Browse > Article

Intestinal absorption of aloin, aloe-emodin, and aloesin; A comparative study using two in vitro absorption models  

Park, Mi-Young (Department of Food and Nutrition, Sookmyung Women's University)
Kwon, Hoon-Jeong (Department of Food and Nutrition, Seoul National University)
Sung, Mi-Kyung (Department of Food and Nutrition, Sookmyung Women's University)
Publication Information
Nutrition Research and Practice / v.3, no.1, 2009 , pp. 9-14 More about this Journal
Abstract
Aloe products are one of the top selling health-functional foods in Korea, however the adequate level of intake to achieve desirable effects are not well understood. The objective of this study was to determine the intestinal uptake and metabolism of physiologically active aloe components using in vitro intestinal absorption model. The Caco-2 cell monolayer and the everted gut sac were incubated with $5-50{\mu}M$ of aloin, aloe-emodin, and aloesin. The basolateral appearance of test compounds and their glucuronosyl or sulfated forms were quantified using HPLC. The % absorption of aloin, aloe-emodin, and aloesin was ranged from 5.51% to 6.60%, 6.60% to 11.32%, and 7.61% to 13.64%, respectively. Up to 18.15%, 18.18%, and 38.86% of aloin, aloe-emodin, and aloesin, respectively, was absorbed as glucuronidated or sulfated form. These results suggest that a significant amount is transformed during absorption. The absorption rate of test compounds except aloesin was similar in two models; more aloesin was absorbed in the everted gut sac than in the Caco-2 monolayer. These results provide information to establish adequate intake level of aloe supplements to maintain effective plasma level.
Keywords
Aloin; aloe-emodin; aloesin; intestinal absorption;
Citations & Related Records
Times Cited By KSCI : 1  (Citation Analysis)
Times Cited By Web Of Science : 7  (Related Records In Web of Science)
연도 인용수 순위
1 McCarthy TJ & Haynes LJ (1967). The distribution of alosein in some south African aloe species. Planta Med 15:342-344   DOI   ScienceOn
2 Muni IA, Leeling JL, Helms RJ & Johnson N (1978). Antiallergic chromones. I. Disposition of 5-(3-p-cyanophenoxy-2-hydroxy-1-propoxy)-2-(1H-tetrazol-5-yl) chromone in four mammalian species. Toxicol Appl Pharmacol 43:527-534   DOI   ScienceOn
3 Ollila F, Halling K, Vuorela P, Vuorela H & Slotte JP (2002). Characterization of flavonoid--biomembrane interactions. Arch Biochem Biophys 399:103-108   DOI   ScienceOn
4 Teng ZH, Zhou SY, Ran YH, Liu XY, Yang RT, Yang X, Yuan CJ & Mei QB (2007). Cellular absorption of anthraquinones emodin and chrysophanol in human intestinal Caco-2 cells. Biosci Biotechnol Biochem 71:1636-1643   DOI   ScienceOn
5 Alves DS, Perez-Fons L, Estepa A & Micol V (2004). Membranerelated effects underlying the biological activity of the anthraquinones emodin and barbaloin. Biochem Pharmacol 68:549-561   DOI   ScienceOn
6 Hadjeri M, Barbier M, Ronot X, Mariotte AM, Boumendjel A & Boutonnat J (2003). Modulation of P-glycoprotein-mediated multidrug resistance by flavonoid derivatives and analogues. J Med Chem 46: 2125-2131   DOI   ScienceOn
7 Hidalgo IJ, Raub TJ & Borchardt RT (1989). Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 96:736-749   DOI
8 Kanai Y, Nakai Y, Nakajima N & Tanayama S (1979). Metabolic disposition of 6-ethyl-3-(1H-tetrazol-5-yl)-chromone, a new antiallergic agent, in the rat, guinea-pig, rabbit, dog and monkey. Xenobiotica 9:33-50   DOI   ScienceOn
9 Keller RP & Neville MC (1986). Determination of total protein in human milk: comparison of methods. Clin Chem 32:120-123
10 Miao H & Yang Z (2000). Regiospecific carbonylative annulation of iodophenol acetates and acetylenes to construct the flavones by a new catalyst of palladium-thiourea-dppp complex. Org Lett 2:1765-1768   DOI   ScienceOn
11 Mailleau C, Capeau J & Brahimi-Horn MC (1998). Interrelationship between the Na+/glucose cotransporter and CFTR in Caco-2 cells: relevance to cystic fibrosis. J Cell Physiol 176:472-481   DOI   ScienceOn
12 Lambert N, Kroon PA, Faulds CB, Plumb GW, McLauchlan WR, Day AJ & Williamson G (1999). Purification of cytosolic beta-glucosidase from pig liver and its reactivity towards flavonoid glycosides. Biochim Biophys Acta 1435:110-116   DOI   ScienceOn
13 Maenthaisong R, Chaiyakunapruk N, Niruntraporn S & Kongkaew C (2007). The efficacy of aloe vera used for burn wound healing: a systematic review. Burns 33:713-718   DOI   ScienceOn
14 Saccu D, Bogoni P & Procida G (2001). Aloe exudate: characterization by reversed phase HPLC and headspace GC-MS. J Agric Food Chem 49:4526-4530   DOI   ScienceOn
15 Tammela P, Laitinen L, Galkin A, Wennberg T, Heczko R, Vuorela H, Slotte JP & Vuorela P (2004). Permeability characteristics and membrane affinity of flavonoids and alkyl gallates in Caco-2 cells and in phospholipid vesicles. Arch Biochem Biophys 425:193-199   DOI   ScienceOn
16 Barthe L, Woodley J & Houin G (1999). Gastrointestinal absorption of drugs: methods and studies. Fundam Clin Pharmacol 13:154-168   DOI   ScienceOn
17 Maurizis JC, Nicolas C, Verny M, Ollier M, Faurie M, Payard M & Veyre A (1991). Biodistribution and metabolism in rats and mice of bucromarone. Drug Metab Dispos 19:94-99
18 Davis RH, Donato JJ, Hartman GM & Haas RC (1994). Antiinflammatory and wound healing activity of a growth substance in Aloe vera. J Am Podiatr Med Assoc 84:77-81   DOI
19 Esmat AY, Tomasetto C & Rio MC (2006). Cytotoxicity of a natural anthraquinone (Aloin) against human breast cancer cell lines with and without ErbB-2: topoisomerase IIalpha coamplification. Cancer Biol Ther 5:97-103   DOI   ScienceOn
20 Moore Z & Cowman S (2008). A systematic review of wound cleansing for pressure ulcers. J Clin Nurs 17:1963-1972   DOI   ScienceOn
21 Park YG, Park MY, Sung MK & Kwon H (2005). Study on the intake pattern of health intended foods depending on inclusion of proclaimed health functional food materials. Journal of the Korean Society of Food Science and Nutrition 34:374-379   DOI   ScienceOn
22 Paine MF & Fisher MB (2000). Immunochemical identification of UGT isoforms in human small bowel and in caco-2 cell monolayers. Biochem Biophys Res Commun 14:1053-1057   DOI   ScienceOn
23 Azuma K, Ippoushi K, Ito H, Higashio H & Terao J (2002). Combination of lipids and emulsifiers enhances the absorption of orally administered quercetin in rats. J Agric Food Chem 50:1706-1712   DOI   ScienceOn
24 Ishii Y, Tanizawa H & Takino Y (1994). Studies of aloe. V. Mechanism of cathartic effect. Biol Pharm Bull 17:651-653   DOI   ScienceOn
25 Speranza G, Morelli CF, Tubaro A, Altinier G, Durì L & Manitto P (2005). Aloeresin I, an anti-inflammatory 5-methylchromone from cape aloe. Planta Med 71:79-81   DOI   ScienceOn
26 Nemeth K, Plumb GW, Berrin JG, Juge N, Jacob R, Naim HY, Williamson G, Swallow DM & Kroon PA (2003). Deglycosylation by small intestinal epithelial cell beta-glucosidases is a critical step in the absorption and metabolism of dietary flavonoid glycosides in humans. Eur J Nutr 42:29-42   DOI   ScienceOn
27 Korkina L, Suprun M, Petrova A, Mikhal'chik E, Luci A & De Luca C (2003). The protective and healing effects of a natural antioxidant formulation based on ubiquinol and aloe vera against dextran sulfate-induced ulcerative colitis in rats. J Am Podiatr Med Assoc 84:77-81   DOI
28 Ni Y, Turner D, Yates K & Tizard I (2007). Stabilization of growth factors relevant to wound healing by a plant cell wall biomaterial. Planta Med 73:1260-1266   DOI   ScienceOn
29 Walgren RA, Lin JT, Kinne RK & Walle T (2000). Cellular uptake of dietary flavonoid quercetin 4'-beta-glucoside by sodium-dependent glucose transporter SGLT1. J Pharmacol Exp Ther 294:837-843
30 Chandan BK, Saxena AK, Shukla S, Sharma N, Gupta DK, Suri KA, Suri J, Bhadauria M & Singh B (2007). Hepatoprotective potential of Aloe barbadensis Mill. against carbon tetrachloride induced hepatotoxicity. J Ethnopharmacol 111:560-566   DOI   ScienceOn
31 Vereczkey L, Jemnitz K, Monostory K, Veres Z & Kóbori L (2005). The role of drug metabolizing enzymes in the effect and side-effect of the drugs. Orv Hetil 146:947-952
32 Wilkinson AP, Gee JM, Dupont MS, Needs PW, Mellon FA, Williamson G & Johnson IT (2003). Hydrolysis by lactase phlorizin hydrolase is the first step in the uptake of daidzein glucosides by rat small intestine in vitro. Xenobiotica 33:255-264   DOI   ScienceOn
33 Gee JM, DuPont MS, Rhodes MJ & Johnson IT (1998). Quercetin glucosides interact with the intestinal glucose transport pathway. Free Radic Biol Med 25:19-25   DOI   ScienceOn
34 Vaidyanathan JB & Walle T (2002). Glucuronidation and sulfation of the tea flavonoid (-)-epicatechin by the human and rat enzymes. Drug Metab Dispos 30:897-903   DOI   ScienceOn
35 Liu X, Tam VH & Hu M (2007). Disposition of flavonoids via enteric recycling: determination of the UDP-glucuronosyltransferase isoforms responsible for the metabolism of flavonoids in intact Caco-2 TC7 cells using siRNA. Mol Pharm 4:873-882   DOI   ScienceOn
36 Olthof MR, Hollman PC, Vree TB & Katan MB (2000). Bioavailabilities of quercetin-3-glucoside and quercetin-4'-glucoside do not differ in humans. J Nutr 130:1200-1203   DOI