227 results about "MCF-7" patented technology

The invention relates to synthesis of benzimidazole-containing naphthalimide derivatives and applications of the benzimidazole-containing naphthalimide derivatives on cancer resistance, and belongs to the field of organic synthesis and pharmaceutical chemistry technology. The benzimidazole-containing naphthalimide derivatives are obtained through a method that a benzimidazole group is introduced into a fourth position of a naphthalene ring of naphthalimide. Experiments of proliferation inhibiting effects of the benzimidazole-containing naphthalimide derivatives on cancer cells adopt a microculture tetrozolium (MTT) reduction method and aim at MCF-7 human breast cancer cells, Hela human cervical cancer cells and PC12 rat adrenal medullary pheochromocytoma differentiated cells. Results of the experiments show that the benzimidazole-containing naphthalimide derivatives have the advantages of good inhibitory activity against cancer cells and good selectivity on cancer cells.

The invention relates to an endogenous protein marking method applied to genome-wide binding spectrum analysis. The method comprises the steps of designing sgRNA for upstream and downstream 50bp regions of an encoding termination site of an NCOA1 gene; verifying cutting efficiency of sgRNA mediated Cas9 by an experiment; building an anti-estrogen therapy tolerant MCF-7 breast cancer cell model; by utilizing a CRISPR/Cas9 homologous recombination technology, selecting and using effective sgRNA and DNA donors, and introducing a Flag tag in the 3' end of the ER alpha co-transcription factor NCOA1 gene; and establishing a stable cell line with the Flag tag. Compared with the prior art, the method has the advantages that gene editing is performed by utilizing the CRISPR/Cas9 technology, so that the tag insertion efficiency of the gene editing is greatly improved; more importantly, chromatin structure parameters are introduced for designing sgRNA, so that effective cutting of Cas9 at a target site of a genome is ensured; and positive clone screening is performed by adopting DNA sequencing and RT-PCR sequencing methods, so that the positive clone identification step is simplified and the manpower and material resources for screening are reduced.

The invention discloses a target quaternary ammonium salt cationic polymer lipid gene carrier, a preparation method and an application thereof. The target quaternary ammonium salt cationic polymer lipid genetic carrier is characterized in that: a polymeric quaternary ammonium salt and lipid are adopted for preparing a quaternary ammonium salt cationic polymer lipid genetic carrier according to a mass ratio, wherein the mass ratio of the polymeric quaternary ammonium salt to the lipid is 0.05-20:1; then a assembly method or a modification method is adopted for modifying to prepare a folic acid or EGFR antibody modified cationic polymer lipid gene carrier. Results of gene transfection experiments show that: gene transfection efficiencies of the target quaternary ammonium salt cationic polymer lipid gene carrier in 293T cells and NIH-3T3 cells are the same as the gene transfection efficiencies of positive control lipofectamine of lipofectamine<TM>2000 in the 293T cells and the NIH-3T3 cells; the gene transfection efficiencies of the EGFR antibody modified cationic polymer lipid genetic carrier in liver cancer Huh-7 cells and breast cancer MCF-7 cells are higher than the gene transfection efficiencies of the lipofectamine<TM>2000 in the liver cancer Huh-7 cells and the breast cancer MCF-7 cells. The cationic polymer lipid genetic carrier system provided by the present invention has good biocompatibility and low cytotoxicity, and can be as an excellent non-viral gene delivery carrier.

The invention discloses a ratio-type two-photon formaldehyde fluorescent probe, a preparation method therefor and use of the ratio-type two-photon formaldehyde fluorescent probe. The ratio-type two-photon formaldehyde fluorescent probe has a structure as follows shown in the description. Molecules of the fluorescent probe disclosed by the invention show relatively high selectivity and sensitivity to formaldehyde in a coexisting system of molecules of the formaldehyde and other aldehydes, amino acids and the like. Proven by cytotoxicity tests, the molecules of the fluorescent probe disclosed by the invention are almost free of toxic action on cells; and shown by two-photon fluorescence microscopy imaging experiments, the molecules of the fluorescent probe disclosed by the invention have good cell permeability to MCF-7 cells, so that the fluorescent probe is applicable to the detection of presence of formaldehyde molecules in the cells.

The invention provides a compound having anticancer activity, which is obtained by cooperation of Norabieta cantharidin and platinum (IV) and modification of a piperazine derivative. The compound is characterized in that a Norabieta cantharidin piperazine derivative ligand is introduced, thereby cytotoxicity of a platinum (IV) compound is reduced, and high antineoplastic activity is provided. The result of the cytotoxicity experiments shows that the provided platinum (IV) compound has less destruction to normal mice fibroblast L929, but has good killing effect to cancer cells such as human breast cancer MCF-7 cell, human cervical carcinoma HeLa cell and human lung adenocarcinoma A549 cell, so that the compound having anticancer activity is capable of reducing the system toxicity and having equal anticancer activity with cisplatin. The compound having anticancer activity has good killing effect by aiming at cisplatin resistance human lung adenocarcinoma A549/DDP cell. Therefore, the toxicity is reduced, the cisplatin resistance can be reversed, and anticancer effect of the platinum medicines can be increased.

The flavonoid family of phytochemicals, particularly those derived from soy, has received attention regarding their hormonal activity and their effects on human health and disease. The types and amounts of these compounds in soy and other plants are controlled by both constitutive expression and stress-induced biosynthesis. The health benefits of soy may therefore be dependent upon the amounts of the various hormonally active phytochemicals present. We have identified increased biosynthesis of the isoflavonoid phytoalexin compounds, Glyceollins I, II and III, in soy plants grown under stressed conditions (elicited soy), which exhibit marked anti-estrogenic effects on ER function. Here we demonstrate that specific glyceollins, isolated from elicited soy, displayed anti-estrogenic activity, suppressing basal and estrogen stimulated colony formation of ER-positive estrogen dependent breast cancer cells and inhibiting ER-dependent gene expression of progesterone receptor (PgR) and stromal derived factor-1 (SDF1/CXCL12). Examining the effects of glyceollin on in vivo tumor formation/growth we demonstrate the ability of glyceollins to significantly suppress basal and estrogen-stimulated tumor growth of ER-positive MCF-7 breast and BG-1 ovarian carcinoma cells in ovariectomized female nude mice. We further demonstrate that the effects of glyceollins on suppression of tumor growth correlate with inhibition of estrogen stimulated PgR expression. In contrast to the uterotropic activity of tamoxifen the glyceollins displayed no uterine agonist activity. The Glyceollin (I-III) compounds may represent an important component of the health effects of soy as well as represent novel anti-estrogens useful in the prevention or treatment of breast and ovarian carcinoma.

The invention relates to a phenothiazine compound and a preparation method thereof. The invention further relates the application of the phenothiazine compound in anti-cancer drug preparation and anti-cancer drugs using the compound as the effective component. The phenothiazine compound has the advantages that the compound with broad-spectrum anti-cancer effect is obtained by modifying phenothiazine ternary interlink parent nucleuses, synthesizing method is simple, and high yield is achieved; the phenothiazine compound has certain restraining effect on human breast cancer cells line MCF-7 and human hepatoma cell line Hep-G2, and a new thought is provided to new drugs satisfying clinic requirements.

By means of biological computer technology, one group of gene sequence relevant to human tumor is obtained from GenBank. Based on RNA interference technology, one group of siRNA capable of inducing RNA interference is designed. Certain amount of siRNA is synthesized chemically and used as novel efficient and specific antitumor medicine. MTT detection shows that siRNA has obvious cytotoxic effect on MCF-7, BEL 7402, KB, HT-29 and other tuomr cells. Western Blotting detection shows that siRNA can lower the expression level of specific protein by 80-90%. Morphological observation shows that siRNA can cause tumor cell produce corresponding morphological change and chromatin concentration. Compared with available technology, siRNA is one antitumor medicine with completely new mechanism, high efficiency and fast speed.

The invention belongs to the technical field of medicines, and particularly discloses an oxygen-bridge bicyclo-[2.2.1]-heptylene compound comprising N-hydroxy-N'-phenyloctanediamide (SAHA) or a like structure, wherein the oxygen-bridge bicyclo-[2.2.1]-heptylene compound has an activity of resisting breast cancer. 3-(4-hydroxy penyl)-4-octanedioic acid monoanilide-furan and a vinyl sulphonate derivative are taken as raw materials and are reacted without a solvent or a catalyst at the temperature of 90 DEG C for 3 hours to further prepare the oxygen-bridge bicyclo-[2.2.1]-heptylene compound comprising the octanedioic acid monoanilide, and then the compound is reacted with oxammonium hydrochloride to obtain the oxygen-bridge bicyclo-[2.2.1]-heptylene compound comprising the N-hydroxy-N'-phenyloctanediamide. The experiments in vitro show that the oxygen-bridge bicyclo-[2.2.1]-heptylene compound has a great inhibitory activity on an MCF-7 cell in comparison to an existing anti-breast-cancer medicine tamoxifen.

The present invention discloses a cyclic pentapeptide with anti-tumour activity, which is cyclic (leucyl-N-methylleucyl-leucyl-leucyl-N-methylleucyl) and the constitutional formula of which is shown in the formula (I). The cyclic pentapeptide of the present invention is separated from galaxaura filamentosa in the South China Sea, and in vitro experiments show that the cyclic pentapeptide has strong inhibiting effect on human hepatoma cell lines (HepG2), human hepatoma cell lines (BEL-7402), human mammary cancer cell lines (MCF-7), human colon cancer cell lines (LOVO), human lung cancer cell lines (PC84045) and human nasopharyngeal cancer (CNE) and can keep the mitotic cycle of BEL-7402 hepatoma cells in G2/M phase. The present invention provides a pilot compound for the research and the development of new anti-tumour drugs and is valuable for the exploitation of the marine pharmaceutical resources of China.

The invention provides a chestnut seed alpha-1,6-glucan, a preparation method for the chestnut seed alpha-1,6-glucan, and application of the chestnut seed alpha-1,6-glucan to anticancer drugs. The structural formula of the chestnut seed alpha-1,6-glucan is [arrow 6)-alpha-Glcp(1 arrow]n, the weight average molecular weight is in the range of 1600-2400 kDa, and the average molecular weight is 2000 kDa; the chestnut seed alpha-1,6-glucan belongs to homopolysaccharides, and has obvious inhibited activity on proliferation of cervical cancer cells HeLa, breast cancer cells MCF-7 and adriamycin-resistant human breast cancer cell MCF-7 in vitro; chestnut is a rare fruit with the edible Chinese herbal function, and has no serious toxic and side effect; the chestnut seed alpha-1,6-glucan obtained according to the preparation method provided by the invention is high in sugar chain structural integrity, and is expected to be developed into anticancer drugs or assisted anticancer drugs.

Prostasin protein has been found to be a useful marker for determination of the invasiveness of and as a means to treat human carcinomas. Using RT-PCR and western blot analyses, prostasin protein and mRNA expression were found in normal human prostate epithelial cells and the human prostate cancer cell line LNCaP, but not in the highly invasive human prostate cancer cell lines DU-145 and PC-3. Imunohistochemistry studies of human prostate cancer specimens revealed a down-regulation of prostasin in high-grade tumors. Using RT-PCR and western blot analyses, prostasin protein and mRNA expression were found in a non-invasive human breast cancer cell line, MCF-7, while invasive human breast cancer cell lines MDA-MB-231 and MDA-MB-435s were found not to express either the prostasin protein or the mRNA. A non-invasive human breast cancer cell line, MDA-MB-453, was shown to express prostasin mRNA but not prostasin protein. Transfection of DU-145 and PC-3 cells with a full-length human prostasin cDNA restored prostasin expression and reduced the in vitro invasiveness by 68% and 42%, respectively. Transfection of MDA-MB-231 and MDA-MB-435s cells with a full-length human prostasin cDNA restored prostasin expression and reduced the in vitro invasiveness by 50% for either cell line. The prostasin gene promoter region was found to be hypermethylated at specific sites in invasive cancer cells.

The invention discloses a benzimidazole-containing Tr*ger's base type compound as well as a preparation method and application thereof. A structural formula of the compound is shown as a formula 3; the compound is prepared by carrying out aldimine condensation reaction on 2,8-dialdehyde-Tr*ger's base and substituted o-phenylenediamine. An in-vivo experiment shows that the benzimidazole-containingTr*ger's base type compound has relatively high inhibition activity on non-small cell lung cancer cells (A549), triple-negative breast cancer cells (231) and triple-positive breast cancer cells (MCF-7), and has low toxicity in human normal cells; the benzimidazole-containing Tr*ger's base type compound can be mixed with human body acceptable acid-forming salt or a medical carrier to form an anti-tumor drug. The invention provides a candidate compound for researching and developing a novel drug for treating triple-negative and triple-positive breast cancer and non-small cell lung cancer. The formula 3 is shown in the description.

Triptolide derivatives and application thereof relate to triptolide. Triptolide and the derivatives thereof has different-degree anticancer activity on HepG2 cell and MCF-7 cell. A method for using tRXRalpha and RXRalpha to evaluate the anticancer activity and toxic and side effects of triptolide and the derivatives thereof is firstly provided. The triptolide and the derivatives thereof are confirmed to have the anticancer activity closely related to the tRXRalpha protein expression lowering capacity, and the stronger rRXRalpha lowering capacity, the higher anticancer acitivty. Also the technical scheme firstly confirms that reduction of the toxic and side effects of the triptolide derivatives is related to the stability of normal-cell full-length RXRalpha protein, and the stronger protection effect of the derivatives on full-length RXRalpha, the smaller toxic and side effects.

The invention discloses tumor antigen Ran HLA-A0201 restricted simulated CTL epitope which is composed of Tyr-Met-Phe-Asp-Val-Thr-Ser-Arg-Val amino acid sequence. Compared with a natural CTL epitope, the simulated CTL epitope has stronger affinity and combination stability with HLA-A0201 molecules; meanwhile, the specific CTL induced by the simulated CTL epitope has IFN-gamma with higher level, and the specific CTL has stronger antigen-specific killing effect on positive MCF-7 cells of the HLA-A0201 and the Ran as well as T2 cells loading with the natural CTL epitope; and the tumor antigen Ran is widely expressed in different tumor tissues. The simulated CTL epitope can be used for preparing therapeutic polypeptide vaccine of Ran positive tumors, and the simulated CTL epitope has good development and application prospect in the tumor-specific immunotherapy field.

The invention provides a 2-(9-methylene anthracene) thiosemicarbazide and TAT modified gold nanoparticle drug delivery system. The 2-(9-methylene anthracene) thiosemicarbazide and TAT modified gold nanoparticle drug delivery system has the advantages that a gold nanosphere drug delivery system with the particle size being 3.8nm (sodium borohydride reduction method) and a gold nanosphere drug delivery system with the particle size being 22.1nm (sodium citrate reduction method) are built, the surfaces of the systems are modified with polypeptide TAT, the systems modified by the polypeptide TAT are used as the carriers of 2-(9-methylene anthracene) thiosemicarbazide, the fact that the drug-resistance index of large-particle-size gold nanospheres to drug-resistance cells is smaller is discovered through the antitumor activity evaluation of MCF-7 sensitive cells and MCF-7/ADR drug-resistance cells, and the fact shows that large-particle-size carriers are more suitable for tumor drug resistance treatment and the 22.1nm gold nanospheres have an enhancing effect on the Raman signal of the 2-(9-methylene anthracene) thiosemicarbazide and can be used for cellular-level Raman imaging.

The invention discloses an oxygen bridge bicyclo-[2.2.1]-heptene compound containing different functional side chain structures, as well as preparation and application thereof. The preparation comprises the following steps that furan derivatives which contain different functional side chain structures (2,3-glycol butyl, N,N-diethoxy ethylamino, 2-pyrrolidinyl ethyl, 2-piperidine ethyl and alkyl acid) and are synthesized from 3,4-bis(4-methyoxy-phenyl)furan reacts with vinyl sulfonamide derivatives at 90 DEG C for 12 hours in one step without solvent or catalyst to prepare the oxygen bridge bicyclo-[2.2.1]-heptene compound containing basic side chains and other functional side chain groups. In-vitro experiments indicate that, compared with an existing anti-breast cancer drug tamoxifen, thenovel sulfamide type oxygen bridge bicyclo-[2.2.1]-heptene compound has stronger inhibiting activity on MCF-7 cells, and has excellent protein degrading activity and equivalent degrading performance as that of existing drug fulvestrant.

The invention discloses a 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound, a preparing method, an application and a drug composite containing the compound thereof. More specifically, the invention discloses a 5,8-disubstituted-1,6-quinazoline-7-amidocarbonylation compound as shown in the formula I, a preparing method and an application thereof. By the growth inhibition test of various tumour cell lines (human breast cancer cells MDA-MB-435, p53-deleted poorly differentiated colorectal adenocarcinoma cells Hct116p53-/-, p53-enriched poorly differentiated colorectal adenocarcinoma cells Hct116p53+/+, human breast cancer cells Mcf-7, NIH189, human breast cancer cells SkBr-3, prostatic cancer cells LnCap, LnHer, human colorectal cancer cells HT29 and human ovarian cancer cellsHEY), the compound has favourable inhibition activity for the above tumour cells and can treat diseases caused by tumour cell malignant proliferation. The invention also discloses a drug composite containing the compound.

The invention relates to a pyrroloquinolines compound and an application thereof. A pyrroloquinoline ring is taken as a matrix and is appropriately and chemically modified to obtain a series of pyrroloquinolines compounds. Preliminary in vitro screen discovers that the pyrroloquinolines compound provided by the invention has a different-degree proliferation inhibition function on multiple tumour cell strains including human cervical cancer cell strain (HeLa), human lung cancer cell strain (A549), human colon cancer cell strain (HCT116), human leukemia cell strain (K562), human breast cancer cell strain (MCF-7) and the like; and moreover, the proliferation inhibition function of most compounds in 5 tumour cells is obviously better or is equivalent to a positive control drug SAHA (N-hydroxy-N'-phenyloctanediamide).

The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a kind of 8-substituted and 11-substituted 5-demethylated iso-cryptolepine derivatives, structurally shown in the general formula (I). The invention further discloses a preparation method for the iso-cryptolepine derivatives and application of the iso-cryptolepine derivatives in the preparation of anti-tumor medicaments. An in-vitro anti-tumor activity test result shows that the iso-cryptolepine derivatives have higher suppression activity to MCF-7, HCT-116 and DU-145 cell strains, GI50 values of a part of the iso-cryptolepine derivatives are equivalent to that of a positive medicament adriamycin, and a novel anti-tumor medicament can be further developed and prepared (referring to the Specification for the general formula (I)).

The invention belongs to the field of radiation sensitizing agents, in particular to an application of BTG2 (B cell translocation gene 2) in preparing a tumor radiation sensitizing agent for ionizing radiation including X-rays. The invention discloses an application of liposome mediated eukaryotic expression plasmid pcDNA3-BTG2 in preparing the radiation sensitizing agent, wherein the liposome mediated eukaryotic expression plasmid pcDNA3-BTG2 is transfected to MCF-7 (macrophage chemotactic factor-7) breast cancer cells and MDA-MB-231 breast cancer cells and expressed successfully, and the BTG2 protein can up-regulate the proapoptosis Bax protein and down-regulate the cell cycle regulatory protein Cyclin D1, and by promoting the cell apoptosis, G0/G1 phase arrest of the cells is promoted, thereby increasing the sensitivity of the breast cancer cells to ionizing radiation including the X-rays.

The invention relates to the fields of marine organism and medical technology, and provides an aaptamine alkaloid compound which is obtained by extraction, separation and purification from marine Aaptos aaptos produced in sea areas nearby the Paracel Islands, wherein the chemical structure of the alkaloid compound is as shown in the formula (I) (in the specification). In-vitro activity tests prove that the alkaloid compound has remarkable inhibitory activity on various different tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal carcinoma cells KB, human liver cancer cells Hep G2 and human colon cancer cells HT-29, and the alkaloid compound can be used for preparing anti-tumor medicines.

A method for preparing berberine hydrochloride composite nanoparticles comprise the following steps: (1) preparing berberine hydrochloride composite nanoparticle; (2) preparing berberine hydrochloridecomposite nanoparticles; as the only active ingredient, the berberine hydrochloride composite nanoparticles prepared by the invention can inhibit MCF-7 cell drugs; the berberine hydrochloride composite nanoparticles prepared by the invention are used as the only active ingredient in preparing anti-staphylococcus aureus and anti-escherichia coli medicines. The above preparation method is simple, the prepared composite nanoparticles have uniform particle size, encapsulation efficiency is high, which can reduce the recognition and phagocytosis of reticuloendothelial phagocytosis system (RES), and has slow release effect, increase the long circulation of carrier in vivo, improve the biological activity of drug, and achieve high efficiency and low toxicity, which provides conditions for the clinical application of berberine hydrochloride, and has significant economic and social benefits.

The invention provides a trichosanthes kirilowii anti-tumor activity protein as well as a preparation method thereof and application of the trichosanthes kirilowii anti-tumor activity protein in preparing anti-tumor drugs. The preparation method comprises the following steps: crushing full trichosanthes kirilowii, adding a protein extracting solution, stirring at 4 DEG C overnight, subsequently adding precooled acetone low-temperature precipitated protein, centrifugalizing, and then dissolving by using the protein extracting solution to obtain trichosanthes kirilowii crude protein; screening, separating and purifying anti-tumor activity components contained in the trichosanthes kirilowii crude protein by adopting fractional precipitation, anion-exchange chromatography and gel filtration chromatography to obtain and trichosanthes kirilowii anti-tumor activity protein. The trichosanthes kirilowii anti-tumor activity protein provided by the invention can be used for obviously inhibiting the survival of colon cancer DLD1 cells, breast cancer MCF-7 cells, bladder cancer T24 cells and cervical carcinoma HeLa cells and can be applied to preparing the anti-tumor drugs.

The invention discloses a sulfoxide alkaloid compound as well as a preparation method and an application for the same, and belongs to the field of microbial technology. The sulfoxide alkaloid compound is obtained by inoculating marine streptomyces into a tryptone soy broth liquid culture medium, culturing for 48-72 hours at a temperature of 28-30 DEG C and with a speed of 180-200 rpm, inoculating the marine streptomyces into a fermentation culture medium according to 10% of inoculum size, culturing for 432-456 hours at a temperature of 28-30 DEG C and with a speed of 180-200 rpm, and separating and purifying the fermentation solution. The compound has a remarkable inhibition effect on various bacteria, in particular, on staphylococcus aureus, and a certain anti-tumour activity for human breast cancer cells MCF-7, human liver cancer cells SMMC-7721, human acute myelomatosis cells U937 and small cell lung cancer cells NCI-H1688 simultaneously. Therefore, the compound has a good prospect for developing new anti-cancer medicines and new antibacterial medicines.

The invention discloses a compound Chinese actinidia root Chinese medicinal composition and a preparation method and application thereof, belonging to the technical field of traditional Chinese medicines. The Chinese medicinal composition is characterized by comprising the following traditional Chinese medicines in parts by weight: 40-80 parts of Chinese actinidia root, 20-40 parts of salvia chinensis, 20-40 parts of herba scutellariae barbatae, 20-40 parts of herba oldenlandiae and 20-40 parts of giant knotweed. The compound Chinese actinidia root Chinese medicinal composition has remarkable proliferation inhibition effects on various cancer cells such as a hepatoma cell line Hep-G2, a lung cancer cell line NCI-H460, a gastric cancer cell line MGC-803, a breast cancer cell line MCF-7, a colon cancer cell line HCT-116 and the like, and can be used for reducing physical and psychological pains of a cancer patient in the chemo-treatment process and solving the problems of difficult and expensive administration.

Using electroporation, it is possible to activate the natural reprogramming potential of living Xenopus laevis oocytes and pass it on to donor cells placed with eggs in one electroporation chamber. We demonstrated that co-electroporation at 150 v/cm/25 μF of mature oocytes with ^˜10⁵ cells/ml of suspension of various normal and cancerous human cell lines, such as bone marrow stromal cells, foreskin fibroblasts, pre-adipocytes, CD4+ T-lymphocytes, cheek cells, cervical carcinoma (HeLa) cells and breast adenocarcinoma (MCF-7) cells, reprograms donor cells into iPSc-like cells, which form colonies on irradiated MEF feeders. The iPSc-like cells generated by this study resemble human embryonic stem cells in colony morphology and expression of stem cell-associated transcription factors, including Oct3/4, Nanog, SOX-2, Rex-1, TRA-1-60 and SSEA-1. New method obviates the use of retroviral or lentiviral gene delivery vectors and other “non-parental” reprogramming approaches.