Co-crystallisation of diphenyl phosphate (Hdpp) with anticancer active Pt(IV) complexes of the type cis,trans,cis-[PtCl(2)(OH)(2)(am(m)ine)(2)] has produced a new type of supramolecular adduct with short hydrogen bonds from the Hdpp molecules to the hydroxide ligands in all cases. X-ray crystallographic analysis showed within the adduct cis,trans-[PtCl(2)(en)(OH(2))(2)](dpp)(2) (1) a hydrogen bond length of 2.341(6) Å; the shortest O ··· O distance reported in the literature. Similar, though longer hydrogen bonds were observed in three other complexes: [PtCl(2)(OH)(NH(3))(2)(OH(2))]dpp·3H(2)O (2), trans-[Pt(mal)(OH)(OH(2))(S,S-chxn)]dpp·3H(2)O (3), and trans-[Pt(ox)(OH)(OH(2))(S,S-chxn)]dpp·2H(2)O (4). Co-crystallisation with Hdpp leads to higher aqueous solubility than the parent complexes indicating the potential of the adducts for use as active pharmaceutical ingredients. Anticancer testing of [Pt(mal)(OH)(OH(2))(S,S-chxn)]dpp·3H(2)O (3) showed in vitro cytotoxicity is low, as expected for Pt(IV) prodrugs, yet substantial tumour growth inhibition was observed in an in vivo ADJ/PC6 tumour model, with activity retained at maximum tolerated dose (MTD)/2 and MTD/4.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.jinorgbio.2012.04.010 | DOI Listing |
J Hazard Mater
January 2025
Laboratory of Environmental Toxicology, Chulabhorn Research Institute, Bangkok 10210, Thailand; Center of Excellence on Environmental Health and Toxicology (EHT), OPS, Ministry of Higher Education, Science, Research and Innovation, Bangkok, Thailand. Electronic address:
2-Ethylhexyl diphenyl phosphate (EHDPP) is a replacement flame-retardant commonly found in several environmental matrices and human biospecimens. Although some adverse effects of EHDPP have been identified, the endocrine-disrupting effects of EHDPP and its key metabolites on the human estrogen receptor (ER) are largely unknown. Herein, we report for the first time that EHDPP, at concentrations found in the environment and humans, significantly promoted estrogenic activity and synergized with 17β-estradiol-induced ER transactivation.
View Article and Find Full Text PDFAntioxidants (Basel)
December 2024
Department of Biomaterials Science (BK 21 FOUR Program), Life and Industry Convergence Research Institute, College of Natural Resources and Life Science, Pusan National University, Miryang 50463, Republic of Korea.
Oxidative stress is the key cause of the etiopathogenesis of several diseases associated with constipation. This study examined whether the green pine cone can improve the symptoms of constipation based on the antioxidant activities. The changes in the key parameters for the antioxidant activity and laxative effects were examined in the loperamide (Lop)-induced constipation of Sprague-Dawley (SD) rats after being treated with the methanol extracts of green pine cone (MPC, unripe fruits of ).
View Article and Find Full Text PDFWater Res
January 2025
College of Environmental Science and Engineering, North China Electric Power University, Beijing 102206, China. Electronic address:
The ubiquitous presence, potential toxicity, and persistence of 2-ethylhexyl diphenyl phosphate (EHDPP) in the environment have raised significant concerns. In this study, we successfully isolate a novel microbial consortium, named 8-ZY, and we demonstrate its remarkable ability to degrade EHDPP using an extremely low concentration of the inoculate. A total of 11 degradation metabolites were identified, including hydrolysis, hydroxylated, methylated, glucuronide-conjugated, and previously unreported byproducts, enabling us to propose new transformation pathways.
View Article and Find Full Text PDFMol Med
January 2025
Jaseng Spine and Joint Research Institute, Jaseng Medical Foundation, Gangnamdae-ro 540, Seoul, 135-896, Republic of Korea.
Background: Inflammation is a critical protective response in the body, essential for combating infections and healing injuries. However, chronic inflammation can be harmful and significantly contribute to the development and progression of chronic diseases, with macrophage-mediated responses being central to these processes. This study presents "SBR-Pel," a new therapeutic blend of Shinbaro tab (SBR), a traditional herbal formula, and pelubiprofen (Pel), a non-steroidal anti-inflammatory drug, and investigated their combined anti-inflammatory effects to create a treatment that both improves efficacy and reduces side effects.
View Article and Find Full Text PDFThe Aim Of The Study: Was to elaborate and assess biocompatible compositions based on oligocarbonate methacrylate filled with hydroxyapatite.
Materials And Methods: The manufacturing methods of the compositions are considered, and their polymerization ability, strength and elastic properties are evaluated.
Results: The highest values of hardness and elasticity were found in the composition containing 0.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!