薄层扫描法测定垂阴茶糖浆中岩白菜素的含量

目的:建立垂阴茶糖浆岩白菜素的测定方法,方法:λs=275 nm,λR=320nm,用薄层色谱法测定岩白菜素的含量.结果:岩白菜素在0.505～3.030μg范围内线性关系良好(r=0.999 9),平均回收率为96.52%.RSD=0.44%.结论:该法灵敏度高,重现性好,可用于该制剂中岩白菜素的含量测定及质量控制.     

正交实验设计优化岩白菜素微囊的制备工艺

目的优化岩白菜素微囊的制备工艺,并对制备的岩白菜素微囊进行质量评价。方法以明胶为囊材,单凝聚法制备岩白菜素微囊,通过正交实验设计优化其制备工艺,并对包封率、载药量、平均粒径、体外溶出率进行研究。结果明胶制备岩白菜素微囊的最佳工艺条件为:明胶质量分数为6%,囊心囊材质量比为1∶2,搅拌速度为750r·min^-1。此最佳工艺制备的岩白菜素微囊包封率为75.90%,载药量为23.09%,体外溶出度测定30min为28.6%,12h累计释放达到90%以上。结论以最佳工艺条件制备岩白菜素微囊工艺稳定,包封率高,同时体外释放实验表明,该微囊具有较好的缓释作用。     

Development and validation of UPLC-PDA method for concurrent analysis of bergenin and menisdaurin in aerial parts of Flueggea virosa (Roxb. ex Willd.)

Bergenin and menisdaurin are biologically active components which are found in plant Flueggea virosa (Phyllanthaceae). Bergenin has pharmacological actions such as chemopreventive and antihepatotoxic while menisdaurin has an anti-viral activity which needs its evaluation by an analytical method (UPLC-PDA method) that can be applied to the quality control of pharmaceutical preparations. The developed UPLC-PDA method was applied for identification and quantification of standards bergenin and menisdaurin in the methanol extract of F. virosa (FVME). The analysis was carried out using Eclipse C18 (4.6?×?100?mm, 3.5?µm) UPLC column. The optimized chromatographic condition was achieved at 0.16?mL/min flow rate using gradient system with acetonitrile and water as mobile phase. Both biomarkers were measured at λ_max 235?nm in PDA detector at ambient temperature. The developed method furnished sharp and intense peaks of menisdaurin and bergenin at Rt?=?2.723 and 3.068?min, respectively along with r2?>?0.99 for both. The recoveries of bergenin and menisdaurin were found in the range of 99.37–101.49% and 98.20–100.08%, respectively. With other validation data, including precision, specificity, accuracy, and robustness, this method demonstrated excellent reliability and sensitivity. The separation parameters i.e. retention, separation, and resolution factors for resolved standards (bergenin and menisdaurin) were >1, which showed good separation. The quantity of bergenin and menisdaurin in the FVME sample was found as 15.16 and 3.28% w/w, respectively. The developed UPLC-PDA method could be conveniently adopted for the routine quality control analysis.     

The influence of Sacoglottis gabonensis stem bark extract and its isolate bergenin, Nigerian alcoholic beverage additives, on the metabolic and haematological side effects of 2,4-dinitrophenyl hydrazine-induced tissue damage

This study was designed to study the influence of Sacoglottis gabonensis stem bark extract on the metabolic and cytotoxic side effects of 2,4-dinitrophenyl hydrazine (2,4-DNPH) on the brain and blood using male weaving rats as the experimental model. This was after the effect of the bark extract and bergenin, its isolate, on membrane lipid peroxidation and tissue natural antioxidant defences was reported. Lipid peroxidation was induced experimentally with a single intraperitoneal phenylhydrazine (2,4-DNPH) administration at the end of 3 days exposure to the bark extract or bergenin in drinking water. Three hours later, the brain, liver and red blood cells of the experimental animals were analysed for glucose level and the blood was analysed for selected key indices of oxidative stress: red blood cell (RBC) count haemoglobin (Hb), packed cell volume (PCV) and white blood cell (WBC) count (total and differential). The bark extract exhibited a protective action on brain glucose, significantly inhibiting the glucose-depleting action of both 2,4-DNPH and ethanol. It also inhibited the lowering action of DNPH and ethanol on PCV, RBC and Hb concentration of rat blood, but inhibited proliferation of white blood cells (total and differential). The data on the effect of bergenin, on the side effects of 2,4-DNPH experimental lipid peroxidation and on ethanol followed an essentially similar trend to those of the bark extract on brain glucose. Bergenin, similar to the bark extract, exerted a protective action on the brain tissue, though to a lesser extent, against the oxidants, 2,4-DNPH and ethanol. It is evident that aqueous ethanol extract of S. gabonensis stem bark has biological antioxidant properties against 2,4-DNPH and ethanol-induced tissue damage exerting its action on the haematological and metabolic side effects of the oxidants. By virtue of its essentially similar activity under the same conditions, bergenin appears to be the phytochemical constituent that is largely responsible for the observed action of the bark extract.     

岩白菜素大鼠在体肠吸收动力学的研究

目的 研究岩白菜素在大鼠肠道内的吸收动力学特征.方法 采用大鼠在体灌流模型,应用HPLC测定回流液和血浆中岩白菜素的含量,从吸收部位、药物浓度、pH值三方面对岩白菜素的肠吸收特性进行研究.结果 岩白菜素在0.07～0.21 mg/mL范围内的吸收具有线性动力学特征;在十二指肠、空肠、回肠和结肠的吸收各不相同;在pH5.40～7.80范围内,吸收速率随pH值增大而减小.结论 岩白菜素在大鼠全肠段均有吸收,但吸收较差,其吸收呈一级动力学过程,吸收机制主要为被动扩散.     

Effects of Astilbe thunbergii rhizomes on wound healing Part 1. Isolation of promotional effectors from Astilbe thunbergii rhizomes on burn wound healing

The dried rhizomes of Astilbe thunbergii (Sieb. et Zucc) Miq (Saxifragaceae) have been traditionally used for the treatments of a sword cut, wound bitten by animals, frost-bite, burn, suppurative dermatitis or skin inflammatory diseases from the Tang period (about 8th century) in China. The physiological actions, especially the wound-healing effects of this drug are not yet well understood. In this study, we examined the effects of an ethanol extract of Astilbe thunbergii rhizomes on burn wound healing in mice. The topical application at a dose of 100mg ointment per wound of 70% ethanol extract (0.5 or 1.0% (w/w) ointment) of this drug promoted the burn wound healing. The ethanol extract was divided into two fractions (ethyl acetate-soluble and -insoluble fractions), and it was found that the topical application at a dose of 100mg ointment per wound of the ethyl acetate-soluble fraction (0.5 and 1.0% ointment) promoted the burn wound healing. Based on this finding, we attempted to isolate the active substance(s) from the ethyl acetate-soluble fraction. Three active substances 1, 2 and 3, were obtained from A. thunbergii rhizomes as promotional effectors of burn wound healing in mice. Based on the analysis of (1)H and (13)C NMR spectra, compounds 1, 2 and 3 were identified as eucryphin (1), bergenin (2) and astilbin (3), respectively. The effective dose (ED(50)) of compounds 1, 2 and 3 on burn wound healing were 4, 190 and 64 microg/wound, respectively. Among these three compounds, eucryphin (1) promoted the burn wound healing most strongly.     

Immunomodulatory effect of bergenin and norbergenin against adjuvant-induced arthritis--a flow cytometric study

Bergenin (1), a C-glycoside of 4-O-methyl gallic acid, isolated from rhizomes of Bergenia stracheyi (Saxifragaceae) and its O-demethylated derivative norbergenin (2), prepared from 1, are reported to show anti-arthritic activity through possible modulation of Th1/Th2 cytokine balance. Flow cytometric study showed that the oral administration of 1 and 2 at doses of 5, 10, 20, 40 and 80 mg/kg per oral dose inhibit the production of proinflammatory Th1 cytokines (IL-2, IFN-gamma and TNF-alpha) while as potentiate anti-inflammatory Th2 cytokines (IL-4 and IL-5) in the peripheral blood of adjuvant-induced arthritic balb/c mice. This shows the potential Th1/Th2 cytokine balancing activity of 1 and 2 which is strongly correlated with their anti-arthritic activity. At similar dose levels, the effect of 2 was found to be more than that of 1. The oral LD(0) for 1 and 2 was more than 2000 mg/kg body weight of the mice.     

翼茎白粉藤药材薄层色谱检测方法研究

目的：建立翼茎白粉藤药材的薄层色谱鉴别。方法：翼茎白粉藤经甲醇提取后,以三氯甲烷-乙酸乙酯-甲醇（2．5：2：1）为展开剂,对翼茎白粉藤中岩白菜素进行薄层鉴别。结果：薄层色谱鉴别斑点清晰,能有效鉴别翼茎白粉藤中岩白菜素。     

岩白菜素的乙酰化修饰

目的研究岩白菜素乙酰化产物的合成．方法在吡啶介质中以乙酸酐对岩白菜素进行乙酰化．结果得到3个未见文献报道的部分乙酰化岩白菜素并阐明其结构．结论在吡啶中用乙酸酐乙酰化,可得到岩白菜素的部分乙酰化产物．     

不同产地矮地茶药材差异成分筛选及标准汤剂的质量研究

目的：建立矮地茶超高效液相色谱法特征图谱以筛选不同产地矮地茶药材差异成分,并同时建立岩白菜素和槲皮苷的含量测定方法以探索饮片及标准汤剂的量值传递。方法：制备矮地茶标准汤剂,同时建立超高效液相色谱法特征图谱及含量测定方法,对不同产地的17批矮地茶样品进行测定,采用判别分析及熵权Topsis法对不同产地矮地茶药材进行评价,筛选其差异化合物,并对其中2个成分进行含量测定。结果：通过建立矮地茶超高效液相色谱法特征图谱指认了4个成分;筛选得到不同产地间的矮地茶样品差异化合物为峰2、峰4（岩白菜素）、峰5（杨梅苷）。标准汤剂岩白菜素含量均值为4.53%,转移率均值为63.05%,槲皮苷含量均值为0.57%,转移率均值为57.31%,量值传递均较好。结论：本研究采用超高效液相色谱法特征图谱结合多指标含量测定评价不同产地矮地茶药材和标准汤剂量值传递规律,结果科学合理,为矮地茶药材和标准汤剂的质量控制及评价提供参考。