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Background OC26 and its pro-drug BOC26P, both ortho-aryl chalcone compounds, showed a well-definedantitumor activity in various cancer cells especially in drug-resistant tumor cell lines.Aim The purpose of this study was to investigate the bile excretion characteristics of OC26 after OC26 and BOC26Padministered in rats respectively.Method An ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) method wasdeveloped and validated for OC26 in rat bile. Liquid-liquid extraction with ethyl acetate method was use to pretreatthe bile samples. After that, a gradient mobile phase at a flow rate 0.5mL/min of acetonitrile and 2mM CH3COONH4with 0.1% aqueous ammonia solution (v/v) and the positive ion alternate mode separated and quantified OC26.Bile samples were collected from rats after intravenous injection (i.v) 12.5mg/kg of OC26 and BOC26P, respectively.Results For method validation, the method showed high extraction recovery. The assay showed a good linearitywith correlation coefficient >0.99 at the concentration ranges of 20-2000ng/mL. All data were within the requiredlimits. The bile excretion results showed that the excretion amount of OC26 was gradually stabilized after 2h. Theaccumulative excretion percentage of OC26 after i.v 12.5mg/kg BOC26P was significantly higher than that of OC26after i.v 12.5mg/kg OC26. Significant gender differences were also observed in bile excretion of OC26.Conclusion This method was selective, sensitive and reliable and successfully applied to the bile excretion of OC26.This study provided theoretical basis for OC26 further research.
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ObjectiveTo investigate the effect of Pien Tze Huang on bile excretion and its analgesic effect in experimental animals. MethodsA total of 30 guinea pigs were randomly divided into Pien Tze Huang group, ursodeoxycholic acid group, and control group. According to body mass, the three groups were treated with Pien Tze Huang (140 mg/kg), ursodeoxycholic acid (22.5 mg/kg), and normal saline, respectively, by gavage for 4 consecutive days. Then bile drainage was performed to measure the volume of bile secretion and the change in bile composition. Related liver function parameters were also measured. A total of 30 mice were randomly divided into Pien Tze Huang group (360 mg/kg), ursodeoxycholic acid group (120 mg/kg), and control group. At one hour after the last administration, the mice were given intraperitoneal injection of 0.6% glacial acetic acid (0.15 ml/10 g), and the writhing test was performed to observe the analgesic effect of Pien Tze Huang. A one-way analysis of variance was used for comparison of continuous data between multiple groups, and the least significant difference t-test was used for further comparison between two groups. ResultsCompared with the control group, the Pien Tze Huang group and the ursodeoxycholic acid group had a significant increase in the volume of bile secretion (P=0.039 and 0.009). There were no significant differences between the three groups in cholesterol, bilirubin, total bile acid, and phospholipid in bile (all P＞0.05) and liver function parameters (alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transpeptidase, total bilirubin, direct bilirubin, indirect bilirubin, and total bile acid) (all P＞0.05). Compared with the control group, the Pien Tze Huang group had a significant reduction in the number of writhing times (P＜0.001), suggesting that Pien Tze Huang had a marked analgesic effect. ConclusionAnimal experiments show that Pien Tze Huang has marked choleretic and analgesic effects, which provides theoretical and data support for the clinical application of Pien Tze Huang.
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ObjectiveTo investigate the effect of Pien Tze Huang on bile excretion and its analgesic effect in experimental animals. MethodsA total of 30 guinea pigs were randomly divided into Pien Tze Huang group, ursodeoxycholic acid group, and control group. According to body mass, the three groups were treated with Pien Tze Huang (140 mg/kg), ursodeoxycholic acid (22.5 mg/kg), and normal saline, respectively, by gavage for 4 consecutive days. Then bile drainage was performed to measure the volume of bile secretion and the change in bile composition. Related liver function parameters were also measured. A total of 30 mice were randomly divided into Pien Tze Huang group (360 mg/kg), ursodeoxycholic acid group (120 mg/kg), and control group. At one hour after the last administration, the mice were given intraperitoneal injection of 0.6% glacial acetic acid (0.15 ml/10 g), and the writhing test was performed to observe the analgesic effect of Pien Tze Huang. A one-way analysis of variance was used for comparison of continuous data between multiple groups, and the least significant difference t-test was used for further comparison between two groups. ResultsCompared with the control group, the Pien Tze Huang group and the ursodeoxycholic acid group had a significant increase in the volume of bile secretion (P=0.039 and 0.009). There were no significant differences between the three groups in cholesterol, bilirubin, total bile acid, and phospholipid in bile (all P＞0.05) and liver function parameters (alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transpeptidase, total bilirubin, direct bilirubin, indirect bilirubin, and total bile acid) (all P＞0.05). Compared with the control group, the Pien Tze Huang group had a significant reduction in the number of writhing times (P＜0.001), suggesting that Pien Tze Huang had a marked analgesic effect. ConclusionAnimal experiments show that Pien Tze Huang has marked choleretic and analgesic effects, which provides theoretical and data support for the clinical application of Pien Tze Huang.
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AIM: To illustrate the effects of drug transporters on the bile efflux of ibuprofen glucuronide(IBG), the difference of bile excretion and plasma concentration of ibuprofen(IB) and its glucuronides was studied in EHBR and normal SD rat(SDR). METHODS: After 20 mg/kg of IB enantiomers administrated intravenously, the bile and blood were collected from the rats and the concentration of IB and their glucuronide were measured by HPLC methods. RESULTS: The bile excretion of IBG was obviously (but no totally) suppressed in EHBR (1.7%±1.0%, 0.6%±0.9% of the dose respectively for S-IBG and R-IBG) compared with that in SDR (18.4%±4.0% and 3.0%±2.4% of the dose respectively for S-IBG and R-IBG), for both kinds of rats, there are more S-IBG excreted than that of R-IBG. As the result of reduction of IBG excreted in bile, the concentration of IBG was higher in blood in EHBRs. CONCLUSION: The results suggest that Mrp2 is the most important transporter for IBG, and other transporter(s) may participate in the process.
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PURPOSE: For good quality of myocardial perfusion images, an approximately 30 min to 1 hour of waiting time after radiopharmaceutical injection and ingestion of fatty meal are asked of the patients. The aim of this study was to investigate the shortening of waiting time after radiopharmaceutical injection and improvement of image quality using natural plant extracts that promote bile excretion. MATERIALS AND METHODS: Ten volunteers participated in protocol 1 (7 men, 3 women; mean age, 24.1+/-2.4 years) and protocol 2 (8 men, 2 women; mean age, 26.1+/-2.9 years), respectively. For the modified method of both protocols, subjects took natural plant extracts 15 minutes before the first injection of 99mTc MIBI without taking fatty meals. Control (Conventional) methods were performed with intake of a fatty meal 20 to 30 minutes after 99mTc MIBI injection. RESULTS: As the results of protocol 1 and 2, the ratio of myocardial to lung ratio were not different between modified and conventional method. Liver to lung ratio of modified method showed significantly lower value than that of conventional method. In modified method, myocardial to liver ratio was higher persistently. In protocol 2, natural plant extracts took before the first injection of 99mTc MIBI exerted accelerating effect of excretion of bile juice into intestine until the end of examination. CONCLUSION: These results represent that natural plant extracts for facilitation of bile excretion before injection of 99mTc MIBI may provide better quality of myocardial perfusion images without the need for preparations such as ingestion of fatty meal within the 2 hours compared with conventional method.