OBJECTIVETo compare the metabolic transformation of four processed rhubarb aqueous extracts in rat intestinal bacteria in vitro.

METHODRat intestinal bacteria test solution and each of four processed rhubarb aqueous extracts were incubated under anaerobic conditions at 37 degrees C. High-performance liquid chromatography with diode-array detection (HPLC-DAD) and tandem mass spectrometry (HPLC-MS/MS) was used for the qualitative analysis on the components that can be bio-transformed by rat intestinal bacteria as well as the trend of metabolic transformation of each parent compounds according to the changes in chromatographic peak areas in different incubation times.

RESULTAnthraquinones, glucose gallates and naphthalenes glucosides could be bio-transformed by rat intestinal bacteria. Of them, anthraquinones were undoubtedly the most prevalent parent compounds, as 12 out of the 17 metabolites were tentatively assigned as metabolites transformed from anthraquinones. Besides, it was also found that each parent compound in four processed rhubarb extract were diverse from each other with the incubation time.

CONCLUSIONThe preparations change composition and proportional relationship of ingredients contained in rhubarb and thus impacting their transformation effect in intestinal bacteria.

Animals ; Bacteria ; metabolism ; Biotransformation ; Chemistry, Pharmaceutical ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Intestinal Absorption ; Intestines ; microbiology ; Rats ; Rheum ; chemistry ; Water ; chemistry

Since pang set up the perfused rat intestine-liver preparation and applied it to study the disposition of enalapril, this model has been widely considered to have the particularly advantage in studying the absorption, metabolism and first-pass effect. Now the methods and applications are to be reviewed and the perspective is to be discussed.
Animals ; Humans ; Intestinal Absorption ; Intestines ; chemistry ; physiology ; Liver ; chemistry ; physiology ; Models, Animal ; Perfusion ; methods ; Rats

Evaluation of the permeability mainly focuses on intestinal absorption in biopharmaceutics classification system (BCS). It is more complicated that the absorption and metabolism under multicomponent environment in biopharmaceutics classification system of Chinese materia medica (CMMBCS) compared with single component environment, which needs suitable mathematical models to be described. Therefore, with full consideration of existing single component mathematical algorithm combining with the characteristics of intestinal absorption and metabolism, we explored and designed a new mathematical algorithm of intestinal absorption and metabolism of multicomponent drug. Then we put forward a new coefficient, P (influence), the relative change rate of the single component's intestinal absorption and metabolism under multicomponent environment compared with single component environment, which described the influences of intestinal absorption and metabolism of the component under multicomponent environment. Moreover, P (influence) highlights the distinctive characteristics of multicomponent drug's intestinal absorption and metabolism, and lays the foundation for the construction of CMMBCS.
Algorithms ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Humans ; Intestinal Absorption ; Intestines ; chemistry ; metabolism ; Models, Theoretical ; Solubility

Animals ; Bacteria, Anaerobic ; metabolism ; Drugs, Chinese Herbal ; isolation & purification ; metabolism ; Humans ; Intestines ; microbiology ; Plants, Medicinal ; chemistry

Focusing on the relationship of intestinal microecology with the physiologic function and pathologic manifestation, literature in recent years on mechanisms of Chinese wedicinal compounds for regulating disease associated intestinal microecology are reviewed in this paper, so as to provide a new approach and idea for scientific research and clinical application of Chinese wedicinal compounds.
Biodiversity ; Drug Combinations ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Intestines ; drug effects ; microbiology ; Medicine, Chinese Traditional

Recent metabolomics research revealed a new ginseng ginsenoside IH901 that is synthesized by intestinal microbial transformation in oral administration of ginseng. IH901 shows various biological activities, including anti-tumor, anti-inflammatory, anti-diabetic, and anti-aging. In recent years, great effort has been made to prepare IH901 by microbial and enzymatic transformation in a large scale. In this paper, we reviewed the biotransformation pathways both in vivo and in vitro and bioactive properties of rare ginsenoside IH901.
Biotransformation ; Ginsenosides ; metabolism ; pharmacokinetics ; Humans ; Intestines ; metabolism ; microbiology ; Panax ; chemistry ; Sapogenins ; metabolism

OBJECTIVETo establish human intestinal bacteria biotransformation model and the standard operation procedure for studying and assessing intestinal biotransformation of chemical constituents of traditional Chinese medicine (TCM).

METHODThe chemical constituent of TCM was incubated together with human intestinal flora or isolated strain, or their secretory enzymes at anaerobic environment and 37 degrees C. The biotransformation products were extracted by solvent extraction methods, separated by column chromatographic methods, and identified by spectroscopic analysis. The biotransformation mechanisms would be deduced by comparison of structural characteristics of the biotransformation products and the parent drug and/or compound, as well as the enzyme(s)-catalysed bioreactions.

RESULTThe established biotransformation model of human intestinal bacteria is facile for operation and has the capability of converting the chemical constituent of traditional Chinese medicine. The growing cells transformation method, the resting cells transformation method or enzyme(s)-catalysed transformation method can all be selected as the transformation approach.

CONCLUSIONThe established human intestinal bacteria biotransformation model can be used to study the intestinal biotransformation of orally administrated chemical constituents of TCM and their biotransformation mechanism.

Bacteria ; chemistry ; metabolism ; Biotransformation ; Drugs, Chinese Herbal ; analysis ; metabolism ; Humans ; Intestines ; chemistry ; metabolism ; microbiology ; Medicine, Chinese Traditional ; Models, Biological

To use the single-pass intestine perfusion (SPIP) model and HPLC to determine the concentration of formononetin, the effect of quality concentrations of formononetin, different intestinal segments and P-glycoprotein inhibitor on intestinal absorption of formononetin, in order to observe the intestinal absorption mechanism of formononetin from Millettia nitita var. hirsutissima in rats. The experimental results showed that the qulaity concentration of formononetin in the perfusate had no significant effect on the absorption rate constant (K(a)) and the apparent absorption coefficient (P(app)); K(a) and P(app) of formononetin in duodenum, jejunum and ileum showed no significant difference. However, K(a) was significantly higher than that in colon (P < 0.05), with significant difference between that in intestinum tenue and colon. P-glycoprotein inhibitor verapamil showed significant difference in K(a) and P(app) in intestinal segments (P < 0.05). This indicated that the absorption mechanism of formononein in rat intestinal tracts passive diffusion, without any saturated absorption. Formononein is absorbed well in all intestines. Their absorption windows were mainly concentrated in the intestinum tenue, without specific absorption sites. Formononein may be the substrate of P-glycoprotein.
Animals ; Drugs, Chinese Herbal ; pharmacokinetics ; Humans ; Intestinal Absorption ; Intestines ; chemistry ; metabolism ; Isoflavones ; pharmacokinetics ; Kinetics ; Male ; Millettia ; chemistry ; Rats

A UPLC-ESI-MS/MS method was used to determinate the main active fractions gallic acid, protocatechuic acid, myricetrin, hyperoside and quercitrin in Polygonum capitatum extracts by in situ intestinal perfusion models; the absorption rate constants and cumulative penetration rate of absorption were calculated. The effect of different drug concentrations, different intestine segments, bile and P-gp inhibitors on the absorption mechanism of Gallic acid and other compositions in P. capitatum extracts. The experimental results showed that gallic acid, protocatechuic acid, myricetrin and quercitrin were observed saturated at high concentration (P < 0.05). Bile had significant inhibition effect on protocatechuic acid absorption and had promotion effect on myricetrin and hyperoside absorption (P < 0.05). P-gp inhibitor verapamil could significantly enhance the absorption of Protocatechuic acid (P < 0.05). The overall trend for absorption of various compositions was that small intestine > colon. This indicated that the absorption mechanism of P. capitatum extracts in rat intestine was in line with fist-order kinetics characteristics. The composition could be absorbed in all of the different intestinal segments, and the absorption was mainly concentrated in small intestine. The protocatechuic acid may be the substrate of P-gp.
Animals ; Drugs, Chinese Herbal ; chemistry ; metabolism ; Female ; Intestinal Absorption ; Intestines ; chemistry ; metabolism ; Male ; Polygonum ; metabolism ; Rats ; Rats, Sprague-Dawley

The complex level of constructing biopharmaceutics classification system of Chinese materia medica CMMBCS) was the study of traditional Chinese compound, on the premise of insisting that the multicomponent simultaneous determination, when carrying out the study of intestinal permeability, the primary task was to define the source of the components that was absorbed through the intestinal wall, namely, which medicinal material the components belonged to in traditional Chinese compound. The technology of chemical fingerprint and in vitro everted gut sac model were used in this research to make multicomponent an intuitive source attribution which permeated the intestine in the classic formula Gegen Qinlian decoction, and to lay the foundation for the further qualitative and quantitative research of intestinal permeability.
Animals ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Intestines ; metabolism ; Male ; Permeability ; Plants, Medicinal ; chemistry ; Rats ; Rats, Wistar