绞股蓝对体外培养肾小管细胞庆大霉素毒性的保护作用

目的:研究绞股蓝(GP)对庆大霉素(GM)引起的近端肾小管细胞(PTC)毒性的保护作用。方法:采用原代培养的 PTC 制作 GM 损伤模型,观察丙氨酸氨基转移酶(ALT)、乳酸脱氢酶(LDH)、N-乙酰-β-氨基葡萄糖酶(NAG)、过氧化氢酶(catalase)、DNA 合成以及形态学变化,同时观察 GP 的保护作用。结果:GP 能激活并保护 ALT、LDH、Catalase 酶活力,降低 NAG酶活力增高、促进 DNA 合成等机制,减轻 GM 的肾毒性损伤。结论:GP 能有效保护 GM 对PTC 损伤。     

人参属植物高温蒸制前后人参皂苷含量的变化和细胞毒活性研究

目的研究人参属植物人参Panax ginseng、三七P. notoginseng和西洋参P. quinquefolium高温蒸制前后主要人参皂苷的含量变化,并测定高温蒸制前后样品对4株肿瘤癌细胞的细胞毒活性。方法采用HPLC建立了测定22种皂苷含量的分析方法,测定这些皂苷在人参属植物及其高温蒸制品中的含量。用MTT法测定人参属植物及其高温蒸制品对4株人类癌细胞(人类骨髓癌HL-60细胞、肝癌SMMC-7721细胞、肺癌A-549细胞、乳腺癌SK-BR-3细胞)的细胞毒活性。结果从人参、三七和西洋参及高温蒸制后的样品中鉴定出22个皂苷,包括人参皂苷Rg1、Re、Rb1、Rc、Rb2、Rd、Rk3、Rh4、Rk1、Rg5、Rb3、Rh3、Rk2,20(S)-人参皂苷Rh1、20(R)-人参皂苷Rh1、三七皂苷Fc、三七皂苷R1、绞股蓝皂苷IX、20(S/R)-三七皂苷Ft1、20(S/R)-人参皂苷Rg3、人参皂苷Rs3、人参皂苷Rh2。人参皂苷Rg1、Re、Rb1、Rc、Rb2和Rd为人参的主要成分;人参皂苷Rg1、Re、Rb1和Rd为西洋参的主要成分;人参皂苷Rg1、Re、Rb1、Rd和三七皂苷R1为三七的主要成分,高温蒸制后这3种植物的主要成分全部转化为人参皂苷Rk3、Rh4、Rk1、Rg5和20(S/R)-人参皂苷Rg3,在高温蒸制后的三七中还检测到20(S)-人参皂苷Rh1和20(R)-人参皂苷Rh1。三七皂苷Fc、人参皂苷Rb3和绞股蓝皂苷IX为三七茎叶的主要成分,高温蒸制后转化为另外8个主要成分20(S/R)-三七皂苷Ft1,20(S/R)-人参皂苷Rg3、Rs3、Rk1、Rg5,20(S/R)-人参皂苷Rh2、Rh3和Rk2。细胞毒活性结果显示,高温蒸制三七的细胞毒活性比高温蒸制人参和高温蒸制西洋参强,高温蒸制三七的细胞毒活性比三七的活性强,说明高温蒸制后三七的细胞毒活性增强。结论人参、西洋参和三七经过高温蒸制后原来的主要成分基本消失,随之转化为其他主要成分,高温蒸制三七的细胞毒活性最强。     

绞股蓝总皂甙对氧化修饰低密度脂蛋白损伤小牛主动脉内皮细胞的防治作用

目的 :探讨绞股蓝总皂甙 (GYP)对氧化修饰低密度脂蛋白 (oxidativelymodifiedlowdensitylipopro tein ,oxLDL)损伤小牛主动脉内皮细胞的防治作用及可能机制。方法 :在体外培养的小牛主动脉内皮细胞 (bovineaorticendothelialcell ,BAEC )中加入oxLDL(终浓度为 0 .1gpr·L- 1)及GYP低、中、高剂量组 (5 .0 ,10 .0 ,2 0 .0mg·L- 1) ,培养 2 4h后 ,采用细胞毒试验、丙二醛 (MDA)测定及细胞计数等方法 ,分别对其贴壁细胞及培养液进行检测。结果 :①细胞毒试验发现 ,oxLDL对BAEC的生长增殖有明显的抑制作用 (2 0 .6 3% ) ,GYP组 (10 .0 ,2 0 .0mg·L- 1)为9.14 %和 6 .5 6 % (P <0 .0 1) ;②加oxLDL组和GYP组BAEC粘附的HL6 0细胞数明显多于对照组 (P <0 .0 1) ;③MDA检测发现oxLDL促进BAEC脂质过氧化物生成 ,并高于GYP组和对照组 (P <0 .0 1)。结论 :绞股蓝总皂甙具有对氧化修饰低密度脂蛋白损伤小牛主动脉内皮细胞的防治作用。     

绞股蓝总皂甙对慢性肾功能不全大鼠血浆内皮素含量和肾功能的影响

目的：研究绞股蓝总皂甙（ＧＰ）对慢性肾功能不全（ＣＲＩ）大鼠血浆内皮素（ＥＴ）含量和肾功能的影响。方法：用腺嘌呤灌胃建立大鼠ＣＲＩ模型，并用ＧＰ进行防治，以放射免疫法测定血浆ＥＴ含量，常规方法测定血尿素氮、血肌酐和血红蛋白（Ｈｂ）含量。结果：ＧＰ加ＣＲＩ组大鼠肾功能明显改善，Ｈｂ明显升高，ＥＴ含量明显降低；与ＣＲＩ组大鼠比较，各项指标均有显著性差异（Ｐ＜０．０１或Ｐ＜０．０５）。结论：ＧＰ对ＣＲＩ大鼠有明显的ＥＴ拮抗作用和改善肾功能作用。     

Gypenoside XLIX, a naturally occurring gynosaponin, PPAR-alpha dependently inhibits LPS-induced tissue factor expression and activity in human THP-1 monocytic cells

Tissue factor (TF) is involved not only in the progression of atherosclerosis and other cardiovascular diseases, but is also associated with tumor growth, metastasis, and angiogenesis and hence may be an attractive target for directed cancer therapeutics. Gynostemma pentaphyllum (GP) is widely used in the treatment of various cardiovascular diseases including atherosclerosis, as well as cancers. Gypenoside (Gyp) XLIX, a dammarane-type glycoside, is one of the prominent components in GP. We have recently reported Gyp XLIX to be a potent peroxisome proliferator-activated receptor (PPAR)-alpha activator. Here we demonstrate that Gyp XLIX (0-300 microM) concentration dependently inhibited TF promoter activity after induction by the inflammatory stimulus lipopolysaccharide (LPS) in human monocytic THP-1 cells transfected with promoter reporter constructs pTF-LUC. Furthermore, Gyp XLIX inhibited LPS-induced TF mRNA and protein overexpression in THP-1 monocyte cells. Its inhibition of LPS-induced TF hyperactivity was further confirmed by chromogenic enzyme activity assay. The activities of Gyp XLIX reported in this study were similar to those of Wy-14643, a potent synthetic PPAR-alpha activator. Furthermore, the Gyp XLIX-induced inhibitory effect on TF luciferase activity was completely abolished in the presence of the PPAR-alpha selective antagonist MK-886. The present findings suggest that Gyp XLIX inhibits LPS-induced TF overexpression and enhancement of its activity in human THP-1 monocytic cells via PPAR-alpha-dependent pathways. The data provide new insights into the basis of the use of the traditional Chinese herbal medicine G. pentaphyllum for the treatment of cardiovascular and inflammatory diseases, as well as cancers.     

Analysis of the Inhibitory Effect of Gypenoside on Na~ , K~ -ATPase in Rats' Heart and Brain and Its Kinetics

Objective:To study the effects of gypenoside(Gyp) on the activity of microsomal Na ,K -ATPase in rat's heart and brain in vitro.Methods:The microsomal Na ,K -ATPase was prepared from rat's heart and brain by differential centrifugation.The activity of microsomal Na ,K -ATPase was assayed by colorimetric technique.Enzyme kinetic analysis method was used to analyze the effect of Gyp on the microsomal Na ,K -ATPase of rats.Results:Gyp reversibly inhibited the brain and heart's microsomal Na ,K -ATPase in a concentration-dependent manner,and showed a more potent effect on enzyme in the brain.The IC50 of Gyp for the heart and brain were 58.79±8.05 mg/L and 52.07± 6.25 mg/L,respectively.The inhibition was enhanced by lowering the Na ,or K concentrations or increasing the ATP concentration.Enzyme kinetic studies indicated that the inhibitory effect of Gyp on the enzyme is like that of competitive antagonist of Na ,the counter-competitive inhibitor for the substrate ATP,and the mixed-type inhibitor for K .Conclusion:Gyp displays its cardiotonic and central inhibitory effects by way of inhibiting heart and brain's microsomal Na ,K -ATPase activities in rats.     

A New Triterpene Saponin from Gynostemma pentaphyllum

Objective To study the triterpene saponins from Gynostemma pentaphyllum with antitumor activities. Methods The 75% EtOH extract of G. pentaphyllum was used for isolation by silica gel column chromatography and preparative HPLC. The structures of pure compounds isolated were identified by the spectral analysis and chemical evidence. Results Two compounds were isolated and identified as 23(S)-3β,20ξ,21ξ-trihydroxy-19-oxo-21,23-epoxydammar-24-ene 3-O-α-L-rhamnopyranosyl (1→2)-[β-D-xylopyranosyl (1→3)]-β-D-arab...     

中药皂苷类化合物生物转化研究进展

皂苷广泛存在于药用植物中,按母核结构可分为三萜和甾体皂苷,具有多种药理活性。众多研究发现皂苷中糖基部分的组成与其药理活性密切相关,改变皂苷分子中的糖基数量和结构能改变皂苷的药理活性及其生物利用度,为开发药物提供更多的化合物资源。相较于传统的化学方法,皂苷生物转化修饰糖基部分具有选择性高、成本低、污染小等优点,被广泛用于次级皂苷与皂苷元的制备。通过对皂苷脱糖基转化生成较高生物活性的次级皂苷与苷元的研究进展进行综述,为皂苷类化合物生物转化研究提供思路和方法。     

绞股蓝总皂苷对大鼠局灶性脑缺血再灌注损伤的保护作用

目的 观察绞股蓝总皂苷对大鼠急性局灶性脑缺血再灌损伤NO的保护作用。方法 采用大脑中动脉内栓线阻断不（MCAO）造成大鼠局灶性脑缺血再灌注模型，测定脑亚细胞器内NO含量的变化并观察病理组织学变化。脑缺血再灌注后脑亚细胞器内NO含量显著升高，海马CA1区存活的锥体细胞数显著降低。绞股蓝总皂苷能显著降低脑亚细胞器内NO含量，升高海马CA1区存活的锥体细胞数。结论 论股蓝总皂苷通过降低NO的毒性，发挥保护脑组织，减轻缺血再灌注损伤。     

HPLC测定绞股蓝中七叶胆苷XLVI和人参皂苷Rb3含量

目的 建立HPLC测定绞股蓝中七叶胆苷XLVI和人参皂苷Rb₃含量的方法。方法 采用Ultimate XB-C₁₈色谱柱（250 mm×4.6 mm，5 μm），以乙腈（A）-水（B）线性梯度洗脱，检测波长203 nm，流速1 mL·min^-1，柱温30℃。结果 七叶胆苷XLVI在3.30~39.62 μg·mL^-1范围内线性良好（r²=0.999 7），平均回收率为113%，RSD为1.84%；人参皂苷Rb₃在3.27~39.26 μg·mL^-1范围内线性良好（r²=0.999 7），平均回收率为102%，RSD为2.82%。结论 该方法有较好的分离效果，准确性、精密度和重复性良好，为绞股蓝的研究和质量控制提供了科学依据。