2.Construction of the pharmacophore model of acetylcholinesterase inhibitor
Yong ZHU ; Xinyue TONG ; Yue ZHAO ; Hui CHEN ; Fengchao JIANG
Acta Pharmaceutica Sinica 2008;43(3):267-276
Based on ninety three acetylcholinesterase inhibitors (AChEIs) which have the same mechanism of action but are different in structural characteristics, the pharmacophore model for acetylcholinesterase inhibitor was constructed by the CATALYST system. The optimal pharmacophore model with three hydrophobic units, a ring aromatic unit and a hydrogen-bond acceptor unit were confirmed (Weight=3.29, RMS=0.53, total cost-null cost=62.75, Correl=0.93, Config=19.05). This pharmacophore model will act on the double active site of acetylcholinesterase and is able to predict the activity of known acetylcholinesterase inhibitors that are used for clinical treatment of Alzheimer's disease (AD), and can be further used to identify structurally diverse compounds that have higher activity treating with Alzheimer's disease (AD) by virtual screening.
3.The bi-pedicled gastrocnemias myocutaneous flap:its anatomic basis and clinical application
Yong-Qing XU ; Jun YANG ; Yue-Liang ZHU ;
Chinese Journal of Orthopaedic Trauma 2004;0(12):-
Objective To provide a clinical anatomic basis for the bi-pedicled gastrocnemius myocuta- neous flap which is to be used to repair defects of the Achilles tendon and posterior skin of the ankle.Methods In anatomic study,out of 30 cadaver specimens,bi-pedicled V-Y gastrocnemius myoeutaneous flaps were harvested to measure the downward sliding lengths of the flap when the knee was at flexion of different degrees.In clinic,12 patients with the Achilles tendon and posterior ankle skin defects were repaired with the bi-pedicled gastrocnemius myocutaneous flaps.The areas of composite defects ranged from 10 cm?6 cm to 6 cm?4 cm.They were followed up for four months to 12 years.Results The maximal sliding length of the flap reached (9.2?0.9)cm when the knee was at flexion of 90?.All the clinical flaps survived and ambulation of the patients recovered.The dorsiflexion and plantarflexion of the ankles reached 11.0??1.4?and 35.0??4.6?respectively.Conclusion This flap is suitable for one-stage repair of composite Achilles tendon defects.
4.Narrow-band ultraviolet-B(311 nm)regulates dendrite formation in cultured B16 melanoma cells
Fuguo ZUO ; Leihong XIANG ; Yong ZHANG ; Yue HU ; Luchuan ZHU ; Zhizhong ZHENG
Chinese Journal of Dermatology 2009;42(6):417-420
Objective To investigate the effect ofnarrow-band ultraviolet-B(NB-UVB)(311 nm)on dendrite formation in B16 melanoma cells.Methods B16 melanoma cells were irradiated with various doses of NB-UVB(0,25,50,100,200,300 mJ/cm2).Atier additional culture of varying durations,irradiated cells were harvested and subjected to the observation of morphological changes and cell cytoskeleton F-actin microfilaments by phase contrast microscopy and laser scanning confocal microscopy(LSCM).respectively,and to the detection of cell proliferation bv MTT colorimetric assay.Pull down assay was performed to detect the activity of GTP-RhoAA and GTP-Rac1 in B16 cells before and after UVB irradiation.Results Twenty-four hours after irradiation with UVB of 100 mJ/cm2.an increase was observed in the cell body of B16 cells which appeared in sphericity,as well as in the number of dendrites(P<0.01)which showed a branch-like appearance.compared with non-irradiated cells which had 2-3 dendrites and obscure branches.LSCM revealed that F-actin microfilaments in B16 cells were well organized with clear textures before irradiation;after irradiation wim NB-UVB of 100 mJ/cm2.stress fibers were disassembled and disrupted and the texture became unclear,which was observed as early as 30 minutes and became more and more evident,and at 6 hours the stress fibers displayed a clumping appearance with obscure textures.Following the irradiation with NB-UVB of 100 mJ/cm2,the expression level of GTP-Rac 1 protein increased at l 5 minutes,and.at 30minutes,reached 2 times of that observed in nonirradiated cells,then decreased a liale,but still remained elevated at 60 minutes and 120 minutes,compared to unirradiated cells;meanwhile.the level of GTP-RhoA dropped a little at 30 minutes,then gradually increased and,at 120 minutes.reached 1.6 times of that observed in unirradiated cells.Conclusion Narrow-band UVB(311 nm)can promote dendrite formation.likely via regulating the expression of GTP-Racl and GTP-RhoA in B16 melanoma cells.
5.Impact of directly compressed auxiliary materials on powder property of fermented cordyceps powder.
Li-Hua CHEN ; Guo-Chao YUE ; Yong-Mei GUAN ; Ming YANG ; Wei-Feng ZHU
China Journal of Chinese Materia Medica 2014;39(1):65-70
To investigate such physical indexes as hygroscopicity, angle of repose, bulk density, fillibility of compression of mixed powder of directly compressed auxiliary materials and fermented cordyceps powder by using micromeritic study methods. The results showed that spray-dried lactose Flowlac100 and microcrystalline cellulose Avicel PH102 had better effect in liquidity and compressibility on fermented cordyceps powder than pregelatinized starch. The study on the impact of directly compressed auxiliary materials on the powder property of fermented cordyceps powder had guiding significant to the research of fermented cordyceps powder tablets, and could provide basis for the development of fermented cordyceps powder tablets.
Cellulose
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chemistry
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Cordyceps
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chemistry
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Drug Compounding
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methods
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Fermentation
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Lactose
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chemistry
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Powders
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chemistry
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Tablets
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chemistry
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Technology, Pharmaceutical
;
methods
6.Distribution and Resistance of Nosocomial Infection Pathogen from Shandong Provincial Nosocomial Infection Surveillance System 2003-2005
Yong REN ; Yue FAN ; Cuihua SHEN ; Weiguang LI ; Ping LI ; Qifeng ZHU
Chinese Journal of Nosocomiology 2006;0(05):-
OBJECTIVE To investigate the distribution and bacterial resistance of nosocomial infection.METHODS The data of 45 hospitals from Shandong Provincial Nosocomial Surveillance System from Jan 2003 to Dec 2005 were analyzed.RESULTS Of total 5 626 isolates strains from the nosocomial infection cases,G-bacilli,G+ cocci and fungi accounted for 58.27%,25.84% and 15.89%,respectively.The ampicillin-resistant rate of commonly encountered G-bacilli was above 89%.There were 72.98% of E.coli resistant to ciprofloxacin.The rates of resistance of S.aureus and coagulase negative Staphylococcus to penicillin,ampicillin and erythromycin were all above 80%;the lincomycin-resistant rate of S.aureus increased gradually to 86.64%.CONCLUSIONS Drug resistance of the nosocomial infective bacteria is a serous problem.Surveillance of bacterial resistance should be strengthened.
7.Operation and tumor metastasis
Fangming XU ; Yong ZHANG ; Jianhua XU ; Jue SUN ; Qiumei ZHU ; Yue LI
Journal of International Oncology 2017;44(5):376-379
Prior to the formation of new metastases,a large number of cancer cells released from the primary tumor enter the dormancy period.Once the dorruancy is broken,tumor cells will recover the capability of proliferation.In recent years,various hypotheses and mechanisms of tumor metastasis have been studied.Primary tumor resection is considered to be an important factor to break tumor dormancy state.It is recognized as an important reason to promote tumor metastasis.The improvement of surgical technique and further study on the mechanism of dormancy may provide new ideas for the treatment of metastatic tumor.
8.Effect of Yi Jin Jing (Sinew-transforming Qigong Exercises) on skeletal muscle strength in the elderly
feng Gao ZHU ; fang Zhi SHEN ; he Qing SHEN ; qin Yue JIN ; yong Zhi LOU
Journal of Acupuncture and Tuina Science 2017;15(6):434-439
Objective: To observe the effect of Yi Jin Jing (Sinew-transforming Qigong Exercises) on the muscle strength in senile sarcopenia. Methods: Sixty-five old people with sarcopenia were randomized into Yi Jin Jing group and a blank control group. Thirty-three patients in Yi Jin Jing group practiced Yi Jin Jing (Sinew-transforming Qigong Exercises), while 32 patients in the blank control group didn't receive any interventions. The muscle strength was measured before and after 12-week training. Results: During the study, each group had 1 dropout. The muscle strength was improved after 12-week training in Yi Jin Jing group, and the difference was statistically significant (P<0.05); there was no significant difference in the blank control group (P>0.05). After the intervention, there was a significant difference between Yi Jin Jing group and the blank control group in comparing the muscle strength (P<0.05). Conclusion: Constant Yi Jin Jing (Sinew-transforming Qigong Exercises) training can notably improve skeletal muscle strength in senile sarcopenia.
9.Construction of the pharmacophore model of acetylcholinesterase inhibitor.
Yong ZHU ; Xin-Yue TONG ; Yue ZHAO ; Hui CHEN ; Feng-Chao JIANG
Acta Pharmaceutica Sinica 2008;43(3):267-276
Based on ninety three acetylcholinesterase inhibitors (AChEIs) which have the same mechanism of action but are different in structural characteristics, the pharmacophore model for acetylcholinesterase inhibitor was constructed by the CATALYST system. The optimal pharmacophore model with three hydrophobic units, a ring aromatic unit and a hydrogen-bond acceptor unit were confirmed (Weight = 3.29, RMS = 0.53, total cost-null cost = 62.75, Correl = 0.93, Config = 19.05). This pharmacophore model will act on the double active site of acetylcholinesterase and is able to predict the activity of known acetylcholinesterase inhibitors that are used for clinical treatment of Alzheimer's disease (AD), and can be further used to identify structurally diverse compounds that have higher activity treating with Alzheimer's disease (AD) by virtual screening.
Acetylcholinesterase
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chemistry
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metabolism
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Alzheimer Disease
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enzymology
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prevention & control
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Cholinesterase Inhibitors
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chemistry
;
classification
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therapeutic use
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Drug Design
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Humans
;
Models, Chemical
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Models, Molecular
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Molecular Structure
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Quantitative Structure-Activity Relationship
;
Structure-Activity Relationship
10.Effect of Tibetan medicine zuotai on the activity, protein and mRNA expression of CYP1A2 and NAT2.
Xiang-Yang LI ; Yong-Nian LIU ; Yong-Ping LI ; Jun-Bo ZHU ; Xing-Chen YAO ; Yong-Fang LI ; Mei YANG ; Ming YUAN ; Xue-Ru FAN ; Yue-Miao YIN
Acta Pharmaceutica Sinica 2014;49(2):267-272
To study the effect of Tibetan medicine Zuotai on the activity, protein and mRNA expression of CYP1A2 and NAT2, three different doses (1.2, 3.8 and 12 mg x kg(-1)) of Zuotai were administrated orally to rats once a day or once daily for twelve days, separately. Rats were administrated orally caffeine (CF) on the second day after Zuotai administration, and the urine concentration of CF metabolite 5-acetylamino-6-formylamino-3-methyl-uracil (AFMU), 1-methyluric acid (1U), 1-methylxanthine (1X), 1, 7-dimethylxanthine (17U) at 5 h after study drug administration was determined by RP-HPLC. The activity of CYP1A2 and NAT2 was evaluated by the ratio of metabolites (AFMU+1X+1U)/17U and the ratio of AFMU/(AFMU+1X+1U), respectively. The protein and mRNA expression of CYP1A2 and NAT2 were determined by ELISA and RT-PCR method, respectively. After single administration of Zuotai 3.8 mg x kg(-1) and repeated administration of Zuotai 3.8 and 12 mg x kg(-1), the activity of CYP1A2 and NAT2 decreased significantly compared with control group and there was no significant difference between other dose group and control group. The protein expression of CYP1A2 was significant lower than that in control group after repeated administration of Zuotai 12 mg x kg(-1), and the mRNA expression of CYP1A2 decreased significantly compared with that of control group after single administration of Zuotai 3.8 mg x kg(-1) and repeated admistration of Zuotai 12 mg x kg(-1), separately. The protein expression of NAT2 decreased significantly compared with that of control group after single and repeated administration of Zuotai 3.8 mg x kg(-1), respectively, and the mRNA expression of CYP1A2 decreased significantly compared with control group after single administration of Zuotai 3.8 mg x kg(-1). This study found that Tibetan medicine Zuotai had significant effect on the activity, protein and mRNA expression of CYP1A2 and NAT2.
Administration, Oral
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Animals
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Arylamine N-Acetyltransferase
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genetics
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metabolism
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Caffeine
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metabolism
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urine
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Cytochrome P-450 CYP1A2
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genetics
;
metabolism
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Dose-Response Relationship, Drug
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Drugs, Chinese Herbal
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administration & dosage
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pharmacology
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Female
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Male
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Medicine, Tibetan Traditional
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RNA, Messenger
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metabolism
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Rats
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Rats, Sprague-Dawley
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Theophylline
;
urine
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Uracil
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analogs & derivatives
;
urine
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Uric Acid
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analogs & derivatives
;
urine
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Xanthines
;
urine