ABSTRACT
V(III)(OH)[O(2)C-C(6)H(4)-CO(2)].(HO(2)C-C(6)H(4)-O(2)H)(x)(DMF)(y)(H(2)O)(z) or MIL-68 was solvothermally synthesised in a non-aqueous medium. Its structure, built up from octahedral chains connected by terephthalate linkers, exhibits large hexagonal channels containing different occluded moieties. Their irreversible removal releases a specific surface area of 603(22) m(2).g(-1)(BET).
ABSTRACT
(V(III)(OH))(2)[C(6)H(2)(CO(2))(4)].4H(2)O (labeled MIL-60) and V(III)(OH)[(2)(O(2)C)C(6)H(2)(COOH)(2)].H(2)O (labeled MIL-61) were hydrothermally synthesized from mixtures of VCl(3), 1,2,4,5-benzenetetracarboxylic acid, and water heated for 3 days at 473 K. The structure of MIL-60 was solved from single-crystal X-ray diffraction data in the triclinic centrosymmetric P1 (No. 2) space group with lattice parameters a = 6.3758(5) A, b = 6.8840(5) A, c = 9.0254(5) A, alpha = 69.010(2) degrees, beta = 85.197(2) degrees, gamma = 79.452(2) degrees, V = 363.53(5) A(3), and Z = 1. The structure of MIL-61 was ab initio determined from an X-ray powder diffraction pattern. MIL-61 crystallizes in the Pnma (No. 62) orthorhombic space group with lattice parameters a = 14.8860(1) A, b = 6.9164(1) A, c = 10.6669(2) A, V = 1098.23(3) A(3), and Z = 4. Both structures contain the same inorganic building block that consists of trans chains of V(III)O(4)(OH)(2) octahedra. The three-dimensional frameworks of MIL-60 and MIL-61 are constituted by the linkage of these chains via the organic molecules so delimiting the channels or cages where the water molecules are encapsulated. The magnetic behavior of these two phases is presented: MIL-60 is paramagnetic, and MIL-61 antiferromagnetically orders below T(N) = 55(5) K.
ABSTRACT
[V(III)(H2O)]3O(O2CC6H4CO2)3.(Cl, 9H2O) (denoted MIL-59) presents a three-dimensional framework built up from octahedral vanadium trimers joined via the isophthalate anionic linkers to delimit cages where water molecules and chlorine anions are occluded; the frustrated magnetic behaviour of MIL-59 is discussed.
ABSTRACT
Non-small-cell lung carcinoma (NSCLC) is a particularly serious disease because of its chemoresistance to current treatments. To investigate the nature of his generally innate resistance, we cloned an established cell line (NSCLC-N6) derived from a non-small cell bronchopulmonary carcinoma. Four cell subpopulations (C15, C65, C92 and C98) were isolated from the mother line. These four clones were studied in comparison with each other for cell doubling time in vitro, ploidy, chemosensitivity in vitro, cytogenetic, expression of the oncogene erb-B2 and other tumor markers (Kr, CEA and Chr A). Each clone shows a distinct biologic pattern for various biological parameters. Our results indicated hat cell doubling time (in vitro) increased when the hyperploid population was prevailing. The clones differ in their chemosensitivity to therapeutic agents. This cellular diversity might help to explain why these tumors are chemoresistant. This heterogeneity within NSCLC tumors should be taken into consideration in the choice of treatment.
Subject(s)
Carcinoma, Non-Small-Cell Lung/pathology , Lung Neoplasms/pathology , Aneuploidy , Antineoplastic Agents/therapeutic use , Biomarkers, Tumor/metabolism , Carcinoembryonic Antigen/metabolism , Carcinoma, Non-Small-Cell Lung/drug therapy , Chromogranin A , Chromogranins/metabolism , Chromosome Aberrations/pathology , Chromosome Disorders , Clone Cells , DNA, Neoplasm/metabolism , Humans , Karyotyping , Keratins/metabolism , Lung Neoplasms/drug therapy , Receptor, ErbB-2/metabolism , Tumor Cells, Cultured/drug effectsABSTRACT
Pachymatismin is a novel glycoprotein extracted from a marine sponge, which has an antiproliferative effect in vitro on cells from a human non-small-cell bronchopulmonary carcinoma (NSCLC-N6). The drug blocks irreversibly the cells in the G0/G1 phase of the cell cycle. Here, we investigate the antitumor activity of pachymatismin against this cell line. Tumor growth was studied after three weeks treatment of nude mice by different doses of pachymatismin. A significant decrease in tumor growth was observed.
Subject(s)
Antineoplastic Agents/pharmacology , Biological Factors/pharmacology , Carcinoma, Non-Small-Cell Lung/drug therapy , Glycoproteins/pharmacology , Lung Neoplasms/drug therapy , Porifera/chemistry , Animals , Dose-Response Relationship, Drug , Female , Humans , Injections, Intravenous , Intercellular Signaling Peptides and Proteins , Mice , Mice, Nude , Transplantation, Heterologous , Tumor Cells, Cultured/drug effects , Tumor Cells, Cultured/transplantationABSTRACT
We studied the pharmacomodulating effects of a marine substance, bistramide D, which is capable of inducing terminal differentiation on the expression of the c-erb-B1, ras, src, myc and p53 genes in the NSCLC-N6 cell line established from a non-small cell lung carcinoma. Analysis (subsequent to treatment) demonstrated that among the genes for which it was possible to detect expression, namely c-erb-B1, c-myc and p53, only the expression of the p53 gene varied significantly. The increase of the expression rate of the p53 gene underlines its prominent role in the control of cell proliferation and differentiation.
Subject(s)
Bronchial Neoplasms/metabolism , Bronchial Neoplasms/pathology , Carcinoma, Non-Small-Cell Lung/metabolism , Carcinoma, Non-Small-Cell Lung/pathology , Lung Neoplasms/metabolism , Lung Neoplasms/pathology , Tumor Suppressor Protein p53/biosynthesis , Antineoplastic Agents/pharmacology , Blotting, Northern , Bronchial Neoplasms/drug therapy , Carcinoma, Non-Small-Cell Lung/drug therapy , Cell Differentiation/drug effects , Cell Differentiation/physiology , ErbB Receptors/biosynthesis , ErbB Receptors/genetics , Ethers, Cyclic/pharmacology , Gene Expression Regulation, Neoplastic/drug effects , Genes, p53 , Humans , Lung Neoplasms/drug therapy , Oncogenes , Proto-Oncogene Proteins c-myc/biosynthesis , Proto-Oncogene Proteins c-myc/genetics , Proto-Oncogene Proteins pp60(c-src)/biosynthesis , Proto-Oncogene Proteins pp60(c-src)/genetics , RNA, Neoplasm/analysis , RNA, Neoplasm/metabolism , Tumor Cells, Cultured , Tumor Suppressor Protein p53/genetics , ras Proteins/biosynthesis , ras Proteins/geneticsABSTRACT
Fucans, sulfated polysaccharides extracted from brown seaweeds, have been shown to be endowed with inhibitory effects cell growth in various experimental models. We studied both the antiproliferative and antitumor properties of a fucoidan extract (HF) obtained from the brown seaweed Ascophyllum nodosum on a cell line derived from a non-small-cell human bronchopulmonary carcinoma (NSCLC-N6), this type of carcinoma is particularly chemo-resistant. HF exerts in vitro a reversible antiproliferative activity with a block observed in the G1 phase the cell cycle. Studies performed with the NSCLC-bearing nude mice show antitumor activity at subtoxic doses. These preliminary results indicate that HF exhibits inhibitory effect both in vitro and in vivo and is very potent antitumor agent in cancer therapy.
Subject(s)
Antineoplastic Agents/pharmacology , Bronchial Neoplasms/drug therapy , Carcinoma, Non-Small-Cell Lung/drug therapy , Lung Neoplasms/drug therapy , Phaeophyceae/chemistry , Plant Extracts/pharmacology , Polysaccharides/pharmacology , Animals , Bronchial Neoplasms/pathology , Carcinoma, Non-Small-Cell Lung/pathology , Cell Cycle/drug effects , Cell Division/drug effects , Female , Humans , Lung Neoplasms/pathology , Mice , Mice, Nude , Neoplasm Transplantation , Transplantation, Heterologous , Tumor Cells, CulturedABSTRACT
The inhibitory effect of natural substances of marine origin on the erb-B2 oncogene of a human NSCLC-N6 line was demonstrated in vitro by simultaneous study of the expression of the gene and its product, using respectively an erb-B2 specific probe and an anti-c-erb-B2 polyclonal antibody. Preliminary results indicate inhibition ranging from 17-77% of oncogene expression and from 77-90% of product expression. The fact that substances of this type, with different chemical structures, have the common ability to induce terminal differentiation in an experimental model after irreversible blockade in G1 phase suggests a relationship between the inhibition of certain oncogenes and terminal differentiation.
Subject(s)
Acetamides , Antineoplastic Agents/pharmacology , Carcinoma, Non-Small-Cell Lung/drug therapy , Carcinoma, Non-Small-Cell Lung/genetics , ErbB Receptors/biosynthesis , Lung Neoplasms/drug therapy , Lung Neoplasms/genetics , Oncogenes/drug effects , Proto-Oncogene Proteins/biosynthesis , Pyrans , Cell Differentiation/drug effects , Diterpenes/pharmacology , Ethers, Cyclic/pharmacology , Gene Expression Regulation, Neoplastic/drug effects , Humans , Receptor, ErbB-2 , Spiro Compounds , Succinimides/pharmacology , Tumor Cells, CulturedABSTRACT
Bistramides A, D and K are substances extracted from the marine ascidian Lissoclinum bistratum Sluiter that are capable of inducing in vitro terminal differentiation (G1DT) of cells from a non-small cell broncho-pulmonary carcinoma (NSCLCN6), but present different in vitro toxicities. This study shows that only the least toxic bistramides D and K possess an antitumor activity. These two substances could be administered as a continuous treatment which would induce terminal differentiation of stem cells at their entry into the cell cycle, thereby causing their destruction.
Subject(s)
Acetamides , Antineoplastic Agents/therapeutic use , Carcinoma, Bronchogenic/drug therapy , Carcinoma, Non-Small-Cell Lung/drug therapy , Ethers, Cyclic/therapeutic use , Lung Neoplasms/drug therapy , Pyrans , Animals , Carcinoma, Bronchogenic/pathology , Carcinoma, Non-Small-Cell Lung/pathology , Cell Division/drug effects , Dose-Response Relationship, Drug , Female , Humans , Lung Neoplasms/pathology , Mice , Mice, Inbred Strains , Mice, Nude , Molecular Structure , Regression Analysis , Spiro Compounds , Structure-Activity Relationship , Transplantation, HeterologousABSTRACT
Vinorelbine (NavelbineR) is a new antitumor agent chemically related to the Vinca alkaloid group, but differentiated by its in vivo activity relative to non-small-cell lung carcinoma (NSCLC). Studies in the NSCLC-bearing nude mouse of vinorelbine associations with drugs currently used clinically in phase III (cisplatin, 5-fluorouracil and actinomycin D) showed that such associations are ineffective or even of negative value and that it would be preferable to use vinorelbine alone in a single dose at the maximum tolerated concentration.
Subject(s)
Antineoplastic Combined Chemotherapy Protocols/therapeutic use , Carcinoma, Non-Small-Cell Lung/drug therapy , Lung Neoplasms/drug therapy , Animals , Cisplatin/administration & dosage , Dactinomycin/administration & dosage , Drug Screening Assays, Antitumor , Fluorouracil/administration & dosage , Humans , Mice , Mice, Nude , Neoplasm Transplantation , Vinblastine/administration & dosage , Vinblastine/analogs & derivatives , VinorelbineABSTRACT
Bistramide A, a new toxin isolated from a New Caledonian Urochordata, shows an antiproliferative effect on a non-small-cell lung carcinoma line in vitro and G1-blockade. In this work, the growth arrest induced by bistramide A was shown to be irreversible as assessed by growth kinetics of pretreated cells. Furthermore, the drug caused an underexpression of the nuclear antigen Ki67. These events are similar to a G1-differentiation cell cycle step blockage and a terminal maturation induction.
Subject(s)
Acetamides , Antineoplastic Agents/pharmacology , Carcinoma, Non-Small-Cell Lung/drug therapy , Ethers, Cyclic/pharmacology , Lung Neoplasms/drug therapy , Pyrans , Cell Cycle/immunology , Cell Division/drug effects , Cell Division/immunology , Humans , Ki-67 Antigen , Neoplasm Proteins/analysis , Nuclear Proteins/analysis , Spiro Compounds , Tumor Cells, CulturedABSTRACT
The antiproliferative activity of two nitrogenous labdane cytotoxic substances from Lissoclinum voeltzkowi Michaelson (Urochordata), dichlorolissoclimide (P2) and chlorolissoclimide (P1), was studied in vitro on a continuous human non-small-cell bronchopulmonary carcinoma line (NSCLC-N6) at the cell cycle level. This antiproliferative effect resulted from a blockade of G1 phase cells. Mortality occurred, regardless of the degree of cell ploidy, with cell transition to an out-of-cycle situation characteristic of a G1D terminal maturation state.
Subject(s)
Carcinoma, Non-Small-Cell Lung/drug therapy , Diterpenes/pharmacology , Lung Neoplasms/drug therapy , Succinimides/pharmacology , Carcinoma, Non-Small-Cell Lung/pathology , Drug Screening Assays, Antitumor , Flow Cytometry , G1 Phase/drug effects , Humans , Lung Neoplasms/pathology , Tumor Cells, CulturedABSTRACT
The antiproliferative effects of bistramide A, a nitrogenous dilactam polyether from Lissoclinum bistratum Sluiter (Urochordata), were studied at the level of the cell cycle in asynchronous cells of the NSCLCN6-L16 line. Bistramide A has a dual mechanism that induces blockade in the G1 phase (compatible with differentiation properties reported elsewhere) and causes polyploidy that is suggestive of inaptitude for cytokinesis. These effects confirm the results of cytomorphology studies in electron microscopy.
Subject(s)
Acetamides , Antineoplastic Agents/therapeutic use , Carcinoma, Bronchogenic/drug therapy , Carcinoma, Non-Small-Cell Lung/drug therapy , Ethers, Cyclic/therapeutic use , Lung Neoplasms/drug therapy , Pyrans , Animals , Antineoplastic Agents/toxicity , Carcinoma, Bronchogenic/ultrastructure , Carcinoma, Non-Small-Cell Lung/ultrastructure , Cell Cycle/drug effects , Cell Line , Drug Screening Assays, Antitumor , Ethers, Cyclic/toxicity , Flow Cytometry , Humans , Lung Neoplasms/ultrastructure , Mice , Mice, Nude , Microscopy, Electron , Neoplasm Transplantation , Spiro Compounds , Tumor Cells, Cultured/drug effects , Tumor Cells, Cultured/ultrastructureABSTRACT
Three personal cases, and the cases of literature of congenital adrenal hypoplasia with cytomegaly allow an histological definition. Clinical and biological findings are described. In 2 cases, a diffused hypertrophy of the cells responsible for corticotrope or melanotrope secretion was discovered; it confirmed the peripheral adrenal origin of the condition, as well as high plasmatic level of ACTH, in the third case. Sex-bound cytomegalic adrenal hypoplasia is differenciated from other cortico-adrenal insufficiencies with cytomegaly.