College of Pharmacy, Chungnam National University, Daejeon, 34134, Republic of Korea.
College of Pharmacy, Woosuk University, Wanju-gun, Jeonbuk, 55338, Republic of Korea.
Arch Pharm Res. 2017 Sep;40(9):1064-1070. doi: 10.1007/s12272-017-0942-x. Epub 2017 Aug 5.
Edible insects have been reported to produce metabolites showing various pharmacological activities, recently emerging as rich sources of health functional food. In particular, the larvae of Protaetia brevitarsis seulensis (Kolbe) have been used as traditional Korean medicines for treating diverse diseases, such as breast cancer, inflammatory disease, hepatic cancer, liver cirrhosis, and hepatitis. However, only few chemical investigations were reported on the insect larvae. Therefore, the aim of this study was to discover and identify biologically active chemical components of the larvae of P. brevitarsis seulensis. As a result, a quinoxaline-derived alkaloid (1) was isolated, which was not reported previously from natural sources. In addition, other related compounds (2, 4-10, 15, 16) were also encountered for the first time from the larvae. The structures of all the isolated compounds were established mainly by analysis of HRESIMS, NMR, and electronic circular dichroism data. Compound 5 exhibited inhibition of tyrosinase with IC value of 44.8 µM.
食用昆虫已被报道能产生具有各种药理活性的代谢物，最近它们作为健康功能性食品的丰富来源而受到关注。特别是 Protaetia brevitarsis seulensis (Kolbe) 的幼虫已被用作传统的韩国药物，用于治疗各种疾病，如乳腺癌、炎症性疾病、肝癌、肝硬化和肝炎。然而，关于这种昆虫幼虫的化学研究报道很少。因此，本研究的目的是发现和鉴定 P. brevitarsis seulensis 幼虫中具有生物活性的化学物质。结果分离得到一种来自天然产物的新型喹喔啉衍生生物碱（1）。此外，还首次从幼虫中分离得到了其他相关化合物（2、4-10、15、16）。所有分离得到的化合物的结构主要通过高分辨质谱、NMR 和电子圆二色谱数据分析确定。化合物 5 对酪氨酸酶的抑制活性的 IC 值为 44.8 μM。
