4.A Progress on the Key Technologies for Discovery of Bioactive Compounds from Traditional Chinese Medicines
Huipeng SONG ; Hua YANG ; Wen GAO ; Jun CHEN ; Ping LI
World Science and Technology-Modernization of Traditional Chinese Medicine 2016;18(7):1093-1098
Traditional Chinese medicines (TCM) is one of the most important sources of new drugs.The rapid development of modern science and technology has brought new opportunities for TCM.Admittedly,new academic theory is getting into a golden period of innovation.Key technologies that enbody TCM features and adapt to modern drug-screening requirements are urgently needed.After five years' endeavor,the authors' group has made great progress in the new theories and methodologies for the discovery of bioactive compounds from TCM.In this review,a total of five key technologies:library-bioactivity-structure integration,biological and chemical fishing technology,ligand-and receptor-based virtual screening,profile-bioactivity relationship and the technology for discovering bioactive equivalent combinatorial components (BECCs),were introduced.In the text,several valuable demonstrations over the TCM-based drug discovery were provided,for uncovering the scientific basis of TCM and accelerating the process of TCM modernization.
5.Relationship between TCM syndrome type and expression of human leucocyte antigen DR gene in patients with systemic lupus erythematosus.
Cheng-Ping WEN ; Zhi-Jun XIE ; Ping SONG
Chinese Journal of Integrated Traditional and Western Medicine 2008;28(6):499-501
OBJECTIVETo explore the expression of human leucocyte antigen DR (HLA-DR) gene in peripheral blood mononuclear cells (PBMCs) of systemic lupus erythematosus (SLE) patients of various TCM syndrome types in order to seek an objective index for syndrome differentiation of SLE.
METHODSSLE patients were sorted into various syndrome types by TCM syndrome differentiation, i. e. Pi-Shen yang-deficiency type (A), yin-deficiency with internal heat type (B), qi-yin deficiency type (C) and Gan-Shen yin-deficiency type (D). Their peripheral blood sample was collected for detecting HLA-DR positive lymphocytes and monocytes in PBMC using flow cytometry.
RESULTSComparisons among patients of various syndrome type showed that the proportion of HLA-DR positive monocytes and lymphocytes in PBMC in patients of type A was the lowest (P < 0.01); proportion of HLA-DR positive lymphocytes in patients of type B was significantly higher than in those of type C and D (P < 0.01), and that in type D was higher than in type C (P < 0.05); total proportion of HLA-DR positive cells in patients of type A was the lowest, that in type B was higher than that in type C and D (P < 0.01, P < 0.05), while no significant difference was found between the latter two types (P > 0.05).
CONCLUSIONHLA-DR could be taken as an objective index for reference in syndrome differentiation of SLE.
Adolescent ; Adult ; Animals ; Female ; Gene Expression Regulation ; HLA-DR Antigens ; metabolism ; Humans ; Leukocytes, Mononuclear ; metabolism ; Lupus Erythematosus, Systemic ; classification ; metabolism ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Syndrome ; Young Adult
6.Epidemiology and characteristics of acute poisoning treated at an emergency center
Feng CHEN ; Jun-Ping WEN ; Xiao-Ping WANG ; Qing-Ming LIN ; Cai-Jing LIN
World Journal of Emergency Medicine 2010;1(2):154-156
BACKGROUND:Acute poisoning is frequently encountered at emergency department. This study was to investigate the epidemiology and characteristics of patients with acute poisoning who were treated at the Emergency Center, Fujian Provincial Hospital, China. METHODS:We retrospectively analyzed the gender, age, causes of poisoning, types of poisons, poisoning route, emergency diagnoses, outcomes, and prognoses of these patients. RESULTS:Altogether 2867 patients with acute poisoning were treated from January 2004 to December 2009. The ratio of male to female was 1:1.04, and their average age was 33.8 years. Of the 2867 patients, 76.39% were between 18 and 40 years old. The incidence of acute poisoning was as high as 11.33% in January each year. The incidence of poisoning was in a descending order:alcohol poisoning (54.55%), medication poisoning (25.95%), pesticide poisoning (5.65%), and drug poisoning (4.88%). Most (56.44%) of the patients with drug poisoning were under 25 years and their mean age was significantly lower than that of patients with medication poisoning or alcohol poisoning (P < 0.01). Approximately 69.54% of the patients were followed up after emergency treatment, 30.39% were hospitalized, and four patients died. CONCLUSIONS:Acute poisoning is largely alcohol poisoning and medication poisoning in a city. The emergency green channel "pre-hospital emergency care-emergency department-hospital treatment"can significantly improve the survival rate of patients with acute poisoning.
7.Effect of Daidzein intravitreal injection on optic nerve injury in rats
Zhong-Jun, TANG ; Zhen-Ping, HUANG ; Wen-Jing, YANG ; Yong-Xiang, ZOU ; Ji-Ping, CAI
International Eye Science 2014;(8):1378-1381
AIM:To discuss Daidzein intravitreal injection whether has protective and recovery effects on acute nerve damages.
METHODS:After the crush models of acute optic nerve were set up, 72 males SD rats were divided into 4 groups randomly as common group without surgery, FBS negative control group, Daidzein treatment group ( 10μmol/L, 100μmol/L, 1000μmol/L ) and positive control group using rats nerve growth factor ( mNGF, 100ng/mL ). Three days after interference, all experimental animals were executed. HE staining was used to evaluate morphologic change of the retina, immunohisochemical staining and western-blot tests for identifying and quantifying the distinct expression of Caspase-3 and GAP-43 among the groups.
RESULTS: Compared with the normal group and negative control group, retinal morphology of different concentrations of each Daidzein treatment group and positive control group was more complete, the expression of Caspase-3 protein was relatively lower, the expression of GAP-43 protein was relatively higher, the differences have statistically significance (P<0. 05).CONCLUSION: Daizein injection in the vitreous cavity has the capacity of protection and restoration in rat's acute nerve damages.
8.Optimization and characterization of curcumin-piperine dual drug loaded self-microemulsifying drug delivery system by simplex lattice design.
Qiu-Ping LI ; Jun-Dong DAI ; Wen-Wen ZHAI ; Qiao-Li JIANG
China Journal of Chinese Materia Medica 2014;39(20):3936-3944
The objective of the study was to prepare and evaluate the quality of curcumin-piperinedual drug loaded self-microemulsifying drug delivery system(Cur-PIP-SMEDDS). Simplex lattice design was constructed using optimal oil phase, surfactant and co-surfactant concentration as independent variables, and the curcumin and piperine were used as model drugs to optimize Cur-PIP-SMEDDS formulation. In the present study, the drug loadings of curcumin and piperine, mean particle size of Cur-PIP-SMEDDS were made as indicators, and the experiment design, model building and response surface analysis were established using Design Expert 8. 06 software to optimize and verify the composition of SMEDDS formulation. The quality of Cur-PIP-SMEDDS was evaluated by observing the appearance status, transmission electron microscope micrographs and determining particle diameter, electric potential, drug entrapment efficiency and drug loading of it. As a result, the optimal formulation of SMEDDS was CapryoL 90-Cremophor RH40-TranscutoL HP (10:60:30). The appearance of Cur-PIP-SMEDDS remained clarified and transparent, and the microemulsion droplets appeared spherical without aggregation with uniform particle size distribution. The mean size of microemulsion droplet formed from Cur-PIP-SMEDDS was 15.33 nm, the drug loading of SMEDDS for Cur and PIP were 40.90 mg · g(-1) and 0.97 mg · g(-1), respectively, the drug entrapment efficiency were 94.98% and 90.96%, respectively. The results show that Cur-PIP-SMEDDS can increase the solubility and stability of curcumin significantly, in the expectation of enhancing the bioavailability of it. Taken together, these findings can provide the reference to a preferable choice of the Cur formulation and contribute to therapeutic application in clinical research.
Alkaloids
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chemistry
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Benzodioxoles
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chemistry
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Chemistry, Pharmaceutical
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methods
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Curcumin
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chemistry
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Drug Carriers
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chemistry
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Drug Combinations
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Drug Delivery Systems
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Drugs, Chinese Herbal
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chemistry
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Emulsions
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chemistry
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Methylmethacrylates
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chemistry
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Particle Size
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Piperidines
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chemistry
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Polystyrenes
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chemistry
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Polyunsaturated Alkamides
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chemistry
9.Screening of Antitumor and Antimicrobial Activities of the Endophytic Fungi Isolated from Cephalotaxus hainanensis Li
Wen-Jun DAI ; Hao-Fu DAI ; Ping CHEN ; Jiao WU ; Wen-Li MEI ;
Microbiology 2008;0(08):-
Seventy-two endophytic fungi isolated from Cephalotaxus hainanensis Li were screened for antitumor and antimicrobial activities. The results showed that 9 strains presented cytotoxic activities to at least one of the tested tumor cells, five strains exhibited strong antimicrobial activity against Staphylococcus aureus, one strain had inhibitory effect on Phytophthora parasitica. It was evidently that the endophytic fungi of C. hainanensis are potential resources to find valuable bioactive components.
10.Effects of nandrolone phenylpropionate on ultrastructure of aorta in rats with or without movement training
ping-ping, WU ; wen-jun, YANG ; ping, ZHU ; meng-wei, SUN ; feng-lei, QIAN ; ai-yun, LU ; hong, CHEN
Journal of Shanghai Jiaotong University(Medical Science) 2006;0(07):-
Objective To observe the influence of nandrolone phenylpropionate(NP) on the ultrastructure of aorta in rats with or without movement training,and investigate the side effects of NP on the cardiovascular system. Methods Forty male SD rats were randomly divided into sedentary control group,sedentary+medicine group,exercise control group and exercise+medicine group.For the groups with medical treatment,NP of 10 mg/kg one time every three days was injected into the rats via gluteus for eight weeks.For the exercise groups,rats were trained to run on treadmill five days per week for eight weeks.The aortae were sampled and specimens were obtained for transmission electron microscopy. Results The ultrastructure of aorta was normal in sedentary control group.For sedentary+medicine group,mitochondrial swelling,vacuolated cytoplasm and lysis of endothelial cells were observed,disruption of intercellular conjunctions,widening of subendothelial spaces and furcation and breakage of internal elastic lamina were found,and smooth muscle cells changed into synthesis type.For exercise control group,no obvious morphologic change was observed,except that part of the internal elastic lamina disrupted.In exercise+medicine group,breakage and lysis of endothelial cells were observed,widening of subendothelial spaces and lysis of internal elastic lamina were found,and autophagosome and myelinoid body were seen in smooth muscle cells. Conclusion NP may lead to the impairment of endothelial cells and the change of smooth muscle cells into synthesis type.Exercise with NP administration may result in more severe impairment in vessel wall.