Search Results (74)

Background: Recently various plants have attracted considerable scientific interest as potential therapeutic alternatives to known drugs used in anti-inflammatory therapy. Therefore, we have investigated the possible anti-inflammatory and analgesic effects of aqueous extracts from flowers of the medical plant Nepeta nuda ssp. nuda L. (naked catmint) in a model of acute peripheral inflammation induced by intraplantar injection of λ-carrageenan in the hind paw of Long Evans rats. Methods: Two routes of N. nuda extract application were used: locally by intraplantar injections at dosages of 2.5 mg/kg and 25 mg/kg and systemically by intraperitoneal administration at dosages of 50 mg/kg and 200 mg/kg, respectively. Paw volume was measured prior to the carrageenan application and 1, 2, 3, and 4 h after carrageenan injection. Spontaneous locomotor activity of the rats was assessed 3 h after carrageenan injection, corresponding to the peak of acute paw inflammation. Results: Local application of the higher N. nuda dose led to a marked reduction in inflammatory paw edema at the 4th hour after carrageenan injection, comparable to the effect of the positive control diclofenac sodium. Interestingly, a similar anti-inflammatory effect was observed at the 1st hour when both extract doses were administered intraperitoneally. Only the higher intraplantar dose of N. nuda extract significantly enhanced the vertical activity in comparison to the group treated with carrageenan alone. Conclusions: Our data indicate that the aqueous N. nuda extract possesses potent anti-inflammatory effects following both local and systemic administration in rats. Furthermore, when administered locally the extract exerts significant analgesic activity in inflammatory pain. Full article

A series of three chalcones with a nitro moiety in ring B (compounds 3a–c) was obtained by following a classic Claisen–Schmidt condensation procedure, which involved hydro-alcoholic conditions at room temperature. The reaction yields are consistently high (>90%), and the spectroscopic data are in close agreement with the anticipated structures. The anti-inflammatory protective effect of 3a–c was evaluated using the carrageenan-induced rat hind paw edema model. Moreover, a Tukey test was conducted to compare the data obtained herein with those for chalcones containing the nitro moiety in Ring A. Full article

Background: Centaurium erythraea Rafn. (C. erythraea) is a medicinal plant traditionally used in European folk medicine for the treatment of wounds, skin inflammations, and other dermatological conditions, in addition to its well-documented systemic antioxidant and anti-inflammatory effects. However, its topical applications remain insufficiently investigated, particularly using plant material collected from Romania. The purpose of this study was to prepare different ointment formulations containing C. erythraea Rafn. extract obtained from the aerial parts of the plant, using various excipients, and to evaluate their in vitro and in vivo efficacy. Methods: The phytochemical profile of C. erythraea extract was characterized using liquid chromatography–tandem mass spectrometry (LC–MS/MS). The lyophilized extract was pre-dissolved in different solubilizing agents—Transcutol^® P (diethylene glycol monoethyl ether), Capryol^® 90 (propylene glycol monocaprylate), or a combination of both—and then incorporated into five ointment formulations. Texture analysis and an in vitro membrane diffusion study were performed. The antioxidant capacity of the formulations was assessed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, ferric reducing antioxidant power (FRAP), and total phenolic content (TPC) assays. Anti-inflammatory activity was evaluated in vitro using tumor necrosis factor-alpha (TNF-α)-induced interleukin-1 beta (IL-1β) production in human keratinocyte (HaCaT) cells, and in vivo using a carrageenan-induced rat paw edema model. Results: LC–MS/MS identified 18 polyphenolic compounds, with hyperoside (3.78 ± 0.05 µg/mL), protocatechuic acid (1.13 ± 0.06 µg/mL), chlorogenic acid (1.07 ± 0.06 µg/mL), and quercetin (0.53 ± 0.03 µg/mL) as the principal constituents. The formulation containing both Transcutol^® P and Capryol^® 90 exhibited the most pronounced antioxidant activity (65% DPPH inhibition; 69.71 ± 0.83 mg gallic acid equivalent/mL) and significantly reduced IL-1β levels by 45.7% compared to the inflamed control. In vivo, this formulation showed comparable anti-edematous effects to a methylprednisolone ointment. Furthermore, it demonstrated the highest skin permeation efficiency, with a quercetin diffusion coefficient of 35.12 × 10⁻⁵ cm²/min. Conclusions: These findings highlight the therapeutic potential of C. erythraea extract from aerial parts in topical formulations and underscore the enhancing role of Transcutol^® P and Capryol^® 90 in improving both the pharmacodynamic and pharmacokinetic properties of bioactive compounds. Full article

The need for new medications to treat diabetes mellitus (DM) is a global health concern due to the cost and impact on patients and their families, health systems, and society. Recent approaches in drug development have focused on multitarget therapy for DM, considering its multifactorial and complex pathophysiology. The present work contributes to the review of the plant species Schinus molle L. (pirul), a tropical tree native to South America but now widespread worldwide, which has demonstrated anticancer, analgesic, antibacterial, and insecticidal properties. According to traditional uses, pirul has been employed as a food condiment, in the preparation of beverages and chewing gums, and in the treatment of DM. The antidiabetic effects of pirul appear to act through several mechanisms involved in DM. The methanolic extract of S. molle fruits collected in Tunisia exhibited a dose-dependent inhibition on both α-amylase and α-glucosidase enzymes (77.49% and 86.45%, respectively). A dose-dependent anti-inflammatory effect was also observed at 1, 2, 3, 4, and 5 h, in the carrageenan-induced rats’ paw edema model. Furthermore, in both the H₂O₂ and the superoxide radical assays, the pirul extract demonstrated moderate antioxidant activity (IC₅₀ = 0.22 mg/mL). Isomasticadienonic acid and Masazino-flavanone, the major components of active fractions and extracts of S. molle represent promising antidiabetic agents. Although pirul appears to be safe in in vivo acute and subchronic administrations, toxicological studies and clinical trials in individuals with DM are still pending. Full article

This study reports the development and optimization of a Melissa officinalis oil-based nanoemulgel for transdermal delivery using a Design-of-Experiments (DoE) approach. A Central Composite Design (CCD) was applied to optimize Tween 80 concentration and homogenization time, resulting in a nanoemulsion with a droplet size of 127.31 nm, PDI of 17.7%, and zeta potential of −25.0 mV, indicating good colloidal stability. FTIR analysis confirmed the presence of functional groups such as O–H, C=O, and C–O–C, supporting the oil’s phytochemical richness and therapeutic potential. DSC analysis revealed enhanced thermal stability and successful encapsulation, while SEM imaging showed a uniform and spherical microstructure. The drug release followed Higuchi kinetics (R² = 0.900), indicating diffusion-driven release, with the Korsmeyer–Peppas model (n = 0.88) suggesting anomalous transport. Antibacterial studies showed inhibition of Staphylococcus aureus (MIC = 250 µg/mL) and Escherichia coli (MIC = 500 µg/mL). In vivo anti-inflammatory testing demonstrated significant edema reduction (p < 0.05) using a carrageenan-induced rat paw model. These results support the potential of Melissa nanoemulgel as a stable and effective topical therapeutic for inflammatory and microbial skin disorders. Full article

Gynostemma pentaphyllum (GP) is a medicinal plant that has long been used as drug for the treatment of rheumatism, liver disease, and diabetes. In this study, GP was extracted with 50% ethanol extract, and then the extract was heat-processed under high pressure to analyze the anti-inflammatory potential of these extract (named actiponin (AP)) and its derived components, damulin A and damulin B, in RAW264.7 cells and carrageenan-induced rat models. Ap had no effect on RAW264.7 cells up to 180 μg/mL, but DA and DB showed cytotoxicity from 18 μM. Pretreatment with AP significantly suppressed the LPS-induced increase in nitric oxide (NO) and inducible nitric oxide synthase (iNOS) protein expression via griess reagent and Western blot analysis, and these effects were similar to those of DA and DB. AP, DA, and DB also significantly suppressed the expression of prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2) protein, which were increased by LPS, in a concentration-dependent manner. In addition, AP, DA, and DB inhibited the LPS-induced increase in pro-inflammatory cytokines, tumor necrosis factor (TNF)-α, and interleukin (IL)-6 in RAW264.7 cells. The anti-inflammatory activities of AP, DA, and DB are mediated by the suppression of the nuclear factor (NF)-κB and phosphorylation of mitogen-activated protein kinases (MAPKs) signaling pathways. Oral administration of 30, 50, 100, or 200 mg/kg (AP) suppressed carrageenan-induced edema in a concentration-dependent manner. Collectively, these results suggest that AP exerts potential anti-inflammatory activity by suppressing the inflammatory-mediators and pro-inflammatory cytokines via the NF-κB and MAPK pathways in vitro and by reducing the thickness of carrageenan-induced paw edema in vivo. Full article

Objectives: Our study aimed to examine the antioxidative and anti-inflammatory potential of the lyophilized aqueous leaf extract of Vitis vinifera. Methods: The antioxidant capacity of the extract was evaluated using the DPPH and FRAP assays. The in vivo phase of the study included 40 male Wistar albino rats. One half of the animals were used to induce the carrageenan model of acute inflammation, while the other half were used for examination of the extract effect on the redox state. Rats from the experimental group drank tap water containing 150 mg/kg Vitis vinifera extract for 14 days, while control animals received saline at the same volume. The molecular docking studies of polyphenols present in the leaf extract were conducted in AutoDock Vina. Results: In vitro assessment of the antioxidative capacity of the applied extract revealed significant free radical scavenging activity (IC₅₀ value 11.63 µg/mL), along with a pronounced ferric reducing ability (0.143 at 700 nm). Moreover, animal treatment with the extract led to significant paw edema inhibition (30.34%, 35.06%, and 41.54% in the second, third, and fourth hours, respectively) and to pro-oxidative marker reduction. Additionally, Vitis vinifera extract significantly increased catalase activity and glutathione levels. The in silico results showed that rutin binds to cyclooxygenase 1 (−8.2 kcal/mol) and 2 (−8.3 kcal/mol), as well as to antioxidant enzymes (catalase: −8.6 kcal/mol, SOD: −7.4 kcal/mol), indicating its key role in mediating the biological activity of the tested extract. Conclusions: This study highlights the significant antioxidant and anti-inflammatory potential of V. vinifera lyophilized aqueous leaf extract from the Serbian market, supported by both in vivo and in silico analyses. Full article

Cannabis sativa root has traditionally been used to relieve pain and inflammation, but its pharmacological properties remain underexplored due to low levels of psychoactive cannabinoids. This study aimed to investigate the anti-inflammatory and antinociceptive effects of the ethyl acetate fraction of Cannabis sativa root (CSREA) using in vivo rodent pain models. Mice were subjected to formalin and acetic acid-induced nociceptive tests, while rats were evaluated using a carrageenan-induced paw edema model. CSREA significantly reduced pain-related behaviors in both early (0–10 min) and late phases (15–30 min) of the formalin test and decreased writhing responses in the acetic acid model. Notably, CSREA also improved survival rates following acetic acid injection. Inflammatory markers, including IL-6 and IL-1β, were significantly lowered in serum. Furthermore, CSREA suppressed paw edema and redness in the carrageenan-induced rat model, demonstrating dose-dependent anti-inflammatory efficacy comparable to diclofenac. CSREA also downregulated pain-related gene expression (SCN9A, ASIC1A, TACR1) and regulated key enzymes involved in endocannabinoid metabolism (FAAH, MAGL, DAGL), suggesting its role in the molecular modulation of pain pathways. These effects are likely mediated via modulation of the endocannabinoid system, particularly by rebalancing the CB1R/CB2R ratio. The findings suggest that CSREA holds promise as a natural therapeutic agent for managing pain and inflammation and warrants further investigation into its molecular mechanisms and long-term effects. Full article

Background/Objectives: This study aimed to investigate the traditionally claimed anti-inflammatory effect of essential oil (EO) derived from pine green cones per se and after encapsulation into liposomes, which is expected to enhance its bioactivity and stability. Methods: The chemical profiling of EO was conducted using GC/GC-MS. The physico-chemical characterization of the liposomal formulation (LEO) included encapsulation efficiency, FTIR spectroscopy, and AFM imaging. Additionally, parameters such as mean particle diameter, polydispersity index, zeta potential, pH, and electrical conductivity were evaluated and reassessed after 30 days and 1 year to determine formulation stability. The in vivo anti-inflammatory effect of the EO and LEO was examined using a carrageenan-induced rat paw edema model. Results: The Pinus halepensis EO contained 14 components, mainly, α-pinene, myrcene, and (E)-caryophyllene. Encapsulation efficiency was 97.35%. AFM analyses confirmed the nanoscale dimensions and spherical shape of liposomes, while FTIR indicated successful encapsulation through overlapping functional groups. The droplet size of blank liposomes (L) ranged from 197.4 to 217 nm, while adding the EO decreased the droplet size and electrical conductivity. The polydispersity index (PDI) remained below 0.2. The zeta potential of the liposomes was between −35.61 and −49.43 mV, while the pH value was in the range of 4.35 to 5.01. These results indicate satisfactory stability across repeated measurements. Administration of LEO significantly inhibited paw edema relative to the controls, with a percentage inhibition of approximately 69%, which does not significantly differ from the effect of hydrocortisone, which was used as a positive control. Conclusions: This is the first study to report liposomal encapsulation and in vivo anti-inflammatory activity of an EO derived specifically from green cones of P. halepensis. Our findings demonstrate that EO-loaded liposomes exhibited favorable physico-chemical properties and notable anti-inflammatory activity, comparable to that of hydrocortisone. These results support their potential application in the development of effective topical anti-inflammatory formulations. Full article

Background: The pursuit of novel anti-inflammatory agents with enhanced efficacy and safety is crucial. Pyrrole-containing compounds, integral to many NSAIDs, exhibit promising anti-inflammatory properties. Compound 3f (2-(3-acetyl-5-(4-chlorophenyl)-2-methyl-1H-pyrrol-1-yl)-3-phenylpropanoic acid), a pyrrole derivative structurally inspired by the COX-2 selective inhibitor celecoxib, was evaluated for its anti-inflammatory and immunomodulatory effects. Methods: Anti-inflammatory activity was assessed in a carrageenan-induced paw edema model in Wistar rats. Compound 3f was administered intraperitoneally at 10, 20, and 40 mg/kg, either as a single dose or daily for 14 days. Diclofenac (25 mg/kg) served as the reference. Edema volume was measured by plethysmometry. Systemic inflammation was induced by lipopolysaccharide (LPS), and serum levels of the pro-inflammatory cytokine TNF-α and anti-inflammatory cytokines IL-10 and TGF-β1 were quantified by ELISA following single and repeated administration of compound 3f. Results: Single-dose administration of compound 3f at 20 mg/kg significantly reduced paw edema at 2 h (p = 0.001). After 14 days, all tested doses significantly inhibited paw edema at all time points (p < 0.001). In the LPS-induced systemic inflammation model, repeated treatment with 40 mg/kg of compound 3f significantly decreased serum TNF-α (p = 0.032). TGF-β1 levels increased significantly after both single and repeated doses (p = 0.002 and p = 0.045, respectively), while IL-10 levels remained unaffected. Conclusions: Compound 3f exhibits potent anti-inflammatory activity, particularly after repeated dosing, reflected by reduced local edema and systemic TNF-α suppression. The marked elevation of TGF-β1 indicates a potential immunomodulatory mechanism, selectively modulating cytokine profiles without altering IL-10. These findings support compound 3f as a promising candidate for targeted anti-inflammatory therapy involving cytokine regulation. Full article

Background: Inflammation abrogates cellular organization and tissue homoeostasis, resulting in redness, swelling, heat, pain, and loss of function. A model of carrageenan-induced paw edema (CIE) is commonly utilized to test anti-inflammatory substances. Based on the ability of Lepisanthes alata (LA), a tropical plant that is rich in phytochemicals like polyphenols, this study assessed the optimal dose and the health benefits of LA in rats that had been induced with carrageenan to develop paw swelling. Methods: Twenty-four male Wistar rats were divided into four groups to which carrageenan was administered, after which, distilled water at oral dose (C + DW), sodium diclofenac 25 mg/kg (C + DS), LA extract in 250 mg/kg (C + LA250), and 500 mg/kg (C + LA500) was given, respectively. Paw edema was assessed in 24 h. Pain was assessed using the Rat Grimace Scale (RGS), cytokines, antioxidant activity, and tissue changes. Results: LA at 250 and 500 mg/kg significantly decreased paw edema and inflammatory markers in the results of both studies. Remarkably, LA 250 mg/kg significantly decreased RGS scores as well as IL-1β, TNF-α, and histological inflammation but had a positive effect on T-SOD levels. Conclusions: LA extract, especially at 250 mg/kg, shows potent anti-inflammatory, analgesic, and antioxidant properties in CIE rats. Full article

Background/Objectives: Inflammation is a crucial and complex mechanism that protects the body against infections. In our study, we propose to provide scientific evidence for the anti-inflammatory properties of 1,3,5-triazine derivatives. Methods: Initially, we ensured the safety of the three synthesized derivatives by administering graded doses of up to 2000 mg/kg intraperitoneally in Wistar rats. Thus, the three derivatives were considered generally safe. We also evaluated their ability to reduce carrageenan-induced rat paw edema. Results: Compounds 1, 2, and 3 demonstrated stronger anti-inflammatory activity than indomethacin (10 mg/kg), achieving maximum inhibition at the fourth hour with percentages of 96.31%, 72.08%, and 99.69%, respectively, at a dose of 200 mg/kg, compared to 57.66% for the standard drug. To explore the mechanism, levels of pro-inflammatory cytokines (TNF-α, IL-1α, IL-1β, IL-6, CRP) and oxidative stress markers were measured in paw tissue. All three compounds significantly reduced these markers more effectively than indomethacin and enhanced antioxidant levels (SOD and GSH) beyond those achieved by the standard treatment. Additionally, the compounds reduced COX-1 and COX-2 levels to values comparable to those in the normal (non-inflamed) control group. Conclusions: Compounds 1, 2, and 3 at doses of 200 mg/kg significantly (p  < 0.05) inhibited the heat-induced hemolysis of red blood cell (RBC) membranes by 94.6%, 93.9%, and 95.2%, respectively, compared to 94.5% produced by indomethacin. Consequently, we concluded that 1,3,5-triazine derivatives are a safe antioxidant agent with significant anti-inflammatory activity. Full article

In the present study, five novel dexketoprofen amide derivatives with a free carboxyl group in their side chains were synthesized. The in vivo anti-inflammatory potential of dexketoprofen derivatives was evaluated using a carrageenan-induced paw edema model of acute inflammation. Additionally, the local and systemic redox status in rats following acute administration of the compounds was assessed by measuring levels of pro-oxidative markers and the activity of antioxidant enzymes. Among the analyzed molecules, derivatives 2 and 4 exhibited the most potent in vivo anti-inflammatory activity, showing effects comparable to those of the parent compound dexketoprofen. In vitro results revealed that all newly synthesized compounds exhibited low inhibitory activity toward COX-1, whereas only compound 4 showed significant COX-2 inhibition. The stronger binding affinity of derivative 4 for COX-2 in comparison to other tested compounds is likely attributed to its ability to form multiple electrostatic interactions within the enzyme’s active site. Furthermore, compounds 2 and 5 demonstrated efficacy comparable to the parent drug in restoring redox balance, indicating their potential antioxidant properties under acute inflammatory conditions. The findings of this study underscore the therapeutic potential of the novel dexketoprofen amide derivatives as dual-function agents with the capacity to modulate both inflammatory responses and oxidative stress. Full article

Background/Objectives: Essential oils are increasingly recognized for their therapeutic potential, yet Ammoides verticillata essential oil (AVEO) remains relatively unexplored, particularly for its anti-inflammatory and analgesic properties. This study aimed to profile AVEO’s chemical composition and evaluate its antioxidant, anti-inflammatory, and analgesic effects, with a focus on its novel pharmacological actions. Methods: The chemical composition of AVEO was determined using GC-MS analysis, and antioxidant capacity was assessed through in vitro assays. Furthermore, the anti-inflammatory potential was investigated using a carrageenan-induced paw edema model in rats, complemented by the inhibition assays of cyclooxygenase (COX) enzymes. The analgesic effects were evaluated through acetic acid-induced writhing and tail immersion tests. Additionally, a computational study was performed to explore the binding affinity of AVEO’s major constituents to COX-2. Results: GC-MS analysis revealed a rich monoterpene profile dominated by carvacrol (32.51%). It was found that AVEO exhibited significant antioxidant activity. Similarly, in vivo, AVEO showed significant anti-inflammatory effects, achieving a percentage inhibition of 52.23% at 200 mg/kg, comparable to diclofenac, along with potent COX-2 inhibition observed (IC₅₀ = 1.51 ± 0.20, SI = 5.56). Moreover, analgesic tests demonstrated dose-dependent pain relief, in which the dose of 200 mg/kg significantly prolonged tail latency to 14.00 ± 1.45 s and markedly reduced abdominal constriction to 21.17 ± 1.62. Computational analysis further corroborated the high binding affinity of carvacrol and thymol with COX-2 (−7.381 and −6.939 Kcal/mol, respectively). Conclusions: These findings underscore AVEO’s potential as a promising therapeutic agent for managing inflammation and pain. Full article

The objective of this work is to study the anti-inflammatory effect in vitro and in vivo of microwave (MW) extracts of Thymus algeriensis. The in vitro study was performed by the human red blood cell protection test, while the in vivo study used the carrageenan-induced rat paw edema model. The experimental results were confirmed by a molecular docking calculation. The results indicated that all the microwave extracts have a moderate anti-inflammatory effect, depending on their richness in phenolic compounds. Among the extracts studied, the one obtained at 100 °C for 15 min exhibited the most pronounced anti-inflammatory effect, with an inhibition of 78.52%, which is attributed to its high flavonoid content. In particular, the flavonoids naringin and catechin showed the best affinity for the target protein, with values of −10.3 kcal/mol and −9.2 kcal/mol, respectively, as well as low inhibition constants of 0.028 μM and 0.18 μM. These results indicate that these flavonoids generate interactions that enhance the stability of the target ligand–protein complex, thus contributing to the observed anti-inflammatory effect. Full article