Journals
2026 EN
Molonia Maria Sofia · Salamone Federica Lina · Cimino Francesco
+6 more
ABSTRACT Salvia officinalis L. essential oil production process generates an exhausted residue of vegetable biomass, returned by hydrodistillation, along with a variable amount of wastewater enriched in water‐soluble compounds of high added value and biological activity. The aim of this study was to investigate the in vitro anti‐inflammatory effects of S. officinalis L. hydrodistillation wastewater using murine macrophage Raw 264.7 cells stimulated with Escherichia coli lipopolysaccharide (LPS) and human intestinal epithelial Caco‐2 cells exposed to E. coli . Polyphenolic compounds in wastewater were identified by high‐performance liquid chromatography‐mass spectrometry analysis, confirming the presence of organic acids (particularly hydroxycinnamic acids), flavones, and flavonols. This phytocomplex protected Raw 264.7 from E. coli LPS‐induced inflammation by reducing nuclear factor kappa B nuclear translocation and its transcriptional activity (interleukin [IL]‐6, IL‐8, and tumor necrosis factor‐alpha messenger RNA levels). Additionally, the wastewater reduced cyclooxygenase‐2 protein expression in Caco‐2 cells challenged with E. coli . Interestingly, E. coli exposure resulted in a significant decrease in trans ‐epithelial electrical resistance values in Caco‐2 cells, reflecting impaired barrier integrity, which was reverted by S. officinalis L. wastewater, and this effect was associated with claudin‐1 and occludin restoration, essential for maintaining intestinal barrier function. Present data confirms the protective effect of S. officinalis L. hydrodistillation wastewater in E. coli ‐induced inflammation, suggesting its potential application in the prevention and/or treatment of intestinal inflammation.
Journals
2026 EN
Craciunescu Oana · Mihai Elena · GasparPintiliescu Alexandra
+5 more
ABSTRACT The aim of this study was to investigate the ultrasound‐assisted extraction (UAE) of antioxidant flavonoids from sunflower ( Helianthus annuus ) ray florets through the optimization of the parameters (temperature, extraction ratio, and solvent concentration) using a response surface methodology (RSM), then to validate the model conducting wet‐lab analyses, and finally, to characterize the optimized extracts for composition and in vitro cardioprotective potential. Within RSM, the parameters of UAE were optimized by maximization of the response variables yield of flavonoid extraction and Trolox equivalent antioxidant capacity. Two optimal solutions obtained in 73% ethanol, at 30:1 (v/w) extraction ratio and 80°C (extract 1′) and in 77% ethanol, at 12:1 (v/w) extraction ratio and 40°C (extract 2′) were validated. HPLC analysis revealed that rutin and myricetin were the main flavonoids in both optimized extracts and slightly higher amounts were quantified in extract 2′. In addition, extract 2′ presented higher free radical scavenging activity and angiotensin‐converting enzyme (ACE) inhibition than extract 1′. Both extracts were cytocompatible in an endothelial cell culture, in a wide range of concentrations (31.25–500 µg/mL) and stimulated the cell metabolism, after 24 h of cultivation. Optimized extract 2′ containing flavonoids from sunflower ray florets with antioxidant properties and cardioprotective potential was also a solution of interest for the bioeconomy, due to less consuming extraction conditions. This extract could be recommended for further testing as a valuable ingredient of novel cardioprotective nutraceuticals.
Journals
2026 EN
dos Santos Barreto Marina · Lisboa de Jesus Wesley · Britto Sá Maria Eduarda
+8 more
ABSTRACT The sunflower ( Helianthus annuus L.) is a plant commonly used in agriculture and the fuel industry, as well as being an ornamental garden plant. However, its biologically active compounds make it an interesting plant for medicinal purposes. This review evaluated the phytochemistry of sunflower leaves, stems, receptacles, flowers, seeds, and sprouts and its pharmacological activities. A search was conducted in the PubMed, Embase, ScienceDirect and Google Scholar in March 2025. This review includes studies on the quantitative phytochemical profile of H. annuus extract and studies that reported some pharmacological activity of sunflower extracts or metabolites. The compounds identified in the parts of the sunflower include phenolic acids, flavonoids, and terpenes, mainly. These classes of metabolites are responsible for the pharmacological effects of the species, especially 5‐O‐caffeoylquinic acid (chlorogenic acid) and its derivates. Fatty acids, vitamins, alkanes, alkaloids, and benzenoids were also found, but in smaller variations. Studies have reported that the effects of sunflowers include antioxidant, anti‐inflammatory, antimicrobial, antidyslipidemic, hypoglycemic, renal, and colon‐protective activity. Thus, sunflowers are plants rich in chemical compounds with pharmacological potential, which can be used as raw materials for the pharmaceutical industry.
Journals
2026 EN
Oliveira Rennan Carlos · Lopes Kheytiany Hellen da Silva · Gonçalves Mariele Rondon Santos
+6 more
ABSTRACT Pythiosis, caused by the oomycete Pythium insidiosum , is a worrying disease with its challenging treatment due to the phylogeny of the pathogen. Natural products are a promising alternative in the treatment of diseases. Cordia insignis (Boraginaceae) is a poorly studied species, but Cordia species exhibit broad bioactivity. This study investigated phytochemically the roots of the species and evaluated the anti‐oomycete activity of the crude extract (CE) and fractions against P. insidiosum . Seven compounds were isolated and identified, including β‐sitosterol, stigmasterol, campesterol, β‐sitosterol‐3‐ O ‐β‐ d ‐glucopyranosyl, tridecanoic acid, scoparone, and gracicleistanthoside. The steroids, saponin and coumarin, were reported of leaves and branches of C. insignis ; the fatty acid and glycoside are being first reported for the genus. The oomyceticidal assays revealed promising potential, with the hexane fraction (FH) being the most potent (minimum inhibitory concentration [MIC]/minimum oomicidal concentration [MOC] of 15.625 µg/mL). In conclusion, this study expands the chemotaxonomic knowledge of C. insignis and highlights the pharmacological potential of its roots against pythiosis.
Journals
2026 EN
Freitas Yanna Julie da Silva · Maciel Jéssica Bezerra · Bezerra Maria Eduarda Uchoa
+9 more
ABSTRACT This study investigated the neuropharmacological effects of arjunolic acid, with a particular focus on its anxiolytic and anticonvulsant properties. To this end, in vivo tests were performed on adult zebrafish (Danio rerio) and in silico molecular docking analyses were conducted. Acute toxicity (96 h) was evaluated with doses of 4, 20, and 40 mg/kg ( i.p .). Motor activity and anxiety levels induced by the different doses were evaluated using open field and light/dark tests, while the anticonvulsant potential was tested by induction with pentylenetetrazol (PTZ). The GABAergic neuromodulation was also investigated using the antagonist flumazenil and the molecular interaction with the GABA A receptor and carbonic anhydrase II (CAII). The results demonstrated that arjunolic acid is not toxic at the tested doses, but it does cause significant motor alterations, like those caused by diazepam. The compound exhibited an anxiolytic effect and increased the latency to the onset of convulsive seizures. These effects were reversed by flumazenil, confirming mediation by the GABAergic system. These results corroborate the in silico study, which demonstrated a possible allosteric effect of arjunolic acid on the diazepam binding region of the GABA A receptor and on the active site of CAII. However, arjunolic acid is pharmacologically relevant to the central nervous system and may serve as a basis for the development of new therapeutic agents.
Journals
2026 EN
Pournara Dimitra T. · Fotopoulou Theano · Paramel Geena
+4 more
ABSTRACT Proinflammatory cytokine interleukin (IL)‐1β is a key mediator of the inflammatory response in atherosclerosis. Targeting IL‐1β represents a new approach for the anti‐inflammatory therapy of cardiovascular diseases. Based on our previous data demonstrating that cardioprotective 6‐piperazinyl purines can effectively inhibit IL‐1β release in vascular cells, in this study, we present the synthesis of a next generation of purine analogues bearing either a furoxan moiety as a nitric oxide (NO) donor, or a (methylsulfonyl)thio group, a benzothioamide, or a 5‐phenyl‐3H‐1,2‐dithiole‐3‐thione as putative hydrogen sulfide (H 2 S) donor moieties. NO and H 2 S are gaseous signaling molecules that can reduce vascular inflammation. The new purine analogues were evaluated for their anti‐inflammatory activity by assessing their inhibitory effect on the secretion of lipopolysaccharide (LPS)‐induced IL‐1β in human aortic smooth muscle cells (HAoSMCs). Our initial findings revealed that compounds bearing a [methylsulfonyl)thio]propanoyl or [methylsulfonyl)thio]hexanoyl group (compounds MK175 and MK169 , respectively) could effectively inhibit LPS‐induced IL‐1β release in HAoSMCs.
Journals
2026 EN
Rasamalla Sai Prasanna · Bharti Jayhind · Gogu Priyadharshini
+5 more
ABSTRACT Justicia betonica L. (Acanthaceae) is a traditionally used medicinal plant with limited evidence on its anticancer mechanisms. This study integrates phytochemical profiling, molecular docking, and in vitro/in vivo evaluations to elucidate its anticancer potential. Gas chromatography–mass spectrometry (GC–MS) and liquid chromatography–mass spectrometry (LC–MS) analyses identified a diverse phytochemical repertoire, including retronecine, maritimetin, hematopodin, mangiferin 6′‐gallate, and quercetin glycosides, many reported here for the first time in J. betonica L. In silico docking revealed high binding affinities of these constituents toward multiple oncogenic targets—CDK‐2, CDK‐6, B‐cell lymphoma 2 (Bcl‐2), vascular endothelial growth factor receptor‐2 (VEGFR‐2), and insulin‐like growth Factor 1 receptor (IGF‐1R)—suggesting multi‐target inhibitory potential. The ethanolic extract of J. betonica L. exhibited selective cytotoxicity against MCF‐7, A549, and HT29 cell lines, with IC 50 values of 42.11 ± 1.64, 35.39 ± 1.02, and 29.66 ± 1.34 µg/mL, respectively, while sparing normal human umbilical vein endothelial cells (HUVECs). Acute toxicity studies confirmed safety up to 2000 mg/kg. In the Ehrlich ascites carcinoma (EAC) model, oral administration of EEJB (400 mg/kg) significantly reduced tumor volume, packed cell volume, and viable cell count, extended mean survival time, and ameliorated tumor‐induced hematological and hepatic alterations. These findings position J. betonica L. as a promising plant‐derived, multi‐target anticancer candidate, meriting further isolation of active principles and mechanistic exploration.
Journals
2026 EN
da Silva Camila Aparecida Pereira · Santos Araujo Nara juliana · OliveiraTintino Cícera Datiane Morais
+8 more
ABSTRACT Antibiotic resistance poses a serious challenge to public health, particularly in the case of Staphylococcus aureus , a Gram‐positive bacterium that employs multiple resistance mechanisms, including efflux pumps such as NorA, which extrude antimicrobial compounds from the cell and reduce antibiotic efficacy. Therefore, the search for substances capable of inhibiting these mechanisms represents a promising strategy to combat bacterial resistance. Betulinic acid (BA), a pentacyclic triterpene of the lupane type, commonly found in different parts of plants, has demonstrated various pharmacological activities, including antibacterial effects. This study investigated, through in vitro and in silico analyses, the inhibitory action of BA on the NorA efflux pump in S. aureus strains SA‐1199 and SA‐1199B. The minimum inhibitory concentrations (MICs) were determined using the broth microdilution method. Subsequently, their effects on efflux pump‐mediated antibiotic resistance were evaluated by reducing the MIC of the antibiotic and ethidium bromide (EtBr), while fluorimetry and permeability potential tests were carried out using the SYTOX Green fluorescence method. Although BA did not show intrinsic antibacterial activity, showing MIC ≥ 1024 µg/mL, it was able to decrease the MIC of norfloxacin and EtBr, as well as influence membrane permeability and increase fluorescence emission. The results, therefore, indicate that BA has considerable potential as an efflux pump inhibitor and could help in the treatment of resistant bacterial infections.
Journals
2026 EN
Oliveira Bentes Izabel Cristina · Abensour Dayane Dantas · Lima da Costa Maria Luiza
+12 more
ABSTRACT Despite its proven efficacy, Bacillus thuringiensis israelensis (Bti) has not yet been incorporated into Brazilian Ministry of Health programs targeting Anopheles spp., the primary malaria vectors. This study evaluated the larvicidal potential of the Brazilian strain BR101. The strain displayed significant activity, with mortality rates ranging from 11% ± 2% to 91% ± 5% (LC 50 = 3.13 µg/mL), accompanied by increased reactive oxygen species (54.67 ± 3 µmol H 2 O 2 ), lipid peroxidation (57.33 ± 4.5 ηmol), and oxidative protein damage (16.67 ± 2.1 nM reactive carbonyls/mg). Biochemical responses included elevated activities of superoxide dismutase (29.00 ± 3 mU/mg protein), catalase (17.00 ± 1 µmol H 2 O 2 ), glutathione peroxidase (29.00 ± 3 mmol NADPH/min/mL), mixed‐function oxidases (11.00 ± 3 nmol cytochrome/mg protein), and esterases ( α : 20.67 ± 2; β : 25.67 ± 1 µmol/min/mg). Acetylcholinesterase activity was slightly reduced (80.33 ± 7 µmol/min/mg). Ecotoxicological assays revealed no lethal effects on nontarget aquatic predators (Notonectidae, Gerridae), with 100% survival over 30 days, equivalent to controls. These findings demonstrate that Bti BR101 is effective against Anopheles larvae while being safe for nontarget organisms.
Journals
2026 EN
Jales Francisco Leandro Medeiros de Lucena · Siqueira Emerson Michell da Silva · DantasMedeiros Renato
+7 more
ABSTRACT This study investigated the phytochemical profile, cytotoxicity, and anti‐herpetic activity of the hydroethanolic extract from Scoparia dulcis L. aerial parts. Mass spectrometry revealed the presence of 15 compounds. The extract showed low cytotoxicity in Vero cells, maintaining over 80% viability at concentrations up to 250 µg/mL. In vitro antiviral assays demonstrated that the extract significantly inhibited HSV‐1 infectivity and increased cell protection at 25, 50, and 100 µg/mL. These results support the traditional medicinal use of S. dulcis and suggest its potential as a natural antiviral agent. The presence of multiple active compounds may contribute to its efficacy through synergistic effects. Overall, the findings encourage further investigation of S. dulcis as a source of bioactive molecules with potential for the development of alternative therapies against herpes simplex virus type 1.