A new monoorganotin Schiff base compound, [N-(3,5-dichloro-2-oxidobenzylidene)-4-chlorobenzyhydrazidato](o-methylbenzyl)aquatin(IV) chloride, (compound C1), was synthesized, and its structural features were investigated by spectroscopic techniques and single-crystal X-ray diffractometry. Compound C1 was exposed to several human cancer cell lines, including breast adenocarcinoma cell lines MCF-7 and MDA-MB-231, ovarian adenocarcinoma cell lines Skov3 and Caov3, and prostate cancer cell line PC3, in order to examine its cytotoxic effect for different forms of cancer. Human hepatic cell line WRL-68 was used as a normal cell line. We concentrated on the MCF-7 cell line to detect possible underlying mechanism involvement of compound C1. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay revealed the strongest cytotoxicity of compound C1 against MCF-7 cells, with a half maximal inhibitory concentration (IC50) value of 2.5±0.50 μg/mL after 48 hours treatment. The IC50 value was >30 μg/mL in WRL-68 cells. Induced antiproliferative activity of compound C1 for MCF-7 cells was further confirmed by lactate dehydrogenase, reactive oxygen species, acridine orange/propidium iodide staining, and DNA fragmentation assays. A significant increase of lactate dehydrogenase release in treated cells was observed via fluorescence analysis. Luminescent analysis showed significant growth in intracellular reactive oxygen species production after treatment. Morphological changes of necrosis and early and late apoptosis stages were observed in treated cells after staining with acridine orange/propidium iodide. DNA fragmentation was observed as a characteristic of apoptosis in treated cells. Results of the present study obviously reveal potential cytotoxic effects of compound C1 against human breast cancer MCF-7 cells.
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http://dx.doi.org/10.2147/DDDT.S87064 | DOI Listing |
Arch Microbiol
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Research Center for Pharmaceutical Ingredients and Traditional Medicine, National Research and Innovation Agency (BRIN), KST B.J. Habibie, Serpong, South Tangerang, 15314, Indonesia.
Antibacterial screening of endophytic fungi from Salacia intermedia identified Diaporthe longicolla as a potent strain exhibiting good activity against multidrug-resistant Staphylococcus aureus and Pseudomonas aeruginosa, with an MIC of 39.1 µg/mL. Scale-up fermentation and chromatographic purification of this strain yielded three known compounds, which were cytochalasin J (1), cytochalasin H (2), and dicerandrol C (3), as identified by liquid chromatography - high mass resolution mass spectrometry (LC-HRMS) and nuclear magnetic resonance (NMR) spectroscopy.
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Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, 100050, China.
Genome mining has revealed that spp. possess numerous down-regulated or cryptic biosynthetic gene clusters (BGCs). This finding hinted that our investigation of fungal secondary metabolomes is limited.
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January 2025
State Key Laboratory of Medicinal Chemical Biology, Haihe Laboratory of Sustainable Chemical Transformations, Frontiers Science Center for New Organic Matter, College of Chemistry, Nankai University, Tianjin, 300350, China.
Hypoxia is a key feature of the tumor microenvironment that leads to the failure of many chemotherapies and induces more aggressive and resistant cancer phenotypes. Up to date, there are very few compounds and treatments that can target hypoxia. BE-43547A from Streptomyces sp.
View Article and Find Full Text PDFArch Biochem Biophys
January 2025
Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok, 10110, Thailand. Electronic address:
Breast cancer is one of the most common cancers found in women worldwide. Besides the availability of clinical drugs, drug resistance and considerable side effects are concerning issues driven the needs for the discovery of novel anticancer agents. Aromatase inhibition is one of the effective strategies for management of hormone-dependent breast cancer.
View Article and Find Full Text PDFACS Appl Bio Mater
January 2025
Department of Applied Chemistry, Rajiv Gandhi Technological University, Bhopal 462033, Madhya Pradesh, India.
Deciphering the most promising strategy for the evolution of cancer patient management remains a multifaceted, challenging affair to date. Additionally, such approaches often lead to microbial infections as side effects, probably due to the compromised immunity of the patients undergoing such treatment. Distinctly, this work delineates a rational combinatorial strategy harnessing stereogenic harmony in the diphenylalanine fragment, tethering it to an amphiphile 12-hydroxy-lauric acid at the N-terminus (compounds -) such that a potential therapeutic could be extracted out from the series.
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