Dalbergioidin exhibits tyrosinase inhibitory activity with an IC50 of 20 mM. It shows a melanin biosynthesis inhibition zone in the culture plate of Streptomyces bikiniensis that has commonly been used as an indicator organism. Dalbergioidin protects MC3T3-E1 osteoblastic cells against H2O2-induced cell damage through activation of the PI3K/AKT/SMAD1 pathway, suggests that it may be useful in bone metabolism diseases, particularly osteoporosis. Dalbergioidin also ameliorates doxorubicin-induced renal fibrosis by suppressing the TGF-β signal pathway.