Jo Yang Hee, Kim Seon Beom, Liu Qing, Do Seon-Gil, Hwang Bang Yeon, Lee Mi Kyeong
College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk, Republic of Korea.
Wellness R&D Center, Univera, Inc., Seoul, Republic of Korea.
PLoS One. 2017 Mar 2;12(3):e0172069. doi: 10.1371/journal.pone.0172069. eCollection 2017.
The composition and content of the active constituents and their biological activity vary according to diverse factors including their maturation stages. A previous study showed that the fruits of Cudrania tricuspidata inhibited pancreatic lipase activity, a key enzyme in fat absorption. In this study, we investigated the chemical composition and pancreatic lipase inhibitory activity of unripe and ripe fruits of C. tricuspidata. Unripe fruits of C. tricuspidata have a higher content of total phenolic and flavonoids and exhibited stronger pancreatic lipase inhibition compared to ripe fruits. HPLC analysis revealed the different chemical compositions of the unripe and ripe fruits. Further fractionation resulted in the isolation of 30 compounds including two new isoflavonoids. Analysis of the chemical constituents of the unripe and ripe fruits revealed that a 2,2-dimethylpyran ring, a cyclized prenyl, was the predominant side chain in the unripe fruits, whereas it was a linear prenyl group in the ripe fruits. In addition, a new isoflavonoid (19) from the unripe fruits showed the most potent inhibition on pancreatic lipase. Taken together, the maturation stage is an important factor for maximum efficacy and that unripe fruits of C. tricuspidata are a good source of new bioactive constituents for the regulation of obesity.
活性成分的组成、含量及其生物活性会因包括成熟阶段在内的多种因素而有所不同。先前的一项研究表明，柘树果实能抑制胰脂肪酶活性，胰脂肪酶是脂肪吸收中的一种关键酶。在本研究中，我们调查了柘树未成熟果实和成熟果实的化学成分及胰脂肪酶抑制活性。与成熟果实相比，柘树未成熟果实的总酚和黄酮含量更高，且对胰脂肪酶的抑制作用更强。高效液相色谱分析揭示了未成熟果实和成熟果实不同的化学成分。进一步分离得到了30种化合物，包括两种新的异黄酮。对未成熟果实和成熟果实化学成分的分析表明，2,2 - 二甲基吡喃环（一种环化的异戊烯基）是未成熟果实中的主要侧链，而在成熟果实中则是线性异戊烯基。此外，从未成熟果实中得到的一种新异黄酮（19）对胰脂肪酶表现出最强的抑制作用。综上所述，成熟阶段是实现最大功效的一个重要因素，柘树未成熟果实是用于调节肥胖的新型生物活性成分的良好来源。
