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The present work aims to design interpenetrating polymer network (IPN) mediated hydrogel microbeads of hydrolyzed polyacrylamide-g-gum kondagogu (H-pAAm-g-GK) and sodium alginate (SA) for pH-sensitive gastroprotective drug delivery of diclofenac sodium (DS). In brief, the pAAm-g-GK was prepared using microwave irradiation, followed by conversion into a pH-sensitive polymer (H-pAAm-g-GK) using alkaline hydrolysis. Then, DS-loaded IPN microbeads were made utilizing an ionotropic gelation method using Ca+2 ions and glutaraldehyde (GA) as a crosslinking agent. After this, different characterizations, such as FT-IR, DSC, PXRD, swelling analysis, drug entrapment, drug release study, in vivo anti-inflammatory activity, etc., were performed. The amorphous state of DS in the microbeads was validated by thermograms and diffractograms, whereas SEM analysis confirmed the spherical shape of the obtained DS-loaded H-pAAm-g-GK@SA mediated microbeads. The pulsatile swelling analysis assured the H-pAAm-g-GK@SA mediated microbeads showed significantly increased swelling as the pH switched from 1.2 to 7.4. Additionally, the microbeads exhibit a 15% DS release in a pH 1.2 buffer medium, while a substantial 94% of the drug was released in a pH 7.4 buffer. It assured the DS release was drastically augmented as the pH of the surrounding medium was switched from acidic to alkaline. Principally, the COOH- groups of hydrogels offer ionization at higher pH levels, wherein the osmotic pressure within the microbeads rises, resulting in more swelling and higher drug release. Finally, the in vivo anti-inflammatory activity assured pH-sensitive sustained release of DS. In conclusion, the H-pAAm-g-GK@SA mediated pH-sensitive IPN hydrogel microbeads show potential in the design of gastroprotective oral delivery systems for DS. In the future, H-pAAm-g-GK can be used for the design of pH-sensitive IPN hydrogel microbeads for targeted delivery. [ABSTRACT FROM AUTHOR]

Artemisinin, artemether, artesunate, and dihydroartemisinin are renowned for their antimalarial potential. The current study aims to repurpose the above-mentioned artemisinic compounds (ACs) by conducting an intercomparison to evaluate their antiinflammatory potential (AIP). In order to develop potential candidates for the evaluation of AIP of ACs (50 and 100 mg/kg BW), carbon tetrachloride (1ml/kg body weight (BW)) was administered intraperitoneally to BALB/c mice. Alterations in animal behavior were assessed weekly through tail suspension test, force swim test, open field test, Y-maze test, inverted screen analysis, and weight lifting test. Aberrations in hematological, serological, endogenous antioxidants, and oxidative stress marker profiles were assessed in all twelve groups. Histological alterations were read using hematoxylin and eosin staining. Levels of inflammatory markers including nuclear factor kappa B (NF-κB), tumor necrosis factor alpha (TNF-α), and nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3), were determined using immunohistochemical analysis (IHCA). Antioxidant markers i.e., nuclear factor erythroid-2-related factor (Nrf-2) and thioredoxin (TRX) were also quantified through IHCA. Comet assay was performed to quantify DNA damage. Oral administration of ACs to mice significantly alleviated the carbon tetrachloride induced inflammation in comparison with silymarin. Reduced levels of several inflammatory markers including nitric oxide, thiobarbituric acid reactive substances, interleukin-1 beta, NF-κB, TNF-α, and NLRP3, underscore the substantial AIP of ACs. IHCA depicted the revitalized percent relative expression of Nrf-2 and TRX in groups treated with ACs. Behavioral analysis revealed that ACs-treated groups significantly (p<0.05) attenuated the memory deficit, anxiety, and depressive-like behavior. Moreover, histopathological, hematological, serological, and endogenous antioxidant profiles indicated substantial AIP of ACs. Findings of comet assay further bolstered the compelling evidence as DNA damage was significantly (p<0.05) curbed down after ACs (100 mg/kg) treatment. All these outcomes implied that ACs exhibited AIP in a dose-dependent manner with maximal AIP imparted by artemisinin (100 mg/kg). This pre-clinical investigation avers the tremendous AIP of ACs targeting key molecular pathways. The current study divulges artemisinin as the most potent antiinflammatory agent among the tested compounds. [ABSTRACT FROM AUTHOR]

Combretum nigricans is a known medicinal plant employed in Nigerian ethnomedicine for the treatment of pain, inflammation and other ailments. This study aims at evaluating the antioxidant, antinociceptive and anti-inflammatory effects of C. nigricans ethanolic leaf extract. The antioxidant activity of C. nigricans ethanolic leaf extract was evaluated in vitro using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) model, while acetic acid writhing test and formalin nociception test were used in evaluating the antinociceptive activity in mice. Formalin-induced inflammation was used to evaluate the anti-inflammatory effect in mice. HPLC analysis of the extract showed the presence of several compounds including ferulic acid. The extract exhibited good DPPH antioxidant activity. Its IC50 value was 0.0003971 mg/mL. Oral acute toxicity test showed the LD50 is greater than 2000 mg/kg. In the acetic acid test, all extract test doses (200 – 800 mg/kg) had significant inhibitory effect against abdominal writhes usually evoked by acetic acid. The different extract doses had antinociceptive effect against phases 1 and 2 pain. Also, the extract doses used for the study (200 – 800 mg/kg) had anti-allodynia effect with the 800 mg/kg dose having a better effect of 44.44 and 79.83 % on days 1 and 2 respectively. Furthermore, the extract demonstrated significant anti-inflammatory activity against formalin induced inflammation in the experimental animals. The study outcome shows that C. nigricans extract has good antioxidant, anti-nociceptive and anti-inflammatory effects. [ABSTRACT FROM AUTHOR]

Artemisinin, artemether, artesunate, and dihydroartemisinin are renowned for their antimalarial potential. The current study aims to repurpose the above-mentioned artemisinic compounds (ACs) by conducting an intercomparison to evaluate their antiinflammatory potential (AIP). In order to develop potential candidates for the evaluation of AIP of ACs (50 and 100 mg/kg BW), carbon tetrachloride (1ml/kg body weight (BW)) was administered intraperitoneally to BALB/c mice. Alterations in animal behavior were assessed weekly through tail suspension test, force swim test, open field test, Y-maze test, inverted screen analysis, and weight lifting test. Aberrations in hematological, serological, endogenous antioxidants, and oxidative stress marker profiles were assessed in all twelve groups. Histological alterations were read using hematoxylin and eosin staining. Levels of inflammatory markers including nuclear factor kappa B (NF-κB), tumor necrosis factor alpha (TNF-α), and nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3), were determined using immunohistochemical analysis (IHCA). Antioxidant markers i.e., nuclear factor erythroid-2-related factor (Nrf-2) and thioredoxin (TRX) were also quantified through IHCA. Comet assay was performed to quantify DNA damage. Oral administration of ACs to mice significantly alleviated the carbon tetrachloride induced inflammation in comparison with silymarin. Reduced levels of several inflammatory markers including nitric oxide, thiobarbituric acid reactive substances, interleukin-1 beta, NF-κB, TNF-α, and NLRP3, underscore the substantial AIP of ACs. IHCA depicted the revitalized percent relative expression of Nrf-2 and TRX in groups treated with ACs. Behavioral analysis revealed that ACs-treated groups significantly (p

Colometric assays were used to quantify the secondary metabolites obtained by a decoction of the extract of Anabasis articulata (DEAA) flowers and leaves. Antioxidant activity was examined using several methods: total antioxidant capacity, the 2,2-diphenyl-1-picrylhydrazy (DPPH) radical scavenging assay, and the β-carotene bleaching assay. Single oral doses of 2000 and 5000 mg/kg body weight were administered to albino mice to assess acute toxicity. In vitro antiinflammatory activity was determined using the egg albumin denaturation test, and the in vivo inflammatory effect was assessed utilizing carrageenan, croton oil, and xylene-induced edema tests. Results showed that DEAA contained high amounts of polyphenols, flavonoids, and tannins and exhibited antioxidant activity in all tested assays. DEAA inhibited protein denaturation and did not cause any mortality or adverse effects. Oral administration of 200 mg/kg DEAA significantly reduced the edema induced by carrageenan, croton oil, and xylene. This study highlights the use of Anabasis articulata (Forssk.) Moq. in traditional herbal medicine. It possesses antioxidant activity and can be considered safe for oral consumption; it also has potential beneficial effects in treating diseases associated with inflammation and pain.

The objective of the present study was to develop film forming polymeric solution for the topical release of diclofenac sodium through the skin. A film forming polymeric solution of diclofenac sodium was prepared by using hydroxypropyl methylcellulose E5, hydroxypropyl methylcellulose E15 and hydroxypropyl methylcellulose E50 as a film forming polymer in different concentrations and dibutyl phthalate used as plasticizer. The prepared solution was tested for pH, viscosity, drying time, outward stickiness, thickness, weight uniformity, folding endurance, drug content uniformity followed by in vitro diffusion study. All the formulations showed the results within acceptable range for various tests. Formulations exhibited pH within the range of 5.7 to 6.1. Drying time of all the formulation ranged between 12±0.6 to 21±0.6 min. It was observed that formulation F1-F4 showed low outward stickiness, F5 and F6 showed medium, F7 to F9 showed high outward stickiness. The weight, thickness and folding endurance of the films were found to be consistent. Percentage cumulative drug release was found to be in the range of 72.05±0.4 to 93.35±13. Formulation F3 showed shortest drying time of 12 min, low outward stickiness, controlled drug release 88.14±2.46 % up to 6 h compared to the other formulations. Hence it was selected has optimized formulation. Kinetics study revealed that drug release from the polymeric solution followed non-Fickian. It can be concluded that topical film forming solution of diclofenac sodium formulated with hydroxypropyl methylcellulose E5, hydroxypropyl methylcellulose E15 and hydroxypropyl methylcellulose E50 as a film forming polymers, appears to be a promising option for the treatment of pain and inflammation. [ABSTRACT FROM AUTHOR]

Dalia A Gaber,1 Amal M Alsubaiyel,1 Alanoud K Alabdulrahim,2 Hanan Z Alharbi,2 Rama M Aldubaikhy,2 Rawan S Alharbi,2 Wades K Albishr,2 Heba A Mohamed3 1Department of Pharmaceutics, College of Pharmacy, Qassim University, Buraidah, 52571, Saudi Arabia; 2College of Pharmacy, Qassim University, Buraidah, 52571, Saudi Arabia; 3Department of Organic Chemistry, National Research Center, Giza, EgyptCorrespondence: Dalia A Gaber, Email dr_daliaahmed@hotmail.comIntroduction: Arthritic disorder is a common disease in elderly patients and the most common cause of joint dysfunction. This study aims to design Piroxicam-loaded nanoemulsion (PXM-NE) formulations to enhance the analgesic and anti-inflammatory activity of the drug for topical use.Methods: The nanoemulsion preparations were designed based on a high-pressure homogenization technique and were characterized for particle size (PS), poly dispersity index (Pi), zeta potential (ZP), drug content, and the selected formula was investigated for its topical analgesic activity and pharmacokinetic parameters.Results: The characterizations showed that the PS was 310.20± 19.84 nm, Pi was 0.15± 0.02, and ZP was − 15.74± 1.6 mV for the selected formula. A morphology study showed that the PXM-NE droplets were spherical with a uniform size distribution. The in vitro release study showed a biphasic release pattern with a rapid release within the first 2 hours followed by a sustained release pattern. The analgesic activity for optimal formula was 1.66 times higher than the commercial gel with a double duration of analgesic activity. The Cmax was 45.73± 9.95 and 28.48± 6.44 ng/mL for the gel form of the selected formula and the commercial gel respectively. The relevant bioavailability of the selected formula was 2.41 higher than the commercial gel.Conclusion: The results showed good physicochemical properties, higher bioavailability, and a longer analgesic effect of PXM from nanoemulsion gel, as compared to the commercial product.Keywords: analgesics, in vivo study, nanocarrier, drug efficacy, anti-inflammatory activity

Organic compounds possessing a comparatively greater number of nitrogens, fascinating attention in the upcoming field of medicine and its research. Synthesizing new drugs with a greater number of nitrogen atoms in their structure skeleton place challenges. Unique feature say lipophilicity carried by Mannich bases and their bivalent metal coordination complexes claim themselves to be potential sources [1-3]. Heterocyclic organic compounds rooted through amines and amides possess enhanced absorption through bio-membranes because of its lipohilicity which results in boundless pharmaceutical applications [4-11]. They considerably shorten the duration of therapy too. Mannich base and its coordination complexes with a range of first transition bivalent metals, such as, Co2+' Mn2+, Ni2+, Cu2+ and Zn2+ are reported along with DPPH free radical scavenging activity and anti-inflammatory activity. The scheme sequenced with 2-acetylthiophene, morpholine and phenyl urea was not yet described, the new Mannich base, l-(l-morpholino-l-(thiophen-2-yl) ethyl)-3-phenylurea (L), was synthesized. The compound and all the complexes were characterized. [ABSTRACT FROM AUTHOR]

As our previous study revealed that N-benzyl-N-methyldecan-1-amine (BMDA), a new molecule originated from Allium sativum, exhibits anti-neoplastic activities, we herein explored other functions of the compound and its derivative [decyl-(4-methoxy-benzyl)-methyl-amine; DMMA] including anti-inflammatory and antioxidative activities. Pretreatment of THP-1 cells with BMDA or DMMA inhibited tumor necrosis factor (TNF)-α and interleukin (IL)-1β production, and blocked c-jun terminal kinase (JNK), p38 mitogen-activated protein kinase (MAPK), MAPKAP kinase (MK)2 and NF-κB inflammatory signaling during LPS stimulation. Rectal treatment with BMDA or DMMA reduced the severity of colitis in 2,4-dinitrobenzenesulfonic acid (DNBS)-treated rat. Consistently, administration of the compounds decreased myeloperoxidase (MPO) activity (representing neutrophil infiltration in colonic mucosa), production of inflammatory mediators such as cytokine-induced neutrophil chemoattractant (CINC)-3 and TNF-α, and activation of JNK and p38 MAPK in the colon tissues. In addition, oral administration of these compounds ameliorated collagen-induce drheumatoid arthritis (RA) in mice. The treatment diminished the levels of inflammatory cytokine transcripts, and protected connective tissues through the expression of anti-oxidation proteins such as nuclear factor erythroid-related factor (Nrf)2 and heme oxygenase (HO)1. Additionally, aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels did not differ between the BMDA-r DMMA-treated and control animals, indicating that the compounds do not possess liver toxicity. Taken together, these findings propose that BMDA and DMMA could be used as new drugs for curing inflammatory bowel disease (IBD) and RA. [ABSTRACT FROM AUTHOR]

In the present study, a series of 5'-(substituted aryl)-2-furanyl}-3,4-dihydro-7/-/-pyrimidine-2-ones has been designed and synthesized with Beginelli reaction derivatives carried out from the reaction of ethyl acetoacetate 1 with substituted ureas 2 and substituted aryl furfuraldehydes 3 in presence of acetic acid to yield {5'-(substituted aryl)- 2-furanyl}-3,4-dihydro-7H-pyrimidine-2-ones [4a-k (X=O), 4l-v (X=S)]. The target candidates were confirmed by FTIR, NMR, Mass spectrometry and by elemental analysis. The present exploration also required for in vitro antibacterial activity against Gram-positive strains of bacteria, namely Bacillus cereus (ATCC 11778), Staphylococcus aureus (ATCC 11633), Staphylococcus epidermidis (ATCC 155), Enterococccus faecalis (ATCC 14506) and Gram negative bacterial strains, namely Shigella dysenteriae (ATCC 13313), Escherichia coli (ATCC11303), Klebsiella pneumoniae (ATCC 10031) and Salmonella typhi (MTCC 733). Tested antimicrobial activity revealed that compounds 4k and 4v showed very promising antibacterial activity and were found to be most effective when tested against strains of K. pneumonia, S. aureus, S. typhi, S. epidermidis and E. faecalis, although rest synthesized derivatives also showed significant antibacterial activity. The novel synthesized compounds also exerted remarkable in vitro anti-inflammatory biological activity as reflected by utilization of the percent inhibition of protein denaturation method. [ABSTRACT FROM AUTHOR]

Bufadienolide, an essential member of the C-24 steroid family, is characterized by an a-pyrone positioned at C-17. As the predominantly active constituent in traditional Chinese medicine of Chansu, bufadienolide has been prescribed in the treatment of numerous ailments. It is a specifically potent inhibitor of Na+/K+ ATPase with excellent anti-inflammatory activity. However, the severe side effects triggered by unbiased inhibition of the whole-body cells distributed a1-subtype of Na+/K+ ATPase, restrict its future applicability. Thus, researchers have paved the road for the structural alteration of desirable bufadienolide derivatives with minimal adverse effects via biotransformation. In this review, we give priority to the present evidence for structural diversity, MS fragmentation principles, anti-inflammatory efficacy, and structure modification of bufadienolides derived from toads to offer a scientific foundation for future in-depth investigations and views. [ABSTRACT FROM AUTHOR]

This work deals with the biological activity of the essential oils of an Algerian plant (Cotula cinerea) which belongs to the Asteraceae family. The study was carried out in the south-west of Algeria. We chose essential oils which are natural substances thanks to their numerous anti-infectious, antioxidant and antibacterial properties, etc. The objective of this work is to study the acute toxicity as well as the evaluation of the anti-inflammatory properties of the essential oils of both organs (leaves and flowers) of Cotula cinerea. As methodological approaches, we used the hydrodistillation technique to obtain the essential oils from leaves and flowers. Thus, the acute toxicity was determined by Lorke's method and the anti-inflammatory activity was evaluated by measuring the plantar oedema of mice induced by carrageenan. The results show that the essential oil extracts of the leaves and flowers are low toxic substances with LD50s of 1131.37 mg/kg and 1264.91 mg/kg respectively. They also show a considerable anti- inflammatory effect at doses not exceeding 300 mg/kg with maximum percentages of 86.16% for leaves and 80.87% for flowers. These results show the efficacy of the essential oils of this plant and their therapeutic richness which can be used in traditional medicine for anti-inflammatory treatment. This study has provided additional knowledge on the biological activity of Cotula cinerea essential oils and has opened perspectives for the research of the active principles contained in this species as well as the application of biotechnology to know the molecular mechanism and valorise this natural wealth. [ABSTRACT FROM AUTHOR]

Background: Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs in the world. The widespread use of NSAIDs is associated with a number of serious side effects and complications observed for both selective and non-selective COX inhibitors. Therefore, the search for new COX inhibitors, which along with their effectiveness will have minimal side effects, is a very important and urgent task. Methods: This work studied the synthesis of new 1,4,5,6-tetrahydropyrimidine-2-carboxamides based on the reaction of 2-morpholin-4-yl-N-(het)aryl-2-thioxoacetamides with 1,3-diaminopropane. All obtained compounds were tested for anti-inflammatory activity in vitro and in silico conditions. All synthesized 1,4,5,6-tetrahydropyrimidine-2-carboxamides were tested for influence on the course of the exudative phase of the inflammatory process based on the carrageenan model of paw edema of laboratory nonlinear heterosexual white rats weighing 220-250 g, using Diclofenac as a reference. Optimization of the geometry of the studied structures and molecular docking was carried out using the ArgusLab 4.0.1 software package. Results: The target products were obtained with yields of 71-98% and easily isolated from the reaction mixture. The best anti-inflammatory activity was found in N-(4-chlorophenyl)-1,4,5,6-tetrahydropyrimidine-2-carboxamide and in N-[4-chloro-3-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydropyrimidine-2-carboxamide, suppression of the inflammatory response was 46.7 and 46.4%, respectively. The results of molecular docking with COX-1 and COX-2 enzymes were in good agreement with the experimental data, R2 ˃ 0.92 and R2 ˃ 0.83, respectively. Conclusion: The compounds under study were shown to be promising as potential anti-inflammatory agents.

It is well known that G protein–coupled receptors (GPCRs) assume multiple active states. Orthosteric ligands and/or allosteric modulators can preferentially stabilize specific conformations, giving rise to pathway-biased signaling. One of the most promising strategies to expand the repertoire of signaling-selective GPCR activators consists of dualsteric agents, which are hybrid compounds consisting of orthosteric and allosteric pharmacophoric units. This approach proved to be very promising showing several advantages over monovalent targeting strategies, including an increased affinity or selectivity, a bias in signaling pathway activation, reduced off-target activity and therapeutic resistance. Our study focused on the cannabinoid receptor type 2 (CB2R), considered a clinically promising target for the control of brain damage in neurodegenerative disorders. Indeed, CB2R was found highly expressed in microglial cells, astrocytes, and even in some neuron subpopulations. Here, we describe the design, synthesis, and biological evaluation of two new classes of potential dualsteric (bitopic) CB2R ligands. The new compounds were obtained by connecting, through different linkers, the pharmacophoric portion of the CB2R positive allosteric modulator (PAM), EC21a, with that of the CB2R selective orthosteric agonist LV62, both developed in our laboratories. A preliminary screening enabled us to identify compound JR64a as the most promising of the series. Indeed, functional examination highlighted a signaling ‘bias’ in favor of G protein activation over βarrestin2 recruitment, combined with high affinity for CB2R and the ability to efficiently prevent inflammation in human microglial cells (HMC3) exposed to LPS/TNFα stimulation, thus demonstrating great promise for the treatment of neurodegenerative diseases.

The essential oil obtained by hydrodistillation from the aerial part of Ammi visnaga L., harvested in the northwest of Algeria was analyzed and its antimicrobial and anti-inflammatory activities were studied. 26 compounds were identified by GC-FID and GC-MS representing 95.1% of the total oil. The major components found were limonene (27.8%), p-cymene (19.9%), carvacrol (18.7%), thymol (14.2%) and gamma-terpinene (10%). The EO was slightly toxic with an LD50 of 500 mg/kg. The antimicrobial activity showed that all strains tasted were sensitive to the EO, with diameter halos ranging from 17.73 to 36.1 mm in the disc diffusion method, the results of MIC and MBC-MFC showed that the activity was microbicidal against all the tasted strains. Concerning the anti-inflammatory activity, Ammi visnaga EO reduced the carrageenan induced paw edema in rats by 56.35% after 6 hours. [ABSTRACT FROM AUTHOR]

Terpenes are one of the most abundant classes of secondary metabolites produced by plants and can be divided based on the number of isoprene units (C5) in monoterpenes (2 units—C10), sesquiterpenes (3 units—C15), diterpenes (4 units—C20), triterpenes (6 units—C30), etc. Chemically, triterpenes are classified based on their structural skeleton including lanostanes, euphanes, cycloartanes, ursanes, oleananes, lupanes, tirucallanes, cucurbitanes, dammaranes, baccharanes, friedelanes, hopanes, serratanes etc. Additionally, glycosylated (saponins) or highly oxidated/degraded (limonoids) triterpenes could be found in nature. The antiinflammatory effect and action as immunomodulators of these secondary metabolites have been demonstrated in different studies. This review reports an overview of articles published in the last 15 years (from 2006 to 2021 using PubMed and SciFinder database) describing the antiinflammatory effects of different triterpenes with their presumed mechanism of action, suggesting that triterpenes could be appointed as natural products with future pharmaceutical applicability. [ABSTRACT FROM AUTHOR]

Myrtus communis L is one of the medicinal plant being used in Ethno pharmacological domain in Algeria and many other parts of the world. The present study deals with the evaluation of the in vitro antioxidant and antiinflammatory activities of leaf extract of M. communis L by using free radical scavenging assay DPPH, Ferric Reducing Antioxidant Potential FRAP, ß-Carotene bleaching, and denaturation test of the (BSA) protein. The chemicals compositions were carried out by Gas chromatography-mass spectrometry (GC/MS). The major constituents of essentials oil were DLimonene (30.45%), a-Pinene (22.11%), 2,6-Octadien-1-ol, 3.7-dimethyl-, acetate (6.29%) respectively. The result showed that the highest antioxidant capacity was exhibited with IC50 = 45.76 µg/ml. A stronger ß carotene bleaching inhibition capacity is observed. The EO exhibited also remarkable activity to reduce iron (Fe), reflected by the optical densities (0,930) obtained at concentration (60 µg/ml). Leaf extracts of myrtle revealed significant anti-inflammatory activity. The results showed that the percentage inhibition of BSA denaturation (0.2%) is proportional to the different concentrations of the EO, where the highest value was recorded at the 200 µg/ml, resulted at approximately (64.08%). The Biological activities of this medicinal plant found so far may direct its use towards as prebiotic in food formulation, additives foods and eth-nopharmacological domain in the long run. [ABSTRACT FROM AUTHOR]

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The strategy of rational approaches to the search for selective COX-2 inhibitors as potential antiinflammatory agents has been proposed and elaborated. It is based on the use of PASS-prediction and molecular docking. The choice of the basic structure of 4-amino-3-thio-1,2,4-triazole as a promising object of chemical modification has been substantiated. Using a modification of the primary molecule, a virtual library of S-derivatives of 5-substituted 4-amino(pyrrol)3-thio-4H-1,2,4-triazoles in the amount of 100 compounds (ten groups) has been obtained by introducing various pharmacophore fragments. Based on the analysis of the results of the PASS-prediction and molecular docking, six of the ten planned groups of compounds have been selected for the synthesis as promising selective COX-2 inhibitors. The reliability of the prediction results has already been confirmed for one of the promising group 4-amino-5-(pyridine-4-yl)-1,2,4-triazole (4Н)-3-yl-thioacetamides.

Artemisinin, artemether, artesunate, and dihydroartemisinin are renowned for their antimalarial potential. The current study aims to repurpose the above-mentioned artemisinic compounds (ACs) by conducting an intercomparison to evaluate their antiinflammatory potential (AIP). In order to develop potential candidates for the evaluation of AIP of ACs (50 and 100 mg/kg BW), carbon tetrachloride (1ml/kg body weight (BW)) was administered intraperitoneally to BALB/c mice. Alterations in animal behavior were assessed weekly through tail suspension test, force swim test, open field test, Y-maze test, inverted screen analysis, and weight lifting test. Aberrations in hematological, serological, endogenous antioxidants, and oxidative stress marker profiles were assessed in all twelve groups. Histological alterations were read using hematoxylin and eosin staining. Levels of inflammatory markers including nuclear factor kappa B (NF-κB), tumor necrosis factor alpha (TNF-α), and nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3), were determined using immunohistochemical analysis (IHCA). Antioxidant markers i.e., nuclear factor erythroid-2-related factor (Nrf-2) and thioredoxin (TRX) were also quantified through IHCA. Comet assay was performed to quantify DNA damage. Oral administration of ACs to mice significantly alleviated the carbon tetrachloride induced inflammation in comparison with silymarin. Reduced levels of several inflammatory markers including nitric oxide, thiobarbituric acid reactive substances, interleukin-1 beta, NF-κB, TNF-α, and NLRP3, underscore the substantial AIP of ACs. IHCA depicted the revitalized percent relative expression of Nrf-2 and TRX in groups treated with ACs. Behavioral analysis revealed that ACs-treated groups significantly (p<0.05) attenuated the memory deficit, anxiety, and depressive-like behavior. Moreover, histopathological, hematological, serological, and endogenous antioxidant profiles indicated substantial AIP of ACs. Findings of comet assay further bolstered the compelling evidence as DNA damage was significantly (p<0.05) curbed down after ACs (100 mg/kg) treatment. All these outcomes implied that ACs exhibited AIP in a dose-dependent manner with maximal AIP imparted by artemisinin (100 mg/kg). This pre-clinical investigation avers the tremendous AIP of ACs targeting key molecular pathways. The current study divulges artemisinin as the most potent antiinflammatory agent among the tested compounds., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2024 Kazmi, Fatima, Naz, Kanwal and Haq.)

This paper includes the result of the first study of the chemical composition, antioxidant, antiinflammatory, and antidiabetic activities of the essential oils of Glebionis coronaria (L.) Cass. ex Spach and Glebionis segetum (L.) Fourr. from Turkey. In the current study, nine and twenty-eight constituents were determined in the essential oils of aerial parts of G. coronaria (GCE) (92.1%) and G. segetum (GSE) (90.0%), respectively. The main components were capillin (65.9%) in GCE, capillene (53.4%) in GSE. The essential oil compositions were evaluated and compared with previous researches. In the current study, the plants are classified as chemotypes of Glebionis species. GCE and GSE showed poor and very poor DPPH radical scavenging activity, respectively. GCE and GSE exhibited significant and strong antiinflammatory activity against the 5-lipoxygenase enzyme, respectively. Also, GCE and GSE displayed moderate and weak antidiabetic activity against the α-glucosidase enzyme, respectively. Polyacetylenes were determined as the main class of compounds in GCE and GSE and had a notable antiinflammatory activity. [ABSTRACT FROM AUTHOR]

Rhamnus prinoides L'Herit belongs to Rhamnaceae family widely distributed in India, Eastern, Central and Southern Africa. In Ethiopia it is commonly known as Gesho (Amharic, Tigrigna and Afan Oromo), Gishe (Guragegna) and Geshu (Agewgna). Decoction of the leaves is recommended as remedy for treatment of variety of diseases such as back pain, malaria, pneumonia, sexually transmitted disease, skin infections, wounds, blood purifiers, water borne diseases and as ethnoveterinary medicine. Various secondary metabolites such as flavonoids, alkaloids, tannins, terpenoids, saponins, steroids and anthraquinones have been reported from the genus of which polyphenols were abundant with tremedousantioxidant, wound healing and antiinflammatory activities. The plant also serve as hopping agent, making traditional alcoholic beverages like tella and tej (in Ethiopia), animal feed, medicine, nectar for bees, soil conservation, ornamental, shade and dyes in textiles. This review presents chemical profile as well as biological activities of the species which confirmed that the plant is a good source natural polyphenols and provided valuable information in support of its use as an alternative medicine for future healthcare practice. [ABSTRACT FROM AUTHOR]

In China, the fruits of Physalis alkekengi L. var. franchetii, which are conventionally utilized as edible berry, have attracted wide attention due to its significant biological activities. In the present study, phytochemical studies on the fruits of Physalis plants afforded six compounds, including two new withanolides (1–2) and four known agnologues (3–6). The inhibitory effects of these compounds on the formation of nitric oxide (NO) stimulated by lipopolysaccharide (LPS) in RAW264.7 macrophages were evaluated. Physapubescin M (1), with IC50 value of 1.58 μM, was selected for further study. The protein expression of COX‐2 and iNOS, and LPS‐induced production of cytokines (IL‐6, IL‐1β and TNF‐α) were reduced by physapubescin M (1) in a dose‐dependent way. In addition, transcriptomic analyses were conducted to profile gene expression alterations in LPS‐induced RAW264.7 cells upon treatment of physapubescin M (1) and the potential antiinflammatory mechanism of withnolides was mentioned. These results provide broad view to the underlying antiinflammatory mechanism of withnolides, and give a theoretical basis for the utilization of the fruits of P. alkekengi L. var. franchetii. [ABSTRACT FROM AUTHOR]

Olea europaea is a medicinal plant widely used in traditional medicine in Algeria. In this study, the antiinflammatory, analgesic and cytotoxic activities of the methanolic extract of Olea auropaea leaves were evaluated. Similarly, a phytochemical study was conducted to identify the different families of chemical compounds contained in these extract. The obtained results showed that the qualitative analysis of extract by HPLC, allowed highlighting majority compounds and minority compounds. The quantitative estimation of total polyphenols and flavonoids showed their existence in this extract, with a rate of 115.35 ± 2.24 mg EAG/g extract and 7.19 ± 0.19 mg EQ/g extract, respectively. The antiinflammatory activity in vivo of methanolic extract of Olea europaea was evaluated by induction of paw and ear edema in mice using the carrageenan and croton oil respectively. The obtained results indicated that all samples exerted an inhibition, more or less effective, of the edema compared to the control. Thus, the oral administration of 400 mg/kg of methanolic extract of Olea europaea to mice induced a strong inhibition of paw edema with a percentage of 96%. This antiinflammatory activity was confirmed topically by ear edema test. Similarly, the obtained results indicated also that the methanolic extract (600 mg/kg) of Olea europaea inhibited the pain caused by acetic acid in mice with a percentage of 77.49%. Finally, the cytotoxicity test against Artemia salina larvae "Brine shrimp test" showed that the methanolic extract of leaves showed no cytotoxicity against these larvae with DL50 value of 9,800 μg/ml. [ABSTRACT FROM AUTHOR]

Emulgels (emulsion gels) are a class of biphasic semi-solid formulations, having aqueous and non-aqueous phases, delivering both hydrophilic and lipophilic agents. The main advantage of an emulgel is that lipophilic drugs can be easily formulated as emulgels. Rutin trihydrate is an herbal drug used for topical treatment of inflammation. However, its poor water solubility (0.125 mg/ml) presents a hindrance for its local bioavailability and limits effective anti-inflammatory activity. The aim of the current study was to formulate and optimize rutin trihydrate emulgel to enhance its efficacy and stability. 28 formulations were developed with various types of gelling agents like Carbapol 934 (0.8 and 1% w/v), Xanthum gum (1.5 and 2% w/v), HPMCk15 (2, 2.5 and 3% w/v), HPMC K100 (2, 2.5% w/v), guar gum (1, 1.5 and 2% w/v), badam gum (1% w/v) and using various permeation enhancers like clove oil, eucalyptus oil and oil of orange (10 and12.5% v/v). The optimised formulation (f8) was yellow in colour, homogeneous with good consistency, possessed pH of 6.51±0.04 that is very close to that of normal skin (6-7), drug content of 98.7%, viscosity of 14,680cps at 30rpm, spreadability 13.5gm.cm/sec and extrudability 36.2% and in vitro drug release of 79.3% for 7 hrs, ex vivo drug release of 70.08% was stable for 3 months and was having comparable anti inflammatory activity with that of marketed formulation. [ABSTRACT FROM AUTHOR]

Introduction: Coriolopsis spp. are broadly used as traditional medicines in India, China, and Japan as antioxidant, antitumor, antiviral, antimicrobial, and immunomodulatory agents to treat many diseases. However, the bioactivities of yunzhi mushroom (Coriolopsis aspera) crude extract have not been studied yet. Materials & Methods: The aims of this study are the determination of chemical composition and antioxidant, anticancer, and anti-inflammatory effects of yunzhi mushroom (Coriolopsis aspera) extract in Vietnam. The chemical constituents of yunzhi mushroom extract were determined via MS, IR, and NMR spectrum analysis, and the antioxidant activity of the extract was evaluated by 1,1-diphenyl-2picryl-hydrazil (DPPH) radical scavenging assay. The anticancer activity of yunzhi mushroom against HeLa and HepG2 cancer cell lines was tested via the MTT assay. The anti-inflammatory effect of the extract was determined through the quantification of nitrite oxide production using the Griess reaction. Results & Discussion: We identified the presence of 9 bioactive compounds in CoAE extract, including trametenolic B, cerevisterol, ergosterol, ergosterol peroxide, trans-p-hydroxy coumaric acid, methyl ferulate, methyl (2-hydroxyphenyl) acetate, umbelliferone, and 8-hydroxy-3,4-dimethyl isocoumarin. Moreover, CoAE extract exhibited stronger antioxidant activity than another crude extract. Of note, anticancer and anti-inflammatory effects of CoAC were also higher than those of another crude extract. The data indicate yunzhi mushroom as potential functional food for treating inflammatory and cancer-related diseases. Conclusion: The data suggest Coriolopsis aspera as one of the promising functional foods for the treatment of inflammatory and cancer-related diseases. [ABSTRACT FROM AUTHOR]

Sesamum indicum is one of the most important ancient oil crops in the world. In fact, this plant, in particular its seeds, is used for food, medicinal and industrial purposes. This article provides an evaluation of the biochemical composition, antioxidant and anti-inflammatory activities of dehulled sesame seeds Sesamum indicum and its coat fraction. Results analysis of our investigation showed that the level of total fatty oil, total protein and total sugars were present with 47.27%, 18.84% and 2.18% respectively. However; these compounds were significantly decreased in the coat fraction. On the contrary, the mineral content can be five times higher in the coat fraction, especially for calcium with a value of 831.11mg/100g, compared to dehulled seeds. Quantity of total phenolic and flavonoids were highest in the hydro-methanolic extract of seeds coat with 3.05±0.08mg GAE/g and 0.99±0.02 mg QE/g respectively. The same extract exhibited antinflammatory activity and antioxidant power, demonstrated by significantly decreasing in inflammation induced by carrageen in rats (85.56%), significant antioxidant activity (DPPH) (IC50: 2.12 mg/ml) and highest total antioxidant activity (95.5Îg/ml). This study suggests that seeds coat of sesamum indicum contain interesting phytochemical potential and significant biological activities. [ABSTRACT FROM AUTHOR]

Introduction: Black shallot is the novel product of shallot (Allium ascalonicum), one of the most famous spices and remedies used in Vietnamese cuisine and in folk medicine, via aging process in a controlled temperature and humidity environment. However, the bioactivities of black shallot ethanol extract have not been studied yet. Materials & Methods: The aims of this study are determination of chemical composition and antioxidant, anticancer, anti-inflammatory effects of black shallot extract. The chemical constituents of black shallot extract were determined via ESIMS/MS analysis and the antioxidant activity of extract was evaluated by 1,1-diphenyl-2picrylhydrazil (DPPH) radical scavenging assay. The anticancer activity of black shallot against human cervical carcinoma (Hela) and human hepatocellular carcinoma (HepG2) cell lines was tested via the MTT assay. The anti-inflammatory effect of extract was measured through quantification of nitrite oxide production using the Griess reaction. Results & Discussion: We identified the presence of 7 bioactive compounds in black shallot extract, including quercetin 3,4-diglucoside, isorhamnetin 3,4-diglucoside, quercetin 3-glucoside, quercetin 4-glucoside, isorhamnetin 4-glucoside, quercetin aglycone, isrohamnetin. Moreover, black shallot extract exhibited the stronger antioxidant activity than fresh shallot extract (25.67 ± 0.65% versus 18.21 ± 0.35%, respectively). Of note, anticancer and anti-inflammatory effects of black shallot were also higher than those of fresh shallot. Conclusion: The data suggest black shallot as one of the promising functional foods for treatment of inflammatory and cancer related diseases. [ABSTRACT FROM AUTHOR]

The present study aims to investigate the antiinflammatory activity of the slime extracts from the giant African snail, Lissachatina fulica. In this study, aqueous and ethanol extracts of the snail slime were evaluated for antiinflammatory activities in vitro. The aqueous extract showed greater antiinflammatory activities than the ethanol extract. The aqueous extract was further tested for antiinflammatory activity in vivo. For acute inflammation, the ear oedema assay was used to screen the slime extract. The results revealed that application of 2 mg/ear extract or phenylbutzone could significantly reduce oedema when compared with ethanol-treated ears. For chronic inflammatory test, the cotton pellet granuloma model was employed to determine the activity of the slime extract. It was found that 2.5 and 6.25 % extract could significantly reduce transudative and granuloma weights. Moreover, the extracts also reduced malondialdehyde and increased superoxide dismutase in the granuloma tissue of the induced rats. In conclusion, the slime extract showed antiinflammatory activity both in vitro and in vivo. The antiinflammatory activity was also observed against acute and chronic inflammations, which suggested that the slime extracts has the potential to be developed into antiinflammatory products. [ABSTRACT FROM AUTHOR]

Present investigation evaluated the impact of poly-herbal formulations comprising extracts of Zingiberofficinale, Curcuma longa, Aloe barbadensis, Citrus aurantium, Emblica officinalis and castor oil on wound healing activity using excision wound model and antiinflammatory activity using formalin-induced pawedema method. Ointments containing 2, 4 and 6 % w/w of extracts were made and used in wound healing action and all the formulations significantly (p<0.01) reduced the wound area. Ointment of 6 % w/w has shown better results than 2 and 4 % w/w. These results were compared to that of the standard framycetin. Poly-herbal formulation-1, poly-herbal formulation-2 and poly-herbal formulation-3 were prepared and used at doses of 100, 300 and 500 mg/kg to determine antiinflammatory activity. All poly-herbal formulations significantly (p<0.01) inhibited formalin-induced rat paw edema. Poly-herbal formulation-3 displayed greater inhibition than poly-herbal formulations 1 and 2. These results were comparable to that of the standard diclofenac. Present work and previous studies on poly-herbal formulations corroborates that these are safer and effective in treating inflammation and wounds. [ABSTRACT FROM AUTHOR]

Two new monoterpene glucosides: xanmonoter A (1) and xanmonoter B (2) were isolated from Xanthium strumarium. Their structures were elucidated on the basis of 1D and 2D NMR, MS and CD analysis. Compounds 1 and 2 were tested for their anti-inflammatory activity with IC50 values of 17.4, 22.1 μM, respectively. [ABSTRACT FROM AUTHOR]

Alzheimer's disease (AD) is a complex, progressive and deadly disorder that exhibits various typical pathological characteristics. Till now no effective treatment has been found that can prevent or reverse AD. Here, the effects of 2 months of treatment with α-D-1,6-glucan (CPA) and selenium-containing α-D-1,6-glucan (Se-CPA) on early cognitive dysfunction and neuropathology were explored in the 3-month-old APP/PS1 transgenic mouse. The results of the Morris water maze and open-field test revealed that Se-CPA exerted more significant effects than CPA in improving cognitive function and depressive-like behavior by attenuating the oxidative stress, decreasing serum LPS level, downregulating the inflammation of astrocytes and microglia through inhibiting the activation of NLRP3 inflammasome, mitigating neuronal cells loss and improving synaptic plasticity. Moreover, Se-CPA exerted beneficial effects on reshaping gut microbiome by increasing the microbial α-diversity, enhancing the proportion of beneficial bacteria such as Akkermansia muciniphila and promoting the SCFAs concentration. These findings provide evidence that Se-CPA might be a potentially viable compound for AD prevention. [ABSTRACT FROM AUTHOR]

Abstract Background: The rhizome of Iris songarica Scherenk has been prescribed as anodyne in Persian traditional medicine system. However, its effects have never been investigated experimentally. Thus, the present study was designed to evaluate the antinociceptive and anti-inflammatory effects of alcoholic extract of Iris songarica Scherenk rhizome in mice. Material and Methods: In this experimental study, adult male balb/c mice were used. 40 animals were allocated into five equal groups (control, morphine 5mg/kg, the extracts at doses of 100, 200 and 300 mg.kg) and tested for antinociceptive evaluation via using hot-plate in 30,60 and 120 minutes after the investigations. Also, the other 36 mice were divided into six equal groups (no-inflammation control, inflammation model, dexamethasone 4 mg/kg and the extracts at doses of 100, 200 and 300 mg.kg) and evaluated for anti-inflammatory activity in xylene induced inflammation model. All the investigations were done via intraperitoneal injection. Data were analyzed using one-way ANOVA or Kruskal-Wallis tests in SPSS. Results: Compared to the control group, the extract at the all doses could increase latency time in hot plate test at 30, 60 and 120 minutes after investigation (p

Objective: Asthma is a multifaceted inflammatory disorder which results into narrowing of airway with broncho-constriction and spasm. As the complex pathophysilogy of asthma, various animal models are generally used to investigate the immunological and physiological pathogenesis of disease. Abrus precatorius Linn (Fabacease) is a climbing shrub. The leaves and roots are sweet in taste and traditionally used for the treatment of asthma, bronchititis, and inflammation. A. precatorius possesses different pharmacological activities. Hence the objective of this study was to evaluate antiasthmatic activity of ethanol extract of A. precatorius leaves using various models. Methods: In present study ethanol extract of A. precatorius leaves was evaluated for antiasthmatic activity using carrageenan induced paw edema in rats [100–150 mg/kg], histamine induced bronchospasm in guinea pig [200–400 mg/kg] and histamine induced contraction of goat tracheal chain [2.5–25 μg/ml]. Results: Result of study revealed that ethanol extract of A. precatorius significantly exhibited anti-inflammatory effects in rats, oral treatment of extract on guinea pig significantly increases histamine induced preconvulsive dysponea times and the ethanol extract of plant increases got tracheal chain precontracted with histamine. Conclusion: Hence present study concludes that ethanol extract of A. precatorius possesses antiasthmatic activity.

Biological activity of naphthoxazoles, fused hetero-benzoxazoles and benzobicyclo[3.2.1]-derivatives was investigated in proliferation and inflammation based assays. The tested compounds were prepared by photocylization or photocycloaddition reactions. Effect of compounds on proliferation of several cancer cell lines was determined by measuring cell metabolic activity through time. Lipopolysaccharide (LPS) stimulation of peripheral blood mononuclear cells (PBMC) was used to investigate antiinflammatory properties of the compounds. Several naphthoxazoles and fused hetero-benzoxazoles inhibited TNFa protein expression in LPS stimulated PBMC, indicating possible antiinflammatory role which would be interesting to further investigate. Physico-chemical properties of tested compounds have been also studied using chromatographic lipophilicity measure, chrom logD and logP was calculated as the importance of physico-chemical properties of compounds at early stage of discovery of new drugs is well established. The similarities in structure and activity of some representative compounds affirm the need to further address their antiinflammatory properties. [ABSTRACT FROM AUTHOR]

Purpose: To review the medicinal uses of Mahonia bealei, an important member of the genus Mahonia, with a focus on its various applications in Traditional Chinese Medicine, as well as published scientific evidence on its effectiveness. Methods: Information in all available literature was retrieved using different search engines including NCBI, ISI Web of Knowledge and Google. Results: Several compounds have been extracted from M. bealei. These include alkaloids, triterpenes, flavonoids, phytosterols and lignans. Traditionally, the plant is used to treat dysentery, diarrhea and inflammation. Globally, scientists have used in vitro and in vivo techniques to evaluate the usefulness of compounds extracted from M. bealei with respect to their antibacterial, anti-inflammatory, antitumor, antioxidant as well as anti-gastrin properties. Conclusion: Different parts of this plant still remain underexplored. Moreover, comparison of the properties of the isolated compounds has not been carried out, nor are there reports on the synergistic effects of extracts of the plant. Therefore, future research to address these areas may be useful in the discovery of new therapeutic agents. [ABSTRACT FROM AUTHOR]

Some 3-(4,6-dichloro-1,3,5-triazin-2-yl)-2-phenylthiazolidin-4-one derivatives were prepared by cyclocondensation reaction between 2-amino-4,6-dichloro-1,3,5-triazine, substituted aromatic aldehyde and ethyl-2-mercaptoacetate, with an yield in the range 76-86 %. Prepared compounds showed antiinflammatory activity. The halogenated electron-withdrawing groups on the phenyl ring of 4-thiazolinone generated antiinflammatory activity. Among the synthesized compounds, 3-(4,6-dichloro-1,3,5-triazin-2-yl)-2-(2,5-difluorophenyl)thiazolidin-4-one showed better antiinflammatory activity with 72 and 79 % inhibition for TNF-α and IL-6, respectively. Also, molecular docking and pharmacophore modelling performed for this active antiinflammatory compound highlighted that hydrophobicity as an important feature for activity optimization. [ABSTRACT FROM AUTHOR]

This study was designed to investigate the antioxidative and anti-inflammatory effects of the extract of Ribes mandshuricum (Maxim.) Kom. leaves. Seven major flavonoids (rutin, hyperoside, isoquercetin, trifolin, astragalin, quercetin and kaempferol) were successfully prepared from the Ribes mandshuricum leaves by MAEDES methods followed by X-5 macroporous resin. Then, the antioxidant activities of Ribes mandshuricum leaves flavonoids were evaluated by DPPH, ABTS and FRAP assays. We revealed that the Ribes mandshuricum leaves flavonoids had the antioxidant abilities. Finally, it was discovered that Ribes mandshuricum leaves flavonoids could effectively inhibit the NO production and increase the IL-10 cytokines production in LPS-induced RAW 264.7 cells. It suggested that the Ribes mandshuricum leaves flavonoids had the potential anti-inflammatory effects. Therefore, the major flavonoids of Ribes mandshuricum leaves have potential use as functional food or cosmetics to delay senescence, guard health and prevent chronic disease. [ABSTRACT FROM AUTHOR]

Abstract Acute Vibrio cholerae infection triggers significant inflammatory response and immense fluid secretion in the intestine. In the present study, methyl gallate (MG) isolated from Terminalia chebula was evaluated to determine the in vivo fluid accumulation-inhibitory, anticolonization and anti-inflammatory and in vitro biofilm-inhibitory activities against multi-drug resistant (MDR) V. cholerae. Bacterial membrane-damaging and biofilm-inhibitory activities were determined by membrane perturbation and transmission electron microscopy (TEM); and microdilution assays, respectively. Fluid accumulation-inhibitory and anticolonization activities of MG (23.80–95.23 mg/kg body weight) were determined in 4–5 days old BALB/c mice with an incubation time of 18 h. The effect of MG (1, 50 and 500 mg/kg body weight) on intestinal inflammatory reaction induced by V. cholerae was studied by performing histology in Swiss albino mice. MIC and MBC of MG against the test strains were 32–64 and 64–256 μg/ml, respectively. MG showed the fluid accumulation-inhibitory activity with inhibition values of 42.86–89.08% at doses between 23.80 and 95.23 mg/kg body weight and significant anticolonization activity (p < 0.0001) against V. choleare in the suckling mouse intestine. MG (500 mg/kg body weight) significantly inhibited the inflammatory reactions induced by V. cholerae compared to the vehicle control. MG exhibited 70% minimum biofilm inhibition concentration of 64 μg/ml and bacterial membrane damaging activity at 1 × MBC. The results obtained in the present study suggest that MG has potential as an effective agent for the treatment of severe secretory and inflammatory diarrheal disease caused by MDR V. cholerae. Graphical abstract Image 1 Highlights • V. cholerae triggers significant inflammatory response and immense fluid secretion. • Methyl gallate (MG) exhibited 70% minimum biofilm inhibition at MIC against V. cholerae. • MG showed significant in vivo fluid accumulation-inhibitory and anticolonization activities against V. choleare. • MG significantly inhibited the inflammatory reactions induced by V. cholerae. [ABSTRACT FROM AUTHOR]

A series of 2,4-disubstituted thiazole derivatives (6a-k) were synthesized by a condensation reaction between 2- amino, 4-substituted phenyl thiazole and 2-(2,3-dimethylanilino)benzoic acid. The structure of synthesized thiazole derivatives 6(a-k) were characterized by using IR, NMR, Mass Spectroscopy and evaluated for their in vitro antiinflammatory activity using albumin denaturation method and compared with standard drug diclofenac sodium. The compounds 2-(2,3-dimethyl phenylamino)-N-(4-(4-methyl phenyl) thiazol-2-yl)benzamide (6a) and 2-(2,3-dimethyl phenylamino)-N-(4-(4-nitrophenyl) thiazol-2-yl)benzamide (6c) showed better anti-inflammatory activity when compared with a standard drug. [ABSTRACT FROM AUTHOR]

The phytochemical study of leaves of Cavendishia compacta was carried out. The separation of extracts and fractions by column chromatography, thin layer and preparative thin layer allowed to obtain a mixture of diterpenes consisting of kaurane, rimunene and biformene; a mixture of aromatic compounds constituted by acetophenone and benzaldehyde; a mixture of triterpenes constituted by α -amirine and β-amirin and the isolation of morine and myricetin. The anti-inflammatory activity was evaluated to the ethanolic extract and fractions of hexane, dichloromethane and ethyl acetate using the model of atrial edema induced by TPA, being the ethanolic extract and the fraction of dicholoromethane those that presented a moderate anti-inflammatory effect of 49.3 % and 39.8% respectivel. [ABSTRACT FROM AUTHOR]

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Leaves of Exacum bicolor are traditionally used as a remedy for the treatment of inflammatory disorders in the form of a tonic by the tribal community of Western Ghats of Karnataka. The present study was designed to evaluate the antiinflammatory activity of the methanol extract of Exacum bicolor leaf using the carrageenan-induced mice paw oedema model. The methanol extract which was shown earlier to possess in vitro antiinflammatory activity was further screened for in vivo antiinflammatory activity at doses of 250 and 500 mg/kg. Diclofenac sodium 10 mg/kg was used as the reference standard. The plant extract showed significant dose-dependent reduction in paw oedema when compared to the control at all the time intervals, which was also comparable to that produced by diclofenac. Histopathological analysis revealed clear and distinguished cellular damage for all the groups. The results of the current study showed that the methanol extract of the leaf of Exacum bicolor possessed significant antiinflammatory potential, which provided supporting evidence to the folklore use of the plant leaves as an antiinflammatory drug. [ABSTRACT FROM AUTHOR]

Three new flavonoid glycosides, 2(S)-5-hydroxy-6,8-dimethoxyflavonone -7-O-β-D-glucopyranosyl-(1→6)-O-β-D-glucopyranoside (1), 5-hydroxy- 3,8-dimethoxyflavone-7-O-β-D-glucopyranosyl-(1→6)-O-β-Dglucopyranoside (2) and 3,7-dihydroxy-8-methoxyflavone-6-O-β-Dglucopyranosyl-( 1→6)-O-β-D-glucopyranoside (3), together with five known flavonoids (4'8) were isolated from the roots of Smilax glabra Roxb. Their structures were elucidated on the basis of chemical and spectral evidence, as well as by comparison with literature data. Three new flavonoids were subjected to evaluate anti-inflammatory activity. Compounds 1'3 inhibited the NF κB induction by 32.2, 55.8 and 61.7%, respectively. [ABSTRACT FROM AUTHOR]