Structurally diverse sesquiterpenoids with anti-MDR cancer activity from Penicillium roqueforti.
10.1016/S1875-5364(25)60857-0
- Author:
Shuyuan MO
1
;
Nanjin DING
2
;
Zhihong HUANG
2
;
Jun YAO
2
;
Weiguang SUN
2
;
Jianping WANG
3
,
4
;
Yonghui ZHANG
5
;
Zhengxi HU
4
,
6
Author Information
1. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China; Department of Pharmacy, Renmin hospital of Wuhan University, Wuhan 430060, China.
2. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
3. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China. Electronic address: jpwang1001@
4. com.
5. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China. Electronic address: zhangyh@mails.tjmu.edu.cn.
6. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China; Hubei Shizhen Laboratory, Wuhan 430061, China. Electronic address: hzx616@
- Publication Type:Journal Article
- Keywords:
Anti-MDR cancer activity;
Nor-sesquiterpenoids;
Penicillium roqueforti;
Sesquiterpenoids
- MeSH:
Penicillium/chemistry*;
Humans;
Sesquiterpenes/isolation & purification*;
Cell Line, Tumor;
Molecular Structure;
Drug Resistance, Neoplasm/drug effects*;
Antineoplastic Agents/pharmacology*;
Drug Resistance, Multiple/drug effects*;
Molecular Docking Simulation
- From:
Chinese Journal of Natural Medicines (English Ed.)
2025;23(4):504-512
- CountryChina
- Language:English
-
Abstract:
Five novel nor-eremophilane-type sesquiterpenoids, peniroqueforins E-H and J (1-4 and 7), two new eremophilane-type sesquiterpenoids, peniroqueforins I and K (5 and 8), and a new eudesmane-type sesquiterpenoid, peniroqueforin L (9), along with four known compounds (6 and 10-12), were isolated and characterized from fungus Penicillium roqueforti (P. roqueforti). The structures and absolute configurations of these compounds were determined through comprehensive spectroscopic analyses, electronic circular dichroism (ECD) data analyses, and single-crystal X-ray diffraction methods. The anti-multi-drug resistance (MDR) cancer activity of these compounds was evaluated using SW620/Ad300 cells. Notably, the half maximal inhibitory concentration (IC50) value of paclitaxel (PTX) combined with 1 in SW620/Ad300 cells was 50.36 nmol·L-1, which was 65-fold more potent than PTX alone (IC50 3.26 μmol·L-1). Subsequent molecular docking studies revealed an affinity between compound 1 and P-glycoprotein (P-gp), suggesting that this nor-eremophilane-type sesquiterpenoid (1) could serve as a potential lead for MDR reversal in cancer cells through P-gp inhibition.
