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Ethnopharmacological Relevance: Plant vernacular names can provide clues about the popular use of a species in different regions and are valuable sources of information about the culture or vocabulary of a population. Several medicinal plants in Brazil have received names of medicines and brand-name products., Aim of the Study: The present work aimed to evaluate the chemical composition and pharmacological activity in the central nervous system of three species known popularly by brand names of analgesic, anti-inflammatory, antispasmodic, and digestive drugs., Materials and Methods: Hydroethanolic extracts of Alternanthera dentata (AD), Ocimum carnosum (OC), and Plectranthus barbatus (PB) aerial parts were submitted to phytochemical analysis by HPLC-PAD-ESI-MS/MS and evaluated in animal models at doses of 500 and 1000 mg/kg. Mice were tested on hot plate, acetic acid-induced writing, formalin-induced licking, and intestinal transit tests. Aspirin and morphine were employed as standard drugs., Results: The three extracts did not change the mice's response on the hot plate. Hydroethanolic extracts of AD and PB reduced the number of writhes and licking time, while OC was only effective on the licking test at dose of 1000 mg/kg. In addition, AD and OC reduced intestinal transit, while PB increased gut motility., Conclusions: Pharmacological tests supported some popular uses, suggesting peripheral antinociceptive and anti-inflammatory effects, while the phytochemical analysis showed the presence of several flavonoids in the three hydroethanolic extracts and steroids in PB, with some barbatusterol derivatives described for the first time in the species., 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 © 2024 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Passiflora coriacea Juss., a medicinal plant in the family Passifloraceae, is widely used to treat anxiety and depression in Mexican folk medicine. However, its chemical profile and biological activity have not been characterized., Aim of the Study: The aim of the study was to determine the antidepressant activity, anxiolytic effect, and chemical profile of Passiflora coriacea., Materials and Methods: An organic fraction (PcEA) from a hydroalcoholic extract of the aerial parts of P. coriacea was obtained, followed by a chemical analysis and separation, yielding six fractions (PcEA, T1, T2, T1.1, T2.1, and T2.2). Male ICR mice were used to determine the antidepressant activity of selected treatments (PcEA, T1, T2, and T1.1) based on a forced swim test (FST). The anxiolytic-like effects of various treatments (PcEA, T1, T2, T2.1, and T2.2) were determined using the elevated plus maze (EPM) test., Results: The organic fraction of P. coriacea decreased anxiety-like behaviors in mice and increased the time of mobility in the FST. After chemical separation, two compounds were isolated from the species with antidepressant activity and anxiolytic-like effects, T1.1 (tricin 7-O-glucoside) and T2.2 (harmane), respectively., Conclusions: Compounds isolated from P. coriacea exerted anxiolytic and antidepressant effects in mice based on the EPM and FST. The flavonoid tricin-7-O-glucoside and the alkaloid harmane contributed to these biological activities., 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 © 2024 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Glinus oppositifolius (L.) Aug. DC. belongs to the family Molluginaceae, an annual prostrate herb traditionally used to treat inflammations, arthritis, malarial, wounds, fevers, diarrhoea, cancer, stomach discomfort, jaundice, and intestinal parasites. However, the anti-arthritic activity of the aerial part has still not been reported., Aim of the Study: To investigate the antioxidant and anti-arthritic activity of G. oppositifolius in Complete Freund's Adjuvant (CFA) induced rats., Materials and Methods: The dried aerial parts of this plant material were defatted with n-hexane and extracted by methanol using a soxhlet apparatus. The in vitro anti-arthritic activity of methanolic extract of G. oppositifolius (MEGO) was evaluated in protein denaturation, membrane stabilization, and inhibition of proteinase assay at 25, 50, 100, 200, and 400 μg/ml concentrations. Female Wistar rats were immunized sub-dermally into the right hind paw with 0.1 ml of CFA. Rats were administered with MEGO at doses of 200 and 400 mg/kg once daily for fourteen days after arthritis induction. Assessment of arthritis was performed by measuring paw diameter, arthritic index, arthritic score, body weight, organ weight, and hematological and biochemical parameters, followed by the analysis of pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), interleukin 6 (IL-6), interleukin-1-beta (IL-1β), cyclooxygenase-2 (COX-2), interleukin 13 (IL-13) and interleukin 10 (IL-10) and histopathological study. In vivo antioxidant effect was investigated in enzymatic assays. The presence of phytoconstituents was analyzed by Gas Chromatography-Mass Spectrometry (GC-MS) and Liquid Chromatography-Mass Spectrometry (LC-MS), respectively. In silico molecular docking study of the compounds was carried out against COX-2, IL-1β, IL-6, and TNF-α using AutoDock 4.2 and BIOVIA-Discovery Studio Visualizer software., Results: MEGO's in vitro anti-arthritic activity showed dose-dependent inhibition of protein denaturation, membrane stabilization, and proteinase inhibition, followed by significant in vivo anti-arthritic activity. The rats treated with MEGO showed tremendous potential in managing arthritis-like symptoms by restoring hematological, biochemical, and histological changes in CFA-induced rats. MEGO (200 and 400 mg/kg) showed a significant alleviation in the levels of hyper expressed inflammatory mediators (TNF-α, IL-1β, and IL-6) and oxidative stress (SOD, CAT, GSH, and LPO) in CFA-induced rats. Spergulagenin-A as identified by LC-MS analysis, exhibited the highest binding affinity against COX-2 (-8.6), IL-1β (7.2 kcal/mol), IL-6 (-7.4 kcal/mol), and TNF-α (-6.5 kcal/mol)., Conclusions: Provided with the comprehensive investigation, methanolic extract of G. oppositifolius against arthritic-like condition is a proof of concept that revalidates its ethnic claim. The presence of Spergulagenin-A might be responsible for the anti-arthritic activity., 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 © 2024 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Caralluma dalzielii (Asclepiadiaceae) is a shrub used in folkloric medicine to treat epilepsy, pain and infertility in sub-Saharan Africa. Previous studies demonstrated its analgesic, antiulcer, anticonvulsant, and anti-inflammatory activities., Aim: This study aimed to determine the neurobehavioural properties of Caralluma dalzielii aqueous aerial parts extract (CDAE) in mice using standard experimental models., Materials and Methods: Neurobehavioural activities of CDAE were evaluated (100, 200, and 400 mg/kg) in Swiss Albino mice using the beam walk, staircase, hole board, object recognition, open field assay, Y-maze and forced swimming tests. Phytochemical constituents were analysed using GC-MS., Results: CDAE significantly increased the mean number of head dips, recognition index and spontaneous alternation in hole board (14.03 at 400 mg/kg and 6.01 in distilled water group; p < 0.05), object recognition (68.16% at 400 mg/kg compared with 51.66% of distilled water group) and Y maze (9.16 at 400 mg/kg as against 4.66 of distilled water group; p < 0.05) tests respectively. It decreased the rearing counts as well as the peripheral and central square crossing in the staircase (4.2 at 400 mg/kg as against 7.87 of the distilled water group; p < 0.05) and open field tests (central, 0.81; peripheral, 1.66 at 400 mg/kg as against central, 5.23; peripheral 11.83 of the distilled water control group; p < 0.05), respectively. There were no significant effects on beam walk assays and forced swim tests. The GC-MS analysis identified a hundred compounds in CDAE. Some compounds which have been reported to possess neurobehavioural activity that were identified include 3,5-Dimethylpyrazole, 2-Amino-5-methylbenzoic acid, Acetophenone, and Tetrahydropyran., Conclusion: CDAE demonstrated anxiolytic, anti-hyperactivity, and memory-improving effects in mice. The extract may possess GABAergic and glutamatergic properties. More studies are needed to confirm this. Isolation of the bioactive compounds is currently ongoing to unravel the bioactive constituents present in C. dalzielii extract., 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 © 2024 Elsevier B.V. All rights reserved.)

This research examined the impact of incorporating Angelica sinensis's aerial components (APA), commonly referred to as "female ginseng", into broilers' diet. Two hundred eighty-eight 1-day-old Cobb 500 broilers were randomly assigned to the 4 experimental groups with 6 replications and 12 birds/replicate. The 4 groups were fed the diets included 4 concentrations of APA (0, 1, 2, and 3%, respectively). The study spanned 42 d, categorized as the starter phase (1-21 d) and the finisher phase (22-42 d). Notably, broilers fed with 3% APA demonstrated a pronounced surge in feed consumption and weight gain during the 22 to 42 d and over the full 42-d period (P < 0.05). Furthermore, when examining the broilers' intestinal structure, there was a notable increase in the villus height and villi ratio across the duodenum, jejunum, and ileum, with a decrease in crypt depth upon 3% APA inclusion (P < 0.05). On a molecular note, certain genes connected to the intestinal mechanical barrier, such as Zona Occludens 1 and Claudin-2, saw significant elevation in the jejunum (P < 0.05). The jejunum also displayed heightened levels of antimicrobial peptides like lysozyme, mucin 2, sIgA, IgG, and IgM, showcasing an enhanced chemical and immune barrier (P < 0.05). Delving into the 16SrDNA sequencing of intestinal content, a higher microbial diversity was evident with a surge in beneficial bacteria, particularly Firmicutes, advocating a resilient and balanced microecosystem. The findings imply that a 3% APA dietary addition bolsters growth metrics and fortifies the intestinal barrier's structural and functional integrity in broilers., (Copyright © 2024 The Authors. Published by Elsevier Inc. All rights reserved.)

The rising geriatric population is expected to increase the demand for drugs treating neurodegenerative diseases. The present work is aimed to discover acetylcholinesterase (AChE) inhibitors from Cissampelos pareira Linn. aerial parts ( Family: Menispermaceae ). Bioassay-guided isolation, AChE inhibition study and estimation of the therapeutic marker in different parts of raw herbs were conducted. The structure of the compound (1) was elucidated as N-methylneolitsine by using NMR (1D and 2D) and ESI-MS/MS spectral data, which is a new natural analogue of neolitsine. It showed good AChE inhibition with an IC 50 value of 12.32 µg/mL. It was densitometrically estimated to be 0.074 - 0.33% in aerial parts of C. pareira, collected from various locations. The alkaloid reported here could be potentially useful for the treatment of various neurodegenerative diseases and the aerial part of C. pareira could be used as a promising ingredient for various preparations treating neurodegenerative diseases.

A new naphthoquinone derivative ( 1 ) together with twenty-three known compounds ( 2 - 24 ), were isolated from the aerial parts of Rubia cordifolia L. Their structures were elucidated on the basis of NMR and HR-ESIMS data. Compounds 1 - 13 were assessed for their inhibitory effects on NO production in LPS-stimulated RAW 264.7 macrophage cells. Compounds 2 - 6 exhibited significant inhibitory activities with IC 50 values of 21.37, 13.81, 24.56, 20.32, and 30.08 μmol·L -1 , respectively.

Eight structurally diverse rearranged sesquiterpenoids, including seven undescribed sesquiterpenoids (1a/1b and 3-8) were obtained from the aerial parts of Daphne penicillata. 1a/1b, 3, 5 and 6 possess rare rearranged guaiane skeletons and 4 represents the first example of rearranged carotene sesquiterpenoids. Their structures and absolute configurations were determined by extensive spectroscopic analyses, NMR and ECD calculations. Interestingly, 1a and 1b were a pair of magical interconverting epimers that may interconvert by retro-aldol condensation. The mechanism of interconversion has been demonstrated indirectly by 9-OH derivatization of 1a/1b and a hypothetical biogenetic pathway was proposed. All compounds were evaluated for anti-inflammatory and cytotoxic activities. Among them, 1a/1b and 2 exhibited potential inhibitory activities on the production of NO against LPS-induced BV2 microglial cells., 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 © 2023 Elsevier Ltd. All rights reserved.)

Cleome viscosa L., a member of the family Cleomaceae, is a potential medicinal plant, known for several bioactive properties such as: anticancer, antidiabetic, antioxidant, anti-inflammatory, antimicrobial, wound healing, etc. Our study aimed to isolate a bioactive compound and assess its antibacterial activity. The crystal compound imperatorin was isolated and reported for the first time from the aerial parts of C. viscosa . The isolation was made using silica gel (100-200 mesh) column chromatography. The structure of imperatorin was investigated through single-crystal XRD, unit cell molecules, FTIR, and ESI-MS spectral analysis. The results validated imperatorin's triclinic crystal structure and P2i/c distance group. The electronic structure was also calculated (4.28/6.21 D) along with the frontier molecular orbital, dipole moment, atomic charges, and electrostatic map of particles in gaseous stage and active site. Imperatorin showed highest activity at 40 µg/mL concentration against Gram + ve bacteria: Staphylococcus aureus (3 ± 0.2 mm), Bacillus subtilis (3 ± 0.6 mm), and Gram -ve bacteria: Klebsiella pneumoniae (3 ± 0.2 mm), Escherichia coli (5 ± 0.2 mm). The study highlights that the compound can be isolated in larger quantities as the plant is easily available across the tropics.

Ethnopharmacological Relevance: Mentha longifolia (L.) (Lamiaceae) is a native plant in Morocco, traditionally used in different countries to treat several disorders notably gastrointestinal illnesses, respiratory disorders, infectious diseases, inflammatory diseases, and menstrual problems. Robust scientific evidence has confirmed multiple pharmacological properties of M. longifolia including antihemolytic, anti-inflammatory, antibacterial, hepatoprotective, anti-cancer, antidiabetic, gastroprotective effect, and antispasmodic activity., Aim of the Study: The current study aimed to determine the phytochemical profile and assess the toxic effect of an aqueous extract of the arial parts of M. longifolia in male and female Swiss albino mice during acute and subacute oral toxicity., Materials and Methods: High-performance Liquid Chromatography Diode Array Detector (HPLC-DAD) was used to provide qualitative and quantitative analyses of phenolic compounds of M. longifolia aqueous extract. In acute toxicity experiments, four distinct groups of mice (n = 5/group/sex) were administered Mentha longifolia aqueous extract at single oral dosages of 0.5; 1; 2; 4, and 8 g/kg BW given by gavage and intraperitoneal for up to 14 days. Regarding the subacute toxicity investigation, Swiss albino mice were given M. longifolia aqueous extract orally at dosages of 100; 500; and 1000 mg/kg BW daily for 28 days. Body weight is measured every 7 days and suggested biochemical and hematological parameters were quantified, at the finish of 28 days of daily administration, sections of the liver, kidney, and spleen were histologically evaluated for showing damage to organs., Results: The data of High-performance Liquid chromatography analysis revealed that M. longifolia aqueous extract was rich in interesting phytochemical compounds, mainly quercetin, and rutin, followed by a hydroxybenzoic acid-like syringic acid. Regarding the acute test in mice, no mortality or symptoms of toxicity were detected following oral administration with a single dose of M. longifolia aqueous extract at any dosage limit up to 4 g/kg, which was the no-observed side effect threshold (NOAEL). The mortality rate as well as acute toxicity of the M. longifolia aqueous extract delivered intraperitoneally, are increased progressively with increasing dosage. The non-observed adverse effect level (NOAEL) for the intraperitoneal dosage was 1 g/kg BW, and the lowest observed adverse effect level (LOAEL) was 2 g/kg BW, the estimated acute toxicity (LD 50 ) of intraperitoneally given M. longifolia aqueous extract in mice was 4.800 g/kg BW. Concerning subacute examinations in mice, the M. longifolia aqueous extract did not induce substantial modifications in biochemical or hematological indicators, preserving a slight increase in creatinine and urea levels. At the end of the experiment, a histopathological examination of the kidneys, liver, and spleen revealed normal architecture, suggesting no morphological damage., Conclusion: The data we obtained indicate that acute or subacute administration of Mentha longifolia aqueous extract is relatively non-toxic in male and female Swiss albino mice., 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 © 2023 Elsevier B.V. All rights reserved.)

Background: Indigofera suffruticosa Mill. is used as a folk medicine for treating patients with leukemia, however very little is known regarding the molecular mechanism of its anti-leukemic activity and the chemical profile of the active extract. The present study aimed to reveal the molecular effect of I. suffruticosa aerial parts extract (ISAE) on leukemia cells and its chemical constituents., Methods: Cytotoxicity of ISAE were determined by resazurin viability assay, multitox - Glo multiplex cytotoxicity assay, and Annexin V staining assay. Cell cycle profiles were revealed by propidium iodide staining assay. The effects of ISAE on G2/M arrest signaling and DNA damage were evaluated by Western blot assay and phospho-H2A.X staining assay. The chemical profile of ISAE were determined by tandem mass spectroscopy and molecular networking approach., Results: We showed that the acute lymphoblastic leukemia cell line Jurkat cell was more responsive to ISAE treatment than other leukemia cell lines. In contrast, ISAE did not induce cytotoxic effects in normal fibroblast cells. Cell cycle analysis revealed that ISAE triggered G2/M arrest in Jurkat cells in dose- and time-dependent manners. Elevation of annexin V-stained cells and caspase 3/7 activity suggested ISAE-induced apoptosis. Furthermore, ISAE alone could increase the phosphorylation of CDK1 at Y15 and activate the ATR/CHK1/Wee1/CDC25C signaling pathway. However, the addition of caffeine, a widely used ATR inhibitor to ISAE, reduced the phosphorylation of ATR, CHK1, and CDK1, as well as G2/M arrest in Jurkat cells. Moreover, increased phospho-H2A.X stained cells indicated the involvement of DNA damage in the anti-leukemic effect of ISAE. Finally, qualitative analysis using UPLC-tandem mass spectroscopy and molecular networking revealed that tryptanthrin was the most abundant organoheterocyclic metabolite in ISAE. At equivalent concentrations to ISAE, tryptanthrin induced G2/M arrest of Jurkat cells, which can be prevented by caffeine., Conclusions: ISAE causes G2/M arrest via activating ATR/CHK1/CDK1 pathway and tryptanthrin is one of the active components of ISAE. Our findings provide subtle support to the traditional use of I. suffruitcosa in leukemia management in folk medicine., (© 2024. The Author(s).)

Gossypol and the related terpenoids are stored in the pigment gland to protect cotton plants from biotic stresses, but little is known about the synthetic sites of these metabolites. Here, we showed that GoPGF, a key gene regulating gland formation, was expressed in gland cells and roots. The chromatin immunoprecipitation sequencing (ChIP-seq) analysis demonstrated that GoPGF targets GhJUB1 to regulate gland morphogenesis. RNA-sequencing (RNA-seq) showed high accumulation of gossypol biosynthetic genes in gland cells. Moreover, integrated analysis of the ChIP-seq and RNA-seq data revealed that GoPGF binds to the promoter of several gossypol biosynthetic genes. The cotton callus overexpressing GoPGF had dramatically increased the gossypol levels, indicating that GoPGF can directly activate the biosynthesis of gossypol. In addition, the gopgf mutant analysis revealed the existence of both GoPGF-dependent and -independent regulation of gossypol production in cotton roots. Our study revealed that the pigment glands are synthetic sites of gossypol in aerial parts of cotton and that GoPGF plays a dual role in regulating gland morphogenesis and gossypol biosynthesis. The study provides new insights for exploring the complex relationship between glands and the metabolites they store in cotton and other plant species., (© 2023 The Authors New Phytologist © 2023 New Phytologist Foundation.)

The relevance of oxylipins as biomarkers of oxidative stress has been established in recent years. Phytoprostanes and phytofurans are plant metabolites derived from peroxidation of α-linolenic acid (ALA) induced by ROS. Previous findings have suggested new valuable biological properties for these new active compounds in the frame of diverse pathophysiological situations and health constraints. Lipidomic profiling of different aerial parts of the same Acacia cyanophylla Lindl. specimen, was evaluated for the first time here, using LC-MS/MS technology. Analysis revealed the existence of six PhytoPs and three PhytoFs. Stems have the highest amount of these metabolites with 179.35 ng/g and 320.79 ng/g respectively. This first complete profile paves the way to explore Acacia cyanophylla Lindl. as a source of plant oxylipins for therapeutic or pharmaceutical uses., Competing Interests: Declaration of Competing Interest The authors declare no conflict of interest., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Two new eudesmane-type sesquiterpene lactones, 1β,3α,8α-trihydroxy-11β,13-dihydroeudesma-4(15)-en-12,6α-olide ( 1 ) and 1β,4α,8α-trihydroxy-11β,13-dihydroeudesma-12,6α-olide ( 2 ), and an unprecedented elemane-type sesquiterpene lactone, 1β,2β,8α-trihydroxy-11β,13-dihydroelema-12,6α-olide ( 3 ) along with a known eudesmanolide artapshin ( 4 ) were isolated from Seriphidium khorassanicum. Structures were elucidated by NMR, HR-ESI-MS, and ECD spectral data analysis. The anti-protozoal activity was evaluated against Leishmania major promastigotes and amastigote-infected macrophages. They showed dose- and time-dependent activity against L. major amastigotes with IC 50 values in the range of 4.9 to 25.3 μM being favourably far below their toxicity against normal murine macrophages with CC 50 values ranging from 432.5 to 620.7 μM after 48 h of treatment. Compound 3 exhibited the strongest activity and the highest selectivity index (SI) with IC 50 of 4.9 ± 0.6 μM and SI of 88.2 comparable with the standard drug, meglumine antimoniate (Glucantime), with IC 50 and SI values of 15.5 ± 2.1 μM and 40.0, respectively.

Ethnopharmacological Relevance: Vetiver (Chrysopogon zizanioides) is indigenous to India where it is traditionally used to relief rheumatisms, lumbagos and sprains. Vetiver anti-inflammatory activity has not been previously investigated, and its specific interactions with body inflammation cascade remain largely unknown., Aim of the Study: The present work was performed to validate the ethnobotanical use of the plant and compare the anti-inflammatory activities of the ethanolic extracts of the most traditionally used part (aerial part) to that of the root. Furthermore, we attempt to reveal the molecular mechanism of this anti-inflammatory activity in correlation to the chemical composition of C. zizanioides aerial (CA) and root parts (CR)., Materials and Methods: Ultraperformance liquid chromatography coupled to high resolution mass spectrometry (UHPLC/HRMS) was used for comprehensive analysis of both CA and CR. The anti-inflammatory effect of both extracts was evaluated in complete Freund's adjuvant (CFA)-induced RA model in Wistar rats., Results: Phenolic metabolites were predominant in CA and 42 were identified for the first time, while only 13 were identified in CR. Meanwhile, triterpenes and sesquiterpenes were confined to the root extract. In CFA arthritis model, CA showed better anti-inflammatory activity than CR marked by an increase in serum level of IL-10 with simultaneous decrease in pro-inflammatory markers; IL-6, ACPA and TNF-α and was evident in histopathological examination. This anti-inflammatory effect was accompanied by down-regulation of JAK2/STAT3/SOCs3, ERK1/ERK2, TRAF6/c-FOS/NFATC1, TRAF6/NF-κB/NFATC1 and RANKL pathways which were all upregulated after CFA injection. These pathways were modulated to larger extent by CA, except for ERK1/ERK2 which was downregulated more effectively by CR. This differential effect between CA and CR can be explained by the variability in their phytoconstituents profile., Conclusion: In agreement with the ethnobotanical preference, CA extract was more effective than CR extract in reducing the symptoms of RA probably due to its enrichment with flavonoids, lignans, and flavolignans. Both CA and CR reduced the production of inflammatory cytokines through modulating various biological signaling pathways. These findings support the traditional use of vetiver leaves as a remedy for RA and suggest that the use of the whole plant may offer advantage by synergistically affecting more inflammatory pathways., 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 © 2023 Elsevier B.V. All rights reserved.)

An LC-MS/MS-guided analysis of the aerial parts of Glycyrrhiza foetida afforded new phenethyl (amorfrutin)- and alkyl (cannabis)-type phytocannabinoids (six and four compounds, respectively). The structural diversity of the new amorfrutins was complemented by the isolation of six known members and the synthesis of analogues modified on the aralkyl moiety. All of the compounds so obtained were assayed for agonist activity on PPARα and PPARγ nuclear receptors. Amorfrutin A ( 1 ) showed the highest agonist activity on PPARγ, amorfrutin H ( 7 ) selectively targeted PPARα, and amorfrutin E ( 4 ) behaved as a dual agonist, with the pentyl analogue of amorfrutin A ( 11 ) being inactive. Decarboxyamorfrutin A ( 2 ) was cytotoxic, and modifying its phenethyl moiety to a styryl or a phenylethynyl group retained this trait, suggesting an alternative biological scenario for these compounds. The putative binding modes of amorfrutins toward PPARα and PPARγ were obtained by a combined approach of molecular docking and molecular dynamics simulations, which provided insights on the structure-activity relationships of this class of compounds.

Background: Endothelial dysfunction (ED) is a marker of vascular damage and a precursor of cardiovascular diseases such as hypertension, which involve inflammation and organ damage. Nitric oxide (NO), produced by eNOS, which is induced by pAKT, plays a crucial role in the function of a healthy endothelium., Methods: A combination of subfractions SF1 and SF3 (C4) of the aqueous fraction from Cucumis sativus (Cs-Aq) was evaluated to control endothelial dysfunction in vivo and on HMEC-1 cells to assess the involvement of pAkt in vitro. C57BL/6J mice were injected daily with angiotensin II (Ang-II) for 10 weeks. Once hypertension was established, either Cs-AqC4 or losartan was orally administered along with Ang-II for a further 10 weeks. Blood pressure (BP) was measured at weeks 0, 5, 10, 15, and 20. In addition, serum creatinine, inflammatory status (in the kidney), tissue damage, and vascular remodeling (in the liver and aorta) were evaluated. Cs-AqC4 was also tested in vitro on HMEC-1 cells stimulated by Ang-II to assess the involvement of Akt phosphorylation., Results: Cs-AqC4 decreased systolic and diastolic BP, reversed vascular remodeling, decreased IL-1β and TGF-β, increased IL-10, and decreased kidney and liver damage. In HMEC-1 cells, AKT phosphorylation and NO production were increased., Conclusions: Cs-AqC4 controlled inflammation and vascular remodeling, alleviating hypertension; it also improved tissue damage associated with ED, probably via Akt activation.

Clivia miniata (Lindl) is a member of the family Amaryllidaceae known for its chemically diverse alkaloids with a wide range of biological activities. Many reports revealed a direct role of oxidative stress in the early stage of Alzheimer's disease (AD). Meanwhile, β-site amyloid precursor protein cleavage enzyme 1 (BACE-1) is a molecular target for the treatment of AD. We aimed to investigate C. miniata root, bulb, and aerial part chemical profiling, antioxidant, BACE-1, and AChE enzyme inhibitory activities. Results showed that the total root had the most potent radical scavenging activity as compared to the total bulb and aerial part, respectively. Ethanol root extract had the most potent BACE-1 inhibitory activity (IC 50 = 0.02 ± 0.001 µg/mL) as compared to the bulb and aerial part (IC 50 = 0.93 ± 0.13, 1.80 ± 0.24 µg/mL), respectively. Moreover, the total root extract mitigated AChE enzyme activity more than total bulb and aerial fractions with IC 50 values of (0.06 ± 0.02, 0.58 ± 0.3, and 1.89 ± 0.42 µg/mL, respectively. Bioassay-guided acid-base fractionation confirmed superior BACE-1 inhibitory activity of the root fractions particularly, methylene chloride and ethyl acetate fractions with (IC 50 values of 0.21 ± 0.60 and 0.01 ± 0.001 µg/mL), respectively. UPLC-MS analysis of ethyl acetate and methylene chloride fractions of C. miniata root led to the identification of eight phenolics and thirteen alkaloids, respectively. Molecular docking studies against BACE-1 protein revealed that lycorine di-hexoside, miniatine, and cliviaaline were the most promising hits. Further investigation of anti-AD potential of the aforementioned small molecules is required., Competing Interests: Declaration of Competing Interest The authors declare no conflict of interest., (Copyright © 2023 The Authors. Published by Elsevier Masson SAS.. All rights reserved.)

Ethanol extract from the aerial parts of Euphorbia tirucalli L. as well as the latex of the plant suspended in water are used by the Brazilian population for the treatment of various diseases, including cancer. The purposes of this study were to determine if the ethanol extract is effective as cytotoxic agent against gastric adenocarcinoma cells (AGS) and its chemical composition by GC-MS, ESI-(-)-FT-ICR MS and (-)-ESI-LTQ-MS/MS. The results were compared with that of latex previously described by us. Hexane and aqueous fractions showed higher cytotoxicity on AGS cells. Nine triterpene compounds were detected by GC-MS in hexane fraction, including euphol and friedelin, while ellagic acid was identified as main phenolic compound in aqueous extract. Therefore, the greater cytotoxic activity of the ethanol extract of the aerial parts of Euphorbia tirucalli for gastric cancer, when compared to latex, seems to originate from the antiproliferative effects of ellagic acid and triterpenes.

Air pollution causes various airway diseases. However, many commonly used treatments can have high risks of side effects or are costly. To examine the anti-inflammatory properties of Inula japonica Thunb. and Potentilla chinensis Ser., a mouse model was generated via inhalation of both particulate matter 10 and diesel particulate matter, and 30% ethanol extracts of either I. japonica (IJ) or P. chinensis (PC) and a mixture of both ethanol extracts (IP) were orally administered to BALB/c mice for 12 days. IJ, PC, and IP inhibited immune cell numbers and their regulation in both the bronchoalveolar lavage fluid (BALF) and lungs. These agents suppressed the levels of interleukin (IL)-1α, IL-17, tumor necrosis factor (TNF)-α, C-X-C motif chemokine ligand (CXCL)-1, and CXCL-2 in BALF, and also inhibited F4/80 and IL-1 receptor-associated kinase (IRAK)-1 in lungs. They reduced the gene expression of TNF-α , CXCL-1 , inducible NOS , COX-2 , Mucin 5AC , and transient receptor potential cation channel subfamily V member 1 in lungs. These extracts also reduced histopathological changes and inflammatory progression, manifested as decreased cell infiltration, collagen deposition, and respiratory epithelial cell thickness. I. japonica and P. chinensis show potential for development as pharmaceuticals that suppress inflammatory progression and alleviate airway inflammation diseases caused by air pollutants.

Plants respond to water shortage by regulating biochemical pathways which result in the biosynthesis of osmotic compounds. Active metabolites and compatible osmolytes control the inhibition of oxygen free radicals and dehydration. The physiological response of scrophularia striata to drought stress, a factorial completely randomized design (FCRD) experiment was conducted in three replication. Drought stress was induced at two levels (100% and 50% field capacity), and salicylic acid (SA) and silicon (Si) and Ecotype were also used at two levels of (0 and 100 PPM), (0 and 1 g/L) and (Ilam and Abdanan) respectively. Data analysis results indicated that the H 2 O 2 content, Malondialdehyde (MDA), glycine betaine (GB) and the activity of the enzyme glutathione reductase (GR; EC 1.6.4.2) of aerial parts increased during the entire stress exposure period. Although the SA + Si + stress + ecotype interaction increased the content of soluble carbohydrate s and the GR activity in aerial parts of Ilam and Abdanan ecotypes, this interaction led to a decrease in MDA, H 2 O 2 in Ilam ecotypes. The interaction between the stress + SA + Si + ecotype led to an increase in the phenylalanine ammonialyase (PAL; EC 4.3.1.5) activity in the Abdanan ecotype, but no important difference was observed. As compared to the control treatment, the content of Polyphenol increased, The interaction between ecotype + stress + Si caused to increased the of proline content in the Abadanan ecotype. The results showed that the increase in antioxidant defense and compatible osmolytes due to the use of SA and Si can improve the drought tolerance in S.striata., 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 © 2023. Published by Elsevier Masson SAS.)