The advancement of structure, bioactivity, mechanism, and synthesis of bufotalin

IF 2.1 4区医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY

Steroids Pub Date : 2025-02-01 DOI:10.1016/j.steroids.2024.109555

Nuo Chen , Yunqiang Wu , Huamao Wei , Shuai Zhi , Liwei Liu

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引用次数: 0

Abstract

Toad venom, a family of toxic yet pharmacologically valuable biotoxins, has long been utilized in traditional medicine and holds significant promise in modern drug development. Bufotalin, a prominent bufotoxin, has demonstrated potent cytotoxic properties through mechanisms such as apoptosis induction, cell cycle arrest, endoplasmic reticulum stress activation, and inhibition of metastasis by modulating key pathways including Akt, p53, and STAT3/EMT signaling—these multi-target mechanisms position bufotalin as a promising agent to combat multidrug resistance in cancer therapy. Additionally, advances in bufotalin synthesis, including chemical and biocatalytic methods, have streamlined production, with strategies such as C14α-hydroxylation and novel coupling techniques enhancing yield and reducing environmental impact. This review consolidates recent progress on bufotalin’s structure, activity, cytotoxic mechanisms, and synthetic methodologies, offering a foundation for further development as an innovative chemotherapy agent.

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丁福他林的结构、生物活性、机理及合成研究进展。

蟾蜍毒液是一种具有毒性但具有药理价值的生物毒素，长期以来一直在传统医学中使用，在现代药物开发中具有重要的前景。Bufotalin是一种著名的蟾毒毒素，通过调节包括Akt、p53和STAT3/EMT信号在内的关键通路，通过诱导凋亡、细胞周期阻滞、内质网应激激活和抑制转移等机制显示出强大的细胞毒性，这些多靶点机制使Bufotalin成为对抗癌症多药耐药的有希望的药物。此外，bufotalin合成的进展，包括化学和生物催化方法，简化了生产，如C14-α-羟基化和新的偶联技术，提高了产量，减少了对环境的影响。本文综述了蟾毒灵的结构、活性、细胞毒性机制和合成方法等方面的最新进展，为蟾毒灵作为一种新型化疗药物的进一步开发奠定了基础。

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来源期刊

Steroids 医学-内分泌学与代谢

CiteScore

5.10

自引率

3.70%

发文量

120

审稿时长

73 days

期刊介绍： STEROIDS is an international research journal devoted to studies on all chemical and biological aspects of steroidal moieties. The journal focuses on both experimental and theoretical studies on the biology, chemistry, biosynthesis, metabolism, molecular biology, physiology and pharmacology of steroids and other molecules that target or regulate steroid receptors. Manuscripts presenting clinical research related to steroids, steroid drug development, comparative endocrinology of steroid hormones, investigations on the mechanism of steroid action and steroid chemistry are all appropriate for submission for peer review. STEROIDS publishes both original research and timely reviews. For details concerning the preparation of manuscripts see Instructions to Authors, which is published in each issue of the journal.