Plenty of data and tests suggested that flavonoids have strong physiological and pharmacological activities. In this paper, the absorption, distribution and metabolism of flavonoids in gaster, gut and liver were introduced. The research of absorption, distribution and metabolism on flavonoids will provide theoretical basis for developing new drugs of flavoniods.
Animals ; Flavonoids ; metabolism ; pharmacokinetics ; Humans ; Intestinal Absorption ; Intestines ; metabolism ; Liver ; metabolism ; Stomach ; metabolism ; Tissue Distribution

To study the expression and distribution of neuropeptide Y (NPY) and long leptin receptor (OB-Rb) in the gastrointestinal tract of giant panda, samples of three animals were collected from the key laboratory for reproduction and conservation genetics of endangered wildlife of Sichuan province, China conservation and research center for the giant panda. Paraffin sections of giant panda gastrointestinal tissue samples were observed using hematoxylin-eosin staining (HE) and strept actividin-biotin complex immunohistochemical staining (IHC). The results show that the intestinal histology of three pandas was normal and no pathological changes, and there were rich single-cell and multi-cell mucous glands, long intestinal villi and thick muscularis mucosa and muscle layer. Positive cells expressing NPY and OB-Rb were widely detected in the gastrointestinal tract by IHC methods. NPY positive nerve fibers and neuronal cell were widely distributed in submucosal plexus and myenteric plexus, especially in the former. They were arranged beaded or point-like shape. NPY positive cells were observed in the shape of ellipse and polygon and mainly located in the mucous layer and intestinal glands. OB-Rb positive cells were mainly distributed in the mucous layer and the laminae propria, especially the latter. These results confirmed that NPY and OB-Rb are widely distributed in the gut of the giant panda, which provide strong reference for the research between growth and development, digestion and absorption, and immune function.
Animals ; China ; Intestines ; metabolism ; Neuropeptide Y ; genetics ; metabolism ; Receptors, Leptin ; genetics ; metabolism ; Ursidae ; genetics ; metabolism

Oral drug bioavailability depends on gastrointestinal absorption, intestinal transporters and metabolism enzymes are the important factors in drug gastrointestinal absorption and they can also be induced or inhibited by the active ingredients of Chinese materia medica. This article presents important application of intestinal transporters and metabolism enzymes on gastrointestinal disposal of the active ingredients of Chinese materia medica, and points out the importance of research on transport and metabolism of the active ingredients of Chinese materia medica in Chinese extract and Chinese medicinal formulae.
Animals ; Carrier Proteins ; metabolism ; Gastrointestinal Tract ; enzymology ; metabolism ; Humans ; Intestines ; metabolism ; Materia Medica ; metabolism

OBJECTIVETo investigate the role of cyclic adenosine monophosphate(cAMP) in the regulation of intestinal epithelial barrier function under hypoxia.

METHODSIntestinal epithelial barrier was established by Caco-2 monolayers. Cells were divided into four groups: normoxia (Nx), normoxia plus Forskolin(Nx+FSK), hypoxia(Hx), hypoxia plus SQ22536(Hx+SQ22536). cAMP concentrations of different groups were assessed by cAMP enzyme immunoassay kit. RT-PCR and Western blotting were used to detect the mRNA and protein expressions of claudin-1 and occludin under normoxic and hypoxic condition. Caco-2 monolayers were grown on Millicell filters, and transepithelial electrical resistance(TER) was measured using a Millipore electric resistance system.

RESULTSThe concentration of cAMP under hypoxic conditions(Hx group) was higher compared with Nx group [(6.30±0.50) pmol/L vs. (2.38±0.18) pmol/L, P<0.01]. At the same time, both mRNA and protein expressions of claudin-1 and occluding were lower in Hx group than those in Nx group(all P<0.05). TER decreased by 76.30±0.64(P<0.01). When the monolayers were exposed to hypoxia plus SQ22536 (Hx+SQ22536 group), the concentration of cAMP was(2.12±0.23) pmol/L, which was lower than that under hypoxic conditions(Hx group, P<0.01). Both mRNA and protein expressions of claudin-1 and occludin were higher compared to Hx group (all P<0.01). TER increased by 32.96±2.16 (P<0.05).

CONCLUSIONWhen Caco-2 cells are exposed to hypoxia, barrier function, claudin-1 and occludin expression are diminished in parallel with a high level of intracellular cAMP compared with the normoxic condition. Inhibition of the intracellular cAMP level under hypoxia can maintain the intestinal epithelial function through regulating the claudin-1 and occludin expression and attenuate the permeability of intestinal mucosa.

Adenosine Monophosphate ; Caco-2 Cells ; Claudin-1 ; metabolism ; Humans ; Intestinal Mucosa ; metabolism ; Intestines ; Occludin ; metabolism

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

The study aims to screen the ability of the bacteria to metabolize ononin and assess the effect of ononin on the intestinal bacteria. Fresh human fecal sample was obtained from a healthy volunteer, diluted serially in sterile water and sixty-nine different bacterial colonies were picked out ultimately. UPLC-Q-TOF/MS with automated data analysis software (MetaboLynx) was applied to fast analysis of ononin metabolites. Furthermore, an E(max) precision microplate reader was employed to determine the growth situation of Enterococcous sp., Enterobacter sp., Lactobacilli sp., and Bifidobacteria sp. Results indicated that hydrogenation, demethylation, hydroxylation and deglycosylation were the major metabolic pathways of ononin by human intestinal bacteria in vitro. Ononin can inhibit the growth of pathogen such as Enterococcus sp., Enterobacter sp. and can promote the growth of probiotics such as Bifidobacteria sp. and Lactobacilli sp. This study suggested that intestinal bacteria have the metabolic effects of ononin and the biotransformation was completed by different bacteria. And ononin can affect the balance of intestinal flora and the degree of influence varies depending on the bacterial species and the concentration of ononin.
Bacteria ; metabolism ; Biotransformation ; Feces ; microbiology ; Glucosides ; metabolism ; Humans ; Intestines ; microbiology ; Isoflavones ; metabolism ; Metabolic Networks and Pathways

Amino Acids ; metabolism ; Hepatic Encephalopathy ; therapy ; Humans ; Intestines ; metabolism ; Liver, Artificial ; Neurotransmitter Agents ; metabolism

This study aimed to elucidate the digestive characteristics of flavonoid components in Xiaoer Chiqiao Qingre Granules(XECQ) in the gastrointestinal environment of infants. An in vitro model was established to simulate the gastric and intestinal environment of infants. UPLC was used to analyze the content change of flavonoid components in XECQ, and their overall content was integrated through the mass fraction weight coefficient method. UPLC-Q-TOF-MS was employed to determine the digestive products of flavonoid components in gastrointestinal fluids and their metabolic pathways. The results showed that in the process of digestion, 11 digestion products were generated by oxidation, reduction, deglycosylation, methylation and other phase Ⅰ metabolism. From flavonoid content and component changes, it was found that the flavonoid components in XECQ were relatively stable in the gastric fluid, while their content in the intestinal fluid was first increased and then maintained stable. This was mainly because flavonoid components were released from proteins, polysaccharides and other macromolecular substances during gastrointestinal digestion. In addition, phase Ⅰ metabolism occurred, but with relatively low metabolic rate, resulting in their stable content. This study preliminarily explored the digestive characteristics of flavonoid components in XECQ in the infant gastrointestinal environment, which laid a foundation for further studying the absorption, transport and metabolism of pharmacodynamics components in XECQ, and facilitated the study of the biopharmaceutical pro-perties of pediatric Chinese medicine.
Infant ; Humans ; Child ; Flavonoids/metabolism* ; Gastrointestinal Tract ; Intestines ; Drugs, Chinese Herbal/metabolism* ; Chromatography, High Pressure Liquid

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

Flavonoids are widely distributed in the nature, and have various biological activities. Flavonoids can be degraded by intestinal bacteria, so as to impact their bioavailability in vivo. Studies on metabolism of flavonoids by intestinal bacteria could provide basis for screening out biotransformation of flavonoids and interpreting their in vivo metabolic process. Being taken as the lead compounds, flavonoids can be modified by intestinal bacteria to achieve new compounds with high efficiency, bioavailability and solubility, which lays a foundation for the research and development of new drugs, selection of drug dosage forms and drug production. This article summarizes the main reaction types and impacting factors of intestinal bacteria on biotransformation of flavonoids, for reference of studies on biotransformation.
Animals ; Bacteria ; metabolism ; Biotransformation ; genetics ; physiology ; Flavonoids ; metabolism ; Humans ; Intestines ; microbiology