1.Comparative study of pharmacokinetics and tissue distribution of 8-cetylberberine and berberine in rats.
Yu-Li HU ; Chao CHEN ; Zong-Yao ZOU ; Xue-Gang LI ; Xiao-Li YE
Acta Pharmaceutica Sinica 2014;49(11):1582-1587
The concentrations of berberine (BBR) and 8-cetylberberine (8-BBR-C16) in rat plasma and tissue were determined by RP-HPLC. Both the plasma pharmacokinetics characteristic and tissue distribution differences of BBR and 8-BBR-C16 were compared to provide experimental data for the mechanism research and further drug development. After the oral administrations of BBR and 8-BBR-C16 at the dose of 80 mg x kg(-1) for rats, the pharmacokinetics result showed that compared with BBR, the C(max) and AUC(0-t), of 8-BBR-C16 increased by 2.8 times and 12.9 times respectively, t1/2 extended from 3.61 h to 11.90 h. The tissue distribution result showed that compared with BBR, the concentration of 8-BBR-C16 in various organizations increased and the retention time extended remarkably. The maximum concentration was achieved in lung and the highest concentration in it was 3 731.82 ng x g(-1). After being derived, the C(max) in plasma and bioavailability of 8-BBR-C16 increased remarkably and the circulation time in vivo extended. The drug concentration in tissue increased remarkably, and the distribution ratio changed too, with strong targeting selection in lung.
Administration, Oral
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Animals
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Berberine
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analogs & derivatives
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pharmacokinetics
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Biological Availability
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Chromatography, High Pressure Liquid
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Rats
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Tissue Distribution
2.Study on membrane injury mechanism of total alkaloids and berberine from Coptidis Rhizoma on Aeromonas hydrophila.
Dong-fang XUE ; Zong-yao ZOU ; Biao CHEN ; Yan-zhi WANG ; Hao WU ; Xiao-li YE ; Xue-gang LI
China Journal of Chinese Materia Medica 2015;40(9):1787-1792
To explore the antibacterial activity and mechanism of total alkaloids and berberine from Coptidis Rhizoma on Aeromonas hydrophila, and determine the effect of total alkaloids and berberine from Coptidis Rhizoma on minimum inhibitory concentrations, permeability and fluidity of cell membrane, conformation of membrane proteins and virulence factors of A. hydrophila. The results showed that both total alkaloids and berberine from Coptidis Rhizoma had antibacterial activities on A. hydrophila, with minimum inhibitory concentrations of 62.5 and 125 mg · L(-1), respectively. Total alkaloids and berberine from Coptidis Rhizoma could increase the fluidity of membrane, change the conformation of membrane porteins and increase the permeability of bacteria membrane by 24.52% and 19.66%, respectively. Besides, total alkaloids and berberine from Coptidis Rhizoma significantly decreased the hemolysis of exotoxin and the mRNA expressions of aerA and hlyA (P < 0.05, P < 0.01), the secretion of endotoxin and the mRNA expression of LpxC (P < 0.05, P < 0.01). The results suggested that the antibacterial activity of total alkaloids and berberine from Coptidis Rhizoma on A. hydrophila may be related to the bacteria membrane injury. They inhibited the bacterial growth by increasing membrane lipid fluidity and changing conformation of membrane proteins, and reduced the secretion of virulence factors of A. hydrophila to weaken the pathogenicity.
Aeromonas hydrophila
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drug effects
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genetics
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metabolism
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Alkaloids
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pharmacology
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Anti-Bacterial Agents
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pharmacology
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Bacterial Proteins
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genetics
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metabolism
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Bacterial Toxins
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biosynthesis
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Berberine
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pharmacology
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Cell Membrane
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drug effects
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genetics
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metabolism
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Coptis
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chemistry
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Drugs, Chinese Herbal
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pharmacology
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Membrane Fluidity
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drug effects
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Rhizome
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chemistry
3.Arousals in children with obstructive sleep apnea-hypopnea syndrome.
Zhen-yun HUANG ; Da-bo LIU ; Shu-yao QIU ; Jian-wen ZHONG ; Zong-yu TAN ; Jie YU ; Chang-zhi SUN ; Yu ZOU ; Jie WANG
Chinese Journal of Otorhinolaryngology Head and Neck Surgery 2008;43(12):929-934
OBJECTIVETo explore the difference of arousal index between the children with obstructive sleep apnea-hypopnea syndrome (OSAHS) and children with primary snoring. Furthermore, to explore the correlation between the above mentioned arousals and the apnea-hypopnea index (AHI) and lowest oxygen saturation (LSaO(2)).
METHODSBetween March 2007 and February 2008, 102 children suspected of OSAHS underwent overnight polysomnogram monitoring in our medicine sleep center. OSAHS was diagnosed according to the general criterion [Draft of guidelines for the diagnosis and treatment of pediatric sleep apnea hypopnea syndrome (Urumqi) which was published in Chin J Otorhinolaryngol Head Neck Surg in February, 2007]. One-hundred and two children were divided into two groups according to the guidelines. Sixty six children [56 boys, 10 girls; aged 4 - 17 years, (7.01 +/- 2.24) years (x(-) +/- s)] who were diagnosed as OSAHS were enrolled in study group and 36 children [29 boys, 7 girls; aged 4 - 13 years, (7.44 +/- 2.68) years] who were diagnosed as primary snoring made up control group. The difference of spontaneous arousal index, total arousal index and arousal index related to respiratory stimuli and limb movement were compared between the two groups. Besides this, the correlation between spontaneous arousal index, total arousal index and arousal index related to respiratory stimuli and limb movement and AHI and LSaO(2) were also analyzed. Furthermore, the study group were divided into three subgroups according to AHI (< or = 10 times/h, 10 times/h < AHI < or = 20 times/h, > 20 times/h). Spontaneous arousal index, total arousal index and arousal index related to respiratory stimuli and limb movement were compared among the three groups.
RESULTSThe increased total arousal index and arousal index related to respiratory stimuli and the decreased spontaneous arousal index of study group were significant as compared to those of control group (Mann-Whitney U, z value, -3.148, -3.866, -2.791; P value, 0.002, 0.000, 0.005, respectively). The increased arousal index related to respiratory stimuli were significant as being compared among the three groups. Arousal index related to respiratory stimuli was correlated with AHI (coefficient correlation: 0.734, P = 0.000). Other kinds of arousals and arousal index related to respiratory stimuli were not correlated with LSaO(2) (Spearman rank correlation analysis). When compared to control group, stage I increased and stage REM decreased and the difference was significant (z were -2.423, -3.519; P were 0.015, 0.000).
CONCLUSIONSThe arousal index related to respiratory stimuli were increased and spontaneous arousal index were decreased in children with OSAHS. Arousal index related to respiratory stimuli is more suitable to show the degree of sleep fragment than other arousal index.
Adolescent ; Arousal ; Case-Control Studies ; Child ; Child, Preschool ; Female ; Humans ; Male ; Polysomnography ; Sleep Apnea, Obstructive ; physiopathology ; Snoring
4.Transcatheter pulmonary valve replacement in sheep: 6-month evaluation of self-expanding valved stents.
Gang-jun ZONG ; Yuan BAI ; Yong-wen QIN ; Hai-bin JIANG ; Hao ZHANG ; Ying-long YAO ; Yi-qing ZOU ; Xian-xian ZHAO ; Hong WU ; Xin-miao HUANG
Chinese Journal of Cardiology 2008;36(2):151-155
OBJECTIVEThe purpose of this study was to determine the feasibility of transcatheter pulmonary valve replacement in sheep up to 6 months post procedure.
METHODSFresh sheep pericardium treated with a 0.6% glutaraldehyde solution for 36 hours was sutured to a valvular ring and then fixed onto a newly designed nitinol self-expandable stent. Thoracotomy was performed in sheep (23.5 +/- 3.1) kg under general anesthesia and the device was delivered into the native pulmonary valve of the sheep via the anterior wall of right ventricle by catheter and fooled for 6 months.
RESULTSOne sheep died 4 months after the procedure due to in-stent thrombosis. Another 4 animals survived the 6-month observing period. Angiographic and hemodynamic measurements confirmed good positioning and function of the stents with a competent valve immediately post procedure and 6 months post the procedure in surviving animals.
CONCLUSIONImplantation of the nitinol self-expandable stent in the pulmonary valve position by a transcatheter approach is feasible and good function of transcatheter implanted memory nitinol valved stents was shown after 6 months of implantation in sheep.
Animals ; Disease Models, Animal ; Female ; Heart Valve Prosthesis ; Heart Valve Prosthesis Implantation ; instrumentation ; methods ; Male ; Pulmonary Valve ; surgery ; Sheep ; Stents
5.A randomized controlled Multi-center clinical trial on mosapride in the treatment of functional dyspepsia.
Shi-yao CHEN ; Ji-yao WANG ; Chou-wen ZHU ; Yao-zong YUAN ; Bing ZOU ; Lu XIA ; Ji-yong LIU ; Hong-wei XU ; Shang-zhong ZHANG ; Qing WANG ; Xiang-jun XIE ; Zhi-quan ZHAO ; Lin LIN ; Nai-zhong HU ; Jian-ming XU
Chinese Journal of Epidemiology 2004;25(2):165-168
OBJECTIVETo evaluate the effectiveness and safety of mosapride on treatment of functional dyspepsia.
METHODSRandomized controlled clinical trial was conducted and patients suffered from functional dyspepsia were included. 5 mg mosapride was given three times daily for 4 weeks in the treatment group. 10 mg domperidone was given three times daily for 4 weeks as control. Changes on symptom score, gastric empty or new occurring events were included as outcomes.
RESULTS231 patients suffered from functional dyspepsia were selected by inclusion and exclusion criteria from August 15 to Oct 22, 1999. Of these, 108 (46.8%) were males, versus 123 (53.2%) females and 118 (51.2%) in the treatment group and 113 (48.9%) as controls. 222 (96.1%) patients were followed up. Results showed that the total efficacy rates in early satiety and abdominal distension were 84.5% and 90.1% in mosapride after the 2 weeks of treatment. Mosapride seemed to be more effective in improving symptoms of belching and heartburn than that in controls (P < 0.05). In 4 weeks, the total efficacy in improving symptoms of abdominal distention and belching showed more effective in mosapride than that in controls (P < 0.05). Decrease of symptoms score was more in mosapride than that in controls (P < 0.05). Mosapride was less effective in controls in improving the gastric empty in terms of proportion (46.2% vs. 25.9%, P = 0.020) and range (46.2% vs. 24.0%, P = 0.003). Side effects would include diarrhea, constipation, headache, dizziness, insomnia, skin scare and the like. There was no significant difference between the two groups (9.6% in mosapride vs. 14.0% in controls).
CONCLUSIONMosapride was safe and effective in improving the symptoms and gastric empty of functional dyspepsia.
Adult ; Benzamides ; adverse effects ; therapeutic use ; Dyspepsia ; drug therapy ; Female ; Gastrointestinal Agents ; adverse effects ; therapeutic use ; Humans ; Male ; Middle Aged ; Morpholines ; adverse effects ; therapeutic use ; Treatment Outcome
6.Effects of Electroacupuncture on Skeletal Muscle Atrophy-associated Protein in Hind Limbs of Traumatic Spinal Cord Injury Rats
Rui FAN ; Zong-hui WU ; Xiao-lin CHEN ; Zuo-qiang ZOU ; Zai-yun LONG ; Lan YAO ; Bin LI
Chinese Journal of Rehabilitation Theory and Practice 2019;25(10):1133-1139
Objective:To explore the effects and mechanism of electroacupuncture (EA) on expression of myostatin (MSTN), muscle-specific ring finger protein 1 (MuRF1/Trim63), F-box only protein 32 (Atrogin-1/ Fbxo32), myogenic differentiation antigen (Myod) and myogenin (Myog) in traumatic spinal cord injury (TSCI) rats. Methods:A total of 45 adult female Sprague-Dawley rats were randomly divided into sham operation group (