Inhibitory effect of Uncaria sinensis on human aortic smooth muscle cell migration is based on matrix metalloproteinase-9 inhibitory activity

Medicinal extracts of Cho-Deung-san and Uncaria sinensis Havil. (UR) have previously been shown to have inhibitory effects on migration of vascular smooth muscle cells (VSMC) and matrix metalloproteinase (MMP)-2/9 production, which play key roles in the development of atherosclerosis. In this study, we have more extensively investigated the inhibitory effect of UR on MMP-9 activity and TNF- induced human aortic smooth muscle cells (HASMC) migration. The result from gelatin zymography showed that UR inhibited MMP-9 activity in a dose-dependent manner (IC₅₀ = 55 μg/ml). In addition, UR strongly inhibited the migration of HASMC induced by TNF- treatment (IC₅₀ = 125 μg/ml), although it has very low cytotoxic effect on HASMC (IC₅₀ > 500 μg/ml). These results suggest that UR is a potential anti-atherosclerotic agent through inhibition of MMP-9 activity and VSMC migration.     

统计学建模在中药谱-效关系研究中的应用

目的构建钩藤药材中钩藤碱、异钩藤碱、柯诺辛及柯诺辛B四种生物碱对谷氨酸酯诱导PCI2细胞氧化应激抑制作用的谱-效关系模型。方法在获得钩藤药材中钩藤碱、异钩藤碱、柯诺辛及柯诺辛B四种生物碱对谷氨酸酯诱导的PCI2氧化应激的抑制作用的谱-效关系基础上,利用SPSS15．0软件进行分析,建立谱-效关系模型。结果钩藤碱和柯诺辛对PCI2细胞氧化应激有显著的抑制作用,其谱-效方程为：Y=44．301-＋0．255X＋0．356X,,经7批药材验证,谱-效关系式计算值与实际值的偏差率不超过10％。结论该谱-效关系模式可用于预测钩藤对谷氨酸酯诱导的PCI2细胞氧化应激的抑制作用。     

An extract of Uncaria tomentosa inhibiting cell division and NF-kappa B activity without inducing cell death

Previous reports have demonstrated that extracts of the plant Uncaria tomentosa inhibit tumor cell proliferation and inflammatory responses. We have confirmed that C-Med 100, a hot water extract of this plant, inhibits tumor cell proliferation albeit with variable efficiency. We extend these findings by showing that this extract also inhibits proliferation of normal mouse T and B lymphocytes and that the inhibition is not caused by toxicity or by induction of apoptosis. Further, the extract did not interfere with IL-2 production nor IL-2 receptor signaling. Since there was no discrete cell cycle block in C-Med 100-treated cells, we propose that retarded cell cycle progression caused the inhibition of proliferation. Collectively, these data suggested interference with a common pathway controlling cell growth and cell cycle progression. Indeed, we provide direct evidence that C-Med 100 inhibits nuclear factor kappa B (NF-kappa B) activity and propose that this at least partially causes the inhibition of proliferation.     

钩藤多动合剂的药效作用及用代谢物组学方法研究其生化机制

目的 用代谢物组学方法研究钩藤多动合剂(简称多动合剂)的药效作用及其治疗儿童多动症的生化机制，观察药物对小鼠脑内神经递质的影响。方法 采用攀爬实验和自发行为实验研究多动合剂对去水吗啡小鼠模型的药效作用，同时用高效液相色谱-电化学检测方法研究其生化机制，观察药物对小鼠脑内及血浆中单胺类神经递质多巴胺(DA)和去甲肾上腺素(NE)的影响。结果 去水吗啡激动黑质纹状体系统内DA受体，使系统内DA功能增强，引起小鼠攀爬行为和自发活动增强，多动合剂可抑制去水吗啡引起的小鼠的攀爬行为，并减弱自发活动的增强。对去水吗啡引起的血浆中DA和NE含量的改变及脑组织中DA含量的改变，多动合剂均能予以校正，使各项指标接近空白对照组水平。实验结果表明多动合剂可提高小鼠血浆中DA含量，并降低脑组织中DA的含量。结论 多动合剂能调整单胺类神经递质的失衡以此达到治疗多动综合征的目的。     

Advances in chemistry and bioactivity of the genus Uncaria

The alkaloids of the pantropical genus Uncaria (Rubiaceae) were reviewed extensively by Phillipson et al. in (1978) Since then a host of papers with new results has been published. The compounds discovered are from three major groups: (1) alkaloids; (2) terpenoids; and (3) flavonoids. Some highly unusual structures have been reported. Although there are at least 35 species of Uncaria known, recent research focussed on a relatively small number of species. During recent years bioactivity of extracts and pure compounds isolated from Uncaria species have been increasingly investigated. These include anticonvulsive, antiinflammatory, antimutagenic, antioxidant, cytoprotective, hypotensive, and immunoregulatory effects. The literature since 1978 is reviewed and 133 references are given.     

Uncaria tomentosa extracts protect human erythrocyte catalase against damage induced by 2,4-D-Na and its metabolites

The effect of ethanolic and aqueous extracts from leaves and bark of Uncaria tomentosa was studied, with particular attention to catalase activity (CAT – EC. 1.11.1.6).     

镇肝熄风汤与天麻钩藤饮对小鼠自发活动抑制作用的药效动力学研究

本文从药效动力学角度，选择对小鼠自发活动抑制作用为效应观测指标，探讨了镇肝熄风扬与天麻钩藤饮两方的体内过程，并求得各方程及相应参数，结果表明：两方的起效剂量较低，作用期及半衰期亦较短。提示两方在用于临床镇静治疗时，似可降低给药量，并缩短给药间隔时间。     

天麻钩藤饮对高血压病患者血压及血清GSH-PX的影响

目的探讨天麻钧藤饮对肝阳上亢型高血压病患者血压的影响及其抗氧化应激的研究.方法选择肝阳上亢型高血压病人60例,随机分为天麻钩藤饮组(治疗组)30例和非洛地平组(对照组)30例,治疗4周,分别检测治疗前后患者血压和血清谷胱甘肽过氧化物酶(GSH-PX)的活力变化,并用20例正常人的血清作参考.结果治疗后两组血压均明显下降,两组间比较差异无显著性(P＞0.05),而治疗组GSH-PX的升高较对照组明显(t=11.48,P＜0.01).结论天麻钩藤饮对肝阳上亢型高血压病患者具有良好的降压效果,并且能增加患者的GSH-PX活力,清除过多的氧自由基,防止血管内皮细胞的脂质过氧化,从而改善患者血管内皮功能.     

中药饮片紫苏子和钩藤的耐热菌考察

目的 考察中药饮片紫苏子和钩藤中耐热菌数随加热时间增加的变化情况,为相关标准制定提供数据支持。方法 按照中国药典2020年版中药饮片微生物限度检查法（增订草案）中的方法对2种饮片进行计数方法适用性检查,然后测定不同沸水浴时间耐热菌数,分离鉴定存活的耐热菌,并进行灭活实验。结果 检验结果符合中国药典2020版通则1107（修订草案）。随着沸水浴时间的延长,耐热菌数量显著下降。鉴定结果显示耐热菌株均为芽孢杆菌属。结论 中药饮片存在一定的耐热菌污染,应建立合理的耐热菌质控标准,保障中药饮片的用药安全。     

采用HPLC-MS-AIS法测定钩藤中四种生物碱含量

目的 采用高效液相-质谱联用-自体内标法（HPLC-MS-AIS）测定钩藤中四种主要的吲哚类生物碱（钩藤碱、异钩藤碱、去氢钩藤碱、异去氢钩藤碱）含量。方法 采用C18色谱柱（3.0 mm×50 mm,3.3μm）;0.1%甲酸水溶液∶乙腈=82∶18为流动相;流速0.5 mL/min;柱温30℃。质谱条件：电喷雾离子源;正离子多反应监测模式;毛细管电压为4 000 v;选择质子数/电荷数（m/z）:385.25/160.10（钩藤碱）、385.30/160.10（异钩藤碱）、383.25/160.15（去氢钩藤碱）、383.25/160.15（异去氢钩藤碱）作为检测离子对;进样量2μL。结果 钩藤碱、异钩藤碱、去氢钩藤碱、异去氢钩藤碱线性范围分别为2.30～600.00 ng/mL(r=0.999 3)、2.30～600.00 ng/mL(r=0.999 2)、2.47～650.00 ng/mL(r=0.999 4)、2.47～650.00 ng/mL(r=0.999 2),精密度和稳定性的相对标准偏差（RSD）均<5.00%,准确度为92.40%～104.10%,加样回收率为9...