Six undescribed lindenane sesquiterpenoid dimers (LSDs), shimianolides A-F (-), were isolated from the whole plants of var. . Shimianolides A-C (-) represent an unprecedented class of LSDs, distinguished by a highly fused 3/5/6/6/6/5/6/6/5/3 decacyclic scaffold. All isolates were evaluated for their inhibitory effects on LPS-induced NO production in RAW264.7 macrophages and their cytotoxicity against five human cancer cell lines. Compound exhibited moderate cytotoxicity against the HL-60 cell line with an IC value of 15.6 ± 1.11 μM, comparable to that of the positive control cisplatin. Further investigation demonstrated that compound induced apoptosis in HL-60 cells, with apoptosis rates of 36.9% at 15.0 μM and 47.5% at 30.0 μM. These results highlight the potential of LSDs as lead compounds for leukemia therapy.
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http://dx.doi.org/10.1021/acs.joc.5c00070 | DOI Listing |
Proc Natl Acad Sci U S A
March 2025
Department of Biomedical Engineering, and Center for Advanced Genomic Technologies, Duke University, Durham, NC 27708.
CRISPR-Cas9 systems have revolutionized biotechnology, creating diverse new opportunities for biomedical research and therapeutic genome and epigenome editing. Despite the abundance of bacterial CRISPR-Cas9 systems, relatively few are effective in human cells, limiting the overall potential of CRISPR technology. To expand the CRISPR-Cas toolbox, we characterized a set of type II CRISPR-Cas9 systems from select bacterial genera and species encoding diverse Cas9s.
View Article and Find Full Text PDFFront Artif Intell
February 2025
Department of Surgery, College of Medicine and Health Science, University of Gondar, Gondar, Ethiopia.
Heart disease is a leading cause of mortality worldwide, making accurate early detection essential for effective treatment and management. This study introduces a novel hybrid machine-learning approach that combines transfer learning using the VGG16 convolutional neural network (CNN) with various machine-learning classifiers for heart disease detection. A conditional tabular generative adversarial network (CTGAN) was employed to generate synthetic data samples from actual datasets; these were evaluated using statistical metrics, correlation analysis, and domain expert assessments to ensure the quality of the synthetic datasets.
View Article and Find Full Text PDFHealth Inf Sci Syst
December 2025
School of Mathematics and Computational Science, Xiangtan University, Yuhu Street, Xiangtan, 411105 Hunan China.
Antimicrobial peptides (AMPs) are natural polypeptides with antibacterial activity and are an important part of the innate immune system. In order to solve the growing problem of conventional antibiotic resistance, AMPs have been applied in different fields as highly potential alternatives. It is of great significance that deep learning-based methods can quickly screen out candidate samples of AMPs from massive protein sequences to help discover new AMPs.
View Article and Find Full Text PDFACS Omega
March 2025
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo namesti 5/542, 16000 Prague, Czech Republic.
The evolution of proteins is primarily driven by the combinatorial assembly of a limited set of pre-existing modules known as protein domains. This modular architecture not only supports the diversity of natural proteins but also provides a robust strategy for protein engineering, enabling the design of artificial proteins with enhanced or novel functions for various industrial applications. Among these functions, oligomerization plays a crucial role in enhancing protein activity, such as by increasing the binding capacity of antibodies.
View Article and Find Full Text PDFJ Am Chem Soc
March 2025
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543, Singapore.
Rylenes, known for their excellent photochemical properties, hold great promise in OLEDs, solar cells, and bioimaging applications. However, the solution-phase synthesis of long rylene molecules is often hindered by poor solubility and low stability. In this work, we present an efficient synthetic strategy for a series of CN-terminated rylenes via base-mediated intramolecular Michael addition and oxidative cyclodehydrogenation (Scholl reaction).
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