高效液相色谱法测定当归龙荟丸中栀子苷的含量

目的建立高效液相色谱法测定当归龙荟丸中栀子苷的含量。方法 AgelaPromosilC18(250mm×4.6mm,5μm)分析柱,流动相为乙腈-水(14:86),流速为1.0mL·min-1,检测波长为240nm。结果栀子苷与其他组分分离良好。线性范围为0.101μg～1.010μg,相关系数r=0.9998,平均加样回收率为98.48%(RSD=0.65%)。结论本法简便、准确可靠,可用于该药的质量控制。     

栀子金花丸中栀子苷含量的胶束毛细管电泳法测定

目的建立测定栀子金花丸中栀子苷含量的胶束毛细管电泳法。方法采用未涂层弹性融硅石英毛细管柱(60 cm×75μm ID,有效长度52 cm);以25 mmol.L-1硼砂+25 mmol.L-1SDS+4 mmol.L-1磺丁基-β-环糊精+8%(体积分数)甲醇(pH 9.5)为运行缓冲液;分离电压14 kV;重力进样10 s(高度15 cm);检测波长238 nm。以维生素B1为内标。结果栀子苷浓度在21.0～63.0μg.ml-1内线性关系良好(r=0.9999),栀子苷平均加样回收率100.5%,方法精密度(RSD)为0.56%(n=6)。结论该方法简便、快速,结果准确可靠,可用于栀子金花丸的质量控制。     

京尼平和栀子苷含量的高效液相色谱法同时测定

目的建立HPLC同时测定栀子苷和京尼平的方法。方法采用C18(4.6 mm×250 mm,5μm)色谱柱,流动相为甲醇-水(60∶40),流速为0.6 ml.min-1,检测波长为238 nm。结果在该色谱条件下,栀子苷和京尼平得到较好的分离,栀子苷和京尼平浓度在0.01～0.2 mg.ml-1范围内峰面积与进样量呈良好的线性关系,平均回收率为102.29%。结论该方法具有重复性好、准确、快速等优点,适用于栀子苷和京尼平的同时测定。     

The effects of notoginsenoside R₁ on the intestinal absorption of geniposide by the everted rat gut sac model

Ethnopharmacological relevance

Geniposide is derived from Gardenia jasminoides Ellis (Rubiaceae). Its anti-inflammatory, antithrombotic effects as well as its preventive effect against ischemic stroke have been reported. Radix notoginseng (Chinese name tienchi or sanqi) is the dried root of Panax notoginseng (Burk.) F.H. Chen, an herb noted for its promotion of blood circulation, blood stasis removal and pain alleviation, and has been widely utilized for the prevention and treatment of microcirculatory disturbances in China and other Asian countries for many years. Notoginsenoside R₁ is an effective and structurally representative bioactive constituent of R. notoginseng. In our preliminary study, notoginsenoside R₁ was able significantly to improve the bioavailability of geniposide in beagle dogs, but the underlying mechanisms remain unknown.

Materials and Methods

The present study aimed to investigate the intestinal kinetic absorptive characteristics of geniposide as well as the absorptive behavior influenced by the co-administration of notoginsenoside R₁ using an in vitro everted rat gut sac model.

Results

The results showed good linear correlation between the geniposide absorption in sac contents and the incubation time from 0 to 120 min. The concentration dependence showed a non-linear correlation between the geniposide absorption and the concentrations 0.356–1.424 mg/mL, the absorption was saturated about 1.424 mg/mL. Notoginsenoside R₁ at 0.1 and 0.2 mg/mL concentrations was able significantly to enhance the absorption of geniposide (1.424 mg/mL) by 1.7- and 1.4-fold. Moreover, verapamil, a well-known P-glycoprotein inhibitor, was able significantly to elevate the absorption of geniposide 2.4-fold. Notoginsenoside R₁ influenced geniposide's absorption in a way similar to that of a P-glycoprotein inhibitor.

Conclusions

In conclusion, notoginsenoside R₁ significantly enhances the intestinal absorption of geniposide. As for the mechanism underlying the improvement of geniposide's bioavailability, it is proposed that notoginsenoside R₁ was able to decrease the efflux transport of geniposide by P-glycoproteins.     

Ameliorating effect of Zhizi (Fructus Gardeniae) extract and its glycosides on scopolamine-induced memory impairment

Objective

To study the chemical constituents of Zhizi (Fructus Gardeniae) and their antiamnesic effect in a mouse model of Alzheimer's disease.

Methods

Ameliorating effects of the extracts, fractions and constituents on scopolamine-induced memory impairment in vivo using a passive avoidance task system and their inhibitory activities on acetylcholinesterase (AChE) in vitro were examined. The isolation of components was performed by chromatographic techniques and their structures were identified on the basis of spectral analysis.

Results

Activity-guided fractionation of the total extracts resulted in the isolation of two glycosides, geniposide and crocin from the n-butanol fraction and genipin and crocetin from the ethylacetate fraction. Among the fractions tested, n-butanol fraction showed the strongest AChE inhibition (43.4% at a final dose of 0.03 mg/mL) and also exhibited outstanding efficacy (65.9% at a dose of 250 mg/kg) in an experimental model of amnesia. Geniposide showed a 22.8% AChE inhibitory activity and a potent ameliorating effect on scopolamine-induced memory impairment in amnesic mice of 93.4% as compared to the control group.

Conclusion

Geniposide, a main constituent of gardenia should be considered a candidate for further clinical study for the purpose of developing a cognition activator and its mechanism of action may be mediated, at least in part, by the acetylcholine enhancing cholinergic nervous system.     

HPLC法测定清火栀麦口服液中脱水穿心莲内酯和栀子苷含量

目的建立高效液相色谱法测定清火栀麦口服液中脱水穿心莲内酯和栀子苷含量的方法。方法采用依利特C18（4.6mm×200mm,5μm）色谱柱,脱水穿心莲内酯的流动相为甲醇-水（55∶45）,检测波长为250nm;栀子苷的流动相为乙腈-水（13∶87）,检测波长为238nm。结果脱水穿心莲内酯在0.24～1.20μg范围内与峰面积呈良好的线性关系,r=0.9999,平均回收率=97.69%,RSD=1.63%;栀子苷在1.68～6.72μg范围内与峰面积积分值呈良好的线性关系,r=0.9999,平均回收率=101.09%,RSD为2.66%。结论HPLC法能准确、快速地测定清火栀麦口服液中脱水穿心莲内酯和栀子苷的含量。     

京尼平苷对慢性前列腺炎大鼠前列腺组织中细胞因子的影响

【目的】探讨京尼平苷对慢性前列腺炎（chronic prostatitis,CP）模型大鼠治疗作用机制。【方法】采用前列腺内注射消痔灵方法复制慢性前列腺炎模型,随机分为模型组、阳性药组（前列康片组,2g／kg）及京尼平苷高、中、低剂量组（20、10、5mg／kg）。28d后处死大鼠,取前列腺组织,观察前列腺病理改变,并对前列腺组织内炎细胞、成纤维细胞、腺体数量和腺腔面积等形态学变化情况进行分析。同时ELISA法检测前列腺组织匀浆中白介素-1β（IL-1β）、白介素-6（IL-6）、肿瘤坏死因子（TNF-α）和白介素-10（IL-10）的含量。【结果】京尼平苷高剂量组、前列康片组与模型组比较,前列腺间质中炎细胞数、成纤维细胞数均显著降低,腺体数量与腺腔面积明显升高（P〈0.05或P〈0.01）;CP大鼠前列腺中IL-1β、IL-6、TNF-α明显降低,IL-10含量显著上升（P〈0.01或P〈0.05）。【结论】京尼平苷对大鼠慢性前列腺炎的治疗作用与其降低前列腺内炎性细胞因子（IL-1β、IL-6、TNF-α）、提高抑炎细胞因子（IL-10）水平、减轻炎细胞浸润、抑制纤维组织增生有关。     

炒制对闽产栀子饮片中栀子苷含量影响

目的:研究炒制对闽产栀子中栀子苷含量的影响。方法:采用高效液相色谱法。Phenomenex C18色谱柱(4.6mm×200mm,5μm);流动相:乙腈-水(15∶85);检测波长:238nm;流速为1.0ml·min-1。结果:用HPLC法测得闽产栀子、炒栀子、焦栀子中栀子苷的含量随着炮制程度的加重依次递减。结论:栀子中栀子苷平均含量为7.13%,炒栀子栀子苷平均含量为6.95%,焦栀子栀子苷平均含量为5.67%。     

HPLC法测定清热暗疮丸中栀子苷的含量

目的寻找测定清热暗疮丸中栀子苷含量的可靠方法,以控制产品的质量。方法高效液相色谱法,乙腈-水(11∶89)为流动相;色谱柱为Diamonsil(钻石)C18柱(250mm×4.6mm×5μm),体积流量为1.0mL/min,检测波长为238nm,采用外标法。结果栀子苷在9.08～105.8μg范围里呈较好的线性关系;栀子苷的回收率为100.19%。结论高效液相色谱法操作简单,结果可靠,重复性好,为清热暗疮丸质量控制提供科学依据。     

高效液相色谱法测定栀子组分中栀子苷含量

目的利用高效液相色谱法以栀子苷为指标对栀子组分进行定量分析,建立栀子组分的含量测定方法。方法采取反相高效液相色谱法,利用C18色谱柱,以乙腈∶水(15∶85)为流动相,在238 nm波长下测定栀子组分中栀子苷含量。结果在上述测定条件下,栀子苷在0.49～7.79μg范围内线性关系良好。测定方法重复性良好,RSD=1.15%(n=6),栀子组分中栀子苷的平均回收率=100.06%(n=5),RSD=1.38%。结论所建立的方法准确性、灵敏度、重复性高,简便,准确,易操作,可作为栀子组分的质量控制方法,色谱法为组分提供有意义的方法学参考。