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Bisabolangelone has anti-tumor, anti-microbial, and antioxidant activities. Bisabolangelone has anti-inflammatory activity, it inhibits dendritic cell functions by blocking MAPK and NF-κB signaling. Bisabolangelone has antimelanogenic activity, the cAMP-binding site of PKA as a putative target ameliorating melanocyte-specific hyperpigmented disorder. Bisabolangelone has inhibitory effects of the melanogenesis against α-melanocyte stimulating hormone (α-MSH)-activated B16 melanoma cells. Bisabolangelone shows minor activity at the GABA(A) receptor.Bisabolangelone has anti-ulcer activity, it is possible that bisabolangelone inhibited the activity of the H(+)/K(+)-ATPase, then reducing the secretion of H(+). Bisabolangelone inhibits the activity of 5alpha-reductase type I in LNCaP cells (IC50 = 11.6 microg/ml).