Ent-pimarane and ent-kaurane diterpenoids from Siegesbeckiapubescens and their anti-endothelial damage effect in diabetic retinopathy.
10.1016/S1875-5364(25)60827-2
- Author:
Mengjia LIU
1
;
Tingting LUO
1
;
Rongxian LI
1
;
Wenying YIN
1
;
Fengying YANG
1
;
Di GE
2
;
Na LIU
3
Author Information
1. School of Biological Science and Technology, University of Jinan, Jinan 250022, China.
2. School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: bio_ged@ujn.edu.cn.
3. School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: mls_liun@ujn.edu.cn.
- Publication Type:Journal Article
- Keywords:
Diabetic retinopathy;
Inflammatory response;
Natural diterpenoid;
Oxidative stress;
Siegesbeckia pubescens
- MeSH:
Diabetic Retinopathy/metabolism*;
Humans;
Oxidative Stress/drug effects*;
Animals;
Diterpenes, Kaurane/administration & dosage*;
Asteraceae/chemistry*;
Male;
Endothelial Cells/drug effects*;
Abietanes/administration & dosage*;
Molecular Structure;
Mice;
Anti-Inflammatory Agents/chemistry*;
Plant Extracts/chemistry*;
Mice, Inbred C57BL
- From:
Chinese Journal of Natural Medicines (English Ed.)
2025;23(2):234-244
- CountryChina
- Language:English
-
Abstract:
Diabetic retinopathy, a prevalent and vision-threatening microvascular complication of diabetes mellitus, is the leading cause of blindness among middle-aged and elderly individuals. Natural diterpenoids isolated from Siegesbeckia pubescens demonstrate potent anti-inflammatory properties. This study aimed to identify novel bioactive diterpenoids from S. pubescens and investigate their effects on oxidative stress and inflammatory responses in diabetic retinopathy, both in vitro and in vivo. Three new ent-pimarane-type diterpenoids (1-3) and six known compounds (4-9) were isolated from the aerial parts of S. pubescens. Their structures were elucidated through spectroscopic data interpretation, and absolute configurations were determined by comparing calculated and experimental electronic circular dichroism (ECD) spectra. Among these compounds, 14β,16-epoxy-ent-3β,15α,19-trihydroxypimar-7-ene (5) exhibited the most potent protective effect against high glucose and interleukin-1β (IL-1β)-stimulated human retinal endothelial cells. Mechanistically, compound 5 promoted endothelial cell survival while ameliorating oxidative stress and inflammatory response in diabetic retinopathy, both in vivo and in vitro. These findings not only suggest that diterpenoids such as compound 5 are important anti-inflammatory constituents in S. pubescens, but also indicate that compound 5 may serve as a lead compound for preventing or treating vascular complications associated with diabetic retinopathy.
