Abstract
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−1 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.
Highlights
Bergamottin, i.e., 5-geranoxypsoralen, is a natural furanocoumarin compound with weak polarity (Figure 1)
Citrus flavedo is a good source of bergamottin
Among different tissues of eight citrus cultivars tested in the present study, the flavedo of YJZXY
Summary
Bergamottin, i.e., 5-geranoxypsoralen, is a natural furanocoumarin compound with weak polarity (Figure 1). Recent studies showed that bergamottin contains various pharmaceutical bioactivities, including anticancer (anti-proliferation, anti-invasion, and anti-migration, etc.) [1,2,3], antimycobacterial activity [4], antimutagenicity [5], and increased drug bioavailability through its interaction with some isoforms of the cytochrome P450 enzyme [6,7,8], etc. Such investigations on bergamottin bioactivities are limited in in vitro cell studies due to the rarity and expensiveness of this compound. Characterization of the distribution of bergamottin in natural resources and establishment of well-defined separation methods for efficient purification of this natural bioactive compound will facilitate its further comprehensive utilization.
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