AIM: To investigate the therapeutic effect of traditional Chinese traditional medicines Da Cheng Qi Decoction (Timely-Purging and Yin-Preserving Decoction) and Glauber's salt combined with conservative measures on...AIM: To investigate the therapeutic effect of traditional Chinese traditional medicines Da Cheng Qi Decoction (Timely-Purging and Yin-Preserving Decoction) and Glauber's salt combined with conservative measures on abdominal compartment syndrome (ACS) in severe acute pancreatitis (SAP) patients. METHODS: Eighty consecutive SAP patients, admitted for routine non-operative conservative treatment, were randomly divided into study group and control group (40 patients in each group). Patients in the study group received Da Cheng Qi Decoction enema for 2 h and external use of Glauber's salt, once a day for 7 d. Patients in the control group received normal saline (NS) enema. Routine non-operative conservative treatments included non-per os nutrition (NPON), gastrointestinal decompression, life support, total parenteral nutrition (TPN), continuous peripancreatic vascular pharmaceutical infusion and drug therapy. Intra-cystic pressure (ICP) of the two groups was measured during treatment. The effectiveness and outcomes of treatment were observed and APACHE Ⅱ scores were applied in analysis. RESULTS: On days 4 and 5 of treatment, the ICP was lower in the study group than in the control group(P < 0.05). On days 3-5 of treatment, acute physiology and chronic health evaluation Ⅱ (APACHE Ⅱ) scores for the study and control groups were significantly different (P < 0.05). Both the effectiveness and outcome of the treatment with Da Cheng Qi Decoction on abdominalgia, burbulence relief time, ascites quantity, cyst formation rate and hospitalization time were quite different between the two groups (P < 0.05). The mortality rate for the two groups had no significant difference. CONCLUSION: Da Cheng Qi Decoction enema and external use of Glauber's salt combined with routine non-operative conservative treatment can decrease the intra-abdominal pressure (IAP) of SAP patients and have preventive and therapeutic effects on abdominal compartment syndrome of SAP.展开更多
Increasing attention is being paid to the scientific evaluation of traditional Chinese medicine （TCM）. As many TCMs are capable of biotransformation in the gastrointestinal tract, attention to biotransforrnation of ...Increasing attention is being paid to the scientific evaluation of traditional Chinese medicine （TCM）. As many TCMs are capable of biotransformation in the gastrointestinal tract, attention to biotransforrnation of TCM in the gastrointestinal tract may lead to discovery of the active components and active mechanisms. In this article, we review reports that host metabolic enzymes and intestinal bacteria may be responsible for the metabolism of TCM. Good understanding of the in vivo course of TCM will help us to know how to conduct metabolism evaluation of TCM by using in vitro human-derived system. This evaluation system will create new views on TCM as effective and safe therapeutic agents.展开更多
Prevalence of dislipidemia is increasing rapidly in China and there has been a growing interest in Chinese herbal medicine for the treatment of hyperlipidemia both inside and outside China. In this article, lipids reg...Prevalence of dislipidemia is increasing rapidly in China and there has been a growing interest in Chinese herbal medicine for the treatment of hyperlipidemia both inside and outside China. In this article, lipids regulating effects of 9 herbs or their extracts and 5 herbal formulae which have been published in English-language literature are reviewed. Although evidence from animals and humans consistently supports the therapeutic activities of these Chinese herbal medicines, few multi-center large-scale clinical trials have been conducted to confirm the efficacy and evaluate their safety.展开更多
Objective To explore the velocity-effect relationship in order to the establish linearization of effect on an equation with regard to the consistency of the Hill dose-effect expression with the metabolic kinetics of r...Objective To explore the velocity-effect relationship in order to the establish linearization of effect on an equation with regard to the consistency of the Hill dose-effect expression with the metabolic kinetics of receptors.Methods The linear velocity-effect expression was obtained by solving multivariant differential equation groups,which were established to compare the coincidences and basic relations between the Hill dose-effect and metabolic kinetic Michaelis-Menten equation for receptors.The validation test was conducted with acetylcholine,adrenaline,and their mixture as model drugs.Results The linear velocity-effect modelling was represented in vivo or in vitro,for single and multidrug systems.Pharmacodynamic parameters,especially suitable for multicomponent CMM formulas,could be determined and calculated for single or multicomponent formulas at high saturating or low linear concentration for receptors.The validation test showed that the pharmacodynamic parameters of acetylcholine were:k,2.675×10^-3s^-1;ka,5.786×10^-9s^-1;km,2.500×10^-7s^-1;α,4.619×10^9张s·mg^-1;E0,13张(P<0.01)and those of adrenaline were:k,1.415×10^-3s^-1;ka,5.846×10^-9s^-1;km,2.300×10^-7s^-1;α,-1.627×10^9张s·m g^-1;E0,9.2张(P<0.01).For the mixture of the two components,the values were:α,1.375×1010张s·m g^-1;-6.150×10^9张s m g^-1for acetylcholine and adrenaline,respectively,and E0was7.08张in both,with the other parameters unchanged(P<0.01).Conclusion The velocity-effect equation can linearize the Hill dose-effect relationship,which can be applied to study the pharmacodynamics and availability of CMM formulations in vivo and in vitro.展开更多
A comparison of the pharmacodynamic effects of two source plants of Murrayae Folium et Cacumen(MFC),Murraya exotica L.and Murraya paniculata(L.)Jack,was performed in order to supply reference for its multi-source rati...A comparison of the pharmacodynamic effects of two source plants of Murrayae Folium et Cacumen(MFC),Murraya exotica L.and Murraya paniculata(L.)Jack,was performed in order to supply reference for its multi-source rationality and interchangeability in clinical practice.According to the traditional efficacy of MFC,the effects of promoting Qi,relieving pain,promoting blood circulation and removing blood stasis were systematically evaluated by the models of writhing response in mice,foot swelling in rats,gastric emptying and small intestine propulsion in mice,and acute blood stasis in rats,respectively.The results showed that both M.exotica and M.paniculata could significantly inhibit the writhing reaction induced by acetic acid in mice and the paw swelling induced by carrageenan in rats,reduce IL-6,TNF-αand PGE2 levels in plasma of paw-swelling rats and increase gastric empty rate and intestinal propulsive rate.The above-mentioned effects were dose-dependent,and there was no significant difference between M.exotica and M.paniculata at the same doses.Therefore,M.exotica and M.paniculata had the similar anti-inflammatory,analgesic and gastrointestinal motility promotion effects,which provided a support for the pharmacodynamic equivalence of the multi-source plants of MFC.展开更多
Multidrug resistance-associated proteins （MRPs） can effiux structurally diverse drugs, drug conjugates, drug metabolites, as well as other small molecules out of the cells, and this is the main cause of producing mu...Multidrug resistance-associated proteins （MRPs） can effiux structurally diverse drugs, drug conjugates, drug metabolites, as well as other small molecules out of the cells, and this is the main cause of producing multidrug resistance （MDR） of some anticaneer drugs. Therefore, it is crucial to uncover the molecular features of MRPs substrates in developing anti-MDR cancer therapy. In the present study, common feature pharmacophore models were developed by employing CATALYST Pharmacophore Modeling and Analysis tools using substrates of MRPs, including MRP1, -2, -3, -4, -5, -6, -8 and MRPs family, respectively. The models were validated using independent decoy sets generated in DUD-E, and the ones with best A UC （area under the curve） scores were chosen to predict endogenous substrates by screening the Human Metabolome Database （HMDB）. A number of molecules obtained by pharmacophore screening have been validated in the literatures. By comparing physical properties （ALOGP, Molecular_PolarSurfaceArea, Molecular_Volume, Molecular_Weight, Num H Acceptors, Num H Donors） and scaffold features of the screened candidates with the known substrates, we found that： 1） The two sets have consistent ALOGP, Molecule_Volume and Molecule_Weight distribution trend; 2） Substrates of MRP1 have a better lipophilicity than the other subtypes, which is consistent with the two hydrophobic centers on the MRP1 pharmacophore; 3） In the aspect of the scaffold structures, they have the identical or similar backbone fragments.展开更多
文摘AIM: To investigate the therapeutic effect of traditional Chinese traditional medicines Da Cheng Qi Decoction (Timely-Purging and Yin-Preserving Decoction) and Glauber's salt combined with conservative measures on abdominal compartment syndrome (ACS) in severe acute pancreatitis (SAP) patients. METHODS: Eighty consecutive SAP patients, admitted for routine non-operative conservative treatment, were randomly divided into study group and control group (40 patients in each group). Patients in the study group received Da Cheng Qi Decoction enema for 2 h and external use of Glauber's salt, once a day for 7 d. Patients in the control group received normal saline (NS) enema. Routine non-operative conservative treatments included non-per os nutrition (NPON), gastrointestinal decompression, life support, total parenteral nutrition (TPN), continuous peripancreatic vascular pharmaceutical infusion and drug therapy. Intra-cystic pressure (ICP) of the two groups was measured during treatment. The effectiveness and outcomes of treatment were observed and APACHE Ⅱ scores were applied in analysis. RESULTS: On days 4 and 5 of treatment, the ICP was lower in the study group than in the control group(P < 0.05). On days 3-5 of treatment, acute physiology and chronic health evaluation Ⅱ (APACHE Ⅱ) scores for the study and control groups were significantly different (P < 0.05). Both the effectiveness and outcome of the treatment with Da Cheng Qi Decoction on abdominalgia, burbulence relief time, ascites quantity, cyst formation rate and hospitalization time were quite different between the two groups (P < 0.05). The mortality rate for the two groups had no significant difference. CONCLUSION: Da Cheng Qi Decoction enema and external use of Glauber's salt combined with routine non-operative conservative treatment can decrease the intra-abdominal pressure (IAP) of SAP patients and have preventive and therapeutic effects on abdominal compartment syndrome of SAP.
文摘Increasing attention is being paid to the scientific evaluation of traditional Chinese medicine （TCM）. As many TCMs are capable of biotransformation in the gastrointestinal tract, attention to biotransforrnation of TCM in the gastrointestinal tract may lead to discovery of the active components and active mechanisms. In this article, we review reports that host metabolic enzymes and intestinal bacteria may be responsible for the metabolism of TCM. Good understanding of the in vivo course of TCM will help us to know how to conduct metabolism evaluation of TCM by using in vitro human-derived system. This evaluation system will create new views on TCM as effective and safe therapeutic agents.
文摘Prevalence of dislipidemia is increasing rapidly in China and there has been a growing interest in Chinese herbal medicine for the treatment of hyperlipidemia both inside and outside China. In this article, lipids regulating effects of 9 herbs or their extracts and 5 herbal formulae which have been published in English-language literature are reviewed. Although evidence from animals and humans consistently supports the therapeutic activities of these Chinese herbal medicines, few multi-center large-scale clinical trials have been conducted to confirm the efficacy and evaluate their safety.
基金funding support from the National Natural Science Foundation of China (No. 81073142 and No. 30901971)
文摘Objective To explore the velocity-effect relationship in order to the establish linearization of effect on an equation with regard to the consistency of the Hill dose-effect expression with the metabolic kinetics of receptors.Methods The linear velocity-effect expression was obtained by solving multivariant differential equation groups,which were established to compare the coincidences and basic relations between the Hill dose-effect and metabolic kinetic Michaelis-Menten equation for receptors.The validation test was conducted with acetylcholine,adrenaline,and their mixture as model drugs.Results The linear velocity-effect modelling was represented in vivo or in vitro,for single and multidrug systems.Pharmacodynamic parameters,especially suitable for multicomponent CMM formulas,could be determined and calculated for single or multicomponent formulas at high saturating or low linear concentration for receptors.The validation test showed that the pharmacodynamic parameters of acetylcholine were:k,2.675×10^-3s^-1;ka,5.786×10^-9s^-1;km,2.500×10^-7s^-1;α,4.619×10^9张s·mg^-1;E0,13张(P<0.01)and those of adrenaline were:k,1.415×10^-3s^-1;ka,5.846×10^-9s^-1;km,2.300×10^-7s^-1;α,-1.627×10^9张s·m g^-1;E0,9.2张(P<0.01).For the mixture of the two components,the values were:α,1.375×1010张s·m g^-1;-6.150×10^9张s m g^-1for acetylcholine and adrenaline,respectively,and E0was7.08张in both,with the other parameters unchanged(P<0.01).Conclusion The velocity-effect equation can linearize the Hill dose-effect relationship,which can be applied to study the pharmacodynamics and availability of CMM formulations in vivo and in vitro.
基金National Natural Science Foundation of China(Grant Nos.81773864,81473106)National Key R&D Program of China(Grant No.2019YFC1711000)。
文摘A comparison of the pharmacodynamic effects of two source plants of Murrayae Folium et Cacumen(MFC),Murraya exotica L.and Murraya paniculata(L.)Jack,was performed in order to supply reference for its multi-source rationality and interchangeability in clinical practice.According to the traditional efficacy of MFC,the effects of promoting Qi,relieving pain,promoting blood circulation and removing blood stasis were systematically evaluated by the models of writhing response in mice,foot swelling in rats,gastric emptying and small intestine propulsion in mice,and acute blood stasis in rats,respectively.The results showed that both M.exotica and M.paniculata could significantly inhibit the writhing reaction induced by acetic acid in mice and the paw swelling induced by carrageenan in rats,reduce IL-6,TNF-αand PGE2 levels in plasma of paw-swelling rats and increase gastric empty rate and intestinal propulsive rate.The above-mentioned effects were dose-dependent,and there was no significant difference between M.exotica and M.paniculata at the same doses.Therefore,M.exotica and M.paniculata had the similar anti-inflammatory,analgesic and gastrointestinal motility promotion effects,which provided a support for the pharmacodynamic equivalence of the multi-source plants of MFC.
基金The National Natural Science Foundation of China(Grant No.21272017 and 21572010)
文摘Multidrug resistance-associated proteins （MRPs） can effiux structurally diverse drugs, drug conjugates, drug metabolites, as well as other small molecules out of the cells, and this is the main cause of producing multidrug resistance （MDR） of some anticaneer drugs. Therefore, it is crucial to uncover the molecular features of MRPs substrates in developing anti-MDR cancer therapy. In the present study, common feature pharmacophore models were developed by employing CATALYST Pharmacophore Modeling and Analysis tools using substrates of MRPs, including MRP1, -2, -3, -4, -5, -6, -8 and MRPs family, respectively. The models were validated using independent decoy sets generated in DUD-E, and the ones with best A UC （area under the curve） scores were chosen to predict endogenous substrates by screening the Human Metabolome Database （HMDB）. A number of molecules obtained by pharmacophore screening have been validated in the literatures. By comparing physical properties （ALOGP, Molecular_PolarSurfaceArea, Molecular_Volume, Molecular_Weight, Num H Acceptors, Num H Donors） and scaffold features of the screened candidates with the known substrates, we found that： 1） The two sets have consistent ALOGP, Molecule_Volume and Molecule_Weight distribution trend; 2） Substrates of MRP1 have a better lipophilicity than the other subtypes, which is consistent with the two hydrophobic centers on the MRP1 pharmacophore; 3） In the aspect of the scaffold structures, they have the identical or similar backbone fragments.
