Ficus carica L., its fruits are delicious and can be eaten by human. Its leaves are commonly used to cure hemorrhoid and clear away heart ache. The milky sap of F. carica have a significant toxic effect against early fourth-stage larvae of Aedes aegypti L with an lethal concentration (LC(50)) value of 10.2 μg/ml and an LC(90) value of 42.3 μg/ml. Two natural furocoumarins, 5-methoxypsoralen and 8-methoxypsoralen were isolated from the milky sap of F. carica. The LC(50) value of 5-methoxypsoralen and 8-methoxypsoralen were 9.4 and 56.3 μg/ml, respectively. The above indicates that major compounds may play a more important role in the toxicity of the milky sap of F. carica.