剑麻提取物的细胞毒活性研究

用溶剂萃取法对剑麻的95%乙醇提取物进行分段处理,利用MTT法测定各提取部位的体外细胞毒活性。正丁醇提取物对肿瘤细胞株K-562、SMMC-7721和SGC-7901显示有生长抑制活性,IC50值分别为5.6、23.8和26.8μg/mL,而石油醚、乙酸乙酯和水溶性部位则没有活性。     

栎金钱菌活性提取物抗衰老研究

用栎金钱菌活性提取物灌胃衰老模型小鼠,观察其对小鼠血清SOD活性、肝组织MDA和脂褐素的含量、脾指数、胸腺指数和肾指数的影响。结果表明,栎金钱菌活性提取物能使雄性小鼠血清SOD活性提高40.16%,肝MDA含量减少47.12%,肝脂褐素含量减少89.48%,脾指数增加35.13%,胸腺指数增加48.92%,肾指数增加11.26%,表明栎金钱菌活性提取物具有良好的抗衰老作用。栎金钱菌活性提取物800mg/kg·d的剂量具有最好的抗衰老效果,且具有性别的差异,对雄性小鼠的抗衰老作用略优于对雌性小鼠的。     

在新疆发现两种珍稀野鸭

1白头硬尾鸭(Oxyura leucocephala)作为IUCN/ICBP鸟类红皮书内的国际性受胁鸟类(EN),白头硬尾鸭(Oxyura leucocephala)一直受到国际上的密切关注。湿地国际(Wetlands International)与鸟类国际(BirdLife International)等国际组织都曾经在欧、亚、非洲组织过对白头硬尾鸭的普查(Hughes et al,2006)。作为特邀参加调查者之一,笔者曾经绞尽脑汁、     

肝炎治疗药苦参碱葡萄糖注射液的研制

为研制供临床直接使用的大容量苦参碱葡萄糖注射液,采用苦参碱浓配,葡萄糖先浓配除热原、后稀配混合苦参碱溶液、精滤、灌封、灭菌等制得苦参碱葡萄糖注射液,并建立质量标准。结果表明：试制3批样品均符合质量标准要求,稳定性考察未见明显变化。研制的苦参碱葡萄糖注射液处方及工艺合理可行、质量标准可控、稳定性良好。     

假马齿苋的生物活性及其临床研究

假马齿苋(Bacopa monniera,BM)具有提高记忆,镇静,抗癫痫和抗炎,镇痛,退烧,强心等生物活性。假马齿苋皂苷(bacosides)是主要的益智活性成分。     

红树林植物木果楝细胞毒活性和化学成分研究

本研究采用MTT法对红树林植物木果楝(Xylocarpus grantum)正己烷提取物进行细胞毒活性筛选,结果显示对宫颈癌Hela细胞有较强的生长抑制活性。为了确定其中的活性成分,利用GC/MS法对正己烷提取物的化学成分进行分析,共鉴定了17种成分,大部分为有机酸类化合物。其中油酸(Oleic acid,24.89%)、棕榈酸(Palmitic acid,24.82%)和亚油酸(Linoleic acid,16.86%)为主要成分,据文献报道亚油酸具有肺腺癌细胞生长抑制活性。     

大叶山楝根化学成分与细胞毒活性的研究

为了解大叶山楝(Aphanamixis grandifolia Bl.)根中的抗肿瘤活性成分,利用各种色谱技术从其95% 乙醇提取物中分离得到9 个化合物,经波谱分析分别鉴定为:7-hydroxycadalene (1)、dregeana-1 (2)、4-oxopinoresinol (3)、4-ketopinoresinol (4)、6-deoxyjacareubin (5)、schleicheol 1 (6)、豆甾醇 (7)、β-谷甾醇 (8)和胡萝卜苷 (9).其中化合物1~6 为首次从山楝属植物中分离得到,并首次报道了化合物1的碳谱数据.生物活性测试结果表明,化合物1和5对慢性髓原白血病细胞K562 有生长抑制活性,化合物1、5 和6 对人胃癌细胞SGC-7901 有生长抑制活性.     

Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs

A series of 26 diarylpyrimidines, characterized by the hydroxymethyl linker between the left wing benzene ring and the central pyrimidine, were synthesized and evaluated for in vitro anti-HIV activity. Most of the compounds exhibited moderate to excellent activities against wild-type HIV-1. Among them, compound 10i, bearing a chlorine atom at the C-2 position of left benzene ring, was the best congener and showed potent activity against wild-type HIV-1 with an EC(50) value of 0.009 μM, along with moderate activities against the double RT mutant (K103N+Y181C) HIV-1(III(B)) and HIV-2(ROD) with an EC(50) value of 6.2 and 6.0 μM, respectively. The preliminary structure-activity relationship (SAR) of this new series of compounds was also investigated.     

Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors

A novel series of naphthyl phenyl ether analogues (NPEs) have been synthesized and evaluated for their in vitro activities against HIV in C8166 cells. Most of the compounds exhibited moderate to excellent anti-HIV activities. Among them the most active compound 12o showed excellent activities against wild-type HIV-1 with an EC(50) value of 4.60 nM, along with moderate activities against the double mutant strain HIV-1(IIIB) A17 (K103N+Y181C) and HIV-2 strain ROD with an EC(50) value of 0.82 and 4.40 μM, respectively. Preliminary structure-activity relationship (SAR) among the newly synthesized NPEs was also investigated.