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Seven new tropane alkaloids, including five monomeric (-), one dimeric (), and one trimeric () 3α-nortropane ester, along with two known monomeric nortropane alkaloids ( and ), were isolated from the leaves and bark of . Their structures, including the absolute configuration of the enantiomeric pair of (±)-, were elucidated by comprehensive spectroscopic analyses. Alkaloids and showed cytotoxicity toward human pancreatic cancer cell lines (AsPC-1, BxPC3, PANC-1, and SW1990). Alkaloids , , and induced a smooth muscle relaxation effect comparable to that of atropine ( 106.1 ± 7.5%, 97.0 ± 5.2%, 100.9 ± 1.4%, 111.7 ± 1.7%, respectively) on isolated rat tracheal rings.
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http://dx.doi.org/10.1021/acs.jnatprod.1c00374 | DOI Listing |
ACS Synth Biol
September 2025
The Key Laboratory of Industrial Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, P. R. China.
Human Bone Morphogenetic Protein-2 (hBMP-2) serves as a critical regulator in bone and cartilage formation; however, its industrial application is hindered by its inherent tendency to form inclusion bodies in prokaryotic expression systems. To address this issue, we established a recombinant hBMP-2 (rhBMP-2) expression system using the pCold II plasmid and the SHuffle T7 strain. We explored several strategies to enhance the solubility of rhBMP-2, including coexpression with molecular chaperones, vesicle-mediated secretory expression, fusion expression with synthetic intrinsically disordered proteins (SynIDPs), and fusion expression with small-molecule peptide tags.
View Article and Find Full Text PDFMol Pharm
September 2025
Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul 06351, Republic of Korea.
Dimeric fibroblast activation protein inhibitor (FAPI) radioligands are promising candidates for theranostic applications because of their enhanced tumor uptake and prolonged retention compared to monomeric radioligands. Several linker strategies have been investigated to connect two FAPI motifs and a radiometal chelator in a dimer design. In this study, we report the development of a novel dimeric FAPI radioligand, [Ga]Ga-, which utilizes a triazine core as a trifunctional linker.
View Article and Find Full Text PDFACS Chem Neurosci
September 2025
Computational Biology and Molecular Simulations Laboratory, Department of Biophysics, School of Medicine, Bahçeşehir University, Istanbul 34349, Turkey.
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by the pathological aggregation of amyloid-beta (Aβ) peptides, particularly Aβ-42, which plays a central role in disease progression. Soluble Aβ dimers have been implicated as the primary neurotoxic species contributing to synaptic dysfunction and cognitive impairment. In this study, we employ a comprehensive computational framework integrating molecular dynamics (MD) simulations, neural relational inference (NRI) modeling, and largest Lyapunov exponent (LLE) analysis to elucidate the molecular mechanisms underlying Aβ-42 dimerization and evaluate the inhibitory potential of small molecules, apigenin and caffeine.
View Article and Find Full Text PDFViruses
August 2025
Department of Chemistry and Biochemistry, Old Dominion University, Norfolk, VA 23529, USA.
Enteroviruses initiate genomic replication via a highly conserved mechanism that is controlled by an RNA platform, also known as the 5' cloverleaf (5'CL). Here, we present a biophysical analysis of the 5'CL conformation of three enterovirus serotypes under various ionic conditions, utilizing CD spectroscopy, size-exclusion chromatography, and small-angle X-ray scattering. In general, a tendency toward a smaller monomeric hydrodynamic radius in the presence of salts was observed, but the exact structural signature of each 5'CL varied depending upon the serotype.
View Article and Find Full Text PDFEBioMedicine
August 2025
Laboratory of Pathogen Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing, 100101, China; Beijing Life Science Academy, Beijing, 102209, China; University of Chinese Academy of Sciences, Beijing, 101408, China. Electronic address:
Background: Respiratory syncytial virus (RSV) poses a significant public health threat, particularly to children and the elderly. Two protein-based vaccines and one mRNA vaccine have been approved, all targeting the prefusion conformation of the fusion (F) trimer. However, it has been reported that the epitope activity of the F protein gradually declines during storage, resulting in a reduction of the vaccines' immunogenicity.
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