Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:Q86TM3 (cage)
 29,987 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Two new bisorbicillinoids possessing an open-ended cage structure, dihydrotrichodimerol (1) and tetrahydrotrichodimerol (2), were isolated from a marine-derived Penicillium terrestre. Their structures were established by spectroscopic methods. Their cytotoxic activities against P388 and A-549 cell lines were preliminarily evaluated by the MTT method.
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PMID:Dihydrotrichodimerol and tetrahydrotrichodimerol, two new bisorbicillinoids, from a marine-derived Penicillium terrestre. 1639 77

Forty-three norditerpenoid alkaloids isolated from Aconitum, Delphinium and Consolida species have been evaluated for their cytotoxic effects on the tumor cell lines CT26 (murine colon adenocarcinoma), SW480 (human colon adenocarcinoma), HeLa (human cervical adenocarcinoma), SkMel25 (human melanoma) and SkMel28 (human malignant melanoma) with several multidrug resistance mechanisms and the non-tumor cell line CHO (Chinese hamster ovary cells). Neoline (5), 8-O-methylcolumbianine (6), 1,14-diacetylcardiopetaline (9), 18-O-demethylpubescenine (13), 14-deacetylpubescenine (14), pubescenine (15), 14-deacetylajadine (25), lycoctonine (26), browniine (28), delphatine (29), dehydrotakaosamine (34), and ajadelphinine (37) exhibited selective cytotoxicity to cancerous versus non-cancerous cells. Some of these compounds had an irreversible effect on SW480 (5, 15, 25, 26, and 34), HeLa (15, 34, and 37) and SkMel25 (15 and 34) cell lines. In order to gain insights into the mechanism of irreversible cytotoxic action of these compounds we compared the cell viability by means of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) and the acid phosphatase (AP) methods. Our results suggest that the effects of these compounds could be related to the inhibition of ATP production.
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PMID:In vitro cytotoxicity of norditerpenoid alkaloids. 1661 Feb 10

One of the significant characteristics of traditional Chinese medicine is the use of insects, other terrestrial arthropods and their products as drugs. In the present work, the extract of housefly (Musca domestica) larvae was studied by an agar well diffusion assay and minimum bactericidal concentration (MBC) determination for detection of antimicrobial activity and by MTT assay method to test its in vitro anti-tumor activity. In our studies, the extract inhibited six tested bacterial pathogens and Escherichia coli Jm109, a gene-modified strain resistant to ampicillin with the MBCs ranging from 200 to 1600 microg/ml, while Gram-positive bacteria were more sensitive than Gram-negative bacteria. The extract showed high in vitro anti-tumor activity against human colon cancer cell line CT26 with the IRs ranging from 62 to 89%. The extract of housefly larvae inoculated with Shigella dysenteriae 51302 exhibited higher antibacterial activity and in vitro anti-tumor activity than that of native larvae, which may indicate the same principle involved in the use of Bombyx mori larvae infected with silk moth fungus Beauveria bassiana and Hepialis larvae infected with Cordiceps fungus in the traditional Chinese medicine. Both extracts did not show any coagulation activity and haemolysis activity against rabbit erythrocytes at 500 and 1000 microg/ml. The results support its use in the traditional Chinese medicine, and warrant the further identification of the active molecule in the housefly larvae.
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PMID:Antibacterial activity and in vitro anti-tumor activity of the extract of the larvae of the housefly (Musca domestica). 1722

To assess the mechanisms of modest hypothermia (MH) and its effects on cellular radiation response, a model of anesthesia-induced modest hypothermia (AIMH) in the adult mice and a model of pure MH in the newborn mice were established. The survival rate of lethally irradiated mice was increased to 72% through AIMH before irradiation. Both apoptosis and necrosis of human fetal bone marrow CD34(+) hematopoietic stem cells cultured under MH were significantly decreased as detected by MTT and flow cytometry, with three-color labeled by PE-CD(34) (+)/ FITC-AnnexinV /7AAD. The survival and proliferation of mouse bone marrow MNC treated with MH after irradiation were also increased. The MH exerted similar protective effects on the leukemia cell lines A20, HL60, K562 to the normal bone marrow cells, but it enhanced the radiation sensitivity of leukemia cell line FBL3 and mouse melanoma B16F10. No effects have been found on the radiation sensitivity of those cells treated with MH before irradiation. The results also showed that MH mediated the effects on radiation sensitivity, in addition to increasing the oxygen tension. These results show different effects of MH on different cells: (i) AIMH exerts a protective effect on the normal hematopoietic stem cells, some leukemia cell lines A20, HL60, K562, and some neoplasma 3LL, LOVO. And MH exhibits a synthetic effect with anesthetic. (ii) MH enhances the radiation sensitivity of another leukemia and neoplasma cell lines FBL3, B16F10 and CT26. Therefore, AIMH has a potential to enhance the effects of radiation-therapy and decrease side effects on some tumors.
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PMID:Effects of anesthesia-induced modest hypothermia on cellular radiation sensitivity. 1876 66

To investigate effect of poly (ADP-ribose) polymerase inhibition on the proliferation of CT26 cells in vitro and the mechanism of this effect. CT26 cells were treated with a range of concentrations of 5-Aminoisoquinolin-1-one (PARP inhibitor) in vitro. MTT assays and flow cytometry were used to determine the proliferation and cell cycle distribution, respectively, of the cells. The expression of PARP-1 was investigated by Western blot. The binding of Nuclear Factor-kappaB to DNA was detected by electrophoretic mobility shift assay. The proliferation of CT26 cells was significantly inhibited by 5-AIQ induced PARP inhibition in a dose-dependent manner. Proliferation was inhibited by 17.5% at 100 microM 5-AIQ, by 27.6% at 500 microM 5-AIQ and by 39.9% at 1000 microM (P < 0.05). After treatment with 5-AIQ, the proportion of cells in G(0)/G(l) phases increased and the proportion of cells in S phase decreased. The expression of PARP-1 was attenuated in 5-AIQ-treated CT26 cells (P < 0.05) and the binding of NF-kappaB to DNA binding was similarly diminished (P < 0.05). These results suggest that PARP inhibition reduced the proliferation of CT26 cells in vitro and influences the cell cycle. This inhibition is mediated by inhibiting PARP-1, which then diminishes the activity of NF-kappaB.
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PMID:Effect of poly (ADP-ribose) polymerase-1 inhibition on the proliferation of murine colon carcinoma CT26 cells. 1898 59

Biot2 is a novel murine testis-specific gene that was first identified using the SEREX technique, and named by our laboratory. Using conventional RT-PCR and real time RT-PCR, we tested the expression profile of Biot2 in normal tissues and various murine tumor cell lines. Using RNA interference, we studied the biological function of Biot2 in tumorigenesis. We applied various types of growth assay, such as the in vitro MTT, colony-forming and BrdU incorporation assays, along with in vivo tumorigenicity assays, to reveal its inhibition of tumor cell proliferation. The results revealed that the Biot2 transcript was detected only and strongly in the testis tissues and abundantly in five types of murine cancer cell line. Treating B16 murine melanoma, LL/2 murine Lewis lung carcinoma and CT26 murine colorectal adenocarcinoma with special shRNA targeting Biot2 can significantly reduce the proliferation rate of these three tumor cell lines in vitro, as measured by the MTT, colony-forming and BrdU incorporation assays. The tumorigenicity of the CT26 cells transfected with special shRNA targeting Biot2 was also decreased distinctly in vivo compared with the control. It was therefore concluded that Biot2 plays a key role in tumorigenesis and could be a potential target for biotherapy.
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PMID:RNA interference against Biot2, a novel mouse testis-specific gene, inhibits the growth of tumor cells. 1927 78

Biocompatible Au nanoparticles with surfaces modified by PEG (polyethylene glycol) were developed in view of possible applications for the enhancement of radiotherapy. Such nanoparticles exhibit preferential deposition at tumor sites due to the enhanced permeation and retention (EPR) effect. Here, we systematically studied their effects on EMT-6 and CT26 cell survival rates during irradiation for a dose up to 10 Gy with a commercial biological irradiator (E(average) = 73 keV), a Cu-Kalpha(1) x-ray source (8.048 keV), a monochromatized synchrotron source (6.5 keV), a radio-oncology linear accelerator (6 MeV) and a proton source (3 MeV). The percentage of surviving cells after irradiation was found to decrease by approximately 2-45% in the presence of PEG-Au nanoparticles ([Au] = 400, 500 or 1000 microM). The cell survival rates decreased as a function of the dose for all sources and nanoparticle concentrations. These results could open the way to more effective cancer irradiation therapies by using nanoparticles with optimized surface treatment. Difficulties in applying MTT assays were also brought to light, showing that this approach is not suitable for radiobiology.
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PMID:Enhancement of cell radiation sensitivity by pegylated gold nanoparticles. 2009 Jan 83

Due to their unique properties, Anticancer dendrimer-based drugs have been displaying promising results in both in vitro and in vivo in the treatment of cancerous cells, as compared to the traditional polymers. In this report, two conjugates (G1+Pt and G2+Pt) of cisplatin [cis-diaminedichloroplatinum; (CDDP)] with two generations (G1, G2) of a biocompatible anionic dendrimer were prepared in an aqueous media. Their potential cytotoxic effects, in two sensitive cancer cell lines HT1080 and CT26 together with one resistant cancer cell line SKOV3, using MTT (methyl thiazolyl tetrazolium) assay were examined. Hemolytic impacts and cell death mechanisms of the conjugates on human blood and HT1080 cell line were also investigated. The conjugate G2+Pt showed greater toxicity up to 9x and 2x in the sensitive and resistant cell lines (IC(50) comparison, inhibitory concentration) respectively when compared to the parent drug. The G1+Pt conjugate showed greater toxicity only in the sensitive HT1080 (2x) and CT26 (3.7x) cell lines. Moreover, the G1+Pt conjugate was less toxic approximately one third of the cisplatin in SKOV3 after 48 hrs of incubation. In summary, the G2+Pt conjugate had greater toxicity than the G1+Pt conjugate and cisplatin, based on the in vitro results. Approximately the same hemolysis behavior was observed for both conjugates and cisplatin. Both apoptosis and necrosis mechanisms (about 2x more than cisplatin) were attributed to conjugates and cisplatin in a direct correlation between the concentration and the degree of cell death. In conclusion, these conjugates with such high potency and minimum hemolysis would be suitable candidates for use against these cancerous cell lines as efficient and novel antitumor agents.
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PMID:Anionic linear-globular dendrimer-cis-platinum (II) conjugates promote cytotoxicity in vitro against different cancer cell lines. 2016 88

C60 and its derivatives are very important nanomaterials in biological and materials science. Unfortunately, due to the high hydrophobicity of the C60 cage, most of these materials are insoluble in water and their usages are quitely restricted. Here we reported the preparation and characterization of (OH)16C60CHCOOH, a new multihydroxylated methanofullerene carboxylic acid (MMFCA) derivative with high aqueous solubility. The elementary analysis, FT-IR and 1HNMR confirmed the structure of this material. Like other C60 and its derivatives, this new derivative also contains the free radical scavenging ability, measured by electron spin resonance (ESR) test. On the other hand, the MTT assay showed it had low cytotoxicity. Therefore, this new MMFCA derivative might be a potential vehicle for the introduction of hydrophobic C60 derivatives into water or a hydrophilic environment.
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PMID:Preparation and characterization of a new hydrophilic C60 derivative (OH)16C60CHCOOH. 2035 38

Fullerenes are condensed ring aromatic compounds with extended pi systems; they have unique cage structures. Current studies suggest that several fullerene derivatives have neuroprotective effects, and it is expected that fullerenes will be useful in drug delivery system and novel medical devices targeting the brain. However, little is known about the effects of fullerenes and its derivative on brain function. We examined the effect of fullerene(OH)24 on the central nervous system in this study. In a V79 colony assay, the IC50 of fullerene(OH)24 was 1.74 microg/ml. In an MTT assay, fullerene(OH)24 reduced proliferation of normal human astrocytes obviously. In an vivo study, 0.25 mg/kg(-1) of fullerene(OH)24 was injected into the lateral ventricle of rat brains. The intracerebral injection of fullerene(OH)24 remarkably decreased body weight and locomotor behavior of rats on day 1, but drastically increased locomotor behavior on day 7. The intracerebral injection of fullerene(OH)24 changed the monoamine concentration greatly on day 1 and slightly on day 30 after the injection. These results suggest that intracerebral injection of fullerene(OH)24 had strong and acute effects on the central nervous system, but that the effects were not permanent. In conclusion, we suggest that fullerene's derivative, fullerene(OH)24 had toxic effects on brain cells and that intracerebral injection of fullerene(OH)24 had acute harmful effects on brain monoamines neurotransmission and locomotor activity.
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PMID:Effects of intracerebral microinjection of hydroxylated-[60]fullerene on brain monoamine concentrations and locomotor behavior in rats. 2035 99


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