Title: Texto
1In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes with
b-cyclodextrin is not inhibited by high-density
lipoproteins Elisabet Fernández-García, Irene
Carvajal-Lérida, Francisco Rincón, José J. Ríos
and Antonio Pérez-Gálvez
aperez_at_cica.es Food Biotechnology
Department Instituto de la Grasa (CSIC) Av. Padre
García Tejero 4, 41012 Sevilla (SPAIN)
2In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- SIGNIFICANCE OF BIOAVAILABILITY STUDIES
- Interest in the screening of bioavailability has
increased for different reasons - Existence of undernourished population
- Epidemiological studies have associated between
consumption of fruit and vegetables to a lower
risk of developing degenerative diseases - Development of food products with added
nutritional value - Food legislation concerning functional foods
3In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- A MULTIFACTORIAL SYSTEM EFFECTS CAROTENOID
ASSIMILATION - Carotenoids are fat soluble compounds
- Liberation from food matrix
- Incorporation to mixed micelles
- Absorption by epithelial cells through
simple/facilitated diffusion mechanisms - Absorption efficiency is relatively low from
fruits and vegetables - Fiber, kind and amount of fat, interaction among
carotenoids - Increase of absorption efficiency from processed
fruits and vegetables (homogenization and thermal
processing)
4In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- INTER-INDIVIDUAL VARIABILITY AND THE
- NON-RESPONDER CONCEPT
- Comparison of the in vivo lutein absorption
efficiency non-responder versus
lutein-responders group
Responders group
non-Responders group
5In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- AIM OF THE STUDY
- Estimation of the bioaccessibility of dietary
carotenoids reached when they are delivered as
inclusion complexes - Dietary carotenoids (b-carotene, lutein and
lycopene) were formulated as micellar solutions
(control) or inclusion complexes with
b-cyclodextrin - BBMVs preparations were used as the in vitro
model to assay carotenoid uptake from both
carotenoid formulations (micellar solution or
carotenoid-CyDIC) at three concentration levels - Comparison of absorption efficiency under
inhibition conditions of membrane protein
transporters (BBMVs pre-incubated with HDLs)
6In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotenoid absorption
efficiency in function of the concentration and
delivering method
Assimilation of b-carotene
- Saturation versus linear trend
- Increase of efficiency at 2.5 mM
7In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotenoid absorption
efficiency in function of the concentration and
delivering method
Assimilation of lycopene
- Saturation versus linear trend
- Increase of efficiency at 1.0 mM
8In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotenoid absorption
efficiency in function of the concentration and
delivering method
Assimilation of lutein
- Saturation versus linear trend
- Increase of efficiency at 2.5 mM
- A lower absorption efficiency
- was observed versus carotenes
9In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Primary effects of the factors concentration,
donor solution type and inhibition
10In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- SUMMARY
- Factors concentration and donor solution type
- Association between concentration and
assimilation mechanism - Structural features (polarity) or different
affinity of transporters may explain the
absorption efficiency data of carotenes and
lutein - Significant increase on efficiency of the
assimilation is reached when carotenoids were
delivered as inclusion complex with CyD
11In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Does delivery of carotenoids as inclusion complex
mean an increase on absorption efficiency? - Absorption rate in pmol/(mg protein x min)
12In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- SUMMARY
- Factors concentration and donor solution type
- At the lowest concentration the carotenoids from
micellar solutions were more efficiently
assimilated - At 1.0 mM a heterogeneous behavior was observed
- Only at the highest concentration, carotenoids
from inclusion complex solutions were more
efficiently assimilated in comparison with the
carotenoid micellar solutions at that
concentration (b-Car 51 Lut 185 Lyc 128).
What absorption mechanism does apply for
inclusion complexes?
13In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Two-stage mechanism for carotenoid assimilation
from inclusion complex solutions release and
absorption
Lysate of BBMVs after assimilation procedure with
lutein inclusion complex at the donor solution
Lutein inclusion complex at the donor solution
14In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Solubility of carotenoids is a rate-limiting step
of absorption. - Dissolution kinetics of the complex is enhanced
at high concentrations and depends on binding
constant of the host-guest complex
K complexation
De-complexation
Assimilation Passive or facilitated diffusion
15In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotenoid absorption
efficiency in function of the concentration and
delivering method with inhibitor
Assimilation of b-carotene
- Decrease of 50 (mean value)
- Saturation versus linear trend
- Increase of efficiency at 0.5 mM
16In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotenoid absorption
efficiency in function of the concentration and
delivering method with inhibitor
Assimilation of lycopene
- Decrease of 40 (mean value)
- Saturation versus linear trend
- Increase of efficiency at 0.5 mM
17In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotenoid absorption
efficiency in function of the concentration and
delivering method with inhibitor
Assimilation of lutein
- Decrease of 70 (mean value)
- Saturation versus linear trend
- Increase of efficiency at 0.5 mM
18In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Primary effects of the factors concentration,
donor solution type and inhibition
19In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- SUMMARY
- Factors concentration, donor solution type and
inhibition - Assimilation of carotenoids from micellar
solutions is significantly inhibited with the use
of HDLs - Significant decrease of the assimilation level,
(70 drop for lutein), although it did not
reached 100. Co-existence of simple diffusion
mechanism and work of transporters not totally
blocked under the established experimental
conditions - Carotenes were more efficiently absorbed than
lutein even under inhibition conditions. They
probably take help of different protein
transporters
20In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- SUMMARY
- Factors concentration, donor solution type and
inhibition - Carotenoid-CyDIC were more efficiently absorbed
than the carotenoid micellar solutions under
inhibition conditions. How did the factor
inhibition affect the carotenoid assimilation
from CyDIC?
21In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotene-CyDIC absorption
efficiency in function of the inhibition factor
Assimilation of b-carotene-CyDIC
- Increase of efficiency from 0.5 mM
- under inhibited transport conditions
- Increase of 86 at 1.0 mM
22In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotene-CyDIC absorption
efficiency in function of the inhibition factor
Assimilation of lycopene-CyDIC
- Increase of efficiency from 0.5 mM
- under inhibited transport conditions
- Increase of 165 at 1.0 mM
23In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotene-CyDIC absorption
efficiency in function of the inhibition factor
24In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the carotene-CyDIC absorption
efficiency in function of the inhibition factor
25In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- RESULTS
- Comparison of the lutein absorption efficiency in
function of the inhibition factor
Assimilation of lutein at 1.0 mM
- 70 drop of micellar lutein
- under inhibited transport conditions
- 28 drop of lutein-CyDIC under
- inhibited transport conditions
26In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- SUMMARY
- Comparison of the carotenoid-CyDIC absorption
efficiency in function of the inhibition factor - A different effect of HDLs was observed for the
assimilation efficiency of carotene-CyDICs or
lutein-CyDICs - Process of competition between HDLs and
lutein-CyDIC may not be efficient enough in
comparison with the same process for
carotene-CyDIC - Inhibition promoted by HDLs affects specific
protein transporters
27In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- SUMMARY
- Comparison of the in vivo lutein absorption
efficiency non-responder versus
lutein-responders group
non-Responders group
Lutein-responders group
28In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- CONCLUSIONS
- Factors concentration, donor solution type and
inhibition - First, inter-individual differences on carotenoid
assimilation efficiency should be evaluated, as
they are a direct consequence of facilitated
diffusion mechanism and expression/location of
transporters. Interaction with drugs - New strategies to increase carotenoid
assimilation to develop food formulae.
Interaction with lipoprotein/apoprotein components
29In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- CONCLUSIONS
- Factors concentration, donor solution type and
inhibition - Data point to the existence of different affinity
of transporters and even different transporters
for carotenes and the xanthophyll lutein.
Non-/low-responder effect - Bringing pharmaceutical concepts to food
technology and nutrition will help to consolidate
functional food
30In vitro intestinal absorption of carotenoids
delivered as molecular inclusion complexes
- ACKNOWLEGMENTS
- Financial support from Spanish Government
(projects AGL2007-61146 AGR-03025) - Scientific and organizing committees of the 6th
International Congress on Pigments in Food -
Budapest
Dr. Antonio Pérez-Gálvez aperez_at_cica.es
Food Biotechnology Department Instituto de la
Grasa (CSIC) Av. Padre García Tejero 4, 41012
Sevilla (SPAIN)
THANKS FOR YOUR ATTENTION!