The invention belongs to the technical field of pharmaceuticals, discloses application of a sarpogrelate containing pharmaceutical composition in treatment of diabetic nephropathy, and specifically discloses the application of a compound pharmaceutical composition taking sarpogrelate and 5-hydroxytryptamine synthesizing inhibitor as pharmaceutical active components in preparation of drugs for treating diabetic nephropathy. The test shows that gene silencing 5-HT synthetase and a 5-HT 2 receptor show good effect on inhibiting in-vitro culture and high glucose-induced oxidative stress of human renal mesangial cell strain, proinflammatory factor and chemotactic factor, and meanwhile, the gene silencing 5-HT synthetase system (Tph1 or AADC) and a 5HT 2 receptor are capable of greatly inhibiting high glucose-inducing effect and performing synergistic effect. With the adoption of the pharmaceutical composition, the diabetic nephropathy caused by high-fat feed feeding and streptozotocin induced diabetic nephropathy can be obviously treated; compared with simple prescription, the compound prescription is high in attenuation, and the lethal amount of mice orally taking the drug is obviouslyhalved.