白屈菜生物碱对鼠慢性毒性试验的研究

本试验以大白鼠为研究对象,肌肉注射不同剂量的白屈菜生物碱,观察30 d后大白鼠行为,检测血液生理、生化指标及脏器病理变化,目的是研究白屈菜生物碱对大白鼠的慢性毒性。结果表明,白屈菜生物碱对大白鼠行为、血液生理、生化指标及脏器病理无不良影响。     

小果博落回生物碱对几种农业害虫的生物活性

为确定小果博落回生物碱的杀虫作用方式和杀虫谱,室内测定小果博落回生物碱对粘虫3龄幼虫、菜青虫5龄幼虫、小菜蛾3龄幼虫、棉铃虫3龄幼虫、桃蚜和麦二叉蚜无翅成虫的杀虫活性.结果表明:小果博落回生物碱对试虫具有拒食、胃毒和杀卵等多种作用方式,其中,对粘虫、菜青虫和小菜蛾48 h AFC50值和96 h LC50值分别为0265、0557、0543 g·L-1和0106、0123、0166 g·L-1;对桃蚜和麦二叉蚜有较高的触杀作用,48 h LC50值分别为0362、0710 g·L-1;对棉铃虫3龄幼虫具有一定的生长发育抑制作用,7 d的生长抑制率为695%(5 g·L-1);此外,对粘虫还具有一定的杀卵作用,5 d的卵孵化率和幼虫存活率仅为588%和226%(25 g·L-1).     

Marine-Derived Indole Alkaloids and Their Biological and Pharmacological Activities

Novel secondary metabolites from marine macroorganisms and marine-derived microorganisms have been intensively investigated in the last few decades. Several classes of compounds, especially indole alkaloids, have been a target for evaluating biological and pharmacological activities. As one of the most promising classes of compounds, indole alkaloids possess not only intriguing structural features but also a wide range of biological/pharmacological activities including antimicrobial, anti-inflammatory, anticancer, antidiabetic, and antiparasitic activities. This review reports the indole alkaloids isolated during the period of 2016–2021 and their relevant biological/pharmacological activities. The marine-derived indole alkaloids reported from 2016 to 2021 were collected from various scientific databases. A total of 186 indole alkaloids from various marine organisms including fungi, bacteria, sponges, bryozoans, mangroves, and algae, are described. Despite the described bioactivities, further evaluation including their mechanisms of action and biological targets is needed to determine which of these indole alkaloids are worth studying to obtain lead compounds for the development of new drugs.     

乌头生物碱对甜菜夜蛾毒杀活性的测定

测定了乌头碱、次乌头碱、中乌头碱3种乌头生物碱对甜菜夜蛾的毒杀活性和作用方式.结果表明,乌头生物碱对甜菜夜蛾有较强的胃毒、拒食和生长抑制作用,基本没有触杀和熏蒸作用;3种乌头生物碱对甜菜夜蛾4龄幼虫的毒杀活性存在一定的差异,乌头碱和次乌头碱的毒杀致死中浓度LC50基本相当,分别为121.51 mg·L-1和146.27 mg·L-1,而中乌头碱为495.09 mg·L-1,与前二者有显著差异.     

Novel Prenylated Indole Alkaloids with Neuroprotection on SH-SY5Y Cells against Oxidative Stress Targeting Keap1–Nrf2

Oxidative stress has been implicated in the etiology of Parkinson’s disease (PD). Molecules non-covalently binding to the Keap1–Nrf2 complex could be a promising therapeutic approach for PD. Herein, two novel prenylated indole alkaloids asperpenazine (1), and asperpendoline (2) with a scarce skeleton of pyrimido[1,6-a]indole were discovered from the co-cultivated fungi of Aspergillus ochraceus MCCC 3A00521 and Penicillium sp. HUBU 0120. Compound 2 exhibited potential neuroprotective activity on SH-SY5Y cells against oxidative stress. Molecular mechanism research demonstrated that 2 inhibited Keap1 expression, resulting in the translocation of Nrf2 from the cytoplasm to the nucleus, activating the downstream genes expression of HO-1 and NQO1, leading to the reduction in reactive oxygen species (ROS) and the augment of glutathione. Molecular docking and dynamic simulation analyses manifested that 2 interacted with Keap1 (PDB ID: 1X2R) via forming typical hydrogen and hydrophobic bonds with residues and presented less fluctuation of RMSD and RMSF during a natural physiological condition.     

沙冬青生物碱成分研究

沙冬青叶干燥粉碎后用甲醇、石油醚、氯仿提取，并采用柱层析和薄层层析等方法分离出三种生物碱，经质谱和核磁共振波谱仪鉴定为羽扇豆碱，斯帕亭和ａ－异斯帕亭生物碱。     

A Series of New Pyrrole Alkaloids with ALR2 Inhibitory Activities from the Sponge Stylissa massa

Twelve new and four known alkaloids including five different structural scaffolds were isolated from the sponge Stylissa massa collected in the South China Sea. Compound 1 is the first identified precursor metabolite of the classic 5/7/5 tricyclic skeleton with unesterified guanidine and carboxyl groups, compounds 2–5 and 13–15 belong to the spongiacidin-type pyrrole imidazole alkaloids (PIAs). Z- and E-configurations of the spongiacidin-type PIAs often appeared concomitantly and were distinguished by the chemical shift analysis of ¹³C NMR spectra. The structures of all twelve new compounds were determined by NMR, MS, and ECD analysis combined with single-crystal data of compounds 1, 5, and 10. In the aldose reductase (ALR2) inhibitory assay, six 5/7/5 tricyclic compounds (2–5, 13–15) displayed significant activities. Compounds 13 and 14, as the representative members of spongiacidin-PIAs, demonstrated their ALR2-targeted activities in SPR experiments with K_D values of 12.5 and 6.9 µM, respectively.     

雷公藤组培产物中雷公藤甲素和总生物碱含量的测定

建立了同一提取物中高效液相色谱法测定雷公藤甲素和紫外分光光度法测定雷公藤总生物碱含量的方法,样品用乙酸乙酯超声提取、过中性氧化铝柱,净化后用45%甲醇溶解,测定雷公藤的根皮、叶、雷公藤组培产物及培养液中雷公藤甲素和雷公藤总生物碱的含量。结果表明,雷公藤甲素的检测范围为1~100 μg/mL(R2= 0.999 9);雷公藤总生物碱在5~100 μg/mL范围内线性关系良好(R2=0.999 8);在同一提取液中,雷公藤甲素和雷公藤总生物碱的添加回收率分别为100.5%(RSD=0.63%)和99.8%(RSD=1.22%)。研究结果表明,根愈伤组织中雷公藤甲素含量为根皮粉中的1.25倍,培养液中雷公藤甲素产量占56%,总生物碱产量占65%。每生产1 g不定根培养物,雷公藤甲素产量为根皮粉中的10倍,雷公藤总生物碱产量为根皮粉中的2倍。     

灵芝有效化学成分的研究

本文从灵芝有效化学成分的结构，提取分离方法，结构鉴定，生理活性及应用价值等方面进行了概述。     

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为科学合理开发金钗石斛药材资源,采用单因素试验分析提取温度、乙醇浓度、提取时间、固液比和提取次数对金钗石斛总生物碱含量的影响,酸碱滴定法测定总生物碱含量.在此基础上,运用正交试验对乙醇浓度、提取时间、固液比和提取次数进行优化.结果表明:金钗石斛总生物碱提取制备的最佳条件为提取温度85℃,乙醇浓度90％,提取时间3h,固液比1∶20,提取次数为2次,在该条件下金钗石斛总生物碱的平均提取率为87.8 mg/g.