Abstract

The development of new anticancer agents with a selective action mechanism has become a significant scientific challenge, especially as cancers remain the world’s leading cause of death. Actinobacteria and its bioactive compounds have recently become a promising perspective alternative to cancer therapy. In this study, some extracted metabolites of Micromonospora exhibited potent antimicrobial with microbial inhibition zone ≥ 7 mm, and cytotoxic activities against MCF-7 and HepG2 cell lines with promising activities ≥ 85%. Additionally, treatment of DENA/CCl4 rats with the strain Micromonospora sp1 has induced a substantial amelioration of the liver functions, enhancing liver architecture near normal and antioxidant properties through elevation of antioxidant enzyme levels. So that these preliminary results can provide metabolites from Micromonospora sp1 as an anti-liver cancer therapy. Finally, we introduced the chemical profiling of Micromonospora sp1 metabolic extract by LC-QTOF-MS-MS technique, where eight compounds with reported antioxidant property anti-liver cancer activity were targeted, validated as iNOS inhibitor through molecular docking studies. The findings in this study can be a significant step towards studying natural bioactive products produced by Micromonospora spp. as agents for anti-liver cancer.

Key points

• Metabolites of Micromonospora strain from unexploited Egyptian habitats were investigated with LC/MS library-based chemical profile and molecular docking studies as iNOS inhibitors.

• Some Micromonospora strains exhibited potent antimicrobial with microbial inhibition zone ≥ 7 mm, and cytotoxic activities against MCF-7 and HepG2 cell lines with promising activities ≥ 85%.

• Micromonospora extract exhibited anti-liver cancer activity in vivo through the antioxidant property by inhibiting the liver cancer biomarkers (LDH and AFP) and enhancing other biochemical parameters.

中文翻译：

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来自极少开发的埃及栖息地的小单孢菌物种：通过抗氧化特性的化学特征，抗菌和抗肿瘤活性

摘要

具有选择性作用机制的新型抗癌药的开发已成为一项重大的科学挑战，特别是因为癌症仍然是世界上主要的死亡原因。放线菌及其生物活性化合物最近已成为癌症治疗的有前景的替代方法。在这项研究中，Micromonospora的一些提取代谢物表现出有效的抗菌作用，其抑菌圈≥7 mm，对MCF-7和HepG2细胞系的细胞毒活性有望达到≥85％。此外，用菌株Micromonospora sp1处理DENA / CCl4大鼠已引起肝脏功能的显着改善，通过提高抗氧化酶水平来增强肝脏结构，使其接近正常水平和抗氧化性能。因此，这些初步结果可以提供Micromonospora sp1的代谢产物作为抗肝癌治疗方法。最后，我们介绍了通过LC-QTOF-MS-MS技术对Micromonospora sp1代谢提取物进行化学分析的方法，其中有八种具有报道的抗氧化性能和抗肝癌活性的化合物被作为目标，并通过分子对接研究确认为iNOS抑制剂。这项研究的发现可能是研究Micromonospora spp生产的天然生物活性产品的重要一步。作为抗肝癌药物。

关键点

•使用基于LC / MS库的化学特征和作为iNOS抑制剂的分子对接研究，研究了来自未开发埃及栖息地的微单孢菌菌株的代谢物。

•一些微单孢菌菌株表现出强效的抗菌作用，其抑菌圈≥7 mm，对MCF-7和HepG2细胞系的细胞毒活性有希望的活性≥85％。

•小单孢菌提取物通过抑制肝癌生物标志物（LDH和AFP）并增强其他生化参数，通过抗氧化特性在体内表现出抗肝癌活性。