AIM: To investigate the absorption characteristics of the total alkaloids from Mahoniae Caulis (TAMC) through the administration of monterpene absorption enhancers or protein inhibitors. METHOD: The absorption behavior was investigated in an in situ single-pass intestinal perfusion (SPIP) assay in rats. RESULTS: The intestinal absorption of TAMC was much more than that of a single compound or a mixture of compounds (jatrorrhizine, palmatine, and berberine). Promotion of absorption by the bicyclic monoterpenoids (borneol or camphor) was higher than by the monocyclic monoterpenes (menthol or menthone), and promotion by compounds with a hydroxyl group (borneol or menthol) was higher than those with a carbonyl group (camphor or menthone). The apparent permeability coefficient (Papp) of TAMC was increased to 1.8-fold by verapamil, while it was reduced to one half by thiamine. The absorption rate constant (Ka) and Papp of TAMC were unchanged by probenecid and pantoprazole. CONCLUSION The intestinal absorption characteristics of TAMC might be passive transport, and the intestinum tenue was the best absorptive site. In addition, TAMC might be likely a substrate of P-glycoprotein (P-gp) and organic cation transporters (OCT), rather than multidrug resistance protein (MRP) and breast cancer resistance protein (BCRP). Compared with a single compound and a mixture of compounds, TAMC was able to be absorbed in the blood circulation effectively.
Alkaloids ; chemistry ; pharmacokinetics ; Animals ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Intestinal Absorption ; Intestinal Mucosa ; metabolism ; Intestines ; chemistry ; Kinetics ; Mahonia ; metabolism ; Male ; Permeability ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo explore the application of a novel device of collecting large amount of fecal mucosa for detecting the DNA methylation and screening colorectal cancer.

METHODSPreoperative complete fecal sample and surgical specimen of 10 patients with colorectal cancer, and complete fecal sample and normal bowel mucosal samples confirmed by colonoscopy of 6 hospitalization cases at The Third Affiliated Hospital, Nanjing University of TCM from March to April 2014 were collected. A self-made bowel mucosa collector (consisting of upper, middle, lower three containers of 1 000 ml volume, with filter screen in each bottom whose pore diameter is 100, 200 and 300 mesh.) was used to collect mucosal exfoliation cells. Fecal DNA kit was applied to extract DNA of exfoliation cells and the concentration and purity of DNA were measured by UV spectrophotometer (A260/A280), meanwhile DNA methylation of fecal fluid and mucosal tissues was detected by bisulfite sequencing pCR(BSP).

RESULTSDNA methylation sequencing showed that FBN1, SPG20, and SNCA genes presented methylation in CpG island in fecal fluid and cancer tissues from 10 colorectal cancer patients, but did not presented methylation in fecal fluid and mucosa from 6 control cases. When fecal amount was below 100 g, collection rate of fecal fluid was 60% to 80%; when fecal amount was over 100 g, collection rate of fecal fluid was unstable. When fecal amount was 50 to 100 g, DNA A260/A280 value was 1.6 to 1.8, and DNA concentration was 5.0 to 56.1 ng/L.

CONCLUSIONCollection rate of fecal fluid with this self-made fecal mucosa collector is quite stable when managing fecal amount of 50 to 100 g once, and can obtain higher purity and concentration of DNA, meeting the demand of methylation detection for screening colorectal cancer.

Colonoscopy ; Colorectal Neoplasms ; diagnosis ; CpG Islands ; DNA Methylation ; Early Detection of Cancer ; methods ; Feces ; chemistry ; Humans ; Intestinal Mucosa

The study was based on the toxic characteristics of the compatibility between "Zaojisuiyuan" and Gancao, with intestinal tract and intestinal bacteria as subject. From the angle of intestinal barrier function, motor function, steady state of intestinal flora and metabolism genes, the toxic and side effects of the compatibility between Qianjinzi and Gancao with similar properties, bases and chemical composition and types were further explored. The results showed that the combined application of Qianjinzi and Gancao enhanced intestinal mucosa damage, and led to abnormal changes in intestinal bacteria structure and metabolic function. It improved the degradation functions of mucus and aromatic amino acids on intestinal bacteria, which may increase the risk of disease and derived from intestinal urotoxin and other toxic substances. This study considered intestinal bacteria as an important target to study the interactions of traditional Chinese medicine. The "drug-intestinal bacteria-metabolism-toxicity" was applied in the experiment. Meanwhile, it provides ideas for exploring incompatible mechanism of traditional Chinese medicines.
Animals ; Drugs, Chinese Herbal ; pharmacology ; Gastrointestinal Microbiome ; drug effects ; Glycyrrhiza uralensis ; chemistry ; Intestinal Mucosa ; drug effects ; pathology ; Medicine, Chinese Traditional

The borneol was included with β-CD and prepared Fufang Danshen intestinal adhesion pellets. GC method for determination of borneol in Fufang Danshen intestinal adhesion pellets was established to study its in vitro dissolution and make a comparison with the Fufang Danshen tablet, in this way, the rationality of dosage form was evaluated. The first method of dissolution determination was used for determining the in vitro dissolution of borneol in Fufang Danshen intestinal adhesion pellets in artificial intestinal juice, and Fufang Danshen tablet in artificial gastric juice and intestinal juice, respectively. Result shows: the concentration of borneol in Fufang Danshen intestinal adhesion pellets and Fufang Danshen tablet was 0.79% and 0.80%, respectively. Its in vitro dissolution was nearly 70% within 12 h in Fufang Danshen intestinal adhesion pellets, and in Fufang Danshen tablet, the dissolution was about 60% within 20 min and more than 90% within 40 min, and in artificial gastric juice, was less than 20% within 40 min but more than 80% till 150 min. Research suggests that in comparison with Fufang Danshen tablet, in vitro dissolution of borneol in the Fufang Danshen intestinal adhesion pellets showed an obvious sustained release behavior. The borneol in Fufang Danshen intestinal adhesion pellets was included with β-CD and prepared enteric preparations. To some extent, the stimulation on stomach and intestinal mucosa can be reduced and safety can be improved.
Bornanes ; adverse effects ; chemistry ; pharmacology ; Chemistry, Pharmaceutical ; methods ; Dosage Forms ; Drugs, Chinese Herbal ; adverse effects ; chemistry ; pharmacology ; Humans ; Intestinal Mucosa ; drug effects ; metabolism ; Models, Biological ; Solubility

The aimed of this study was to prepare stabilized thiomers to overcome the poor stability character of traditional thiomers. Poly(acrylic acid)-cysteine (PAA-Cys) was synthesized by conjugating cysteine with poly(acrylic acid) and poly(acrylic acid)-cysteine-6-mercaptonicotinic acid (PAA-Cys-6MNA, stabilized thiomers) was synthesized by grafting a protecting group 6-mercaptonicotinic acid (6MNA) with PAA-Cys. The free thiol of PAA-Cys was determined by Ellmann's reagent method and the ratio of 6MNA coupled was determined by glutathione reduction method. The study of permeation enhancement and stabilized function was conducted by using Franz diffusion cell method, with fluorescein isothiocyanate dextran (FD4) used as model drug. The influence of polymers on tight junctions of Caco-2 cell monolayer was detected with laser scanning confocal fluorescence microscope. The results indicated that both PAA-Cys and PAA-Cys-6MNA could promote the permeation of FD4 across excised rat intestine, and the permeation function of PAA-Cys-6MNA was not influence by the pH of the storage environment and the oxidation of air after the protecting group 6MNA was grafted. The distribution of tight junction protein of Caco-2 cell monolayer F-actin was influenced after incubation with PAA-Cys and PAA-Cys-6MNA. In conclusion, stabilized thiomers (PAA-Cys-6MNA) maintained the permeation function compared with the traditional thiomers (PAA-Cys) and its stability was improved. The mechanism of the permeation enhancement function of the polymers might be related to their influence on tight junction relating proteins of cells.
Acrylic Resins ; chemistry ; Actins ; metabolism ; Animals ; Caco-2 Cells ; Cysteine ; chemistry ; Dextrans ; Fluorescein-5-isothiocyanate ; analogs & derivatives ; Glutathione ; Humans ; Intestinal Absorption ; Intestinal Mucosa ; drug effects ; Nicotinic Acids ; chemistry ; Rats ; Sulfhydryl Compounds ; chemistry

OBJECTIVETo research the principle of match-pair of huanglian-rougui.

METHODA rat intestinal model in vitro had been applied to investigate the absorption and transport characteristics of total huanglian alkali across intestinal mucosa, as well as the influence of match-pair of huanglian-rougui on its intestinal absorption. The identification of alkalis in primitive solution, serosal solution and intestinal homogenate were analyzed by TLC.

RESULTThe transport and uptake characteristic of total alkali in huanglian solution was similar to berberine. The uptake and transport of total alkali across intestinal mucosa was concentration-and time-dependent. Transport directions had strong effects on the transport of total alkali. The amount of total alkali transport from serosal side to mucosal side was much more than that from mucosal side to serosal side. After matching with rougui as some ration, the intestinal absorption of total alkali increased significantly comparing with huanglian alone, and there was an optimal ration among match-pair of huanglian-rougui.

CONCLUSIONChemical reaction in vitro and intestinal absorption were the key factors of match-pair of huanglian-rougui.

Alkaloids ; isolation & purification ; pharmacokinetics ; Animals ; Biological Transport ; drug effects ; Cinnamomum ; chemistry ; Coptis ; chemistry ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Intestinal Absorption ; drug effects ; Intestinal Mucosa ; metabolism ; Male ; Matched-Pair Analysis ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley

An in vitro detection method of the gastrointestinal absorption of Pilose Antler protein was established for mixed protein activity. Five bands of protein with molecular weight of 17.8-160 kD derived from the Pilose Antler were extracted and sufficiently labeled with FITC (FITC-PE). The stability and variation of FITC-PE in gastrointestinal circumstances were detected by native polyacrylamide gel electrophoresis and confocal laser scanning microscope. Results showed that the main component of FITC-PE kept invariant after being reacted with artificial gastric fluid and artificial intestinal fluid. The fluorescence signal was detected 20 min after administration in the valgus intestinal purse experiment, and three kinds of protein, with molecular weight of 45, 25, and 17.8 kD, were detected in the mixture of absorbent protein. The research laid the foundation for the further in vivo study of Pilose Antler protein. Meanwhile, it would be an in vitro screening method for the absorption, distribution and metabolism of mixed protein from traditional Chinese medicine.
Animals ; Antlers ; chemistry ; Deer ; Fluorescein-5-isothiocyanate ; Intestinal Absorption ; Intestinal Mucosa ; metabolism ; Male ; Materia Medica ; chemistry ; isolation & purification ; pharmacokinetics ; Microscopy, Confocal ; Molecular Weight ; Native Polyacrylamide Gel Electrophoresis ; Proteins ; chemistry ; isolation & purification ; pharmacokinetics ; Rats ; Rats, Wistar ; Stomach ; metabolism

BACKGROUND/AIMS: Ulcerative colitis (UC) is sometimes associated with autoimmune pancreatitis (AIP). Infiltration of immunoglobulin G4 (IgG4)-positive plasma cells is sometimes detected in the colonic mucosa of AIP or UC patients. This study aimed to clarify the relation between UC and IgG4. METHODS: Associations with UC were reviewed in 85 AIP patients. IgG4 immunostaining was performed on biopsy specimens from the colonic mucosa of 14 AIP and 32 UC patients. RESULTS: UC was confirmed in two cases (type 1 AIP, n=1; suspected type 2 AIP, n=1). Abundant infiltration of IgG4-positive plasma cells in the colonic mucosa was detected in the case of suspected type 2 AIP with UC and two cases of type 1 AIP without colitis. Abundant infiltration of IgG4-positive plasma cells was detected in 10 UC cases (IgG4-present, 31%). Although 72% of IgG4-absent UC patients showed mild disease activity, 70% of IgG4-present patients showed moderate to severe disease activity (p<0.05). CONCLUSIONS: UC is sometimes associated with AIP, but it seems that UC is not a manifestation of IgG4-related disease. Infiltration of IgG4-positive plasma cells is sometimes detectable in the colonic mucosa of UC patients and is associated with disease activity.
Adult ; Aged ; Colitis, Ulcerative/*blood/complications ; Colon/*chemistry ; Female ; Humans ; Immunoglobulin G/*analysis ; Intestinal Mucosa/*chemistry ; Male ; Middle Aged ; Pancreatitis/*blood/complications ; Retrospective Studies

The ideal treatment and recovery of osteoarticular injury remain to be resolved. Small intestinal submucosa (SIS), a naturally-occurring decellularized extracellular matrix, has been recognized as an ideal scaffold for tissue engineering and widely used in repairing various tissues and organs. Nowadays its application has also been gradually increased in the field of orthopedics. We reviewed laboratorial studies and clinical trails about the application of SIS in bone and joint repair, aiming to evaluate its effects on the repair of bone, cartilage, meniscus, ligament and tendon. SIS has showed promising results in repairing bone, meniscus, ligament or tendon. However, additional studies will be required to further evaluate its effects on articular cartilage and tendon-bone healing. How to optimize SIS material,is also a focused problem concerned with making SIS a potential therapeutic option with high value for orthopedic tissue repair.
Animals ; Cell- and Tissue-Based Therapy ; Humans ; Intestinal Mucosa ; cytology ; Intestine, Small ; cytology ; Joint Diseases ; physiopathology ; surgery ; therapy ; Tissue Engineering ; instrumentation ; methods ; Tissue Scaffolds ; chemistry

OBJECTIVETo study the induced change of tumor necrosis factor alpha (TNF-alpha) level in serum and colon tissue of guinea pig model with melanosis coli and its significance induced by rhubarb (RB).

METHODSOne hundred and twelve guinea pigs of clean grade were randomly divided into four groups: the 16 in the normal group (untreated) and the 3 RB groups (32 in each) treated with low (3 g/kg d), medium (6 g/kg d), and high (12 g/kg d) dose of rhubarb respectively, administered by gastrogavage for 60 successive days. All guinea pigs were sacrificed at the terminal of the experiment and their blood serum and colon tissue were taken for detecting TNF-alpha level and TNF-alpha mRNA expression qualitatively and quantitatively using ELISA and RT-PCR.

RESULTSCompared with the normal group, serum and colonic tissue levels of TNF-alpha and TNF-alpha mRNA expression in the RB groups were higher significantly (P<0.01), while no significant difference was found among the later three groups (P>0.05).

CONCLUSIONRB could induce change of TNF-alpha level in serum and colon tissue of guinea pig with melanosis coli.

Animals ; Colonic Diseases ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; Female ; Guinea Pigs ; Intestinal Mucosa ; metabolism ; Male ; Melanosis ; metabolism ; Random Allocation ; Rheum ; chemistry ; Tumor Necrosis Factor-alpha ; metabolism