Standard Anti-inflammatory Drug Research Articles

Design, Synthesis, Drug-Likeness, anti-Inflammatory, Antimicrobial Activity, and Molecular Docking Studies of Pyrimidine Analogs

Grounded on medicinal significances of pyrimidines, herein we are reporting initially the design and synthesis of 1-(2-benzylthiopyrimidin-4-yl)-benzimidazol-2-thioacetic acid/thioacetate 2(a, b), 1-(2-benzylthiopyrimidin-4-yl)-3,5 diaryl-2-pyrazoline (3) and 1-(2-benzylthiopyrimidin-4-yl)-3,5-dimethylpyrazole (4). In silico screening such as molecular docking studies of these compounds with inflammation-causing enzyme cyclooxagenase-2 (COX-2) suggests that only 2a has shown a strong affinity for the COX-2 (−9.0 kcal/mol) and forms three hydrogen bonds with active amino acid residues in comparison with standard anti-inflammatory drugs celecoxib (-8.8 kcal/mol) and indomethacin (-7.7 kcal/mol). However, in vitro, anti-inflammatory activity reveals that IC50 of compound 2a was 3.5 μM compared to celecoxib with IC50 of 0.65 μM. Also, 2a has displayed comparable activity of standard antibacterial drug gentamycin against E. coli with MIC 6.5 μM. Furthermore, the drug-likeness of potent compounds was studied using Swiss ADME and Mol inspiration software. All the compounds showed optimum drug-likeness without violating Lipinski’s rule of five. With our best observation and based on comparative SAR studies of these analogs with celecoxib and indomethacin, we conclude that compound 2a could develop as a therapeutically potent anti-inflammatory agent.

Synthesis and biological evaluation of gallic acid esters as phagocyte oxidative burst inhibitors

Several degenerative diseases, including cancer, are caused by oxidative stress, which is caused by the overproduction and accumulation of free radicals. The purpose of the study was to synthesize gallic acid (GA or 3,4,5-trihydroxybenzoic acid) esters and evaluate their anti-inflammatory potential through the inhibition of reactive oxygen species (ROS). The compounds methyl gallate (2), sec-butyl gallate (3), ethyl gallate (4), isopropyl gallate (5), 2-methoxyethyl gallate (6), 4-methoxybutyl gallate (7), 2-methylbutyl gallate (8) and pentan-3-yl gallate (9) were synthesized. 1H NMR, MS and IR data are reported for compounds 2-9, and 13C NMR data for compounds 2, 3, 5, and 6. The molecular formulae of compounds 3 and 7-9 were established by HREI-MS spectroscopic data. All the synthesized compounds were tested for their anti-inflammatory and cytotoxic activities by chemiluminescence and MTT cytotoxicity assay respectively. The results revealed the anti-inflammatory potential of compounds 2-8 with an IC50 range between (13.3 – 54.3 µM) as compared to the standard anti-inflammatory drug, Ibuprofen (IC50 = 54.3 ± 9.2 μM). The most potent inhibitors were found to be compound 3 (ROS IC50 = 15.0 ± 6.6 µM) and compound 7 (ROS IC50 = 13.3 ± 0.8 µM). All compounds were found to be non-cytotoxic in the NIH-3T3 fibroblast cell line. Compounds 3, 7- 9 were identified as new compounds.

Formulation and Development of Polyherbal Ointment containing Clerodendrum serratum, Solanum xanthocarpum, and Nyctanthes arbortristis Extracts and Assessment of Anti-inflammatory Activity in Carrageenan-Induced Paw Edema Model

In this study, our objective was to explore the phytochemical constituents of Clerodendrum serratum (CS), Solanum xanthocarpum (SX), and Nyctanthes arbortristis (NA) and evaluate their anti-inflammatory activity. Subsequently, we aimed to develop a polyherbal ointment formulation incorporating these extracts. The phytochemical screening of the CS extract showed carbohydrates, steroids, terpenoids, flavonoids, saponins, and tannins. Similarly, the SX extract exhibited the presence of all these constituents, along with the additional presence of alkaloids. The NA extract demonstrated the presence of alkaloids, tannins, glycosides, and flavonoids. CS roots exhibited notable inhibition of inflammation at the given doses and periods of 1 to 5 hours, surpassing the effectiveness of the standard anti-inflammatory drug, indomethacin. The polyherbal ointments were found to be greenish, non-transparent, and with acceptable pH. F3 formulation demonstrated excellent viscosity of 1200 cp, making it easy to apply on the skin. Furthermore, formulation F3 demonstrated exceptional spreadability, covering a diameter of 1.8 cm, surpassing the other formulations. Importantly, all polyherbal formulations were non-irritant when applied to the skin, as evidenced by the absence of edema or erythema upon application to rat skin. F3 formulation indicated no physicochemical variations in comparison to initial results in stability studies. Even after the 6-month stability study, the ointment formulation maintained a smooth and greenish consistency, signifying its durability and stability. These findings suggest that the developed polyherbal ointment formulation can be stored at room temperature without any additional requirements. Overall, this polyherbal ointment formulation represents a promising alternative approach to existing topical formulations for the effective treatment of inflammatory conditions.

Facing the Challenges in the COVID-19 Pandemic Era: From Standard Treatments to the Umbilical Cord-Derived Mesenchymal Stromal Cells as a New Therapeutic Strategy

Coronavirus disease 2019 (COVID-19), the pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which counts more than 650 million cases and more than 6.6 million of deaths worldwide, affects the respiratory system with typical symptoms such as fever, cough, sore throat, acute respiratory distress syndrome (ARDS), and fatigue. Other nonpulmonary manifestations are related with abnormal inflammatory response, the “cytokine storm”, that could lead to a multiorgan disease and to death. Evolution of effective vaccines against SARS-CoV-2 provided multiple options to prevent the infection, but the treatment of the severe forms remains difficult to manage. The cytokine storm is usually counteracted with standard medical care and anti-inflammatory drugs, but researchers moved forward their studies on new strategies based on cell therapy approaches. The perinatal tissues, such as placental membranes, amniotic fluid, and umbilical cord derivatives, are enriched in mesenchymal stromal cells (MSCs) that exert a well-known anti-inflammatory role, immune response modulation, and tissue repair. In this review, we focused on umbilical-cord-derived MSCs (UC-MSCs) used in in vitro and in vivo studies in order to evaluate the weakening of the severe symptoms, and on recent clinical trials from different databases, supporting the favorable potential of UC-MSCs as therapeutic strategy.

Multicomponent Photocomposition as A Source for Development New Anti-Inflammatory Medicines

The results of experimental studies on mature white male rats showed that phytocompositions 1, 2 and 3 containing various extracts of medicinal plants have a distinct antiphlogogenic activity. Among the studied phytocollections, composition 3 showed a higher anti-inflammatory activity compared to other studied phytocollections. The studied new mixtures of medicinal plants have a higher antiphlogogenic activity than canephron, especially phytocomposition 3, and in terms of their pharmacological activity, it is not inferior to the gold standard non-steroidal anti-inflammatory drug - sodium diclofenac.

Bio-guided isolation of potential anti-inflammatory constituents of some endophytes isolated from the leaves of ground cherry (Physalis pruinosa L.) via ex-vivo and in-silico studies

BackgroundDue to the extensive potential of previously studied endophytes in addition to plants belonging to genus Physalis as a source of anti-inflammatory constituents, the present study aimed at isolation for the first time some endophytic fungi from the medicinal plant Physalis pruinosa.MethodsThe endophytic fungi were isolated from the fresh leaves of P. pruinosa then purified and identified by both morphological and molecular methods. Comparative evaluation of the cytotoxic and ex vivo anti-inflammatory activity in addition to gene expression of the three pro-inflammatory indicators (TNF-α, IL-1β and INF-γ) was performed in WBCs treated with lipopolysaccharide (LPS) for the identified endophytes, isolated compounds and the standard anti-inflammatory drug (piroxicam). For prediction of the binding mode of the top-scoring constituents-targets complexes, the Schrödinger Maestro 11.8 package (LLC, New York, NY) was employed in the docking study.ResultsA total of 50 endophytic fungal isolates were separated from P. pruinosa leaves. Selection of six representative isolates was performed for further bioactivity screening based on their morphological characters, which were then identified as Stemphylium simmonsii MN401378, Stemphylium sp. MT084051, Alternaria infectoria MT573465, Alternaria alternata MZ066724, Alternaria alternata MN615420 and Fusarium equiseti MK968015. It could be observed that A. alternata MN615420 extract was the most potent anti-inflammatory candidate with a significant downregulation of TNF-α. Moreover, six secondary metabolites, alternariol monomethyl ether (1), 3’-hydroxyalternariol monomethyl ether (2), alternariol (3), α-acetylorcinol (4), tenuazonic acid (5) and allo-tenuazonic acid (6) were isolated from the most potent candidate (A. alternata MN615420). Among the tested isolated compounds, 3’-hydroxyalternariol monomethyl ether showed the highest anti-inflammatory potential with the most considerable reductions in the level of INF-γ and IL-1β. Meanwhile, alternariol monomethyl ether was the most potent TNF-α inhibitor. The energy values for the protein (IL-1β, TNF-α and INF-γ)–ligand interaction for the best conformation of the isolated compounds were estimated using molecular docking analysis.ConclusionsThe results obtained suggested alternariol derivatives may serve as naturally occurring potent anti-inflammatory candidates. This study opens new avenues for the design and development of innovative anti-inflammatory drugs that specifically target INF-γ, IL-1β and INF-γ.

Tailoring of Novel Bile Salt Stabilized Vesicles for Enhanced Transdermal Delivery of Simvastatin: A New Therapeutic Approach against Inflammation.

Simvastatin (SMV), a cholesterol-lowering agent, has antioxidant and anti-inflammatory effects. Nevertheless, the oral use of SMV is linked with poor systemic bioavailability owing to its limited aqueous solubility and extensive first-pass metabolism. The aim of this study was to evaluate the feasibility of transdermal delivery of SMV using bile salt stabilized vesicles (bilosomes) for enhancing the anti-inflammatory potential of SMV. SMV-loaded bilosomes (SMV-BS) were prepared by the thin film hydration technique and optimized by 33 Box-Behnken design. The fabricated SMV-BS were assessed for vesicle size, entrapment efficiency (% EE) and cumulative drug release. The optimized formula was incorporated into HPMC gel and investigated for physical properties, ex vivo permeation, in vivo pharmacokinetic study and anti-inflammatory potential in inflamed paw edema rat model. The optimized SMV-BS showed vesicle size of 172.1 ± 8.1 nm and % EE of 89.2 ± 1.8%. In addition, encapsulating SMV within bilosomal vesicles remarkably sustained drug release over 12 h, compared to plain drug suspension. Furthermore, SMV-loaded bilosomal gel showed a three-fold enhancement in SMV transdermal flux, compared to plain drug suspension. Most importantly, the relative bioavailability of SMV-BS gel was ~2-fold and ~3-fold higher than those of oral SMV suspension and SMV gel, respectively. In carrageenan-induced paw edema model, SMV-BS gel induced a potent anti-inflammatory effect, as evidenced by a remarkable reduction in paw edema, which was comparable to that of the standard anti-inflammatory drug, indomethacin. Collectively, bilosomes might represent a plausible transdermal drug delivery system that could enhance the anti-inflammatory activity of SMV by boosting its skin permeation and its systemic bioavailability.

In Silico Study on Anti-inflammatory Effect of Bioactive Compounds of Velvet Bean (Mucuna pruriens) Leaves Against NF-kB Activation Pathway

Activation of nuclear factor-kB (NF-ĸB) receptors potently enhances pro-inflammatory cytokines production thereby promoting inflammatory reactions. NF-ĸB receptor inhibition is one of the targets in overcoming inflammatory reactions. One of the natural ingredients that have the potential as an anti-inflammatory is velvet bean leaf extract (Mucuna pruriens L. (DC.)) which is used by the local people of West Sumatra. This study aimed to investigate the anti-inflammatory mechanism of the bioactive compounds detected in velvet bean leaf extract against NF-ĸB (1U36) activation pathway using an in silico approach. The phytochemical analysis of the ethanolic extract of velvet bean leaves was performed using GC-MS. Subsequently, their potential bioactivities were explored using PASS online test, preparation of ligands, receptors, and molecular docking. The results showed that the 34 compounds contained in the miang bean leaf extract had anti-inflammatory bioactivity with a probability activity value of >0.7 based on PASS online. The docking results showed that the highest binding affinity value was found in artemin (-7.5 kcal/mol) which was higher than the standard anti-inflammatory drug ketoconazole (-7.2 kcal/mol). Therefore, one of the mechanisms of miang bean leaves as an anti-inflammatory is due to the inhibitory action of artemin on the NF-kB activation pathway.

Nimbolide attenuates complete Freund's adjuvant induced arthritis through expression regulation of toll-like receptors signaling pathway.

Nimbolide is an active constituent of Azadirachta indica and is known for its anti-inflammatory, anti-oxidant, immune-modulatory, and anti-cancer effects. Few studies suggest that nimbolide treatment influences the responses to rheumatoid arthritis, but the underlying molecular mechanisms involved are not yet well established. Therefore, the present study was designed to determine the effect of nimbolide on expression regulation of toll-like receptors to attenuate rheumatoid arthritis. The rheumatoid arthritis model was established by injecting complete Freund's adjuvant (CFA) intra-dermally into the sub-plantar region of the left hind paw of rats. Nimbolide (20 mg/kg) and piroxicam (10mg/kg) were given to arthritic rats. Rats treated with nimbolide showed a significant reduction in inflammatory cells, rheumatoid factor, ESR, and improved the body weight. The results indicated that nimbolide possesses the capacity to attenuate rheumatoid arthritis by downregulating toll-like receptors, IL-17, IL-23, HSP70, and IFN-γ expression levels. Nimbolide treatment showed significant reduction in the severity of inflammation and destruction of joints and showed comparable effects to piroxicam, which is a standard non-steroidal anti-inflammatory drug used for the treatment of rheumatoid arthritis. It can be concluded that nimbolide can be considered as a potential candidate for therapeutic targeting of the toll-like receptors pathway in rheumatoid arthritis.

Influence of laboratory-controlled ethanolic wheatgrass extract on acetic acid-induced changes in biochemical and antioxidant indices in the colitis of Wistar rats

Introduction and Aim: Triticum aestivum (wheatgrass) is a good source of mineral nutrients and antioxidant enzymes. It also acts as a detoxifying agent and helps to revive healthy cells. The present study aimed to assess the effects of acetic acid on biochemical and antioxidant indices in the colitis of Wistar rats using an ethanolic extract derived from the dried shoots of wheatgrass maintained under specified growth conditions.
 
 Materials and Methods: Aqueous and ethanolic extract of wheatgrass was subjected to preliminary phytochemical screening and in-vitro antioxidant activity. Effects of the ethanolic wheatgrass extract were investigated in the acetic acid-induced rat colitis model. Sulphasalazine was used as the standard anti-inflammatory drug. Malondialdehyde (MDA), myeloperoxidase (MPO), total antioxidant capacity (TAC), catalase (CAT), and reduced glutathione (GSH) levels were estimated in the rat blood. Colitis was quantified with a clinical score and colon length/weight index was measured. Histopathological analyses were also performed on the colon tissue of rats.
 
 Results: The presence of phytochemical elements such as saponins, tannins, alkaloids, and terpenes in aqueous and ethanolic wheatgrass extract was discovered. These compounds have the potential to boost antioxidant and anti-inflammatory effects. The ethanolic extract significantly reduced MDA, MPO, and antioxidant levels (TAC, CAT, and GSH) in colon tissue and blood. Biochemical measurements corroborated the conclusions of histopathological investigation.
 
 Conclusion: According to macroscopic, microscopic, histological, and other biochemical studies, ethanolic wheatgrass extract significantly inhibits experimental colitis in rats.

Targeting of Nrf2/PPARγ/NLRP3 Signaling Pathway by Stevia rebudiana Bertoni Extract Provides a Novel Insight into Its Protective Effect against Acute Gouty Arthritis-Induced Synovial Inflammation, Oxidative Stress and Apoptosis in a Rat Model

Our research work examined the potential protection of Stevia rebaudiana extract against monosodium urate crystals (MSU)-induced acute gouty arthritis in a rat model and its possible underlying mechanism. Forty rats were allocated into four groups (n = 10); a control group; an MSU group, whose rats received 0.1 of MSU single intra-articular injection in the ankle joint on the fifth day of the experiment; an MSU + Stevia group, which received 250 mg/kg/day of Stevia extract orally for seven days and MSU crystals on the fifth day; and an MSU + colchicine group, which was administered colchicine at 0.28 mg/kg daily for seven days and MSU crystals on the fifth day. Pretreatment with Stevia extract mitigated MSU-induced inflammation as evidenced by a decrease of the ankle edema and inflammatory cell infiltration and a significant downregulation of the protein level of NFκB, TNFα, IL-1β, IL6, and IL18 as well as NLRP3 gene expression. Additionally, there was a markedly increased PPARγ gene expression (p < 0.001) compared with the MSU group (p < 0.001) and alleviated oxidative stress via significant upregulating of Nrf2/HO-1. Moreover, the pretreatment attenuated apoptosis by significantly decreasing cytochrome c, Bax, Caspase-3, and by increasing Bcl-2 protein. In conclusion, Stevia extract exhibited strong anti-inflammatory, antioxidant, and antiapoptotic effects against MSU-induced gouty arthritis similar to the standard anti-inflammatory colchicine drugs.

Evaluation of anti-microbial and anti-inflammatory properties of ethanol extract of Allium sativum linn

This study evaluated the anti-microbial and anti-inflammatory properties of ethanol extract of Allium sativum linn. The ethanol extract yielded two distinct layers which differed in phytochemical composition, anti-microbial and anti-inflammatory properties. In the base filtrate (BF), tannins, carbohydrates, alkaloids, glycosides, reducing sugars, flavonoids, saponins, acidic compounds and resins were found present. The methanol fraction of the base filtrate was however found to have resins and tannins. The acute toxicity (oral) in this study was 3,750 mg/kg. Anti-microbial activity was tested using clinical isolates of Staphylococcus aureus, Streptococcus pneumonia, Escherichia coli, Salmonella typhi, and Klebsiella pneumonia, with Penicillin-G, Erythromycin, Gentamicin, Ciprofloxacin and Ceftriazone as standard drugs. The upper filtrate and base filtrate of the extract were found to exhibit a statistically significant and dose-dependent inhibitory effect on all test micro-organisms when compared with control. The result of the systemic anti-inflammatory study showed that the extract had a statistically significant, dose and time dependent systemic anti-inflammatory effect when compared with the negative and positive controls. The topical anti-inflammatory study showed a statistically significant, dose and time dependent topical anti-inflammatory effect at all tested doses. In conclusion, this study was able to establish that extract of Allium sativum had a statistically significant (p< 0.05) anti-microbial and anti-inflammatory effects, which is comparable to standard anti-microbial and anti-inflammatory drugs. This pharmacological effect may be due to the abundant presences of phytochemical constituents in the ethanol extract of Allium sativum L. This goes a long way to support its extensive use as an anti-microbial and anti-inflammatory agent in ethno medicine.

Synthesis of PVA capped naproxen conjugated MgO nanoparticles and its bioactivity screening

The prescribed use of non-steroidal anti-inflammatory drugs is associated with numerous life-threatening side effects. There is a great need to develop low-dose NSAID formulations to prevent the rate of adverse events while retaining the therapeutic efficacy. In this context, we prepared nanoformulated naproxen using MgO as a nanocarrier and PVA as coating agent and investigated its biological activity in comparison to free form naproxen sodium (NPRS) and standard anti-inflammatory drugs. MgO nanoparticles with a hydrodynamic size of approximately 140–484 nm were prepared and conjugated with NPRS and capped with hydrophilic polymer (PVA) successfully. Conjugation of NPRS with MgO nanoparticles was confirmed by UV–Visible, FTIR, XRD, DLS, LIBS techniques. The hydrodynamic size and surface charge of nanoformulated naproxen were found to be 161 nm and −8.85 mV, respectively. Nanoformulated naproxen showed maximal and sustained release (>95%) at pH 6.8 within 24 h. Investigation of thermal attributes showed that the nanoformulated naproxen was more stable at a higher temperature than free NPRS. In vivo anti-inflammatory, analgesic, and antipyretic activities of nanoformulated naproxen revealed that in all cases, the potency and efficacy of nanoformulated naproxen were found to be higher than NPRS. Moreover, nanoformulated naproxen was well tolerated up to 2000 mg/kg b.w with an LD50 of 2574.77 mg/kg. The ratio between the minimum effective dose (1 mg/kg) and LD50 indicated a broader therapeutic window. Since the concentration of NPRS in nanoformulated naproxen was only 43.2 ± 2%, our results indicated that conjugation to MgO nanocarrier boosts the biological activity of NPRS by approximately 2.3 times. In addition, nanoformulated naproxen is found to be biocompatible and hemocompatible. We conclude that the nanosizing of a drug offer much promise as a better alternative to standard anti-inflammatory drugs for the treatment of various diseases.

In vitro, in vivo and in silico evaluation of the anti-inflammatory potential of Hyssopus officinalis L. subsp. aristatus (Godr.) Nyman (Lamiaceae)

Ethnopharmacological relevanceMedicinal properties of hyssop have been used in traditional medicine since ancient times, inter alia, in diseases/conditions with an inherent inflammatory process.Aim of the study: Accordingly, the aim of this study was to investigate the anti-inflammatory properties of hyssop herb preparations (essential oil and methanol extracts) in vivo, in vitro and in silico. Materials and methodsFor in vitro testing of essential oils and extracts of hyssop herb, the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme assays were used. In vivo anti-inflammatory potential of the extracts (at doses of 50, 100 and 200 mg/kg) was assessed using the carrageenan-induced rat paw edema test. Molecular docking and dynamics were used for in silico testing of the inhibitory activity of chlorogenic (CA) and rosmarinic (RA) acids, as the dominant compounds in the tested methanol extracts against COX-1 and COX-2 enzymes. ResultsSignificant inhibitory activity was shown in the COX-2 test regarding extracts (essential oils did not exhibit any significant activity). Namely, all analyzed extracts, at a concentration of 20 μg/mL, showed a percentage of inhibition of COX-2 enzyme (54.04–63.04%), which did not indicate a statistically significant difference from the positive control of celecoxib (61.60%) at a concentration of 8.8 μM. In vivo testing showed that all methanol extracts of hyssop herb, at the highest test dose of 200 mg/kg in the third and fourth hours, after carrageenan administration, exhibited a statistically significant (p < 0.05) inhibitory effect on the increase in rat paw edema in relation to control. This activity is comparable or higher in relation to the reference substance, indomethacin, at a concentration of 8 mg/kg. The preliminary in silico results suggest that investigated compounds (RA and CA) showed better inhibitory activity against COX-1 and COX-2 than standard non-steroidal anti-inflammatory drug (NSAID), ibuprofen, as evident from the free binding energy (ΔGbind in kJ mol−1). The binding energies of the docked compounds to COX-1 and -2 were found to be in the range between −47.4 and −49.2 kJ mol−1. Ibuprofen, as the one NSAID, for the same receptors targets, showed remarkably higher binding energy (ΔGbind = −31.3 kJ mol−1 to COX-1, and ΔGbind = −30.9 kJ mol−1 to COX-2). ConclusionThe results obtained not only support the traditional use of hyssop herb in inflammatory conditions in folk medicine, but also open the door to and the need for further in vivo testing of extracts in order to examine the molecular mechanism of anti-inflammatory activity in living systems and possibly develop a new anti-inflammatory drug or supplement.

Formulation and Evaluation of Enteric Coated Matrix Tablets of Mesalamine for Inflammatory Bowel Disease

Mesalamine is a gold standard anti-inflammatory drug used to treat inflammatory bowel illnesses. It's usually used to treat and keep Ulcerative Colitis in remission in mild to moderate cases. Mesalamine is rapidly cleared from circulation after being consumed orally, with an elimination half-life of only one hour. Oral intake of delayed or slow released matrix formulations can acquire therapeutic concentration in the intestines. The goal of this study was to use guar gum as a carrier to develop colon-specific delivery methods for mesalamine. The matrix tablets were made using the direct compression process, which is today regarded as a cost-effective and straightforward manufacturing method. Dip coating was used to coat the tablets with varied concentrations of Eudragit L100 polymer. Tablets were studied in vitro in a variety of dissolution solutions, including 0.1 N HCl (pH 1.2), phosphate buffers pH 6.8 and 7.4, and others. The optimized formulation was subjected to swelling tests. All of the formulations' physicochemical parameters were confirmed to be in line with pharmacopoeial norms. All formulations were subjected to stability tests in accordance with ICH recommendations. The tablets coated with Eudragit L100 (20 percent w/v) had a sustained release of 78.39 percent over 12 hours, while the uncoated tablets released the medication in 9 hours. Tablet stability tests revealed that under accelerated and room temperature storage settings for 6 months, there was reduced degradation. In the colon, the enteric-coated Eudragit L100 coated matrix tablets of mesalamine demonstrated promising site-specific drug delivery.&#x0D; Keywords: Mesalamine, Guar gum, Eudragit L100, Direct compression, Inflammatory bowel illnesses

Assessment of the Anti-inflammatory and Anti-oxidant Activities of Flavonoid-rich Fraction of &amp;lt;i&amp;gt;Pleiocarpa mutica &amp;lt;/i&amp;gt;Leaves

<i>Pleiocarpa mutica</i> is a medicinal plant that is native to large areas of tropical Africa and belongs to the family of <i>Apocynaceae</i>. It is a medicinal herb used in traditional Nigerian medicine to treat a variety of diseases, including inflammatory disorders. The present study investigated the anti-inflammatory and anti-oxidant effects of flavonoid-rich fraction of <i>Pleiocarpa mutica</i> leaves (FRFPML) using both <i>in-vivo </i>and <i>in-vitro </i>based assays. A total of thirty (30) adult male albino rats (110-150g) were divided into five (5) groups of six (6) rats each for the <i>in-vivo</i> anti-inflammatory assay. Group 1 untreated; Group 2 was given 10 mg/kg body weight of Indomethacin and Groups 3, 4 and 5 were given 200, 400 and 600 mg/kg body weight of FRFPML respectively. Tannins, phenols, flavonoids, alkaloids, steroids, terpenoids and saponins were found in varied amounts in the plant secondary metabolites according to quantitative analysis. The extract demonstrated no harm in an acute toxicity assay when dosed up to 5000 mg/kg b.w. Scalar dosages of the FRFPML significantly (p<0.05) suppressed the development of paw oedema induced by egg albumin in the systemic rat paw oedema model. This compares favorably to the standard anti–inflammatory drug indomethacin (10 mg/kg b.w) which at 24 hours inhibited egg albumin-induced rat paw oedema (11.82%). Varying doses of the extract significantly (p<0.05) inhibited egg albumin denaturation, hypotonicity-induced membrane stabilization, protease inhibition and phospholipase A₂ in a concentration-dependent manner, causing inhibition comparable to that of the standard anti-inflammatory drug used. The extract at different concentrations (0.2-0.8 mg/ml), significantly (p<0.05) exhibited DPPH (1-1diphenyl-2-picrylhydrazyl) and H₂O₂ (hydrogen peroxide) radical scavenging activities in a concentration-dependent manner similar to the standard antioxidant ascorbic acid used. Results from the study revealed that the FRFPML exhibited remarkable anti-inflammatory and anti-oxidant activity.

Antioxidant, antidiabetic, anti-inflammatory and anticancer potential of some seaweed extracts

This study aims to evaluate the secondary metabolites, cytotoxicity, antioxidant, antidiabetic, anti-inflammatory, and anticancer activities of four selected seaweeds Padina pavonica, Taonia atomaria, Jania rubens, and Corallina elongata. The maximum value of phenolic content (176.7 ± 6.9 mg gallic acid equivalents/g crude extract) and tannin content (26.5 ± 4.3 mg tannic acid equivalents/g crude extract), was shown in the methanol extract of J. rubens and P. pavonica, respectively. While the ethanol extract of T. atomaria recorded the highest values of total flavonoid content (374.1 ±27.4 mg quercetin equivalents/g crude extract) and total saponins content (30.2 ± 0.7 mg cholesterol equivalents/g crude extract, respectively) compared to other seaweeds. Methanol extract of J. rubens and C. elongata exhibited the greatest content of alkaloids (25.8 ± 4.4 and 22.7 ± 2.6 mg/g d wt.). The methanol extract of P. pavonica established the highest DPPH radical scavenging activity (55.7% ± 0.1) at 50 μg/mL. Among the selected seaweed extracts, the ethanol extract of T. atomaria demonstrated the maximum α-amylase inhibition capacity (66.3% ± 0.0). Methanol extract of J. rubens and P. pavonica species effectively prevented the hypotonicity-induced haemolysis in a concentration-dependent manner compared with the diclofenac potassium as a standard anti-inflammatory drug. In vitro, the reported results also supported the safety and non-toxicity of the four seaweed extracts on WI-38 cell line at lower concentrations. J. rubens and P. pavonica methanol extracts recorded the highest cell growth inhibition of the HeLa Cancer Cell Lines compared to other seaweed extracts and the standard drug Cisplatin.

Anti-inflammatory and healing activity of an hydroethanolic extract of Voacanga africana stapt ex Scoot-Elliot (Apocynaceae): In vivo model

Background: The mastery and supervision of traditional medicine in our country, particularly Senegal, would be of capital importance for the population. We were interested in the physiological effects of Voacanga africana (VOC) extracts in wound healing and topical inflammation. Aims and Objectives: This work was to evaluate the effects on inflammation and tissue repair of an hydroethanolic extract of V. africana. Materials and Methods: Wounds were created from a rat burn model and wound healing was evaluated (Kamoshida method) topical inflammation in a murine model of croton oil-induced inflammatory edema. For each experiment, batches of rats or of a mouse were formed, and every batch included five animals. Results: VOC’s 30% root bark ointment showed complete healing by day 16 for the burn test. As for inflammation, the 10% ointment inhibits 80% of the inflammatory edema in the same manner as indomethacin, used as the standard anti-inflammatory drug. Conclusion: VOC could have dose-dependent effects on inflammation and burn healing.

Evaluation of Anti-Inflammatory and Antioxidant Properties of Cayratia trifolia

Introduction: Cayratia trifolia is a plant belonging to the family Vitaceae and genus Cayratia. Anti-inflammatory activity is the property of a substance or treatment that reduces inflammation or swelling. Antioxidants are defined as substances that delay or inhibit oxidative damage to a target molecule and its principal function is its ability to trap free radicals. The alcoholic leaf extract of Cayratia trifolia has anti-inflammatory as well as antioxidant properties against inflammations and swelling and DPPH free radicals respectively and can be evaluated using both in vitro and in vivo assays. The principal aim of the study is to employ in-vitro assays to evaluate the anti-inflammatory and antioxidant properties of Cayratia trifolia.&#x0D; Materials and Methods: Plant extract of Cayratia trifolia was purchased and tested for anti-inflammatory and antioxidant properties. In case of evaluating the antioxidant activity, the methanolic extract of the plant was utilised. The examination of the anti-inflammatory properties of Cayratia trifolia involves acetyl salicylic acid as a positive control and aspirin and aspirin was employed as a standard anti-inflammatory drug.&#x0D; Results: The anti-inflammatory activity of Cayratia trifolia extract was examined and it was observed that the plant extract showed an increased percentage of inhibition of trypsin with increasing concentration. Similarly, the antioxidant activity was compared to Vitamin C and the percentage of inhibition of DPPH free radicals increased with the increase in concentration of the extract.&#x0D; Conclusion: Within the limits of the study, the plant extract of Cayratia trifolia was observed to possess both antioxidant and anti-inflammatory properties.

High Efficiency In Vitro Wound Healing of Dictyophora indusiata Extracts via Anti-Inflammatory and Collagen Stimulating (MMP-2 Inhibition) Mechanisms.

Dictyophora indusiata or Phallus indusiatus is widely used as not only traditional medicine, functional foods, but also, skin care agents. Biological activities of the fruiting body from D. indusiata were widely reported, while the studies on the application of immature bamboo mushroom extracts were limited especially in the wound healing effect. Wound healing process composed of 4 stages including hemostasis, inflammation, proliferation, and remodelling. This study divided the egg stage of bamboo mushroom into 3 parts: peel and green mixture (PGW), core (CW), and whole mushroom (WW). Then, aqueous extracts were investigated for their nucleotide sequencing, biological compound contents, and wound healing effect. The anti-inflammatory determination via the levels of cytokine releasing from macrophages, and the collagen stimulation activity on fibroblasts by matrix metalloproteinase-2 (MMP-2) inhibitory activity were determined to serve for the wound healing process promotion in the stage 2–4 (wound inflammation, proliferation, and remodelling of the skin). All D. indusiata extracts showed good antioxidant potential, significantly anti-inflammatory activity in the decreasing of the nitric oxide (NO), interleukin-1 (IL-1), interleukin-1 (IL-6), and tumour necrosis factor-α (TNF-α) secretion from macrophage cells (p < 0.05), and the effective collagen stimulation via MMP-2 inhibition. In particular, CW extract containing high content of catechin (68.761 ± 0.010 mg/g extract) which could significantly suppress NO secretion (0.06 ± 0.02 µmol/L) better than the standard anti-inflammatory drug diclofenac (0.12 ± 0.02 µmol/L) and their MMP-2 inhibition (41.33 ± 9.44%) was comparable to L-ascorbic acid (50.65 ± 2.53%). These findings support that CW of D. indusiata could be an essential natural active ingredient for skin wound healing pharmaceutical products.