Objective: To analyze quantitatively the synergistic and antagonistic effects of combined oxymatrine (OMT) and 5-fluorouracil (5-GU) on a cell line of human liver cancer (HepG2) with median-effect principle in vitro. ...Objective: To analyze quantitatively the synergistic and antagonistic effects of combined oxymatrine (OMT) and 5-fluorouracil (5-GU) on a cell line of human liver cancer (HepG2) with median-effect principle in vitro. Methods: The median-effect principle and MTT method were used in the quantitative analysis of effects of the two drugs. Results: Cytotoxic activity of the individual drugs enhanced as drug concentration increased. As fa=0.41, a CI equal to 1 indicated additivity; fa<0.41, a CI less than 1 indicated synergy; and fa>0.41, a CI greater than 1 indicated antagonism. The sequence of administration did not influence the cytotoxic activity of the combined antitumor drugs. The ratio of drug concentration was a factor that can influence the killing effect. Conclusion: The combined drugs interaction (CI<1) was synergistic at lower concentration and antagonistic at higher concentration. The ratio of drug concentration is a factor that can influence the killing effect.展开更多
This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide der...This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives(8a–x). The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv(MTB) revealed that 2-chloro-N-(4-(5-(4-chlorophenyl)-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)benzamide(8n) is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative(8o) is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity(MIC = 3.13 mg/m L). Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development.展开更多
AIM:To investigate the safety and efficacy of sticky silicone oil(SSO)removal using a 22-gauge vein detained needle and inner limiting membrane(ILM)wrap-and-peel technique.METHODS:This retrospective consecutive case s...AIM:To investigate the safety and efficacy of sticky silicone oil(SSO)removal using a 22-gauge vein detained needle and inner limiting membrane(ILM)wrap-and-peel technique.METHODS:This retrospective consecutive case series reviewed the records of patients with a history of retinal detachment who had received silicone oil and perfluorocarbon liquid(PFCL)as intraocular tamponades.Patients were included in the analysis if they exhibited SSO remnants during silicone oil removal.The aspiration of most of the SSO remnants was performed by a 22-gauge vein detained needle.The small amounts of droplets adhered to the macula and epi-macular membrane were subsequently removed by the ILM warp-and-peel technique.The anatomical and functional outcomes,and postoperative complications were recorded.In vitro experiments were performed to simulate the formation of SSO remnants in four groups.RESULTS:Of 711 patients who underwent silicone oil removal during the study period,9 patients exhibited SSO remnants and underwent follow-up for at least 3mo.Seven eyes(78%)underwent the ILM wrap-and-peel technique to completely remove small droplets of SSO that were glued to the macula and epi-macular membrane.No obvious complications occurred.Postoperative optical coherence tomography revealed normal retinal structure in all patients.In vitro analyses showed that balanced salt solution and prolonged vibration(for 1wk)had the strongest effects on silicone oil and PFCL compound opacities.CONCLUSION:SSO remnants could be removed in an intact manner and without complications,using a vein detained needle-assisted and ILM wrap-and-peel technique.The findings suggest that PFCL and infusion fluid should be completely removed before silicone oil injection to prevent SSO formation.展开更多
文摘Objective: To analyze quantitatively the synergistic and antagonistic effects of combined oxymatrine (OMT) and 5-fluorouracil (5-GU) on a cell line of human liver cancer (HepG2) with median-effect principle in vitro. Methods: The median-effect principle and MTT method were used in the quantitative analysis of effects of the two drugs. Results: Cytotoxic activity of the individual drugs enhanced as drug concentration increased. As fa=0.41, a CI equal to 1 indicated additivity; fa<0.41, a CI less than 1 indicated synergy; and fa>0.41, a CI greater than 1 indicated antagonism. The sequence of administration did not influence the cytotoxic activity of the combined antitumor drugs. The ratio of drug concentration was a factor that can influence the killing effect. Conclusion: The combined drugs interaction (CI<1) was synergistic at lower concentration and antagonistic at higher concentration. The ratio of drug concentration is a factor that can influence the killing effect.
基金National Institute of Technology Karnataka,India for the financial support and laboratory facility
文摘This article demonstrates the synthesis, characterization and the study of in vitro antitubercular activities of twenty four new N-(4-(5-aryl-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)-4-amide derivatives(8a–x). The antitubercular activity of the compounds against Mycobacterium tuberculosis H37Rv(MTB) revealed that 2-chloro-N-(4-(5-(4-chlorophenyl)-3-(5-methyl-1,3,4-oxadiazol-2-yl)-1H-pyrazol-1-yl)phenyl)benzamide(8n) is the most promising lead molecule with a MIC of1.56 mg/m L, while the corresponding unsubstituted benzamide derivative(8o) is the next most active molecule with a MIC of 3.13 mg/m L. Interestingly, the pyrazole intermediate 5b containing chlorophenyl and N-acylcarbohydrazide substituents also showed significant activity(MIC = 3.13 mg/m L). Further, the active molecules did not show toxicity against a normal NIH 3T3 cell line, signifying their suitability for further drug development.
基金the Wenzhou Basic ScientificResearch Program (No.20211003).
文摘AIM:To investigate the safety and efficacy of sticky silicone oil(SSO)removal using a 22-gauge vein detained needle and inner limiting membrane(ILM)wrap-and-peel technique.METHODS:This retrospective consecutive case series reviewed the records of patients with a history of retinal detachment who had received silicone oil and perfluorocarbon liquid(PFCL)as intraocular tamponades.Patients were included in the analysis if they exhibited SSO remnants during silicone oil removal.The aspiration of most of the SSO remnants was performed by a 22-gauge vein detained needle.The small amounts of droplets adhered to the macula and epi-macular membrane were subsequently removed by the ILM warp-and-peel technique.The anatomical and functional outcomes,and postoperative complications were recorded.In vitro experiments were performed to simulate the formation of SSO remnants in four groups.RESULTS:Of 711 patients who underwent silicone oil removal during the study period,9 patients exhibited SSO remnants and underwent follow-up for at least 3mo.Seven eyes(78%)underwent the ILM wrap-and-peel technique to completely remove small droplets of SSO that were glued to the macula and epi-macular membrane.No obvious complications occurred.Postoperative optical coherence tomography revealed normal retinal structure in all patients.In vitro analyses showed that balanced salt solution and prolonged vibration(for 1wk)had the strongest effects on silicone oil and PFCL compound opacities.CONCLUSION:SSO remnants could be removed in an intact manner and without complications,using a vein detained needle-assisted and ILM wrap-and-peel technique.The findings suggest that PFCL and infusion fluid should be completely removed before silicone oil injection to prevent SSO formation.