Construction of targeted 10B delivery agents and their uptake in gastric and pancreatic cancer cells

Song Wang; Zhengchao Zhang; Lele Miao; Jiaxing Zhang; Futian Tang; Muzhou Teng; Yumin Li

doi:10.3389/fonc.2023.1105472

Construction of targeted ¹⁰B delivery agents and their uptake in gastric and pancreatic cancer cells

Front Oncol. 2023 Feb 9:13:1105472. doi: 10.3389/fonc.2023.1105472. eCollection 2023.

Authors

Song Wang^{1

2}, Zhengchao Zhang^{1

2}, Lele Miao^{1

2}, Jiaxing Zhang^{1

2}, Futian Tang^{1

2}, Muzhou Teng^{1

2}, Yumin Li^{1

2}

Affiliations

¹ Department of General Surgery, Second Hospital of Lanzhou University, Lanzhou, China.
² Key Laboratory of the Digestive System Tumors of Gansu Province, Second Hospital of Lanzhou University, Lanzhou, China.

Abstract

Boron Neutron Capture Therapy (BNCT) is a new binary radiation therapy for tumor tissue, which kills tumor cells with neutron capture reaction. Boron neutron capture therapy has become a technical means for glioma, melanoma, and other diseases has been included in the clinical backup program. However, BNCT is faced with the key problem of developing and innovating more efficient boron delivery agents to solve the targeting and selectivity. We constructed a tyrosine kinase inhibitor-L-p-boronophenylalanine (TKI-BPA) molecule, aiming to improve the selectivity of boron delivery agents by conjugating targeted drugs while increasing the molecular solubility by adding hydrophilic groups. It shows excellent selectivity in differential uptake of cells, and its solubility is more than 6 times higher than BPA, leading to the saving of boron delivery agents. This modification method is effective for improving the efficiency of the boron delivery agent and is expected to become a potential alternative with high clinical application value.

Keywords: boron delivery agent; boron neutron capture therapy (BNCT); selectivity; solubility; tumor.

Grants and funding

This research was funded by Natural Science Foundation of Gansu Province (22JR5RA496), Foundation of Lanzhou University Second Hospital (CYXZ2022-22), Cuiying Scientific and Technological Innovation Program of Lanzhou University Second Hospital (CY2021-QN-A02).