去甲去氢斑蝥素新衍生物的合成

以顺丁烯二酸酐和呋喃为起始原料,经Diels-Alder[4+2]缩合反应,制备去甲去氢斑蝥素,同时在去甲去氢斑蝥素分子中引入电负性较大的氧原子、氮原子。去甲去氢斑蝥素经SN2取代、缩合和过氧酸氧化三步反应,合成了5,6-环氧去甲去氢斑蝥素衍生物,去甲去氢斑蝥素经S_N2取代、缩合、过氧酸氧化和取代四步反应,得到5,6-二羟基去甲去氢斑蝥素衍生物。所得化合物均经~1HNMR和ESI-MS确证。     

Contrasting reactions of loggerhead shrikes to two types of chemically defended insect prey

Feeding tests with loggerhead shrikes (Lanius ludovicianus) showed this bird to acceptUtetheisa ornatrix, a moth (Arctiidae) protected by pyrrolizidine alkaloids, but to avoidLytta polita, a beetle (Meloidae) containing cantharidin.Paper no. 130 of the series Defense Mechanisms of Arthropods; no. 129 is T. Eisner and J. Meinwald,Proc. Natl. Acad. Sci. U.S.A. 92:50–55, 1995.     

色谱分析法在斑蝥黄测定中的研究进展

本文从斑蝥黄的稳定性、样品的前处理技术和检测方法等方面,着重阐述了色谱技术在斑蝥黄测定中的应用,包括高效液相色谱法、高效液相色谱-串联质谱法。     

斑蝥素及其药理作用研究进展

斑蝥属鞘翅目芫菁科昆虫,是我国最早发现的具有抗肿瘤作用的中药材之一,其药用成分是一种单萜类有毒物质——斑蝥素。本为就斑蝥素的资源分布、生化特性、在虫体中的分布及药理学作用进行了综述,为人类进一步认识和利用斑蝥素提供了理论基础。     

Inclusion complex of cantharidin with β‐cyclodextrin: Preparation,characterization, in vitro and in vivo evaluation

Because of low aqueous solubility and slow dissolution rate, cantharidin has a low oral bioavailability. Our research aims to prepare the inclusion complex of cantharidin and β‐cyclodextrin (β‐CD) and accomplish characterization, in vitro and in vivo evaluation. CA‐β‐CD inclusion complex was prepared by saturated solution method. The CA was demonstrated by HPLC in vitro experiment and by GC‐MS in vivo experiment. CA‐β‐CD inclusion complex was characterized by differential scanning calorimetry (DSC), X‐ray diffractometry (XRD), and nuclear magnetic resonance (NMR). Through complexation with β‐CD, the solubility of CA in neutral aqueous solution was improved significantly. CA‐β‐CD inclusion complex also shows a significantly improved dissolution rate in comparison with free CA. Comparison of the pharmacokinetics between CA‐β‐CD inclusion complex and free CA was performed in rats. The in vivo results show that CA‐β‐CD inclusion complex has earlier t_max, higher C_max, and higher bioavailability than free CA after oral dosing. By comparing the AUC_0–t of CA and CA‐β‐CD inclusion complex, the relative bioavailability of CA‐β‐CD inclusion complex to free CA was 506.3%, which highlighted the evidence of significantly improved bioavailability of formulation of CA with β‐CD. Thus, this β‐CD‐based drug delivery system should be an effective oral dosage form to improve oral bioavailability of CA. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012     

高效液相色谱法测定斑蝥中斑蝥素的含量

目的建立测定斑蝥中斑蝥素含量的高效液相色谱方法。方法以C18色谱柱为分析柱,乙腈-水(80:20)为流动相,检测波长为209nm。结果斑蝥素进样量在0.4012～2.0060范围内与峰面积呈线性关系,平均回收率为100.1%,RSD为2%。结论本方法准确可靠,能有效地控制斑蝥药材的质量。     

毛细管气相色谱法测定药用真菌生物转化液中微量斑蝥素的含量

采用毛细管气相色谱法对药用真菌培养液中斑蝥素的含量进行了测定。色谱条件：色谱柱为SPB-5弹性石英毛细管柱；进样口温度240℃；柱温：120℃（5min）→8℃／min→240℃（2min）；检测器为FID，检测温度240℃。栽气：99．999％高纯氮气，流量1．5mL／min；尾吹气：99．999％高纯氮气，流量25mL／min。以香兰素作为内标，采用内标法定量。斑蝥素在1—200mg／L范围内线性关系良好，检测限为0．01mg／L。     

斑蝥素含量测定方法研究进展

斑蝥素是一种具有特殊作用的天然活性物质,具有抗恶性肿瘤等重要临床应用,添加到生发类化妆品中,还具有对皮肤止痒、改善局部神经营养及刺激毛根,促进毛发生长的作用,但其毒性也很强烈,化妆品卫生规范对其添加量有严格规定。本文对斑蝥素的含量测定方法进行了详细介绍。     

Pressurized CO2 Extraction of Cantharidin from Mylabris for Anticancer Bioactive Component

The use of pressurized liquid carbon dioxide to extract cantharidin from Mylabris was investigated. The study resulted in green extraction of bioactive ingredients from the insect, with extraction efficiency of 95% (three repetitions) obtained at a pressure of 1 MPa, temperature of 60°C, static extraction time of 30 minutes, and with 4 ml of acetonitrile as modifier. In addition to the identification of the extract, i.e., cantharidin, by chromatography, an in vitro assay for the effect of the extract on a cell was performed. The result reveals that cantharidin-extract is effective for primary medicinal use.     

天然源农药0.1%斑蝥素水溶剂的应用技术

报道了天然源农药0．1％斑螫素水溶剂的应用技术可行性研究。结果表明，0．1％斑蝥素水溶剂200-250g a.i.／hm^2，可有效的控制菜蚜、菜青虫、桃蚜、梨二叉蚜等害虫的为害，对小菜蛾具有一定作用，对作物无毒害影响。