Antioxidant flavonoid baicalein as a dual purpose radiomodifier with promising bench to bedside potential

Despite the potential of drug-radiotherapy combinations, a limited number of oncology drugs are approved by FDA for use along with radiotherapy. Currently, there is no agent available in the clinic that can exhibit dual radiomodifying behavior. Despite availability of sophisticated, high-precision techniques in radiotherapy for accurate targeting of tumors, normal tissue toxicity impedes its use in curative settings. Combining radiotherapy with an agent that can protect normal tissue and augment tumor killing can improve therapy outcomes. Other than combining drugs for therapeutic radiation exposure, there is a pressing need of identifying agents for management of unwanted effects of accidental radiation exposure. There is a serious deficit in the repertoire of currently available safe and effective radiation countermeasures. Baicalein, a bioactive component from the roots of traditional Chinese medicinal herb Scutellaria baicalensis has been shown to protect against acute as well as chronic effects of radiation exposure including normal tissue injury to lungs, gut, hematopoietic system, intestine, endothelial and neuronal cells by us and other labs worldwide. Further, administration of baicalein alone or in combination with other agents prevents radiation-induced mortality in mice. Additionally, numerous studies have reported radiosensitizing potential of baicalein in lung, breast, esophageal, cervical and prostate cancer. Moreover, safety, tolerability, and pharmacokinetics of baicalein is well established in healthy human subjects. Here we provide a succinct overview of the distinctive radiomodifying potential of baicalein, safety, pharmacology underscoring its utility as a prospective radiomodifier in clinical settings.