Department of Technology for Organic Synthesis, Chemical Technology Institute, Ural Federal University, Mira 19, 620002 Yekaterinburg, Russia.
Center for Advanced Biotechnology and Medicine, Rutgers University, Piscataway, NJ 08854-8021, USA.
Biomolecules. 2023 Jul 12;13(7):1105. doi: 10.3390/biom13071105.
Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Despite having a wide range of pharmacological targets, no studies have proposed betulin as a multitarget compound. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It reduces postprandial hyperglycemia by inhibiting α-amylase and α-glucosidase activity, combats tumor cells by inducing apoptosis and inhibiting metastatic proteins, and modulates chronic inflammation by blocking the expression of proinflammatory cytokines via modulation of the NFκB and MAPKs pathways. Given its potential to influence diverse biological networks with high target specificity, it can be hypothesized that betulin may eventually become a new lead for drug development because it can modify a variety of pharmacological targets. The summarized research revealed that the diverse beneficial effects of betulin in various diseases can be attributed, at least in part, to its multitarget anti-inflammatory activity. This review focuses on the natural sources, pharmacokinetics, pharmacological activity of betulin, and the multi-target effects of betulin on signaling pathways such as MAPK, NF-κB, and Nrf2, which are important regulators of the response to oxidative stress and inflammation in the body.
桦木醇是一种天然的三萜类化合物,通常来源于桦树皮,具有潜在的伤口愈合特性。尽管桦木醇具有广泛的药理学靶点,但尚无研究将其作为一种多靶点化合物进行报道。桦木醇对心血管疾病和肝脏疾病、癌症、糖尿病、氧化应激和炎症具有保护作用。它通过抑制α-淀粉酶和α-葡萄糖苷酶的活性来降低餐后高血糖,通过诱导细胞凋亡和抑制转移蛋白来对抗肿瘤细胞,通过阻断促炎细胞因子的表达来调节慢性炎症,通过调节 NFκB 和 MAPKs 途径。鉴于其具有影响具有高靶特异性的多种生物网络的潜力,可以假设桦木醇最终可能成为药物开发的新先导化合物,因为它可以修饰多种药理学靶点。综述研究表明,桦木醇在各种疾病中的多种有益作用至少部分归因于其多靶点抗炎活性。本综述重点介绍了桦木醇的天然来源、药代动力学、药理学活性,以及桦木醇对 MAPK、NF-κB 和 Nrf2 等信号通路的多靶点作用,这些信号通路是机体对氧化应激和炎症反应的重要调节剂。