虫草复方对博莱霉素致大鼠肺纤维化的作用及其机制

目的 探讨虫草复方对博莱霉素致大鼠肺纤维化的作用及其机制。方法 Wistar大鼠随机分为对照组,模型组,复方虫草高、低剂量（150、75 mg/kg）组和醋酸泼尼松（3.33 mg/kg）组,每组18只。除对照外其余各组大鼠采用气管内一次性滴注盐酸博莱霉素造模,对照组大鼠气管内一次性滴注等体积生理盐水。造模后第2天开始给药,对照组和模型组分别ig给予等体积生理盐水。各组动物于7、14、28 d随机处死6只,分别观察大鼠肺指数、肺组织羟脯氨酸（Hyp）、丙二醛（MDA）和超氧化物歧化酶（SOD）活性及血清中MDA的量和SOD的活性。同时取固定部位肺组织进行病理组织学检查,并应用免疫组织化学法检测转化生长因子-β1（TGF-β1）、I型胶原、III型胶原在肺组织中的表达;观察各组大鼠动脉血气的变化。结果 虫草复方能明显降低肺纤维化大鼠肺指数和肺组织Hyp的量,并可提高血清和肺组织中SOD活性,降低血清和肺组织中MDA和肺组织TGF-β1、I型胶原、III型胶原的表达;虫草复方可使肺纤维化大鼠动脉二氧化碳分压[p(CO₂)]降低和血氧分压[p(O₂)]提高;虫草复方明显改善实验性大鼠肺纤维化程度。结论 虫草复方对大鼠肺纤维化具有一定的干预作用,其机制可能与抗脂质过氧化、抑制TGF-β1表达、减少肺泡间质胶原沉积及改善肺呼吸功能有关。     

复方大青叶注射液对体外培养HT-H9细胞CXCR4启动子活性的影响

目的:探讨复方大青叶注射液对体外培养HT-H9细胞中CXCR4启动子活性的作用.方法:克隆人CXCR4启动子序列,构建报告载体pGL4.17-CXCR4;转染HT-H9细胞株,G418筛选后分组,高、低剂量实验组分别用200、100 mg/L大青液注射液处理,设注射水对照组、空白对照组和未转染对照组;各组处理24 h后...     

河南产尾叶香茶菜叶部位化学成分的分离与纯化

目的:分离纯化河南产尾叶香茶菜(Rabdosia excisa)叶部位的化学成分.方法:利用硅胶柱色谱法对尾叶香茶菜叶部位的化学成分进行分离和纯化,通过理化性质和波谱数据鉴定结构.结果:从尾叶香茶菜叶中分离鉴定了10个化合物:1α,6,11β,15β-四乙酰基-6,7-断裂-7,20-内酯-对映-贝壳杉-16-烯(I)...     

Diastereoselective synthesis and bioactivity of long-chain anti-2-amino-3-alkanols

An improved four-step approach for the stereoselective synthesis of long-chain anti-2-amino-3-alkanols is described. Using this method, the syntheses of antiproliferative (antitumoral) compounds, spisulosine (ES-285, 2), clavaminols A and B (3 and 4), the deacetylated products of clavaminols H and N (7 and 8), as well as (2S,3R)-2-aminododecan-3-ol (9) and xestoaminol C (10), have been achieved in excellent diastereoselectivities. In vitro study showed that these compounds induced cell death and dose-dependently inhibited cell proliferation in human glioblastoma cell line SHG-44, indicating the anti-tumor property of this series of compounds.     

Synthesis of 9-substituted 2,3,4,9-tetrahydro-1H-carbazole derivatives and evaluation of their anti-prion activity in TSE-infected cells

2,3,4,9-Tetrahydro-9-[2-hydroxy-3-(1-piperidinyl)propyl]-6-methyl-1H-carbazol-1-one (GJP14) is a novel anti-prion compound that we previously discovered by in silico screening and cellular assay. In this study, a variety of GJP14 derivatives were prepared using pyrrole derivatives, (haloalkyl)oxiranes, and amines, and their anti-prion activity was evaluated in TSE-infected cells. It was found that the tricyclic aromatic ring, a hydroxy group at the 2-position and an amino group at the 3-position of the N-propyl group were the basic requirements for anti-prion activity. The derivatives bearing an N-ortho-halobenzyl group exhibited an improved activity, and the most potent derivative was 8 times as effective as the original lead compound, GJP14.     

Optimization of 3-(phenylthio)quinolinium compounds against opportunistic fungal pathogens

Ring-opened benzothieno[3,2-b]quinolinium salts (3) were designed and synthesized with substitution on the thiophene moiety. In vitro screenings were carried out against fungal pathogens including Cryptococcus neoformans, Candida albicans, Candida glabrata, Candida krusei and Aspergillus fumigatus. In all, by replacing the N-methyl group (2) with N-ω-phenylpentyl or ω-cyclohexylpentyl group to form substituted 3-(phenylthio)quinolinium compounds produced remarkable potencies, as high as 300-fold (cf, cryptolepine (1) = 250 μg/mL vs 11p = 0.8 μg/mL for C. albicans) over the starting tetracyclic parent. In addition, all the N-ω-cyclohexylpentyl analogs produced superior activity against all the microorganisms tested than the N-ω-phenylpentyl substituted compounds. The potential of these compounds to induce toxicity in Vero cells was also investigated and the majority of them showed lower or no cytotoxicity at 10 μg/mL than amphotericin B, the gold standard in antifungal drug development. For instance, the trifluoromethyl substituted analogs (11n-p) have selectivity indices over 2-fold better than those of amphotericin B in C. neoformans. Overall, this ring-opened scafford of benzothienoquinolines, with substitution on the thiophenyl moiety, serves as a new lead for further development.     

经颅视神经管减压联合复方樟柳碱治疗外伤性视神经损伤的疗效

目的 观察经颅视神经管减压术联合复方樟柳碱治疗外伤性视神经损伤的治疗效果,探讨外伤性视神经病变的有效治疗方法.方法 将 32例(32眼)外伤性视神经患者随机分为经颅视神经管减压术联合复方樟柳碱治疗组(治疗组)16例(16眼),经颅视神经管减压术联合其他药物治疗组(对照组)16例(16眼).比较2组临床疗效.结果 治疗组显效6例,有效4例,无效6例,总有效率62.5%,对照组显效3例,有效3例,无效10例,总有效率37.5%.2组总有效率相比,差异有统计学意义(P<0.01),结论经颅视神经管减压联合复方樟柳碱治疗外伤性视神经病变是一种可供选择的,确切、彻底、安全有效的治疗手段.     

高效液相色谱法测定蒙药复方述达格-4有效部位中山奈素和高良姜素的含量

目的：建立同时测定蒙药复方述达格-4有效部位中高良姜素、山奈素的高效液相色谱含量测定方法。方法：采用反相高效液相色谱法,色谱柱为Diamosil C18（4.6mm×250mm,5μm）,以乙腈（A）-0.5%磷酸水溶液为流动相,梯度洗脱（0～20min,34%A→37%A;20～60min,37%A）,流速1.0mL/min检测波长为286nm,柱温30℃,进样量20μL。结果：高良姜素、山奈素的线性范围分别为0.04～0.4μg（r=0.9999）,0.01656～0.1656μg（r=0.9999）;平均加样回收率（n=6）分别为99.92%、98.92%;RSD为2.09、2.33。结论：本法准确、简便,具有良好的重复性,可为蒙药复方述达格-4质量控制提供依据。     

口服复方谷氨酰胺肠溶胶囊辅助治疗溃疡性结肠炎临床观察

目的:探讨口服复方谷氨酰胺肠溶胶囊辅助治疗溃疡性结肠炎的临床疗效。方法:收集72例溃疡性结肠炎患者,按入组编号随机分为观察组与对照组,每组36例,观察组患者应用复方谷氨酰胺肠溶胶囊联合美沙拉嗪缓释片治疗,而对照组仅用美沙拉嗪缓释片治疗,观察两疗程并随访半年后,比较两组患者临床疗效、不良反应及治愈时间,并进行统计学分析。结果:观察组临床有效率94.44%明显优于对照组72.22%,两组相比经统计学处理有显著性差异(P<0.05);观察组不良反应发生例数明显少于对照组,两组发生率相比有显著性差异(P<0.05);且观察组平均治愈时间明显短于对照组,两组相比亦有统计学意义(P<0.05)。结论:口服复方谷氨酰胺肠溶胶囊辅助治疗溃疡性结肠炎效果肯定,可显著提高临床疗效,缩短疗程,减轻不良反应,临床值得推广应用。     

复方丹参联合阿司匹林对大鼠糖尿病肾病的治疗作用

目的:复制大鼠糖尿病肾病模型,研究复方丹参联合阿司匹林对大鼠糖尿病肾病的治疗作用及其机制。方法:选择体重180～200g的健康雄性SD大鼠64只,随机选取54只复制大鼠糖尿病肾病（DN）模型,其余大鼠作为正常对照（NC）组。实验第8周后,随机将模型组大鼠分为糖尿病肾病（DN）对照组、阿司匹林（DN+A）治疗组、复方丹参（DN+S）治疗组、复方丹参联合阿司匹林（DN+A+S）治疗组各10只。自模型成功之日起分别按相应方案治疗。检测空腹血糖（FBG）、血尿素氮（BUN）、血肌酐（Scr）、尿24h微量白蛋白（mALb）、肾组织丙二醛（MDA）、血栓素B₂（TXB₂）,光镜观察大鼠肾组织形态学变化。比较治疗后各组之间上述指标的差异。结果:与DN对照组相比,DN+A+S组FBG、BUN、Scr、24hmAlb、MDA、TXB2均明显降低（P<0.05）;DN+A组BUN、Scr、MDA、TXB2也明显降低（P<0.05）,但FBG、24hmAlb无显著降低（P>0.05）;DN+S组也见FBG、BUN、Scr、24hmAlb、MDA、TXB2明显降低（P<0.05）。DN+A+S组同DN+A组相比,上述指标变化更显著（P<0.05）;同DN+S组相比,上述指标的改善同样更明显,P<0.05（FBG除外）。结论:复方丹参联合阿司匹林对大鼠DN的改善作用与其降低血糖、抗氧化应激损伤和改善肾脏微循环等有关。