Abstract
About two thirds of biological damage due to low linear energy transfer (LET) radiation, such as X-rays and the plateau region of heavy-ion beams, is known to be caused by the hydroxyl radical (˙OH), the most powerful reactive oxygen species (ROS), generated via ionisation and excitation of water molecules. Thus, compounds having an efficient scavenging activity against ROS are expected to exhibit a radioprotective activity. A planar catechin analogue, where an isopropyl fragment was introduced into the catechol ring of (+)-catechin, showed an efficient protective effect against X-ray induced apoptosis in rat thymocytes compared to (+)-catechin. The planar catechin scavenged 2,2-diphenyl-1-picrylhydrazyl radicals (DPPH˙) solubilised in water by β-cyclodextrin about 10-fold faster than (+)-catechin in phosphate buffer (0.1 M, pH 7.4) at 298 K. Furthermore, the experimental log P value of the planar catechin (1.22) is reported to be significantly larger than that of (+)-catechin (0.44). The higher radical-scavenging activity and lipophilicity of the planar catechin than those of (+)-catechin may contribute in part to the higher protective activity against X-ray-induced apoptosis in rat thymocytes.
Highlights
Ionising radiation is one of the effective methods for cancer treatment
The radioprotective activity of chemical compounds is estimated by quantifying the frequency of apoptosis induced by radiation in rat thymocytes
Thymocytes from rats were placed in cell culture medium (RPMI 1640) supplemented with 10% fetal bovine serum (FBS)
Summary
Ionising radiation is one of the effective methods for cancer treatment. To maintain the quality of life (QOL) of cancer patients, the demand for radiotherapy that can maintain the shape of internal organs has been increasing in recent years. The biological data using rat thymocytes together with chemical data, such as radical-scavenging rates of the catechins as well as their lipophilicity provide fundamental and valuable information to develop effective radioprotective agents without toxicity.
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