G.B. Elyakov Pacific Institute of Bioorganic Chemistry FEB RAS, 690022, Vladivostok, Russia.
Institute of Cytology RAS, 194064, St. Petersburg, Russia.
J Antibiot (Tokyo). 2024 Dec;77(12):812-822. doi: 10.1038/s41429-024-00771-x. Epub 2024 Sep 10.
A new biological activity was discovered for marine fungal meroterpenoid meroantarctine A with unique 6/5/6/6 polycyclic system. It was found that meroantarctine A can significantly reduce biofilm formation by Staphylococcus aureus with an IC of 9.2 µM via inhibition of sortase A activity. Co-cultivation of HaCaT keratinocytes with a S. aureus suspension was used as an in vitro model of skin infection. Treatment of S. aureus-infected HaCaT cells with meroantarctine A at 10 µM caused a reduction in the production of TNF-α, IL-18, NO, and ROS, as well as LDH release and caspase 1 activation in these cells and, finally, recovered the proliferation and migration of HaCaT cells in an in vitro wound healing assay up to the control level. Thus, meroantarctine A is a new promising antibiofilm compound which can effective against S. aureus caused skin infection.
一种具有独特 6/5/6/6 多环系统的海洋真菌混合萜类化合物 meroantarctine A 被发现具有新的生物活性。研究发现，meroantarctine A 通过抑制 sortase A 活性，能显著降低金黄色葡萄球菌生物膜的形成，IC 为 9.2 μM。将 HaCaT 角质形成细胞与金黄色葡萄球菌悬浮液共培养作为皮肤感染的体外模型。用 10 μM 的 meroantarctine A 处理感染金黄色葡萄球菌的 HaCaT 细胞，可减少 TNF-α、IL-18、NO 和 ROS 的产生，以及 LDH 释放和这些细胞中 caspase 1 的激活，最终使体外伤口愈合试验中 HaCaT 细胞的增殖和迁移恢复到对照水平。因此，meroantarctine A 是一种有前途的新型抗生物膜化合物，可有效对抗金黄色葡萄球菌引起的皮肤感染。
