基于雷公藤和雷公藤多苷片提取物肝毒性检测的微流控肝器官芯片技术研究

目的 使用一种在微米尺度空间对流体进行操控,以模拟体内微环境为主要特征的微流控肝器官芯片技术,评价雷公藤提取物（Tripterygium wilfordii extract,TWE）和雷公藤多苷片提取物（Tripterygium Glycosides Tablet extract,TGE）的肝脏毒性,比较微流控-精密肝切片、静态-精密肝切片、微流控-HepaRG细胞培养体系的差异性。方法 将新鲜的大鼠肝脏进行精密切片处理后,分别置于静态/微流控培养体系中进行培养,微流控-HepaRG细胞培养体系则是将HepaRG细胞接种到已预先接种人脐静脉内皮细胞（human umbilical vein endothelial cells,HUVECs）的培养小室中加药培养;TWE终质量浓度为0.30、0.60、1.20 mg/mL（以生药量计）,TGE终质量浓度为31.25、62.50、125.00μg/mL,共孵育24 h后进行肝脏损伤标志物的测定及形态学观察。结果 在不额外添加药物的正常培养情况下,微流控/静态精密肝切片培养上清中丙氨酸氨基转移酶（alanine aminotransferas...     

不同产源雷公藤多苷对SD雄鼠生育力的影响

目的比较不同产源的雷公藤多苷对SD雄鼠生育力影响的差异性。方法 SD大鼠随机分为4组,给予不同产源的雷公藤多苷灌胃。8周后随机处死一半,取睾丸组织检测指标。化学发光法检测血清性激素,光镜观察睾丸组织形态学变化,免疫组织化学法检测睾丸雌激素β受体(ERβ)。剩余大鼠与雌鼠1∶1合笼2周,然后计算活产率、产仔率评价生育力。结果各组血清性激素比较无统计学意义。各组ERβ表达,空白组表达值最高,湖南组最低。组间差异比较,3组与空白组间差异均有统计学意义(P0.05,P0.01);江苏组与湖北组间差异没有统计学意义,湖南组与另外两组间差异有统计学意义(P0.05)。本实验计数产仔数,结果是空白组产仔最多,江苏组次之,湖南、湖北两组接近。组间比较发现,江苏组与空白组之间差异没有统计学意义,湖南、湖北两组与空白组间差异有统计学意义(P0.05);但是3组间比较差异没有统计学意义。产仔率结果显示,湖南组最低,该组中有3只雌鼠最终没有受孕。湖南组大鼠不仅产仔率低,并且同期合笼,其雌鼠最早分娩时间比其他组晚10d;其他3组分娩时间一致。各组均无畸形、死产。结论 3种不同产源的雷公藤多苷对雄性幼鼠的生育力影响存在差异性。     

Effects of α-Glucosylhesperidin,a Bioactive Food Material,on Collagen-Induced Arthritis in Mice and Rheumatoid Arthritis in Humans

Hesperidin (Hsp) is an abundant flavonoid in citrus fruits, and the oral administration of Hsp has been recently reported to suppress collagen-induced arthritis in mice. Therefore, we sought to determine whether α-glucosylhesperidin (Hsp-G), which is an Hsp derivative with enhanced water-solubility, is effective on treating arthritis in both mice and humans. Hsp-G was orally administered to mice with collagen-induced arthritis, and its effects were evaluated clinically and histologically. Oral administration of Hsp-G improved collagen-induced arthritis when administered before the onset of arthritis as well as when administered after its onset. A decrease in tumor necrosis factor-α production was found to cause this improvement. In the human study, 19 patients with rheumatoid arthritis (RA) were enrolled in a 12-week double-blind, placebo-controlled trial. Patients were administered beverages containing 3 g Hsp-G (n?=?9) or placebo (n?=?10) every morning for the duration of the 3-month trial. Additionally, patients received standard therapy from a physician every 4 weeks. As a result, 3 of 9 patients in the Hsp-G group improved, while only 1 of 10 patients in the placebo group improved; this was in accordance with the American College of Rheumatology criteria. The present study revealed that the food material Hsp-G was effective when administered with standard anti-rheumatoid therapy in ameliorating RA in mice and humans without any adverse effects and may improve the quality of life for patients with RA as a complementary/alternative medicine.     

Monoterpenoid derivatives from Paeonia delavayi

Three new monoterpene glycosides, 4- O -ethylpaeoniflorin ( 1 ), 6'- O -benzoyl-4"-hydroxy-3"-methoxy-paeoniflorin ( 2 ), 6'- O -benzoylalbiflorin ( 3 ), and a new monoterpenoid, 9-hydroxy-paeonilactone-A ( 4 ) were isolated from the root cortex of Paeonia delavayi . Their structures were elucidated on the basis of spectral methods.     

龙胆总裂环环烯醚萜苷质量标准研究

目的：建立总裂环环烯醚萜苷（龙胆）的质量标准.方法：采用TLC（薄层色谱）法对提取物中的龙胆进行了定性鉴别;用紫外分光光度法测定了有效部位总裂环环烯醚萜苷的含量;用高效液相色谱法测定了龙胆苦苷的含量.结果：在TLC图谱中可检出龙胆的特征斑点;龙胆苦苷在7.187～35.94μg/ml间线性关系良好,r=0.9992,平均回收率为96.8%,RSD=1.06%（紫外分光光度法）;龙胆苦苷在0.8488μg～4.244μg间线性关系良好,r=.9997,平均回收率为97.3%,RSD=0.7%（高效液相色谱法）.结论：所建立的方法可行、重现性好,能有效地控制提取物中龙胆总裂环环烯醚萜苷的质量.     

雷公藤多甙诱导类风湿关节炎滑膜细胞凋亡的研究

目的:评估抗风湿中药雷公藤多甙(TripterygiumGlycosides,TG)诱导滑膜细胞凋亡(Apo)在类风湿关节炎(RA)治疗中的作用,探讨其药理机制。方法:用光镜、电镜、共聚焦显微镜、流式细胞仪(FCM)及DNA凝胶电泳检测不同浓度TG诱导RA滑膜细胞凋亡情况。结果:TG组凋亡细胞百分率显著高于骨性关节炎(OA)组(P<0.01)和正常人组(P<0.01),TG组凋亡细胞百分率为(55±11.2)%。结论:TG可以诱导滑膜细胞凋亡,并且这可能是其治疗RA的机制之一。     

The reactivation of the proscillaridin-inhibited membrane ATPase by specific antibodies

Summary The action of proscillaridin (p.) on a partially purified Na⁺–K⁺-ATPase preparation was studied, using a linked optical enzyme assay. A half maximal ATPase inhibition was obtained with 6.3×10^–7 M p. Testing 5 additional glycosides and genins we observed a maximal suppression of the enzyme activity of up to 80%. Following the immunization of rabbits against a p.-human serum albumin complex, the antibody was shown to prevent and rapidly reverse the inhibition of the enzyme in a linear dose-dependent fashion.Supported by the Deutsche Forschungsgemeinschaft.     

Cardiac glycosides: Correlations among Na+, K+-ATPase,sodium pump and contractility in the guinea pig heart

Summary Relationships among positive inotropic response to cardiac glycosides, Na⁺,K⁺-ATPase inhibition and monovalent cation pump activities were studied using paced Langendorff preparations of guinea-pig heart. Na⁺,K⁺-ATPase activity was estimated from the initial velocity of (³H)-ouabain binding in ventricular homogenates, and cation pump activity from ouabain-sensitive ⁸⁶Rb uptake of ventricular slices. These parameters were assayed in control, ouabain- or digitoxintreated hearts either at the time of inotropic response to the cardiac glycosides or during the course of drug washout. Development and loss of the inotropic response during ouabain or digitoxin perfusion and washout was accompanied by reduction and subsequent recovery of the initial ouabain binding velocity, respectively. If homogenates from glycoside-treated hearts were incubated at 37°C for 10 min during ouabain-binding studies, the levels of binding were not different from those of control hearts, indicating a rapid dissociation of the glycosides from cardiac Na⁺,K⁺-ATPase in this species. Despite differences in the time course of the loss of inotropic responses produced by ouabain or digitoxin, the relationship between Na⁺,K⁺-ATPase inhibition and inotropic responses were similar. Inotropic responses to digitoxin during perfusion, and subsequent los during washout, also were accompanied by a reduction and subsequent recovery of ⁸⁶Rb uptake. A correlation between inhibition of cation pump activity and positive inotropy has hitherto not been demonstrated. Thus, it appears that with cardiac glycosides, a relationship exists among contractility, cardiac Na⁺,K⁺-ATPase and monovalent cation pump activities.     

Four glycosides from the leaves of Abeliophyllum distichum with inhibitory effects on angiotensin converting enzyme

The bioassay-guided fractionation of the n-BuOH extract of Abeliophyllum distichum afforded acteoside (1), isoacteoside (2), rutin (3), and hirsutrin (4). Compounds 1-3 moderately inhibited the angiotensin I converting enzyme activity in a dose-dependent manner. Compounds 1-3 showed the 50% inhibitory concentration values of 228 micro g/mL, 290 micro g/mL, and 278 micro g/mL, respectively.