Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Nghiado, Caugiay, Hanoi, Viet Nam; College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
Bioorg Med Chem Lett. 2014 Jan 1;24(1):228-32. doi: 10.1016/j.bmcl.2013.11.033. Epub 2013 Nov 22.
Four new cembranoid diterpenes lobocrasols A-D (1-4), were isolated from the methanol extract of the soft coral Lobophytum crassum. Their structures were elucidated by spectroscopic analysis and by comparison of the spectroscopic data with those of similar compounds previously reported in literature. The anti-inflammatory effects of isolated compounds were evaluated using NF-κB luciferase and reverse transcription polymerase chain reaction (RT-PCR). Compounds 1 and 2 significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC50 values of 6.30±0.42 and 6.63±0.11μM, respectively. Furthermore, the transcriptional inhibition of these compounds was confirmed by a decrease in cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) gene expression levels in HepG2 cells.
从软珊瑚 Lobophytum crassum 的甲醇提取物中分离得到了四个新的海松烷二萜 lobocrasols A-D（1-4）。通过光谱分析和与文献中报道的类似化合物的光谱数据比较，阐明了它们的结构。采用 NF-κB 荧光素酶和逆转录聚合酶链反应（RT-PCR）评估了分离化合物的抗炎作用。化合物 1 和 2 以剂量依赖的方式显著抑制 TNFα 诱导的 HepG2 细胞中 NF-κB 的转录活性，IC50 值分别为 6.30±0.42 和 6.63±0.11μM。此外，这些化合物的转录抑制作用通过降低 HepG2 细胞中环氧化酶-2（COX-2）和诱导型一氧化氮合酶（iNOS）基因表达水平得到证实。
