Increased bioavailability of hesperetin-7-glucoside compared with hesperidin results in more efficient prevention of bone loss in adult ovariectomised rats.
Hesperidin (Hp), a citrus flavonoid predominantly found in oranges, shows bone-sparing effects in ovariectomised (OVX) animals. In human subjects, the bioavailability of Hp can be improved by the removal of the rhamnose group to yield hesperetin-7-glucoside (H-7-glc). The aim of the present work was to test whether H-7-glc was more bioavailable and therefore more effective than Hp in the prevention of bone loss in the OVX rat. Adult 6-month-old female Wistar rats were sham operated or OVX, then pair fed for 90 d a casein-based diet supplemented or not with freeze-dried orange juice enriched with Hp or H-7-glc at two dose equivalents of the hesperetin aglycone (0.25 and 0.5 %). In the rats fed 0.5 %, a reduction in OVX-induced bone loss was observed regarding total bone mineral density (BMD):+7.0 % in OVX rats treated with Hp (HpOVX) and +6.6 % in OVX rats treated with H-7-glc (H-7-glcOVX) v. OVX controls (P < 0.05). In the rats fed 0.25 % hesperetin equivalents, the H-7-glcOVX group showed a 6.6 % improvement in total femoral BMD v. the OVX controls (P < 0.05), whereas the Hp diet had no effect at this dose. The BMD of rats fed 0.25 % H-7-glc was equal to that of those given 0.5 % Hp, but was not further increased at 0.5 % H-7-glc. Plasma hesperetin levels and relative urinary excretion were significantly enhanced in the H-7-glc v. Hp groups, and the metabolite profile showed the absence of eriodictyol metabolites and increased levels of hesperetin sulphates. Taken together, improved bioavailability of H-7-glc may explain the more efficient bone protection of this compound.
Habauzit
Véronique
V
UMR, ASM, INRA, Clermont-Ferrand/Theix, St-Genès Champanelle, France.
Nielsen
Inge-Lise
IL
Gil-Izquierdo
Angel
A
Trzeciakiewicz
Anna
A
Morand
Christine
C
Chee
Winnie
W
Barron
Denis
D
Lebecque
Patrice
P
Davicco
Marie-Jeanne
MJ
Williamson
Gary
G
Offord
Elizabeth
E
Coxam
Véronique
V
Horcajada
Marie-Noëlle
MN
D000818:Animals; D001682:Biological Availability; D015519:Bone Density / Q000187:drug effects; D016723:Bone Remodeling / Q000187:drug effects; D019587:Dietary Supplements; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005260:Female; D005269:Femur / Q000473:pathology / Q000503:physiopathology; D006569:Hesperidin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D009929:Organ Size / Q000187:drug effects; D010024:Osteoporosis / Q000517:prevention & control*; D010052:Ovariectomy; D051381:Rats; D017208:Rats, Wistar; D014599:Uterus / Q000473:pathology; D015430:Weight Gain / Q000187:drug effects
C545247:hesperetin-7-glucoside; D006569:Hesperidin