As an important member of the adisintegrin and metalloproteinase (ADAM) superfamily,ADAM17 can mediate a variety of membrane molecular hydrolysis off,such as adhesion molecules,cytokines,growth factors,etc,and play an important role in regulating tumor cell adhesion,apoptosis,metastasis and proliferation through the EGFR-PI3K-Akt pathway,Notch signaling pathway and other signaling pathways.The research of ADAM17 targeted drugs provides a new direction for cancer therapy.

OBJECTIVE: To compare the differences of macrophages phagocytic activities between Dioscorea opposita Thunb. cv. Tiegun(abbreviated as TG) and Dioscorea opposita Thunb. but not Tiegun(abbreviated as NTG). METHODS: CCK-8 assay was used to test the cytotoxicity. On the basis of non-toxic dose, the high content screening(HCS) cell imaging analysis was applied to test the phagocytic ability of RAW264.7 cells engulfing GFP-E. coli in vitro, and the phagocytic rates between different kinds of samples at various concentrations were calculated. Furthermore, the biological potency was measured according to the qualitative response parallel method to better evaluate the difference of TG and NTG, by translating phagocytic rates into biological potency. RESULTS: At the range of 0.695 - 5.56 mg(crude drug) •mL-1, all 11 batches samples have no toxicity. The results of HCS displayed that every sample could promote cell phagocytic activity in varying degrees at a certain concentration. RAW264.7 cells could engulf the GFP-E. coli, and the images of HCS reflected the situation of phagocytosis clearly. In addition, the results of biopotency showed that the biopotency value of different samples was between 39.56 to 100, and the average biopotency value of TG was significantly higher than NTG (P < 0.05). CONCLUSION: In vitro experiments showed that all the samples could promote the phagocytic activity of RAW264.7 cells at different degrees. And the average biopotency value of TG was significantly higher than NTG, which is consistent with the saying that "TG has a better quality".

METHODS: Female Kunming mice were randomly divided into five groups, ie, blank control group, low-dose group, middle-dose group, high-dose group, and the positive control group. The three treatment groups were given various doses of Rhodiola granules, ie, 0. 1, 1, 3 g��kg-1 respectively, the positive control group were given Nuodikang capsules at 280 mg��kg-1, and the blank control group was given deionized water for 35 d. The levels of SOD, MDA, GSH-PX in serum, liver, and brain were determined. For the experiment in vitro, with vitamin C as the control drug, the absorbance of Rhodiola granule solution at concentrations of 0.01, 0.1, 1, 10 mg��mL-1 was measured, and the activity of scavenging superoxide anion free radicals and hydroxyl free radicals was calculated.

AIM:To analyze the expression profile of long non-coding RNA (lncRNA) in the liver tissues of drug-induced liver injury ( DILI) and immune liver injury ( ILI) .METHODS:The technique of lncRNA microarray was used to inspect the lncRNA expression profile in the mouse liver tissues that the liver injury was induced by acetaminophen or concanavalin A .The raw data of lncRNA were pretreated for normalization .RESULTS:Compared with normal hepatic tissue, the lncRNA which had more than 1.5-fold variation and significant difference (P<0.05) by statistical analysis were regarded as lncRNA with differential expression .A total of 68 lncRNA with differential expression were found in the hepatic tissues of DILI, with 21 increased more than 1.5 folds and 47 reduced more than 1.5 folds.A total of 60 lncRNA with differential expression in the liver tissues of ILI were observed , with 17 increased more than 1.5 folds and 43 reduced more than 1.5 folds.In all lncRNA, 8 was simultaneously up-regulated in 2 liver injury models , accounting for 38%and 47%respectively, while 28 was simultaneously down-regulated in 2 liver injury models, accounting for 59%and 65%re-spectively .CONCLUSION:lncRNA expression profiles of DILI and ILI change significantly in comparison with normal hepatic tissue , and there are also differences between 2 hepatic damage models .The simultaneous changes of lncRNA may participate in the same or similar pathophysiological process , while the differences may be involved in relatively particular mechanisms .

Background:Tripterygium glycosides(TG)is effective for treatment of ulcerative colitis(UC)in clinical practice, however,the underlying mechanism has not been clarified yet. Aims:To investigate the therapeutic effect of TG on dextran sulfate sodium(DSS)-induced experimental colitis in mice and its possible mechanisms. Methods:Sixty healthy male BALB/ c mice were randomly divided into six groups:model control group,low,medium and high-dose TG group,blank control group and normal control group. Mice in the first four groups drank 5% DSS freely for 7 days to induce experimental colitis;simultaneously,distilled water,9. 01,27. 03 or 81. 09 mg/(kg·d)TG were given intragastrically for 21 days in these four groups,respectively. Histopathological changes of colonic mucosal tissues were observed;expressions of TLR4 mRNA and protein were determined by RT-PCR and Western blotting;expression of NF-κB p65 was detected by immunohistochemistry;concentrations of IL-1α,TNF-α and IL-13 were measured by ELISA. Results:Tissue damage and inflammation in varying degrees were observed in colonic mucosal tissues in TG groups with different dosage,but all were less severe than those in model control group. Expressions of TLR4 mRNA,TLR4 protein,and NF-κB p65 in colonic mucosal tissues,as well as concentrations of IL-1α and TNF-α in supernatant of colonic homogenate were significantly lower in TG groups than those in model control group(P < 0. 01). These parameters in medium and high-dose TG groups were significantly lower than those in low-dose TG group(P < 0. 05),but higher than those in blank control group and normal control group(P < 0. 05). Except for TNF-α,no significant differences were seen between medium and high-dose TG groups(P > 0. 05). Conclusions:TG exerts a protective effect on DSS-induced experimental colitis in mice. The underlying mechanism of its anti-inflammatory effect might be related with the inhibition of TLR4 / NF-κB signaling pathway activation and subsequently suppressing downstream proinflammatory cytokines expression and secretion.

Chemical constituents of Swertia patens. The whole plant of air-dried Swertia patens was extracted with 90% EtOH. The water extract was suspended in H₂O and extracted with petroleum ether, EtOAc and n-BuOH, successively. The compounds were isola- ted and purified by column chromatography from the EtOAc fraction, and identified based on spectral analyses (MS, ¹H-NMR, ¹³C- NMR). Eighteen compounds were isolated and elucidated as 3, 4-dihydro-1H,6H,8H-naptho [1,2-c:4,5-c', d'dipyrano-1, 8-dione (1), angelone (2), gentiogenal (3), erythricin (4), erythrocentaurin (5), gentianine (6), swertiakoside B (7), swertiamarin (8), 2'-O-actylswertiamarin (9), amarogentin (10), 1, 3, 5-trihydroxyxanthone (11), 1, 3-dihydroxy-5-methoxyxanthone (12), 1-hydroxy- 2, 3, 5-trimethoxyxanthone (13), gentiocrucine (14), 3-hydroxyphenylketone (15), n-hexacosyl ester 4-hydroxy-trans-cinnamate (16), n-hexacosyl ester 4-hydroxy-cis-cinnamate (17), and cholest-4-en-3-one (18). Compounds 1-7, 9-18 were obtained from S. patens for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Swertia ; chemistry

Child ; Female ; Gastric Mucosa ; pathology ; Gastritis, Hypertrophic ; diagnosis ; Humans ; Hypertrophy ; diagnosis

This present work is to study the chemical constituents of Swertia angustifolia. The whole plants of air-dried Swertia angustifolia was extracted with 90% EtOH. The water extract was suspended in H2O and extracted with petroleum ether, EtOAc and nBuOH, successively. The compounds were isolated and purified by column chromatography from the EtOAc fraction, and identified based on spectral analyses (MS, 1H-NMR, 13C-NMR). Fourteen compounds were isolated and characterized as 1, 8-dihydroxy-3, 7-dimethoxyxanthone (1), 1, 8-dihydroxy-3, 5, 7-trimethoxyxanthone (2), 7-hydroxy-3, 8-dimethoxyxanthone-1-O-β-D-glucopyranoside (3), 8-0-[β-D-xylopyranosyl-(1-6) -β-D-glucopyranosyl] -1, 7-dihydroxy-3-methoxyxanthone (4), (+) -syringaresinol (5), ferulic acid (6), trans-coniferyl aldehyde (7), sinapaldehyde (8), trans-coniferyl alcohol (9), 3, 4-dihydroxybenzoic acid (10), 2-hydroxybenzoic acid (11), isophthalic acid (12), 2-furoic acid (13), and 2-methyl-4(3H)-quinazolinone(14). Compounds 2-14 were obtained from this plant for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure ; Swertia ; chemistry

This study is to investigate the chemical constituents of Swertia kouitchensis. The whole plants of air-dried Swertia kouitchensis was extracted with 90% EtOH. The water extract was suspended in H2O and extracted with petroleum ether, EtOAc and n-BuOH, successively. The compounds were isolated and purified by column chromatography from the EtOAc fraction, and their structures were identified based on spectral analyses (MS, 1H-NMR, 13C-NMR). Twenty-eight compounds were obtained, and characterized as erythrocentaurin (1), erythrocentaurin dimethylacetal (2), swertiamarin (3), vogeloside (4), 2'-O- actylswertiamarin (5), swertianoside D (6), gentiocrucines A-B (7-8), gentiocrucine (9), 1-hydroxy-3, 7, 8-trimethoxyxanthone (10), 1-hydroxy-3, 5, 6-trimethoxyxanthone (11), 3-epitaraxerol (12), erythrodiol 3-O-palmitate (13), (+) -syringaresinol (14), caffeic acid (15), trans-coniferyl aldehyde (16), trans-coniferyl alcohol (17), 3, 4-dihydroxybenzoic acid (18), 4-hydroxy-3-methoxybenzoic acid (19), 3, 4-dihydroxybenzoic aldehyde (20), 2, 3-dihydroxybenzoic acid (21), 4-hydroxybenzoic acid (22), 3-acetoxybenzoic acid (23), 3-hydroxybenzoic acid (24), 3-hydroxybenzoic alcohol (25), nicotinic acid (26), 2-furoic acid (27), and uracil (28). Compounds 1-4, 6-28 were obtained from S. kouitchensis for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Molecular Structure ; Swertia ; chemistry

Objective To construct eukaryotie vector of human neronal pentraxin 2 (NPTX2),and obtain the sstable transfected PANC1 cell lines.Metods The full-length cDNA of NPTX2 was diget EcoRl and Notl,and was cloned into plasmid pcDNA3,1,which were confirmed by sequencing,then the PcDNA3,1(+)and pcDNA3,1(+)-NPTX2 vectors were transfected into PANC1 cells by LipofectamineTM 2000,The stable transfected PANC1 cell lines were selected by the abiliy of resistanc to G418.The NPTX2 mRNA expression of PANC1 in the selected clones was detected by real-time quantitative PCR.Results The eukaryotic vector pcDAN3,1(+)-NPTX2 was constructed successfully,stable transfected PANC1 cell line was established and confirmed by real-time quantitative PCR.Conclusions The construction of eukaryotic vector targeting NPTX2 and the established sstable transfected PANC1 cell line provided a solid experimental foundation for further studies on the function of NPTX2 in pancreatic cancer cells.