Effects of Tianma(Rhizoma Gastrodiae)and Gouteng(Ramulus Uncariae Rhynchophyllae cum Uncis)on cytochrome P450 enzyme activities in rats

OBJECTIVE:To investigate the efficacy of Tianma(Rhizoma Gastrodiae)and Gouteng(Ramulus Uncariae Rhynchophyllae cum Uncis)on cytochrome P450(CYP450)enzyme activities in rats.METHODS:A cocktail strategy was followed to evaluate the influence of Tianma(Rhizoma Gastrodiae)and Gouteng(Ramulus Uncariae Rhynchophyllae cum Uncis)on the activities of CYP450 isoforms(CYP1A2,CYP3A4,CYP2E1,CYP2C19,CYP2C9,CYP2D6),which were determined by changes in the pharmacokinetic parameters of six probe drugs,theophylline,dapsone,chlorzoxazone,omeprazole,tolbutamide and dextromethorphan.Study groups included,Control group(CG),Tianma(Rhizoma Gastrodiae)group(TM),Gouteng(Ramulus Uncariae Rhynchophyllae cum Uncis)group(GT)and Tianma Gouteng(Gastrodia Uncaria)group(TMGT).RESULTS:No significant differences between Tianma(Rhizoma Gastrodiae)and control groups were found.Compared with the control group,in the Gouteng(Ramulus Uncariae Rhynchophyllae cum Uncis)group both the AUC and t1/2 of dapsone and tolbutamide were reduced,whereas the CL(clearance rate)of dapsone and tolbutamide were increased.Compared with the control group,in the Tianma Gouteng group,the AUC and t1/2 of dapsone and tolbutamide were reduced,the CL of dapsone and tolbutamide were increased,and the AUC and t1/2 of chlorzoxazone were increased and the CL of chlorzoxazone was reduced.CONCLUSION:Tianma(Rhizoma Gastrodiae)has no significant effect on the six CYP450 subtypes.The activities of CYP3A4 and CYP2C9 were increased by Gouteng(Ramulus Uncariae Rhynchophyllae cum Uncis).The activities of CYP3A4 and CYP2C9 were increased,whereas the activity of CYP32E1 was reduced by combined Tianma(Rhizoma Gastrodiae)and Gouteng(Ramulus Uncariae Rhynchophyllae cum Uncis).

HPLC法测定钩藤提取物中钩藤碱的含量

[目的]测定钩藤提取物中有效成分钩藤碱的含量。[方法]采用HPLC法测定钩藤提取物中钩藤碱的含量,色谱柱为DiamonsilC18(250 mm×4.6 mm,5μm);流动相为无水甲醇-水(60∶40,V/V)并含10 mmol/L三乙胺,冰醋酸调pH 7.5;柱温为30℃;流速为1.0ml/min;紫外检测波长为254 nm。[结果]钩藤碱浓度在11.0～110.0μg/ml范围内与峰面积的线性关系良好(R=0.999 6),平均回收率为96.84%,RSD为1.46%。[结论]该方法简单、快速、准确,可用于钩藤提取物中钩藤碱的含量测定。

钩藤的化学成分研究

[目的]对钩藤的化学成分进行研究。[方法]利用柱层析对钩藤的化学成分进行分离纯化,然后根据化合物的理化性质和光谱数据鉴定所得到化合物的结构。[结果]从钩藤中分离得到了5个化合物,分别鉴定为乌苏酸、β-谷甾醇、β-胡萝卜苷、柯诺辛碱和钩藤碱。[结论]该方法分析研究了钩藤的化学成分,为钩藤的进一步开发和利用提供参考。

钩藤中钩藤碱的提取和含量测定

[目的]研究钩藤中钩藤碱的提取和含量测定方法。[方法]采用生物碱回流提取方法提取,采用高效液相色谱法对钩藤中钩藤碱的含量进行测定并计算提取率。[结果]专属性考察结果显示,钩藤碱的保留时间约为18.843 min,异钩藤碱的保留时间约在22.323min,两峰分离度良好,且钩藤药材中其他成分不干扰测定;含量测定结果显示,钩藤碱和异钩藤碱的含量分别为23.23、129.17μg/g,加样回收试验平均回收率分别为99.12%、101.33%,RSD分别为1.84%、1.56%。[结论]该方法稳定、有效、准确度高,可用于钩藤中钩藤碱的含量测定。

中国商事仲裁的国际化挑战——以最高人民法院的裁判观点为视角

国际仲裁在我国的演进呈现出与西方相反的发展态势,即我国只承认机构仲裁。而现代仲裁法的发展特征之一即在于对国内仲裁与国际仲裁进行区分。在近3年的中国仲裁实践中,最高人民法院的裁判折射出明显的国际化与包容化立场,尤其是在针对境外仲裁机构在中国内地仲裁的开放、中国仲裁机构适用境外仲裁机构仲裁规则的自由等例证。但在无涉外因素纠纷能否约定境外仲裁的问题上,最高人民法院的立场却相对保守,且其裁判理由难以自洽。

UFLC‑PDA‑MS/MS Profling of Seven Uncaria Species Integrated with Melatonin/5‑Hydroxytryptamine Receptors Agonistic Assay

Uncariae Ramulus Cum Uncis(Gou-Teng),the dried hook-bearing stems of several Uncaria plants(Rubiaceae),is a wellknown herbal medicine in China.The clinical application of Gou-Teng is bewildered for the morphological and chemical similarity between diferent species.In order to discern their chemical and biological diference,an ultra-fast liquid chromatography equipped with ion trap time-of-fight mass spectrometry(UFLC-IT/TOF-MS)combining with melatonin(MT1 and MT2)and 5-hydroxytryptamine(5-HT1A and 5-HT2C)receptors agonistic assay in vitro was conducted on seven Uncaria species.As a result,57 compounds including 35 indole alkaloids,ten favonoids,fve triterpenoids,fve chlorogenic analogues,and two other compounds were characterized based on their MS/MS patterns and UV absorptions.Specifcally,cadambine-type and corynanthein-type alkaloids were exclusively present in U.rhynchophylla and U.scandens,whereas corynoxine-type alkaloids were commonly detected in all the seven Uncaria plants.Three Uncaria species,U.rhynchophylla,U.macrophylla,and U.yunnanensis showed obviously agnostic activity on four neurotransmitter receptors(MT1,MT2,5-HT1A,and 5-HT_(2C)).This frst-time UFLCMS-IT-TOF analyses integrated with biological assay on seven Uncaria plants will provide scientifc viewpoints for the clinical application of Gou-Teng.