Synthesis,Anticancer Activity,Structure-Activity Relationship and Mechanistic Investigations of Falcarindiol Analogues

Forty samples of optically active falcarindiol analogues are synthesized by using the easily available C2 symmetric (R)- and (S)-1,1’-binaphth-2-ol (BINOL) in combination with Ti(OⁱPr)₄, Zn powder and EtI. Their anticancer activities on Hccc-9810, HepG2, MDA-MB-231, Hela, MG-63 and H460 cells are assayed to elucidate their structure-activity relationships. These results showed that the falcarindiol analogue (3R,8S)- 2 i with the terminal double bond has the most potent anti-proliferation effect on Hccc-9810 cells with IC₅₀ value of 0.46 μM. The falcarindiol analogue (3R,8S)- 2 i can induce obvious Hccc-9810 cell apoptosis in a concentration-dependent manner by Hoechst staining and flow cytometry analysis. The proposed mechanism suggests that the falcarindiol analogue (3R,8S)- 2 i increases LDH release and MDA content, and reduces the levels of SOD activity, which lead to the accumulation of oxidative stress and induce apoptosis in Hccc-9810 cells.     

Highly stable γ-NiOOH/ZnCdS photocatalyst for efficient hydrogen evolution

It is extremely desirable to develop high hydrogen evolution activity and stable visible-light-driven photocatalysts. The sluggish oxidation process and holes accumulation are the main obstacles to high catalysis activity and photo-stability. An efficient γ-NiOOH/ZnCdS photocatalyst was prepared by in-situ hydrothermal method. The γ-NiOOH nanosheets distribute on ZnCdS nanospheres surface and accelerate holes transfer. The hydrogen evolution rate is up to 48.60 mmol g^?1 h^?1 under visible-light illumination (λ = 400–780 nm), about 10.8 times of pure ZnCdS (4.50 mmol g^?1 h^?1) and 1.8 times of general β-NiOOH modified ZnCdS (27.40 mmol g^?1 h^?1). And apparent quantum yield of γ-NiOOH/ZCS-100 is up to 18.23% (400 nm). The carrier lifetime extends from 5.50 ns (ZnCdS) to 6.10 ns (γ-NiOOH/ZCS), examined by steady photoluminescence and time-resolved photoluminescence. Moreover, the γ-NiOOH/ZCS photocatalyst has exhibited excellent photo-stability even after one-year of storage. The γ-NiOOH nanosheets can be an excellent co-catalyst on accelerating both holes transfer and oxidation process for high photo-stability and photo-activity.     

Comparison of γ-aminobutyric acid accumulation capability in different mung bean (Vigna radiata L.) varieties under heat and relative humidity treatment,and its correlation with endogenous amino acids and polyamines

In this study, the accumulation of GABA and its inherent factors across different varieties of mung bean (Vigna radiata L.) in response to heat and relative humidity (HRH) were investigated. Results showed the average GABA content in mung bean varieties was increased 7.52 times following HRH treatment, and the black mung bean variety (A8) exhibited the highest GABA accumulation capability (1.76–84.57 mg per 100 g DW). From the perspective of GABA shunt metabolites, the free glutamic acid content of mung beans significantly decreased (P < 0.05) after HRH treatment and presented a significant correlation (P < 0.05) with GABA content. In polyamine degradation pathway, although the average levels of spermine and spermidine of mung bean varieties significantly decreased (P < 0.05) after HRH treatment, no significant correlation with GABA content was identified. Hence, the GABA accumulation was predominantly attributed to GABA shunt. Besides, free amino acids including glutamic acid, serine, ornithine, arginine and glycine in mung beans showed a significant positive correlation (P < 0.05) with GABA content and increment following HRH treatment, which suggested that mung beans enriched in these free amino acids might accumulate higher amounts of GABA after HRH treatment and be useful for industrial applications.     

Btk/JAK3双靶点共价抑制剂的设计、合成及其活性研究

布鲁顿式酪氨酸激酶(Btk)和两面神激酶3(JAK3)均是自身免疫性疾病和血液系统恶性肿瘤的潜力靶标。以4-氯吡咯并嘧啶为原料,经7步反应合成了一系列7H-吡咯并[2,3-d]嘧啶-4-胺衍生物,其结构经¹HNMR、¹³CNMR和MS(ESI)分析证实。体外依次考察了所得化合物分别对Btk和JAK3激酶的活性、以及对部分B淋巴细胞瘤细胞系的抗增殖活性。结果表明,四氢吡咯烷基取代的衍生物NB1~4对Btk(IC₅₀<3 nmol/L)和JAK3(IC₅₀<165 nmol/L)均能有效抑制,其余化合物只对Btk显示抑制效果;而且NB2和NB4对所测试的多种B细胞淋巴瘤细胞系的抗增殖活性均优于阳性对照泛激酶抑制剂依鲁替尼及Btk单靶点抑制剂。其中,对Jeko-1细胞的抑制能力最佳(IC₅₀<3μmol/L),其次是OCI-LYI(IC₅₀<4μmol/L)、SUDHL-6(IC₅₀<6μmol/L)和HBL-1^*(IC₅₀<6.5μmol/L),最差为SUDHL-4细胞(IC₅₀<11μmol/L)。这些发现可为开发B细胞淋巴瘤的多靶点药物提供新的思路。     

磨削表面粗糙度对γ-TiAl合金抗弯强度的影响

为了研究表面加工质量对硬脆性高温合金抗弯性能的影响,对不同磨削表面粗糙度的全片层γ-TiAl(Ti-47.5Al-2.5V-1.0Cr)合金进行了抗弯性能试验,分析了表面粗糙度对其抗弯强度的影响规律。试验结果表明,随着表面粗糙度的增大,全片层γ-TiAl合金的抗弯强度明显降低。结合断裂形貌图分析了全片层γ-TiAl合金组织中裂纹的萌生、扩展及最终发生宏观断裂的方式,全片层γ-TiAl合金裂纹大多起裂于因加工纹理引起的应力集中区域附近的片层间,并优先在层间扩展,最终的断裂形式多为穿层的脆性瞬断。     

Isolation and characterization of components responsible for neuroprotective effects of Allium cepa outer scale extract against ischemia reperfusion induced cerebral injury in mice

The antioxidant-mediated neuroprotective effect of Allium cepa outer scale extract (ACE) in mice with cerebral ischemia-reperfusion (I-R) injury was demonstrated in our earlier work. The current investigation aimed at establishing the bioactive component(s) responsible for this activity. Thus ACE was fractionated into ethyl acetate (EF) and aqueous (AF) fractions. These fractions were evaluated against cerebral I-R injury in mice. I-R injury in mice was induced by bilateral common carotid artery occlusion followed by 24 hr reperfusion. Memory, sensorimotor functions, cerebral infarct size, and oxidative stress were measured to address the neuroprotective mechanism of test substances. EF showed marked improvement of memory and sensorimotor functions by reducing brain oxidative stress and infarct size in mice after I-R injury. The bioactive EF was subjected to chromatographic (HPLC-PDA, HPLC-MS, preparative HPLC) and spectroscopic studies to isolate and identify the neuroprotective compounds. This lead to separation of three components, namely quercetin, quercetin 4′-O-glucoside, and the remaining fraction, from EF. The separated components were biologically evaluated. These components showed improvement in mice with I-R injury. But, EF displayed more marked neuroprotective effects as compared to the isolated components. The distinct neuroprotective outcome of EF may be credited to the synergistic action of compounds present in EF. Further studies such as evaluation of neurotoxic effects and other possible neuroprotective mechanisms are required to develop EF as a neuroprotective drug.     

PCR-DGGE技术检测速冻饺子馅料中微生物区系

以速冻饺子为研究对象,对速冻饺子冻前的微生物多样性进行研究分析,为速冻饺子馅料的存放期限及防腐技术提供参考,避免后期出现卫生问题。利用传统分离培养的方法,对饺子肉馅中的细菌进行分离,得到30株纯菌株。通过菌株形态学鉴定、基因组DNA提取、聚合酶链式反应(polymerase chain reaction,PCR)扩增及16S rDNA测序及序列比对分析来鉴定菌株的属种、构建种群结构进化树。结果表明:30株纯菌株中有14个属,22个种,优势菌分布在γ-变形菌纲中的假单胞菌属。