Good Anti-inflammatory Activity Research Articles

Three new compounds from the fruits of Solanum virginianum L. and their anti-inflammatory activities

Three new compounds 1-glyceryl 9(β), 10(α), 11(β)-trihydroxy-12(Z)-octadecenoate, 2’S-20-O-p-hydroxyphenylpropionyloxy-20-hyd­roxyarachidic acid glycerol ester (2), 3-O-α-l-arabinopyranosyl-(1→6)-β-d-glucopyranoside of ethyl (3S)-hydroxybutanoate (3), as well as a new natural product (4) were isolated from the fruits of Solanum virginianum L. The structures of 26 compounds were determined by comprehensive spectroscopic analyses, NMR calculation, chemical methods, and comparisons of spectroscopic data. Compounds 2 and 16 exhibited good anti-inflammatory activity in the LPS-induced RAW 264.7 inflammatory model with IC50 values of 16.75 ± 1.54 and 22.43 ± 2.01 μM, respectively.

Salvia verticillata (L.)—Biological Activity, Chemical Profile, and Future Perspectives

Species belonging to the genus Salvia, Lamiaceae, have been deeply involved in the folk medicine of different nations since ancient times. Lilac sage, or Salvia verticillata L. (S. verticillata) is a less studied species from the genus. However, it seems to have a prominent potential for the future drug discovery strategies of novel phytopharmaceuticals. This review aims to summarise the data on the biological activity and the phytochemical profile of extracts and essential oils derived from S. verticillata. This review is based on data from 57 in vitro and in vivo studies. The chemical profile of S. verticillata includes different synergic compounds like phenolic acids, flavonoids, terpenes, and salvianolic acids. Although some small amounts of salvianolic acid B were found in S. verticillata extracts, the major compound among the salvianolic acids is salvianolic acid C, a compound associated with the potential for improving liver fibrosis, cardio- and hepatoprotection, and the inhibition of SARS-CoV-2 infection. The cannabinoid type 2 receptor agonist β-caryophyllene is one of the major compounds in S. verticillata essential oils. It is a compound with a prominent potential in regenerative medicine, neurology, immunology, and other medical fields. The in vivo and the in vitro studies, regarding S. verticillata highlighted good antioxidant potential, anti-inflammatory, antibacterial, and antifungal activity. S.verticillata was also reported as a potential source of drug candidates for the treatment of neurodegenerative diseases such as Alzheimer’s disease, because of the inhibitory activity on the acetylcholinesterase. However, the number of studies in this direction is limited.

ECM-mimetic, NSAIDs loaded thermo-responsive, immunomodulatory hydrogel for rheumatoid arthritis treatment

BackgroundRheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease, and it leads to irreversible inflammation in intra-articular joints. Current treatment approaches for RA include non-steroidal anti-inflammatory drugs (NSAIDs), disease-modifying anti-rheumatic drugs (DMARDs), corticosteroids, and biological agents. To overcome the drug-associated toxicity of conventional therapy and transdermal tissue barrier, an injectable NSAID-loaded hydrogel system was developed and explored its efficacy.ResultsThe surface morphology and porosity of the hydrogels indicate that they mimic the natural ECM, which is greatly beneficial for tissue healing. Further, NSAIDs, i.e., diclofenac sodium, were loaded into the hydrogel, and the in vitro drug release pattern was found to be burst release for 24 h and subsequently sustainable release of 50% drug up to 10 days. The DPPH assay revealed that the hydrogels have good radical scavenging activity. The biocompatibility study carried out by MTT assay proved good biocompatibility and anti-inflammatory activity of the hydrogels was carried out by gene expression study in RAW 264.7 cells, which indicate the downregulation of several key inflammatory genes such as COX-2, TNF-α & 18s.ConclusionIn summary, the proposed ECM-mimetic, thermo-sensitive in situ hydrogels may be utilized for intra-articular inflammation modulation and can be beneficial by reducing the frequency of medication and providing optimum lubrication at intra-articular joints.Graphical

Structure of Polysaccharide from Dendrobium nobile Lindl. and Its Mode of Action on TLR4 to Exert Immunomodulatory Effects.

Dendrobium nobile Lindl. polysaccharide (DNP1) showed good anti-inflammatory activity in our previous study. In this study, the structural characterization of DNP1 and its mode of action on TLR4 were investigated. Structural characterization suggested that DNP1 was a linear glucomannan composed of (1 → 4)-β-Manp and (1 → 4)-β-Glcp residues, and the acetyl group was linked to the C-2 of Manp. The possible repeating structural units of DNP1 were [→4)-2-OAc-β-Manp-(1→]3 →4)-β-Glcp-(1→. Surface plasmon resonance (SPR) binding test results showed that DNP1 did not bind directly to TLR4. The TLR4 and MD2 receptor blocking tests confirmed that DNP1 needs MD2 and TLR4 to participate in its anti-inflammatory effect. The binding energy of DNP1 to TLR4-MD2 was -7.9 kcal/mol, indicating that DNP1 could bind to the TLR4-MD2 complex stably. Therefore, it is concluded that DNP1 may play an immunomodulatory role by binding to the TLR4-MD2 complex and inhibiting the TLR4-MD2-mediated signaling pathway.

Effectiveness of Graptophyllum pictum L. Griff Extract as a Complementary Therapy for Peri-Implantitis: An In Vitro and In Silico Study

Background: Dental peri-implantitis is an inflammation that occurs in the peri-implant soft tissue and is accompanied by bone resorption, decreased osseointegration, and pockets. Graptophyllum pictum L. Griff extract may act as complementary therapy for peri-implantitis. Objectives: To investigate the effectiveness of G. pictum L. Griff extract as a complementary therapy for peri-implantitis. Materials and Methods: A phytochemical test was performed to determine the active compounds using each compound's reagents. Antioxidant assay to examine the antioxidant activity compared with vitamin C. Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) tests were used to investigate the antibacterial activity of Aggregatibacter actinomycetemcomitans (Aa), Porphyromonas gingivalis (Pg), Fusobacterium nucleatum (Fn), and Provotella intermedia (Pi) as peri-implantitis-related bacteria. Molecular docking is an in-silico test to visualize the interaction of G. pictum L. Griff molecules with targeted proteins using several software programs and databases. This study was analyzed by parametric and non-parametric variance analysis and continued with a post-hoc test. Results: G. pictum L. Griff extract contained flavonoids, alkaloids, saponins, tannins, steroids, and terpenoids. The antibacterial effect of G. pictum L. Griff can inhibit the growth of dental peri-implantitis-related bacteria such as Aa, Pg, Pi, and Fn with a minimum 25% extract concentration. In silico, the interaction of ethylcholest and proteins shows possible pharmalogical effects such as anti-inflammatory, antibacterial, and antioxidant activity. Conclusion: G. pictum L. Griff extract possesses good antibacterial, antioxidant, and anti-inflammatory activity that may be effective for dental peri-implantitis complementary therapy as documented in silico and in vitro.

In-vitro Anti-inflammatory Activity for Combination of Ethanol Extract from Sappan Wood (Caesalpinia sappan L.) and Red Ginger Rhizome (Zingiber officinale Roxb.)

Sappan wood and red ginger rhizome have been utilized as herbal medicine due to their anti-inflammatory, anti-oxidant, anti-microbial, analgesic, and immunomodulatory activities. Previous study revealed that sappan wood and red ginger rhizome showed good anti-inflammatory activity. However, the studies are focused on single extract. There are no research about combining the sappan wood extract and red ginger rhizome extract for antiinflammatory agent. Therefore, this study was conducted to determine the anti-inflammatory activity of the combination of sappan wood and red ginger rhizome ethanol extracts for antiinflammatory properties using red blood cell (RBC) membrane stabilization test. The tested samples consisted of sappan wood ethanol extract, red ginger rhizome ethanol extract, combination formulas (F1, F2, and F3), and positive control (diclofenac sodium). F1 comprises a 1:1 mixture of ethanol extract of sappan wood and red ginger rhizome, while F2 and F3 are composed of 2:1 and 1:2, respectively. The IC50 values for sappan wood ethanol extract, red ginger rhizome ethanol extract, and formulas F1, F2, and F3 were 47.63, 181.26, 101.93, 94.98, and 104.98 ppm, respectively. Statistical analysis using the one-way Anova followed by the Games-Howell post-hoc test revealed a statistically significant difference (p < 0.05) in the IC50 of each sample. For single extracts, sappan wood is better as an anti-inflammatory. Meanwhile, in the formulations, Formula F2 is superior as an anti-inflammatory agent

Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel Disease.

Inflammatory bowel disease (IBD) is a multifactorial chronic inflammation of the intestine and has become a global public health concern. A farnesoid X receptor (FXR) was recently reported to play a key role in hepatic-intestinal circulation, intestinal metabolism, immunity, and microbial regulation, and thus, it becomes a promising therapeutic target for IBD. In this study, we identified a series of nonbile acid FXR agonists, in which 33 novel compounds were designed and synthesized by the structure-based drug design strategy from our previously identified hit compound. Compound 33 exhibited a potent FXR agonistic activity, high intestinal distribution, good anti-inflammatory activity, and the ability to repair the colon epithelium in a DSS-induced acute enteritis model. Based on the results of RNA-seq analysis, we further investigated the therapeutic potential of the combination of compound 33 with 5-ASA. Overall, the results indicated that compound 33 is a promising drug candidate for IBD treatment.

Efficient biogenesis of calcium oxide nanoparticles using the extract of Eleusine coracana seeds and their application against multidrug-resistant ocular bacterial pathogens

Visual impairment due to corneal keratitis-causing bacteria is becoming a matter of health concern. The bacterial colonization and their resistance to multiple drugs need imperative attention. To overcome the issue of alternative remedial therapeutic agents, particularly for topical application, a study was carried out to synthesize calcium oxide nanoparticles (CaO NPs) using the biomaterial Eleusine coracana seed aqueous extract. The biosynthesized calcium oxide nanoparticles (CaO NPs) are non-toxic or less-toxic chemical precursors. Moreover, CaO NPs are eco-friendly and are used for several industrial, biomedical, and environmental applications. Biosynthesized CaO NPs were characterized using ultraviolet–visible spectroscopy, Fourier transform-infrared spectroscopy, scanning electron microscopy, and dynamic light scattering study. The synthesized CaO NPs exhibit with good anti-inflammatory activities with dose dependant (50–250 μg/mL). Moreover, Eleusine coracana-mediated CaO NPs significantly inhibited the multiple drug-resistant Gram-positive Staphylococci epidermidis and Enterococcus faecalis and Gram-negative Escherichia coli and Klebsiella pneumoniae that were isolated from the corneal ulcer. This study provides a potential therapeutic option for multiple drug-resistant corneal pathogens that cause vision impairment.

Flavonoid extracted from Epimedium attenuate cGAS-STING-mediated diseases by targeting the formation of functional STING signalosome.

Hyperactivation of the cyclic-GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING) signalling pathway has been shown to be associated with the development of a variety of inflammatory diseases, and the discovery of an inhibitor of the cGAS-STING signalling pathway holds great promise in the therapeutic interventions. Epimedium flavonoid (EF), a major active ingredient isolated from the medicinal plant Epimedium, has been reported to have good anti-inflammatory activity, but its exact mechanism of action remains unclear. In the present study, we found that EF in mouse bone marrow-derived macrophages (BMDMs), THP-1 (Tohoku Hospital Pediatrics-1) as well as in human peripheral blood mononuclear cells (hPBMC) inhibited the activation of the cGAS-STING signalling pathway, which subsequently led to a decrease in the expression of type I interferon (IFN-β, CXCL10 and ISG15) and pro-inflammatory cytokines (IL-6 and TNF-α). Mechanistically, EF does not affect STING oligomerization, but inhibits the formation of functional STING signalosome by attenuating the interaction of interferon regulatory factor 3 (IRF3) with STING and TANK-binding kinase 1 (TBK1). Importantly, in vivo experiments, EF has shown promising therapeutic effects on inflammatory diseases mediated by the cGAS-STING pathway, which include the agonist model induced by DMXAA stimulation, the autoimmune inflammatory disease model induced by three prime repair exonuclease 1 (Trex1) deficiency, and the non-alcoholic steatohepatitis (NASH) model induced by a pathogenic amino acid and choline deficiency diet (MCD). To summarize, our study suggests that EF is a potent potential inhibitor component of the cGAS-STING signalling pathway for the treatment of inflammatory diseases mediated by the cGAS-STING signalling pathway.

Evaluation of the Antioxidant and Anti-inflammatory Activity of the Anacyclus Valentinus L. Essential Oil and its Oxygenated Fraction.

Synthetic antioxidants and anti-inflammatories are widely used by the food and pharmaceutical industries. Like any synthetic product, these are toxic and represent a significant health risk. The objective of this study was to determine the chemical composition of Anacyclus valentinus essential oil and its oxygenated fraction, as well as their in-vitro antioxidant and anti-inflammatory properties. The essential oil was hydrodistilled using a Clevenger-type device and the oxygenated fraction was obtained by column chromatography using diethyl ether. The essential oil and its oxygenated fraction were analysed by GC and GC/MS. The antioxidant activities were performed using three different methods Radical scavenging activity (DPPH), β-carotene bleaching test, and the Ferric-Reducing Antioxidant Power (FRAP), using BHT as a positive control. The activity of antiinflammatory of essential oil and its oxygenated fraction was assessed by the protein denaturation method using the diclofenac sodium as a positive control. The essential oil of Anacyclus valentinus was represented mainly by oxygenated sesquiterpene compounds (37.7%), hydrocarbon sesquiterpenes (14.7%), oxygenated monoterpenes (18.4%) and non-terpenic compounds (15.6%). The oxygenated fraction was composed mainly of oxygenated sesquiterpenes (40.6%), oxygenated monoterpenes (38.5%), and non-terpene compounds (19.4%). Essential oil and oxygenated fraction showed antioxidant activity. The most potent activity was observed by the oxygenated fraction in the DPPH (IC50 = 8.2 mL/L) and β - carotene bleaching (IC50 = 5.6 mL/L) tests. While the essential oil of A. valentinus showed very good anti-inflammatory activity with an IC50 of 0.3 g/L higher than that of diclofenac (IC50= 0.53 g/L). The results showed that the essential oil and the oxygenated fraction of A. valentinus are rich in sesquiterpene compounds and possess interesting antioxidant and anti-inflammatory properties. However, other studies are necessary to be able to offer these extracts to the pharmaceutical and food industries.

Development of dental varnish based on red propolis for the treatment and prevention of dental caries

Caries is one of the most common chronic diseases in the world. To control and prevent the disease, it is important to expand the treatment options. The various types of propolis have been studied as alternatives. Studies have shown that Brazilian red propolis has important activity against S. mutans, as well as good anti-inflammatory activity. For the effective use of this alternative, it is necessary to develop pharmaceutical forms that make it feasible to handle and apply them. This study aims to produce a dental varnish based on red propolis, for later application in in vitro and in vivo studies. It is hoped that the formulation produced will conserve the good antimicrobial and anti-inflammatory activity of propolis and that it will be able to generate an innovative product for depositing patents with the National Institute of Industrial Property (INPI).

Phenolics and terpenoids with good anti-inflammatory activity from the fruits of Amomum villosum and the anti-inflammatory mechanism of active diterpene

The fruits of Amomum villosum are often considered a medicinal and food homologous material and have been found to have therapeutic effects in chronic enteritis, gastroenteritis, and duodenal ulcer. The aim of this study is to discover the anti-inflammatory active ingredients from dried ripe fruits of A. villosum and to elucidate the molecular mechanisms. We verified that the inhibitory activity of the ethyl acetate extract was superior to Dexamethasone (Dex), so we ultimately chose to study the ethyl acetate extract from the fruits of A. villosum. A total of 33 compounds were isolated from its ethyl acetate extract, including nine known diterpenoids (compounds 1–9), twelve known sesquiterpenoids (compounds 10–21), ten known phenolics (compounds 22, 23, 25–29, 31–33) and two new phenolics (24 and 30). On the basis of chemical evidences and spectral data analysis (UV, ECD, Optical rotation data, 1D and 2D-NMR, HR-ESI-MS, NMR chemical shift calculations), the structures of new compounds were elucidated. Among these compounds, isocoronarin D (5) was found to have good anti-inflammatory activity. Further research has found that isocoronarin D can down-regulate the protein levels of COX2 and NOS2, activate Nrf2/Keap1 and suppress NF-κB signaling pathway in LPS-induced RAW264.7 cells. In addition, isocoronarin D inhibited inflammasome assembly during inflammasome activation by hampering the binding of NLRP3 and ASC. Further evidence revealed that isocoronarin D suppressed the assembly of the NLRP3 inflammasome via blocking the formation of ASC specks. From these results, isocoronarin D may be the important bioactive compound of A. villosum and exhibits anti-inflammatory effects by regulating the NF-κB/Nrf2/NLRP3 axis in macrophages.

Tauroursodeoxycholic acid liposome alleviates DSS-induced ulcerative colitis through restoring intestinal barrier and gut microbiota

Ulcerative colitis (UC) is a chronic and progressive inflammatory disease that damages the colonic mucosa and disrupts the intestinal epithelial barrier. The current clinical treatment for UC is mainly chemotherapy, which has the limited effectiveness and severe side effects. It mainly focuses on the treatment of inflammation while neglecting the repair of the intestinal mucosa and the restoration of the microbiota balance. Here, we aimed to address these challenges by using an amphipathic bile acid -tauroursodeoxycholic acid (TUDCA) to replace cholesterol (CHL) in conventional liposomes. We prepared TUDCA/Emodin liposomes by incorporating the hydrophobic drug emodin. The experimental results indicated that TUDCA/Emodin Lip had uniform particle size distribution, good stability, low cytotoxicity, and exhibited good mucus permeability and anti-inflammatory activity in in vitro experiments, and was able to protect cells from oxidative stress. After oral administration, TUDCA/Emodin Lip significantly alleviated the severity of UC. This was evidenced by increased colon length, decreased inflammation and reduced colonic endoplasmic reticulum stress (ERS). Furthermore, TUDCA/Emodin Lip maintained the normal levels of the tight junction proteins Claudin-1 and ZO-1, thereby restoring the integrity of the intestinal barrier. Importantly, TUDCA/Emodin Lip also promoted the ecological restoration of the gut microbiota, increased overall abundance and diversity. Taken together, TUDCA/Emodin Lip can fundamentally restore intestinal homeostasis, this work provides a new, efficient and easily transformable treatment for UC.

Anti-inflammatory activity of a new lactone isolated from the leaves of Ardisia crenata Sims.

One new lactone (1) named Ardisicreolide C, together with three saponin compounds, Ardisiacrispin B (2), Ardisicrenoside A (3), Ardisiacrispin A (4) were isolated and identified from the leaves of Ardisia crenata Sims. The structures of 1-4 were elucidated by 1D, 2D-NMR and HR-MS spectra and together with the published data. In view of structures with lactone moieties showed good anti-inflammatory activity, the anti-inflammatory effects of Ardisicreolide C on LPS-induced RAW264.7 cells were evaluated by enzyme linked immunosorbent assay (ELISA) method. As a result, Ardisicreolide C could reduce release of nitric oxide (NO), tumour necrosis factor α (TNF-α), interleukin 1β (IL-1β), interleukin 4 (IL-4) and interleukin 10 (IL-10) of the cell supernatant to exert anti-inflammatory activity. This indicates that the leaves as non-medicinal parts of Ardisia crenata Sims contain compounds with good anti-inflammatory activity, which provides a new direction for the discovery of anti-inflammatory drugs.

Neocarya macrophylla (Chrysobalanaceae): Review of taxonomy, ethnobotany, phytochemistry and biological activities

The Neocarya macrophylla plant is used traditionally for food, medicinal, spiritual and industrial purposes. It is also used as a soap, dye, glue, fodder, termite repellent, firewood and for structural materials. Few studies on the physicochemical, nutritional content, phytochemical and pharmacological activities have validated the benefits of N. macrophylla to humanity as a food, in cosmetics or pharmaceutical products. The major bioactive constituents identified in the plant so far are steroids and flavonoids, such as, stigmasterol, quercetin, catechin and its related glycosides, as well as glucosamines. Extracts of the plant have shown good antivenom, antimicrobial, analgesic, anti-inflammatory, antimycobacterial, anthelmintic and antioxidant activities. Acute toxicity studies have confirmed the plant to be toxic. More studies on the plant are required in order to exploit other biological activities as claimed by traditional healers and also to isolate more bioactive compounds. In addition, the safety and tolerability assessment of N. macrophylla should be undertaken due to its widespread usage.

In vitro and in vivo anti-inflammatory models demonstrate oligopeptides play a significant role in anti-inflammatory properties of white tea

White tea is a kind of tea abundant in oligopeptides. The study aims to reveal the potential association between white tea oligopeptides and anti-inflammatory ability. Crude oligopeptide extracts of two subtype white tea (named BaiMudan and ShouMei) were prepared by removing known active substances including pigments, polyphenols, caffeine, polysaccharides, and free amino acids. Four abundant oligopeptides (LCAY, LLLSKKL, EVFAG, and ECDSCG) were identified through high-resolution mass spectrometry sequencing, and synthesized for anti-inflammation evaluation. In vitro experiments showed, expect there was no effect of EVFAG on TNF-α, the rests oligopeptides were all good at inhibit NO, IL-6, and TNF-α. In vivo experiments indicated a notable decrease in neutrophils of zebrafish yolk sac. Specifically, performance of LCAY was particularly outstanding, with its anti-inflammatory effect at 250 μg·mL−1 could exceed 100 μM dexamethasone. The prominent significance of this study is that it confirms white tea oligopeptides have a good anti-inflammatory activity.

Comparative Study of Cinchona Cinnamon Bark

Cinchona which belongs to family Rubiaceae, got its importance from the centuries because of its antimalarial activity. Alkaloids present in this herb, quinine, chichonine, quinidine and cinchonidine are the main, but percentage may vary in species to species. since the early 17 century, the sealkaloid are frequently used in Indian ayurvedic, siddha and traditional folk medicine to treating fever and still now in modern medicine cinchona alkaloids are used for the treatment of malaria as well as for other diseases and became the well-known drug after the treatment of malaria caused by Plasmodium Sp. Literature study revealed that along with the antimalarial activity the cinchona alkaloids has other potentially like anti-obesity, anticancer, anti-oxidant, anti-inflammatory , antimicrobial activity. Many herbal remedies have been employed in various medical systems for the treatment and management of different disease.Cinnamon is ever green tree of tropical area,a member of family Lauraceae, has been used in day to day routine as spice .Literature review on cinnamon releved that in mainly contain essential oil and important compounds like cinnamaldehyde, eugenol, cinnamic acid and cinnamon. It has got good anti-inflammatory, antioxidant, antimicrobial, antidiabetic, memory enhancer and many other Activities

Metabolomic analysis of black sesame seeds: Effects of processing and active compounds in antioxidant and anti-inflammatory properties

Black sesame seeds (BSS) have been recognized as a functional food due to their nutritional and therapeutic value for many years. In China, BSS is traditionally processed and consumed through two methods, namely, nine steaming nine sun-drying and stir-frying. The present study aimed to evaluate the effects of these processing techniques on the antioxidant and anti-inflammatory activities of BSS. UPLC-QTOF/MS was used for untargeted metabolomics to analyze the composition changes. The results indicated that the different samples had good antioxidant and anti-inflammatory activities, but thermal treatment reduced their activities. Untargeted metabolomics identified a total of 196 metabolites. Molecular docking studies targeting proteins associated with inflammation (iNOS) demonstrated that compounds acting as inhibitors were significantly reduced under both treatments. These results indicate that both nine steaming nine sun-drying and stir-frying lead to substantial loss of antioxidant, anti-inflammatory, and bioactive metabolites in BSS, which provides an important reference for its rational utilization.

Metabolites-Based Network Pharmacology to Preliminarily Verify In Vitro Anti-Inflammatory Effect of Ardisiacrispin B

Ardisiae Crenatae Radix is an ethnic medicinal herb with good anti-inflammatory activity. Ardisiacrispin B is one of the main components in Ardisiae Crenatae Radix extract, with a content of up to 16.27%, and it may be one of the pharmacological components through which Ardisiae Crenatae Radix exerts anti-inflammatory activity. At present, reports on ardisiacrispin B mainly focus on anti-tumor effects, and there have been no reports on anti-inflammatory activities. As a triterpenoid saponin, due to its large molecular weight and complex structure, the composition of substances that function in the body may include other forms after metabolism, in addition to compounds with original structures. Exploring the anti-inflammatory effects on the prototypes and metabolites of the compound may provide a more comprehensive response to the characteristics of ardisiacrispin B’s anti-inflammatory action. In this study, ardisiacrispin B was analyzed for metabolites to explore its metabolic processes in vivo. Subsequently, the anti-inflammatory effects of the prototypes and metabolites were further analyzed through network pharmacology, with the expectation of discovering the signaling metabolic pathways through which they may act. Finally, the anti-inflammatory effects of ardisiacrispin B in vitro and the effects on key signaling pathways at the protein level were explored. The results of this study showed that the isolated compounds were confirmed to be ardisiacrispin B. After the metabolite analysis, a total of 26 metabolites were analyzed, and the metabolism process in rats mainly involves oxidation, dehydration, glucuronide conjugation, and others. Speculation as to the anti-inflammatory molecular mechanisms of the prototypes and metabolites of ardisiacrispin B revealed that it may exert its anti-inflammatory effects mainly by affecting the PI3K-AKT pathway. Further anti-inflammatory mechanisms demonstrated that ardisiacrispin B had a good anti-inflammatory effect on LPS-induced RAW264.7 cells and a strong inhibitory effect on NO, TNF-α, and IL-1β release in cells. Furthermore, it had significant inhibitory effects on the expression of PI3K, P-PI3K, AKT, and P-AKT. This study supplements the gaps in the knowledge on the in vivo metabolic process of ardisiacrispin B and explores its anti-inflammatory mechanism, providing an experimental basis for the development and utilization of pentacyclic triterpenoids.

Combating Obesity: Harnessing the Synergy of Postbiotics and Prebiotics for Enhanced Lipid Excretion and Microbiota Regulation

Obesity is a chronic metabolic disease that can be induced by a high-fat diet (HFD) and predisposes to a variety of complications. In recent years, various bioactive substances, such as probiotics, prebiotics, and postbiotics, have been widely discussed because of their good anti-lipid and anti-inflammatory activities. In this paper, soybean protein isolate was used as a substrate to prepare the postbiotic. Compound prebiotics (galactose oligosaccharides, fructose oligosaccharides, and lactitol) preparation Aunulife Postbiotics and Prebiotics Composition (AYS) is the research object. Weight loss and bowel movements in mice induced by a high-fat diet were studied. Moreover, qualitative and quantitative analyses of small-molecule metabolites in AYS were performed to identify the functional molecules in AYS. After 12 weeks of feeding, the weight gain of mice that were fed with high-dose AYS (group H) and low-dose AYS (group L) from 4 to 12 weeks was 6.72 g and 5.25 g (p < 0.05), both of which were significantly lower than that of the high-fat diet (group DM, control group) group (7.73 g) (p < 0.05). Serum biochemical analysis showed that TC, TG, and LDL-C levels were significantly lower in mice from the H and L groups (p < 0.05). In addition, the fecal lipid content of mice in the L group reached 5.89%, which was significantly higher than that of the DM group at 4.02% (p < 0.05). The study showed that AYS changed the structure of the intestinal microbiota in mice on a high-fat diet, resulting in a decrease in the relative abundance of Firmicutes and Muribaculaceae and an increase in the relative abundance of Bacteroidetes, Verrucomicrobia, and Lactobacillus. The metabolomics study results of AYS showed that carboxylic acids and derivatives, and organonitrogen compounds accounted for 51.51% of the AYS metabolites, among which pantothenate, stachyose, betaine, and citrate had the effect of preventing obesity in mice. In conclusion, the administration of prebiotics and postbiotic-rich AYS reduces weight gain and increases fecal lipid defecation in obese mice, potentially by regulating the intestinal microbiota of mice on a high-fat diet.