• Nutrition Research and Practice
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• 제13권4호
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• pp.295-301
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• 2019

BACKGROUND/OBJECTIVES: Consumption of cholesterol-rich foods, such as eggs, has a minimal effect on circulating cholesterol levels in healthy humans. To gain insight, we investigated whether phospholipids rich in eggs (EPL) interfere with intestinal cholesterol absorption in vivo. MATERIALS/METHODS: To investigate the acute effect of EPL on intestinal cholesterol absorption, male C57BL/6J mice were orally administered with 6, 11, or 19 mg of EPL for three days. We also tested the effect of chronic EPL consumption on cholesterol metabolism in the small intestine and the liver in mice with diet-induced hypercholesterolemia. Male C57BL/6J mice were fed a high fat/high cholesterol (HF/HC; 35% fat, 0.25% cholesterol, w/w) diet for 4 weeks to induce hypercholesterolemia, and subsequently the mice were either fed 0, 0.4 or 0.8% (w/w) of EPL for 6 weeks. RESULTS: Intestinal cholesterol absorption was significantly decreased by the highest dose of acute EPL administration compared to control. Chronic EPL supplementation did not significantly alter intestinal cholesterol absorption nor plasma levels of total cholesterol and low-density lipoprotein cholesterol. In the small intestine and the liver, EPL supplementation minimally altered the expression of genes which regulate cellular cholesterol levels. CONCLUSION: Although chronic EPL consumption was not able to counteract hypercholesterolemia in HF/HC-fed mice, acute EPL administration decreased intestinal cholesterol absorption. This study provides in vivo evidence that acute administration of PLs in eggs prevent cholesterol absorption in the intestine, suggesting a mechanism for a minimal effect of egg consumption on circulating cholesterol levels.

• 운동영양학회지
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• 제24권4호
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• pp.24-27
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• 2020

[Purpose] Dehydroepiandrosterone (DHEA) administration reportedly recovers osteoporosis, a bone disorder associated with bone deficiency in postmenopausal women. However, the physiological mechanism of DHEA in osteoporosis remains elusive, especially in terms of intestinal calcium absorption. Therefore, we investigated the effect of DHEA administration on calcium absorption in ovariectomized (OVX) female rats using an estrogen receptor antagonist. [Methods] Female Sprague-Dawley rats (n=23, 6 weeks old) were randomized into three groups: OVX control group (OC, n=7), OVX with DHEA treatment group (OD, n=8), and OVX with DHEA inhibitor group (ODI, n=8) for 8 weeks. [Results] Intestinal calcium accumulation, as well as the rate of absorption, demonstrated no significant differences during the experimental period among investigated groups. The bone mineral density (BMD) of the tibia at the proximal metaphysis was higher in the OD group than that in the OC group (p<0.05); however, BMD of the ODI group showed no significant difference from investigated groups. Furthermore, the BMD of the tibia at the diaphysis did not significantly differ among these groups. [Conclusion] We revealed that DHEA administration does not involve intestinal Ca absorption, although this treatment improves BMD levels in OVX rats. These observations indicate that the effect of DHEA on the bone in postmenopausal women is solely due to its influence on bone metabolism and not intestinal calcium absorption.

• The Korean Journal of Physiology and Pharmacology
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• 제17권1호
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• pp.9-13
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• 2013

The aim of the present study was to examine the effect of micellar systems on the absorption of beta-lapachone (b-lap) through different intestinal segments using a single-pass rat intestinal perfusion technique. B-lap was solubilized in mixed micelles composed of phosphatidylcholine and sodium deoxycholate, and in sodium lauryl sulfate (SLS)-based conventional micelles. Both mixed micelles and SLS micelles improved the in situ permeability of b-lap in all intestinal segments tested although the mixed micellar formulation was more effective in increasing the intestinal absorption of b-lap. The permeability of b-lap was greatest in the large intestinal segments. Compared with SLS micelles, the effective permeability coefficient values measured with mixed micelles were 5- to 23-fold higher depending on the intestinal segment. Our data suggest that b-lap should be delivered to the large intestine using a mixed micellar system for improved absorption.

• 약학회지
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• 제27권2호
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• pp.163-168
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• 1983

The effect of ginseng butanol fraction (total sponin) on the absorption rate of ethanol in rat intestine was examined. Ginseng butanol fraction showed inhibitory effect on the intestinal absorption of ethanol in situ as well as in vitro test. Ginseng butanol fraction markedly decreased the ethanol blood level, delayed onset time of ethanol effect and shortened sleeping time when it was adminstered orally together with ethanol. These results suggest that ginseng may alter the ethanol blood level by decreasing the intestinal absorption of ethanol.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.119-119
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• 1997

Valacyclovir is a L-valyl ester prodrug of acyclovir which is a highly effective and selective antiviral agent in the treatment of herpes virus diseases. Valacyclovir is rapidly and almost completely converted to acyclovir and increases the oral bioavailability of acyclovir three to five fold. However, the intestinal absorption mechanism of valacyclovir is not clear. If the improved absorption mechanism of valacyclovir is fully understood, it will provide a rationale of designing the amino acid ester prodrugs of polar drugs containing hydroxyl group. The main objective of our present study is to characterize the membrane transport mechanism of valacyclovir. Methods : Intestinal absorption of valacyclovir was investigated by using in-situ rat perfusion study and its wall permeability was estimated by modified boundary layer model. The membrane transport mechanism was also investigated through the uptake study in Caco-2 cells and in CHO-hPepTl cells. Results : In the rat perfusion study, the wall permeability of valacyclovir was ten times higher than acyclovir and showed concentration dependency, Valacyclovir also demonstrated a D,L stereo-selectivity with L-isomer having an approximately five-fold higher permeability than D-isomer. Mixed dipeptides and cephalexin, which are transported by dipeptide carriers, strongly competed with valacyclovir for the intestinal absorption, while L-valine did not show any competition with valacyclovir. This indicated that the intestinal absorption of valacyclovir could be dipeptide carrier-mediated. In addition, the competitive uptake study in Caco-2 cells presented that dipeptides reduced the valacyclovir uptake but valine did not. Also, in IC$\sub$50/ study, valacyclovir showed strong inhibition on the $^3$H-gly-sar uptake in CHO-hPepTl cells over-expressing a human intestinal peptide transporter. Taken together, the result from our present study indicated that valacyclovir utilized the peptide transporter for the intestinal absorption.

• Journal of Pharmaceutical Investigation
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• 제28권1호
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• pp.25-33
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• 1998

Intestinal absorption of ${\beta}-lactam$ antibiotics and angiotensin converting enzyme(ACE) inhibitors has been shown to use the carrier-mediated transport system. In vitro experiments have established that the efficacy of uptake by enterocytes depends on an inwardly directed proton gradient. It was suggested that benazepril was mediated by tripeptide transport system and that amoxicillin was transported by dipeptide transport carrier. The aim of this study is to assess the influence of amoxicillin on the intestinal absorption of benazepril using in vitro diffusion chamber and in situ single pass perfusion technique in the rat in order to elucidate whether the above transport systems are competitive or not. We obtained the gastrointestinal pemeability coefficient of amoxicillin, benazepril and both of them using in vitro diffusion chamber. And also the gastrointestinal absorption clearance of amoxicillin, benazepril and both of them using in situ single-pass perfusion method at steady state were calculated. Amoxicillin and benazepril were analyzed by HPLC. The results by the use of diffusion chamber in vitro indicated that the apparent intestinal permeability coefficient of benazepril was significantly(p<0.01) decreased by amoxicillin(45.2%) and vice versa significantly(p<0.01) decreased(89.1%). The results by the in situ gastrointestinal single-pass perfusion method indicated that the intestinal absorption clearance of benazepril was significantly(p<0.05) decreased by amoxicillin (40.2%) and vice versa significantly(p<0.05) decreased(54.8%). These results might suggest that they share the same peptide carrier pathway for oral absorption.

• Preventive Nutrition and Food Science
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• 제8권1호
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• pp.1-6
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• 2003

Catechins exhibit a hypocholesterolemic effect in cholesterol-fed animals. The present study was conducted to examine whether (+)-catechin influences the absorption of cholesterol in rats. Male Sprague-Dawley rats were fed ad libitum an AIN-93G diet containing soybean oil for 5 wk. Rats with lymph cannulae were infused at 3.0 mL/h for 8 h via a duodenal catheter with a lipid emulsion containing radiolabeled cholesterol with or without (+)-catechin. Lymph was collected hourly for 8 h. The enteral infusion of (+)-catechin significantly lowered the lymphatic absorption of $^{14}$ C-cholesterol (21.1 $\pm$ 3.6% dose/B h) compared with controls infused with the lipid emulsion devoid of (+)-catechin (38.2 $\pm$ 1.2% dose/8 h). The intestinal absorption of $\alpha$-tocopherol (24.2$\pm$3.0% dose/8 h) also was significantly decreased by (+)-catechin infusion, relative to controls (32.2$\pm$2.2% dose/8 h). However, the lymphatic outputs of oleic acid and phospholipid were not affected by enteral (+)-catechin infusion. The results indicate that (+)-catechin has a profound inhibitory effect on the intestinal absorption of cholesterol and $\alpha$-tocopherol without affecting the absorption of fat.

• Nutrition Research and Practice
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• 제3권1호
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• pp.9-14
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• 2009

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.

• 한국식품영양과학회:학술대회논문집
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• 한국식품영양과학회 2004년도 Annual Meeting and International Symposium
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• pp.47-52
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• 2004

This study was conducted to determine the effects of egg phospholipids [(Phosphatidylcholine (PC) and sphingomyelin (SM)] on intestinal absorption of cholesterol and other lipids. Each rat with Iymph cannula was infused via a duodenal catheter at 3.0 mL/h for 8 h with a lipid emulsion containing triolein, cholesterol and PC in 24 mL PBS. The PC in the lipid emulsion was egg PC (EPC), hydrogenated egg PC (HPC), or soy PC (SPC). The EPC in the lipid emulsion markedly lowered the Iymphatic absorption of cholesterol, compared with SPC and a lipid emulsion containing no PC. The HPC further lowered the absorption of cholesterol. The phospholipid output was not affected by the source of PC infused. The total Iymphatic output of oleic acid (18: 1), the major fatty acid infused in the form of triolein, did not differ among the NPC, SPC and EPC groups, but was significantly lower in the HPC group. The findings provide the first evidence that EPC markedly lowers the Iymphatic absorption of cholesterol under in vivo conditions. The inhibitory effect of EPC appears to be due to the higher degree of saturation of its acyl groups relative to SPC, suggesting that the intestinal absorption of egg cholesterol may be reduced by the presence of PC in e99 yolk. Experiment 2 was designed to determine whether egg SM, structurally similar to PC, also inhibits the Iymphatic absorption of cholesterol. Egg SM lowered the Lymphatic absorption of cholesterol in a dose dependent manner. Likewise, SM lowered the Iymphatic absorption of oleic acid, whereas it had no effect on retinol absorption. SM at a high dose lowered the Iymphatic outputs of both PC and SM, whereas there was no such effect at a lower dose. These results also indicate that luminal egg SM has an inhibitory effect on the intestinal absorption of cholesterol and other lipids of relatively high hydrophobicity.

• Food Science and Biotechnology
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• 제16권6호
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• pp.879-883
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• 2007

This study examined whether dietary supplementation with sea tangle alters the intestinal morphology of streptozotocin-induced diabetic rats and affects the glucose absorption rate. Forty male Sprague-Dawley rats were divided into 2 groups and fed either a control (AIN76-based) diet or a sea tangle-supplemented diet. After 3 weeks, 10 rats in each group received an intramuscular injection of streptozotocin (45 mg/kg BW), and feeding was continued for 3 additional weeks. Dietary supplementation with sea tangle resulted in a lower fasting plasma glucose level compared with the control diet in diabetic rats. Scanning electron micrographs revealed serious damage to the jejunal villi of diabetic rats fed the control diet, whereas supplementation with sea tangle alleviated the damage. In a separate experiment, 20 male Sprague-Dawley rats were divided into 2 groups and fed either a control diet or a sea tangle-supplemented diet for 5 weeks, and fasted rats were subjected to in situ single-pass perfusion. The glucose absorption rate determined in the absence of digesta was decreased by 34% in the jejunum of rats fed a sea tangle diet compared with those fed a control diet. In conclusion, sea tangle supplementation lowered glucose absorption rate, altered intestinal morphology, and appeared to protect villi from damage caused by diabetes mellitus.