白芍总苷对雷公藤多苷治疗狼疮性肾炎减毒增效作用的实验研究

目的 探讨白芍总苷(TGP)对雷公藤多苷(TG)治疗狼疮性肾炎(lupus nephritis,LN)小鼠的减毒增效作用.方法 取B6D2F1代杂交小鼠建立慢性移植物抗宿主病(cGVHD)LN小鼠模型,将成模小鼠随机分为3组,模型(LN)组、TG组、TG+TGP组,每组6只,另设正常对照组6只.TG组给予雷公藤多苷灌胃,剂量为30 mg·kg~(-1)·d~(-1);TG+TGP组给予雷公藤多苷及白芍总苷灌胃,剂量分别为30 mg·kg~(-1)·d~(-1)和200 mg·kg~(-1)·d~(-1),正常对照组和LN组分别给予等容量生理盐水灌胃,每日给药1次,各组给药方法及时间均相同,共计4周.实验结束时,观察并比较各组小鼠的24 h尿蛋白排泄率(UPE)、肝肾功能及肾脏病理改变.结果 与LN组相比,TG组、TG+TGP组小鼠的24 h UPE、尿素(BUN)、肌酐(SCr)显著降低(P＜0.05或P＜0.01),TG+TGP组显著低于TG组(P＜0.05或P＜0.01).与LN组相比,TG组小鼠的ALT、AST和MDA均显著增高(P＜0.01),SOD、GSH均显著降低(P＜0.05或P＜0.01).与TG组相比,TG+TGP组的ALT、AST、MDA均显著降低(P＜0.01),SOD、GSH均显著增高(P＜0.01).TG+TGP组对LN肾脏病理改变的改善作用显著优于TG组(P＜0.05或P＜0.01).结论 TGP对TG治疗LN具有减毒增效的作用.     

白芍总甙对大鼠腹腔巨噬细胞产生肿瘤坏死因子的调节机制

目的：研究不同浓度白芍总甙（ＴＧＰ）调节大鼠腹腔巨噬细胞（ＭΦ）产生肿瘤坏死因子（ＴＮＦ）作用。方法：在ＭΦ培养系统中有或无环氧酶抑制剂和钙调蛋白抑制剂等工具药，测定４５Ｃａ内流、ＰＧＥ２和ＴＮＦ含量。结果：ＴＧＰ（０．５～１０ｍｇ·Ｌ－１）明显促进ＬＰＳ诱导ＭΦ的４５Ｃａ内流和ＴＮＦ产生。线性回归分析表明，４５Ｃａ内流和ＴＮＦ产生呈明显正相关。三氟拉嗪（４０μｍｏｌ·Ｌ－１）可阻断ＴＧＰ促进ＬＰＳ诱导ＭΦ产生ＴＮＦ。ＴＧＰ－ＬＰＳ的ＴＮＦ释放曲线呈钟罩形，而ＴＧＰ－ＬＰＳ的ＰＧＥ２产生曲线呈浓度依赖性升高。当ＴＧＰ在低浓度（０．５～１２．５ｍｇ·Ｌ－１）时，ＴＮＦ与ＰＧＥ２产生明显正相关，而高浓度（１２．５～２５０ｍｇ·Ｌ－１）两者呈明显负相关。吲哚美辛（１０μｍｏｌ·Ｌ－１）可使ＴＮＦ量效曲线下降支消失，而Ｎω亚硝基－Ｌ－精氨酸（１５μｍｏｌ·Ｌ－１）对此无明显影响。结论：低浓度ＴＧＰ对ＴＮＦ产生上调作用可能与促进４５Ｃａ内流，提高钙调蛋白活性从而促进ＰＧＥ２分泌等有关，而高浓度下调作用是可能与ＭΦ自身产生大量ＰＧＥ２介导有关。     

Urinary β-1-galactosyl-0-hydroxylysine (GH) as a marker of collagen turnover of bone

Summary β-1-galactosyl-0-hydroxylysine (GH) was measured in the urine of 59 women and 48 men, aged 30–79 years, by High Performance Liquid Chromatography (HPLC) of the dansylated derivative. Vertebral mineral density, measured by quantitative computed tomography (QCT), and urinary GH were inversely correlated (r=−0.74;P<0.001). High rate of bone mineral loss is associated with a high urinary GH excretion. Measurement of GH in urine provides a simple and noninvasive method for the evaluation of the extent of bone resorption in large groups of subjects and appears to be more specific than urinary hydroxyproline excretion.     

北青龙衣细胞毒活性部位中的萘酚苷

目的研究北青龙衣细胞毒活性部位中的化学成分。方法利用MTT法测定北青龙衣醇提取物经大孔树脂柱色谱得到的4个组分对胃癌细胞BGC803的细胞毒作用,对其中活性最强的30%乙醇洗脱部位经硅胶柱色谱和反相硅胶柱色谱进行化学成分的分离。结果得到4个萘酚苷类化合物并经核磁共振谱确定了它们的结构,分别为1,4,5-三羟基萘-1,4-二-O-β-D-吡喃葡萄糖苷（1）,1,4,5-三羟基萘-1,5-二-O-β-D-吡喃葡萄糖苷（2）,1,4,8-三羟基萘-1-O-β-D-吡喃葡萄糖苷（3）,1,4,8-三羟基萘-1-O-β-D-[6＇-O-（3＇＇,4＇＇,5＇＇-三羟基苯甲酰）]吡喃葡萄糖苷（4）。结论北青龙衣细胞毒活性部位中含有萘酚苷类化合物,可能在其抗肿瘤活性中起重要作用。     

雷公藤多苷对白塞病患者免疫指标的调节作用观察

目的探讨雷公藤多苷对白塞病患者免疫指标的调节作用。方法对本院2009年2月至2012年6月收治的32例白塞病患者为研究对象,并选择30例健康者为对照组,比较两组患者的免疫指标变化情况。结果 32例患者的总有效率为87.5%。治疗组治疗前IL-4明显低于对照组,IL-6、IL-8明显高于对照组;而治疗组治疗后IL-4明显高于治疗前,IL-6、IL-8明显低于治疗前,差异有统计学意义(P<0.05);治疗组32例患者治疗后血沉、C反应蛋白明显降低,差异有统计学意义(P<0.05)。结论雷公藤多苷治疗白塞病疗效较佳,且可明显改善患者的免疫功能。     

Phenolic acid glucosides from the seeds of Entada phaseoloides Merill

Phytochemical investigation of the defatted seeds of Entada phaseoloides Merill. (Mimosaceae) led to the isolation of three new phenolic acid glucosides, which were characterized as 2-hydroxy-5-methylbenzoyl-β-l-glucopyranoside (p-cresotyl glucoside, 1), 2-hydroxy-5-methylbenzoyl-β-l-glucopyranosyl (2 → 1)-β-l-glucopyranosyl (2 → 1)-β-l-glucopyranoside (p-cresotyl triglucoside, 2), and 2-hydroxybenzoyl-β-l-glucopyranosyl (2 → 1)-β-l-glucopyranosyl (2 → 1)-β-l-glucopyranosyl (2 → 1)-β-l-glucopyranoside (salicylic acid tetraglucoside, 5), along with sucrose and triglucoside. The structures of these phytoconstituents have been established on the basis of spectral data analysis and chemical reactions.     

Antioxidant phenolic glucosides from Gentiana piasezkii

An extract of Gentiana piasezkii afforded a new arbutin derivative 6′-O-vanilloylarbutin (1) and a new flavone-C-glucoside 7-O-feruloylorientin (2), together with four known flavonoids lutonarin (3), saponarin (4), isoorient (5) and luteolin (6). Their structures were established based on spectroscopic methods including 2D NMR (COSY and gHMBC) techniques. Compounds 1, 2, 5 and 6 were evaluated for the antioxidant activity in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay system.     

Clemochinenosides C and D,two new macrocyclic glucosides from Clematis chinensis

Abstract

The EtOH extract of the roots and rhizomes of Clematis chinensis afforded two new macrocyclic glucosides clemochinenosides C (1) and D (2). Their structures were elucidated on the basis of spectroscopic means and hydrolysis products. These compounds were evaluated for inhibitory activity against lipopolysaccharides-induced TNF-α production in RAW 246.7 macrophages. Compounds 1 and 2 showed moderate inhibitory activity with IC₅₀ values of 12.9 ± 2.3 and 18.4 ± 2.7 μM, respectively. In addition, a proliferation study was used to evaluate the anti-angiogenic effects of these compounds in vitro (VEGF-induced human umbilical vein endothelial cell proliferation). Compounds 1 and 2 displayed weak inhibitory effects with inhibition rates of 26.3 ± 1.8 and 19.2 ± 2.6% at 50 μM, respectively.     

Water-soluble constituents from the leaves of Ilex oblonga

Four new water-soluble constituents, oblongaroside A (1), oblongar ester A (2), oblongaroside B (3), and oblongaroside C (4), were isolated along with four known compounds: 4-O-β-d-glucopyranosyl-3-hydroxybenzalcohol (5), 7-methoxyl-4-O-β-d-glucopyranosyl-3-hydroxybenzalcohol (6), 4-O-β-d-glucopyranosyl-3-hydroxybenzoic acid (7), and 3,4-dihydroxybenzoic acid (8) from the leaves of Ilex oblonga. Identification of their structures was achieved by 1D and 2D NMR experiments, including ¹H–¹H COSY, NOESY, HMQC, and HMBC methods and FAB mass spectral data.     

胡黄连总苷的高效液相色谱特征图谱研究

目的 采用高效液相色谱法建立胡黄连总苷的特征图谱。方法 Luna C18色谱柱（250 mm×4.6 mm,5 μm）,流动相为乙腈–0.5%冰醋酸水溶液（15.5∶84.5）,体积流量为1.0 mL/min,柱温为35 ℃,检测波长为275 nm,进样量为10 μL。结果 建立了胡黄连总苷的特征图谱及其技术参数,即供试品特征图谱中应有11个特征峰,参照物峰相应的峰为S峰,计算各特征峰与S峰的相对保留时间,其相对保留时间应在规定值的±5%之内。采用国家药典委员会《中药色谱指纹图谱相似度评价系2004A版》自动处理,10批胡黄连总苷的相似度均大于0.998。结论 本方法操作简便,准确可靠,可用于控制胡黄连总苷的内在质量。