Maleimide and maleic anhydride derivatives from the mycelia of Antrodia cinnamomea and their nitric oxide inhibitory activities in macrophages

On cultivation of the fungus Antrodia cinnamomea (BCRC 36799) on a medium, the mycelium was extracted and evaluated for nitric oxide (NO) inhibitory activity. Bioactivity-directed fractionation led to the isolation of two new maleimide derivatives, antrocinnamomins A (1) and B (2), and two new maleic anhydride derivatives, antrocinnamomins C (3) and D (4), along with three known compounds, 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]furan-2,5-dione (5), 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]-1H-pyrrole-2,5-dione (6), and 3-isobutyl-4-[4-(3-methyl-2-butenyloxy)phenyl]-1H-pyrrol-1-ol-2,5-dione (7). Structural elucidation of compounds 1-4 was carried out by spectroscopic data. Compound 1 displayed significant inhibitory effect on nitric oxide (NO) production.     

Autonomic nervous system mediates the cardiovascular effects of Rhodiola sacra radix in rats

ETHNOPHARMACOLOGICAL RELEVANCE: Rhodiola sacra (Crassulaceae) exhibits cardiovascular bioactivities and is used in Tibetan medicine for promoting circulation and preventing hypertension. However, the underlying mechanisms of its cardiovascular effects are poorly understood. AIM OF THE STUDY: The aim of this study was therefore to evaluate the cardiovascular activity of water-soluble fraction (WtF) and n-butanol-soluble fraction (BtF) of Rhodiola sacra radix and to explore its mechanism of action in propofol anesthetized Sprague-Dawley rats. MATERIALS AND METHODS: The changes of blood pressure, heart rate and cardiac contractility after systemic administration of the extracts (10-75mg/kg) were examined for at least 40min. Different antagonists were used to evaluate the mechanisms of cardiovascular effects of the extracts. RESULTS: Intravenous injection of the WtF (10, 25, 35, 50 or 75mg/kg) exhibited dose-dependent hypotension and increases in heart rate and cardiac contractility. In contrast, mild alterations in the same cardiovascular parameters were detected only at high dose (75mg/kg) BtF. The WtF-induced hypotensive, positive inotropic and chronotropic effects were significantly abolished by pretreatment with hexamethonium (30mg/kg, i.v.) or reserpine (5mg/kg, i.v.), whereas the hypotensive, but not the positive inotropic or chronotropic effect was potentiated by captopril (2.5mg/kg, i.v.). Pretreatment with methylatropine (1mg/kg, i.v.), on the other hand, reversed the positive inotropic and chronotropic but not the hypotensive effects of WtF. The WtF-induced cardiovascular responses were not affected in rats pretreated with N(G)-nitro-l-arginine methyl ester (20mg/kg, i.v.). CONCLUSIONS: We conclude that systemic administration of the WtF of Rhodiola sacra radix elicited a potent hypotensive effect that was mediated by the withdrawal of sympathetic vasomotor tone and interaction with the circulatory angiotensin system. The positive inotropic and chronotropic effects of WtF may result from a direct vagal inhibition on the heart.     

肠炎愈片对大鼠溃疡性结肠炎血清白介素-2、一氧化氮的影响研究

目的观察肠炎愈片对大鼠慢性溃疡性结肠炎血清白介素-2(IL-2)、一氧化氮(NO)的影响。方法用免疫法建立大鼠慢性溃疡性结肠炎模型,将造模后的大鼠随机分为模型组、肠炎愈片高、中、低剂量组、补脾益肠丸组、柳氮磺吡啶组6组,另设正常对照组,共7组。观察肠道形态和组织学改变,采用ELISA法测定血清中IL-2、检测用药后血清NO的含量。结果与模型组比较,肠炎愈片各剂量组血清IL-2含量升高(P<0.05);肠炎愈片高、中剂量组血清NO含量显著低于模型组(P<0.01)。肠炎愈片高、中、低剂量组形态和组织学损伤评分明显下降(P<0.05)。结论肠炎愈片各剂量组治疗UC的机制可能与其恢复提高IL-2水平,从而使Th1/Th2的细胞因子恢复平衡有关;减少NO的生成亦是肠炎愈片治疗UC的作用机制之一。     

颈部彩色超声在食管上段癌放射治疗中的应用

目的：观察颈部彩色超声在食管上段癌调强放射治疗（intensity-modulated radiation therapy,IMRT）中的应用价值。方法选取食管上段癌患者68例,随机分为2组各34例,A 组 IMRT 前行颈部彩色超声检查,发现有淋巴结转移的作为累及野治疗,B 组不行彩色超声检查,均采用5个野 IMRT。结果放射治疗结束后2组总有效率比较差异无统计学意义（P ＞0．05）。2组1年和2年生存率差异无统计学意义（P ＞0．05）。A 组3年生存率高于 B 组,差异有统计学意义（P ＜0．05）。放射治疗不良反应主要以1～2级为主,2组不良反应发生率比较差异无统计学意义（P ＞0．05）。A 组病死率低于 B 组,差异有统计学意义（P ＜0．05）。结论在食管上段癌的 IMRT 前颈部彩色超声检查作为颈部照射野的依据,可提高患者的3年生存率,且近期疗效好,不良反应可耐受。     

Mining Health Social Media with Sentiment Analysis

With the rapid development of the Internet, more and more users utilize health communities (known as forums) to find health-related information, share their medical stories and experiences, or interact with other people in the communities. In this paper, we propose a framework to analyze the user-generated contents in a health community. The proposed framework contains three phases. First, we extract medical terms, including conditions, symptoms, treatments, effectiveness and side effects to form a virtual document for each question in the community. Next, we modify Latent Dirichlet Allocation (LDA) by adding a weighted scheme, called conLDA, to cluster virtual documents with similar medical term distributions into a conditional topic (C-topic). Finally, we analyze the clustered C-topics by sentiment polarities, and physiological and psychological sentiment. The experiment results show that conLDA outperforms the original LDA, and can cluster relevant medical terms and relevant questions together. The C-topics clustered by conLDA are more thematic than those clustered by the original LDA. The results of sentiment analysis may provide a quick reference and valuable insights for patients, caregivers and doctors.     

抗癌先导物T-OA在不同介质中的平衡溶解度及表观油水分配系数

目的测定抗癌先导物T-OA在不同pH（1¹0）缓冲溶液和表面活性剂溶液中的平衡溶解度,在正辛醇-水/缓冲液体系中的表观油水分配系数。方法采用高效液相法测定了T-OA在不同pH（1¹0）缓冲溶液和表面活性剂溶液中的浓度,采用摇瓶-HPLC法测定了T-OA的表观油水分配系数。结果 T-OA在37℃缓冲液中随pH的增高平衡溶解度逐渐增大,最大平衡溶解度为5.10 mg/L;在32 g/L的十二烷基硫酸钠溶液中其平衡溶解度提高到706.97 mg/L;T-OA的表观油水分配系数为544.71(Ig P_app=2.74),且随溶液pH的增高逐渐降低。结论 T-OA的水溶性较差,可采用适当浓度的十二烷基硫酸钠和吐温80作为溶出介质,这为今后的剂型选择提供了参考。     

高糖对体外培养兔视网膜Müller细胞AQP4表达的影响

目的：观察体外培养兔视网膜Müller细胞在高糖条件下水通道蛋白-4（AQP4）表达的变化。方法：采用体外培养的兔视网膜Müller 细胞,分为正常对照组及高糖组（葡萄糖浓度：30、40和50 mmol•L^-1）,分别培养1、3和5 d;采用免疫细胞化学、流式细胞术及RT-PCR方法对Müller 细胞AQP4的表达情况进行检测。结果：高糖组Müller 细胞AQP4表达的绿色荧光明显弱于正常对照组（P<0.01）;流式细胞仪检测中波峰位置明显提前,AQP4表达强度较对照组明显减弱（P<0.01）,且随着葡萄糖浓度的增高和作用时间的延长,AQP4表达强度逐渐减弱;血糖浓度50 mmol•L^-1培养3 d时,RT-PCR半定量分析显示,AQP4 mRNA的表达比对照组明显降低（P<0.01）。结论：高糖能降低视网膜Müller细胞AQP4的表达,且随着葡萄糖浓度的增高和作用时间的延长,AQP4的表达强度也逐渐减弱;高糖时AQP4的表达下降可能是机体对糖尿病视网膜病变的一种保护性反应。     

积雪草提取纯化工艺的研究

目的研究积雪草的提取纯化工艺。方法采用正交试验进行工艺优化,薄层色谱扫描法测定羟基积雪草苷含量。结果提取工艺最佳条件为:水提取2次,第1次加10倍量水提取2h,第2次加8倍量水提取1.5h。纯化工艺最佳条件为壳聚糖用量0.4mL/g,药液浓缩比例1.2:1,絮凝温度70℃。结论本方法可节省原料,缩短工时,降低成本,利于工业化大生产。