Good Anti-inflammatory Activity Research Articles

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.

Highly swellable, cytocompatible and biodegradeable guar gum-based hydrogel system for controlled release of bioactive components of liquorice (Glycyrrhiza glabra L.): Synthesis and evaluation

Glycyrrhiza glabra Linn (liquorice) has been widely used for therapeutic purposes to treat digestive disorders, immunomodulatory disorders, inflammatory disorders, diabetes, viral infections, and cancer. Liquorice contains a wide variety of bioactive compounds, including glycyrrhizin, flavonoids, and terpenoids. Several factors compromise their therapeutic efficacy, such as poor pharmacokinetic profiles and physicochemical properties. Therefore, to improve its overall effectiveness, liquorice solid dispersion (LSD) was incorporated into biopolymer-based guar gum-grafted-2-acrylamido-2-methylpropane sulfonic acid (Guar gum-g-AMPS) hydrogels designed for controlled delivery via the oral route and characterized. The qualitative analysis of LSD revealed 51 compounds. Hydrogel structural properties were assessed for their effect on swelling and release. The highest swelling ratio (6413 %) and drug release (84.12 %) occurred at pH 1.2 compared to pH 7.4 (swelling ratio of 2721 % and drug release of 79.36 %) in 48 h. The hydrogels exhibited high porosity (84.23 %) and biodegradation (9.30 % in 7 days). In vitro hemolysis tests have demonstrated the compatibility of the hydrogel with blood. CCK-8 assay confirmed the biocompatibility of the synthesized hydrogel using osteoblasts and RIN-m5f cells. LSD exhibited good anti-inflammatory activity when loaded into hydrogels after being subjected to protein denaturation experiments. Moreover, LSD-loaded hydrogels have good antioxidant and antibacterial properties.

Enzymatic and ultrasound assisted β-cyclodextrin extraction of active ingredients from Forsythia suspensa and their antioxidant and anti-inflammatory activities

With the proposal of the 2030 Agenda for Sustainable Development, the Chinese medicine extraction technology has been innovatively improved to prioritize low energy consumption, sustainability, and minimized organic solvent utilization. Forsythia suspensa (FS) possesses favorable pharmacological properties and is extensively utilized in traditional Chinese medicine. However, due to the limitations of the composition and extraction methods, its potential has not been fully developed. Thus, a combination of ultrasound-assisted extraction (UAE), enzyme-assisted extraction (EAE), and β-cyclodextrin extraction (β-CDE) was employed to isolate and purify rutin, phillyrin, and forsythoside A from FS. The results demonstrated that the efficiency of extracting enzymatic and ultrasound assisted β-cyclodextrin extraction (EUA-β-CDE) was highly influenced by the temperature and duration of hydrolysis, as well as the duration of the extraction process. According to the results of the single-factor experiment, Box-Behnken design (BBD) in Response surface method (RSM) was used to optimize the experimental parameters to achieve the maximum comprehensive evaluation value (CEV) value. The EUA-β-CDE compared with other extraction methods, has good extraction effect and low energy consumption by high performance liquid chromatography (HPLC), scanning electron microscopy (SEM), calculation of power consumption and CO2 emission The EUA-β-CDE compared with other extraction methods, has good extraction effect and low energy consumption by HPLC, SEM, calculation of power consumption and CO2 emission. Then, the structural characteristics of EUA-β-CDE of FS extract had significant interaction with β-CD by Fourier infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). In addition, EUA-β-CDE extract has good antioxidant and anti-inflammatory activities. The establishment of EUA-β-CDE of FS provides a new idea for the development and application of other sustainable extraction methods of traditional Chinese medicine.

Synthesis, characterization and evaluation of new anti-inflammatory iron charge transfer complexes

The novelty and the essential purpose of this research is the preparation of new anti-inflammatory iron complexes in water green solvent using critical micelle concentration of anionic surface active agent (SAA). Three new anti-inflammatory iron complexes have been prepared. Thiophene-electron (es) donor (D) Schiff base (2-(2-OH-benzylidene)-amino)-4, 5, 6, 7-tetrah ydrobenzo[b] thiophene-3-carbonitrile) has been prepared. Molecular structures of all samples were confirmed based on CNH analysis, 1H NMR and 13C NMR spectra. The molecular structure of Schiff base is further confirmed by computational chemistry using the DFT-B3LYP method, 6-31G (d) basis set. Observed and simulated 1H NMR, UV–Vis. IR/Raman spectra confirmed the molecular structure of D. This Schiff base is intercalated to ferric chloride (FeCl3) giving pure iron charge transfer complex (CTCs). In vitro and kinetic studies confirmed Fe-CTC complexes had (concentration-dependent) potent antimicrobial-, good anti-inflammatory activities. Free radical scavenging activity nitrous oxide (NO.) of Fe (III)CTCs is attributed to geometry Fe(III) ions as distorted octahedral (either monoclinic or triclinic single crystals) via functional groups (-C]N–O, NH2). Elemental analysis and EDS spectra confirmed strong binding between iron and hetero atoms (N, S, O) of D molecules.

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

MORIN, A BIOFLAVONOID, ATTENUATES MYOCARDIAL ISCHEMIA-REPERFUSION INJURY BY ATTENUATING RISK/SAPK PATHWAY

Objective: It is important to address the impact of rising incidence of mortality and morbidity associated with myocardial infarction (MI). There is need to explore new safer and efficacious drugs with novel mechanisms to manage MI. Morin, (2-(2,4-Dihydroxyphenyl)-3, is a bioflavanoid which is found in Maclura cochinchinensis, Maclura tinctoria, Maclura pomifera and leaves of Psidium guajava. It possesses good anti-apoptotic, anti-inflammatory, and antioxidant activity. Hence, we have evaluated the cardio-protective effect of Morin in Myocardial Ischemia-Reperfusion (IR) injury model of rat. Design and method: Male albino Wistar rats were pre-treated with Morin (40 and 80 mg/kg; p.o.) for 28 days and on the 29th day, the chest cavity was opened and myocardial ishemia was induced for 45 minutes by ligatiing the LAD coronary artery. Thereafter, reperfusion was carried out for 60 minutes. The hemodynamic parameters as well as left ventricular pressures (±LV dp/dt and LVEDP) were recorded throughout the ischemia and reperfusion. At the end of the procedure, the blood and heart were collected for evaluation of cardiac-injury markers, antioxidant-oxidant parameters, inflammatory markets, histopathological evaluation and molecular signalling pathway protein expressions. Results: Morin pretreatment for 28 days at 40 mg/kg and 80 mg/kg doses significantly controlled hemodynamic parameters, reduced cardiac injury markers, inflammation and apoptosis and reduced oxidative stress and mitigated histological changes following IR injury in rat heart. Morin also downregulated expression of pro-inflammatory and pro-apoptotic SAPK pathway proteins (p38 and JNK), and upregulated the survival kinase protein expression i.e. RISK pathway (ERK, eNOS). Conclusions: Morin reduced myocardial oxidative stress, inflammation and apoptosis in ischemia-reperfusion induced cardiac injury through upregulation of RISK and downregulation of SAPK pathways proteins.

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.

Fabrication of injectable alginate hydrogels with sustained release of 4-octyl itaconate for articular anti-inflammatory.

Osteoarthritis (OA) is a chronic and degenerative joint disease that remains a great challenge in treatment due to the lack of effective therapies. 4-octyl itaconate (4-OI) is a novel and potent modulator of inflammation for the treatment of inflammatory disease. However, the clinical usage of 4-OI is limited due to its poor solubility and low bioavailability. As a promising drug delivery strategy, injectable hydrogels offers an effective approach to address these limitations of 4-OI. The aim of the study was to verify that the composite 4-OI/SA hydrogels could achieve a controlled release of 4-OI and reduce damage to articular cartilage in the group of osteoarthritic rats treated with the system. In this study, an injectable composite hydrogel containing sodium alginate (SA) and 4-octyl itaconate (4-OI) has been developed for continuous intra-articular administration in the treatment of OA. After intra-articular injection in arthritic rats, the as-prepared 4-OI/SA hydrogel containing of 62.5μM 4-OI effectively significantly reduced the expression of TNF-α, IL-1β, IL-6 and MMP3 in the ankle fluid. Most importantly, the as-prepared 4-OI/SA hydrogel system restored the morphological parameters of the ankle joints close to normal. 4-OI/SA hydrogel shows a good anti-inflammatory activity and reverse cartilage disruption, which provide a new strategy for the clinical treatment of OA.

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.