State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources/Guangdong Key Laboratory for Innovative Development and Utilization of Forest Plant Germplasm, College of Forestry and Landscape Architecture, South China Agricultural University, Guangzhou 510642, China.
Guangdong Provincial Key Laboratory of Silviculture, Protection and Utilization, Guangdong Academy of Forestry, Guangzhou 510520, China.
Molecules. 2022 May 22;27(10):3334. doi: 10.3390/molecules27103334.
Three new polycyclic phenol derivatives, 2-acetyl-4-hydroxy-6H-furo [2,3-g]chromen-6-one (), 2-(1',2'-dihydroxypropan-2'-yl)-4-hydroxy-6H-furo [2,3-g][1]benzopyran-6-one () and 3,8,10-trihydroxy-4,9-dimethoxy-6H-benzo[c]chromen-6-one (), along with seven known ones (-, and ) were isolated for the first time from the leaves of . Their structures were determined by spectroscopic analysis and comparison with literature-reported data. These compounds were tested for their in vitro antibacterial activity against four Gram-(+) bacteria: (), methicillin-resistant (), (), (), and the Gram-(-) bacterium . Compounds , , and showed antibacterial activity toward , and with MIC values ranging from 7.8 to 62.5 µg/mL, but they were inactive to . Compound not only showed the best antibacterial activity against , and , but it further displayed significant antibacterial activity against (MIC 1.95 µg/mL) even stronger than vancomycin (MIC 3.9 µg/mL). No compounds showed inhibitory activity toward . Further bioassay indicated that compounds , , , , and showed in vitro -glucosidase inhibitory activity, among which compound displayed the best -glucosidase inhibitory activity with IC value (0.026 mM) about 15-fold stronger than the reference compound acarbose (IC 0.408 mM). These results suggested that compounds , and were potentially highly valuable compounds worthy of consideration to be further developed as an effective anti- agent or effective -glucosidase inhibitors, respectively. In addition, the obtained data also supported that was rich in structurally diverse bioactive compounds worthy of further investigation, at least in searching for potential antibiotics and -glucosidase inhibitors.
从 叶片中首次分离得到三个新的多环酚衍生物：2-乙酰基-4-羟基-6H-呋喃并[2,3-g]色烯-6-酮（）、2-（1'，2'-二羟基丙-2'-基）-4-羟基-6H-呋喃并[2,3-g][1]苯并吡喃-6-酮（）和 3,8,10-三羟基-4,9-二甲氧基-6H-苯并[c]色烯-6-酮（），以及另外七个已知化合物（-，-，-，-，-，-和-）。通过光谱分析和与文献报道的数据比较确定了它们的结构。这些化合物的体外抗菌活性测试结果表明，它们对四种革兰氏阳性（+）细菌：（）、耐甲氧西林（）、（）、（）和革兰氏阴性（-）细菌 具有抗菌活性。化合物 、 、 和 对 、 和 表现出抗菌活性，MIC 值范围为 7.8 至 62.5 µg/mL，但对 无活性。化合物 不仅对 、 和 表现出最好的抗菌活性，而且对 （MIC 1.95 µg/mL）的抗菌活性甚至比万古霉素（MIC 3.9 µg/mL）更强。没有化合物对 表现出抑制活性。进一步的生物测定表明，化合物 、 、 、 、和 对 -葡萄糖苷酶具有体外抑制活性，其中化合物 对 -葡萄糖苷酶的抑制活性最强，IC 值（0.026 mM）约为参考化合物阿卡波糖（IC 0.408 mM）的 15 倍。这些结果表明，化合物 、 和 可能是具有潜在价值的化合物，值得进一步开发为有效的抗 药物或有效的 -葡萄糖苷酶抑制剂。此外，获得的数据还表明， 富含结构多样的生物活性化合物，值得进一步研究，至少在寻找潜在的抗生素和 -葡萄糖苷酶抑制剂方面是如此。
