狭基线纹香茶菜的化学成分

目的对唇形科香茶菜属植物狭基线纹香茶菜(Isodon lophanthoides(Buch.Ham.ex D.Don)Haravar.gerandianus(Benth.)Hara)即中药溪黄草的化学成分进行研究。方法体积分数为95%乙醇提取物的水混悬液经环己烷、乙酸乙酯、正丁醇分步萃取,再对乙酸乙酯层运用硅胶、D101大孔树脂S、ephadex LH 20、ODS等柱层析手段并配合HPLC进行分离、纯化;通过化学方法及波谱分析鉴定其结构。结果分离得到并鉴定了6个化合物:既6去羟基迷迭香酸甲酯(methyl 6 dehy-droxyl rosmarinate,1)、迷迭香酸甲酯(methyl rosmarinate,2)、咖啡酸(caffeic acid,3)、6,7二羟基香豆素(6,7 dihydroxycoumarin,4)、槲皮素(quercetin,5)、蓟黄素(cirsimaritin,6)。结论化合物1为新天然产物,化合物4为首次从该属中分离得到,化合物3、6为首次从该植物中分离得到。     

Pharmacological evaluation of the anxiolytic-like effects of Lippia graveolens and bioactive compounds

Context: Lippia species (Verbenaceae) are widely used in Latin America and Africa as folk medicine for their tranquilizing properties.

Objective: To evaluate the anxiolytic-like effects and safety of Lippia graveolens Kunth. by exploring its aqueous and organic leaf extracts and identifying the responsible chemical constituents.

Material and methods: Aqueous and organic extracts (hexane, ethyl acetate and methanol) were pharmacologically evaluated at several doses. Chemical constituents were identified using MS, NMR and GC-MS analysis. The isolated compounds (3?mg/kg, i.p.), extracts (1, 3, 10 and 30?mg/kg, i.p.), and the reference drug diazepam (0.1?mg/kg, i.p.) were assessed in CD-1 mice using experimental behavioural models: open-field, cylinder, hole-board, plus-maze and sodium pentobarbital-induced hypnosis, as well as their acute toxicity (LD₅₀).

Results: After administration of the extracts and bioactive compounds, a significant anxiolytic-like response from 1?mg/kg, i.p. was observed, resembling the effect of diazepam. Major presence of thymol (33.40%) was observed in the hexane extract; whereas for the first time in this species a p-cymene?+?thymol mixture (9.78%), naringenin (0.18%) and cirsimaritin (1.16%) were obtained as bioactive constituents of the ethyl acetate crude extract. Acute toxicity was calculated to be LD₅₀ =?1000?mg/kg for the crude hexane extract, lower in comparison to the other extracts analyzed (LD₅₀ >?2000?mg/kg).

Discussion and conclusion: Our results suggest that L. graveolens exerts anxiolytic-like activity involving many kinds of constituents, mainly of the terpenoid and flavonoid nature. These results reinforce the potential use of this species in the therapy of anxiety.     

乌药的化学成分研究

目的研究乌药Lindera aggregata根的化学成分。方法应用硅胶、Sephadex LH-20等多种色谱技术进行分离纯化,并利用波谱分析方法(MS,1D、2D-NMR)鉴定化合物结构。结果从乌药根95%乙醇提取物中分离得到14个化合物,其中化合物1为新化合物,命名为乌药双查耳酮(1),其余已知化合物分别鉴定为乌药环戊烯二酮甲醚(2)、乌药环戊烯二酮(3)、帕夏查耳酮(4)、球松素(5)、甲基赤芝酮(6)、松属素(7)、5,7-二羟基-6,8-二甲氧基黄酮(8)、赤芝酮(9)、乙基赤芝酮(10)、肉桂酸(11)、球松素查耳酮(12)、蓟黄素(13)和β-谷甾醇(14)。结论化合物1为新化合物,化合物13为首次从该属植物中分离得到。     

苦竹嫩茎化学成分的研究

目的 研究苦竹Pleiobtastus amarus 嫩茎的化学成分.方法 采用色谱分离技术进行分离和纯化,并根据谱学数据鉴定化合物的结构.结果 从苦竹嫩茎的甲醇提取物中分离得到15个酚类化合物,分别鉴定为苜蓿素(1)、芹菜素(2)、5,7,2',4',6'-五羟基黄酮(3)、5,7-二羟基-3',4',5'-三羟基黄酮(4)、金合欢素(5)、木犀草素(6)、蓟黄素(7)、对羟基苯甲醛(8)、邻羟基苯甲酸(9)、反式对羟基肉桂酸(10)、2,4-二羟基苯甲醛(11)、没食子酸(12)、没食子酸甲酯(13)、questin(14)和isorhodoptilometrin(15).结论 化合物2～7、10～13为首次从苦竹中分离得到,化合物14和15为首次从苦竹属植物中分离得到.     

Bioactivity-guided isolation of anti-proliferative compounds from endemic Centaurea kilaea

Context: The genus Centaurea L. (Asteraceae) is one of the largest genera in Turkey. Compounds and extracts obtained from different Centaurea species have significant anti-cancer activity against various cancer cell lines.

Objective: To determine the anti-proliferative activity of isolates from the chloroform extract of C. kilaea Boiss.

Materials and methods: Eleven compounds were isolated using column chromatography and preparative TLC from the chloroform extract of aerial parts of endemic C. kilaea. The structures of the isolated compounds were elucidated by various spectroscopic methods, including UV, ^lH-NMR and ¹³C-NMR. Anti-proliferative activity of compounds (0.5–50?μg/mL) were measured against one normal cell line (L-929, mouse fibroblast) and three human cancer cell lines (Hela, cervix carcinoma; MCF-7, breast carcinoma; PC-3, prostate carcinoma) using MTT assay. Results were expressed as IC₅₀ values.

Results: None of the 11 compounds displayed activity against L-929 and HeLa. Two of these compounds, cnicin and cirsimaritin, showed fairly strong activity against MCF-7 and PC-3 with IC₅₀ values of 3.25 and 4.3?μg/mL, respectively.

Discussion and conclusion: This is the first report on cirsimaritin. Cirsimaritin and cnicin could serve as potential anti-cancer drug candidates against breast and prostate cancer, respectively.     

基于UHPLC-Q-TOF-MS技术和网络药理学的金莲花抗炎药效物质基础及作用机制研究

目的 基于超高效液相色谱–四级杆–飞行时间串联质谱（UHPLC-Q-TOF-MS）法、网络药理学和分子对接验证探讨金莲花抗炎的药效物质及机制。方法 根据质谱信息结合对照品、文献和数据库指认金莲花中化学成分信息;借助Swiss ADME平台及查询文献来筛选金莲花潜在活性成分;通过Swiss Target Prediction数据库预测金莲花活性成分的作用靶点;采用OMIM、GeneCards、DrugBank、DisGeNET数据库获取炎症的相关靶点;利用Venn图取药物活性成分靶点与疾病靶点交集后,用STRING数据库构建蛋白质相互作用网络（PPI）;用Metascape数据库对核心靶点进行基因本体论（GO）富集分析和京都基因与基因组百科全书（KEGG）通路分析;借助Cytoscape软件构建“活性成分–炎症靶点–富集通路”网络;采用分子对接技术进行初步验证。结果 从金莲花中共鉴别出38个化合物,包括黄酮类23个,有机酸类10个,香豆素类1个,单糖2个以及苯乙素类2个;网络药理学研究表明,金莲花可能通过鼠尾草素、蓟黄素、香叶木素、阿魏酸、槲皮素和芹菜素等成分,作用于肿瘤坏死因子（TNF...