Metabolomics research on treatment of primary liver cancer with Cortex Juglandis Mandshuricae on LC-MS/MS technology.

Diethylnitrosamine (DEN) was applied to create the primary liver cancer (PLC) animal model. In the study, the normal group, model group, cyclophosphamide (CTX) group, Cortex Juglandis Mandshuricae (CJM) extract group, myricetin group and myricitrin group were divided. LC-MS/MS technology was applied to determine the metabolites of liver tissue samples from different locations (nodular and non-nodular parts of liver tissue) in each group of rats. Through metabolomics research, the connection and difference of anti-PLC induced by the CJM extract, myricetin and myricitrin was analyzed. The surface of the liver tissues of rats in the model group was rough, dimly colored, inelastic, on which there were scattered gray white cancer nodules and blood stasis points. The number of cancer nodules was significantly reduced, and the degree of cell malignancy was low, but there were some inflammatory cell infiltrations, necrosis area and karyokinesis in the CJM extract group, myricetin group, myricitrin group and CTX group. The result of metabolic research indicated that 45 potential biomarkers of the PLC were found, as gamma-aminoisobutyrate, taurochenodeoxycholate, xanthurenic acid, etc. There were 22 differential metabolites in the CTX group, 16 differential metabolites in the CJM extract group, 14 differential metabolites in the myricetin group, 14 differential metabolites in the myricitrin group.

Corrigendum: 6-Shogaol inhibits oxidative stress-induced rat vascular smooth muscle cell apoptosis by regulating OXR1-p53 axis.

[This corrects the article DOI: 10.3389/fmolb.2022.808162.].

Silicon-mediated regulation of cadmium transport and activation of antioxidant defense system enhances Pennisetum glaucum resistance to cadmium stress.

Pennisetum glaucum is an important forage grass for livestock. However, the large accumulation of cadmium (Cd) in plant tissues increases the risk of heavy metals entering the food chain in Cd-contaminated soils. Silicon (Si) can inhibit cadmium (Cd) uptake and enhance tolerance of plant to Cd toxicity, but whether and how Si alleviates Cd toxicity in grass and the underlying mechanisms are unclear. The present study explored the differential mechanisms of silicon-induced Cd transport in apoplast and symplast, Cd distribution in root tissue and antioxidant defense system in P. glaucum under Cd stress through hydroponic and pot experiments. The present results showed that exogenous Si supply significantly reduced Cd concentrations in apoplast and symplast; Si treatment increased monosilicic acid concentration in apoplast and symplast of the roots and shoots under Cd stress. Elemental analysis of root microdomains showed that Si treatment increased the distribution of Cd and Si in the endodermis by 42.6% and 14.0%, respectively. Si alleviated the adverse influences of Cd on plant growth, which were manifested in root morphological traits and root activity. In addition, Si addition significantly increased the activities of catalase and superoxide dismutase by 37.0% and 72.7%, and improved the efficiency of the ascorbate-glutathione cycle in Cd-stress shoots. Furthermore, Si significantly reduced the contents of hydrogen peroxide and superoxide anion in Cd-stressed shoots by 16.6% and 48.7%, respectively. These findings demonstrate that Si enhances the resistance of P. glaucum to Cd stress through regulating Cd transport pathways and activating antioxidant defense systems.

Bioinformatics-based and molecular docking study on the mechanism of action of Galla chinensis in the treatment of diabetic foot ulcers.

Based on transcriptome sequencing and molecular biology, the active ingredient of Galla chinensis in the treatment of diabetic foot ulcers was identified, and its mechanism of action was analyzed.

(1) Searching for the main components of the compounds contained in G. chinensis in the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) and literature research. (2) Prediction of their targets using the PubChem, SwissTargetPrediction, and BATMAN databases. (3) The CTD, Genecards. and NCBI databases were used to mine the transcriptome sequencing data for target genes related to diabetic foot ulcers. (4) Cytoscape 3.7.0 software was used to construct protein/gene interaction network maps for G. chinensis. (5) GO and KEGG analysis was carried out using the DAVID database. (6) Heatmap and volcano map analysis was carried out with R software. (7) The preliminary validation and visualization of molecular docking were performed using AutoDockVina and PyMOL software. After the screening of TCMSP and literature research, we obtained nine active ingredients of G. chinensis, 53 targets for diabetic foot ulcers; 40 biological processes, 30 cell compositions, and 30 molecular functions by GO analysis; and 24 signaling pathways, including the HIF-1 signaling pathway and VEGF signaling pathway. were obtained by KEGG analysis. The molecular docking results showed that the main active ingredients of Galla chinensis had good binding activities with their corresponding target proteins. In this study, G. chinensis was analyzed for its potential value in the treatment of diabetic foot ulcers due to its anti-inflammatory and wound-healing effects.

Silica nanoparticles activate defense responses by reducing reactive oxygen species under Ralstonia solanacearum infection in tomato plants.

Silica nanoparticles (SNPs) play an important positive role in enhancing stress resistance of plants. However, their absorption and the mechanisms of resistance in plants are not yet fully understood. In this study, we investigated the uptake of SNPs in tomato plants and explored the physiological and molecular mechanisms of SNPs-mediated bacterial wilt resistance. Folia application of SNPs significantly increased silicon content in tomato leaves and roots by 5.4-fold and 1.8-fold compared with healthy control, respectively. Moreover, foliar-applied SNPs mainly accumulated in the shoots of plants. Interestingly, we found that SNPs significantly reduced wilt severity by 20.71%-87.97%. Under pathogen infection conditions, the Hydrogen peroxide (H2O2) levels and Malondialdehyde (MDA) content in SNPs treated leaves significantly decreased by 16.33%-24.84% and 22.15%-38.54%, respectively, compared to non-treated SNPs leaves. The application of SNPs remarkably increased peroxidase (78.56-157.47%), superoxide dismutase (46.02-51.68%), and catalase (1.59-1.64 fold) enzyme activities, as well as upregulated the expression of salicylic acid-related genes (PR-1, PR-5, and PAL) in tomato leaves. Taken together, our findings demonstrate that SNPs function as important nanoparticles to maintain ROS homeostasis in plants by increasing antioxidant enzyme activity in tomato plants and enhancing plant tolerance to bacterial wilt disease by regulating the expression of salicylic acid-related genes. This study expands our understanding of how plants utilize these nanoparticles to deal with pathogen infection.

Silicon enhances the submergence tolerance of rice by regulating quiescence strategy and alleviating oxidative damage.

The safety of rice production under submergence is one of the research hotspots worldwide. Although the effects of silicon (Si) on enhancing plant stress tolerance have been widely investigated, the underlying mechanisms mediated by Si under submergence remains poorly understood. In this study, wild type (WT) and Si-defective mutant (lsi1) rice were chosen to investigate the mechanisms of Si-mediated rice resistance to submergence. Our results showed that Si addition effectively mitigated oxidative damages under submergence by reducing the content of hydrogen peroxide (H2O2) and superoxide (O2.-) in WT rice plants. Moreover, Si treatment increased rice yield by 21.5% for WT rice under submergence. The application of Si significantly inhibited the elongation and internode length in WT rice under submergence, through the synergistic regulation of endogenous hormones ethylene (ET), gibberellic acid (GA) and jasmonic acid (JA). Further investigation showed that the ethylene-responsive factor (ERF) SUB1A gene was expressed under submergence in WT and lsi1 rice, but Si addition did not influence the expression of SUB1A. Interestingly, exogenous Si down-regulated the relative expression levels of Si transporter genes Lsi1 and Lsi2 in WT rice roots by 51.7% and 48.0%, respectively. However, the physiological characteristics and genes expression of lsi1 rice were not affected by Si application regardless of submergence. The present study indicated that Si enhances the submergence tolerance and reduce the adverse effects of yield loss through the removal of reactive oxygen species and the adjustment of quiescence strategy.

Role of Silica Nanoparticles in Abiotic and Biotic Stress Tolerance in Plants: A Review.

The demand for agricultural crops continues to escalate with the rapid growth of the population. However, extreme climates, pests and diseases, and environmental pollution pose a huge threat to agricultural food production. Silica nanoparticles (SNPs) are beneficial for plant growth and production and can be used as nanopesticides, nanoherbicides, and nanofertilizers in agriculture. This article provides a review of the absorption and transportation of SNPs in plants, as well as their role and mechanisms in promoting plant growth and enhancing plant resistance against biotic and abiotic stresses. In general, SNPs induce plant resistance against stress factors by strengthening the physical barrier, improving plant photosynthesis, activating defensive enzyme activity, increasing anti-stress compounds, and activating the expression of defense-related genes. The effect of SNPs on plants stress is related to the physical and chemical properties (e.g., particle size and surface charge) of SNPs, soil, and stress type. Future research needs to focus on the "SNPs-plant-soil-microorganism" system by using omics and the in-depth study of the molecular mechanisms of SNPs-mediated plant resistance.

6-Shogaol Inhibits Oxidative Stress-Induced Rat Vascular Smooth Muscle Cell Apoptosis by Regulating OXR1-p53 Axis.

Apoptosis of vascular smooth muscle cells (VSMCs) is closely related to the pathogenesis of cardiovascular diseases, and oxidative stress is an important cause of VSMCs' death. Inhibiting VSMCs apoptosis is an effective preventive strategy in slowing down the development of cardiovascular disease, especially for atherosclerosis. In this study, we found that oxidation resistance protein 1 (OXR1), a crucial participator for responding to oxidative stress, could modulate the expression of p53, the key regulator of cell apoptosis. Our results revealed that oxidative stress promoted VSMCs apoptosis by overexpression of the OXR1-p53 axis, and 6-shogaol (6S), a major biologically active compound in ginger, could effectively attenuate cell death by preventing the upregulated expression of the OXR1-p53 axis. Quantitative proteomics analysis revealed that the degradation of p53 mediated by OXR1 might be related to the enhanced assembly of SCF ubiquitin ligase complexes, which is reported to closely relate to the modification of ubiquitination or neddylation and subsequent degradation of p53.

Silicon Enhances Plant Resistance of Rice against Submergence Stress.

Flooding is an important natural disaster limiting rice production. Silicon (Si) has been shown to have an important role in alleviating varied environmental stress. However, very few studies have investigated the effects and mechanisms of Si in alleviating flood stress in rice. In the present study, wild type rice (cv. Oochikara, WT) and Si-defective mutant (lsi1) were chosen to examine the impacts of Si application on plant growth, photosynthesis, cell structure, and antioxidant enzyme activity of rice exposed to submergence stress at tillering stage. Our results showed that Si application improved root morphological traits, and increased Si uptake and plant biomass of WT under submergence stress, but non-significantly influenced lsi1 mutant. Under submergence stress, leaf photosynthesis of WT was significantly inhibited, and Si application had no significant effects on photosynthetic rate, transpiration rate, stomatal conductance, and intercellular carbon dioxide concentration for both of WT and lsi1 mutant, but the photochemical quenching of WT was increased and the integrity of cell structure was improved. In addition, Si application significantly reduced malondialdehyde concentration and increased the activity of peroxidase and catalase in WT leaves under submergence stress. These results suggested that Si could increase rice plant resistance against submergence stress by improving root morphological traits and chloroplast ultrastructure and enhancing antioxidant defense.

Antibacterial and anti-biofilm effects of fatty acids extract of dried Lucilia sericata larvae against Staphylococcus aureus and Streptococcus pneumoniae in vitro.

Development of new effective antimicrobial drugs is still a big challenge to date due to microbial infection remains an inevitable problem against human health. In this study, fatty acids extract of Lucilia sericata larvae (LFAs) was obtained and evaluated by gas chromatograph-mass spectrometry (GC-MS), and its antibacterial activity against Staphylococcus aureus (S. aureus) and Streptococcus pneumoniae (S. pneumoniae) was investigated. We found that LFAs exhibited effective antibacterial activity against S. aureus and S. pneumoniae with minimal inhibitory concentrations (MICs) of 125 µg/mL and 100 µg/mL, respectively. The bacterial wall and membrane were the main targets, which was confirmed by fluorescence microscopy, scanning electron microscopy and transmission electron microscopy. Furthermore, a notable anti-biofilm activity against S. aureus and S. pneumoniae was also observed, which was able to both prevent biofilm formation and eradicate mature biofilms of these bacteria. As a promising antibacterial agent, LFAs showed good application prospects in clinical practice.

Flavonoids Regulate Inflammation and Oxidative Stress in Cancer.

Cancer is the second leading cause of death globally. Millions of persons die due to cancer each year. In the last two decades, the anticancer effects of natural flavonoids have become a hot topic in many laboratories. Meanwhile, flavonoids, of which over 8000 molecules are known to date, are potential candidates for the discovery of anticancer drugs. The current review summarizes the major flavonoid classes of anticancer efficacy and discusses the potential anti-cancer mechanisms through inflammation and oxidative stress action, which were based on database and clinical studies within the past years. The results showed that flavonoids could regulate the inflammatory response and oxidative stress of tumor through some anti-inflammatory mechanisms such as NF-κB, so as to realize the anti-tumor effect.

Fatty acid extracts facilitate cutaneous wound healing through activating AKT, ERK, and TGF-ß/Smad3 signaling and promoting angiogenesis.

Fatty acids (FAs) are potential therapeutic agents for cutaneous wound healing; however, the mechanisms underlying this effect have not been clearly defined. In this study, we extracted and characterized FAs from dried Lucilia sericata larvae and investigated the molecular basis by which FAs promote cutaneous wound healing. We first confirmed that FA sodium salts (FASSs) stimulated proliferation, migration, and tube formation of cultured human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner. We then showed that FASSs promoted endothelial-to-mesenchymal transition (EndMT), which plays an important role in stabilizing the neovasculature during angiogenesis. Mechanistically, FASSs up-regulated the expression of angiogenesis-related growth factors, platelet-derived growth factor (PDGF), transforming growth factor-ß1 (TGF-ß1), and vascular endothelial growth factor A (VEGFA), and activated angiogenesis-related signaling pathways, AKT, ERK, and TGF-ß/Smad3. In a rat acute cutaneous-wound model, FAs promoted wound healing. Following treatment, we further found that expression of anti-apoptosis-related factors (c-Myc and Bcl-2) was up-regulated and expression of apoptosis-related factors (p53 and Bad) was down-regulated. Our findings suggest that FAs can promote cutaneous wound healing by inducing angiogenesis, partly by activating AKT, ERK, and TGF-ß/Smad3 signaling.

Protective effect of phenolic acids from Chebulae Fructus immaturus on carbon tetrachloride induced acute liver injury via suppressing oxidative stress, inflammation and apoptosis in mouse.

Chebulae Fructus immaturus, a traditional Tibetan medicine, originated from the immature fruit of Terminalia chebula Retz., has been proven to have antioxidat function. However, its protection to injury liver cell caused by carbon tetrachloride (CCl4) has not been clarified. This study evaluated the effect of phenolic acid from Chebulae Fructus immaturus (PATC) on CCl4-induced acute liver injury in mice and related molecular mechanisms. Our data showed that PATC had convincing protective effects on the CCl4-induced acute liver injury by enhancing the anti-oxidative defense system, ameliorating inflammation and inhibiting the hepatocyte apoptosis.

Composition, Antivirulence Activity, and Active Property Distribution of the Fruit of Terminalia chebula Retz.

The fruit of Terminalia chebula Retz., or Tibet Olive, is widely used as a food supplement in China. It possesses some natural antimicrobial properties; however, its chemical composition and antivirulence effects have not been identified. In this work, 29 compounds were identified from the peel of T. chebula fruit by ultra-high-performance liquid chromatography-tandem quadrupole time-of-flight mass spectrometry. Both the extract of T. chebula and its phenolic acid, corilagin, showed antivirulent activity against Staphylococcus aureus. Specifically, they inhibited biofilm formation. The half maximal inhibitory concentration was 0.13 and 3.18 µg/mL for the extract and corilagin, respectively, whereas for α-hemolysin secretion, the respective concentrations were 30 and 10 µg/mL. Its mechanism of action may be due to reducing the transcription of genes related to quorum sensing. These genes included staphylococcal accessory regulator A, intercellular adhesion accessory gene regulator A, and RNAIII. These findings provide evidence that this food supplement could be an effective antivirulent with corilagin as its active ingredient. PRACTICAL APPLICATION: Corilagin from the fruit of Terminalia chebula Retz. may be used as an antibacterial for its antivirulent activity against Staphylococcus aureus.

Lonicerin, an anti-algE flavonoid against Pseudomonas aeruginosa virulence screened from Shuanghuanglian formula by molecule docking based strategy.

ETHNOPHARMACOLOGICAL RELEVANCE: The Shuanghuanglian formula (SF) is a famous antimicrobial and antiviral traditional Chinese medicine that is made of Lonicera japonica Thunb., Scutellaria baicalensis Georgi, and Forsythia suspensa (Thunb.) Vahl. According to the Chinese Pharmacopoeia, the SF is commonly administered in the forms of oral liquid, tablets, and injection. It has long been used to treat acute respiratory tract infections, especially lung infection. AIM OF THE STUDY: In the light of the increasing incidence of multidrug resistance to conventional antibiotics, the aim of this study was to screen potential anti-virulence agents against Pseudomonas aeruginosa from the extract of the SF. MATERIALS AND METHODS: The SF was used for effective compounds screening via the combination of the molecule docking approach and ultra-high-performance liquid chromatography-quadrupole/time of flight mass spectrometry. Fifty-one anti-virulence-related proteins were docked, 26 identified compounds were from SF. Subsequently, the top-scoring screened compound was assessed via bioactive-related assays, including the quantification of alginate biosynthesis, anti-biofilm assays, and the A549 human lung cells infection. RESULT: A flavonoid Lonicerin was found to be bonded with the active site of the alginate secretion protein (AlgE) with the highest score in molecule docking. Furthermore, we validated that Lonicerin could significantly reduce alginate secretion (25 µg/mL) and biofilm formation (12.5 µg/mL) at a sub-MIC concentration without inhibiting the proliferation of P. aeruginosa or influencing the expression of AlgE, which suggested that Lonicerin may directly inhibit AlgE. In addition, Lonicerin was proven to inhibit the infection of P. aeruginosa in the A549 cells. CONCLUSION: This work reported on the first potential AlgE antagonist that was derived from herbal resources. Lonicerin was proven to be an effective inhibitor in-vitro of P. aeruginosa infection.

Exploring the Therapeutic Composition and Mechanism of Jiang-Suan-Chu-Bi Recipe on Gouty Arthritis Using an Integrated Approach Based on Chemical Profile, Network Pharmacology and Experimental Support Using Molecular Cell Biology.

BACKGROUND: Gouty arthritis is a common metabolic disease caused by long-term purine metabolic disorder and elevated serum uric acid. Jiang-Suan-Chu-Bi recipe (JSCBR), a traditional Chinese herbal formula prescribed according to utilization frequency and cluster analysis, has been clinically validated remedy for gouty arthritis. However, its therapeutic composition and mechanism remains unclear. METHODS: In the present study, a simple, rapid, and sensitive ultraperformance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS)-based chemical profiling was firstly established for comprehensively identifying the major constituents in JSCBR. A phytochemistry-based network pharmacology analysis was further performed to explore the potential therapeutic targets and pathways involved in JSCBR bioactivity. Finally, THP-1 cell model was used to verify the prediction results of network pharmacology by western blot analysis. RESULTS: A total of 139 compounds containing phenolic acids, flavonoids, triterpenoid saponins, alkaloids, amino acids, fatty acids, anthraquinones, terpenes, coumarins, and other miscellaneous compounds were identified, respectively. 175 disease genes, 51 potential target nodes, 80 compounds, and 11 related pathways based on network pharmacology analysis were achieved. Among these pathways and genes, NOD-like receptor signaling pathway may play an important role in the curative effect of JSCBR on gouty arthritis by regulation of NRLP3/ASC/CASP1/IL1B. The results of cellular and molecular experiments showed that JSCBR can effectively reduce the protein expression of ASC, caspase-1, IL-1ß, and NRLP3 in monosodium urate-induced THP-1 cells, which indicated that JSCBR mediated inflammation in gouty arthritis by inhibiting the activation of NOD-like receptor signaling pathway. CONCLUSION: Thus, the integrated approaches adopted in the present study could contribute to simplifying the complex system and providing directions for further research of JSCBR.

Wedelolactone inhibits osteoclastogenesis but enhances osteoblastogenesis through altering different semaphorins production.

Our previous study showed that wedelolactone, isolated from Ecliptae herba, enhanced osteoblastogenesis but inhibited osteoclastogenesis through Sema3A signaling pathway. This study aims to investigate the role of other semaphorins in wedelolactone-enhanced osteoblastogenesis and -inhibited osteoclastogenesis. Wedelolactone inhibited RANKL-induced Sema4D and Sema7A production, but had no effect on RANKL-reduced Sema6D expression in osteoclastic RAW264.7 cells. In mouse bone marrow mesenchymal stem cells (BMSC), wedelolactone reversed osteogenic medium(OS)-reduced Sema7A expression and OS-enhanced Sema3E mRNA expression, but no effect on OS-reduced Sema3B mRNA expression. Addition of Sema4D antibody promoted wedelolactone-reduced TRAP activity and bone resorption pit formation. Wedelolactone combined with Sema4D antibody inhibited the formation of Sema4D-Plexin B1 complex. In co-culture of BMSC with RAW264.7 cells, Sema7A antibody, similar with Sema 3A antibody, reversed wedelolactone-enhanced ALP activity and mineralization level, but promoted wedelolactone-inhibited TRAP activity. However, Sema3E and Sema3B antibodies had no effect. Further, wedelolactone enhanced the binding of Sema7A with PlexinC1 and Beta1, but addition of Sema7A antibody partially blocked this binding. Our data demonstrated that wedelolactone inhibited Sema4D production and Sema4D-PlexinB1 complex formation in RAW264.7 cells, thereafter inhibiting osteoclastogenesis. At the same time, wedelolactone enhanced osteoblastogenesis through promoting Sema7A production and Sema7A-PlexinC1-Beta1 complex formation in BMSC.

Wedelolactone Enhances Osteoblastogenesis through ERK- and JNK-mediated BMP2 Expression and Smad/1/5/8 Phosphorylation.

Our previous study showed that wedelolactone, a compound isolated from Ecliptae herba, has the potential to enhance osteoblastogenesis. However, the molecular mechanisms by which wedelolactone promoted osteoblastogenesis from bone marrow mesenchymal stem cells (BMSCs) remain largely unknown. In this study, treatment with wedelolactone (2 µg/mL) for 3, 6, and 9 days resulted in an increase in phosphorylation of extracellular signal-regulated kinases (ERKs), c-Jun N-terminal protein kinase (JNK), and p38. Phosphorylation of mitogen-activated protein kinases (MAPKs), ERK and JNK started to increase on day 3 of treatment, and p38 phosphorylation was increased by day 6 of treatment. Expression of bone morphogenetic protein (BMP2) mRNA and phosphorylation of Smad1/5/8 was enhanced after treatment of cells with wedelolactone for 6 and 9 days. The addition of the JNK inhibitor SP600125, ERK inhibitor PD98059, and p38 inhibitor SB203580 suppressed wedelolactone-induced alkaline-phosphatase activity, bone mineralization, and osteoblastogenesis-related marker genes including Runx2, Bglap, and Sp7. Increased expression of BMP2 mRNA and Smad1/5/8 phosphorylation was blocked by SP600125 and PD98059, but not by SB203580. These results suggested that wedelolactone enhanced osteoblastogenesis through induction of JNK- and ERK-mediated BMP2 expression and Smad1/5/8 phosphorylation.

Wound-healing promoting effect of total tannins from Entada phaseoloides (L.) Merr. in rats.

The healing of wounds has always provided challenges for the medical community whether chronic or acute. Modern and traditional medicine has proved that herbal medicine shown superiority over chemical drugs. Herein, we report an Entada phaseoloides (L.) Merr. extract with a total tannin content of 76.18% showed wound-healing promoting effect in rat model. We found significantly accelerated wound closure already on day 7 in animals treated with total Entada phaseoloides (L.) Merr. tannins (TEPT) as compared to vaseline treated controls (p<0.05). At day 15, histologically, the wounds in animals treated with TEPT were completely closed as compared to controls. In vitro, TEPT promotes fibroblast proliferation and migration into wounds of NIH3T3 with concentration range of 9.38-37.50µg/ml. TEPT also had an inhibitory action against Staphylococcus aureus with MBC of 1.5mg/ml and the result was further proved by transmission electron microscope. Thus, TEPT could promote wound shrinkage, improve healing rate and promote healing of infectious wounds in rats. And this effect may due to antibacterial activities and NIH3T3 cell pro-proliferative effect of the tannins compounds, which indicating that TEPT can be used as efficient treatment in traumatic injury.

Antibacterial constituents of Fructus Chebulae Immaturus and their mechanisms of action.

BACKGROUND: To extract, purify, and identify the effective constituents of aqueous extract of Fructus Chebulae Immaturus, and analyze the bactericidal effects of total tannins. METHODS: Preparative thin layer chromatography and semi-preparative high performance liquid chromatography were used to isolate and purify the total tannin fraction. (1)H- and (13)C- NMR spectroscopy were used to elucidate compound structures. The antibacterial activities of total tannins and ethyl gallate on Klebsiella pneumoniae (KP) and Staphylococcus aureus (SA) were determined through minimum inhibitory concentration and minimum bactericidal concentration assays. Their antibacterial mechanisms of action were explored by transmission electron microscopy and scanning electron microscopy. RESULTS: Five compounds were isolated: ellagic acid, ethyl gallate, arjugenin, ß-sitosterol, and tri-n-butyl chebulate. Tri-n-butyl chebulate is a newly-reported compound. Total tannins and ethyl gallate both had favorable bactericidal effects against KP and SA. CONCLUSION: In vivo and in vitro pharmacodynamic experiment demonstrated that the effective components of Fructus Chebulae Immaturus possessed significant antibacterial effects, and were nontoxic and safe. TRIAL REGISTRATION: No results of a health care intervention on human participants.