第十五届海洋药物学术年会暨2021国际海洋药物研讨会

18 / 2021-10-08 21:30:35

Cytotoxicity assessment of metal complexes coordinated with marine alkaloid isoquinolin and ruthenium

marine alkaloid isoquinolin,ruthenium,3D multicellular tumor spheroid (MCTS)

Anti-tumor is a major research direction of Marine alkaloids.A novel dimeric isoquinoline alkaloid, jorumycin, has been isolated from the Pacific nudibranch (Jorunna funebris) [1]. In addition, 3D multicellular tumor spheroid (MCTS) model has received increasing interest in recent years, since it can realistically mimics the extracellular matrix (ECM) and the in vivo situations and therefore have been widely applied in the drug discovery process [2]. In this work, we evaluated the cytotoxicities of novel  synthesised Ru(II)-IQ complexes RuIQ-3, RuIQ-4, and RuIQ-5 by MTT assay, 3D multicellular tumor spheroids(MCTSs) model and zebrafish embryos.And demonstrate that the new ruthenium complexes Ru-IQ3-Ru-IQ5 could effectively kill cancer cells, even the drug resistant cell, A549R. The 3D multicellular tumor spheroids (MCTSs) model also confirmed the good anti-tumor activity of Ru-IQ3-Ru-IQ5. Especially, Ru-IQ5 is expected to be a low-toxicity drug for lung cancer treatment because Ru-IQ5 does not induce embryonic toxicity or toxicity in zebrafish embryos and larvae during development at concentrations less than 16μM (13.6 μg/mL).