埃博霉素是治疗实体瘤的常用抗癌药物之一，因其与 β-微管蛋白微管具有特殊的结合亲和力，稳定其分解，最终阻止细胞生长。埃博霉素最初是从纤维素纤维中分离出来的，然而，其生长速度极慢且埃博霉素产量低是挑战。因此，筛选一种新型内生真菌栖息的药用植物，具有较高的埃坡霉素生产力和生长操纵的可行性。黑曲霉 EFBL-SR OR342867 是 Latania loddegesii 的内生菌，已被认为是令人兴奋的埃博霉素生产者 (140.2 µg/L)。通过 HPLC、FTIR 和 LC-ESI-MS/MS 分析，解析了 TLC 纯化的假定黑曲霉样品的化学结构特性，其分子结构与正品埃坡霉素 B 相同。纯化的黑曲霉埃坡霉素 B显示出针对 MCF-7 (0.022 μM)、HepG-2 (0.037 μM) 和 HCT-116 (0.12 μM) 的弹性活性，选择性指数分别为 21.8、12.9 和 4。与未处理的细胞相比，纯化的埃坡霉素 B 在 24 小时后对 HepG-2 和 MCF-7 细胞表现出潜在的抗伤口愈合活性，分别提高了 54.07 % 和 60.0%。纯化的埃博霉素具有显着的抗增殖作用，将 MCF-7 细胞的生长抑制在 G2/M 期 2.1 倍，诱导总细胞凋亡 12.2 倍（与对照细胞相比）。通过响应面法优化了黑曲霉的埃坡霉素 B 生产率，比对照增加了 1.4 倍（266.9 μg/L）。在 4 °C 下斜坡培养 6 个月后，黑曲霉的埃坡霉素生产力降低了 2.4 倍，然而，L. loddegesii 的乙酸乙酯提取物的埃坡霉素生产力略有恢复，证实了植物来源的化学信号：部分触发黑曲霉埃坡霉素的生物合成基因。因此，这是第一份强调黑曲霉（L. loddegesii 的内生菌）生产埃坡霉素 B 的代谢效力的报告，这可能成为该药物工业生产的新平台。© 2024。作者。

Epothilones are one of the common prescribed anticancer drugs for solid tumors, for their exceptional binding affinity with β-tubulin microtubule, stabilizing their disassembly, causing an ultimate arrest to the cellular growth. Epothilones were initially isolated from Sornagium cellulosum, however, their extremely slow growth rate and low yield of epothilone is the challenge. So, screening for a novel fungal endophyte dwelling medicinal plants, with higher epothilone productivity and feasibility of growth manipulation was the objective. Aspergillus niger EFBL-SR OR342867, an endophyte of Latania loddegesii, has been recognized as the heady epothilone producer (140.2 μg/L). The chemical structural identity of the TLC-purified putative sample of A. niger was resolved from the HPLC, FTIR and LC-ESI-MS/MS analyses, with an identical molecular structure of the authentic epothilone B. The purified A. niger epothilone B showed a resilient activity against MCF-7 (0.022 μM), HepG-2 (0.037 μM), and HCT-116 (0.12 μM), with selectivity indices 21.8, 12.9 and 4, respectively. The purified epothilone B exhibited a potential anti-wound healing activity to HepG-2 and MCF-7 cells by ~ 54.07 and 60.0%, respectively, after 24 h, compared to the untreated cells. The purified epothilone has a significant antiproliferative effect by arresting the cellular growth of MCF-7 at G2/M phase by ~ 2.1 folds, inducing the total apoptosis by ~ 12.2 folds, normalized to the control cells. The epothilone B productivity by A. niger was optimized by the response surface methodology, with ~ 1.4 fold increments (266.9 μg/L), over the control. The epothilone productivity by A. niger was reduced by ~ 2.4 folds by 6 months storage as a slope culture at 4 °C, however, the epothilone productivity was slightly restored with ethylacetate extracts of L. loddegesii, confirming the plant-derived chemical signals that partially triggers the biosynthetic genes of A. niger epothilones. So, this is the first report emphasizing the metabolic potency of A. niger, an endophyte of L. loddegesii, to produce epothilone B, that could be a new platform for industrial production of this drug.© 2024. The Author(s).