Inhibitory effect of sodium ferulate on inflammatory response in migraine rats based on c-Jun N-terminal kinase / p38 mitogen-activated protein kinase signaling pathway / 解剖学报

[Abstract] Objective To explore the inhibitory effect of sodium ferulate (SF) on the inflammatory response in migraine rats by regulating the c-Jun N-terminal kinase (JNK) / p38 mitogen-activated protein kinase (p38 MAPK) signaling pathway. Methods The migraine rat model was prepared by intraperitoneal injection of nitroglycerin. After successful modeling, the rats were randomly grouped into model group, SF low dose (SF-L) group (50 mg/ kg), SF high dose (SF-H) group (100 mg/ kg), SF+JNK inhibitor (SF + SP600125) group (SF 100 mg/ kg +SP600125 10 mg/ kg), and SF+JNK activator [SF + anisomycin(AN)] group (SF 100 mg/ kg +AN 5 mg/ kg), 12 in each group, another 12 SD rats without treatment were taken as blank group. The behavioral changes of the rats in each group were observed 24 hours after the administration, the levels of 5-hydroxytryptamine (5-HT), nitric oxide (NO), tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in serum were detected by ELISA, the neuronal apoptosis in brain tissue was observed by TUNEL staining, immunohistochemistry was used to evaluate the expressions of TNF-α, IL-6 and calcitonin gene-related peptide (CGRP) in brain tissue, Western blotting was used to detect the expressions of JNK/ p38 MAPK pathway-related proteins in brain tissue. Results Compared with the blank group, the number of times of scratching the head and climbing the cage of the rats in the model group increased significantly, and the apoptosis rate of neurons increased significantly; the content of 5-HT in serum decreased significantly, and the levels of NO, TNF-α and IL-6 increased significantly; the expressions of TNF-α, IL-6 and CGRP, and the ratios of phosphorylated JNK (p-JNK) / JNK and phosphorylated p38 MAPK(p-p38 MAPK) / p38 MAPK in brain tissue obviously increased (all P<0. 05). Compared with the model group, the number of times of scratching the head and the times of climbing the cage of the rats in the SF-L group and the SF-H group reduced significantly, and the neuron apoptosis rate reduced significantly; the content of 5-HT in serum increased significantly, and the levels of NO, TNF-α and IL-6 decreased significantly; the expressions of TNF-α, IL-6 and CGRP, and the ratios of p-JNK/ JNK and p-p38 MAPK/ p38 MAPK in brain tissue obviously decreased (all P<0. 05). Compared with SF-H group, the protective effect of SF on migraine rats in SF+SP600125 group enhanced significantly; the protective effect of SF on migraine rats in the SF+AN group reversed significantly. Conclusion SF may inhibit the expression of JNK/ p38 MAPK signaling pathway, effectively inhibit neurogenic inflammatory response in migraine rats, reduce neuronal apoptosis, and achieve a protective effect on migraine rats.

Effect and potential mechanism of sodium ferulate on corneal endothelial dysfunction and CEC injury / 中国药房

OBJECTIVE To investigate the effect and potential mechanism of sodium ferulate （SF） on corneal endothelial dysfunction and corneal endothelial cell （CEC） injury. METHODS The male New Zealand rabbits were divided into control group， benzalkonium chloride （BAK） group and BAK+SF group， with 6 rabbits in each group. Except for control group， the other groups were given BAK into the anterior chamber to induce bullous keratopathy model， and BAK+SF group then given SF solution 200 mg/kg intraperitoneally the next day after surgery， twice a day， for consecutive 14 d. The transparency of corneal and edema of corneal stroma in each group of rabbits （before and on the 1st， 7th， and 14th day after surgery） were observed， and the corneal thickness （14th day after surgery） and intraocular pressure （1st to 14th day after surgery） were measured. On the 14th day after operation， the corneal endothelial structure was evaluated and the expressions of functionally related proteins [phalloidin， zonula occludens-1 （ZO-1）， Na+/K+-ATPase， Ki67] were detected. On the 14th day after surgery， the corneal tissue was collected in BAK group， the primary rabbit CECs were isolated and cultured， and they were divided into blank group and SF groups with different mass concentrations. The cell viabilities after being cultured for different time， and the protein expressions of Ras homologous gene family A （RhoA）， bone morphogenetic protein receptor 1A （BMPR1A） and BMRP2 were determined in each group. RESULTS Compared with BAK group， the transparency of corneal and edema of corneal stroma were gradually improved， and the corneal thickness was significantly decreased in BAK+SF group （P＜0.05）. The rabbit CECs in BAK+SF group were only damaged to zone B and showed a normal hexagonal endothelial cells structure. The protein expressions of phalloidin， ZO-1， Na+/K+-ATPase and Ki67 in BAK+SF group were significantly increased （P＜0.05）. When SF concentration was lower than and equal to 200 mg/L， it could promote the proliferation of rabbit CEC， in concentration manner （P＜0.05） and time-dependent trend. SF at concentrations of 50， 100， and 200 mg/L could up-regulate the protein expressions of RhoA， BMPR1A and BMPR2 in concentration-dependent manner （P＜0.05）. CONCLUSIONS SF can improve the transparency of corneal and edema of corneal stroma in bullous keratopathy model rabbits， reduce corneal thickness， maintain the integrity of corneal endothelium structure， and promote the recovery of corneal endothelial function； this compound can promote the proliferation of CEC， the mechanism of which may be related to the activation of RhoA-ROCK-BMP pathway.

Study on protective effects of methyl ferulate on mitochondria of H 9c2 cardiomyocytes injured by hypoxia / 中国药房

OBJECTIVE To investigate the e ffects of methyl ferulate （MF） on the mitochondrial function of H 9c2 cardiomyocytes after hypoxia-induced injury. METHODS H9c2 cardiomyocytes were divided into normal group （no administration，no modeling ），hypoxia model group （modeling alone ），MF high-dose ，medium-dose and low-dose groups （40， 20，10 μmol/L）and positive control drug group （cyclosporin A ，1 μmol/L）. After drug pretreatment and inducing hypoxia-induced injury，the levels of lactate dehydrogenase （LDH），malondialdehyde（MDA），creatine kinase （CK）and adenosine triphosphate （ATP）were tested. The intracellular reactive oxygen species （ROS），mitochondrial membrane potential （MMP），the opening of mitochondrial membrane permeability transition pore （mPTP） were detected with flow cytometry. RESULTS Compared with hypoxia model group ，the levels of LDH ，MDA，CK and ROS fluorescence intensity were decreased significantly in MF high-dose，medium-dose and low-dose groups ，while the level of ATP was increased significantly （P＜0.01 or P＜0.05）. The red/ green fluorescence intensity ratio of MMP and the green fluorescence intensity of mPTP were increased significantly （P＜0.01 or P＜0.05）. CONCLUSIONS MF can reverse the levels of biochemical indexes in H 9c2 cardiomyocyte after hypoxia-induced injury，keep MMP stable ，reduce the opening of mPTP ，and has an obvious protective effect on the mitochondrial function of H9c2 cardiomyocytes injured by hypoxia ，and this protective effect is dose-dependent.

Research progress on the role of transient receptor potential canonical 6 in ischemia-reperfusion injury / 器官移植

Ischemia-reperfusion injury (IRI) refers to the reperfusion injury caused by the recovery of blood supply of ischemic tissues or organs, which commonly occurs in organ transplantation and other surgical procedures. IRI may cause a series of severe clinical issues, such as delayed graft function, acute kidney injury, myocardial infarction, ischemic stroke and circulatory arrest, etc. These events yield high incidence and fatality. At present, no effective solution has been available. Transient receptor potential canonical 6 (TRPC6), a member of Ca2+ channel family, is highly expressed in multiple types of cells. It may adjust many physiological functions by regulating intracellular Ca2+ concentration, which has become an important target for developing therapeutic drugs for multiple diseases. In this article, research progresses on the introduction and function of TRPC6, the association between TRPC6 and IRI and the therapeutic prospect of TRPC6 targeted drugs in IRI were reviewed, aiming to provide novel insights into the prevention and treatment of IRI during organ transplantation

Protective effects of sodium ferulate on flap transplantation via anti-inflammatory modulation and oxidative stress inhibition

Ischemia-reperfusion injury (IRI) has brought attention to flap failure in reconstructive surgery. To improve the prognosis of skin transplantation, we performed experimental IRI by surgical obstruction of blood flow and used sodium ferulate (SF) to prevent IRI in rats. After SF treatment, the morphological and histological changes of the skin flaps were observed by H&E and Masson's trichrome staining. We also detected the expression levels of COX-1, HO-1, and Ki67 by immunohistochemical and western blot analysis. Moreover, enzyme-linked immunosorbent assay was used to identify the content of tumor necrosis factor (TNF)-α, myeloperoxidase (MPO), malondialdehyde (MDA), and nitric oxide (NO) in peripheral blood and skin tissue. Compared with the model group, SF treatment significantly improved the recovered flap area (%) and promoted collagen synthesis. Cyclooxygenase-2 (COX-2) expression was significantly inhibited by heme oxygenase-1 (HO-1) induction after SF treatment. Furthermore, SF significantly inhibited the levels of TNF-α in peripheral blood, MPO and MDA in the skin tissue, and the increased synthesis of NO. Our results showed the protective effects of SF on IRI after flap transplantation and we believe that the protective effects of SF was closely related to the alleviation of the inflammatory response and the inhibition of the oxidative stress injury.

Protective Effect and Mechanism of Sodium Ferulate on Cerebral Ischemia-reperfusion Inflammatory Injury in Rats / 中国实验方剂学杂志

Objective: To investigate the protective effect of sodium ferulate on cerebral ischemia-reperfusion injury in rats and to explore its possible mechanism.Method: The cerebral ischemia reperfusion injury model was established by middle cerebral artery occlusion (MCAO) in SD male rats. 36 modeled rats with neurologic damage were randomly divided into 4 groups:model group, low,medium,high-dose sodium ferulate groups (25,50,100 mg·kg-1).Another nine rats were selected as a sham operation group.Neurological function was assessed by neurological scoring system in rats.Hematoxylin-eosin (HE) staining was performed to observe the pathological changes of the rats' brain. The levels of tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β) and interleukin-6 (IL-6) in serum and brain tissues were detected by enzyme-linked immunosorbent assay (ELISA). Western blot was used to detect the protein expression of nucleus and cytoplasm nuclear factor-kappa B p65 (NF-κB p65) in brain tissues.Result: As compared with normal group, neurological deficit score was increased; the neuronal necrosis and inflammatory cell number were present;the serum and brain tissue levels of TNF-α, IL-1β and IL-6 were increased; nucleus/cytoplasm NF-κB p65 protein expression ratio was increased significantly in model group (PPPα, IL-1β and IL-6(PPκB p65 protein(PPConclusion: Sodium ferulate protects the brain against focal cerebral ischemia reperfusion injury, and the mechanism may be related to inhibiting nuclear translocation of NF-κB p65 protein to alleviate inflammatory response.

Protective effect of cycloartenyl ferulate on lipopolysaccharide induced endothelial cell apoptosis and its mechanism / 中华急诊医学杂志

Objective@#To investigate the effect of cycloartenyl ferulate (CF) on lipopolysaccharide (LPS)-induced apoptosis in human umbilical vein endothelial cells (HUVEC), and to explore its relative mechanism.@*Methods@#Human umbilical vein endothelial cells were cultured in vitro, and the experiment was divided into the normal group, CF group, LPS group, and LPS+CF groups at different concentrations. After the corresponding treatment of cells in each group, the cell viability and apoptosis of each group were tested by the cell counter Kit-8 (CCK-8) assay and TdT-mediated dUTP nick end labeling (TUNEL) assay. The protein expression of Bax, Bcl-2, caspase-3 and the effect of CF on the protein expression of Nrf2/HO-1 pathway were determined by Western blot. One-way ANOVA were performed in multigroup mean comparison, LSD-t test was used to compare the mean values of two samples, and P<0.05 was considered statistically significant.@*Results@#Compared with the LPS group, the survival rate of HUVECs cells in the CF group was significantly increased with different doses, and the survival rate increased significantly in the 320 μmol/L CF group [(69.85±1.2)% vs ( 100.2±1.824)%, P< 0.01]. TUNEL staining showed that compared with the LPS group, the number of apoptotic positive cells in the 320 μmol/L CF group was significantly reduced [(27.33 ± 3.40) vs (11.67 ± 2.04), P<0.01]. Compared with the LPS group, Bcl-2 protein expression level was significantly increased in the CF group at different doses (P<0.01), caspase-3 and Bax protein expression were significantly decreased (P<0.01). Nrf2 protein expression level increased significantly (P<0.01), and HO-1 protein level increased significantly (P<0.01).@*Conclusion@#CF can alleviate LPS-induced apoptosis of HUVEC, which may be related to the increase of bcl-2 expression, the decrease of caspase-3 and Bax protein expression and the activation of Nrf2/ HO-1 signaling pathway.

Pharmacological research progress of sodium ferulate in cardio-cerebral vascular disease / 中草药

Sodium ferulate is the sodium salt of ferulic acid, an extract of traditional Chinese herbal medicines for promoting blood circulation and detoxification, and it is rich in sources, with few side effects and high safety. Sodium ferulate has many pharmacological effects, which is a cardiovascular drug researched and developed independently in China. It was first approved in 1990 for the clinical treatment of cardiovascular diseases. In recent years, the clinical application of sodium ferulate has become increasingly widespread, and the research field is continuously expanding. Sodium ferulate is effective in treating respiratory diseases, diabetes and complications, and protecting the liver and kidney from damage. Meanwhile it has been widely used in cardiovascular diseases. Here we reviewed the research status of the prominent pharmacological effects of sodium ferulate on cardiovascular diseases in the past 30 years, mainly focusing on the antithrombotic effects, the protection of blood vessels, and the anti-oxidative effect of sodium ferulate. It is expected to provide guidance for clinical applications of sodium ferulate.

Chemical constituents from plant of Fritillaria palldiflora / 中草药

Objective: To study the chemical constituents from Fritillaria pallidiflora. Methods: The constituents were isolated from F. pallidiflora and purified by column chromatography, and the structures were identified by spectra analysis and chemical methods. Results: Sixteen compounds were isolated from F. pallidiflora, including phenolic acids, esters, alkaloids, and the structures were identified as 1,4-diphenylbutane (1), cis-cinnamic acid (2), 4-hydroxy-3-methoxybenzaldehyde (3), acetovanillone (4), 9-octadecenoicacidmethylester (5), methyl ferulate (6), 1-O-feruloylglycerol (7), trans-isoferulic acid (8), syringaresinol (9), pinoresinol (10), 2,3-O-diferuloylglycerol (11), 1,3-O-diferuloyl-glycerol (12), cyclo (L-Pro-L-Ala) (13), cyclo (L-Leu-L-Val) (14), bis (diethylene glycol)phthalate (15), and cyclo-(Phe-Val) (16). Conclusion: All compounds are isolated from F. pallidiflora for the first time, and componds 1, 3-8, 10-13, 15, and 16 are isolated from the genus of Fritillaria for the first time.

Study on chemical constituents of Ligularia veitchiana / 中草药

Objective: To study the chemical constituents of the aerial parts of Ligularia veitchiana. Methods: The isolation and purification were carried out by macroporous resin, silica gel column chromatography, Sephadex LH-20, and semi-preparative HPLC. Their structures were elucidated on the basis of physicochemical properties and spectroscopic data. Results: A total of 16 compounds were isolated and elucidated from the aerial parts of Ligularia veitchiana, their structures were identified as: 2-hydroxplatyphyllide (1), ligudentatin A (2), 2-metyoxy-platyphillide (3), 7-hydroxy-11-hydroperoxybisabol-2,9E-diene (4), bisabola-2,11-diene-7α,10ζ-diol (5), 8β,10β-dihydroxyeremophilenolide (6), 3β(ax)-hydroxyeremophillenolide (7), 6β-hydroxy- 8α-ethoxyeremophil-7(11)-en-12,8β-olide (8), 3β,28-dibydroxylup-20(29)-ene (9), oleanolic acid (10), 3β-hydroxyolean-12-en-27- oic acid (11), ursolic acid (12), coniferyl ferulate (13), 4-O-Geranyl-sinapyl alcohol (14), 4-O-geranyl-coniferyl alcohol (15), auraptene (16). Conclusion: All compounds are isolated from Ligularia veitchiana for the first time. Compounds 4, 5, 7, 8, 11 are isolated from the genus Ligularia for the first time.

Effect of ferulate-heparin-poloxamer thermosensitive hydrogels on nerve regeneration in rats with spinal cord injury / 中国药理学通报

Aim To investigate the effect of ferulate-heparin-poloxamer (SF-HP) thermosensitive hydrogels on nerve regeneration in ratswith spinal cord injury, and provide experimental basis for clinical application. Methods SD rats were randomly divided into five groups: sham group, SCI group, SCI + HP group, SCI + SF group and SCI + SF-HP group. Rats were performed moderate contusion injuries using a vascular clip for 2 min to establish SCI animal model, then rats were given BBB score and inclined plate scoring function test after SCI. BDA tracing was employed to observe the recovery of nerve conduction function. Moreover, immunohistochemical staining and Western blot-were used to measure GAP43, Nestin and GFAP levels. Results BBB score and inclined plane test score significantly increased in SF-HP treated group as compared with the model group (P < 0. 01). Staining data showed that the structure of spinal cord was void, and this phenomenon was reversed after SF-HP administration. Data showed that the level of GAP43 and Nestin increased after SF treatment (P < 0. 05), the expression of GFAP decreased (P <0. 05), and the treatment effect of SF-HP hydrogels were better than those of SF alone (P < 0. 0 5) . BDA tracing data showed that the number of positive neurons markedly increased and the repair of nerve conduction function was significantly improved in SF-HP hydrogel group compared with SF group. Conclusion HP hydrogels enhance the effect of SF on the nerve regeneration in damaged spinal cord in rats.

Protective effect of cycloartenyl ferulate on lipopolysaccharide induced endothelial cell apoptosis and its mechanism / 中华急诊医学杂志

Objective To investigate the effect of cycloartenyl ferulate (CF) on lipopolysaccharide (LPS)-induced apoptosis in human umbilical vein endothelial cells (HUVEC),and to explore its relative mechanism.Methods Human umbilical vein endothelial cells were culturedin vitro, and the experiment was divided into the normal group, CF group, LPS group, and LPS+CF groups at different concentrations. After the corresponding treatment of cells in each group, the cell viability and apoptosis of each group were tested by the cell counter Kit-8 (CCK-8) assay and TdT-mediated dUTP nick end labeling (TUNEL) assay. The protein expression of Bax, Bcl-2, caspase-3 and the effect of CF on the protein expression of Nrf2/HO-1 pathway were determined by Western blot. One-way ANOVA were performed in multigroup mean comparison, LSD-t test was used to compare the mean values of two samples, andP<0.05 was considered statistically significant.Results Compared with the LPS group, the survival rate of HUVECs cells in the CF group was significantly increased with different doses,and the survival rate increased significantly in the 320 μmol/L CF group [(69.85±1.2)％vs ( 100.2±1.824)％,P< 0.01]. TUNEL staining showed that compared with the LPS group, the number of apoptotic positive cells in the 320 μmol/L CF group was significantly reduced [(27.33 ± 3.40)vs (11.67 ± 2.04),P<0.01]. Compared with the LPS group, Bcl-2 protein expression level was significantly increased in the CF group at different doses (P<0.01), caspase-3 and Bax protein expression were significantly decreased (P<0.01). Nrf2 protein expression level increased significantly (P<0.01), and HO-1 protein level increased significantly (P<0.01).Conclusion CF can alleviate LPS-induced apoptosis of HUVEC, which may be related to the increase of bcl-2 expression, the decrease of caspase-3 and Bax protein expression and the activation of Nrf2/ HO-1 signaling pathway.

Protective effect of sodium ferulate against lipopolysaccharide-induced preterm delivery and intra-uterine fetal death in mice / 中国药理学与毒理学杂志

OBJECTIVE To investigate the effect of sodium ferulate (SF) on lipopolysaccharide (LPS)-induced preterm delivery and intra-uterine fetal death (IUFD). METHODS Pregnant Kunming mice were subcutaneously pretreated with SF (25 or 50 mg · kg-1) from gestational day (GD) 10 to GD 15 and with the single injection of LPS (150μg·kg-1, ip) on GD15.5. The incidence of preterm delivery and IUFD was observed. HE staining was used for uterine and placental histological evaluation. The levels of thiobarbituric acid reactive substances (TBARS) and reduced glutathione (GSH) as well as the activities of glutathione S-transferase (GST) and glutathione peroxidase (GSH-Px) were detected in the maternal liver, placenta, and fetal liver using commercial kits. Interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) levels in amniotic fluid were evaluated by enzyme linked immunosorbent assay. RESULTS For LPS group, the incidence of preterm was 47.8%, delivery time was (17.5 ± 1.3) d, and the pups′survival rate was only 42.6%. Compared with LPS-treated group, SF 50 mg · kg-1 group showed a lower incidence of preterm (14.3%, P<0.01), longer gestational days (18.4 ± 0.5, P<0.05), and a higher pups′survival rate (75.6%, P<0.01). SF 50 mg · kg-1 restored the LPS-induced GSH both in the maternal and fatal liver (a tendency without statistical significance), GST activity〔(163±82) kU·g-1 protein vs (95±90) kU·g-1 protein, P<0.01)〕in the placenta, TBARS content〔(2.5±0.4)μmol·g-1 protein vs (3.1±0.6)μmol·g-1 protein, P<0.01〕in the fetal liver, and TNF-αlevel〔(11±8) ng·L-1 vs (20±8) ng·L-1, P<0.01〕in the amniotic fluid. SF also attenuated LPS-induced placental congestion and neutrophil infiltra?tion in the uterus. CONCLUSION SF may protect against LPS-induced preterm delivery and IUFD, and anti-oxidation as well as anti-inflammation may contribute to these effects.

Determination of Related Substances in Piperazine Ferulate by HPLC / 中国药师

Objective:To establish an HPLC method for the determination of related substances in piperazine ferulate. Methods:An HPLC method was used to determine the related substances in piperazine ferulate. The separation was performed on an Xtimate C18 column (250 mm × 4. 6 mm, 5 μm). The mobile phase was 0. 5% acetic acid-methanol-acetonitrile with gradient elution. The flow rate was 1. 0 ml·min-1 and the column temperature was 30℃. The detection wavelength was 286 nm and the injection volume was 20μl. Results:Ferulic acid had a good linear relationship within the range of 5-30 μg·ml-1(r=1.0000). The detection limit was 0. 02 ng. Conclusion:The method is reliable, simple, accurate, stable and durable, and suitable for the determination of related sub-stances in piperazine ferulate.

Effects of Shenfukang Capsule Combined with Sodium Ferulate on Inflammatory Factors and Immune Function of Patients with Chronic Glomerulonephritis / 现代生物医学进展

Objective:To study the effect of shenfukang capsule combined with sodium ferulate on the inflammatory factors and immune function of patients with chronic glomemlonephritis.Methods:78 patients with chronic glomerulonephritis who admitted in our hospital from February 2015 to January 2016 were divided into the observation group and the control group according to the random number method.The control group was treated with sodium ferulate,and the treatment group was treated with Shenfukang capsule combined with sodium ferulate.The clinical curative effect,serum inflammatory factors levels and immune function before and after treatment were compared between two groups.Results:After treatment,the total clinical efficacy of observation group was significantly higher than that of the control group (P ＜0.05).The serum serum levels ofIL-6 observation group,TNF-α and hs-CRP,CD8 in the two groups were significantly higher than those before treatment,which were significantly lower in the observation group than those of the control group (P ＜0.05).After treatment,the levels of CD3,CD4 and CD4 / CD8 in the two groups were significantly higher than those before treatment (P ＜0.05),which were significantly higher in the observation group than those of the control group(P＜0.05).Conclusion:Shenfukang capsule combined with sodium ferulate could effectively relieve the inflammatory response and improve the immune function with good clinical curative effect in the treatment of chronic glomerulonephritis.

Chemical constituents from Picrorhiza scrophulariiflora / 中草药

Objective: To study the constituents in the roots of Picrorhiza scrophulariiflora. Methods: The constituents of P. scrophulariiflora were separated and purified with chromatographic methods. The structures were elucidated by spectroscopic methods and chemical analyses. Results: Ten compounds were isolated from the roots of P. scrophulariiflora and identified as β-sitosterol (1), palmitic acid (2), octacosyl trans-ferulate (3), 3β-hydroxystigmast-5-en-7-one (4), 6β-hydroxystigmast-4-en-3-one (5), caffeic acid methyl ester (6), protocatechuic acid methyl ester (7), vanillic acid (8), caffeic acid (9), and piceoside (10). Conclusion: Compounds 2-7 and 9 are obtained from the plants of Picrorhiza Royle for the first time.

Bioassay of antiplatelet aggregation bioactivity in Chuanxiong Rhizoma with related Chinese patent drugs / 中草药

Objective: To develop a bioassay method to quantify the antiplatelet aggregation bioactivity (AAB) of crude Chuanxiong Rhizoma, decotion pieces, and its Chinese patent medicine for quality assessment. Methods: Chuanxiong Rhizoma sample was extracted in water by reflux. The level of AAB in extract was quantified in vitro. The blood was taken from the heart of rabbit. The platelet aggregating in platelet-rich plasma was induced by adenosine-5'-diphosphate disodium salt. The ratio of platelet inhibition was chosen as AAB marker. Sodium ferulate was a reference. The amount of AAB in aqueous extract was quantified by the Amount reaction of parallel line analysis (2.2) method. The AAB data of herbal sample was calculated by combining the AAB of extract with its extraction rate. Moreover, AAB amounts were quantified in the eight samples including crude Chuanxiong Rhizoma, decoction pieces, and Chinese patent medicines to verify this developed method. Results: Both sodium ferulate and Chuanxiong extract showed significant AAB (P < 0.01). The reliability test for quantifying AAB in solidum ferulate and Chuanxiong Rhizoma extract was passed through, and the measured value was valid. The correlation coefficient was 0.993 4 (n = 4) between the amounts of solidum ferulate in the concentration range of 15-60 mg/mL and their ratios of platelet inhibition. The RSD for the amounts of AAB was 3.43% (n = 6) by six replicated tests with the confidence limit rate of 23.90% (n = 6). The AAB amounts were significantly different among tested samples, i.e. 3.183, 2.068, 1.957, and 1.931 U/g for four Chuanxiong Rhizoma crude samples, 1.304 and 1.021 U/g for Chuanxiong Rhizoma decotion pieces and processed slice with yellow wine, 0.506 and 0.919 U/g for Suxiao Jiuxin Pills and Lemai Granule. Conclusion: The developed method can accurately quantify the level of AAB in Chuanxiong Rhizoma crude, decoction pieces, and Chinese patent medicines, which can be used to assess the product quality of Chuanxiong Rhizoma.

Effects of piperazine ferulate tablets combined with Huangqi injection on β2-microglobulin, NGAL and clinical efficacy in patients with acute renal failure / 中国生化药物杂志

Objective To investigate the effects of piperazine ferulate tablets combined with Huangqi injection on β2-microglobulin,NGAL and clinical efficacy in patients with acute renal failure.Methods A total of 56 patients with acute renal failure from June 2012 to October 2015 in our hospital were collected and randomly divided into the experimental group and the control group with 28 cases in each group.All patients before the treatment of conventional care,diuretics and vasodilators to increase the patient's serum protein and vitamins,so that patients with the body's pH,moisture and electrolyte balance,and gave hemodialysis and low molecular heparin anticoagulant therapy.Patients in the control group were treated on the base of the conventional therapy withastragalus injection 20mL/time,one time a day,intravenous drip,treatment of four weeks; patients in the experimental group were treated on the base of the control group with piperazine ferulate tablet 200mg/time,three times/day,treatment of four weeks.After treatment,compared patients' β2 microsphere protein,NGAL and KIM-1 levels.Results There was no significant difference in the survival rate between the two groups.Compared with before treatment,β2 microsphere protein,NGAL and KIM-1 levels in two groups were lower(P<0.05);Compared with control group,β2 microsphere protein,NGAL and KIM-1 levels in the experimental group were lower(P<0.05).Conclusion Piperazine ferulate tablets combine with astragalus injection in the treatment of patients with acute renal failure have a better clinical curative effect,speculate that the mechanism is relate to reduce β2 microsphere protein,NGAL and KIM-1 levels.

Determination of Residual Organic Solvents in Piperazine Ferulate by GC / 中国药师

Objective:To establish a method for the determination of benzene, chlorine alcohol and pyridine residues in piperazine ferulate. Methods:GC was used with a DB-624 (30 m × 0. 53 mm, 1. 0 μm) elastic quartz capillary column. The flame ionization detector was used with nitrogen as the carrier gas. The initial temperature was 50℃, maintaining for 5 min, and raised to 80℃ at the rate of 10℃·min-1 , and then raised to 200℃ at the rate of 50℃·min-1 , and maintaining for 4 minutes. The inlet temperature was 200℃, and the detector temperature was 220℃. The split ratio was 1 ∶1 and the injection volume was 1μl. The flow rate was 3 ml· min-1. Results:The linear range of benzene was 0.16-0.96 μg·ml-1(r=0.999 5), the average recovery was 95.7% (RSD =2.1, n=9), and the detection limit was 0.16 ng. The linear range of chlorine alcohol was 16.11-96.65 μg·ml-1(r=0.999 7), the average recovery was 97. 8% (RSD=2. 1, n=9), and the detection limit was 0. 62 ng. The linear range of pyridine was 15. 87-95. 23 μg·ml-1(r=0. 999 8), the average recovery was 99. 2% (RSD=1. 3, n=9), and the detection limit was 0. 15 ng. Con-clusion:The method is reliable, simple, accurate and stable, and suitable for the determination of benzene, chlorine alcohol and pyri-dine residues in piperazine ferulate.

Effect of Sodium ferulate on glucocorticoid-induced osteoporosis / 中国药理学通报

Aim To study the influence of Sodium fer-ulate ( SF) on bone metabolism in glucocorticoid–in-duced osteoporosis rats. Methods Thirty cases of fe-male Wistar Rats(3-month-old) were divided into con-trol group, model group and SF group ( low-dose group, middle-dose group, high-dose group ) by ran-domized block design. Double fluorochrome labeling with calcein was performed before necropsy. The left tibia was taken for bone histomorphometry. Results In static parameters, the proximal tibia cancellous bone trabecular thickness, trabecular quantity and area ratio were significantly reduced in model group compared with control group;while compared with model group, those were increased in middle and high-dose SF group. Trabecular separation degree was increased in model group compared with control group, while it was decreased in middle and high-dose SF group compared with model group. In dynamic parameters, the calcula-tion parameters of cancellous bone mark perimeter rate and the bone formation rate were increased in model group compared with control group, in middle and high-dose SF group the bone formation rate was in-creased compared with model group. In bone cells, os-teoclast number per mm, osteoblast number per mm, percent osteoblast surface perimeter and percent osteo-clast surface perimeter were increased in model group compared with control group. In growth-plate, the thickness of growth-plate was increased in model group compared with control group. In bone cells and growth-plate there was no statistical significance between treat-ment group and model group. Conclusion This study demonstrates that SF can increase bone mass and im-prove bone structure,which may be related to the im-provement of bone formation. SF is effective for GIOP in rats.