A new procedure was developed for the rapid isolation of the A, E and F series prostaglandins from plasma extracts. This new procedure involves the use of mini-columns packed with acid-washed Florisil to rapidly separate the A, E and F series prostaglandins. These new mini-columns give flow rates of around 1 ml/min. and they generate a well-resolved chromatographic pattern while at the same time producing good recoveries for [3H]-labeled prostaglandins of the A, E and F series. Using these new mini-columns, large numbers of plasma extracts can be processed in a short period of time.
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http://dx.doi.org/10.1016/0090-6980(79)90038-8 | DOI Listing |
J Clin Med
December 2024
Department of Ophthalmology, Shimane University Faculty of Medicine, Izumo 693-8501, Japan.
: To report the role of prostaglandin-associated periorbitopathy (PAP) severity on the surgical efficacy of Ahmed Glaucoma Valve (AGV) implantation. : Retrospective observational case series. Participants were the consecutive 102 eyes from 102 Japanese subjects (55 males, 47 females; mean age ± standard deviation, 74.
View Article and Find Full Text PDFBioorg Med Chem Lett
January 2025
Department of Chemistry, Simon Fraser University Burnaby British Columbia Canada. Electronic address:
Prostaglandin E receptor type 4 (EP4) agonists have been shown to be effective in treating experimental ulcerative colitis (UC) in animals and in human clinical trials, but their development has been impeded by unacceptable systemic side effects. In this study, a series of methylene phosphate prodrugs of a highly potent and selective prostaglandin EP4 receptor agonist were designed to target and remain localized in the gastrointestinal (GI) tract after either oral or rectal instillation. The prodrugs were designed to be converted to liberate active EP4 agonist by intestinal alkaline phosphate (IAP), a ubiquitous enzyme found at the luminal of the intestinal wall thus exposing the colon epithelial barrier while reducing systemic exposure to the active agonist.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Medical Department III, Munich University Hospital, 81377 Munich, Germany.
There is a high medical need to develop new strategies for the treatment of patients with acute myeloid leukemia (AML) refractory to conventional therapy. In vitro, the combinations of the blast-modulatory response modifiers GM-CSF + Prostaglandin E1, (summarized as Kit M) have been shown to convert myeloid leukemic blasts into antigen-presenting dendritic cells of leukemic origin (DC) that were able to (re-)activate the innate and adaptive immune system, direct it specifically against leukemic blasts, and induce memory cells. This study aimed to investigate the immune modulatory capacity and antileukemic efficacy of Kit M in vivo.
View Article and Find Full Text PDFJ Med Chem
January 2025
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai 200241, China.
The development of dual prostaglandin E receptors 2/4 (EP2/EP4) antagonists represents an attractive strategy for cancer immunotherapy. Herein, a series of 4,7-dihydro-5-thieno[2,3-]pyran derivatives with potent EP2/EP4 dual antagonism were discovered by fine-tuned structural modifications. The biphenyl side chain was found to be the key pharmacophore for the transition from EP4 antagonism to EP2/EP4 dual antagonism.
View Article and Find Full Text PDFACS Omega
December 2024
Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, 29 Geumgu-gil, Jeongeup 56212, Republic of Korea.
Inducible cyclooxygenase-2 (COX-2) is a crucial enzyme involved in the processes of inflammation and carcinogenesis, primarily by catalyzing the production of prostaglandin E2 (PGE2), a significant mediator of inflammation. In this study, we designed and synthesized a series of novel chrysin derivatives to evaluate their anti-inflammatory potential through COX-2 inhibition using cultures of RAW264.7 macrophages and molecular docking assays.
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