Novel class of antitumor amphiphilic amines causes death in several cancer cell lines.
A new chemotherapy treatment involving a novel class of antitumor amphiphilic amines (RCn) was found to be effective against both pediatric and adult cancers.
In a study published in Pharmaceutical Research, scientists evaluated RCn for cytotoxicity and mechanism of cell death in several cancer cell lines, for antitumor efficacy in mouse tumor models, and for the ability to encapsulate chemotherapy drugs.
“We tested RCn’s tumor killing efficacy in cell lines of numerous cancers, including sarcomas, lymphoma, and neuroblastoma,” said principal study investigator Timothy Cripe, MD, PhD. “We observed anticancer activity of the RCn amines in all the cancer cell lines analyzed.”
The results of the study revealed that RCn and RC16, in particular, was 10 times more effective attacking tumor cells compared with regular cells. The findings indicate that only a low dose would be needed to kill the cancer, and have only minimal effects on the normal cells.
Furthermore, when the drug was administered orally or intravenously, it was found to be effective in shrinking the human tumors that researchers implanted into mice, as well as in a metastatic model of murine neuroblastoma.
“This is particularly important for proving the safety of a potential therapy,” Cripe said.
The chemical structure of RC16 caused it to self-assemble into micelles in water, and allowed complexation of the cancer drugs doxorubicin, etoposide, and paclitaxel. The micelles were found to significantly improve the in vitro antitumor activity of the drugs by enhancing their solubility in water.
“The antitumor activity of lipophilic amines was interesting because of its action on the mitochondria and lysosomes of cells,” said lead study scientist Isabella Orienti, PhD. “Moreover, their amphiphilic character improves their bioavailability. We correctly hypothesized these amphiphilic amines would have high antitumor activity and high bioavailability.”
The findings show promise in the potential use of cancer therapies, but future research is required for the drug.
“We are in the process of determining our next steps with testing this new drug,” Cripe said. “This is a promising new therapy for adult and pediatric cancers, and we look forward to further testing its merits.”