Esterification of 3-hydroxyl group in 11-acyloxyestra-1,3,5(10)-trienes with p-[bis(2-chloroethyl)amino]phenylacetic acid led to antitumor steroids displaying antiestrogenic and cytotoxic activities. Our substances exhibit their activities on the model of murine mammary adenocarcinoma Ca-755, with inhibition of the tumor growth being 94-99%. A new approach was used for the 11alpha-hydroxylation of estra-1,3,5(10)-trienes.
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Int J Mol Sci
December 2024
Department of Pharmacology and Nutritional Sciences, University of Kentucky College of Medicine, Lexington, KY 40536, USA.
Sepsis is a life-threatening condition resulting from a dysregulated host response to infection. Currently, there is no effective therapy for sepsis due to an incomplete understanding of its pathogenesis. Scavenger receptor BI (SR-BI) is a high-density lipoprotein (HDL) receptor that plays a key role in HDL metabolism by modulating the selective uptake of cholesteryl ester from HDL.
View Article and Find Full Text PDFBioorg Chem
January 2025
Department of Chemistry, Faculty of Sciences and Mathematics, University of Niš, Višegradska 33, 18000 Niš, Serbia. Electronic address:
Numerous compounds with useful biological activities were previously prepared by tethering ferrocene to natural product scaffolds. Some conjugates of ferrocene and steroids in particular were demonstrated to act as both potent and selective antiproliferative agents. Motivated by a lack of structural diversity in the pregnane series of conjugates, we performed chemical modifications of several naturally occurring progestogens, their biosynthetic precursors and chemically related derivatives so as to obtain conjugates 1-8, in which the steroid skeleton and ferrocene core are linked by the steroid sidechain.
View Article and Find Full Text PDFTherap Adv Gastroenterol
December 2024
Department of Gastroenterology, Asan Medical Center, University of Ulsan College of Medicine, 88 Olympic-ro 43-gil, Songpa-gu, Seoul 05505, Republic of Korea.
Background: Immune checkpoint inhibitor (ICI)-induced colitis is a significant adverse event associated with ICI therapy, known to be linked to increased cytotoxic T-cell activity.
Objectives: To compare T-cell subsets based on the endoscopic features of ICI-induced colitis and to compare these findings with those of inflammatory bowel disease (IBD).
Design: Prospective cohort study.
J Fungi (Basel)
December 2024
Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, College of Chemistry and Chemical Engineering, Hainan Normal University, Haikou 571158, China.
The genus have long been recognized as a source of structural novel, pharmaceutically relevant natural products. We reviewed the structures and activities of secondary metabolites isolated from the genus of from January 1995 to June 2024, and 280 compounds, including six major categories-terpenoids, alkaloids, polyketides, polyphenols, steroids, and other classes-are presented in this review. Among these metabolites, 196 were identified as new structures.
View Article and Find Full Text PDFMar Drugs
December 2024
Centre for Bioinnovation, University of the Sunshine Coast, Maroochydore BC, QLD 4558, Australia.
Saponins are a diverse class of secondary metabolites that are often reported to exhibit a variety of pharmacological applications. While research into the elucidation and application of plant and class Holothuroidea-derived saponins (i.e.
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