金樱子黄酮两种提取工艺优化及比较

以金樱子果实为研究对象,用黄酮得率作为衡量提取工艺的指标。通过单因素实验、正交实验优化传统加热提法和微波助提法提取金樱子果实中黄酮的提取工艺,并比较其工艺条件。验证实验表明,传统加热提法最佳工艺测得金樱子果实黄酮得率为7.84%,相对标准偏差(RSD)为0.89%;微波助提法最佳工艺测得金樱子果实黄酮得率为9.06%,相对标准偏差(RSD)为1.01%。运用微波技术提取金樱子果实中黄酮含量减少了提取时间,提高了效率。因此,恰当的提取条件可使金樱子果实中黄酮的得率更高。     

高效液相色谱法监控左旋甲状腺素钠生产中的偶联反应

提出了用高效液相色谱法监控左旋甲状腺素钠合成关键步骤偶联反应.色谱条件:YMC-Pack Pro C18反相色谱柱(4.6 mm×100 mm,5μm);甲醇-1‰磷酸水溶液为流动相,梯度洗脱;检测波长225 nm;流速1.0 mL/min.偶联反应液在0.05～0.25 mg/mL范围内线性关系良好(相关系数r=0....     

离子液体在生物大分子中的应用研究进展

离子液体作为一种可设计性的绿色溶剂和高效催化剂,以其热稳定性好,催化性强,电导率高,溶解能力强,零蒸汽压等特性,在诸多领域具有广泛的应用。本文总结了离子液体的历史、制备、应用,主要介绍了目前离子液体在纤维素、胶原蛋白、角蛋白等生物大分子中的应用研究。同时重点介绍了离子液体在制革固废物和废水处理中的应用,并指出离子液体在皮革应用领域具有巨大前景。     

Effects of process and source on elastic modulus of single cellulose fibrils evaluated by atomic force microscopy

A test method to measure cellulose fibril elastic modulus using atomic force microscopy was used to investigate the effects of process and source on the moduli of single cellulose fibrils. The cellulose fibrils were generated from cellulose by mechanical treatments. Individual fibrils were suspended over a micro scale groove etched on a silicon wafer. A nano-scale three-point bending test was performed to obtain the elastic moduli. The results indicated that the elastic moduli of cellulose fibrils were not significantly different between 30 min and 60 min of high intensity ultrasonic treatment for Lyocell fiber, between isolation methods of ultrasonic and homogenizer treatment for pure cellulose fiber, and between different cellulose sources of pulp fibers treated by homogenizer regardless the effects of sample size coupled with inherent variation in the raw material. The elastic modulus of Lyocell fibrils with diameters from 150 to 180 nm was evaluated to be 98 ± 6 GPa. Modulus values decreased dramatically when the diameter was more than 180 nm.     

Cyanobacteria-based near-infrared light-excited self-supplying oxygen system for enhanced photodynamic therapy of hypoxic tumors

Tumor hypoxia has been considered to induce tumor cell resistance to radiotherapy and anticancer chemotherapy,as well as predisposing for increased tumor metastases.Therefore,strategies for the eradication of the hypoxic tumor are highly desirable.Photodynamic therapy(PDT)is a new technique that can be used to treat tumors using laser irradiation to photochemically activate a photosensitizer.Compared to traditional radiotherapy and chemotherapy,photodynamic therapy has many advantages,such as good selectivity,low toxicity,and less trauma and resistance.However,PDT is oxygen-dependent,and the lack of oxygen in hypoxic tumors renders photodynamic therapy ineffective.Cyanobacteria,the earliest photosynthetic oxygen-generating organisms,can utilize water as an electron donor to reduce CO₂ into organic carbon compounds along with continuously releasing oxygen under sunlight.Inspired by this,herein,cyanobacteria were used as a living carrier of photosensitizer conjugated upconversion nanoparticles(UCNP)to construct a self-supplying oxygen PDT system.Improvement in the PDT efficiency for hypoxic tumors can be achieved as a result of in situ oxygen production by cyanobacteria under near-infrared(NIR)light using UCNP as a light harvesting antenna.A successful demonstration of this concept would be of great significance and could open the door to a new generation of carrier systems in the field of hypoxia-targeted drug transport platforms.     

Oxa Analogues of Nexturastat A Demonstrate Improved HDAC6 Selectivity and Superior Antileukaemia Activity

The acetylome is important for maintaining the homeostasis of cells. Abnormal changes can result in the pathogenesis of immunological or neurological diseases, and degeneration can promote the manifestation of cancer. In particular, pharmacological intervention in the acetylome with pan-histone deacetylase (HDAC) inhibitors is clinically validated. However, these drugs exhibit an undesirable risk-benefit profile due to severe side effects. Selective HDAC inhibitors might promote patient compliance and represent a valuable opportunity in personalised medicine. Therefore, we envisioned the development of HDAC6-selective inhibitors. During our lead structure identification, we demonstrated that an alkoxyurea-based connecting unit proves to be beneficial for HDAC6 selectivity and established the synthesis of alkoxyurea-based hydroxamic acids. Herein, we report highly potent N-alkoxyurea-based hydroxamic acids with improved HDAC6 preference compared to nexturastat A. We further validated the biological activity of these oxa analogues of nexturastat A in a broad subset of leukaemia cell lines and demonstrated their superior anti-proliferative properties compared to nexturastat A.     

Enantioselective Cascade Biocatalysis for Deracemization of Racemic β-Amino Alcohols to Enantiopure (S)-β-Amino Alcohols by Employing Cyclohexylamine Oxidase and ω-Transaminase

Optically active β-amino alcohols are very useful chiral intermediates frequently used in the preparation of pharmaceutically active substances. Here, a novel cyclohexylamine oxidase (ArCHAO) was identified from the genome sequence of Arthrobacter sp. TYUT010-15 with the R-stereoselective deamination activity of β-amino alcohol. ArCHAO was cloned and successfully expressed in E. coli BL21, purified and characterized. Substrate-specific analysis revealed that ArCHAO has high activity (4.15 to 6.34 U mg⁻¹ protein) and excellent enantioselectivity toward the tested β-amino alcohols. By using purified ArCHAO, a wide range of racemic β-amino alcohols were resolved, (S)-β-amino alcohols were obtained in >99 % ee. Deracemization of racemic β-amino alcohols was conducted by ArCHAO-catalyzed enantioselective deamination and transaminase-catalyzed enantioselective amination to afford (S)-β-amino alcohols in excellent conversion (78–94 %) and enantiomeric excess (>99 %). Preparative-scale deracemization was carried out with 50 mM (6.859 g L⁻¹) racemic 2-amino-2-phenylethanol, (S)-2-amino-2-phenylethanol was obtained in 75 % isolated yield and >99 % ee.     

微生物菌种选育中基因组重排技术应用的研究进展

基因组重排(genome shuffling)技术是通过传统诱变育种结合原生质体融合技术开发出的一种新型微生物菌种选育和改良技术,具有易操作、效率高和适用广等特点。本文对基因组重排技术的原理、操作过程及其在增加次生代谢产物产量、增强菌株耐受性和提高底物利用能力等方面的应用进行了综述。     

6-Azauridine Induces Autophagy-Mediated Cell Death via a p53- and AMPK-Dependent Pathway

6-Azauridine (6-AZA), a pyrimidine nucleoside analogue, is known to exhibit both antitumor and antiviral activities. Although 6-AZA was discovered more than 60 years ago, the cellular effects of this compound are yet to be elucidated. Here, we report that 6-AZA regulates autophagy-mediated cell death in various human cancer cells, where 6-AZA treatment activates autophagic flux through the activation of lysosomal function. Furthermore, 6-AZA exhibited cytotoxicity in all cancer cells studied, although the mechanisms of action were diverse. In H460 cells, 6-AZA treatment induced apoptosis, and the extent of the latter could be reduced by treatment with chloroquine (CQ), a lysosomal inhibitor. However, 6-AZA treatment resulted in cell cycle arrest in H1299 cells, which could not be reversed by CQ. The cytotoxicity associated with 6-AZA treatment could be linearly correlated to the degree of autophagy-mediated cell death. In addition, we demonstrated that the cytotoxic effect of 6-AZA was dependent on AMPK and p53. These results collectively indicate that autophagy-mediated cell death triggered by 6-AZA contributes to its antitumor effect.