Toxicological assessment of dihydroberberine

A battery of studies was conducted to examine the toxicological potential of dihydroberberine (DHBBR), a derivative of berberine (BBR). The genotoxicity studies conducted on DHBBR, including the bacterial reverse mutation test, the mouse lymphoma assay, and the in vivo micronucleus test, showed that DHBBR is non-mutagenic and non-clastogenic. An acute oral toxicity study revealed that the LD₅₀ of DHBBR in female Sprague Dawley rats was greater than 2000 mg/kg bw. In a 14-day oral dose range finding study, the maximum tolerated dose was the high dose, 120 mg/kg bw/day. Based on a 90-day oral toxicity study in male and female Sprague Dawley rats, it was concluded that the NOAEL for DHBBR is 100 mg/kg bw/day, the highest dose tested.