Abstract

Furanocoumarins (FCs) are a group of related plant defense metabolites occurring in several plant families, including some species in the genus citrus, such as grapefruit and pummelo. FCs function as toxins against pathogens, insects and other plant pests and some are toxic to humans at high levels. Although the levels of FCs in grapefruits are non-toxic to humans, they inhibit the intestinal enzyme CYP3A, thus preventing degradation of medicines, such as statins, and causing dangerous overdose effects. This overdosing can cause devastating side effects, ranging from stomach bleeding to kidney problems, muscle aches and irregular heartbeats. In the present study, we utilize LC/MS to characterize the levels of FCs pathway intermediates and end products in twelve citrus cultivars, including mandarin (Citrus reticulata), orange [Citrus sinensis (L.) Osbeck], Pummelo [Citrus maxima (Burm.) Merr.], grapefruit (Citrus paradisi Macf.), and two newly selected grapefruit like varieties [(Citrus reticulate) X [Citrus maxima (Burm.) Merr]. The orange and mandarin varieties do not contain FCs or FCs precursor compounds suggesting that this biosynthetic pathway is absent or inactive in mandarins and oranges and therefore a good genetic source for null alleles to FCs biosynthesis. We report the selection and characterization of two new low FCs and seedless grapefruit-like varieties, “Aliza” and “Coocki”, developed by a cross between pummelo and mandarin. Fruits of these varieties resemble grapefruit and contain high levels of the flavanone naringin, typical of grapefruit, but contain only trace amounts of FCs (based on LCMS analysis). Based on the variability of FCs content and inheritance in citrus species, the results suggest that future development of new low-FCs grapefruit varieties is an achievable objective.

Highlights

  • Furanocoumarins (FCs) are plant defense compounds that function as toxins against pathogens, insects and other plant pests [1] [2]

  • FCs were found at varied concentrations in different cultivars, but were completely absent from mandarins, oranges and were close to absent in the new grapefruit-like varieties “Aliza” and “Cookie” (Figure 2)

  • Bergamottin and 6,7-DHB were found at higher concentrations than other FCs, probably because they are final products that accumulate over time

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Summary

Introduction

Furanocoumarins (FCs) are plant defense compounds that function as toxins against pathogens, insects and other plant pests [1] [2]. Some FCs are carcinogenic and teratogenic, i.e. they can cause cancer and birth defects, respectively [3]-[5]. FCs are found in several plant families, including edible plant species such as the citrus species pummelo and grapefruit, but the levels of mutagenic FCs (such as psoralen) in pummelo and grapefruits are rather low, and there is no risk associated with consumption of their fruit and juice for healthy individuals [3]. In recent years, there has been a decline in grapefruit consumption, especially in the US, as a result of the “grapefruit juice effect”, attributed to FCs: FC-containing grapefruit juice negatively affects the body’s degradation of medicines, including statins, leading to overdose effects

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