Ye Qingmei, Zhou Xin, Ren Han, Han Fangxuan, Lin Rong, Li Juan
Hainan General Hospital & Hainan Affiliated Hospital of Hainan Medical University, Haikou, Hainan, China.
Key Laboratory of Tropical Medicinal Resource Chemistry of Ministry of Education, Key Laboratory of Tropical Medicinal Plant Chemistry of Hainan Province, College of Chemistry and Chemical Engineering, Hainan Normal University, Haikou, Hainan, China.
Front Pharmacol. 2023 Oct 4;14:1274336. doi: 10.3389/fphar.2023.1274336. eCollection 2023.
Profound progress has been made in cancer treatment in the past three decades. However, drug resistance remains prevalent and a critical challenge. Drug resistance can be attributed to oncogenes mutations, activated defensive mechanisms, ATP-bind cassette transporters overexpression, cancer stem cells, Chinese traditional medicine toad venom has been used for centuries for different diseases, including resistant cancers. Bufalin is one of the bufadienolides in toad venom that has been extensively studied for its potential in refractory and drug-resistant cancer treatments and . In this work, we would like to critically review the progress made in the past decade (2013-2022) of bufalin in overcoming drug resistance in cancers. Generally, bufalin shows high potential in killing certain refractory and resistant cancer cells via multiple mechanisms. More importantly, bufalin can work as a chemo-sensitizer that enhances the sensitivity of certain conventional and targeted therapies at low concentrations. In addition, the development of bufalin derivatives was also briefly summarized and discussed. We also analyzed the obstacles and challenges and provided possible solutions for future perspectives. We hope that the collective information may help evoke more effort for more in-depth studies and evaluation of bufalin in both lab and possible clinical trials.
在过去三十年里，癌症治疗取得了巨大进展。然而，耐药性仍然普遍存在且是一个关键挑战。耐药性可归因于癌基因突变、激活的防御机制、ATP结合盒转运体过表达、癌症干细胞。几个世纪以来，中国传统中药蟾酥一直被用于治疗包括耐药癌症在内的各种疾病。蟾毒灵是蟾酥中的一种蟾蜍二烯羟酸内酯，其在难治性和耐药性癌症治疗中的潜力已得到广泛研究。在这项工作中，我们将批判性地回顾过去十年（2013 - 2022年）蟾毒灵在克服癌症耐药性方面取得的进展。一般来说，蟾毒灵通过多种机制在杀死某些难治性和耐药性癌细胞方面具有很高的潜力。更重要的是，蟾毒灵可以作为一种化疗增敏剂，在低浓度下增强某些传统疗法和靶向疗法的敏感性。此外，还简要总结和讨论了蟾毒灵衍生物的开发情况。我们还分析了障碍和挑战，并为未来展望提供了可能的解决方案。我们希望这些汇总信息可能有助于激发更多努力，以便在实验室和可能的临床试验中对蟾毒灵进行更深入的研究和评估。
