Chen Lingling, Feng Cheng, Shi Zhenyu, Wang Jianzhe, Wang Tao, Wang Yibing, Lin Lisong, Wu Ye
Fujian Key Laboratory of Oral Diseases & Stomatological Key Lab of Fujian College and University, School and Hospital of Stomatology, Fujian Medical University, Fuzhou, 350002, Fujian Province, China.
Department of Oral and Maxillofacial Surgery, The First Affiliated Hospital of Fujian Medical University, Fuzhou, 350004, Fujian Province, China.
BMC Complement Med Ther. 2025 Jul 2;25(1):217. doi: 10.1186/s12906-025-04957-0.
Oral squamous cell carcinoma (OSCC) is a significant public health issue worldwide. Conventional chemotherapeutic agents do not adequately meet the treatment demands because of their low efficacy and adverse side effects. Toosendanin (TSN) is a natural extract with potential anticarcinogenic activity. Nonetheless, its clinical application is constrained by its poor water-solubility and limited bioavailability. Therefore, we prepared TSN-loaded poly (lactic-co-glycolic acid) nanoparticles (TSN-PLGA NPs) to improve the water-solubility of TSN and potentially further enhance its bioavailability. TSN-PLGA NPs were synthesized and characterized, and we showed their exceptional properties for sustained release in vitro. TSN-PLGA NPs exhibited cytotoxic effects against OSCC cells, potentially inhibiting proliferation and promoting apoptosis by inducing cell-cycle arrest in the S-phase at low concentrations. RNA-sequencing analysis revealed the potential regulation of OSCC cell viability by TSN-PLGA NPs through signaling pathways such as JAK/STAT and PI3K-Akt. Furthermore, animal models provided evidence of the in vivo antitumor activity of TSN-PLGA NPs, with no observable side effects in nude mice, which indicated potential biocompatibility. Consequently, TSN-PLGA NPs may be a promising chemotherapy candidate for OSCC treatment.
口腔鳞状细胞癌（OSCC）是全球范围内一个重大的公共卫生问题。传统化疗药物由于疗效低和副作用大，无法充分满足治疗需求。川楝素（TSN）是一种具有潜在抗癌活性的天然提取物。然而，其临床应用受到水溶性差和生物利用度有限的限制。因此，我们制备了载有TSN的聚乳酸-羟基乙酸共聚物纳米颗粒（TSN-PLGA NPs），以提高TSN的水溶性，并有可能进一步提高其生物利用度。对TSN-PLGA NPs进行了合成和表征，我们展示了它们在体外持续释放的优异性能。TSN-PLGA NPs对OSCC细胞表现出细胞毒性作用，在低浓度下可能通过诱导细胞周期停滞在S期来抑制增殖并促进凋亡。RNA测序分析揭示了TSN-PLGA NPs通过JAK/STAT和PI3K-Akt等信号通路对OSCC细胞活力的潜在调节作用。此外，动物模型提供了TSN-PLGA NPs体内抗肿瘤活性的证据，裸鼠未观察到明显副作用，这表明其具有潜在的生物相容性。因此，TSN-PLGA NPs可能是一种有前途的用于OSCC治疗的化疗候选药物。
