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The present study investigates the chemical profile and biological activities of Polygonum istanbulicum M. Keskin, a species endemic to Turkey, aiming to explore its potential applications in pharmacology. We assessed its phenolic and flavonoid content by employing ethyl acetate, methanol, and water as extraction solvents. The methanol extract demonstrated the highest concentrations of these compounds, with liquid chromatography–quadrupole time-of-flight tandem mass spectrometry (LC-MS-qTOF) analysis identifying a wide range of bioactive substances, such as derivatives of quercetin and myricetin. Antioxidant capacity was evaluated using 2,2-Diphenyl-1-picrylhydrazyl (DPPH), 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), cupric-reducing antioxidant capacity (CUPRAC), ferric-reducing antioxidant power (FRAP), and phosphomolybdenum assays, with the methanol extract showing the most potent activity (DPPH: 892.22 mg Trolox equivalent (TE)/g; ABTS: 916.21 mg TE/g; CUPRAC: 1082.69 mg TE/g; FRAP: 915.05 mg TE/g). Enzyme inhibition assays highlighted the efficacy of P. istanbulicum extracts against key enzymes, with potential implications for managing Alzheimer's disease, hyperpigmentation, and type 2 diabetes. Cytotoxicity tests against various cancer cell lines showed notable activity, particularly with the aqueous extract on the HGC-27 cell line (IC50: 29.21 µg/mL), indicating potential for targeted anti-cancer therapy. Molecular docking and molecular dynamics simulations further supported the binding affinities of quercetin and myricetin derivatives to cancer-related proteins, suggesting significant therapeutic potential. This study underscores the value of P. istanbulicum as a source of bioactive compounds with applications in antioxidant, anti-cancer, and enzyme-inhibitory treatments. [ABSTRACT FROM AUTHOR]

Aim: Colon cancer is the most common cancer worldwide. Surgery and chemotherapy are widely used in treatment. Recently, the therapeutic properties of natural products, including Cedrus libani, have been investigated for drug development. Cedrus libani extract (cedar tar) has antimicrobial and anticancer properties that can mediate metabolic pathways. Metabolic changes have been identified as the hallmark of cancer, and therefore research has focused on metabolic biology and drugs in basic and clinical studies. This study aims to investigate the effects of cedar tar on the amino acid metabolism in the colon cancer cell line of HCT-116. Materials and Methods: HCT-116 was homogenized in the phosphate buffered saline medium after being incubated with 30 µg/mL of cedar tar for 24 hours. The intracellular free amino acid profile in the samples was analyzed by liquid chromatography-mass spectrometry/mass spectrometry. Statistical data analysis was performed with SPSS V22 and MetaboAnalyst 5.0 programs. Results: We uncovered with cedar tar treatment that apoptotic β-alanine and anserine levels increased, p<0.05, and pro-tumorigenic O-phosphorylethanolamine level decreased, p<0.05. Conclusion: Cedar tar may be speculated to suppress the metastatic character and inhibits energy metabolism by increasing antiproliferative β-alanine and anserine amino acids and diminishing pro-tumorigenic O-phosphorylethanolamine amino acid in colon cancer cells. However, future interventional studies mediating β-alanine, anserine and O-phosphorylethanolamine amino acid levels in cancer and wild-type cells are required to conclude those as biomarkers or therapy candidates. [ABSTRACT FROM AUTHOR]

The objective of this investigation was to assess the cytotoxic, antioxidant, and enzyme inhibitory properties of the aerial portions of Nitraria schoberi (family Nitrariaceae). Extracts were prepared by sequential maceration in hexane, dichloromethane (DCM), ethyl acetate and methanol (MeOH) and water extract was prepared by infusion. DCM and MeOH extracts accumulated the highest amount of metabolites where the former was characterized by the presence of octadecyl ferulate (16.96 mg/100 mg), methoxyluteolin (8.48 mg/100 mg) and isorhamnetin (5.35 mg/100 mg) and the alkaloids perlolyrine (5.03 mg/100 mg), (+)-5a-hydroxylemannine (2.43 mg/100 mg) and matrine (2.40 mg/100 mg). Results of antioxidant activity showed that the MeOH extract exerted the highest anti-2,2-diphenyl-1-picrylhydrazyl (DPPH) (28.13 mg Trolox equivalent (TE)/g) and Fe+++ (54.38 mg TE/g) reducing capacity. All extracts exerted significant acetylcholinesterase (3.71–4.37 mg galantamine equivalent (GALAE)/g) and tyrosinase (86.40–109.63 mg kojic acid equivalent (KAE)/g) inhibition activity. The best α-amylase and α-glucosidase inhibition was exhibited by the DCM (0.81 mmol ACAE/g) and MeOH (1.34 mmol ACAE/g) extracts respectively. The highest cytotoxic effect was exerted against the breast adenocarcinoma (MDA-MB-231) (IC 50 : 26.71 μg/mL) and cervix adenocarcinoma (HELA) (IC 50 : 29.10 μg/mL) cell lines by the MeOH and DCM extracts respectively. In addition, we performed molecular docking analysis to understand the interaction between chemical components and tested enzymes and cellular targets for cancer. Chrysoeriol-3-O-rutinoside bound strongly to AChE. Furthermore, a good interaction between vascular endothelial growth factor receptor 2 (VEGFR2) and isovitexin-2″-O-arabinoside was observed. We employed network pharmacology to understand the role of N. schoberi's compounds in neurological disorder like Alzheimer and multiple sclerosis. Therefore, the results of this study indicate that N. schoberi may serve as a viable starting point for the future creation of phytopharmaceuticals that target particular diseases associated with oxidative stress, such as diabetes and certain neurological disorders. [ABSTRACT FROM AUTHOR]

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AbstractObjectivesMethodsResultsConclusionFive solvent extracts (n-hexane, ethyl acetate, ethanol, ethanol/water (70%), and water) of Gladiolus italicus Mill. from Turkey were evaluated for chemical and biological properties.Antioxidant activities, inhibitory properties against key enzymes involved in the etiology of chronic diseases were tested, as well as cytotoxic effects on different cell lines. Chemical characterization was also carried out to determine the most abundant compounds of each extract.The highest total phenolic content (TPC) was observed in the water extract while highest TFC in ethanol/water extract. The most abundant compounds in the extracts were hyperoside (69041.06 mg kg−1), isoquercitrin (46239.49 mg kg−1), delphindin-3,5-diglucoside (42043.81 mg kg−1), myricetin (21486.61 mg kg−1), and kaempferol-3-glucoside (21199.76 mg kg−1). Molecular dynamic (MD) simulations confirmed the structural stability and dynamic conformational integrity of these complexes over a period of 100 ns. In network pharmacology, A total of 657 unique target genes were screened: 52 associated with programmed cell death-1 (PD-1), 85 with vascular endothelial growth factor receptor-2 (VEGFR2), and 130 with fibroblast growth factor receptor-2 (FGFR2), identifying crucial gene interactions for these proteins. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted, revealing significant interactions and pathways such as the advanced glycation end products (AGE) and their receptors (RAGE) signaling pathway in diabetic complications and T- helper 17 (Th17) cell differentiation, among others. This elucidation of complex networks involving key genes like AKT Serine/Threonine Kinase 1 (AKT1), MYC proto-oncogene (MYC), tumor protein 53 (TP53), Interleukin 6 (IL6), and tumor necrosis factor (TNF) provides a promising foundation for the development of targeted therapies in the treatment of non-communicable diseases.These results show that G. italicus could be a natural source of potent antioxidants and enzyme inhibitors which need to be further explored for the development of biopharmaceuticals. [ABSTRACT FROM AUTHOR]