Two heterodimeric diterpenoids (1 and 2) comprising abietane lactone and nor-rosane constituent units were isolated from Euphorbia ebracteolata roots. Compound 1 exhibited a moderate inhibitory effect on α-glucosidase (IC = 7.94 μM), with a K value of 10.8 μM. In silico molecular docking has been performed to investigate the inhibition mechanism. Compound 2 inhibited the acetyl transfer activity of Mycobacterium tuberculosis GlmU (IC = 41.85 μM), which is a novel tuberculosis treatment target.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.jnatprod.7b00595 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Redefining retinoic acid receptor expression in zebrafish embryos using Hybridization Chain Reaction.
Differentiation
December 2024
University of Louisville, School of Medicine, Department of Biochemistry and Molecular Genetics, 580 S Preston St, Louisville, KY, 40202, USA. Electronic address:
Retinoic Acid (RA) is the key signaling molecule during embryonic development with the RA pathway playing multiple roles in throughout development. Previous work has shown RA signaling to be key in development of the craniofacial skeleton. RA signaling is driven by RA binding to the nuclear transcription factors, retinoic acid receptor (RAR) and retinoic X receptor (RXR).
View Article and Find Full Text PDFSelf-Boosting Programmable Release of Multiple Therapeutic Agents by Activatable Heterodimeric Prodrug-Enzyme Assembly for Antitumor Therapy.
Adv Sci (Weinh)
January 2025
Marshall Laboratory of Biomedical Engineering, International Cancer Center, Guangdong Key Laboratory for Biomedical Measurements and Ultrasound Imaging, Laboratory of Evolutionary Theranostics, School of Biomedical Engineering, Shenzhen University Medical School, Shenzhen University, Shenzhen, 518055, China.
Endogenous stimuli-responsive prodrugs, due to their disease lesion specificity and reduced systemic toxicity, have been widely explored for antitumor therapy. However, reactive oxygen species (ROS) as classical endogenous stimuli in the tumor microenvironment (TME) are not enough to achieve the expected drug release. Herein, a ROS-activatable heterodimeric prodrug-loaded enzyme assembly is developed for self-boosting programmable release of multiple therapeutic agents.
View Article and Find Full Text PDFRetinoic acid in Parkinson's disease: Molecular insights, therapeutic advances, and future prospects.
Life Sci
October 2024
Discipline of Medical Biochemistry, School of Laboratory Medicine and Medical Sciences, University of KwaZulu-Natal, Durban 4041, South Africa. Electronic address:
Parkinson's disease (PD) is a common and progressively worsening neurodegenerative disorder characterized by abnormal protein homeostasis and the degeneration of dopaminergic neurons, particularly in the substantia nigra pars compacta. The prevalence of PD has doubled in the past 25 years, now affecting over 8.5 million individuals worldwide, underscoring the need for effective management strategies.
View Article and Find Full Text PDFDevelopment and validation of CYP26A1 inhibition assay for high-throughput screening.
Biotechnol J
June 2024
Division of Pre-clinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland, USA.
Article Synopsis
- All-trans retinoic acid (atRA), derived from vitamin A, acts as a signaling molecule and is regulated by CYP26 enzymes, specifically CYP26A1, during development.
- This study developed a high-throughput screening assay for identifying inhibitors of CYP26A1, achieving a strong performance indicated by favorable statistical metrics.
- The assay successfully confirmed known inhibitors and identified new potential inhibitors, highlighting its utility in assessing the developmental toxicity of various chemicals related to atRA signaling.
The retinoid X receptor has a critical role in synthetic rexinoid-induced increase in cellular all-trans-retinoic acid.
PLoS One
April 2024
Department of Biochemistry and Molecular Genetics, Heersink School of Medicine, University of Alabama at Birmingham, Birmingham, AL, United States of America.
Article Synopsis
- Rexinoids, which activate nuclear receptors to regulate gene transcription, face challenges in clinical use due to side effects and unclear mechanisms across different cells.
- Treatment with the rexinoids UAB30 and UAB110 increased levels of all-trans-retinoic acid (ATRA), a key ligand for RXR-RAR complexes, in human epidermis.
- Overexpression of a dominant negative RXRα reduced the effects of these rexinoids, indicating that their biological actions depend on the RXRα activation function and could potentially normalize ATRA levels in epithelial tissues affected by certain pathologies.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!