The invention provides a botanical drug active part of aquilaria sinensis (Lour.) Spreng., a preparation method thereof, a pharmaceutical composition composed of the active part, and application of the botanical drug active part and the pharmaceutical composition in preparation of drugs for treating tumors or cancers. The preparation method comprises the following steps: extracting and extracting dried flos aquilaria sinensis by using a solvent to prepare PXS65, PXS66, PXS66-1, PXS66-2 and PXS66-3; the pharmaceutical composition has remarkable inhibitory activity on cancer cell strains, such as lung cancer SPC-A-1 cells, lung cancer NCI-H520 cells, lung cancer A549 cells, cervical cancer HeLa cells, human neuroblastoma SH-SY5Y cells, ovarian cancer SK-OV-3 cells, leukemia MT4 cells, prostate cancer PC-3 cells, liver cancer SMMC-7721 cells, breast cancer MDA-MB-231 cells, lung cancer NCI-H446 cells, lung cancer taxol drug-resistant strain A549/Taxol cells and the like. The flos aquilaria sinensis extract disclosed by the invention provides a new choice for drugs for treating or preventing tumors or cancers and drugs for improving tumor or cancer drug resistance.