ABSTRACT
Gastrointestinal motility disorder is an important cause of digestive system diseases. Patients often suffer from nausea， vomiting， gastric retention， gastroparesis， constipation， and many other symptoms， and their quality of life is seriously reduced. Prokinetic agents are routinely used in clinical practice， but their long-term use is prone to problems such as reduced efficacy and increased adverse reactions. Since the incidence of gastrointestinal diseases has continued to rise globally in recent years， there is an urgent need for clinical development of safe and effective treatment strategies. Aurantii Fructus， a traditional Chinese medicine， has the effect of smoothing Qi and eliminating distention， and it has been used to treat gastrointestinal diseases for thousands of years. In modern clinical practice， it is mainly used for the treatment and auxiliary treatment of various gastrointestinal diseases such as functional dyspepsia， functional constipation， and irritable bowel syndrome. The efficacy is remarkable， and no adverse reactions have been reported at conventional doses. Therefore， it can greatly improve the symptoms of patients with gastrointestinal diseases and improve their quality of life. Modern research has revealed that there are many active components in Aurantii Fructus， among which flavonoids have the highest content and the most types. Flavonoids are the main active components in Aurantii Fructus to regulate gastrointestinal motility. Aurantii Fructus and its active components can affect gastrointestinal hormones， neural pathways， Cajal mesenchymal cells， and other multiple mechanisms. They can adjust gastrointestinal motility and correct gastrointestinal motility disorders， showing potential application value in the treatment of gastrointestinal motility disorders. However， a comprehensive analysis of Aurantii Fructus in this aspect is still lacking. This study summarized the pharmacological activities of active components of Aurantii Fructus extract and its flavonoids， volatile oils， alkaloids， and coumarin on the regulation of gastrointestinal motility and explored the latest research progress on its mechanism. Finally， the adverse reactions of Aurantii Fructus were summarized. It aims to provide a scientific basis for the research and clinical application of Aurantii Fructus and its active components in the regulation of gastrointestinal motility.
ABSTRACT
Objective: To compare the pharmacokinetics of naringin and neohesperidin after oral administration of Zhishi total flavonoid glycosides (ZSTFG) extracted from Aurantii Fructus Immaturus in normal and gastrointestinal motility disorders (GMD) mice. Methods: ZSTFG was orally given to normal and GMD mice induced by atropine or dopamine. The plasma samples were incubated with β-glucuronidase/sulfatase, the total (free + conjugated) naringenin and hesperitin were extracted with acetonitrile. The validated HPLC-MS/MS method was successfully applied to the pharmacokinetic study. Results: The results showed that, compared with the normal group, AUC0–∞, AUC0–t and Cmax for total naringenin and hesperitin were significantly higher (P < 0.01 or P < 0.05), while CLZ/F for total naringenin and hesperitin was significantly lower (P < 0.01) in the GMD group. Tmax, t1/2z, MRT0-t, and MRT0-∞ for naringenin were longer (P < 0.01) in the GMD group than those in the normal group. Conclusion: The results showed that there were significant differences in pharmacokinetic parameters of naringenin and hesperitin between normal and GMD groups. It was suggested that the absorption of naringenin and hesperitin was increased, and the elimination processes of naringenin and hesperitin were slower in the GMD group than the normal group. The data are of value for further pharmacological studies of ZSTFG and would be useful to provide a reference for improving the therapeutic regimen of ZSTFG in clinical trials.
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Objective To investigate the effect of dopamine receptor in intestinal mucosal barrier function after brain injury in rats.Methods Twenty-four rats were allocated to control group,brain injury group,dopamine receptor group,and dopamine antagonist group according to the random number table,with 6 rats per group.Feeney' s weight-drop model was introduced to generate rat models of brain injury.Intestinal mucosal specimens were harvested at postoperative 7 days to evaluate intestinal mucosal morphology by HE staining,expressions of dopamine receptor D1 (DRD1) and dopamine receptor D2 (DRD2) by immunohistochemistry,and mRNA and protein expressions of DRD1 and DRD2 by real-time PCR and Western blot.Meantime,urinary samples were collected to measure lactulose to mannitol ratio (L/M) by high performance liquid chromatography (HPLC).Results Intestinal villus integrity was disrupted in brain injury group and dopamine receptor group when compared to control group,but it remained relatively intact in dopamine antagonist group.Ratio of L/M in brain injury group and dopamine receptor group was similar (0.192 ± 0.080 vs 0.183 ± 0.090,P ＞ 0.05),far higher than 0.037 ± 0.008 in control group (P ＜0.01),but it was reversed in dopamine antagonist group (0.071 ± 0.008,P ＜ 0.01).Real-time PCR showed DRD1 and DRD2 mRNAs expressed in brain injury group and dopamine receptor group were similar (0.764 ± 0.074 vs 0.718 ± 0.065,0.439 ± 0.051 vs 0.408 ± 0.090,P ＞ 0.05),far higher than 0.189 ± 0.008 and 0.076 ± 0.011 in control group (P ＜ 0.01),but both lowered in dopamine antagonist group (0.386 ± 0.071,0.270 ± 0.092,P ＜ 0.01).estern blot analysis showed DRD1 and DRD2 proteins in brain injury group and dopamine receptor group were similar,but both were far higher when compared to control group (P ＜ 0.01).Conclusion Impaired intestinal mucosal barrier may be relate to the up-regulated dopamine receptor in intestinal mucosa after brain injury in rats.
ABSTRACT
Gastrointestinal motility disorders are in high incidence in children.Due to moderate prokinetic effects,poor symptomatic responses and the presence of adverse effects,there is a clear need for new classes of prokinetics.Currently available drug classes in adult include antidopami-nergic agents,serotonergic agents,and motilin-receptor while there are less available drug classes in children.The aim of the present article is to review and address the present use of promotility drugs in the treatment of different gastrointestinal motor disorders,as well as the potential for future developments.
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From 1991 to 2000, thirty patients with gastrointestinal motility disorders were diagnosed in Department of Pediatrics, Siriraj Hospital. They were divided into 3 groups ; in group 1, 15 patients had normal psychomotor development with chronic intestinal pseudo-obstruction (CIP) or intestinal dysmotility; in group 2, 9 patients had psychomotor retardation with CIP or intestinal dysmotility and in group 3, 6 patients had gastroparesis. Three cases in group 1 had underlying causes including megacystis-microcolon-intestinal-hypoperistalsis syndrome (MMIHS), SLE, and Strongyloid infestation. MMIHS was diagnosed during pregnancy. This patient did not respond to any medications and died at 5 months. Nine cases in group 2 and 1 case in group 1 were diagnosed as CIP due to their persistent symptoms of obstruction and radiologically demonstrated dilated intestine with air /fluid levels. The main presenting symptoms were abdominal distention (27 cases), constipation (14 cases), abdominal pain (13 cases), vomiting (9 cases), diarrhea (9 cases), and refusal of feeds (3 cases). X-ray studies were the most useful investigation to diagnose the disorders. All patients received cisapride as a prokinetic drug in order to improve the motility of the GI tract. A good response was obtained in14 cases, a fair response in 15 cases and a poor response in 1 case. GI motility disorder is not uncommon in Thai children. The severity of the motility disorder varied from mild to severe. The majority of cases had a good prognosis except in the cases with psychomotor retardation in addition.
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In recent years, gastrointestinal pace-maker or electrical stimulation has been proposed as a therapeutic option. The interstitial cells of Cajal (ICC) are the pacemaker cells in the gastrointestinal tract.They have special properties that make them unique in their ability to generate and propagate slow waves in gastrointestinal muscles which determine the frequency, the direction and velocity of the propagation of peristaltic activity, in concert with the enteric nervous system for GI motility. Gastrointestinal pacing has been used in the treatment of gastroparesis syndrome, morbid obesity, irritable bowel syndrome, functional dyspepsia and gastroesophageal reflux disease. To better understand the gastrointestinal pacing, a review of its effects and mechanism is presented in this series of papers.
ABSTRACT
Current scintigraphic tests of gastrointestinal motor function provides relevant pathophysiologic information, but their clinical utility is controversial. Many scintigraphic methods are developed to investigate gastrointestinal motility from oral cavity to colon. These are esophageal transit scintigraphy, oropharyngeal transit study, gastric emptying test, small bowel transit time measurement, colon transit study and gastroesopahgeal reflux scintigraphy. Scintigraphy of gastrointestinal tract is the most physiologic and noninvasive method to evaluate gastrointestinal motility disorders. Stomach emptying test is regarded as a gold standard in motility study. Gastrointestinal transit scintigraphy also has a certain role in assessment of drug effect to GI motility and changes after therapy of motility disorders. Scintigraphy provides noninvasive and quantitative assessment of physiological transit throughout the gastrointestinal tract, and it is extremely useful for diagnosing gastrointestinal motor dysfunction. This article reviews the current procedures, indications, significance and guidelines for gastrointestinal motility measurements by scintigraphy.