Ngan Nguyen Thi Thanh, Quang Tran Hong, Kim Kwan-Woo, Kim Hye Jin, Sohn Jae Hak, Kang Dae Gill, Lee Ho Sub, Kim Youn-Chul, Oh Hyuncheol
College of Pharmacy, Wonkwang University, Iksan, 54538, Republic of Korea.
Institute of Genome Research, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi, Vietnam.
Arch Pharm Res. 2017 Mar;40(3):328-337. doi: 10.1007/s12272-017-0890-5. Epub 2017 Jan 10.
After the chemical investigation of the ethyl acetate extract of the marine-derived fungal strain Penicillium sp. SF-5629, the isolation and structural elucidation of eight secondary metabolites, including (3R,4S)-6,8-dihydroxy-3,4,7-trimethylisocoumarin (1), (3S,4S)-sclerotinin A (2), penicitrinone A (3), citrinin H1 (4), emodin (5), ω-hydroxyemodin (6), 8-hydroxy-6-methyl-9-oxo-9H-xanthene-1-carboxylate (7), and 3,8-dihydroxy-6-methyl-9-oxo-9H-xanthene-1-carboxylate (8) were carried out. Evaluation of the anti-inflammatory activity of these metabolites showed that 4 inhibited nitric oxide and prostaglandin E2 production in lipopolysaccharide-stimulated BV2 microglia, with IC values of 8.1 ± 1.9 and 8.0 ± 2.8 μM, respectively. The inhibitory function of 4 was confirmed based on decreases in inducible nitric oxide synthesis and cyclooxygenase-2 gene expression. In addition, 4 was found to suppress the phosphorylation of inhibitor kappa B-α, interrupt the nuclear translocation of nuclear factor kappa B, and decrease the activation of p38 mitogen-activated protein kinase.
对海洋来源的真菌菌株青霉属SF-5629的乙酸乙酯提取物进行化学研究后，开展了8种次生代谢产物的分离和结构解析，这些次生代谢产物包括(3R,4S)-6,8-二羟基-3,4,7-三甲基异香豆素(1)、(3S,4S)-菌核盘菌素A(2)、青霉环酮A(3)、桔霉素H1(4)、大黄素(5)、ω-羟基大黄素(6)、8-羟基-6-甲基-9-氧代-9H-呫吨-1-羧酸酯(7)和3,8-二羟基-6-甲基-9-氧代-9H-呫吨-1-羧酸酯(8)。对这些代谢产物的抗炎活性评估表明，化合物4在脂多糖刺激的BV2小胶质细胞中抑制一氧化氮和前列腺素E2的产生，其IC值分别为8.1±1.9和8.0±2.8μM。基于诱导型一氧化氮合成和环氧化酶-2基因表达的降低，证实了化合物4的抑制作用。此外，发现化合物4可抑制抑制性κB-α的磷酸化，阻断核因子κB的核转位，并降低p38丝裂原活化蛋白激酶的激活。
