Evaluation of free radical scavenging and antityrosinase activities of standardized longan fruit extract.

The protective effects of fruits and vegetables against chronic diseases have been attributed to the antioxidant properties of some secondary metabolites present in these foods. Plant polyphenols have been reported to exhibit bioactive properties, and in particular antioxidant activities. Longan seeds are found to contain high levels of some beneficial polyphenolic compounds such as corilagin, gallic acid and ellagic acid. The present study examined the free radical scavenging activity of longan seed extract by using three different assay methods. Longan extracts contained corilagin ranging from zero to 50.64 mg/g DW, gallic acid from 9.18 to 23.04 mg/g DW, and ellagic acid from 8.13 to 12.65 mg/g DW depending on the cultivars. Dried longan seed extracts of cultivar Edor contained high levels of gallic acid and ellagic acid and also exhibited the highest radical scavenging activities when comparing fresh seed and dried pulp extracts. For scavenging activity of DPPH and superoxide radicals, longan seed extract was found to be as effective as Japanese green tea extract while dried longan pulp and mulberry green tea extracts showed the least scavenging activities. In the ORAC assay, both fresh and dried longan seed also had higher activity than dried pulp and whole fruit. However, the results demonstrate that three polyphenolics may not be the major contributors of the high antioxidant activity of longan water extracts but this high activity may be due to other phenolic/flavonoid glycosides and ellagitannins present in longan fruit. In addition, longan seed also showed tyrosinase inhibitory activity with IC(50) values of 2.9-3.2 mg/ml. Therefore, the preliminary observations suggest that longan seed extract could be another potential source of potent natural dietary antioxidants and also in an application as a new natural skin-whitening agent.     

Transcriptional up-regulation of SOD1 by CEBPD: A potential target for cisplatin resistant human urothelial carcinoma cells

Bladder cancer is the fourth most common type of cancer in men (ninth in women) in the United States. Cisplatin is an effective agent against the most common subtype, urothelial carcinoma. However, the development of chemotherapy resistance is a severe clinical problem for the successful treatment of this and other cancers. A better understanding of the cellular and molecular events in response to cisplatin treatment and the development of resistance are critical to improve the therapeutic options for patients. Here, we report that expression of the CCAAT/enhancer binding protein delta (CEBPD, C/EBPδ, NF-IL6β) is induced by cisplatin in the human bladder urothelial carcinoma NTUB1 cell line and is specifically elevated in a cisplatin resistant subline. Expression of CEBPD reduced cisplatin-induced reactive oxygen species (ROS) and apoptosis in NTUB1 cells by inducing the expression of Cu/Zn-superoxide dismutase (SOD1) via direct promoter transactivation. Several reports have implicated CEBPD as a tumor suppressor gene. This study reveals a novel role for CEBPD in conferring drug resistance, suggesting that it can also be pro-oncogenic. Furthermore, our data suggest that SOD inhibitors, which are already used as anti-angiogenic agents, may be suitable for combinatorial chemotherapy to prevent or treat cisplatin resistance in bladder and possibly other cancers.     

HPLC测定注射用复方三维B中盐酸呋喃硫胺、盐酸吡多胺与维生素B12的含量

目的 建立HPLC测定注射用复方三维B中盐酸呋喃硫胺、盐酸吡多胺与维生素B₁₂的含量。 方法 色谱柱C₁₈柱(250 mm×4.6 mm,5 μm),流动相为庚烷磺酸钠溶液-乙腈-甲醇,采用梯度洗脱,流速为1.0 mL·min^-1,检测波长为220 nm,理论板数按盐酸吡多胺峰计不低于3 000,柱温为30 ℃。 结果 盐酸呋喃硫胺、盐酸吡多胺与维生素B12分别在2.04~20.4 μg,2.05~20.5 μg,0.020 6~0.206 μg内与峰面积呈良好的线性关系(r分别为1.000,0.999 9,1.000);平均回收率分别为101.0%,101.6%,98.3%(n=9,RSD分别为0.5%,1.4%,0.3%)。 结论 本法简便、准确、重复性好,适用于注射用复方三维B中盐酸呋喃硫胺、盐酸吡多胺与维生素B₁₂的含量测定。     

盐酸曲美他嗪健康人中的药动学研究和生物等效性评价

目的:建立LC-MS方法测定盐酸曲美他嗪在健康人血浆中的浓度,并进行药物动力学研究和生物等效性评价。方法:18名男性健康受试者,随机分成2组,交叉口服受试制剂和参比制剂各20 mg,采用LC-MS法测定人血浆中曲美他嗪的浓度。结果:受试制剂与参比制剂的各主要药动学参数:t_(1/2)分别为(7.31±2.36)和(6.74±2.17)h,t_(max)分别为(2.1±0.9)和(1.8±0.6)h,C_(max)分别为(92.05±19.64)和(96.71±22.31)ng·ml~(-1),AUC_(0-24)分别为(691.24±171.82)和(706.31±189.60) ng·h·ml~(-1)。对两种制剂的参数C_(max)、AUC_(0-24)对数转换后先进行方差分析,再进行双单侧t检验。双单侧t检验结果表明上述两个参数生物等效,t_(max)经非参数法检验差异没有显著性意义(P>0.05),这表明两种制剂生物等效,相对生物利用度(101.5±26.7)%。结论:两种制剂具有生物等效。     

注射液二盐酸奎宁复方奎宁和硫酸庆大霉素的化学配伍

本文探讨了二盐酸奎宁注射液、复方奎宁注射液分别与硫酸庆大霉素注射在注射器中的化学配伍，两者直接混合后在５ｍｉｎ内产生白色或淡黄色沉淀，提示不宜混配注射。     

应用光动力治疗幽门螺旋杆菌相关性胃炎的实验研究

目的:观察在不同照射强度下血卟啉介导的光动力疗法(PDT)治疗鼠幽门螺旋杆菌(Hp)相关性胃炎的疗效。方法:制备Hp相关性胃炎动物模型,分为A1和A2组,应用血卟啉衍生物(HpD)进行灌胃,C组(感染对照组),应用等量的生理盐水灌胃;3个感染组按顺序(A1,A2,C)均给予波长630nm输出功率分别为50、100、100 mW/cm~2经灌胃器照射,能量密度累积15 J/cm~2,非感染对照组(D组)未经PDT照射。照射后4周,处死所有小鼠,取胃窦和胃体部组织,行快速尿素酶试验和改良吉姆萨染色及H-E病理染色。结果:经PDT处理后,结合快速尿素酶试验和改良吉姆萨染色结果显示A2组Hp阴性率为73.33%(P<0.05)。H-E病理染色显示各感染组经PDT治疗后炎症明显减轻,非感染组经PDT治疗后可见轻微炎症反应。结论:PDT能明显减轻Hp相关性胃炎的炎症程度,并可杀灭Hp,不损伤正常胃黏膜。     

Effects of tyrosine kinase inhibitor E7080 and eNOS inhibitor L-NIO on colorectal cancer alone and in combination

Objective：To investigate the effects of E7080 and N5-（1-iminoethyl）-L-ornithine dihydrochloride （L-NIO）on colorectal cancer alone and in combination.Methods：HT29 colorectal cancer cell line from Sap Institute was used.Real-time cell analysis （xCELLigence system） was performed to determine the effects of E7080 and L-NIO on colorectal cell proliferation.While apoptosis was determined with Annexin V staining,and the effect of agents on angiogenesis was determined with chorioallantoic membrane （CAM） model.Results：We found that E7080 has a strong antiproliferative effect with an half maximum inhibition of concentration （IC50） value of 5.60×10-8 mol/L.Also it has been observed that E7080 showed antiangiogenic and apoptotic effects on HT29 colorectal cancer cells.Antiangiogenic scores of E7080 were 1.2,t.0 and 0.6 for 100,10 and 1 nmol/L E7080 concentrations,respectively.Furthermore,apoptosis has been detected in 71％ of HT29 colorectal cancer cells after administration of 100 nmol/L E7080 which may indicate strong apoptotic effect.Meanwhile administration of L-NIO alone did not show any effect,but the combination of E7080 with L-NIO increased the antiproliferative,antiangiogenic and apoptotic effects of E7080.Conclusions：Results of this study indicate that E7080 may be a good choice in treatment of colorectal tumors.Furthermore the increased effects of E7080 when combined with L-NIO raise the possibility to use a lower dose of E7080 and therefore avoid/minimize the side effects observed with E7080.     

Mucosal bromodomain-containing protein 4 mediates aeroallergen-induced inflammation and remodeling

1. Download high-res image (248KB)
2. Download full-size image

     

3‐[(2,4‐dimethoxy)benzylidene]‐anabaseine dihydrochloride protects against 6‐hydroxydopamine‐induced parkinsonian neurodegeneration through α7 nicotinic acetylcholine receptor stimulation in rats

To explore a novel therapy against Parkinson's disease through enhancement of α7 nicotinic acetylcholine receptor (nAChR), we evaluated the neuroprotective effects of 3‐[(2,4‐dimethoxy)benzylidene]‐anabaseine dihydrochloride (DMXBA; GTS‐21), a functionally selective α7 nAChR agonist, in a rat 6‐hydroxydopamine (6‐OHDA)‐induced hemiparkinsonian model. Microinjection of 6‐OHDA into the nigrostriatal pathway of rats destroys dopaminergic neurons selectively. DMXBA dose dependently inhibited methamphetamine‐stimulated rotational behavior and dopaminergic neuronal loss induced by 6‐OHDA. The protective effects were abolished by methyllycaconitine citrate salt hydrate, an α7 nAChR antagonist. Immunohistochemical study confirmed abundant α7 nAChR expression in the cytoplasm of dopaminergic neurons. These results indicate that DMXBA prevented 6‐OHDA‐induced dopaminergic neuronal loss through stimulating α7 nAChR in dopaminergic neurons. Injection of 6‐OHDA elevated immunoreactivities to glial markers such as ionized calcium binding adaptor molecule 1, CD68, and glial fibrillary acidic protein in the substantia nigra pars compacta of rats. In contrast, these immunoreactivities were markedly inhibited by comicroinjection of DMXBA. Microglia also expressed α7 nAChR in both resting and activated states. Hence, we hypothesize that DMXBA simultaneously affects microglia and dopaminergic neurons and that both actions lead to dopaminergic neuroprotection. The findings that DMXBA attenuates 6‐OHDA‐induced dopaminergic neurodegeneration and glial activation in a rat model of Parkinson's disease raisethe possibility that DMXBA could be a novel therapeutic compound to prevent Parkinson's disease development. © 2012 Wiley Periodicals, Inc.