The calcium channel blocker,verapamil,has been shown to reduce scar formation by inhibiting fibroblast adhesion and proliferation in vitro.It was not clear whether topical application of verapamil after surgical repai...The calcium channel blocker,verapamil,has been shown to reduce scar formation by inhibiting fibroblast adhesion and proliferation in vitro.It was not clear whether topical application of verapamil after surgical repair of the nerve in vivo could inhibit the formation of excessive scar tissue.In this study,the right sciatic nerve of adult Sprague-Dawley rats was transected and sutured with No.10-0 suture.The stoma was wrapped with gelfoam soaked with verapamil solution for 4 weeks.Compared with the control group(stoma wrapped with gelfoam soaked with physiological saline),the verapamil application inhibited the secretion of extracellular matrix from fibroblasts in vivo,suppressed type I and III collagen secretion and increased the total number of axons and the number of myelinated axons.These findings suggest that verapamil could reduce the formation of scar tissue and promote axon growth after peripheral nerve repair.展开更多
Objective:The majority of the patients with posttraumatic stress disorders(PTSD) embrace augmented urinary flow of Vanillylmandelic Acid(VMA) than normal subjects owing to superior sympathetic doings,which steer to ca...Objective:The majority of the patients with posttraumatic stress disorders(PTSD) embrace augmented urinary flow of Vanillylmandelic Acid(VMA) than normal subjects owing to superior sympathetic doings,which steer to cardiovascular catastrophe.Urinary flow of VMA was evaluated as sympathoadrenal bustle marker in patients with posttraumatic stress disorder.Calcium ion shows a noteworthy dependability in nervousness owing to its special effects on brain synaptosomes.So this study was conducted to explore the effects of Verapamil on sympathoadrenal motion in patients with PTSD.Methods:Placebo controlled clinical tryout was conducted. At first hundred(100) PTSD patients were chosen and enrolled in the study,from department of Psychological Medicine Dow University of Health Sciences,Karachi.Verapamil 120 mg/day was specified in divided doses to group-Ⅰ(n=50)patients and group-Ⅱ(n =50) patients received placebo therapy on a daily basis for nine weeks.Each and every patient was monitored weekly,all the way through extent of study.Results:Underneath the posttraumatic stress disorder,urinary excretion of VMA was greater.Calcium channel blocker verapamil additionally abolished the embellished retort in urinary flow of VMA appreciably in patients with PTSD. Conclusion:Verapamil was experiential to be exceedingly effectual treatment.It reduces VMA levels in urine, and on the whole cardiovascular threat in PTSD patients.展开更多
The effects of captopril (Cap) and verapamil (Ver)alone and in combination on intracellular Na+ concentration ([Na+]i) in cultured aortic smooth muscle cells (ASMC) of rabbits was evaluated by a direct measurement of ...The effects of captopril (Cap) and verapamil (Ver)alone and in combination on intracellular Na+ concentration ([Na+]i) in cultured aortic smooth muscle cells (ASMC) of rabbits was evaluated by a direct measurement of [Na+]i with fluorescent dye sodium-binding benzofuran isophthalate (SBFI) combined with digital image. [Na+]i in resting cells was found to be 11.9 ± 0. 7 mmol/L. Angiotensin II (Ang-II, 0.1-10μmol/L) induced an increase of [Na+]i in concentration-dependent manner. Ver (0.1-10μmol/L) inhibited Ang-II (1 μmol/L)-induced increase in [Na+]i, while Cap enhanced Ang-II-induced increase in [Na+]i at 10μmol/L but not at 0.1-1μmol/L. Ver (0.1-1μmol/L)abolished enhancement of Ang-II-induced increase in [Na+]i by Cap. Thus, the inhibition of Capenhanced [Na+]i by Ver may provide a new hypothesis for the underlying molecular mechanism of synergistic effect of the combination of Ca2+ antagonists and angiotensinconverting enzyme inhibitors in controlling blood pressure.展开更多
This article discusses the characteristics of the drugresistant human cervical carcinoma cell line HeLa/MMC and investigates reversal effect of SDZ-PSC833(PSC833) and Verapamil (Ver) upon HeLa/MMC. Relative conten...This article discusses the characteristics of the drugresistant human cervical carcinoma cell line HeLa/MMC and investigates reversal effect of SDZ-PSC833(PSC833) and Verapamil (Ver) upon HeLa/MMC. Relative content of cell DNA detection, H3-TdR incorporation test and drug-resistance have been experimented, meanwhile a tumor transplant model in the nude mice for Hela/MMC has been established. Then the volume of cancer, tumor weight, curve line of growing up in tumor -bearing nude mouse and its morphological variation of carcinoma organism are observed to evaluate the reversal effect of PSC833 and VER. It has been found that: (1) Compared with HeLa cells,subline HeLaJ MMC Cells' drug-resistant capability against Mitomycin(MMC) or cisplatin(DDP) is as 5.02 folds or 2 folds as that of the former, respectively. The Hela/MMC cell line has characteristics of multi- drug resistance and stronger multiplication; (2) PSC833 and VER can reverse resistance of HeLa/MMC to Mitomycin in vivo.PSC833 will be a better candidate for reversing multidrug resistant than verapamil in clinic application.展开更多
Objective: To establish a HPLC method using fluorometric detection for quantitatively determinating intracellular accumulation of verapamil (VER). Methods: Chromatography column was packed with spherisorb ODS(250&...Objective: To establish a HPLC method using fluorometric detection for quantitatively determinating intracellular accumulation of verapamil (VER). Methods: Chromatography column was packed with spherisorb ODS(250×4.6 mm,10 μm).The mobile phase consisted of the mixture of methanol:NaAC (0.01 mol/L): diethylamine (65:35:0.25). The detect wavelength was 280/310 nm (Ex/Em). Results: The standard curve showed a good correlation between concentration and peak area within the range of 5-50 ng/ml. RSD was 0.86%, and recovery radio of loading sample, 100%. The detection limit for cell sample was 0.2-148 ng/ml. Intracellular accumulation of VER was observed to decrease from a 13 fold to 5 fold in K562/ADM cells, and from a 3.5 fold to 4.3 fold in K562/VER cells and from a 2.1 fold to 6.5 fold in K562/ADM/VER cells, compared with the relevant control cells. Conclusion: HPLC method was proved to be sensitive and specific for using to quantitatively determine the intracellular accumulation of VER.展开更多
In order to investigate the effects of verapamil on the proliferation of meningiomas cells in vitro and in vivo, the cultured meningiomas cells were cultured with verapamil at different concentrations for 24 h and the...In order to investigate the effects of verapamil on the proliferation of meningiomas cells in vitro and in vivo, the cultured meningiomas cells were cultured with verapamil at different concentrations for 24 h and the inhibitory effects of verapamil on cell proliferation were observed by MTT method. The meningiomas model was established by implanting the newly removed tumor fragments into the nude mice subcutaneously. The nude mice with tumors were divided into two groups: verapamil-treated group and control group. Tumor volumes were measured and after 12 weeks the tumors were taken out and examined histologically. The expression of proliferating cell nuclear antigen (PCNA) in the tumors was detected by using immunohistochemistry. It was found that verapamil could inhibit the growth of cultured meningiomas cells in a concentration-dependant manner. The inhibitory effect could be observed in the concentration of 1 μmol/L verapamil and the most obvious effects appeared in the concentration of 100 μmol/L. Tumor volume in the verapamiltreated group was obviously smaller than that in the control group (211.40±5.50 vs 163.94±3.62, P〈0.01) and the expression of PCNA was also lower (1.52±0.24 vs 2.86±0.53, P〈0.05). Tumor inhibition rate was about 22.45%. It was suggested that verapamil could inhibit the proliferation and growth of meningiomas cells in vitro and in vivo.展开更多
Dementia is currently the only leading cause of death that is still on the rise,with its overall costs already surpassing those of cancer and heart disease combined,it has developed into a worldwide crisis.In response...Dementia is currently the only leading cause of death that is still on the rise,with its overall costs already surpassing those of cancer and heart disease combined,it has developed into a worldwide crisis.In response to its serious and far-reaching effects,the US government has established the"National Alzheimer's Project Act"(Public Law 111-375).展开更多
Objective: To achieve pulsed release system of verapamil on the basis of circadian rhythms of hypertensive patients. Methods: Factors affecting the lag time of the system were tested. Three swelling disintegrates (L-H...Objective: To achieve pulsed release system of verapamil on the basis of circadian rhythms of hypertensive patients. Methods: Factors affecting the lag time of the system were tested. Three swelling disintegrates (L-HPC,CMS-Na, CMC-Ca) of different contents were used- Various compositions of out shell were tested throughthe uniform design and dealt with multipleregression. Two basic formulations whose lag time is 3 and 5 h were decided- Results: The lag time 5 h formulation: CMS-Na was the preferable disintegrate with content 15 mg/tablet,out shell composition were chosen as PEG 6000 110 mg, HCO 105 mg, EVA 25 mg each tablet. Hardness 5 kg/cm2. Conclusion: A new press-coated tablets for the pulsed release of drug after a programmable period of time isachieved in the in vitro dissolution test.展开更多
Verapamil is a calcium channel blocker drug which reduces heart rhythm and blood pressure in high blood pressure patient.The steady state of this drug has to be continually controlled to obtain optimal efficacy.In add...Verapamil is a calcium channel blocker drug which reduces heart rhythm and blood pressure in high blood pressure patient.The steady state of this drug has to be continually controlled to obtain optimal efficacy.In addition,patient compliance needs to be considered.Therefore,controlled release tablet of verapamil hydrochloride was essentially developed using hydrophilic matrix polymer,namely hydroxypropylmethyl cellulose(HPMC)and sodium alginate,and compared to marketed product[1].HPMC,a pH-independent polymer,hydrates to form a gel layer at the surface of the tablet to sustain the drug release.Sodium alginate,a pH-dependent gelling polymer,converts to insoluble alginic acid after exposure to acidic condition in stomach.展开更多
基金supported by the Natural Science Foundation of Hubei Province of China,No.2011CDB392
文摘The calcium channel blocker,verapamil,has been shown to reduce scar formation by inhibiting fibroblast adhesion and proliferation in vitro.It was not clear whether topical application of verapamil after surgical repair of the nerve in vivo could inhibit the formation of excessive scar tissue.In this study,the right sciatic nerve of adult Sprague-Dawley rats was transected and sutured with No.10-0 suture.The stoma was wrapped with gelfoam soaked with verapamil solution for 4 weeks.Compared with the control group(stoma wrapped with gelfoam soaked with physiological saline),the verapamil application inhibited the secretion of extracellular matrix from fibroblasts in vivo,suppressed type I and III collagen secretion and increased the total number of axons and the number of myelinated axons.These findings suggest that verapamil could reduce the formation of scar tissue and promote axon growth after peripheral nerve repair.
文摘Objective:The majority of the patients with posttraumatic stress disorders(PTSD) embrace augmented urinary flow of Vanillylmandelic Acid(VMA) than normal subjects owing to superior sympathetic doings,which steer to cardiovascular catastrophe.Urinary flow of VMA was evaluated as sympathoadrenal bustle marker in patients with posttraumatic stress disorder.Calcium ion shows a noteworthy dependability in nervousness owing to its special effects on brain synaptosomes.So this study was conducted to explore the effects of Verapamil on sympathoadrenal motion in patients with PTSD.Methods:Placebo controlled clinical tryout was conducted. At first hundred(100) PTSD patients were chosen and enrolled in the study,from department of Psychological Medicine Dow University of Health Sciences,Karachi.Verapamil 120 mg/day was specified in divided doses to group-Ⅰ(n=50)patients and group-Ⅱ(n =50) patients received placebo therapy on a daily basis for nine weeks.Each and every patient was monitored weekly,all the way through extent of study.Results:Underneath the posttraumatic stress disorder,urinary excretion of VMA was greater.Calcium channel blocker verapamil additionally abolished the embellished retort in urinary flow of VMA appreciably in patients with PTSD. Conclusion:Verapamil was experiential to be exceedingly effectual treatment.It reduces VMA levels in urine, and on the whole cardiovascular threat in PTSD patients.
文摘The effects of captopril (Cap) and verapamil (Ver)alone and in combination on intracellular Na+ concentration ([Na+]i) in cultured aortic smooth muscle cells (ASMC) of rabbits was evaluated by a direct measurement of [Na+]i with fluorescent dye sodium-binding benzofuran isophthalate (SBFI) combined with digital image. [Na+]i in resting cells was found to be 11.9 ± 0. 7 mmol/L. Angiotensin II (Ang-II, 0.1-10μmol/L) induced an increase of [Na+]i in concentration-dependent manner. Ver (0.1-10μmol/L) inhibited Ang-II (1 μmol/L)-induced increase in [Na+]i, while Cap enhanced Ang-II-induced increase in [Na+]i at 10μmol/L but not at 0.1-1μmol/L. Ver (0.1-1μmol/L)abolished enhancement of Ang-II-induced increase in [Na+]i by Cap. Thus, the inhibition of Capenhanced [Na+]i by Ver may provide a new hypothesis for the underlying molecular mechanism of synergistic effect of the combination of Ca2+ antagonists and angiotensinconverting enzyme inhibitors in controlling blood pressure.
基金Supported by the Key Scientific and Technical Research Project of Hubei Provicial Department of Education (EK980038)
文摘This article discusses the characteristics of the drugresistant human cervical carcinoma cell line HeLa/MMC and investigates reversal effect of SDZ-PSC833(PSC833) and Verapamil (Ver) upon HeLa/MMC. Relative content of cell DNA detection, H3-TdR incorporation test and drug-resistance have been experimented, meanwhile a tumor transplant model in the nude mice for Hela/MMC has been established. Then the volume of cancer, tumor weight, curve line of growing up in tumor -bearing nude mouse and its morphological variation of carcinoma organism are observed to evaluate the reversal effect of PSC833 and VER. It has been found that: (1) Compared with HeLa cells,subline HeLaJ MMC Cells' drug-resistant capability against Mitomycin(MMC) or cisplatin(DDP) is as 5.02 folds or 2 folds as that of the former, respectively. The Hela/MMC cell line has characteristics of multi- drug resistance and stronger multiplication; (2) PSC833 and VER can reverse resistance of HeLa/MMC to Mitomycin in vivo.PSC833 will be a better candidate for reversing multidrug resistant than verapamil in clinic application.
文摘Objective: To establish a HPLC method using fluorometric detection for quantitatively determinating intracellular accumulation of verapamil (VER). Methods: Chromatography column was packed with spherisorb ODS(250×4.6 mm,10 μm).The mobile phase consisted of the mixture of methanol:NaAC (0.01 mol/L): diethylamine (65:35:0.25). The detect wavelength was 280/310 nm (Ex/Em). Results: The standard curve showed a good correlation between concentration and peak area within the range of 5-50 ng/ml. RSD was 0.86%, and recovery radio of loading sample, 100%. The detection limit for cell sample was 0.2-148 ng/ml. Intracellular accumulation of VER was observed to decrease from a 13 fold to 5 fold in K562/ADM cells, and from a 3.5 fold to 4.3 fold in K562/VER cells and from a 2.1 fold to 6.5 fold in K562/ADM/VER cells, compared with the relevant control cells. Conclusion: HPLC method was proved to be sensitive and specific for using to quantitatively determine the intracellular accumulation of VER.
文摘In order to investigate the effects of verapamil on the proliferation of meningiomas cells in vitro and in vivo, the cultured meningiomas cells were cultured with verapamil at different concentrations for 24 h and the inhibitory effects of verapamil on cell proliferation were observed by MTT method. The meningiomas model was established by implanting the newly removed tumor fragments into the nude mice subcutaneously. The nude mice with tumors were divided into two groups: verapamil-treated group and control group. Tumor volumes were measured and after 12 weeks the tumors were taken out and examined histologically. The expression of proliferating cell nuclear antigen (PCNA) in the tumors was detected by using immunohistochemistry. It was found that verapamil could inhibit the growth of cultured meningiomas cells in a concentration-dependant manner. The inhibitory effect could be observed in the concentration of 1 μmol/L verapamil and the most obvious effects appeared in the concentration of 100 μmol/L. Tumor volume in the verapamiltreated group was obviously smaller than that in the control group (211.40±5.50 vs 163.94±3.62, P〈0.01) and the expression of PCNA was also lower (1.52±0.24 vs 2.86±0.53, P〈0.05). Tumor inhibition rate was about 22.45%. It was suggested that verapamil could inhibit the proliferation and growth of meningiomas cells in vitro and in vivo.
基金supported by the National Institute of Health,No.R01-NS097800(to TI).
文摘Dementia is currently the only leading cause of death that is still on the rise,with its overall costs already surpassing those of cancer and heart disease combined,it has developed into a worldwide crisis.In response to its serious and far-reaching effects,the US government has established the"National Alzheimer's Project Act"(Public Law 111-375).
文摘Objective: To achieve pulsed release system of verapamil on the basis of circadian rhythms of hypertensive patients. Methods: Factors affecting the lag time of the system were tested. Three swelling disintegrates (L-HPC,CMS-Na, CMC-Ca) of different contents were used- Various compositions of out shell were tested throughthe uniform design and dealt with multipleregression. Two basic formulations whose lag time is 3 and 5 h were decided- Results: The lag time 5 h formulation: CMS-Na was the preferable disintegrate with content 15 mg/tablet,out shell composition were chosen as PEG 6000 110 mg, HCO 105 mg, EVA 25 mg each tablet. Hardness 5 kg/cm2. Conclusion: A new press-coated tablets for the pulsed release of drug after a programmable period of time isachieved in the in vitro dissolution test.
文摘Verapamil is a calcium channel blocker drug which reduces heart rhythm and blood pressure in high blood pressure patient.The steady state of this drug has to be continually controlled to obtain optimal efficacy.In addition,patient compliance needs to be considered.Therefore,controlled release tablet of verapamil hydrochloride was essentially developed using hydrophilic matrix polymer,namely hydroxypropylmethyl cellulose(HPMC)and sodium alginate,and compared to marketed product[1].HPMC,a pH-independent polymer,hydrates to form a gel layer at the surface of the tablet to sustain the drug release.Sodium alginate,a pH-dependent gelling polymer,converts to insoluble alginic acid after exposure to acidic condition in stomach.