加压溶剂法提取雷公藤多苷及其条件优化

目的:对卫矛科药用植物雷公藤提取方法进行研究。方法:利用加压溶剂提取方法进行提取分离,根据理化性质用显色-比色法进行定量分析,并在单因素试验基础上,根据中心组合试验设计原理采用3因素3水平的响应面分析法进行工艺优化。结果:经过响应面分析法得出优化的工艺条件为料液比1∶9.5,提取温度115℃,提取时间80 m in,在此条件下雷公藤多苷的浸膏得率可达0.21%,纯度为0.52%。结论:加压溶剂提取方法与常规提取法相比优势明显,是一种有效的提取分离方法。     

昆明山海棠碱诱导Jurkat淋巴瘤细胞核DNA链断裂和DNA片段化

目的 探讨昆明山海棠碱对淋巴瘤细胞核DNA的影响，以了解THH碱诱导细胞凋亡的机制。方法 THH碱诱导Jurkat细胞后，TUNEL荧光标记DNA链断裂，细胞DNA含量分析方法分析DNA片段化，均以流式细胞术检测。结果 THH碱能诱导Jurkat淋巴瘤细胞DNA链断裂，之后DNA发生片段化。结论 提示在THH碱诱导Jurkat凋亡过程中，核DNA发生重要变化。     

东北雷公藤对胶原诱导实验性关节炎抑制作用的免疫学研究 Ⅲ。雷公藤给药对模型动物一般免疫功能状态的影响

东北雷公藤给药对关节炎模型动物一般免疫功能状态的影响与在正常动物给药时所观察到的结果相似。给药能降低模型动物血清IgC的浓度;抑制ConA诱导的大鼠血单个核细胞体外增殖反应,抑制血单个核细胞产生IL-2的活性。但对LPS诱导的大鼠血单个核细胞体外增殖反应无明显抑制作用,这点与氢化考地松给药的效果不同。     

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.     

Comparative observation on the effects of Radix Tripterygium hypoglaucum tablet and Tripterygium glycosides tablet in treating erosive oral lichen planus

From2002to2003,94patientswitherosiveorallichenplanus(EOLP)weretreatedbydivid ingthemintotwogroups,receivingRadixTripterygiumhypoglaucumtablet(THT)or Tripterygiumglycosidestablet(TGT),respec tively.Theresultswerereportedasfollows. METHODS ClinicalMaterialsForacceptanceintothestudy,enrolledpa tientswerediagnosedwithEOLP,accordingtothediagnosticstandardissuedinthe Periodontal Diseases"(1)andconfirmedbypathologicalexami nation.Patientswerealsoexcludediftheyhadre ceivedpriorsystematic…     

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.     

雷公藤多苷致雌性小鼠肾虚生殖功能低下动物模型的研究

目的探讨雷公藤多苷(GTW)致育龄期雌性小鼠生殖功能低下的药理作用机理,建立GTW致雌性小鼠生殖功能低下的动物模型。方法采用7～8周龄雌性性成熟昆明种小鼠,随机分为GTWA(60mg·kg-1·d-1)、B(40mg·kg-1·d-1)、C(30mg·kg-1·d-1)、D(20mg·kg-1·d-1)、E(15mg·kg-1·d-1)5组及正常对照组。观察给药后小鼠动情周期,分别在部分小鼠周期延长,周期均延长、不规则,周期完全紊乱、甚至消失等3个时段分批处死小鼠,考察GTW在不同时段对小鼠生殖功能的影响。采用放免法检测血清E2、P水平,计算卵巢、子宫指数,卵巢、子宫作组织形态学观察,计数各级卵泡、黄体数,测量子宫内膜、肌层厚度。结果给药10周时,A、B、C组子宫指数明显降低,子宫内膜、肌层变薄,卵巢成熟卵泡数及黄体数减少;A、B组E2水平降低,各组P水平及卵巢指数无明显变化。结论GTW连续给药10周,可损伤雌性小鼠生殖功能,造成肾虚生殖功能低下状态。建议GTW40mg·kg-1·d-1给药10周建立雌性小鼠肾虚生殖功能低下模型。     

雷公藤中具有抗癌活性的二萜类化合物

目的研究雷公藤的化学成分及其细胞毒活性。方法用硅胶柱色谱、凝胶柱色谱分离,制备高效液相色谱纯化,得到单体化合物,用各种有机波谱鉴定化合物结构;以MTT法测试各化合物的抗癌活性。结果分离得到5个萜类化合物,鉴定为雷酚萜L(3-epi-triptobenzeneB,Ⅰ)、雷酚萜B(3β,14-dihydroxy-abieta-8,11,13-triene,triptobenzeneB,Ⅱ)、雷酚萜E(wilforolE,Ⅲ)、雷酚萜酸(triptohairicacid,Ⅳ)、雷酚萜酸甲醚[11-hydroxy-14-methoxy-18(4→3)-abeo-abietan-3,8,11,13-tetraen-18-oic-acid,hypoglicacid,Ⅴ]。结论化合物Ⅰ为新化合物,命名为雷酚萜L(triptobenzeneL),化合物Ⅳ为首次分离得到。细胞毒实验表明各化合物均有一定的抗癌活性。     

Treatment of pyoderma gangrenosum with oral Tripterygium wilfordii multiglycoside

Two patients with refractory pyoderma gangrenosum (PG) were treated with oral Tripterygium wilfordii multiglycoside (TWG). TWG is a Chinese medicine extracted from a medicinal herb, Tripterygium wilfordii Hook F, and has potent anti-inflammatory and immunosuppressive effects. The effect of TWG on PG was demonstrated by clinical findings. Improvement of the lesions occurred within two weeks, and the ulcers healed about a month. Mild side effects such as gastrointestinal disturbances were observed in both patients. These side effects were patient-acceptable, and there was no need to stop the treatment. Transient elevation of serum ALT was observed in one patient; the serum ALT returned completely to normal after the discontinuation of TWG. These results suggest that TWG may be an effective alternative for refractory PG and that careful monitoring of liver function during TWG treatment is necessary.