钩藤生物碱对中枢神经系统的药理作用研究进展

钩藤是我国一种常用药材,对心血管系统、中枢神经系统和血液系统等均具有比较广泛的药理活性,临床上主要用于治疗高血压、焦虑等疾病。现代中药药理研究表明,钩藤对中枢神经系统的药理作用主要表现为镇静、抗癫痫、抗惊厥和对神经元的保护等,其中对神经元的保护作用与多种神经递质相关,具有多种作用机制,已被国内外越来越多的医药工作者所重视,综述钩藤生物碱对中枢神经系统的药理作用研究进展。     

Prevention of experimental diabetes by Uncaria tomentosa extract: Th2 polarization, regulatory T cell preservation or both?

Ethnopharmacological relevance

Uncaria tomentosa (Willd.) DC (Rubiaceae) is a species native to the Amazon rainforest and surrounding tropical areas that is endowed with immunomodulatory properties and widely used around the world. In this study we investigated the immunomodulatory potential of Uncaria tomentosa (UT) aqueous-ethanol extract on the progression of immune-mediated diabetes.

Materials and methods

C57BL/6 male mice were injected with MLDS (40 mg/kg) and orally treated with UT at 10-400 mg/kg during 21 days. Control groups received MLDS alone or the respective dilution vehicle. Pancreatic mononuclear infiltrate and β-cell insulin content were analyzed by HE and immunohistochemical staining, respectively, and measured by digital morphometry. Lymphocyte immunophenotyping and cytokine production were determined by flow cytometry analysis.

Results

Treating the animals with 50-400 mg/kg of UT caused a significant reduction in the glycemic levels, as well as in the incidence of diabetes. The morphometric analysis of insulitis revealed a clear protective effect. Animals treated with UT at 400 mg/kg presented a higher number of intact islets and a significant inhibition of destructive insulitis. Furthermore, a significant protection against the loss of insulin-secreting presented β-cells was achieved, as observed by a careful immunohistochemical evaluation. The phenotypic analysis indicated that the groups treated with higher doses (100-400 mg/kg) presented CD4⁺ and CD8⁺ T-cell values similar to those observed in healthy animals. These same higher doses also increased the number of CD4⁺CD25⁺Foxp3⁺ regulatory T-cells. Moreover, the extract modulated the production of Th1 and Th2, with increased levels of IL-4 and IL-5.

Conclusions

The extract was effective to prevent the progression of immune-mediated diabetes by distinct pathways.     

天麻钩藤饮控释胶囊的制备及体外释放度试验

目的:对天麻钩藤饮控释胶囊的制备工艺、体外释放度进行研究,为天麻钩藤饮控释胶囊的新药申报提供部分实验数据资料。方法:以乙基纤维素为辅料,制备天麻钩藤饮控释胶囊。以体外释放性能和成品外观性状为综合指标,对乙基纤维素乙醇液的浓度进行优选,优选出最佳处方和制备工艺。结果:验证实验结果表明,天麻钩藤饮控释胶囊释药基本达到零级过程,通过零级方程拟合,r=0.9991。加入天麻钩藤饮浸膏粉作为速释部分可提高控释胶囊的释药速率。结论:该控释胶囊的制备方法可行,达到了控释目的。     

鼻冠状位CT研究钩突解剖变异与慢性鼻窦炎的关系

目的通过鼻冠状位CT对钩突解剖变异与慢性鼻窦炎的关系进行分析研究。方法此次研究,选取我院接受CT检查的130例患者,检查时间为2017年9月至2019年11月期间,检查结果无鼻窦炎患者为对照组,慢性鼻窦炎患者为研究组,对比分析两组患者检查后钩突解剖变异与鼻窦炎的关系。结果研究组患者的钩突高度、钩突角度以及筛漏斗宽度明显高于对照组患者的各项数据(P<0.05);钩突头端附着类型与鼻窦炎关系分析中,研究组患者与对照组患者之间纸样板型、中鼻甲型发生率相对比有明显差异(P<0.05),研究组与对照组患者之间分叉型、筛顶型发生率相对比无明显差异(P>0.05);钩突其他解剖变异与鼻窦炎关系中,研究组与对照组患者之间钩突偏曲、以及肥大两项具有较为明显的差异(P<0.05),且研究组与对照组患者之间钩突气化、以及钩突缺失发生率相对比无明显差异(P>0.05)。结论数据中表明,慢性鼻窦炎患者出现钩突解剖变异几率明显较高,其中较为常见的包括纸样板型、中鼻甲型,钩突解剖变异与慢性鼻窦炎的关系较为紧密,对于慢性鼻窦炎患者治疗有着极为重要的临床意义。     

Mixtures of Uncaria and Tabebuia extracts are potentially chemopreventive in CBA/Ca mice: a long‐term experiment

A long‐term experimental animal model was developed by our research group for the evaluation of potential chemopreventive effects. The inhibitory effects of agents on carcinogen (7,12‐dimethylbenz[a]anthracene (DMBA) induced molecular epidemiological biomarkers, in this case the expression of key onco/suppressor genes were investigated. The expression pattern of c‐myc, Ha‐ras, Bcl‐2, K‐ras protooncogene and p53 tumour suppressor gene were studied to elucidate early carcinogenic and potential chemopreventive effects. The consumption of so‐called Claw of Dragon tea (CoD? tea) containing the bark of Uncaria guianensis, Cat's Claw (Uncaria sp. U. tomentosa) and Palmer trumpet‐tree (Tabebuia sp. T. avellanedae) was able to decrease the DMBA‐induced onco/suppressor gene overexpression in a short‐term animal experiment. In a following study CBA/Ca mice were treated with 20 mg/kg bw DMBA intraperitoneally (i.p.) and the expression patterns of onco/suppressor genes were examined at several time intervals. According to the examined gene expression patterns in this long‐term experiment the chemopreventive effect of CoD? tea consumption could be confirmed. Copyright © 2010 John Wiley & Sons, Ltd.     

不同产地及不同采收期钩藤中异钩藤碱的含量分析

目的：研究不同产地及不同采收期钩藤中异钩藤碱的含量。方法应用HPLC测定8个不同产地及不同采收期钩藤中异钩藤碱含量,采用Waters Symmetry C18色谱柱(250 mm34.6 mm,5μm),流动相为甲醇-0.01 mol/L醋酸铵缓冲液(pH 8.0)(60∶40),柱温25℃,进样体积20μl,流速1.0 ml/min,检测波长246 nm。结果不同产地及不同采收期的钩藤中异钩藤碱含量不同,其中含量最高的地区为宁明县;含量最高的采收时间为每年9月至次年2月。结论不同产地钩藤药材异钩藤碱的含量不同,每年9月至次年2月采收的钩藤中异钩藤碱含量较高。     

罗布麻降压片的薄层色谱鉴别

目的:鉴别罗布麻降压片中的罗布麻、钩藤、泽泻。方法:采用薄层色谱法。结果:鉴别方法简便迅速。结论:建立的方法可有效地控制本制剂质量。     

半夏生物总碱和钩藤生物总碱抗小鼠、大鼠惊厥的协同作用（英文）

目的研究半夏生物总碱（PTA）和钩藤生物总碱（UTA）抗惊厥的协同作用,并探讨其相互作用机制。方法采用小鼠最大电休克惊厥试验和急性毒性试验检测PTA和UTA单用和三种比例（1：1,1：4,4：1）配伍的抗惊厥作用及毒性效应,并采用bliss’s法分别计算它们的ED50和LD50。用等效线法评价其协同作用并计算各组配伍的受益指数（BI）。制备大鼠运动皮层定位注射青霉素惊厥模型,同时采用高效液相色谱法（HPLC）测定海马区癫痫相关递质Glu、Asp、Gly、GABA的含量。结果半夏、钩藤生物总碱4：1配伍的抗惊厥作用呈现协同,而毒性呈现相互拮抗,是PTA和UTA合用的最佳比例。而两药1：4和1：1比例配伍尽管在最大电休克惊厥试验中抗惊厥作用呈现协同,但是在毒性试验中毒性效应却呈现相加。PTA和UTA单用和4：1合用,均可明显减少海马Glu的水平,增加GABA的水平,且4：1合用组的GABA水平要比两单药组高。但对Asp、Gly无明显影响。结论PTA和UTA以4：1合用时抗癫痫效应协同、毒性拮抗。两药合用的抗惊厥作用机制可能与其同时降低Glu能神经的兴奋性,并协同提高GABA能神经功能有关。     

钩藤碱含量测定方法研究进展

钩藤碱是中药钩藤中的主要生物碱之一,目前测定钩藤药材中异钩藤碱含量,主要采用高效液相色谱、反相高效液相色潽、高效毛细管电泳、非水毛细管电泳、薄层色谱、薄层色谱傅里叶变换表面增强喇曼散射等方法。本文就上述内容作一综述。     

大叶钩藤茎三萜类成分研究（英文）

从大叶钩藤茎中分离得到19个三萜类成分,包括11个乌苏烷型三萜和8个齐墩果烷型三萜,其化学结构通过波谱学方法鉴定。19个化合物中12个化合物为首次从大叶钩藤中分离得到,6个化合物为首次从钩藤属植物中分离得到。