草问荆总生物碱对小鼠脑单胺氧化酶-B活性的影响

目的 研究草问荆总生物碱(TAEP)对小鼠脑单胺氧化酶—B(MAO—B)活性的影响，揭示TAEP对中枢神经系统抑制作用的机制。方法 采用紫外分光光度法测定MAO—B的活性。结果 TAEP对小鼠脑MAO—B具有明显的激活作用，并具有对抗烟肼酰胺抑制小鼠脑MAO—B活性的作用。结论 TAEP是MAO—B的激动药，有单胺代谢作用，这可能是TAEP中枢抑制作用的作用机制之一。     

吴茱萸化学成分的研究

从中药吴茱萸（Evodia rutaecarpa [juss] Benth)中分离出9个吲哚类生物碱和1个芳香胺，经光谱分析鉴定其结果为：evodiamine(1),rutaecarpine(2),formyldihydrorutaecarpine(3),goshuyuamide-I(4),evodiamide(5 ），hy挹minβ-carboline(7),1,2,3,4,-tetrahydro-1-oxo-β-carbolie(8),dehydroevodiamine(9)的N－methylanthranylamide(10),其中9是新的天然产物，7是首次从该属植物中分离得到。     

延胡索总生物碱提取工艺研究

目的：建立并优选延胡索总生物碱的提取工艺。方法：采用酸性染料比色法测定延胡索总生物碱含量,通过正交试验,优选总生物碱的提取工艺。结果：每1000g延胡索粗粉,加0.3%醋酸溶液1000ml,拌匀,浸润6小时,添加至渗漉装置中,0.3%醋酸浸泡12小时后,用0.3%的醋酸,以4ml/min的速度渗漉提取,收集提取液12000ml。结论按照此工艺生产的三批样品,结果：表明该工艺稳定可行。     

天南星炮制过程中总生物碱的动态变化

目的：研究炮制过程中天南星总生物碱含量的动态变化,建立天南星总生物碱的含量测定方法。方法采用酸性染料比色法测定天南星总生物碱的含量。结果方法学考察结果,线性范围2．2～11μg? mL －1,r＝0．9995,平均加样回收率为99％,RSD％＝2．8％（n＝6）;天南星生品、中间品、制品总生物碱含量均值分别为1．286mg? g－1、0．806mg? g－1、0．727mg? g－1。结论总生物碱在炮制过程中含量逐步降低;该含量测定方法稳定可靠,重复性好。     

Ergot Alkaloids in Feed for Pekin Ducks: Toxic Effects,Metabolism and Carry Over into Edible Tissues

Hardened sclerotia (ergots) of Claviceps purpurea contaminate cereal grains and contain toxic ergot alkaloids (EA). Information on EA toxicity in ducks is scarce. Therefore, the aim of the growth experiment (Day 0–49, n = 54/group) was to titrate the lowest observed adverse effect level (LOAEL) for total ergot alkaloids (TEA). A control diet was prepared without ergots, and the diets designated Ergot 1 to 4 contained 1, 10, 15 and 20 g ergot per kg diet, respectively, corresponding to TEA contents of 0.0, 0.6, 7.0, 11.4 and 16.4 mg/kg. Sensitivity of ducks to EA was most pronounced at the beginning of the experiment when feed intake decreased significantly by 9%, 28%, 41% and 47% in groups Ergot 1 to 4, respectively, compared to the control group. The experiment was terminated after two weeks for ducks exposed to Ergot 3 and 4 due to significant growth retardation. Ergot alkaloid residues in edible tissues were lower than 5 ng/g. Bile was tested positive for ergonovine (=ergometrine = ergobasine) with a mean concentration of 40 ng/g. Overall, the LOAEL amounted to 0.6 mg TA/kg diet suggesting that ducks are not protected by current European Union legislation (1 g ergot/kg unground cereal grains).     

Links between Genetic Groups,Indole Alkaloid Profiles and Ecology within the Grass-Parasitic Claviceps purpurea Species Complex

The grass parasitic fungus Claviceps purpurea sensu lato produces sclerotia with toxic indole alkaloids. It constitutes several genetic groups with divergent habitat preferences that recently were delimited into separate proposed species. We aimed to 1) analyze genetic variation of C. purpurea sensu lato in Norway, 2) characterize the associated indole alkaloid profiles, and 3) explore relationships between genetics, alkaloid chemistry and ecology. Approximately 600 sclerotia from 14 different grass species were subjected to various analyses including DNA sequencing and HPLC-MS. Molecular results, supported by chemical and ecological data, revealed one new genetic group (G4) in addition to two of the three known; G1 (C. purpurea sensu stricto) and G2 (C. humidiphila). G3 (C. spartinae) was not found. G4, which was apparently con-specific with the recently described C. arundinis sp. nov, was predominantly found in very wet habitats on Molinia caerulea and infrequently in saline habitats on Leymus arenarius. Its indole-diterpene profile resembled G2, while its ergot alkaloid profile differed from G2 in high amounts of ergosedmam. In contrast to G1, indole-diterpenes were consistently present in G2 and G4. Our study supports and complements the newly proposed species delimitation of the C. purpurea complex, but challenges some species characteristics including host spectrum, habitat preferences and sclerotial floating ability.     

Synthesis of Novel Hybrids Inspired from Bromopyrrole Alkaloids Inhibiting MMP‐2 and ‐12 as Antineoplastic Agents

Synthesis of novel set of forty semicarbazide/thiosemicarbazide hybrids inspired from marine bromopyrrole alkaloids is reported. Biological screening of these hybrids against a panel of five human cancer cell lines identified a number of hits endowed with interesting cytotoxicity profile. Compounds 5c and 5e (IC₅₀ = 0.03 μm ), 5t (IC₅₀ = 0.03 μm ), 4s (IC₅₀ = 0.07 μm ), and 5n (IC₅₀ = 0.01 μm ) displayed maximum cytotoxicity toward hormone‐dependent breast cancer cells MCF 7 , hepatic cancer cells WRL 68 , colon cancer cells Ca CO 2 and mouth and oral cancer cells KB 403 , respectively. The most active hits were further investigated for their potential to inhibit MMP‐2 and MMP‐12. Compound 5e showed maximum activity (IC₅₀ = 1.8 μm ) toward MMP‐2. Further, we preformed anti‐invasive assay on the most active compounds, where Ca CO 2 tumor cell migration was significantly decreased (77.9%) by hybrid 5e . The non‐toxicity toward human VERO cells (IC₅₀ = 83.1 to 231.8 μm ) indicated the selectivity of most active hits ( 5c , 5e , 5t and 5n ) toward cancer cells.     

Cytotoxic Indole Alkaloids against Human Leukemia Cell Lines from the Toxic Plant Peganum harmala

Bioactivity-guided fractionation was used to determine the cytotoxic alkaloids from the toxic plant Peganum harmala. Two novel indole alkaloids, together with ten known ones, were isolated and identified. The novel alkaloids were elucidated to be 2-(indol-3-yl)ethyl-α-l-rhamnopyranosyl-(1 → 6)-β-d-glucopyranoside (2) and 3-hydroxy-3-(N-acetyl-2-aminoethyl)-6-methoxyindol-2-one (3). The cytotoxicity against human leukemia cells was assayed for the alkaloids and some of them showed potent activity. Harmalacidine (compound 8, HMC) exhibited the highest cytotoxicity against U-937 cells with IC₅₀ value of 3.1 ± 0.2 μmol/L. The cytotoxic mechanism of HMC was targeting the mitochondrial and protein tyrosine kinase signaling pathways (PTKs-Ras/Raf/ERK). The results strongly demonstrated that the alkaloids from Peganum harmala could be a promising candidate for the therapy of leukemia.     

益母草总碱对老龄大鼠前列腺增生模型的影响

目的探讨益母草总碱对老龄大鼠前列腺增生模型的作用及相关机制。方法采用雌雄激素诱导法复制老龄大鼠前列腺增生模型,将造模大鼠随机分为5组,分别ig 50.0、25.0、12.5 mg/kg益母草总碱溶液,阳性对照组给予30 mg/kg癃闭舒混悬液,模型组给予同体积的生理盐水,另设老龄大鼠及青年大鼠各1组为对照,ig同体积生理盐水,每天给药1次,连续给药30 d;实验结束测定大鼠的前列腺湿质量,计算前列腺指数;检测血清中雌二醇(E2)和前列腺组织中双氢睾酮(DHT)、睾酮(T)及前列腺组织中碱性成纤维细胞生长因子(b FGF)、转化生长因子-β1(TGF-β1)、表皮细胞生长因子(EGF)、胰岛素样生长因子-1(IGF-1)表达,光镜及电镜观察大鼠前列腺组织形态及超微结构的变化。结果前列腺增生模型复制成功,与模型组比较,益母草总碱低剂量组可明显降低大鼠前列腺湿质量及前列腺指数(P0.05),益母草总碱中剂量组可明显降低大鼠前列腺指数(P0.05);益母草总碱各剂量组可显著降低模型大鼠前列腺中的T及DHT水平(P0.01),以及前列腺组织中b FGF、EGF、IGF-1表达(P0.05、0.01),益母草总碱低剂量组可显著升高前列腺组织中TGF-β1的表达(P0.01);益母草总碱各剂量组可显著降低模型大鼠前列腺的体密度(P0.05、0.01),显著增加前列腺比膜面及比表面值(P0.01),可使模型所致的前列腺细胞胞浆内线粒体显著减少,减轻线粒体嵴等的病理变化。结论益母草总碱对雌雄激素诱导法所致的老龄大鼠前列腺增生模型有较好的治疗作用。