Carrageenan-induced Paw Edema Research Articles

Multiple drug-delivery strategies to enhance the pharmacological and toxicological properties of Mefenamic acid

ObjectiveTo improve the biological and toxicological properties of Mefenamic acid (MA), the galactosylated prodrug of MA named MefeGAL was included in polymeric solid dispersions (PSs) composed of poly(glycerol adipate) (PGA) and Pluronic® F68 (MefeGAL-PS). MefeGAL-PS was compared with polymeric solid formulations of MA (MA-PS) or a mixture of equal ratio of MefeGAL/MA (Mix-PS). MethodsThe in vitro and in vivo pharmacological and toxicological profiles of PSs have been investigated. In detail, we evaluated the anti-inflammatory (carrageenan-induced paw edema test), analgesic (acetic acid-induced writhing test) and ulcerogenic activity in mice after oral treatment. Additionally, the antiproliferative activity of PSs was assessed on in vitro models of colorectal and non-small cell lung cancer. ResultsWhen the PSs were resuspended in water, MefeGAL’s, MA’s and their mixture’s apparent solubilities improved due to the interaction with the polymeric formulation. By comparing the in-vivo biological performance of MefeGAL-PS with that of MA, MefeGAL and MA-PS, it was seen that MefeGAL-PS exhibited the same sustained and delayed analgesic and anti-inflammatory profile as MefeGAL but did not cause gastrointestinal irritation. The pharmacological effect of Mix-PS was present from the first hours after administration, lasting about 44 hours with only slight gastric mucosa irritation. In-vitro evaluation indicated that Mix-PS had statistically significant higher cytotoxicity than MA-PS and MefeGAL-PS. ConclusionsThese preliminary data are promising evidence that the galactosylated prodrug approach in tandem with a polymer-drug solid dispersion formulation strategy could represent a new drug delivery route to improve the solubility and biological activity of NSAIDs.

Acute Toxicity, Analgesic, and Anti-inflammatory Activities of Folk Thai Herbal Medicine: Yafon Formula

Yafon (YF), a formula composed of 14 herbal constituents, has been used in folk Thai herbal medicine to treat various indications, including pain relief, antipyretics, and anti-inflammatory properties. Nevertheless, this formula lacks adequate toxicological and efficacy data. Hence, this study aims to assess the safety and efficacy of YF in animal models. The study on acute oral toxicity was conducted by the Organization for Economic Co-operation and Development (OECD) number 420 guidelines. The results demonstrated that the administration of YF at a high dose of 2000 mg/kg did not result in fatality or exhibit any toxicity. The analgesic effect of YF in mice was investigated using the acetic acid-induced writhing test and the formalin test. The anti-inflammatory activity of YF was assessed in rats using the carrageenan-induced paw edema test. This investigation employed YF doses of 200, 400, and 800 mg/kg/day. The study found that all YF doses reduced writhing in the acetic acid, and YF doses of 400 and 800 mg/kg/day reduced the licking time in the late phase of the formalin test. In addition, all YF doses effectively suppressed paw edema in the carrageenan-induced paw edema test. This study demonstrated that the YF formula showed no acute toxicity and possessed acute anti-inflammatory and analgesic effects by blocking pain signals originating from the peripheral nervous system. These findings provided empirical evidence supporting the use of YF formula as an analgesic and anti-inflammatory agent.

Oxidative Coupling Assembly Induced Bio-engineered Quercetin Microspheres for the Gastrosparing Delivery of Diclofenac Sodium.

The study aimed to develop microspheres of quercetin by oxidative coupling assembly and these microspheres were used to deliver diclofenac sodium without causing gastrotoxicity. The oxidative coupling assembly of quercetin was carried out in the presence of copper sulfate to yield quercetin microspheres. The microsphere of quercetin was loaded with diclofenac sodium (QP-Diclo). The carrageenan induced paw edema in rats was used for anti-inflammatory action was studied by using and acetic acid-induced writhing in mice was used to study the analgesic potential of the QP loaded microspheres. The ulcerogenecity and gastrotoxicity comparison was made between diclofenac and QP-Diclo. The oxidative coupling assembly of quercetin resulted in microspheres of 10-20 μm in size, which were loaded with diclofenac sodium (QP-Diclo). The marked anti-inflammatory activity was observed by QP-Diclo treatment using carrageenan induced paw edema (in rats) and better analgesic activity than diclofenac sodium in mice. The administration of QP-Diclo significantly elevated the diminished overall nitrite/nitrate extent and thiobarbituric acid reactive and significantly increased the diminished superoxide dismutase activity in comparison to diclofenac sodium in gastric mucosa. The results suggested that dietary polyphenol quercetin can be converted to microspheres by oxidative coupling assembly and can be used to deliver diclofenac sodium without causing gastrotoxicity.

Protective effects of hops (Humulus lupulus L.) extract on analgesic activity and oxidative stress markers in the brain of rats with carrageenan-induced paw edema

Hops (Humulus lupulus L.) are widely utilized worldwide as a raw material for various medical applications due to their numerous beneficial health effects. This study aimed to assess the potential neuroprotective effects of hop extract on cerebral oxidative markers and pain using rat models. In the experimental study, rats were divided into five groups and administered varying doses of Humulus lupulus L. extract (HLE) for a period of 15 days prior to the administration of carrageenan. To induce acute inflammation in rats, carrageenan (1 %) was injected into the sub-plantar region of the left paw. Subsequently, analgesic responses, the antioxidant activity and lipid peroxidation in the cerebral cortex were assessed. In the investigation of pain tolerance caused by inflammation in the hot plate test, the HLE treatment groups as exhibited a significant increase (P < 0.001) in delay time for removing the paw from the hot plate compared to the carrageenan group. The results demonstrate that HLE treatment significantly increased the activity of CAT (P < 0.001) and SOD (P < 0.01) enzymes, while decreasing the level of MDA (P < 0.01). It can be concluded that the consumption of hops may alleviate pain caused by inflammation and mitigate cerebral oxidative stress in rats.

Exploring Non-Cytotoxic, Antioxidant, and Anti-Inflammatory Properties of Selenium Nanoparticles Synthesized from Gymnema sylvestre and Cinnamon cassia Extracts for Herbal Nanomedicine

The study aimed to synthesize non-toxic selenium nanoparticles (SeNPs) using Gymnema sylvestre (G. sylvestre) and Cinnamon cassia (C. cassia) extracts. It also sought to develop and evaluate versatile nanomedicine formulations i.e. selenium nanoparticles of G. sylvestre and C. cassia (SeNPs), drug (lupeol) loaded SeNPs (DLSeNPs), drug-loaded and coated (PEG) SeNPs (DLCSeNPs) without side effects. The SeNPs formulations were hydrothermally synthesized, loaded with lupeol to improve efficacy, coated with polyethylene glycol (PEG) for targeted delivery, and characterized using UV-Vis spectrophotometry, Fourier-transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), zeta potential analysis, size distribution analysis, and X-ray diffraction (XRD). Hemolytic cytotoxicity, 2,2-Diphenyl-1-picrylhydzayl (DPPH), total Reducing power, and total antioxidant capacity (TAC) antioxidant assays, carrageenan-induced paw edema, and histological studies were used to estimate the acute anti-inflammatory activity of the synthesized SeNPs. The final form of PEGylated and drug (lupeol)-loaded selenium nanoparticles (DLCSeNPs) exhibited an average particle size ranging from 100 to 500 nm as evidenced by SEM, and Zeta potential results. These nanoparticles demonstrated no cytotoxic effects and displayed remarkable antioxidant (IC50 values 19.29) and anti-inflammatory capabilities. These results were fed into Graph-pad Prism 5 software and analyzed by one-way ANOVA, followed by Tukey's post hoc test (p < 0.001). All nano-formulations exhibited significant overall antioxidant activity, with IC50 values ≤ 386 (p < 0.05) as analyzed by ANOVA. The study's results suggest that G. sylvestre outperformed C. cassia in terms of reducing 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) free radical, potassium ferricyanide, and ammonium molybdate in respective antioxidant assays. As far as anti-inflammatory activities are concerned drug (lupeol)-loaded and PEG-coated G. sylvestre SeNPs exhibited the highest anti-inflammatory potential from all other nano-formulations including drug (lupeol)-loaded and PEG-coated C. cassia SeNPs, as exhibited to reduce the release of pro-inflammatory signals i.e. cytokines and NF-kB, making them innovative anti-inflammatory nanomedicine. The study synthesized lupeol-loaded and PEG-coated SeNPs, showcasing the potential for biocompatible, cost-effective anti-inflammatory nanomedicines. G. Sylvester's superior antioxidant and anti-inflammatory performance than Cinnamon cassia emphasizes medicinal plant versatility.

Analgesic and Anti-Inflammatory Activity: A Comprehensive Review on Invitro and In Vivo Screening Methods

Modern pharmacotherapy includes analgesic and anti-inflammatory medicines as essential components to relieve pain and inflammation brought on by a variety of medical diseases. Robust screening techniques are essential for the identification of possible candidates with appropriate safety and effectiveness profiles in the search and development of new analgesic and anti-inflammatory medications. This study looks at the many screening methods used in preclinical studies to assess new drugs' analgesic and anti-inflammatory quality. Conventional techniques like the tail flick, hot plate, and writhing’s tests measure analgesic activity by having animals respond to unpleasant stimuli. Comparably, anti-inflammatory activity is frequently assessed using assays like the cotton pellet granuloma test, which gauges tissue granuloma formation, and the carrageenan-induced paw edema model, which measures inflammation. These traditional techniques offer insightful information about the pharmacological effects of test substances. Despite the wide range of screening techniques available, each strategy has advantages and disadvantages. Preclinical studies are more reliable and have higher predictive value when various assays and techniques are integrated into a tiered screening strategy. Furthermore, the successful translation of preclinical findings to human applications depends on taking into account translational variables including species differences and clinical relevancies. As a result, choosing the right screening techniques is critical to the effective identification and characterization of new analgesic and anti-inflammatory drugs.

Synthesis and anti-inflammatory activity of benzimidazole derivatives; an in vitro, in vivo and in silico approach

Many non-steroidal anti-inflammatory drugs (NSAIDs) concurrently inhibit both COX-1 and COX-2, with a preference for specifically targeting COX-2 due to its significant involvement in various pathologies. In addition to COX enzymes, several other targets, including Aldose reductase, Aldo-ketoreductase family 1-member C2, and Phospholipase A2, have been identified as contributors to inflammation and a myriad of other diseases.In this context, a series of 2-substituted benzimidazole derivatives was synthesized and assessed for their anti-inflammatory potential through both in vitro and in vivo assays. Molecular docking studies were conducted to elucidate the mechanism of action of these compounds against COX enzymes and other therapeutic targets associated with NSAIDs, such as Aldose reductase, AIKRC, and Phospholipase A2.Among the synthesized compounds, B2, B4, B7, and B8 demonstrated IC50 values lower than the standard ibuprofen, as determined by the Luminol-enhanced chemiluminescence assay. Validation of these findings was achieved through an in vivo carrageenan-induced mice paw edema model, confirming a comparable anti-inflammatory effect to diclofenac sodium observed in vitro. Notably, these compounds exhibited significant binding affinity with all therapeutic targets investigated in this study.These results suggest that the newly synthesized derivatives possess noteworthy anti-inflammatory potential, warranting further exploration for the development of novel multi-targeting inhibitors.

In-silico design and synthesis of curcumin derivatives with enhanced antibacterial and anti-inflammatory activities

Since curcumin and curcuminoids include potential functional groups (such as α, β-unsaturated β-diketone, α, β-unsaturated ketone, and β 0-hydroxy-α, β-unsaturated ketone linked with aromatic rings on both sides), they have been the subject of much discussion. These groups have anti-inflammatory, anti-cancer, and antioxidant qualities, among other bioactivities. Using spectroscopic techniques, novel compounds of curcumin were created and described. This study assessed the antibacterial and anti-inflammatory properties of PDB ID:1IU 4 and PDB ID: 4LHF molecular docking, utilizing in silico models. In terms of binding affinity, compounds C-04 and C-05 they had a greater affinity for the 1IU4 and 4LHF, respectively. Using the Agar disc diffusion plate method (500μg/mL), the derivatized compounds were evaluated for their in-vitro antibacterial properties against two strains: S. Aureus and E. coli. When compared to conventional ciprofloxacin, compound C-04 demonstrated good to exceptional antibacterial efficacy against two distinct strains. they were further tested utilizing the carrageenan-induced paw edema method for anti-inflammatory efficacy. By using the HRBC membrane stabilizing test method, Compound C-05 showed strong anti-inflammatory action, while Compounds C-05 &amp;and C-06 demonstrated noteworthy anti-inflammatory activity.

Exploring the anti-inflammatory, sedative, antidiabetic, and antioxidant potential in in-vitro and in-vivo models and phenolic profiling of Atractylis aristata Batt.

Ethnopharmacological relevanceAtractylis aristata batt., as an endemic plant from the Asteraceae family, holds a significant position in the Ahaggar region of southern Algeria's traditional medicine. The aerial parts of Atractylis aristata was used to cure inflammation, fever, and stomach disorders. Aim of the studyThe objective of the present investigation was to ascertain the overall bioactive components and phytochemical components and examine the antioxidant, antidiabetic, anti-inflammatory, acute toxicity, and sedative properties of the crude extract obtained from the aerial portions of Atractylis aristata (AaME). Materials and methodsThe AaME's antioxidant activity was assessed by the use of pyrogallol autoxidation, (1,1 diphenyl-2-picrylhydrazyl) (DPPH), 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), and reducing power (RP) techniques. 1 mg/mL of AaME was used to evaluate the antidiabetic activity by applying the enzyme α-amylase inhibitory power test. At the same time, the bovine serum albumin (BSA) denaturation method was employed to quantify the in vitro anti-inflammatory activity at different concentrations (1.5625, 0.78125, 0.390625, 0.1953125 and 0.09765625 mg/mL). In contrast, following the Organization for Economic Co-operation and Development (OECD) guideline No. 423, which covers acute oral toxicity testing protocols, the limit dosage test was employed to assess in vivo acute toxicity. At the dose of 0.08 mg/mL, the carrageenan-induced paw edema approach was used to assess the anti-inflammatory efficacy in vivo, and the sedative activity was carried out at the dose of 0.08 mg/mL using the measurement of the locomotor method. Different bioactive compounds were identified within AaME using LC-MS/MS and HPLC-UV analysis. ResultsThe acute toxicity study showed no fatalities or noticeable neurobehavioral consequences at the limit test; this led to their classification in Globally Harmonized System (GHS) category Five, as the OECD guideline No 423 recommended. At a concentration of 0.08 mg/mL (2000 mg/kg), AaME showed apparent inhibition of paw edema and a significant (p = 0.01227) reduction in locomotor activity compared to the control animals. Our findings showed that AaME exhibited considerable antioxidant (IC50 = 0.040 ± 0.003 mg/mL (DPPH), IC50 = 0.005 ± 5.77 × 10-5 mg/mL (ABTS), AEAC = 91.15 ± 3.921 mg (RP) and IR% = 23.81 ± 4.276 (Inhibition rate of pyrogallol) and rebuts antidiabetic activities (I% = 57.6241% ± 2.81772). Our findings revealed that the maximum percentage of BSA inhibition (70.84 ± 0.10%) was obtained at 1.562.5 mg/mL. Thus, the AaME phytochemical profile performed using phytochemical screening, HPLC-UV, and LC-MS/MS analysis demonstrated that A. aristata can be a valuable source of chemicals with biological activity for pharmaceutical manufacturers. ConclusionThe phytochemical profiling, determined through HPLC-UV and LC-MS/MS applications, reveals this plant's therapeutic value. The aerial parts of Atractylis aristata contain bioactive molecules such as gallic acid, ascorbic acid, and quercetin, contributing to its significant antioxidant capabilities. Furthermore, identifying alizarin, the active compound responsible for its anti-inflammatory properties, could provide evidence supporting the anti-inflammatory capabilities of this subspecies.

Safety, Analgesic, and Anti-Inflammatory Effects of Aqueous and Methanolic Leaf Extracts of Hypericum revolutum subsp. keniense

In light of the enduring obstacles encountered in analgesia and anti-inflammatory therapeutics despite the strides made in contemporary medical sciences, the quest for alternative efficacious strategies is an imperative pursuit. Thus, this study investigated the safety profiles, as well as the analgesic and anti-inflammatory attributes, of aqueous and methanolic leaf extracts derived from Hypericum revolutum subsp. keniense—a botanical entity entrenched in historical ethnomedicinal practices in the Kenyan context. The assessment of acute oral toxicity of these extracts was conducted in accordance with the Up- and-Down method advocated by the Organisation for Economic Cooperation and Development (OECD), utilizing Swiss albino mice as the experimental subjects. Subsequent investigation entailed the evaluation of antinociceptive and anti-inflammatory properties employing the acetic acid-induced writhing and carrageenan-induced paw oedema methodologies, respectively, in the same murine model. The findings of this study evince the safety of both aqueous and methanolic extracts, with LD50 values surpassing 2000 mg/kg body weight and the absence of discernible signs of toxicity. Furthermore, a notable dose-dependent (P&lt;0.05) manifestation of analgesic effects was observed for both extracts, with the aqueous variant demonstrating heightened potency compared to its methanolic counterpart (P&lt;0.05). Moreover, the anti-inflammatory efficacy escalated significantly with escalating extract doses and prolonged treatment duration (P&lt;0.05), wherein the aqueous extract showcased superior effectiveness vis- à-vis the methanolic extract across all dosage regimens and temporal checkpoints (P&lt;0.05). Therefore, this investigation underscores the latent promise of the examined extracts as reservoirs of safe and efficacious analgesic and anti-inflammatory agents, thereby meriting further meticulous exploration. Subsequent research endeavours ought to pivot towards elucidating the phytochemical constituents underpinning the observed effects, alongside unravelling their mechanistic underpinnings across a spectrum of animal models and clinical milieus.

Analgesic, Anti-Inflammatory, and Chondroprotective Activities of Siraitia grosvenorii Residual Extract.

Inflammation is crucial to osteoarthritis (OA) pathogenesis. The aim of this study was to evaluate Siraitia grosvenorii residue extract (NHGRE) obtained by extracting S. grosvenorii fruits with water as a potential food supplement for treating arthritis based on its analgesic, anti-inflammatory, and chondroprotective effects and the remaining residue with 70% ethanol. We observed the analgesic activity of NHGRE based on the acetic acid-induced writhing response in mice, examined its anti-inflammatory efficacy against carrageenan-induced paw oedema in mice, and investigated its effect on inflammatory cytokine expression in interleukin (IL)-1β-induced SW1353 cells. Furthermore, we determined its effects on cartilage protection in interleukin-1β (IL-1β)-treated SW1353 cells. NHGRE at 200 mg/kg significantly reduced the acetic acid-induced writhing response and prevented oedema formation in the carrageenan-induced paw oedema model. In IL-1β-induced SW1353 cells, NHGRE at 400 µg/mL reduced the expression of inflammation mediators such as tumour necrosis factor (TNF)-α (55.3%), IL-6 (35.4%), and prostaglandin E2 (PGE2) (36.9%) and down-regulated the expression of matrix metalloproteinase (MMP)-1 (38.6%), MMP-3 (29.3%), and MMP-13 (44.8%). Additionally, it restored degraded collagen II levels in chondrocytes. NHGRE plays a protective role in chondrocytes by regulating Nuclear factor kappa B (NF-κB) activation. Overall, NHGRE may be a useful therapeutic agent for OA by controlling pain, oedema formation, and inflammation-related mechanisms.

ETHNOPHARMACOLOGICAL INVESTIGATION OF PLEUROTUS OSTREATUS FOR ANTI-OXIDATIVE AND ANTI-INFLAMMATORY ACTIVITY IN EXPERIMENTAL ANIMALS

Objective: This particular study was aimed to evaluate the anti-oxidant effect of Pleurotus ostreatus using the in vitro method and also against inflammation. Methods: A methanolic extract of P. ostreatus (MEPO) was prepared by the cold maceration technique. Different tests. In vitro anti-oxidant activity was investigated using the 1,1-diphenyl-1-picryl hydrazyl (DPPH) method. Wistar rats were chosen for the study; animals weighing 150–200 g were divided into six groups of six each (n=6). Control animals were grouped as I, group II was administered with approximately 100 μL of 1% suspension of carrageenan in saline and injected into the plantar surface of the right hind paw, group III, IV, V, and VI were given with carrageenan, followed by diclofenac sodium (150 mg/kg body weight, p.o.) and MEPO at the dose of 200, 400, and 800 mg/kg orally for 21 days. The paw volume and percentage of inhibition of the paw were measured in all animals. Results: The IC50 values of the test extract in the DPPH free radical scavenging assay were found to be 44.02±0.09 as compared with the standard drug 35.01±0.12, which was considered significant (***p&lt;0.001). The test extract at the dose of 400 and 800 mg/kg significantly decreased (**p&lt;0.001) the paw volume thereby, the inflammation, the % percentage of inhibition in paw volume was compared to the positive control in the carrageenan-induced paw edema. Conclusion: The study explored a potential source for anti-oxidants in the MEPO, which also seems to be effective in chemical-induced inflammation.

A novel diselenide attenuates the carrageenan-induced inflammation by reducing neutrophil infiltration and the resulting tissue damage in mice

Selenium-containing compounds have emerged as promising treatment for redox-based and inflammatory diseases. This study aimed to investigate the in vitro and in vivo anti-inflammatory activity of a novel diselenide named as dibenzyl[diselanediyIbis(propane-3-1diyl)] dicarbamate (DD). DD reacted with HOCl (k = 9.2 x 107 M−1s−1), like glutathione (k = 1.2 x 108 M−1s−1), yielding seleninic and selenonic acid derivatives, and it also decreased HOCl formation by activated human neutrophils (IC50=4.6 μM) and purified myeloperoxidase (MPO) (IC50=3.8 μM). However, tyrosine, MPO-I and MPO-II substrates, did not restore HOCl formation in presence of DD. DD inhibited the oxidative burst in dHL-60 cells with no toxicity up to 25 µM for 48h. Next, an intraperitoneal administration of 25, 50, and 75 mg/kg DD decreased total leukocyte, neutrophil chemotaxis, and inflammation markers (MPO activity, lipid peroxidation, albumin exudation, nitrite, TNF-α, IL-1β, CXCL1/KC, and CXCL2/MIP-2) on a murine model of carrageenan-induced peritonitis. Likewise, 50 mg/kg DD (i.p.) decreased carrageenan-induced paw edema over 5h. Histological and immunohistochemistry analyses of the paw tissue showed decreased neutrophil count, edema area, and MPO, carbonylated, and nitrated protein staining. Furthermore, DD treatment decreased the fMLP-induced chemotaxis of human neutrophils (IC50=3.7 μM) in vitro with no toxicity. Lastly, DD presented no toxicity in a single-dose model using mice (50 mg/kg, i.p.) over 15 days and in Artemia salina bioassay (50 to 2000 µM), corroborating findings from in silico toxicological study. Altogether, these results demonstrate that DD attenuates carrageenan-induced inflammation mainly by reducing neutrophil migration and the resulting damage from MPO-mediated oxidative burst.

Exploring the Anti-Inflammatory Potential of Cyperus pangorei Rhizome Extracts An In Vitro and In Vivo Study

Background and aim: Inflammation is a pivotal process implicated in various physiological and pathological conditions, necessitating the exploration of alternative anti-inflammatory agents with minimal side effects. This study aimed to investigate the anti-inflammatory potential of the standardized ethyl acetate (EtAc) fraction derived from Cyperus pangorei rhizomes. Methods: The rhizomes of C. pangorei were collected, processed, and subjected to extraction and fractionation to obtain the EtAc fraction. RP-HPLC analysis was employed to standardized the EtAc fraction against standard quercetin, luteolin, and apigenin. In vitro studies utilized peritoneal macrophages isolated from male Swiss albino rats to assess NO production and cytokine levels (IL-1β, IL-6, TNF-α) upon treatment with the EtAc fraction. In vivo evaluation was conducted using a carrageenan-induced rat paw edema model. Results: RP-HPLC analysis revealed the presence of quercetin, luteolin, and apigenin in the EtAc fraction. In vitro studies demonstrated dose-dependent inhibition of LPS-induced NO production and suppression of inflammatory cytokines (IL-1β, IL-6, TNF-α) by the EtAc fraction. Furthermore, in the carrageenan-induced rat paw edema model, the EtAc fraction exhibited dose-dependent inhibition of paw edema. Conclusion: The findings of this study highlight the significant anti-inflammatory potential of C. pangorei rhizome extracts, particularly the EtAc fraction. The identified compounds, quercetin, luteolin, and apigenin, contribute to its anti-inflammatory activity by modulating key inflammatory mediators. These results support the potential therapeutic use of C. pangorei in managing inflammation-related disorders. Further research is warranted to elucidate the underlying mechanisms and evaluate the long-term efficacy and safety of C. pangorei extracts as anti-inflammatory agents.

Sodium Cromolyn Modulates Carrageenan-Induced Acute Inflammation Through the Interleukin-6 Levels

Background: Previous studies have indicated that sodium cromolyn does not negatively affect steroidal and nonsteroidal anti-inflammatory drugs (NSAIDs). Objective: This study aimed to investigate the anti-inflammatory effects of sodium cromolyn on carrageenan-induced paw edema in rats and assess its impact on IL-6, an anti-inflammatory cytokine. Methods: The carrageenan-induced paw edema model is widely used for studying inflammatory mechanisms and evaluating anti-inflammatory drugs. The test groups received intraperitoneal injections of sodium cromolyn at doses of 25, 50, and 100 mg/kg alongside a positive control group (indomethacin at 5 mg/kg) and a negative control group (which received the solvent, saline). Thirty minutes after drug administration, carrageenan (1% w/v) was injected into the right hind paws of the rats. Changes in paw volume were measured using a plethysmometer at 0.5, 1, 2, and 3 hours post-carrageenan injection. Blood and paw tissue samples were collected three hours after carrageenan administration, and IL-6 levels were determined using the standard rat Interleukin-6 ELISA kit. Results: The plasma and tissue IL-6 levels in the group treated with cromolyn (25 mg/kg) were significantly higher than those in the positive control group (indomethacin 5 mg/kg). Sodium cromolyn at a dose of 25 mg/kg had a negligible effect on reducing paw edema and IL-6 levels in serum and paw tissues compared to indomethacin (5 mg/kg). The IL-6 levels in plasma and tissues for the group receiving 50 mg/kg of cromolyn were not significantly different from those in the indomethacin group (5 mg/kg). However, IL-6 levels in the group treated with 100 mg/kg of cromolyn were significantly lower than those in the indomethacin group. Among the groups treated with sodium cromolyn, the highest and lowest IL-6 levels were observed in the groups receiving 25 mg/kg and 100 mg/kg of sodium cromolyn, respectively. The anti-inflammatory effects of sodium cromolyn at doses of 25 mg/kg, 50 mg/kg, and 100 mg/kg were analyzed, revealing that 25 mg/kg of cromolyn sodium was not significantly effective at any time point (P &lt; 0.05). Additionally, no significant differences (P &lt; 0.05) were observed between the 50 mg/kg and 100 mg/kg doses at any study hour. Sodium cromolyn at a 50 mg/kg dose was as effective as indomethacin (5 mg/kg) in significantly reducing paw edema. Conclusions: Sodium cromolyn, at doses of 50 and 100 mg/kg, effectively reduced paw edema and the concentration of serum and paw tissue IL-6 (P &lt; 0.05), demonstrating significant anti-inflammatory activity. Sodium cromolyn at a 50 mg/kg dose is recommended as the anti-inflammatory dose of this drug.

Antinociceptive and anti-inflammatory effect of Passiflora edulis leaves extract in acetic acid-induced pain and carrageenan-induced paw oedema in vivo

Background: In Indonesia, people commonly treat pain and inflammation with herbs. Passiflora edulis leaves extract (PLE) is known to contain many chemical compounds that are useful as analgesic and anti-inflammatory treatments. However, there is very limited scientific literature that reports the results of P. edulis in reducing pain and inflammation. Objective: This research aims to evaluate the antinociceptive and anti-inflammatory effects of PLE. Method: PLE was extracted by Ultrasonic-Assisted Extraction (UAE). The PLE at doses of 20, 40 and 80 mg/200g BW (PLE-20, PLE-40, and PLE-80) and diclofenac sodium (Dic. sod. at a dose of 2.7 mg/200g BW as a positive control group was tested for antinociceptive and anti-inflammatory effects in experimental animal models (n=5). The effect of antinociceptive was evaluated by the wriggling in mice by acetic acid-induced, and the effect of acute anti-inflammatory was evaluated by carrageenan-induced in rats. Result: PLE at doses of 20, 40, and 80 mg/200g BW showed a significant antinociceptive effect at acetic acid-induced wriggling and inhibition of the oedema. Higher doses lead to more pronounced effects. The greater effect of antinociceptive was observed at PLE-80 (64.55%), and inhibition of the oedema was observed at PLE-80 (34.33%). Conclusion: PLE significantly reduced pain and acute inflammation in the animal-tested models.

Investigations of the highly efficient processing technique, chemical constituents, and anti-inflammatory effect of N-ethyl-2-pyrrolidinone-substituted flavan-3-ol (EPSF)-enriched white tea

N-Ethyl-2-pyrrolidinone-substituted flavan-3-ols (EPSFs) are a newly discovered compound class in tea with various bioactivities. This study aimed to develop a novel processing technique to enhance EPSF contents in white tea efficiently. Using optimal processing parameters of 125 °C and 30 min in a high-temperature sterilizing oven, total EPSF content significantly increased by 1.42–18.80-fold to 1.57–6.22 mg/g without impacting sensory characteristics. Metabolomics analysis revealed elevated levels of nucleosides, nucleotides, bases, theaflavins, flavonol aglycones, EPSFs, and most flavone-C-glycosides, as well as decreased levels of amino acids, procyanidins, theasinesins, several flavanols, and flavonol-O-glycosides after EPSF-enrichment treatment. Furthermore, the EPSF-enriched white tea exhibited notable anti-inflammatory effects, mitigating xylene-induced ear edema in mice and carrageenan-induced paw edema and cotton ball-induced granulomas in rats. This study developed a new processing technique for highly efficient enhancement of EPSFs in white tea and demonstrated that EPSF-enriched white tea has a potential to serve as effective anti-inflammatory dietary supplement.

Broad spectrum antimicrobial, anti-inflammatory and peripheral analgesic activities of heteroaryl nitazoxanide analogs

Background The antiparasitic drug nitazoxanide possesses diverse biological activity. However, very few investigation was accomplished with nitazoxanide analogs. Therefore, herein we focused on the screening of bioactivities using some nitazoxanide-like synthesized molecules. Objectives Four heteroaryl nitazoxanide analogs synthesized in our laboratory were investigated for antimicrobial, anti-inflammatory, and analgesic activity. Materials and methods Disc diffusion method was used for assessing antimicrobial potency against several Gram-positive bacteria, Gram-negative bacteria, and fungi. Carrageenan-induced rat paw edema model was performed to evaluate anti-inflammatory activity. The analgesic property was evaluated using the acetic acid-induced writing inhibition method in the mice model. Molecular docking simulations against cyclooxygenase-1, cyclooxygenase-2, phospholipase A2, NF-κB inducing kinase, and interleukin-1 receptor-associated kinase 4 were also performed. Results and conclusion All the synthesized compounds exhibited broad spectrum antimicrobial property against a number of Gram-positive, Gram-negative species and unicellular fungi. Compound 4 or N-(5-nitrothiazol-2-yl)-furan-3-carboxamide emerged as the most prominent antimicrobial agent exhibiting zone of inhibition ranging in 14–22 mm. These zone diameters are sometimes greater than that displayed by nitazoxanide. Compounds 2 and 3 also showed remarkable broad-spectrum antimicrobial activity with a zone of inhibition 10–20 mm and 12–20 mm, respectively. Compound 4 also displayed potential anti-inflammatory activity which is comparable to standard aceclofenac. Compound 4 also showed mild analgesic effects. The compounds also exhibited moderate binding affinities against the selected target receptors and enzymes during in silico molecular docking. Heteroaryl nitazoxanide analogs showed prominent broad-spectrum antimicrobial, anti-inflammatory, and mild analgesic properties. This study indicates that heteroaryl nitazoxanide analogs might be interesting candidates for new drug discovery.

Multifaceted chemical and bioactive features of Ag@TiO2 and Ag@SeO2 core/shell nanoparticles biosynthesized using Beta vulgaris L. extract

Due to increasing concerns about environmental impact and toxicity, developing green and sustainable methods for nanoparticle synthesis is attracting significant interest. This work reports the successful green synthesis of silver (Ag), silver-titanium dioxide (Ag@TiO2), and silver-selenium dioxide (Ag@SeO2) nanoparticles (NPs) using Beta vulgaris L. extract. Characterization by XRD, SEM, TEM, and EDX confirmed the successful formation of uniformly distributed spherical NPs with controlled size (25 ± 4.9 nm) and desired elemental composition. All synthesized NPs and the B. vulgaris extract exhibited potent free radical scavenging activity, indicating significant antioxidant potential. However, Ag@SeO2 displayed lower hemocompatibility compared to other NPs, while Ag@SeO2 and the extract demonstrated reduced inflammation in a carrageenan-induced paw edema animal model. Interestingly, Ag@TiO2 and Ag@SeO2 exhibited strong antifungal activity against Rhizoctonia solani and Sclerotia sclerotium, as evidenced by TEM and FTIR analyses. Generally, the findings suggest that B. vulgaris-derived NPs possess diverse biological activities with potential applications in various fields such as medicine and agriculture. Ag@TiO2 and Ag@SeO2, in particular, warrant further investigation for their potential as novel bioactive agents.

Evaluation of In-vivo Anti-inflammatory activity of methyl 2-(5-butyl-6-thioxo-1, 3, 5-thiadiazinan-3yl), butanoate

Inflammation is the body's way of fending off damage. Nonetheless, continuous and increasing inflammation may lead to the development of some chronic illnesses. It is still needed to evaluate new and safe anti-inflammatory therapies because existing medications have major side effects. Objective: To examine a novel compound's anti-inflammatory properties of methyl 2-(5-butyl-6-thioxo-1, 3, 5-thiadiazinan-3yl), butanoate (MBTTB) in albino mice models. Method: To test the anti-inflammatory effects in vivo, carrageenan-induced paw edema in albino mice of both sexes was utilized, and inflammation was measured by using Digital Plethysmometer. After extraction of carrageenan induced paw edematous, tissue level of inflammatory mediators like TNF-α, IL-1β, NF-ĸβ, and cox2 was ascertained by Western Blot analysis. Result: Based on in-vivo anti-inflammatory effects, compound MBTTB was shown to exhibit a maximum percentage inhibition of 16.7% after 1 hour, which is comparable to the standard drugs 12.8%. Following three hours, compound MBTTB showed the highest percentage inhibition of 23.2%, while the standard was 14.5%. Compound MBTTB showed the highest percentage inhibition after five hours (26.2 %), while the standard was 15.4%. The expression of many mediators' proteins, including TNF-α, IL-1β, NF-ĸβ, and COX-2, was ascertained. The computational analysis was carried out to forecast the level of decline of various mediators, including Tumor Necrosis Factor-α, (TNF) Interleukin-1β, NF-ĸβ, and COX-2. Conclusion: When considered as a whole, our current research indicates that MBTTB is a viable option for preventing inflammation in mice that has been caused by carrageenan in edematous paw.