Abstract
Background: Oral squamous cell carcinoma (OSCC) is a major epithelial malignancy of the head and neck with high morbidity and mortality. The conventional antineoplastic medications used in clinical practice have become less effective due to the heterogeneity of tumors, accompanied by severe side effects. Therefore, the development of novel chemotherapeutic agents has become an important goal of anti-OSCC therapy. Methods: Our group has previously developed a novel wogonin-aloperine co-amorphous (Wog-Alop). In this study, the anti-OSCC efficacy of Wog-Alop was evaluated by a patient-derived tumor xenograft (PDX) model. Subsequently, network pharmacology was employed to predict the key targets of Wog-Alop on OSCC, and the predicted key targets were further confirmed by Western blot and immunochemistry. Results: The results revealed that Wog-Alop manifests the higher efficacy in inhibition of OSCC proliferation by regulating the expression of the key targets, Bcl-2, Bax, P53, and Caspase3, implying that the apoptotic mechanism is implicated in Wog-Alop-induced inhibition of proliferation in OSCC. Conclusions: Collectively, the present work demonstrated anti-OSCC bioactivity of Wog-Alop, suggesting that Wog-Alop could be developed as an innovative therapeutic agent for OSCC therapy.