INTRODUCTION: Hypochlorous acid (HOCl) is a physiological molecule synthesised by neutrophils during phagocytosis and plays an active role in the destruction of all microorganisms. In general, HOCl has been demonstrated to function as an antiseptic and an agent that induces apoptosis or cell necrosis in cells, depending on the ambient concentration.The aim of this study was to examine the impact of sodium hypochlorite (NaOCI) and zinc hypochlorite (ZnOCI), derived from diverse chlorine salts, on cellular proliferation and migration in keratinocyte and fibroblast cell lines in vitro. METHODS: The effects of different concentrations of NaOCl and ZnOCl on keratinocyte and fibroblast cell lines were compared using cell viability, colony formation and wound healing assays. In addition, the presence of apoptosis in the cells was determined using the tunel method. RESULTS: The application of NaOCI and ZnOCI resulted in a notable enhancement in colony formation within keratinocyte cell lines, whereas this effect was not observed in fibroblast cell lines. In the fibroblast cell line, the application of NaOCI and ZnOCI was observed to result in the closure of the wound site. The keratinocyte cell line did not demonstrate a comparable effect. The application of NaOCI resulted in a notable reduction in apoptosis within the keratinocyte cell line, in comparison to the control group. DISCUSSION AND CONCLUSION: NaOCL and ZnOCl increased colony formation in the keratinocyte cell line and enhanced wound healing in the fibroblast cell line. These hypochlorous acid derivatives were not superior to each other in terms of activity on cell lines.

Objectives Cancer is a leading global health issue with complex causes. Conventional treatments often face challenges like drug resistance and toxicity. Plant-derived compounds such as artemisinin have gained interest due to their diverse anticancer mechanisms, including ROS generation and apoptosis induction. In this study, the biological activities of ART-FB, a hybrid compound combining benzothiophene and artemisinin, were systematically investigated for the first time. Methods ART-FB's cytotoxicity was tested on various human cancer cell lines (Caco-2, LNCaP, HeLa, A549) and HUVEC via MTT assay. Colony formation, scratch-wound, and Annexin V/PI assays were used to assess proliferation, migration, and apoptosis. Apoptotic gene expression was analyzed by qPCR. Anti-inflammatory effects were studied in LPS-stimulated RAW264.7 cells via Griess assay and qPCR. Results ART-FB showed selective cytotoxicity in Caco-2, LNCaP, HeLa, and A549 cancer cell lines, with lower toxicity in non-cancerous HUVEC cells. It effectively suppressed proliferation, colony formation, and migration, especially in LNCaP and A549 cells, suggesting potential anti-metastatic activity. Annexin V/PI staining and gene expression analysis confirmed that ART-FB induces apoptosis via both intrinsic and extrinsic pathways, with the strongest effects in LNCaP and Caco-2 cells. In LPS-stimulated RAW264.7 macrophages, ART-FB significantly reduced nitric oxide levels and downregulated iNOS, COX-2, TNF-alpha, and IL-6, while upregulating IL-10, suggesting dual anticancer and anti-inflammatory action. Conclusions ART-FB exhibits both anticancer and anti-inflammatory properties, targeting key pathways involved in tumor growth and immune response. These findings indicate that ART-FB is a promising candidate for further preclinical development as a multifunctional therapeutic agent.

Recently, increasing surgical operations and the associated rises in bacterial infections and biofilm formation have attracted interest in antibacterial coating studies. Although many studies describe antibacterial titanium (Ti) coatings, comparative evaluation of zinc oxide (ZnO) and silver nitrate (AgNO3) effects on wound healing and efficacy in chitosan systems remains limited. In this study, Ti plates were subjected to chemical etching, alkaline treatment, and silanization with (3-aminopropyl)triethoxysilane (APTES) to obtain surface activation suitable for cross-linking. Then, the activated Ti surfaces were coated by dip-coating with a chitosan-based biopolymer matrix containing antibacterial AgNO3, nano ZnO and nano hydroxyapatite (nHAp) prepared by the sol-gel method. The characterization of the samples was carried out using Fourier Transform Infrared Spectroscopy (FT-IR), Scanning Electron Microscopy (SEM), and Energy Dispersive X-ray Spectrometry (EDS). FT-IR analysis confirmed surface functionalization with peaks at 1195 cm⁻¹ (Si–OH) and 1560 cm⁻¹ (–NH₂), while SEM and EDS analyses demonstrated good coating adhesion and a homogeneous distribution of additives within the chitosan matrix. Disk diffusion tests showed that coatings containing AgNO3 exhibited high antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli, while samples containing nZnO exhibited relatively partial antibacterial activity. Moreover, both additives inhibited biofilm formation, with AgNO3 coatings showing higher inhibition, while fluorescence microscopy confirmed reduced biofilm density surfaces. Cytotoxicity and wound healing tests showed low additive concentrations supported viability and accelerated wound closure by enhancing migration. In conclusion, biopolymer coatings provide a promising strategy for Ti implants by reducing bacterial infection and biofilm formation while maintaining biocompatibility.

Natural products derived from plants are valuable sources of bioactive compounds with potential anticancer properties. This study primarily investigated the cytotoxic activities of gall extracts of Andricus caputmedusae (ACA), Andricus curtisii (ACU), and Andricus quercustozae (AQU) in human cancer cell lines (LNCaP, Caco-2, HeLa) and a non-cancerous cell line (HEK293). The phenolic compositions of the extracts were analyzed by LC-MS/MS to help interpret their biological effects. The extracts contained notable levels of shikimic acid, gallic acid, protocatechuic acid, and catechin, with AQU exhibiting the richest phenolic profile. All extracts showed marked cytotoxicity, particularly against Caco-2 cells (EC50: 17.64-19.67 µg/mL), followed by HeLa (37.06-81.31 µg/mL) and LNCaP (59.33-160.19 µg/mL), while higher EC50 values in HEK293 indicated selective anticancer potential. Apoptosis assays demonstrated that these cytotoxic effects were associated with apoptosis induction, especially in LNCaP and HeLa cells. Overall, the findings suggest that cynipid gall extracts possess promising anticancer potential linked to their phenolic constituents, warranting further in vitro and in vivo studies.

Olive oil is a natural, unrefined product obtained mechanically from olives and consumed without refining. Ranging from green to yellow, it is valued for its distinctive sensory properties. It retains bioactive compounds that enhance stability and health benefits, including anti-inflammatory, antimicrobial, antioxidant, circulation-improving, and wound-healing effects (Viola & Viola, 2009; Nasiri et al., 2015). In this study in November 2025, memecik-type olive oils were produced in six formulations: Early Harvest Cold-Pressed (EHCP), Cold-Pressed (B1), bay laurel (Laurus nobilis) leaf-flavored (D1), Origanum-flavored (K1), bitter orange (Citrus aurantium)-flavored (T1), and sage (Salvia fruticosa)-flavored (A1). Flavoring involved adding 10 kg bay laurel, 10 kg thyme, 50 kg bitter orange, or 10 kg sage to 1 ton of olives during processing. Samples were analyzed for free acidity, peroxide value, UV absorbance, aroma, and fatty acids. Biocompatibility (MTT, L929), anti-inflammatory activity (NO in LPS-stimulated RAW264.7 cells), and wound-healing activity (against L929 cell lines) were also evaluated in vitro. Aroma analysis revealed that B1 contained the highest trans-2-hexenal (42.30%). D1, K1, and A1 were rich in 1,8-cineole (22.11%, 20.97%, 17.00%), whereas T1 was dominated by D-limonene (78.36%). After 24 h, NO levels increased by 48% in the LPS control; EHCP and A1 showed no change, while B1 and D1 reduced NO by 33% and 21%, and K1 and T1 showed stronger inhibition (43% and 47%), restoring near-baseline levels. After 72 h, wound closure reached 85% in the control, with the highest healing in D1 (95%), followed by EHCP (82%), B1 (67%), T1 (62%), and K1 (42%). These findings confirm that flavoring plants enhance olive oil’s anti-inflammatory and wound-healing effects by transferring bioactive metabolites.

The development of anticancer agents capable of affecting multiple cancer-related cellular processes remains an important strategy in cancer drug discovery. In this study, a novel series of benzofuran-furan-pyrano[2,3-c]pyrazole hybrids was synthesized and comprehensively investigated through in vitro biological assays and in silico analyses. The synthesized compounds exhibited concentration-dependent cytotoxicity against LNCaP, MDA-MB-231, A549, and Caco-2 cancer cells, with EC50 values ranging from 20.49 to 274.37 µM while displaying lower toxicity toward non-malignant HUVEC cells. Among the synthesized derivatives, compounds 4j, 4h, and 4d showed the strongest antiproliferative activities and significantly suppressed cancer cell migration, invasion, and colony formation. Mechanistic studies demonstrated that the active hybrids induced G1/S phase cell cycle arrest, increased intracellular reactive oxygen species (ROS) production, disrupted mitochondrial membrane potential, and promoted apoptotic cell death. These findings were further supported by quantitative real-time PCR, which revealed downregulation of BCL2 together with upregulation of BAX, CASP3, CASP8, CASP9, and TP53, indicating activation of both intrinsic and extrinsic apoptotic pathways. In silico analysis of absorption, distribution, metabolism, excretion, and toxicity (ADMET) predicted favorable drug-likeness and pharmacokinetic properties for the synthesized hybrids. Molecular docking suggested potential interactions with CDK2, the androgen receptor, VEGFR-2, and Bcl-2, with compound 4f exhibiting the most favorable overall docking profile. Collectively, these findings demonstrate that benzofuran-furan-pyrano[2,3-c]pyrazole hybrids possess promising multifaceted in vitro anticancer activity by inhibiting cancer cell proliferation, migration, invasion, and clonogenicity while inducing ROS-mediated mitochondrial apoptosis, highlighting these hybrid scaffolds as attractive candidates for further anticancer drug development.

Colorectal, liver, and uterine cancers remain major clinical challenges due to their high prevalence and mortality. In this study, a series of artesunate-benzofuran hybrid compounds (5A-5E) were designed and synthesized through a multistep approach and structurally characterized by 1H/13C NMR, FTIR, and LC-MS/MS analyses. Their anticancer and anti-inflammatory potential was evaluated using complementary in silico and in vitro methodologies. Drug-likeness and ADMET predictions indicated favorable pharmacokinetic behavior and low toxicity. Molecular docking studies demonstrated strong binding affinities toward key cancer-related targets, DNA polymerase beta (POLB), caspase-8 (CASP8), and protein kinase A (PKA), with binding energies ranging from -91.66 to -170.97 a.u., exceeding those of tamoxifen (TAM) (-88.40 to -114.88 a.u.) and 5-fluorouracil (5FU) (-52.27 to -53.79 a.u.). Molecular dynamics simulations further confirmed the stability of the ligand-protein complexes. In vitro cytotoxicity assays against Caco-2, HepG2, and Ishikawa cell lines revealed selective anticancer activity with minimal toxicity. Compounds 5A and 5C displayed the most pronounced effects, with half maximal inhibitory concentration (IC50) values of 51.48 & micro;M (Caco-2) and 35.16 & micro;M (HepG2) for 5A, and 58.32 & micro;M (Caco-2) and 50.98 & micro;M (HepG2) for 5C. Mechanistic investigations showed apoptosis induction via caspase activation, inhibition of cell migration, G0/G1 cell-cycle arrest, and suppression of colony formation. In addition, compounds 5A-5C significantly reduced lipopolysaccharide-induced nitric oxide production in RAW 264.7 macrophages. These results support artesunate-benzofuran hybrids as promising multitarget candidates for the development of anticancer agents with concurrent anti-inflammatory activity.

Plants have long been used in the treatment of human diseases, including cancer. Recent research has increasingly focused on plant-derived secondary metabolites as potential sources of anticancer agents with reduced toxicity to healthy tissues. Essential oils represent a promising reservoir for drug discovery due to their diverse chemical compositions. This study investigated the chemical composition and anticancer potential of the essential oil obtained from Ziziphora clinopodioides subsp. rigida (ZEO), a species widely distributed and frequently consumed in Iran. Thirty-seven different compounds were identified from the essential oil, among which piperitone (22.26%), isomenthone (14.00%) and menthol (9.82%) were the main components. Cytotoxicity was evaluated against colorectal cancer cell lines (Caco-2 and HCT-116) and noncancerous cell lines (CCD-18Co and HEK293) using EC50 values, followed by apoptosis analyses through Annexin V-FITC/PI staining. The gene expression levels of apoptosis-related markers (Bax, Bcl-2, caspase-3, -8, -9, and p53) were quantified via qRT-PCR. ZEO exhibited stronger cytotoxicity in cancer cells (EC50: 19.27 mu g/mL for Caco-2; 22.72 mu g/mL for HCT-116) than in noncancerous cells (25.11 mu g/mL for CCD-18Co and 46.59 mu g/mL for HEK293). Moreover, ZEO induced apoptosis (41.01% in Caco-2; 27.58% in HCT-116), downregulated Bcl-2, and upregulated pro-apoptotic genes. To our knowledge, this is the first study highlighting the therapeutic potential of Z. clinopodioides subsp. rigida against colorectal cancer.

This study evaluated the anticancer potential of essential oils from Cedrus libani cones. Gas chromatography-mass spectrometry identified 23 compounds, mainly α-pinene (51.29%), β-pinene (31.12%), and β-phellandrene (4.12%). The cone essential oil (CEO) showed strong cytotoxicity against human melanoma (A375) cells, with an IC50 value of 7.64 μg/mL in MTT assays. Annexin V-FITC/PI staining revealed a twofold increase in apoptosis, and qRT-PCR analysis confirmed an elevated Bax/Bcl-2 ratio. CEO also suppressed proliferation and migration: colony formation decreased by nearly 40%, and wound closure was 37.8% in treated cells versus 4% in controls. These findings suggest that C. libani cone oil exerts potent cytotoxic, pro-apoptotic, anti-proliferative, and anti-migratory effects, supporting its potential as a natural anticancer agent.

Euphorbia clementei Boiss. is a perennial subshrub native to the western Mediterranean and Northwest Africa, where species of the genus Euphorbia have been traditionally used against skin irritations, digestive disorders, inflammatory conditions, and microbial illnesses. Despite this ethnopharmacological relevance, E. clementei remains underexplored. This study presents a comprehensive multi-technique analytical characterization of E. clementei, integrating HPLC-DAD, GC-MS, and ICP-MS to profile phytochemicals and minerals, correlated with bioactivity assessment. HPLC-DAD quantified key phenolics in the methanol extract, notably epicatechin (20.58 mg/g), catechin (13.92 mg/g), and pyrocatechol (14.52 mg/g), with method validation confirming excellent linearity (R2 > 0.99) and recovery (95–102

Current study was purposed to reveal the cytotoxic, apoptotic, antimicrobial and antioxidant potentials of oil extracted from Dictyota dichotoma (Hudson) J.V. Lamouroux 1809 collected from Antalya coast of Turkiye. Dictyota dichotoma oil showed better cytotoxic activity towards two different adenocarcinoma cell lines (Caco-2 (8.83 μg/mL) and LnCap (10.86 μg/mL)) compared to HEK293 cells (non-cancerous). Annexin V/PI staining and qPCR studies revealed that oil caused induction of apoptosis. Dictyota dichotoma oil inhibited the growth of Aspergillus niger ATCC 16404 and Enterococcus faecalis ATCC 29212. Nevertheless, the lower antioxidant activity of Dictyota dichotoma oil was determined compared with trolox standard for both DPPH and ABTS assays (4.8 fold less). In conclusion, Dictyota dichotoma oil has a promising potential in medical usage.

Sulfur-containing compounds exhibit diverse biological activities, including anti-inflammatory, anticancer, antioxidant, antibacterial, and antidiabetic properties. In this study, for the first time, the biological properties of methyl(2-(phenylethynyl)phenyl)sulfane (MPPS), including its antioxidant, antimicrobial, cytotoxic, anti-inflammatory, and anticancer activities, were evaluated. According to the results, MPPS did not show any remarkable antioxidant activity. However, MPPS demonstrated modest antimicrobial activity against S. aureus ATCC 25923 (MIC value: 512 mu g/mL) and B. subtilis ATCC 6633 as well as other indicator strains (MIC value: 256 mu g/mL). Additionally, the MBC values of MPPS were found to be 512 mu g/mL for the two gram-negative strains, E. coli ATCC 25922 and P. aeruginosa ATCC 27853. Furthermore, MPPS showed a dose-dependent cytotoxic effect in all tested cell lines. The EC50 values of MPPS were determined as 202.68 mu M for PANC-1, 226.63 mu M for LNCaP, and 166.27 mu M for Ishikawa cells, respectively. MPPS significantly inhibited colony formation and induced apoptosis in the cancer cell line. Moreover, MPPS exhibited notable anti-inflammatory activity in RAW264.7 cells. These findings suggest that MPPS has potential for cancer treatment and as an anti-inflammatory and antimicrobial agent. However, further studies are required to confirm these effects.

The search for novel therapeutic agents has led to increasing interest in natural products, driven by the recognition that they may offer safer and more sustainable alternatives to synthetic drugs. This study aims to fill the gap in knowledge regarding the biological activity and safety of the water extract of chestnut (Castanea mollissima) (chestnut), a plant species with a long history of use in traditional medicine, by conducting a comprehensive evaluation of its antioxidant, antidiabetic, and neuroprotective properties. This study presents a comprehensive analysis of the water extract of chestnut for the first time using various bioanalytical antioxidant methods. The extract's inhibitory effects on key enzymes like acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase were evaluated due to their relevance in metabolic and neurodegenerative disorders such as diabetes and Alzheimer's disease. Developmental toxicity and cytotoxicity were assessed using zebrafish (Danio rerio) embryos to evaluate the extract's biological safety. The major phenolic compounds present in the extract were identified by liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS), revealing catechin, gallic acid, taxifolin, and epicatechin as the predominant constituents. Antioxidant capacity was determined through radical scavenging assays using 2,2-diphenyl-1-picrylhydrazyl (DPPH•) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•+), alongside ferric (Fe3+), cupric (Cu2+), and Fe3+-TPTZ (ferric-tripyridyltriazine) reducing power assays. The findings highlight the significant antioxidant, antidiabetic, and neuroprotective potential of the chestnut water extract, supporting its prospective use in pharmaceutical and nutraceutical applications.

The cytotoxic activities of apolar extract of Lactarius salmonicolor and its fractions and subfractions were screened against colon (CaCo-2), prostate (LNCaP), lung (H1299), and breast (MCF-7) cancerous cell lines. The main extract of Lactarius salmonicolor that was cytotoxic to CaCo-2 (EC50: 137.1 +/- 2.7 mu g/mL) and LNCap (EC50: 131.2 +/- 2.6 mu g/mL) mainly contains fatty acids (99.9%). To characterize the cytotoxic activity, it was fractionated by a silica gel column. Two cytotoxic fractions were re-fractionated to obtain subfractions. The extract, four cytotoxic fractions, and all subfractions were analyzed by gas chromatography-mass spectrometry (GC-MS). The GC-MS data and the cytotoxic activity (EC50) results were classified using principal component analyses (PCA). According to PCA, the cytotoxic fractions containing abundant benzoic acid (0.01%-0.35%), cinnamic acid (0.01%-0.36%), azelaic acid (0.01%-0.92%), 2,4-decadienal (0.01%-0.12%), (Z)-9-palmitoleic acid (0.01%-1.09%), 18-hydroxy 2,4-diene oleic acid (0.01%-26.71%), arachidic acid (0.01%-6.70%), desmosterol (0.01%-12.27%), and steroids (0.01%-9.51%) were clustered. LSP.9-10, which causes another cluster, is caused by 8,11,14- eicosatrienoic acid, 11,14,17-eicosatrienoic acid, 9(Z)-decenoic acid compounds, and saturated fatty acids with 10 and 16 carbons. Hence, these compounds may be responsible for the cytotoxic activity. This study demonstrates that GC-MS and chemometric analysis can identify the components responsible for biological activity in combination with biological activity data.

An amide-bridged artesunate-indole hybrid molecule (TRY-ART) was investigated for its anticancer and anti-inflammatory activities. Cytotoxicity studies revealed that TRY-ART exhibited significant cytotoxicity against Caco-2, LNCaP, HepG2, Ishikawa, and A549 cancer cell lines, with EC50 values of 120.2 +/- 1.14, 79 +/- 0.54, 137.9 +/- 0.78, 94 +/- 2.37, and 183 +/- 1.65 mu M, respectively. Apoptosis analysis demonstrated that TRY-ART significantly induced apoptotic events in all tested cancer cell lines. It revealed its pro-apoptotic potential by upregulating the expression levels of pro-apoptotic genes (BAX, CASP3, CASP8, CASP9, and P53) and downregulating the anti-apoptotic gene BCL2. Colony-formation assays showed a reduction in colony formation capacity, and wound-healing assays indicated its efficacy against cell migration. qRT-PCR analysis revealed strong anti-migration effects by downregulating migration-related genes (MMP2 and MMP9) and upregulating their inhibitors (TIMP1 and TIMP2). Furthermore, anti-inflammatory evaluation by the Griess method in Lipopolysaccharide (LPS)-induced RAW264.7 macrophages revealed that TRY-ART suppressed nitric oxide production by 35% and significantly downregulated pro-inflammatory genes (Cox-2, Inos, Tnf-alpha, and Il6) while upregulating the anti-inflammatory gene Il10. In conclusion, the newly synthesized amide-bridged artesunate-indole hybrid molecule, TRY-ART, exhibits promising anticancer and anti-inflammatory properties.

The pomegranate (Punica granatum L.) is recognized for its wide-ranging applications in phytotherapy, traditional cuisine, and the agri-food sector. In this study, we investigated the phytochemical composition, antioxidant potential, and cytotoxic activity of lyophilized peel extracts from three Algerian cultivars: “Hamedh,” “Adhmi,” and “Sefri.” These locally cultivated varieties were selected for their commercial relevance and phenotypic differences. The results revealed significant inter-cultivar variations in total phenolics, flavonoids, flavonols, and tannins, with the Hamedh cultivar exhibiting the highest levels of key bioactive compounds. LC-MS/MS profiling identified ten major constituents, including phenolic acids (gallic acid and p-coumaric acid) and flavonoids (quercetin and rutin), which are known to modulate oxidative stress and induce apoptosis in cancer cells. The Hamedh extract demonstrated the strongest antioxidant activity across DPPH, ABTS, and CUPRAC assays. All extracts exhibited selective cytotoxic effects against Caco-2 colorectal cancer cells, while the LnCap prostate cancer cell line showed notable sensitivity to the Adhmi extract. No significant cytotoxicity was observed in H1299 or MCF-7 cells. These findings suggest that Algerian pomegranate peels—particularly from the Hamedh cultivar—are a promising natural source of antioxidant and anticancer agents. They hold potential for application in pharmaceutical formulations and as bio-based preservatives in the food industry.

Viscum album L. (mistletoe) is known to have important medicinal properties despite being a semiparasitic plant living in trees. The plant is widely described as effective in treating diseases such as hypertension, diabetes, arthritis, inflammation, and cancer thanks to its important bioactive components. In our study, the cytotoxic effects of methanol extract obtained from V. album subsp. austriacum (VAA) on human colon (Caco-2), human embryonic kidney (HEK293), and human prostate cancer (LNCaP) cells were investigated. Also, the phytochemical content (LC-ESI-MS/ MS), antioxidant (ABTS(center dot)+, DPPH center dot), enzyme inhibitory (alpha-amylase and alpha-glucosidase) properties of the extract were investigated. Moreover, the inhibitory property of the main component molecule against human androgen receptor and the sodium-glucose transporter (SGLT) protein was calculated theoretically by molecular docking. Additionally, the stability of the complex was studied by performing molecular dynamic (MD) simulations and this was confirmed by calculating the binding energy with MM/PBSA. The LC-ESI-MS/MS results showed that chlorogenic acid (155.681 mu g/100 g) was detected at high concentrations in the plant extract. Although the extract exhibited lower activity than the standards in ABTS(center dot)+, DPPH center dot results, it displayed higher activity against alpha-glucosidase and alpha-amylase. Besides this, chlorogenic acid and the SGLT protein were found to have a high binding energy (8.20 kcal/mol) in their interactions. Also, the MTT cell viability test showed a cytotoxic effect against LNCaP (EC50: 53.075 mu g/mL) and Caco-2 (EC50: 68.88 mu g/mL) cell lines. According to the MD result, chlorogenic acid was more stable and had a higher binding energy (-40.69 kcal/mol) towards the human androgen receptor. The data shows that V. album exhibits antioxidant, antidiabetic, and anticancer activities.

This study evaluated the bioactivity of pomegranate peel, particularly after simulated gastrointestinal digestion, in an in-vitro Alzheimer's disease model. Human glioblastoma U87MG cells exposed to Aβ1-42 were used to assess the effects of both digested and non-digested pomegranate peel on Aβ aggregation and inflammatory responses. In-vitro digestion simulated oral, gastric, and intestinal phases, and polyphenol profiles were analyzed before and after digestion. Cytotoxicity was examined using MTT assays, Aβ disaggregation by ELISA, and fibril morphology by field emission scanning electron microscopy (FESEM). Anti-inflammatory activity was evaluated via qRT-PCR in LPS-stimulated Raw264.7 macrophages, focusing on iNOS, IL-6, TNF-α, NF-κB, COX-2, and IL-10 expression. Despite partial degradation during digestion, both forms of peel retained bioactivity. At non-toxic concentrations, they supported cell viability and reduced Aβ aggregation (57.21% for non-digested, 42.11% for digested peel). FESEM confirmed fibril disruption, and both forms downregulated pro-inflammatory genes while enhancing IL-10 expression. These findings suggest that pomegranate peel, even after digestion, preserves anti-amyloidogenic and immunomodulatory activities in-vitro, supporting its potential as a dietary ingredient that merits further investigation in the context of Alzheimer's disease.

Background: Heterocyclic compounds hold a significant position in pharmaceutical chemistry owing to their extensive range of biological activities. Objective: It was aimed to investigate the antioxidant, anticancer and antimicrobial activities of two newly synthesized thiophene derivatives (3 and 5), their basic ADME/T properties in silico and their effects on the acetylcholinesterase enzyme in vitro and in silico. Methods: Thiophene derivatives were synthesized via Sonogashira Coupling reaction. These derivatives were characterized using HRMS, 1H NMR and 13C NMR. The biological evaluation encompassed antioxidant, antimicrobial, and apoptotic assays, as well as enzyme inhibition studies. Computational analysis included molecular docking and ADME/T profiling. Results: Compound 3 exhibited significantly high cytotoxic activity than 5 on A549, Caco-2 and HepG2 cancer cell lines, except LNCaP. Similarly, Compound 3 exhibited better apoptotic activity than 5 in all cancer cell lines when compared by the Annexin V-FITC/PI method. Furthermore, 3 showed better apoptotic activity than paclitaxel in the LNCaP cell line. qPCR analysis showed that 3 and 5 upregulated proapoptotic genes (BAX, CASP3, CASP8 and CASP9) and downregulated antiapoptotic gene BCL2. ADME analysis showed that both thiophene derivatives passed Lipinski's rule of five and could pass almost freely through the gastrointestinal and especially the Blood-Brain Barrier. In addition, 3 was more embedded in the narrow gorge formed by the catalytic triad in the active site (SER203-GLU334-HIS447) than 5 by molecular docking analysis. Conclusion: Consequently, 3, which was synthesized for the first time and whose biological properties were investigated within the scope of this study, seems to have potential in both cancer and Alzheimer's disease treatment.

Natural products are essential sources for the discovery and development of new anticancer drugs due to their biological activities and minimal side effects. Artemisinin is the best natural product with anti-malarial agent, and it has a variety of biological activities. Moreover, benzothiophene is a heteroaromatic compound known for its diverse biological activities. In this study, the cytotoxic, apoptotic, and anti-inflammatory activities of benzothiophene-artemisinin hybrids (BTPART and BTFART) were investigated. The MTT assay confirmed that these hybrids exhibited dose-dependent cytotoxic effects on Caco-2, HepG2, LNCaP, MDA-MB-231, MCF-7, HeLa, and Ishikawa cell lines. These hybrids also significantly reduced colony formation and demonstrated antimetastatic properties in Caco-2, HepG2, LNCaP, and MDA-MB-231 cell lines. The apoptotic effects of the hybrids were analyzed by using flow cytometry and qPCR by evaluating apoptosis-related genes (Bcl-2, Bax, Casp-3, Casp-8, Casp-9, and P53). The results indicated that both hybrids effectively induced apoptosis. In addition, both molecules display anti-inflammatory properties by reducing nitric oxide (NO) production and suppressing key inflammatory markers, including COX2, iNOS, IL-6, and TNF-alpha, while increasing IL-10 expression. As a result, benzothiophene-artemisinin hybrids have potential as therapeutic candidates for cancer treatment, particularly in liver and prostate cancers, and may also be beneficial in managing inflammatory diseases.