Liu Yilong, Ren Chuanhong, Cao Yunlin, Wang Yue, Duan Wenyi, Xie Linfeng, Sun Chongde, Li Xian
Zhejiang Provincial Key Laboratory of Horticultural Plant Integrative Biology, Zhejiang University, Zijingang Campus, Hangzhou 310058, China.
Laboratory of Fruit Quality Biology, Zhejiang University, Zijingang Campus, Hangzhou 310058, China.
Molecules. 2017 Jul 20;22(7):1227. doi: 10.3390/molecules22071227.
Bergamottin is a natural furanocoumarin compound with weak polarity. Characterization and quantification of bergamottin were carried out in different fruit tissues of various citrus cultivars. Among the four citrus tissues tested, i.e., flavedo, albedo, segment membrane (SM), and juice sacs (JS) in eight citrus cultivars, the highest bergamottin content was found in the flavedo of Citrus grandis (L.) Osbeck cv. Yongjiazaoxiangyou (YJZXY, 666.54 μg·g DW). A combination of silica gel column chromatography and high-speed counter-current chromatography (HSCCC) was established to efficiently purify bergamottin from the flavedo of YJZXY. Bergamottin showed significant antiproliferative activity on three cancer cell lines, i.e., human liver cancer HepG2, promyelocytic leukemia HL-60, and gastric cancer BGC-823 cells, which showed a marked inhibition effect on these cell lines in a dose-dependent manner. In addition, bergamottin significantly increased glucose consumption in HepG2 cells also in a dose-dependent manner, which is the first report of its potential in anti-diabetes applications.
佛手柑内酯是一种极性较弱的天然呋喃香豆素化合物。对佛手柑内酯在不同柑橘品种的不同果实组织中进行了表征和定量分析。在测试的四种柑橘组织中，即八个柑橘品种的外果皮、内果皮、囊衣（SM）和汁胞（JS），在柚（Citrus grandis (L.) Osbeck）品种永嘉早香柚（YJZXY）的外果皮中发现了最高的佛手柑内酯含量（666.54 μg·g干重）。建立了硅胶柱色谱法和高速逆流色谱法（HSCCC）相结合的方法，从永嘉早香柚的外果皮中高效纯化佛手柑内酯。佛手柑内酯对三种癌细胞系，即人肝癌HepG2、早幼粒细胞白血病HL-60和胃癌BGC-823细胞具有显著的抗增殖活性，对这些细胞系呈剂量依赖性的明显抑制作用。此外，佛手柑内酯还以剂量依赖的方式显著增加HepG2细胞的葡萄糖消耗，这是其在抗糖尿病应用潜力方面的首次报道。
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