MSBA-S - A pentacyclic sulfamate as a new option for radiotherapy of human breast cancer cells.

Abstract

Many pentacyclic triterpenoids show anti-cancer and anti-inflammatory properties. Recently, we detected a pronounced cytotoxicity and radiosensitivity of two betulinyl sulfamates in human breast cancer cells. Besides betulinic acid scaffold (BSBA-S), we synthesized several new sulfamate-coupled scaffolds from oleanolic acid (OSBA-S), ursolic acid (USBA-S), platanic acid (PSBA-S) and maslinic acid (MSBA-S). Highest cytotoxicity was monitored in breast cancer cell lines after MSBA-S treatment showing in SRB assays IC50 values between 3.7 μM and 5.8 μM. Other sulfamate/triterpene conjugates, however, were less cytotoxic holding IC50 values between 6.6 μM and >50 µM, respectively. MSBA-S-treated breast cancer cells displayed significantly reduced clonogenic survival and an increased rate of apoptosis as compared to the other conjugates. In addition, MSBA-S in combination with irradiation resulted in effects on radiosensitivity in MDA-MB-231 cells (DMF10 = 1.14). In particular, ROS formation was strongly assessed in MSBA-S-treated breast cancer cells. Our findings suggest that the sulfamate derivative of maslinic acid MSBA-S might be a new option for the radiation therapy in breast cancer cells.

• Authors: Marina Petrenko, Antje Güttler, Elena Pflüger, Immo Serbian, Michael Kahnt, Yvonne Eiselt, Jacqueline Keßler, Anne Funtan, Reinhard Paschke, René Csuk, Dirk Vordermark, Matthias Bache
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 224 Pg. 113721 (Nov 15 2021) ISSN: 1768-3254 [Electronic] France
• PMID: 34365127 (Publication Type: Journal Article)
• Copyright: Copyright © 2021 Elsevier Masson SAS. All rights reserved.

Chemical References

• Herbicides
• Sulfonic Acids
• sulfamic acid

Topics

• Breast Neoplasms (drug therapy, radiotherapy)
• Female
• Herbicides (pharmacology, therapeutic use)
• Humans
• Molecular Structure
• Sulfonic Acids (pharmacology, therapeutic use)