苦豆子提取物与埃玛菌素混用对小菜蛾生长发育和繁殖的影响

将苦豆子甲醇和水提取物分别与埃玛菌素混合,在室内测定了两混合物对小菜蛾生长发育和繁殖的影响.结果表明:苦豆子甲醇提取物 埃玛菌素和苦豆子水提取物 埃玛菌素对小菜蛾3龄幼虫口服毒力明显高于埃玛菌素,其LC50值分别为0.19、0.32和0.51 mg.L-1;用两混合物以及埃玛菌素亚致死剂量处理3龄幼虫,试虫化蛹率、羽化率和成虫的繁殖力均呈现明显不良影响.     

苦豆子提取物与埃玛菌素混合剂剂对小菜蛾实验种群生长的影响

将苦豆子甲醇提取物和苦豆子水提取物分别与埃玛菌素混合,得到苦豆子甲醇提取物·埃玛菌素(简称苦醇·埃)和苦豆子水提取物·埃玛菌素(简称苦水·埃)2种混合剂,在室内用特定年龄生命表法,研究了2种混合剂低致死剂量对小菜蛾的影响,并对其F_1代幼虫、蛹以及成虫进行了观察。结果表明,埃玛菌素、苦醇·埃和苦水·埃3个处理对小菜蛾F_1代各龄期均有影响。其种群趋势指数(I)分别为6.23、4.81和5.70,而对照组种群趋势指数则为28.03。     

半夏和苦豆子生物碱的抗线虫活性

首次研究了半夏和苦豆子生物总碱,以及3种主要的苦豆子单体生物碱(槐定碱、氧化苦参碱和氧化槐果碱)的抗线虫活性。半夏生物总碱处理24 h,对松材线虫、南方根结线虫、全齿复合线虫和秀丽隐杆线虫的半抑制浓度(IC50)分别为16.18、20.25、33.24和20.77μg/m L。苦豆子生物总碱处理24 h,对上述4种线虫表现出更强的抑制活性,IC50值分别为0.622、0.383、1.476和1.224μg/m L,抗线虫活性强于或接近阳性对照阿维菌素。3种苦豆子单体生物碱均表现出明显的抗线虫活性,其中氧化槐果碱的抗线虫活性最强。研究结果为植物源杀线虫剂的研究和开发提供了依据。     

苦豆子生物碱抗烟曲霉、须癣毛癣菌和新生隐球菌的作用研究

目的对比研究苦豆子总碱、槐果碱、苦参碱、槐定碱、氧化苦参碱体外抗烟曲霉、须癣毛癣菌和新生隐球菌的敏感性,为苦豆子进一步开发利用奠定基础。方法分别用管碟扩散法和微量液基稀释法,测定苦豆子总碱、槐果碱、苦参碱、槐定碱、氧化苦参碱对烟曲霉、须癣毛癣菌和新生隐球菌的抗菌活性。结果管碟法显示上述5种生物碱体外对烟曲霉、须癣毛癣菌和新生隐球菌均有不同程度的抗菌活性。前4种生物碱对烟曲霉的最低杀菌浓度(MFC)分别为25.0、4.25、5.0、3.125 mg·mL~(-1),氧化苦参碱对烟曲霉MFC500 mg·mL~(-1);对须癣毛癣菌的MFC分别为3.125、2.125、5.0、1.5625、125 mg·mL~(-1);对新生隐球菌的MFC分别为3.125、4.25、10、6.25、1000 mg·mL~(-1)。结论槐果碱、苦参碱及槐定碱其抗真菌活性与苦豆子总碱相当,氧化苦参碱的作用不显著。     

苦豆子生物碱对萝卜蚜的毒力及其对几种酯酶的影响

苦豆子Sophoraalopecuroids（L．）的次生代谢物质为喹诺里西定生物碱类。本研究明确了该生物碱中的野靛碱对萝卜蚜（Lipaphiserysimi）有很高的毒杀作用,对其无翅成蚜的致死中浓度（LC50,浸渍法）为（4325±2．12）mg／L,优于著名的杀蚜生物碱毒黎碱和烟碱,两者对该试虫的LC50分别为（684．70±2．28）mg／L和（1090．65±2．01）mg／L。用小菜蛾（Plutellaxylostella）幼虫作试虫,得知苦豆子7种主要生物碱对昆虫的乙酰胆碱酯酶（AChE）有抑制作用,其抑制程度排序为：总碱＞野靛碱＞槐胺碱＞槐定碱＞槐果碱＞氧化苦参碱＞苦参碱＞苦豆碱。野靛碱和苦豆碱对α-乙酸萘酯酶、α-乙酸萘酯羧酸酯酶及酯酶同功酶的活性亦表现不同程度的抑制作用。     

苦豆子的抗生成分

苦豆子茎叶水提取液对小麦幼芽、幼根的生长表现出明显的抑制作用。水溶液含有苦豆碱,槐定和槐果碱。实验表明,当这些生物碱作用于小麦幼苗时,引起强烈的抑制作用,结果如下:(1)苦豆子水提取液对小麦幼苗的生长有强烈的抑制作用,对幼芽的最低抑制浓度为5％,对幼根的最低抑制浓度为0.1％。(2)薄层层析实验表明,水溶液中苦豆碱、槐定和槐果碱为主要抑制成分,它们可被小麦幼根吸收,但不能传入幼芽中。(3)苦豆碱的抑制作用大于槐定和槐果碱。它们的最低抑制浓度分别为8.6×10~(-5) M、2.0×10~(-3)和2.0×10~(-3)至8.1×10~(-4)M。3种生物碱对幼根的抑制作用大于对幼芽的抑制作用。(4)根据含量测定,在相同浓度作用下,苦豆碱在小麦幼根根尖中的含量均比槐定和槐果碱高,表明苦豆碱容易被小麦幼根吸收。同时,苦豆碱的毒性大于槐定和槐果碱。     

苦豆子生物碱对萝卜蚜的毒力及其对几种酯酶的影响

苦豆子Sophora alopecuroids(L.)的次生代谢物质为喹诺里西定生物碱类。本研究明确了该生物碱中的野靛碱对萝卜蚜(Lipaphis erysimi)有很高的毒杀作用,对其无翅成蚜的致死中浓度(LC₅₀浸渍法)为(432.59±2.12)mg/L,优于著名的杀蚜生物碱毒黎碱和烟碱,两者对该试虫的LC₅₀分别为(684.70±2.28)mg/L和(1090.65±2.01)mg/L。用小菜蛾(Plutella xylostella)幼虫作试虫,得知苦豆子7种主要生物碱对昆虫的乙酰胆碱酯酶(AChE)有抑制作用,其抑制程度排序为：总碱>野靛碱>槐胺碱>槐定碱>槐果碱>氧化苦参碱>苦参碱>苦豆碱。野靛碱和苦豆碱对a-乙酸萘酯酶、a-乙酸萘酯羧酸酯酶及酯酶同功酶的活性亦表现不同程度的抑制作用。     

几种苦豆子生物碱对小菜蛾部分生理指标的影响

四龄小菜蛾幼虫经苦豆子7种生物碱处理后,表现呼吸强度增加,完成完整呼吸次数减少,其中,苦参碱、苦豆碱和槐胺碱均显著促进试虫二氧化碳释放量和释放过程。槐果碱处理试虫体内总糖含量显符降低。所有处理试虫的生长发育均显著受到抑制。     

苦豆子中生物碱的分布及其在生长期内的含量变化

采用高效液相仪测定苦豆子植株不同部位和不同生长期间的生物碱含量。结果表明：苦豆子植株不同部位的总生物碱含量为21.346-41mg．g-1（DW）,以种子中为最高,花、根、果皮、根状茎、叶片、地上茎次之,复叶轴中最低;苦参碱含量为0．55-1．30m2．g-1（DW）,含量由高到低依次为种子〉花〉根〉果皮〉根状茎〉叶片〉地上茎〉复叶轴;氧化苦参碱和氧化槐果碱含量分别为3．76～12．29mg．g-1（DW）和3．36—13．33mg·g-1（DW）,这2种生物碱含量由高到低依次为种子〉花〉根〉果皮〉根状茎〉地上茎〉复叶轴〉叶片：根、根状茎、地上茎、叶中的苦参碱、氧化苦参碱和氧化槐果碱含量在7月份达到峰值;总生物碱含量在8月达到峰值。     

黄花棘豆生物碱成分研究

采用硅胶柱层析、Sephadex LH-20和半制备HPLC等色谱手段对草原毒草黄花棘豆(Oxytropis ochrocephala Bunge)生物碱成分进行分离纯化,从全草提取物中分离得到8个生物碱成分。利用MS、1H NMR和13C NMR波谱技术鉴定化合物结构为槐定碱(1)、槐胺(2)、异槐定碱(3)、苦参碱(4)、7,11-去氢苦参碱(5)、槐果碱(6)、羽扇豆碱(7)和苦马豆素(8)。化合物1~6为首次从棘豆属植物中分离得到。     

苦豆子生物碱对小菜蛾体内部分杀虫剂代谢酶活性的影响

以苦豆子Sophora alopecuroids 7种生物碱和小菜蛾Plutella xylostella幼虫为试材,研究了该生物碱对小菜蛾体内降解杀虫剂的羧酸酯酶、磷酸酯酶、谷胱甘肽-S-转移酶活性的影响。结果表明: 野靛碱和苦豆碱对羧酸酯酶活性有显著的抑制,为可逆抑制类型的非竞争性抑制作用;野靛碱等5种生物碱对酸性磷酸酯酶有明显的抑制,野靛碱对碱性磷酸酯酶有弱抑制作用;其中野靛碱等3种生物碱对谷胱甘肽-S-转移酶有明显的抑制作用。     

Spatio‐Temporal Variation of Alkaloids in Annona purpurea and the Associated Influence on Their Antifungal Activity

Annona purpurea grows in the areas of low elevation in deciduous forests of Mexico, those areas have marked rainy and dry seasons. This species produces more than 30 bioactive alkaloids that could have potential in the control of phytopathogens. This research provides data on the variation of the content and number of alkaloids during an annual cycle and the associated inhibitory potential of the compounds against three phytopathogenic fungi. For one year, alkaloidal extracts of stems and leaves were obtained every two months. The extract profiles were determined by gas chromatography with tandem mass spectrometry and their antifungal activity was examined in vitro. The alkaloids, annomontine and oxopurpureine, obtained from the roots and leaves, respectively, were also evaluated individually. The yields, profiles and activities of the extracts, as well as the abundance of annomontine and oxopurpureine in the extracts, were contrasted with the seasonality and phenological phases of the plant. The data indicate that the alkaloid content was higher at the height of the dry season. High yields also occurred during flowering. The strongest inhibitory effect was obtained from the root extracts during the last month of dry season. This finding seems to be explained by the higher chemodiversity of alkaloids in extracts from this season. Annomontine and oxopurpureine inhibited all three phytopathogens; however, they were not solely responsible for the activity of A. purpurea.     

Stimulation of topoisomerase II-mediated DNA cleavage by three DNA-intercalating plant alkaloids: cryptolepine, matadine, and serpentine.

Cryptolepine, matadine, and serpentine are three indoloquinoline alkaloids isolated from the roots of African plants: Cryptolepis sanguinolenta, Strychnos gossweileri, and Rauwolfia serpentina, respectively. For a long time, these alkaloids have been used in African folk medicine in the form of plant extracts for the treatment of multiple diseases, in particular as antimalarial drugs. To date, the molecular basis for their diverse biological effects remains poorly understood. To elucidate their mechanism of action, we studied their interaction with DNA and their effects on topoisomerase II. The strength and mode of binding to DNA of the three alkaloids were investigated by spectroscopy. The alkaloids bind tightly to DNA and behave as typical intercalating agents. All three compounds stabilize the topoisomerase II-DNA covalent complex and stimulate the cutting of DNA by topoisomerase II. The poisoning effect is more pronounced with cryptolepine than with matadine and serpentine, but none of the drugs exhibit a preference for cutting at a specific base. Cryptolepine which binds 10-fold more tightly to DNA than the two related alkaloids proves to be much more cytotoxic toward B16 melanoma cells than matadine and serpentine. The cellular consequences of the inhibition of topoisomerase II by cryptolepine were investigated using the HL60 leukemia cell line. The flow cytometry analysis shows that the drug alters the cell cycle distribution, but no sign of drug-induced apoptosis was detected when evaluating the internucleosomal fragmentation of DNA in cells. Cryptolepine-treated cells probably die via necrosis rather than via apoptosis. The results provide evidence that DNA and topoisomerase II are the primary targets of cryptolepine, matadine, and serpentine.     

离子交换树脂用于角蒿总生物碱的纯化研究

本文以角蒿总生物碱溶液为对象,以其主要有效成分角蒿酯碱（incarvillateine）为指标,研究了阳离子交换树脂纯化角蒿总生物碱的方法,包括树脂类型的选择、氨水浓度和乙醇浓度对洗脱效果的影响.试验结果表明强酸性阳离子交换树脂DOWEX 50WX2对角蒿生物碱成分的交换能力最强,且被树脂吸附的生物碱成分可用氨性乙醇溶液快速洗脱.验证试验结果表明,用含2.0 N氨水的不同浓度乙醇溶液（60%、70%和80%）进行洗脱,得到的总生物碱含量均在60%以上,且随着乙醇浓度的提高,总生物碱的含量也不断提高.     

苦豆子碱和烟碱的联合杀蚜作用

【目的】以豆蚜Aphis craccivora Koch为试虫,对苦豆子碱和烟碱的联合杀蚜活性进行了测定,以期为开发新型植物源杀蚜剂奠定基础。【方法】单体化合物对豆蚜的毒力测定采用微量点滴法;制剂对豆蚜的毒力测定采用波特喷雾法;田间药效试验参照国家标准进行,其中施药方法采用常量喷雾法;制剂加工及化合物之间的联合杀蚜作用测定均采用常规方法。【结果】苦豆子碱和烟碱混用具有明显的杀蚜增效作用,在最佳质量配比（苦豆子碱∶烟碱=13∶1）下,共毒系数（common toxicity coefficient, CTC）值达185.82。结合对溶剂、乳化剂等助剂的筛选,研制出15.7% 苦豆子碱·烟碱环保型乳油,配方为：苦豆子碱（14.6%）、烟碱（1.1%）、环保溶剂（74.3%）、乳化剂（10%）。质量检测结果表明该制剂各项指标均达到商品农药的要求。大田药效试验表明,该制剂在质量浓度为0.354 g/L时,常量喷雾,药后7 d对月季长管蚜Macrosiphum rosirvorum的防效仍为85.91%。【结论】苦豆子碱和烟碱混用具有显著的杀蚜相互增效作用,具有进一步开发潜力。     

Acetylcholinesterase inhibitory activity of some Amaryllidaceae alkaloids and Narcissus extracts

Amaryllidaceous plants produce pharmacologically active alkaloids, galanthamine being the most interesting for its use in the treatment of Alzheimer's disease as a cholinesterase inhibitor. The aim of this work was to test 23 pure Amaryllidaceae alkaloids and 26 extracts from different species of the genus Narcissus for their acetylcholinesterase inhibitory activity using galanthamine as a reference. Only seven alkaloids, belonging to the galanthamine and lycorine skeleton types, exhibited such an effect, sanguinine being the most active, even more than galanthamine. All the extracts with the highest acetylcholinesterase inhibitory activity contained galanthamine except that of N. assoanus, a lycorine type alkaloid-bearing species.     

Toxicity evaluation of botanical insecticides and their mixture against the spiraling whitefly,Aleurodicus dispersus

【背景】螺旋粉虱是新入侵海南省的严重为害经济作物及园林苗木的害虫。目前,植物源杀虫剂因具有高效和环境友好等特性而被广泛用于害虫防治中。【方法】采用喷雾法和药膜接触法分别测定了9种植物性杀虫剂对螺旋粉虱的毒力。【结果】在供试的9种植物性杀虫剂中,除虫菊素和鱼藤酮对螺旋粉虱成虫的毒力最强,24h的LC50分别为2.56和34.15mg·L-1;印楝素和苦瓜叶提取物的毒力次之,LC50分别为158.36和311.02mg·L-1。除虫菊素对螺旋粉虱若虫和卵也有一定的触杀作用,LC50分别为61.42和77.39mg·L-1。将印楝素和鱼藤酮分别与除虫菊素以1:1的比例混合,对螺旋粉虱成虫的毒力表现出明显的增效作用,其共毒系数(CTC)分别为193.11和224.35。【结论与意义】除虫菊素、鱼藤酮、印楝素和苦瓜叶提取物对螺旋粉虱均具有较强的毒性;印楝素或鱼藤酮与除虫菊素(1:1)的混合物不仅能增强触杀效果,而且能延缓害虫抗药性的产生。