注册分类改革视角下药品数据保护制度效应分析

在国际趋势的压力下,兼受跨太平洋伙伴关系协定（TPP）影响,我国实施药品数据保护制度已成大势所趋。鉴于药品数据保护与药品注册审批体系紧密相关,我国化学药注册分类改革后,药品数据保护对医药产业发展必然会带来不同影响。结合我国分类注册改革新标准,在理论上对数据保护制度实施效果进行研究,进而探讨新注册分类下数据保护的实施对1至4类药品及医药产业的影响。     

Synthesis and anti-oomycete activity of novel quinazolin- and benzothiazol-6-yloxyacetamides: Potent aza-analogs and five-ring analogs of quinoline fungicides

Novel quinazolin- and benzothiazol-6-yloxyacetamides show excellent in vivo activity against the three economically most important Oomycete pathogens Phytophthora infestans, Plasmopara viticola and Pythium ultimum. They are polar analogs of known quinolin-6-yloxyacetamides, which are not active against the soil-borne damping-off disease caused by Pythium ultimum. The Bogert quinazoline synthesis, an almost forgotten heterocyclization technique, proved to be highly useful for the concise construction of required quinazolin-6-ol building blocks.     

郊野公园植物多样性的生态恢复与重建——以上海滨江森林公园为例

植物作为自然界生态系统的重要组成部分,其多样性的保护与发展是人类可持续发展的物质基础之一,对维护生态环境的平衡与稳定具有重要意义,也是当今中国生态园林城市建设的重要内容。以上海滨江森林公园一期工程为例,通过总结建设过程中自然生境的恢复与重建、现状植物保护和开发的经验,探索郊野公园设计建造中植物多样性保护的有效措施,为今后城市郊野公园的建设和原有绿地的绿化改造等提供参考借鉴。     

生脉注射液联合曲美他嗪治疗缺血性心肌病合并肾功能不全的临床疗效分析

目的:研究生脉注射液联合曲美他嗪治疗缺血性心肌病合并肾功能不全的临床疗效。方法:选取2015年3月至2017年3月我院收治的100例缺血性心肌病合并肾功能不全患者,按照随机数表法分为观察组(n=50)和对照组(n=50)。对照组采用曲美他嗪治疗,观察组采用生脉注射液联合曲美他嗪治疗。观察和比较两组的治疗疗效、治疗前后心功能指标(左心室射血分数(LVEF)、左室收缩末径(LVESD)、左室舒张末期内径(LVEDD))、肾功能指标(血肌酐(Scr),尿素氮(BUN))、心肌损伤标志物(血清胱抑素(Cys C)、同型半胱氨酸(HCY)、脑钠肽(BNP))水平的变化。结果:治疗后,观察组总有效率显著高于对照组[92.30%(48/52) vs.70.83%(34/48)](P0.05),LVEDD、LVESD水平均显著低于对照组[(51.21±8.54)mm vs.(56.63±10.83)mm,(42.91±6.30)mm vs.(45.86±7.32)mm](P0.05),LVEF水平均显著高于对照组[(46.02±7.85)%vs.(41.20±8.84)%](P0.05),Scr、BUN水平均显著低于对照组[(164.30±17.95)μmol/L vs.(211.75±19.31)μmol/L;(8.12±0.76)mmol/L vs.(11.74±1.72)mmol/L](P0.05)。血清Cys C、HCY、NT-Pro BNP水平均显著低于对照组[(0.90±0.21)mg/L vs 1.52±0.34)mg/L (12.34±3.89)μmol/L vs.(20.86±5.28)μmol/L,(298.47±78.41)ng/L vs.(402.35±92.76)ng/L](P0.05)。结论:生脉注射液联合曲美他嗪治疗缺血性心肌病合并肾功能不全的的临床疗效显著优于单用曲美他嗪治疗,其可有效改善患者心、肾功能,减轻心肌细胞损伤。     

The aspartimide problem persists: Fluorenylmethyloxycarbonyl‐solid‐phase peptide synthesis (Fmoc‐SPPS) chain termination due to formation of N‐terminal piperazine‐2,5‐diones

Aspartimide (Asi) formation is a notorious side reaction in peptide synthesis that is well characterized and described in literature. In this context, we observed significant amounts of chain termination in Fmoc‐SPPS while synthesizing the N‐terminal Xaa‐Asp‐Yaa motif. This termination was caused by the formation of piperazine‐2,5‐diones. We investigated this side reaction using a linear model peptide and independently synthesizing its piperazine‐2,5‐dione derivative. Nuclear magnetic resonance (NMR) data of the side product present in the crude linear peptide proves that exclusively the six‐membered ring is formed whereas the theoretically conceivable seven‐membered 1,4‐diazepine‐2,5‐dione is not found. We propose a mechanism where nucleophilic attack of the N‐terminal amino function takes place at the α‐carbon of the carbonyl group of the corresponding Asi intermediate. In addition, we systematically investigated the impact of (a) different adjacent amino acid residues, (b) backbone protection, and (c) side chain protection of flanking amino acids. The side reaction is directly related to the Asi intermediate. Hence, hindering or avoiding Asi formation reduces or completely suppresses this side reaction.     

BRCA1 Haploinsufficiency Is Masked by RNF168-Mediated Chromatin Ubiquitylation

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木麻黄海防林种子雨的时空动态

为了解木麻黄(Casuarina equisetifolia)种子雨的时空间分布格局和萌发性能对其天然更新的影响,对海口木麻黄海防林种子雨的时空分布特征和种子雨的萌发动态进行了研究。结果表明,木麻黄种子落雨时间始于7月中旬,结束于次年4月中旬,持续长达9个月,期间种子雨年际平均密度为1 764.63 grain m~(-2)a~(-1);种子雨高峰期在12月上中旬,落种量占总散落量的43.38%;种子雨呈聚集分布,且种子雨密度与附近球果数量呈极显著正相关;种子雨萌发率较低,仅为11.31%,但由于种子雨密度较大,可萌发的种子雨密度仍然较大,为199.58grainm~(-2)a~(-1)。因此,种子数量和质量均不是制约木麻黄天然更新困难的主要障碍因子,但聚集分布特征使木麻黄种子在林内扩散能力十分有限。     

仁化县野生白毛茶群落特征及保护对策

以广东仁化县董塘镇及红山镇5个分布有野生白毛茶Camellia sinensis var. pubilimba的生存群落为对象,开展样方调查及群落生态学分析,以期明确野生白毛茶的生长状况及保护对策。结果表明：(1) 5个有野生白毛茶分布的群落,共分布有维管植物177种,隶属于63科119属,其中蕨类植物13科17属21种,被子植物49科101属155种;(2) 白毛茶野生种群分布于毛竹Phyllostachys heterocycla、杉木Cunninghamia lanceolata群落演替而成的次生林,群落上层以毛竹、杉木、华润楠Machilus chinensis、罗浮柿Diospyros morrisiana为优势种,灌木层以白毛茶、红背山麻杆Alchornea trewioides、绒毛山胡椒Lindera nacusua、八角枫Alangium chinense为优势种,草本层以乌毛蕨Blechnum orientale、蔓生莠竹Microstegium fasciculatum、三叶崖爬藤Tetrastigma hemsleyanum等占优势;(3) 除次生林外,其余群落中草本层Simpson指数、Shannon-wiener指数及均匀度均高于乔木层及灌木层,这可能是自然演替进程与人类砍伐活动综合作用的结果;(4) 野生白毛茶更适合处于中度干扰的次生林中,较为湿润的阳坡利于其发展;(5) 野生白毛茶数量虽多,共258株,却均为小苗,且生长状况并不理想,需及时采取有效的保护措施就地保护、适度干扰,同时加强民众教育保护现有野生资源,扩大野生种群调查范围,兼顾回归实验。