毒死蜱对蚊蝇和蟑螂毒杀作用的研究

本文系统地报道了毒死蜱对蚊、蝇和蟑螂的药效。实验室试验结果表明，毒死蜱对淡色库蚊幼虫的ＬＣ５０为０．００３４ｐｐｍ；对家蝇雌、雄虫的ＬＤ５０分别为０．０２４５和０．０１９７ｕｇ／虫；对德国小蠊雌、雄虫的ＬＤ５０分别为０．２１４２和０．１４５５ｕｇ／虫；对蚊、蝇和蟑螂在４种载体表面具有相当长的残留药效；按１３ｍｇ／ｍ＾３剂量喷雾后，对蚊、蝇的ＫＴ５０分别为４．２和４．７ｍｉｎ，２４ｈ死亡率均达１００     

95%顺式氯氰菊酯对蚊蝇的毒力研究

目的：测定９５％顺式氯氰菊酯对蚊幼虫、蝇成虫的毒力。方法浸液法和自动微量点滴法。结果：９５％顺式氯氰菊酯对蚊幼虫的ＬＣ５０为０．００１８１ｍｇ／Ｌ,是溴氰菊酯的１．３１倍,其相对毒力是溴氰菊酯的０．７６倍;对蝇成虫的ＬＤ５０为０．００３５９μｇ／虫,是溴氰菊酯的１．７７倍,其相对毒力是溴氰菊酯的０．５６倍。结论：国产９５％顺式氯氰菊酯对蚊蝇有很高的毒力,具有很好的应用前景。     

几种改进的漂浮颗粒剂灭中华按蚊和致倦库蚊的效果

目的：比较几种改进的漂浮颗粒剂灭中华按蚊和致倦库蚊幼虫的效果。方法：现场试验。结果：室内生物测定,Ｂ．ｔ．ｓ－１８７漂浮颗粒剂（荷叶型）ＬＤ５０为０．４０８７μｇ／ｍｌ,Ｂａｃｔｉｍｏｓ颗粒剂（荷叶型）ＬＤ５０为０．９３４４μｇ／ｍｌ,Ｂ．ｓ－Ｃ３－４１漂浮颗粒剂（荷叶型）ＬＤ５０为０．０５９９μｇ／ｍｌ。稻田灭中华按蚊幼虫的效果显示：两种Ｂ．ｔ．ｓ漂浮颗粒剂（荷叶型）０．８１ｇ／ｍ２剂量时,２４ｈ灭蚊效果均可达１００％。１８７漂浮颗粒剂持效可达１１ｄ,Ｂａｃｔｉｍｏｓ漂浮颗粒剂持效为８ｄ。１８７颗粒剂和Ｂ．ｓ－Ｃ３－４１颗粒剂现场灭致倦库蚊的效果显示：在０．６８ｇ／ｍ２剂量时,２４ｈ蚊幼密度下降率分别为１００％和９９．１％,持效分别为９ｄ和８ｄ。结论：采用荷叶粉为主要载体,在自然界中易于分解,不造成污染,而且灭蚊即效和持效均较好。     

一种新菊酯的合成及药效

本文介绍二氯菊酸酰氯与胺醇缩合制得一种新型菊酯类杀虫剂，并报道其合成路线。所得样品通过元素分析，理论值与实测值相符。其药效，对淡色库蚊幼虫的ＬＣ５０为０．００２６４ｐｐｍ，对家蝇为０．００１６５～０．００１８２μｇ／虫；以５ｍｇ／ｍ３剂量喷雾，对淡色库蚊成虫的ＫＴ５０为４．７ｍｉｎ，对家蝇为３．７ｍｉｎ，两者２４ｈ死亡率均为１００％。按５４ｍｇ／ｍ２剂量强迫接触试验，对美洲大蠊的ＫＴ５０为６．２ｍｉｎ，对德国小蠊为６．０ｍｉｎ。     

不同剂量奋斗呐浸泡不同布质蚊帐灭蚊效果观察

本文使用５％奋斗呐可湿性粉剂，分别以２．５ｍｇａ．ｉ／ｍ２、５ｍｇａ．ｉ／ｍ２、１０ｍｇａ．ｉ／ｍ２、２０ｍｇａ．ｉ／ｍ２和３０ｍｇａ．ｉ／ｍ２五个不同剂量浸泡棉纱，尼龙纱两种不同布质的蚊帐，进行蚊虫防制试验。同等剂量比较，速效和残效尼龙纱较锦质蚊帐毒杀效果为好。各剂量组ＫＴ５０均在３０ｍｉｎ以内，２４ｈ死亡率达１００％；用加热加速试验方法观察，所获指标推算持效可达１年以上。结果还表明，所用剂量尼龙纱蚊帐１０ｍｇａ．ｉ／ｍ２、棉纱蚊帐２０ｍｇａ．ｉ／ｍ２防制效果均较理想。     

家蝇对三种杀虫剂的抗性调查

用点滴法对合肥市家蝇的抗药性测定结果表明，９５年家蝇对ＤＤＶＰＬＤ５０为３．９２６６μｇ／♀抗性增长是８８年的２１倍，对二氯苯醚菊酯ＬＤ５０为０．１８７４ｕｇ／♀，是８８年的６．２倍，对胺菊酯ＬＤ５０为２．７４１８ｕｇ／♀。     

拟除虫菊酯混配水剂和单用水剂毒效比较

用拟除虫菊酯杀虫济制成２种混配水剂和２种单用水剂。经多次选配试验制成８号和２０１号两种混配水剂，对绥慢细蛋（Ｌ．ｓｅｇｎｉｓ）的毒力测定结果：ＫＴ５０分别为１ｍｉｎ１２ｓ和６ｍｉｎ５０ｓ；而ＬＣ５０分别为０．６９６４ＰＰｍ和２．１２２６ＰＰｍ；ＬＤ５０分别为０．００１２μｇ／ｃｍ２和０．００４４μｇ／ｃｍ２。毒力均较常用的奋斗呐和溴氰菊酯强。其中尤以８号毒力显著，是溴氰菊酯的８６～１１６倍左右；ＫＴ５０可加快约５倍。模拟试验结果：４种水剂处理砖面和大板面经５ｍｉｎ和５ｈ后，吸血印鼠客（Ｘ．ｃｈｅｏｐｉｓ）接触５分别的灭效为８０～１００％。     

苏云金杆菌以色列变种漂浮块剂现场灭致乏库蚊效果

应用湖北省医学科学院寄生虫病防治研究所研制的苏云金杆菌以色列变种（Ｂｔｉ）漂浮块剂在现场进行了灭致乏库蚊的效果评价，室内生物测定结果表明；Ｂｔｉ漂浮块剂对致加蚊ＬＤ５０为０．５２０７μｇ／ｍｌ，效价为２３３Ｉ／ｍｌ，在０．４－０．８ｍ＾２现场水缸中，用１０ｇ／ｍ＾２的剂量，第一次投药持１０天出现２龄幼虫，第二次投药特效可保持１１天，因此每１０天投一次药可有效控制水缸中蚊幼虫孳生。     

康其尔蟑螂克星的研究报告

实验室、模拟现场和现场一系列试验结果表明，康其尔牌蟑螂克星对蟑螂具有击倒快、灭效高、持效长、性能稳定、安全低毒等特点。其１：９水溶液按国家标准圆筒法测定，对德国小蠊的ＫＴ５０为２．３４０８ｍｉｎ，２４ｈ死亡率为１００％。按２５ｍｌ／ｍ２，５０ｍｌ／ｍ２剂量玻璃板滞留喷洒，１６周时ＫＴ５０分别为７．９２０６、５．２６５１ｍｉｎ，７２ｈ死亡率仍达９１．７％、９８．３％；模拟现场按２或１ｍｌ／ｍ３直接喷雾，其ＫＴ５０分别为９．１９７９、１２．１８４３ｍｉｎ，７２ｈ死亡率分别为１００％、９８．９％；现场试验按２５ｍｌ／ｍ２一次施药，灭效达９５．７～９６．７％。康其尔牌蟑螂克星１：９水溶液对小白鼠急性经口ＬＤ５０为６０６４．６ｍｇ／ｋｇ，对大白鼠急性经口ＬＤ５０为１０５５６ｍｇ／ｋｇ，对大白兔经皮ＬＤ５０（♀）＞９７５．６ｍｇ／ｋｇ，ＬＤ５０（♂）＞６３０．９ｍｇ／ｋｇ，大白鼠急性吸入ＬＣ５０＞１１０００ｍｇ／ｍ３／２ｈ，均属低毒，对大白兔眼、鼻无明显刺激症状。     

肉中喹诺酮药物残留的HPLC简易分析法

报道了用ＨＰＬＣ法同时测定畜禽肉中６种喹诺酮类药物［Ｂｅｎｏｆｌｏｘａｃｉｎ（ＢＦＬＸ）、Ｄａｎｏｆｌｏｘａｃｉｎ（ＤＮＦＸ）、Ｄｉｆｌｏｘａｃｉｎ（ＤＦＬＸ）、Ｅｎｒｏｆｌｏｘａｃｉｎ（ＥＲＦＸ）、Ｏｆｌｏｘａｃｉｎ（ＯＦＬＸ）、Ｏｒｂｉｆｌｏｘａｃｉｎ（ＯＢＦＸ）］残留的简易分析方法。用于猪肉、牛肉及鸡肉中６种药物的测定,回收率均为８０％以上,检出限为０００２５～００５ｍｇ／ｋｇ范围。ＨＰＬＣ条件　分析柱：ＴＳＫｇｅｌＯＤＳ８０Ｔｓ（４６ｍｍｉ．ｄ．×２５ｃｍ）;流动相：００５ｍ…     

右旋反式氯丙炔菊酯的合成及其药效研究

目的研制一种新型卫生杀虫剂--右旋反式氯丙炔菊酯.方法采用右旋反式DV菊酸与S-炔丙醇酮为原料,经化学拆分、酰氯化及酯化等反应合成右旋反式氯丙炔菊酯,并采用GB/T13917.1-1992和GB/T17322.2-1998标准方法测定了对致倦库蚊和德国小蠊的药效.结果右旋反式氯丙炔菊酯对致倦库蚊及德国小蠊的KT50值分别为8.5 min和3.46min.结论右旋反式氯丙炔菊酯对蚊虫和蟑螂等害虫具有良好的击倒作用和杀灭能力,可以作为一种新型卫生杀虫剂加以推广和应用.     

Enhanced antifertility activity of non-steroidal molecules with 3-n-butylamino-2-hydroxypropyloxy side chain

A comparative study of relative binding affinity (RBA) for estradiol-17 beta-receptors, estrogenicity and antifertility activity of compounds 2,2-dimethyl-3-phenyl-4-p-(3-n-butylamino-2-hydroxypropyloxy-pheny l)- 7-methoxycoumarin 4, 2,2-dimethyl-3-phenyl-4-p-(3-n-butylamino-2-hydroxy-propyloxyphenyl++ +)-7-methoxy chromene 5 and trans-2,2-dimethyl-3-phenyl-4-p-(3-n-butylamino-2-hydroxypropyloxyphe nyl)- 7-methoxychroman 6 with the corresponding 4-p-(beta-pyrrolidinoethoxyphenyl) compounds 1-3, is reported. It has been found that the introduction of the novel 3-n-butylamino-2-hydroxypropyloxy moiety in place of the classical tert-beta-aminoethoxy group leads to enhancement of antifertility activity.     

Theoretical,antioxidant and cytotoxic activities of caffeic acid phenethyl ester and chrysin

The structure–activity relationship was used to describe the antioxidant pharmacophore of caffeic acid phenethyl ester (CAPE) and chrysin by using quantum chemical calculations and the density functional theory method. The Becke three-parameter hybrid exchange functional in combination with the Lee–Yang–Parr correction functional protocol was employed for structure optimization and other computations. Theoretical calculations were conducted to explain the structure–activity relationship and pharmacokinetic behavior of CAPE and chrysin. The free radical scavenging activities of CAPE and chrysin were evaluated by using the 2,2-diphenyl-1-picrylhydrazyl assay. The cytotoxic effects of CAPE and chrysin on the human leukemia cell line (HL-60) were evaluated by using the 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide assay.     

In vitro neuroprotective effects of the leaf and fruit extracts of Juglans regia L. (walnut) through enzymes linked to Alzheimer's disease and antioxidant activity

Several extracts of the leaves and fruits of Juglans regia L. were assessed for their neuroprotective effects through antioxidant and anti-cholinesterase methods. Anticholinesterase activity was determined against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the enzymes vital for Alzheimer's disease, at 50, 100 and 200 μg ml(-1). Antioxidant activity was tested using radical scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), N,N-dimethyl-p-phenylenediamine (DMPD), superoxide (SO), nitric oxide (NO) and hydrogen peroxide (H(2)O(2)) radicals, as well as ferric ion-chelating capacity, ferric- and phosphomolybdenum-reducing antioxidant power at 500, 1000 and 2000 μg ml(-1). Total phenol and flavonoid quantification of the extracts was calculated. The extracts scavenged DPPH radical in varying degrees; however, they did not scavenge DPMD and H(2)O(2). Only the dichloromethane and water extracts were able to quench SO (10.09 ± 1.38%) and NO (24.09 ± 2.19%) radicals, respectively, at low level. The extracts showed either low or no BChE inhibition and no AChE inhibition.     

Synthesis and antitumor activity of cis-dichloridoplatinum(II) complexes of 1,1′-biisoquinolines

A simple approach to 1,1′,2,2′,3,3′,4,4′-octahydro-1,1′-biisoquinolines is described. Reaction of phenethylamines with oxalyl chloride led to N,N′-bis(phenethyl) oxamides (1). Cyclization of oxamides by using Bischler – Napieralski conditions gave 3,3′,4,4′-tetrahydro-1,1′-biisoquinoline(3) and unusual products 2, 4, 5. Reduction of 3,3′,4,4′-tetrahydro-1,1′-biisoquinolines with sodium boron hydride gave both rac-1,1′,2,2′,3,3′,4,4′-octahydro-1,1′-biisoquinolines(6) and meso-1,1′,2,2′,3,3′,4,4′ -octahydro-1,1′-biisoquinolines(7). Compound 6 was resolved to (1S, 1S′) (8) and (1R, 1R′) (9) furtherly. By treating all the biisoquinolines with K₂PtCl₄ afforded their cis-dichloridoplatinum (II) complexes (12–18). The antitumor activity of these complexes was evaluated.     

Structure elucidation of some minor components of the polybromobiphenyl mixture,Firemaster

The polybrominated biphenyl known as “Firemaster” is a flame retardant that accidentally became mixed with cattle feed in Michigan in 1973. The resulting toxicosis to animals and humans prompted extensive study to determine Firemaster's toxic components. Although 4 of 12 major Chromatographic peaks of Firemaster produce mixed enzyme induction, they do not account for the total toxicity. By capillary gas chromatography, it was observed that Firemaster FF-1, lot FH 7042, consisted of at least 60 compounds. We have isolated or otherwise determined the structure for 10 minor components of Firemaster: 3,3′,4,4′-tetra-,2,2′,3,5′, 6-penta-,2,2′,4,4′,5-penta-,3,3′, 4,4′,5-penta-,2,3,3′, 4,4′, 5-hexa-,2,3,3′,4,4′,5′-hexa-, 3,3′,4,4′,5,5′-hexa-, 2,2′, 3,3′,4,5,5′- hepta-,2,3,3′,4,4′,5,5′- hepta-and 2,2′,3,3′,4,5,6′- hepta-bromobiphenyl. All of these polybromobiphenyl congeners except 2,2′,4,4′,5-pentabromobiphenyl are in the latest eluting (most polar) fraction by normal-phase high-performance liquid chromatography of Firemaster. This fraction exhibits biological activity. Hyperkeratosis induction tests were carried out on rabbit ears with 3,3′,4,4′-tetra-,2,2′,3,5′, 6-penta-, 2,3,3′,4,4′,5-hexa-, 3,3′,4,4′,5,5′-hexa-, and 2,2′,3,3′,4,5,6′-heptabromobiphenyl, but only 3,3′,4,4′-tetra- and 3,3′,4,4′,5,5′-hexabromobiphenyl gave positive responses. Apparently, these two compounds and 3,3′,4,4′,5-pentabromobiphenyl are significant contributors to the hyperkeratotic activity of Firemaster.     

Carbamate resistance in mosquitos: The metabolism of propoxur by susceptible and resistant larvae of Culex pipiens fatigans*

Toxicity tests on Culex pipiens fatigans with propoxur (o-isopropoxyphenyl methylcarbamate) and carbofuran (2,2-dimethyl-2,3-dihydrobenzofuranyl-7-methylcarbamate) indicated that both compounds are fast-acting insecticides. Transfer of treated larvae to fresh water results in their partial recovery from knockdown.     

Antioxydant activity of β-carboline derivatives in the LDL oxidation model

A series of β-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO4 or 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH). The protective actions of these compounds against the cytotoxicity were evaluated with lactate dehydrogenase (LDH) activity in bovine aortic endothelial cells (BAECs) and cellular vitality by measuring mitochondrial activity in the presence of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). Most of compounds showed an higher antioxidant activity than GWC22 derivative (R=1.6 for 5 μM CuSO4). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R=1.9 to 2.8 for 1 μM CuSO4. These substances have protective actions and increase significantly the cell viability.     

江汉平原部分地区媒介按蚊对溴氰菊酯抗性监测分析

目的了解媒介按蚊对溴氰菊酯抗性,为合理使用杀虫剂提供科学依据。方法采用WHO成蚊滤纸接触法,观察首只蚊虫击倒时间、击倒率和死亡率,以区分剂量判定抗性级别,以开始击倒时间和击倒率评估Kdr抗性。结果江汉平原区媒介按蚊首只被溴氰菊酯击倒时间为6～25 min,接触60 min击倒率为1.00%～9.62%,KT50为1 003.5～24 099.78 min,抗性指数4.41～105.79,观察24 h死亡率为2.00%～8.65%,为高抗性群体。结论江汉平原按蚊对溴氰菊酯已产生高度抗性,应交替使用不同类型卫生杀虫剂,确保防治效果,延缓蚊虫抗性升级。     

Effect of heat treatment on total phenolic and anthocyanin contents as well as antioxidant activity of the extract from Aspergillus awamori-fermented black soybeans,a healthy food ingredient

Aspergillus awamori-fermented black soybeans, a healthy food ingredient, were subjected to heating at 40–100°C for 30 min. After heat treatment, the methanol extract of the fermented black soybeans was examined for antioxidant activity including the 2,2-diphenyl-1-picryl-hydrozyl radical-scavenging effect and the Fe²⁺-chelating ability. It was found that antioxidant activity exerted by the methanol extract was stable with heating at a temperature up to 80°C for 30 min. The extract showed a reduced antioxidant activity after heating the fermented black soybeans at 100°C for 30 min. However, it showed approximately 70% and 40%, respectively, of the original 2,2-diphenyl-1-picryl-hydrozyl radical-scavenging effect and the Fe²⁺-chelating ability. Heating also reduced the total phenolic and anthocyanin content in the fermented black soybeans, but this reduction did not coincide closely with the reduction of antioxidant activity observed.