Table 4.
Impact of proanthocyanidins on enzymes and transporters involved in the digestion and absorption of lipids.
| Type of PACs | Type of interaction | Model | Effect | Reference |
|---|---|---|---|---|
| Water grape seed extract (WGSE, 26.7 mg PACs/g) and ethanol grape seed extract (EGSE, 32.6 mg PACs/g) of red grape seeds | Inhibition of pancreatic lipase (PL) in vitro | Extract concentration: 400, 800, 1,300, and 1,800 ppm Substrate: olive oil emulsion |
Inhibition of lipase: 52.66% EGSE; 45.44% WGSE (at 1,800 ppm) (enzyme preincubated with extract) 61.41% EGSE; 42.63% WGSE (at 1,800 ppm) (substrate preincubated with extract) |
(106) |
| Apple polyphenol extract (AP) and the procyanidins (PCs) contained in the extract | Inhibition of PL in vitro | Substrate: 4MUO | Inhibition of lipase [IC50 (μg/ml)]: PCs (1.4 µg/ml) > AP (5.6 µg/ml) > other polyphenol fraction (115.9 µg/ml) | (135) |
| Triglyceride (TG) absorption in mice | 1,000 mg/kg of AP compared with control (water) and 10 ml/kg body weight of corn oil | AP completely prevent the increase of plasma TG level | ||
| TG absorption in humans | 600 mg of AP and 40 g of TG | Inhibition of TG elevation at 6 h after ingestion | ||
| Cocoa (PCs) (>85% purity) [degree of polymerization (DP) between 2 and 10] | Inhibition of PL and secreted phospholipase A2 (PLA2) in vitro | PL: PCs: 0–20µM and 4-NPB as substrate. Orlistat as control PLA2: PCs: 0–100μM and Red/Green BODIPY PC-A2, 1.67µM as substrate |
PCs with DP ≥ 5 inhibited PL by 37 to 53% at 20µM. Orlistat 72% at 10µM PCs with DP between 2 and 5 inhibited PLA2 by 46–74% at 100µM PCs with DP between 6 and 10 inhibited PLA2 by approximately 90% at 50µM (IC50 < 5µM) |
(136) |
| Tannins from persimmon | Capacity to bind primary and secondary bile acids in vitro and in vivo | Tannins concentration: 1% (w/v). Bile acids concentration: 1 mM solutions. Cholestyramine positive control | Tannins adsorbed approximately 80% of all bile acids (cholic, taurocholic, glycocholic, and deoxycholic acid), similar to a cholestyramine | (138) |
| Mice supplemented for 14 days with a tannins diet [1% (w/w)] Cholestyramine as positive control | Tannin supplementation: twofold more excretion of bile acids in feces compared with a control (without supplementation) | |||
| Grape seed extract (GSE, 49.8% PCs) | Inhibition of PL | GSE 4.75–0.62 mg/ml. Orlistat as positive control | Inhibitory activity: GSE (IC50 44.5 mg/ml); Orlistat (IC50 3.7 mg/ml) | (139) |
| Inhibition of pancreatic cholesterol (CS) esterase | GSE 50–3.12 µg/ml. Simasvatin as positive control | Inhibitory activity: GSE (IC50 27.27 µg/ml); Simasvatin (IC50 0.08 µg/ml) | ||
| Effect on CS micellization | GSE at 10, 20, and 40 mg/ml on artificially micelles. Gallic acid as positive control | Inhibition of CS solubility: gallic acid (27.26%) > GSE 40 mg/ml (11.87%) > GSE 20 mg/ml (6.84%) > GSE 10 mg/ml (3.18%) | ||
| Capacity to bind bile acid | GSE 1 mg/ml. Bile acid 2 mM. Cholestyramine as positive control | % Bile acid binding: glycodeoxycholic (70%) > taurocholic (25%), both similar to cholestyramine. Taurodeoxycholic acid was slightly bound | ||
| Serum TG and CS concentrations | Oral administration of 5 ml/kg body weight of olive oil emulsion (3.33 ml of olive oil, 44.3 mg of cholic acid, 0.48 g of CS, and 1.67 ml of distilled water) GSE: 100, 250, and 500 mg/kg |
↓ in serum TG concentrations (2–6 h after administration) at 250 and 500 mg/kg GSE [area under the curve (AUC) 19 and 27% lower than control group, respectively] Suppression of the increase in serum CS concentration (after 4 h of loading fat emulsion) at 250 and 500 mg/kg (AUC 8 and 11% lower than in control group, respectively) |
||
| Aqueous CE (4.1% type-A polymers) |
Expression of genes of Niemann–Pick C1-like protein 1 (NPC1L1) and CD36 | Enterocytes treated with 10 or 100 µg/ml of CE for 0, 0.5, 2, and 4 h | ↓ NPC1L1 mRNA at 2 h (10 µg/ml) and at 4 h (100 µg/ml) ↓ CD36 mRNA at 4 h (10 µg/ml) and at 0.5 h (100 µg/ml) |
(140) |
| Grape seed proanthocyanidin extract (GSPE) | Intestinal expression of NPC1L1 and CD36 | Rats fed with lard (2,5 ml/kg of body weight), supplemented or not with GSPE (250 mg/kg of body weight) | Lard induces a decrease in the expression of all genes evaluated. GSPE do not induce changes in the expression of genes | (141) |
| Polyphenol extracts from grape (41% PACs), cranberry (32% PACs), avocado (29% PACs), and apple (22% PACs) | Inhibitory activity on PL in vitro | Lipase: 2 mg/ml. PACs extracts: 0; 0.065; 0.125; 0.25; 0.5; and 1 mg/ml. Substrate: 4-MUO (4-metilumbeliferil oleate) (0.1mM) | Inhibitory activity: Grape > cranberry > avocado > apple |
(137) |
| Plasma TG concentrations in vivo | Subjects: normal weight (NW) and overweight/obese (OW/Ob) Extract: 1 g of extract or placebo High-fat test meal: 63 g fat |
Absorption of TG was 2 times higher in the OW/Ob than in the NW subjects and was unaffected by the treatment | ||