The invention discloses a type of isoquinoline as well as a preparation method and application thereof, and belongs to the field of medicine. The isoquinoline is 1-methoxy-4,5-dihydroxy isoquinoline, is extracted from centipede, and can be used for treating malaria, killing pathogen, and treating solid tumors, wherein malaria is caused by plasmodium vivax, plasmodium malariae, plasmodium falciparum and plasmodium ovale which are parasitic on a human body; the pathogen can be colibacillus, staphylococcus aureus, pseudomonas aeruginosa, alpha / beta hemolytic streptococcus, streptococcus pneumoniae and haemophilus influenzae; the tumors are primary or secondary cancer or sarcomas sourced from a human head, neck, brain, thyroid, pancreas, lung, liver, esophagus, stomach, mammary gland, kidney, gallbladder, colon / rectum, ovary, uterus, uterine cervix, prostate, bladder, and testis. The isoquinoline is relatively little in toxic or / and side effects, and can be used for treating and adjuvant treating of various cancer.