Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Agarperoxinols A and B (), two naturally occurring humulene-type sesquiterpenoids with an unprecedented tricyclic 6/6/7 ring, were discovered from the agarwood of . Their structures were unambiguously determined by various spectroscopic data, experimental ECD calculations, and single-crystal X-ray diffraction analysis. Agarperoxinol B showed significant and dose-dependent neuroinflammatory inhibitory effects on various proinflammatory mediators, including NO, TNF-α, IL-6, and IL-1β, and suppressed iNOS and COX-2 enzymes in LPS-activated microglial cells. A mechanistic study demonstrated that agarperoxinol B remarkably inhibited the phosphorylation of the Akt and JNK signaling pathways. Agarperoxinol B also significantly reduced the expression of the microglial markers Iba-1, COX-2, and TNF-α in the mouse cerebral cortex. Our findings introduce a bioactive compound from natural products that decreases proinflammatory factor production and has application for the treatment of neurodegenerative diseases.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10666226 | PMC |
| http://dx.doi.org/10.1021/acsomega.3c05783 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Divergent Total Syntheses of Elisapterane and Relevant Diterpenoids Assisted by Structure Reassignment.
J Am Chem Soc
August 2025
Department of Chemistry, Zhejiang University, Hangzhou 310058, China.
Herein, we describe our synthetic endeavors toward elisapterane and relevant diterpenoids through a bioinspired divergent strategy based on an unprecedented late-stage D-ring formation logic. The key tricyclic intermediate bearing a norneoelisabane skeleton could be efficiently prepared an ODI-(5 + 2) cycloaddition/1,2-acyl migration cascade and a SmI-mediated pinacol coupling/Grob fragmentation/deoxygenation orchestration. The synthesis of the misassigned structure of elisapterosin F led us to revisit the structure elucidation of these natural products.
View Article and Find Full Text PDFLabdane and norlabdane diterpenoids from Amomum sericeum rhizomes and their potential anti-inflammatory activities.
Bioorg Chem
August 2025
Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, China. Electronic address:
Phytochemical investigation of the rhizomes of Amomum sericeum led to the isolation and identification of twenty-seven labdane and norlabdane diterpenoids, including two unprecedented rearranged dinorditerpenoids (1 and 2), two novel norditerpenoids (3 and 4), seven undescribed labdane and norlabdane diterpenoids (5-11), along with sixteen known analogs (12-27). Their structures were established by comprehensive analysis of spectroscopic data, single crystal X-ray diffraction, Rh(OCOCF)-induced electronic circular dichroism (ECD), and quantum chemistry calculations. Compounds 1 and 2 represented two unique labdane dinorditerpenoid skeletons, with a 6/6/5 tricyclic system and a 6/9 bicyclic system, respectively.
View Article and Find Full Text PDFUnprecedented triterpenes with anti-inflammatory activity from Limax maximus.
J Nat Med
September 2025
Guangxi Institute of Botany, Guangxi Zhuang Autonomous Region and Chinese Academy of Sciences, Guangxi Key Laboratory of Plant Functional Phytochemicals and Sustainable Utilization, Guilin, 541006, China.
Four triterpenes with the unprecedented pentacyclic skeletons were isolated from Limax maximus, the traditional medicine of the Zhuang ethnic group in Guangxi. Notably, compounds 1-4 were characterized by rare 7/6/5 tricyclic ring moiety linked to 6/5 bicyclic moiety via three carbon chain. The structures of compounds 1-4 were elucidated by comprehensive spectroscopic analysis.
View Article and Find Full Text PDFExpanding the Diversity of the Terpene Skeleton and Structure through Identification of Noncanonical Class IE and IF Terpene Synthase-Formed Products.
Org Lett
June 2025
Department of Life and Food Sciences, Graduate School of Science and Technology, Niigata University, Ikarashi 2-8050, Nishi-ku, Niigata 950-2181, Japan.
Noncanonical class IE and IF terpene synthases have recently been discovered from bacterial genomes through the nonsequence-similarity-based method: protein-structural-model-based genome mining. This study identified the class IE product as a new diterpene comprising the first hydrocarbon skeleton among all terpenoids. The skeleton with a 6/6/6-fused tricyclic structure and six methyl groups could be synthesized through an unprecedented terpene-forming reaction.
View Article and Find Full Text PDFDiazepine Agonists of the 5-HT Receptor with Unprecedented Selectivity: Discovery of Bexicaserin (LP352).
J Med Chem
June 2025
Eurofins Beacon Discovery, 6118 Nancy Ridge Drive, San Diego, California 92121, United States.
The clinical development of novel 5-HT receptor (5-HTR) therapies has been limited due to concerns over lack of selectivity and potential for off-target effects. Here, we report that the introduction of a secondary amide substituent into a 6,5,7-tricyclic benzodiazepine scaffold provided compounds with unprecedented selectivity for the 5-HTR in both functional and binding assays. An early lead compound, , had an in vivo half-life that was shorter than desired, which was improved by a targeted reduction in renal clearance.
View Article and Find Full Text PDF