1.Metabolism of trans-resveratrol-3-O-glucoside in vitro in rat tissues.
Mao-Jin ZHOU ; Xiao-Yan CHEN ; Da-Fang ZHONG
Acta Pharmaceutica Sinica 2007;42(5):520-524
To study the metabolism of trans-resveratrol-3-O-glucoside (TRG) in vitro in rat tissues, the incubation with cell-free extracts from rat stomach, duodenum, jejunum, ileum and liver was performed, separately. After TRG was incubated with the tissue extracts at 37 degrees C for up to 90 min, the deglycosylation of TRG was (3.50 +/- 0.24) % for stomach, (65.7 +/- 5.94)% for duodenum, (83.5 +/- 6.43)% for jejunum, (77.6 +/- 6.26)% for ileum and (9.62 +/- 1.21)% for liver, separately. It was observed that the small intestine extracts were more active in deglycosylation of TRG than the liver extract, which suggested that the small intestine mucosa played an important role in deglycosylation of TRG. It was assumed that the deglycosylation of TRG was catalyzed by beta-glucosidase in small intestine mucosa.
Animals
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Duodenum
;
metabolism
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Female
;
Glucosides
;
metabolism
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Ileum
;
metabolism
;
Intestinal Mucosa
;
metabolism
;
Intestine, Small
;
metabolism
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Jejunum
;
metabolism
;
Liver
;
metabolism
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Male
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Rats
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Rats, Wistar
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Stilbenes
;
metabolism
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Stomach
;
metabolism
2.Absorption kinetics of dehydrocavidine in rats' stomachs and intestines.
Xiaoye LIU ; Jianfang FENG ; Congbo JIN ; Mancang CHEN
China Journal of Chinese Materia Medica 2009;34(8):1022-1026
OBJECTIVETo study the absorption kinetics of dehydrocavidine in rats' stomachs and intestines.
METHODThe absorption kinetics was investigated by the in situ perfusion in rats and the concentrations of drug perfusion solutions were determined by HPLC.
RESULTThe hourly absorption percentages of dehydrocavidine in stomach, small intestine were 8.88%, 2.08%, respectively. Although the absorption rate constants of dehydrocavidine in duodenum and jejunum are more than that in ileum and colon, there is no significance difference between them. The absorption rate constants kept at the same level when the concentrations of drug perfusion solution are at middle and high level. The increase of the pH of perfusion solution didnt significantly affect the absorption rate constants of the drug.
CONCLUSIONDehydrocavidine was absorbed poorly at stomach and all segments of intestine in rats, but the absorptions in stomach are better than intestine. Dehydrocavidine was absorbed mainly via passive transport mechanism between middle and high concentration levels.
Animals ; Berberine Alkaloids ; pharmacokinetics ; Colon ; metabolism ; Duodenum ; metabolism ; Hydrogen-Ion Concentration ; Ileum ; metabolism ; Intestines ; metabolism ; Jejunum ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley ; Stomach ; metabolism
3.Stereoselectivity in absorption of trans tramadol in rat intestine.
Hui-chen LIU ; Bao-xin LI ; Bin DUN ; Yong-li WANG
Acta Pharmaceutica Sinica 2003;38(12):893-896
AIMTo investigate the stereoselectivity in absorption of trans tramadol (trans T) in rat intestine.
METHODSThe duodenum, jejunum and ileum were separately perfusated in situ with trans T dissolved in Krebs-Ringer buffer. Trans T enantiomers in the perfusate were analyzed with a high performance capillary electrophoresis (HPCE) method.
RESULTSThe absorbed fractions of trans T enantiomers were similar among the different segments of the rat intestine. The absorbed fraction of (+)-trans T was lower than that of (-)-trans T when the concentration of trans T was not higher than 40 mumol.L-1. As the concentration of trans T increased, the absorbed fractions of trans T enantiomers were reduced and the difference in absorbed fractions between trans T enantiomers became not significant.
CONCLUSIONTrans T enantiomers can be absorbed in different parts of the rat intestine. The intestinal absorption of trans T was stereoselective, (-)-trans T being preferentially absorbed.
Analgesics, Opioid ; pharmacokinetics ; Animals ; Duodenum ; metabolism ; Female ; Ileum ; metabolism ; Intestinal Absorption ; Intestine, Small ; metabolism ; Jejunum ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley ; Stereoisomerism ; Tramadol ; pharmacokinetics
4.Comparative study of absorption kinetics in intestines of rats on Xianlinggubao capsule prepared by different technologies.
Huichao WU ; Shouying DU ; Yang LU ; Wen CHEN ; Yong MA ; Pengyue LI
China Journal of Chinese Materia Medica 2011;36(8):992-996
OBJECTIVETo study the characteristics of intestinal absorption of psoralen and isopsoralen of Xianlinggubao capsule, and compare the absorption of Xianlinggubao capsule prepared by different technologies.
METHODNon everted gut sac method was applied to investigate the influence of absorption sites and drug concentration on psoralen and isopsoralen absorption, which were determined by HPLC.
RESULTAlthough the absorption rate constants of psoralen and isopsoralen in duodenum were more than that in jejunum and ileum, there was no significance difference between them. The absorption rate constants of psoralen kept at the same level when the concentrations of drug solution were at middle and low level, while the absorption rate constant at high level was absolutely lower than them (P < 0.05). The results of isopsoralen were the same as psoralen's.
CONCLUSIONIntestinal absorption of psoralen and isopsoralen may be affected by the dissolution. The absorption rate constants of psoralen and isopsoralen in new Xianlinggubao capsules are higher. The absorptions of active components absorption has significant difference in different preparation processes of Xianlinggubao capsule.
Animals ; Capsules ; pharmacokinetics ; Drug Compounding ; Drugs, Chinese Herbal ; pharmacokinetics ; Duodenum ; metabolism ; Ficusin ; pharmacokinetics ; Furocoumarins ; pharmacokinetics ; Ileum ; metabolism ; Intestinal Absorption ; Intestines ; metabolism ; Jejunum ; metabolism ; Rats
5.The pathway of absorption and conveying of puerarin microemulsion-in-oil.
Lei WANG ; Hong-Fei WU ; Chuan-Hua LU ; Yan-Ni FAN
Acta Pharmaceutica Sinica 2009;44(7):798-802
The best absorption location of puerarin microemulsion-in-oil in intestine parva of rat and pharmacokinetic characteristics, and the pathway of absorption and conveying of puerarin microemulsion were studied. In situ rat perfusion method was used to investigate the intestinal absorption of puerarin. Through the changes of drug concentration in blocked and unblocked lymphs, to determine the pathway of absorption and conveying. Puerarin microemulsion-in-oil can be absorbed in any part of intestine, and the K(a), P(app) of every part is ileum > duodenum > jejunum > colon, and the K(a), P(app) of ileum is significantly larger than that of others. The absorption rate of different concentrations is not significantly different (P > 0.05). The puerarin transited by gastrointestinal tract, about 36.8% is absorbed by the lymphatic channels to enter the systemic circulation and 63.2% is absorbed by the non-lymphatic channels. The best part of intestine to absorb puerarin microemulsion is ileum, and it is passive transport. The pathway of conveying is lymphoid and non-lymphoid transit.
Absorption
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Animals
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Colon
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metabolism
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Duodenum
;
metabolism
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Ileum
;
metabolism
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Intestinal Absorption
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Isoflavones
;
administration & dosage
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pharmacokinetics
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Jejunum
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metabolism
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Nanostructures
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Particle Size
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Rats
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Rats, Sprague-Dawley
6.The absorption kinetics of silymarin microemulsion in rat intestine.
Quan YUAN ; Xin-ru LI ; Hui-juan WANG ; Xiao-yan LI ; Yan LIU
Acta Pharmaceutica Sinica 2004;39(8):631-634
AIMTo survey the morphology and size distribution of silymarin microemulsion, to investigate the absorption of silymarin microemulsion in rat intestine compared with the absorption of silymarin micelle in rat Jejunum.
METHODSThe intestine in rats was canulated for in situ recirculation.
RESULTSThe absorption rate constants (Ka) of silymarin microemulsion at the entire intestine, ileum jejunum, duodenum and colon were 6.22 x 10(-2), 2.27 x 10(-2), 1.9 x 10(-2), 1.9 x 10(-2), 1.05 x 10(-2) and 0.43 x 10(-2) h(-1), respectively. The absorption rate constants of two kinds of silymarin micelle at jejunum were 0.36 x 10(-2), 0.65 x 10(-2) h(-1).
CONCLUSIONSilymarin microemulsion was well absorbed at the middle and lower segments of intestine in rats. The absorption was a first-order process with the passive diffusion mechanism.
Animals ; Colon ; metabolism ; Duodenum ; metabolism ; Emulsions ; Ileum ; metabolism ; Intestinal Absorption ; Jejunum ; metabolism ; Male ; Micelles ; Particle Size ; Rats ; Rats, Sprague-Dawley ; Silymarin ; pharmacokinetics
7.Studies on absorption mechanism of loganin in intestines of rats.
Wen-Lan LI ; Zheng-Ting HU ; Yu-Bin JI ; Xiao-Dong WANG ; Dong XU
China Journal of Chinese Materia Medica 2008;33(9):1052-1055
OBJECTIVETo investigate the absorption mechanism of loganin at different intestine segments of rats and the influence of the drug solution concentration, pH, P-gp inductor.
METHODRats were randomly divided into 10 groups, high, middle and low concentration groups (0.1, 0.025, 0.012 5 mg x mL(-1)), duodenum, jejunum and ileum groups (0.013 mg x mL(-1)), high, middle and low pH groups (0.013 mg x mL(-1)), inducer group (0.013 mg x mL(-1)). The intestine cannulation was performed for in situ recirculation. Loganin concentration in the flux was measured by the reversed phase HPLC.
RESULTWhen the concentration was raised from 0.012 5 to 0.1 mg x mL(-1), the uptake of loganin was linearly increased, and no change of Ka is not found. The pH of flux has no effect on drug absorption. The absorbed dose and Ka sequence (from high to low) of loganin at different intestine segments is ileum, duodenum, jejunum. Furthermore, P-gp inductor RFP has effect on the intestinal absorption.
CONCLUSIONThe absorption of loganin in intestine of rat is a first-order kinetics, the absorption mechanism is probably the passive diffusion. It has specific absorption locus and access to locating administration, meanwhile it's the P-gp substrate, and could increase its fraction of bioavailability by corporation with P-gp inhibitor.
Animals ; Drugs, Chinese Herbal ; pharmacokinetics ; Duodenum ; metabolism ; Hydrogen-Ion Concentration ; Ileum ; metabolism ; In Vitro Techniques ; Intestines ; metabolism ; Iridoids ; pharmacokinetics ; Jejunum ; metabolism ; Kinetics ; Male ; Rats ; Rats, Wistar
8.Role of duodenum in regulation of plasma ghrelin level and body mass index after subtotal gastrectomy.
Hai-tao WANG ; Qi-cheng LU ; Qing WANG ; Rong-chao WANG ; Yun ZHANG ; Hai-long CHEN ; Hai-xin QIAN
Chinese Journal of Gastrointestinal Surgery 2008;11(5):436-439
OBJECTIVETo investigate the role of duodenum in regulation of ghrelin and body mass index (BMI) and the correlation between ghrelin and BMI after subtotal gastrectomy.
METHODSForty-two patients with T(0-1)N(0-1)M(0) gastric cancer were divided into two groups after gastrectomy according to digestive reconstruction pattern, Billroth I group (n=23) and Billroth II group (n=19) respectively. Plasma ghrelin levels were determined by radioimmunoassay (RIA) before and at day 1, 7, 30 and 360 after gastrectomy,and BMIs were also measured.
RESULTSTwo groups had identical postoperative trends in ghrelin alterations during the early stage, both dropping to nadir at day 1 (36.7% vs 35.7%), then markedly increasing at day 7 (51.0% vs 51.1%). At day 30, ghrelin level of Billroth I group was slightly higher than that of Billroth II group. At day 360, ghrelin level of Billroth I group recovered to 93.6%, approaching though lower than preoperative level and no significant difference was displayed, while ghrelin level of Billroth II group recovered only to 81.6% of preoperational level and significant difference existed (P=0.033). Compared with preoperative levels, ghrelin of two groups decreased by 6.9% and 18.4% while BMI by 3.3% and 6.4% respectively, liner regression correlations were revealed in both groups between decrease magnitudes(R(1)(2)=0.297,P=0.00;R(2)(2)=0.559,P<0.001).
CONCLUSIONSAnatomico-physiological duodenum compensatively promotes ghrelin recovery, accordingly enhances BMI after gastrectomy. Regarding patients with insufficient ghrelin secretion, ghrelin is positively correlated with BMI.
Adult ; Body Mass Index ; Duodenum ; metabolism ; Female ; Gastrectomy ; methods ; Ghrelin ; blood ; Humans ; Male ; Middle Aged ; Stomach Neoplasms ; blood ; physiopathology ; surgery
9.Effect of electroacupuncture at "Zusanli" (ST 36) on duodenal mast cells, NGF and NTRK1 in rats with functional dyspepsia.
Jia-Zi DONG ; Pei-Jing RONG ; Xiao-Tong WANG ; Dan WANG ; Ming-Hui LENG ; Lu-Jia XIAO
Chinese Acupuncture & Moxibustion 2022;42(7):767-772
OBJECTIVE:
To observe the effect of electroacupuncture (EA) at "Zusanli" (ST 36) on duodenal mast cells, nerve growth factor (NGF) and neurotrophic tyrosine kinase receptor type 1 (NTRK1), and to explore the mechanism of electroacupuncture at Zusanli (ST 36) on functional dyspepsia (FD).
METHODS:
Sixty SPF-grade 10-day-old SD rats were randomly divided into a normal group, a model group, a ketotifen group and an EA group, 15 rats in each group. The FD model was prepared by iodoacetamide combined with rat tail clamping method in the model group, the ketotifen group and the EA group. The rats in the ketotifen group were injected intraperitoneally with ketotifen (1 mg•kg-1•d-1) for 7 days; the rats in the EA group were treated with EA at bilateral "Zusanli" (ST 36), with disperse-dense wave, frequency of 2 Hz/50 Hz and intensity of 0.5 mA, 20 min each time, once a day for 14 days. The gastric emptying rate and small intestinal propulsion rate in each group were observed; the morphology of duodenal mucosa was observed by HE staining; the toluidine blue staining was used to observe the number and degranulation of mast cells in duodenal mucosa; the protein and mRNA expressions of NGF, NTRK1 in duodenum were detected by Western blot and real-time PCR; the level of interleukin-1β (IL-1β) in duodenum was measured by ELISA.
RESULTS:
Compared with the normal group, the gastric emptying rate and small intestinal propulsion rate in the model group were decreased (P<0.01); compared with the model group, the gastric emptying rate and small intestinal propulsion rate in the ketotifen group and the EA group were increased (P<0.01); the small intestinal propulsion rate in the EA group was higher than that in the ketotifen group (P<0.01). In the model group, local defects in duodenal mucosa were observed with a small amount of inflammatory cell infiltration; no obvious abnormality was found in duodenal mucosa of the other groups. Compared with the normal group, the mast cells of duodenal mucosa in the model group were increased significantly with significant degranulation; compared with the model group, the mast cells of duodenal mucosa in the ketotifen group and the EA group were decreased significantly, and the degranulation was not obvious. Compared with the normal group, the protein and mRNA expressions of NGF, NTRK1 as well as the level of IL-1β in duodenum in the model group were increased (P<0.01); compared with the model group, the protein and mRNA expressions of NGF, NTRK1 as well as the levels of IL-1β in duodenum in the ketotifen group and the EA group were decreased (P<0.01, P<0.05); compared with the ketotifen group, the mRNA expression of NGF, as well as the protein and mRNA expressions of NTRK1 in duodenum in the EA group were decreased (P<0.05, P<0.01).
CONCLUSION
EA at "Zusanli" (ST 36) could inhibit the activation of duodenal mast cells and regulate the expressions of NGF and its receptor to improve the low-grade inflammatory response of duodenum, resulting in treatment effect on FD.
Acupuncture Points
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Animals
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Duodenum/metabolism*
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Dyspepsia/therapy*
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Electroacupuncture
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Ketotifen
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Mast Cells/metabolism*
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Nerve Growth Factor/metabolism*
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RNA, Messenger
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Rats
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Rats, Sprague-Dawley
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Receptor, trkA/genetics*
10.Expression of iron regulatory protein-2 and ferritins in intestinal mucosa of rats with iron deficiency.
Wen-Li ZUO ; Yu-Xian XUE ; Yu-Feng LIU
Journal of Experimental Hematology 2008;16(3):565-568
In order to investigate the influence of iron deficiency on the mRNA expression of iron regulatory protein (IRP(2)) mRNA and ferritins (FN) in intestinal mucosa of rat, the animal model of rat with nutritional iron deficiency was established. According to the measurement of serum iron (sI), serum fertitin (sFn) and Hb, the experiments were divided into 4 groups: control group, recessive iron deficiency group, mild iron deficiency group and moderate iron deficiency group. sI was measured by flame assay and sFN was measured by radioimmunoassay, the expressions of irp(2) mRNA and fn mRNA were detected by RT-PCR. The results showed that (1) with aggravation of iron deficiency, the levels of sI and sFN in experimental groups decreased and had significant difference from that in control group, except sI level in the recessive iron deficiency group; (2) with aggravation of iron deficiency, the expression of irp(2) mRNA in duodenum mucosa elevated, and the expressions of irp(2) mRNA in moderate iron deficiency group and mild iron deficiency group were higher than that in control group (p < 0.01), the expression of irp(2) mRNA in moderate iron deficiency group was higher than that in recessive iron deficiency group (p < 0.05), but the expression of irp(2) mRNA did not showed statistical difference between mild iron deficiency group and moderate iron deficiency group (p > 0.05); (3) with aggragation of iron deficiency, the expression of fn mRNA in dudemum mucosa decreased, the expression levels fn mRNA in control and moderate groups were highest and lowest, respectively, there were significant differences between experimental and control groups (p < 0.05), and between experimental groups (p < 0.05); (4) the expression of irp(2) mRNA and fn mRNA in moderate iron difficiency group showed negative correlation (r = 0.662, p < 0.05). It is concluded that IRP(2) protein serves as an important regulator of iron metabolism in the human body, and regulates iron uptake from the intestine by controlling the expression of fn mRNA at the post transcriptional level.
Anemia, Iron-Deficiency
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metabolism
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Animals
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Duodenum
;
metabolism
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Female
;
Ferritins
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genetics
;
metabolism
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Intestinal Mucosa
;
metabolism
;
Iron Regulatory Protein 2
;
genetics
;
metabolism
;
RNA, Messenger
;
genetics
;
metabolism
;
Random Allocation
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Rats
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Rats, Wistar