The protective effect of terpinen-4-ol on inflammatory injury of VSMCs induced by high glucose through improving autophagic flux disorder / 中国药理学通报

Aim To investigate the effect of terpinen-4-ol (T40) on inflammatory injury of vascular smooth muscle cells (VSMCs) induced by high glucose based on the improvement of autophagic flow disorder and involved molecular signals. Methods The scratch test was used to analyze the migration ability of VSMCs, the levels of IL-1β and IL-6 in cell culture supernatant were measured by ELISA, the expression levels of inflammation-related proteins NF-κb p65, p-NF-κb p65, IL-1β, IL-18 and autophagy-related proteins p62, LC3-HYLC3-I, Beclinl, p-Beclinl were de-tected by Western blot. Results T40 inhibited migration of VSMCs induced by high glucose, reduced the secretion and release of pro-inflammatory factors IL-1β and IL-6, inhibited the expression of p-NF-κb p65/ NF-κb p65, IL-1β, IL-18, downregulated the expression of p62, LC3-TJ/LC3- I and p-Beclinl at same time. After interfering the autophagic flux of VSMCs with autophagy inhibitor chloroquine (CQ) , T40 pre-treatment significantly inhibited the protein expression levels of the above inflammatory factors and autophagy-related signals which mediated by CQ. Conclusion T40 inhibits the inflammatory injury of VSMCs induced by high glucose through improving the autophagic flow disorder.

Research progress of lipomics in liver diseases / 中国药理学通报

Liver disease is a kind of common and frequently occurring disease, which seriously threatens human life and health. The study of liver disease has become a hotspot and difficulty in the field of organic diseases. In recent years, scholars have found a close relation between liver disease and the metabolism of lipid compounds in body. Lipomics, an important branch of metabolomics, can evaluate liver diseases by analyzing the level of lipid changes in the body, find biomarkers of liver diseases, and study the possible mechanism of liver diseases. It plays an important role in the study of liver diseases. In order to provide reference for further study of liver diseases and their clinical treatment, the research methods of lipomics have been reviewed, and the application of lipomics in liver diseases summarized and analyzed based on different types of liver diseases in this paper.

Research Progress in Treatment of Chemical Liver Injury with Chinese Medicine Based on Metabolomics / 中国实验方剂学杂志

Liver， as a critical organ of metabolism and detoxification， can be damaged by viral infection， drug abuse， and heavy drinking. Liver diseases pose a serious threat to people's health and life in China.At present， drug therapy has been primarily adopted clinically in the treatment of the liver injury.In-depth investigation of the mechanism of liver-protective drugs is of great significance to the prevention and treatment of clinical liver diseases.In recent years， with the development of the medical industry in China， an increasing number of studies have focused on the treatment of liver injury with Chinese medicine.Compared with western medicine， Chinese medicine is advantageous in few side effects and overall regulation， which plays a pivotal role in liver protection.However， its underlying mechanism in liver protection still needs to be further studied due to its complex compositions and diverse targets.Metabolomics， a new approach to studying the metabolic pathway of biological systems， provides integral and systematic views in the investigation of liver protection with Chinese medicine. By virtue of metabolomics， the mechanism of Chinese medicine in multi-target and multi-pathway liver protection can be analyzed comprehensively， and the corresponding biomarkers can also be screened out. The authors analyzed the studies of the treatment of chemical liver injury models induced by carbon tetrachloride （CCl4）， dimethylnitrosamine （DMN）， α-naphthyl isothiocyanate （ANIT）， and alcohol by Chinese medicinal compounds， single herbal medicines， and monomers of Chinese medicine based on metabolomics， and summarized the biomarkers and related metabolic pathways of Chinese medicine in the intervention of each type of liver injury， aiming at providing a reference for the further research and clinical application in the treatment of different types of liver injuries by Chinese medicine.

Research progress on hepatotoxicity of traditional Chinese medicine based on metabonomics / 中国中药杂志

With the continuous development of Chinese medicine, traditional Chinese medicine(TCM) has been widely used in the treatment of diseases and health care. At the same time, the toxic and side effects of TCM have been gradually concerned. The liver, as an important place for drug metabolism, is a major target organ for drug toxicity. Clinical reports on liver injury caused by TCM are common, and the problem of liver toxicity of TCM has become an important reason to limit the internationalization of TCM. Metabono-mics is a newly booming subject to study the metabolic pathway of biological system. It shows integrity and systematicness in the study of hepatotoxicity of TCM, which provides a new technical method for finding the early biomarkers of liver injury of TCM and exploring the mechanism of hepatotoxicity of TCM. In this paper, the methods of metabonomics in the study of hepatotoxicity of TCM, as well as the research progress of hepatotoxicity monomer, extract and attenuation of hepatotoxic TCM based on metabonomics were reviewed in order to provide reference for the further study of hepatotoxicity of TCM.

Preparation of Oxymatrine Phospholipid Complex Solid Lipid Nanoparticles Lyophilized Powder and Evaluation of Its Quality / 中国实验方剂学杂志

Objective: To prepare oxymatrine phospholipid complex solid lipid nanoparticles(OMT-PC-SLN) lyophilized powder and evaluate its pharmaceutical properties. Method: Pseudo-ternary phase diagram was employed to optimize the formula of microemulsion;single factor experiments were adopted to optimize the formulation process of OMT-PC-SLN lyophilized powder with encapsulation efficiency as index;the morphology of this preparation was observed by transmission electron microscope(TEM).The particle size was measured by particle size analyzer and the in vitro release performance of OMT-PC-SLN lyophilized powder was examined. Result: Optimal formulation process was as following:taking soybean phospholipid and polyethylene glycol 15-hydroxystearate(Kolliphor HS 15) as the emulsifier,ethanol as co-emulsifier,ratio of emulsifier to co-emulsifier(Km)=3:2,oil phase:(emulsifier+co-emulsifier)=1:9,oxymatrine phospholipid complex-stearic acid-soybean phospholipid-Kolliphor HS 15-ethanol(30:100:180:360:360);taking 50 mL of 4%mannitol solution as the external aqueous phase,ice bath stirring at 1 000 r·min-1 and solidifying for 1 h,precooled at -20℃ for 24 h,took out and dried for 24 h.OMT-PC-SLN lyophilized powder was spherical in appearance with encapsulation efficiency of (38.09±1.24)%,average particle size of 785.5 nm,polydispersity coefficient(PDI) of 0.456 and the Zeta potential of -24.82 mV.The cumulative release rates of OMT-PC-SLN lyophilized powder were 72.63%at 2 h and 98.42%at 12 h;the cumulative release rate of oxymatrine(crude drug) was 98.60%at 2 h. Conclusion: This optimized formulation process of OMT-PC-SLN lyophilized powder is stable with good repeatability;compared with oxymatrine,OMT-PC-SLN lyophilized powder has a certain sustained-release effect.

Analysis of Pharmacokinetic Behavior of Five Components in Qingkailing (Lyophilized) for Injection in Normal Rats and Cerebral Ischemia Rats by UPLC-MS/MS / 中国实验方剂学杂志

Objective: To establish a UPLC-MS/MS analysis method for determination of baicalin, geniposide, chlorogenic acid, cholic acid and hyodeoxycholic acid in Qingkailing (lyophilized) for injection in rat plasma, and to investigate the pharmacokinetic behavior of this preparation in normal and cerebral ischemic rats. Method: Rats were randomly divided into normal group and cerebral ischemia model group. The rat model of cerebral ischemia was established by suture embolization. The rats were given by intraperitoneal injection, and normal saline was used as the solvent. Blood samples were taken at the corresponding time points. After treatment, UPLC-MS/MS was used to determine the blood concentration of five components. The main detection conditions were mobile phase of 0.1%formic acid aqueous solution-acetonitrile for gradient elution (0-0.25 min, 90%A; 0.25-1 min, 90%-75%A; 1-2 min, 75%-50%A; 2-2.6 min, 50%-45%A; 2.6-2.65 min, 45%-90%A; 2.65-4.0 min, 90%A), the flow rate of 0.4 mL·min-1, the column temperature at 40℃, electrospray ionization under negative ion mode. The pharmacokinetic parameters were fitted and the bioavailability was calculated, the differences of treatment process of five components from Qingkailing (lyophilized) for injection in normal and cerebral ischemic rats were analyzed. Result: Compared with the normal group, the area under the curve (AUC0-t) of geniposide in rats from cerebral ischemia model group decreased significantly after intraperitoneal injection of Qingkailing (lyophilized) for injection (PTmax) of chlorogenic acid in rats from cerebral ischemia model group was significantly earlier than that in the normal group (PConclusion: Qingkailing (lyophilized) for injection has a certain difference in the treatment process between normal and cerebral ischemic rats, which has certain guiding significance for the clinical treatment of cerebral ischemic diseases with this preparation.