Ortho-carboranyl glycosides for the treatment of cancer by boron neutron capture therapy. |
| |
Authors: | L F Tietze U Bothe U Griesbach M Nakaichi T Hasegawa H Nakamura Y Yamamoto |
| |
Affiliation: | 1. Pharmacy College, Jiangxi University of Traditional Chinese Medicine, 818 Xinwan Road, Nanchang 330004, Jiangxi, PR China;2. Technology Center, Jiangzhong Group, 618 Huoju Road, Nanchang 330096, Jiangxi, PR China;3. Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China |
| |
Abstract: | Distinct biological properties of the ortho-carboranyl (1,2-dicarba-closo-dodecaboranyl) glycosides 1, 2 and 3 were evaluated to estimate the suitability of these compounds for cancer treatment by boron neutron capture therapy. The boron uptake into B16-Melanoma cells was significantly higher by incubating the cells with aqueous solutions of carboranyl glucoside 1 (11.2 ppm after 3h), lactoside 2 (13.2 ppm after 12h) and maltoside 3 (20.0 ppm after 24h) compared with solutions of clinically used p-boronophenylalanine (BPA) 5 (3.1 ppm after 24h). Carboranyl maltoside 3 was more effective than boron-10 enriched 5 in killing C-6 rat glioma cells by incubating the cells with the compound and subsequent treatment with thermal neutrons. 3 was also administrated iv, in concentrations of 25 mg boron/kg body weight to rats bearing brain tumors. After a period of 4h after administration the concentration of boron in the tumor tissue was 3.0 ppm. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|