芫菁科不同种类成虫体内斑蝥素的含量

芫菁体内含有斑蝥素,是一种重要的药用昆虫。近年来我国对斑蝥素的临床应用研究表明：斑蝥素及其衍生物对治疗原发性肝癌疗效显著。为了摸清我国芫菁科昆虫的自然资源和虫体内斑蝥素的含量,作者调查了不同地区、不同寄主植物上芫菁科昆虫的种类分布,并利用气相色谱内标法测定了不同性别以及交尾高峰前后的芫菁成虫体内斑蝥素的含量。发现雄性成虫体内斑蝥素的含量均高于雌性成虫。交配高峰后的芫菁雌性成虫体内斑蝥素含量高于交配高峰前的芫菁雌性成虫体内斑蝥素含量。     

芫菁科昆虫体内斑蝥素的气相色谱法测定

分别采用酸水解法和直接浸提法处理不同种芫菁样品、短翅豆芫菁Epicauta aptera Kaszab的卵和大斑芫菁Mylabris phalerata Pallas的不同虫体部位,后用气相色谱仪测定斑蝥素含量。结果表明:用酸水解法处理后的芫菁体内斑蝥素含量较之用直接浸提法处理后有显著提高,增高幅度在1~9倍之间,其中以豆芫菁属Epicauta昆虫的增高幅度最大,一般在7倍以上,而斑芫菁属Mylabris的斑蝥素含量增幅不高,芫菁卵中斑蝥素含量变化不显著;斑蝥素主要富集于大斑芫菁的腹部。     

中国药用甲虫——芫菁科的资源考察与利用

芫菁是重要的药用甲虫。为了摸清我国芫菁科的自然资源,作者自1989-1991年系统的调查了我国南、北方6个省区的芫菁科的种类与分布,明确了其中分布广数量大的优势种,从而为芫菁科的自然资源利用提供了理论依据。对优势种所含斑蟊素的测定,首先用薄层层析法鉴别其斑蟊素斑点的颜色和显著程度,然后用气相色谱法进行含量测定。结果表明测定的19种中有80%。左右的种类其斑蟊素含量超过了《中华人民共和国药典》中写明的斑蟊素含量不得低于0.35%始能人药的规定,明显地扩大了可以人药的种类。作为对照：作者选择了医药部门经常与芫菁混杂出售或使用的红斑郭公虫以及过去文献中记载含有斑蟊素的红蝉(同翅目),用气相色谱法进行斑蟊素的含量测定,结果表明二者均不含斑蟊素。     

芫菁体内斑蝥素的含量及存在形式

【目的】测定芫菁体内斑蝥素的含量及其存在形式。【方法】利用气相色谱法测定了8种芫菁和作为对照的黑翅红蝉体内总斑蝥素和游离斑蝥素的含量,总斑蝥素含量是通过酸水解法测得的,游离斑蝥素含量是通过直接浸提法测得的,以总斑蝥素与游离斑蝥素含量之差作为结合斑蝥素含量; 并比较了结合斑蝥素与钙、镁含量之间的相关性。【结果】芫菁体内总斑蝥素的含量为游离斑蝥素含量的1～9倍,总斑蝥素的含量一般多于虫体干重的2.0%,而游离斑蝥素的含量均低于虫体干重的1.7%。黑翅红蝉体内不含任何形式的斑蝥素。斑芫菁属和豆芫菁属昆虫中的结合斑蝥素含量与钙元素呈正相关,斑芫菁属中结合斑蝥素含量与镁元素呈正相关,而豆芫菁属中结合斑蝥素含量与镁元素呈负相关。斑芫菁属昆虫体内钙元素的摩尔量要低于结合斑蝥素的摩尔量。【结论】芫菁体内总斑蝥素含量远高于游离斑蝥素的含量;结合斑蝥素可能是以斑蝥素酸钙和斑蝥素酸镁形式存在。     

中国药用甲虫──芫菁科的资源考察与利用

芫菁是重要的药用甲虫。为了摸清我国芜菁科的自然资源,作者自１９８９—１９９１年系统的调查了我国南、北方６个省区的芜菁科的种类与分布,明确了其中分布广数量大的优势种,从而为芫菁科的自然资源利用提供了理论依据。对优势种所含斑蟊素的测定,首先用薄层层析法鉴别其斑蟊素斑点的颜色和显著程度,然后用气相色谱法进行含量测定。结果表明测定的１９种中有８０％左右的种类其斑蟊素含量超过了。中华人民共和国药典。中写明的斑合素含量不得低于０．３５％始能人药的规定。明显地扩大了可以人药的种类。作为对照,作者选择了医药部门经常与芫菁混杂出售或使用的红斑郭公虫以及过去文献中记载含有斑蟊素的红蝉（同翅目）,用气相色谱法进行斑蟊素的含量测定,结果表明二者均不含斑蟊素。     

斑蝥素合成期的芫菁蛋白质表达差异分析

研究斑蝥素大量合成期的芫菁体内可溶性蛋白,有助于阐明斑蝥素合成相关酶蛋白的种类和合成机理.本研究采用SDS-PAGE、双向电泳技术,分析了苹斑芫菁Mylabris calida Palla在斑蝥素合成前期、大量合成早期和末期的蛋白质组成的变化.SDS-PAGE电泳分析显示,芫菁从羽化1 h到25 d过程中分子量约为80 kDa,45 kDa,30 kDa的蛋白组分存在着显著地表达差异.进而通过双向电泳分析,发现合成前期蛋白质与其它时期有明显差异:蛋白质大多分布在Pl值4～7,分子量20～80 kDa的区域,其中20～45 kDa蛋白质差异明显.芫菁羽化后1h、2d、4d的蛋白质点数目分别为471个、569个、645个;大量合成早期和合成末期为827个和999个,增长25%以上.研究结果显示:3个时期蛋白质组成的变化趋势恰好与芫菁合成斑蝥素含量显著峰值变化相吻合,表明芫菁体内斑蝥素的合成是多种蛋白参与的复杂过程,这些蛋白分子量范围在20～45 kDa.     

人工饲养条件下眼斑芫菁不同发育阶段斑蝥素含量的变化

【目的】分析人工饲养条件下眼斑芫菁Mylabris cichorii Linnaeus不同发育阶段体内斑蝥素含量的变化。【方法】收集不同发育阶段的眼斑芫菁,通过热碱浸提法提取斑蝥素,而后以气相色谱法检测含量。【结果】在幼虫期,1龄幼虫斑蝥素相对含量最高,2龄幼虫斑蝥素相对含量降到最低点;以后随着虫体的发育,幼虫体重和斑蝥素含量都逐渐增加。羽化后的成虫经隔离饲养,雄虫在羽化后5～30天大量合成斑蝥素,而雌虫体内斑蝥素含量则极低,具有典型的性二型现象;雌雄混合饲养组中,20～30天雌虫体内可以检测到大量斑蝥素,而同期雄虫斑蝥素含量远低于隔离饲养组。【结论】幼虫期斑蝥素含量随虫体发育而增加;成虫期主要由雄虫合成斑蝥素。混合饲养组成虫平均单头斑蝥素含量高于隔离饲养组雌雄虫平均斑蝥素含量。成虫身体各部位的斑蝥素含量以腹部最高,胸部次之。     

疆芫菁科的区系组成及药用价值(鞘翅目：芫菁科)

调查表明,新疆芫菁科(Meloidlc)昆虫有41种,分隶于5属,以斑芫菁属Mylabris F.种类最多,达32种,占78.0%;在41种中,有10种为我国首次纪录。区系组成含中亚细亚,蒙古,欧洲,准噶尔和泛古北种五种成分,其中以中亚细亚种最多,达23种,约占56.0%。芫菁是药用昆虫,对常见的10种芫菁药用有效成分-斑蝥素含量进行了测定,发现其中,种含量较高,药用价值明显。     

芫菁斑蝥素对几种动物蛋白磷酸酶2A的抑制作用

研究斑蝥素对马、兔、猪、鸡、眼斑芫菁Mylabris cichorii(L.)等几种动物体内PP2A的抑制作用。将斑蝥素作用于马、兔、猪、鸡、眼斑芫菁等几种动物体内的PP2A,采用蛋白磷酸酶抑制法-比色法测定斑蝥素对PP2A的抑制率。斑蝥素对马、兔、猪等哺乳动物体内的PP2A有明显的抑制作用,IC50分别为0.07、0.12、0.23 g/L;斑蝥素对鸡体内的PP2A有一定的抑制作用,而对于眼斑芫菁体内PP2A抑制作用不明显。马、兔、猪体内的PP2A对斑蝥素很敏感,而鸡和眼斑芫菁体内的PP2A对斑蝥素较不敏感。     

甘肃哈思山区芫菁科主要药用昆虫的分布特征

芫菁科Meloidae昆虫是豆类作物常见害虫,同时多具有重要药用价值.甘肃哈思山区是甘肃芫菁科昆虫聚集的典型代表区域,探索芫青科主要药用昆虫在该区域的分布特征,以期为该地区芫菁科药用昆虫资源开发奠定基础,也为防治该科昆虫因数量过度造成农业危害的决策建立提供理论依据.本研究调查了该区域各代表型样地中目标昆虫的数量、种类及...     

Intraspecific transfer of cantharidin within selected members of the family Meloidae (Insecta: Coleoptera)

The use of deuterium-labelled cantharidin (CAN-D(2)) to study details of cantharidin transfer in blister beetles indicates that the dynamics of organ-selective cantharidin accumulation may differ over time. Although the accessory glands absorb a high amount of CAN-D(2) in the short term, they ultimately accumulate less than the testes. Confirming previous studies, the last steps in the pathway of biosynthesis of cantharidin occur in the male's body distantly from the reproductive system but the ultimate product, cantharidin, is transported into the male reproductive tract via the membrane of the accessory glands. From there it first transfers preferentially to the epididimis and the vas deferens, followed by final deposition in the testes. Most, if not all, of the cantharidin passes internally within the sexual organs; hemolymph transport is not involved. In female meloids, cantharidin enters the genitalia from the male as a nuptial gift. High amounts are first absorbed by the spermatophoral receptacle followed by spreading through the ovaries and an ultimate accumulation in the eggs. The amount taken up by the ovaries remains considerably lower than that of the receptacle. Over time these two organs stop accumulating cantharidin, while the bursa copulatrix starts to incorporate the gift actively. The accumulated amount taken up by bursa is mainly supplied by the receptacle and ovaries suggesting that an internal transfer of cantharidin is used in females as the main transport route.     

斑蝥麦在细纹豆芫菁成虫体内的变化和配偶间的运转

将采自野外的同一批细纹豆芫菁在虫用半人工饲料饲养,取刚结束交配（A组）,交配结束后单养4天（B组）和未交配（C组）的两性成虫的血淋巴和各器官,分别测其斑蝥素含量,结果显示,斑蝥素含量在两性个体内和配偶间的器官间呈规律性地起伏,探讨了规律发生的过程和起因。     

斑蝥素及其衍生物的研究现状与应用

斑蝥素(Cantharidin)是一种可从昆虫斑蝥虫体提取或人工合成的具有抗肿瘤作用的药物,因其毒性强烈,受限于临床应用。人工合成的斑蝥素衍生物如去甲斑蝥素、斑蝥酸钠、去甲斑蝥酸钠、甲基斑蝥胺等,毒性低,疗效显著。本文对斑蝥素及其衍生物在抗肿瘤作用及分子机理方面的研究现状进行综述,为充分利用斑蝥素这一中药资源提供参考。     

Males of a Strongly Polygynous Species Consume More Poisonous Food than Females

We present evidence of a possible case of self-medication in a lekking bird, the great bustard Otis tarda. Great bustards consumed blister beetles (Meloidae), in spite of the fact that they contain cantharidin, a highly toxic compound that is lethal in moderate doses. In addition to anthelminthic properties, cantharidin was effective against gastrointestinal bacteria that cause sexually-transmitted diseases. Although both sexes consumed blister beetles during the mating season, only males selected them among all available insects, and ingested more and larger beetles than females. The male-biased consumption suggests that males could use cantharidin to reduce their parasite load and increase their sexual attractiveness. This plausibly explains the intense cloaca display males perform to approaching females, and the meticulous inspection females conduct of the male''s cloaca, a behaviour only observed in this and another similar species of the bustard family. A white, clean cloaca with no infection symptoms (e.g., diarrhoea) is an honest signal of both, resistance to cantharidin and absence of parasites, and represents a reliable indicator of the male quality to the extremely choosy females. Our results do not definitely prove, but certainly strongly suggest that cantharidin, obtained by consumption of blister beetles, acts in great bustards as an oral anti-microbial and pathogen-limiting compound, and that males ingest these poisonous insects to increase their mating success, pointing out that self-medication might have been overlooked as a sexually-selected mechanism enhancing male fitness.     

细纹豆芫菁3-羟甲基戊二酰辅酶A-还原酶基因全长cDNA克隆及生物信息学分析

3-羟甲基戊二酰辅酶A-还原酶（3-hydroxy-3-methylglutaryl coenzyme A reductase, HMGR）是甲羟戊酸途径的关键酶。获得芫菁体内HMGR基因信息是确定甲羟戊酸途径与斑蝥素合成相关性的基础。本研究利用RACE技术从细纹豆芫菁Epicauta mannerheimi (Maklin)体内克隆获得HMGR基因全长cDNA序列, 命名为EmHMGR（GenBank登录号为JQ690539）。该基因全长3 118 bp, 其中5′端非翻译区178 bp, 3′端非翻译区414 bp, 开放阅读框2 526 bp, 编码842个氨基酸。推测的蛋白质分子量为92.8 kDa, 理论等电点为6.0, 预测分子式为C₄₁₃₅H₆₆₀₄N1₀₉₈O₁₂₁₆S₅₀, 不稳定系数为43.37, 总亲水性系数为0.091, 为疏水性不稳定蛋白。序列分析发现该基因编码的蛋白与已报道的其他昆虫HMGR的氨基酸序列一致性达50%以上, 而且包含HMGR_Class I保守功能域、 固醇敏感多肽区及HMGR蛋白的其他保守功能位点。系统进化分析发现该基因与叶甲科昆虫HMGR基因的关系最近。本研究首次从芫菁科昆虫体内克隆获得甲羟戊酸途径的关键酶EmHMGR基因, 为后期芫菁体内斑蝥素生物合成途径的研究奠定了基础。     

Cantharidin poisoning associated with specific binding site in liver

Cantharidin, the potent vesicant and toxicant of blister beetles, was prepared as a radioligand to probe its mechanism of action. [3H]Cantharidin interacts in a saturable and specific manner with a binding site in mouse liver cytosol with apparent Kd and Bmax values of 30 nM and 1.8 pmol/mg protein, respectively. Comparisons of cantharidic acid, the related herbicide endothal, and 20 other oxabicycloheptane-dicarboxylic acids show that their potency as inhibitors of [3H]cantharidin binding is closely correlated with their intraperitoneal toxicity to mice. This binding site is also inhibited in vivo by toxic doses of cantharidin. The [3H]cantharidin binding site in mouse liver cytosol therefore represents, or serves as a model for, the site of toxic action of cantharidin and structurally-related compounds.