Ten compounds were isolated from the EtOAc soluble part of the MeOH extract of Saussureae Radix, with their effects on melanin production also evaluated in B-16 mouse melanoma cell lines stimulated with 3-isobutyl-1-methylxanthine (IBMX), an elevator of cellular cAMP. The compounds were identified as aplotaxene (1), 1${eta}$-hydroxy arbusculin A (2), costunolide (3), dehydrocostuslactone (4), 11${eta}$,13-dihydrocostunolide (5), reynosin (6), heptadec-(9Z)-enoic acid (7), ${eta}$-sitosterol (8), linoleic acid methyl ester (9) and betulinic acid methyl ester (10). Compounds 2, 9 and 10 were identified from Saussureae Radix for the first time. Furthermore, compounds 2, 3 and 6 showed potent inhibitory effects on the IBMX-induced melanogenesis, in dose-dependent manners, with $IC_{50}$ values of 11, 3 and 2.5 ${mu}g/mL$, respectively. As a positive control, arbutin exhibited an $IC_{50}$ value of 29 ${mu}g/mL$.