A diverse natural product-like (NPL) synthetic abietane diterpenoid library containing 86 compounds were obtained and the SARs were studied based on their antibacterial potential. Further in vitro cytotoxic and in silico drug-like properties evaluation showed that the potent antibacterial compound 84 had good drug-like properties and displayed low cytotoxicity toward noncancerous mammalian cells, indicating the study of AA and DHAA might be a good starting point for the search of novel antimicrobial molecules. Future work should be focused on the optimization of their potency and selectivity.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmcl.2017.11.014 | DOI Listing |
Int J Biol Macromol
October 2024
Guangdong Provincial Key Lab of Biotechnology for Plant Development, School of Life Sciences, South China Normal University, Guangzhou 510631, China. Electronic address:
Hypertension is the most prevalent non-communicable disease, affecting billions of people worldwide. Discovery and development of natural antihypertensive lead compounds or drugs are important to resolve the limitations of existing antihypertensive drug safety and resistance. This investigation verified that carnosic acid (CA), an important active ingredient of rosemary, an edible spice plant, indicates a significant anti-hypertensive activity in spontaneous hypertension rats by targeting AT1R.
View Article and Find Full Text PDFFood Chem
December 2024
Research Group for Food Production Engineering, National Food Institute, Technical University of Denmark, 2800, Kongens Lyngby, Denmark.
Sci Rep
July 2024
CBIOS - Center for Research in Biosciences and Health Technologies, Universidade Lusófona, 1749-024, Lisboa, Portugal.
Protein kinase C is a family of kinases that play important roles in carcinogenesis. Medicinal plants from Plectranthus spp. (Lamiaceae) are a well-known source of interesting abietanes, such as 7α-acetoxy-6β-hydroxyroyleanone (Roy).
View Article and Find Full Text PDFMolecules
June 2024
Postgraduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraiba, João Pessoa 58051-900, Brazil.
Seven new abietane diterpenoids, comprising medusanthol A-G (-, , -) and two previously identified analogs ( and ), were isolated from the hexane extract of the aerial parts of The structures of the compounds were elucidated by HRESIMS, 1D/2D NMR spectroscopic data, IR spectroscopy, NMR calculations with DP4+ probability analysis, and ECD calculations. The anti-neuroinflammatory potential of compounds - was evaluated by determining their ability to inhibit the production of nitric oxide (NO) and the proinflammatory cytokine TNF-α in BV2 microglia stimulated with LPS and IFN-γ. Compounds - and exhibited decreased NO levels at a concentration of 12.
View Article and Find Full Text PDFMolecules
April 2024
Department of Molecular Biotechnology and Genetics, Faculty of Biology and Environmental Protection, University of Lodz, Banacha 12/16, 90-237 Lodz, Poland.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!