半枝莲化学成分及药理活性研究进展(综述)

半枝莲Scutellaria barbata为我国传统中药,具清热解毒、化瘀止痛、排石利尿等多重功效。化学成分研究表明,半枝莲含有大量黄酮类、二萜类、挥发油类及多糖等化学成分;药理研究表明,半枝莲具有抗肿瘤、抗氧化、抗菌及免疫调节等药理活性。本文综述半枝莲的化学成分及其药理活性研究概况,为其进一步开发利用提供参考。     

基于PI3K/AKT/mTOR信号通路探讨半枝莲总黄酮对脑缺血再灌注损伤大鼠神经功能和氧化应激损伤的影响

摘要 目的：基于磷脂酰肌醇3激酶（PI3K）/丝氨酸苏氨酸蛋白激酶（Akt）/哺乳动物的雷帕霉素（mTOR）信号通路探究半枝莲总黄酮对脑缺血再灌注损伤（CIRI）大鼠神经功能和氧化应激损伤的影响。方法：选取70只SPF级雄性SD大鼠,采用线栓法制备大脑中动脉闭塞（MCAO）模型,将造模成功的60只大鼠随机分为模型组、半枝莲总黄酮低剂量组（半枝莲L组）、半枝莲总黄酮中剂量组（半枝莲M组）、半枝莲总黄酮高剂量组（半枝莲H组）、control组、LY294002组,每组10只,剩余10只大鼠作为sham组。半枝莲L、M、H组分别给予半枝莲总黄酮0.1、0.2、0.4 g/kg溶于2 mL生理盐水灌胃,control组给予尼莫地平0.3 g/kg溶于2 mL生理盐水灌胃,LY294002组给予半枝莲总黄酮0.4 g/kg溶于2 mL生理盐水灌胃,同时侧脑室注射PI3K抑制剂LY294002 20 μmol/L,模型组和sham组给予等量的生理盐水灌胃。分别比较各组大鼠神经功能评分、脑组织积水量、脑梗死体积、脑组织病理学变化、脑组织氧化应激水平、脑组织中p-PI3K/PI3K、p-Akt/Akt、p-mTOR/mTOR蛋白表达。结果：各组大鼠神经功能评分、脑组织含水量、脑梗死体积、丙二醛（MDA）水平比较,模型组明显高于sham组,半枝莲L、M、H组、control组均低于模型组,且半枝莲H组优于半枝莲L、M组,但LY294002组高于半枝莲H组（P<0.05）;各组大鼠超氧化物岐化酶（SOD）水平和p-PI3K/PI3K、p-Akt/Akt、p-mTOR/mTOR蛋白表达比较,模型组明显低于sham组,半枝莲L、M、H组、control组均高于模型组,且半枝莲H组优于半枝莲L、M组,但LY294002组低于半枝莲H组（P<0.05）。结论：半枝莲总黄酮可能通过激活PI3K/Akt/mTOR信号通路发挥对CIRI大鼠神经功能和氧化应激损伤的改善作用,且高剂量半枝莲总黄酮的改善作用最显著。     

半枝莲、白花蛇舌草及其药对提取物抗氧化及清除自由基活性

采用几种化学及生物学模型考察了半枝莲、白花蛇舌草及其药对提取物抗氧化及清除自由基活性.研究结果表明三种提取物中,半枝莲提取物还原能力、清除DPPH及·OH自由基能力最强,药对提取物螯合Fe2 能力以及保护DNA免受自由基损伤能力最强.提示提取物抗氧化及清除自由基活性可能与其黄酮组成及含量相关.推测药对的抗癌作用机理可能与金属离子的螯合能力和对DNA损伤的保护作用等有关.     

优良的地被花卉─—马缨丹、半枝莲

作者结合生产实践经验,介绍了优良地被花卉植物马缨丹和半枝莲的形态特征,培育技术和应用、观赏价值。     

半枝莲地上部分的化学成分

半枝莲(Scutellaria barbata D.Don)为唇形科(Labiatae)黄芩属(Scutellaria L.)植物,其干燥全草可入药,具有清热解毒、利尿消肿的功效,用于治疗疮痈肿毒、蛇虫咬伤、肝炎及肝肿大等症.     

半枝莲中二萜内酯和黄酮化合物的分离和鉴定

半枝莲（Scutellaria barbata D.Don）为唇形科黄芩属植物,全草入药,具有清热解毒,化瘀利尿,消肿止痛和抗癌等功效。国内学者报道从全草中分得红花素（carthamidin）、异红花素（isocarthamidin）、印黄芩甙（scutellarein）、β-谷甾醇（β-sitosterol）、硬脂酸（stearic acid）和生物碱。台湾学者从中分离得汉黄芩素（wogonin）、5-羟基-7,8-二甲氧基黄酮（5-hydroxy-7,8-dimethoxyflavone）、半枝莲素（Rivularin）。我们从全草的乙醇提取液中分得两个化合物,经鉴定为汉黄芩素、新穿心莲内酯,该内酯在本植物中属首次发现。     

半枝莲多糖的分离、纯化及其理化性质

唇形科植物半枝莲全草的热水提取液经乙醇沉淀、去蛋白、逆向流水透析、DEAE-纤维素柱层析和Sephadex G-100柱层析得纯品半枝莲多糖(S-BP)。凝胶过滤及聚丙烯酰胺凝胶电泳证明为单一均匀成分。SBP的比旋度为[α]_D~(20)=+26.2°,不含氮,分子量13000,具有890cm~(-1)红外吸收峰。经纸层析和气相色谱分析,SBP含鼠李糖、阿拉伯糖、木糖、甘露糖、半乳糖和葡萄糖,其克分子比为1.14:1.50:0.20:0.75:1.0:2.18。     

优良的地被花卉——马缨丹,半枝莲

作者结合生产实践经验,介绍了优良地被花卉植物马缨丹和半枝莲的形态特征,培育技术和应用,观赏价值。     

卡那霉素产生菌26号的获得

在卡那霉素产生菌育种过程中,结合自然选育先后用过激光、快中子、紫外线钴60、氯化锂、亚硝基胍、亚硝酸钠以及中草药半枝莲等。多次实践后,发现紫外线在卡那霉素产生菌育种过程中效果较好。优点是操作简单,菌落外观形态差异明显,易于针对不同的形态进行挑选。1978年底,我们利用紫外线和自然分离间歇处理,获得变异菌株26号大缶生产六十批,平均单位5,218r/ml,提高351     

半枝莲中印黄芩甙的R－HPLC分析

半枝莲中印黄芩甙的Ｒ－ＨＰＬＣ分析代雪平魏波（河南省药检所,郑州４５０００３）（河南省人民医院药剂科,郑州４５０００３）Ｒ┐ＨＰＬＣａｎａｌｙｓｉｓｏｆｓｃｕｔｅｌａｒｉｎｆｒｏｍＳｃｕｔｅｌａｒｉａｂａｒｂａｔａＤ．ＤｏｎＤａｉＸｕｅ－Ｐｉｎｇ（Ｈ...     

neo-Clerodane diterpenoids from Scutellaria barbata with cytotoxic activities

Three neo-clerodane diterpenoids, named barbatins A-C (1-3), and the neo-clerodane diterpenoid nicotinyl ester, named scutebarbatine B (4), were isolated from the whole plant of Scutellaria barbata D. Don. Their structures were elucidated by spectroscopic analyses (UV, IR, HRFAB-MS, 1D NMR and 2D NMR). In vitro, compounds 1-4 showed significant cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, with IC50 values in the range 3.5-8.1 microM.     

Two new neo-clerodane diterpenoids from Scutellaria barbata

Two new neo-clerodane diterpenoids, 6,7-dibenzoyloxybarbatin C (1, named barbatin D) and 6-(2-acetoxy-3-methylbutanoloxy)-7-(2-carbonyl-3-methylbutanoyloxy) barbatin C (2, named barbatin E) were Isolated from the whole plant of Scutellaria barbata D. Don. Their structures were elucidated by spectroscopic methods including extensive 1D and 2D NMR analyses. In vitro, compounds 1-2 showed cytotoxic activities against three human cancer lines, namely, HONE-4 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, and with ICso values in the range of 3.5-6.7 μM.     

Anticancer activity and mechanism of Scutellaria barbata extract on human lung cancer cell line A549

Scutellaria barbata (S. barbata), a traditional Chinese herbal medicine native to southern China, is widely used as an anti-inflammatory and a diuretic in China. Several studies have indicated that extracts of S. barbata have growth inhibitory effects on a number of human cancers. Treatment of lung cancer, digestive system cancers, hepatoma, breast cancer, and chorioepithelioma by S. barbata extracts was reported. However, the mechanism underlying the antitumor activity was unclear. In this study, we studied the growth inhibitory effect of S. barbata and determined its mechanism of antitumor activity using human lung cancer cell line A549. Our results showed that ethanol extracts of S. barbata greatly inhibited A549 cell growth, with IC50 of 0.21 mg/ml. The major mechanisms of inhibition included cell apoptosis and cytotoxic effects. cDNA microarray analysis showed that 16 genes, involved in DNA damage, cell cycle control, nucleic acid binding and protein phosphorylation, underwent more than 5-fold change. These data indicated that these processes are involved in S. barbata-mediated killing of cancer cells. A surprising finding is that CD209, related to dendritic cell (DC) function, was dramatically downregulated by 102-fold. Further functional studies are needed to assess the role of the array-identified genes in S. barbata mediated anticancer activity.     

半枝莲的一个新的克罗烷二萜

从半枝莲（Scutellaria barbara）植物地上部分的甲醇提取物中分离得到一个新的克罗烷二萜。通过现代波谱技术鉴定为15β-甲氧基-6α-O-乙酰基-19-O-丙酰基-4α,18;11,16;15,16-环氧-新克罗烷二萜。     

Chemical composition and antimicrobial activity of the essential oil of Scutellaria barbata

The essential oil of Scutellaria barbata was obtained by hydrodistillation with a 0.3% (v/w) yield and analysed by GC and GC-MS. The main compounds in the oil were hexahydrofarnesylacetone (11.0%), 3,7,11,15-tetramethyl-2-hexadecen-1-ol (7.8%), menthol (7.7%) and 1-octen-3-ol (7.1%). The antimicrobial activity of the oil was evaluated against 17 microorganisms using disc diffusion and broth microdilution methods. The gram-positive bacteria, including methicillin-resistant Staphlococcus aureus, were more sensitive to the oil than gram-negative bacteria and yeasts.     

Effects of turbidity on life history parameters of two species of Daphnia

SUMMARY. 1. Life table experiments were carried out in a range of turbidities on D. pulex , representing a 'clear-water', and on D. barbata , representing a 'turbid-water' species.
2. In contrast to predictions based on seasonal occurrence patterns, D. pulex had a higher intrinsic rate of increase ( r _c)s over most of the turbidity range than D. barbata. Consistent differences in life history between the two species were found, but life history characteristics were rather insensitive to turbidity levels. Although turbidity per se appears to have little direct effect on life history parameters, it could influence the seasonal succession of these two species by interacting with other factors.
3. It is suggested that visual predation by fish rather than turbidity per se probably influenced the seasonality of Daphnia species. During the warmer months, selective removal of D. pulex by visually foraging fishes may allow D. barbata to gain dominance. Effects of temperature and nutrition also merit further study.     

Systematics and health effects of chemically distinct tannins in medicinal plants

The research began with an investigation of tannins from traditional medicinal plants and resulted in isolation and structure determination of hundreds of ellagitannins and dehydroellagitannins, as well as their oligomers and oxidized derivatives with various structures specific to each plant species. These polyphenols have been classified according to the stage of oxidative structural transformation and oligomerization, into types I-IV and I+ to IV+, etc. Parallels were found between their oxidative transformations and plant evolution. They were also classified by the linkage units between the monomers, into DOG, GOD, GOG and DOGOD types (D=Diphenoyl, G=Galloyl, O=Oxygen), etc. Besides their fundamental activities, e.g., reduction and anti-peroxidation properties, remarkable biological and pharmacological activities of various potencies have also been found, including, amongst others, inhibition of lipid-peroxidation, mutagenicity of carcinogens and tumor promotion, host-mediated antitumor effects specific to particular tannin structures, antiviral activity and potentiation of antibacterial activity.     

孟仁草的花序发育研究

在光学显微镜和扫描电镜下观察了禾本科(Poaceae)虎尾草属(Chloris Sw.)孟仁草(Chloris barbata Sw.)的花序发育过程,以寻找适于虎尾草群(Chloris group)分支分析的发育性状.结果发现了未见于成熟花序的23个发育性状.阐明盂仁草花序的本质是二级长侧枝包围平截的主轴构成指形花序.该类型花序仅见于单子叶植物和少数高度特化的双子叶植物.涉及花序分枝的分子遗传机制研究亟待开展.