Dos Santos Rafael Ferreira, Velez Afonso Santine M M, Dos Santos Gabriel Fulgencio, Pitasse-Santos Paulo, de Oliveira Bruno Sena, Freire de Lima Marco Edilson, Sant'Anna Carlos Mauricio R, Braz Filho Raimundo, Decote-Ricardo Debora, Castro Rosane Nora
Instituto de Química, Departamento de Química Orgânica, Universidade Federal Rural do Rio de Janeiro, CEP 23890-000 Seropédica, RJ, Brasil.
Leicester Institute of Structural and Chemical Biology, University of Leicester, Leicester LE1 7RH, U.K.
ACS Omega. 2025 May 27;10(22):23397-23408. doi: 10.1021/acsomega.5c01804. eCollection 2025 Jun 10.
Geopropolis is a natural antibiotic produced by stingless bees, supplemented with earth and clay. Bee products are a promising source of natural bioactive compounds with potential for the development of new drugs for neglected tropical diseases, such as Chagas disease. This study analyzed extracts of geopropolis from the Bosque da Barra da Tijuca (RJ, Brazil) and evaluated their activity against . The extracts were obtained using commercial grain alcohol 96° GL and fractionated with hexane and dichloromethane. The antichagasic activity was determined, with IC values ranging from 4.54 to 53.02 μg/mL. Phytochemical investigation of the dichloromethane fraction resulted in the isolation of two -methylated flavanones, (2)-strobopinin and (2)-cryptostrobin, which were identified for the first time in Brazilian geopropolis. These compounds showed IC values of 21.21 μM and 21.55 μM, respectively, with distinct cytotoxities: 33.80 μM for strobopinin and 99.79 μM for cryptostrobin. Molecular modeling studies were conducted to propose a mechanism of action on a candidate enzyme target, glyceraldehyde-3-phosphate dehydrogenase, and possible reasons for the selectivity differences caused by -methylation. The results highlight geopropolis as a promising natural source of antiparasitic agents, supporting its potential for drug development.
地蜂胶是一种由无刺蜂生产的天然抗生素，添加了泥土和黏土。蜂产品是天然生物活性化合物的一个有前景的来源，具有开发用于治疗被忽视热带病（如恰加斯病）新药的潜力。本研究分析了来自巴西里约热内卢蒂茹卡巴拉森林的地蜂胶提取物，并评估了它们对……的活性。提取物使用96°GL商业谷物酒精获得，并用己烷和二氯甲烷进行分馏。测定了抗恰加斯病活性，IC值范围为4.54至53.02μg/mL。对二氯甲烷馏分进行植物化学研究，分离出两种甲基化黄烷酮，（2）-异水飞蓟宾和（2）-隐水飞蓟宾，这两种化合物在巴西地蜂胶中首次被鉴定。这些化合物的IC值分别为21.21μM和21.55μM，具有不同的细胞毒性：异水飞蓟宾为33.80μM，隐水飞蓟宾为99.79μM。进行了分子模拟研究，以提出对候选酶靶点甘油醛-3-磷酸脱氢酶的作用机制，以及甲基化导致选择性差异的可能原因。结果突出了地蜂胶作为一种有前景的抗寄生虫剂天然来源，支持其在药物开发方面的潜力。
