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).

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.

Animals ; Diabetic Neuropathies ; drug therapy ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Humans ; Nerve Growth Factors ; drug effects ; Nerve Regeneration ; drug effects ; Peripheral Nervous System Diseases ; drug therapy ; Phytotherapy ; Schwann Cells ; drug effects

Health Knowledge, Attitudes, Practice ; Humans ; Occupational Diseases ; prevention & control ; Rural Population ; Sampling Studies ; Surveys and Questionnaires ; Transients and Migrants

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.

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.

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.

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.

Objective To investigate the inducing effect of acitrotin on the growth and apoptosis of human cutaneous squamous cell carcinoma cell line SCC13 and on caspases expression.Methods Human cutaneous squa-mous cell carcinoma cell line SCC13 was treated with five different concentrations of acitrefin [5×10-7,1×10-6,5×10-6,1×10-5,5×10-5mol/L].Cell proliferation was evaluated by MTT assay.Apoptosis was assessed by en-zyme-linked immunosorbent assay.The cell cycle was assessed by flow cytometry.The protein expressions of caspase-8 and caspase-9 were examined with Western blot.Results Acitretin inhibited the growth ( F = 83.64,96.34 and 123.17, respectively on the first, third and fifth day)and induced the apoptosis of SCC13 cells(F=74.45,107.37,and 64.28, respectively on the first, third and fifth day) in a dose- and time-dependent manner(P<0.05).Acitretin altered cell cycle distribution of SCC13 cells as compared with controls, the G1-phase population increased by 77.66% 72 hours after acitretin treatment, while the control increased only by 63.55%.An active fragment of caspase-8 occurred following 12 hours treatment of acitretin on SCC13 cells, whereas the caspase-9 active fragment occurred 24 hours after acitretin treatment, which increased time-dependently (P<0.01).Conclusion Acitretin plays an important role on the growth inhibition and apoptosis of cutaneous squamous cell carcinoma cells, which may be affected through both Fas receptor way and mitochondria way.

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.