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Environmental concerns have driven the need to remove sulfur-containing compounds to an extremely low level for transportation fuels. Conventional hydrodesulfurization catalysts can be used to remove a significant portion of the sulfur from petroleum distillates for the blending of refinery transportation fuels. Removing the last traces of sulfur compounds where the sulfur atom is sterically hindered, as in multi-ring aromatic sulfur compounds, is a significant challenge. One recent area of innovation to remove sulfur from upgraded crude is oxidative desulfurization, a process that can operate under mild conditions and without the need for external H2. In this article, the mechanism, process, and the new inventions of selectively oxidative desulfurization are reviewed. [ABSTRACT FROM AUTHOR]

Introduction: Cancer is the second most widespread cause of mortality following cardiovascular disorders, and it imposes a heavy global burden. Nowadays, herbal nutraceutical products with a plethora of bioactive metabolites represent a foundation stone for the development of promising chemopreventive and anticancer agents. Certain members of the family Malvaceae have traditionally been employed to relieve tumors. The literature concerning the chemopreventive and anticancer effects of the plant species along with the isolated cytotoxic phytometabolites was reviewed. Based on the findings, comprehensive computational modelling studies were performed to explore the pharmacokinetic and pharmacodynamic profiles of the reported cytotoxic metabolites to present basis for future plant-based anticancer drug discovery., Methods: All the available information about the anticancer research in family Malvaceae and its cytotoxic phytometabolites were retrieved from official sources. Extensive search was carried out using the keywords Malvaceae, cancer, cytotoxicity, mechanism and signalling pathway. Pharmacokinetic study was performed on the cytotoxic metabolites using SWISS ADME model. Acute oral toxicity expressed as median lethal dose (LD 50 ) was predicted using Pro Tox 3.0 web tool. The compounds were docked using AutoDock Vina platform against epidermal growth factor receptor (EGFR kinase enzyme) obtained from the Protein Data Bank. Molecular dynamic simulations and MMGBSA calculations were performed using GROMACS 2024.2 and gmx_MMPBSA tool v1.5.2., Results: One hundred forty-five articles were eligible in the study. Several tested compounds showed safe pharmacokinetic properties. Also, the molecular docking study showed that the bioactive metabolites possessed agreeable binding affinities to EGFR kinase enzyme. Tiliroside (25), boehmenan (30), boehmenan H (31), and isoquercetin (22) elicited the highest binding affinity toward the enzyme with a score of -10.4, -10.4, -10.2 and -10.1 Kcal/mol compared to the reference drug erlotinib having a binding score equal to -9 Kcal/mol. Additionally, compounds 25 and 31 elicited binding free energies equal to -42.17 and -42.68 Kcal/mol, respectively, comparable to erlotinib., Discussion: Overall, the current study presents helpful insights into the pharmacokinetic and pharmacodynamic properties of the reported cytotoxic metabolites belonging to family Malvaceae members. The molecular docking and dynamic simulations results intensify the roles of secondary metabolites from medicinal plants in fighting cancer., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. The author(s) declared that they were an editorial board member of Frontiers, at the time of submission. This had no impact on the peer review process and the final decision., (Copyright © 2024 Sameh, Elissawy, Al-Sayed, Labib, Chang, Yu, Chang, Yang and Singab.)

Introduction: Pomegranate (Punica granatum L.) peels are rich in various bioactive compounds. Characterization of these compounds is crucial for the utilization of peel waste in industrial processing., Objective: The study aimed (1) to establish and compare the metabolic profiles of the peel of seven pomegranate cultivars and (2) to identify bioactive compounds contributing to the larvicidal activity against the third instar larvae of Culex pipiens., Materials and Methods: UPLC-ESI-MS/MS was utilized to analyze peel methanol extracts of different pomegranate cultivars. The larvicidal activity was determined by calculating the larval mortality among the third instar larvae of C. pipiens. Multivariate data analysis was conducted to identify the metabolites that exhibited a larvicidal effect., Results: A total of 24 metabolites, including hydrolyzable tannins, flavonoids, and alkaloids, were tentatively identified in both negative and positive ionization modes. The extract of cultivar 'Black' exhibited the most potent larvicidal effect with LC 50 values of 185.15, 156.84, and 138.12 ppm/mL after 24, 48, and 72 h of treatment, respectively. By applying chemometric techniques, the larvicidal activity could be directly correlated to the bioactive compounds punicalagin, quercetin-O-rhamnoside, quercetin-O-pentoside, and galloyl-HHDP-glucose., Conclusion: The present study implemented UPLC-ESI-MS/MS and chemometric techniques as potential tools for metabolomics analysis and differentiation between peels of different pomegranate cultivars. In addition, cultivar 'Black' extract could be a promising natural insecticide against mosquitoes since it is rich in bioactive compounds with larvicidal activity., (© 2023 John Wiley & Sons, Ltd.)

Background: Endophytic Aspergillus species produce countless valuable bioactive secondary metabolites. In the current study, Aspergillus flavus an endophyte from the soft coral Sarcophyton ehrenbergi was chemically explored and the extracted phytoconstituents were subsequently evaluated for antimicrobial activity. This is accomplished by employing nuclear magnetic resonance (NMR) spectroscopy and computational techniques. Additionally, An in vitro anticancer analysis of A. flavus total extract against breast cancer cells (MCF-7) was investigated., Result: Six compounds were separated from the crude alcohol extract of the endophytic Aspergillus flavus out of which anhydro-mevalonolactone was reported for the first time. The anti-fungal and anti-Helicobacter pylori properties of two distinct compounds (Scopularides A and B) were assessed. Additionally, computational research was done to identify the binding mechanisms for all compounds. Both the compounds were found to be active against H. pylori with minimum inhibitory concentration (MIC) values ranging from 7.81 to 15.63 µg/ mL as compared with clarithromycin 1.95 µg/ mL. Scopularides A was potent against both Candida albicans and Aspergillus niger with MIC values ranging from 3.9 to 31.25 µg/ mL, while scopularides B only inhibits Candida albicans with MIC value of 15.63 µg/ mL and weak inhibitory activity against A. niger (MIC = 125 µg/ mL). Furthermore, cytotoxic activity showed a significant effect (IC 50 : 30.46 mg/mL) against MCF-7 cells., Conclusion: Our findings report that cytotoxic activity and molecular docking support the antimicrobial activity of Aspergillus flavus, which could be a promising alternative source as a potential antimicrobial agent., (© 2023. The Author(s).)

Alzheimer's disease (AD) is a major health problem. Cholinergic transmission is greatly affected in AD. Phytochemical investigation of the alkaloid rich fraction (AF) of Erythrina corallodendron L leaves resulted in isolation of five known alkaloids: erysodine, erythrinine, 8-oxoerythrinine, erysovine N-oxide and erythrinine N-oxide. In this study, eysovine N-oxide was reported for the second time in nature. AF was assayed for cholinesterase inhibition at the concentration of 100 μg mL -1 . AF showed a higher percent inhibition for butyrylcholinesterase enzyme (BuChE) (83.28 %) compared to acetylcholinesterase enzyme (AChE) (64.64 %). The isolated alkaloids were also assayed for their anti-BuChE effect. In-silico docking study was done for the isolated compounds at the binding sites of AChE and BuChE to determine their binding pattern and interactions, also molecular dynamics were estimated for the compound displaying the best fit for AChE and BuChE. In addition, ADME parameters and toxicity were predicted for the isolated alkaloids compared to donepezil., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

Cestrum diurnum L. (Solanaceae) is a fragrant ornamental tree cultivated in different parts around the world. In this study, the essential oil (EO) of the aerial parts was extracted by hydrodistillation (HD), steam distillation (SD) and microwave-assisted hydro-distillation (MAHD). GC/MS analysis of the three EOs revealed that phytol represents the major component in SD-EO and MAHD-EO (40.84 and 40.04 %, respectively); while in HD-EO it only represented 15.36 %. The SD-EO showed a strong antiviral activity against HCoV-229E with IC 50 of 10.93 μg/mL, whereas, MAHD-EO and HD-EO showed a moderate activity with IC 50 values of 119.9 and 148.2 μg/mL, respectively. The molecular docking of EO major components: phytol, octadecyl acetate and tricosane showed a strong binding to coronavirus 3-CL (pro). Moreover, the three EOs (50 μg/mL) decreased the levels of NO, IL-6 and TNF-α and suppressed IL-6 and TNF-α gene expression in LPS-induced inflammation model in RAW264.7 macrophage cell lines., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

The COVID-19 pandemic caused a huge health crisis all over the globe. SARS-CoV-2 is the virus responsible for the disease and it is highly contagious leaving millions of confirmed infected cases and a dangerous death toll. Carica papaya is a tropical plant known for its antiviral activity since it possesses different classes of compounds that are believed to combat various viral classes. In this study, the extracts prepared from C. papaya leaves cultivated in Egypt were evaluated for their anti-SARS-CoV-2 activity using crystal violet assay and for their cytotoxicity through MTT assay. The total methanolic extract, n -hexane, ethyl acetate, and n -butanol fractions of papaya leaves were used in the study and the results revealed that the n -hexane fraction has a high anti-SARS-CoV-2 activity with an IC 50 value = 1.98 μg mL -1 . Moreover, it also showed a high selectivity index value = 104.7. Dereplication of the secondary metabolites in the crude methanolic extract of C. papaya leaves revealed the presence of different classes of compounds including sterols, terpenes, fatty acid, alkaloids and flavonoids that are known to possess antiviral activities against various classes of viruses. The current study was assisted by molecular docking, molecular dynamics simulation and MM-PBSA calculations for the annotated compounds against 6 SARS-CoV-2 target proteins. The results of these in silico -based investigations showed high to moderate binding on the targeted proteins. This postulation may instigate further research studies concerning the compounds responsible for this high anti-SARS-CoV-2 activity of the n -hexane fraction of C. papaya leaves., Competing Interests: The authors declare that they have no conflicts of interests., (This journal is © The Royal Society of Chemistry.)

Bontia daphnoides L. has been utilized in traditional medicine for treatment of herpes, cough and colds. The aim of this study was to analyze the volatile constituents of this plant by GC/MS (Gas Chromatography coupled to Mass Spectrometry) and to assess their antiviral activity. A total of 64 compounds were identified where dehydroepingaione represented 83.60, 72.36, 58.78 and 34.18% in the leaves, stems, flowers and fruits, respectively. Principal component and hierarchical cluster analysis revealed the discrimination of the organs as the leaves and stems were distributed in the same cluster in contrast to the flowers and fruits. Furthermore, the antiviral activity was assessed where the oils of leaves and stems exhibited potent antiviral activity displaying IC 50 of 11.98, 12.62 µg/ml against HSV-1 and 13.34, 14.50 µg/ml against CoxB4, respectively. Dehydroepingaione was isolated from the n-hexane fraction of the leaves and showed activity against HSV-1 and CoxB with IC 50 of 24.46 and 25.32 µg/ml, respectively. Molecular modelling studies illustrated that the major compounds showed good affinity towards HSV type-1 thymidine kinase. Therefore, it can be concluded that the oils from B. daphnoides have promising antiviral activity that may be attributed to the major oxygenated sesquiterpenes., (© 2022. The Author(s).)

Leucophyllum frutescens (Scrophulariaceae) is a medicinal plant of Mexican traditional medicine. The aim of this study was to analyse the volatile components from the leaves and flowers by GC/MS and to assess their anti-aging activity for the first time. A total of 30 compounds were identified where 1-octen-3-ol (73.56%) and D-limonene (11.12%) represented the major ingredients in the leaves, while n -heneicosane (32.30%) and dehydroepingaione (15.15%) were the major components in the flowers. In vitro anti-aging activity was measured via assessing collagenase and elastase inhibition. Essential oils from the leaves and flowers showed potential collagenase inhibitory activity with IC 50 of 55.7 and 47.4 µg/mL. However, the oils from the leaves and flowers showed moderate anti-elastase activity with IC 50 of 60.8 and 97.7 µg/mL. Therefore, the oil of Leucophyllum frutescens could afford a promising natural anti-aging drug.

Molybdenum blues (MBs) are a distinct class of polyoxometalates, exhibiting versatile/impressive architectures and high structural flexibility. In acidified and reduced aqueous environments, isopolymolybdates generate precisely organizable building blocks, which enable unique nanoscopic molecular systems (MBs) to be constructed and further fine-tuned by hetero elements such as lanthanide (Ln) ions. This Review discusses wheel-shaped MB-based structure types with strong emphasis on the ∼30 Ln-containing MBs as of August 2021, which include both organically hybridized and nonhybridized structures synthesized to date. The spotlight is thereby put on the lanthanide ions and ligand types, which are crucial for the resulting Ln-patterns and alterations in the gigantic structures. Several critical steps and reaction conditions in their synthesis are highlighted, as well as appropriate methods to investigate them both in solid state and in solution. The final section addresses the homogeneous/heterogeneous catalytic, molecular recognition and separation properties of wheel-shaped Ln-MBs, emphasizing their inimitable behavior and encouraging their application in these areas., Competing Interests: The authors declare no competing financial interest., (© 2022 The Authors. Published by American Chemical Society.)

Culex pipiens mosquitoes are vectors to many viruses and can transmit diseases such as filariasis and avian malaria. The present study evaluated the larvicidal activity of marine-derived endophytic fungi Aspergillus nomius and Aspergillus flavus from the soft coral Sarcophyton ehrenbergi along with two known cyclodepsipeptide compounds, scopularide A ( 1 ) and B (2), isolated from A. flavus extract, against third-instar larvae of C. pipiens , using distilled water as a negative control and toosenedanin as a positive control. The structures of the isolated compounds were confirmed by various spectroscopic analyses. The lethal concentrations (LC 50 and LC 90 ) were calculated by probit analysis. Scopularide A was the most potent after 96 h treatment, with LC 50 and LC 90 values of 58.96 and 994.31 ppm, respectively, and with 82.66% mortality at a concentration of 300 ppm. To unravel the biochemical mechanism of the tested extracts and compounds, their effects against protease, chitinase, phenoloxidases and lipase enzymes from the whole-body tissue of C. pipiens were evaluated after 72 h treatment at LC 50 dose. Superior activity was observed for A. flavus extract against all tested enzymes. A molecular docking study was conducted for scopularide A and B on the four tested enzymes, to further verify the observed activity. Results revealed good binding affinities for both compounds as compared to the docked ligands, mainly via a number of hydrogen bonds. This was the first study to report the isolation of endophytic fungi A. flavus and A. nomius from the marine soft coral S. ehrenbergi. The endophytic fungal extract of A. flavus was found to be a promising source for a natural larvicidal agent against C. pipiens populations.

The hybridized lanthanide-containing molybdenum blue (Ln-MB) wheel Na 4 [Mo 2 O 2 (OH) 4 (C 6 H 4 NO 2 ) 2 ] 2 [Mo 120 Ce 6 O 366 H 12 (OH) 2 (H 2 O) 76 ]∼200H 2 O ({Mo 2 (C 6 H 4 NO 2 ) 2 } 2 {Mo 120 Ce 6 }) was assembled in an aqueous one-pot synthesis. The Ln-MB was hybridized with 2-picolinic acid through the generation of the organometallic counter-ion [Mo 2 O 2 (OH) 4 (C 6 H 4 NO 2 ) 2 ] 2+ . Control experiments demonstrated that the position of the carboxylic acid group (2-position to the N atom) in the hybridization component is critical in yielding single crystals of Ln-MB. In addition to single-crystal X-ray diffraction (XRD) analysis, which revealed a `Japanese rice-ball'-shaped Ln-MB as the anion, elemental analyses, IR spectroscopy, and thermogravimetric analysis (TGA) were performed to confirm its structure and composition. Bond-valence-sum calculations (BVS) revealed that {Mo 2 (C 6 H 4 NO 2 ) 2 } 2 {Mo 120 Ce 6 } is composed of a 24-electron reduced anionic ring, which was confirmed by Vis-NIR spectroscopy., (open access.)

Background : Essential oils represent a major class of natural products which are known for their antimicrobial activity. This study aimed to determine the composition of four Piper essential oils by gas chromatography mass spectrometry, attenuated total reflection infrared, and chemometric analysis. Results : Monoterpene was the most predominant class in Piper nigrum and white pepper (87.6 and 80%, respectively) with the dominance of α-pinene, β-pinene, 3-carene, limonene, and β-caryophyllene. Sesquiterpenes represented 50, 19.6, and 12.3% of the essential oils of Piper longum , white pepper, and P. nigrum , respectively. Unlike other species, Piper cubeba oil was found to be rich in aromatics (59%), with eugenol (10.7%) and methyl eugenol (47.4%) representing the major components along with β-myrcene (21.2%) and 1,8-cineole (6.4%). Only P. longum essential oil comprised about 18.2% of alkanes and 13.6% of alkenes. Application of chemometric analysis utilizing GC/MS and ATR-IR data displayed the same segregation pattern where both principal component analysis and hierarchal cluster analysis revealed that white pepper was most closely related to P. nigrum while being completely discriminated from other Piper species. The Piper oils showed promising inhibitory effects on Helicobacter pylori . P. longum oil recorded the most efficient anti- Helicobacter activity [minimum inhibitory concentration (MIC) value of 1.95 μg/ml, which is the same as the MIC of clarithromycin], followed by the oil of white pepper (MIC = 3.90 μg/ml), while P. cubeba and P. nigrum produced the lowest activity (MIC value of 7.81 μg/ml). Conclusion: Piper essential oils can be used as nutritional supplements or therapeutic drugs to protect against H. pylori infection., Competing Interests: The authors declare no competing financial interest., (© 2021 The Authors. Published by American Chemical Society.)

Introduction: The leaves and cones of Pinus plants as well as their essential oils have been used in traditional medicine for the treatment of several ailments., Objectives: Phytochemical discrimination of Pinus species and investigation of their anti-Helicobacter pylori activity in vitro and in silico., Materials and Methods: Gas chromatography-mass spectrometry (GC-MS) and attenuated total reflectance infrared (ATR-IR) metabolic profiling of the essential oils of Pinus species. Principal component analysis (PCA) and hierarchal cluster analysis (HCA) were applied for discrimination and segregation of Pinus species., Results: GC-MS revealed the presence of 76 constituents, where monoterpenes represented the major class with the dominance of α-pinene (72%) followed by β-pinene (16%) for P. canariensis. β-Pinene was the dominant component in P. pinea (24%) followed by terpinolene (11%). α-Pinene (17%) and caryophyllene (12%) were the major components in P. halepensis, while, 3-carene (33%) and α-pinene (17%) represented the major constituents of P. roxburghii oil. By applying PCA and HCA on GC-MS and ATR-IR data analysis, ATR-IR displayed much better discrimination for Pinus species. The pine oils showed promising inhibitory effects on Helicobacter pylori. Furthermore, in silico molecular modelling was carried out where the calculated free binding energies of phytochemicals identified ranged from -33.71 to -19.67 kcal/mol for urease and -41.18 to -16.57 kcal/mol for shikimate kinase. This suggests favourable binding of pine essential oil components to both enzymes, thus explaining their potential inhibitory activity on H. pylori., Conclusion: GC-MS and ATR-IR based metabolic analyses could discriminate between Pinus species. Pine essential oils can be used as promising therapeutic drugs to protect against H. pylori infection., (© 2021 John Wiley & Sons, Ltd.)

The ever-growing interest in sustainable energy sources leads to a search for an efficient, stable, and inexpensive homogeneous water oxidation catalyst (WOC). Herein, the PO 4 3- templated synthesis of three abundant-metal-based germanotungstate (GT) clusters Na 15 [Ge 4 PCo 4 (H 2 O) 2 W 24 O 94 ] ⋅ 38H 2 O (Co 4 ), Na 2.5 K 17.5 [Ge 3 PCo 9 (OH) 5 (H 2 O) 4 W 30 O 115 ] ⋅ 45H 2 O (Co 9 ), Na 6 K 16 [Ge 4 P 4 Co 20 (OH) 14 (H 2 O) 18 W 36 O 150 ] ⋅ 61H 2 O (Co 20 ) with non-, quasi-, or full cubane motifs structurally strongly reminiscent of the naturally occurring {Mn 4 Ca} oxygen evolving complex (OEC) in photosystem II was achieved. Under the conditions tested, all three GT-scaffolds were active molecular WOCs, with Co 9 and Co 20 outperforming the well-known Na 10 [Co 4 (H 2 O) 2 (PW 9 O 34 ) 2 ] {Co 4 P 2 W 18 } by a factor of 2 as shown by a direct comparison of their turnover numbers (TONs). With TONs up to 159.9 and a turnover frequency of 0.608 s -1 Co 9 currently represents the fastest Co-GT-based WOC, and photoluminescence emission spectroscopy provided insights into its photocatalytic WOC mechanism. Cyclic voltammetry, dynamic light scattering, UV/Vis and IR spectroscopy showed recyclability and integrity of the catalysts under the applied conditions. The experimental results were supported by computational studies, which highlighted that the facilitated oxidation of Co 9 was due to the higher energy of its highest occupied molecular orbital electrons as compared to Co 4 ., (© 2021 The Authors. ChemSusChem published by Wiley-VCH GmbH.)

Oxidative stress has been identified as an underlying factor in the development of insulin resistance, β-cell dysfunction, impaired glucose tolerance and type 2 diabetes mellitus and it also play major role in kidney stone formation. The present study is aimed to elucidate the in vitro nephroprotective activity of two isoflavonoid glycosides, tectorigenin 7- O- β-D-glucosyl-(1→6)-β-D-glucoside ( 1 ) and tectorigenin 7- O -β-D-glucosyl-4'- O -β-D-glucoside ( 2 ) isolated from the n -BuOH fraction of Iris spuria L. (Zeal) rhizome MeOH extract against oxalate and high glucose-induced oxidative stress in NRK-49F cells. The results revealed that compounds 1 and 2 significantly increased the antioxidant enzyme activities and decreased MDA levels in both oxalate and high glucose stress. Treatment with these phytochemicals effectively down-regulated expression of crystal modulator genes and pro-fibrotic genes in oxalate and high glucose-mediated stress respectively. This study indicates cytoprotective, antioxidant, anti-urolithic and anti-diabetic effects of compounds 1 and 2 against oxalate and high glucose stress.[Figure: see text].

The plants belonging to the genus Vicia are of great interest as a source of many bioactive compounds and micronutrients. A snapshot of their cultivation, habitat, main components, from which essential oils can be obtained, is given. The traditional medicinal uses of Vicia plants are also reported, as well as the wide spectrum of the main biological activities attributed to Vicia plants is discussed regarding potential health beneficial properties, in particular anti-Parkinson, anticholinesterase, antidepressant, anticonvulsant, antimicrobial, cytotoxic, antioxidant, antiinflammatory and antinociceptive, antidiabetic, antihemolytic, anticoagulant, estrogenic, diuretic, antihypoxic activities., (© 2020 John Wiley & Sons Ltd.)

We report on a family of five new 4f- and 4d-doped sandwich-type germanotungstates with the general formula [( n -C 4 H 9 ) 4 N] l / m H 2 [(M(H 2 O) 3 )(γ-GeW 10 O 35 ) 2 ]·3(CH 3 ) 2 CO [M(H 2 O) 3 (GeW 10 ) 2 ] (M = Ce III , Nd III , Gd III , Er III , l = 7; Zr IV , m = 6), which have been synthesized at room temperature in an acetone-water mixture. Among the compound series, [Zr(H 2 O) 3 (GeW 10 ) 2 ] 8 - , which has been obtained in the presence of 30% H 2 O 2 , represents the first example of a 4d-substituted germanotungstate incorporating the intact dilacunary [γ-Ge IV W 10 O 36 ] 8- building block. All compounds were characterized thoroughly in the solid state by single-crystal and powder X-ray diffraction (XRD), IR spectroscopy, thermogravimetric analysis (TGA), and elemental analysis and in solution by NMR and UV-vis spectroscopy. The phosphoesterase activity of [Ce(H 2 O) 3 (GeW 10 ) 2 ] 9- and [Zr(H 2 O) 3 (GeW 10 ) 2 ] 8- toward the model substrates 4-nitrophenyl phosphate (NPP) and O , O -dimethyl O -(4-nitrophenyl) phosphate (DMNP) was monitored with 1 H- and 31 P-NMR spectroscopy revealing an acceleration of the hydrolytic reaction by an order of magnitude ( k corr = 3.44 (±0.30) × 10 -4 min -1 for [Ce(H 2 O) 3 (GeW 10 ) 2 ] 9- and k corr = 5.36 (±0.05) × 10 -4 min -1 for [Zr(H 2 O) 3 (GeW 10 ) 2 ] 8- ) as compared to the uncatalyzed reaction ( k uncat = 2.60 (±0.10) × 10 -5 min -1 ). [Ce(H 2 O) 3 (GeW 10 ) 2 ] 9- demonstrated improved antibacterial activity toward Moraxella catarrhalis (MIC 32 μg/mL), compared to the unsubstituted [GeW 10 O 36 ] 8- POM (MIC 64 μg/mL).

Ellagitannins have a marked antioxidant effect and can prevent liver injury induced by free radicals. An undescribed ellagitannin named styphelioidin was isolated from Melaleuca styphelioides Sm. The structure of styphelioidin was elucidated by using various spectroscopic methods. The hepatoprotective activity of styphelioidin (25, 50, and 100 μM) was tested using the CCl 4 -challenged HepG2 cell model by measuring alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in HepG2 cells treated with styphelioidin for 1 h followed by 40 mM CCl 4 . Glutathione (GSH), superoxide dismutase activity (SOD) and lipid peroxidation (MDA) were evaluated to determine the mechanisms of the hepatoprotective activity. Styphelioidin significantly reduced the levels of ALT, AST, and MDA at all tested concentrations. Moreover, it conferred a marked increase in the GSH levels and the SOD activity compared to the CCl 4 -treated groups. Styphelioidin also exerted DPPH· radical-scavenging effects with an IC 50 value of 3.67 μM. Results indicated the hepatoprotective therapeutic potential of styphelioidin comparable to silymarin. Moreover, anti-inflammatory activity was assessed and styphelioidin inhibited fMLF/CB-induced elastase release in human neutrophils with IC 50 2.51 μM. Cell-free experiments with human neutrophil elastase indicated a direct enzymatic inhibitory effect of styphelioidin on the enzyme activity (IC 50 2.58 μM). The potential of styphelioidin to interact with human neutrophil elastase binding sites was further confirmed by molecular docking of styphelioidin into human neutrophil elastase crystal structure using AutoDock 4.2. Styphelioidin represents a potent hepatoprotective and antioxidant agent with effects on ALT, AST, MDA, GSH, and SOD comparable to silymarin. The beneficial anti-elastase properties hold the potential for drug development against elastase-related inflammatory diseases. This study highlights a promising natural hepatoprotective and anti-inflammatory candidate derived from M. styphelioides., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Anthocyanins are natural phenolic pigments with biological activity. They are well-known to have potent antioxidant and antiinflammatory activity, which explains the various biological effects reported for these substances suggesting their antidiabetic and anticancer activities, and their role in cardiovascular and neuroprotective prevention. This review aims to comprehensively analyze different studies performed on this class of compounds, their bioavailability and their therapeutic potential. An in-depth look in preclinical, in vitro and in vivo , and clinical studies indicates the preventive effects of anthocyanins on cardioprotection, neuroprotection, antiobesity as well as their antidiabetes and anticancer effects., (Copyright © 2020 Salehi, Sharifi-Rad, Cappellini, Reiner, Zorzan, Imran, Sener, Kilic, El-Shazly, Fahmy, Al-Sayed, Martorell, Tonelli, Petroni, Docea, Calina and Maroyi.)

Genus Erythrina (Fabaceae) comprises several species, which are widely distributed in tropical and subtropical regions of the world. The plants of this genus exhibited significant role in traditional medicine targeting different diseases. Alkaloids and flavonoids were reported as the chief bioactive constituents of this genus with a wide range of biological activities. About 143 alkaloids were isolated from Erythrina sp. Anticonvulsant, anxiolytic, curare-like activity, insecticidal and cytotoxic activities were reported for Erythrina sp. alkaloids. The present work is an overview of the isolated alkaloids from Erythrina sp. with their reported biological activities.[Figure: see text] Abbreviations: CHCl3: Chloroform; CNS: Central nervous system; DCM: Methylene chloride; DPPH: 2,2-Diphenyl-1-picrylhydrazyl; E.: Erythrina ; ERα/β: Estrogen receptors α/β; EtOAc: Ethyl acetate; EtOH: Ethanol; Hep-G2: Human liver carcinoma cell lines; HIV: Human immunodeficiency virus; HL-60: Human promyelocytic leukemia cells; K-562: Human immortalized myelogenous leukemia cell line; LPS: Lipopolysaccharide; MeOH: Methanol; MOLT-4: Acute lymphoblastic leukemia cell line; nAChRs: nicotinic acetylcholine receptors; NO: Nitric oxide; NREM: non-rapid eye movement; Pet. ether: Petroleum ether; RBA: Receptor binder affinity; TRAIL: Tumor necrosis factor (TNF)-related apoptosis-inducing ligand.

The genus Achillea genus houses more than 100 species, a number of them are popularly used in traditional medicine for spasmodic gastrointestinal, gynecological and hepatobiliary disorders, hemorrhages, pneumonia, rheumatic pain, inflammation, wounds healing etc. Members of the genus contain a wide variety of volatile and non-volatile secondary metabolites, including terpenes, polyphenols, flavonoids and others. Multiple studies have assessed the biological effects and other aspects of Achillea spp. In a number of preclinical studies, Achillea plants and their essential oils have demonstrated promising antibacterial properties against a number of human and plant pathogens. Besides, the plants have displayed strong antioxidative and potent anti-proliferative and anticancer properties in various cellular and animal models. Achillea plants have widely been used as food preservative in food industry. Clinical studies have indicated its potential against multiple sclerosis (MS), irritable bowel syndrome (IBS), ulcerative colitis, episiotomy wound, primary dysmenorrhea, oral mucositis etc. The present work focuses to provide a brief overview on folk knowledge, phytochemistry, biological activity and applications of Achillea plants. There is a close relationship between the traditional ethnobotanical usage and pharmacological and clinical data from different Achillea spp. The application of Achillea plants and their extracts seems to be a promising alternative for antimicrobial and antioxidant purposes in food, pharmaceutical and cosmetic industries.

The first synthetic pathway using a series of four nonlacunary 4f-heterometal-substituted polyoxotungstate clusters Na 21 [(Ln(H 2 O)(OH) 2 (CH 3 COO)) 3 (WO 4 )(SbW 9 O 33 ) 3 ]· n H 2 O ( NaLnSbW 9 ; Ln = Tb III , Dy III , Ho III , Er III , Y III ) as precursors for the directed preparation of nine new 3d-4f heterometallic tungstoantimonates K 5 Na 12 H 3 [TM(H 2 O)Ln 3 (H 2 O) 5 (W 3 O 11 )(SbW 9 O 33 ) 3 ]· n H 2 O ( KTMLnSbW 9 ; TM = Co II , Ni II ; Ln = Tb III , Dy III , Ho III , Er III , Y III ) has been developed. Systematic studies revealed an increased K content in the aqueous acidic reaction mixture to be the key step in the cation-directed preparation of 3d-4f compounds; among those, the Co-containing members represent the first examples of KCoLnSbW 9 (Ln = Tb III , Dy III , Ho III , Er III , Y III ) heterometallic tungstoantimonates exhibiting the SbW 9 building block. All 13 compounds have been characterized thoroughly in the solid state by powder and single-crystal X-ray diffraction (XRD), revealing a cyclic trimeric polyoxometalate architecture with three SbW 9 units encapsulating a planar triangle of Ln III ions in the case of NaLnSbW 9 and a heterometallic core of one TM II and three Ln III for KTMLnSbW 9 (TM = Co II , Ni II ; Ln = Tb III , Dy III , Ho III , Er III , Y III ). The results obtained by XRD are supplemented by complementary characterization methods in the solid state such as IR spectroscopy, thermogravimetric analysis, and elemental analysis as well as in solution by UV-vis spectroscopy. Detailed magnetic studies on the representative compounds KTMDySbW 9 (TM = Co II , Ni II ) and KCoYSbW 9 of the series revealed field-induced slow magnetic relaxation.

Cupressus macrocarpa is a windbreak tree and is reported to have various cytotoxic effects. A natural product study on the leaves of C. macrocarpa has yielded ten secondary metabolites, including three new diterpenoids (1-3), four known diterpenoids (4-7), and three known lignans (8-10). The structures of all isolated compounds were elucidated via the interpretation of spectroscopic methods, especially 2D NMR and mass analyses. In the cytotoxic assays, compounds 1-3 and 7-10 showed inhibition effect against HepG2, MDA-MB-231, and A549 cells with IC 50 values ranging from 0.004 to 19.9 μg/mL. Moreover, the anti-inflammatory assays revealed that (-)-matairesinol (8) had significant inhibitory activities on superoxide anion generation (IC 50  = 2.7 ± 0.3 μM) and elastase release (IC 50  = 6.6 ± 0.7 μM)., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Ethnopharmacological Relevance: Members of the genus Erythrina have been traditionally used in the treatment of various ailments such as inflammation and gastrointestinal disorders. Erythrina speciosa (Fabaceae) is a spiny, deciduous shrub or small tree native to Southern America in Brazil. It is cultivated in Africa and Asia. The traditional usage of E. speciosa indicated its antibacterial, analgesic, and anti-inflammatory activities., Aim of the Study: Evaluation of the phytochemical constituents, gastroprotective effects and possible mechanism of action of the ethyl acetate fraction obtained from the methanol extract of E. speciosa leaves (ESLE)., Materials and Methods: Chemical characterization of ESLE was done using high performance liquid chromatography coupled to mass spectrometry (HPLC-MS). The gastroprotective activity of ESLE was evaluated using ethanol-induced gastric-ulcer model in rats. Rats were pre-treated with ESLE 25, 50 and 100 mg/kg 1 h before the administration of absolute ethanol. Histological analysis, mucin content, and total acidity were evaluated. The possible mechanism of action of ESLE was studied through the examination of oxidative stress and inflammatory markers, PGE2, and NF-κB, iNOS, COX-2, and HSP-70 immunoexpression. In vitro, anti-Helicobacter pylori activity of ESLE was also studied using micro-well dilution method., Results: Fourteen compounds were tentatively identified including alkaloids, flavonoids, and saponins. ESLE exerted a powerful gastroprotective effect. The pre-treatment with ESLE at different doses resulted in a significant reduction in gastric lesions and significant elevation in the mucin production. These effects could be partially mediated by the potent anti-inflammatory activity of ESLE as evidenced by the significant reduction in the immunoexpression of NF-κB, COX-2, iNOS and the reduction in the pro-inflammatory marker, TNF-α. ESLE counteracted the ethanol-induced oxidative stress by increasing the levels of depleted GSH and catalase as well as significantly attenuating the ethanol-induced lipid peroxidation tissue levels. In addition, ESLE exhibited in vitro antibacterial activity against H. pylori., Conclusions: The chemical constituents of ESLE strongly support its potent gastroprotective effect suggesting its future potential application in the management of gastric ulcer by eliminating its symptoms and causes including H. pylori., (Copyright © 2019 Elsevier B.V. All rights reserved.)

The in vitro cytotoxic activity in Vero cells and the antiviral activity of Erythrina speciosa methanol extract, fractions, and isolated vitexin were studied. The results revealed that E. speciosa leaves ethyl acetate soluble fraction of the methanol extract (ESLE) was the most active against herpes simplex virus type 1 (HSV-1). Bioactivity-guided fractionation was performed on ESLE to isolate the bioactive compounds responsible for this activity. One sub-fraction from ESLE (ESLE IV) showed the highest activity against HSV-1 and Hepatitis A HAV-H10 viruses. Vitexin isolated from ESLE VI exhibited a significant antiviral activity (EC 50 =35±2.7 and 18±3.3 μg/mL against HAV-H10 and HSV-1 virus, respectively), which was notably greater than the activity of the extract and the fractions. Molecular docking studies were carried out to explore the molecular interactions of vitexin with different macromolecular targets. Analysis of the in silico data together with the in vitro studies validated the antiviral activity associated with vitexin. These outcomes indicated that vitexin is a potential candidate to be utilized commendably in lead optimization for the development of antiviral agents., (© 2019 Wiley-VHCA AG, Zurich, Switzerland.)

Gastric ulcer is a major health problem. Current treatment options of gastric ulcer, including antagonists of histamine H 2 receptor and inhibitors of the proton pump, do not cure gastric ulcers, but only provide temporary relief of symptoms and can be associated with severe side effects. The lack of effective and safe medications for this global health problem urges for the discovery of novel classes of compounds with potent activity and an acceptable safety profile. Ethanol-induced ulceration in rats was used to evaluate the gastroprotective activity of casuarinin, an ellagitannin isolated from Melaleuca leucadendra . Casuarinin (25, 50, and 100 mg/kg) reduced the ulcer area by 45, 78, and 99%, respectively, compared with the ulcer group. Casuarinin (100 mg/kg) increased mucin content by 1.8-fold and reduced acidity by 42%. At the same dose, it also increased the levels of reduced glutathione by 194%, catalase by 586%, and prostaglandin E2 to its normal level. In contrast, it attenuated the ethanol-increased levels of malondialdehyde by 56%, TNF- α by 58%, and caspase-3 by 87%. Histological findings demonstrated that casuarinin exhibited a protective effect against tissue alterations in response to the ethanol-induced ulcer. Casuarinin suppressed the immunoexpression of nuclear factor-kappa B, cyclooxygenase-2, and inducible nitric oxide synthase to their normal values. It also induced the expression of heat shock protein-70, reaching up to 4.9-fold in comparison with the ulcer group. The potent gastroprotective effect of casuarinin was thus attributed to its anti-inflammatory, antioxidant, and antiapoptotic effects. Our results suggest the potential application of casuarinin as an antiulcer agent from natural sources., Competing Interests: The authors declare that they have no conflict of interest., (Georg Thieme Verlag KG Stuttgart · New York.)

The hepatoprotective activity of praecoxin A, an ellagitannin from Melaleuca ericifolia, was determined against CCl 4 -induced toxicity in mice. Praecoxin A was administered (25, 50, and 100 mg/kg) for 5 days followed by CCl 4 . Praecoxin A markedly ameliorated the CCl 4 -induced increase in AST (by 19, 52, and 56%), ALP (22, 45, and 48%), ALT (11, 47, and 54%), total bilirubin (14, 27, and 28%), and MDA (26, 44, and 51%) at the tested doses, respectively, as compared with CCl 4 group. It was evident that praecoxin A significantly (p < 0.001) increased the antioxidant parameters GSH (45, 99, and 137%) and SOD (61, 129, and 159%). Histological findings revealed a marked amelioration of hepatocyte degeneration, necrosis, inflammatory cell infiltration, and hemorrhage in the groups treated with praecoxin A. COX-2 and caspase-3 hepatic expressions were significantly downregulated (p < 0.001) in praecoxin A-treated groups (up to 57, 83, and 93% for COX-2 and by 30, 82, and 99% for caspase-3). These findings suggest that praecoxin A exerts a beneficial effect against oxidative stress by reducing lipid peroxidation, enhancing the antioxidant defense status, and protecting against the histopathological changes induced by CCl 4 . This study highlights a promising natural hepatoprotective candidate derived from M. ericifolia that might be an alternative to silymarin., (© 2018 John Wiley & Sons, Ltd.)

A concise and efficient total synthesis of the lignan natural product larreatricin as well as an unambiguous assignment of configuration of its enantiomers are reported, resolving a long-held controversy. Enzyme kinetic studies revealed that different polyphenol oxidases show high and remarkably divergent enantioselective recognition of this secondary metabolite., (© 2017 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.)

The gastroprotective effect of Ocimum basilicum L. (Basil) hexane extract (OBHE) in aspirin-induced gastric ulcers in mice and its ameliorative effect on behavioral alterations were determined. Pretreatment with OBHE (100 or 200 mg kg-1) or misoprostol (50 μg kg-1) alleviated the aspirin-induced oxidative stress by significantly decreasing (p < 0.001) gastric ulcer index scores (57, 76 and 79%), gastric TBARS (by 49, 51 and 52%), NO (21, 28 and 29%), H2O2 (24, 42 and 45%), and the serum pro-inflammatory mediator TNF-α (21, 53 and 53%) and IL-6 (29, 30 and 31%), as well as by markedly increasing gastric GSH (41, 61 and 70%), GSH-Px (21, 32 and 34%), GST (33, 63 and 70%), GR (90, 99 and 112%), CAT (167, 211 and 267%) and serum PGE-2 levels (22, 135 and 200%) and IL-4 (64, 81 and 104%), respectively, compared with the aspirin-treated group. Meanwhile, OBHE and misoprostol induced a significant decrease (p < 0.001) in the freezing time (53, 56 and 64%), and the grooming time (by 25, 43 and 44%), respectively, compared to the aspirin treated group. This study provides evidence that OBHE confers anxiolytic, antioxidant and anti-inflammatory prophylactic effects on aspirin-induced gastric ulcers. GC/MS was used for the characterization of OBHE components. Based on the findings of this study, basil may be used as a nutritional supplement or therapeutic drug to protect against aspirin-induced gastric ulcers, a common problem resulting from the use of aspirin.

The antibacterial activity of 29 different polyoxometalates (POMs) against Moraxella catarrhalis was investigated by determination of the minimum inhibitory concentration (MIC). The Preyssler type polyoxotungstate (POT) [NaP 5 W 30 O 110 ] 14- demonstrates the highest activity against M. catarrhalis (MIC = 1 μg/ml) among all tested POMs. Moreover, we show that the Dawson type based anions, [P 2 W 18 O 62 ] 6- , [(P 2 O 7 )Mo 18 O 54 ] 4- , [As 2 Mo 18 O 62 ] 6- , [H 3 P 2 W 15 V 3 O 62 ] 6- , and [AsW 18 O 60 ] 7- are selective on M. catarrhalis (MIC range of 2-8 μg/ml). Among the six tested Keggin type based POTs ([PW 12 O 40 ] 3- , [H 2 PCoW 11 O 40 ] 5- , [H 2 CoTiW 11 O 40 ] 6- , [SiW 10 O 36 ] 8- , [SbW 9 O 33 ] 9- , [AsW 9 O 33 ] 9- ), only the mono-substituted [H 2 CoTiW 11 O 40 ] 6- showed MIC value comparable to those of the Dawson type group. Polyoxovanadates (POVs) and Anderson type POMs were inactive against M. catarrhalis within the tested concentration range (1-256 μg/ml). Four Dawson type POMs [P 2 W 18 O 62 ] 6- , [(P 2 O 7 )Mo 18 O 54 ] 4- , [As 2 Mo 18 O 62 ] 6- , [H 3 P 2 W 15 V 3 O 62 ] 6- and the Preyssler POT [NaP 5 W 30 O 110 ] 14- showed promising antibacterial activity against M. catarrhalis (MICs < 8 μg/ml) and were therefore tested against three additional bacteria, namely S. aureus, E. faecalis , and E. coli . The most potent antibacterial agent was [NaP 5 W 30 O 110 ] 14- , exhibiting the lowest MIC values of 16 μg/ml against S. aureus and 8 μg/ml against E. faecalis . The three most active compounds ([NaP 5 W 30 O 110 ] 14- , [P 2 W 18 O 62 ] 6- , and [H 3 P 2 W 15 V 3 O 62 ] 6- ) show bacteriostatic effects in killing kinetics study against M. catarrhalis . We demonstrate, that POM activity is mainly depending on composition, shape, and size, but in the case of medium-size POTs (charge is more than -12 and number of addenda atoms is not being higher than 22) its activity correlates with the total net charge.

Phytochemicals serve as potential therapeutic agents for the prevention and treatment of diseases. In this study, we elucidate the renoprotective activity of compounds isolated from Eucalyptus globulus and Melaleuca styphelioides extracts in glucose- and oxalate-challenged NRK-49F cell model. The antioxidant potential of isolated compounds was evaluated based on their effect on antioxidant enzyme activities and lipid peroxidation levels. The results demonstrated that exposure of NRK-49F cells to glucose and oxalate stress augmented cell damage and attenuated antioxidant enzyme activities. The phytochemicals 2,2,8-trimethyl-6-formyl-chrom-3-ene-7-O-β-D-glucopyranoside, Cornusiin B and tellimagrandin I treatment restored antioxidant enzyme activity, significantly lowered lipid peroxidation levels and effectively protected cells from glucose and oxalate stress equivalent to the known antioxidant, N-acetyl cysteine. Pterocarinin A significantly reversed cellular damage owing to glucose stress. In conclusion, the compounds isolated from E. globulus and M. styphelioides showed potential cytoprotective and anti-oxidative property against glucose- and oxalate-induced oxidative stress in NRK-49F cells.

Hit, Lead & Candidate Discovery The acetic acid-induced writhing and hot plate models in mice were utilized to determine the analgesic effect of epicatechin gallate (ECG) isolated from Bauhinia hookeri. The anti-inflammatory activity of ECG was determined using carrageenan-induced paw edema model. The pro-inflammatory mediators (PGE 2 , TNF-α, IL-1β, and IL-6) were estimated in the plasma of different treatment groups. ECG was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard drug (100 mg/kg) in all experiments. ECG significantly (p < .001) suppressed the writhing response in mice. The inhibition percentages were 32, 52, and 62%, at the tested doses of ECG, respectively as compared to the positive control group receiving acetic acid only. Furthermore, ECG significantly (p < .001) increased the reaction time in hot plate model. The maximum analgesic effect was evident after 120 min. ECG demonstrated a significant anti-inflammatory activity as evidenced by the inhibition of carrageenan-induced paw edema (46, 50, and 58%, at the tested doses, respectively). This effect was persistent all over the experimental period. ECG produced a significant (p < .001) reduction in plasma PGE 2 (by 27, 38, and 50%), TNF-α (15, 33, and 41%), IL-1β (17, 25, and 33%), and IL-6 (22, 32, and 43%), at the tested doses, respectively. This study supports the use of ECG as both analgesic and anti-inflammatory agent., (© 2018 Wiley Periodicals, Inc.)

Polyoxometalates (POMs) are transition metal complexes that exhibit a broad diversity of structures and properties rendering them promising for biological purposes. POMs are able to inhibit a series of biologically important enzymes, including phosphatases, and thus are able to affect many biochemical processes. In the present study, we analyzed and compared the inhibitory effects of nine different polyoxotungstates (POTs) on two P-type ATPases, Ca 2+ -ATPase from skeletal muscle and Na + /K + -ATPase from basal membrane of skin epithelia. For Ca 2+ -ATPase inhibition, an in vitro study was performed and the strongest inhibitors were determined to be the large heteropolytungstate K 9 (C 2 H 8 N) 5 [H 10 Se 2 W 29 O 103 ] (Se 2 W 29 ) and the Dawson-type POT K 6 [α-P 2 W 18 O 62 ] (P 2 W 18 ) exhibiting IC 50 values of 0.3 and 0.6 μM, respectively. Promising results were also shown for the Keggin-based POTs K 6 H 2 [CoW 11 TiO 40 ] (CoW 11 Ti, IC 50 = 4 μM) and Na 10 [α-SiW 9 O 34 ] (SiW 9 , IC 50 = 16 μM), K 14 [As 2 W 19 O 67 (H 2 O)] (As 2 W 19 , IC 50 = 28 μM) and the lacunary Dawson K 12 [α-H 2 P 2 W 12 O 48 ] (P 2 W 12 , IC 50 = 11 μM), whereas low inhibitory potencies were observed for the isopolytungstate Na 12 [H 4 W 22 O 74 ] (W 22 , IC 50 = 68 μM) and the Anderson-type Na 6 [TeW 6 O 24 ] (TeW 6 , IC 50 = 200 μM). Regarding the inhibition of Na + /K + -ATPase activity, for the first time an ex vivo study was conducted using the opercular epithelium of killifish in order to investigate the effects of POTs on the epithelial chloride secretion. Interestingly, 1 μM of the most potent Ca 2+ -ATPase inhibitor, Se 2 W 29 , showed only a minor inhibitory effect (14% inhibition) on Na + /K + -ATPase activity, whereas almost total inhibition (99% inhibition) was achieved using P 2 W 18 . The remaining POTs exhibited similar inhibition rates on both ATPases. These results reveal the high potential of some POTs to act as P-type ATPase inhibitors, with Se 2 W 29 showing high selectivity towards Ca 2+ -ATPase.

It is believed that many degenerative diseases are due to oxidative stress. In view of the limited drugs available for treating degenerative diseases, natural products represent a promising therapeutic strategy in the search for new and effective candidates for treating degenerative diseases. This review focuses on the genus Spondias which is widely used in traditional medicine for the treatment of many diseases. Spondias is a genus of flowering plants belonging to the cashew family (Anacardiaceae). This genus comprises 18 species distributed across tropical regions in the world. A variety of bioactive phytochemical constituents were isolated from different plants belonging to the genus Spondias . Diverse pharmacological activities were reported for the genus Spondias including cytotoxic, antioxidant, ulcer protective, hepatoprotective, anti-inflammatory, antiarthritic, and antidementia effects. These attributes indicate their potential to treat various degenerative diseases. The aim of this review is to draw attention to the unexplored potential of phytochemicals obtained from Spondias species, thereby contributing to the development of new therapeutic alternatives that may improve the health of people suffering from degenerative diseases and other health problems.

Hit, Lead & Candidate Discovery Inflammation is a complex biological process that is generally occurs in response to pathological triggers. Both neurodegenerative diseases and cancer have been linked to inflammation. The analgesic and anti-inflammatory effects of cupressuflavone (CUF) isolated from Cupressus macrocarpa were examined. The analgesic effects of CUF (40, 80 and 160 mg/kg po) were assessed in the acetic acid-induced writhing and hot plate models in mice with diclofenac sodium as the reference standard (100 mg/kg). CUF dose-dependently inhibited the writhing response in mice by 25, 48, and 62%, at the three CUF doses with 160 mg/kg being equivalent to the diclofenac control. CUF dose-dependently increased the hot plate model reaction time with a maximal effect after 120 min. In the carrageenan-induced paw edema model of inflammation, CUF demonstrated anti-inflammatory activity by inhibiting paw edema by 55, 60, and 64% at doses of 40, 80, and 160 mg/kg po, respectively. CUF also reduced the plasma pro-inflammatory mediators PGE 2 (44, 54, and 58%), TNF-α (26, 37, and 53%), IL-1β (19, 33, and 41%), and IL-6 (32, 44, and 55%) at the three doses tested with the highest dose having similar effects to diclofenac sodium (100 mg/kg). This finding from this study indicates that CUF has both analgesic and anti-inflammatory effects., (© 2017 Wiley Periodicals, Inc.)

Preclinical Research The anti-inflammatory and analgesic activities of a polyphenol-rich fraction (TMEF) obtained from Terminalia muelleri Benth. were measured. The analgesic activity of TMEF was tested using acetic acid-induced writhing and hot plate models in mice. The anti-inflammatory activity was assessed using carrageenan-induced paw edema model by measuring PGE 2 , TNF-α, IL-1β, and IL-6 plasma levels as well as the paw thickness. TMEF was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard (100 mg/kg) in all experiments. The group treated with 400 mg/kg of TMEF showed a greater inhibition in the number of writhes (by 63%) than the standard-treated group (61%). Pretreatment with TMEF increased the analgesic effect in hot plate test in a dose-dependent manner with a maximum effect after 120 min. TMEF pretreatment alos reduced the edema thickness by 48, 53, and 62% at the tested doses, respectively. TMEF administration inhibited the carrageenan-induced elevations in PGE 2 (by 34, 43, and 47%), TNF-α (18, 28, and 41%), IL-1β (14, 22, and 29%), and IL-6 (26, 31, and 46%). Four phenolic compounds were isolated from Terminalia muelleri for the first time. Drug Dev Res 78 : 146-154, 2017. © 2017 Wiley Periodicals, Inc., (© 2017 Wiley Periodicals, Inc.)