• Title/Summary/Keyword: intestinal phase

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Fabrication of Compound K-loaded Polymeric Micelle System and its Characterization in vitro and Oral Absorption Enhancement in vivo

  • Hong, Sun-Mi;Jeon, Sang-Ok;Seo, Jo-Eun;Chun, Kyeung-Hwa;Oh, Dong-Ho;Choi, Young Wook;Lee, Do Ik;Jeong, Seong Hoon;Kang, Jae Seon;Lee, Sangkil
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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    • pp.3188-3194
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    • 2014
  • Compound K (CK) was formulated as polymeric micelles (PM) using Pluronic$^{(R)}$ F-127 to enhance the oral absorption of CK, an intestinal bacterial metabolite of ginseng protopanaxadiol saponin. The physicochemical properties of Ck-loaded PM were characterized and an in vitro transport study using the Caco-2 cell system as well as an in vivo pharmacokinetic study using SD rats was carried out. The hydrodynamic mean particle size of CK-loaded PM (CK-PM) was $254{\pm}23.45nm$ after rehydration and the drug loading efficiency was ca. 99.9%. The FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy data supported the presence of a new solid phase in the PM. The $P_{app}$ value of in vitro Caco-2 cell permeation of CK-PM and the oral absorption of CK was enhanced about 1.2-fold and 2.6-fold compared to CK suspension, respectively, showing that the present PM formulation enabled an enhancement of oral CK absorption.

In vivo anti-metastatic action of Ginseng Saponins is based on their intestinal bacterial metabolites after oral administration

  • Saiki, Ikuo
    • Journal of Ginseng Research
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    • v.31 no.1
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    • pp.1-13
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    • 2007
  • We found that the main bacterial metabolite M1 is an active component of orally administered protopanxadiol-type ginsenosides, and that the anti-metastatic effect by oral administration of ginsenosides may be primarily mediated through the inhibition of tumor invasion, migration and growth of tumor cells by their metabolite M1. Pharmacokinetic study after oral administration of ginsenoside Rb1 revealed that M1 was detected in serum for 24 h by HPLC analysis but Rb1 was not detected. M1, with anti-metastatic property, inhibited the proliferation of murine and human tumor cells in a time- and concentration-dependent manner in vitro, and also induced apoptotic cell death (the ladder fragmentation of the extracted DNA). The induction of apoptosis by M1 involved the up-regulation of the cyclin-dependent kinase(CDK) inhibitor $p27^{Kip1}$ as well as the down-regulation of a proto-oncogene product c-Myc and cyclin D1 in a time-dependent manner. Thus, M1 might cause the cell-cycle arrest (G1 phase arrest) in honor cells through the up/down-regulation of these cell-growth related molecules, and consequently induce apoptosis. The nucleosomal distribution of fluorescence-labeled M1 suggests that the modification of these molecules is induced by transcriptional regulation. Tumor-induced angiogenesis (neovascularization) is one of the most important events concerning tumor growth and metastasis. Neovascularization toward and into tumor is a crucial step for the delivery of nutrition and oxygen to tumors, and also functions as the metastatic pathway to distant organs. M1 inhibited the tube-like formation of hepatic sinusoidal endothelial (HSE) cells induced by the conditioned medium of colon 26-L5 cells in a concentration-dependent manner. However, M1 at the concentrations used in this study did not affect the growth of HSE cells in vitro.

Purification of Oxytocin-related Peptide, Isotocin from the Brain of Conger Eel Conger myriaster (붕장어(Conger myriaster)의 뇌로부터 Oxytocin-related Peptide, Isotocin의 정제)

  • GO Hye-Jin;KIM Chan-Hee;KIM Eun Jung;KIM In Hae;AN Sang Hyun;SOHN Hee-Young;PARK Jin-IL;PARK HEE Yun;YOON Ho Dong;PARK Nam Gyu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.38 no.5
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    • pp.286-290
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    • 2005
  • Oxytocin (OT)-related peptide, isotocin was purified from the brain extract of conger eel (Conger myriaster) using reverse-phase, ion-exchange and size exclusion high performance liquid chromatography (HPLC). The sequence of the peptide, with a molecular weight of 967.30 Da, was determined as Cys-Tyr-Ile-Ser-Asn­Cys-Pro-Ile-Gly-$NH_2$, where the Cys between 1st and 6th residues made an intramolecular disulfide bridge by the automated amino acid sequence analysis and MALDI-TOF mass spectrometry. The sequence was confirmed by identical elution with the purified and synthetic peptide using the HPLC system. As a result of homology investigation, the primary structure of this peptide was the same as that of OT -superfamily member, isotocin. The synthetic peptide showed a contractile activity at a minimal effective concentration of $10^{-7}M$ on the intestinal smooth muscle of goldfish (Carassius auratus).

Bioconversion of Piceid to Piceid Glucoside Using Amylosucrase from Alteromonas macleodii Deep Ecotype

  • Park, Hyunsu;Kim, Jieun;Park, Ji-Hae;Baek, Nam-In;Park, Cheon-Seok;Lee, Hee-Seob;Cha, Jaeho
    • Journal of Microbiology and Biotechnology
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    • v.22 no.12
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    • pp.1698-1704
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    • 2012
  • Resveratrol, or its glycoside form piceid, is a dietary antioxidant polyphenolic compound, found in grapes and red wine that has been shown to have protective effects against cardiovascular disease. However, very low water solubility of the compound may limit its application in the food and pharmaceutical industries. The amylosucrase (AMAS) of Alteromonas macleodii Deep ecotype was expressed in Escherichia coli and showed high glycosyltransferase activity to produce the glucosyl piceid when piceid was used as an acceptor. The conversion yield of piceid glucoside was 35.2%. Biotransformation using culture of the E. coli harboring the amas gene increased the yield up to 70.8%. The transfer product was purified by reverse phase chromatography and recycling preparative HPLC, and the molecular structure of the piceid glucoside was determined using NMR spectroscopy. The piceid glucoside was identified as glucosyl-${\alpha}$-($1{\rightarrow}4$)-piceid. The solubility of glucosyl piceid was 5.26 and 1.14 times higher than those of resveratrol and piceid, respectively. It is anticipated that dietary intake of this compound is more effective by enhancing the bioavailability of resveratrol in the human body because of its hydrophilic properties in the intestinal fluid.

Effect of vitamin C on azoxymethane (AOM)/dextran sulfate sodium (DSS)-induced colitis-associated early colon cancer in mice

  • Jeon, Hee-Jin;Yeom, Yiseul;Kim, Yoo-Sun;Kim, Eunju;Shin, Jae-Ho;Seok, Pu Reum;Woo, Moon Jea;Kim, Yuri
    • Nutrition Research and Practice
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    • v.12 no.2
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    • pp.101-109
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    • 2018
  • BACKGROUD/OBJECTIVES: The objective of this study was to investigate the effects of vitamin C on inflammation, tumor development, and dysbiosis of intestinal microbiota in an azoxymethane (AOM)/dextran sulfate sodium (DSS)-induced inflammation-associated early colon cancer mouse model. MATERIALS/METHODS: Male BALB/c mice were injected intraperitoneally with AOM [10 mg/kg body weight (b.w)] and given two 7-d cycles of 2% DSS drinking water with a 14 d inter-cycle interval. Vitamin C (60 mg/kg b.w. and 120 mg/kg b.w.) was supplemented by gavage for 5 weeks starting 2 d after the AOM injection. RESULTS: The vitamin C treatment suppressed inflammatory morbidity, as reflected by disease activity index (DAI) in recovery phase and inhibited shortening of the colon, and reduced histological damage. In addition, vitamin C supplementation suppressed mRNA levels of pro-inflammatory mediators and cytokines, including cyclooxygenase-2, microsomal prostaglandin E synthase-2, tumor necrosis $factor-{\alpha}$, Interleukin $(IL)-1{\beta}$, and IL-6, and reduced expression of the proliferation marker, proliferating cell nuclear antigen, compared to observations of AOM/DSS animals. Although the microbial composition did not differ significantly between the groups, administration of vitamin C improved the level of inflammation-related Lactococcus and JQ084893 to control levels. CONCLUSION: Vitamin C treatment provided moderate suppression of inflammation, proliferation, and certain inflammation-related dysbiosis in a murine model of colitis associated-early colon cancer. These findings support that vitamin C supplementation can benefit colonic health. Long-term clinical studies with various doses of vitamin C are warranted.

Purification of Vasopressin-related Peptide, [Arg8]-vasotocin, from the Brain of Conger Eel (Conger myriaster) (붕장어 (Conger myriaster)의 뇌로부터 Vasopressin-related Peptide, [Arg8]-vasotocin의 정제)

  • Go Hye-Jin;KIM Chan-Hee;KIM Eun Jung;KIM In Hye;PARK Hee Yeon;YOON Ho Dong;HONG Yong-Ki;PARK Nam Gyu
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.38 no.1
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    • pp.6-11
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    • 2005
  • Vasopressin (VP)-related peptide was purified from the brain extract of conger eel (Conger myriaster) by reverse-phase, ion-exchange high performance liquid chromatography (HPLC). This peptide with a molecular weight of 1,051.2 Da was determined as $H-Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Arg-Gly-NH_2$, whose Cys residues made an intramolecular disulfide bridge by the automated amino acid sequence analysis, MALDI- TOF mass spectrometry. It's sequence was confirmed by identity of the elution position with the synthetic peptide in HPLC system. As a result of homology investigation, the primary structure of this peptide was the same as that of VP-superfamily member, $[Arg^8]-vasotocin$. The synthetic peptide showed a contractile activity at a minimal effective concentration of $10^{-10}\;M$ on the intestinal smooth muscle of goldfish.

Initial assessment of hemorrhagic shock by trauma computed tomography measurement of the inferior vena cava in blunt trauma patients

  • Lee, Gun Ho;Choi, Jeong Woo
    • Journal of Trauma and Injury
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    • v.35 no.3
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    • pp.181-188
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    • 2022
  • Purpose: Inferior vena cava (IVC) collapse is related to hypovolemia. Sonography has been used to measure the IVC diameter, but there is variation depending on the skill of the operator and it is difficult to obtain accurate measurements in patients who have a large amount of intestinal gas or are obese. As a modality to obtain accurate measurements, we measured the diameters of the IVC and aorta on trauma computed tomography scans and investigated the correlation between the IVC to aorta ratio and the shock index in blunt trauma patients. Methods: We retrospectively analyzed the medical records of 588 trauma patients who were transferred to the regional trauma center (level 1) of Wonkang University Hospital from March 2020 to February 2021. We included trauma patients 18 years or older who met the trauma activation criteria and underwent trauma computed tomography scans with intravenous contrast within 40 minutes of admission. The shock index was calculated from vital signs before trauma computed tomography scan, and measurements of the anteroposterior diameter of the IVC (AP), the transverse diameter of the IVC (T), and aorta were made 10 mm above the right renal vein in the venous phase. Results: Overall, 271 patients were included in this study, of whom 150 had a shock index ≤0.7 and 121 had a shock index >0.7. The T to AP ratio and AP to aorta ratio were significantly different between groups. Cutoffs were identified for the T to AP ratio and AP to aorta ratio (2.37 and 0.62, respectively) that produced clinically useful sensitivity and specificity for predicting a shock index >0.7, demonstrating moderate accuracy (T to AP ratio: area under the curve, 0.71; sensitivity, 59%; specificity, 87% and AP to aorta ratio: area under the curve, 0.70; sensitivity, 55%; specificity, 91%). Conclusions: The T to AP ratio and AP to aorta ratio are useful for predicting hemorrhagic shock in trauma patients.

Cerebrovascular Events in Pediatric Inflammatory Bowel Disease: A Review of Published Cases

  • Rohani, Pejman;Taraghikhah, Nazanin;Nasehi, Mohammad Mehdi;Alimadadi, Hosein;Aghdaei, Hamid Assadzadeh
    • Pediatric Gastroenterology, Hepatology & Nutrition
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    • v.25 no.3
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    • pp.180-193
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    • 2022
  • Pediatric inflammatory bowel disease (PIBD) is a multisystem disorder characterized by intestinal and extraintestinal manifestations and complications. Cerebrovascular events (CVE) are rare extraintestinal complications in patients with PIBD. Statistics show that 3.3% patients with PIBD and 1.3-6.4% adult patients with inflammatory bowel disease (IBD) experience CVE during the course of the disease. Therefore, this study aimed to review the records of children with IBD who developed CVE during the course of the disease. We retrospectively reviewed 62 cases of PIBD complicated by CVE. The mean patient age at the time of thrombotic events was 12.48±4.13 years. The incidence of ulcerative colitis was significantly higher than that of Crohn's disease (43 [70.5%] vs. 13 [21.3%] patients). Most patients (87.93%) were in the active phase of IBD at the time of CVE. The mean time interval between the onset of IBD and CVE was 20.84 weeks. Overall, 11 (26.83%) patients showed neurological symptoms of CVE at disease onset. The most frequent symptom on admission was persistent and severe headaches (67.85%). The most common site of cerebral venous thrombosis was the transverse sinuses (n=23, 53.48%). The right middle cerebral artery (n=3, 33.34%) was the predominant site of cerebral arterial infarction. Overall, 41 (69.49%) patients who were mostly administered unfractionated heparin or low-molecular-weight heparin (56.09%) recovered completely. Patients with IBD are at a risk of thromboembolism. CVE may be the most common type of thromboembolism. Based on these findings, the most common risk factor for CVE is IBD flares. In patients with CVE, anticoagulant therapy with heparin, followed by warfarin, is necessary.

Effects of Supplementation of Multienzymes in Diets Containing Different Energy Levels on Growth Performance, Nutrient Digestibility, Blood Metabolites, Microbiota and Intestinal Morphology of Broilers (에너지 수준이 다른 사료에 복합효소제의 첨가가 육계의 사양성적, 영양소 소화율, 혈액성상, 장내미생물 균총 및 소장 융모에 미치는 영향)

  • Shim, Young Ho;Kim, Jin Soo;Hosseindoust, Abdolreza;Ingale, Santosh Laxman;Choi, Yo Han;Kim, Min Ju;Ohh, Seung Min;Ham, Hyung Bin;Chae, Byung Jo
    • ANNALS OF ANIMAL RESOURCE SCIENCES
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    • v.28 no.3
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    • pp.97-107
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    • 2017
  • The present study was conducted to investigate the effects on growth performance, nutrient digestibility, and gut health of broiler chickens when a dietary supplementation of multienzymes was added to diets, containing different energy levels. A total of 480 broiler chickens of similar body weight (Ross 308, 1-day-old) were randomly subjected to four treatments. The dietary treatments included a corn-soybean meal-based diet supplemented with: multienzyme (amylase+protease+ mannanase+xylanase+phytase), 0.05% enzyme, and different energy levels (3010 and 3060 kcal/kg). The experimental diets were fed to the chicks in a mash form for 35 days in two phases (1-21 d, phase I; and 22-35 d, phase II). During the overall period, chicks fed with diets supplemented with multienzymes had a better weight gain (p<0.05) and feed conversion ratio (FCR) than those fed with diets without enzymes. There was no difference in the growth rate and FCR among the chicks fed with diets supplemented with enzymes, even though the dietary energy levels were different. The apparent fecal and ileal digestibility of dry matter, gross, crude protein, calcium, and phosphorus were significantly enhanced (p<0.05). The population of cecal and ileal Lactobacillus spp. was significantly increased (p<0.05), and Clostridium spp. and coliforms were significantly decreased (p<0.05) in diets supplemented with enzymes. Villus height and villus height to crypt depth ratio in the small intestine was also significantly enhanced (p<0.05) in diets supplemented with enzymes. In conclusion, multienzyme supplementation had positive effects on the weight gain of broilers, FCR, digestibility of nutrients, and on the growth of intestinal microbiota.

Bactericidal Effect of Bacteriocin of Lactobacillus plantarum K11 Isolated from Dongchimi on Escherichia coli O157

  • Lim, Sung-Mee;Im, Dong-Soon
    • Journal of Food Hygiene and Safety
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    • v.22 no.3
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    • pp.151-158
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    • 2007
  • Among 68 strains of lactic acid bacteria (LAB) isolated from Dongchimi, a strain K11 was selected due to its bactericidal activity against Escherichia coli O157 The strain K11 was identified as Lactobacillus plantarum, based on physiological and biochemical characteristics. In the late exponential phase, La. plantarum K11 showed maximum bacteriocin activity (12,800 BU/mL) and maintained until the early stationary phase. The bacteriocin activity was completely inactivated by all the proteolytic enzymes such as pepsin, protease, proteinase K, papain, chymotrypsin, and trypsin, but the activity was not affected by catalase, a-amylase, lysozyme, and lipase, suggesting proteinaceous nature of the bacteriocin. Additionally, this activity was not affected in the pH range from 3.0 to 9.0 and under storage conditions like 30 days at -20,4, or $25^{\circ}C$. Although the bacteriocin activity was absolutely lost after 15 min treatment at 121, it was relatively stable at $70^{\circ}C$ for 60 min or $100^{\circ}C$ for 30 min. The activity was disappeared by treatment with acetone, benzene, ethanol, or methanol, but it was not affected by treatment with chloroform or hexane. The antibacterial activity of the bacteriocin was good against some LAB including Lactobacillus spp., Enterococcus spp., and Streptococcus spp., but not against food-borne pathogens such as Bacillus spp., Listeria spp., and Staphylococcus spp. as well as yeasts and molds. Especially, some intestinal bacteria such as Enterobacter aerogenes and E. coli were significantly affected by the bacteriocin of La, plantarum K11. Furthermore, the addition of 640 BU/mL resulted in the complete clearance of E. coli O157 after 10 hr.