Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0345904 (liver cancer)
 15,188 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Polyethylene glycol-polybenzyl-L-glutamate copolymer (PEG-PBLG) was synthesized and paclitaxel-loaded core-shell type nano-micelles with amphiphilic copolymer PEG-PBLG was prepared by the dialysis method. The drug loading content and entrapment efficiency were determined by HPLC. The average size and its distribution were determined by dynamic light scattering method. The paclitaxel release rate in vitro from micelles was measured by HPLC. The cell cytotoxicity in vitro was observed with MTT assay. The anti-tumor activity of paclitaxel-loaded micelles were evaluated in tumor-inhibiting test of nude mice using human liver cancer HepG-2. The results indicated that paclitaxel could be entrapped in PEG-PBLG copolymer micelles and its size was in the range of 80-265 nm which increased with an increase in molecular weight of PBLG in copolymer; in vitro the paclitaxel could be released sustainably from the micelles. In high concentration of paclitaxel (>20 microg x mL(-1)) the paclitaxel-loaded PEG-PBLG micelles displayed much less cell cytotoxicity than paclitaxel injections with Cremophor EL (P<0.05); the tumor inhibiting activity of paclitaxel-loaded PEG-PBLG micelles was similar to that of paclitaxel injections with Cremophor EL in the same paclitaxel concentration. It was concluded that the paclitaxel-loaded PEG-PBLG micelles had more uniform size and size distribution, excellent drug sustainable-release behavior, less cytotoxicity, good anti-tumor activity similar to paclitaxel injections with Cremophor EL. So paclitaxel-loaded PEG-PBLG micelles would be a novel paclitaxel preparation in clinic for the treatment of tumor.
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PMID:[Preparation and properties of self-assemble paclitaxel-loaded core-shell type nano-micelles]. 1866 5

A series of novel unsymmetrically N,N'-substituted ureas were synthesized from dehydroabietic acid and their structures were characterized by IR, 1H-NMR, 13C-NMR spectroscopy and single crystal X-ray diffraction. Three six-membered rings of urea 4c exhibited plane, half-chair and chair configurations, respectively. Their cytotoxicity activities against SMMC7721 liver cancer cells were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The results showed that the title compounds exhibited highly effective cytotoxicity activities against SMMC7721 cells. Their IC50 values are between 8.8 and 14.2 micromol/l. The change of N' substituted groups resulted little difference to the cytotoxicity activities of ureas, which indicated that the cytotoxicity of this kind of ureas depend strongly on the tricyclic hydrophenanthrene structure.
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PMID:Synthesis, structure analysis and cytotoxicity studies of novel unsymmetrically n,n'-substituted ureas from dehydroabietic Acid. 1898 8

The interactions of cobalt sulphate and nickel acetate with ofloxacin (ofo, I), a 4-quinoline derivative, were studied. The hydrothermal technique was adopted in this work. The isolated solid complexes were characterized by elemental analysis, infrared spectra, electronic spectra, fluorescence spectra and thermal analysis. The results support the formation of complexes of the formula Co(ofo)2 x 4H2O (II) and Ni(ofo)2 x 4H2O (III). The infrared spectra of the isolated solid complexes suggested that ofo acts as bidentate ligands through one of the oxygen atoms of the carboxylic group and the ring carbonyl oxygen atom. Thermogravimetric (TG) and its differential (DTG) were carried out for the complexes. The data obtained indicated that the thermal decomposition of the two complexes in inert atmosphere proceeded approximately with two main degradation steps. I showed a intense fluorescence in solid state at lamda(ex)/lamda(em) = 365 nm/461 nm, and two complexes displayed weakly similar emission maximum at 470 nm in the powder samples at ambient temperature, while the emission of II and III may be mainly originated from the intraligand excited states of I. I, II and III were assayed against two kinds of gram-positive and two kinds of gram-negative bacteria by in vitro doubling dilutions method. The results indicated that II and III have the similar minimal inhibitory concentration (MIC) as the I against S. Aureus, M. Lutens, E. Coli and P. Aeruginosa. The inhibitory effect of I, II and III on leukemia HL-60 cell line has been measured by using MTT (Methyl-Thiazol-Tetrozolium) method and that on liver cancer BEL-7402 cell line measured by SRB (Sulphurhodamin B) method. The results indicated that the complexes in the high concentration have inhibitory effect on HL-60 cell line.
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PMID:[Synthesis, spectral analysis, antibacterial and antitumor activities of Co(II) and Ni(II) ofloxacin complexes]. 1912 13

Phloretin (Ph), a natural product found in apples and pears with glucose transporter (GLUT) inhibitory activity, exerts antitumor effects. However, little is known about its effects on human liver cancer. The purpose of this study is to test the cytotoxic effects of Ph on HepG2 cells and to identify the underlying molecular pathways. Human hepatocellular carcinoma specimens and HepG2 show a high level of GLUT2 transporter activity in the cell membrane. Real-time PCR and MTT assays demonstrate that Ph-induced cytotoxicity correlates with the expression of GLUT2. Flow cytometry and DNA fragmentation studies show that 200 microM Ph induces apoptosis in HepG2, which was reversed by glucose pretreatment. GLUT2 siRNA knockdown induced HepG2 apoptosis, which was not reversed by glucose. Western blot analysis demonstrates that both intrinsic and extrinsic apoptotic pathways in addition to Akt and Bcl-2 family signaling pathways are involved in Ph-induced cell death in HepG2 cells. Furthermore, using flow cytometry analysis, a mitochondrial membrane potential assay and Western blot analysis, we show that cytochalasin B, a glucose transport inhibitor, enhances the Ph-induced apoptotic effect on HepG2 cells, which was reversed by pretreatment with glucose. Furthermore, we found significant antitumor effects in vivo by administering Ph at 10 mg/kg intraperitoneally to severe combined immune deficiency mice carrying a HepG2 xenograft. A microPET study in the HepG2 tumor-bearing mice showed a 10-fold decrease in (18)F-FDG uptake in Ph-treated tumors compared to controls. Taken together, these results suggest that Ph-induced apoptosis in HepG2 cells involves inhibition of GLUT2 glucose transport mechanisms.
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PMID:In vitro and in vivo study of phloretin-induced apoptosis in human liver cancer cells involving inhibition of type II glucose transporter. 1912 83

A new series of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones were synthesized via a five-steps procedure starting from 2-amino-5-methylbenzoic acid. The cytotoxicity of the resulting compounds against A-549 (human lung cancer), HCT-8 (human colon cancer), HepG2 (human liver cancer), and K562 (human myelogenous leukaemia) cell lines was determined by the MTT assay. Preliminary screening results of these compounds are reported.
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PMID:Synthesis and cytotoxicity screening of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones. 1921 84

Four novel porphyrins containing nitric oxide (NO) donors were synthesized, and the structures of all the products were characterized by IR, UV-vis, (1)H NMR, and elementary analysis. Interestingly, these new compounds not only were able to release NO, but also showed cancer cell-oriented accumulation. Higher accumulation of these new porphyrins containing NO donors in BEL-7402 liver cancer cells than in L-02 liver normal cells was corroborated by UV-vis spectroscopy. The biological activity of these porphyrins against BEL-7402 liver cancer cells was tested with a MTT assay. The studies indicated that they had more effective killing of BEL-7402 liver cancer cells than that of L-02 liver normal cells, and they had similar activity against MCF-7 breast cancer cells when compared to 5-fluorouracil in the absence of light.
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PMID:Porphyrins containing nitric oxide donors: Synthesis and cancer cell-oriented NO release. 1923 50

During the search of new anti-cancer agent from high fungi, the ethyl acetate extract of the mushroom Suillus placidus was found to exhibit a significant cytotoxic activity against human hepatoma HepG2 cells. With bioassay-guided fractionation, a cytotoxic component suillin was isolated from the extract. The anti-cancer effect of suillin was subsequently examined in 8 human cancer cell lines by using MTT assay. It is of interest to note that human liver cancer cells (HepG2 cells, Hep3B cells, and SK-Hep-1) were preferentially killed by suillin with an IC(50) of approximately 2microM in a 48h treatment. Mechanistically. suillin was found for the first time to induce apoptosis in HepG2 cells as characterized by DNA fragmentation, phosphatidyl-serine (PS) externalization, activation of caspase-3, -8, -9, depolarization of mitochondrial membrane potential, as well as release of cytochrome c into the cytosol. Moreover, the apoptosis induced by suillin was suppressed by both caspase-8 and -9 inhibitors. Western blot analysis revealed significant increases in the protein levels of Fas death receptor, adaptor FADD protein, pro-apoptotic protein Bad and a decline of Bid. These results suggest that the induction of apoptosis by suillin is through both death receptor and mitochondrial pathways. Taken together, our results suggest that suillin might be an effective agent to treat liver cancer.
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PMID:Suillin from the mushroom Suillus placidus as potent apoptosis inducer in human hepatoma HepG2 cells. 1961 21

Recently, indole-3-acetic acid (IAA) has been introduced as a new cancer therapeutic agent through oxidative decarboxylation by horseradish peroxidase (HRP). The purpose of this study was to determine the therapeutic feasibility of IAA/light combination against liver cancer. SK-HEP-1 cells were irradiated with UVB or visible light (518 nm) in the presence of IAA. Cell viability was measured using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Then, IAA was injected in SK-HEP-1 liver cancer cell-implanted nude mice, and the tumor area was irradiated with intense pulsed light (IPL). Then, tissue was taken for terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick-end labeling (TUNEL) assay and immunohistochemical staining for 8-hydroxy-deoxyguanosine (8-OHdG), p53, caspase-3, and proliferating cell nuclear antigen (PCNA). In vitro experiments demonstrated that IAA alone was not cytotoxic, but activated IAA by HRP or light caused cell death. In vivo experiments showed that IAA/IPL treatment caused regression of tumor cells in SK-HEP-1-implanted nude mice. The TUNEL assay showed that IAA/IPL induced cancer cell apoptosis, and this was confirmed by increases in 8-OHdG, p53, and caspase-3 in IAA/IPL-treated mice. In contrast, IPL alone did not induce apoptosis, indicating that the apoptotic effect resulted from activated IAA by light. In summary, we showed that IAA/light induced tumor regression in SK-HEP-1-implanted nude mice. These results suggest the potential use of IAA/light combination in liver cancer.
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PMID:Experimental photodynamic therapy for liver cancer cell-implanted nude mice by an indole-3-acetic acid and intense pulsed light combination. 1972 Dec 41

Cavernous hemangioma is vascular malformation with developmental aberrations. It was assumed that the abnormality of endothelial cells contributed greatly to the occurrence of cavernous hemangioma. In our previous study, we have found distinct characteristics of endothelial cells derived from human liver cavernous hemangioma (HCHEC). Here, we reported the abnormal vascular vessels formed by primary HCHEC in nude mice and that the drug podophyllotoxin can destroy HCHEC in vitro and in vivo. HCHEC was isolated from a human liver cavernous hemangioma specimen, and the HCHEC generated a red hemangioma-like mass 7 days after subcutaneously co-inoculating HCHEC and human liver cancer cells (Bel-7402) in nude mice. Lentiviral expression of GFP and immunohistochemistry for human CD31 was used to confirm that the HCHEC formed the blood vessels in nude mice. And the pathological features of vascular vessels formed by HCHEC were very similar to clinical cavernous hemangioma. In addition, by MTT assay, the drug podophyllotoxin was found inhibiting HCHEC viability, and by TUNEL and DNA ladder assays, podophyllotoxin was found inducing apoptosis of HCHEC. Moreover, podophyllotoxin was also effective for destroying the abnormal vascular vessels in the hemangioma-like mass in nude mice. In summary, the HCHEC can form abnormal blood vessels in nude mice, and we can evaluate drugs for cavernous hemangioma by using HCHEC in vitro and in vivo.
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PMID:Abnormal blood vessels formed by human liver cavernous hemangioma endothelial cells in nude mice are suitable for drug evaluation. 1972 28

Cisplatin is one of the most potent chemotherapeutic anticancer drugs for the treatment of various cancers. The cytotoxic action of the drug is often thought to be associated with its ability to bind DNA to form cisplatin-DNA adducts. Impaired DNA repair processes including base excision repair (BER) play important roles on its cytotoxicity. XRCC1 is a key protein known to play a central role at an early stage in the BER pathway. However, whether XRCC1 contributes to decrease the cisplatin cytotoxicity and cisplatin-induced DNA damage in HepG2 still remains unknown. Hence, the purpose of this study was to explore whether abrogation of XRCC1 gene expression by short hairpin RNAs (shRNA) could reduce DNA repair and thus sensitize liver cancer cells to cisplatin. We abrogated the XRCC1 gene in HepG2 cell using shRNA transfection. Cell viability was measured by MTT assay and clonogenicity assay. Comet assay was used to detect the DNA damage induced by cisplatin. The host cell reactivation was employed to assess the DNA repair capacity of cisplatin-damaged luciferase reporter plasmid. Flow cytometry analysis was used to determine cisplatin-induced apoptosis, cell cycle and reactive oxygen species (ROS). The results showed that abrogation of XRCC1 could sensitize HepG2 cells to cisplatin. This enhanced cytotoxicity could be attributed to the increased DNA damage and reduced DNA repair capacity. Increasing cell cycle arrest and intracellular ROS production lead to more tumor cell apoptosis and then enhanced the cisplatin cytotoxicity. Our results suggested that the cisplatin cytotoxicity may increase by targeting inhibition of XRCC1.
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PMID:Increase the cisplatin cytotoxicity and cisplatin-induced DNA damage in HepG2 cells by XRCC1 abrogation related mechanisms. 1985 26


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