The inclusion mode of Limaprost in the presence of α- and β-cyclodextrins (CDs) was investigated to gain insight into the stabilization mechanism of Limaprost-alfadex upon the addition of β-CD in the solid state. The inclusion sites of α- and β-CDs were studied by NMR spectroscopic and kinetic methods. With the addition of α- and β-CDs, displacements in (13)C chemical shifts of prostaglandin F2α (PGF2α) were observed in the ω-chain and the five-membered ring, respectively, of the drug. Similar shift changes were observed with the addition of both α- and β-CDs. In two-dimensional (2D) (1)H-NMR spectra, intermolecular correlation peaks were observed between protons of PGF2α and protons of both α- and β-CDs, suggesting that PGF2α interacts with α- and β-CDs to form a ternary complex by including the ω-chain with the former CD and the five-membered ring with the latter. In kinetic studies in aqueous solution, Limaprost was degraded to 17S,20-dimethyl-trans-Δ(2)-PGA1 (11-deoxy-Δ(10)) and 17S,20-dimethyl-trans-Δ(2)-8-iso-PGE1 (8-iso). The addition of α-CD promoted the dehydration to 11-deoxy-Δ(10), while β-CD promoted the isomerization to 8-iso, under these conditions. In the presence of both α- and β-CDs, dehydration and isomerization were also accelerated, supporting the formation of the ternary Limaprost/α-CD/β-CD complex.
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http://dx.doi.org/10.1248/cpb.c14-00733 | DOI Listing |
Sci Rep
January 2025
Department of Immunology, Genetics and Pathology, Uppsala University, Rudbeck Laboratory, C11, 75185, Uppsala, Sweden.
The existence of transmissible amyloid fibril strains has long intrigued the scientific community. The strain theory originates from prion disorders, but here, we provide evidence of strains in systemic amyloidosis. Human AA amyloidosis manifests as two distinct clinical phenotypes called common AA and vascular AA.
View Article and Find Full Text PDFBreast Cancer Res Treat
January 2025
Google Health, 1600 Amphitheatre Pkwy, Mountain View, CA, 94043, USA.
Purpose: Many breast centers are unable to provide immediate results at the time of screening mammography which results in delayed patient care. Implementing artificial intelligence (AI) could identify patients who may have breast cancer and accelerate the time to diagnostic imaging and biopsy diagnosis.
Methods: In this prospective randomized, unblinded, controlled implementation study we enrolled 1000 screening participants between March 2021 and May 2022.
Int J Colorectal Dis
January 2025
Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Rende, Italy.
Purpose: Acute appendicitis (AA) is the leading cause of acute abdomen worldwide, with an incidence of 90-100 cases per 100,000 individuals annually and a lifetime risk of 7-12%. Despite its prevalence, historical accounts of AA are limited, particularly when compared to conditions like haemorrhoids, likely due to the appendix's internal location. This article traces the historical evolution of AA treatment from ancient times to the present, highlighting key contributions.
View Article and Find Full Text PDFMol Psychiatry
January 2025
Department of Psychiatry, Rutgers Robert Wood Johnson Medical School, Piscataway, NJ, 08854, USA.
The hypothalamic neuropeptide system of orexin (hypocretin) neurons provides projections throughout the neuraxis and has been linked to sleep regulation, feeding and motivation for salient rewards including drugs of abuse. However, relatively little has been done to examine genes associated with orexin signaling and specific behavioral phenotypes in humans. Here, we tested for association of twenty-seven genes involved in orexin signaling with behavioral phenotypes in humans.
View Article and Find Full Text PDFSci Rep
January 2025
Digestive Disease Center, CHA Bundang Medical Center, CHA University School of Medicine, 59 Yatap-ro, Seongnam-si, 13496, Gyeonggi-do, Republic of Korea.
The recent clinical outcomes of multi-regimen chemotherapy included prolonged survival and a high rate of conversion to surgery in Asian patients with advanced biliary tract cancer. The ability of single-operator cholangioscopy (SOC) to detect and stage extrahepatic cholangiocarcinoma (CCC) in intraductal lesions is becoming more important in determining the extent of surgery. The aim of this study was to evaluate the role of SOC in surgical planning for extrahepatic CCC.
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