1.Histone deacetylase 6: structure, functions and development of selective inhibitors.
Acta Pharmaceutica Sinica 2015;50(1):7-14
Histone deacetylase 6 (HDAC6) is an unique subtype of histone deacetylases with two tandem deacetylase domains and substrate specificity for non-histone proteins. It is involved in many important physiological and pathological processes and has become a promising therapeutic target in recent decades. Different kinds of potent HDAC6-selective inhibitors have been reported around the world. This paper reviews the progress in the study of structure and functions of HDAC6 as well as the development of HDAC6-selective inhibitors.
2.Determination of contents of berberine type alkaloids in Huanglian Shangqing Pills(Tablets)
Chinese Traditional Patent Medicine 1992;0(12):-
AIM: To separate and determine berberine type alkaloids in Huanglian Shangqing Pills(tablets)(Rhizoma Coptidis,Fructus Gardeniae,Fructus Forsythiae,Cortex Phellodendri Chinensis,etc.). METHODS: RP-HPLC was used,and the mobile phase consisted of acetonitrile-solution of potassium phosphate(3.4 g?L~(-1),adjust pH to 3.0 with H_3PO_4)(40∶60),with 1.7 g?L~(-1) SDS.The detecting wavelength was at 345 nm. RESULTS: The contents of five kinds of berberine type alkaloids,berberine,palmatine,coptisine,epiberberine and jatrorrhizine in Huanglian Shangqing Pills(tablets) produced by 10 pharmaceutical factories were determined. CONCLUSION: The method is simple,accurate with a good recovery and repeatability.The method can be used to control the quality of Huanglian Shangqing Pills(Tablets).
3.Histone deacetylase 6: structure, functions and development of selective inhibitors.
Acta Pharmaceutica Sinica 2015;50(1):7-14
Histone deacetylase 6 (HDAC6) is an unique subtype of histone deacetylases with two tandem deacetylase domains and substrate specificity for non-histone proteins. It is involved in many important physiological and pathological processes and has become a promising therapeutic target in recent decades. Different kinds of potent HDAC6-selective inhibitors have been reported around the world. This paper reviews the progress in the study of structure and functions of HDAC6 as well as the development of HDAC6-selective inhibitors.
Histone Deacetylase Inhibitors
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pharmacology
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Histone Deacetylases
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chemistry
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Humans
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Substrate Specificity
4.The Effect of A Novel Class Ⅲ Antiarrhythmic Drug-Nifekalant On Action Potential of Atrium And Pulmonary Vein
Hao HAN ; Pihua FANG ; Xiulan LIU
Chinese Journal of Practical Internal Medicine 2006;0(16):-
Objective To investigate the effect of Nifekalant on action potential of atrium and pulmonary vein and the possible clinical efficacy of Nifekalant against atrial tachyarrhythmias.Methods left and right atrium and pulmonary vein removed from 15 white rabbits were made into tissue preparations(0.5 cm?1.5 cm).Action potential was induced by electric stimulation with twofold capture threshold and recorded by standard glass microelectrode technique.Effective refractory periods of left and right atrial and pulmonary vein tissues were measured with burst and programmed stimulation.The Action potentials and effective refractory periods of various tissues were compared between before and after irrigation of Tyrodes fluid containing Nifekalant of 2.13 mg/L.Results After irrigation of Tyrodes fluid containing Nifekalant,APD90 was prolonged[(51?16)ms vs(78?33)ms,P
5.Epidemiology of serum lipid abnormality in patients with coronary artery disease
Hao LIU ; Jinming YU ; Fang CHEN
Chinese Journal of Practical Internal Medicine 2000;0(12):-
Objective To investigate the lipidemia of patients with coronary artery disease(CAD)in China.Methods The survey engaged 52 centers in 7 cities in China recruiting patients with coronary artery disease in a hospital-based setting.Each center was asked to recruit all hospitalized patients with CHD from 1-Jun-2005 to 31-Sep-2005.The study population consisted of 3513 patients with CAD.Results Of the 3513 patients,the prevalence of the lipidemia was 79.7%.And the prevalence of the lipidemia in
6.Ultrasound-guided percutaneous injection of lauromacrogol for the treatment of hepatic hemangiomas
Guochen SHANG ; Hao LIU ; Fang LIU ; Weigang CHEN
Journal of Interventional Radiology 2014;(6):522-524
Objective To investigate the effect of ultrasound- guided percutaneous injection of lauromacrogol in treating hepatic hemangiomas. Methods During the period from June 2010 to Jan. 2013 at authors’ hospital, a total of 32 patients with hepatic hemangiomas were treated with ultrasound-guided percutaneous injection of lauromacrogol. The largest lesion was 6.0 cm × 5.6 cm in size, and the smallest lesion was 3.0 cm × 2.6 cm in size. Before and after the treatment ultrasonography, hepatic functions and measurement of tumor size were performed, and the results were evaluated. Results A total of 54 times of puncturing were carried out for the 32 patients. Three times of puncturing were made in 2 cases , two times of puncturing in 18 cases, and single time of puncturing in 12 cases. Complete cure was achieved in 25 cases (78.1%) and effective result was obtained in 7 cases, with an effective rate of 100%. After the treatment, all patients complained of different degrees of pain at hepatic region, which were relieved spontaneously. Two patients developed fever (37.5 - 38.5℃), and after physical cooling the body temperature fell to normal within two days. One patient developed mild nausea and vomiting, which disappeared after symptomatic treatment. No severe complications occurred. Conclusion Ultrasound- guided percutaneous injection of lauromacrogol is a simple, safe and effective treatment for hepatic hemangiomas. Besides, this technique has no serious complications.
7.Determination of Solubility and Apparent Oil and Water Partition Coefficient of Saponin H1
Qilong FANG ; Hongwei LIU ; Jiangyun LIU ; Lili HAO ; Shilin YANG
China Pharmacy 2016;27(3):364-366
OBJECTIVE:To determine the solubility and apparent oil and water partition coefficient (lg P) of saponin H1,and provide reference for dosage form design and druggability research of saponin. METHODS:HPLC-ELSD was conducted to deter-mine the equilibrium solubility of saponin H1 in different organic solvents and pH buffer solutions;shaking flask was applied to de-termine lg P value of saponin H1. RESULTS:The equilibrium solubility of saponin H1 in water,methanol and ethanol at 25 ℃ was 0.09175 g/L,96.51 g/L and 46.89 g/L,respectively. The solubility increased apparently at high pH within pH range at 7.6-10.0;the lg P value was between 0.695-0.773 in buffers within pH range at 6.0-8.0. CONCLUSIONS:Saponin H1 and the oleanolic acid type saponins belong to low solubility, low transmission components, so it is not suitable for use as a conventional oral formulation is developed.
8.Effect of acupuncture plus swallowing disorder therapeutic apparatus on deglutition disorder caused by early stroke
Bo LIU ; Fang ZHANG ; Yachuan LIU ; Shuang HAO ; Yun LAN
Chinese Journal of Primary Medicine and Pharmacy 2016;23(13):1986-1990
Objective To observe the effect of acupuncture plus thunder fire moxibustion plus deglutition training plus VitalStim electrical stimulation on patients with deglutition disorder of early stroke.Methods 80 patients with deglutition disorder of early stroke were randomly divided into treatment group and control group,40 cases in each group.The treatment group was treated with acupuncture plus thunder fire moxibustion plus deglutition training plus VitalStim electrical stimulation,while the control group was only treated with deglutition training.The therapeutic effects of all patients were assessed by using drinking experiment before therapy and twenty times after therapy. Results The total effective rate of the treatment group was 97.5%,which was significantly higher than 82.5% of the control group,the difference was statistically significant(χ2 =12.50,P <0.05).Watian integration of the two groups were decreased after treatment,the difference was significant(t =5.606,9.056,all P <0.05),which of the treatment group was significantly lower than the control group,the difference was statistically significant(t =3.044,P <0.05). The lung infection rate and malnutrition rates in the control group were 10.0% and 20.0%,which were significantly higher than those in the treatment group(2.5% and 5.0%),the differences were statistically significance(χ2 =4.80, 10.29,all P <0.05).Conclusion Acupuncture plus thunder fire moxibustion plus deglutition training plus VitalS-tim electrical stimulation are beneficial to the recovery of swallowing functions to early swallowing disorder in patients and could avoid the incidence of aspiration pneumonia and malnutrition.
9.The inhibitory effect of dexamethasone on the expression of IL-1?in the lung and the visceral sensory afferent system of asthmatic guinea pigs
Deshou CAO ; Hao TONG ; Xiaoxiang LIU ; Li LIU ; Xiubin FANG
Chinese Pharmacological Bulletin 1986;0(06):-
Aim To explore the inhibitory effect of dexamethasone on the expression of IL-1? in the lung and the visceral sensory afferent system(C_7-T_5 spinal ganglia and the corresponding posterior horn of the spinal cord) of asthmatic guinea pigs. Methods Experimental asthma model of guinea pigs was induced by ovalbumin in vivo. The expression of IL-1? was detected by means of immunohistochemistry in the C_7-T_5 spinal ganglia and the corresponding posterior horn of the spinal cord of all guinea pigs. The expression of IL-1? protein was investigated by Western blot in the lung, C_7-T_5 spinal ganglia and the corresponding posterior horn of the spinal cord of all guinea pigs. Results The expression of IL-1? in the lung, C_7-T_5 spinal ganglia and the corresponding posterior horn of the spinal cord of the asthmatic guinea pigs was much higher than that of the control groups(P
10.Effects of suppressing the expression of miRNA-21 on the apoptosis and invasion abilities of cholangiocarcinoma cells and its target gene
Hao YOU ; Qiang HUANG ; Chenhai LIU ; Fang XIE ; Kai ZHU
Chinese Journal of Hepatobiliary Surgery 2011;17(9):760-763
ObjectiveTo discuss the effects of apoptosis and invasion of RBE cells caused by miRNA 21 suppression and further investigate the potential role of miRNA-21 plays on target mRNA regulation. MethodsThe RNAi technology was employed to suppress the expression of RBE cells.The changes in RECK mRNA and protein expressions were detected by RT-PCR and Western blotting respectively. Changes occurred in apoptosis was closely monitored by flow cytometry (FCM). The invasion of RBE cells was analyzed in vitro by invasion assay (transwell). ResultsThe expression of miRNA-21 was clearly suppressed while the RECK mRNA and protein were over-expressed. The rate of apoptosis was significantly accelerated and there was a dramatic decrease in RBE cells' ability to invade after miRNA-21 knockdown. ConclusionThrough miRNA-21 suppression, the rate of apoptosis of RBE cells was accelerated whereas their invasion ability was greatly reduced. RECK was found to be the target gene of miRNA-21 which participates in the regulation process of regulation.