Synthesis and biological evaluation of isoflavone fatty acid esters with potential weight loss and hypolipidemic activities

A series of isoflavone fatty acid esters were designed on the basis of endogenous oleoyl-estrone using estrogen moiety modification strategy. Ten new compounds were synthesized, and their body weight loss and hypolipidemic bioactivities were assayed. Some of these novel compounds could effectively inhibit the differentiation of 3T3-L1 preadipocytes in vitro. The most potent compound 1a significantly decreased the body weight and white adipose tissue weight in a high-fat diet-induced rat model. Also, compound 1a showed good hypolipidemic activity and low toxicity.     

中国亚热带地区柑桔的气候适宜性

应用生态适宜度理论和模糊数学方法,建立柑桔气候适宜度模型,对中国亚热带地区柑桔生产的气候适宜性及其时空差异进行了计算、评价,并分析了中国亚热带地区柑桔各生育期气候适宜性以及中国亚热带地区各县区的平均气候适宜度.结果表明:柑桔花芽分化期、发芽期、果实成熟期的适宜性较低、风险较高,其他各生育期的适宜性较高、风险较低,影响中国亚热带地区柑桔生产的关键问题是冷害和伏旱.柑桔温度适宜性的地域分异呈纬度地带性规律;降水适宜度最适宜型分布在亚热带中部"射阳-那坡"一线区域,其东南为适宜型区,西北为次适宜型区,高山区为不适宜型区;日照适宜度与实际日照时数的区域变化规律基本一致,大致呈高纬度区高于低纬度区、高海拔区高于低海拔区;受温度因子的限制,气候适宜度与温度适宜度的分布情况大体一致,南部大于北部,基本也呈纬度地带性规律.从中国亚热带地区柑桔气候适宜度的年际变化分析可知,整个亚热带地区柑桔气候适宜度呈下降趋势,且存在区域差异,说明气候变化引起了中国亚热带柑桔适宜区和关键生育期的变动.     

在脉冲污染环境中具有阶段结构的捕食食饵Gompertz模型的动力学性质

研究了在脉冲污染环境中,捕食者具有阶段结构的捕食食饵Gompertz模型的动力学性质,获得了捕食者灭绝周期解全局吸引和系统持续生存的条件.     

2009年中国植物科学若干领域重要研究进展

2009年中国植物科学在水稻和拟南芥研究等方面取得＂爆发性＂的快速发展。中国科学家在植物科学各领域中取得了大量的原创性研究成果,尤其是在基于新一代测序技术和计算生物学理论的基因组学、水稻功能基因挖掘、激素受体和信号转导以及转基因作物产业化和生态安全性研究等方面取得一系列重大进展,受到了国内外广泛关注。该文对2009年中国本土植物生命科学若干领域取得的重要研究进展进行概括性评述,旨在全面追踪当前中国植物科学领域发展的最新前沿和热点事件,并展现我国科学家们所取得的杰出成就。     

儿童医院门诊益生菌制剂使用情况的调查分析

目的了解儿科临床益生菌制剂使用现状及存在问题,为儿科医生合理使用益生菌制剂提供帮助。方法抽取重庆医科大学附属儿童医院2009年1月至12月门诊处方1627024张,并将2月、10月含益生菌制剂的处方9173张按临床诊断进行分类,统计益生菌制剂使用情况,使用制剂,用药年龄,用药科室及疾病,益生菌制剂间的联用及与抗生素联用。结果1627024张门诊处方中含益生菌制剂处方为54950张,占总处方数的3．38％。54950张含益生菌制剂处方中,含双歧杆菌四联活菌片的处方最多,为19052张,占34．67％（19052／54950）;用药患者年龄≤1岁的处方43163张,占78．33％（43163／54950）;来自感染消化科的处方31048张,占56．50％（31048／54950）;2种益生菌制剂合用的处方765张,占1．39％（765／54950）;与抗生素联用的处方13641张,占24．82％（13641／54950）。2月、10月共9173张含益生菌制剂处方中,用于消化道疾病5717张,占62．32％（5717／9173）;呼吸系统疾病2389张,占26．04％（2389／5717）;新生儿黄疸541张,占5．90％（541／5717）;过敏性疾病525张,占5．72％（525／5717）。结论儿科门诊常用双歧杆菌为主成分的益生菌制剂,主要治疗肠道疾病,1岁以下婴儿为主要施治对象,符合微生态制剂药理机制;医生对微生态制剂的成分和耐药益生菌情况不够清楚,造成益生菌制剂与抗生素联用较普遍,并存在组成菌相同或类似的益生菌制剂联用。     

栀子黄色素制备藏红花酸研究

以栀子黄色素为原料,对其水解反应制备藏红花酸及其纯化条件进行了研究,结果表明,栀子黄色素经碱水解法制备藏红花酸的最佳条件为:KOH溶液10%、温度为60℃、反应时间120 min,水解所得藏红花酸通过甲醇除杂,重结晶后,所得结晶其mp.、uv与文献报道一致,其质谱的诱导碰撞解离技术获得碎片裂解信息均表明所得到的结晶为藏红花酸,经HPLC检测纯度达到98.43%,得率为8.42%。     

芦蒿不同浸提物化感活性的比较研究

采用水、甲醇、乙醇、丙酮和乙酸乙酯等不同溶剂对整株芦蒿进行浸提,并用生菜和紫花苜蓿作为受试植物,对不同浸提物进行了化感活性的比较研究。5种不同溶剂的芦蒿浸提物对种子的萌发率和幼苗生长均表现出化感潜势,与对照组相比,0.005 g/mL的芦蒿甲醇提取物对生菜和紫花苜蓿种子的萌发具有轻微的促进作用,当浓度达到0.04 g/mL以上时,对生菜和紫花苜蓿种子的萌发和幼苗生长均具有不同程度的抑制作用（p〈0.05）。不同浓度的提取液对植物的化感作用强度不同,对种子萌发率、根长、芽长均有不同程度的影响。根据比较,甲醇溶剂提取物的化感活性最强,其是深入研究芦蒿化感物质有效的提取剂。     

Apoptotic Regulation by MCL-1 through Heterodimerization

Myeloid cell leukemia 1 (MCL-1), an anti-apoptotic BCL-2 family member active in the preservation of mitochondrial integrity during apoptosis, has fundamental roles in development and hematopoiesis and is dysregulated in human cancers. It bears a unique, intrinsically unstructured, N-terminal sequence, which leads to its instability in cells and hinders protein production and structural characterization. Here, we present collective data from NMR spectroscopy and titration calorimetry to reveal the selectivity of MCL-1 in binding BCL-2 homology 3 (BH3) ligands of interest for mammalian biology. The N-terminal sequence weakens the BH3 interactions but does not affect selectivity. Its removal by calpain-mediated limited proteolysis results in a stable BCL-2-like core domain of MCL-1 (cMCL-1). This core is necessary and sufficient for BH3 ligand binding. Significantly, we also characterized the in vitro protein-protein interaction between cMCL-1 and activated BID by size exclusion chromatography and NMR titrations. This interaction occurs in a very slow manner in solution but is otherwise similar to the interaction between cMCL-1 and BID-BH3 peptides. We also present the solution structure of complex cMCL-1·hBID-BH3, which completes the family portrait of MCL-1 complexes and may facilitate drug discovery against human tumors.     

Amino Acid Residue Val362 Plays a Critical Role in Maintaining the Structure of C Terminus of Connexin 50 and in Lens Epithelial-fiber Differentiation

We have previously shown that connexin (Cx) 50, unlike the other two lens connexins, Cx43 and Cx46, promotes chicken lens epithelial-fiber differentiation in a channel-independent manner. Here, we show that deletion of the PEST motif at the C terminus (CT) domain of Cx50 attenuates the stimulatory effect of Cx50 on lens fiber differentiation. Valine 362, a residue located within the PEST domain, is functionally involved. The structure of the Cx50 CT predicted by molecular modeling revealed four α-helices and Val³⁶² was found to be located in the middle of the 3rd helix. Replacement of Val³⁶² with amino acid residues that disrupt the α-helical structure predicted by molecular modeling, such as arginine, glutamate, or phenylalanine, attenuated the stimulatory effects of Cx50 on lens differentiation, whereas replacement with threonine, isoleucine, leucine, or proline, which maintain the structure preserved the function of Cx50. Circular dichroism (CD) studies supported the structural predictions and showed that the substitution with Glu, but not Thr or Pro, disrupted the α-helix, which appears to be the structural feature important for lens epithelial-fiber differentiation. Together, our results suggest that Val³⁶² is important for maintaining the helical structure and is crucial for the role of Cx50 in promoting lens epithelial-fiber differentiation.