发霉叉蕊薯蓣中的甾体皂甙元

前报报道了从国产野生叉蕊薯蓣(Dioscorea collettii Hook.f.)根茎的水解物中分得了10个甾体化合物,其中约莫皂甙元(yamogenin)和薯蓣皂甙元(diosgenin)为主要成分。从根茎中还分得4个约莫皂甙元的甾体皂甙。在研究国产野生薯蓣属植物化学成分的工作中,我们曾观察到一些薯蓣属植物的根茎长时间发霉后可生成表丝兰皂甙元(epi-smilagenin)和丝兰皂甙元酮(smilagenone)。这些皂甙元的存在造成薯蓣皂甙元产品的熔点降低,质     

薯蓣属植物中薯蓣皂甙元的含量测定

以穿龙薯蓣(Dioscorea nipponica Makino)为对象,研究了根中薯蓣皂甙元的定量方法,并进一步試用于测定其他四种薯蓣植物。植物的根剪碎成小粒状,加酸迴流水解,用苯提取皂甙元,提出物經氧化鋁柱层离分出薯蓣皂甙元后,以改良Liebermann試剂显色,比色测定。本法簡便易行,結果稳定,适于作一般例行分析。     

橙黄茄中的薯蓣皂甙元

近年来,有些学者报道了许多茄属植物中含有甾体生物碱与皂甙,如某些植物的果实中澳洲茄胺(Solasodine)的含量可达2～5％。由于它们可作为合成甾体激素的薯蓣皂甙元的代用品,这就引起更大的重视。本文作者采用气相层析和质谱分析法测定橙黄茄(Solanum aurantiacobaccatum)中薯蓣皂甙元的含量。     

薯蓣属植物化学成分的研究——Ⅹ.蜀葵叶薯蓣中甾体皂甙和皂甙元的分离和鉴定

蜀葵叶薯蓣(Dioscorea althaeoides Kunth)为我国特有薯蓣品种,主产于四川、云南等省。根茎含薯蓣皂甙元。我们在系统研究国产薯蓣属植物化学成分的工作中,对蜀葵叶薯蓣中的甾体皂甙和皂甙元进行分离和鉴定。     

薯蓣属植物化学成分的研究Ⅳ——从低熔点薯蓣皂甙元中分离丝兰皂甙元酮

利用国产野生薯蓣属植物生产的薯蓣皂甙元(Diosgenin),有时熔点偏低,达不到现行熔点标准。为了查明其原因,以及阐明以熔点判断薯蓣皂甙元的质量优劣是否合理,国内正在从事这方面的研究工作。我们前曾报道由野生叉蕊薯蓣(Dioscorea collettii Hook.f.)的根茎中得到的甾体皂甙,经酸解获得约莫皂甙元及其C_(25)-异构化物薯蓣皂甙元。此混合甙元的熔点为186～188℃,低于薯蓣皂甙元的熔点。我们对一些低熔点的薯蓣皂甙元作了化学分离     

薯蓣属植物化学成分的研究Ⅴ——薯蓣属发霉植物中的甾体皂甙元

前文我们报道了从国产的某些低熔点薯蓣皂素(商品名,化学名称为薯蓣皂甙元Diosgenin)中分得了丝兰皂甙元酮(Smila-genone),并证明该成分的存在是造成薯蓣皂素熔点偏低的因素之一。1982年我们收集到另一批低熔点的薯蓣皂素,库仑滴定法测定着蓣皂甙元的含量为76％,薄层主要示有薯蓣皂甙元的斑点和另一比薯蓣皂甙元Rf     

薯蓣属植物中薯蓣皂苷元的研究进展

薯蓣属植物是一类极其重要的经济作物 ,其中 30多种薯蓣属植物所含薯蓣皂苷 (元 )是合成多种甾体激素比较理想的重要原料。此文对我国薯蓣属植物的资源分布、薯蓣皂苷元的提取和生产工艺、化学成分、组织培养进行了概述 ,展望了该产业的发展前景。     

苦木科植物的Balanites roxburghii的叶及果仁中的薯蓣皂甙元

目前世界各国都在致力于寻找薯蓣皂甙元产量高的薯蓣属植物,同时对能够提供薯蓣皂甙元及其类似物的其它植物,也正在进行探索。本文对苦木科植物 B.roxburghii 的叶子和果仁部分作了较系统的研究。研碎的值物果仁(180克)在索氏提取器中以甲醇回流提取,所得稠厚浓缩物经己烷及乙醚浸渍处理后,将其溶于最少量的乙醇中,加入大量乙醚使皂     

浙江产薯蓣属萆薢组药材的化学成分综述

萆薢组植物隶薯蓣科薯蓣属,在我国有悠久的药用历史。古代主要用于利湿去浊,祛风通痹,现经科学研究,发现并证实了许多药理作用与临床疗效。更重要的是该组植物药材含甾体皂甙元(主要为薯蓣皂甙元),它是半合成甾体激素类药物(肾上腺皮质激素,男、女性激素,蛋白同化激素)的主要原料。甾体激素类药物临床应用日益广泛,而且目前的计划生育用药多为各种甾体激素药物制综述     

林生薯蓣和洪都拉斯薯蓣中皂甙元含量的季节性变化

甾体皂甙元为许多有效的甾体药物的前体,其中最重要的为薯蓣皂甙元。本文报导薯蓣皂甙元来源较富的二个品种——林生薯蓣(Dioscorea sylvatica)~*_1及洪都拉斯薯蓣(D.hondurensis)~*_1中含量的季节性变化。研究样品中的林生薯蓣系自南非地区采集的种子,栽植于Nottingham大学温室。洪都拉斯薯蓣系栽植于洪都拉斯,每月寄来新鲜样品。林生薯蓣的块茎为扁平圆形,洪都拉斯薯蓣的块茎为纵长分枝状。试验时从挖掘的块茎切取不同部位作为样品。含量测定系用Blunden及Hardman(1963)法,即     

Diosgenin, a steroidal sapogenin, enhances antigen-specific IgG2a and interferon-gamma expression in ovalbumin-sensitized BALB/c mice

The effect of diosgenin, the most abundant sapogenin in Chinese yam, on humoral immunity was investigated. Ovalbumin (OVA)-sensitized and challenged BALB/c mice were administered daily with diosgenin for 34 days. The production of OVA-specific serum IgG2a was significantly enhanced by diosgenin treatment, whereas total IgE and OVA-specific IgG1, IgG2a and IgM were unaffected. In parallel with the enhancement of IgG2a, OVA-induced IFN-gamma secretion and mRNA expression were markedly elevated in splenocytes of diosgenin-treated mice, whereas IL-4 expression was unaltered. Furthermore, the expression of T-bet, but not of GATA-3, in splenocytes was up-regulated by diosgenin administration. However, diosgenin treatment did not modulate IL-4 mRNA expression and inflammatory cell infiltration in the lung of OVA-sensitized and challenged mice. Collectively, these data suggest that diosgenin regulates the systemic immune response towards the Th1 direction in response to OVA sensitization. The present study provides evidence to show that intake of diosgenin modulates certain aspects of acquired immunity, including the enhancement of antigen-specific IgG2a and IFN-gamma expression, which may be mediated through the up-regulation of Th1 differentiation.     

薯蓣皂苷元衍生物与M3受体的分子对接研究

目的研究薯蓣皂苷元衍生物与M3受体相互作用可能的构效关系,为薯蓣皂苷元舒张平滑肌的结构改造提供更多的理论基础。方法运用AutoDock4.0研究薯蓣皂苷元衍生物与M3受体的分子对接,并分析了对接结果与薯蓣皂苷元衍生物对离体豚鼠气管平滑肌舒张活性的结果,对接模型中的M3受体分子模型为以牛视紫红质的晶体结构为模板同源建模搭建的人M3受体的三维结构模型。结果薯蓣皂苷元衍生物与M3受体的对接结果与离体豚鼠气管平滑肌舒张的活性结果有一定联系。结论薯蓣皂苷元衍生物Ⅰ～Ⅴ的舒张活性有在一定范围内随碳链增长而提高的趋势;芳香酯类(Ⅵ～Ⅸ)的舒张活性可能与苯环取代基的供电性有关;带苯环的支链酯类(Ⅹ～Ⅺ)的位阻可能对舒张活性影响较大。因此,薯蓣皂苷元衍生物与M3受体的对接对其进一步的修饰有一定的指导作用。     

Timing of Diosgenin Appearance in Suspension Cultures of Dioscorea deltoidea

Cycloheximide and compactin were added to cell suspension cultures of DIOSCOREA DELTOIDEA. Cycloheximide inhibited growth and diosgenin biosynthesis completely at 40 mg/l when added during the growth phase. Compactin partially inhibited growth and diosgenin production at 100 microg/l when added during the growth phase. [1- (14)C]-Acetate incorporation into diosgenin was about 20-fold higher when added during the early stages of growth as compared to addition in the stationary phase. Incorporation of [1- (14)C]-acetate into diosgenin was inhibited by compactin only during the early stages of growth. These results indicate the formation of an accumulating intermediary metabolite during the early stages of growth which is transformed into diosgenin when D. DELTOIDEA cells are in the stationary phase.     

不同剂量薯蓣皂苷元的大鼠体内药动学研究

目的： 研究不同剂量薯蓣皂苷元的大鼠体内药物动力学特征,为阿尔茨海默病的临床前研究提供理论依据。方法： 大鼠灌胃低（17.5 mg·kg^-1）、中（35 mg·kg^-1）、高剂量（70 mg·kg^-1）薯蓣皂苷元后,于不同时间眼眶取血,以延龄草苷作为内标,血浆样品经液-液萃取后采用LC-MS/MS进行测定。利用DAS 2.0计算药动学参数。色谱、质谱条件：采用Sun Fire C₁₈（150 mm×2.1 mm,5 μm）为色谱柱,以甲醇-乙腈-10 mmol·L^-1乙酸铵（86∶11∶3）为流动相,流速为0.3 mL·min^-1,柱温40℃。采用电喷雾离子源（ESI源）,以选择反应监测（MRM）方式并在正离子模式下进行检测,用于定量的离子对分别为m/z 415.5→271.5（薯蓣皂苷元）和m/z 577.5→271.5（内标延龄草苷）。结果： 薯蓣皂苷元血药浓度在1~2 000 ng·mL^-1内线性关系良好,方法回收率在81.7%~83.9%之间,定量下限（LLOQ）为1 ng·mL^-1,日内、日间精密度RSD小于10%。药动学结果表明不同剂量薯蓣皂苷元药-时曲线符合二室模型,主要药动学参数为AUC_0-t分别为1 872,3 144,6 625 ng·min·mL^-1;C_max分别为136,276,470 ng·mL^-1;t_1/2分别为5.73,5.31,6.42 h。结论： 薯蓣皂苷元在17.5~70.0 mg·kg^-1范围内其药动学行为呈线性相关,无动力学行为差异。     

非水毛细管电泳法同时测定麦冬中薯蓣皂苷元和鲁斯可皂苷元的含量

采用非水介质毛细管电泳法同时测定了麦冬中薯蓣皂苷元和鲁斯可皂苷元的含量。以70%甲醇为非水介质,20 mmol.L-1硼砂-HCl为缓冲溶液(pH 7.61),运行为25 kV高压,+0.70 V工作电极电位的条件下,实现了被测组分的有效分离。测得麦冬中薯蓣皂苷元的含量为0.018 mg·g-1,鲁斯可皂苷元的含量为0.008 mg·g-1,薯蓣皂苷元和鲁斯可皂苷元的平均回收率分别为102%和99.2%。本法为麦冬中薯蓣皂苷元和鲁斯可皂苷元的质量控制提供了新方法。     

Mechanisms involved in the vasodilator effect induced by diosgenin in rat superior mesenteric artery

The aim of this study was to investigate the vasorelaxant effect induced by diosgenin in superior mesenteric rings. In rings pre-contracted with phenylephrine (10 microM), diosgenin caused concentration-dependent relaxations [EC(50) = (3.3 +/- 1.2) x 10(- 4)M, E(max) = 94.2 +/- 2.6 %]. Vascular relaxation induced by diosgenin was significantly inhibited after removal of the endothelium (E(max) = 46 +/- 8.8%, p < 0.001) or after pre-treatment of the rings with N-nitro-L-arginine methyl esther (l-NAME) 100 or 300 microM (E(max) = 35.3 +/- 4%; 28.1 +/- 3.3%, respectively, p < 0.001), atropine 1 microM (E(max) = 24.6 +/- 3.4%, p < 0.001), hydroxocobalamin 30 microM (E(max) = 54.0 +/- 9.6%, p < 0.001), 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one (ODQ) 10 microM (E(max) = 46.0 +/- 8.0%, p < 0.001) or indomethacin 1 microM (E(max) = 22.6 +/- 11.8%, p < 0.001). Vasorelaxation evoked by diosgenin was significantly inhibited after pre-treatment of preparations with both selective and non-selective inhibitors of large conductance Ca(2+)-activated K(+) (BK(Ca)) channels, iberiotoxin 100 nM or tetraethylammonium (TEA) 1mM, respectively (E(max) = 62.5 +/- 9.1%; 65.7 +/- 1.1%, p < 0.001). Conversely, in endothelium-denuded vessels, none of BK(Ca) channel blockers modified the relaxant effect induced by diosgenin. In mesenteric endothelial cells loaded with FURA-2 diosgenin was able to increase intracellular calcium concentrations, which were significantly decreased by atropine 1 microM. In addition, in isolated mesenteric rings, diosgenin induced marked increase in nitric oxide (NO) levels, which was completely abolished after functional endothelium removal. The results obtained here demonstrated that diosgenin-induced relaxation appears to involve endothelial muscarinic receptor activation with increase in intracellular calcium concentrations and consequent release of endothelium-derived relaxing factors (EDRFs), mainly NO and cyclooxygenase derivatives, which activate BK(Ca) channels. Nevertheless, further studies are necessary to clearly elucidate residual endothelium-independent relaxation induced by diosgenin.     

白英不同药用部位不同生长期薯蓣皂苷元含量分布规律的研究

目的:探讨白英不同药用部位不同生长期薯蓣皂苷元的含量分布规律。方法:分别于5、6、7、8、9、10、11月份采集白英的根、茎、叶、果等药用部位作为样品,采用高效液相色谱法测定样品中薯蓣皂苷元的含量。色谱柱为Agilent ZorbaxODSC18(250mm×4.6mm,5μm),流动相为乙腈-水(93∶7,V/V),流速为1.0mL·min-1,柱温为30℃,检测波长为203nm。结果:薯蓣皂苷元的检测浓度在0.0525～1.0500mg·mL-1范围内与峰面积积分值呈良好的线性关系(r=0.9994);平均加样回收率为100.53%,RSD=1.62%(n=6)。白英根中薯蓣皂苷元的含量最高,平均为1.216mg·g-1,其次依次为果实、下部茎、叶、上部茎;白英根、叶中的薯蓣皂苷元含量8月份最高,上、下部茎含量9月份最高,果实含量10月份最高。结论:白英不同药用部位不同生长期薯蓣皂苷元的含量差别较大,以8、9月份采收质量较好。     

Effects of diosgenin on cell proliferation induced by IGF-1 in primary human thyrocytes

Others and our previous studies showed that the increase of IGF-1 was involved in the formation of goiter. Our aim here was to evaluate the possible effects of diosgenin on cell proliferation induced by IGF-1 in primary human thyroid cells. The cells were treated with or without different concentrations of diosgenin in the present or absent of IGF-1 for 24, 48 and 72 h, respectively. Cell viability was determined by MTT, and cell proliferation was tested by EdU assay, and cell cycle analysis was performed by FACS. In addition, Cyclin D1 and B1 protein expression was tested by Western Blotting, respectively. We found that IGF-1 promoted cell cycle progression to S phase and increased the primary human thyroid cells proliferation. Diosgenin decreased the protein expression of cyclin D1 and resulted in cell G(0)/G(1) arrest. Importantly, when the human thyrocytes were exposed to diosgenin in the present of IGF-1, the IGF-1 inducing proliferation was significantly decreased and the proportion of the cells in G(0)/G(1) phase was increased, while that of S phase was decreased. This study shows that diosgenin inhibited cell proliferation, caused G(0)/G(1) arrest, and could inhibit cell proliferation induced by IGF-1 in primary human thyroid cells.     

薯蓣皂苷元衍生物的抗肿瘤活性研究

目的研究薯蓣皂苷元衍生物在体外的抗肿瘤活性。方法采用MTT法对人恶性黑色素瘤细胞A375、人肺腺癌细胞A549、人肝癌细胞HepG-2及人慢性髓原白血病细胞株K562进行体外抗肿瘤活性试验。结果薯蓣皂苷元衍生物对4个肿瘤细胞株A375、A549、K562、HepG-2具有不同程度的抗肿瘤活性。结论绝大部分薯蓣皂苷元衍生物对4个肿瘤细胞株有较好的抗肿瘤活性,IC50值都低于30μmol.L-1。化合物22对细胞株A375的IC50=4.48μmol.L-1,化合物9、10对细胞株K562的IC50分别为2.51、2.38μmol.L-1;显示其抗肿瘤活性与对照化合物1-(3β-薯蓣皂苷元)-3-苄基咪唑溴盐相当。     

薯蓣皂苷元的制备及其抗甲亢活性研究

目的 考查薯蓣皂苷元对甲亢大鼠的活性。方法 穿山龙饮片用含1.5 mol·L^-1硫酸的75%乙醇水溶液在沸水浴中回流提取4.5 h,再经柱层析法分离、精制纯化得薯蓣皂苷元提取物,并进行结构表征。采用优甲乐灌胃法制作大鼠甲亢模型,并将大鼠随机分成正常对照组、甲亢模型组、甲巯咪唑治疗组、薯蓣皂苷元治疗组(低、中、高剂量),分别于给药21 d后测定大鼠血清中T₃、T₄及TSH值。结果 薯蓣皂苷元提取制备工艺正确适当,所得薯蓣皂苷元提取物经氢谱、碳谱、质谱和高效液相色谱表征确定为薯蓣皂苷元。与甲亢模型组比较,薯蓣皂苷元治疗组(低、中、高)血清中T₃、T₄和TSH值均有不同程度改善。结论 薯蓣皂苷元制备工艺合理可行,得率较高。薯蓣皂苷元可使甲亢大鼠的各项甲状腺功能血清值恢复正常,还可增加其体质量,功效与甲巯咪唑相似,值得进一步研究。