PDF(Pubmed)
Abstract：
Hederagenin (HG) is a natural pentacyclic triterpenoid that can be isolated from various medicinal herbs. By modifying the structure of HG, multiple derivatives with superior biological activities and safety profiles have been designed and synthesized. Accumulating evidence has demonstrated that HG and its derivatives display multiple pharmacological activities against cancers, inflammatory diseases, infectious diseases, metabolic diseases, fibrotic diseases, cerebrovascular and neurodegenerative diseases, and depression. Previous studies have confirmed that HG and its derivatives combat cancer by exerting cytotoxicity, inhibiting proliferation, inducing apoptosis, modulating autophagy, and reversing chemotherapy resistance in cancer cells, and the action targets involved mainly include STAT3, Aurora B, KIF7, PI3K/AKT, NF-κB, Nrf2/ARE, Drp1, and P-gp. In addition, HG and its derivatives antagonize inflammation through inhibiting the production and release of pro-inflammatory cytokines and inflammatory mediators by regulating inflammation-related pathways and targets, such as NF-κB, MAPK, JAK2/STAT3, Keap1-Nrf2/HO-1, and LncRNA A33/Axin2/β-catenin. Moreover, anti-pathogen, anti-metabolic disorder, anti-fibrosis, neuroprotection, and anti-depression mechanisms of HG and its derivatives have been partially elucidated. The diverse pharmacological properties of HG and its derivatives hold significant implications for future research and development of new drugs derived from HG, which can lead to improved effectiveness and safety profiles.
摘要：
Hederagenin（HG）是一种天然的五环三萜类化合物，可以从各种草药中分离出来。通过修改HG的结构，已设计并合成了具有优异生物活性和安全性的多种衍生物。越来越多的证据表明，HG及其衍生物对癌症具有多种药理活性。炎症性疾病，传染病,代谢性疾病，纤维化疾病,脑血管和神经退行性疾病，和抑郁症。以前的研究已经证实，HG及其衍生物通过发挥细胞毒性来对抗癌症，抑制增殖，诱导细胞凋亡，调节自噬，逆转癌细胞的化疗耐药性，涉及的行动目标主要包括STAT3、AuroraB、KIF7,PI3K/AKT,NF-κB,Nrf2/ARE,Drp1和P-gp。此外,HG及其衍生物通过调节炎症相关通路和靶点,抑制促炎细胞因子和炎症介质的产生和释放,从而拮抗炎症,如NF-κB，MAPK,JAK2/STAT3、Keap1-Nrf2/HO-1和LncRNAA33/Axin2/β-catenin。此外，抗病原体，抗代谢紊乱，抗纤维化，神经保护,HG及其衍生物的抗抑郁机制已部分阐明。HG及其衍生物的多种药理特性对未来HG衍生新药的研究和开发具有重要意义。这可以提高有效性和安全性。
