Ailanthone

DescriptionAilanthone is a quassinoid that has been found in Ailanthus and has diverse biological activities. It is active against the P. falciparum strains HB-3 and Dd-2 in vitro (IC50s = 0.003 and 0.037 μg/ml, respectively). Ailanthone is phytotoxic, inhibiting radish seed germination by 88% when used at a concentration of 1 mM. It inhibits dihydrotestosterone-induced androgen receptor transcriptional activity (IC50 = 69 nM in a reporter assay), as well as the growth and colony formation of LNCaP and 22RV1 androgen receptor-expressing cells, but not androgen receptor-negative PC3 and DU145 cells, when used at a concentration of 0.1 μM. Ailanthone (2 mg/kg) reduces tumor volume in 22Rv1, LNCaP, and VCaP castration-resistant prostate cancer (CRPC) mouse xenograft models.

UsesAilanthone has potent antineoplastic activity against anti-hepatocellular carcinoma (HCC) and has been shown to inhibit Huh7 cancer cell growth through cell cycle arrest and apoptosis in vitro and in vivo.

PreparationTake fresh bark or root bark of Ailanthus altissima, soak it in 5-10 times its weight of alkaline water with pH=9-13 for 24-72 hours, filter, adjust the pH of the filtrate to neutral with acid, concentrate, and pass the concentrate through a macroporous adsorption resin column for adsorption. Wash with water to remove impurities, elute with 60-85% ethanol, collect 3-8 times the column volume of eluent, recover the ethanol under reduced pressure, refrigerate for 12-36 hours to crystallize, filter, take the filter residue, add acetone to recrystallize, wash and dry to obtain ailanthone.