Triterpenoid Saponins Research Articles

Simultaneous determination and pharmacokinetics study of three triterpenoid saponins in rat plasma by ultra-high-performance liquid chromatography tandem mass-spectrometry after oral administration of Astragalus Membranaceus leaf extract.

A selective and sensitive ultra-high-performance liquid chromatography-tandem mass spectrometry method was developed and validated for the determination of three triterpenoid saponins isolated from Astragalus membranaceus leaf extract. In this article, a method for simultaneous determination of Huangqiyenin A, Huangqiyenin E, and Huangqiyenin K was established for the first time. The method was successfully applied to the pharmacokinetic study of Astragalus membranaceus leaf extract after oral administration. Liquid-liquid extraction was applied to plasma sample preparation. Multiple reaction monitoring mode with an electrospray ion source in positive electrospray ionization was chosen to quantify the analytes. Chromatographic separation was performed on a Waters HSS T3 column, using gradient elution with a mobile phase composed of acetonitrile and 5mM ammonium acetate/water. The pharmacokinetic results showed that all three compounds had the characteristics of rapid absorption-slow metabolism trend. The time of maximum plasma concentration of Huangqiyenin A is higher than Huangqiyenin E and Huangqiyenin K. And the maximum plasma concentration of Huangqiyenin A is higher as well. The pharmacokinetic results revealed the pharmacokinetic characteristics of the three analytes in rat plasma, which could provide a helpful reference for the further study of Astragalus membranaceus leaf extract.

Central and peripheral analgesic active components of triterpenoid saponins from Stauntonia chinensis and their action mechanism.

Triterpenoid saponins from Stauntonia chinensis have been proven to be a potential candidate for inflammatory pain relief. Our pharmacological studies confirmed that the analgesic role of triterpenoid saponins from S. chinensis occurred via a particular increase in the inhibitory synaptic response in the cortex at resting state and the modulation of the capsaicin receptor. However, its analgesic active components and whether its analgesic mechanism are limited to this are not clear. In order to further determine its active components and analgesic mechanism, we used the patch clamp technique to screen the chemical components that can increase inhibitory synaptic response and antagonize transient receptor potential vanilloid 1, and then used in vivo animal experiments to evaluate the analgesic effect of the selected chemical components. Finally, we used the patch clamp technique and molecular biology technology to study the analgesic mechanism of the selected chemical components. The results showed that triterpenoid saponins from S. chinensis could enhance the inhibitory synaptic effect and antagonize the transient receptor potential vanilloid 1 through different chemical components, and produce central and peripheral analgesic effects. The above results fully reflect that "traditional Chinese medicine has multi-component, multi-target, and multi-channel synergistic regulation".

Characterisation of saponins from Hedera nepalensis in Vietnam northwest mountainous areas with the aid of high-resolution mass spectrometry

This research aims to explore the saponins composition of H. nepalensis in four northwest mountainous areas of Vietnam including Ha Giang, Lai Chau, Lao Cai, and Lang Son with the aid of high-resolution mass spectrometry. As a result, 42 saponins are successfully identified in H. nepalensis leaves by UHPLC‐Q‐TOF-MS/MS analyses, in which two 30-noroleanane and four oleanane triterpene saponins structures have been reported for the first time. Two structures of compound 20 were discovered in four samples. Two structures of compound 8 were found in H. nepalensis from Ha Giang and Lao Cai, while two structures of compound 28 were not observed in Lang Son. Different environmental and climatic circumstances in various places may have an impact on chemical constituents of H. nepalensis. By providing the phytochemicals profile of H. nepalensis leaves, our study supports the orientation for future research on this medicinal plant as well as other Hedera species.

In-Silico Validation of Glycyrrhizin against Proinflammatory Mediator COX-2: Anti-Proliferative Potential

Background: Licorice's scientific name is Glycyrrhiza glabra. It is a well-known medicinal plant that grows in numerous locations throughout the world. It is one of the most ancient and widely utilised plants and has been used for a very long period in both western and eastern nations. The primary source of the triterpenoid saponin, glycyrrhizic acid (also known as glycyrrhizin), which is a sweeter component and around 50 times sweeter than sugar, was the Glycyrrhiza glabra (Fabaceae) root. Glycyrrhetinic acid has been found as the chemical constituent of glycyrrhizin. Aim: The current work sought to elucidate the molecular basis for glycyrrhizin's antiproliferative activity against the COX-2 enzyme, which functions as a proinflammatory factor in proliferation. Method: A molecular docking method was employed in the current work to look for COX 2 protein inhibitors. The binding was determined by the Auto Dock software utilising a grid-based docking method. Compounds' 2D structures were constructed using the Merck Molecular Force Field, converted to 3D, and then energetically reduced up to an arms gradient of 0.01. (MMFF). Results: The molecular docking result revealed that glycyrrhizin showed encouraging docking score. The docking score found to be -7.7 kcal mol–1. Conclusion: The interaction of ligand hits to targeted site and docking score finding it can be predicted that glycyrrhizin found in the plants G.glabra exhibited good inhibitor of COX 2 protein inhibitors.

Characterization of the horse chestnut genome reveals the evolution of aescin and aesculin biosynthesis

Horse chestnut (Aesculus chinensis) is an important medicinal tree that contains various bioactive compounds, such as aescin, barrigenol-type triterpenoid saponins (BAT), and aesculin, a glycosylated coumarin. Herein, we report a 470.02 Mb genome assembly and characterize an Aesculus-specific whole-genome duplication event, which leads to the formation and duplication of two triterpenoid biosynthesis-related gene clusters (BGCs). We also show that AcOCS6, AcCYP716A278, AcCYP716A275, and AcCSL1 genes within these two BGCs along with a seed-specific expressed AcBAHD6 are responsible for the formation of aescin. Furthermore, we identify seven Aesculus-originated coumarin glycoside biosynthetic genes and achieve the de novo synthesis of aesculin in E. coli. Collinearity analysis shows that the collinear BGC segments can be traced back to early-diverging angiosperms, and the essential gene-encoding enzymes necessary for BAT biosynthesis are recruited before the splitting of Aesculus, Acer, and Xanthoceras. These findings provide insight on the evolution of gene clusters associated with medicinal tree metabolites.

Total Content of Saponins, Phenols and Flavonoids and Antioxidant and Antimicrobial Activity of In Vitro Culture of Allochrusa gypsophiloides (Regel) Schischk Compared to Wild Plants.

Allochrusa gypsophiloides is a rare Central Asian species, a super-producer of triterpene saponins with pharmacological and technical value. In this work, a comparative evaluation of the in vitro culture of adventitious roots (ARs), in vitro adventitious microshoots (ASs), natural roots and aboveground parts of wild plants from Kazakhstan to define the total saponin (TS), phenol (TP) and flavonoid (TF) content, as well as antioxidant (AOA) and antimicrobial activity, is presented for the first time. In the AR culture, growth index (GI), TS, TP and TF were evaluated on days 25, 45 and 60 of cultivation on ½ MS medium without (control) and with auxin application. It was found out that TS and TF were higher in the in vitro AR culture. The amount of TP and TF are higher in the aerial part of vegetative plants with maximum AOA. The concentration of the extract required to inhibit 50% of 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical formation (ICO50) in extracts from natural material negatively correlated with TS, TP, TF and in the in vitro AR culture with TF. Control extracts from the in vitro AR culture with high TS levels showed growth-inhibitory activity against S. thermophillus, S. cerevisiae and C. albicans. The influence shares of medium composition factor, cultivation duration factor and their interaction with GI, TS, TP and TF were determined. The in vitro AR culture is promising for obtaining triterpene saponins TSR with high antibacterial and antifungal activity, and the in vitro ASs culture-for shoot multiplication with antioxidant properties.

Is bitter actually better? Targeting a soyasaponin acetyltransferase affects soybean seed germination.

This Highlight features a recent study showing that the soybean BAHD-type soyasaponin acetyltransferase GmSSAcT1 is responsible for three or four sequential acetylation steps in type-A soyasaponin biosynthesis and that loss of GmSSAcT1 function strongly inhibits soybean seed germination.

Four new triterpene saponins from Cephalaria speciosa and their potent cytotoxic and immunomodulatory activities

Four new triterpene saponins, namely speciosides A-D (1–4) along with six known saponins were isolated from the n-butanol extract of Cephalaria speciosa. In addition to these, three new prosapogenins (2a–4a) were obtained after alkaline hydrolysis. Elucidation of the structures of the isolated compounds was carried out by 1D, 2D NMR, HR-ESI/MS and GC–MS analyses. Cytotoxic activity was investigated on A549, CCD34-Lu, MDA-MB-231, PC-3, U-87MG, HeLa, HepG-2 cells by MTT method. Additionally, the immunomodulatory effect of compounds was evaluated for macrophage polarization with/without inactivated IBV D274 antigen treatment on THP-1 cells originated macrophage cells in terms of M1 or M2. According to the cytotoxicity results, compound 1 and prosapogenin 2a exhibit significant cytotoxicity than doxorubicin by comparison. The results demonstrated that saponin molecules treated THP-1 originated macrophages were induced M1 and/or M2 polarization. Additionally, macrophage cells treated with/without IBV D274 antigen contained saponin compounds were triggered significantly M2 polarization relative to M1. Notably, monodesmosidic saponins (1 and 2a–4a) in comparison with bisdesmosidic ones (2–4) demonstrated the most effect on M2 polarization. In conclusion, the results showed that all the isolated new saponins and their prosapogenins have immunomodulatory potential on macrophage cells increasing immune response without significant cytotoxic effect on THP-1 originated macrophages.

Pharmacological Mechanisms and Adjuvant Properties of Licorice Glycyrrhiza in Treating Gastric Cancer.

Licorice is a remarkable traditional Chinese medicine obtained from the dried root and rhizomes of the Glycyrrhiza genus, and t has been utilized in China for many centuries. It consists of more than 300 compounds that are mainly divided into triterpene saponins, flavonoids, polysaccharides, and phenolic components. The active compounds of licorice have been found to possess multiple biological activities, including antitumor, anti-inflammatory, antiviral, antimicrobial, immunoregulatory, cardioprotective, and neuroprotective functions. In addition to providing a brief overview of licorice's adjuvant properties, this review describes and analyzes the pharmacological mechanisms by which licorice components function to treat gastric cancer. Furthermore, licorice compounds are also found to be potent adjuvant chemotherapy agents, as they can improve the quality of life of cancer patients and alleviate chemotherapy-induced adverse effects.

The chemical constituents and metabolite profiles of Huangqin decoction in normal and ulcerative colitis rats by UHPLC-Q-TOF/MS analysis

Ulcerative colitis (UC) is a recurrent and palliative inflammatory bowel disease (IBD) begins in distal colon and spreads proximally to the entire colon, characterized by mucosal inflammation which reduces patients' quality of life and increases the risk of bowel cancer. Huangqin decoction (HQD), a classical Chinese formula recorded in Treatise on Febrile Diseases has been widely used for the treatment of UC. Studies found that HQD has good curative effect on UC. However, the chemical constituents and metabolites of it has not been fully elucidated due to lack of in vitro and in vivo studies, which also limits the pathogenesis study and clinical application of UC. In this study, a rapid and high-throughput UHPLC-Q-TOF/MS method was established and applied to analyse the chemical constituents and metabolites of HQD. Besides, we established an UC rat model and compared the differences of metabolite profiles between normal and UC rats both in plasma and urine. A total of 139 constituents were chemically defined or tentatively identified, including 98 flavonoids, 10 triterpene saponins, 10 monoterpene glycosides, 4 phenols, 5 phenylethanoid glycosides and 12 other types of compounds. A total of 175 and 147 HQD-related xenobiotics were detected in normal and UC rats, respectively. The main metabolic pathways of HQD were methylation, hydrolysis, hydroxylation, glucuronidation and sulfation. The holistic metabolic profiles of HQD revealed that normal and UC rats had certain differences in drug absorption and metabolism. This study can provide references for the follow-up study of HQD, and provide essential data for the further study of the relationships between chemical constituents and pharmacological activities of HQD.

CHEMICAL ANALYSIS AND BIOLOGICAL ACTIVITY OF TURKESTAN SOAPROOT ALLOCHRUSA GYP-SOPHILOIDES (REGEL) SCHISCHK GROWING IN THE SOUTH OF KAZAKHSTAN

Allochrusa gypsophiloides (Regel) Schischk. Turkestan soaproot (TSR), a Central Asian endemic has commercial value as a producer of triterpene saponins. Spectrophotometric determination of saponins was carried out in the roots and the aerial part of wild plants during vegetation in the south of Kazakhstan. The level of saponins, phenols, and flavonoids in the seeds, aerial parts, and roots was assessed. The following ascending order in the saponins content: seeds-aerial part-root, was revealed. An increase in the saponins levels in the roots during the growing season with a maximum of 9.6% in fruiting was established. A high saponins amount (6%) was detected in the aerial part during the flowering which decreased twice at the fruiting. The antioxidant activity and foaming index of the total ethanol extracts from the initial and deposited plant materials were determined. The maximum antioxidant activity (35.5%) and antiradical properties (IC50 1480) in vitro were found in extracts from the aerial part with the highest content of flavonoids and phenols. It was revealed that long-term storage of roots contributes to an increase in saponins levels and in their surfactant properties. The data obtained indicate the possibility of alternative use of the aerial parts of Allochrysa gypsophiloides at the flowering for obtaining triterpene saponins and phenolic substances with antioxidant activity.

Application of UPLC-Triple TOF-MS/MS metabolomics strategy to reveal the dynamic changes of triterpenoid saponins during the decocting process of Asian ginseng and American ginseng.

Triterpenoid saponins are the main bioactive components contributed to the nutritional value of ginseng, and different process conditions will affect their content and quality. To study the holistic characterization and dynamic changes of triterpenoid saponins in Asian ginseng (ASG) and American ginseng (AMG) during soaking and decoction, a UPLC-Triple TOF-MS/MS-based metabolomics strategy was used to characterize and discover differential saponin markers. In total, 739 triterpenoid saponins (including 225 potential new saponins) were identified from ASG and AMG in untargeted metabolomics. Based on PCA and OPLS-DA, 51 and 48 saponin markers were screened from soaked and decocted ASG and AMG, respectively. Additionally, targeted metabolomics analysis and HCA of 22 ginsenoside markers suggested that decoction of ASG and AMG for 2h to 4h could significantly increase the contents of rare ginsenosides (G), such as G-Rg3, G-Rg5, G-F4. This study provides a scientific insight that high boiling combined with simmering enriches ASG and AMG extracts with rich rare ginsenosides that are more beneficial to human health.

Steroid and triterpenoid saponins from the rhizomes of Paris polyphylla var. stenophylla.

Five new saponins, including three steroid saponins, paristenoids A-C (1-3), and two triterpenoid saponins, paristenoids D-E (4-5), along with four known ones (6-9) were isolated from the rhizomes of Paris polyphylla var. stenophylla. The structures of the isolated compounds were identified mainly by detailed spectroscopic analysis, including extensive 1D and 2D NMR, MS, as well as chemical methods. Compound 3 is a new cyclocholestanol-type steroidal saponin with a rare 6/6/6/5/5 fused-rings cholestanol skeleton, and this skeleton has been first found from the genus Paris. The cytotoxicities of the isolated compounds against three human three glioma cell lines (U87MG, U251MG and SHG44) were evaluated, and compound 7 displayed certain inhibitory effect with IC50 values of 15.22 ± 1.73, 18.87 ± 1.81 and 17.64 ± 1.69 μmol·L-1, respectively.

Chemical constituents and mechanism of Chuanzhi Tongluo Capsules based on UPLC-Q-Exactive Orbitrap-MS and network pharmacology

The chemical constituents of Chuanzhi Tongluo Capsules were analyzed and identified using ultra-high performance liquid chromatography-quadrupole/electrostatic field orbitrap high-resolution mass spectrometry(UPLC-Q-Exactive Orbitrap-MS) to clarify the pharmacological substance basis. In addition, network pharmacology was employed to explore the mechanism of Chuanzhi Tongluo Capsules in the treatment of cerebral infarction. Gradient elution was performed using acetonitrile and 1% acetic acid in water as the mobile phase. Mass spectrometry was performed in positive and negative ion modes. Xcalibur 4.2 software was used for compound analysis, including accurate mass-to-charge ratio and MS/MS fragment information, combined with the comparison of reference standards and literature data. A total of 152 compounds were identified, including 32 organic acids, 35 flavonoids and their glycosides, 33 diterpenes, 13 phthalides, 12 triterpenes and triterpene saponins, 23 nitrogen-containing compounds, and 4 other compounds, and their fragmentation patterns were analyzed. SwissTargetPrediction, GeneCards, DAVID, and other databases were used to predict and analyze the core targets and mechanism of Chuanzhi Tongluo Capsules. Protein-protein interaction(PPI) network topology analysis identified 10 core targets, including TNF, VEGFA, EGFR, IL1B, and CTNNB1. KEGG enrichment analysis showed that Chuanzhi Tongluo Capsules mainly exerted their effects through the regulation of lipid and atherosclerosis, glycoproteins in cancer, MicroRNAs in cancer, fluid shear stress, and atherosclerosis-related pathways. Molecular docking was performed between the key constituents and core targets, and the results demonstrated a strong binding affinity between the key constituents of Chuanzhi Tongluo Capsules and the core targets. This study comprehensively elucidated the chemical constituents of Chuanzhi Tongluo Capsules and explored the core targets and mechanism in the treatment of cerebral infarction based on network pharmacology, providing a scientific reference for the study of the pharmacological substance basis and formulation quality standards of Chuanzhi Tongluo Capsules.

Chemical Composition and Therapeutic Effects of Some <i>Astragalus</i> (Fabaceae) Species

Abstract—The review integrates information on the studies of component composition and biological activity of some Astragalus L. (Fabaceae) species published over the last 5–7 years. The aerial and underground parts of 34 Astragalus species contain triterpene saponins, flavonoids, polisaccharides, tannins, free organic acids, higher fatty acids, vitamins, trace elements, and other constituents. Among Astragalus species, the best studied in relation to component composition and biological activity is A. membranaceus (Fisch.) Bunge. In vitro and in vivo experimental studies suggest that total amount of bioactive substances, fractions of and individual compounds extracted from different parsts of A. membranaceus and A. membranaceus var. mongholicus exhibit anti-inflammatory, immunomodulatory, antioxidant, anticancer, cardiportactive, and hepathoprotective activity. The composition and biological effects of other Astragalus species have been little studied. The review synthesizes recent advances in the studies of new compounds extracted from Astragalus species, and on their biological activity.

Bidesmosidic and monodesmosidic triterpenoid saponins from the grain of Amaranthus hypochondriacus

Five known bidesmosidic triterpenoid saponins (1–5) and their hydrolysates, namely two new monodesmosidic triterpenoid saponins (1′ and 2′) and three known saponins (3′–5′), were isolated from Amaranthus hypochondriacus seeds. The structures of the new compounds were determined using interpreting 1D and 2D nuclear magnetic resonance (NMR) data and high-resolution electrospray ionisation mass spectrometry (HRESI-MS) analyses as 3-O-β-D-glucuronopyranosyl-30-normedicagenic acid (1′) and 3-O-[α-L-rhamnopyranosyl (1 → 3)-β-D-glucuronopyranosyl] bayogenin (2′). For the first time, 5 and 5′ were isolated from Medicago plants as the first examples of glycosides in medicagenic acid from Amaranthus plants. While bidesmosidic saponins showed no cytotoxicity, monodesmosidic saponins, except for 1′, showed moderate cytotoxicity against human cervix adenocarcinoma (HeLa) cells. In addition, monodesmosidic saponins showed anti-fungal activity against the rice blast fungus (Pyricularia oryzae).

Calenduloside E ameliorates non-alcoholic fatty liver disease via modulating a pyroptosis-dependent pathway.

Ethnopharmacological relevanceNon-alcoholic fatty liver disease (NAFLD) is a prevalent chronic liver condition that can have multiple underlying causes. There are no satisfactory chemical or biological drugs for the treatment of NAFLD. Longyasongmu, the bark and root of Aralia elata (Miq.) Seem, is used extensively in traditional Chinese medicine (TCM) and has been used in treating diverse liver diseases including NAFLD. Based on Aralia elata (Miq.) Seem as the main ingredient, Longya Gantai Capsules have been approved for use in China for the treatment of acute hepatitis and chronic hepatitis. Calenduloside E (CE), a natural pentacyclic triterpenoid saponin, is a significant component of saponin isolated from the bark and root of Aralia elata (Miq.) Seem. However, the role and mechanism of anti-NAFLD effects of CE is still unclear. Aim of the studyThe objective of this study was to examine the potential mechanisms underlying the protective effect of CE on NAFLD. Materials and methodsIn this study, an NAFLD model was established by Western diet in apoE−/− mice, followed by treatment with various doses of CE (5 mg/kg, 10 mg/kg). The anti-NAFLD effect of CE was assessed by the liver injury, lipid accumulation, inflammation, and pro-fibrotic phenotype. The mechanism of CE in ameliorating NAFLD was studied through transcriptome sequencing (RNA-seq). In vitro, the mouse hepatocytes (AML-12) were stimulated in lipid mixtures with CE and performed the exploration and validation of the relevant pathways using Western blot, immunofluorescence, etc. ResultsThe findings revealed a significant improvement in liver injury, lipid accumulation, inflammation, and pro-fibrotic phenotype upon CE administration. Furthermore, RNAseq analysis indicated that the primary pathway through which CE alleviates NAFLD involves pyroptosis-related inflammatory cascade pathways. Furthermore, it was observed that CE effectively suppressed inflammasome-mediated pyroptosis both in vivo and in vitro. Remarkably, the functional enrichment analysis of RNA-seq data revealed that the PI3K-Akt signaling pathway is the primarily Signaling transduction pathway modulated by CE treatment. Subsequent experimental outcomes provided further validation of CE's ability to hinder inflammasome-mediated pyroptosis through the inhibition of PI3K/AKT/NF-κB signaling pathway. ConclusionsThese findings present a novel pharmacological role of CE in exerting anti-NAFLD effects by inhibiting pyroptosis signaling pathways.

A new triterpene saponin and known compounds from the polar extract of Salvia argentea L. and evaluation of their antioxidant activity

A new triterpene saponin, 2, 3, 21, 23-tetrahydroxyolean-12-en-28-oic-acid-28-O-β-D- glucosyl-(2’’→1’)-β-D-glucoside (1), was isolated from the n-butanol extract of dried aerial parts of Salvia argentea L. (Lamiaceae) in addition to two known flavonoids, apigenin 7-O-β-D-glucoside (2), threo-guaiacylglycerol 3-O-[6-O-p-hydroxybenzoyl]-β-D-glucoside (3), luteolin 7-O-β-D-glucoside (4), verbascoside (5) and rosmarinic acid (6). The structure elucidation of these compounds was based on analyses of spectroscopic data including 1D-, 2D-NMR and HR-ESI-MS techniques and by comparing their NMR data with those reported in the literature. Compound 6 exhibited the highest antioxidant activity in DPPH assay (IC50<3.00 µg/mL) which was better than the standards BHA, BHT, Trolox and ascorbic acid.

Efficient remediation of soils contaminated with petroleum hydrocarbons using sustainable plant-derived surfactants

Surfactant-enhanced multiphase extraction is recognized as an effective method to remove petroleum related contaminants from soil. Owing to the high biodegradability and low biotoxicity, plant-derived surfactants are considered as promising alternatives to synthetic surfactants. In this study, two plant surfactants were respectively extracted from Sapindus mukorossi (PS-1) and Fructus Gleditsiae sinensis (PS-2). Component analysis and chemical structure characterization indicated that triterpenoid saponins were the main components of both plant surfactants. The removal efficiency of tetradecane by PS-1 and PS-2 was 75.6% and 62.2%, respectively, which was comparable with that by Tween-80. The results were validated by column leaching experiments. The abundant hydroxyl, aldehyde and epoxy groups in the plant surfactants made them readily self-assemble to form micelles via hydrogen bonding and van der Waals interactions, which promoted the solubilization of tetradecane in the liquid phase, particularly at appropriate ionic strength and temperature. Due to the reduced electrostatic attraction by the acidic and ionizable functional groups in the plant surfactants, their sorption capacities (0.15 and 0.24 g1−n Ln·kg−1 for PS-1 and PS-2, respectively) onto the soil were much lower than that of Tween-80, making them much easier to be extracted from contaminated soil. This study would deepen our understanding to improve the performances of plant surfactants in petroleum hydrocarbons-contaminated soil remediation.

Asperosaponin VI protects alcohol-induced hepatic steatosis and injury via regulating lipid metabolism and ER stress

BackgroundAsperosaponin VI (AVI) is a natural triterpenoid saponin isolated from Dipsacus asper Wall with documented anti-inflammatory and bone protective effects. Our previous work reported that AVI protects the liver of septic mice from acute inflammatory damage. In this paper, we further explored the protective effect and the potential mechanisms of AVI in alcoholic fatty liver disease (AFLD). MethodsThe Lieber-Decarli model was constructed to evaluate the effect of AVI on AFLD in C57BL/6 J mice. Additional in vitro work was performed to investigate HepG2 cells exposed to alcohol, then analyzed the degree of liver injury by detecting the ALT and AST levels both in the liver and serum. H&E staining and Sirius red staining were used to evaluate the histopathology variations in the liver. Further, observe lipid droplets in the cytoplasm by Oil Red O staining. We detected the expression of inflammatory cytokines with qualitative PCR; ROS, MDA, SOD, and GSH-px levels were analyzed to observe oxidative stress. Finally, exploring the activation of AMPK signaling pathway by real-time PCR and Western blotting. ResultsHistological examination of liver tissue combined with serum ALT and AST levels showed a significant protective effect of AVI against alcoholic liver injury in AFLD mice. Compared with the model group, AVI evidently improved antioxidant capacity, reduced inflammatory response and lipid accumulation both in vitro and in vivo. For mechanically, it was found that AVI up-regulated phosphorylation level of AMP-activated protein kinase (AMPK) and inhibited the endoplasmic reticulum stress (ER) pathway in AFLD. ConclusionAVI protects mice from alcohol-induced hepatic steatosis and liver injury through activating AMPK signaling and repress ER stress, suggesting that it might be a potential therapeutic agent for AFLD.