Graduate Institute of Marine Biology, National Dong Hwa University, Pingtung 94450, Taiwan.
Planning & Research Division, National Museum of Marine Biology and Aquarium, Pingtung 94450, Taiwan.
Mar Drugs. 2018 Feb 27;16(3):75. doi: 10.3390/md16030075.
Four new briarane diterpenoids, briaviolides K-N (-), have been obtained from the cultured-type octocoral . Using a spectroscopic approach, the structures of briaranes - were identified. This study employed an in vitro model of lipopolysaccharide (LPS)-induced inflammation in the murine macrophage RAW 264.7 cell line, and found that among the four briaranes, briarane possessed anti-inflammatory activity against inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein expressions in cells. In addition, principal component analysis using the chemical global positioning system (ChemGPS) for natural products (ChemGPS-NP) was employed in order to analyze the structure-activity relationship (SAR), and the results indicated that the ring conformation of the compound has a leading role in suppressing the expressions of pro-inflammatory iNOS and COX-2 proteins in macrophages.
四种新的石蒜烷二萜类化合物，briaviolide K-N（-），已从培养型八放珊瑚中获得。通过光谱方法，鉴定了 briaranes 的结构。本研究采用脂多糖（LPS）诱导的小鼠巨噬细胞 RAW 264.7 细胞系炎症的体外模型，发现这四种石蒜烷中二萜类化合物中，briarane 对诱导型一氧化氮合酶（iNOS）和环氧合酶-2（COX-2）蛋白在细胞中的表达具有抗炎活性。此外，还采用基于天然产物的化学全球定位系统（ChemGPS-NP）的主成分分析（PCA）来分析构效关系（SAR），结果表明化合物的环构象在抑制巨噬细胞中促炎 iNOS 和 COX-2 蛋白的表达方面起着主导作用。
