A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) an...A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) and colon cancer (WIDR). Thus, in order to predict the cytotoxic potentials of these compounds, quantitative structure-activity relationship studies were carried out using the methods of quantum chemistry. Five Quantitative Structure Activity Relationship (QSAR) models were obtained from the determined quantum descriptors and the different activities. The models present the following statistical indicators: regression correlation coefficient R2 = 0.986 - 0.905, standard deviation S = 0.516 - 0.153, Fischer test F = 106.718 - 14.220, correlation coefficient of cross-validation = 0.985- 0.895 and = 0.010 - 0.001. The statistical characteristics of the established QSAR models satisfy the acceptance and external validation criteria, thereby accrediting their good performance. The models developed show that the variation of the free enthalpy of reaction , the dipole moment μ and the charge of the ligand in the complex Ql, are the explanatory and predictive quantum descriptors correlated with the values of the anti-cancer activity of the studied complexes. Moreover, the charge of the ligand is the priority descriptor for the prediction of the cytotoxicity of the compounds studied. Furthermore, QSAR models developed are statistically significant and predictive, and could be used for the design and synthesis of new anti-cancer molecules.展开更多
Objective:To evaluate the effect of heat-clearing and detoxifying method on the macrophages polarization in patients with acute myocardial infarction with heat toxin syndrome after intervention.Methods:Sixty patients ...Objective:To evaluate the effect of heat-clearing and detoxifying method on the macrophages polarization in patients with acute myocardial infarction with heat toxin syndrome after intervention.Methods:Sixty patients with acute myocardial infarction and undergoing percutaneous coronary intervention with heat toxin syndrome were randomly divided into a control group and a test group with 30 cases each.The control group was given conventional treatment,and the test group was given Huanglian Jiedu Decoction,the representative of the method of clearing heat and detoxification,orally on the basis of the control group.The intervention time of both groups was 2 weeks.Comparing The Seattle Angina Pectoris Scale(SAQ)before and after treatment,creatine kinase(CK),creatine kinase MB isoenzyme(CKMB),high-sensitivity troponin I(hs-TnI),and Lipoprotein-associated phospholipaseA2(LPPLA_2)),the phenotype ratio of M1 and M2 macrophages,and observe the adverse reactions.Results:After treatment,the SAQ scores of the two groups of patients were improved,and the levels of CK,CK-MB,hs-TnI,and LP-PLA_2 decreased significantly.The scores of AS,AF,TS,and DP in the SAQ of the test group were all higher than those of the control group,and the hs-TnI and LP-PLA_2 were better than those of the control Group(P<0.05 or P<0.01).After treatment,the proportion of M1 type macrophages in the two groups of patients'macrophages decreased significantly(P<0.05 or P<0.01),the ratio of M2 type macrophages increased(P<0.05),and the M1/M2 ratio decreased.The ratio of M1/M2 in the test group of the control group was significantly lower than that of the control group(P<0.01).There were no obvious adverse reactions in both groups.Conclusions:The method of clearing heat and detoxifying has a definite effect on patients with acute myocardial infarction of heat toxin syndrome after interventional operation.It can reduce myocardial damage,improve myocardial function,and reduce inflammation.And it is safe for clinical treatment without any increasing risk of bleeding or other risk of cardiovascular events.展开更多
Objective:To explore the effects of Huoxue Huayu detoxification method on the levels of GSK-3βandβ-catenin in OSF patients and its mechanism.Methods:A total of 120 patients with oral submucosal fibrosis(OSF)treated ...Objective:To explore the effects of Huoxue Huayu detoxification method on the levels of GSK-3βandβ-catenin in OSF patients and its mechanism.Methods:A total of 120 patients with oral submucosal fibrosis(OSF)treated in our hospital from May 2018 to December 2019 were selected and divided into routine treatment group and Huoxue Huayu detoxification group of 60 cases according to the lottery method.The routine treatment group was treated with triamcinolone acetonide injection,and the Huoxue Huayu detoxification group was treated with Huoxue Huayu detoxification.The lesion area,mouth opening degree,SFRP1 level in gingival crevicular fluid and saliva,TCM symptom score,TGF-β1,IL-6,GSK-3β,β-catenin expression and clinical effect were observed in the two groups.Results:After treatment,the lesion area of oral mucosa in the Huoxue Huayu detoxification group was smaller than that in the routine treatment group(P<0.05),and the mouth opening degree in the Huoxue Huayu detoxification group was larger than that in the routine treatment group(P<0.05);After treatment,the level of SFRP1 in gingival crevicular fluid and saliva and clinical effect in the Huoxue Huayu detoxification group were higher than those in the routine treatment group(P<0.05);the TCM syndrome score,TGF-β1,IL-6,GSK-3β,β-catenin expression in the Huoxue Huayu detoxification group were lower than those in the routine treatment group(P<0.05).Conclusion:By acting on Wnt/β-catenin signaling pathway,Huoxue Huayu detoxification method can regulate the expression of TGF-β1,IL-6,GSK-3β,β-catenin,improve the clinical symptoms of patients with oral submucous fibrosis,alleviate the body inflammation,alleviate the pain,with remarkable effect.展开更多
The present method gives a detailed description for the development and validation of a simple stability indicating reverse phase liquid chromatographic method for 10-hydroxycamptothecin(10-HCTN) in the presence of it...The present method gives a detailed description for the development and validation of a simple stability indicating reverse phase liquid chromatographic method for 10-hydroxycamptothecin(10-HCTN) in the presence of its impurities namely Imp A and Imp B along with degradation products generated from forced degradation studies. The drug was subjected to stress conditions of hydrolysis (acid, base and neutral), oxidative, photolytic and thermal stress degradation. Degradation was observed when subjected to treatment with peroxides or under conditions normally used for typical acid and base hydrolysis. The drug was found to be stable under other stress conditions attempted such as photolytic and thermal. Successful separation and isolation of the drug from related impurities and degradation products formed under stress conditions was achieved on an Inertsil ODS-3V (250 mm × 4.6 mm, 5 μm) column using a phosphate buffer, acetonitrile, methanol and Nanopure water. The developed HPLC method was validated with respect to specificity, linearity, accuracy, precision, sensitivity, robustness and solution stability. The assay method was found to be linear in the range of 0.16 mg/mL to 0.24 mg/mL with a correlation coefficient of 0.999 and the linearity of the impurities was established from 0.02% (LOQ) to 0.3%. Recoveries of assay and impurities were found between 99.4% and 100.3%. The developed HPLC method can be used to determine the related substances and assay determinations of 10-HCTN and also to evaluate the quality and long term stability of production samples.展开更多
文摘A series of ruthenium azopyridine complexes have recently been investigated due to their potential cytotoxic activities against renal cancer (A498), lung cancer (H226), ovarian cancer (IGROV), breast cancer (MCF-7) and colon cancer (WIDR). Thus, in order to predict the cytotoxic potentials of these compounds, quantitative structure-activity relationship studies were carried out using the methods of quantum chemistry. Five Quantitative Structure Activity Relationship (QSAR) models were obtained from the determined quantum descriptors and the different activities. The models present the following statistical indicators: regression correlation coefficient R2 = 0.986 - 0.905, standard deviation S = 0.516 - 0.153, Fischer test F = 106.718 - 14.220, correlation coefficient of cross-validation = 0.985- 0.895 and = 0.010 - 0.001. The statistical characteristics of the established QSAR models satisfy the acceptance and external validation criteria, thereby accrediting their good performance. The models developed show that the variation of the free enthalpy of reaction , the dipole moment μ and the charge of the ligand in the complex Ql, are the explanatory and predictive quantum descriptors correlated with the values of the anti-cancer activity of the studied complexes. Moreover, the charge of the ligand is the priority descriptor for the prediction of the cytotoxicity of the compounds studied. Furthermore, QSAR models developed are statistically significant and predictive, and could be used for the design and synthesis of new anti-cancer molecules.
基金Guangdong Provincial Medical Science and Technology Research Fund Project(No.A2019507)Traditional Chinese Medicine Bureau of Guangdong Provincial Project(No.20191117)+1 种基金Science and Technology Program of Guangzhou(No.202102020927)National Administration of Traditional Chinese Medicine Clinical Research Base Business Construction Research Project(No.JDZX2015241)。
文摘Objective:To evaluate the effect of heat-clearing and detoxifying method on the macrophages polarization in patients with acute myocardial infarction with heat toxin syndrome after intervention.Methods:Sixty patients with acute myocardial infarction and undergoing percutaneous coronary intervention with heat toxin syndrome were randomly divided into a control group and a test group with 30 cases each.The control group was given conventional treatment,and the test group was given Huanglian Jiedu Decoction,the representative of the method of clearing heat and detoxification,orally on the basis of the control group.The intervention time of both groups was 2 weeks.Comparing The Seattle Angina Pectoris Scale(SAQ)before and after treatment,creatine kinase(CK),creatine kinase MB isoenzyme(CKMB),high-sensitivity troponin I(hs-TnI),and Lipoprotein-associated phospholipaseA2(LPPLA_2)),the phenotype ratio of M1 and M2 macrophages,and observe the adverse reactions.Results:After treatment,the SAQ scores of the two groups of patients were improved,and the levels of CK,CK-MB,hs-TnI,and LP-PLA_2 decreased significantly.The scores of AS,AF,TS,and DP in the SAQ of the test group were all higher than those of the control group,and the hs-TnI and LP-PLA_2 were better than those of the control Group(P<0.05 or P<0.01).After treatment,the proportion of M1 type macrophages in the two groups of patients'macrophages decreased significantly(P<0.05 or P<0.01),the ratio of M2 type macrophages increased(P<0.05),and the M1/M2 ratio decreased.The ratio of M1/M2 in the test group of the control group was significantly lower than that of the control group(P<0.01).There were no obvious adverse reactions in both groups.Conclusions:The method of clearing heat and detoxifying has a definite effect on patients with acute myocardial infarction of heat toxin syndrome after interventional operation.It can reduce myocardial damage,improve myocardial function,and reduce inflammation.And it is safe for clinical treatment without any increasing risk of bleeding or other risk of cardiovascular events.
基金National natural science foundation of China(No.81874496)Project of Hunan administration of traditional Chinese medicine(No.201808)Hunan education department project(No.18C0408)。
文摘Objective:To explore the effects of Huoxue Huayu detoxification method on the levels of GSK-3βandβ-catenin in OSF patients and its mechanism.Methods:A total of 120 patients with oral submucosal fibrosis(OSF)treated in our hospital from May 2018 to December 2019 were selected and divided into routine treatment group and Huoxue Huayu detoxification group of 60 cases according to the lottery method.The routine treatment group was treated with triamcinolone acetonide injection,and the Huoxue Huayu detoxification group was treated with Huoxue Huayu detoxification.The lesion area,mouth opening degree,SFRP1 level in gingival crevicular fluid and saliva,TCM symptom score,TGF-β1,IL-6,GSK-3β,β-catenin expression and clinical effect were observed in the two groups.Results:After treatment,the lesion area of oral mucosa in the Huoxue Huayu detoxification group was smaller than that in the routine treatment group(P<0.05),and the mouth opening degree in the Huoxue Huayu detoxification group was larger than that in the routine treatment group(P<0.05);After treatment,the level of SFRP1 in gingival crevicular fluid and saliva and clinical effect in the Huoxue Huayu detoxification group were higher than those in the routine treatment group(P<0.05);the TCM syndrome score,TGF-β1,IL-6,GSK-3β,β-catenin expression in the Huoxue Huayu detoxification group were lower than those in the routine treatment group(P<0.05).Conclusion:By acting on Wnt/β-catenin signaling pathway,Huoxue Huayu detoxification method can regulate the expression of TGF-β1,IL-6,GSK-3β,β-catenin,improve the clinical symptoms of patients with oral submucous fibrosis,alleviate the body inflammation,alleviate the pain,with remarkable effect.
文摘The present method gives a detailed description for the development and validation of a simple stability indicating reverse phase liquid chromatographic method for 10-hydroxycamptothecin(10-HCTN) in the presence of its impurities namely Imp A and Imp B along with degradation products generated from forced degradation studies. The drug was subjected to stress conditions of hydrolysis (acid, base and neutral), oxidative, photolytic and thermal stress degradation. Degradation was observed when subjected to treatment with peroxides or under conditions normally used for typical acid and base hydrolysis. The drug was found to be stable under other stress conditions attempted such as photolytic and thermal. Successful separation and isolation of the drug from related impurities and degradation products formed under stress conditions was achieved on an Inertsil ODS-3V (250 mm × 4.6 mm, 5 μm) column using a phosphate buffer, acetonitrile, methanol and Nanopure water. The developed HPLC method was validated with respect to specificity, linearity, accuracy, precision, sensitivity, robustness and solution stability. The assay method was found to be linear in the range of 0.16 mg/mL to 0.24 mg/mL with a correlation coefficient of 0.999 and the linearity of the impurities was established from 0.02% (LOQ) to 0.3%. Recoveries of assay and impurities were found between 99.4% and 100.3%. The developed HPLC method can be used to determine the related substances and assay determinations of 10-HCTN and also to evaluate the quality and long term stability of production samples.
