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Inflammation assists in the healing process as a part of the natural defensive mechanism. Apart from the healing process, inflammatory mechanisms contribute to the progression and development of a range of ailments, including asthma, rheumatoid arthritis, cancer, neurodegenerative diseases, and so on. A new anti-inflammatory medication that is safe, potent, non-toxic, or less toxic is now required as the existing anti-inflammatory and non-steroidal drugs are associated with various side effects. In this context, we have reviewed the genus Ilex for traditional uses related to inflammation and anti-inflammatory properties (in vitro and in vivo) by utilizing databases like PubMed, Google Scholar, and Science Direct. According to ethnomedicinal information, these plants have been used to treat various inflammatory conditions. A total of 12 species were found with anti-inflammatory potential, where some studies were conducted using crude extracts and others with pure compounds. Many chemical compounds have been reported from the Ilex species; however, the bioactive composition explored for anti-inflammatory effects include rotundarpene, triterpenoid saponins, chlorogenic acid, ursolic acid, ilexgenin A, isoquercetin, kaempferol, ilexchinenosides J-Q and salicifoneoliganol. The mechanistic insights into how Ilex species deal with inflammatory stimuli in the mitogen-activated protein kinase, nuclear factor-κB, PI3K/Akt/mTOR, Janus kinase-signal transducer and activator of transcription, and arachidonic acid pathways have also been highlighted. The toxicity profile of studies has also been discussed to assess safety. These plants can be developed as drug-developing candidates after detailed follow-up studies. [ABSTRACT FROM AUTHOR]

Purpose: This study presents a green approach for synthesizing silver and zinc-based nanoparticles (NPs)/nanocomposites (NCs) utilizing aqueous extracts of palmyra palm (Borassus flabellifer) sprouts and mature fruit pulp. Methods: The formation of nanomaterial (NM) was confirmed with several characterization techniques. Plant extracts and plant-derived Ag/Ag2O NPs, ZnO NPs, and Ag/Ag2O/ZnO NCs were analyzed to determine their efficacies as antioxidant, anti-inflammatory, and antibacterial agents with standard biological assays. Results: Under optimized conditions, pulp and sprout-mediated Ag/Ag2O NPs, ZnO NPs, and Ag/Ag2O/ZnO NCs exhibited surface plasmon resonance peaks at 436–438 nm, 350–354 nm, and 350–450 nm, respectively. SEM imaging revealed of quasi-spherical Ag/Ag2O NPs, hexagonal rod-shaped ZnO NPs, and both morphologies arranged into the formation of Ag/Ag2O/ZnO NCs. The average sizes of all biogenic NMs were between 11 and 120 nm. Ag and Ag2O were of face-centered cubic symmetries alongside hexagonal wurtzite ZnO crystallinities. Sprout-mediated Ag/Ag2O/ZnO NCs revealed superior antioxidant potential, (IC50 of 48 ppm for DPPH and 87 ppm for ABTS assays, 74 mg AAE/1 g for FRAP assay). Sprout-mediated Ag/Ag2O NPs demonstrated significantly high (p ≤ 0.05) anti-inflammatory properties, (IC50; 414 ppm for protein denaturation inhibition and 438 ppm for HRBC membrane stabilization assay). The sprout-mediated Ag/Ag2O NPs exhibited the maximum growth inhibition zones (19 mm against E. coli and 17 mm against S. aureus). Conclusion: To the best of our knowledge, this study remains the first comparative report on the anti-inflammatory and antibacterial activities of Ag/Ag2O/ZnO NCs and their NP counterparts. The biological activities were size, morphology, and dose-dependent, and the synergistic combination of plant polyphenolics and NMs enhanced bioactivities. [ABSTRACT FROM AUTHOR]

This study investigated the anti-inflammatory effects of OJlipo1, a lipocalin-like protein derived from Oenanthe javanica. Through cloning and expressing OJlipo1 in E. coli, and subsequent rigorous characterization including amino acid analysis and mass spectrometry, its potential against inflammation was evaluated. Studies on lipopolysaccharide-stimulated RAW 264.7 cells highlighted its capability to suppress nitric oxide synthase and cyclooxygenase-2 expression, as well as its interference with nuclear factor kappa B and mitogen-activated protein kinase pathways, which are essential for toll-like receptor 4 (TLR4) signaling. Utilizing TAK242, a TLR4 pathway inhibitor, reinforced OJlipo1's specific targeting mechanism. These findings underscore OJlipo1's significant anti-inflammatory potential, aligning with the traditional uses of O. javanica, and suggest new therapeutic avenues, especially for diseases associated with TLR4 dysregulation. This validates the traditional application of O. javanica in inflammation and positions OJlipo1 as a promising therapeutic candidate, enriching our understanding of its molecular underpinnings and therapeutic prospects. [ABSTRACT FROM AUTHOR]

In this work, with the aim to find new and biologically active natural compounds, the chemical content of the apolar and polar extracts (aerial part) of Silene popovii has been investigated. The obtained extracts of Silene popovii Schischk were purified by column chromatography (CC), and four compounds were isolated: one of them is a new saponin compound—silepovin (1), as well as three known secondary metabolites, 2-deoxy-α-ecdysone (2), cauloside A (3) and 20-hydroxyecdysone 22-benzoate (4). The structural elucidation of isolated compounds was performed using the 1D and 2D NMR spectroscopy analyses and LC-MS analysis, and all four structures were confirmed. For the new compound 1, an in vivo study of anti-inflammatory activity was conducted. The in vivo analysis has shown significant anti-inflammatory effects. [ABSTRACT FROM AUTHOR]

Background: Montanoa grandiflora, a plant species native from Mexico to Central America, locally known as "Teresita" in Yucatán, México, is used to alleviate anxiety, rheumatism, and stomach issues. This study aims to investigate the anti-inflammatory properties of the methanol extract of Montanoa grandiflora leaves (MMG) in experimental models of inflammation. Methods: Gas chromatography-mass spectroscopy was used to characterize the MMG; cytotoxicity was assessed by MTT assay on murine macrophages and hemolysis assay. The in vitro anti-inflammatory activity was evaluated on LPS-stimulated murine macrophages by measuring of pro- and anti-inflammatory cytokines, NO and H2O2 release. The in vivo anti-inflammatory activity was evaluated using carrageenan-induced mouse paw edema, 12-O-tetradecanoylphorbol 13-acetate induced-ear edema, and 1-fluoro-2,4-dinitrobenzene induced-delayed-type hypersensitivity. In addition, the serum levels of prostaglandins and leukotrienes were assessed. Results: The main compounds found in MMG were terpenes (i.e., β-caryophyllene, (-)-α-cubebene, alloaromadendrene, (+)-δ-cadinene, β-eudesmol), alkaloid ((±)-nor-β-hydrastine), cyclic polyol (quinic acid), carbohydrates and their derivatives, and fatty acids (octadecatrienoic acid and octadecanoic acid). MMG did not exhibit cytotoxic or hemolytic activity. However, it demonstrated in vitro anti-inflammatory effects by increasing the production of IL-10, decreasing the levels of TNF-α, IL-1β, IL-6, NO and H2O2. MMG significantly reduced carrageenan-induced paw edema, TPA-induced ear edema, and DNFB-induced delayed-type hypersensitivity in mice with effects comparable to those of standard drugs, as well as serum levels of prostaglandins and leukotrienes. Conclusion: The anti-inflammatory activity of MMG is associated with increased IL-10 levels and inhibiting inflammatory cell migration mechanisms, without causing cytotoxic or hemolytic damage in both in vitro and in vivo assays. [ABSTRACT FROM AUTHOR]

Determination of the botanical origin of plant-originated bee products like propolis is a highly crucial task especially for the standardization of the extract and prediction of its health benefits. While there are various propolis types across globe, the existence of two main propolis types originating from black poplar and Eurasian aspen poplar have been revealed in Türkiye up to date. This study focused on the chemical characterization and bioactivities of unique propolis samples which showed a distinct chemical profile from the known types of propolis. Accordingly, the botanical origin of this new type of propolis was determined by comparative analysis of hydroalcoholic extracts of propolis with that of Cistus laurifolius extract by HPTLC. Marker compounds such as luteolin, apigenin, quercetin, and 3-O-methylquercetin were detected in both extracts along with an unknown compound. Moreover, this unidentified compound was purified by successive chromatographic methods and its chemical structure was elucidated as 3,7-O-dimethylquercetin by NMR and MS analyses. Besides, LC-MS/MS was used for the quantification of the compounds. The results of bioactivity studies showed that standardized hydroalcoholic propolis extract led to a decrease in nitrite release from LPS-activated RAW264.7 cells at 10 µg/mL indicating its remarkable anti-inflammatory activity. Additionally, propolis extract showed potent anticancer activity against pancreatic cancer cell lines MIA PaCa-2 in both 2D and 3D models in a concentration-dependent manner. The strongest effect on spheroid size change was observed at the concentration of 1 mg/mL. [ABSTRACT FROM AUTHOR]

Hypericum beanii, a traditional folk medicine plant, has been employed in treating various inflammation-related diseases. In this study, three new prenylated xanthones, named beanigenin A (1), beanigenin B (2), and beanigenin C (3), along with twenty-five known compounds (4–28), were isolated from the aerial parts of H. beanii. The new xanthones were elucidated based on modern spectroscopic experiments, including nuclear magnetic resonance spectroscopy (NMR) techniques, high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS), and electronic circular dichroism (ECD). All the compounds were evaluated for their anti-inflammatory effects by measuring their inhibitory effect on nitric oxide (NO) production in LPS-stimulated RAW 264.7 macrophages. Our findings showed that compounds 1–10, 12, 14, 21–23, 26, and 28 displayed significant anti-inflammatory effects, with IC50 values ranging from 0.82 to 9.71 μM. The MOE software was utilized to conduct an in silico evaluation of the potential inhibitory activity of the three new xanthones against inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) proteins. The results indicated that the three new xanthones demonstrated a high binding affinity with both iNOS and COX-2 proteins. [ABSTRACT FROM AUTHOR]

Tea polysaccharide (TP), as a naturally occurring bioactive polysaccharide derived from tea leaves, exhibits diverse pharmacological activities, which extensively utilized in healthcare products. However, previously reported applications did not include wound repair until now. In this study, TPs isolated from Tibetan tea was compound with bacterial cellulose (BC) via a novel membrane–liquid interface (MLI) culture resulted in obtained a novel TP-based dressing. The results of SEM and AFM confirmed successful attachment of TPs onto the surface of BC fibers. The obtained TP/BC composite exhibited robust thermal stability, excellent water absorption, acceptable water retention, and improved mechanical properties. The introduction of TP also conferred the dressing notable antioxidant properties (DPPH clearance rate was up to 85%), acceptable antibacterial properties (the antibacterial rate against S. aureus and E. coli were above 80%), and potent anti-inflammatory activity (the secretion of pro-inflammatory factor TNF-α was inhibited, while the secretion of anti-inflammatory factor TGF-β was promoted). Furthermore, the TP/BC composite exhibited improved cytocompatibility to promote NIH3T3 cells proliferation and spread compared with BC. All results indicated that the obtained TP/BC composite has an enormous potential for wound dressing, and the application of TP will be broadened. [ABSTRACT FROM AUTHOR]

Symphorema polyandrum belongs to the Lamiaceae family and is locally known as Badichang or mahasindhu. In this study, we performed Soxhlet extraction to prepare methanolic and hydromethanolic extracts, followed by quantification of their total phenolic content and total flavonoid content. Qualitative analysis of both the extracts was conducted to determine the presence of different phytochemicals. In addition, we aimed to identify the important phytochemical constituents in the methanolic extracts of S. polyandrum (SPM) using ultra-performance liquid chromatography hyphenated with high-resolution mass spectrometry (UPLC–ESI–QTOF–MSE). Furthermore, this study investigated the antioxidant, anticancer and anti-inflammatory properties of SPM and its safety profile in the normal fibroblast cell line L929. A colony proliferation assay and a Griess assay were performed to evaluate the effects of SPM on colony formation and nitric oxide (NO) production. A total of 13 important phytochemicals were identified and reported. The methanolic extract of SPM demonstrated significant antioxidant activity. SPM also showed substantial antiproliferative activity on MDA-MB-231 triple-negative breast cancer cells, with an IC50 value of 45.53 ± 1.63 µg/ml, and also reduced the survival of these cancer cells by promoting nuclear fragmentation and condensation without causing harm to normal cells. SPM inhibits the colony formation and reduces the nitric oxide (NO) production. The anti-inflammatory potential of SPM was assessed utilizing the murine alveolar macrophages (J774.A.1) as an in vitro model, and SPM effectively lowered the levels of proinflammatory cytokines such as TNF-α and IL-6. These findings emphasized the antiproliferative potential of SPM to cancer cells, along with its anti-inflammatory, and antioxidant capabilities, indicating the therapeutic efficacy of this medicinal plant. [ABSTRACT FROM AUTHOR]

Therapeutic effect of many plants is associated with the presence of various bioactive substances in them. The plant hormones—phytohormones—can be distinguished among these substances. When ingested into the human body, they affect physiological processes such as inflammation, glucose uptake, cell division, and resistance to diseases. It is hypothesized that phytohormones may be used as drugs with no side effects. One of them could be the phytohormone indolyl-3-acetic acid (IAA), which is a heteroauxin and can be synthesized by some microorganisms and animals, including mammals. This phytohormone is an important derivative of indole, which is catabolized from dietary tryptophan by the intestinal microbiota. IAA can scavenge free radicals, inhibit oxidative stress, and reduce the production of proinflammatory cytokines. As a ligand of the aryl hydrocarbon receptor, IAA can regulate intestinal homeostasis and suppress inflammatory responses. This review summarizes the current literature data on the vital role of IAA in the treatment of cancer, type 2 diabetes, rheumatoid arthritis, liver disease, Alzheimer's disease, dental diseases, and microbial skin diseases. The purpose of this review is to draw attention and interest to IAA as a promising therapeutic drug. [ABSTRACT FROM AUTHOR]

Chronic wounds characterized by prolonged inflammation and persistent infection pose a significant burden to global healthcare systems. Currently, antibiotics and non-steroidal anti-inflammatory drugs (NSAIDs) are administered to patients. Prolonged use of antibiotics is severely discouraged owing to the rapid rise in antimicrobial resistance, and the use of NSAIDs can also increase the risk of infection. Thus, the discovery of novel therapeutics for chronic wounds is crucial. Antimicrobial peptides (AMPs) are an emerging class of therapeutics, which are effective and has no known mechanism of inducing resistance. Anti-inflammatory peptides (AIPs) are another class of therapeutic peptides that can reduce inflammation by eliciting anti-inflammatory cytokine response. A single peptide possessing both AMP and AIP activities can be an ideal therapeutic for the treatment of chronic wounds. However, the discovery of peptides with multiple properties via experimental testing is a daunting task. In this work, we propose a classification framework using machine learning for the identification of wound healing peptides (WHPs) i.e., which possess both AMP and AIP activities. The proposed framework uses XGBoost algorithm with amino-acid composition, sequence analysis and physicochemical properties as feature representation methods (FRMs) to develop binary classifiers. The model developed by combining all the three FRMs, resulted in the highest accuracy of 93.3 and 76.2% for AMP and AIP classifications, respectively. An easy-to-use freely accessible web tool (WHP-Pred) has also been developed. [ABSTRACT FROM AUTHOR]

Prim-O-glucosylcimifugin (POG) is a chromone derived primarily from Saposhnikovia divaricata (Turcz) Schischk and Cimicifuga simplex. Previous research has shown that POG possesses antibacterial, anticancer, anti-inflammatory, antioxidant, anticonvulsant, antipyretic, and analgesic properties. However, the specific impact of POG on influenza-virus-induced pneumonia is not well understood. In this study, we investigated the protective effects and underlying mechanisms of POG in pneumonia caused by influenza A virus (IAV). In vitro, POG was found to have a protective effect against infections caused by the respiratory viruses respiratory syncytial virus (RSV), human coronavirus OC43, and influenza A virus. POG inhibited A/FM/1/1947(H1N1) infection with an EC50 ranging from 3.01 to 10.43 in vitro. Intraperitoneal infection of mice with POG at a dose of 5 or 10 mg/kg resulted in a reduction in IAV-induced pneumonia, as evidenced by decreased pulmonary edema, improved lung histopathology, and reduced inflammatory cell accumulation. At the higher dose (10 mg/kg), POG treatment significantly increased survival rates, decreased viral titres in the lungs, improved lung histology, and reduced lung inflammation in IAV-infected mice. POG also effectively alleviated pulmonary fibrosis by reducing the levels of fibrotic markers (hydroxyproline [Hyp] and transforming growth factor β1 [TGF-β1]) and suppressing the expression of alpha smooth muscle actin (α-SMA), p focal adhesion kinase (p-FAK), and TGF-β1 in lung tissues. In addition, POG inhibited the expression of the RELA proto-oncogene (RELA), phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (PIK3CD), and mitogen- and stress-activated protein kinase 2 (MSK2) in lung tissues. These results indicate that POG may have a protective effect against IAV-induced pneumonia by downregulating the TGF-β1/PI3KCD/MSK2/RELA signalling pathway in the lungs. [ABSTRACT FROM AUTHOR]

The anti-inflammatory activity of new 3-pyrrolin-2-one derivatives, namely, 5-aryl-4-hetaroyl-3-hydroxy-1-hydroxyalkyl-3-pyrrolin-2-ones, was studied. The studied 5-aryl-4-hetaroyl-3-hydroxy-1-hydroxyalkyl-3-pyrrolin-2-ones exhibited an anti-inflammatory effect, inhibiting swelling of rat paws in an acute exudative inflammation model caused by subplantar injection of carrageenan solution (1%) and did not change the absorption activity of peripheral blood leukocytes. The studied compounds reduced the number of abdominal muscle contractions in mice in a peritovisceral pain model caused by intraperitoneal injection of acetic-acid solution (0.75%). [ABSTRACT FROM AUTHOR]

Green synthesis leverages biological resources such as plant extracts to produce cost-effectively and environmentally friendly NPs. In our study, silver nanoparticles (AgNPs) are biosynthesized using blank roasted grams (Cicer arietinum) as reducing agents. CA-AgNPs were characterized by a characteristic surface plasmon resonance (SPR) peak at 224 nm in the UV–Vis spectrum. FTIR analysis revealed functional groups with O–H stretching at 3410 cm−1, C–H stretching at 2922 cm−1, and C=O stretching at 1635 cm−1. XRD patterns exhibited sharp peaks at 33.2°, 38.4°, 55.7°, and 66.6°, confirming high crystallinity. Morphological analysis through FESEM indicated spherical CA-AgNPs averaging 500 nm in size, with EDS revealing Ag at 97.51% by weight. Antimicrobial assays showed zones of inhibition of 14 mm against Candida albicans, 18 mm against Escherichia coli., and 12 mm against Propionibacterium acnes. The total phenolic content of CA-AgNPs was 26.17 ± 13.54 mg GAE/g, significantly higher than the 11.85 ± 9.57 mg GAE/g in CA extract. The ABTS assay confirmed the antioxidant potential with a lower IC50 value of 1.73 ± 0.41 µg/mL, indicating enhanced radical scavenging activity. Anti-melanogenesis was validated through tyrosinase, showing inhibition rates of 97.97% at the highest concentrations. The anti-inflammatory was evaluated by western blot, which showed decreased expression of iNOS and COX-2. This study demonstrates the green synthesis of CA-AgNPs and its potential biomedical applications. The results of this study demonstrate that biosynthesized CA-AgNPs have key biological applications. [ABSTRACT FROM AUTHOR]

Objective: The aim of this study is to produce novel of the new functionally substituted nicotinohydrazones, analyze their anti-inflammatory activity, and assess their toxicity. A promising avenue for the advancement of novel bioactive compounds is the pursuit of "hybrid molecules" that contain pharmacophore fragments within their structural composition, with a particular focus on the examination of these molecules for the discovery of novel biological activities. Methods: The synthesis of nicotinic acid hydrazones (II–VI) was performed by condensation of nicotinic acid hydrazide with various aldehydes in ethanol when refluxing the reaction mixture at 60–70°C. The anti-inflammatory activity was studied using the formalin paw edema method in non-linear white rats. The acute inflammatory reaction was reproduced by subplantar (i.e., underplantar or plantar aponeurosis) injection of 0.1 mL of a 2% formalin solution into the right paw using a conventional insulin syringe. Results and Discussion: The structure of the new functionally substituted nicotinohydrazones has been confirmed by a combination of the 1H and 13C NMR methods, and COSY (1H-1H), HMQC (1H–13C), and HMBC (1H–13C) two-dimensional NMR spectroscopy methods.1H, and 13C NMR spectroscopy were used to investigate all the prepared derivatives. The acute toxicity of the aforementioned compounds was preliminarily evaluated using a specially developed Toxicity Assessment Software Tool within the United States Environmental Protection Agency. The LD50 values for rats following oral administration of the compounds tested by the QSAR method. According to the projected toxicological effects, compounds (II), (III) can be classified into Class 4 in terms of toxicity. Compounds (IV), (V) and (VI) have low toxicity and very low toxicity, respectively. Conclusions: The anti-inflammatory activity of the synthesized hydrazones has been evaluated and it has been demonstrated that these compounds were ineffective in comparison with ibuprofen at a dosage of 100 mg/kg (p2 < 0.05). The low toxicity level of all the tested compounds was predicted by the computer modeling. The LD50 values of the compounds range from 445.461 to 1491.991 mg/kg. The studies on the model of formalin paw edema in nonlinear white rats indicate the absence of an anti-inflammatory effect of the tested compounds. [ABSTRACT FROM AUTHOR]

Objective: In the present work synthesis and characterization of new heterocyclic derivatives containing dihydropyrano[2,3-c]pyrazoles. Methods: Synthesis of compounds was done using the conventional method via multicomponent reaction using substituted aldehyde, hydrazine hydrate or phenyl hydrazine, malononitrile, and L-proline as a catalyst with good yield. Reaction optimization is also performed. Results and Discussion: All synthesized compounds were tested for their in vitro anti-inflammatory and a comparison was done against the standard drug Diclofenac sodium. Conclusions: Some of the newly synthesized compounds demonstrated good to moderate anti-inflammatory activity. [ABSTRACT FROM AUTHOR]

Caesalpinia sappan L. has generally been used in Asian folk medicines for disease treatment. C. sappan heartwood is commonly utilized as a dyeing agent in food items, beverages, cosmetics, and clothing. The effects of three extraction techniques (maceration, reflux, and ultrasonic-assisted extraction) of C. sappan heartwood extract (CSE) on the brazilin content and potential of biological activities were investigated. The brazilin content was determined using high-performance liquid chromatography (HPLC). Quantifications of the antioxidant properties (DPPH and ABTS), the total phenolic contents, and the antimicrobial activity were also examined. Additionally, the effect of CSE on pro-inflammatory cytokine and mediator production was investigated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophage cells. The results showed that the CSE from the maceration and reflux methods produced high levels of brazilin and total phenolic contents, as well as having excellent antioxidant and antimicrobial activities. The macerated extract showed significant antioxidant activities with IC50 values of 2.88 ± 0.01 and 0.32 ± 0.01 mg/mL from DPPH and ABTS assays, respectively. Furthermore, the CSE from the maceration method which was rich in brazilin had an anti-inflammatory response by decreasing the levels of nitric oxide (NO), interleukin (IL)-6, and tumor necrosis factor (TNF)-α on LPS-stimulated RAW 264.7 macrophage cells. These results confirmed CSE as a potential source of biological components. Antioxidant and anti-inflammatory assays proved maceration was the best extraction method.Article Highlights: Three extraction methods (maceration, reflux, and ultrasonic-assisted extraction) were applied to study the brazilin content and biological activities of Caesalpinia sappan L. The maceration method is illustrated as the most efficient extraction technique. The heartwood extract of C. sappan from maceration contained a high level of brazilin and exhibited antioxidant and anti-inflammatory properties. [ABSTRACT FROM AUTHOR]

Traditional medicine has long employed the shrub Hibiscus sabdariffa to treat a variety of illnesses. The biochemical characteristics of silver nanoparticles made using the plant extract of Hibiscus sabdariffa were examined in this work. According to the results, the plant extract of Hibiscus sabdariffa had a total phenolic quantity of 84.9 mg/gm and a total quantity of flavonoids of 41.50 mg/gm. The extract also showed antibacterial action against Escherichia coli and Staphylococcus aureus (75.15% scavenging activity). The silver nanoparticles of plant extracts were stable in PBS solution for at least 30 days and had a mean size of particles of 21.22 nm. Silver nanoparticles were shown to both be cytotoxic on human lung cancer cell line A-549 and have anti-inflammatory action. Overall, the research's findings demonstrate the fascinating biological activity of the silver nanoparticles made from the extract of the Hibiscus sabdariffa plant. To assess these compounds' potential as medicines, more research is required. [ABSTRACT FROM AUTHOR]

The present work focuses on the synthesis of novel heterocycles 2-(aryloxy)-3-(4,5-diaryl-1H-imidazol-2-yl)quinolines (6k-v) by an effective condensation reaction. These molecules exhibited fluorescent properties and hence for the proper understanding of their optical behavior and quantum yields, solvatochromic studies have been carried out. Further, frontier molecular orbitals, molecular electrostatic potential (MEP), and geometrical structure optimization have been investigated using the B3LYP/6-311G ++ (d, p) method. The energy gap between the HOMO, LUMO of the optical and energy band gap is determined by DFT and UV–visible spectra for TD-DFT studies are done. The screening of these compounds for in vitro COX-1 and COX-2 inhibition and DPPH free radical scavenging ability assays produced promising results. The binding interactions of these molecules against the COX-2 enzyme (PDB: 5IKR) were validated by docking studies. [ABSTRACT FROM AUTHOR]

Synthesis of N-substituted 4-aryl-2-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-4-oxobut-2-enamides by the reaction of the substituted 2-[(5-aryl-2-oxofuran-3(2H)-ylidene)amino]-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitriles with primary amines was developed. Anti-inflammatory activity and acute toxicity of the synthesized compounds were examined. It was found that the synthesized compounds possess pronounced anti-inflammatory activity and low toxicity. According to the classification of toxicity of drugs, the synthesized amides belong to toxicity class V of practically nontoxic substances. [ABSTRACT FROM AUTHOR]

A series of {1-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]-1H-pyrazol-4-yl}(2-hydroxyphenyl)metha-nones 5 were synthesized from 1-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazine 3 and substituted 3-formyl-chromones 4. Compounds 5 were converted into 2-[(E)-{1-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]-1H-pyrazol-4-yl}(hydroxyimino)methyl]phenols 6. The synthesized compounds were characterized by spectral techniques screened for their anti-inflammatory activity. Compounds 6c and 6e showed good percent inhibition of haemolysis when compared with the standard drug celecoxib. The molecular docking study explored the essential binding mode and possible thermodynamic interactions within the binding site of COX-2 enzyme. [ABSTRACT FROM AUTHOR]

In search of novel anti-inflammatory and antioxidant agents with improved potency, a small focused library of 1,2,3-triazole-based chalcone derivatives has been efficiently prepared via the click chemistry approach. All synthesized compounds' Structures were characterized with the help of IR, 1H NMR, 13C NMR, and mass spectroscopic techniques. All the synthesized novel derivatives were evaluated for their anti-inflammatory activity. Molecular docking studies against COX-2 gave valuable insights into the mechanistic basis of the demonstrated anti-inflammatory activity. Further, the synthesized compounds were found to have potential antioxidant activity. [ABSTRACT FROM AUTHOR]

Argemone mexicana belonging to family Papaveraceae is a traditional medicinal plant widely utilized by tribal people in India for treating various ailments like skin infections, wounds and inflammation. This plant is very rich in alkaloidal content, which has a great potential in the treatment of anti-inflammatory disorders. Therapeutically promising bioactive molecules are often produced by endophytic fungi associated with medicinal plants. In this investigation, endophytic fungi were isolated from various parts of A. mexicana and screened for alkaloidal content. Among these, one of the fungal isolate, Acremonium alternatum AMEF-5 producing maximum alkaloids showed significant anti-inflammatory activity. Fractionation of this crude fungal extract through column chromatography yielded eight fractions, which were further screened for anti-inflammatory activities. Fraction 3 exhibited significant anti-inflammatory activity by the inhibition of lipoxygenase enzyme (IC50 15.2 ± 0.09 µg/ml), scavenging of the nitric oxide radicals (IC50 11.38 ± 0.35 µg/ml), protein denaturation (IC50 14.93 ± 0.4 µg/ml), trypsin inhibition (IC50 12.06 ± 0.64 µg/ml) and HRBC stabilization (IC50 11.9 ± 0.22 µg/ml). The bioactive alkaloid in fraction 3 was identified as aconitine which was confirmed by UV, FTIR, HPLC, HRMS, 1H NMR, and 13C NMR analysis. This study demonstrates that endophytic fungi serve a potential source for sustainable production of therapeutically important alkaloids. [ABSTRACT FROM AUTHOR]

Rising global mortality rates due to antimicrobial infections and cancer underscore the urgent need for effective therapeutic interventions. Here, we present a sustainable approach utilizing biomass-free filtrate from the endophytic fungus Aspergillus sp. LCJ315 for the eco-friendly synthesis of strontium oxide nanoparticles (SrONPs) using strontium nitrate as the precursor. The color change in the reaction solution and UV peak at 280 nm infers the formation of SrONPs. FTIR analysis revealed the absorption spectrum 3429 cm−1, 2924 cm−1, 1641 cm−1, and 1075 cm−1 denoting the presence of the characteristic functional groups OH, CH, CO, and CN bonds, respectively, indicating the synthesis of SrONPs. XRD analysis revealed crystalline SrONPs with an average size of 27.75 nm, while SEM imaging depicted spherical nanoparticles ranging from 25 to 50 nm. EDX confirmed the presence of strontium and oxygen elements. Antimicrobial, antioxidant, anti-inflammatory, and lethal toxicity studies were conducted to assess the therapeutic potential and safety profile of SrONPs. Antimicrobial activity revealed that the SrONPs exhibited antagonistic activity against Candida albicans (14 ± 0.46 mm). SrONPs exhibited potent antioxidant activity of 78.59 ± 1.99% in hydrogen peroxide radical scavenging assay and 87.35 ± 1.69% in DPPH assay at 50 µg/mL concentration. Furthermore, SrONPs exhibited excellent anti-inflammatory activity of 78.37 ± 2.1% inhibition in bovine serum albumin denaturation assay and 79.69 ± 2% inhibition in egg albumin denaturation assay at 50 µg/mL concentration with minimal toxicity observed. The eco-friendly synthesized SrONPs from Aspergillus sp. LCJ315 exhibited the antimicrobial, antioxidant, and anti-inflammatory properties, coupled with low toxicity levels, suggesting their potential for use in nanomedicine formulations to combat life-threatening diseases. [ABSTRACT FROM AUTHOR]

Aceclofenac (ACE) is a drug that was precisely devised to circumvent the shortcomings associated with diclofenac. However, ACE too corresponds to nonsteroidal anti-inflammatory drug (NSAID)-related adverse effects, but with a lower amplitude. The present investigation seeks to develop liposomes loaded with ACE adopting a central composite design (CCD) and formulate a chitosan-based hydrogel for synergistic anti-inflammatory efficacy and improved ACE dermal administration. On the basis of preliminary vesicle size, Poly Dispersity Index (PDI), and drug entrapment, the composition of lipid, cholesterol, and vitamin E TPGS were chosen as independent variables. The formulation composition met the specifications for an optimum liposomal formulation, with total lipid concentration (13.5% w/w), cholesterol concentration (10% w/w), and surfactant concentration (2% w/w). With particle size and PDI of 174.22 ± 5.46 nm and 0.285 ± 0.01 respectively, the optimised formulation achieved an entrapment effectiveness of 92.08 ± 3.56%. Based on the CCD design, the optimised formulation Acec-Lipo opt was chosen and was subsequently transformed to a chitosan-based gel formulation for in vitro drug release, penetration through the skin, in vivo analgesic therapeutic activity, and skin irritation testing. % age oedema inhibition was found to be greatest with the Acec-Lipo opt gel formulation, followed by Acec gel. These results reinforce the notion that the inclusion of chitosan resulted in a synergistic effect despite the same strength of the drug. The findings suggested that Acec-Lipo incorporated in chitosan gel for skin targeting might be an effective formulation for topical ACE administration in clinical subjects. [ABSTRACT FROM AUTHOR]

Two new lindenane-type sesquiterpenoid dimers, chlotrichenes C and D (1 and 2) together with five known lindenane-type sesquiterpenoid dimers (3–7) were isolated from the roots of Chloranthus holostegius var. trichoneurus, a famous natural medicine named as "Sikuaiwa" for subduing swellings and relieving pain. The structures including absolute configuration were elucidated by their 1D and 2D NMR, HRESIMS, and ECD data. Compounds 1 and 2 were classical [4 + 2] lindenane-type sesquiterpenoid dimers that differed from known analogs in oxidation profile, side chain profile, and double bond position. The new isolates and compound 3 exhibited significant inhibitory activity on IL-1β production (IC50: 1–15 μM) in LPS-induced THP-1 cells and other compounds exhibited inhibitory activity on NO production in LPS-induced RAW 264.7 cells (IC50: 24–33 μM). [ABSTRACT FROM AUTHOR]

The anti-inflammatory activity of 17 derivatives of 5-N-arylaminocarbonyl-6-aryl-4-methyl-1,2,3,6-tetrahydropyrimidine-2-thiones was studied. The molecular structure of one of them was established. Ten compounds that inhibited the inflammatory reaction in experimental animals in the range 56-81% were identified. [ABSTRACT FROM AUTHOR]

This study focuses on six Eucalyptus species, namely E. badjensis, E. benthamii, E. dunnii, E. grandis, E. globulus, and E. saligna aiming at a sustainable use of their green biomass. These species were grown at the same location and stage of development. Leaf essential oils were extracted by hydrodistillation using a Clevenger apparatus during the four seasons. Gas chromatography–mass spectrometry (GC–MS) and high-performance thin-layer chromatography (HPTLC) techniques were used to analyze the chemical composition. E. badjensis consistently exhibited a dominant composition, with 1,8-cineole being the predominant component. Notably, the proportion of 1,8-cineole in E. badjensis was 77.35% in spring (SP), 69.46% in summer (SU), 95.30% in autumn (AU), and 89.30% in winter (WI). E. globulus also exhibited 1,8-cineole as its primary constituent, with proportions fluctuating slightly across seasons at 84.87%, 79.94%, 81%, and 85.88%, respectively. The proportions and constituents of various species differed significantly. HPTLC was successfully used as a swift technique to monitor the chemical composition of essential oils (EOs) in various Eucalyptus species during the seasonality. GC–MS and HPTLC analysis showed that different Eucalyptus species displayed unique chemical compositions, while both the chemical profile and productivity of all analyzed EOs were affected by seasonality. This finding was demonstrated in the principal components cluster. The analysis of six species has revealed that the EO of E. benthamii is the most potent in thwarting the infestation of Cimex lectularius. Additionally, all six EOs demonstrated antioxidant activity in the ABTS model. EOs of E. benthamii, E. dunnii, and E. grandis showed significant anti-inflammatory activities in experimental models.Highlights: E. badjensis, E. dunnii, and E. globulus are promising sources for the commercial exploitation of 1,8-cineole E. benthamii, E. grandis, and E. dunni presented anti-inflammatory activity The essential oils of six species showed antioxidant activity. E. benthamii EO presented a potent insecticide against Cimex lectularius adults. Eucalyptus leaf biomass as a novel resource for the pharmaceutical, nutraceutical, and insecticidal industries [ABSTRACT FROM AUTHOR]

The goal of the present study was to prepare meloxicam (MX) entrapped hybrid particles (HPs) to enhance intestinal permeation and anti-inflammatory activity. MX-HPs were prepared by nanoprecipitation method using lipid, chitosan, poloxamer, and TPGS. The formulations (MX-HPs1, MX-HPs2, MX-HPs3) were evaluated for particle size, entrapment efficiency, and drug release to select the optimized composition and further evaluated for permeation study, stability study, morphology, interaction study, and anti-inflammatory activity by carrageenan-induced rat paw edema test. The prepared MX-HPs showed nano sized particles (198.5 ± 3.7 to 223.8 ± 2.1 nm) and PDI (<0.3), zeta potential (16.5 ± 2.7 to 29.1 ± 3.6 mV), and high entrapment efficiency (75.1 ± 4.7 to 88.5 ± 3.9%). The surface morphology was assessed by transmission electron microscopy and showed non-aggregated particles. Infra-red (IR) spectroscopy of pure MX as well as formulation revealed no drug-polymer interaction and X-ray diffraction confirmed the conversion of crystalline MX into amorphous form. The release study data revealed prolonged MX release for 24 h. The selected optimized hybrid particles (MX-HPs2) revealed a 2.3-fold improved enhancement ratio than free MX. The storage stability and gastrointestinal stability data demonstrated a stable formulation in SIF as well as SGF. The anti-inflammatory activity showed better therapeutic action than pure MX dispersion. From the study, it can be concluded that the prepared MX-HPs may be a promising delivery system for MX in treating inflammatory disorders. [ABSTRACT FROM AUTHOR]

Copper oxide nanoparticles are synthesized by the green approach method which is sustainable and eco-friendly perhaps other physical and chemical methods. The attention towards noble metal (Ag, Au, etc.) is reducing and that is now covered by copper oxide nanoparticles owing to its potency and being economically cheaper. For the first time, the copper oxide nanoparticles were synthesized utilizing an aqueous petal extract of Wedelia trilobata as a reducing agent. The UV–vis spectrum is observed at 412 nm. The XRD peaks correspond to the face-centered cubic structure. FT-IR bands detected for nanoparticles obtained from petal extracts exhibits the functional groups, 436.09 cm-1 and 456.50 cm-1 validates the Cu – O stretching vibrations. The morphology of nanoparticles is spherical which is confirmed by SEM. Elemental analysis is also performed to know the purity of the nanoparticles obtained. Antibacterial activity of nanoparticles is measured by minimal inhibitory concentration assay for which three different bacterial strains are used Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. The antioxidant activity of the nanoparticles and aqueous petal extract is assessed by DPPH assay. BSA protein is used to check the denaturation activity of the nanoparticle, petal extract. The crystalline size of the nanoparticles is 4.2 nm which is measured by DLS and zeta potential is observed to be stable. [ABSTRACT FROM AUTHOR]

A new isoflavone, 4′-hydroxy-5,7,2′-trimethoxyisoflavone (1), has been isolated from the fruits of Myristica elliptica var. simiarum, together with seven known compounds, 2′-hydroxygenistein (2), licarin A (3), accuminatin (4), guaiacin (5), virolane (6), elimicin (7), and β-sitosterol (8). The structure of the new compound 1 was determined through spectroscopic and MS analyses. Among the isolated compounds, 4′-hydroxy-5,7,2′-trimethoxyisoflavone (1), 2′-hydroxygenistein (2), licarin A (3), and guaiacin (5) showed potent inhibition with IC50 values of 24.18 ± 2.09, 16.39 ± 1.26, 22.68 ± 2.30, and 27.01 ± 2.42 μM, respectively, against LPS-induced NO generation. [ABSTRACT FROM AUTHOR]

Ulcerative colitis (UC), an inflammation of the colon lining, represents the main form of inflammatory bowel disease IBD. Nutritional therapy is extremely important in the management of ulcerative colitis. Fish oil contains long-chain omega-3 polyunsaturated fatty acids, which have beneficial effects on health, including anti-inflammatory effects. This study aims to investigate the benefits of bluefin tuna oil extracted by the Soxhlet method in vitro by determining the anti-radical and anti-inflammatory activities and in vivo by evaluating the preventive and curative effects. The experiments were carried out using two doses of oil (100 and 260 mg/kg) and glutamine (400 and 1000 mg/kg) on the acetic acid-induced UC model. UC has been induced in Wistar rats by intrarectal administration of a single dose of 1 mL acetic acid (5% v/v in distilled water). The obtained results indicate that tuna oil and glutamine have a significant anti-free radical effect. Tuna oil has a marked anti-inflammatory power based on membrane stabilization and inhibiting protein denaturation. The reduction of various UC parameters, such as weight loss, disease activity score DAS, and colonic ulceration in rats pre-treated with tuna oil and glutamine, demonstrate that these treatments have a significant effect on UC. Total glutathione GSH, superoxide dismutase SOD, and catalase activities are significantly restored in the tuna oil and glutamine groups, while lipid peroxidation has been markedly reduced. [ABSTRACT FROM AUTHOR]

Vigna trilobata, belonging to the Fabaceae family, has been extensively used in traditional medicine in different societies due to its diverse medicinal attributes and potential therapeutic applications. The current study aimed to assess the antioxidant and antibacterial efficacy of protein extract derived from Vigna trilobata seeds. The extracted seed protein sample was precipitated using the ammonium sulphate method, at 80% concentration. Subsequent analysis of the crude sample was conducted using RP-HPLC (reverse phase high-performance liquid chromatography) and LC–MS (liquid chromatography–mass spectrometry). The antioxidant assays demonstrated that at a concentration of 10 mg/ml, the maximum percentage of inhibition of DPPH (1,1-diphenyl-2-picrylhydrazyl) radical was found to be 87.88 ± 0.01%. The ABTS (2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) assay revealed the most significant scavenging activity (22.69 ± 0.22%) at a concentration of 10 mg/ml of crude protein. Furthermore, the FRAP (ferric reducing antioxidant power) assay identified the highest scavenging activity in the crude protein at a concentration of 25 mg/ml, amounting to 2.344 mol Fe2+/mg. The anti-inflammatory efficacy was assessed by the protein denaturation and proteinase inhibition assays. The antibacterial activity of protein extract was also evaluated against Gram-positive and Gram-negative bacteria. In conclusion, the evaluation of the protein extract of Vigna trilobata shows its potential as a natural health-promoting agent due to its antioxidant, anti-inflammatory, and antibacterial properties. The protein can help in reducing oxidative stress related to chronic diseases. It also helps in alleviating inflammation-linked ailments. Additionally, its antibacterial activity shows that it helps in combating microbial infections. Further analysis and purification of the protein extract could impact the food industry, where the purified proteins could potentially be used as a natural preservative, to improve the longevity and safety of food products. [ABSTRACT FROM AUTHOR]

Twelve novel camptothecin derivatives with a carbamate substituent at position 20 were designed and synthesized. Most of the targeted compounds indicated potent anti-inflammatory activity in a lipopolysaccharide stimulation of peritoneal macrophage model. Among them, the benzyl(methyl)amine derivative showed the most pronounced anti-inflammatory activity at a concentration of 1 μM and TNF-α inhibitory rate is increased by 10.2% compared to the lead compound (N,N-dimethylethylenediamine derivative). [ABSTRACT FROM AUTHOR]

Based on their high antioxidant capacity and noteworthy phytochemistry, Terminalia ferdinandiana fruit and leaves have attracted considerable recent interest for their therapeutic potential. Whilst those studies have reported a variety of therapeutic properties for the fruit, the anti-inflammatory potential of T. ferdinandiana has been largely neglected and the leaves have been almost completely ignored. This study investigated the immune-modulatory and anti-inflammatory properties of T. ferdinandiana fruit and leaf extracts by evaluating their inhibition of multiple pro- and anti-inflammatory cytokines and chemokines secretion in lipopolysaccharide (LPS)-stimulated and unstimulated RAW 264.7 macrophages using multiplex bead immunoassays and ELISA assays. The methanolic extracts were particularly good immune-modulators, significantly inhibiting the secretion of all the cytokines and chemokines tested. Indeed, the methanolic extracts completely inhibited IL-10, IFN-γ, IL-1β, IL-6, MCP-1, and MIP-2a secretion, and almost completely inhibited the secretion of TNF-α. In addition, the methanolic T. ferdinandiana extracts also significantly inhibited cytosolic COX-2 levels (by 87–95%) and the synthesis of the PGE2 (by ~ 98%). In contrast, the methanolic extracts stimulated LTB4 secretion by ~ 60–90%, whilst the aqueous extracts significantly inhibited LTB4 secretion (by ~ 27% each). Exposure of RAW 264.7 cells to the methanolic T. ferdinandiana extracts also significantly down-regulated the cytosolic levels of NF-κB by 33–44%, indicating that the immune-modulatory and anti-inflammatory properties of the extracts may be regulated via a decrease in NF-κB transcription pathways. Taken together, these results demonstrate potent anti-inflammatory properties for the extracts and provide insights into their anti-inflammatory mechanisms. [ABSTRACT FROM AUTHOR]

This study aimed to screen a mutant of Candida utilis SE-172 with high selenite tolerance and glutathione (GSH) biosynthesis capability via 60Co γ-radiation mutagenesis to prepare selenium (Se)-enriched yeast. The maximal intracellular contents of GSH and organic Se of 22.94 mg/g and 1308.1 μg/g were obtained, respectively, under a batch culture of SE-172. The physiological mechanism underlying increased GSH and organic Se contents in Se/GSH-enriched C. utilis SE-172 was revealed based on assaying activities of γ-glutamylcysteine synthase (γ-GCS) involved in GSH biosynthesis and selenophosphate synthase (SPS) related to organic Se bioconversion, and by determining intracellular ATP and NADH contents and ATP/ADP and NADH/NAD+ ratios associated with energy supply and regeneration. Moreover, the effect of this selenized yeast on anti-inflammatory and antioxidant activities in mice with colitis was investigated. The supplementation of Se/GSH-enriched yeast decreased the dextran sodium sulfate-induced damage to colon tissues, reduced the expression of pro-inflammatory factors [interleukin (IL)-6, IL-1β, and tumor necrosis factor-α (TNF-α)] in serum, increased the antioxidant-related enzyme [superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px)] activities, and decreased the malondialdehyde content in colon. The Se/GSH-enriched C. utilis SE-172 showed potent anti-inflammatory and antioxidant activities in mice with colitis. [ABSTRACT FROM AUTHOR]

A new homoisoflavonoid, (R)-3-(2,4-dihydroxybenzyl)-5,7-dihydroxy-8-methoxychroman-4-one (1), has been isolated from the rhizomes of Polygonatum alte-lobatum, together with seven known compounds (2–8). The structure of the new compound 1 was determined through spectroscopic and MS analyses. Among the isolated compounds, compounds 1, 3, 5, and 6 showed potent inhibition with IC50 values of 18.04 ± 2.14, 19.87 ± 2.70, 16.88 ± 1.35, and 18.50 ± 1.52 μM, respectively, against LPS-induced NO generation. [ABSTRACT FROM AUTHOR]

A new phenanthrenoid dimer, junceffusin (1), has been isolated from the inflorescences of Juncus effusus var. decipiens, together with eight known compounds, effususin C (2), quercetin (3), nobiletin (4), luteolin (5), luteolin-5,3′-dimethyl ether (6), luteolin 7-glucoside (7), eriodictyol (8), and 5,7,2′,5′-tetrahydroxyflavone (9). The structure of the new compound 1 was determined using spectroscopic and MS analyses. Among the isolates, quercetin (3), luteolin (5), luteolin 7-glucoside (7), eriodictyol (8), and 5,7,2′,5′-tetrahydroxyflavone (9) showed potent inhibition, with IC50 values of 25.54 ± 2.24, 17.13 ± 1.36, 28.01 ± 2.88, 15.63 ± 1.15, and 27.44 ± 2.47 μM respectively, against lipopolysaccharide-induced nitric oxide generation. [ABSTRACT FROM AUTHOR]

Seven undescribed compounds, including three flavones (1–3), one phenylpropanoid (19), three monoaromatic hydrocarbons (27–29), were isolated from the twigs of Mosla chinensis Maxim together with twenty-eight known compounds. The structures were characterized by HRESIMS, 1D and 2D NMR, and ECD spectroscopic techniques. Compound 20 displayed the most significant activity against A/WSN/33/2009 (H1N1) virus (IC50 = 20.47 μM) compared to the positive control oseltamivir (IC50 = 6.85 µM). Further research on the anti-influenza mechanism showed that compound 20 could bind to H1N1 virus surface antigen HA1 and inhibit the early attachment stage of the virus. Furthermore, compounds 9, 22, 23, and 25 displayed moderate inhibitory effects on the NO expression in LPS inducing Raw 264.7 cells with IC50 values of 22.78, 20.47, 27.66, and 30.14 µM, respectively. [ABSTRACT FROM AUTHOR]

Rhanteriumepapposum Oliv. (locally known as Al-Arfaj) belongs to the family Asteraceae. This study was designed to discover the bioactive components and phytochemicals of the methanol extract of the aerial parts of Rhanterium epapposum, using Agilent Gas Chromatography-Mass Spectrometry (GC-MS), while the mass spectra of the compounds found in the extract matched with the National Institute of Standards and Technology (NIST08 L). GC-MS analysis of the methanol extract of Rhanterium epapposum aerial parts showed presence of sixteen compounds. The major compounds among these were 9,12,15-octadecatrienoic acid, (Z, Z, Z)- (9.89), n-hexadecenoic acid (8.44), 7-hydroxy-6-methoxy-2H-1-benzopyran-2-one (6.60), benzene propanoic acid, β-amino-4-methoxy- (6.12), 1.4-isopropyl-1,6-dimethyl-1,2,3,4,4 a,7,8,8a-octahedron-1-naphthalenol (6.00), 1-dodecanol, 3,7,11-trimethyl- (5.64), and 9,12-octadecadienoic acid (Z, Z)- (4.84), whereas the minor compounds were 9-Octadecenoic acid, (2-phenyl-1,3-dioxolan-4-yl)methyl ester, trans- (3.63), Butanoic acid (2.93), Stigmasterol (2.92), 2-Naphthalenemethanol (2.66), (2,6,6-Trimethylcyclohex-1-phenylmethanesulfonyl)benzene (2.45), 2-(Ethylenedioxy) ethylamine, N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl]- (2.00), 1-Heptatriacotanol (1.69), Ocimene (1.59), and β-Sitosterol (1.25). Furthermore, the study was extended to determine the phytochemicals in the methanol extract of Rhanterium epapposum, which indicated the positive presence of saponins, flavonoids, and phenolic compounds. Moreover, quantitative analysis revealed the presence of high content of flavonoids, total phenolic, and tannins. This study outcome suggests a podium of using Rhanterium epapposum aerial parts as a herbal remedy for various diseases especially cancers, hypertension, and diabetes. [ABSTRACT FROM AUTHOR]

The rapid development of Lentinula edode industry in China has led to the production of large amounts of waste substrates, which has brought enormous pressure to ecological environment. Thus, it is of great significance to study utilization of spent substrate. In this study, complex enzyme combined with high pressure pretreatment were applied to extract polysaccharide from spent substrate of L. edode in order to improve the utilization efficiency of its residue and explore more biological application of the polysaccharides from spent L. edodes substrate. The optimal extraction conditions were as follows: complex enzyme (cellulase, xylanase, β-glucanase) ratio, 3:2:1; total amount of enzyme, 660 U·g-1; liquid/material ratio, 20 mL/g; temperature, 45 ℃; time, 6 h; The yield of purified polysaccharide (LE-UE) was 5.98% and the content was 51.60%. LE-UE could markedly improve inflammatory damage of LPS-induced macrophages RAW264.7 by inhibiting release of NO and secretion of inflammatory cytokines. Animal experiments showed that LE-UE could markedly improve the histopathological damage and inflammation in ulcerative colitis mice by regulating the level of oxidative stress, and reduce the release of inflammatory cytokines by down-regulating mRNA expression and proteins levels. Therefore, LE-UE has anti-inflammatory activity and may be used as a novel anti-inflammatory agent for treatment. This study could provide scientific evidence for the high-value utilization of spent substrates and also provide theoretical basis for the development of functional feed additives. [ABSTRACT FROM AUTHOR]

Objective: Design and synthesis of two chalcone derivatives, evaluation of their anticancer and antiinflamatory activities. Methods: The ring-closure through an intramolecular Friedel-Crafts reaction followed by an alkaline-catalyzed Claisen-Schmidt condensation. MTT assay was conducted in anticancer activity. The chalcone derivatives tested for anti-inflammatory immunomodulatory potential by measuring pro-inflammatory cytokines production levels. Results and Discussion: Both compounds displayed anti-inflammatory effects on activated mammalian cells without being cytotoxic. Their low toxicity resulted in high IC50 values in glioblastoma cells, indicating they are safe anti-inflammatory agents, yet lack anti-cancer properties. Conclusions: Synthesized and characterized two chalcone derivatives that displayed comparable anti-inflammatory effects, reducing TNF, IL6, GMCSF, and IL12p40 levels without harming macrophages. Their high IC50 values in glioblastoma cells suggest low toxicity and highlight their potential as effective anti-inflammatory agents [ABSTRACT FROM AUTHOR]

Recently, in human and animal diseases, inflammation and pain have become the focus of scientific research as it affects more people than any other disease. Inflammation is the natural phenomenon of the immune response to remove stimuli when the body is exposed to external/internal injury. Eulophia nuda Lindl. is a perennial orchid and belongs to the family Orchidaceae. This plant is used according to folklore for the treatment of human breast cancer, inflammation, pain and as an antioxidant. The present study aims to evaluate the anti-inflammatory and analgesic potential of the ethanolic extract of tubers and different fractions of Eulophia nuda. The ethanolic extract (ENEE) and different fractions of E. nuda were prepared by liquid-liquid extraction. ENEE and obtained fractions were used to evaluate anti-inflammatory activity assessed on carrageenan-induced inflammation using the cotton pellet method. The ENEE and different fractions were also used to evaluate analgesic activity by assessing via the tail immersion test and hot plate method. The significant results from the present study indicate that ethanolic extract and its different fractions possess anti-inflammatory and analgesic potential, supporting the traditional uses of the plant. Further investigation is required to reveal the exact metabolites responsible for the observed result. [ABSTRACT FROM AUTHOR]

This study investigates the anti-inflammatory properties of extracts prepared from the leaves of eight southern African medicinal plants used traditionally to treat inflammation and pain. The inhibitory effect of aqueous and ethanol extracts on the release of pro-inflammatory cytokines was determined in lipopolysaccharide (LPS) stimulated and unstimulated RAW 264.7 murine macrophage cells. The levels of interleukin (IL)-1β, IL-6, tumour necrosis factor-α (TNF-α), interferon-gamma (IFN-γ), monocyte chemoattractant protein 1 (MCP-1) and macrophage inflammatory protein (MIP)-2 release were determined using cytokine multiplex-bead assays. The ethanol extracts of Melianthus comosus Vahl (commonly known as honey flower), Tetradenia riparia (Hochst.) Codd (misty plume bush) and Warburgia salutaris (G. Bertol.) Chiov. (pepper-bark tree), demonstrated the most significant inhibitory activity, with over 50-fold inhibition of IL-1β, IL-6 and TNF-α levels in LPS-stimulated RAW 264.7 macrophages. The aqueous extract of M. comosus also significantly inhibited the secretion of all the tested cytokines and chemokines. Phytochemical investigation of M. comosus ethanol leaf extract using ultra-high-performance liquid chromatography coupled with high-resolution mass spectrometry (UHPLC-HRMS) led to the detection of crassolide, deoxylimonoic acid D-ring-lactone, 2-hydroxynonanoic acid and 5-noniloxytryptamine. To the best of our knowledge, the cytokine inhibition properties of most of the medicinal plants screened in this study are reported for the first time. Our results support the use of southern African medicinal plants as anti-inflammatory remedies and provide an insight into the immunomodulatory mechanisms of action. [ABSTRACT FROM AUTHOR]

The design, synthesis, and biological screening of novel 4-aryl-6-[6-(2,4-dichlorophenyl)-2-methyl-pyridin-3-yl]-3,4-dihydropyrimidine-2(1H)-thiones and 2′-amino-6′-aryl-6-(2,4-dichlorophenyl)-2-methyl[3,4′-bipyridine]-3′-carbonitriles are described. The reaction involves Claisen–Schmidt condensation to afford the target compounds in up to 93% yield. The synthesized compounds were characterized by using FT-IR, 1H NMR, 13C NMR, mass spectrometry, and elemental analysis and were screened for their antibacterial activity against both gram-negative and gram-positive bacterial strains. Methoxy-, hydroxy-, and halogen-substituted deriva-tives showed good inhibitory effect against the tested microorganisms. Also, some of the compounds showed better anti-inflammatory activity when compared to the standards. The electron-donor properties of the novel pyrimidine derivatives were confirmed by quantum chemical studies. [ABSTRACT FROM AUTHOR]

Edible insects possess several health enhancing properties and play an important role in human nutrition. Coridius chinensis is an edible insect that is considered food and claimed as traditional medicine. In the present study, nutritional contents, chemical composition, antioxidant, and anti-inflammatory properties of C. chinensis were analyzed. It was found that the insect sample contains 50.46% moisture, 44.65% protein, 4.45% carbohydrate, 39.42% crude fats, 3.53% ash and 576.11 (Kcal/100 g) energy. Our study highlighted the presence of a significant amount of phenol and flavonoids. The C. chinensis hydro-alcoholic extract showed high antioxidant property and anti-inflammatory activity. GCMS analysis identified 61 volatile compounds. LC–MS analysis of hydroalcoholic extract of C. chinensis revealed the presence of compounds such as etodolac glucuronide, morphine 3-glucuronide, ecgonine, ecgonine methyl ester, sufentanil, and palmitoyl ethanololamide. These findings suggest that C. chinensis species can be employed as a valuable food source with excellent therapeutic properties. [ABSTRACT FROM AUTHOR]

The extraction and isolation of biomolecules were carried out from the active fractions of Muntingia calabura which exhibited stronger antibacterial activity. Among all the extracts, methanol and ethyl acetate extracts of M. calabura stem bark showed strong antimicrobial activity. Bioassay guided fractionation of methanol and ethyl acetate extracts acquired from the hardwood stem of M. calabura was done using silica gel column chromatography (100 – 200 mesh) to identify the active fractions and to eliminate the non-active fractions. Hexane and ethyl acetate were used as eluent in different ratios. 5,8-Dihydroxy-6,7,4′-trimethoxy flavones, 6,4′-dihydroxy-3′-propen chalcone, 7-(alloxy)-2-phenyl-4H-chromen-4-one, 7-hydroxy-4-oxo-2-phenyl-4Hchromen-8-carbaldehyde were isolated and identified as flavonols. The structures were established from IR, 1H NMR, 13C NMR, and mass spectral data. [ABSTRACT FROM AUTHOR]

5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-thiadiazole-2(3H)-thione] was synthesized by oxidative condensation in the presence of chloride ions. The structure of the resulting compound was identified by an x-ray crystal structure analysis, for which the crystallographic data were obtained. The anti-inflammatory activity of the synthesized disulfide was studied for the first time in a carrageenan edema model. 5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-diazole-2(3H)-thione] was shown to have anti-inflammatory and antiexudative activity at doses of 10 and 20 mg/kg. Its effect was close to that of the drug Nimesil. [ABSTRACT FROM AUTHOR]

Schiff bases of the tetrahydropyran series have been synthesized by the condensation of 2-(tetra-hydropyran-4-yl)ethanamines and tetrahydropyran-4-amine with 4-chloro, 4-fluoro-, and 4-(dimethylamino)-benzaldehydes and thiophene-2-carbaldehyde. The synthesized compounds showed lower anti-inflammatory, analgesic, and antipyretic activities than those of diclofenac and indomethacin used as reference drugs. [ABSTRACT FROM AUTHOR]

The public preference for healthy and natural products has prompted the development of innovative formulations for developing food products. Hence, in this study, Himalayan buckwheat (Fagopyrum esculantum Moench) was used to develop biscuits and was evaluated for their nutritional, structural, sensorial properties, and anti-inflammatory efficacy. Results revealed that buckwheat-incorporated biscuits are promising baked goods with high protein and phenolic content (12.20% and 39.86 µg gallic acid equivalents (GAE)/g, respectively). Water absorption index and Oil absorption index of biscuits varied significantly (p < 0.05) from 1.31 to 1.65 and 1.33 to 1.77 g/g, respectively. Moreover, after buckwheat incorporation, in vitro investigation on starch digestion showed a significant reduction in starch hydrolysis index, concomitantly decreasing the glycaemic index of biscuits from 94.08 to 59.80. During storage, the buckwheat addition decreased microbiological growth in biscuits as compared to the control. The study revealed that biscuits prepared with buckwheat significantly inhibited nitric oxide production, reactive oxygen species accumulation, and cytokines (tumour necrosis factor-α, interleukin-6) expression. Biscuits developed with up to 40% buckwheat flour showed improved nutritional quality with acceptable sensory attributes. Hence, Himalayan buckwheat exhibits potential anti-inflammatory activity, making it a promising functional food ingredient for further product development especially in the bakery industries. [ABSTRACT FROM AUTHOR]