ABSTRACT
Objective: To study the therapeutic effect of point injection of Salvia Miltiorrhiza and Ligustrazine Hydrochloride Injection (SMLHI) on diabetic peripheral neuropathy (DPN) patients and its effect on oxidative stress response. Methods: A total of 100 DPN patients were selected from the Neurology Department of the Fifth Affiliated Hospital of Zhengzhou University from March 2016 to February 2018. According to the random number table method, the patients were divided into observation group and control group with 50 cases in each group. Each group was treated with routine hypoglycemic drugs, diet control and exercise control, while the control group was treated with Mecobalamin Tablets. The observation group was treated with Mecobalamin Tablets combined with SMLHI at acupoints for 4 weeks as a course of treatment for two consecutive courses of treatment. The clinical symptom score, serum superoxide dismutase (SOD), gamma-glutamyltransferase (GGT), ferritin (SF), total anti-oxidant capacity (T-AOC), and malondialdehyde (MDA) levels, median nerve and peroneal nerve conduction velocity (MNCV), median nerve, peroneal nerve conduction velocity (SNCV), and curative effect were observed and compared before and after treatment. Results: After treatment, the clinical symptom score of the observation group was significantly lower, and the total effective rate of the observation group was 84.00%, which was higher than that of the control group 64.00% (P < 0.05). The SOD level in the observation group was higher, while the GGT, SF, T-AOC, and MDA levels were lower (P < 0.05). The MNCV and SNCV in the observation group were higher (P < 0.05). Conclusion: Acupoint injection of SMLHI for DPN patients can significantly reduce oxidative stress reaction in vivo, promote the recovery of nerve function, improve clinical symptoms of patients with high safety, which is worthy of clinical promotion.
ABSTRACT
Objective To investigate the efficacy and mechanism of Salviae Miltiorrhiza and Ligustrazine Hydrochloride Injection (SMLHI). Methods The targets of chemical components of SMLHI were predicted and the compounds-targets (C-T) network was constructed. The key targets were screened through the topology analysis of the C-T network. Also, protein-protein interaction (PPI) network was established, and the Gene ontology and KEGG pathway was enriched and analyzed. The pharmacological action mechanism of SMLHI was predicted, and the mechanism was preliminarily verified by pretreating with SMLHI on the MARK expression of cerebral ischemia rats. Results Fifteen main compounds in SMLHI act on 94 targets and PRSS1, PTGS2, F2, and PTGS1 were key targets in the C-T network. There were 71 targets in the PPI network including several key nodes such as SRC, MAPK-1, MMP-9, MAPK-14, PTGS2, BCL-2, and so on. All the targets were enriched in 26 GO items and six KEGG pathways. Conclusion Results in this study preliminarily verified the action of SMLHI on cerebral infarction and diabetic peripheral neuropathy, thus laying a solid foundation for further study on the mechanism of action.
ABSTRACT
To evaluate therapeutic efficacy and safety of Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection in the treatment of chronic obstructive pulmonary diseases (COPD). All clinical trial databases were retrieved from PubMed, EMBase, ClinicalTrials, Cochrane Library, CNKI, CBM, VIP, and Wanfang. Data were searched from inception to February 2018, randomized controlled trials (RCTs) by Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection combined with chemotherapy (experimental group) compared with conventional therapy (control group) in the treatment of COPD were included. All included studies were critically appraised by two independent reviewers according to the cochrane systematic review method and using Revman 5.3 Software and State 12.0 for Meta-analysis. There were 16 RCTs were included in the evaluation and screening of selected articles with a total of 1 259 patients. The Meta-analysis showed that the total clinical efficacy of the patients in the experimental group after treatment was significantly better than that in the control group [OR = 4.67, 95% CI (3.03, 7.19), P < 0.000 01]; The improvement of forced expiratory volume in one second (FEV1) was significantly better than control group [SMD = 1.43, 95% CI (1.14, 1.72), P < 0.000 01]; Forced vital capacity (FVC) was significantly better than control group [SMD = 1.53, 95% CI (1.17, 1.90), P < 0.000 01]; FEV1/FVC was significantly better than control group [SMD = 1.12, 95% CI (0.90, 1.34), P < 0.000 01]; FEV1 in the percentage of the predicted value forced vital capacity (FVC) was significantly better than control group [SMD = 0.62, 95% CI (0.31, 0.93), P < 0.000 1] and the blood gas index of PaO2 was significantly higher than control group [MD= 9.7, 95% CI (7.92, 11.65), P < 0.000 01]; PaCO2 was significantly lower than control group [SMD =-1.51, 95% CI (-1.90, -1.12), P < 0.000 01]; SaO2 was significantly higher than control group [SMD = 0.94, 95% CI (0.48, 1.40), P < 0.000 1]. For the treatment of chronic obstructive pulmonary disease, Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection combined with chemotherapy can significantly improve the lung function of patients, but the conclusions of the study still need to be confirmed by more high-quality clinical trials.
ABSTRACT
Objective To discuss the efficacy of Ginkgo Leaf Extract and Dipyridamole Injection and Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection in treatment of acute myocardial infarction.Methods 60 cases of acute myocardial infarction were randomly divided into two groups.They were treated with routine treatment.The observation group (30 cases) was treated with Ginkgo Leaf Extract and Dipyridamole Injection on the basis of routine treatment.The control group (30 cases) was treated with Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection on the basis of routine treatment.The efficacy of Ginkgo Leaf Extract and Dipyridamole Injection and Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection in treatment of acute myocardial infarction was evaluated by the efficacy,hemorheology before and after treatment,adverse reaction during treatment.Results The effective rate of observation group was 86.7％.The effective rate of control group was 90.0％.There was no statistical significance on effective rate between two groups.Before treatment,there were no statistical significance on blood viscosity,hematocrit,platelet aggregation rate between two groups.After treatment,the blood viscosity,hematocrit,platelet aggregation rate were decreased in two groups (P ＜ 0.05).The observation group ofhematocrit and platelet aggregation rate was lower than the control group (P ＜ 0.05).But the blood viscosity of two groups had no significant difference.According to the cost and the efficiency of single drug treatment,calculate the cost/effect ratio,the Ginkgo Leaf Extract and Dipyridamole Injection of cost/effect ratio was significantly less than that of Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection (P ＜ 0.05).During treatment,there was no statistical significance on adverse reaction rate between two groups.Conclusion Ginkgo Leaf Extract and Dipyridamole Injection and Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection had a therapeutic effect on acute myocardial infarction with high safety.The Ginkgo Leaf Extract and Dipyridamole Injection could inhibit the platelet aggregation,reduce the hematocrit with low cost/effect value.
ABSTRACT
OBJECTIVE:To investigate therapeutic efficacy and safety of Salviae miltiorrhizae and ligustrazine hydrochloride injection in the treatment of vertebro-basilar artery insufficiency(VBI)after cerebral infraction. METHODS:128 patients with VBI after cerebral infraction were divided into observation group and control group according to random number table,with 64 cases in each group. Both group received general treatment. Control group was additionally given Shuxuetong injection 6 ml added into 0.9%Sodium chloride injection 250 ml,ivgtt,qd. Observation group was additionally given Salviae miltiorrhizae and ligustrazine hy-drochloride injection 10 ml into 0.9% Sodium chloride injection 250 ml,ivgtt,qd. Both groups received treatment for consecutive 2 weeks. Clinical efficacies of 2 groups were observed as well as blood lipid,vertebro-basilar artery blood velocity and blood viscosity before and after treatment. The occurrence of ADR was compared between 2 groups. RESULTS:The total effective rate of observa-tion group was 95.31%,which was significantly higher than 79.69% of control group,with statistical significance(P0.05). After treatment,above indexes of 2 groups were improved significantly,and blood lipid and vertebro-basilar ar-tery blood velocity of observation group were significantly better than control group,with statistical significance(P<0.05). No obvi-ous ADR was found in 2 groups. CONCLUSIONS:Salviae miltiorrhizae and ligustrazine hydrochloride injection shows significant therapeutic efficacy for VBI after cerebral infraction,can significantly improve blood lipid,vertebro-basilar artery blood velocity and blood viscosity with good safety.
ABSTRACT
Objective: To establish a RP-HPLC method for the determination of ligustrazine hydrochloride, ferulic acid, hydrosafflower yellow A, ginsenoside Rg1, ginsenoside Rb1, ginsenoside Re, and notoginsenoside R1 in Shuxiong prescription. Methods: The Inertsil ODS-SP (250 mm × 4.6 mm, 5 μm) was used. The mobile phase, consisting of acetonitrile-0.05% phosphoric acid solution, was programmed for a gradient elution. The flow rate was 1.0 mL/min, the detection wavelength was 203 nm, and the column temperature was 30℃. Results: The excellent linearity with correlation coefficients (r) of 0.999 3-0.999 9 was obtained. The average recoveries of the seven compounds were 97.25%-103.52% and all RSD values were less than 3%. Conclusion: The method appears to be simple, accurate, and well reproducible, which could be used for the simultaneous determination of the above-mentioned seven compounds in Shuxiong prescription.
ABSTRACT
To study the chemical constituents of Tianshu Capsule in vivo and in vitro. UPLC-Q-TOF-MS was used as the analytic method. The ferulic acid, caffeic acid, ligustrazine hydrochloride, gastrodin, 5-hydroxymethy furfural, and ligustilide were used as the reference compounds. The information on the total ion chromatogram, extraction chromatogram and the mass spectrogram were synthetically analyzed to confirm the constituents of Tianshu Capsule in vivo and in vitro. Twenty-four compounds from Tianshu Capsule were detected among five constituents came from Tianma and 19 constituents came from Chuanxiong. After oral administration of Tianshu Capsule, 13 compounds were absorbed into plasma. The findings obtained from the study can provide the useful information for the determination of bioactive substances and the perfection of quality standard of Tianshu Capsule.
ABSTRACT
Objective: The absolute bioavailability of the preparation of Chuanxiong Radix components in rats was simultaneously studied by two methods of area under absorbance-wavelength curve (AUAWC) and high performance liquid chromatography (HPLC), which would confirm the feasibility that AUAWC could be used to determine the absolute bioavailability of components of Chinese materia medica (CMM). Methods: Based on the random two-way cross-over design, 60 SD rats were given the injection of Chuanxiong Radix components by iv and the same amount of drug suspension of the tablet of Chuanxiong Radix components by ig, respectively. Blood samples were collected at various time points after the administration. Plasma concentration of the total components, sodium ferulate, and ligustrazine hydrochloride of the two preparations of Chuanxiong Radix components in rats was measured by AUAWC combined with HPLC. Pharmacokinetic parameters and absolute bioavailability were calculated by DAS 2.0 program and the data obtained by the two methods were compared. Results: After ig administration, AUC0-∞ of total components was (77.218±13.492) mg·min/L by AUAWC and AUC0-∞ of total component was (169.775±18.252) mg∙min/L for iv injection. The absolute bioavailability of tablet of ligustrazine hydrochloride were (69.134±4.853) and (16.422±2.584) mg∙min/L, respectively by HPLC. As for iv injection, AUC0-∞ of sodium ferulate and ligustrazine hydrochloride were (155.244±28.994) and (36.754±6.645) mg∙min/L, respectively. The absolute bioavailabilities of ig administration were 44.53% and 44.68%, respectively. The data obtained by AUAWC were similar to by HPLC. Conclusion: The method of AUAWC can be used to determine the absolute bioavailability on the mixed drugs in the tablet of Chuanxiong Radix components, which will be helpful to solve the problem that the total and individual drugs of the preparation can be coanalyzed together under the combination method of HPLC. It will provide better enlightenment to study the absolute bioavailability of the mixed drugs from Western compound chemicals or complex components in CMM.
ABSTRACT
Objective To observe the effect of Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection in inauxiliary treatment of ischemic stroke and its clinical efficacy. Methods 142 cases of patients with ischemic stroke, were randomly divided into experimental group and control group. Control group(n=71) were treated with conventional therapy. Test group(n=71) were treated with Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection on the basis of conventional therapy. Hemorheological changes, nerve function improvement and treatment efifcacy in two groups before and after treatment were observed and analyzed. Results After treatment, the plasma viscosity and hematocrit in control group were 1.91±0.35, (49.58±1.04)%; while experimental group were 1.17±0.28, (38.97±1.31)%, the differences between two groups were signiifcant(P<0.05). Before treatment, the neurological function score in control group was 22.49±1.21, while experimental group was 23.18±1.74, there was no signiifcant difference between two groups. After treatment, the neurological function score in control group was 10.58±0.94, while experimental group was 4.62±2.05, the difference was signiifcant(P<0.05). The total effective rate was 80.3%in control group ,while 88.7% in experimental group, the difference was signiifcant(P<0.05). Conclusion The clinical efifcacy of Salviae Miltiorrhizae and Ligustrazine Hydrochloride Injection in auxiliary treatment of ischemic stroke was accurate, and it can alleviate the symptom of patients.
ABSTRACT
OBJECTIVE: To observe the effect of ligustrazine hydrochloride on 3HSC-T6 apoptosis and to explore the possible mechanism. METHODS: LDH kit was used to detect the effect of ligustrazine hydrochloride on LDH activity. 3H-TdR incorporation assay was used to detect the effect of drug on HSC-T6 proliferation. Apoptosis was measured by using flow cytometry (FCM) analysis with Annexin-V/PI dual staining for apoptotic cell ratio. Western blotting and Real-time PCR were used to detect the protein and mRNA expression of Bcl-2, Bax and caspase-3. RESULTS: No obvious cytotoxic effect was found when the final concentration of ligustrazine hydrochloride was less than 80 μmol · L-1. 3H-TdR incorporation assay showed that ligustrazine hydrochloride inhibited HSC-T6 proliferation at the concentrations of 50 and 70 μmol · L-1. FCM detection showed that ligustrazine hydrochloride dose-dependently stimulated apoptosis of HSC-T6. Western blotting results showed that ligustrazine hydrochloride promoted HSC-T6 apoptosis by inhibiting Bcl-2, and increasing Bax and caspase-3 protein expression. Further use of real-time PCR showed that ligustrazine hydrochloride inhibited Bcl-2 mRNA expression, and promoted the mRNA expression of Bax and caspase-3. CONCLUSION: Ligustrazine hydrochloride has the function of promoting the apoptosis of HSC-T6 by inhibiting Bcl-2, and promoting Bax and caspase-3 at both protein and mRNA levels.
ABSTRACT
OBJECTIVE: To set up a rapid and simple HPLC method for the determination of ligustrazine hydrochloride in plasma and tissues in mice, and study the pharmacokinetic characteristics and tissue distribution in healthy Kunming mice after intravenous injection of Salviae miltiorrhiza ligustrazine hydrochloride injection and ligustrazine hydrochloride.
ABSTRACT
Objective To observe the effect of ligustrazine hydrochioridc(LHC) injection on TGF-β1 -induced proliferation and type IV collagen secretion in the human mesangial cells(HMCs). Methods The interstitial fibrosis in kidney disease was mimicked by inducing proliferation and type IV collagen secretion in HMCs with TGF- β1. The experiment was divided into 5 groups: blank, control, low, medium, and high(10, 30, and 100 μg/ml)ligustrazinc hydrochloride groups. MTT method was adopted to examine the proliferation and inhibition rate of HMCs. Enzyme-linked immunosorbent assay was used to determine the production of type IV collagen in cultured HMCs. Results LHC at high concentration (100 μg/ml) significantly inhibited the proliferation of HMCs (P<0. 01). LHC also inhibited the production of type IV collagen, with the significant inhibition found when at the concentration of 100 μg/ml (P
ABSTRACT
Objective To investigate the clinical efficacy of Tongluohuayu decoction treating ankylosing spondylitis (AS). Methods 100 cases of AS were randomly recruited into a treatment group ( 50 cases) and a control group ( 50 cases). In control group, aceclofenac enteric-coated tablets and methotrexatum were administered. On the basis of control group, the treatment group was taken with Tongluohuayu decoction in addition. Results After the treatment, abnormal indexes was improved markedly in the treatment group (P<0.01 or P<0.05 ) . The total effective rate (96%) in treatment group was significantly higher than the control group (70%) , while the adverse reactive rate ( 21.6%) was significantly lower than the control group (34%) . Conclusion Tongluohuayu decoction has good therapeutic effects in treating ankylosing spondylitis clinically.
ABSTRACT
Objective To observe the clinical efficacy of incipient diabetic nephropathy treated with Ligustrazine Hydrechloride Injection plus Candesartan Cilexetil.Methods 80 cases of incipient diabetic nephropathy were randomly divided into a treatment group and a control group,with 40 cases in each group.On the basis of treated with insulin and antidiabetic drugs,The control group was given Candesartan Cilexetii and the treatment group was given Candesartan Cilexetil together with Ligustrazine Hydrochloride Injection.Results Plasma level of ET and NO,UAER and Ua1-MG of the two groups were all reduced,while the improvement of the treatment group was better than the control group.Conclusion The combination treatment of Ligustrazine Hydrochloride Injection and Candesartan Cilexetil was an ideal one for patients with incipient diabetic nephropathy.
ABSTRACT
Objective To optimize the proportion of three transdermal penetration enhancers on transdermal absorption of ligustrazine hydrochloride.Methods Permeation tests in vitro through BALB/c nude mouse skin in two compartment diffusion cells were performed to study the effect of synthetic borneol,menthol,and Azone on trandermal absorption of ligustrazine hydrochloride by changing their concentrations,and uniform design method was used to determine the penetration coefficient of ligustrazine hydrochloride and optimize the proportion of three transdermal penetration enhancers.ResultsThe optimal proportion and contents of synthetic borneol,menthol,and Azone were 1.5%∶1.5%∶1.5%(15 mg/mL∶15 mg/mL∶15 mg/mL),the real penetration coefficient of ligustrazine hydrochloride was 69.575 ?g/(h?cm2),while the theoretical penetration coefficient was 69.749 ?g/(h?cm2).Conclusion Uniform design method is an effective way to optimize the proportion of three transdermal penetration enhancers on trandermal absorption of ligustrazine hydrochloride.
ABSTRACT
Objective:To investigate the effect of synthetic borneol on penetration mechanism of ligustrazine hydrochloride. Methods: Permeation tests in vitro through rabbit skin in two compartment diffusion cells were performed to study the effect of synthetic borneol on transdermal absorption of ligustrazine hydrochloride by changing concentrations of synthetic borneol and rabbit skin condition. Results: Ligustrazine hydrochloride permeation coefficient increased linearly with incerease of concentrations of synthetic borneol, while those through strippde stratum corneum skin were not varied. Synthetic borneol enhanced the deposit functions of whole skin and stripped stratum corneum skin. Conclusions: Synthetic borneol could enhance the percutaneous absorption of ligustrazine hydrochloride, mainly through the stratum corneum, and increase the deposit function.
ABSTRACT
AIM: To investigate the therapeutic effect of Ligustrazine Hydrochloride Injection(LHI) plus Salvia miltiorrhiza Injection(SMI) and LHI plus Ginkgo leaf extract and Dipydamole Injection(GDI) in treating diabetic microalbuminuria. METHODS: 75 inpatients were randomly divided into group SMI(n=35) and group GDI(n=40).Group SMI was treated with LHI 160 mg plus SMI 20 mL intravenous drip daily for 14 days and group GDI with LHI 160 mg plus GDI 20 mL.Their blood samples were collected for measuring glucose,insulin,HbA1c,lipid,creatine and uroacid, and their urine samples for measuring microalbuminuria before and after treatment.The results were statistically(analyzed.)(RESULTS: Before)(treatment,) triglyceride and cholesterol concentrationincreased significantly in group SMI than in group GDI(all P
ABSTRACT
OBJECTIVE:To study the preparation of the ligustrazine hydrochloride liposome and evaluate its quality.METHODS:The liposome was prepared by various methods on a trial basis.The entrapped efficiency(EE)of the liposome derived from passive loading and active loading was compared.RESULTS:The ammonim sulfate gradient technology had the highest EE of 48.63%and its mean size was 6.5?m and the pH was 5.93.It was stable in refrigeratory(4℃～10℃)storage for 30 days.CONCLUSION:The ammonim sulfate gradient technology of preparation of the ligustrazine hydrochloride liposome is feasible.
ABSTRACT
Objective:To study the regulatory effects of Ligustrazine Hydrochloride(LHC)on tumor-induced immunosuppression by Colon26 cells in vitro.Methods:Colon26 cells were cultured for 48 h in the presense of LHC and either the cell fraction or the cultural supernatants was collected,with the untreated Colon26 cells as control for the study.The down-regulating effects of LHC on tumor immunosuppressions (including the suppressed NK killing and ConA induced transformation of murine spleen cells detected by MTT,and the reduced expression levels of IL-2R?,CD3?+?+ and CD3?-?+ detected by FCM) were determined.The concentrations of immunosuppressive cytokines,including TGF-?1,VEGF,IL-4,IL-6 and IL-10,in the supernatants were analyzed by quantitative ELISA.The relationship among the down-regulatory effects of LHC on secretion immunosuppressive cytokines and tumor immunosuppressions were evaluated by multiple linear regression analysis.Results:All of the cytokines assayed were found in the supernatant of Colon26 treated without LHC,in which TGF-?1 was the highest,and the significant inhibition of five immune functions mentioned above was showed.To the Colon26 treated by LHC,the concentrations of TGF-?1,IL-6 and IL-10 in the first re-cultured supernatant and its inhibition of five immunol functions decreased greatly.The concentrations of TGF-?1 and IL-6 in the second re-cultured supernatant and its inhibitions of transformation,CD3+?+ and CD3-?+resumed highly.The positive correlations existed between TGF-?1 and inhibition of immunol functions except for transformation,between IL-6 and inhibition of transformation or CD3-?+,between IL-10 and inhibition of NK killing or IL-2R? or CD3+?+,respectively.Conclusion:LHC can exert down-regulate effects on Colon26 secretion of immunosuppressors and its tumor immunosuppression.Reducing tumor immunosuppression of Colon26 through decreasing its secretion of immunosuppressors should be one of anti-tumor mechanisms of LHC.