This study was undertaken to characterize the pectin from four citrus species and to determine their in vitro inhibitory activities on the binding of fibroblast growth factor (FGF) to the FGF receptor (FGFR). Pectin from various parts of lemon, grapefruit, tangerine, and orange were isolated and characterized. Tangerine had the highest pectin content among the four citrus species. Segment membrane contained as much as or more pectin than flavedo/albedo. Anhydrogalacturonic content was highest in pectin from segment membrane of tangerine and flavedo/albedo of grapefruit. Lemon pectin contained the highest methoxyl content (MC), and grapefruit contained the largest proportion of lower molecular weight (<10000 Da) pectin. Tangerine contained the highest neutral sugar in both flavedo/albedo and segment membrane. The interdependency of heparin on factor-receptor interaction provides a means for identifying new antagonists of growth factor activity and thus for treatment of various diseases. These results showed that pectin significantly inhibited the binding of FGF-1 to FGFR1 in the presence of 0.1 microg/mL heparin. The pectin from the segment membrane of lemon was the most potent inhibitor. The inhibition activity was significantly correlated with sugar content, MC, and size of pectin. Kinetic studies revealed a competitive nature of pectin inhibition with the heparin, a crucial component of the FGF signal transduction process. The observation that the heparin-dependent biological activity of FGF signal transduction is antagonized by citrus pectin should be further investigated for the use of these pectins as anti-growth factor agents for potential health benefits.
Seasonal changes in pectin content and chemical composition were studied in three anatomical layers of`Rio Red' grapefruit (Citrus paradisi Macf), a currently popular cultivar in the Rio Grande Valley in Texas, USA. Fruits were harvested at intervals between August 1998 and May 1999. Pectin content in¯avedo decreased throughout the season, while in albedo and segment membrane the pectin content was lowest in mid-season (November and January). In all three layers the anhydrogalacturonic acid (AGA) content of pectin was highest in mid-season. While the methoxyl content (MC) of pectin increased, the total neutral sugar (TNS) content of pectin decreased in all three layers throughout the season. The in vitro effect of grapefruit pectin on ®broblast growth factor (FGF)± FGF receptor (FGFR) interaction was also investigated. The strong interdependence of heparin on factor±receptor interaction provides means for identifying new antagonists of growth factor activity and thus for treatment of various diseases. Our results showed that grapefruit pectin signi®cantly inhibited the binding of FGF-1 to FGFR1 in the presence of 0.1 mg ml À1 heparin. Pectin of albedo from grapefruits harvested in January was the most potent inhibitor. The in vitro inhibitory activity was signi®cantly correlated with the percentage of rhamnose. Kinetic studies revealed a competitive nature of pectin on FGF signal transduction with heparin. The observation that the biological activity of heparin can be antagonised by citrus pectin suggests that pectins should be investigated further as antigrowth factor agents for potential health bene®ts.
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