Zou Denglang, Wang Qiqi, Chen Tao, Sang Duocheng, Yang Tingqin, Wang Yuhan, Gao Mengze, He Fangfang, Li Yulin, He Liangliang, Longzhu Duojie
School of Life Science, Qinghai Normal University, Xining, China.
College of Pharmacy, Jinan University, Guangzhou, China.
Front Pharmacol. 2022 Oct 19;13:1044027. doi: 10.3389/fphar.2022.1044027. eCollection 2022.
Bufadienolide, an essential member of the C-24 steroid family, is characterized by an α-pyrone positioned at C-17. As the predominantly active constituent in traditional Chinese medicine of Chansu, bufadienolide has been prescribed in the treatment of numerous ailments. It is a specifically potent inhibitor of Na/K ATPase with excellent anti-inflammatory activity. However, the severe side effects triggered by unbiased inhibition of the whole-body cells distributed α1-subtype of Na/K ATPase, restrict its future applicability. Thus, researchers have paved the road for the structural alteration of desirable bufadienolide derivatives with minimal adverse effects biotransformation. In this review, we give priority to the present evidence for structural diversity, MS fragmentation principles, anti-inflammatory efficacy, and structure modification of bufadienolides derived from toads to offer a scientific foundation for future in-depth investigations and views.
蟾毒配基是C-24甾体家族的重要成员，其特征是在C-17位有一个α-吡喃酮。作为中药蟾酥的主要活性成分，蟾毒配基已被用于治疗多种疾病。它是一种特异性的Na/K ATP酶强效抑制剂，具有出色的抗炎活性。然而，对全身分布的Na/K ATP酶α1亚型的无差别抑制所引发的严重副作用，限制了其未来的适用性。因此，研究人员通过生物转化为具有最小副作用的理想蟾毒配基衍生物的结构改变铺平了道路。在这篇综述中，我们优先考虑目前关于蟾蜍来源的蟾毒配基的结构多样性、质谱裂解原理、抗炎功效和结构修饰的证据，为未来的深入研究和观点提供科学依据。
