Screening Antibacterial Constituents of Scutellaria Radix Based on Spectrum-Effect Relationships Between HPLC Fingerprints and the Inhibition of Oral Bacteria.

Scutellaria Radix (SR) is a widely used traditional Chinese medicine in clinics for the therapy of upper respiratory tract infectious diseases. Modern pharmacological investigations indicate that SR exerts a significant bacteriostatic effect on different oral bacteria, but few studies have systematically investigated the main active constituents of SR causing this activity. Spectrum-effect correlation analysis was applied to screening anti-oral-microbial constituents from SR. The aqueous extract of SR was divided into fractions of different polarity and the active fraction was screened using the agar diffusion method. Eighteen batches of SR were further prepared and the chromatography fingerprint was established using high-performance liquid chromatography. The antibacterial activities of these constituents were examined against different oral bacteria. Finally, the spectrum-effect relationship between the fingerprint and those antibacterial effects was analyzed by gray correlation analysis and partial least squares regression. Five active constituents were screened out and their antibacterial activity was systematically confirmed by a knockout/in strategy combined with a biofilm extraction method, which indicated that these five compounds were responsible for the antibacterial activity of SR. These results form the basis for further development and improved quality control of SR in the treatment of oral diseases.

Comprehensive treatment strategy for diesel truck exhaust.

At present, diesel vehicles still play an irreplaceable role in the traditional energy field in China. Diesel vehicle exhaust contains hydrocarbons, carbon monoxide, nitrogen oxides, and particulate matter, which can lead to haze weather, photochemical smog, and the greenhouse effect; endanger human health; and damage the ecological environment. In 2020, the number of motor vehicles in China reached 372 million, and the number of automobiles reached 281 million, of which 20.92 million are diesel vehicles, accounting for only 5.6% of the number of motor vehicles and 7.4% of the number of automobiles. Nevertheless, diesel vehicles emitted 88.8% of nitrogen oxides and 99% of particulate matter in total vehicle emissions. Diesel vehicles, especially diesel trucks, have become the top priority of motor vehicle pollution control. However, there are few reviews on the comprehensive treatment of diesel vehicle exhaust. This review provides an overview of exhaust gas composition, hazards, and treatment techniques. Phytoremediation, three-way catalytic conversion, rare earth catalytic degradation, and nanoscale TiO2 catalytic degradation are briefly described.

Design, synthesis, and anticancer activity of three novel palbociclib derivatives.

Cancer is one of the most serious diseases threatening human health, so it is particularly important to develop effective tumor-targeting drugs. As the first CDK4/6 inhibitor, palbociclib effectively inhibits tumor proliferation by blocking the cell cycle to the G1 phase. 10-HCPT is a Topo I inhibitor; however, its clinical application has been greatly limited due to its high toxicity. Based on the successful development of double target inhibitors, three novel palbociclib derivatives (HP-1, HP-2, and HP-3) were designed and synthesized from Palbociclib and 10-HCPT, and their biological activities were investigated. At first, the possible binding sites of the three compounds to Topo I and CDK4/6 were predicted by molecular docking. Then, we evaluated the anti-proliferative effects of the three palbociclib derivatives. In general, human lung cancer cells were more sensitive to HP-1, HP-2, and HP-3, especially NCI-H460. In addition, cell cycle arrest and apoptosis induction were investigated by flow cytometry. The three palbociclib derivatives, especially HP-1, had obvious cell cycle arrest phenomenon on NCI-H460 cells and induced apoptosis of NCI-H460 cells significantly. In the end, it was proved that these three drugs had obvious cyclin-dependent kinase inhibitory activities. In short, all the data showed that HP-1, HP-2, and HP-3 could play anti-cancer roles by acting on dual targets and had the characteristics of high efficiencies and low toxicities, which opened up a new idea for the study of palbociclib derivatives.

Detection of Amino Acids and Polypeptides by Electrospray Ionization-Ion Mobility Spectrometry / 分析化学

The electrospray ionization-ion mobility spectrometric (ESI-IMS) technique has the potential as an analytical separation tool in analyzing polypeptides and amino acids for fast screening unknown samples in anti-chemical and biological terror attacks. A method for detecting several polypeptides and amino acids was developed based on ESI-IMS using air as drift gas at room temperature. The ion mobility of four amino acids and two polypeptides dissolved in methanol was determined on the system at elution rate of 2 mL/ min. The spectra of these compounds had characteristics of finger-printing maps. The limit of detection of this instrument for Substance P could reach 855 ng / mL in 1 min. The results showed that a small, self-contained ESI-IMS instrument with reservoirs of air could be used to quickly detect and accurately identify polypeptides and amino acids.

One-time ray-tracing optimization method and its application to the design of an illuminator for a tube photo-bioreactor.

This study details a one-time ray-tracing optimization method for the optimization of LED illumination systems [S.-C. Chu and H.-L. Yang, "One-time ray-tracing method for the optimization of illumination system," in Proceedings of International Conference on Optics in Precision Engineering and Nanotechnology (icOPEN, 2013), 87692M]. This method optimizes the performance of illumination systems by modifying the light source's radiant intensity distribution with a freeform lens, instead of modifying the illumination system structure. Because illumination system structures are unchanged in the design process, a designer can avoid the common problems faced when designing illumination systems, i.e., the repeated and time-consuming ray-tracing process when optimizing the illumination system parameters. The easy approaches of the proposed optimization method to sample the target illumination areas and to divide the light source radiant intensity distribution make the proposed method can be applied to both direct-lit and non-direct-lit illumination systems. To demonstrate the proposed method, this study designs an illuminator for a tube photo-bioreactor using the proposed one-time ray-tracing method. A comparison shows that in the designing of the photo-bioreactor, tracing all rays one time requires about 13 hours, while optimizing the light source's radiant intensity distribution requires only about twenty minutes. The considerable reduction in the ray-tracing time shows that the proposed method is a fast and effective way to design illumination systems.

The role of SOCS2 in recombinant human growth hormone (rhGH) regulating lipid metabolism in high-fat-diet-induced obesity mice.

In addition to regulate body growth and development process, growth hormone (GH) also involved in lipid metabolism, decreasing fat mass and improving lipolysis. To normal mice, GH could reduce their fat content, but events turned uncertain coming to the pattern of feeding high-fat-diet. In order to investigate the role of GH in adipogenesis of mice with high-fat-diet, the high-fat-diet feeding mice were randomly assigned into three groups and treated with recombinant human growth hormone (rhGH) and the somatostatin analogue octreotide respectively. Results demonstrated that both rhGH and octreotide could reduce the body weight but the trends diminished in the end. HDL-C level was increased in octreotide treated groups but the activity of lipase was increased significantly in both two groups. RhGH remarkable increased the expression of SOCS2, FAS (P < 0.01) and SREBP-1c (P < 0.05), decreased the expression of SOCS1, SOCS3 (P < 0.05) and HSL (P < 0.01) in subcutaneous fat mass. In visceral fat tissue, all genes were increased except SOCS2 (P < 0.01), at the same time the visceral fat mass was decreased. The protein phosphorylation of JAK2 and STAT5 which were treated with octreotide were increased in subcutaneous fat, visceral fat and liver (P < 0.01) and were increased significant in visceral fat by rhGH treated (P < 0.01). In liver, only JAK2 protein phosphorylation was raised (P < 0.01). In conclusion, rhGH and octreotide could decrease the whole body mass before 6 days; the trend was weaken in later period with high-fat-diet. RhGH could increase the subcutaneous fat mass and reduce the visceral fat mass, and SOCS2 might be involved in regulation of the mechanism through JAK2/STAT5 signaling pathway.

Effect of suppressor of cytokine signaling 2 (SOCS2) on fat metabolism induced by growth hormone (GH) in porcine primary adipocyte.

SOCS2, a member of suppressor of cytokine signaling (SOCS) family, is a negative regulator of the signal pathway Janus kinase/signal transducers and activators of transcription (JAK/STAT). Growth hormone (GH) could stimulate lipolysis in adipose tissue. To demonstrate the specific influence of SOCS2 on porcine adipocytes differentiation and lipid metabolism induced by GH, we induced porcine primary adipocytes with 500 ng/ml GH and then tested the triglyceride (TG) accumulation and mRNA expressions of crucial genes in lipid metabolism like peroxisome proliferator-activated receptor gamma (PPARγ), fatty acid synthase (FAS), adipose triglyceride lipase (ATGL), hormone-sensitive lipase (HSL), SOCS2 and SOCS3. Then we retested these genes expressions in different time point after further treatment that over expressed SOCS2 in primary adipocytes and treated with 500 ng/ml GH. Results showed 500 ng/ml GH significantly restrained the porcine primary adipocytes differentiation. Specifically, 0.5 h after the induction with GH, accumulation of TG began to increase, and turned down since 8 h after. GH could promote PPARγ and FAS expressions during earlier stage (0-1 h), restrain from 4 h. However, ATGL and HSL mRNA expressions were stabile increasing. The expression of SOCS2 increased steadily after GH stimulation while SOCS3 expression was instantaneous rise. Overexpression of SOCS2 significantly decreased GH-induced the increase of PPARγ, FAS, ATGL and HSL mRNA expressions in earlier stage (0-1 h), as well as FAS and ATGL protein expression. Otherwise SOCS2 overexpression significantly decreased signal transducers and activators of transcription 3 (STAT3), signal transducers and activators of transcription 5 (STAT5) mRNA expressions and tyrosine phosphorylation levels with GH stimulation. At the same time SOCS3 mRNA kept in a lower level in Ad-SOCS2 transfected adipocytes. In conclusion, SOCS2 might be an important negative regulator of GH signaling in porcine adipocytes, which would provide the ground work for the mechanism of SOCS2 regulation fat metabolism.