Icariin ameliorates LPS-induced acute lung injury in mice via complement C5a-C5aR1 and TLR4 signaling pathways.

Acute lung injury (ALI) is an acute respiratory-related progressive disorder, which lacks specific pharmacotherapy. Icariin (ICA) has been shown to be effective in treating ALI. However, the targets and pharmacological mechanisms underlying the effects of ICA in the treatment of ALI are relatively lacking. Based on network pharmacology and molecular docking analyses, the gene functions and potential target pathways of ICA in the treatment of ALI were determined. In addition, the underlying mechanisms of ICA were verified by immunohistochemistry, immunofluorescence, quantitative Real-time PCR, and Western blot in LPS-induced ALI mice. The biological processes targeted by ICA in the treatment of ALI included the pathological changes, inflammatory response, and cell signal transduction. Network pharmacology, molecular docking, and in vivo experimental results revealed that ICA inhibited the complement C5a-C5aR1 axis, TLR4 mediated NF-κB, MAPK, and JAK2-STAT3 signaling pathways related gene and protein expressions, and decreased inflammatory cytokine, chemokine, adhesion molecule expressions, and mitochondrial apoptosis in LPS-induced ALI.

The influence of pH and dissolved organic carbon on the ecotoxicity of ampicillin and clarithromycin.

The impacts of water chemistry properties including pH and dissolved organic carbon (DOC) on the ecotoxicity of active pharmaceutical ingredients (APIs) are increasingly evident. These impacts are a result of alterations in API bioavailability: pH regulates the bioavailability of many ionizable APIs via chemical speciation, whereas DOC interacts with several APIs to inhibit the APIs from traversing the membrane system of organisms. In this study, we examined the influences of pH and DOC on the bioavailability of ampicillin (AMP) and clarithromycin (CLA) with the help of a bioavailability model. The effects on bioavailability were quantified by ecotoxicity observed in cyanobacteria growth inhibition tests with Microcystis aeruginosa PCC7806. The median effect concentration (96 h-EC50total) of AMP increased by 5-fold when pH raised from 7.4 to 9.0, suggesting the zwitterionic AMP+/- species being higher in bioavailability than the negatively charged AMP- species. CLA ecotoxicity showed no significant pH-dependency, suggesting CLA+ and CLA0 species to be equally bioavailable, albeit it correlated significantly with M. aeruginosa growth rate in negative controls. In addition, DOC demonstrated no significant effects on the ecotoxicity of AMP or CLA. Overall, together with earlier results on ciprofloxacin, our data show that bioavailability relations with pH and DOC are variable among different antibiotics. Factors other than chemical speciation alone could play a role in their bioavailability, such as their molecular size and polarity.

Effect of Oat ß-Glucan on the Structure and Properties of Soybean Protein Isolate During Maillard Reaction.

Maillard reaction (MR) with oat ß-glucan changed the structure of soybean protein isolate (SPI), further leading to the enhancement of its functional properties. SPI was unfolded by MR, and the SPI conjugates with high molecular weight were identified. The water solubility of SPI was improved by cross-linking with hydrophilic ß-glucan, while the hydrophobicity also increased along with the unfolding of the SPI. Cross-linking with ß-glucan elevated the viscosity of SPI, thus enhancing viscosity-related physiological activities, including bile acid binding ability, fat binding capacity, and hypoglycemic activity, and the functional properties increased as the ßG content involved in MR increased.

Water brownness regulates the bioavailability of a fluoroquinolone antibiotic: UV-absorbance as a predictor of ciprofloxacin ecotoxicity.

Dissolved organic carbon (DOC) is a powerful regulator of the ecotoxicity of ciprofloxacin (CIP), a widely applied fluoroquinolone antibiotic. In this study, we investigated the impact of DOC from a variety of sources on CIP bioavailability, using a cyanobacteria growth inhibition test with Microcystis aeruginosa. We analyzed the impact from two perspectives: (1) DOC concentration, and (2) water brownness, defined in this work as the light absorbance of DOC solutions. The toxicity tests were conducted with (1) unprocessed freshwater DOC in the naturally occurring state, (2) DOC extracted from a freshwater stream (Schwarzbach stream, Küchelscheid, Belgium), and (3) the commercial DOC product Suwannee River organic matter. Across all DOC sources investigated, a strong negative correlation was observed between CIP ecotoxicity and light absorbance at four wavelengths across the ultraviolet-visible range (e.g., A350), whereas CIP ecotoxicity correlated poorly with the DOC concentration. In addition, the interactions between CIP and DOC were modelled as a CIP-DOC binding process to allow the quantification of the inhibitory effects of DOC on CIP toxicity via binding constants (Kd,CIPx, with x being the ionic charge + or +/-, L g-1). Processed DOC sources showed higher binding potency than most of the unprocessed DOC sources, suggesting that toxicity tests employing only processed DOC potentially overestimates the impact of DOC in natural environments. Nonetheless, the light absorption coefficient (i.e., ε350) appeared a reliable predictor of the Kd,CIP+/- (and thus of the potential of the DOC source to reduce ecotoxicity of CIP) of both processed and unprocessed DOC. The relationship can be further incorporated into model simulations to estimate CIP bioavailability in dynamic environments. It is concluded that the brownness of water is a better predictor of the impact of DOC on CIP bioavailability than the DOC concentration itself.

Physicochemical and functional property of the Maillard reaction products of soy protein isolate with L-arabinose/D-galactose.

BACKGROUND: Soy protein isolate (SPI) is widely used in the food industry because of its nutritional and functional properties. During food processing and storage, the interaction with co-existing sugars can cause changes in the structural and functional properties of SPI. In this study, SPI-l-arabinose conjugate (SPI:Ara) and SPI-d-galactose conjugate (SPI:Gal) were prepared using Maillard reaction (MR), and the effects of five-carbon/six-carbon sugars on the structural information and function of SPI were compared. RESULTS: MR unfolded and stretched the SPI, changing its ordered conformation into disorder. Lysine and arginine of SPI were bonded with the carbonyl group of sugar. The MR between SPI and l-arabinose has a higher degree of glycosylation compared to d-galactose. MR of SPI enhanced its solubility, emulsifying property and foaming property. Compared with SPI:Ara, SPI:Gal exhibited better aforementioned properties. The functionalities of amphiphilic SPI were enhanced by MR, SPI:Gal possessed better hypoglycemic effect, fat binding capacity and bile acid binding ability than SPI:Ara. MR endowed SPI with enhanced biological activities, SPI:Ara showed higher antioxidant activities, and SPI:Gal exhibited stronger antibacterial activities. CONCLUSION: Our work revealed that l-arabinose/d-galactose exhibited different effects on the structural information of SPI, and further affected its physicochemical and functional property. © 2023 Society of Chemical Industry.

Salvianolic acid A alleviates lipopolysaccharide-induced disseminated intravascular coagulation by inhibiting complement activation.

INTRODUCTION: Disseminated intravascular coagulation (DIC) is a syndrome characterized by coagulopathy, microthrombus, and multiple organ failure. The complement system in DIC is overactivated, and the functions of complement and coagulation pathways are closely related. Our previous screening revealed that salvianolic acid A (SAA) has anti-complement activity. The hyper-activated complement system was involved in the lipopolysaccharide (LPS) induced DIC in rats. The effects of SAA anti-complement action on LPS-induced DIC in rats were investigated. METHODS: The complement activity of the classical pathway and alternative pathway was detected through an in vitro hemolysis assay. The binding sites of SAA and complement C3b were predicted by molecular docking. LPS-induced disseminated coagulation experiments were performed on male Wistar rats to assess coagulation function, complement activity, inflammation, biochemistry, blood routine, fibrinolysis, and survival. RESULTS: SAA had an anti-complement activity in vivo and in vitro and inhibited the complement activation in the classical and alternative pathway of complement. The infusion of LPS into the rats impaired the coagulation function, increased the plasma inflammatory cytokine level, complemented activation, reduced the clotting factor levels, fibrinogen, and platelets, damaged renal, liver, and lung functions, and led to a high mortality rate (85%). SAA treatment of rats inhibited complement activation and attenuated the significant increase in D-dimer, interleukin-6, alanine aminotransferase, and creatinine. It ameliorated the decrease in plasma levels of fibrinogen and platelets and reversed the decline in activity of protein C and antithrombin III. The treatment reduced kidney, liver, and lung damage, and significantly improved the survival rate of rats (46.2 and 78.6% for the low- and high-dose groups, respectively). CONCLUSION: SAA reduced LPS-induced DIC by inhibiting complement activation. It has considerable potential in DIC treatment.

A Bioavailability Model to Predict the Impact of pH and Dissolved Organic Carbon on Ciprofloxacin Ecotoxicity to the Cyanobacterium Microcystis aeruginosa.

Ciprofloxacin (CIP) is a pseudopersistent antibiotic detected in freshwater worldwide. As an ionizable chemical, its fate in freshwater is influenced by water chemistry factors such as pH, hardness, and dissolved organic carbon (DOC) content. We investigated the effect of pH, DOC, and Ca2+ levels on the toxicity of CIP to Microcystis aeruginosa and developed a bioavailability model on the basis of these experimental results. We found that the zwitterion (CIP+/- ) is the most bioavailable species of CIP to M. aeruginosa, whereas DOC is the most dominant factor reducing CIP toxicity, possibly via binding of both CIP+/- and CIP+ to DOC. pH likely also regulates CIP-DOC binding indirectly through its influence on CIP speciation. In addition, higher tolerance to CIP by M. aeruginosa was observed at pH < 7.2, but the underlying mechanism is yet unclear. Calcium was identified as an insignificant factor in CIP bioavailability. When parameterized with the data obtained from toxicity experiments, our bioavailability model is able to provide accurate predictions of CIP toxicity because the observed and predicted total median effective concentrations deviated by <28% from each other. Our model predicts that changes in pH and DOC conditions can affect CIP toxicity by up to 10-fold, suggesting that CIP in many natural environments is likely less toxic than in standard laboratory toxicity experiments. Environ Toxicol Chem 2022;41:2835-2847. © 2022 SETAC.

Traditional Chinese Medicine Constitution Discrimination Model Based on Metabolomics and Random Forest Decision Tree Algorithm.

Constitution refers to the comprehensive and relatively stable characteristics of the genetic or acquired morphological structure, physiological function, and psychological state in the process of human individual life. A special metabolomics data processing method is established to find the unique m/z value of each constitution. Combined with the random forest decision tree algorithm, the discrimination model of 9 constitutions in traditional Chinese medicine is constructed, and the model is verified and tested. The test results show that the classification accuracy of each constitution is higher than 80%, indicating that the model can well identify nine constitutions of traditional Chinese medicine. The classification accuracy is related to the difficulty of distinguishing between constitutions. In a word, this study provides a fast and accurate method to distinguish the constitution of traditional Chinese medicine, provides an objective representation for the classification and judgment of clinical constitution of traditional Chinese medicine, and provides a scientific basis for the modernization of traditional Chinese medicine.

Elucidation of the Transport Mechanism of Puerarin and Gastrodin and Their Interaction on the Absorption in a Caco-2 Cell Monolayer Model.

Puerarin (PUR) and gastrodin (GAS) are often used in combined way for treating diseases caused by microcirculation disorders. The current study aimed to investigate the absorption and transportation mechanism of PUR and GAS and their interaction via Caco-2 monolayer cell model. In this work, the concentration in Caco-2 cell of PUR and GAS was determined by HPLC method. The bidirectional transport of PUR and GAS and the inhibition of drug efflux including verapamil and cyclosporine on the transport of these two components were studied. The mutual influence between PUR and GAS, especially the effect of the latter on the former of the bidirectional transport were also investigated. The transport of 50 µg·mL-1 PUR in Caco-2 cells has no obvious directionality. While the transport of 100 and 200 µg·mL-1 PUR presents a strong directionality, and this directionality can be inhibited by verapamil and cyclosporine. When PUR and GAS were used in combination, GAS could increase the absorption of PUR while PUR had no obvious influence on GAS. Therefore, the compatibility of PUR and GAS is reasonable, and GAS can promote the transmembrane transport of PUR, the effect of which is similar to that of verapamil.

Metabonomic Study on the Plasma of High-Fat Diet-Induced Dyslipidemia Rats Treated with Ge Gen Qin Lian Decoction by Ultrahigh-Performance Liquid Chromatography-Mass Spectrometry.

Gegen Qinlian decoction (GGQLD) has a definite effect on T2DM in clinic, and it has the effect of lowering blood sugar, improving insulin resistance, and improving the blood lipid level of rats with dyslipidemia, but the intervention mechanism of GGQLD on dyslipidemia has not been clarified. The changes in endogenous metabolites in the plasma of high-fat diet-induced dyslipidemia rats treated with Ge Gen Qin Lian Decoction (GGQLD) were studied to elucidate the therapeutic effects and mechanism of action of GGQLD in dyslipidemia. Based on ultrahigh-performance liquid chromatography coupled with quadrupole-time-of-flight tandem mass spectrometry (UHPLC-Q-TOF-MS), the metabolic profiles of rat serum samples were collected. The rat model of dyslipidemia was induced by a 60% fat-fed high-fat diet. After feeding the rats with a high-fat diet for 4 weeks, dyslipidemia appeared. After 5 weeks of GGQLD (14.85 g kg-1) administration, the metabonomics of rats' plasma samples in the normal group, model group, and administration group were analyzed. Mass profiler professional (MPP), SIMCA-P 14.1, and Graphpad prism 6.0 software were used combined with METLIN biological database and human metabolite database HMDB to screen and identify endogenous biomarkers. Metaboanalyst 4.0 software was used by combining with HMDB and KEGG databases; the enrichment and metabolic pathway of biomarkers were analyzed to explore the metabolic mechanism of dyslipidemia rats induced by high-fat diet and the intervention mechanism of Gegen Qinlian decoction. After 5 weeks of administration of GGQLD, the levels of serum TC and TG were significantly decreased (P < 0.05, P < 0.01), while HDL-C and LDL-C were not significantly affected. After administration, the food intake of rats in the administration group decreased gradually, and the change trend of body weight gradually slowed down. The metabonomics of rat plasma samples results showed that 23 potential biomarkers including α-linolenic acid, arachidonic acid, and lysophosphatidylcholine were significantly changed in positive ion mode. Studies have shown that GGQLD has a significant lipid-lowering effect on dyslipidemia rats induced by a high-fat diet, and its preventive mechanism is related to tryptophan metabolism, fatty acid biosynthesis, α-linolenic acid metabolism, arachidonic acid, and glycerophosphatidyl metabolism pathway.

Deciphering the Formulation Secret Underlying Chinese Huo-Clearing Herbal Drink.

Herbal teas or herbal drinks are traditional beverages that are prevalent in many cultures around the world. In Traditional Chinese Medicine, an herbal drink infused with different types of medicinal plants is believed to reduce the 'Shang Huo', or excessive body heat, a status of sub-optimal health. Although it is widely accepted and has a very large market, the underlying science for herbal drinks remains elusive. By studying a group of herbs for drinks, including 'Gan' (Glycyrrhiza uralensis Fisch. Ex DC.), 'Ju' (Dendranthema morifolium (Ramat.) Tzvelev), 'Bu' (Microcos paniculata L.), 'Jin' (Lonicera japonica Thunb.), 'Xia' (Prunella vulgaris L.), and 'Ji' (Plumeria rubra L.), the long-term jargon is connected with the inflammation of modern immunology through a few pro-inflammatory markers. In vitro studies have indicated that cellular inflammation is lowered by Ju and Jin either individually or synergistically with Gan. Among all herbs, only Gan detoxicated cellular toxicity of Bu in a dose dependent manner. The synergistic formulation of Ju and Gan, or Jin and Gan, in a reduction of Shang Huo, was tested in vivo. Both combinations exhibited a lower percentage of neutrophils, monocytes, and CD4+/CD8+ ratio in the blood, as well as inflammatory cytokines. Furthermore, body weight in the combinatory groups was more stable than treatments using single herbs. The combination of old traditional oriental methods with Western science logistics, has resulted in the formulation of different herbs into one concoction for the use of detoxification and synergism.

Facile preparation of robust dual MgO-loaded carbon foam as an efficient adsorbent for malachite green removal.

This study developed a facile approach for the fabrication of dual MgO-loaded carbon foam (DMCF) via carbonization of a cured MgO/cyanate ester resin mixture, which underwent self-foaming of the resin followed by the carbothermal reduction of MgO. The features of the prepared DMCF prepared were characterized by FESEM, TEM, XRD, FTIR, XPS and so on, and the effects of adsorption conditions, adsorption isotherms, kinetics, and thermodynamics on malachite green (MG) removal using the DMCF as adsorbents were investigated through batch adsorption experiments. Results demonstrate that the DMCF possesses a unique dual loading of MgO particles which are not only loaded onto its foam walls but also filled within the walls with a graphene-wrapped core-shell structure. The experimental maximum adsorption capacity of MG reaches up to 1874.18 mg/g with a partition coefficient of 10.87 mg/g/µM. The adsorption process can be better described with Langmuir, pseudo-second-order, and intraparticle diffusion models. Moreover, the DMCF exhibits a removal percentage of 84.85% after five reuses, indicating that it is an efficient and promising adsorbent for MG adsorption.

Simultaneous Determination of Ten Bioactive Components from Shenling Baizhu San in Rat Plasma by UHPLC-MS/MS: Application to a Comparative Pharmacokinetic Study in Normal and Two Models of Ulcerative Colitis Rats.

Shenling Baizhu San, a traditional formula, has a long history of treating spleen asthenic diarrhea by invigorating the spleen and dispelling dampness in China. A rapid and accurate UHPLC-MS/MS method was developed and fully validated for the simultaneous determination of ten active constituents in rat plasma: panaxadiol, ginsenoside Rg1, atractylenolide I, atractylenolide III, pachymic acid, neferine, nuciferine, diosgenin, platycodin D, and isoliquiritigenin. The plasma samples were pretreated by the protein precipitation method with acetonitrile. The analytes and puerarin (internal standard) were determined with high selectivity and sensitivity (LLOQ, 0.31-0.68 ng·mL-1) within 10 minutes. The validation parameters, including intra-/interday precisions, accuracy, recovery, matrix effect, and stability, were within acceptable ranges. The validated method was successfully applied to the pharmacokinetics study of ten components in normal and two rat models of ulcerative colitis (i.e., spleen deficiency with dampness retention-ulcerative colitis (SDDR-UC) rats and pure-ulcerative colitis (P-UC) rats). The pharmacokinetic parameters were significantly different among the three groups of rats. Overall, the absorption of the components was shown as follows: normal group > SDDR-UC group > P-UC group. The study could provide a scientific basis for further studies on pharmacokinetics and clinical differential application of SDDR-UC and P-UC patients.

A stiff ZnO/carbon foam composite with second-level macroporous structure filled ZnO particles for heavy metal ions removal.

A stiff zinc oxide/carbon foam (ZnO/CF) composite as a desirable adsorbent for heavy metal ions was innovatively designed and fabricated by loading ZnO particles into a carbon foam with capsule-like second-level macropores. The features of the resulting composite were characterized by FESEM, XRD, BET, FTIR, and XPS. The effects of adsorption parameters on the Pb(II), Cr(III), and Cu(II) ions removal were studied through batch experiments. Results show that the ZnO/CF composite possesses a second-level macroporous structure filled ZnO particles, which has both mesoporous structure and Zn-O-C bond with the strongly synergistic effect. And meanwhile, it has a relatively high compression strength of 2.18 MPa at a density of 0.18 g cm-3. The experimental maximum adsorption capacities for Pb(II), Cr(III), and Cu(II) ions reach 170.85 mg g-1, 168.74 mg g-1, and 104.61 mg g-1 with relatively high partition coefficients of 5.803 mg g-1 µM-1, 1.169 mg g-1 µM-1, and 0.648 mg g-1 µM-1, respectively. The experimental data are in accordance with Langmuir isotherm and pseudo-second-order kinetic model. Moreover, the composite still exhibits a good adsorption performance even after five cycles.

A novel hierarchical stiff carbon foam with graphene-like nanosheet surface as the desired adsorbent for malachite green removal from wastewater.

A novel hierarchical stiff carbon foam (HSCF) was successfully prepared via a carbothermal reduction between the carbon foam with two-level pore structure and the Al2O3 from aluminum sulfate, and used as a bulk adsorbent for removing malachite green (MG) dye. The structures of the HSCF were characterized using SEM, XRD, FTIR, BET, and XPS, and the effects of adsorption condition on the MG removal were studied through batch adsorption experiments. Results show that large-sized and complex-shaped HSCF can be easily fabricated with a high compression strength of 1.58 MPa at a low bulk density (0.10 g cm-3). The HSCF possesses a fluffy graphene-like nanosheet surface with a mesoporous structure and meanwhile exhibits good hydrophilicity loaded with aluminum hydroxide. The experimental maximum adsorption capacity for MG reaches 425.2 mg g-1 with a relatively high partition coefficient of 9.38 mg g-1 µM-1 at the optimal condition. The experimental data are in good agreement with Langmuir isotherm and pseudo-second-order kinetic model, and meanwhile, the adsorption of MG onto the HSCF is a spontaneous and endothermic process. Also, the HSCF still exhibits good adsorption ability and stability after seven regeneration cycles.

Simultaneous Determination of Seven Active Components in Rat Plasma by UHPLC-MS/MS and Application to a Quantitative Study after Oral Administration of Huang-Lian Jie-Du Decoction in High Fat-Induced Atherosclerosis Rats.

Huang-Lian Jie-Du decoction (HLJDD) has been used to treat cardiovascular and cerebrovascular disease for many years in China. Currently, the determination of effect components in HLJDD is focusing either on the formula or on the extract, while quantification of that in biological samples is scarce, especially simultaneous determination of multicomponent. In this paper, a rapid, specific, and sensitive ultra-high performance liquid chromatography-tandem mass spectrometry method was developed and fully validated for the simultaneous determination of seven main active constituents, i.e., baicalin, baicalein, wogonoside, wogonin, berberine, palmatine, jatrorrhizine in rat plasma. The method was also successfully applied to a quantitative study after oral administration of HLJDD at different doses of 1.5, 3, and 6 g/kg body weight to high fat-induced atherosclerosis rats. The analytes were detected by ESI source and multiple reactions monitoring (MRM) using positive scanning mode. The blood was collected from the abdominal aorta of rats at predetermined time and preprepared with icariin and tetrahydropalmatine as internal standards (IS). Sample preparation was achieved by protein precipitation (PPT). The validation parameters (linearity, sensitivity, intra-/interday precision and accuracy, extraction recovery, and matrix effect) were within acceptable ranges, and biological extracts were stable during the entire storing and preparing process. And the result of determination of HLJDD-containing plasma, baicalin, baicalein, wogonoside, and wogonin could be highly detected in a dose-dependent manner while berberine, jatrorrhizine, and palmatine were determined in a very low level and in a dose-independent mode. Thus, the established method was sensitive enough and successfully applied to the determination of seven effective components in plasma taken from 24 high fat-induced atherosclerosis rats after oral administration of three dosages of HLJDD.

A Comprehensive and Rapid Quality Evaluation Method of Traditional Chinese Medicine Decoction by Integrating UPLC-QTOF-MS and UFLC-QQQ-MS and its Application.

Decoction is one of the oldest forms of traditional Chinese medicine and it is widely used in clinical practice. However, the quality evaluation and control of traditional decoction is a challenge due to the characteristics of complicated constituents, water as solvent, and temporary preparation. ShenFu Prescription Decoction (SFPD) is a classical prescription for preventing and treating many types of cardiovascular disease. In this article, a comprehensive and rapid method for quality evaluation and control of SFPD was developed, via qualitative and quantitative analysis of the major components by integrating ultra-high-performance liquid chromatography equipped with quadrupole time-of-flight mass spectrometry and ultra-fast-performance liquid chromatography equipped with triple quadrupole mass spectrometry. Consequently, a total of 39 constituents were tentatively identified in qualitative analysis, of which 21 compounds were unambiguously confirmed by comparing with reference substances. We determined 13 important constituents within 7 min by multiple reaction monitoring. The validated method was applied for determining five different proportion SFPDs. It was found that different proportions generated great influence on the dissolution of constituents. This may be one of the mechanisms for which different proportions play different synergistic effects. Therefore, the developed method is a fast and useful approach for quality evaluation of SFPD.

Engineering a yeast double-molecule carrier for drug screening.

With the advantages of unicellular eukaryotic structure and easy manipulation, yeast becomes a popular tool for biochemical, genetic and medicinal studies. In order to construct an efficient anti-inflammatory drug screening platform, we engineered yeast as a double-molecule carrier, of which an inserted domain (I domain) of lymphocyte function-associated antigen 1 was displayed on yeast surface and a green fluorescent protein (GFP) was expressed inside cytosol. The I domain specifically targeted a surface marker of mammalian cells, intercellular adhesion molecule 1, whose number is correlated with the level of cellular inflammation. Examination of GFP intensity enables swift quantification of the yeast-mammalian cell binding and thus it reflects inflammatory potency, herein the inflammatory index, of a chemical imposed to cells. The inflammatory potency of a total of 1340 chemicals was indexed. Among them, 1 inflammation-inducing and 1 inflammation-reducing compounds were verified both in vitro and in vivo. Our method demonstrated a swift, facile and high-throughput screening platform at the protein level for inflammation and related diseases drug discovery without using sophisticated instruments.

Characterization of Anti-bacterial Compounds from the Seed Coat of Chinese Windmill Palm Tree (Trachycarpus fortunei).

The increasing of multidrug resistance in bacterial associated infections has impaired the current antimicrobial therapy and it forces the search for other alternatives. In this study, we aimed to find the in vitro antibacterial activity of seed coat of Trachycarpus fortunei against a panel of clinically important bacterial species. Ethanolic extracts of target tissues were fractionated through macro porous resin by column chromatography, using ethanol as an organic solvent with a concentration gradient of 0-100%, each along with 20% concentration increment. The minimum inhibitory (MIC) concentrations of all fractions were measured. It is found that 20% ethanolic fraction showed the most significant inhibition against tested bacterial species. All fractions were analyzed by Ultra-Performance Liquid Chromatography/mass spectrometry (UPLC/MS) and compounds were identified by comparing mass spectra with standard libraries. By pairing the identified compounds from different fractions with the antibacterial activity of each fraction, it was shown that compounds stearamide (7), 1-(4-Fluorophenyl)-2-(methylthio)-1H-imidazole-5-carboxylic acid (9) and 2,4,5 triacetoxybiphenyl (10) topped in the list for anti-bacterial activity. Further experiment with pure chemicals verified that compounds 9 and 10 have antibacterial activity against Gram-negative bacteria. Whereas, the lowest MIC value (39.06 µg/mL) was obtained by compound 10 against Staphylococcus epidermidis. Hence, the seed coat of T. fortunei with its antimicrobial spectrum could be a good candidate for further bactericidal research.

Improved ganoderic acids production in Ganoderma lucidum by wood decaying components.

Ganoderma lucidum is a legendary Traditional Chinese Medicine (TCM) over a few thousands of years and one kind of its major active components are Ganoderic acids (GAs). GAs are largely produced in the mushroom primordium and fruiting body but much less in mycelium stage. However, little is known on the underlying regulatory mechanism. As a saprophytic fungus, G. lucidum solely obtains nutrients by wood decaying. Wood in general contains sophisticated chemical components with diverse structural units. To explore a strategy that extensively leads to GAs induction in the submerged liquid fermentation, all chemical components that might be possibly from the wood decaying were tested individually as GAs inducers. It was found that GAs production increased 85.96% by 1.5% microcrystalline cellulose (MCC) and 63.90% by 0.5% D-galactose. The transcription level of a few rate-limiting or chemically diverting enzymes responsible for GAs biosynthesis was greatly induced by MCC and D-galactose. The concentration and time-course titration study indicated that these two chemicals might not be utilized as carbon sources but they played a comprehensive role in the secondary metabolites synthesis. Our data indicated that MCC and D-galactose might be further industrialized for higher GAs production in G. lucidum in submerged fermentation.