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Apichart Suksamrarn - One of the best experts on this subject based on the ideXlab platform.

  • inhibitory effects of Choleretic hydroxyacetophenones on ileal bile acid transport in rats
    Life Sciences, 2006
    Co-Authors: Jainuch Kanchanapoo, Apichart Suksamrarn, Mrinalini C Rao, Samaisukh Sophasan, Pawinee Piyachaturawat
    Abstract:

    The effects of the Choleretic and cholesterol lowering compound, 2,4,6-trihydroxyacetophenone (THA) and its analog, 2,6-dihydroxyacetophenone (DHA), on ileal bile acid absorption were investigated in rats. THA inhibited taurocholate (TC) uptake into ileal brush-border membrane vesicles (BBMV), showing a maximum inhibition of 50%, whereas DHA completely inhibited TC uptake into ileal BBMV. THA exhibited competitive inhibition with a Ki of 9.88 mM, while DHA showed non-competitive inhibition with a Ki of 7.65 mM. Both total and ouabain-sensitive basolateral membrane (BLM) Na+-K+-ATPase activities, which are essential for maintenance of the Na+-gradient for bile acid transport, were inhibited by THA and DHA in a dose-dependent manner. The inhibition of BLM ATPase was uncompetitive with a Ki of 10.1 and 5.0 mM for THA and DHA, respectively. Administration of THA or DHA (400 micromol/kg) twice a day, to hypercholesterolemic rats for 3 weeks caused similar and marked reductions in plasma cholesterol to 60% of the cholesterol-fed controls. The data suggest that the inhibitory actions of THA and DHA on two essential components of ileal bile acid recycling to liver could, in part, contribute to the cholesterol lowering effect of the hydroxyacetophenone compounds. These effects on decreasing bile acid recycling, in combination with their potent Choleretic effect, accelerating biliary excretion of bile acids, are responsible for the effective cholesterol lowering capacities of these compounds.

  • cholesterol lowering effects of a Choleretic phloracetophenone in hypercholesterolemic hamsters
    European Journal of Pharmacology, 2002
    Co-Authors: Pawinee Piyachaturawat, Aporn Chuncharunee, Prayad Komaratat, Pornpikul Srivoraphan, Apichart Suksamrarn
    Abstract:

    The plasma cholesterol-lowering effect and mechanism thereof of a Choleretic phloracetophenone or 2,4,6-trihydroxyacetophenone (THA) were investigated in hypercholesterolemic male hamsters. Intragastric administration of THA (300-600 micromol/kg) twice a day for 7 days to these animals caused a dose- and time-dependent decrease in both plasma cholesterol and triglyceride levels. THA at a dose of 400 micromol/kg reduced the cholesterol and triglyceride levels in plasma to 52% and 25% of the level in corresponding cholesterol-fed controls, respectively, with decreases in both plasma very low density lipoprotein and low density lipoprotein cholesterol but not in high density lipoprotein cholesterol. THA did not significantly alter total hepatic cholesterol content but significantly increased the excretion of both bile acids and cholesterol into the intestinal lumen for elimination. Corresponding to the increase in bile acid excretion, THA caused a seven-fold increase in hepatic cholesterol 7alpha-hydroxylase activity. These results suggest that THA exerts its cholesterol lowering effect by increasing hepatic cholesterol 7alpha-hydroxylase activity which increases hepatic conversion of cholesterol to bile acid for disposal via biliary secretion. This compound may have a potential for future development as a therapeutic agent for lowering lipids in hypercholesterolemic patients.

  • evaluation of the acute and subacute toxicity of a Choleretic phloracetophenone in experimental animals
    Toxicology Letters, 2002
    Co-Authors: Pawinee Piyachaturawat, Aporn Chuncharunee, Prayad Komaratat, Chatsuda Tubtim, Apichart Suksamrarn
    Abstract:

    Abstract Toxicity of a Choleretic compound, phloracetophenone (2,4,6-trihydroxyacetophenone; THA) was investigated in mice, rats and hamsters. Acute toxicity of THA was observed to be dependent on species and route of administration, but not sex and age. LD50 values for an acute toxicity of a single i.p. administration to adult male hamsters and mice were 338 and 365 mg/kg BW, respectively. It was significantly increased to 489 mg/kg BW in adult male rats and greatly increased by i.g. route. Subacute toxicity was investigated in adult male mice by giving THA at a doses of 37–300 mg/kg BW/day, i.g. for 30 consecutive days. High doses of THA induced periportal hepatocyte degeneration whereas plasma concentrations of alanine and aspartate aminotransferases, bilirubin, and blood urea nitrogen, and hepatic triglyceride content were only slightly increased. The possible therapeutic effect of the Choleretic THA was evaluated in the ethinylestradiol (EE)-induced cholestasis. THA enhanced the hepatic clearance of sulfobromophthalein and decreased the elevated plasma alkaline phosphatase in EE-cholestatic rats to control levels. These results suggested that THA at biologically active Choleretic dose had low toxicity, it might be safe for further development as a therapeutic agent for a short period of treatment in cholestasis.

  • Choleretic activity of phloracetophenone in rats structure function studies using acetophenone analogues
    European Journal of Pharmacology, 2000
    Co-Authors: Pawinee Piyachaturawat, Nitjagan Chaingam, Aporn Chuncharunee, Prayad Komaratat, Apichart Suksamrarn
    Abstract:

    The relationship between the chemical structure and Choleretic activity of phloracetophenone (2,4,6-trihydroxyacetophenone) was investigated in adult male rats. Fourteen acetophenone analogues, with different substituents on the benzene nucleus, were intraduodenally administered and bile samples were collected via a bile fistula. All of the compounds tested immediately induced choleresis. For the same number of substituents on the benzene ring, hydroxy analogues induced a greater choleresis. The number and position of hydroxy substituents on the benzene nucleus play an important role in determining Choleretic activity and biliary secretion of bile acid, but had no relation to biliary excretion of cholesterol. The Choleretic activity of the hydroxylated compounds was inversely related to hydrophobicity, as inferred by thin-layer chromatography (TLC). Among the hydroxylated acetophenone analogues, 2,4,6-trihydroxyacetophenone was identified as the most potent, with a Choleretic activity of 231.8+/-6.1 microl/mmol/min. It induced both a high bile flow rate and a high bile salt output and led to lower plasma cholesterol levels. This bile had a low lithogenic potential. The results suggest that a structural requirement for high Choleretic activity of 2,4,6-trihydroxyacetophenone is a substituent hydroxy group at 4-position. Additional hydroxy groups at 2- and 6-positions are essential for the induction of higher an output of bile acid, and possibly, other solid materials.

  • a phloracetophenone glucoside with Choleretic activity from curcuma comosa
    Phytochemistry, 1997
    Co-Authors: Apichart Suksamrarn, Pawinee Piyachaturawat, Salinee Eiamong, Lindsay T Byrne
    Abstract:

    Abstract Three known diarylheptanoids, 1,7-diphenyl-5-hydroxy-(1E)-1-heptene, 5-hydroxy-7-(4-hydroxyphenyl)-1-phenyl-(1E)-1-heptene and 7-(3,4-dihydroxyphenyl)-5-hydroxy-1-phenyl-(1E)-1-heptene, were isolated from the ethyl acetate extract of Curcuma comosa rhizomes. A phloracetophenone glucoside, 4,6- dihydroxy -2-O-(β- d -glucopyranosyl)acetophenone , was isolated from the ethyl acetate and n-butanol extracts. This compound exhibited Choleretic activity in rats.

Pawinee Piyachaturawat - One of the best experts on this subject based on the ideXlab platform.

  • inhibitory effects of Choleretic hydroxyacetophenones on ileal bile acid transport in rats
    Life Sciences, 2006
    Co-Authors: Jainuch Kanchanapoo, Apichart Suksamrarn, Mrinalini C Rao, Samaisukh Sophasan, Pawinee Piyachaturawat
    Abstract:

    The effects of the Choleretic and cholesterol lowering compound, 2,4,6-trihydroxyacetophenone (THA) and its analog, 2,6-dihydroxyacetophenone (DHA), on ileal bile acid absorption were investigated in rats. THA inhibited taurocholate (TC) uptake into ileal brush-border membrane vesicles (BBMV), showing a maximum inhibition of 50%, whereas DHA completely inhibited TC uptake into ileal BBMV. THA exhibited competitive inhibition with a Ki of 9.88 mM, while DHA showed non-competitive inhibition with a Ki of 7.65 mM. Both total and ouabain-sensitive basolateral membrane (BLM) Na+-K+-ATPase activities, which are essential for maintenance of the Na+-gradient for bile acid transport, were inhibited by THA and DHA in a dose-dependent manner. The inhibition of BLM ATPase was uncompetitive with a Ki of 10.1 and 5.0 mM for THA and DHA, respectively. Administration of THA or DHA (400 micromol/kg) twice a day, to hypercholesterolemic rats for 3 weeks caused similar and marked reductions in plasma cholesterol to 60% of the cholesterol-fed controls. The data suggest that the inhibitory actions of THA and DHA on two essential components of ileal bile acid recycling to liver could, in part, contribute to the cholesterol lowering effect of the hydroxyacetophenone compounds. These effects on decreasing bile acid recycling, in combination with their potent Choleretic effect, accelerating biliary excretion of bile acids, are responsible for the effective cholesterol lowering capacities of these compounds.

  • cholesterol lowering effects of a Choleretic phloracetophenone in hypercholesterolemic hamsters
    European Journal of Pharmacology, 2002
    Co-Authors: Pawinee Piyachaturawat, Aporn Chuncharunee, Prayad Komaratat, Pornpikul Srivoraphan, Apichart Suksamrarn
    Abstract:

    The plasma cholesterol-lowering effect and mechanism thereof of a Choleretic phloracetophenone or 2,4,6-trihydroxyacetophenone (THA) were investigated in hypercholesterolemic male hamsters. Intragastric administration of THA (300-600 micromol/kg) twice a day for 7 days to these animals caused a dose- and time-dependent decrease in both plasma cholesterol and triglyceride levels. THA at a dose of 400 micromol/kg reduced the cholesterol and triglyceride levels in plasma to 52% and 25% of the level in corresponding cholesterol-fed controls, respectively, with decreases in both plasma very low density lipoprotein and low density lipoprotein cholesterol but not in high density lipoprotein cholesterol. THA did not significantly alter total hepatic cholesterol content but significantly increased the excretion of both bile acids and cholesterol into the intestinal lumen for elimination. Corresponding to the increase in bile acid excretion, THA caused a seven-fold increase in hepatic cholesterol 7alpha-hydroxylase activity. These results suggest that THA exerts its cholesterol lowering effect by increasing hepatic cholesterol 7alpha-hydroxylase activity which increases hepatic conversion of cholesterol to bile acid for disposal via biliary secretion. This compound may have a potential for future development as a therapeutic agent for lowering lipids in hypercholesterolemic patients.

  • evaluation of the acute and subacute toxicity of a Choleretic phloracetophenone in experimental animals
    Toxicology Letters, 2002
    Co-Authors: Pawinee Piyachaturawat, Aporn Chuncharunee, Prayad Komaratat, Chatsuda Tubtim, Apichart Suksamrarn
    Abstract:

    Abstract Toxicity of a Choleretic compound, phloracetophenone (2,4,6-trihydroxyacetophenone; THA) was investigated in mice, rats and hamsters. Acute toxicity of THA was observed to be dependent on species and route of administration, but not sex and age. LD50 values for an acute toxicity of a single i.p. administration to adult male hamsters and mice were 338 and 365 mg/kg BW, respectively. It was significantly increased to 489 mg/kg BW in adult male rats and greatly increased by i.g. route. Subacute toxicity was investigated in adult male mice by giving THA at a doses of 37–300 mg/kg BW/day, i.g. for 30 consecutive days. High doses of THA induced periportal hepatocyte degeneration whereas plasma concentrations of alanine and aspartate aminotransferases, bilirubin, and blood urea nitrogen, and hepatic triglyceride content were only slightly increased. The possible therapeutic effect of the Choleretic THA was evaluated in the ethinylestradiol (EE)-induced cholestasis. THA enhanced the hepatic clearance of sulfobromophthalein and decreased the elevated plasma alkaline phosphatase in EE-cholestatic rats to control levels. These results suggested that THA at biologically active Choleretic dose had low toxicity, it might be safe for further development as a therapeutic agent for a short period of treatment in cholestasis.

  • Choleretic activity of phloracetophenone in rats structure function studies using acetophenone analogues
    European Journal of Pharmacology, 2000
    Co-Authors: Pawinee Piyachaturawat, Nitjagan Chaingam, Aporn Chuncharunee, Prayad Komaratat, Apichart Suksamrarn
    Abstract:

    The relationship between the chemical structure and Choleretic activity of phloracetophenone (2,4,6-trihydroxyacetophenone) was investigated in adult male rats. Fourteen acetophenone analogues, with different substituents on the benzene nucleus, were intraduodenally administered and bile samples were collected via a bile fistula. All of the compounds tested immediately induced choleresis. For the same number of substituents on the benzene ring, hydroxy analogues induced a greater choleresis. The number and position of hydroxy substituents on the benzene nucleus play an important role in determining Choleretic activity and biliary secretion of bile acid, but had no relation to biliary excretion of cholesterol. The Choleretic activity of the hydroxylated compounds was inversely related to hydrophobicity, as inferred by thin-layer chromatography (TLC). Among the hydroxylated acetophenone analogues, 2,4,6-trihydroxyacetophenone was identified as the most potent, with a Choleretic activity of 231.8+/-6.1 microl/mmol/min. It induced both a high bile flow rate and a high bile salt output and led to lower plasma cholesterol levels. This bile had a low lithogenic potential. The results suggest that a structural requirement for high Choleretic activity of 2,4,6-trihydroxyacetophenone is a substituent hydroxy group at 4-position. Additional hydroxy groups at 2- and 6-positions are essential for the induction of higher an output of bile acid, and possibly, other solid materials.

  • a phloracetophenone glucoside with Choleretic activity from curcuma comosa
    Phytochemistry, 1997
    Co-Authors: Apichart Suksamrarn, Pawinee Piyachaturawat, Salinee Eiamong, Lindsay T Byrne
    Abstract:

    Abstract Three known diarylheptanoids, 1,7-diphenyl-5-hydroxy-(1E)-1-heptene, 5-hydroxy-7-(4-hydroxyphenyl)-1-phenyl-(1E)-1-heptene and 7-(3,4-dihydroxyphenyl)-5-hydroxy-1-phenyl-(1E)-1-heptene, were isolated from the ethyl acetate extract of Curcuma comosa rhizomes. A phloracetophenone glucoside, 4,6- dihydroxy -2-O-(β- d -glucopyranosyl)acetophenone , was isolated from the ethyl acetate and n-butanol extracts. This compound exhibited Choleretic activity in rats.

Miao Yang - One of the best experts on this subject based on the ideXlab platform.

  • research on Choleretic effect of menthol menthone pluegone isomenthone and limonene in danshu capsule
    International Immunopharmacology, 2015
    Co-Authors: Guanying Hu, Sanyin Zhang, Ruru Wang, Chunjie Wu, Zhigang Wu, Miao Yang, Xiao Ke
    Abstract:

    Abstract Danshu capsule (DSC) is a medicinal compound in traditional Chinese medicine (TCM). It is commonly used for the treatment of acute & chronic cholecystitis as well as choleithiasis. To study its Choleretic effect, healthy rats were randomly divided into DSC high (DSCH, 900 mg/kg), medium (DSCM, 450 mg/kg), and low (DSCL, 225 mg/kg) group, Xiaoyan Lidan tablet (XYLDT, 750 mg/kg), and saline group. The bile was collected for 1 h after 20-minute stabilization as the base level, and at 1 h, 2 h, 3 h, and 4 h after drug administration, respectively. Bile volume, total cholesterol, and total bile acid were measured at each time point. The results revealed that DSC significantly stimulated bile secretion, decreased total cholesterol level and increased total bile acid level. Therefore, it had Choleretic effects. To identify the active components contributing to its Choleretic effects, five major constituents which are menthol (39.33 mg/kg), menthone (18.02 mg/kg), isomenthone (8.18 mg/kg), pluegone (3.31 mg/kg), and limonene (4.39 mg/kg) were tested on our rat model. The results showed that menthol and limonene could promote bile secretion when compared to DSC treatment ( p > 0.05); Menthol, menthol and limonene could significantly decrease total cholesterol level ( p p p p

  • research on Choleretic effect of menthol menthone pluegone isomenthone and limonene in danshu capsule
    International Immunopharmacology, 2015
    Co-Authors: Xing Yuan, Sanyin Zhang, Ruru Wang, Miao Yang
    Abstract:

    Danshu capsule (DSC) is a medicinal compound in traditional Chinese medicine (TCM). It is commonly used for the treatment of acute & chronic cholecystitis as well as choleithiasis. To study its Choleretic effect, healthy rats were randomly divided into DSC high (DSCH, 900mg/kg), medium (DSCM, 450mg/kg), and low (DSCL, 225mg/kg) group, Xiaoyan Lidan tablet (XYLDT, 750mg/kg), and saline group. The bile was collected for 1h after 20-minute stabilization as the base level, and at 1h, 2h, 3h, and 4h after drug administration, respectively. Bile volume, total cholesterol, and total bile acid were measured at each time point. The results revealed that DSC significantly stimulated bile secretion, decreased total cholesterol level and increased total bile acid level. Therefore, it had Choleretic effects. To identify the active components contributing to its Choleretic effects, five major constituents which are menthol (39.33mg/kg), menthone (18.02mg/kg), isomenthone (8.18mg/kg), pluegone (3.31mg/kg), and limonene (4.39mg/kg) were tested on our rat model. The results showed that menthol and limonene could promote bile secretion when compared to DSC treatment (p > 0.05); Menthol, menthol and limonene could significantly decrease total cholesterol level (p<0.05 or p<0.01) as well as increase total bile acid level (p<0.05 or p<0.01); Isomenthone, as a isomer of menthone, existed slightly Choleretic effects; Pluegone had no obvious role in bile acid efflux. These findings indicated that the Choleretic effects of DSC may be attributed mainly to its three major constituents: menthol, menthone and limonene.

Brigitte Kopp - One of the best experts on this subject based on the ideXlab platform.

  • distribution of phenolic compounds in middleeuropean taxa of the achillea millefolium l aggregate
    Chemistry & Biodiversity, 2007
    Co-Authors: Birgit Benedek, Noela Gjoncaj, Johannes Saukel, Brigitte Kopp
    Abstract:

    Achillea millefolium L. s.l. is a cytogenetically, morphologically, and chemically polymorphic aggregate. Besides the sesquiterpenes that possess chemotaxonomic relevance and mediate the antiphlogistic activity, the plant contains phenolic compounds such as dicaffeoylquinic acids and flavonoids causing Choleretic and spasmolytic effects. To evaluate their contribution to the chemotaxonomy of European taxa of the A. millefolium group, we developed a SPE-HPLC/UV method that allows quantification of the phenolic constituents in the different taxa. The investigated species displayed differences in the quantitative and qualitative composition of phenolic acids and flavonoids. Hence, they seem to be of chemotaxonomic significance, especially for the distinction of the diploid taxa. Combining the obtained results with the data of the sesquiterpene analyses gives a comprehensive insight into the distribution of those pharmacologically relevant plant constituents in the A. millefolium group.

  • achillea millefolium l s l revisited recent findings confirm the traditional use
    Wiener Medizinische Wochenschrift, 2007
    Co-Authors: Birgit Benedek, Brigitte Kopp
    Abstract:

    Yarrow (Achillea millefolium L. s.l.) is traditionally used in the treatment of inflammatory and spasmodic gastro-intestinal disorders, hepato-biliary complaints and inflammation. Now we could show that the flavonoids mediated the antispasmodic properties of yarrow, whereas the dicaffeoylquinic acids caused the Choleretic effects. Moreover, we observed an in vitro-inhibition of human neutrophil elastase, a protease involved in the inflammatory process, by extracts and fractions from yarrow, which suggests additional mechanisms of antiphlogistic action. The presented results confirm the traditional use of yarrow.

  • Choleretic effects of yarrow achillea millefolium s l in the isolated perfused rat liver
    Phytomedicine, 2006
    Co-Authors: B Benedek, N Geisz, Walter Jager, Theresia Thalhammer, Brigitte Kopp
    Abstract:

    Different species from the Achillea millefolium aggregate are used against gastrointestinal and hepato-biliary disorders in traditional European medicine. In this work, a fraction enriched in dicaffeoylquinic acids (DCCAs) and luteolin-7-O-β-d-glucuronide was investigated on its Choleretic effect in the isolated perfused rat liver (IPRL) compared to cynarin (1,3-DCCA), the main Choleretic compound of Cynara scolymus L. A fraction containing 3,4-, 3,5- and 4,5-DCCA and luteolin-7-O-β-d-glucuronide was prepared by solid phase extraction from a 20% methanolic extract of yarrow. A total amount of 48.8% DCCAs and 3.4% luteolin-7-O-β-d-glucuronide was determined by HPLC analysis with cynarin as internal standard. IPRL experiments revealed a dose-dependant increase in bile flow (23–44–47%) by the Achillea fraction. Choleresis was two- to three-fold higher than that of cynarin. The combined effect of DCCAs and luteolin-7-O-β-d-glucuronide stimulated bile flow more effectively than the single compound cynarin. Due to their polar structure, these compounds are quantitatively extracted into teas and tinctures; hence, they seem to be the Choleretic active principles in the traditional application forms of yarrow.

  • Choleretic effects of yarrow achillea millefolium s l in the isolated perfused rat liver
    Phytomedicine, 2006
    Co-Authors: B Benedek, N Geisz, Walter Jager, Theresia Thalhammer, Brigitte Kopp
    Abstract:

    Different species from the Achillea millefolium aggregate are used against gastrointestinal and hepato-biliary disorders in traditional European medicine. In this work, a fraction enriched in dicaffeoylquinic acids (DCCAs) and luteolin-7-O-beta-D-glucuronide was investigated on its Choleretic effect in the isolated perfused rat liver (IPRL) compared to cynarin (1,3-DCCA), the main Choleretic compound of Cynara scolymus L. A fraction containing 3,4-, 3,5- and 4,5-DCCA and luteolin-7-O-beta-D-glucuronide was prepared by solid phase extraction from a 20% methanolic extract of yarrow. A total amount of 48.8% DCCAs and 3.4% luteolin-7-O-beta-D-glucuronide was determined by HPLC analysis with cynarin as internal standard. IPRL experiments revealed a dose-dependant increase in bile flow (23-44-47%) by the Achillea fraction. Choleresis was two- to three-fold higher than that of cynarin. The combined effect of DCCAs and luteolin-7-O-beta-D-glucuronide stimulated bile flow more effectively than the single compound cynarin. Due to their polar structure, these compounds are quantitatively extracted into teas and tinctures; hence, they seem to be the Choleretic active principles in the traditional application forms of yarrow.

B N Dhawan - One of the best experts on this subject based on the ideXlab platform.

  • Choleretic effect of andrographolide in rats and guinea pigs
    Planta Medica, 1992
    Co-Authors: Binduja Shukla, P K S Visen, G K Patnaik, B N Dhawan
    Abstract:

    Andrographolide from the herb Andrographis paniculata (whole plant) per se produces a significant dose (1.5-12 mg/kg) dependent Choleretic effect (4.8-73%) as evidenced by increase in bile flow, bile salt, and bile acids in conscious rats and anaesthetized guinea pigs. The paracetamol induced decrease in volume and contents of bile was prevented significantly by andrographolide pretreatment. It was found to be more potent than silymarin, a clinically used hepatoprotective agent.

  • Choleretic effect of picroliv the hepatoprotective principle of picrorhiza kurroa
    Planta Medica, 1991
    Co-Authors: Binduja Shukla, P K S Visen, G K Patnaik, B N Dhawan
    Abstract:

    Picroliv, the hepatoprotective principle of the plant Picrorhiza kurroa, showed a dose-dependent (1.5-12 mg/kg x 7) Choleretic effect in conscious rats and anaesthetised guinea pigs. It also possessed a marked anticholestatic effect against paracetamol- and ethynylestradiol-induced cholestasis. It antagonised the changes in bile volume as well as the contents (bile salts and bile acids). Silymarin, a known hepatoprotective agent, was tested simultaneously for comparison. Picroliv was found to be a more potent Choleretic and anticholestatic agent than silymarin.