CN104855398A - Application of beta-sitosterol linoleate and acaricide - Google Patents

Application of beta-sitosterol linoleate and acaricide Download PDF

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CN104855398A
CN104855398A CN201510158336.5A CN201510158336A CN104855398A CN 104855398 A CN104855398 A CN 104855398A CN 201510158336 A CN201510158336 A CN 201510158336A CN 104855398 A CN104855398 A CN 104855398A
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acaricide
sitosterol
linoleate
sitosterol linoleate
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CN104855398B (en
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代光辉
陈义娟
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Shanghai Jiao Tong University
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Abstract

The invention provides application of beta-sitosterol linoleate and an acaricide. The acaricide is composed of beta-sitosterol linoleate and conventional accessory materials, wherein the mass of beta-sitosterol linoleate accounts for 0.05 to 99% of the mass of the beta-sitosterol linoleate acaricide while the accessory materials account for 1 to 99.95%. The acaricide is a novel, harmonious and environment-friendly acaricide safy to people and livestock and is of profound significance to protection of the ecological environment, human health and comprehensive control of diseases.

Description

β-谷甾醇亚油酸酯的用途及杀螨剂The use and acaricide of β-sitosterol linoleate

技术领域technical field

本发明涉及一种农药技术领域,具体的,涉及一种β-谷甾醇亚油酸酯的用途和β-谷甾醇亚油酸酯杀螨剂。The invention relates to the technical field of pesticides, in particular to the use of β-sitosterol linoleate and a miticide of β-sitosterol linoleate.

背景技术Background technique

植食性螨类在世界各地的农作物上都有发现,它具有体积小、繁殖快、适应性强以及易产生抗药性等特点,是公认的很难防治的有害生物群落。目前中国的农药市场上所用的杀螨剂大多依赖进口,进口杀螨剂的费用占总进口农药费用的88.8%。而且螨类对作物造成的损失,在过去30年有了明显的增加。主要原因是密集的单一栽培和使用非专一性杀虫剂。其次是由于螨类一个世代的生长时间较短,对原有杀螨剂能迅速产生抗性。这些杀虫剂往往杀螨活性并不高,在杀死螨类的同时也消灭了螨类天敌。目前,化学农药的3R问题即残留(Residue)、抗性(Resistance)及害虫再猖獗(Resurgence)普遍受到人们的关注,人类对农药的认识也越来越深刻,农药的使用并不注重杀死害虫,而是更注重调节。因此,使用专性杀螨剂成为防治植食性螨类的主要措施,杀螨剂的发展必然朝着高效、广谱、低毒、安全的生物农药及昆虫激素型农药方向发展,满足市场的需求。Herbivorous mites are found on crops all over the world. They have the characteristics of small size, fast reproduction, strong adaptability and easy resistance to pesticides. They are recognized as harmful biological communities that are difficult to control. At present, most of the acaricides used in China's pesticide market rely on imports, and the cost of imported acaricides accounts for 88.8% of the total cost of imported pesticides. Moreover, the loss of crops caused by mites has increased significantly in the past 30 years. The main reasons are intensive monoculture and the use of non-specific insecticides. Secondly, due to the short growth time of one generation of mites, they can quickly develop resistance to the original acaricides. These insecticides often have low acaricidal activity, and they also eliminate the natural enemies of the acarids while killing the acarids. At present, the 3R problems of chemical pesticides, namely Residue, Resistance and Resurgence, are generally concerned by people, and people's understanding of pesticides is becoming more and more profound. pests, but more focus on regulation. Therefore, the use of specific acaricides has become the main measure to prevent and control phytophagous mites, and the development of acaricides is bound to develop in the direction of high-efficiency, broad-spectrum, low-toxicity, and safe biological pesticides and insect hormone-based pesticides to meet the needs of the market .

β-谷甾醇亚油酸酯(β-sitosterol linoleate),淡黄色油状物,分子式:C47H8002,分子量:676,是一种重要的植物甾醇酯,可由β-谷甾醇和亚油酸经酯化而得,像如可以采用有机相酶催化酯化反应,也可以从植物中提制获得,像如川赤芍、栀子皮等。它不仅可以改善甾醇的油溶性,方便在食品加工中应用,还兼有β-谷甾醇和亚油酸两种活性成分的生物学功能,并且现有研究报道其具有很强的抗氧化以及杀菌作用。β-sitosterol linoleate (β-sitosterol linoleate), pale yellow oil, molecular formula: C 47 H 80 0 2 , molecular weight: 676, is an important phytosterol ester, which can be synthesized from β-sitosterol and linoleum The acid is obtained through esterification, such as by using an organic phase enzyme to catalyze the esterification reaction, or it can be extracted from plants, such as Radix Paeoniae Rubra, Gardenia Bark, etc. It can not only improve the oil solubility of sterols and facilitate its application in food processing, but also has the biological functions of the two active ingredients of β-sitosterol and linoleic acid, and existing research reports that it has strong antioxidant and bactericidal properties effect.

经对现有的技术文献检索发现,目前尚无β-谷甾醇亚油酸酯在制备杀螨剂中的应用报道;目前也没有一种与环境兼容性好、对哺乳动物安全的和谐杀螨剂。After searching the existing technical literature, it is found that there is no report on the application of β-sitosterol linoleate in the preparation of acaricides; there is no harmonious acaricide that is compatible with the environment and safe for mammals. agent.

发明内容Contents of the invention

本发明针对现有技术存在的上述不足,提供一种高效、无残留、生产成本低、经济实用、环境友好、综合性能优良的一种β-谷甾醇亚油酸酯杀螨剂及其制备和新用途。The present invention aims at the above-mentioned deficiencies existing in the prior art, and provides a kind of β-sitosterol linoleate acaricide with high efficiency, no residue, low production cost, economical and practical, environment-friendly, and excellent comprehensive performance and its preparation and new use.

本发明目的是通过如下技术方案实现的:The object of the invention is achieved through the following technical solutions:

本发明提供一种β-谷甾醇亚油酸酯的用途,即将β-谷甾醇亚油酸酯应用于制备杀螨剂。The invention provides the use of β-sitosterol linoleate, that is, the application of β-sitosterol linoleate to prepare acaricide.

优选地,所述螨可以是朱砂叶螨,二斑叶螨等植物害螨。Preferably, the mite may be plant pest mites such as Tetranychus cinnabarinus and Tetranychus urticae.

本发明提供一种β-谷甾醇亚油酸酯杀螨剂,所述杀螨剂是由β-谷甾醇亚油酸酯(即原料药)与常规辅料组成。其中β-谷甾醇亚油酸酯的质量占β-谷甾醇亚油酸酯杀螨剂质量的0.05%-99%,常规辅料占β-谷甾醇亚油酸酯杀螨剂质量的1%-99.95%。The invention provides a β-sitosterol linoleate acaricide, and the miticide is composed of β-sitosterol linoleate (ie raw material medicine) and conventional auxiliary materials. Wherein the quality of β-sitosterol linoleate accounts for 0.05%-99% of the quality of β-sitosterol linoleate acaricide, and conventional auxiliary materials account for 1% of the quality of β-sitosterol linoleate acaricide- 99.95%.

优选地,所述常规辅料为增溶剂、增效剂、乳化剂、渗透剂等等一种或多种。Preferably, the conventional auxiliary materials are one or more of solubilizers, synergists, emulsifiers, penetrating agents and the like.

优选地,所述增溶剂是十二烷基苯磺酸钠、十二烷基苯磺酸钾、聚山梨酯、聚乙二醇、山梨醇聚氧乙醚、木质素磺酸盐、茶枯、搭皂角等等所有中的一种或多种。Preferably, the solubilizer is sodium dodecylbenzenesulfonate, potassium dodecylbenzenesulfonate, polysorbate, polyethylene glycol, sorbitol polyoxyethyl ether, lignosulfonate, tea, Take one or more of all the saponins and so on.

优选地,所述乳化剂为司盘类、吐温类、乙二醇酯类、丙二醇酯类和/或聚乙二醇型非离子表面活性剂等中一种或多种。Preferably, the emulsifier is one or more of Spans, Tweens, ethylene glycol esters, propylene glycol esters and/or polyethylene glycol-type nonionic surfactants.

优选地,所述增效剂为茶皂素、聚氧乙烯醚等中一种或多种。Preferably, the synergist is one or more of tea saponin, polyoxyethylene ether and the like.

优选地,所述渗透剂为氮酮等。Preferably, the penetrating agent is azone or the like.

称取一定的β-谷甾醇亚油酸酯用溶剂溶解,选择加入各种辅料,像如,增溶剂、增效剂、乳化剂、渗透剂等等,按照各种工艺,制成各种形式的杀螨剂,例如:粉剂,乳油、悬浮剂、干悬浮剂,浓乳剂、缓释剂、水乳剂、喷雾剂等。其中,溶剂可以是水、乙醇、甲醇、丙酮、环己酮、石油醚、石油芳烃、纯苯、乙酸乙酯、甲苯、二甲苯等所有有机溶剂中的一种或多种。Weigh a certain amount of β-sitosterol linoleate and dissolve it in a solvent, choose to add various auxiliary materials, such as solubilizers, synergists, emulsifiers, penetrants, etc., and make various forms according to various processes Acaricides, such as: powder, emulsifiable concentrate, suspension concentrate, dry suspension concentrate, concentrated emulsion, sustained release agent, water emulsion, spray, etc. Wherein, the solvent can be one or more of all organic solvents such as water, ethanol, methanol, acetone, cyclohexanone, petroleum ether, petroleum aromatics, pure benzene, ethyl acetate, toluene, and xylene.

本发明上述β-谷甾醇亚油酸酯杀螨剂的应用,具体为:在常温搅拌下将水加入到β-谷甾醇亚油酸酯杀螨剂中,使其稀释至β-谷甾醇亚油酸酯即原料药占0.5-40wt%的浓度后喷洒施用。The application of the above-mentioned β-sitosterol linoleate acaricide of the present invention is specifically: adding water to the β-sitosterol linoleate acaricide under normal temperature stirring, making it dilute to β-sitosterol linoleate The oleic acid ester, that is, the crude drug, accounts for 0.5-40 wt% concentration and then is sprayed.

与现有技术相比,本发明具有以下有益效果:Compared with the prior art, the present invention has the following beneficial effects:

本发明提供了一种对人畜安全、环境友好型的新型和谐杀螨剂,对生态环境保护、人类健康以及病害的综合治理都具有深远的意义。与传统的农药相比,本发明具有以下特点和优点:The invention provides a novel harmonious acaricide that is safe for humans and animals and friendly to the environment, and has far-reaching significance for ecological environment protection, human health and comprehensive control of diseases. Compared with traditional pesticides, the present invention has the following characteristics and advantages:

(1)β-谷甾醇亚油酸酯是一种天然产物,具有无毒,易降解等特点,对于人、畜和生态环境是友好的,安全的;(1) β-sitosterol linoleate is a natural product, which is non-toxic and easy to degrade, and is friendly and safe to humans, animals and the ecological environment;

(2)β-谷甾醇亚油酸酯来源容易,可以利用酯化反应合成,也可以从植物中直接提取,方法简单易行,可进行大规模工业化生产;(2) The source of β-sitosterol linoleate is easy, can be synthesized by esterification reaction, and can also be directly extracted from plants. The method is simple and easy, and can be used for large-scale industrial production;

(3)本发明是首次发现β-谷甾醇亚油酸酯具有杀螨生物活性,并首次将其配制成杀螨剂。经实验,对朱砂叶螨防效可达95.3%。(3) The present invention is the first discovery that β-sitosterol linoleate has acaricidal biological activity, and it is formulated as acaricide for the first time. Through experiments, the control effect on Tetranychus cinnabarinus can reach 95.3%.

具体实施方式Detailed ways

下面结合具体实施例对本发明进行详细说明。以下实施例将有助于本领域的技术人员进一步理解本发明,但不以任何形式限制本发明。应当指出的是,对本领域的普通技术人员来说,在不脱离本发明构思的前提下,还可以做出若干变形和改进。这些都属于本发明的保护范围。The present invention will be described in detail below in conjunction with specific embodiments. The following examples will help those skilled in the art to further understand the present invention, but do not limit the present invention in any form. It should be noted that those skilled in the art can make several modifications and improvements without departing from the concept of the present invention. These all belong to the protection scope of the present invention.

实施例1Example 1

称取β-谷甾醇亚油酸酯2.5g,用20g乙醇溶液溶解,添加5g吐温-80,溶解,按照常规工艺,制成本发明β-谷甾醇亚油酸酯杀螨剂,然后在所制的β-谷甾醇亚油酸酯杀螨剂中加水稀释,使β-谷甾醇亚油酸酯,即原料药的浓度为1%。最后,将稀释后的β-谷甾醇亚油酸酯杀螨剂对朱砂叶螨进行室内生物活性测定,方法根据国家南方农药创制中心生测SOP中的叶螨浸茎浸渍法进行。24小时后调查各处理的死活虫数,其防效为77.8%。Take by weighing β-sitosterol linoleate 2.5g, dissolve with 20g ethanol solution, add 5g Tween-80, dissolve, according to routine process, make β-sitosterol linoleate acaricide of the present invention, then in The prepared β-sitosterol linoleate acaricide is diluted with water so that the concentration of β-sitosterol linoleate, that is, the bulk drug, is 1%. Finally, the diluted β-sitosterol linoleate acaricide was tested for indoor biological activity against Tetranychus cinnabarinus, and the method was carried out according to the dipping method of spider mite stems in the Bioassay SOP of the National Southern Pesticide Innovation Center. After 24 hours, the number of dead and alive insects in each treatment was investigated, and the control effect was 77.8%.

实施例2Example 2

称取β-谷甾醇亚油酸酯38g,用12g乙酸乙酯溶解,在其中加入乳化剂等25g,按照常规工艺,制成本发明β-谷甾醇亚油酸酯杀螨剂,然后在所制的β-谷甾醇亚油酸酯杀螨剂中加水稀释,使β-谷甾醇亚油酸酯,即原料药的浓度为24%。最后,将稀释后的β-谷甾醇亚油酸酯杀螨剂对朱砂叶螨进行室内生物活性测定,方法根据国家南方农药创制中心生测SOP中的叶螨浸茎浸渍法进行。24小时后调查各处理的死活虫数,其防效为93.8%。Take by weighing β-sitosterol linoleate 38g, dissolve with 12g ethyl acetate, add emulsifying agent etc. 25g therein, according to routine process, make β-sitosterol linoleate acaricide of the present invention, then in place The prepared β-sitosterol linoleate acaricide is diluted with water so that the concentration of β-sitosterol linoleate, that is, the bulk drug, is 24%. Finally, the diluted β-sitosterol linoleate acaricide was tested for indoor biological activity against Tetranychus cinnabarinus, and the method was carried out according to the dipping method of spider mite stems in the Bioassay SOP of the National Southern Pesticide Innovation Center. After 24 hours, the number of dead and alive insects in each treatment was investigated, and the control effect was 93.8%.

实施例3Example 3

称取β-谷甾醇亚油酸酯80g,用10g乙醇溶解,在其中加入乳化剂司盘-20等10g,按照常规工艺,制成本发明β-谷甾醇亚油酸酯杀螨剂,然后在所制的β-谷甾醇亚油酸酯杀螨剂中加水稀释,使β-谷甾醇亚油酸酯即原料药的浓度为37%。最后,将稀释后的β-谷甾醇亚油酸酯杀螨剂对朱砂叶螨采用室内盆栽法进行生测,24小时后统计死亡率,其防效为98.6%。Take by weighing β-sitosterol linoleate 80g, dissolve with 10g ethanol, add emulsifier Span-20 etc. 10g therein, according to routine process, make β-sitosterol linoleate acaricide of the present invention, then Add water to dilute the prepared β-sitosterol linoleate acaricide, so that the concentration of β-sitosterol linoleate, that is, the bulk drug, is 37%. Finally, the diluted β-sitosterol linoleate acaricide was used for biotesting against Tetranychus cinnabarinus by indoor pot method, and the mortality rate was counted after 24 hours, and its control effect was 98.6%.

实施例4Example 4

称取β-谷甾醇亚油酸酯200g,用550g甲醇溶解,在其中加入乳化剂吐温-245,司盘-20等250g,按照常规工艺,制成本发明β-谷甾醇亚油酸酯杀螨剂,然后在所制的β-谷甾醇亚油酸酯杀螨剂中加水稀释,使β-谷甾醇亚油酸酯即原料药的浓度为7%。最后,将稀释后的β-谷甾醇亚油酸酯杀螨剂对朱砂叶螨采用室内盆栽法进行生测,24小时后统计死亡率,其防效为95.3%。Take by weighing 200g of β-sitosterol linoleate, dissolve with 550g methanol, add emulsifier Tween-245 therein, 250g of Span-20 etc., according to conventional process, make β-sitosterol linoleate of the present invention The acaricide is then diluted with water in the prepared β-sitosterol linoleate acaricide, so that the concentration of the β-sitosterol linoleate, that is, the bulk drug, is 7%. Finally, the diluted β-sitosterol linoleate acaricide was used to conduct a biotest against Tetranychus cinnabarinus in an indoor pot method, and the mortality was counted after 24 hours, and its control effect was 95.3%.

实施例5Example 5

称取β-谷甾醇亚油酸酯500g,用40g石油醚溶解,在其中加入乳化剂、增效剂、增溶剂等辅料15g,按照常规工艺,制成本发明β-谷甾醇亚油酸酯杀螨剂,然后在所制的β-谷甾醇亚油酸酯杀螨剂中加水稀释,使β-谷甾醇亚油酸酯即原料药的浓度为16%。最后,将稀释后的β-谷甾醇亚油酸酯杀螨剂对朱砂叶螨采田间小区实验进行田间药效试验,48小时后统计死亡率,防效达到92.3%。Take by weighing β-sitosterol linoleate 500g, dissolve with 40g sherwood oil, add emulsifier, synergist, solubilizing agent etc. adjuvant 15g therein, according to routine process, make β-sitosterol linoleate of the present invention The acaricide is then diluted with water in the prepared β-sitosterol linoleate acaricide, so that the concentration of the β-sitosterol linoleate, that is, the bulk drug, is 16%. Finally, the field efficacy test of the diluted β-sitosterol linoleate acaricide against Tetranychus cinnabarinus was carried out in field experiments, and the mortality rate was counted after 48 hours, and the control effect reached 92.3%.

以上对本发明的具体实施例进行了描述。需要理解的是,本发明并不局限于上述特定实施方式,本领域技术人员可以在权利要求的范围内做出各种变形或修改,这并不影响本发明的实质内容。Specific embodiments of the present invention have been described above. It should be understood that the present invention is not limited to the specific embodiments described above, and those skilled in the art may make various changes or modifications within the scope of the claims, which do not affect the essence of the present invention.

Claims (9)

1.一种β-谷甾醇亚油酸酯的用途,其特征在于,将β-谷甾醇亚油酸酯应用于制备杀螨剂。1. the purposes of a kind of β-sitosterol linoleate, it is characterized in that, β-sitosterol linoleate is applied to prepare acaricide. 2.根据权利要求1所述的β-谷甾醇亚油酸酯的用途,其特征在于,所述螨是朱砂叶螨或二斑叶螨。2. The purposes of β-sitosterol linoleate according to claim 1, characterized in that, the mite is Tetranychus cinnabarinus or Tetranychus urticae. 3.一种β-谷甾醇亚油酸酯杀螨剂,其特征在于,所述杀螨剂是由β-谷甾醇亚油酸酯与常规辅料组成,其中β-谷甾醇亚油酸酯的质量占β-谷甾醇亚油酸酯杀螨剂质量的0.05%-99%,常规辅料占β-谷甾醇亚油酸酯杀螨剂质量的1%-99.95%。3. a β-sitosterol linoleate acaricide, is characterized in that, described acaricide is made up of β-sitosterol linoleate and conventional adjuvant, wherein the β-sitosterol linoleate The mass accounts for 0.05%-99% of the mass of the β-sitosterol linoleate acaricide, and the conventional auxiliary materials account for 1%-99.95% of the mass of the β-sitosterol linoleate acaricide. 4.根据权利要求3所述的β-谷甾醇亚油酸酯杀螨剂,其特征在于,所述常规辅料是指增溶剂、增效剂、乳化剂、渗透剂中一种或多种。4. β-sitosterol linoleate acaricide according to claim 3, is characterized in that, described conventional adjuvant refers to one or more in solubilizer, synergist, emulsifier, penetrant. 5.根据权利要求4所述的β-谷甾醇亚油酸酯杀螨剂,其特征在于,所述增溶剂是十二烷基苯磺酸钠、十二烷基苯磺酸钾、聚山梨酯、聚乙二醇、山梨醇聚氧乙醚、木质素磺酸盐、茶枯、搭皂角中的一种或多种。5. β-sitosterol linoleate acaricide according to claim 4, is characterized in that, described solubilizer is sodium dodecylbenzenesulfonate, potassium dodecylbenzenesulfonate, polysorbate One or more of esters, polyethylene glycol, sorbitol polyoxyethyl ether, lignosulfonate, tea dead, and saponin. 6.根据权利要求4所述的β-谷甾醇亚油酸酯杀螨剂,其特征在于,所述乳化剂为司盘类、吐温类、乙二醇酯类、丙二醇酯类和/或聚乙二醇型非离子表面活性剂中的一种或多种。6. β-sitosterol linoleate acaricide according to claim 4, is characterized in that, described emulsifier is Span class, Tween class, ethylene glycol esters, propylene glycol esters and/or One or more of polyethylene glycol type nonionic surfactants. 7.根据权利要求4所述的β-谷甾醇亚油酸酯杀螨剂,其特征在于,所述增效剂为茶皂素、聚氧乙烯醚中的一种或多种。7. The β-sitosterol linoleate acaricide according to claim 4, characterized in that, the synergist is one or more of tea saponin and polyoxyethylene ether. 8.根据权利要求4所述的β-谷甾醇亚油酸酯杀螨剂,其特征在于,所述渗透剂为氮酮。8. The β-sitosterol linoleate acaricide according to claim 4, characterized in that, the penetrating agent is azone. 9.一种权利要求3-8任一项所述的β-谷甾醇亚油酸酯杀螨剂的应用,其特征在于,在常温搅拌下将水加入到β-谷甾醇亚油酸酯杀螨剂中,使其稀释至β-谷甾醇亚油酸酯即原料药占0.5-40wt%的浓度后喷洒施用。9. An application of the β-sitosterol linoleate acaricide described in any one of claims 3-8, characterized in that, water is added to the β-sitosterol linoleate miticide under normal temperature stirring. In the acaricide, it is diluted to the concentration of β-sitosterol linoleate, that is, the raw material drug accounts for 0.5-40wt%, and then it is sprayed and applied.
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