Ufa Institute of Chemistry, UFA Federal Research Centre of the Russian Academy of Sciences, Pr. Oktyabrya, 450054 Ufa, Russia.
Laboratory of Metabotropic Drugs, Scientific Center for Innovative Drugs, Volgograd State Medical University, Novorossiyskaya St. 39, 400087 Volgograd, Russia.
Int J Mol Sci. 2022 Jan 19;23(3):1075. doi: 10.3390/ijms23031075.
This review comprehensively describes the recent advances in the synthesis and pharmacological evaluation of steroid polyamines squalamine, trodusquemine, ceragenins, claramine, and their diverse analogs and derivatives, with a special focus on their complete synthesis from cholic acids, as well as an antibacterial and antiviral, neuroprotective, antiangiogenic, antitumor, antiobesity and weight-loss activity, antiatherogenic, regenerative, and anxiolytic properties. Trodusquemine is the most-studied small-molecule allosteric PTP1B inhibitor. The discovery of squalamine as the first representative of a previously unknown class of natural antibiotics of animal origin stimulated extensive research of terpenoids (especially triterpenoids) comprising polyamine fragments. During the last decade, this new class of biologically active semisynthetic natural product derivatives demonstrated the possibility to form supramolecular networks, which opens up many possibilities for the use of such structures for drug delivery systems in serum or other body fluids.
这篇综述全面描述了甾体聚胺鲨胺、曲多沙胺、神经酰胺、克拉胺及其多种类似物和衍生物的合成和药理学评价的最新进展，特别关注它们从胆酸的全合成，以及抗菌和抗病毒、神经保护、抗血管生成、抗肿瘤、抗肥胖和减肥、抗动脉粥样硬化、再生和抗焦虑特性。曲多沙胺是研究最多的小分子变构 PTP1B 抑制剂。鲨胺的发现是动物来源的先前未知的天然抗生素新类别的第一个代表，这激发了对包含聚胺片段的萜类化合物（特别是三萜类化合物）的广泛研究。在过去的十年中，这类新的生物活性半合成天然产物衍生物展示了形成超分子网络的可能性，这为将此类结构用于血清或其他体液中的药物输送系统开辟了许多可能性。
