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Tongue cancer, a prevalent form of oral malignancy, particularly manifests as tongue squamous cell carcinoma (TSCC), which holds the highest incidence among oral squamous cell carcinoma cases, representing 43.4 % of occurrences. Presently, surgical resection stands as the primary treatment for TSCC, with no effective pharmaceutical interventions identified. This study aims to search for the potential anti-tumor properties and molecular mechanisms of a rearranged abietane diterpenoid extracted from Clerodendrum mandarinorum. Within this investigation, six known rearranged abietane diterpenoids (1–6) were isolated and characterized from C. mandarinorum. Notably, compound 1 demonstrated the most robust inhibitory effect against CAL-27 cells. Pharmacological assays further substantiated that compound 1 significantly restrained the proliferation, migration, and invasion of CAL-27 cells. Moreover, it was revealed that compound 1 directly interacted with TGFβR2, a pivotal receptor in the downstream signaling pathways of TGF-β/Smad and PI3K/AKT. Transcriptome analysis provided additional confirmation of these observations. Overall, our study highlights the promising potential of compound 1 as a therapeutic agent for the treatment of oral squamous cell carcinoma.

A novel redox-responsive PEG-sheddable copolymer of disulfide-linked polyethylene glycol 5000-lysine-di-tocopherol succinate (P5kSSLV) was designed and synthesized. Thin-film hydration method was used to prepare DOX-loaded P5kSSLV nanomicelle. To optimize the preparation technology, we investigate the effects of dosage, type of organic solvent, hydration temperature and time, and cryoprotectant on drug-loading content, encapsulation efficiency, particle size, and zeta potential. The mean particle size and zeta potential were determined by Zetasizer. The morphology of the P5kSSLV-DOX nanomicelles was visualized by transmission electron microscopy. The drug-loading content and encapsulation efficiency of P5kSSLV-DOX nanomicelle were investigated by UV. The drug-loading content, encapsulation efficiency, particle size, and zeta potential of the final optimized nanomicelles were 4.58%, 97.20%, 30.21 nm and −0.84 mV, respectively. In addition, the stability of nanomicelles was investigated, which included dilution stability and storage stability. The results showed that P5kSSLV-DOX nanomicelle had good dilution stability and storage stability at 4 °C. The preparation method of P5kSSLV-DOX nanomicelle with thin-film hydration method was practical and simple, which was valuable to be further studied.