Structurally diverse sesquiterpenoids with anti-MDR cancer activity from Penicillium roqueforti  

作　　者：Shuyuan Mo Nanjin Ding Zhihong Huang Jun Yao Weiguang Sun Jianping Wang Yonghui Zhang Zhengxi Hu 

机构地区：[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 [2]Hubei Shizhen Laboratory,Wuhan 430061,China [3]Department of Pharmacy,Renmin hospital of Wuhan University,Wuhan 430060,China

出　　处：《Chinese Journal of Natural Medicines》2025年第4期504-512,共9页中国天然药物(英文版)

基　　金：supported by the National Natural Science Foundation of China(Nos.82273811,32470417,and U22A20380);the National Program for Support of Top-notch Young Professionals(No.0106514050);the Hubei Provincial Natural Science Foundationof China(No.2024AFA028);the National Key R&D Program of China(No.2021YFA0910500);the Science and Technology Major Project of Hubei Province(Nos.2021ACA012 and 2024BCB021);the Chinese Medicine Research Foundation of the Health Commission of Hubei Province(No.ZY2025Z013)。

摘　　要：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(6and 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(IC503.26μmol·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.

关 键 词：Penicillium roqueforti SESQUITERPENOIDS Nor-sesquiterpenoids Anti-MDR cancer activity 

分 类 号：R284[医药卫生—中药学]