桦木酸抗纤维化作用及其机制研究进展

Research progress on anti-fibrotic effect and mechanism of betulinic acid

五环三萜类化合物广泛存在于自然界,如齐墩果酸,是目前被批准在中国治疗肝纤维化疾病如急慢性肝炎的五环三萜类化合物,其能够降低患者血清肝酶,延缓肝纤维化进展。中药活性成分是研究热点,桦木酸(betulinic acid,BA)又称为白桦酸,是一种羽扇豆烷型五环三萜类化合物,广泛存在于植物中,目前已经发现BA有着多种较强的生物活性,如抗癌、抗炎、抗氧化应激、抗菌、免疫调节、抗寄生虫、抗溃疡及抗疟疾等。组织器官纤维化是临床常见疾病的最终病理表现,严重危害人们的健康,死亡率高、预后差,且目前没有靶向完全逆转纤维化疾病药物。BA先天具有多重药理作用,近来有证据显示BA兼顾着抗纤维化作用,甚至在肺纤维化模型研究中BA疗效优于一线治疗药物吡非尼酮,表明其很可能是治疗纤维化疾病的新星。本文对BA抗纤维化作用及其机制进行简要综述,为未来纤维化疾病药物治疗提供一种新的选择。

Pentacyclic triterpenoids are widely found in nature,such as oleanolic acid,which is currently approved in China to treat liver fibrosis diseases such as acute and chronic hepatitis.It can reduce serum liver enzymes and delay the progression of liver fibrosis.The active ingredient of traditional Chinese medicine is a research hotspot.Betulinic acid(BA)is a lupin-type pentacyclic triterpenoid,which is widely found in plants.It has been found that BA has a variety of strong biological activities,such as anticancer,anti-inflammatory,anti-oxidative stress,antibacterial,immunomodulatory,antiparasitic,antiulcer and antimalarial effects.Tissue and organ fibrosis is the final pathological manifestation of common clinical diseases,seriously endangering people's health,with high mortality and poor prognosis,and there are currently no targeted drugs to completely reverse fibrotic diseases.BA innately has multiple pharmacological effects.Recently,evidence has shown that BA has both anti-fibrotic effects.Even in the model study of pulmonary fibrosis,the efficacy of BA is better than that of the first-line treatment drug pirfenidone,indicating that it is likely to be a new star in the treatment of fibrotic diseases.This paper briefly reviews the anti-fibrotic effect of BA and its mechanism,and provides a new option for the future drug treatment of fibrotic diseases.