High Anti-inflammatory Activity Research Articles

Neuroprotective effect of mealworm protein hydrolysate-derived bioactive peptides in human microglial cells

Abstract The larva of Tenebrio molitor, better known as mealworm, is one of the most studied insects today, since it was recently classified as safe for human consumption. Specifically, its high protein content makes it a splendid candidate for the search for bioactive peptides, with properties ranging from anti-inflammatory to neuroprotective. In this study, the effect of a digested hydrolysate on microglia cells (which previously demonstrated high anti-inflammatory activity in intestinal CACO-2 cells) was analysed, specifically on their levels of gene expression of various cytokines, such as IL-6, IL-10, or IL-1β, among others. In addition, four chemically synthesised peptides, selected from this digested hydrolysate based on in silico analysis, including the estimation of the bioactive properties of these peptides, their physicochemical properties and their toxicokinetic, were evaluated in the microglia cells as well. In addition, molecular docking assays of the peptides were performed with two receptors relevant to inflammation. Relevant changes in the expression of IL-6, IL-1β, and BDNF were observed due to the action of the peptides, especially in the case of IYVDAVIN and SLPSLPEPV. These results provide an insight on how specific peptides found in Tenebrio molitor could be used as therapeutics agent in the immunomodulation of brain cells.

096. The Effectiveness of Cardamom Seed Extract (Amomum compactum) Against Urea Creatinine and Histopathology Obese Rat Kidney

Background: There are several factors that can cause kidney damage, one of which is obesity. Obesity itself can cause complex metabolic disorders that can affect kidney physiology. The biological activity of flavonoid components in A. compactum showed that cardamom extract had high anti-inflammatory and antioxidant activity. This study aimed to analyze the effect of Cardamom Seed Extract (Amomum Compactum) on urea creatinine and histopathology obese rat kidney. Methods: This study was a true experimental with post tests only of control group design and was conducted from July to August 2022 at Pusat Study Pangan dan Gizi (PSPG), Gadjah Mada University. A total of 30 Wistar rats were used in this study and which randomly divided into normal control, negative control, 45 mg dose cardamom, 90 mg dose cardamom, 180 mg dose cardamom groups. Obesity was obtained by high fat and high carbo diet. At the end of the study, the rats will be terminated and urea, creatinine was examined, renal histopathology changes were observed using hematoxylin and eosin strain. Results: There was differences in urea levels between groups K and P1, P2, P3; P1 and P2, P1 and P3, and P2 and P3 (p<0.005). There was differences in creatinine levels between groups K and P1, P2, P3; P1 and P2, and P1 and P3 (p<0.005). There was a significant difference in renal histology between groups normal control, negative control, and P1 (p<0.001). Conclusion: Cardamom seed extract is effective in reducing urea creatinine levels and improving histopathology obese rat kidney.

Mining and Engineering the Di-O-glycosylation Pattern of UGT72B1 for the Highly Efficient O-Glycosylation of Endogenous Quercetin.

Compared with mono-O-glycosylation, di-O-glycosylation endows the precursor with better performance. However, the mining and engineering of di-O-glycosylation patterns of glycosyltransferases are limited, hindering their synthetic applications. Here, an Arabidopsis xenobiotic-transforming glycosyltransferase, UGT72B1, was found to catalyze the glycosylation of endogenous quercetin and its monoglycosides, generating di-O-glucosides. Mutating M17/G18/Y315 into L/T/Q in UGT72B1 altered its regioselectivity toward quercetin 7-O-glucoside, enzymatically generating another 3,7-di-O-glycoside with up to a 100% conversion rate, and increased the sugar donor preference. Altering the regiospecificity of glycosyltransferases likely required coordination between the entrance and the active site, where the orientations of the sugar acceptors and donors shift to adopt a lower binding energy state. Moreover, quercetin 3,4'-di-O-β-d-glucoside and quercetin 3,7-di-O-β-d-glucoside synthesized were found to have the highest anti-inflammatory activities. Overall, this work presents an efficient strategy to engineer glycosylation patterns for the synthesis of quercetin di-O-β-d-glucosides to be used as food additives, therapeutics, and nutraceuticals.

Tannic Acid-Based Biomimetic Nanomedicine with Pathological Reactive Oxygen Species-Responsive Cargo Release for Relieving Inflammation in Rheumatoid Arthritis.

Rheumatoid arthritis (RA) is a chronic disease characterized by immune cell infiltration and cartilage damage. The local lesion of RA shows severe oxidative stress and proinflammatory cytokine secretion. For drug therapy, the efficacy of agents, such as methotrexate (MTX), may be greatly limited, resulting from the low bioavailability, immune clearance, and toxic side effects. A nanocarrier (TA-PBA NPs) was developed with anti-inflammatory and antioxidant activities, combined with MTX to prepare nanomedicine (MTX NPs) for synergistic treatment of RA. Moreover, inspired by the biological functions homing to inflammation lesion of macrophages, the biomimetic nanomedicine camouflaged with macrophage membrane (MM@MTX NPs) was constructed. TA-PBA NPs could timely promote MTX release in response to the overaccumulated ROS to exhibit high anti-inflammatory and antioxidant activities for alleviating RA progression. The experimental results confirmed that MM@MTX NPs could significantly reduce the secretion of proinflammatory cytokines (TNF-α) while significantly increasing the typical anti-inflammatory cytokines (IL-10), promote the phenotype transformation of macrophages from M1 to M2, and up-regulate the Nrf2-keap1 pathway-related proteins (HO-1 and NRF2) to positively regulate the local inflammation for effectively inhibiting RA development. Thus, MM@MTX NPs represent a possible candidate as a safe and efficient nanotherapy platform for RA management.

Effects of thermal processing and pH on the physicochemical properties, stability, and structure of taxifolin-loaded nanostructured lipid carriers

In the present study the potential of nanolipid carriers (transfersomes) for improving the oral delivery of taxifolin, a poorly water-soluble bioactive compound with high antioxidant and anti-inflammatory activity was evaluated. Two transfersome formulations were prepared using lecithin, Span®60, and Tween®80, with cholesterol as a stabilizer (FA) and without cholesterol (FB), by the Ethanol Injection Method (EIM). The influences of thermal treatment (60–90 °C) and pH (2, 4, 6, and 8) on physical stability, structure, and taxifolin degradation were evaluated. The transfersomes were physically and chemically stable during heating at lower temperatures (≤70 °C), while thermal treatment at 80–90 °C led to an increase in particle size (an increase of around 200 nm) and a decrease in taxifolin encapsulation. Moreover, there was no significant difference in particle size or polydispersity index (PDI) at high temperatures. The particle sizes of transfersomes FA and FB increased from 128 to 182 nm at pH 7 to 224 and 331 nm at pH 2, respectively. Both transfersome preparations remained relatively stable, with consistent antioxidant activity (IC50 = 0.64 mg ml−1) over four weeks of storage at different temperatures (4, 25, and 40 °C), showing higher stability at lower temperatures. The in vitro digestion experiment indicated physical stability after exposure to the simulated stomach stage. However, the reduction in the nanovesicles' surface charge after incubation with gastric juice, increased particle size. Based on these results, taxifolin-loaded transfersomes can be pasteurized at low temperatures, for incorporation into enriched food and beverage products.

Position Matters: Effect of Nitro Group in Chalcones on Biological Activities and Correlation via Molecular Docking

A series of nine nitro group-containing chalcones were synthesized to investigate their anti-inflammatory and vasorelaxant activities via in vivo, ex vivo, and in silico studies. The anti-inflammatory effects of the compounds were evaluated via a TPA-induced mouse ear edema model, and the vasorelaxant effects were evaluated via an isolated organ model in addition to molecular docking studies. The compounds with the highest anti-inflammatory activity were 2 (71.17 ± 1.66%), 5 (80.77 ± 2.82%), and 9 (61.08 ± 2.06%), where the nitro group is located at the ortho position in both rings, as confirmed by molecular docking with COX-1 and COX-2. The compounds with the highest vasorelaxant activity were 1 (81.16 ± 7.55%), lacking a nitro group, and 7 (81.94 ± 2.50%), where the nitro group is in the para position of the B ring; both of these compounds interact with the eNOS enzyme during molecular docking. These results indicate that the position of the nitro group in the chalcone plays an important role in these anti-inflammatory and vasorelaxant activities.

Synthesis of New Indazole Analogs of Curcumin as Antioxidant and Anti-inflammatory Candidates: An <i>In Vitro</i> Investigation

The development of analog curcumin compounds by modifying the structure of monocarbonyl into an analog indazole of curcumin (AIC) is recognized to have a great potential. Still, only a few reports have been available. Rarely occurring in nature, indazole molecules are typically created through chemical synthesis. Therefore, this study aimed to synthesize six new AIC compounds with a particular focus on testing in vitro antioxidant activity using the DPPH and FRAP methods, as well as anti-inflammatory activity using the protein denaturation method. The results showed that the compounds formed had high anti-inflammatory activity but low antioxidant activity. All synthesis products produced higher anti-inflammatory activity than standard diclofenac sodium and curcumin compounds. Specifically, compound 3a showed the highest anti-inflammatory activity with an IC50 = 0.548 ± 0.062 μM. Therefore, it was concluded that compound 3a has the potential to be further studied for anti-inflammatory activity.

Propagación in vitro de Anredera vesicaria

Anredera vesicariais a plant whit high anti-inflammatory activity. The work objective was to establish in vitropropagation of A. vesicaria. Nodal segments were used as explants and two disinfection times in 1% sodium hypochlorite (15 and 20 minutes) were evaluated during in vitroestablishment. Combinations of AG3 (2,5 and 5,0 mg/L) and IAA (0,05 and 0,1 mg/L) were evaluated in the multiplication phase and the effect of IBA (0,5 and 1,0 mg /L) and Pectimorf (1,0 and 5,0 mg/L) for in vitrorooting. Acclimatization was carried out in a mixture of soil-cow manure-zeolite. Disinfection was achieved with 1% sodium hypochlorite for 15 minutes and in vitroestablishment in the MS (1962) culture medium. High values of multiplication and rooting in vitrowere obtained, as well as acclimatization of plants in vitro.

Viola stocksii: A rich source of antioxidant and anti-inflammatory flavonoid glycosides with converged therapeutic potential against SARS-CoV-2 MPro, spike trimer, and surface glycoproteins

This research presents the first comprehensive investigation into the phytochemical and nutraceutical properties of Viola stocksii. The study aimed to identify the therapeutic efficacy and bioactive constituents of this medicinal herb, traditionally used as an herbal tea for managing respiratory and abdominal issues in remote areas of Pakistan. The therapeutic efficacy of the plant was assessed as an anti-oxidant-rich health tonic coupled with anti-inflammatory and immunomodulatory activities against COVID-19 and its evolving variants. The study involved sequential extraction, bio-assay guided fractionation, isolation, characterization, and biological evaluation. Preliminary in vitro studies have demonstrated that polar fractions of the plant possess significant antioxidant and antiinflammatory potential. A diverse combination of chromatographic techniques (Diaion resin HP-20, Sephadex LH-20, ODS-C18, and RP-HPLC) facilitated the purification of active constituents of the plant. Comprehensive analysis of NMR (1H, 13C, and 2D NMR) and mass (EIMS, HR-EIMS, and FAB-HRMS) spectral data lead to characterize the isolated compounds (1–4) as flavonoid glycosides. Results from in vitro and in-silico evaluations revealed that the isolated glycosides exhibit high antioxidant, antiinflammatory, and immunomodulatory activities, which synergistically show promising potential in combating SARS-CoV-2 variants. Besides MPro, therapeutic potential against two unexplored proteins i.e. the spike trimer (7WZ1) and surface glycoproteins (7QTJ) was studied for the first time. Kaempferol (KamGluαRh) and quercetin (QurGluαRh) carrying rutinoside, were identified as the most active constituents of the plant, with the highest binding affinities in the range of −10 to −13 kcal/mol. Ten distinct active regions were explored on the spike trimer, including strong binding affinity with the essential RBD region, spike head, and tail of the protein. MD simulation validated the stability of Mpro-KamGluαRh and Mpro-QurGluαRh complexes evidenced by an average RMSD of 0.2 nm led to the mechanistic understanding of Mpro inhibition. ADMET and pharmacokinetic studies authenticated the therapeutic ability and drug-likeness profiling of all extracted compounds. Results revealed the beneficial role of glycosides in boosting the medicinal effectiveness of flavonoids and the potential of Viola stocksii as an immunity booster against respiratory infections like COVID-19.

Clinical case of colchicum poisoning

Introduction. Autumn colchicum or crocus is a popular plant among gardeners, characterized by early beautiful flowering, but few people know that it is poisonous. Acute colchicum poisoning is a dangerous urgent clinical situation with high mortality rates. By disrupting cell division, colchicum venom leads to multiple organ failure and death in just a few days. However, colchicum extract in small doses is often used in modern medicine to treat various diseases, due to its high antimitotic and moderate anti-inflammatory activity. The article describes the clinical observation of a patient admitted to the toxicology department after a suicide attempt using a crocus flower, containing the alkaloid colchicine. The results of laboratory and pathological studies are presented. Clinical observation. A clinical case of acute crocus poisoning with the development of hemodynamic disorders, dyspeptic syndrome, respiratory failure, cytolysis syndrome, and oliguria is presented. Treatment was aimed at restoring organ functions and consisted of infusion, detoxification, and hemostatic therapy. Limitations. To carry out this scientific work, a study was conducted within the framework of only one clinical case committed on the territory of the Udmurt Republic. In this case report, there was no comparison group or observation group. The described documents were provided by the Budgetary Health Institution of the Udmurt Republic "City Clinical Hospital no. 6" of the Ministry of Health of the Udmurt Republic and the Budgetary Health Institution of the Udmurt Republic “Bureau of Forensic Medical Examination of the Ministry of Health of the Udmurt Republic” by prior agreement. Conclusion. Colchicum poisoning is a rare and extremely severe pathology, leading to multiple organ failure, agranulocytosis and death. Considering the rapid absorption in the gastrointestinal tract and the initial symptoms in the form of gastrointestinal lesion syndrome, early diagnosis in the absence of anamnesis is difficult, therefore, it is necessary to highlight the issues of diagnosing this poisoning, as well as the study and implementation of modern methods of treating colchicine poisoni

Phytochemical Analysis and Evaluation of the Antioxidant, Anti-Inflammatory, Hemolytic, and Antibacterial Effects of Astragalus gombo (L.) Leaves.

The purpose of this study is to determine the phytochemical content and biological activities of the Astragalus gombo (endemic specie). While identification and quantification of individual secondary metabolites were performed by analysis HPLC. Antioxidant (DPPH and FRAP), anti-inflammatory, anti-hemolytic and antibacterial activities were evaluated. For analysis HPLC, we obtained 65 peaks and identified 6 major bioactive compounds. The total concentration in polyphenols, flavonoids and condensed tannins varied respectively from 66.306±0.88 mg GA eq/g, 34.312±1.4 mg Q eq/g and 5.343±2.74 mg Ca eq/g. In terms of antioxidant activity, we found that this extract had high inhibitory ratios equivalent to IC50=62.813±0.006 µg/mL for DPPH and IC50=19.375±0.041 µg/mL for FRAP. A high anti-inflammatory activity was estimated at 1615.81µg/mL, and a weak anti-hemolytic activity, the other hand the antibacterial activity is somewhat moderate against the five strains studied. This study demonstrated that the aqueous extract of A. gombo from El Oued region has tremendous antioxidant, anti-inflammatory and antibacterial abilities.

Construction of a one-stop N-doped negatively charged carbon dot nanoplatform with antibacterial and anti-inflammatory dual activities for wound infection based on biocompatibility

The development of bacterial resistance significantly contributes to the persistence of infections. Although previous studies have highlighted the benefits of metal-doped positive carbon nanodots in managing bacterial wound infections, their mechanism of action is relatively simple and they may pose potential hazards to human cells. Therefore, it is essential to develop a one-stop carbon dot nanoplatform that offers high biocompatibility, antibacterial properties, and anti-inflammatory activities for wound infection management. This study explores the antibacterial efficacy, without detectable resistance, and wound-healing potential of nitrogen-doped (N-doped) negatively charged carbon dots (TPP-CDs). These carbon dots are synthesized using tannic acid (TA), polyethylene polyamine, and polyethylene glycol (PEG) as precursors, with a focus on their biocompatibility. Numerous systematic studies have shown that TPP-CDs can effectively destroy bacterial biofilms and deoxyribonucleic acid (DNA), while also inducing oxidative stress, leading to a potent antimicrobial effect. TPP-CDs also demonstrate the ability to scavenge excess free radicals, promote cellular proliferation, and inhibit inflammatory factors, all of which contribute to improved wound healing. TPP-CDs also demonstrate favorable cell imaging capabilities. These findings suggest that N-doped negatively charged TPP-CDs hold significant potential for treating bacterial infections and offer practical insights for their application in the medical field.

A Review of the Benefits of the Sustainable Utilization of Shrimp Waste to Produce Novel Foods and the Impact on Human Health

In recent years, there has been an increase in the industrial processing of shrimp, aiming to cover the increasing demand for shrimp products for human consumption, and, consequently, an increase in shrimp by-products as shrimp waste. This waste includes the cephalothoraxes, heads, shells, tails, pleopods, and exoskeleton appendages of processed shrimps. The appropriate method for the enzymatic hydrolysis of shrimp waste can recover its bioactive substances, including carotenoids. Thus, these xanthophylls and carotenes are of high financial interest and have high antioxidant, anti-inflammatory, and anti-cancer activities. Therefore, these substances can be incorporated into fish feed as ingredients that improve fish health and simultaneously lead to the production of aquaculture fishes similar in coloration to the wild ones. Thus, the consumption of such novel food acts as a preventive factor for human health. In this regard, β-carotene has antioxidant and fat-soluble activities owing to vitamin A sufficiency and has an anti-cancer effect, too. Canthaxanthin can be used as a product for personal care and as a natural tanning agent for human skin. Zeaxanthin and lutein have positive effects on various eye and heart diseases, neuronal damage, human skin diseases, and certain types of cancer. Astaxanthin also has anti-diabetic and anti-obesity properties. Therefore, the purpose of this review is to highlight the sustainable utilization of shrimp waste via enzymatic hydrolysis, the benefits of a fish diet enriched with astaxanthin, the consumption of fish enriched with carotenoids, and the effects of carotenoids on human health. The problem of shrimp waste disposal affects the environment, does not contribute to sustainable development, and is directly related to the phenomenon of environmental change.

Exploring the bioactive potential of Mentha longifolia from Northeast India: an inclusive study on phytochemical composition and biological activities

Mentha longifolia (Lamiaceae) is regarded as highly valuable aromatic medicinal species with wide range of pharmaceutical application. In the present work, leaf essential oil of M. longifolia was applied for the assessment of in vitro pharmacological potentials and compositional analysis. A sum of 15 compounds were detected by GC-FID and GC-MS analysis of M. longifolia essential oil with total area of 99.98% where major compounds were carvone (59.56%), D-limonene (20.81%), eucalyptol (10.08%). The anti-oxidant potency of M. longifolia was estimated using two methods viz., ABTS (2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid) and DPPH (2,2-diphenyl-1-picrylhydrazyl) assay where M. longifolia essential oil showed moderate anti-oxidant potency. M. longifolia essential oil revealed high anti-inflammatory and tyrosinase inhibitory activity with an IC50 value 3.68 μL/mL and 1.22 μL/mL respectively compared to standard sodium diclofenac (5.33 μL/mL) and kojic acid (2.28 μL/mL). The acetylcholinesterase (AchE) inhibitory and genotoxic assay was performed, where M. longifolia essential oil revealed strong anti-acetylcholinesterase and anti-genotoxic activity. Anti-microbial potential of M. longifolia essential oil was also where strong anti-bacterial activity was shown against Salmonella typhimurium, Bacillus cereus, Staphylococcus aureus, Micrococcus luteus. For anti-fungal activity, M. longifolia essential oil showed no zone of inhibition against any used strains except Aspergillus flavus. From the present research it was established that M. longifolia essential oil possesses pharmaceutical potential with strong AchE inhibitory, anti-inflammatory, anti-microbial, anti-tyrosinase, anti-genotoxic and anti-oxidant activity which can be used for plant-based drug development in future endeavor.

Formulation of Neem and Echinacea Gel for Oral Health Along With the Evaluation of Antimicrobial, Cytotoxic, Anti-inflammatory, and Free Radical Scavenging Activity: An In Vitro Study.

Background Herbs have been used in medical practice for centuries and continue to play a significant role in modern complementary and alternative medicine.Phytochemicals in these herbs possess strong antioxidant and anti-inflammatory properties, which are beneficial in targetingoral health issues, such as dental plaque, gingivitis, and oral microbial infections.As research progresses, the challenge remains to translate these natural compounds into safe, effective, and accessible treatments for a wide range of diseases. Aim The aim of this research was to formulate the neem and echinacea gel along with the evaluation of antimicrobial, anti-inflammatory, free-radical scavenging activity, and cytotoxic potential. Materials and methods The neem and echinacea gel was prepared using a concentrated powdered mixture of neem and echinacea (5 grams each) to which 100 ml of distilled water was added, and the mixture was boiled for 30 minutes at 60°C. The 10 ml concentrate was mixed with 20 ml of a carbopol and carboxymethyl cellulose (CMC) mixture and mixed thoroughly, which resulted in neem and echinacea gel. Then, theantimicrobial, anti-inflammatory, cytotoxic potential, and free-radical scavenging activity of the gel were evaluated. The data obtained were statistically analyzed with the help of a paired t-test, where a p-value of less than 0.05 was considered statistically significant. Results The antimicrobial assay showed that neem and echinacea gel at the concentration of 100 micrograms showed a greater zone of inhibition against Staphylococcus aureus(3.15 ± 0.26), Streptococcus mutans (2.48 ± 0.45), Enterococcus faecalis (2.89 ± 0.15), and Candida albicans (4.28 ± 0.87). The cytotoxic test revealed that even at an 80 µg concentration of the extract,more than 70% of the nauplii were vital, which indicated that the gel was not cytotoxic.The highest anti-inflammatory activity (78.39 ± 1.82) of the gel was seen at 50 micrograms when compared with diclofenac sodium (73.16 ± 1.80). The free radical scavenging activity showed that the 2,2-diphenyl-1-picrylhydrazyl (DPPH) absorbance of the neem and echinacea extract was highest at 50 micrograms. Conclusion The combination of neem and echinacea extract-based gel possessed high antimicrobial and anti-inflammatory activity when compared with standard drugs, such as amoxicillin and diclofenac sodium. The antioxidant activity of the gel was equal to butylated hydroxytoluene (BHT), and also the gel has a low cytotoxic potential even at its higher concentrations. Hence, the gel can be used as a natural remedy with minimal side effects, making it a valuable alternative to chemical agents.

Study of PT1 Peptide Analgesic and Anti-Inflammatory Activity on a Local Inflammation Model in Mice CD-1.

PT1 peptide isolated from the venom of spider Geolycosa sp. is a modulator of P2X3 receptors that play a role in the development of inflammation and the transmission of pain impulses. The anti-inflammatory and analgesic efficacy of the PT1 peptide was studied in a model of complete Freund's adjuvant-induced paw inflammation in CD-1 mice. The analgesic activity of PT1 peptide was maximum after intramuscular injection at a dose of 0.01 mg/kg, which surpassed the analgesic effect of diclofenac at a dose of 1 mg/kg. The anti-inflammatory activity was maximum after intramuscular injection at a dose of 0.0001 mg/kg; a decrease in paw thickness was observed as soon as 2 h after the administration of the PT1 peptide against the background of inflammation development. All tested doses of PT1 peptide showed high anti-inflammatory activity 4 and 24 h after administration. PT1 peptide at a dose of 0.01 mg/kg when injected intramuscularly simultaneously produced high anti-inflammatory and analgesic effects compared to other doses of the peptide. Increasing the dose of PT1 peptide led to a gradual decrease in its analgesic and anti-inflammatory activity; increasing the dose of intramuscular injection to 0.1 and 1 mg/kg is inappropriate.

Byakangelicin alleviates sepsis-associated acute kidney injury by inhibiting inflammation and apoptosis.

Inflammation and apoptosis are common in many pathological conditions. Studies have shown that many natural compounds can regulate the signal pathways related to inflammation and apoptosis and can prevent sepsis-associated acute kidney injury (SA-AKI). Several studies have reported the potential anti-inflammatory effect of byakangelicin (BK), a component from the roots of Angelica gigas. However, the role of BK in SA-AKI remains unknown. Here, we report that BK is a potential therapeutic drug for SA-AKI. Experimental results show that BK has high anti-inflammatory activity, inhibits the activation of the NF-κB signaling pathway, and then reduces the production of IL-6, TNF-a, and IFN-γ. In addition, we study the effect of BK on renal cell apoptosis and find that BK significantly reduces the expression of apoptosis-related genes. Further research suggests that BK may exert the above pharmacological effects through 26S protease regulatory subunit 8 (PSMC5). These findings indicate that BK, as an inhibitor of inflammation and apoptosis, can be used to treat SA-AKI.

Evaluation of Anti-Inflammatory Activity in Methanolic Seed Extracts of International Sorghum bicolor L. Resources

Sorghum is an important cereal with high value as a health food ingredient because it contains various phenolic compounds. Anti-inflammatory activity was assessed using 12 sorghum resources collected from various countries to explore their potential as medicinal resources. The findings revealed that, at extract concentrations of 25 µg/mL and 50 µg/mL, cell survival rates were observed to be between 70 and 80% for most varieties, with the exception of K159081. In the analysis of anti-inflammatory activity, measured by the rate of nitric oxide (NO) production, sorghum varieties K159041 and K159081 exhibited NO production rates of 0.46 ± 0.38% and 2.58 ± 0.20%, respectively, indicating significant anti-inflammatory properties. The investigation into anti-inflammatory effects also included examining the expression of the inducible nitric oxide synthase (iNOS) gene, which is related to the inflammatory response triggered by LPS in macrophages. Varieties K159041, K159048, K159077, K159078, K159081, K159089, and K159096 were analyzed for this purpose. Further, an expression test of the cyclooxygenase 2 (COX-2) gene revealed values less than 0.4 in K159077, K159081, and K159089, suggesting these sorghum lines possess higher anti-inflammatory activity compared to others. Additionally, the expression analysis of tumor necrosis factor alpha (TNF-α), a gene identified as an inflammatory cytokine, showed that the mRNA levels in the lines K159048, K159077, K159078, K159088, K159089, K159093, and K159096 were expressed at lower levels relative to other sorghum resources, categorizing them as having high anti-inflammatory activity. Notably, the K159081 line exhibited the lowest expression level of all genes associated with inflammation, marking it as a valuable medicinal resource with potential development as an anti-inflammatory agent.

Selection of NSAIDs for rational pharmacotherapy of chronic musculoskeletal pain: a clinical pharmacologist's perspective

Chronic musculoskeletal pain (CMSP) is one of the most common pathological conditions that limits patients' physical activity and reduces their quality of life. The analgesic and anti-inflammatory effects of non-steroidal anti-inflammatory drugs (NSAIDs) make them the basis of pharmacotherapy for patients with chronic conditions affecting various parts of the musculoskeletal system. The main target of NSAIDs, cyclooxygenase (COX), exists in the form of two main isoforms, COX-1 and COX-2, the inhibition of each of which leads to a cascade of reactions at the cellular and tissue level that can cause both targeted pharmacological effects and side effects. The diversity of the chemical structures of NSAIDs leads to differences in their pharmacodynamic and pharmacokinetic parameters and correspondingly to differences in their efficacy and safety profile. Selective COX-2 inhibitors, coxibs, have shown an increased risk of cardiovascular side effects, which has led to significant restrictions on their use. Cardiotoxicity is not as pronounced with the non-selective COX inhibitors, but the range of their side effects is extremely wide. These side effects are dose-dependent and are characteristic, first of all, of systemic NSAIDs.The combination of systemic and topical NSAIDs makes it possible to reduce the dose of the former and improve the safety profile of anti-inflammatory therapy. Among the non-selective COX inhibitors with a satisfactory safety profile and high anti-inflammatory activity, the group of oxicams and especially tenoxicam should be emphasised, which are characterised by a maximum duration of action, which is an advantage in the treatment of patients with CMSP. This review addresses the issues of rational selection of NSAIDs based on comparative data on pharmacodynamics, pharmacokinetics and clinical trial results.

Anti-Inflammatory and Antioxidant Effects of Rosmarinic Acid Trimetallic (Cu0.5Zn0.5Fe2O4) Nanoparticles.

Newly, green metallic-nanoparticles (NPs) have received scientists' interest due to their wide variable medicinal applications owned to their economical synthesis and biologically compatible nature. In this study, we used rosmarinic acid (RosA) to prepare Cu0.5Zn0.5FeO4 NPs and later encapsulated them using PEG polymer. Characterization of NPs was done using the XRD method and SEM imaging. Further, we explored the encapsulated NPs for anti-inflammatory properties by downregulating the expression of pro-inflammatory cytokines mRNA in LPS-stimulated Raw 264.7 cells. Besides, employing DPPH, NO and ABTS radical scavenging assays to examine the antioxidant activity of the synthesized Cu0.5Zn0.5FeO4 NPs. Cu0.5Zn0.5FeO4 NPs revealed moderate antioxidant activity by scavenging DPPH and nitric oxide. We demonstrated that the NPs showed high potential anti-inflammatory activity by suppressing the mRNA and protein levels of pro-inflammatory cytokines in a dose-dependent manner, in LPS-induced Raw 264.7 cells. To our best knowledge, this is the first report where RosA was found to be a suitable phyto source for the green synthesis of Cu0.5Zn0.5FeO4 NPs and their in vitro anti-inflammatory and antioxidant effects. Taken together, our findings suggest that the RosA is a green resource for the eco-friendly synthesis of Cu0.5Zn0.5FeO4/PEG NPs, which further can be employed as a novel anti-inflammatory therapeutic agent.