• The Korean Journal of Physiology and Pharmacology
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• v.17 no.1
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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.

• Journal of Convergence for Information Technology
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• v.10 no.10
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• pp.109-114
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• 2020

The aim of the study was to observe the influence and related mechanism of rebamipide on the intestinal contraction. Intestinal contraction includes the activation of thick or thin filament regulation. However, there are few reports addressing the question whether this regulation is involved in rebamipide-induced regulation. We hypothesized that rebamipide plays a role in intestinal contraction evoked by carbachol in rat intestine. Interestingly, rebamipide alone didn't inhibit and rather slightly increased the contraction in the denuded muscle. Therefore, rebamipide alone and together with indomethacin increases the ileal contraction suggesting that additional pathways might be involved in the regulation of ileal contractility. In conclusion, rebamipide has some effect on the regulation of contractility and anti-ulcer by NSAIDs.

• Biotechnology and Bioprocess Engineering:BBE
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• v.10 no.6
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• pp.516-521
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• 2005

Drug delivery to the lymphatic system may be important in terms of the treatment with lymphatic involvement, such as tumor metastases and immunization. Especially, drug transport via the intestinal lymphatics after oral administration has been attracted lots of interests. The purpose of this study was to prepare cyclosporin A (CSA)-loaded liposomes, with different characteristics, and evaluate their mucoadhesivity. Three liposome preparations were formulated: cationic stearylamine liposomes (SA-Lip), anionic phosphatidylserine liposomes (PS-Lip), Polymer (chitosan)-coated liposomes (CS-Lip), and characterized. The liposome preparations were found to be spherical in shape, with PS-Lip being the smallest. The liposome preparations exhibited entrapment efficiencies in the order: PS-Lip $(52.5{\pm}2.9%)$ > SA-Lip $(48.8{\pm}3.3%)$ > CS-Lip $(41.7{\pm}4.2%)$. Finally, mucoadhesive tests were carried out using rat intestine, with SA-Lip (67%) showing the best adhesive rate of the three preparations (PS-Lip: 56%, CS-Lip: 61%). These results suggest that a positive charge on the surface of drug carriers may be an important factor for the intestinal drug delivery.

• Parasites, Hosts and Diseases
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• v.37 no.2
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• pp.101-107
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• 1999

Rats were immunized through an initial infection with 1,000 filariform larvae (L3) of Nippostrongylus brasiliensis and after complete expulsion of worms they were challenged with 1,000 L3 of Strongyloides venezuelensis to investigate whether cross-resistance developed against a heterologous parasite. Nippostrongylus brasiliensis immunized rats developed a partial cross-resistance against S.venezuelensis migrating larvae (MSL3) in the lungs and adult worms in the small intestine. The population of MSL3 in the lungs were significantly lower (p<0.05) in immunized rats($22.0{\;}{\pm}{\;}7.4$) compared with controls ($105.0{\;}{\pm}{\;}27.6$). The populations of adult worms, egg output and fecundity were initially decreased but from day 14 post-challenge they did not show any significant difference between immunized and control rats. However, the length of worm in immunized rat was revealed as retardation. Peripheral blood eosinophilia was significantly decreased (P<0.05) on day 7 post-challenge and then gradually increased which peaked on da 42 post-challenge when most of the worms were expelled. these results suggest that peripheral blood eosinophilia is strongly involved in the worm establishment and expulsion mechanisms.

• Journal of fish pathology
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• v.22 no.3
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• pp.343-352
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• 2009

Natural-killer-cell-enhancing factor (NKEF) belongs to the newly defined peroxiredoxin (Prx) family. It was originally isolated from human erythroid cells. The black rockfish NKEF cDNA was identified through the expressed sequence tag (EST) analysis of PBLs libraries. The full-length NKEF cDNA was 1433 bp long and contained an open reading frame (ORF) of 594 bp that encoded 198 amino-acid residues. The 5' UTR had a length of 39 bp, and the 3’UTR 800 bp. The deduced amino-acid sequence of the black rockfish had a density 93.4, 92.9, 87.8, 85.8, 84.8, 83.8, 80.3, 79.7, 77.2, and 75.2% that of the pufferfish, olive flounder, channel catfish, zebrafish, chicken, common carp, Myotis lucifugus, cattle, human PrxI, rat PrxI, human NKEF-A, and Xenopus tropicalis, respectively. The NKEF gene was expressed in all the tissues of the black rockfish. The RT-PCR indicated that the NKEF transcripts were predominantly in the spleen and gill, less dominantly in the PBLs, head kidney, trunk kidney, and liver, and least in the intestine and muscles. This is the first report on the existence of the NKEF-A gene in black rockfish.

• Journal of Pharmaceutical Investigation
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• v.39 no.4
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• pp.243-248
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• 2009

The purpose of this study was to investigate the effects of morin, an antioxidant, on the bioavailability of doxorubicin (DOX) in rats. Thus, DOX was administered intravenously (10 mg/kg) or orally (50 mg/kg) with or without oral morin (0.5, 3 and 10 mg/kg). In the presence of morin, the total area under the plasma concentration-time curve (AUC) of DOX was significantly greater than that of the control. In the presence of 3 and 10 mg/kg of morin, the peak concentration $C_{MAX}$) was significantly higher than that of the control. Consequently, the absolute bioavailability (AB) of DOX in the presence of morin was 3.7-8.3%, which was significantly enhanced compared with those of the control group (2.7%). The relative bioavailability (RB) of DOX was 1.36 to 3.02 times higher than those of the control group. Compared to the intravenous control, the presence of morin increased the AUC of DOX, but was not significantly affected. The enhanced bioavailability of oral DOX by oral morin may be due to the inhibition of both P-glycoprotein (P-gp) and cytochrome P450 (CYP) 3A in the intestine and/or liver by morin. This result may suggest that the development of oral DOX combination with morin is feasible, which is more convenient than the i.v. dosage forms. The present study raised the awareness about the potential drug interactions by concomitant use of DOX with morin.

• Food Science and Biotechnology
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• v.18 no.1
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• pp.239-244
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• 2009

In the current study, inhibitory activity of 8 selected Korean edible plants of Lamiaceae family against $\alpha$-glucosidases, prepared from rat small intestine acetone powder was evaluated. Total flavonoids and oxygen radical absorbance capacity (ORAC) were also investigated. Methyl alcohol extracts of Scutellaria indica (SI) had the highest $\alpha$-glucosidase inhibitory activity relevant for potentially managing hyperglycemia, followed by Clinopodium gracile (CG) and Thymus quinquecostatus (TQ). These 3 species also showed significant antioxidant activity in ORAC system. The $\alpha$-glucosidase inhibitory activity of the extracts was compared to selected phenolics. Among the standard phenolics tested quercetin which was major flavonoid in the extracts had the highest $\alpha$-glucosidase inhibitory activity. CG, TQ, and SI which had high quercetin content and ORAC values also exhibited significant sucrase inhibitory activity. Results suggested that selected 3 Korean Lamiaceae species have the potential development of effective dietary strategy for postprandial hyperglycemia and oxidative stress-linked diabetes complications.

• YAKHAK HOEJI
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• v.25 no.1
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• pp.27-35
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• 1981

Etomidoline is a new synthetic atropine-like drug. The present investigation aimed to study the combined effects of etomidoline and neofopam hydrochloride which has an analgesic and muscle relaxant activity, compared with the effects of each drugs. Acute toxicities (ID$_{50}$) in mouse were 132mg/Kg (p.o.) and 49mg/Kg (i.p.) when combination ratio of etomidoline and neofopam was 1:5 and 103 mg/Kg (p.o.) and 30mg/Kg (i.p.) with the ratio of 1:10. Etomidoline showed more potent anticholinergic effects than neofopam in the isolated rat intestine. Whereas, antibarium effects were twice as active with neofopam than with etomidoline. When etomidoline and neofopam were added in combination ratio of 1 : 5, papaverine-like avtivity was increased, but no changes of anticholinergic effect were observed. Analgesic effect was measured by the anti-writhing method of Whittle in mice. Both of the concurrent and single administration of etomidoline and nefopam reduced significantly the writhing number and the effect of the concurrent administration was more active than that of single, and 1 : 5 combination was slightly more potent than 1:10. Each drug or the combined drug was administered to mice and observed the change of the pupil size. Pupil sizes were increased with each drug and with combined drug, although there were no significant differences between the each group of drugs. However, those effects were less than that of atropine sulfate.e.

• Journal of Yeungnam Medical Science
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• v.15 no.1
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• pp.75-96
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• 1998

The local arrangement of sensory nerve cell bodies and nerve fibers in the brain stem, spinal ganglia and nodose ganglia were observed following injection of cholera toxin B subunit(CTB) and wheat germ agglutinin-horseradish peroxidase(WGA-HRP) into the rat intestine. The tracers were injected in the stomach(anterior and posterior portion), duodenum, jejunum, ileum, cecum, ascending colon or descending colon. After survival times of 48-96 hours, the rats were perfused and their brain, spinal and nodose ganglia were frozen sectioned ($40{\mu}m$). These sectiones were stained by CTB immunohistochemical and HRP histochemical staining methods and observed by dark and light microscopy. The results were as follows: 1. WGA-HRP labeled afferent terminal fields in the brain stem were seen in the stomach and cecum, and CTB labeled afferent terminal fields in the brain stem were seen in all parts of the intestine. 2. Afferent terminal fields innervating the intestine were heavily labeled bilaterally gelalinous part of nucleus of tractus solitarius(gelNTS), dorsomedial part of gelNTS, commissural part of NTS(comNTS), medial part of NTS(medNTS), wall of the fourth ventricle, ventral border of area postrema and comNTS in midline dorsal to the central canal. 3. WGA-HRP labeled sensory neurons were observed bilaterally within the spinal ganglia, and labeled sensory neurons innervating the stomach were observed in spinal ganglia $T_2-L_1$ and the most numerous in spinal ganglia $T_{8-9}$. 4. Labeled sensory neurons innervating the duodenum were observed in spinal ganglia $T_6-L_2$ and labeled cell number were fewer than the other parts of the intestines. 5. Labeled sensory neurons innervating the jejunum were observed in spinal ganglia $T_6-L_2$ and the most numerous area in the spinal ganglia were $T_{12}$ in left and $T_{13}$ in right. 6. Labeled sensory neurons innervating the ileum were observed in spinal ganglia $T_6-L_2$ and the most numerous area in the spinal ganglia were $T_{11}$ in left and $L_1$ in right. 7. Labeled sensory neurons innervating the cecum were observed in spinal ganglia $T_7-L_2$ and the most numerous area in the spinal ganglia were $T_{11}$ in left and $T_{11-12}$ in right. 8. Labeled sensory neurons innervating the ascending colon were observed in spinal ganglia $T_7-L_2$ in left, and $T_9-L_4$ in right. The most numerous area in the spinal ganglia were $T_9$ in left and $T_{11}$ in right. 9. Labeled sensory neurons innervating the descending colon were observed in spinal ganglia $T_9-L_2$ in left, and $T_6-L_2$ in right. The most numerous area in the spinal ganglia were $T_{13}$ in left and $L_1$ in right. 10. WGA-HRP labeled sensory neurons were observed bilaterally within the nodose ganglia, and the most numerous labeled sensory neurons innervating the abdominal organs were observed in the stomach. 11. The number of labeled sensory neurons within the nodose ganglia innervating small and large intestines were fewer than that of labeled sensory neurons innervating stomach These results indicated that area of sensory neurons innervated all parts of intestines were bilaterally gelatinous part of nucleus tractus solitarius(gelNTS), dorsomedial part of gelNTS, commissural part of NTS (comNTS), medial part of NTS, wall of the fourth ventricle, ventral border of area postrema and com NTS in midline dorsal to the central canal within brain stem, spinal ganglia $T_2-L_4$ and nodose ganglia. Labeled sensory neurons innervating the intestines except the stomach were observed in spinal ganglia $T_6-L_4$. The most labeled sensory neurons from the small intestine to large intestine came from middle thoracic spinal ganglia to upper lumbar spinal ganglia.

• Journal of the Korean Society of Food Science and Nutrition
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• v.34 no.1
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• pp.21-26
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• 2005

Although the sesame lignans, sesamol, have been shown to possess antioxidative activity, less is known about the metabolism and antioxidative properties of sesamol, a major constituent of sesame oil. To determine the ability of sesamol to act as an antioxidant in vivo, we fed rats a diet containing 0.5% sesamol for 3 wk and studied its metabolism and its effects on oxidative stress. Body weight gain and weight of liver, kidneys were significantly higher in the rats fed sesamol than in rats fed the control diets. GST and GST-Px activities in rat liver microsomes were higher in rats fed sesamol and CAT activities were found to be significantly increased in rats fed sesamol. The formation of TBARS was decreased in the liver of rat fed the 0.5% sesamol diet than in controls. We detected sesamol metabolites in liver and kidneys of rats fed sesamol and its metabolites were present as conjugated glucuronides and sulfates. In contrast, not detected sesamol peak in other organs such as colon, small intestine and pancreas.