背景:β-榄香烯(IUPAC名称:(1S,2S,4R)-1-乙烯基-1-甲基-2,4-双(丙-1-烯-2-基)环己烷),是在姜黄根中发现的天然化合物。研究表明其具有多种生物学功能,包括它的抗肿瘤特性,已被广泛调查。然而,这些尚未审查。这篇综述的目的是提供对β-榄香烯研究的全面总结,关于疾病治疗。
方法:在PubMed中发现了与β-榄香烯相关的文章,ScienceDirect,和谷歌学者数据库系统地总结其结构,药代动力学,新陈代谢,和药理活性。我们还在中药系统药理学数据库中搜索了β-榄香烯的治疗靶点。我们进一步将这些靶标与KEGG和GO分析的相关文献相结合。
结果:对β-榄香烯活性的分子机制的研究表明,它调节多种途径,包括STAT3,MAPK,细胞周期蛋白依赖性激酶1/细胞周期蛋白B,缺口,PI3K/AKT,活性氧,METTL3,PTEN,p53,FAK,MMP,TGF-β/Smad信号传导。通过这些分子途径,β-榄香烯与肿瘤细胞增殖有关,凋亡,迁移,和入侵和改善免疫微环境。此外,β-榄香烯通过抑制DNA损伤修复和调节CTR1,pak1,ERK1/2,ABC转运蛋白等途径来提高化疗药物的敏感性和逆转耐药性,Prx-1和ERCC-1。尽管如此,由于其亲脂性和低生物利用度,额外的结构修饰可以提高该药物的疗效.
结论:β-榄香烯毒性低,安全性好,通过体内和体外的不同机制抑制各种肿瘤类型。当与化疗药物联合使用时,它增强了功效,减少毒性,并提高肿瘤的杀伤能力。因此,β-榄香烯具有巨大的研究和开发潜力。
BACKGROUND: β-Elemene (IUPAC name: (1 S,2 S,4 R)-1-ethenyl-1-methyl-2,4-bis(prop-1-en-2-yl) cyclohexane), is a natural compound found in turmeric root. Studies have demonstrated its diverse biological functions, including its anti-tumor properties, which have been extensively investigated. However, these have not yet been reviewed. The aim of this review was to provide a comprehensive summary of β-elemene research, with respect to disease treatment.
METHODS: β-Elemene-related articles were found in PubMed, ScienceDirect, and Google Scholar databases to systematically summarize its structure, pharmacokinetics, metabolism, and pharmacological activity. We also searched the Traditional Chinese Medicine System Pharmacology database for therapeutic targets of β-elemene. We further combined these targets with the relevant literature for KEGG and GO analyses.
RESULTS: Studies on the molecular mechanisms underlying β-elemene activity indicate that it regulates multiple pathways, including STAT3, MAPKs, Cyclin-dependent kinase 1/cyclin B, Notch, PI3K/AKT, reactive oxygen species, METTL3, PTEN, p53, FAK, MMP, TGF-β/Smad signaling. Through these molecular pathways, β-elemene has been implicated in tumor cell proliferation, apoptosis, migration, and invasion and improving the immune microenvironment. Additionally, β-elemene increases chemotherapeutic drug sensitivity and reverses resistance by inhibiting DNA damage repair and regulating pathways including CTR1, pak1, ERK1/2, ABC transporter protein, Prx-1 and ERCC-1. Nonetheless, owing to its lipophilicity and low bioavailability, additional structural modifications could improve the efficacy of this drug.
CONCLUSIONS: β-Elemene exhibits low toxicity with good safety, inhibiting various tumor types via diverse mechanisms in vivo and in vitro. When combined with chemotherapeutic drugs, it enhances efficacy, reduces toxicity, and improves tumor killing. Thus, β-elemene has vast potential for research and development.