Monaspin B, a Novel Cyclohexyl-furan from Cocultivation of Monascus purpureus and Aspergillus oryzae, Exhibits Potent Antileukemic Activity,Journal of Agricultural and Food Chemistry

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Monaspin B, a Novel Cyclohexyl-furan from Cocultivation of Monascus purpureus and Aspergillus oryzae, Exhibits Potent Antileukemic Activity
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2024-01-03 , DOI: 10.1021/acs.jafc.3c08187
Zitong Meng _{1,

2} , Yingao Tan _{1,

3} , Ya-Li Duan _{1,

3} , Mu Li _{1,

3}

Affiliation

Natural products are a rich resource for the discovery of innovative drugs. Microbial cocultivation enables discovery of novel natural products through tandem enzymatic catalysis between different fungi. In this study, Monascus purpureus, as a food fermentation strain capable of producing abundant natural products, was chosen as an example of a cocultivation pair strain. Cocultivation screening revealed that M. purpureus and Aspergillus oryzae led to the production of two novel cyclohexyl-furans, Monaspins A and B. Optimization of the cocultivation mode and media enhanced the production of Monaspins A and B to 1.2 and 0.8 mg/L, respectively. Monaspins A and B were structurally elucidated by HR-ESI-MS and NMR. Furthermore, Monaspin B displayed potent antiproliferative activity against the leukemic HL-60 cell line by inducing apoptosis, with a half-maximal inhibitory concentration (IC₅₀) of 160 nM. Moreover, in a mouse leukemia model, Monaspin B exhibited a promising in vivo antileukemic effect by reducing white blood cell, lymphocyte, and neutrophil counts. Collectively, these results indicate that Monaspin B is a promising candidate agent for leukemia therapy.

中文翻译：

Monaspin B 是一种由红曲霉和米曲霉共培养的新型环己基呋喃，具有有效的抗白血病活性

天然产物是发现创新药物的丰富资源。微生物共培养能够通过不同真菌之间的串联酶催化发现新型天然产物。在本研究中，红曲霉作为一种能够产生丰富天然产物的食品发酵菌株，被选为共培养配对菌株的例子。共培养筛选表明， M. purpureus和Aspergillus oryzae产生了两种新型环己基呋喃：Monaspins A 和 B。共培养模式和培养基的优化将 Monaspins A 和 B 的产量分别提高到 1.2 和 0.8 mg/L 。通过 HR-ESI-MS 和 NMR 阐明了 Monaspins A 和 B 的结构。此外，Monaspin B 通过诱导细胞凋亡，对白血病 HL-60 细胞系表现出有效的抗增殖活性，半数最大抑制浓度 (IC ₅₀ ) 为 160 nM。此外，在小鼠白血病模型中，Monaspin B 通过减少白细胞、淋巴细胞和中性粒细胞计数，表现出良好的体内抗白血病作用。总的来说，这些结果表明 Monaspin B 是一种有前途的白血病治疗候选药物。

更新日期：2024-01-03

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