Lipoxygenase Inhibitory Activity Research Articles

Biogenic Synthesis of Silver Nanoparticles Mediated by Aronia melanocarpa and Their Biological Evaluation.

In the present study, two A. melanocarpa berry extracts were used for the synthesis of silver nanoparticles (AgNPs). After the optimization of synthesis, the AgNPs were characterized using UV-Vis, FTIR, EDX, DLS, and STEM analyses. The stability in different media, phytotoxicity, as well as antimicrobial and antioxidant activities were also evaluated. The ideal synthesis conditions were represented by a 3 mM AgNO3 concentration, 1:9 extract:AgNO3 volume ratio, alkaline medium, and stirring at 40 °C for 120 min. The synthesis was confirmed by the surface plasmon resonance (SPR) peak at 403 nm, and the strong signal at 3 keV from the EDX spectra. FTIR analysis indicated that polyphenols, polysaccharides, and amino acids could be the compounds responsible for synthesis. Stability tests and the negative zeta potential values showed that phytocompounds also play a role in the stabilization and capping of AgNPs. The preliminary phytotoxicity studies on T. aestivum showed that both the extracts and their corresponding AgNPs had an impact on the growth of roots and shoots as well as on the microscopic structure of leaves. The synthesized AgNPs presented antimicrobial activity against S. aureus, E. coli, and C. albicans. Moreover, considering the results obtained in the lipoxygenase inhibition, the DPPH and hydroxyl scavenging activities, and the ferrous ion chelating assay, AgNPs exhibit promising antioxidant activity.

Rhododendron luteum Sweet Flower Supercritical CO2 Extracts: Terpenes Composition, Pro-Inflammatory Enzymes Inhibition and Antioxidant Activity.

Terpenes are plant secondary metabolites known for their anti-inflammatory and antioxidant activities. According to ethnobotanical knowledge, Rhododendron luteum Sweet was used in traditional medicine against inflammation. The present study was conducted to determine the triterpene profile and antioxidant and anti-inflammatory activity of supercritical CO2 (SC-CO2) extracts of Rhododendron luteum Sweet flower (RLF). An LC-APCI-MS/MS analysis showed the presence of eight pentacyclic triterpenes and one phytosterol in the extracts obtained with pure CO2 as well as CO2 with the addition of aqueous ethanol as a co-solvent. Among the compounds detected, oleanolic/ursolic acid, β-sitosterol and 3β-taraxerol were the most abundant. The extract obtained with pure SC-CO2 was additionally subjected to HS-SPME-GC-FID-MS, which revealed more than 100 volatiles, mainly eugenol, β-phenylethanol, dodecane, β-caryophyllene, estragole and (Z)- and (E)-cinnamyl alcohol, followed by δ-cadinene. The extracts demonstrated significant hyaluronidase inhibition and exhibited varying modes of lipoxygenase and xanthine oxidase inhibitory activities. The studies of RLF have shown that their SC-CO2 extracts can be a rich source of triterpenes with anti-inflammatory potential.

Physiological, metabolome, and transcriptome analysis revealed the effect of ethyl 3-amino-3-thioxopropanoate on the browning of fresh-cut banana during storage

The quality of fresh-cut bananas is often affected by surface browning, which does not meet consumer expectations. The ethyl 3-amino-3-thioxopropanoate (EAT) is an ethyl ester organic compound screened from Maillard reaction products that may have browning inhibition effects. However, there is still a lack of research on the practical application of EAT. This study investigated the impact of exogenous EAT on the browning process and the underlying mechanisms in fresh-cut banana through a comprehensive analysis involving physiological, metabolomic, and transcriptomic approaches. Treatment with EAT effectively mitigated the discoloration of the cut surface of slices and decreased the browning index by 74 % at the end of storage. Additionally, EAT application significantly reduced polyphenol oxidase activity, increased phenylalanine ammonia-lyase activity and total phenolic content, inhibited lipoxygenase activity, decreased malondialdehyde accumulation, enhanced antioxidant enzyme activity, and improved DPPH free radical scavenging rate to 68.49 %. Moreover, 839 metabolites were identified through non-targeted metabolomics analysis. Metabolomic and transcriptomic analysis further highlighted the importance of lipid metabolism, amino acid metabolism and secondary metabolites in influencing the sensitivity to post-cutting browning. EAT treatment also influenced the expression levels of key genes related to browning. Thus, it could be speculated that the mechanism by which EAT produces its anti-browning effect may be by reducing phenolase activity, improving levels of phenols and amino acids, enhancing the antioxidant capacity of the fruit, and alleviating membrane lipid peroxidation. In summary, this study provides valuable insights into the response mechanism employed by exogenous EAT to inhibit browning in freshly cut bananas. However, the application security and mass production methods of EAT still need further clarification.

One-Pot Syntheses and Enzyme Inhibition Studies of New C-28 Ester Derivatives of Betulinic Acid

Abstract: Betulinic acid and its various synthetic derivatives have been reported to possess diverse biological activities and some of these may serve as useful therapeutic agents for a variety of human disorders. In this perspective, we have now developed convenient one-pot syntheses of new C-28 esters (2-7) of betulinic acid by esterification of the carboxylic moiety of betulinic acid (1) with various alkylating agents. All the target compounds were subjected to enzyme inhibition studies to ascertain their possible therapeutic utility. Compound 5 showed very potent lipoxygenase inhibitory activity with an IC50 value of 13.2 μM, being much lower than the IC50 value of 22.4 μM of baicalein, which was used as the standard. Butulinic acid itself and compound 6 also showed significant inhibitory potential (IC50: 32.4 and 25.1 μM) against the same enzyme. The activities of both compounds 5 and 6 have been justified by intensive docking studies. Compounds 2 and 3 exhibited substantial inhibition (IC50: 18.4 and 21.5 μM) against the enzyme butrylcholinesterase, compared to serine used as the standard (IC50: 7.8 μM).

Anti-Inflammatory, Antioxidant, and Genoprotective Effects of Callus Cultures Obtained from the Pulp of Malus pumila cv Miller (Annurca Campana Apple).

Apples are rich in phytochemicals useful for human health. However, environmental factors can greatly affect the accumulation of these compounds. To face this problem, the callus culture technique was used to obtain large quantities of phytochemicals. Specifically, two callus cultures were obtained from ripe Annurca apple pulp (Malus pumila cv Miller) and cultivated under different light conditions: darkness and an 18-h photoperiod. The hydro-alcoholic extracts from the calli underwent analysis using GC-MS, GC-FID, and HPLC-DAD-ESI-MSn to determine the qualitative and quantitative content of phenolic and triterpenic acids. The study revealed the predominant presence of triterpenic compounds in both calli. Furthermore, we investigated their radical scavenging and antioxidant activities through DPPH, ABTS, ORAC assays, and lipoxygenase inhibition activity. Genoprotection was evaluated via nicking assay, and the anti-inflammatory effect was investigated via Griess assay on LPS-injured murine macrophages. All the analyses performed were compared with peel and pulp hydroalcoholic extracts. The results showed that both calli primarily show anti-inflammatory activity and moderate antioxidant effect and can protect DNA against oxidative stimuli. This data encouraged further research aimed at utilizing callus as a bioreactor to produce secondary metabolites for use in preventive and therapeutic applications to combat acute or chronic age-associated diseases.

An Overview of the Synthesis of 3,4-Fused Pyrrolocoumarins of Biological Interest.

3,4-Fused pyrrolocoumarins, synthetically prepared or naturally occurring, possess interesting biological properties. In this review, the synthetic strategies for the synthesis of the title compounds are presented along with their biological activities. Two routes are followed for that synthesis. In one, the pyrrole ring is formed from coumarin derivatives, such as aminocoumarins or other coumarins. In the other approach, the pyranone moiety is built from an existing pyrrole derivative or through the simultaneous formation of coumarin and pyrrole frameworks. The above syntheses are achieved via 1,3-dipolar cycloaddition reactions, Michael reaction, aza-Claisen rearrangement reactions, multi-component reactions (MCR), as well as metal-catalyzed reactions. Pyrrolocoumarins present cytotoxic, antifungal, antibacterial, α-glucosidase inhibition, antioxidant, lipoxygenase (LOX) inhibition, and fluorescent activities, as well as benzodiazepine receptor ability.

Tyrosinase, Elastase, Lipoxygenase Inhibition Activities and chemical composition of essential oils from Menthaspicata, Thymus vulgaris, Citrus aurantium and Juniperusphoenica from Tunisia

Tyrosinase, Elastase, Lipoxygenase Inhibition Activities and chemical composition of essential oils from Menthaspicata, Thymus vulgaris, Citrus aurantium and Juniperusphoenica from Tunisia

Protocatechuic acid as an inhibitor of lipid oxidation in meat

Lipid oxidation is the principal driver of meat and meat product deterioration during shelf life, causing the loss of fresh meat color, flavor, and aroma. Currently, synthetic antioxidants are used to prevent oxidation, but increasing consumer demand for natural ones leaves the industry with few alternatives. In this study, protocatechuic acid (PCA), known to have high antioxidant activity, was evaluated as a potential inhibitor of meat lipid oxidation. For this purpose, the antioxidant capacity and lipoxygenase (LOX) inhibitory activity of PCA were evaluated in vitro, and a set of four experiments was conducted, treating minced meat with water (control), lactic acid (LA), rosmarinic acid (RA) and PCA, at different concentrations (1–12 mg mL−1), depending on the experiment. The potential antioxidant effect of PCA when applied to meat cubes was also evaluated, as well as the potential of carboxymethyl cellulose (CMC) as a delivery system for PCA. The in vitro results showed that PCA is a potent antioxidant and an effective LOX inhibitor at 1 mg mL−1. PCA effect on meat lipid oxidation prevention was dose-dependent, and at 2 mg mL−1, it inhibited color change by 50% and lipid peroxidation by up to 70% when compared to water-treated samples, performing better than RA at 0.25 mg mL−1. These results suggest that PCA is a promising molecule to the meat industry as a natural preservative for meat and meat products directly or in a formulation.

Marrubiin Inhibits Peritoneal Inflammatory Response Induced by Carrageenan Application in C57 Mice.

Marrubiin is a diterpene with a long history of a wide range of biological activities. In this study, the anti-inflammatory effects of marrubiin were investigated using several in vitro and in vivo assays. Marrubiin inhibited carrageenan-induced peritoneal inflammation by preventing inflammatory cell infiltration and peritoneal mast cell degranulation. The anti-inflammatory activity was further demonstrated by monitoring a set of biochemical parameters, showing that the peritoneal fluid of animals treated with marrubiin had lower levels of proteins and lower myeloperoxidase activity compared with the fluid of animals that were not treated. Marrubiin exerted the most pronounced cytotoxic activity towards peripheral mononuclear cells, being the main contributors to peritoneal inflammation. Additionally, a moderate lipoxygenase inhibition activity of marrubiin was observed.

Studies on Phytochemicals and Bioactivities of Methanolic Extract of Leucaena leucocephala (Lam.) de Wit Fruit Pods

Objectives: The study was designed to screen for the phytochemical constituents, and investigate the antioxidant, antibacterial, and anti-inflammatory activities of Leucaena leucocephala fruit pods methanolic extract (LLFPME).
 Materials and Methods: Matured and dried fruit pods were pulverized and extracted with methanol using maceration method. The filtrate was concentrated in a rotary evaporator under reduced pressure to obtain powdery form termed LLFPME. The LLFPME was tested for the presence of phytochemicals using TLC and GC-MS technique. The phenolic and flavonoid contents of the extract were quantified; the antioxidant potential of the extract was examined using DPPH and H2O2 radical scavenging, metal chelating, FRAP and TAC assays. The anti-inflammatory potential was evaluated using the membrane stabilizing and lipoxygenase inhibitory activities while the antibacterial activity was investigated by determining the zone of inhibition, minimum inhibition concentration (MIC) and minimum bactericidal concentration (MBC) of extract against the test bacterial isolates.
 Results: TLC revealed the presence of flavonoids, saponins, alkaloids, tannins, and others while the GC-MS analysis also showed the presence of 27 compounds. It was shown that the LLFPME displayed measurable antioxidant activity by exhibiting DPPH and H2O2 free radical scavenging potential and dose dependent metal chelating ability. FRAP and TAC were estimated to be 14.88 ± 0.04 and 25.53 ± 0.21 mgAAE/g of extract, respectively. The extract protected the RBC membrane integrity of RBC subjected to heat and hypotonic stress; and inhibited the activity of lipoxygenase. The extract inhibited the growth of some bacterial strains but had no visible effect on Pseudomonas aeuroginosa growth. The zone of inhibition, MIC and MBC exhibited by the extract against susceptible test bacteria ranges between 13 - 17 mm, 2.5 - 20 and 20 mg/ml, respectively..
 Conclusion: It was concluded that LLFPME exhibited antioxidant potential through various mechanisms that possibly aided its ability to stabilize stressed cell membrane and similarly inhibited the growth of some bacterial strain.

Phytochemical characterization and multifaceted bioactivity assessment of essential oil from Ptychotis verticillata Duby: Anti-diabetic, anti-tyrosinase, and anti-inflammatory activity

The aim of this study is to explore the pharmacological properties of the essential oil derived from Ptychotis verticillata Duby (PVEO), a medicinal plant native to Morocco, focusing on its antidiabetic, anti-tyrosinase, and anti-inflammatory effects. Additionally, the study aims to characterize the phytochemical composition of PVEO and evaluate its potential as a natural therapeutic alternative for various health conditions. To achieve this, phytochemical analysis was conducted using gas chromatography-mass spectrometry (GC-MS). Furthermore, in vitro assessments were conducted to investigate PVEO's antidiabetic activity by inhibiting α-amylase, xanthine oxidase, and α-glucosidase. Tests were also undertaken to evaluate the anti-inflammatory effect of PVEO on RAW 264.7 cells stimulated by lipopolysaccharide (LPS), as well as its efficacy as an anti-tyrosinase agent and its lipoxygenase inhibition activity. The results of the phytochemical analysis revealed that PVEO is rich in terpene compounds, with percentages of 40.35 % γ-terpinene, 22.40 % carvacrol, and 19.77 % β-cymene. Moreover, in vitro evaluations demonstrated that PVEO exhibits significant inhibitory activity against α-amylase, xanthine oxidase, and α-glucosidase, indicating promising antidiabetic, and anti-gout potential. Furthermore, PVEO showed significant anti-tyrosinase activity, with an IC50 of 27.39 ± 0.44 μg/mL, and remarkable lipoxygenase inhibition (87.33 ± 2.6 %), suggesting its candidacy for dermatoprotection. Additionally, PVEO displayed a dose-dependent capacity to attenuate the production of NO and PGE2, two inflammatory mediators implicated in various pathologies, without compromising cellular viability. The findings of this study provide a solid foundation for future research on natural therapies and the development of new drugs, highlighting the therapeutic potential of PVEO in the treatment of gout, diabetes, pigmentation disorders, and inflammation.

Synthesis and Antioxidant Activities of Novel Pyrimidine Acrylamides as Inhibitors of Lipoxygenase: Molecular Modeling and In Silico Physicochemical Studies.

The pyrimidine ring is present in various biomolecules such as DNA and RNA bases, aminoacids, vitamins, etc. Additionally, many clinically used drugs including methotrexate and risperidone contain the pyrimidine heterocyclic scaffold as well. Pyrimidine derivatives present diverse biological activities including antioxidant and anticancer activities and can be considered as privileged scaffolds in drug discovery for the treatment of various diseases. Piperidine pyrimidine amides have gained significant attention due to their enzymatic inhibitory activity. Based on our experience and ongoing investigation on cinnamic acid derivatives, their hybrids and substituted pteridines acting as lipoxygenase inhibitors, antioxidants, anti-cancer, and anti-inflammatory agents a series of novel piperidine pyrimidine cinnamic acids amides have been designed and synthesized. The novel hybrids were studied for their antioxidant and anti-inflammatory potential. They exhibit moderate antioxidant activity in the DPPH assay which may be related to their bulkiness. Moreover, moderate to good lipid peroxidation inhibition potential was measured. With regards to their lipoxygenase inhibitory activity, however, two highly potent inhibitors out of the nine tested derivatives were identified, demonstrating IC50 values of 10.7 μM and 1.1 μM, respectively. Molecular docking studies to the target enzyme lipoxygenase support the experimental results.

Characterization of Phenolic Compounds from Pavetta graciliflora Wall. ex Ridl. (Rubiaceae) and their Lipoxygenase Inhibitory Activity

Characterization of Phenolic Compounds from Pavetta graciliflora Wall. ex Ridl. (Rubiaceae) and their Lipoxygenase Inhibitory Activity

Evaluation of antiproliferative effect of doxorubicin loaded zinc selenium quantum dots to MCF-7 cell lines by linagliptin functionalized lignin nanoparticles

In this research study, biocompatible linagliptin functionalized lignin (LL) nanomaterial is synthesized to deliver doxorubicin and zinc selenide quantum dots (ZnSe QDs). Afterward, doxorubicin and ZnSe QDs are loaded in LL to form LLQD-Doxo and analyzed its tumor cell proliferation. Drug carriers are characterized by SEM, FTIR, XRD, DSC, TGA, and zeta potential. In vitro studies are performed at different temperatures, pH, time, and concentration. According to the results, maximum drug encapsulation efficiency is 78.91 %, and rapid drug release is observed at 45 °C and pH 6.5. Linagliptin attached to lignin acts as an inhibitor of xanthine-based non-peptidomimetic DPP-4, an antiproliferative cancer agent. LLQD-Doxo is released from lignin by diffusion at pH 6.5, which is favorable for the tumor microenvironment (TME). LLQD-Doxo exhibits significant therapeutic, anti-inflammatory, antioxidant, cytotoxic, and increased antioxidant activity for MCF-7 cells. The best anti-inflammatory and lipoxygenase inhibitory activity is 48.05 ± 1.05 % and 76.93 ± 2.03 %, respectively. LLQD-Doxo shows antioxidant activity due to lignin polyphenolic compounds in DPPH assay and free radical scavenging activity with IC = 64 μg/mL. Cytotoxicity assay also shows promising results, i.e., 82.32 ± 3.68 % of viable cells after treatment with LLQD-Doxo. The results depict that this drug carrier is suitable for drug delivery at acidic pH and high temperature conditions in tumor cells compared to normal cells.

Bioactivity assay of Arundina graminifolia (D.Don) Hochr. extracts from diverse plant parts in Thailand: An assay-based investigation

This research involved surveying and collecting 16 samples of Arundina graminifolia from 8 different subpopulation areas. The main objectives were to analyze the preliminary phytochemical fingerprints and biological activity of the crude extracts obtained from various parts of the plant (roots, rhizomes, stems, and leaves). The findings indicated that rhizome extracts generally yielded a higher percentage of crude extract compared to the dry plant weight in comparison to other plant parts. Moreover, the Thin layer chromatography (TLC) fingerprint data revealed distinct compositions for each part of the plant, with rhizomes exhibiting more prevalent bands of compounds than other parts. Regarding antioxidant activity, the root and rhizome crude extracts from various populations displayed stronger inhibitory activity against DPPH, ABTS, and FRAP methods compared to stems and leaves. High total phenolic content was also found to effectively inhibit free radicals. The lipoxygenase inhibition test, which serves as an in vitro anti-inflammatory activity evaluation, demonstrated that most root extracts exhibited higher lipoxygenase inhibitory activity than the rhizome extracts at a concentration of 0.1 mg/mL. The antibacterial activity demonstrated that rhizome extracts from different regions exerted lower MIC and MBC values against all tested bacteria compared to the root extracts. The findings offer valuable information for selecting specific populations of A. graminifolia as potential sources of bioactive compounds for future nutraceutical applications.

Ginger essential oil-loaded hydrogels: preparation, characterization, cytotoxicity, antimicrobial and anti-inflammatory activity

ABSTRACT The present study aimed to develop ginger essential oil hydrogel formulations, using sodium carboxymethyl cellulose (Na CMC), Carbopol, and xanthan gum for dental and oromucosal infections. The physicochemical properties of the hydrogels were evaluated, and their bioadhesive characteristics were determined. Antimicrobial activity, cytotoxicity, and lipoxygenase (LOX) inhibitory activities of the essential oil and its formulations were investigated, respectively. The major components of ginger essential oil were confirmed as α-zingiberene (39.0%) and ar-curcumene (23.7%) by GC-FID and GC/MS analyses. The initial results showed that none of the tested gel formulations selected for the application were non-cytotoxic. According to antimicrobial and LOX enzyme activity studies, the essential oil-loaded xanthan gum gel (X3) was more effective compared to the essential oil itself. The initial formulation and biological evaluation studies concluded that ginger essential oil hydrogels (X3, C3) can be further developed for oral and dental health by providing a long residence time due to their bioadhesive properties.

HPLC/ESI-MS Characterization of Phenolic Compounds from Cnicus benedictus L. Roots: A Study of Antioxidant, Antibacterial, Anti-Inflammatory, and Anti-Alzheimer's Activity.

The phenolic composition of Cnicus benedictus roots from four Algerian regions was investigated. Extractions were performed in both hydro-methanolic (30 : 70, v/v) and hydro-ethanolic (30 : 70, v/v) solvents. Their efficiency was determined in terms of the qualitative and quantitative composition in phenolic compounds by HPLC-LC/MS of the different extracts isolated from C. Benedictus roots. Cnicus benedictus roots extract have been characterized by high content of phenolic compounds, where the trans chalcone, 2,3-dihydro flavone, 3-hydroxy flavone and cinnamic acid constitute the major components, in addition to fourteen minor acidic compounds and flavonoids as rutin. The hydro-methanolic extract was the richest in phenolic compounds yield from C benedictus. On the other hand, hydro methanolic (30 : 70, v/v) and hydro ethanolic (30 : 70, v/v) extracts exhibited a high anti-inflammatory activity by in vitro 5-lipoxygenase inhibitory activity (IC50 : 6.05±94.16 μg/mL) as well as by in silico docking according two methods. Likewise, anti-Alzheimer activity of extracts was confirmed by this last technique taking into account the major compounds identified. Antibacterial tests revealed interesting results compared to amoxicillin for the different regions studied with a high content in trans chalcone and 3-hydroxy Flavone.

Phytochemical analysis, GC–MS profile and determination of antibacterial, antifungal, anti-inflammatory, antioxidant activities of peel and seeds extracts (chloroform and ethyl acetate) of Tamarindus indica L

Tamarindus indica L., is widely used tree in ayurvedic medicine. Here, we aimed to understand the presence of important constituents in seeds and peel of Tamarind fruits and their biological activities. Hence, seeds and peel of Tamarind fruits are used for further extraction process by soxhlet method (chloroform and ethyl acetate solvents). Results suggest that the ethyl acetate extract (seeds) consists of terpenoids (72.29 ± 0.513 mg/g), phenolic content (68.67 ± 2.11 mg/g) and flavonoids (26.36 ± 2.03 mg/g) whereas chloroform extract (seeds) has terpenoids (42.29 ± 0.98 mg/g). Similarly, chloroform extract (peel) has terpenoids (25.96 ± 3.20 mg/g) and flavonoids (46.36 ± 2.03 mg/g) whereas ethyl acetate extract (peel) has terpenoids (62.93 ± 0.987 mg/g). Furthermore, anti-inflammation activity results revealed that the chloroform extract of peel was found to be more effective with IC50 of 226.14 µg/ml by protein denaturation analysis and with IC50 of 245.5 µg/ml on lipoxygenase inhibition activity. Chloroform extract (peel and seeds) shown better antioxidant activity using DPPH than ethyl acetate extract (peel and seeds). Ethyl acetate extract of seeds showed impressive potency by inhibiting the growth of fungus, Candida albicans. Additionally, ethyl acetate extract of seeds showed impressive potency inhibiting the growth of Escherichia coli than Bacillus cereus. GC–MS analysis shown the existence of diverse set of phytochemicals in each extract. Overall, comparative studies highlight the effectiveness of seeds extracts than peel extracts. Moreover, GC–MS results suggest that the seeds and peel extracts (chloroform and ethyl acetate) contains a wide range of compounds (including flavonoids, isovanillic acid, fatty acids and phenolic compounds) which can be utilized for therapeutic purpose.

Synthesis, molecular docking, analgesic, anti-inflammatory, and ulcerogenic evaluation of thiophene-pyrazole candidates as COX, 5-LOX, and TNF-α inhibitors.

The thiophene bearing pyrazole derivatives (7a-j) were synthesized and examined for their in vitro cyclooxygenase, 5-lipoxygenase, and tumour inducing factor-α inhibitory activities followed by the in vivo analgesic, anti-inflammatory, and ulcerogenic evaluations. The synthesized series (7a-j) were characterized using 1H NMR, 13C NMR, FT-IR, and mass spectral analysis. Initially, the compounds (7a-j) were evaluated for their in vitro cyclooxygenase, 5-lipoxygenase, and tumour inducing factor-α inhibitory activities and the compound (7f) with two phenyl substituents in the pyrazole ring and chloro substituent in the thiophene ring and the compound (7g) with two phenyl substituents in the pyrazole ring and bromo substituent in the thiophene ring were observed as potent compounds among the series. The compounds (7f and 7g) with effective in vitro potentials were further analyzed for analgesic, anti-inflammatory, and ulcerogenic evaluations. Also, to ascertain the binding affinities of compounds (7a-j), docking assessments were carried out and the ligand (7f) with the highest binding affinity was docked to know the interactions of the ligand with amino acids of target proteins.

Browning inhibition in fresh-cut Chinese water chestnut under high pressure CO2 treatment: Regulation of reactive oxygen species and membrane lipid metabolism.

Fresh-cut Chinese water chestnut (CWC) was treated with high pressure CO2 (HPCD) to inhibit the browning reactions, and the underlying mechanism was investigated in this study. Results showed that HPCD at 2MPa pressure significantly inhibited lipoxygenase activity and enhanced superoxide dismutase activity, leading to decreased malondialdehyde and H2O2 contents in surface tissue. Moreover, HPCD could reduce total phenols/flavonoids content of surface tissue. Compare with control, homoeriodictyol, hesperetin, and isorhamnetin contents of 2MPa HPCD-treated samples on day 10 were reduced by 95.72%, 94.31%, and 94.02%, respectively. Furthermore, HPCD treatment enhanced antioxidant enzyme activities, and improved the O2- scavenging ability and reducing power of inner tissue. In conclusion, by regulating ROS and membrane lipid metabolism, HPCD treatment with appropriate pressure could retard the biosynthesis of flavonoids and enzymatic oxidation of phenolic compounds in surface tissue, and enhance antioxidant activity of inner tissue, thereby, delaying the quality deterioration of fresh-cut CWC.