The invention relates to a targeting active molecule in a natural product and an application thereof, and in particular relates to a GPR35 receptor new agonist in the natural product and an application thereof. The GPR35 receptor new agonist comprises the active ingredients of one or more than two of compounds of rheinic acid, quercetin, 7-demethylated gingko biflavone, prohypericin, baicalin, tetrahydrodimethoxydibenzoquinoline diol, aloe-emodin, norbodine, daidzein, tanshinone IIA, sweet clover, magnoflorine, cryptotanshinone and isofulvic alcohol and corresponding pharmaceutically acceptable salt forming compounds. In-vitro cell experiments show that natural compounds included in the GPR35 receptor new agonist have an agonistic effect on the GPR35 receptor. At present, researches show that the GPR35 receptor is closely related to asthma, heart failure, hypertension, inflammation, coronary heart disease, metabolic syndrome, pain, cancer and other diseases. The GPR35 receptor novel agonist provides candidate compounds for drug development of the related diseases.