Galli Gigerii Endothelium Corneum (GGEC) is a commonly used traditional Chinese medicine for digestion. Its odor is unpleasant, which decreases children's compliance with taking this traditional medicine. Traditional processing methods utilize heat processing methods such as stir-frying and vinegar processing to deodorize the medicine, but this affects the activity of digestive enzymes, so there is a need to find a new method for removing the fishy odor while retaining the beneficial effect of GGEC. Here we have developed the use of supercritical CO₂ low-temperature fluid extraction to eliminate the odor while retaining the medicinal benefits. Headspace-solid-phase microextraction-gas chromatography-triple quadrupole mass spectrometry (HS-SPME/GC-QQQ-MS/MS) combined with the gas activity value method was used to determine compositional differences in the product before and after supercritical CO₂ extraction and separation. Then, based on the sensory evaluation of volunteers, combined with the analysis of volatile components, the fishy odor intensity and the types of fishy odorants were compared between the raw product, stir-fried product, vinegar product and the supercritical CO₂ extract. Pepsin and amylase activity were used to compare the differences in the digestive enzyme activities with the four forms of GGEC, and Fourier transform infrared spectroscopy (FT-IR) was used to compare the differences in the structure. We compared the content of total amino acids, digestive amino acids and bitter amino acids, and an animal model of delayed gastric emptying in mice with soybean oil, based on a phenol red indicator, was used to determine differences in the efficacy of gastric emptying in vivo. The results show that the fishy odor of GGEC powder is significantly reduced after supercritical extraction, and the substances that contribute the fishy odor are only 12.8% of the raw material. The results of FT-IR analysis show that the supercritical extract of GGEC is not changed in its material structure compared with the raw product. The digestive enzyme activity titers showed that amylase and pepsin activity in the raw products are about 3.9 and 1.4 times higher than those of stir-fried products and vinegar products. The activity titers of amylase and pepsin in the supercritical CO₂extracts are about 2.7 and 1.3 times higher than those of stir-fried products and vinegar products, and there was no significant difference in the content of digestive-promoting amino acids in the four types of GGEC. The in vivo validation experiment showed that the average gastric emptying rates of the mice in the raw product group, the supercritical extract group, the stir-fried product group, and the vinegar product group were 69%, 59%, 40% and 51%, respectively. Compared with the stir-frying method and the vinegar-simmering method, the supercritical CO₂ fluid extraction method retained the gastric emptying effect of GGEC. In general, the supercritical CO₂ fluid low-temperature extraction method removes the fishy odor of GGEC as compared with the traditional stir-frying method and vinegar method, and retains the biologically active components and the effect on digestion of GGEC.

Identification of metabolites of Danshen-Honghua herb pairs in isolated rat intestinal flora based on HPLC-Q-TOF-MS/MS technique. By incubating enterobacteria in isolated rats as well as inactivated enterobacteria in the incubation solution. The extracts of Danshen-Honghua herb pairs were added separately and co-incubated under anaerobic conditions. Animal experiments and protocols were approved by the Laboratory Animal Ethics Committee of Shaanxi University of Traditional Chinese Medicine (approval number: TCM-2020-030-E05). A total of 14 compounds, including 5 prototypes and 9 metabolites, were identified in the isolated rat intestinal incubation fluid. In contrast, no metabolites were detected in the inactivated enterobacterial fluid, except for the prototype component. The results showed that the main components of the Danshensu, salvianolic acid B, rosmarinic acid, lithospermic acid, and hydroxysafflor yellow A, could be metabolized by the intestinal flora, and these active ingredients were mainly metabolized in the rat intestinal flora in isolation by hydroxylation, decarboxylation, deoxygenation, decarboxylation and dehydration in phase Ⅰ, sulfate esterification and methylation in phase Ⅱ. This proved that the Danshen-Honghua herb pair could be transformed into various metabolites by the action of rat intestinal flora, further clarifying the role of intestinal flora in the metabolic transformation of the active ingredients of Chinese medicine and laying the foundation for perfecting the potent substances of the pair.

The purpose of this study was to explore the mechanism of Sanzi Yangqin decoction (SYD) from the perspective of hypothalamic metabonomics to prevent the development of prehypertension (PHT) and excessive phlegm-dampness syndrome in rats. WKY rats were randomly divided into a normal group, a model group and a SYD group. The high-fat + high-salt method was used to induce PHT and excessive phlegm-dampness syndrome in the model and SYD rats. Different doses of SYD were used as an intervention over 8 weeks. Food consumption, weight, height, blood lipid and blood pressure were recorded for each group. The results show that, compared with the model group, the diet, weight and blood pressure of rats in SYD group decreased. Metabolites in the hypothalamus which differed in their expression between the three groups were identified and analyzed by LC-MS and the metabolic pathways were then determined. Fourteen metabolites in the hypothalamus were down-regulated and were mainly related to amino acid metabolism, glutathione metabolism, sphingolipid metabolism and glyceride metabolism, suggesting that SYD might alter hypothalamic dietary behavior, thereby affecting amino acid metabolism and energy metabolism. This study was approved by the Animal Ethics Review Committee of Shandong University of Traditional Chinese Medicine (approval number: SDUTCM20211103001).

We have identified anti-inflammatory quality markers (Q-markers) of Jiangzhenxiang. The chemical components of Jiangzhenxiang were identified by mass spectrometry and the substances that contribute to its anti-inflammatory activity, their targets and signaling pathways were analyzed by network pharmacology to identify potential Q-markers of the anti-inflammatory action of Jiangzhenxiang. The potential Q-markers were verified by high performance liquid chromatography, and in vitro experiments verified the anti-inflammatory activity and the target of the potential Q-markers. The experimental scheme was approved the Guangxi University of Chinese Medicine Institutional Animal Ethical and Welfare Committee. The results show that 31 chemical components were identified by mass spectrometry from the Jiangzhenxiang extract. Through network pharmacological screening, 727 component targets, 422 disease targets and 110 targets including prostaglandin G/H synthase 2 (PTGS2) were obtained. These targets were mainly enriched in 498 biological processes including inflammatory response and response to lipopolysaccharide, with 101 pathways that included the TNF signaling pathway, toll-like receptor signaling pathway and others. Isorhamnetin, formononetin, naringenin, glycitein, ursolic acid and oleanolic acid were detected by high performance liquid chromatography. Jiangzhenxiang medicated serum and 6 components thereof could significantly reduce the content of nitric oxide, interleukin-6 (IL-6) and tumor necrosis factor-α in RAW264.7 cells induced by lipopolysaccharide (P < 0.01 or P < 0.05). These six components are regarded as the potential anti-inflammatory Q-markers of Jiangzhenxiang. Isorhamnetin was screened and verified from the 6 potential Q-markers as an inhibitor of PTGS2 by molecular docking and in vitro cyclooxygenase 2 (COX-2) activity assay. The half-inhibitory concentration of isorhamnetin was 9.55μmol·L^-1. In summary, extracts of Jiangzhenxiang showed significant in vitro anti-inflammatory actions. The anti-inflammatory mechanism of Jiangzhenxiang appears to be related to regulation of TNF signaling pathway and Toll-like receptor signaling pathway meditated by IL-6, RAC alpha serine/threonine protein kinase, PTGS2 and other targets. Isorhamnetin, formononetin, naringenin, glycitein, ursolic acid and oleanolic acid could be regarded as the Q-markers of Jiangzhenxiang. Isorhamnetin appears to act as a COX-2 inhibitor.

Acute lung injure (ALI) is a severe diffused lung disease, which is caused by pathogen-induced infections, inhalation of irritates, and so on. It could lead to acute respiratory distress syndrome (ARDS). Long oil (LO) is a lipidic mixture extracted from multiple medicinal animals and plants. It has been used for clinical wound repair. Here, an O/W LO emulsions (LOE) was prepared, which was composed of LO, Tween-80, propylene glycol, xanthan gum, and water. The droplet size of LOE was 671.63 ± 7.21 nm, and the zeta potential was-17.8± 1.26 mV. The size of LOE was small and homogenous, and the stability was satisfied. The aerosols had an aerodynamic diameter of 2.25 ± 0.05 μm after atomization of LOE with a vibrating screen atomizer, where the percentage of particle sizes within 1-5 μm was 81.40%, indicating effective deep lung deposition and suitable pulmonary inhalation. The safe dose of LOE was high to 12.50 μg·mL^-1 on human embryonic lung fibroblast MRC-5 cells. In the range of 0.02-2.50 μg·mL^-1 of LOE, the proliferation and migration of mouse fibroblast L929 cells were improved. Animal experiments were approved by the Ethics Committee of Institute of Radiation Medicine, Academy of Military Medical Sciences, and the experiments were conducted by relevant guidelines and regulations. No significant toxicity was observed after intratracheal (i.t.) administration of LO (3.25 mg·kg^-1) to mice. Mouse i.t. administration of LOE remarkably attenuated lung injury induced by lipopolysaccharide with mitigations of inflammatory factors (tumor necrosis factor-α, interleukin-6) and total proteins. LOE is a promising inhaled formulation for the treatment of ALI.

Linezolid is the first oxazolidinone antibacterial drug approved by the FDA, which can effectively treat various gram-positive bacterial infections, including blood infections, skin and soft tissue infections, community and hospital-acquired pneumonia. It has become one of the most commonly used antibiotics in clinical. In addition to the recently launched tedizolid phosphate (TR701) and contezolid (MRX-I), several oxazolidinone anti-infective candidates are currently under clinical research. This review briefly introduces the oxazolidinone antibiotics that have been marketed and are in clinical trials, and recent progress on the structure optimization of oxazolidinone drugs is also summarized.

We predicted the anti-ulcerative colitis (UC) mechanism of Fructus Amomi based on network pharmacology. The anti-UC activity of Fructus Amomi were investigated by in vivo animal experiment, and the active components of Fructus Amomi were obtained through TCMSP, PubChem database and literature research. Animal welfare and experimental procedures follow the regulations of the Animal Ethics Committee of Institute of Materia Medica of Chinese Academy of Medical Sciences. The potential targets of the active components and UC were predicted by SwissTargetPrediction, GeneCards and TTD databases. The protein-protein interaction (PPI) network was constructed by String database and Cytoscape software was used to construct a visual network of active component-disease target and perform topological analysis. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were performed using Metascape platform. The molecular docking of key components and core targets was carried out by Sybyl X software. We screened out a total of 12 active components and 189 disease-component overlapping targets. Enrichment analyses obtained 227 related GO items and 168 signaling pathways. According to the results of molecular docking, most active components of Fructus Amomi showed good affinity with the JAKs receptor family. Furthermore, Western blot results verified that Fructus Amomi could effectively inhibit JAK/STAT signaling pathway, indicating that Fructus Amomi might exert the anti-UC activity by regulating JAK/STAT signaling pathway.

The GPCR family component leukotriene B4 receptor 1 (LTB4R1) is the receptor of leukotriene B4 (LTB4), the metabolic product of ω6 fatty acid. LTB4R1 is a potential therapeutic target for the treatment of insulin resistance, chronic inflammation and type 2 diabetes. Here we established a LTB4R1 inhibitor screen model based on the GPCR family protein property that its activation causes the cytosolic escalation of calcium. The cytosolic calcium probe Fluo-8 represents the change of calcium ion. After adding LTB4, the fluorescent signal of Fluo-8 in the CHO cells which are co-transfected with LTB4R1 and Gα16 will change with the increase of cytosolic calcium, and LTB4R1 inhibitor blocked the effect of LTB4 on fluorescent signal of Fluo-8 in the CHO cells. Here, we used 0.2% DMSO as a negative control, and cp-105696 as a positive control in the screen model. After stimulation with LTB4, the Fluo-8 signal in 0.2% DMSO treated CHO cells increased 2 fold and fell back slowly, while the signal in inhibitor (cp-105696) treated cells was not induced by LTB4. The results showed that LTB4 increased the cytosolic calcium detected by Fluo-8 in a dose dependent manner. Similarly, cp-105696 inhibited the Fluo-8 signal dose dependently, indicating that this method can quantify the inhibitory activity of the compounds. The Z'-factor, reflecting the robustness of the screen model, was 0.777 with a series of experiments. In sum, we over-expressed LTB4R1α and Gα16 in CHO cell, used Fluo-8 to detect the calcium signal activated by LTB4, and established the in vitro screen model for LTB4 receptor 1.

We have established a quantitative analysis of multi-components by single marker method (QAMS) for the simultaneous determination of apigenin-7-glucuronide, quercitrin, yuankanin, luteolin, apigenin, hydroxygenkwanin, and genkwanin in Qutan Zhike Granules. The chromatographic column used was an Agilent EC-C18(150 mm × 4.6 mm, 4 μm), the mobile phase was methanol-0.15% phosphoric acid solution (gradient elution), and the detection wavelength was 338 nm. Apigenin was chosen as the internal reference standard, the relative correction factors for the six components were determined by multi-point correction method and included apigenin-7-glucuronide, quercitrin, yuankanin, luteolin, hydroxygenkwanin and genkwanin. According to the two-point correction method combined with the relative retention time correction of the components to be tested, the peak location was determined. The contents of these seven compounds in 10 batches of Qutan Zhike Granules samples were determined with relative correction factors, and the relative error (RE) was used to compare the results to that of the external standard using the External Standard Method to verify the accuracy of QAMS. The relative correction factors for apigenin-7-glucuronide, quercitrin, yuankanin, luteolin, hydroxygenkwanin and genkwanin were 1.762 8, 2.310 4, 1.898 4, 1.282 8, 1.191 3 and 1.066 9, respectively. RSDs of the relative correction factors were all lower than 3%. The peaks for each constituent were accurately located by the two-point correction method combined with relative retention time correction, and the predicted retention time was close to the actual retention time. The relative error of the contents by QAMS and determined by ESM in 10 batches of Qutan Zhike Granules were between -5% and 5%. This content determination method can be used for the simultaneous determination of seven components in Qutan Zhike Granules.

Synthetic organoselenium compounds can be used as antioxidants, enzyme inhibitors, neuroprotective agents, antitumor agents, anti-infectious agents, and immunomodulators. Diphenyl diselenide (DPDS) is a synthetic organoselenium compound with simple and stable structure, and possesses lower toxicity than inorganic selenium and most organoselenium compounds. Moreover, DPDS has strong antioxidant properties due to its strong glutathione peroxidase-mimetic activity, involvement in thioredoxin reductase catalytic reactions, and activation of the nuclear factor E2 associated factor 2 (Nrf2)/Kelch like epichlorohydrin associated protein-1 (Keap1) signaling pathway. DPDS has been shown to possess a variety of pharmacological activities including anti-inflammatory, anti-diabetic, antifungal, neuroprotective, antitumor, hepatoprotective, renoprotective, and cardiovascular protective effects in a variety of animal and cellular models. This paper reviews the research progress on the physicochemical properties, main pharmacological effects and mechanisms of DPDS by compiling relevant research results, so as to provide reference for future research and reasonable development and application of DPDS.