Drug resistance to the classically used chemotherapeutic drugs is the major challenge in their treatment of cancer needing the discovery of novel anticancer drugs. In terms of finding novel therapeutics, endophytes are quite promising as they are an excellent source of novel structures, which exhibit bioactivity. The present study demonstrated a dose-dependent antiproliferative activity of mycelial-derived secondary metabolites from a macroalgae associated endophyte Aspergillus unguis AG 1.1 (G). The antiproliferative activity of A. unguis mycelial extract (AUME) was observed on different human cancer cell lines. PI live/dead assay further confirmed the cytotoxic potential of the mycelial extract. Furthermore, AUME caused mitochondrial membrane aberration and generated ROS production as well indicating its potential to induce cell death by apoptosis. The metabolic profiling of the mycelial extract using GC-MS and LC-MS/MS revealed the presence of fatty acids, a benzoquinolinone derivative, imidazolidinedione derivative, diethyl phthalate and phthalate acid ester, a difuraxanthone, two prenylxanthone analogs and a phthalide derivative and some unknown metabolites. Presence of 4-(4-Hydroxy-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-benzo[h]quinolin-2-one, 1-hydroxy-3,5-dimethoxy-2-prenylxanthone, 1,6-dihydroxy-3-methoxy-2-prenylxanthone and 3-butylidene-7-hydroxyphthalide in AUME could be correlated to the notable cytotoxicity exhibited by the endophyte. The additional presence of many unidentified compounds heightened the prospects of finding some novel bioactive metabolites. Our results indicated that secondary metabolites produced by A. unguis AG 1.1 (G) have therapeutic potential as anticancer agents.

中文翻译：

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来自海洋大型藻类 Enteromorpha sp. 的 Aspergillus unguis AG 1.1 (G) 次级代谢物的抗增殖作用。通过诱导细胞内 ROS 产生和线粒体膜电位损失导致细胞凋亡

对经典使用的化疗药物的耐药性是其治疗癌症的主要挑战，需要发现新的抗癌药物。在寻找新疗法方面，内生菌是非常有前途的，因为它们是具有生物活性的新型结构的极好来源。本研究证明了来自大型藻类相关内生菌 Aspergillus unguis AG 1.1 (G) 的菌丝体衍生次级代谢物的剂量依赖性抗增殖活性。在不同的人类癌细胞系上观察到 A. unguis 菌丝体提取物 (AUME) 的抗增殖活性。PI 活/死测定进一步证实了菌丝体提取物的细胞毒性潜力。此外，AUME 引起线粒体膜畸变并产生 ROS，这表明其通过细胞凋亡诱导细胞死亡的潜力。使用 GC-MS 和 LC-MS/MS 对菌丝体提取物进行的代谢分析表明存在脂肪酸、苯并喹啉酮衍生物、咪唑烷二酮衍生物、邻苯二甲酸二乙酯和邻苯二甲酸酯、双呋喃酮、两种异戊二烯酮类似物和一种苯酞衍生物以及一些未知代谢物。4-(4-羟基-3,5-二甲氧基-苯基)-3,4-二氢-1H-苯并[h]喹啉-2-酮、1-羟基-3,5-二甲氧基-2-异戊二烯酮的存在， AUME 中的 1,6-二羟基-3-甲氧基-2-异戊二烯酮和 3-丁叉基-7-羟基苯酞可能与内生菌表现出的显着细胞毒性有关。许多未知化合物的额外存在增加了发现一些新型生物活性代谢物的前景。我们的结果表明，A. unguis AG 1.1 (G) 产生的次级代谢物具有作为抗癌剂的治疗潜力。