Health Sciences Center, Federal University of Paraiba, Cidade Universitária, João Pessoa, PB, 58051-900, Brazil.
Education and Health Center, Professora Maria Anita Furtado Coelho, Bairro Sítio Olho D'água da Bica, Federal University of Campina Grande, Cuité, PB, 58175-000, Brazil.
Braz J Microbiol. 2024 Mar;55(1):133-142. doi: 10.1007/s42770-023-01158-0. Epub 2023 Nov 23.
Infections of fungal origin are mainly caused by Candida spp. Some species, such as C. albicans, C. glabrata, C. parapsilosis, and C. tropicalis, stand out as promoters of diseases in humans. This study evaluated the synthesis and antifungal effects of (E)-3-(furan-2-yl)acrylic acid. The synthesis of the compound showed a yield of 88%, considered high. The minimum inhibitory concentration of the synthetic compound, amphotericin B, and fluconazole isolated against four Candida species ranged from 64 to 512 μg/mL, 1 to 2 μg/mL, and 32 to 256 μg/mL, respectively. The synergistic effect of the test compound was observed when associated with amphotericin B against C. albicans and C. tropicalis, with no antagonism between the substances against any of the strains tested. The potential drug promoted morphological changes in C. albicans, decreasing the amount of resistance and virulence, and reproduction structures, such as the formation of pseudohyphae, blastoconidia, and chlamydospores. Furthermore, it was also possible to identify the fungistatic profile of the test substance by studying the growth kinetics of C. albicans. Finally, it was observed that the test compound stimulated ergosterol biosynthesis by the yeast, probably by activating microbial resistance responses.
真菌感染主要由念珠菌属引起。一些物种，如白色念珠菌、光滑念珠菌、近平滑念珠菌和热带念珠菌，是人类疾病的主要病原体。本研究评估了（E）-3-（呋喃-2-基）丙烯酸的合成和抗真菌作用。该化合物的合成产率为 88%，被认为是高产率。合成化合物、两性霉素 B 和氟康唑对四种念珠菌的最低抑菌浓度分别为 64 至 512μg/mL、1 至 2μg/mL 和 32 至 256μg/mL。该测试化合物与两性霉素 B 联合使用时对白色念珠菌和热带念珠菌表现出协同作用，而在测试的任何菌株中，两种物质之间均没有拮抗作用。该潜在药物可使白色念珠菌发生形态变化，降低其耐药性和毒力，并减少假菌丝、芽生孢子和厚垣孢子等繁殖结构的形成。此外，通过研究白色念珠菌的生长动力学，还可以确定该测试物质的抑菌特性。最后，观察到该测试化合物刺激酵母甾醇生物合成，这可能是通过激活微生物的抗性反应。
