98%
921
2 minutes
20
Anithiactin D (), a 2-phenylthiazole class of natural products, was isolated from marine mudflat-derived actinomycetes sp. 10A085. The chemical structure of was elucidated based on the interpretation of NMR and MS data. The absolute configuration of was determined by comparing the experimental and calculated electronic circular dichroism (ECD) spectral data. Anithiactin D () significantly decreased cancer cell migration and invasion activities at a concentration of 5 μM via downregulation of the epithelial-to-mesenchymal transition (EMT) markers in A549, AGS, and Caco-2 cell lines. Moreover, inhibited the activity of Rho GTPases, including Rac1 and RhoA in the A549 cell line, suppressed RhoA in AGS and Caco-2 cell lines, and decreased the mRNA expression levels of some matrix metalloproteinases (MMPs) in AGS and Caco-2 cell lines. Thus , which is a new entity of the 2-phenylthiazole class of natural products with a unique aniline-indole fused moiety, is a potent inhibitor of the motility of cancer cells.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10889970 | PMC |
http://dx.doi.org/10.3390/md22020088 | DOI Listing |
Med Oncol
August 2025
Department of Molecular Biology and Genetics, Faculty of Science, Istanbul University, Istanbul, 34134, Türkiye.
Digestive system tumors, including gastric and colorectal cancers, have notable global incidence and mortality rates. While 5-Fluorouracil (5-FU) is widely used in treating gastrointestinal (GI) cancers, resistance often limits its effectiveness. Recent research has focused on the potential of natural products, such as propolis, a resin produced by honeybees, as adjuncts in cancer therapy.
View Article and Find Full Text PDFMolecules
April 2025
Centro de Química, Universidade do Minho (CQ-UM), Campus de Gualtar, 4710-057 Braga, Portugal.
Tricyclic and tetracyclic lactone derivatives of thieno[2,3-]pyrazine or thieno[2,3-]quinoline, and 2-pyrones were prepared using different methodologies. Pd/Cu-catalyzed Sonogashira coupling using EtN as a base, of methyl 7-bromothieno[2,3-]pyrazine-6-carboxylate and (het)arylalkynes to yield the Sonogashira ester products, gave also the corresponding tricyclic lactones as minor products. However, the major products did not cyclize with TFA.
View Article and Find Full Text PDFEur J Pharm Biopharm
May 2025
Department of Pharmaceutics, University of Minnesota, Minneapolis, MN 55455, USA; Department of Biomedical Engineering, University of Minnesota, Minneapolis, MN 55455, USA. Electronic address:
The objective of this study was to develop a scheme to predict intestinal and plasma concentration-time profiles of the weakly basic BCS-II drug, dipyridamole (DPD), using an Artificial Gut Simulator (AGS) integrated with a compartment-based disposition model. In vivo data for this study was obtained from previously published literature. A 3-compartment disposition model was developed using the plasma concentration-time profile of DPD following an intravenous bolus dose.
View Article and Find Full Text PDFJ Complement Integr Med
June 2025
Department of Bioengineering, Faculty of Chemical and Metallurgical Engineering, Yildiz Technical University, Istanbul, Türkiye.
Objectives: Colorectal cancer and gastric cancer are one of the most prevalent types of cancer and are leading causes of cancer-related mortality worldwide. The chemotherapy is insufficient due to the poor targeting and affinity of drugs, low therapeutic effectiveness, and significant side effects. Consequently, developing effective therapeutic formulations is crucial for treating colorectal and gastric cancers.
View Article and Find Full Text PDFActa Crystallogr C Struct Chem
April 2025
Screening of Biological Activity Assays and Collection of Biological Material Laboratory, Wrocław Medical University Biobank, Faculty of Pharmacy, Wrocław Medical University, 211A Borowska, 50-556 Wrocław, Poland.
The newly obtained compound 7-(4-chlorophenyl)-1-hydroxy-5-methylpyrido[3,4-d]pyridazin-4(3H)-one (CPM) was crystallized as two new variable solvates, namely, the dimethyl sulfoxide monosolvate, CHClNO·CHSO (I), and the sesquisolvate, CHClNO·1.5CHSO (II), and their structures were confirmed by single-crystal X-ray diffraction analysis. In previous work, 1-hydroxy-5-methyl-7-phenylpyrido[3,4-d]pyridazin-4(3H)-one (PM) was found to display anticancer activity.
View Article and Find Full Text PDF