PUBLICATION
Brasilterpenes A-E, Bergamotane Sesquiterpenoid Derivatives with Hypoglycemic Activity from the Deep Sea-Derived Fungus Paraconiothyrium brasiliense HDN15-135
- Authors
- Wang, W., Shi, Y., Liu, Y., Zhang, Y., Wu, J., Zhang, G., Che, Q., Zhu, T., Li, M., Li, D.
- ID
- ZDB-PUB-220528-4
- Date
- 2022
- Source
- Marine drugs 20(5): (Journal)
- Registered Authors
- Li, Mingyu
- Keywords
- ascomycete fungus Paraconiothyrium brasiliense, bergamotane sesquiterpenoids, hypoglycemic activity, marine-derived fungus
- MeSH Terms
-
- Animals
- Ascomycota*/chemistry
- Hypoglycemic Agents/pharmacology
- Sesquiterpenes*/chemistry
- Zebrafish
- PubMed
- 35621989 Full text @ Mar. Drugs
Citation
Wang, W., Shi, Y., Liu, Y., Zhang, Y., Wu, J., Zhang, G., Che, Q., Zhu, T., Li, M., Li, D. (2022) Brasilterpenes A-E, Bergamotane Sesquiterpenoid Derivatives with Hypoglycemic Activity from the Deep Sea-Derived Fungus Paraconiothyrium brasiliense HDN15-135. Marine drugs. 20(5).
Abstract
Five bergamotane sesquiterpenoid derivatives, brasilterpenes A-E (1-5), bearing an unreported spiral 6/4/5 tricyclic ring system, were isolated from the deep sea-derived ascomycete fungus Paraconiothyrium brasiliense HDN15-135. Their structures, including absolute configurations, were established by extensive spectroscopic methods complemented by single-crystal X-ray diffraction analyses, electronic circular dichroism (ECD), and density-functional theory (DFT) calculations of nuclear magnetic resonance (NMR) data including DP4+ analysis. The hypoglycemic activity of these compounds was assessed using a diabetic zebrafish model. Brasilterpenes A (1) and C (3) significantly reduced free blood glucose in hyperglycemic zebrafish in vivo by improving insulin sensitivity and suppressing gluconeogenesis. Moreover, the hypoglycemic activity of compound 3 was comparable to the positive control, anti-diabetes drug rosiglitazone. These results suggested brasilterpene C (3) had promising anti-diabetes potential.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping