An Insecticidal and Acaricidal Polysulfide Metabolite from the Roots of Petiveria alliacea

The present study reports on the insecticidal and acaricidal potentials of dibenzyltrisulfide (DBTS) isolated from the roots of Petiveria alliacea L. using thin layer and high performance liquid chromatography. The 96-h LD₅₀ value (μg per tick) obtained for adult Boophilus microplus (Canestrini) topically treated with DBTS was 0·920. The LD₅₀ values obtained for three commercial acaricides dimethoate, lindane and carbaryl were 4·6, 9·3 and 6·9 μg per tick respectively. The IOD₅₀ and IHD₅₀ (concentrations inhibiting egg laying and hatching by 50% respectively) in μg per tick doses for DBTS were 0·22 and 0·24 respectively. The 24-h LD₅₀ dose (μg per insect) obtained for DBTS on adult Cylas formicarius elegantulus (Summer) was 0·193 μg per insect. The vapour from a stock solution of 5 g litre^-1 of DBTS was highly toxic to adult Hypothenemus hampei Ferr. inside coffee berries, inflicting 89% mortality within 24 h. © 1997 SCI.     

烟草茎粗提取物对朱砂叶螨活性的初步研究

用浸渍法分别以石油醚、苯、乙醇、丙酮和水对烟草茎进行平行浸提,然后对浸提物进行了系统的室内杀螨活性试验。结果表明烟茎的石油醚、苯、乙醇、丙酮和水提取物均有一定的杀螨活性。其中,丙酮提取物活性最强。在2. 5 mg/mL浓度下,对朱砂叶螨24、48 h和72 h的校正死亡率分别为42.12%、75.84%和100%,对朱砂叶螨的致死中浓度为0.972 4 mg/mL。     

Acaricidal activity of triketone analogues derived from Leptospermum scoparium oil against house‐dust and stored‐food mites

BACKGROUND: Various attempts to control the populations of house‐dust and stored‐food mites have been implemented using synthetic chemicals. Although effective, the repeated use of these chemicals has led to resistance owing to the mite's high reproductive potential and short life cycle. Therefore, this study aimed to develop natural acaricides using oils derived from Leptospermum scoparium JR & G Forst., which may affect the overall biological activity of a mite without adverse effects. Results were compared with those from using benzyl benzoate and N,N‐diethyl‐3‐methylbenzamide (DEET). RESULTS: The LD₅₀ values of L. scoparium oil were 0.54, 0.67 and 1.12 µg cm^?2 against Dermatophagoides farinae (Hughes), D. pteronyssinus (Troussart) and Tyrophagus putrescentiae (Schrank) respectively. The active constituent isolated from L. scoparium was identified as leptospermone (6‐isovaleryl‐2,2,4,4‐tetramethyl‐1,3,5‐cyclohexanetrione) by spectroscopic analysis. Based on the LD₅₀ values of leptospermone and its derivatives, the most toxic compound against D. farinae was leptospermone (0.07 µg cm^?2), followed by 2,2,4,4,6,6‐hexamethyl‐1,3,5‐cyclohexanetrione (1.21 µg cm^?2), benzyl benzoate (10.03 µg cm^?2) and DEET (37.12 µg cm^?2). Furthermore, similar results were observed when the leptospermone and its derivatives were tested against D. pteronyssinus and T. putrescentiae. CONCLUSIONS: These results indicate that L. scoparium oil‐derived materials, particularly leptospermone and 2,2,4,4,6,6‐hexamethyl‐1,3,5‐cyclohexanetrione, have potential for development as new agents for the control of three species of mite. Copyright © 2008 Society of Chemical Industry     

马铃薯花杀螨活性成分分离、鉴定及其杀螨活性

以马铃薯花乙酸乙酯粗提物为分离对象,以朱砂叶螨Tetranychus cinnabarinus等4种叶螨为供试靶标,采用生物活性追踪法,分离得到2种具有杀螨活性的化合物 (     6a    和     2′a    )。依据质谱、核磁共振氢谱和碳谱,并结合相关文献数据鉴定了其化学结构,分别为江户樱花苷 (5, 7, 4′-三羟基二氢黄酮-7-O-β-D-吡喃葡萄糖苷)(     6a    ) 和α-卡茄碱 (     2′a    ),前者系首次从茄科植物马铃薯中分离得到。采用玻片浸渍法测定了2个化合物对朱砂叶螨等4种叶螨的触杀活性。结果表明,化合物     6a    (江户樱花苷) 对朱砂叶螨、二斑叶螨T. urticae和山楂叶螨T. viennensis 24 h LC₅₀值分别为461.98、338.76和732.08 mg/L,其触杀活性强于对照药剂鱼藤酮,相对毒力分别为鱼藤酮的1.17、1.52和3.07倍;化合物     2′a    (α-卡茄碱) 对二斑叶螨和山楂叶螨24 h LC₅₀分别为480.79和834.98 mg/L,相对毒力分别为鱼藤酮的1.07和2.69倍。可见,江户樱花苷和α-卡茄碱具有一定的杀螨活性和潜在的应用价值。     

瑞香狼毒中黄酮类化合物的化学成分及其对朱砂叶螨触杀活性的研究

为研究瑞香狼毒(Stellera chamaejasme L)中黄酮类化合物的杀螨活性,采用多种色谱技术分别对瑞香狼毒乙酸乙酯和正丁醇萃取物进行了分离纯化并获得3个黄酮类化合物。利用各种光谱技术鉴定其化学结构为瑞香狼毒素A（1）、槲皮素（2）和(+)-表枇杷素(3)。三种黄酮类化合物对朱砂叶螨（Tetranychus cinnabarinus B.）触杀活性的半致死浓度（LC50）值分别为 4.9434 mg?mL-1、7.6930 mg?mL-1、2.2494 mg?mL-1。实验结果表明,瑞香狼毒素A、槲皮素和(+)-表枇杷素均具有一定的杀螨活性, 其中表枇杷素杀螨活性最强。     

青蒿粗提物对朱砂叶螨生物活性的初步研究

用青蒿Artem isia annuaL.的石油醚、苯、乙醚、丙酮和水的平行提取物和顺序提取物对朱砂叶螨进行了系统的触杀活性研究。结果表明青蒿石油醚、苯、乙醚、丙酮和水提取物有一定的杀螨活性,其中10 g/L丙酮顺序粗提物活性最强,对朱砂叶螨48,72 h的校正死亡率分别为90.64%和100%,对该螨的致死中浓度为0.206 6 g/L。     

Efficacy of Chinese Herbal Medicine Canine Acariasis Spirit on Demodex canis

In order to screen the Chinese herbal medicine for the treatment of Demodex canis, canine acariasis spirit was prepared by Foeniculum vulgare, Fructus cnidii and Bauhinia by water alcohol precipitation and distillation extraction methods. To observe the effect on Demodex canis, canine acariasis spirit was set to high, medium and low concentrations, the content of crude drug were 2.0, 1.0 and 0.5 g/mL, respectively. The experiment of killing Demodex canis was carried out by drop method. On this basis, 12 dogs inoculated with Demodex canis were treated. In order to verify the therapeutic effect, 45 clinically diagnosed dogs with Demodex canis were divided into three groups. The results showed that 3 doses of the traditional Chinese medicine canine acariasis spirit all had strong inhibition effect to kill mites, the high dose group could completely kill Demodex canis only 4 h after treatment, the action of 1% ivermectin control group was 8 h after treatment; 3 weeks later, a large number of new hair grew, rash and skin nodules disappeared, the skin lesion had healed in the affected area of high dose group, in 1% ivermectin treatment group, the dog skin improved, only a small amount of new hair grew, it couldn't cure standard; In the high and middle dose group, the average number of the ratio of skin scraping mites and the recurrence rate after drug withdrawal was 0 in one month later; The average number of mites proportion and recurrence rates of skin scrapings in 1% ivermectin treatment group were 10.63% and 9.17% in one month later; After 3 weeks of treatment, the total average eggs negative rate, cure rate and average cure days were 100.00%, 93.33% and 19.56 d in high dose traditional Chinese medicine canine acariasis spirit and 1% ivermectin combined treatment group, the results were better than the traditional Chinese medicine canine acariasis spirit and 1% ivermectin alone treatment group. The results showed that the effect of the high dose group self-made Chinese medicine canine acariasis spirit on killing Demodex canis in vitro, inoculation of Demodex canis and clinical therapeutic effect of natural infection cases were significantly better than 1% ivermectin control group, canine acariasis spirit as a traditional Chinese medicine preparation would have a good market development prospects.     

五种外用中药制剂对兔螨病的疗效比较

分别采用药物与离体螨虫成虫直接接触法和药物外用于螨病患部,比较了花椒制剂、苦参水煎剂、苦楝皮水煎剂、明雄散、擦疥散5种外用中药制剂的杀螨作用和对兔螨病的疗效。通过5种中药制剂杀螨作用和治疗效果观察,结果表明花椒制剂杀螨效果最好,治愈螨病所需时间最短。     

含取代2-苯基吡啶基团的甲氧基氨基甲酸酯类化合物的合成及杀螨活性

以取代2-溴吡啶和羟基苯硼酸为原料,经Suzuki偶联和亲核取代两步反应合成了9个未见报道的含取代2-苯基吡啶基团的甲氧基氨基甲酸酯类化合物,其结构均经红外光谱、核磁共振氢谱及质谱(ESI-MS)表征。初步生物活性测定结果表明:在500 mg/L下,部分化合物对朱砂叶螨Tetranychus cinnabarinus的致死率达100%,具有作为杀螨剂先导结构的潜力。