1.Clinicopathological and prognostic significance of NQO1 protein expression in patients with colorectal carcinoma
Yue MA ; Lijuan LIN ; Junjie PIAO ; Huixin LV ; Zhenhua LIN
Chinese Journal of Clinical and Experimental Pathology 2014;(4):366-370
Purpose To investigate the prognostic significance of NQO1 protein expression in colorectal carcinoma ( CRC) patients. Methods 192 cases of primary CRC, 28 of colonic dysplasia, and 44 of adjacent non-tumor tissues were selected for immunohisto-chemical staining of NQO1 protein. Correlation between NQO1 overexpression and clinicopathologic characteristics, and the survival rates were calculated by the statistical methods. Results The strongly positive rate of NQO1 protein in CRC was significantly higher than that in gastric dysplasia and adjacent non-tumor tissues (P<0. 01, respectively). NQO1 high-expression rate was positively cor-related with differentiation, serosal invasion, lymph node metastasis, and clinical stage (P <0. 05, respectively). Survival curve showed that the disease-free survival and 5-year survival rates of the patients with high NQO1 expression were obviously shorter than those of patients with low NQO1 expression (P<0. 001, respectively). Further analysis showed that, high expression of NQO1 predic-ted the lower disease-free survival and 5-year survival rates in late-stage patients (P<0. 01, respectively). Importantly, NQO1 was an independent risk factor for the prognosis of CRC using Cox proportional hazards regression model ( HR: 1. 398,95%CI: 1. 011 ~1. 934, P=0. 043). Conclusions Detection of NQO1 protein expression in CRC has an important clinical significance, and it is ex-pected to become a new biomarker for CRC.
2.Synthesis and HIV-1 inhibitory activity of natural products isolated from Gnetum parvifolium and their analogues.
Zhisong PIAO ; Yabing FENG ; Lin WANG ; Xingquan ZHANG ; Mao LIN
Acta Pharmaceutica Sinica 2010;45(12):1509-15
Resveratrol, isorhapontigenin and pinosylvin, isolated from Gnetum parvifolium, and their analogues have been synthesized and tested for their inhibitory activity of HIV-1. Natural product 12a and analogues (12d, 12e, 12g) display significant inhibitory activity of HIV-1 replication. Among them, compound 12d (trans-3, 4, 5, 4'-tetrahydroxystilbene) exhibits the most potent anti-HIV-1 activity with an IC50 value of 1.84 micromol x L(-1).
3.Studies on chemical constituents of marine sponge Aplysinopsis sp.
Xue LI ; Shaojiang SONG ; Shujuan PIAO ; Tao DONG ; Houwen LIN
Chinese Journal of Marine Drugs 1994;0(04):-
Five compounds were isolated from marine sponge Aplysinopsis sp.collected from the South China Sea.Their structures were elucidated by ~1H-NMR,~(13)C-NMR and MS as (E)-3'-deimino-3'-oxoaplysinopsin(Ⅰ),(Z)-3'-deimino-3'-oxoaplysinopsin(Ⅱ),3-(2- oxopropyl )- 3-hydroxyind-olin-2-one(Ⅲ),1H-indole-3-carboxaldehyde(Ⅳ),5?,6?-epoxystigmasta -7-en-3?-ol(Ⅴ).CompoundsⅢ,Ⅴwere isolated from Aplysinopsis sp.for the first time.
6.Research status of anti-tumor targted drugs
Xiuquan QUAN ; Huishun PIAO ; Lin KANG ; Xuezhe YIN ; Zhonggao GAO
Chinese Pharmacological Bulletin 2015;(5):610-614
Traditional treatments for malignant tumor are far from meeting the clinical demands.Recently,research on anti-tumor targeted drugs has made a significant breakthrough,which brings new hope for the treatment of malignant tumor.Anti-tumor targe-ted drugs can specifically target malignant tumor and directly in-hibit the growth of tumor cells,showing no toxicity to the normal tissues and organs.Herein we reviewed the research progress of small molecular targeted drugs and antibody targeting new drugs.
7.Study of ultrastructure and neuron quantitative determination in nigra-striatum of newborn rabbits with bilirubin encephalopathy
Xiaojie LI ; Wenhua PIAO ; Lin LI ; Zhimei JIANG
Chinese Journal of Rehabilitation Theory and Practice 2003;9(5):261-262
ObjectiveTo explore the noxious effect and the extent of damage in nigra-striatum neuron of bilirubin.Methods30 newborn rabbits were divided into 3 groups randomly:control group(group C,12 rabbits) which were injected normal salt intraperitoneally,model group 1(group N1,12 rabbits) which were injected bilirubin 100mg/kg intraperitoneally, model group 2(group N2,12 rabbits) which were injected bilirubin 200mg/kg intraperitoneally. All the rabbits in group C and 6 rabbits in group N1(group N1a) and group 2(group N2a) were killed 6 hours after injection.Other 6 rabbits in group N1(group N1b) and group 2(group N2b) were killed 16 hours after injection. The quantity of neuron in nigra-striatum were determined,and the changes of ultrastructure were observed by electron microscope.ResultsThe neuron in nigra-striatum in group N2b were decreased compared with group C and group N1a(P<0.05),as well as with group N1b and N2a. The ultrastructure of the neuron was changed.ConclusionsThe changes in utrastructure and the quantity of nigra-striatum neuron were associated with the concentration and time of exposure under bilirubin. It is consisted with the changes of ultrastructrue and quantity in nigra-striatum.
8.Evaluation of the protective function of NO precursor/donator on cerebral ischemia injury with DWI and PWI
Xiangyu PIAO ; Changkai SUN ; Yongzhong LIN ; Lin SHA ; Xu TONG ; Ruitan SUN ; Peng ZHOU
Journal of Chinese Physician 2008;10(4):433-436
Objective To establish a rat model of middle cerebral artery occlusion (MCAO)by blockage or obstruction of middle cerebral artery. NO precursor L-Arginine (L-ARG) and NO donator Nitroglycerine (NG)are administrated from intraearotid arteries. DWI and PWI are applied to evaluate blood circulation and brain damage of the effected region to elucidate the piotective function of L-ARG and NG in the early stage of brain ischemia. Methods The middle cerebral artery was occluded by insertion of a suture through the internal carotid artery of SD male rats to duplicate ischemia-reperfusion model. Reperfusion was established by suture withdrawal. After 2 hours of blockage, reperfusion and administrate L-ARG,NG by interventional therapy through the internal carotid artery simultaneously. Image indexes such as T1WI, T2WI, DWI and PWI are utilized to assess the changes in different time points. These indexes, Longa score and TTC stain were compared. Results There were obvious decrease in DWI high signal region and Trc pale region in drugs groups, compared with MCAO group(P<0.01).ADC and rADC values in DWI high signal region increased gradually from 2 hours after ischemia to 24 hours after reperfusion in each group. ADC and rADC values in DWI high signal region of the drugs groups increased obviously(P<0.01).Conclusion Interventional therapy with NO precursor/donator showed significant protective function in the early stage of brain ischemia.
9.Effects of Dihuangyinzi on behaviors and RAGE/p38 pathway in APP/PS1 mice
Zhongyuan PIAO ; Lifen YAO ; Lin SONG ; Yichan LU ; Zhuo JIANG ; Yang ZHENG ; Zhiyong DI ; Limei AO
Chinese Journal of Behavioral Medicine and Brain Science 2017;26(7):577-581
Objective To investigate the effects of Dihuangyinzi(DHYZ) on behaviors and RAGE/p38 pathway in APP/PS1 mice.MethodTwenty APP/PS1 dementia mice were randomly divided into model group(n=10) and Chinese medicine group(n=10).The blank group was C57 BL/6 J normal mouse(n=10).The mice in Chinese medicine group were intragastric administration with DHYZ (9.75 g·kg-1·d-1).The mice in model group and blank group were treated with distilled water.After 30 days,the abilities of learning and memory of mice were detected by Morris water maze.The expression of amyloid-beta1-42(Aβ1-42) in the hippocampus and cortex was detected by immunohistochemistry.Reactive oxygen species of brain tissue were detected by DCFH-DA Methods in the brain of APP/PS1 mice.Gene expression level of receptor for advanced glycation end products(RAGE) was measured by real-time polymerase chain reaction (RT-PCR) in the cortex and hippocampus of APP/PS1 mice.The expression of phospho-mitogen-activated protein kinases (p38) was analyzed with Western blot and immunofluorescence analysis in the cortex and hippocampus of APP/PS1 mice.Results Behavioral Results showed that DHYZ significantly increased the distance((23.088±7.083)cm) and residence time((1.961±1.230)s)of effective area in Morris water maze on the fifth day(P<0.05,P<0.01)and remarkably increased the number of effective area crossings((1.607±0.405) times) and plats((0.893±0.283) times) in Morris water maze on the fifth day(P<0.01,P<0.05).DHYZ also significantly reduced the intracelluar ROS level(122.611±7.630) in the brain(P<0.01),and DHYZ could depress the expression of RAGE(1.467±0.081,7.983±0.136) and phosphorylation of p38 (0.376±0.026,0.538±0.016)in the cortex and hippocampus of APP/PS1 mice(P<0.01,P<0.05).Conclusions The Results demonstrate that DHYZ can partly improve memory impairment of APP/PS1 mice by the inhibition of RAGE/p38 pathway.
10.Effects of Dihuang Yinzi on RAGE/ROS/Apoptosis Pathway in SH-SY5Y Cells Induced by Aβ1-42
Zhongyuan PIAO ; Yafen WEI ; Lin SONG ; Limei AO ; Yichan LU ; Zhuo JINAG ; Lifen YAO ; Yanli LIU
Journal of Guangzhou University of Traditional Chinese Medicine 2017;34(4):543-550
Objective To investigate the effects of Dihuang Yinzi (DY) on the receptor for advanced glycation end-products(RAGE)/reactive oxygen species(ROS)/apoptosis pathway in SH-SY5Y cells induced by amyloid-beta1-42 (Aβ1-42) oligomer. Methods Firstly, we adopted methyl thiazolyl tetrazolium(MTT) method to detect the cell vitality in fetal bovine serum (FBS) group, blank serum group, and low-, middle- and high- dose DY-containing serum groups, so as to confirm the optimal concentration and treatment time of DY-containing serum. Secondly, we applied MTT method to detect cell vitality and applied Annexin V/propidium iodide (PI) staining method to observe the apoptosis of SH-SY5Y cells treated with 0~20 μmol/L Aβ1-42 for 24 and 48 h, so as toconfirm the optimal concentration and treatment time of Aβ1-42 for establishing Alzheimer's disease (AD) model in vitro. Thirdly, MTT method was used for the detection of cell vitality, and Annexin V/PI staining method was used for detection of the apoptosis of SH-SY5Y cells in blank serum group, model group, western medicine control group and low-, middle-and high-dose DY-containing serum groups, and Dihydroethidium (DHE) method was used for the assay of ROS contents, so as to observe the effect of DY on the recovery of injured SH-SY5Y cells induced by Aβ1-42. Finally, we applied Western blot method to detect the expression level of RAGE in SH-SY5Y cells of blank group, model group and DY-containing serum group; after Aβ1-42-induced SH-SY5Y cells were transfected with RAGE gene, we adopted DHE staining method and Annexin V/PI staining method to detect ROS content and cell apoptotic rate in all of the above groups, so as to observe the effect of DY on SH-SY5Y cell apoptosis and RAGE expression. Results The cell vitalities were increased in low- and middle-dose DY-containing serum groups at 24 h (P < 0.05 or P < 0.01 compared with that in the blank serum group). The conditions for the establishment of AD model in vitro were as follows: the optimal concentration of Aβ1-42 was 5μmol/L, and the treatment time was 24 h. The cell vitalities were significantly enhanced, the cell apoptotic rate and ROS content were significantly lowered in Aβ1-42-induced SH-SY5Y cells of the medication groups(P <0.05 or P < 0.01 compared with those in the model group) , and the cell vitality was the highest and the cell apoptotic rate was the lowest in the middle-dose DY-containing serum group. The RAGE expression level was decreased in Aβ1-42-induced SH-SY5Y cells of the middle-dose DY-containing serum group(P < 0.05 compared with that in the model group) . ROS content and cell apoptotic rate were decreased in Aβ1-42-induced SH-SY5Y cells transfected with RAGE gene in the middle-dose DY-containing serum group (P<0.01). Conclusion DY may play an anti-oxidative role through inhibiting the production of ROS and cell apoptosis, thus to suppress RAGE protein and to achieve the preventive and therapeutic effect for AD.