A spermine-conjugated lipophilic Pt(iv) prodrug designed to eliminate cancer stem cells in ovarian cancer

Morgan Stilgenbauer; Amarasooriya M D S Jayawardhana; Payel Datta; Zhizhou Yue; Michael Gray; Frederick Nielsen; David J Bowers; Haihua Xiao; Yao-Rong Zheng

doi:10.1039/c9cc02081k

A spermine-conjugated lipophilic Pt(iv) prodrug designed to eliminate cancer stem cells in ovarian cancer

Chem Commun (Camb). 2019 May 28;55(43):6106-6109. doi: 10.1039/c9cc02081k. Epub 2019 May 9.

Authors

Morgan Stilgenbauer¹, Amarasooriya M D S Jayawardhana¹, Payel Datta¹, Zhizhou Yue¹, Michael Gray¹, Frederick Nielsen¹, David J Bowers¹, Haihua Xiao², Yao-Rong Zheng¹

Affiliations

¹ Department of Chemistry and Biochemistry, Kent State University, 224 Williams Hall, Kent, Ohio 44242, USA. yzheng7@kent.edu.
² Beijing National Laboratory for Molecular Sciences, State Key Laboratory of Polymer Physics and Chemistry, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, P. R. China. hhxiao@iccac.ac.cn.

PMID: 31070201
DOI: 10.1039/c9cc02081k

Abstract

We developed a spermine-conjugated lipophilic Pt(iv) prodrug that is able to reduce the cancer stem cell population in ovarian cancer. The therapeutic effect is attributed to the hydrophobic tail and cationic spermine head group, the combination of which allows the Pt(iv) prodrug to localize in mitochondria and induce corresponding damage.

MeSH terms

Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Female
Flow Cytometry
Humans
Hydrophobic and Hydrophilic Interactions
Neoplastic Stem Cells / drug effects*
Ovarian Neoplasms / pathology*
Platinum Compounds / pharmacology*
Prodrugs / chemistry
Prodrugs / pharmacology*
Spectrophotometry, Atomic
Spermine / chemistry*
Spermine / pharmacology

Substances

Antineoplastic Agents
Platinum Compounds
Prodrugs
Spermine