大叶钩藤中表儿茶素含量的测定

目的：充分利用中药钩藤的植物资源,测定并比较大叶钩藤Ｕｎｃａｒｉａ ｍａｃｒｏｐｈｙｌｌａ Ｗａｌｌ．的叶和钩茎中的表儿茶素含量。方法：利用ＲＰ－ＨＰＬＣ测定。结果：钩藤钩茎中含表儿茶素０．３８％,叶中含０．８２％。结论：大叶钩藤中含有较多的表儿茶素,叶中含量大于钩茎中含量。     

HPLC测定黔产钩藤不同部位钩藤碱和异钩藤碱的含量

目的 HPLC测定黔产钩藤不同部位中钩藤碱和异钩藤碱的含量,并比较其差异。方法 以钩藤碱、异钩藤碱为对照品,采用CAPCELL PAK C₁₈色谱柱（4.6 mm×250 mm,5μm）,以乙腈-0.1%三乙胺水溶液（1%磷酸调pH=9）为流动相,流速1 mL·min^-1,检测波长245 nm,柱温30℃,进样量10µL。结果 钩藤碱与异钩藤碱分离良好,线性、重复性以及回收率均符合要求,钩藤不同部位中的含量存在差异,由高到低依次为皮 > 茎 > 带钩茎枝 > 叶,而茎薄壁组织与木质部未检测到钩藤碱与异钩藤碱。结论 该含量测定结果为钩藤资源的充分利用提供了科学依据。     

基于网络药理学和分子对接研究钩藤治疗动脉粥样硬化的有效成分和作用机制

[目的]基于网络药理学和分子对接研究钩藤治疗动脉粥样硬化的有效成分、靶点及通路。[方法]利用TCMSP数据库并结合筛选条件,确定钩藤的主要有效成分和有效成分相应的靶点,构建有效成分-靶点网络;利用GeneCards、DisGeNET、OMIM及TTD数据库确定动脉粥样硬化的疾病靶点,获取药物靶点与疾病靶点的交集,并对交集靶点进行PPI网络分析、GO生物功能富集分析和KEGG通路富集分析,应用Cytoscape 3.9.0软件中的“Analyze Network”工具,构建有效成分-靶点-通路网络,筛选出核心成分、核心靶点、核心通路,并对核心成分与核心靶点之间的亲和力进行分子对接验证。[结果]筛选出33种有效成分,其中一种有效成分没有相应的靶点,筛选出1 608个疾病靶点和115个药物与疾病的交集靶点。PPI分析得到的主要靶点为AKT1、TNF、IL-6、IL-1β、TP53、JUN、CASP3、MMP9、PTGS2等。GO生物功能富集分析获得生物过程条目22个、细胞成分条目57个、分子功能条目100个。KEGG通路富集分析筛选出20条信号通路,主要为脂质和动脉粥样硬化、MAPK、癌症信...     

Effects of the hook of Uncaria rhynchophylla on neurotoxicity in the 6-hydroxydopamine model of Parkinson's disease

Ethnopharmacological relevance

While the hook of Uncaria rhynchophylla (URH) is a traditional herb used in northeast Asia for the treatment of Parkinson's disease (PD)-like symptoms such as tremor, it has not been experimentally evaluated in a PD model.

Aim of the study

We investigated the effects of URH on 6-hydroxydapamine (6-OHDA)-induced neurotoxicity in in vitro and in vivo models of PD.

Materials and methods

The cell viability, anti-oxidative activity, and anti-apoptotic activity of a water extract of URH (URE) were assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide, reactive oxygen species (ROS), total glutathione (GSH), and caspase-3 assays in PC12 cells stressed by 6-OHDA. We also investigated the behavioral recovery and dopaminergic neuron protection of URE using an apomorphine-induced rotation test and tyrosine hydroxylase immunohistochemistry in the hemi-parkinsonian rat model of the unilateral 6-OHDA lesion of the medial forebrain bundle.

Results

In PC12 cells, URE significantly reduced cell death and the generation of ROS, increased GSH levels, and inhibited caspase-3 activity induced by 6-OHDA. In 6-OHDA-lesioned rats, posttreatment with URE (5 mg/kg/day for 14 days) significantly reduced apomorphine-induced rotation, and it lowered dopaminergic neuronal loss in substantia nigra pars compacta.

Conclusions

URE possesses neuroprotective activity against 6-OHDA-induced toxicity through anti-oxidative and anti-apoptotic activities in PD models.     

天麻钩藤饮对脑缺血大鼠的神经保护机制研究

目的 观察天麻钩藤饮对脑缺血大鼠学习记忆能力,VEGF及其受体VEGFR-2/FLK-1的影响,探讨天麻钩藤饮的脑保护作用机制.方法 采用大鼠双侧颈动脉永久性结扎制备脑缺血模型,于术后次日开始给予天麻钩藤饮[5g/(kg·d)]灌胃,分别于2周及4周通过Morris水迷宫观察大鼠行为学的改变,免疫组化观察VEGF及FLK-1的改变.结果 模型组大鼠的潜伏期较假手术组明显延长,记忆能力明显下降.治疗组较模型组明显好转,4周较2周更为明显.2周模型组VEGF、FLK-1主要在神经元表达,较假手术组明显增多,4周表达下降;治疗组VEGF、FLK-1在神经元的表达较模型组明显增多,4周仍高表达.结论 该研究提示,天麻钩藤饮可能通过促进VEGF和特异性受体FLK-1的表达,启动神经元保护机制,发挥脑保护作用,改善脑缺血后大鼠的行为学表现.     

Protective effect of hexane extracts of Uncaria sinensis against photothrombotic ischemic injury in mice

Ethnopharmacological relevance

Uncaria sinensis (US) has been used in traditional Korean medicine to treat vascular disease and to relieve various neurological symptoms.

Aim of the study

Scientific evidence related to the effectiveness or action mechanism of US on cerebrovascular disease has not been examined experimentally. Here, we investigated the cerebrovascular protective effect of US extracts on photothrombotic ischemic injury in mice.

Materials and methods

US hexane extracts (HEUS), ethyl acetate extracts (EAEUS) and methanol extracts (MEUS) were administered intraperitoneally 30 min before ischemic insults. Focal cerebral ischemia was induced in C57BL/6J mice and endothelial nitric oxide synthase knockout (eNOS KO) mice by photothrombotic cortical occlusion. We evaluated the infarct volume, neurological score and the activation of Akt and eNOS in ischemic brain.

Results

HEUS more significantly reduced infarct volume and edema than did EAEUS and MEUS following photothrombotic cortical occlusion. HEUS produced decreased infarct volume and edema size, and improved neurological function in a concentration-dependent manner (10, 50, and 100 mg/kg). However, HEUS did not reduce brain infarction in eNOS KO mice, suggesting that the protective effect of HEUS is primarily endothelium-dependent. Furthermore, HEUS (10-300 μg/ml) produced a concentration-dependent relaxation in mouse aorta and rat basilar artery, which was not seen in eNOS KO mouse aorta, suggesting that HEUS cause vasodilation via an eNOS-dependent mechanism. This correlated with increased phosphorylation of Akt and eNOS in the brains of HEUS-treated mice.

Conclusion

HEUS prevent cerebral ischemic damage by regulating Akt/eNOS signaling. US, herbal medicine, may be the basis of a novel strategy for the therapy of stroke.     

Oral Uncaria rhynchophylla (UR) reduces kainic acid-induced epileptic seizures and neuronal death accompanied by attenuating glial cell proliferation and S100B proteins in rats

Aim of the study

Epilepsy is a common clinical syndrome with recurrent neuronal discharges in cerebral cortex and hippocampus. Here we aim to determine the protective role of Uncaria rhynchophylla (UR), an herbal drug belong to Traditional Chinese Medicine (TCM), on epileptic rats.

Materials and methods

To address this issue, we tested the effect of UR on kainic acid (KA)-induced epileptic seizures and further investigate the underlying mechanisms.

Results

Oral UR successfully decreased neuronal death and discharges in hippocampal CA1 pyramidal neurons. The population spikes (PSs) were decreased from 4.1 ± 0.4 mV to 2.1 ± 0.3 mV in KA-induced epileptic seizures and UR-treated groups, respectively. Oral UR protected animals from neuronal death induced by KA treatment (from 34 ± 4.6 to 191.7 ± 48.6 neurons/field) through attenuating glial cell proliferation and S100B protein expression but not GABAA and TRPV1 receptors.

Conclusions

The above results provide detail mechanisms underlying the neuroprotective action of UR on KA-induced epileptic seizure in hippocampal CA1 neurons.     

Uncaria tomentosa aqueous-ethanol extract triggers an immunomodulation toward a Th2 cytokine profile

Uncaria tomentosa (Willd.) DC (Rubiaceae) is a large woody vine that is native to the Amazon and Central American rainforests and is used widely in traditional medicine for its immunomodulatory and antiinflammatory activities. The present work used in vivo immunotoxic and in vitro immunomodulatory experiments to investigate the effects of a pentacyclic oxindole alkaloid extract from U. tomentosa bark on lymphocyte phenotype, Th1/Th2 cytokine production, cellular proliferation and cytotoxicity. For the in vivo immunotoxicity testing, BALB/c male mice were treated once a day with 125, 500 or 1250 mg/kg of U. tomentosa extract for 28 days. For the in vitro protocol, lymphocytes were cultured with 10–500 μg/mg of the extract for 48 h. The extract increased the cellularity of splenic white pulp and the thymic medulla and increased the number of T helper lymphocytes and B lymphocytes. Also, a large stimulatory effect on lymphocyte viability was observed. However, mitogen‐induced T lymphocyte proliferation was significantly inhibited at higher concentrations of U. tomentosa extract. Furthermore, an immunological polarization toward a Th2 cytokine profile was observed. These results suggest that the U. tomentosa aqueous‐ethanol extract was not immunotoxic to mice and was able to modulate distinct patterns of the immune system in a dose‐dependent manner. Copyright © 2011 John Wiley & Sons, Ltd.     

天麻钩藤饮对肝阳上亢型高血压病患者血压及血清SOD的影响

目的探讨天麻钩藤饮对高血压病 (肝阳上亢型 )患者疗效和血清超氧化物歧化酶 (SOD)活性的影响 ,为临床高血压病患者的治疗提供有力的理论依据。方法将 60例患者随机分为天麻钩藤组 (治疗组 ,3 0例 )和对照组 ( 3 0例 ) ,4周后 ,观察两组治疗前后血压的改变及血清SOD的改变 ,并与 1 0例正常人血清SOD作比较。结果两组患者治疗后血压均明显降低 ,两组比较无显著性差异 (P >0 .0 5 ) ,天麻钩藤 (治疗 )组和对照组的SOD活性在治疗前分别为 ( 85 .6± 1 1 .2 )U mL和 ( 86.3± 1 2 .5 )U mL ,在治疗后分别为 ( 1 0 5 .1±1 2 .8)U mL和 ( 95 .1± 1 3 .2 )U mL ,治疗后两组比较有明显差异 (P <0 .0 1 )。结论天麻钩藤饮能显著降低高血压病患者血压 ,并能通过提高SOD活性保护机体 ,提高机体的抗氧化能力