PDF(Pubmed)
Abstract：
The increasing antifungal resistance rates against conventional drugs reveal the urgent need to search for new therapeutic alternatives. In this context, natural bioactive compounds have a critical role in antifungal drug development. Since evidence demonstrates that abietic acid, a diterpene found in Pinus species, has significant antimicrobial properties, this study aimed to evaluate the antifungal activity of abietic acid against Candida spp and its ability to potentiate the activity of fluconazole. Abietic acid was tested both individually and in combination with fluconazole against Candida albicans (CA INCQS 40006), Candida krusei (CK INCQS 40095), and Candida tropicalis (CT INCQS 40042). The microdilution method was used to determine the IC50 and the cell viability curve. Minimum Fungicidal Concentration (MFC) was determined by subculture in a solid medium. The plasma membrane permeability was measured using a fluorescent SYTOX Green probe. While the IC50 of the drugs alone ranged between 1065 and 3255 μg/mL, the IC50 resulting from the combination of abietic acid and fluconazole ranged between 7563 and 160.1 μg/mL. Whether used in combination with fluconazole or isolated, abietic acid exhibited Minimum Fungicidal Concentration (MFC) values exceeding 1024 μg/mL against Candida albicans, Candida krusei and Candida tropicalis. However, it was observed that the antifungal effect of fluconazole was enhanced when used in combination with abietic acid against Candida albicans and Candida tropicalis. These findings suggest that while abietic acid alone has limited inherent antifungal activity, it can enhance the effectiveness of fluconazole, thereby reducing antifungal resistance.
摘要：
对常规药物的抗真菌耐药率增加表明迫切需要寻找新的治疗替代方案。在这种情况下，天然生物活性化合物在抗真菌药物开发中起着至关重要的作用。由于证据表明松香酸，在松属物种中发现的一种二萜，具有显著的抗菌性能，本研究旨在评估松香酸对念珠菌的抗真菌活性及其增强氟康唑活性的能力。分别和联合氟康唑对白色念珠菌(CAINCQS4006)测试了阿霉素酸,克鲁斯念珠菌（CKINCQS40095），和热带念珠菌（CTINCQS40042）。使用微量稀释法测定IC50和细胞活力曲线。通过在固体培养基中传代培养来测定最小杀真菌浓度(MFC)。使用荧光SYTOXGreen探针测量质膜渗透性。虽然单独药物的IC50在1065和3255μg/mL之间，松香酸和氟康唑组合产生的IC50在7563和160.1μg/mL之间。无论是与氟康唑联合使用还是分离使用，松香酸对白色念珠菌的最低杀菌浓度（MFC）值超过1024μg/mL，克鲁斯念珠菌和热带念珠菌。然而,观察到，当与松香酸联合使用时，氟康唑对白色念珠菌和热带念珠菌的抗真菌作用增强。这些发现表明，虽然单独的松香酸具有有限的固有抗真菌活性，它可以增强氟康唑的有效性，从而降低抗真菌耐药性。
