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31.
复方必清片的提取工艺优选   总被引:1,自引:0,他引:1  
目的: 优选复方必清片的提取工艺。 方法: 在单因素试验基础上,以薯蓣皂苷元、秋水仙碱含量和浸膏得率的综合评分为指标,通过正交试验优选菝葜等7味药材的乙醇提取工艺;以总多酚含量和浸膏得率为综合评价指标,通过正交试验优选余甘子等5味药材的水提取工艺。采用HPLC测定薯蓣皂苷元和秋水仙碱的含量,色谱条件为Cosmosil C18色谱柱(4.6 mm×250 mm,5 μm),柱温35 ℃,流速1.0 mL·min-1,进样量10 μL,检测波长分别为203,350 nm,流动相分别为甲醇-水(90:10),甲醇-水(37:63);采用紫外分光光度法测定总多酚含量。 结果: 菝葜等7味药材的最佳提取工艺为加10倍量70%乙醇提取2次,每次1.0 h;余甘子等5味药材的最佳提取工艺为加10倍量水提取3次,每次1.0 h。 结论: 优选的提取工艺稳定可行,为复方必清片的质量控制提供实验依据。  相似文献   
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目的 研究秋水仙素(Ce)和秋水仙碱(Cd)对人外周血淋巴细胞有丝分裂效应的影响。方法 应用外周血淋巴细胞培养法,分析有丝分裂指数(MI)和C-有丝分裂效应。结果 Ce和Cd的MI与相应对照组相比,差异有显著性(P〈0.01),C-有丝分裂效应Ce和Cd处理组与相应对照组之间差异亦有显著性(P〈0.01)。MI和C-有丝分裂效应,Cd的作用均较Ce强。并对C-有丝分裂效应与非整倍体诱导活性之间的关  相似文献   
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INTRODUCTION  Tumorinvasionisclearlyanactiveprocessundergoingthreestages:attach-ment,migrationandmetastasis〔1〕.Infacts,tumorinvasioncouldbeconsideredady-namicadhesiveprocess,whichcontainedmuchcomplexandsubtlephysiologicalandbiochemicalinteractionsbetw…  相似文献   
35.
In this review, an attempt has been made to throw light on the mechanism of action of colchicine and its different analogs as anti-cancer agents. Colchicine interacts with tubulin and perturbs the assembly dynamics of microtubules. Though its use has been limited because of its toxicity, colchicine can still be used as a lead compound for the generation of potent anti-cancer drugs. Colchicine binds to tubulin in a poorly reversible manner with high activation energy. The binding interaction is favored entropically. In contrast, binding of its simple analogs AC or DAAC is enthalpically favored and commences with comparatively low activation energy. Colchicine-tubulin interaction, which is normally pH dependent, has been found to be independent of pH in the presence of microtubule-associated proteins, salts or upon cleavage of carboxy termini of tubulin. Biphasic kinetics of colchicines-tubulin interaction has been explained in light of the variation in the residues around the drug-binding site on beta-tubulin. Using the crystal structure of the tubulin-DAMAcolchicine complex, a detailed discussion on the pharmacophore concept that explains the variation of affinity for different colchicine site inhibitors (CSI) has been discussed.  相似文献   
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1 Background

The aim of the study was to investigate the effects of colchicine on cytokine production, apoptosis, alveolar bone loss, and oxidative stress in an experimental model of periodontitis in rats.

2 Methods

Forty‐eight rats were divided equally into four groups: healthy (H); periodontitis (P); periodontitis+colchicine low dose (CL, 30 μg/kg/day), and periodontitis+colchicine high dose (CH, 100 μg/kg/day). After 11 days, interleukin (IL) ‐1β, IL‐8, and IL‐10 were analyzed in gingival samples using Enzyme‐Linked ImmunoSorbent Assay. Receptor activator of nuclear factor kappa‐B ligand (RANKL), osteoprotegerin (OPG), total oxidative stress (TOS), total antioxidant status (TAS), and oxidative stress index (OSI) were measured in gingiva and serum. Alveolar bone volume was evaluated via micro‐CT. Apoptotic cells were detected by terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay in histological sections.

3 Results

Colchicine treatment significantly reduced IL‐1β, IL‐8, RANKL, RANKL/OPG, TOS, OSI, and bone volume ratio levels, and increased TAS levels compared to group P (p < 0.05). High dose colchicine treatment (CH) significantly decreased TUNEL+ cell counts compared to group P (p < 0.05).

4 Conclusions

These finding suggest that colchicine has a prophylactic potential for the prevention of periodontal tissue destruction through anti‐inflammatory, anti‐oxidative, anti‐apoptotic, and bone‐protective effects.  相似文献   
40.

Objectives

The authors sought to evaluate the plaque-modifying effects of low-dose colchicine therapy plus optimal medical therapy (OMT) in patients post-acute coronary syndrome (ACS), as assessed by coronary computed tomography angiography (coronary CTA).

Background

Colchicine therapy has been postulated to have beneficial anti-inflammatory effects in patients with ACS, translating into reduction in future adverse cardiovascular events. However, whether favorable plaque modification underpins this is yet unproven.

Methods

In this prospective nonrandomized observational study of 80 patients with recent ACS (<1 month), patients received either 0.5 mg/day colchicine plus OMT or OMT alone and were followed for 1 year. Our primary outcome was change in low attenuation plaque volume (LAPV), a marker of plaque instability on coronary CTA and robust predictor of adverse cardiovascular events. Secondary outcomes were changes in other coronary CTA measures and in high-sensitivity C-reactive protein (hsCRP).

Results

Mean duration of follow-up was 12.6 months; mean age was 57.4 years. Colchicine therapy significantly reduced LAPV (mean 15.9 mm3 [?40.9%] vs. 6.6 mm3 [?17.0%]; p = 0.008) and hsCRP (mean 1.10 mg/l [?37.3%] vs. 0.38 mg/l [?14.6%]; p < 0.001) versus controls. Reductions in total atheroma volume (mean 42.3 mm3 vs. 26.4 mm3; p = 0.28) and low-density lipoprotein levels (mean 0.44 mmol/l vs. 0.49 mmol/l; p = 0.21) were comparable in both groups. With multivariate linear regression, colchicine therapy remained significantly associated with greater reduction in LAPV (p = 0.039) and hsCRP (p = 0.004). There was also a significant linear association (p < 0.001) and strong positive correlation (r = 0.578) between change in LAPV and hsCRP.

Conclusions

Our findings suggest, for the first time, that low-dose colchicine therapy favorably modifies coronary plaque, independent of high-dose statin intensification therapy and substantial low-density lipoprotein reduction. The improvements in plaque morphology are likely driven by the anti-inflammatory properties of colchicine, as demonstrated by reductions in hsCRP, rather than changes in lipoproteins. Colchicine may be beneficial as an additional secondary prevention agent in patients post-ACS if validated in future studies.  相似文献   
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