a plastic ring (diameter: 6 cm, height: 5 cm), and the inner wall of the plastic ring was coated with PTFE to prevent bed bugs from escaping. Before the experiment began, a bed bug interceptor (diameter: 15.2 cm, height: 2.3 cm), also known as a bed bug interceptor or bed bug trap, was placed under each leg of a three-legged wooden stool (diameter: 25 cm, height: 32 cm). To prevent bed bugs from climbing up the stool legs, the inner wall of the interceptor was coated with PTFE. The outer wall of the interceptor was covered with cloth surgical tape (Model: 1530C-1; 3M Medical Devices & Materials Manufacturing Co., Ltd., Shanghai, China) treated with 100% ethanol, 5% (v / v) DEET solution, or 5% (v / v) (E)-8-decene-5-lactone solution. The compounds were allowed to dry for 30 min before the experiment, and then the tape-covered interceptor was placed in the arena and placed under the legs of a stool approximately 1 h into the dark cycle. At the beginning of the experiment, CO2 was released into the glass bottle above the wooden stool at a rate of 220 mL / min, and the plastic ring containing the bed bugs was subsequently removed. The number of bed bugs captured by the interceptor was recorded 1, 2, and 4 h after the start of the experiment, and the experiment was repeated 4 times.

[0082] c. Statistical methods

[0083] Petri dish test: repellency rate = (C–T) / C × 100%, where C is the number of bed bugs staying on the side of the filter paper treated with ethanol, and T is the number of bed bugs staying on the side of the filter paper treated with DEET or (E)-8-decene-5-lactone solution.

[0084] Field experiment: The percentage of bed bugs captured under different setting conditions in the same field experiment is used to reflect the repellency effect, T = P / S × 100%, where T is the percentage of bed bugs captured in a specified interceptor, P is the number of bed bugs captured in the interceptor, and S is the total number of bed bugs captured in all interceptors. Experimental settings with higher capture percentages (T) indicate that the corresponding compounds have lower repellency rates.

[0085] Tick ​​repellency test The ticks used in the experiment were Haemaphysalis longicornis , which were cultured under experimental conditions of a temperature of 22-25°C, a photoperiod of 12 h light / 12 h dark, and a relative humidity of 85%.

[0086] a. Petri dish experiment

[0087] A culture dish (diameter: 6 cm, height: 2 cm) was used as the experimental field ( Figure 4 ). Filter paper (diameter: 6 cm) was cut in half; one half was treated with about 1 mL of 100% ethanol, and the other half was treated with about 1 mL of DEET (2% v / v) or (E)-8-decene-5-olide solution (2% v / v and 0.2% v / v). The filter paper was dried under laboratory conditions for 30 minutes and then fixed to the bottom of a petri dish. 40-60 ticks were placed in the center of the petri dish, and the number of ticks moving toward or away from the treated filter paper was recorded for 30 minutes. The experiment was repeated 3 times.

[0088] b. Statistical method: The calculation method of repellency rate is the same as the previous bed bug petri dish experiment.

[0089] Blood-sucking midge repellent experiment

[0090] Blood-sucking midges prefer moist and warm environments, and only female midges suck blood. The blood-sucking midge repellent experiment in this paper was conducted outdoors.

[0091] a. Experimental location: The experimenter will find an area with a suitable density of blood-sucking midges in the wild for on-site experiments. The experimenter's lower legs will be exposed, and the blood-sucking midges will be closely observed for landing. If a blood-sucking midge is found to land, it will be driven away before its mouth needle pierces the skin, and one landing will be recorded. A location with more than 10 landings within 15 minutes is considered a qualified experimental location.

[0092] b. Blood-sucking midge attack test: For each sample to be tested, select 2 testers (do not drink alcohol, tea or coffee before and during the test, and do not use products containing fragrances). Spray one calf evenly with the sample to be tested, and do not spray any sample on the other calf as a control. Expose the calf, observe for 15 minutes, and record the number of blood-sucking midges landing; test again after 3 hours, and record the number of blood-sucking midges landing.

[0093] c. Statistical method: Repellency = (C–T) / C × 100%, where C is the number of landings on the blank control (calf not sprayed with any sample) and T is the number of landings on the experimental group (calf sprayed with the sample to be tested).

[0094] Human repetitive injury patch test

[0095] The Human Repeat Insult Patch Test (HRIT) is a test used to evaluate whether a product is irritating or sensitizing to human skin. The test involves exposing the subject to the chemical nine times over three weeks, each for 24 or 48 hours. After a two-week rest period, challenge tests are then performed on the exposed and unexposed areas. The challenge test is performed via a 24 or 48-hour patch test and is scored based on clinical responses. It is commonly used for safety verification of cosmetics, skin care products, and other personal care products. In this article, this test was commissioned to a third-party testing agency.

[0096] Example 1: Repellent effect of (E)-8-decene-5-lactone and (Z)-7-decene-5-lactone on Aedes aegypti

[0097] Hand test: The mosquito repellent effect of (E)-8-decene-5-lactone was evaluated by comparing it with DEET at the same concentration in the concentration range of 0.1% (v / v) to 2% (v / v). At a concentration of 2% (v / v), (E)-8-decene-5-lactone showed a 100% repellent effect, slightly better than the 97% protection effect of DEET. In addition, the repellent effect of DEET decreased significantly with decreasing concentration, falling to 64% at 1% (v / v). In contrast, (E)-8-decene-5-lactone still achieved a 90% repellent rate even at a low concentration of 1% (v / v), maintaining a high protective effect. At concentrations of 0.5% (v / v), 0.2% (v / v) and 0.1% (v / v), (E)-8-decene-5-lactone performed better than DEET (see Figure 5 ).

[0098] Double-end experiment: At a concentration of 2% (v / v), (E)-8-decene-5-lactone showed a strong repellent effect, with only 1.3% of female mosquitoes entering the cylindrical mosquito trap containing (E)-8-decene-5-lactone. In the 2% (v / v) DEET control group, 12.7% of mosquitoes entered the cylindrical mosquito trap. As the concentration decreased, the proportion of mosquitoes entering the cylindrical mosquito trap increased (2.7% of mosquitoes entered the mosquito trap treated with 1% (v / v) (E)-8-decene-5-lactone, and 8.0% of mosquitoes entered the mosquito trap treated with 0.1% (v / v) (E)-8-decene-5-lactone). In contrast, a significantly higher proportion of mosquitoes entered traps treated with DEET, with 25.1% of mosquitoes entering traps treated with 1% (v / v) DEET and 35% of mosquitoes entering traps treated with 0.1% (v / v) DEET (see Figure 6 ).

[0099] In order to investigate the durability of the repellent effect of (E)-8-decene-5-lactone, the repellent effect of fabrics on Aedes aegypti was observed after 6 and 8 hours after they were soaked in 5% (v / v) (E)-8-decene-5-lactone solution (100% ethanol solvent). The repellent rates of 99.44% and 98.67% were obtained after 6 and 8 hours respectively (see Figure 7 ). This result indicates that 5% (v / v) (E)-8-decene-5-lactone has excellent repellency persistence. Those skilled in the art can appropriately adjust the solution components based on conventional technical knowledge in this field or adjacent fields (such as cosmetics and perfumes) to achieve a complete protection effect of 8 hours, that is, a 100% repellency rate. For example, the water phase content can be appropriately increased, and moisturizers such as propylene glycol or glycerol can be added to reduce volatility and prolong the repellency effect. For example, a new 5% (v / v) (E)-8-decene-5-lactone solution (mixed solvent) is prepared according to the following volume ratio, in which the volume ratio of (E)-8-decene-5-lactone, ethanol, propylene glycol and water is 5:60:15:20. Testing using the aforementioned hand experiment method confirmed that the repellency rates for 6 hours and 8 hours both reached 100%. In comparison, in order to achieve complete protection for up to 8 hours, the concentration of common mosquito repellent compounds such as DEET, picaridin and immonin needs to be at least 20% to 30%. The use of such compounds in high concentrations will have adverse effects on safety, odor, greasiness and solution stability.

[0100] The isomer (Z)-7-decene-5-lactone of (E)-8-decene-5-lactone was further tested for its repellent effect on Aedes aegypti. Figure 8 As shown, 2% (v / v) (Z)-7-decene-5-lactone also has excellent repellent effect on Aedes aegypti, and its performance is comparable to that of 2% (v / v) (E)-8-decene-5-lactone, with a repellency rate of 100%, and is better than the 97.36% shown by 2% (v / v) DEET. (E)-8-decene-5-lactone and (Z)-7-decene-5-lactone are isomers of each other, and are both included in the entry "Jasmine lactone" in Baidu Encyclopedia (last visited on December 31, 2024). Therefore, those skilled in the art can foresee that (Z)-7-decene-5-lactone and (E)-8-decene-5-lactone have highly similar physical and chemical properties. The researchers in this article verified the equivalence of the two as repellent compounds through various experiments, and they can replace each other. In order to make the specification and its drawings more concise, the subsequent examples only show the data represented by (E)-8-decene-5-lactone. Similarly, those skilled in the art can foresee that other compounds belonging to the general formula (I) described herein also have effects very similar to those in the embodiments.

[0101] Example 2: Repellent effect of (E)-8-decene-5-lactone on Culex pipiens quinquefasciatus

[0102] In the Culex mosquito blood feeding experiment, 52% of the female Culex mosquitoes in the control group successfully sucked rabbit blood from the blood feeding probe sprayed with solvent (ethanol). However, a significant difference was observed when (E)-8-decene-5-lactone (2% (v / v)) was sprayed, and all female mosquitoes did not choose to suck blood from the blood feeding probe (see Fig. 9 ).

[0103] Example 3: Repellent effect of (E)-8-decene-5-lactone on bed bugs

[0104] At 2% (v / v) and 5% (v / v) concentrations, DEET and (E)-8-decene-5-lactone showed good repellency against bed bugs in the petri dish experiment, and there was no significant difference. The repellency was maintained even after 6 hours, showing good persistence (see Fig.10 ).

[0105] In the field test, (E)-8-decene-5-olide was less effective than DEET in repelling bed bugs, but still showed good repellency compared with the negative control. Its repellency did not significantly decay within 1 to 4 hours (see Fig.11 ).

[0106] Example 4: Repellent effect of (E)-8-decene-5-lactone on ticks

[0107] like Fig.12 As shown in the figure, (E)-8-decene-5-lactone at concentrations of 0.2% (v / v) and 2% (v / v) can cause most ticks to distribute to the control side and stay away from the treated side. The repellent effect of 2% (v / v) DEET on ticks is slightly better than that of 2% (v / v) (E)-8-decene-5-lactone.

[0108] Example 5: Repellent effect of (E)-8-decene-5-lactone on blood-sucking midges

[0109] This embodiment is an outdoor experiment. The experimental site is located in Shiping Village, Heqing Town, Danzhou City, Hainan Province (19°35'06.0"N, 109°39'49.0"E), and the surrounding environment has lychee trees, longan trees and green trees. The experimental time is 10:30-14:30 on August 3, 2024. The weather is sunny. The highest temperature during the period is 37°C and the lowest temperature is 31°C. There is no abnormal weather. The experimenters investigated the density and aggressiveness of blood-sucking midges on the spot and confirmed that they met the experimental conditions described in the materials and methods above.

[0110] The common concentration of commercially available DEET-based mosquito repellent products is 10%. In outdoor environments, affected by high temperatures and airflow, the effective protection time against mosquitoes is usually about 2 hours, although the packaging may indicate that it can reach 4 hours under laboratory conditions. There is little information on the effectiveness of such products against blood-sucking midges, so the experiment was designed with reference to the concentration of mosquito repellents and their protection time. In this experiment, two test samples, 10% (v / v) DEET solution and 10% (v / v) (E)-8-decene-5-lactone solution, were prepared. The experiment was conducted immediately after application (0 H) and 3 hours after application (3 H) as two time points for detecting the repellent effect. The experimental results are shown in Table 1.

[0111] Table 1. The effect of two samples in repelling blood-sucking midges outdoors

[0112] As shown in the results of Table 1, when the experiment was conducted immediately after spraying, both DEET and (E)-8-decene-5-lactone at a concentration of 10% (v / v) were able to achieve a 100% repellency rate against blood-sucking midges outdoors. After 3 hours, the repellency rate of the DEET group dropped significantly to 57.57%, and in fact, it was no longer able to effectively prevent blood-sucking midges from attacking humans; while (E)-8-decene-5-lactone still maintained a 100% repellency rate after 3 hours. From this result, it can be seen that the persistence of 10% (v / v) (E)-8-decene-5-lactone in repelling blood-sucking midges outdoors is significantly better than DEET at the same concentration.

[0113] Example 6: Safety of (E)-8-decene-5-lactone and (Z)-7-decene-5-lactone

[0114] The repellent compounds proposed in this article are often used as flavors and fragrances. However, many compounds used as flavors and fragrances have adverse reactions such as irritation and sensitization, so their use is usually limited. For example, according to the EU Cosmetics Regulation (EC) No 1223 / 2009, cosmetics must not contain substances such as citronellol, citral, and linalool (see Appendix III: "List of substances that cosmetics must not contain unless they meet the prescribed restrictions." Note: The restrictions on the above compounds are that they must be marked when used beyond the limited concentration, among which leave-on (no-rinse) products ≤ 0.001%, and cleansing products ≤ 0.01%). Therefore, it is necessary to conduct a safety analysis of the compounds provided in this article.

[0115] Interestingly, the compounds mentioned in the previous paragraph are common ingredients in some mosquito repellent products, especially those positioned as natural or plant essential oils. For example, the ingredient list of a mosquito repellent product is: 9% lemon eucalyptus oil, 3% camphor, and 1% menthol. According to the material composition of lemon eucalyptus oil, the citronellol content in the product is about 0.663%; another example is the ingredient list of a mosquito repellent product, which is 18% lemon eucalyptus oil and 2% lemon citronella oil. According to the material composition of lemon eucalyptus oil, the citronellol content in the product is about 1.32%. As "substances and preparations that come into contact with the human epidermis", these mosquito repellent products will inevitably lead to safety considerations if they are viewed from the perspective of cosmetics (see the EU's definition of cosmetics: substances and preparations that come into contact with the external organs of the human body (epidermis, hair, nails, lips and external genitalia), or teeth and oral mucosa in the mouth, with the main purpose of cleaning, emitting fragrance, improving appearance, improving body odor or protecting the body to keep it in good condition). The mandatory regulations on skin safety for mosquito repellent products are not as strict as those for cosmetics, so their irritation and allergenicity have not received sufficient attention. They may even be mistakenly believed to be safer because they only contain natural products.

[0116] In order to test whether the composition provided in this article has concerns about skin safety, the researchers of this article commissioned a third-party testing agency, ALS Global, to conduct a human repetitive injury patch test (HRIPT) on the 5% (v / v) (E)-8-decene-5-lactone solution (mixed solvent) described in Example 1 to evaluate skin irritation (contact dermatitis) and sensitization potential (contact allergy). The test process is as described in the Materials and Methods section above. The test results of the 5% (v / v) (E)-8-decene-5-lactone solution (mixed solvent) were that no obvious adverse skin reactions were observed in all volunteers during the induction and stimulation periods, indicating that under the HRIPT test conditions, the sample had no significant irritation or sensitization potential to the skin and was therefore deemed safe.

[0117] In addition to the consideration of irritation and sensitization, the impact of repellents on the ecological environment should also be considered because they are used in large quantities and remain in the environment. As mentioned above, citronella oil, picaridin and nootkatone are toxic to aquatic organisms. However, the exemplary repellent compounds (E)-8-decene-5-lactone and (Z)-7-decene-5-lactone in this article do not have such environmental risks in the evaluation reports published by the American Flavor Materials Research Institute (DOI: 10.1016 / j.fct.2021.112734; DOI: 10.1016 / j.fct.2022.112853).

[0118] Therefore, the composition provided in this article shows good safety in terms of skin and ecological environment, proving its potential as a compliant repellent product, and further confirming its application value in personal care products and cosmetics, which can effectively enhance the repellent effect of existing products on mosquitoes and other vector-borne pests.

[0119] Summary and discussion of examples

[0120] The above examples demonstrate that (E)-8-decene-5-lactone or its isomer (Z)-7-decene-5-lactone can effectively repel common pests such as mosquitoes, bed bugs, ticks and blood-sucking midges, and has a wide range of repellent effects. And under various experimental conditions, it shows better persistence than DEET, especially for mosquitoes and blood-sucking midges. Therefore, the repellent compound described herein has the potential to replace DEET, which is the gold standard of repellents, and be formulated into a new repellent composition together with a suitable carrier and / or excipient.

[0121] As a compound widely found in spices, pharmaceutical products, and food and beverage condiments, (E)-8-decene-5-lactone or its isomer (Z)-7-decene-5-lactone has accumulated safety data within its designated use through long-term use. This paper further evaluates its effects on human skin and the ecological environment when used as a repellent product, verifying its superior safety.

[0122] In terms of smell, DEET has a pungent and unpleasant organic solvent smell. In contrast, the (E)-8-decene-5-lactone and (Z)-7-decene-5-lactone mentioned in this article emit a floral and jasmine petal-like scent, with a delicate fruity aroma reminiscent of peaches, apricots and coconut milk. Therefore, the compounds described in this article are more suitable for preparing repellents or other daily care products that are easily accepted by consumers (especially children) than DEET.

Claims

1. A composition for repelling one or more disease-carrying insects selected from the order Diptera, Hemiptera and Acarina, the composition comprising one or more compounds conforming to the following general formula (I) and one or more carriers: (I) in, R 1 It is a C5 alkenyl group.

2. The composition according to claim 1, wherein the one or more compounds conforming to the general formula (I) are independently selected from the group of compounds conforming to the following general formula (Ia) and general formula (Ib): ， (Ia) (Ib).

3. The composition of claim 2, wherein the compound conforming to the general formula (Ia) is (E)-8-decene-5-lactone, and wherein the compound conforming to the general formula (Ib) is (Z)-7-decene-5-lactone.

4. A composition according to any one of claims 1 to 3, comprising two or more compounds of formula (I) and one or more carriers.

5. A composition according to claim 2 or 3, comprising a compound conforming to the general formula (Ia), a compound conforming to the general formula (Ib) and one or more carriers.

6. The composition according to any one of claims 1 to 3, wherein the carrier is an aqueous solvent, an organic solvent, or a mixture thereof.

7. The composition according to any one of claims 1 to 3, further comprising other substances having activity of repelling the disease-repelling insects.

8. A method for repelling one or more disease-causing pests selected from the order Diptera, Hemiptera and Acarina, the method comprising exposing the disease-causing pests to the composition of any one of claims 1 to 3.

9. The method according to claim 8, wherein the disease-carrying pests are mosquitoes, bed bugs, blood-sucking midges or ticks.

10. The method of claim 8, wherein the disease-causing pest is a mosquito.

11. The method of claim 10, wherein the mosquito belongs to the genus Aedes, Culex or Anopheles.

12. The method of claim 10, wherein the mosquito belongs to Aedes aegypti, Culex quinquefasciatus, Anopheles sinensis or Anopheles gambiae.

13. The method of claim 8, wherein exposing the pest to the composition comprises contacting the composition with an object or article. The method of claim 13 , wherein the subject is a human.

15. The method of claim 13, wherein the subject is a domesticated animal.

16. The method of claim 13, wherein the article is selected from the group consisting of furniture, clothing, candles, air diffusers, tablets, cosmetics, netting, building materials, and incense.

17. Use of a compound according to any one of claims 1 to 3 in the preparation of a preparation or product that can effectively repel one or more disease-carrying insect pests selected from the order Diptera, Hemiptera and Acarina, characterized in that: The compounds are useful as repellent active ingredients.

18. The use according to claim 17, wherein the disease-carrying pests are selected from mosquitoes, bed bugs, ticks and blood-sucking midges.

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