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三萜类天然化合物桦木酸用于治疗被忽视热带病的潜力:新型疗法

Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments.

作者信息

Rocha Vinícius, Quadros Helenita, Meira Cássio, Silva Laís, Carvalho Dahara, Hodel Katharine, Moreira Diogo, Soares Milena

机构信息

Institute of Health Technology (SENAI CIMATEC ITS), Salvador 41650-010, BA, Brazil.

Gonçalo Moniz Institute, Oswaldo Cruz Foundation (IGM-FIOCRUZ/BA), Salvador 40296-710, BA, Brazil.

出版信息

Biomedicines. 2022 Apr 1;10(4):831. doi: 10.3390/biomedicines10040831.

Abstract

Neglected tropical diseases are one of the most important public health problems in many countries around the world. Among them are leishmaniasis, Chagas disease, and malaria, which contribute to more than 250 million infections worldwide. There is no validated vaccine to prevent these infections and the treatments available are obsolete, highly toxic, and non-effective due to parasitic drug resistance. Additionally, there is a high incidence of these diseases, and they may require hospitalization, which is expensive to the public health systems. Therefore, there is an urgent need to develop new treatments to improve the management of infected people, control the spread of resistant strains, and reduce health costs. Betulinic acid (BA) is a triterpene natural product which has shown antiparasitic activity against , and . Here, we review the main results regarding the in vitro and in vivo pharmacological activity of BA and its derivatives against these parasites. Some chemical modifications of BA have been shown to improve its activities against the parasites. Further improvement on studies of drug-derived, as well as structure-activity relationship, are necessary for the development of new betulinic acid-based treatments.

摘要

被忽视的热带病是世界上许多国家最重要的公共卫生问题之一。其中包括利什曼病、恰加斯病和疟疾,这些疾病在全球造成了超过2.5亿例感染。目前尚无经过验证的疫苗来预防这些感染,而且现有的治疗方法过时、毒性高,并且由于寄生虫产生耐药性而无效。此外,这些疾病的发病率很高,可能需要住院治疗,这对公共卫生系统来说成本高昂。因此,迫切需要开发新的治疗方法,以改善对感染者的管理,控制耐药菌株的传播,并降低医疗成本。桦木酸(BA)是一种三萜类天然产物,已显示出对[具体寄生虫1]、[具体寄生虫2]和[具体寄生虫3]的抗寄生虫活性。在此,我们综述了关于BA及其衍生物对这些寄生虫的体外和体内药理活性的主要研究结果。已证明对BA进行一些化学修饰可提高其对寄生虫的活性。为了开发新的基于桦木酸的治疗方法,有必要进一步改进药物衍生研究以及构效关系研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2af9/9027248/32182ea8344f/biomedicines-10-00831-g002.jpg

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