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【Objective】 To explore the action mechanism of vinpocetine in improving learning and memory disorders in depressive rats after modified electroconvulsive therapy (MECT). 【Methods】 The models of depressive rats were constructed by chronic unpredictable mild stress (CUMS) method. A total of 30 rats with depression were randomly divided into depression group, MECT group, and MECT+vinpocetine (10 mg/kg) group, with 10 in each group. A total of 10 untreated healthy rats were enrolled as control group. The learning and memory ability were tested by Morris water maze test and novel object recognition test. The depression state was evaluated by sugar preference test. The brain slices of the hippocampus were prepared for electrophysiological experiments. The density of dendritic spine was detected by Golgi staining. The expressions of endocannabinoids related genes [diacylglycerol lipase (DAGLα), monoacylglycerol lipase (MAGL), and endocannabinoid type-I receptor (CB1R)] were detected by qPCR and Western blotting. The lentivirus was injected to downregulate the expressions of CB1R and DAGLα in the hippocampus. After re-modeling and treatment, behavioral tests were performed. 【Results】 Compared with control group, sugar preference, spatial exploration time, relative discrimination index, long-term potentiation (LTP), density of dendritic spine, expressions of DAGLα and CB1R were decreased, while escape latency and MAGL were increased in depression group (P<0.05). Compared with depression group, sugar preference, escape latency, and MAGL were increased, while spatial exploration time, relative discrimination index, LTP, density of dendritic spine, expressions of DAGLα and CB1R were decreased in MECT group (P<0.05). Compared with depression group, sugar preference, spatial exploration time, relative discrimination index, LTP, density of dendritic spine, expressions of DAGLα and CB1R were increased, while escape latency and MAGL were decreased in MECT+vinpocetine group (P<0.05). Compared with MECT group, sugar preference, spatial exploration time, relative discrimination index, LTP, density of dendritic spine, expressions of DAGLα and CB1R were increased, while escape latency and MAGL were decreased in MECT+vinpocetine group (P<0.05). The down-regulation of DAGLα or CB1R by lentivirus could inhibit the improvement effect of vinpocetine on behavioral performance of depressive rats after MECT. 【Conclusion】 Vinpocetine can significantly improve learning and memory disorders in depressive rats after MECT, which may be related to regulating the expressions of endocannabinoid-related genes and enhancing synaptic plasticity.
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Objective:To investigate the effects of deafness capsule combined with vinpocetine injection on hearing function, hemorheology and T lymphocyte subsets in patients with sudden deafness.Methods:Eighty patients with sudden deafness who received treatment in Wenzhou Central Hospital from April 2017 to October 2019 were included in this study. They were randomly assigned to undergo treatment either with vinpocetine injection (control group, n = 40) or with deafness capsule combined with vinpocetine injection (observation group, n = 40) for 1 month. Efficacy, hearing function, hemorheology, T lymphocyte subsets and adverse reactions were compared between the control and observation groups. Results:Total response rate in the observation group was significantly higher than that in the control group [90.00% (36/40) vs. 67.50% (27/40), χ2 = 6.050, P = 0.014). There was no significant difference in the incidence of adverse reactions between the two groups ( P > 0.05). After 1 month of treatment, plasma viscosity, high-shear whole blood viscosity, low-shear whole blood viscosity in the observation group were (1.21 ± 0.29) mPa·s, (2.41 ± 0.31) mPa·s, (5.25 ± 1.29) mPa·s respectively, which were significantly lower than those in the control group [(1.65 ± 0.22) mPa·s, (4.94 ± 0.36) mPa·s, (8.64 ± 1.32) mPa·s, t = 7.64, 33.68, 11.61, all P < 0.001). The percentages of CD 8+, CD 4+, and CD 4+/CD 8+ T lymphocyte subsets in the observation group were (24.28 ± 2.16)%, (46.05 ± 6.52)% and (1.90 ± 0.28) respectively, and they were (27.41 ± 2.09)%, (40.54 ± 5.48)%, (1.48 ± 0.24) respectively in the control group ( t = 6.58, 4.09, 7.20, all P < 0.001). Pure tone threshold in the observation group was significantly lower than that in the control group [(38.07 ± 4.82) dB vs. (51.97 ± 5.96) dB, t = 11.46, P < 0.001). Conclusion:Deafness capsule combined with vinpocetine injection is highly effective on sudden deafness. The combined therapy can improve the hearing function, hemorheology, and the immunological function of T lymphocyte subsets in patients with sudden deafness.
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OBJECTIVE To study the pharm acokinetics of venlafaxine（VEN）combined with vinpocetine （VIN）in rats ，and to investigate the interaction between them. METHODS Healthy male SD rats were randomly divided into VEN group （13.5 mg/kg）， VIN group （1.8 mg/kg） and VEN + VIN group （13.5 mg/kg VEN + 1.8 mg/kg VIN ），with 6 rats in each group. Before administration，rats in each group fasted but didn ’t deprived of water for 12 hours，and were given corresponding drugs intragastrically at one time. Blood was collected from rats in each group through orbital venous plexus at different time points after administration. After plasma sample was pretreated （domperidone as internal standard ），LC-MS/MS method was adopted to determine the concentration of VEN ，active metabolite O-desmethylvenlafaxine of VEN （ODV）and active metabolite apovinblastic acid of VIN （AVA）in plasma. DAS 2.0 software was used to calculate and compare the pharmacokinetic parameters of VEN ，ODV and AVA. RESULTS Compared with VEN group ，the pharmacokinetic parameters cmax，AUC0－t，AUC0－∞，MRT0－t（except for VEN），MRT0－∞（except for VEN ）of VEN and ODV in VEN+VIN group were increased significantly ，while CL/ F and Vz/F were decreased significantly （P＜0.05 or P＜0.01）. Compared with VIN group ，there was no statistical difference in the pharmacokinetic parameters of AVA in rat plasma of VEN+VIN group （P＞0.05）. CONCLUSIONS After the combination of VEN and VIN ，VIN can affect the metabolism of VEN by increasing the absorption of VEN and ODV and slowing down their elimination.
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Resumen Introducción: La vinpocetina de liberación prolongada ha demostrado ser efectiva en el control de crisis de inicio focal en pacientes epilépticos con una baja frecuencia de eventos adversos. Se realizó un estudio clínico para evaluar la eficacia y tolerabilidad de la vinpocetina como tratamiento adyuvante en pacientes con este padecimiento. Métodos: Se realizó un estudio clínico, doble ciego, de grupos paralelos. Se reclutaron 87 pacientes con diagnóstico de epilepsia focal tratados con uno a tres fármacos antiepilépticos. Los pacientes se aleatorizaron para ser tratados con vinpocetina (n = 41) o placebo (n = 46) de manera adyuvante a su tratamiento, e ingresaron a la fase basal (4 semanas), a la fase de titulación (4 semanas) y a la fase de evaluación (8 semanas) conservando estables las dosis de la vinpocetina y de los fármacos antiepilépticos. Resultados: La vinpocetina fue más efectiva que el placebo en la reducción de las crisis al finalizar la fase de evaluación (p < 0.0001). El 69% de los pacientes tratados con vinpocetina presentaron una reducción mayor al 50% en las crisis en comparación con el 13% de los pacientes tratados con placebo. No se presentaron diferencias significativas en cuanto a la presencia de efectos adversos en los pacientes tratados con vinpocetina comparados con los tratados con placebo. Los eventos adversos más frecuentes observados con vinpocetina fueron cefalea (7.9%) y diplopía (5.2%). Conclusiones: Como tratamiento adyuvante, la vinpocetina (2 mg/kg/día) redujo eficazmente la frecuencia de crisis epilépticas y demostró ser bien tolerada. Presenta un amplio perfil de seguridad y eventos adversos conocidos, que son transitorios y sin secuelas.
Abstract Background: Extended-release vinpocetine is effective to control focal onset epileptic seizures with a low rate of adverse events. A clinical study was performed to evaluate the efficacy and tolerability of vinpocetine as an adjuvant treatment in patients with this condition. Methods: A double-blind clinical study of parallel groups was conducted, in which 87 patients with a diagnosis of focal epilepsy treated with one to three antiepileptic drugs were recruited. Patients were randomized to receive vinpocetine (n = 41) or placebo (n = 46) adjuvant to their treatment. Patients entered the baseline phase (4 weeks), the titration phase (4 weeks) and the evaluation phase (8 weeks), maintaining stable doses of vinpocetine and their respective antiepileptic drug treatment. Results: Vinpocetine was more effective than placebo in reducing seizures at the end of the evaluation phase (p < 0.0001). Sixty-nine percent of the vinpocetine-treated patients had a 50% reduction in seizures compared to 13% of placebo-treated patients. No significant differences in the presence of adverse effects in patients treated with vinpocetine compared to those treated with placebo were observed. The most frequent adverse events observed with vinpocetine were headache (7.9%) and diplopia (5.2%). Conclusions: As an adjuvant treatment, vinpocetine (2 mg/kg/day) effectively reduced the frequency of epileptic seizures and proved to be well tolerated. Vinpocetine has a wide safety profile and well-known adverse events, which are transient and with no sequelae.
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Adolescent , Adult , Child , Female , Humans , Male , Middle Aged , Young Adult , Vinca Alkaloids/administration & dosage , Epilepsies, Partial/drug therapy , Anticonvulsants/administration & dosage , Vinca Alkaloids/adverse effects , Double-Blind Method , Longitudinal Studies , Treatment Outcome , Delayed-Action Preparations , Anticonvulsants/adverse effectsABSTRACT
Objective: Nauclea latifolia (Rubiaceae) stem-bark enjoys wide patronage in ethnomedicine due to multiplicity of usage. Acute and subacute hematological and biochemical toxicity studies are available in literature but none underpins its ameliorative effect with a histone deacetylase inhibitor (HDAC), valproic acid (VPA) which mediates multifocal toxicity in different histological milieu. Methods: Subacute exposure of experimental albino rats with a high dose of valproic acid (500 mg/kg) was executed orally one hour before post-treatment with Nauclea latifolia stem-bark (NLS) extract in three doses (50, 100, 200 mg/kg) and with another group of rats with reference drug, vinpocetine, 25 mg/kg daily for 28 consecutive days after which hematological and biochemical analyses were executed. The liver, kidney and lungs were abstracted for histopathological evaluation. Results: The HDAC inhibitor, Valproic acids induced multifocal biochemical insults on liver function enzymes, lipid profiles, electrolytes and kidney function which were dose- dependently and significantly (P < 0.05 – 0.001) abrogated by the varying doses of administered NLS extract. On the histology the NLS extract effects corroborated the biochemical study in the liver and kidney. The NLS did not demonstrate significant toxicological impingement on the hematology and did not alter VPA-induced histomorphological injury in the lungs cytoarchitecture. The reference drug, vinpocetine was unresponsive to VPA-induced alteration in all the tissues investigated in the administered posology. Conclusion: The NLS extract was effective in abrogating toxicological insults in the liver and kidney but not in the lungs. Further studies are required to understand the mechanism of pharmacological effects of NLS extract and the differential in tissue response.
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Vinpocetine (VP) has been widely used to treat cerebrovascular disorders and nerve injury. Borneol (BN), as an important traditional Chinese medicine, is commonly used to promote the absorption and distribution of central nervous system drugs. In this work, a LC-MS/MS method was developed to determine the level of VP in rat plasma and tissues, and to evaluate the effect of co-administration of BN with VP by oral gavage on the absorption and tissue distribution of VP in rats. Rats were divided into VP (10 mg·kg-1), VP (10 mg·kg-1) + BN (75 mg·kg-1) and VP (10 mg·kg-1) + BN (150 mg·kg-1) groups for pharmacokinetic study, and divided into VP (10 mg·kg-1) and VP (10 mg·kg-1) + BN (150 mg·kg-1) groups for tissue distribution study. The animal experiment was approved by Ethics Committee of Hubei University, and complied with the guideline for caring and using of laboratory animals. Compared to VP group, the AUC0-∞, MRT0-∞ and t1/2z of VP + BN (150 mg·kg-1) group increased significantly, by 1.98-, 1.22- and 1.42-fold respectively, and the exposure in plasma, liver, kidney and brain increased by 2-, 1.5-, 1.5- and 1.3-fold respectively. The pharmacokinetic results suggested that co-administration of BN with VP is beneficial for overcoming the undesirable pharmacokinetic characteristics of VP, such as short residence time, low oral bioavailability and brain exposure in clinical usage.
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Objective To observe the effect of vinpocetine combined with butylphthalide in the treatment of large artery atherosclerotic infarction.Methods From October 2014 to October 2016,Ninety patients with large artery atherosclerotic cerebral infarction in Datong Coal Mine Group Three Hospital were selected and randomly divided into two groups,with 45 cases in each group.The treatment group was given vinpocetine injection ,and the observation group was given vinpocetine injection combined with butylphthalide soft capsules .The ability of daily life ( Barthel) score,neurological deficit score (NIHSS),hemodynamics indicators [ high blood viscosity (HSV),plasma viscosity index(PSV)] and adverse reactions were compared between the two groups.Results After treatment,the Barthel score,NIHSS score of the observation group were (79.84 ±18.57) points,(9.54 ±3.22) points,respectively,which of the control group were (62.67 ±16.48)points,(13.69 ±3.47)points,respectively,there were statistically significant differences between the two groups (t ＝4.64,5.88,all P ＜0.05).The HSV,PSV of the observation group were (3.96 ±2.14)mPa/s,(1.12 ±0.74)mPa/s,respectively,which of the control group were (5.77 ±2.69)mPa/s, (3.10 ±1.02)mPa/s,respectively,there were statistically significant differences between the two groups (t＝3.53, 10.54,all P＜0.05).The incidence rate of adverse reactions of the observation group was 4.44%,which was lower than 17.78%of the control group,the difference was statistically significant (χ2＝4.05,P＝0.04).Conclusion Vinpocetine injection combined with butylphthalide soft capsules in the treatment of large artery atherosclerotic infarction can improve neurological function and hemodynamics ,the effect is superior to single vinpocetine treatment.
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Objective To investigate the clinical efficacy of vinpocetine in the treatment of coronary heart disease (CHD).Methods 70 patients with CHD were selected,and they were randomly divided into observation group(35 cases) and control group (35 cases) according to the digital table.The control group received routine treatment,the observation group received vinpocetine therapy combined with fluoxetine on the basis of routine treatment.The changes of serum high sensitivity C reactive protein(hs-CRP) and interleukin 6(IL-6) were observed before and after treatment in the two groups,and the clinical efficacy of the two groups was compared.Results Before treatment,there were no statistically significant differences in hs-CRP and IL-6 levels between the two groups (all P ＞ 0.05).Mter treatment,the serum hs-CRP and IL-6 levels in the observation group were (4.18 ± 0.67) mg/mL,(4.42 ±0.52) pg/mL,respectively,which in the control group were (4.51 ± 0.54) mg/mL,(5.96 ± 0.73) pg/mL,respectively,there were statistically significant differences between the two groups(t =2.376,3.218,all P ＜ 0.05).The effective rate of the observation group was 94.3％,which was significantly higher than 80.0％ of the control group,there was statistically significant difference between the two groups (x2 =4.841,P ＜ 0.05).Conclusion On the basis of routine treatment,vinpocetine in the treatment of CHD can significantly reduce the serum levels of hs-CRP and IL-6,and improve the clinical efficacy.
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Aim To evaluate the efficacy and safety of different routes for vinpocetine injection by intravenous or trans-angiographic catheter on cerebral vasospasm(CVS).Methods A total of 105 aneurysmal subarachnoid hemorrhage(aSAH)patients with CVS following intracranial aneurysm embolization were chosen and randomly divided into group C, B and A, with 35 cases in each group.Patients in group C were treated with 3H therapeutic regimen, while those in group B and A were with 3H therapeutic regimen plus vinpocetine by intravenous injection or trans-angiographic catheter, respectively.The index including middle cerebral artery(MCA) blood flow velocity, National Institutes of Health stroke scale(NIHSS) score, Glasgow outcome scale(GOS) grading, clinical efficacy, hypotension rate and rehaemorrhagia rate were detected and compared among three groups.Results After the 7 d and 14 d treatment, the MCA blood flow velocity of group A and B was observed to be significantly lower than that of group C(P0.05) observed in the hypotension rate between group A and C.Also, there was no statistical difference(P>0.05)found in the rehaemorrhagia rate among three groups.However, the GOS grading of group A and B was significantly better than that of group C(P<0.05), and the grading of group A was significantly better than that of group B(P<0.05)after 3 months treatment.Conclusions Using vinpocetine by intravascular injection or by trans-angiographic catheter could be the efficient treatment for the CVS after intracranial aneurysm embolization, and vinpocetine injection by trans-angiographic catheter is the better mode of administration with the consideration of efficacy and safety.
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Objective To explore the mechanism of sulfotanshinone sodium injection in treatment of patients with sudden deafness (SD).Methods Sixty patients with SD admitted to the Department of Otorhinolaryngology of Wuxi Traditional Chinese and Western Medicine Hospital from January to December 2016 were enrolled, and they were randomly divided into a study group and a control group (each 30 cases). The same basic treatment was given in the two groups, the patients in the study group were treated with sulfotanshinone sodium 40 mg intravenous (IV) drip, while the patients in the control group were treated with vinpocetine sodium chloride 20 mg IV drip, once a day for consecutive 14 days to complete a therapeutic course, and two courses were carried out in bothgroups. Before and after treatment, the changes of hearing threshold, indexes of hemorheology and immune function were compared between the patients in the two groups, and the clinical efficacy and adverse reactions in the two groups were observed.Results After treatment, the hearing threshold, hemorheology indexes, immune function index of CD8+ were significantly lower than those before treatment, while the CD3+, CD4+, CD4+/CD8+ ratio were significantly higher than those before treatment in the two groups, and the above changes of indexes were more obvious in the study group than those in the control group hearing [threshold (dB): 16.63±2.04 vs. 17.15±1.88, plasma viscosity (PV, mPa·s): 1.27±0.14 vs. 1.31±0.11, whole blood middle shearing viscosity (mPa·s): 4.77±0.33 vs. 4.95±0.28, whole blood high shearing viscosity (mPa·s): 3.86±0.25 vs. 4.00±0.31, erythrocyte aggregation index (EAI): 1.57±0.29 vs. 1.72±0.34, CD3+: 0.70±0.05 vs. 0.64±0.05, CD4+: 0.43±0.04 vs 0.37±0.03, CD8+: 0.32±0.04 vs. 0.34±0.03, CD4+/CD8+: 1.36±0.32 vs. 1.18±0.27]; the degree of whole blood low shearing viscosity (mPa·s: 6.72±0.80 vs. 7.01±1.13) and hematocrit (HCT: 0.38±0.04 vs. 0.40±0.03) decreasing weremore significant in the control group than those in the study group. The total effective rate was higher in study group than that in the control group [86.67% (26/30) vs. 83.33% (25/30)], but the difference between the two groups was not statistically significant (P > 0.05); the incidence of adverse reactions in the study group was markedly lower than that in the control group [3.33% (1/30) vs. 20.00% (6/30),P < 0.05].Conclusions Sulfot anshinone sodium injection can effectively enhance the SD patients' hearing, and improve their hemorheology indexes and immune function; the therapeutic results of sulfotanshinone sodium injection in safety and improvement in immune function are superior to those of vinpocetine sodium chloride injection.
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AIM: To observe the inhibitory effects of vinpocetine injection on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in the rats and to explore the underlying mechanisms.METHODS: Male Wistar rats (n=50) were randomly divided into 5 groups: control group, ALI model group, and low, medium and high doses of vinpocetine treatment groups.The rats in control group were injected with 0.9% NaCl at 5 mL/kg through femoral vein.The rats in ALI model group received LPS at 10 mg/kg through femoral vein.After injected with LPS, the rats in vinpocetine treatment groups received vinpocetine at 0.2 mg/kg, 0.7 mg/kg or 1.2 mg/kg via intraperitoneal injection.The pathological changes of the lung tissues were observed under microscope with HE staining.The cell apoptosis in the lung tissues was detected by TUNEL staining.Myeloperoxidase (MPO) activity was measured by the method of spectrophotometry.The protein expression of NF-κB, ICAM-1, VCAM-1, Bax and Bcl-2 was determined by Western blot.RESULTS: Compared with ALI group, administration of vinpocetine significantly attenuated the structural injury of the lung and the infiltration of inflammatory cells.Moreover, vinpocetine decreased cell apoptosis and MPO activity in the lung tissues of ALI rats.In addition, the protein expression of NF-κB, ICAM-1, VCAM-1 and Bax was inhibited after vinpocetin treatment, whereas Bcl-2 expression was increased.CONCLUSION: Vinpocetine attenuates LPS-lung injury by reducing MPO activity and regulating NF-κB, ICAM-1, VCAM-1, Bax and Bcl-2 protein expression.
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OBJECTIVE:To observe the clinical efficacy and safety of vinpocetine combined with xueshuantong in the treatment of cerebral infarction.METHODS:56 patients with acute cerebral infarction were randomly divided into control group (28 cases) and observation group (28 cases).On the basis of routine treatment,control group was given Vinpocetine for injection 20 mg,once a day.Observation group was additionally given Xueshuantong for injection (lyophilized) 150 mg,intravenously,once a day,on the basis of control group.Both groups received treatment for 2 weeks.Clinical efficacies of 2 groups were observed.The levels ofNIHSS score、VEGF,vWF,sVCAM-1,sICAM-1,CRP and IL-8,the occurrence of ADR were observed before and after treatment.RESULTS:Total response rate of observation group (96.43％) was significantly higher than that of control group (78.57％),with statistical significance (P＜0.05).After treatment,the serum levels of VEGF in 2 groups were significantly higher than before treatment,and the observation group was significantly higher than the control group.The serum levels of NIHSS score、vWF,sVCAM-1,sICAM-1,CRP and IL-8 in 2 groups were significantly lower than before treatment,and the observation group was significantly lower than the control group,with statistical significance (P＜0.05).There was no statistical significance in the incidence of ADR between 2 groups (P＞0.05).CONCLUSIONS:Based on routine treatmem,vinpocetine combined with xueshuantong show good therapeutic efficacy and safety for cerebral infarction.
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OBJECTIVE:To investigate clinical efficacy of Sofren injection combined with Vinpocetine injection in the treatment of acute massive cerebral infarction,and its effects on hemorheological indexes and serum NOS.METHODS:A total of 60 patients with acute massive cerebral infarction in our hospital during Jan.2014-Jun.2016 were selected as research objects and divided into trial group and control group according to random number table,with 30 cases in each group.Control group was given Citicoline injection 0.5 g,ivgtt,qd.Trial group was additionally given Vinpocetine injection 20 mg added into 0.9％ Sodium chloride injection 250 mL,ivgtt,qd;1 h later washing tube,they were given Sofren injection 10 mL added into 0.9％ Sodium chloride injection 250 mL,ivgtt,for consecutive 14 d.Clinical efficacies and safety of 2 groups were observed,and hemorheological indexes and NOS levels were observed before and after treatment.RESULTS:The total response rate (83.33％)of trial group was significantly higher than that (50.00％) of control group,with statistical significance (P＜0.05).Before treatment,there was no statistical significance in hemorheological indexes or serum NOS levels between 2 groups (P＞0.05).After treatment,hemorheological indexes of 2 groups were decreased significantly,and the trial group was significantly lower than the control group.The level of serum NOS in 2 groups were increased significantly,and the trial group was significantly higher than the control group,with statistical significance (P＜0.05).No obvious ADR was found in 2 groups.CONCLUSIONS:Sofren injection combined with Vinpocetine injection show significant therapeutic efficacy for acute massive cerebral infarction,can reduce blood viscosity and increase blood perfusion with good safety.
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AIM:To investigate the effects of vinpocetine on inflammation of brain in intracerebral hemorrhage ( ICH) rats and to explore the underlying mechanisms .METHODS:All rats were randomly divided into sham group , ICH group, ICH with low dose of vinpocetine treatment group , ICH with medium dose of vinpocetine treatment group , and ICH with high dose of vinpocetine treatment group .Except sham group , the rats in other groups were injected with type VII col-lagenase to establish ICH model , and then the rats in vinpocetine treatment groups were received vinpocetine at 0.5, 1.0 or 1.5 mg/kg by intraperitoneal injection once a day for 7 days.After corresponding treatment , the impairment of neurological function in the rats was scored and the water content of the brain tissues was measured .Moreover, the activity of myeloper-oxidase (MPO) was determined by ELISA, and the protein expression of Toll-like receptors 4 (TLR4), nuclear factor-κB (NF-κB), intercellular cell adhesion molecule-1 (ICAM-1) and vascular cell adhesion molcule-1 (VCAM-1) in the brain tissues was determined by Western blot .RESULTS: Compared with ICH group , vinpocetine treatment significantly de-creased the scores of the impairment of neurological function and the water content of the brain tissues .Moreover, the activ-ity of MPO and the protein expression of TLR4, NF-κB, ICAM-1 and VCAM-1 were also reduced after vinpocetine treat-ment (P<0.05).CONCLUSION:Vinpocetine improves neurological function in ICH rats via suppression of inflamma -tion by inhibiting NF-κB signaling and expression of ICAM-1 and VCAM-1.
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Objective: To prepare voriconazole long-circulation liposomes and evaluate the characteristics of pharmacokinetics in rats.Methods: Voriconazole long-circulation liposomes were prepared by a thin film dispersion extrusion method.The drug release of voriconazole from the long-circulation liposomes was investigated in phosphate buffer solution (PBS) and in rat plasma.The physicochemical properties of the long-circulation liposomes before and after the freeze-drying were studied, such as the particle diameter and the particle shape.The concentration of voriconazole in plasma was determined after tail-vein injection of the long-circulation liposomes in rats.Results: The mean particle size of voriconazole long-circulation liposomes was (192.1±49.3)nm with homogeneous small spherical morphology as seen under a transmission electron microscope.Voriconazole was released in a sustained manner in PBS while much faster in plasma from the long-circulation liposomes.The t1/2 and AUC0-t of the long-circulation liposomes was respectively 2.17 and 2.31 times higher than that of voriconazole injection.Conclusion: Long-circulation liposomes prolong the circulation time and increase the bioavailability of voriconazole.
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OBJECTIVE:To investigate clinical efficacy and safety of breviscapine combined with vinpocetine in the treatment of acute cerebral infraction. METHODS:A total of 80 patients with acute cerebral infraction were selected from our hospital during Jan. 2014-Dec. 2015,and then divided into observation group and control group according to random number table,with 40 cases in each group. Control group was given Vinpocetine injection 20 mL+0.9％ Sodium chloride injection 250 mL,ivgtt,qd. Observa-tion group was additionally given Breviscapine injection 20 mL+5％ Glucose injection 250 mL,ivgtt,qd,at intervals of 2-3 h on the basis of control group. Both groups were treated for 2 weeks. Clinical efficacies as well as serum copeptin,NT-proBNP,albu-min cobalt binding(ACB)value,European stroke scale(ESS)and functional independence measurement(FIM)score before and after treatment were observed in 2 groups,and the occurrence of ADR was recorded. RESULTS:Total response rate of observation group(90.0％)was significantly higher than that of control group(67.5％),with statistical significance(P0.05). After treatment,serum copeptin and NT-proBNP levels of 2 groups were decreased significantly,while ACB value,ESS and FIM score were increased significantly;the improvement of observation group was significantly better than that of control group,with statistical significance(P<0.05). No obvious ADR was found in 2 groups. CONCLUSIONS:Breviscapine combined with vinpocetine can improve neurological function of acute cerebral infraction patients and show good therapeutic efficacy with good safety.
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Rhodamine B (RhB) was used to decorate an amphipathic block polymers (β-CD-[P(AA-co-MMA)-b-PVP]4) in this study. First, after activated by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, rhodamine B was marked with hydroxyethyl methacrylate (HEMA) through ester exchange reaction. Second, the labeled amphipathic block polymers (β-CD-[P(AA-(HEMA-RhB)-MMA)-b-PVP]4) were synthesized after polymerization reaction of double bones between RhB-HEMA and other reactants. Finally, the structure of product was measured by FT-IR spectra and fluorospectro photometer (FLUORO). The critical micelle concentration of RhB-labeled and unlabeled amphipathic block polymers were 4.96×10-3, 5.09×10-3 mg·L-1, respectively, indicating no change of their micellization behavior. In vivo tissue distribution and whole-body fluorescent imaging were studied by vinpocetine (VP)-loaded polymeric micelles which were prepared through a solvent evaporation method. Compared to the result of in vivo tissue distribution and whole-body fluorescence imaging, a similar bio-distribution behavior of VP-loaded polymeric micelles was found. Those proved the successful fluorescence modification with a labeling yield of 4.13%. With in vivo fluorescence imaging technology, we established a fluorescence method for modification of amphipathic block polymers.
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Objective To expose the effect and its potential mechanism of vinpocetine (Vinp) on the restenosis of dia?betic grafted veins. Methods Thirty-six Sprague-Dawley rats were randomized into saline control group and Vinp treat?ment group. The autologous jugular vein to carotid artery transplantation was performed in diabetic model rats. Normal sa?line or Vinp were intraperitoneally injected. The rats were sacrificed at 0, 2 or 4 weeks after surgery, then the grafted veins were harvested. The pathological sections were used to detect the effect of Vinp on intimal hyperplasia. The protein expres?sion of proliferating cell nuclear antigen (PCNA) was detected by immunohistochemical method, and which was described by cell proliferation index. The phosphorylation of NF-κB was detected by Western blot assay. Results The treatment of Vinp on intimal hyperplasia in vivo was significant at two weeks after surgery (17.06±5.10)μm versus control group (39.79±7.84μm, P<0.01), (30.94±5.18)μm versus (63.67±18.09)μm at four weeks after surgery (P<0.01). Vinp treatment effectively reduced the protein expression of PCNA [2 weeks:(21.07±1.38)%vs. (28.13±1.35)%,P<0.01;4 weeks:(31.73±1.38)%vs. (63.67 ± 18.09)%, P<0.01]. The treatment of Vinp inhibited phosphorylation of NF-κB at two weeks (1.08 ± 0.42 vs. 0.84 ± 0.12, P < 0.01). Conclusion Vinpocetine can effectively attenuate intimal hyperplasia in diabetic grafted veins, which might be related to its effect on inhibiting phosphorylation of NF-κB as well as inflammation.
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Objective:To investigate the clinical application and adverse events of vinpocetine injection. Methods:The application of vinpocetine injection in the patients in neurology department during December 2013 and December 2014 in a hospital was statistically analyzed. The adverse reactions of the injection reported in the professional literatures and relevant documents were also retrieved and statistically analyzed. Results:The infusion concentration of vinpocetine injection for 363 patients was more than 0. 06 mg·ml -1 ,and 3 cases of adverse reactions appeared with the main symptoms of rash and drug fever. Among 28 published literatures,19 articles were with the infusion concentration of vinpocetine injection above 0. 06 mg·ml-1 and 8 articles reported adverse reactions in varying degrees. Conclusion:Clinicians should pay attention to the instructions in the clinical course of medication in order to improve the safe and rational use of drugs.
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OBJECTIVE:To establish a method for the bacterial endotoxin test of vinpocetine raw material. METHODS:Ac-cording to the bacterial endotoxin test in the Chinese Pharmacopoeia(2010 edition,Ⅱ)Appendix Ⅺ E,the samples with different batches were used for interference test and bacterial endotoxin test by tachypleus amebocyte lysate from 2 manufacturers. RE-SULTS:The vinpocetine solutions with high concentration have interference effect on the agglutination reaction of bacterial endotox-in and the interference can be eliminated by diluting. CONCLUSIONS:The non-interference concentration of vinpocetine solutions is 0.25 mg/ml. Bacterial endotoxin test can be used to control the quality.