1.A simulating method for dripping process of Ginkgo biloba leaf dripping pills based on computational fluid dynamics technology
Acta Pharmaceutica Sinica 2023;57(10):2909-2913
A simulating method for dripping process of
3.Influence of antiepileptic drugs at therapeutic level to immature brain
Hai-Xia ZHU ; Fang-Cheng CAI ; Xiao-Ping ZHANG ;
Chinese Journal of Neurology 2001;0(03):-
Objective To explore the different influence of antiepileptic drugs(AEDs)at therapeutic levels to the maturation of brain.Methods 180 healthy Sprague-Dawley(SD)rats were divided into infant and adult group.Each age group was administered with PB,CNP,VPA,TPM or normal saline respectively in persistent 5 weeks.The steady-state plasma concentrations of AEDs at the experimental dosage were coincided with the range of clinical therapeutic concentrations.After AEDs withdrawed,the effects of AEDs on cognitive function were assessed by Morris water maze and two-way shuttle box at different time points.Body and brain weight were got immediately when the rats were sacrificed.Histological changes of brain were observed by HE staining,Nissl staining and transmission electron microscopy.Results(1) For immature rats,1 day or 14 days after AEDs withdrawed,there were significant differences between groups exposed to PB or CNP and control group in escape response latency(ERL)in the two-way shuttle box.Even after one month ERLs of immature rats receiving CNP((6.05?2.04)s)or PB((5.81? 1.75)s)were still longer than that of untreated controls((4.75?2.43)s,P
4.Meningeal hemangiopericytoma: a clinicopathologic study of 17 cases.
Hai-Bo WU ; Hai-Yan WENG ; Min DING ; Ping GU ; Xiao-Qiu WANG ; Wen ZHONG
Chinese Journal of Pathology 2011;40(4):251-252
Adult
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Aged
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Antigens, CD34
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metabolism
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Chondrosarcoma, Mesenchymal
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metabolism
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pathology
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Diagnosis, Differential
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Female
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Follow-Up Studies
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Hemangiopericytoma
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metabolism
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pathology
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radiotherapy
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surgery
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Humans
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Male
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Meningeal Neoplasms
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metabolism
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pathology
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radiotherapy
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surgery
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Meningioma
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metabolism
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pathology
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Middle Aged
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Neoplasm Recurrence, Local
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Proto-Oncogene Proteins c-bcl-2
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metabolism
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Solitary Fibrous Tumors
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metabolism
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pathology
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Vimentin
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metabolism
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Young Adult
5.Recent progress of non-viral vector polyethylenimine in the application of gene delivery
Cui-ping JIANG ; Yuan WANG ; Hai-yan XIAO ; Hai-yue ZHAO ; Qiang LIU
Acta Pharmaceutica Sinica 2020;55(12):2869-2882
In recent years, non-viral gene vectors have attracted great attention for efficient gene delivery due to the advantages, including low toxicity, low immunogenicity and simple preparation. Polyethylenimine (PEI) is one of the typical non-viral gene carriers that have been widely utilized for gene delivery owing to its superior capabilities in gene compression and buffering capacity. This article discusses the processes of gene delivery and the barriers of PEI-based carrier during the gene delivery, such as low biocompatibility, cytotoxicity, lack of specific targeting and insufficient gene release, etc
6.Immune response after injecting polysaccharide nucleic acid of Bacillus Calmette-Guerin under mucous membrane of bladder in rabbits
Shi-Ping SUN ; Yu-Feng ZHANG ; Xiao-Long YUE ; Hai-Ping WANG ;
Chinese Journal of Cancer Biotherapy 2006;0(05):-
Objective:To investigate the immune response after injecting polysaccharide nucleic acid of Bacillus Calmette-Guerin(BCG-PSN)under the mucous membrane of bladder in rabbits and to search for the most suitable dose of BCG-PSN.Methods:The rabbits were randomly divided into 5 groups:high dose(0.35 mg/ml)BCG-PSN group,mid- dle dose(0.175 mg/ml)BCG-PSN group,low dose(0.0875 mg/ml)BCG-PSN group,BCG(0.35 mg/ml)control group and BCG-PSN(0.35 mg/ml)intra-bladder perfusion control group.T lymphocyte subsets(CD4~+,CD8~+)in the peripheral blood were determined by flow cytometry before and 1 week,2 weeks,1 month and 3 months after the treatment; the levels of IL-2,TNF-?,and IFN-?of peripheral blood were determined by enzyme-linked immunosorbent assay;H-E and Masson staining was used for the pathological examination of the bladder.Results:(1)BCG-PSN injection increased the number of CD4~+ and CD8~+ T lymphocytes in a time- and dose-dependent manner,with the peak numbers appeared 2 weeks after BCG-PSN injection;the numbers restored to the normal levels 3 months after BCG-PSN injection.BCG control group had a similar changing pattern to the BCG-PSN injection group.The number of CD4~+ T cells BCG-PSN perfusion group was significantly lower than that in the high-dose BCG-PSN injection group(P
7.Study on dosage-toxicity/efficacy relationship of prepared rhubarb on basis of symptom-based prescription theory.
Yan-Hui WANG ; Hai-Ping ZHAO ; Jia-Bo WANG ; Yan-Ling ZHAO ; Xiao-He XIAO
China Journal of Chinese Materia Medica 2014;39(15):2918-2923
OBJECTIVETo investigate the dosage-efficacy/toxicity relationship of prepared rhubarb, in order to explore the bidirectional effects in hepatoprotection and hepatotoxicity of prepared rhubarb and the objective authenticity for attenuating toxicity by processing.
METHODNormal and pathological animals were adopted simultaneous to investigate the effect of total extracts from prepared rhubarb within a high dose range (2.0, 5.4, 14.7, 40.0 g x kg(-1) x d(-1)) on normal state, biochemical index and histopathology of experimental animals. The factor analytic approach was used to analyze the dosage-efficacy/toxicity relationship of prepared rhubarb.
RESULTThe factor analytic approach was used to extract two common factors from the nine biochemical indexes. The firs common factor was mainly dominated by HA, LN and TGF-β1, and could be explained as fibrotic factors. The second common factor was mainly dominated by ALT, AST and ALP, and could be explained as cellular factor. The results of the factor analysis suggested that prepared rhubarb showed significant bidirectional effects in hepatoprotection and hepatotoxicity, which could protect liver in CC14 injured chronic hepatic injury, but had a certain hepatotoxic effect to normal animals. The pathological examination showed consistent results with the factor analysis. Under comparable dosages, prepared rhubarb showed a stronger liver protecting effect than crude rhubarb, with a lower toxicity.
CONCLUSIONAlthough prepared rhubarb has a certain hepatotoxic effect to normal animals, it has also a significant therapeutic effect to animals with liver injury. The results proved the symptom-based prescription theory and the scientificity of the symptom-based medication. The symptom-based prescription theory is important to correctly realize the dosage-efficacy/toxicity relationship of traditional Chinese medicines and guide the symptom-based medication.
Animals ; Dose-Response Relationship, Drug ; Drug Prescriptions ; Drugs, Chinese Herbal ; pharmacology ; toxicity ; Female ; Fibrosis ; Liver ; drug effects ; metabolism ; pathology ; Male ; Rats ; Rats, Sprague-Dawley ; Rheum ; chemistry ; Toxicity Tests
8.The Progress of Biological Research of Medicinal Fungus Shiraia bambusicola
Xiao-Ming JIA ; Xiao-Hong XU ; Bai-Chuan ZHUANG ; Hai-Ping LIN ;
Microbiology 1992;0(03):-
The research status is reviewed on taxonomic position, ecology, biological active matter and artificial cultivation of Shiraia bambusicola. Following problems are presented: whether there are new species and host specificity of Shiraia bambusicola. Since the artificial cultivation of stroma of Shiraia bambusicola has not been success, Shiraia bambusicola is in situation of emerge of itself and perish of itself so that it is not beneficial to resource protection and continual utilization of this medicinal fungus. It is pointed out that molecular biology of Shiraia bambusicola should be further researched and technology of artificial cultivation of Shiraia bambusicola should be explored in order to exploit and usage of Shiraia bambusicola.
9.Design, synthesis and biological evaluation of novel para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones as human PARP-1 inhibitors.
Hai-Ping YAO ; Zhi-Xiang ZHU ; Ming JI ; Xiao-Guang CHEN ; Bai-Ling XU
Acta Pharmaceutica Sinica 2014;49(4):497-503
Poly(ADP-ribose) polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. It can polymerize ADP-ribose units on its substrate proteins which are involved in the regulation of DNA repair. In this work, a novel series of para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones was designed and synthesized, and the inhibitory activities against PARP-1 of compounds 7a-7e, 8a-8f, 9a-9c and 10a-10c were evaluated. Of all the tested compounds, nine compounds displayed inhibitory activities with IC50 values ranging from 4.6 to 39.2 micromol x L(-1). In order to predict the binding modes of the potent molecules, molecular docking was performed using CDOCKER algorithm, and that will facilitate to further develop more potent PARP-1 inhibitors with a quinazolinedione scaffold.
Antineoplastic Agents
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chemical synthesis
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chemistry
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pharmacology
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Drug Design
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Enzyme Inhibitors
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chemical synthesis
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chemistry
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pharmacology
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Molecular Docking Simulation
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Molecular Structure
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Poly (ADP-Ribose) Polymerase-1
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Poly(ADP-ribose) Polymerases
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Quinazolinones
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chemical synthesis
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chemistry
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pharmacology
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Structure-Activity Relationship
10.Preparation and characterization of cucurbitacin B sodium deoxycholate/phospholipid-mixed oral fast dissolving film and antitumor activity study.
Chao YU ; Yun-Zhi XIAO ; Ping-Hua XUN ; Ling DAI ; Jin HAN ; Hai-Long YUAN
China Journal of Chinese Materia Medica 2014;39(10):1799-1804
A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.
Animals
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Antineoplastic Agents
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administration & dosage
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chemistry
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Cell Line, Tumor
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Deoxycholic Acid
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chemistry
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Drug Carriers
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chemistry
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Humans
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Male
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Mice
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Neoplasms
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drug therapy
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Phospholipids
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chemistry
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Solubility
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Triterpenes
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administration & dosage
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chemistry