用2DNMR鉴定倍半萜多元酯的结构

利用2DNMR结合其他波谱方法从苦皮藤种子油中鉴定了2个新倍半萜多元酯,它们分别是1α-苯甲酰氧-8β-烟酰氧-9α、11β-2乙酰氧-β-二氢沉香呋喃,1β-苯甲酰氧-2α、8β、9α、11β-4乙酰氧-β-二氢沉香呋喃,命名为苦皮藤酯2和3。     

一株AEC^hrL—赖氨酸产生菌

从乳糖发酵短杆菌Brevibacterium Lactofermentum2645菌株出发选育L-赖氨酸产生菌,经分离复壮后,用硫酸二乙酯(DES)诱变处理,由添加S-(2-氨基乙基)—L—半胱氨酸(AEC)和L-苏氨酸的药物平板定向筛选,最后获得了一株L—赖氨酸高产菌E_(16-2)(AHV~(hr)SAM~gAEC~(hr))。进而通过正交试验、工艺条件试验最终获得了该菌株的最佳发酵条件,并考查了在此条件下的L-赖氨酸发酵过程,结果表明该菌具有生长、耗糖、产酸速度快、发酵周期短的明显特点。     

含人口迁移的性传染病模型

本文研究一类含人口迁移的性传染病模型,应用摄动方法和定性方法研究平衡点的稳定性和迁移率的影响。普举例说明。     

光氮互作对闽楠幼苗叶片光合生理特性的影响

以5月龄闽楠幼苗为材料,采用4种光照水平(100%、41.3%、14.3%、3.6%自然光)和4种氮素水平(0、0.5、1、2 mol/L纯氮)的双因素盆栽试验,研究光氮互作下闽楠幼苗的光合生理特性,以探讨其对环境适应性的生理机制。结果表明:(1)遮荫和施氮均能显著提高闽楠叶片光合色素含量;在同一氮素水平下,随光照强度下降,闽楠幼苗叶片可溶性糖(SS)、可溶性蛋白(SP)、净光合速率(P_n)、气孔导度(G_s)、最大净光合速率(P_(max))、暗呼吸速率(R_d)、表观量子系数(AQY)均呈先增后降趋势,并在41.3%自然光照水平时最高;而同期叶片胞间CO_2浓度(C_i)、蒸腾速率(T_r)、光饱和点(LSP)、光补偿点(LCP)均呈下降趋势;闽楠幼苗的叶片PSⅡ最大光化学效率(F_v/F_m)和PSⅡ潜在活性(F_v/F_o)则随光照减弱逐渐增加。(2)同一光照水平下,随着氮素施用量增加,闽楠幼苗叶片SS、SP、光合气体交换参数、光响应曲线特征参数总体呈现先升高后降低的趋势,F_v/F_m和F_v/F_o呈先降后增趋势。(3)不同光照和氮素水平之间存在显著的互作效应,隶属函数分析结果以41.3%自然光照、0.5 mol/L纯N处理的效果最优。研究表明,闽楠幼苗为喜光耐荫植物;适宜遮荫和施氮处理组合可显著改善闽楠渗透调节能力,提高光能利用率,促进光合作用进行,而全光照、过度遮荫、缺氮、或过量施氮均不利于闽楠正常生理代谢。     

Design,synthesis, and biological evaluation of novel substituted thiourea derivatives as potential anticancer agents for NSCLC by blocking K-Ras protein-effectors interactions

Abstract

Mutation of the proto-oncogene K-Ras is one of the most common molecular mechanisms in non-small cell lung cancer. Many drugs for treating lung cancer have been developed, however, due to clinical observed K-Ras mutations, corresponding chemotherapy and targeted therapy for such mutation are not efficient enough. In this study, on the basis of the crystal structure of K-Ras, 21 analogues (TKR01–TKR21) containing urea or thiourea were rationally designed, which can effectively inhibit the lung cancer cell A549 growth. The designing of these compounds was based on the structure of K-Ras protein, and the related groups were replaced by bioisosteres to improve the affinity and selectivity. Biological testing revealed that compound TKR15 could significantly inhibit the proliferation of A549 cell with IC₅₀ of 0.21?µM. Docking analysis showed that the TKR15 can effectively bind to the hydrophobic cavity and form a hydrogen bond with the Glu37. In addition, through flow apoptosis assay and immunofluorescence staining assay, it confirmed that this compound can inhibit A549 cell proliferation with the mechanism of blocking K-Ras^G12V protein and effector proteins interactions through the apoptotic pathway. In conclusion, our studies in finding novel potent compound (TKR15) with confirmed mechanism showed great potential for further optimisation and other medicinal chemistry relevant studies.     

Hypoxia induces the activation of hepatic stellate cells through the PVT1-miR-152-ATG14 signaling pathway

Molecular and Cellular Biochemistry - Shrm4 is a protein that is exclusively expressed in polarized tissues. The physiological function of Shrm4 in the brain was required to be elucidated. Thus, we...     

SNHG16 as the miRNA let-7b-5p sponge facilitates the G2/M and epithelial-mesenchymal transition by regulating CDC25B and HMGA2 expression in hepatocellular carcinoma

Long noncoding RNAs (lncRNAs) play crucial roles in hepatocellular carcinoma (HCC). However, the underlying molecular mechanisms of small nucleolar RNA host gene 16 (SNHG16) for regulating the cell cycle and epithelial to mesenchymal transition (EMT) remain elusive. In this study, SNHG16 expression profiles of HCC tissues or cell lines were compared with those of normal tissues or hepatocyte cell line. The effect of SNHG16 knockdown in HCC cell lines was investigated by using in vitro loss-of-function experiments and in vivo nude mouse experiments. The potential molecular regulatory mechanism of SNHG16 in HCC progression was investigated by using mechanistic experiments and rescue assays. The results revealed that SNHG16 was highly expressed in HCC tissues and cell lines, which predicted poor prognosis of HCC patients. On one hand, the downregulation of SNHG16 induced G2/M cell cycle arrest, inducing cell apoptosis and suppression of cell proliferation. On the other hand, it inhibited cell metastasis and EMT progression demonstrated by in vitro loss-of-function cell experiments. Besides, knockdown of SNHG16 increased the sensitivity of HCC cells to cisplatin. For the detailed mechanism, SNHG16 was demonstrated to act as a let-7b-5p sponge in HCC. SNHG16 facilitated the G2/M cell cycle transition by directly acting on the let-7b-5p/CDC25B/CDK1 axis, and promoted cell metastasis and EMT progression by regulating the let-7b-5p/HMGA2 axis in HCC. In addition, the mechanism of SNHG16 for regulating HCC cell proliferation and metastasis was further confirmed in vivo by mouse experiments. Furthermore, these results can provide new insights into HCC treatment and its molecular pathogenesis, which may enlighten the further research of the molecular pathogenesis of HCC.     

天山雪莲LEA14基因克隆及功能分析

从天山雪莲叶片低温诱导的EST文库中获得了1个胚胎发育晚期丰富蛋白基因(LEA)cDNA全长序列。序列分析表明,该基因含有1个468bp编码155个氨基酸的开放阅读框。NCBI保守域预测此蛋白属于LEA_2家族,命名为SiLEA14。系统进化分析表明,该蛋白与北柴胡的LEA-2蛋白亲缘关系最近。荧光定量PCR结果显示,SiLEA14表达量在低温、盐和干旱胁迫条件下迅速升高。亚细胞定位结果表明,SiLEA14蛋白定位于细胞核中。利用农杆菌介导法将该基因导入烟草,测定并分析转基因植株在冷冻和盐胁迫处理下的生理指标,结果表明,SiLEA14基因在烟草中的过量表达提高了烟草的抗冻和耐盐能力。     

SNARE Proteins Synaptobrevin,SNAP-25, and Syntaxin Are Involved in Rapid and Slow Endocytosis at Synapses

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