Department of Chemistry, University of South Florida, 4202 E. Fowler Avenue, CHE205, Tampa, FL 33620, USA.
Department of Cell Biology, Microbiology, and Molecular Biology, University of South Florida, 4202 E. Fowler Avenue, ISA2015, Tampa, FL 33620, USA.
Mar Drugs. 2020 Jun 23;18(6):327. doi: 10.3390/md18060327.
The Antarctic sponge is rich in defensive terpenoids with promising antimicrobial potential. Investigation of this demosponge has resulted in the generation of a small chemical library containing diterpenoid secondary metabolites with bioactivity in an infectious disease screening campaign focused on , , and methicillin-resistant (MRSA) biofilm. In total, eleven natural products were isolated, including three new compounds designated dendrillins B-D (-). Chemical modification of abundant natural products led to three semisynthetic derivatives (-), which were also screened. Several compounds showed potency against the leishmaniasis parasite, with the natural products tetrahydroaplysulphurin-1 () and dendrillin B (), as well as the semisynthetic triol , displaying single-digit micromolar activity and low mammalian cytotoxicity. Triol displayed the best profile against the liver-stage malaria parasites, while membranolide () and dendrillin C () were strong hits against MRSA biofilm cultures.
南极海绵富含具有潜在抗菌作用的防御性萜类化合物。对这种普通海绵的研究产生了一个小型化学文库，其中包含具有生物活性的二萜类次生代谢产物，这些产物在针对耐甲氧西林金黄色葡萄球菌（MRSA）生物膜的传染病筛选活动中具有活性。总共分离出 11 种天然产物，包括 3 种新化合物，分别命名为 dendrillins B-D (-)。对丰富的天然产物进行化学修饰得到了 3 种半合成衍生物 (-)，也对其进行了筛选。几种化合物对利什曼原虫表现出了很强的活性，天然产物四氢阿朴硫因-1 () 和 dendrillin B (),以及半合成三醇, 显示出个位数微摩尔的活性和低哺乳动物细胞毒性。三醇 对肝期疟原虫表现出最好的活性，而 membranolide () 和 dendrillin C () 则是抗 MRSA 生物膜培养物的强抑制剂。
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