玳玳果黄酮降脂提取物体内组织分布规律及特征研究

目的：建立UPLC-MS/MS分析方法同时测定玳玳果黄酮降脂提取物效应组分新橙皮苷和柚皮苷在大鼠10种脏器组织中含量，分布规律及特征。方法：采用UPLC-MS/MS技术建立提取物效应组分新橙皮苷及柚皮苷在大鼠心、肝、脾、肺、肾、脑、胃、小肠、脂质、肌肉组织中的定量分析方法；大鼠给药后分别于0.33，0.67，1，4，8 h的5个时间点，分别摘取以上10种脏器组织，测定脏器组织及血液中效应组分的质量浓度，采用DAS（V 2.0）药动学软件对各样本的药物浓度-时间数据进行房室拟合，并计算不同组织效应组分的药-时曲线下面积（AUC）及平均滞留时间（MRT）。结果：所建立的UPLC-MS/MS定量分析方法具备良好的专属性、标准曲线及线性范围良好、方法准确度与精密度、定量下限均符合有关规定；玳玳果黄酮降脂提取物效应组分在血液中的分布符合一室模型，除肾脏及脑组织外，其余脏器中提取物效应组分的房室特征多为静脉注射的二室模型，柚皮苷在肾脏中的拟合结果为非静脉注射的二室模型，新橙皮苷在脑组织拟合结果为静脉注射的三室模型，给药后8 h各组织中效应组分新橙皮苷及柚皮苷AUC值大小顺序均为小肠 > 胃 > 肾 > 脂质 ≈ 脾脏 > 肺 > 肌肉 > 肝 > 心 > 脑，效应组分在各脏器中均无明显蓄积；效应组分在血液、肾脏、肝脏中的滞留时间较长，MRT均大于2 h，脂质最短，MRT不足1 h；各脏器中新橙皮苷的药-时曲线下面积约是柚皮苷的3倍，而心、肝、肾中则是3.5，2.1和3.4倍。结论：玳玳果黄酮降脂提取物效应组分在大鼠组织中分布迅速，达峰时间早于血液；效应组分在肠道内消除缓慢，给药8 h后在各脏器中的含量均显著下降且无特异的蓄积部位。研究结果揭示玳玳果黄酮降脂提取物效应组分在大鼠体内的分布特征及规律，为进一步理解玳玳果黄酮降脂提取物在体内的作用靶点及机制奠定了基础。     

桃红四物汤联合银杏酮酯滴丸治疗老年出血性玻璃体混浊的临床疗效研究

目的:探究桃红四物汤联合银杏酮酯滴丸治疗老年出血性玻璃体混浊的临床疗效。方法:收集2016年12月-2018年12月我院收治的老年出血性玻璃体混浊患者67例,共67眼,根据随机对照表分为对照组和试验组,其中试验组34例,对照组33例,对照组予以银杏酮酯滴丸;试验组在对照组的基础上联用桃红四物汤。两组均服用30 d。治疗结束后对比分析两组患者临床疗效、出血吸收时间、血液流变学及视网膜中央动脉血流动力学。结果:治疗后两组患者高切全血粘度、低切全血粘度、纤维蛋白原、阻力指数(Resistance Index,RI)低于治疗前,收缩期峰值速度(Peak Systolic Velocity,PSV)、舒张末期血流速度(End Diastolic Velocity,EDV)高于治疗前,差异具有统计学意义(P<0.05);治疗后试验组临床总有效率、PSV、EDV高于对照组,出血吸收时间、高切全血粘度、低切全血粘度、纤维蛋白原、RI低于对照组,差异具有统计学意义(P<0.05)。结论:桃红四物汤联合银杏酮酯滴丸治疗老年出血性玻璃体混浊临床疗效显著,适宜临床应用推广。     

Antiproliferative, cytotoxic and apoptogenic activity of Indian toad (Bufo melanostictus, Schneider) skin extract on U937 and K562 cells.

The antiproliferative, cytotoxic and apoptogenic activities of Bufo melanostictus (Indian common toad) skin extract (TSE) on U937 and K562 leukemic cell line has been investigated. TSE significantly (P<0.001) reduced the time-dependent cell proliferation and decreased MTT values in U937 and K562 cells. TSE (IC50 doses) suppressed the proliferating cell nuclear antigen expression in both the cells. It was demonstrated that, TSE (IC50 doses) primarily arrested the U937 and K562 cells at G1 phase of the cell cycle. Confocal microscopy showed the altered fragmented nuclei and apoptotic bodies formation in TSE (IC50 doses) treated U937 and K562 cells. Membrane blebbing, cell surface shrinkage and perforation were observed through scanning electron microscope. TSE-induced DNA fragmentation in U937 and K562 cells was reflected in single-cell gel electrophoresis. TSE significantly (P<0.001) increase the length-width ratio of DNA mass as compared to control in comet assay. The flow cytometric analysis of annexin-V binding to the cancer cells further supported the apoptotogenic activity of TSE. The effect of TSE on normal human peripheral blood mononuclear cells viability and cytotoxicity was studied in culture and found to be less cytotoxic than on the U937 and K562 cells. The findings from the present study suggested that TSE might possess potent antineoplastic agent having antiproliferative, cytotoxic and apoptogenic activity against U937 and K562 myeloid leukemic cells.     

银杏叶提取物联合脑蛋白水解物治疗脑梗塞68例

目的观察银杏叶提取物与脑蛋白联用治疗脑梗塞的疗效及对血液流变学指标的影响。方法132例脑梗塞患者随机分为治疗组及对照组。治疗组给舒血宁20 mL,脑蛋白注射液60 mg,1次/d静滴,连用14 d观察治疗前后疗效及血流变指标变化。结果与对照组比较治疗前后疗效及血流变指标均有显著改善。结论银杏叶提取物(舒血宁)合用脑蛋白注射液治疗脑梗塞,可降低血粘度,促进神经功能改善。     

Lipid extract from completely sporoderm‐broken germinating Ganoderma sinensis spores elicits potent antitumor immune responses in human macrophages

Ganoderma sinensis has been used widely in Oriental countries for the prevention and treatment of various diseases including cancer. Previous studies have shown that the lipid extract from Ganoderma exhibits direct cytotoxicity against tumor cells. Here, it is reported that the lipid extract from germinating G. sinensis spores, at lower concentrations that have no direct tumoricidal activity, induce potent antitumor immune responses in human monocytes/macrophages. Upon stimulation with the lipid extract, monocytes/macrophages exhibited markedly increased production of proinflammatory cytokines and surface expression of costimulatory molecules. Conditioned medium from stimulated cells effectively suppressed the growth of tumor cells. Apparently, the lipid extract triggered macrophage activation via a mechanism different from that associated with LPS. Moreover, it was observed that the lipid extract could partially re‐establish the antitumor activity of the immunosuppressive tumor‐associated macrophages. These results indicated that in addition to its direct tumoricidal activity, the lipid extract from G. sinensis spores could exert antitumor activity by stimulating the activation of human monocytes/macrophages. Copyright © 2008 John Wiley & Sons, Ltd.     

中药内外并用抗尖锐湿疣复发的临床研究

目的：观察中药消疣丸/消疣擦剂内服外用防止尖锐湿疣复发的作用.方法：应用免疫学方法，检测患者治疗前后外周血T淋巴细胞亚群CD3、CD4、CD8的百分率和CD4/CD8的比值.结果：局部消除疣体后中药消疣丸/消疣擦剂内服外用对防止尖锐湿疣复发有显著疗效，痊愈率为99.66%，复发率为3.33%，与对照组相比有显著差异（P〈0.05）.结论：中药内服外用抗尖锐湿疣复发效果好。     

葛根素治疗2型糖尿病周围神经病变53例疗效观察

目的　观察葛根素对糖尿病周围神经病变的临床疗效。方法　在治疗糖尿病的同时 ,用0 9%氯化钠注射液 30 0mL 葛根素 0 4g静脉滴注 ,每天 1次 ,10d为 1疗程 ,共 3个疗程。结果　用葛根素治疗糖尿病周围神经病变 5 3例 ,显效 31例 ,有效 12例 ,总有效率达 81% ,无明显副作用。结论　葛根素治疗糖尿病周围神经病变效果较好 ,副作用小 ,值得推广运用     

Seasonal variation in the content of a febrifugine and isofebrifugine alkaloid mixture in aerial parts of <Emphasis Type="Italic">Hydrangea macrophylla</Emphasis> var. <Emphasis Type="Italic">Otaksa</Emphasis>, with special reference to its antimalarial activity

Febrifugine and isofebrifugine alkaloid mixtures extracted from the leaves and buds of Hydrangea macrophylla var. Otaksa, collected during different months, in Japan, were quantified using high-performance liquid chromatography. Leaves collected during the flowering season, namely from June to August, contained 0.16–0.31 mg/g of the alkaloid mixture, whereas those collected from September to December had less than 0.03 mg/g of the mixture. However, extracts of buds harvested from October to February contained a consistently larger amount (more than 0.49 mg/g) of the alkaloids. Hot-water extracts from the leaves and buds collected during different seasons were evaluated for antimalarial activity against Plasmodium yoelii 17XL in mice. The extract of leaves collected in August demonstrated high antimalarial activity, and all mice that received the extract survived the infection. In contrast, the extract of leaves collected in December showed little activity. The extract of buds collected in December cleared parasites, but with subsequent mortality to mouse. The present results show that the amount of antimalarial agent—febrifugine and isofebrifugine mixture—in H. macrophylla var. Otaksa is both part- and season-dependent, suggesting that the choice of plant parts and their harvesting season are important factors worth considering in the pharmacological use of medicinal plants.     

Triterpenoid saponins, new metalloprotease snake venom inhibitors isolated from Pentaclethra macroloba.

We report here the antiproteolytic and antihemorrhagic properties of triterpenoid saponin inhibitors, named macrolobin-A and B, from Pentaclethra macroloba, against Bothrops snake venoms. The inhibitors were able to neutralize the hemorrhagic, fibrin(ogen)olytic, and proteolytic activities of class P-I and P-III metalloproteases isolated from B. neuwiedi and B. jararacussu venoms. Clotting and fibrinogenolytic activities induced by snake venoms and isolated thrombin-like enzymes were partially inhibited. Furthermore, the potential use of these inhibitors to complement antivenom therapy as an alternative treatment and/or used as molecular models for development of new therapeutical agents in the treatment of snake bite envenomations needs to be evaluated in future studies.