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。     

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.     

Effects of d-amphetamine injected into the nucleus accumbens on ethanol reinforced behavior

Rats, initiated to self-administer 10% (v/v) ethanol in an operant situation using the sucrose-fading procedure, received bilateral n. accumbens microinjections of d-amphetamine prior to operant sessions. Doses of 4 micrograms, 10 micrograms and 20 micrograms/brain were administered and some animals also received a 4 microgram/brain dose of LY171555. Three different effects were observed: increased, decreased and no change in total session responding. There was no clear relation between injection area in the n. accumbens and type of effect observed. For either an increase or decrease in total session responding, momentary response rates were decreased. Both d-amphetamine and LY171555 produced similar results. The data support the hypothesis that dopamine in the n. accumbens is involved with ethanol reinforced operant responding but in a complex manner.     

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.     

山芋干酒精废糟粗滤液全回流新工艺的研究

本文介绍了对山芋干酒精废糟进行粗滤,所得滤液全部回用于酒精生产的实验室研究结果。其方案之一是将粗滤液先培养丝状茵,再将二次过滤液回用;方案二是将粗滤液直接回流。经过十三到十五次的全回流表明,粗滤液全回流是可行的。另外,每100ml酒糟粗滤时可得到含干物质15%左右的湿滤渣约33g,其粗蛋白含量为17.5%(干基)。将粗滤液摇瓶培养根霉26号茵株10小时可得粗干茵体1.5—2.0g/100ml,其粗蛋白含量25%左右。     

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     

胃饲乙醇预处理诱导肝脏缺血耐受性的可行性探讨

目的探讨胃饲乙醇预处理对肝脏缺血再灌流损伤的影响,并初步评价其预处理的可行性。方法40%乙醇胃饲Wistar大鼠。分组:①大鼠36只,随机分6组:A组8g/kg、B组7g/kg、C组6g/kg、D组5g/kg、E组4g/kg、正常组0g/kg;以中毒症状及肝组织病理为指标,判定大鼠乙醇急性中毒剂量。②大鼠78只,随机分为4组:正常对照组(N)、单纯乙醇组(E)、单纯缺血组(ISCH)、胃饲乙醇预处理组(EPC);采用尾叶转流下的肝缺血模型,于再灌流3、6、12、24h留取标本。结果急性胃饲乙醇≤5g/kg预处理后,动物中毒症状轻,无死亡;乙醇预处理可以在一定程度上减轻肝脏90min的缺血再灌流损伤。结论适当剂量的乙醇胃饲预处理是一种安全的预处理措施,有望成为增强肝脏对缺血再灌流损伤耐受性的一种较好的预处理方式。     

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.