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42 results about "Colonic Carcinoma" patented technology

Indolone derivatives having different positions substituted and application thereof

The invention relates to indolone derivatives having different positions substituted and an application thereof, and particularly relates to preparation of the indolone derivatives having the different positions substituted and the application of the indolone derivatives in preparation of anti-tumor drugs, wherein in the structural formula, R1 is one of benzyl or alkyl compounds, R2 is one of hydrogen or halogen or aryl compounds, R3 is one of hydrogen or halogen or aryl or five-membered heterocyclic or six-membered heterocyclic compounds, R4 is one of hydrogen or halogen or aryl compounds, and R5 is one of hydrogen or halogen or aryl compounds. The indolone derivatives having the different positions substituted are synthesized for the first time, anti-tumor activity tests of the synthesized compounds aiming at human hepatoma cells (HepG2), human leukemia cells (K562) and human colon cancer cells (HT-29) are performed, and results show that IC50 of the derivatives is less than 10 [mu]M.
Owner:TIANJIN UNIV OF SCI & TECH

Cu-Eu exotic-metal-substituted arsenotungstate as well as preparation method and application thereof

The invention relates to Cu-Eu exotic-metal-substituted arsenotungstate which has a chemical formula as follows: Na2K3.5Eu0.5[Eu(H2O)7][As2W19Cu2O67(H2O)3].22H2O. A compound is prepared by reacting EuCl3, CuCl2.2H2O, NaCl and an arsenotungstate precursor-K14[As2W19O67(H2O)] in an aqueous solution. A preparation method is simple, easy to operate and relatively low in cost. Tests discover that the compound has a remarkable inhibition effect on the growth of human hepatocarcinoma cells HepG2 and human colonic cancer cells HCT-116 and can be used for preparing drugs for resisting cancers, especially liver cancers and colonic cancers, and research results provide an experimental basis for application of the compound to an aspect of drug activity.
Owner:HENAN UNIVERSITY

Compositions and methods for selected tumour treatment

Disclosed are novel compositions, methods and vaccines, which upon administration to a patient suffering from a melanoma, colon carcinoma tumor or breast cancer, postpone and / or reduce the need for chemotherapy treatment, slow the progression of or eliminate the tumor and / or alleviate the symptoms of the tumor. The compositions comprise stressed colon carcinoma, melanoma or breast cancer cells, preferably autologous such cells.
Owner:VASOGEN IRELAND LTD

Chalcone analogue containing 2-methyl-4-oxo-quinazoline-6-base, and preparation method and application thereof

The invention discloses a chalcone analogue containing 2-methyl-4-oxo-quinazoline-6-base, shown in a general formula (I), wherein the definitions of Ar1 and Ar2 are shown in the description. Besides, the invention further discloses a preparation method and a medical composition of the chalcone analogue containing 2-methyl-4-oxo-quinazoline-6-base. The chalcone analogue containing 2-methyl-4-oxo-quinazoline-6-base, shown in the general formula (I), has an inhibiting effect on cell proliferation of human colonic carcinoma (HCT-116) and human breast cancer (MCF-7), and can be used as an antitumor drug.
Owner:CAPITAL NORMAL UNIVERSITY

Compound BA-X having antitumor effect, preparation method and applications thereof

The present invention provides a class of compounds having a structure represented by a general formula 1, and a preparation method thereof, and applications in preparation of antitumor drugs. According to the present invention, the compound can significantly inhibit the growth of tumor cell lines (HepG-2, HT-29, Hela, BGC-823 and A549) while has low toxicity on Madin-Darby canine kidney (MDCK) cells, wherein the compound BH-26 has good anti-proliferative activity against colonic carcinoma cell line HT-29, human cervical cancer cell line Hela and human gastric cancer cell line BGC823 comparedto the positive drug cisplatin, and has significantly low cytotoxicity to normal Madin-Darby canine kidney (MDCK) cells compared to the positive drug cisplatin. The formula 1 is defined in the specification.
Owner:雷鹏程

Application of cynanchum ascyrifolium extract in preparation of tumor cell multidrug resistance reversal agents

The invention discloses an application of a cynanchum ascyrifolium extract in the preparation of tumor cell multidrug resistance reversal agents. The cynanchum ascyrifolium extract reverses the drug-resistant actions of human gastric tumor multidrug resistance cells, human colonic carcinoma multidrug resistance cells and human lung carcinoma multidrug resistance cells on clinical commonly used drugs such as taxol, adriamycin, 5-fluorouracil and cis-platinum. The cynanchum ascyrifolium extract disclosed by the invention is simple and convenient in preparation method, is combined with antitumor drugs to be applied to clinical application and has wide application prospects, and the curative effect of chemotherapy is improved.
Owner:QINGDAO UNIV

Composition capable of preventing and treating respiratory system diseases like novel coronavirus infection and other diseases

The invention belongs to the technical field of formulas of medicament for preventing and treating physical diseases and particularly relates to composition capable of preventing and treating respiratory system diseases like novel coronavirus infection and other diseases. Alliin, alliinase and type II transmembrane serine protease inhibitor are taken as basic effective ingredients, the compositionis administered in a way of inhalation by the lung, can kill physical diseases caused by bacteria such as methicillin-resistant staphylococcus aureus, multidrug resistance type escherichia coli, multidrug resistance type pseudomonas aeruginosa, multidrug resistance type mycobacterium tuberculosis and the like, viruses such as SARS-CoV-2 and the like, fungi such as multidrug resistance type candida albicans and the like, parasites and the like in a respiratory system and also can prevent fat accumulation in blood vessels of a human body, reduce the blood pressure, the cholesterol level in blood and destroy cancer cells of multiple epithelial tumors of breast cancer, ovarian cancer, colon cancer, renal carcinoma, liver cancer, lung cancer, mesothelioma and prostatic cancer, and the composition has no any toxic or harmful functions and risks and has broad application prospects.
Owner:WUXI HONGRUI BIOMEDICAL TECH CO LTD

Method for evaluating biosecurity of 76 nm nano silver on base of intestinal epithelial cells

The invention provides a method for evaluating the biosecurity of 76 nm nano silver on the base of intestinal epithelial cells. According to the method, cell lines of human colon carcinoma epithelial cells Caco-2 are selected as an object of study, nano zinc oxide (90.81 nm) with higher cytotoxicity is taken as a positive control, normal cells without the nano material are taken as a blank control, and the cytotoxicity of the nano material is preliminarily explored by an AO / EB double staining method and a CCK-8 method. The oxidative damage effect and the possible mechanism of nano silver on cells are studied by an oxidative stress method through detecting the influence of emission of ROS, SOD and GSH in the cells Caco-2. The result shows that 76.29nm silver particles (smaller than 200 mu g / ml) don't influence the activity of the cells Caco-2 obviously and cause no oxidative stress damage on the cells Caco-2, but the oxidation resistance of the cells is enhanced and is up to the highest level when the concentration of nano silver is 50 mu g / ml.
Owner:CHINA JILIANG UNIV

Pyridopyrimidine ketones derivative and application in preparing antitumor drugs thereof

The invention relates to pyridopyrimidine ketones derivatives and application of the pyridopyrimidine ketones derivatives in preparing antitumor drugs, belongs to the chemical pharmaceutical area, particularly relates to application of a compound with a structure shows as formula (I), wherein Ar represents a substituted benzene ring or a heterocyclic ring Het; R1 represents H or CH3; and R2 represents a substituted benzene ring, a heterocyclic ring or alkane. Experiments show that compound with a structure shown as formula (I) has varying degrees of inhibitory activity in vitro to A549 (human lung adenocarcinoma cell), HepG2 (human hepatocellullar carcinoma cell), SKOV-3 (human ovarian neoplasm), Hela (human cervical carcinoma cell) and SW620 (human colonic cancer cell), and in particular has good inhibitory activity to SW620, so that a new choice is provided for preparation of the antitumor drugs.
Owner:SICHUAN UNIV

Application of compound in tumor resistance

The invention relates to the technical field of medicines, in particular to application of a compound with a structure shown in a formula (I) (shown in the description) in preparation of a medicine for preventing or treating malignant tumor associated with cyclin-dependent kinase 2 (CDK2). Based on researches, the compound and pharmaceutically acceptable salt thereof have excellent inhibitory activity to the CDK2, remarkably inhibit the growth activity of a human colonic cancer cell HCT-116, a human breast cancer cell MCF-7, a human lung cancer cell A549 and a human liver cancer cell SMMC-7721, can block the cell cycle of cancer cells and facilitate apoptosis of the cancer cells; the compound and the pharmaceutically acceptable salt thereof can be applied to treatment of various malignant tumors.
Owner:WUHU YANGYAN PHARMA

Composition for adjuvant containing poly-gamma-glutamic acid

The present invention relates to a composition for an immunopotentiator(adjuvant) containing poly-gamma-glutamic acid and a composition for a vaccine containing the immunopotentiator, and more particularly, to an immunopotentiator containing poly-gamma-glutamic acid capable of enhancing antibody production rate by administering it to an animal together with antigen having low immunogenicity, and a composition for a vaccine containing the immunopotentiator and antigen. The inventive adjuvant has almost no toxicity and side effects, and show high antibody titer even when it is used with antigenhaving poor immunogenicity, so it can be used by adding to medical composition including preventive or curative vaccine for non-contagious chronic diseases as well as cancer, especially prostatic carcinoma, colon carcinoma, lung cancer, breast cancer, ovarian cancer, head and neck cancer, pudendum cancer, bladder cancer, brain tumor and glioma.
Owner:BIOLEADERS CORP +1

Oral medicine for colorectal carcinoma fistulation later-stage nursing, and its preparation method

The invention discloses an oral medicine for colorectal carcinoma fistulation later-stage nursing, and its preparation method. The medicine comprises 50-80 parts of Semen Phaseoli, 35-70 parts of Holothuria leucospilota, 40-90 parts of Meliosma fordii, 30-60 parts of roxburgh rose root, 24-60 parts of baccate sedge herb, 32-56 parts of shrubalthea root, 18-30 parts of radix paeoniae rubra, 22-46 parts of Inonotus cuticularis (Bull.: Fr.) Karst., 18-34 parts of konjac, 8-20 parts of Ajuga pantantha, 20-38 parts of Coriolus versicolor(L.ex Fr.)Quel., 20-50 parts of Cinnamomum wilsonii Gamble and 45-86 parts of Begonia yunnanensis Levl.. The medicine has strict composition and reasonable compatibility, has the efficacies of heat clearing, blood activating, diuresis inducing, channel freeing, intestine widening, qi rectifying, intestine damp heat removing, intestine moistening, bowel relaxing, blood circulation invigorating, bleeding stopping, qi moving, pain relieving, and stomach and intestine distention qi mitigating, comprises Chinese herbal medicines benefiting the rehabilitation of alimentary canal tumors and adjusting the immune function, can condition colorectal carcinoma patients subjected to fistulation, and has a good nursing efficacy on later-stage fistulization stoma complications.
Owner:张焕秀

Application of bacillus subtilis protein AMEP412 in inhibition of tumor cell proliferation

ActiveCN113788882ADiscovery of inhibitory functionDepsipeptidesAntineoplastic agentsSquamous CarcinomasGlioblastoma cell
The invention relates to an application of a bacillus subtilis protein AMEP412 with an amino acid sequence as shown in SEQ ID NO: 1 in inhibition of tumor cell proliferation. The tumor cells are any one of liver cancer cells, cervical cancer cells, pancreatic cancer cells, colon cancer cells, prostate cancer cells, lung cancer cells, uterine squamous cell carcinoma cells, gastric adenocarcinoma cells, malignant glioblastoma cells and breast cancer cells. According to the invention, the inhibition function of the protein AMEP412 on tumor cells is found; the protein can generate an inhibition effect on 10 kinds of tumor cells, has selective specificity on inhibition effects on different kinds of tumor cells, and has the best effect on breast cancer cells; transcriptomics research finds that the protein AMEP412 can cause the change of a plurality of pathways related to apoptosis and death in tumor cells, and a new material is accumulated for inhibiting the activity of the tumor cells.
Owner:HEILONGJIANG BAYI AGRICULTURAL UNIVERSITY +1

Antiangiogenic brassinosteroid compounds

A method of treating a solid tumor in a mammal by inhibiting angiogenesis, including administering to the mammal which has a solid tumor selected from the group consisting of breast carcinoma, lung carcinoma, prostate carcinoma, colon carcinoma, ovarian carcinoma, neuroblastoma, central nervous system tumor, multiform glioblastoma and melanoma; a composition including brassinosteroids of general formula (I)wherein can be a single or double bond and the configurations of carbon atoms C22 and C23 respectively linked to the substituents HO are S for both carbon atoms and a pharmaceutically acceptable additive.
Owner:CONSEJO NAT DE INVESTIGACIONES CIENTIFICAS Y TECH CONICET +1

Macrolactam compound FW05328-d and efficient fermentation method thereof

The invention belongs to the technical field of microbial fermentation, particularly relates to a structural analogue FW05328-d of a macrolactam compound FW05328-1, and further discloses an efficient fermentation method of the structural analogue by utilizing amino acid induction. The macrolactam compound FW05328-d is the structural analogue of the developed macrocyclic lactam compound FW05328-1, the structure of the compound FW05328-d is one -OH less than that of the compound FW05328-1 on the tenth site, the substance structure and chemical performance of the compound FW05328-d are more stable, and the macrolactam compound FW05328-d is more suitable for large-scale production. The antitumor activity test of the macrolactam compound FW05328-d proves that the compound has the activity of resisting mouse melanoma cell strains, human esophageal cancer cell strains and human colon cancer cell strains, and has better medical value.
Owner:FUJIAN INST OF MICROBIOLOGY

CEA recombinant adeno-associated virus, construction process thereof and applications

The invention relates to a CEA recombined gland-associated viral vector, a method for constructing the same and an application of the same. The recombined gland-associated viral vector is obtained through replacing a gland-associated virus structural gene in a gland-associated viral vector by a carcinoembryonic antigen CEA gene or a recombined gland-associated viral vector obtained by the mutant gene of the CEA gene. The CEA recombined gland-associated viral vector can convey the wild type or mutant carcinoembryonic antigen gene carried by the vector into a monocyte-macrophage-dendritic cell line; moreover, cells carrying the specific antigen genes can be used to stimulate the effector cells of an immune system. Experiments show that CTL, which is induced by DC infected by the rAAV of the PSA recombined gland-associated viral vector, can effectively inhibit the growth of malignant cells, or kill tumor cells in the body of a patient; therefore, the CEA recombined gland-associated viral vector or products related to the recombined gland-associated viral vector can be used to make medicines used to cure breast carcinoma, cancer of colon, gastric cancer and adenocarcinoma of lung.
Owner:GUANGZHOU BOWOJIN BIOLOGICAL TECH

Hedgehog-related prophylaxis, therapy and diagnosis of gi tract carcinogenesis

The present invention is based on the key roles played by Hedgehog proteins in the regulation of homeostasis of the adult intestinal epithelium. Ihh is expressed in the adult mammalian colon and provides a lineage-instructive signal and regulates colonic epithelial morphogenesis in a compartmental fashion. Loss of Ihh expression precedes morphological change in colon tumorigenesis, i.e. carcinogenesis, and Ihh was absent in HT-29 colon carcinoma cells. Treatment of cancerous HT-29 cells with exogenous Hedgehog protein restored their differentiation. Ihh thus plays a pivotal role in the maintenance of colonic epithelial homeostasis in the differentiation of the GI tract cells and is essential for the enrolment of these GI tract cells on the Death program thus maintaining homeostasis to avoid or treat carcinogenesis. In addition, in gastric cancer expression of Shh is lost and loss of Shh expression precedes morphological changes in the parietal cells of the stomach. Shh is specifically expressed in fundic glands as well as in gastric heterotopia in the esophagus in Meckel's diverticulum. Shh thus has a unique role as a morphogen in fundic gland homeostasis. The present invention relates to methods in which a source of Hedgehog proteins is used prophylactically or therapeutically to maintain homeostasis of the adult intestinal epithelium. In particular the invention relates methods whereby sources of Hedgehog protein are used to prevent or treat carcinogenesis in adult gastric and colonic tissues. The invention also relates to Hedgehog-based method of diagnosing susceptibility for or the presence of carcinogenesis in the adult GI tract, particularly in gastric and colonic tissues. The invention further provide for compositions to be used in the Hedgehog-based methods of diagnosing, preventing and treating epithelial tumorigenesis in the adult GI tract.
Owner:ACADEMISCH ZIEKENHUIS BIJ DE UNIV VAN AMSTERDAM ACADEMISCH MEDISCH CENT

Targeted PD-L1IGV affinity peptide D2 with antitumor activity

The invention belongs to the technical field of biopharmaceuticals, and specifically relates to a PD-L1-targeted drug with anti-tumor activity. IgV D-configuration affinity peptide D2 product and its preparation and application. The affinity peptide D2 specifically binds to PD-L1? The IgV region has an amino acid sequence of KHAHHTHNLRLP and a molecular weight of 1459.8. The affinity peptide D2 is prepared by the Fomc solid-phase peptide synthesis method, and plays a role as the main active ingredient in the preparation of anti-colon cancer drugs. The affinity peptide D2 provided by the present invention uses D-PD-L1? IgV was obtained by high-throughput screening as the target. Through tumor-bearing experiments in mice, the inventors proved that the affinity peptide D2 has good anti-tumor activity and can significantly inhibit the growth of tumors in mice, thus providing new ideas and ideas for the research and development of drugs based on PD-L1. theoretical basis.
Owner:ZHENGZHOU UNIV

Novel pyrido sulfur nitrogen 7-membered ring derivatives adopted as anti-tumor drugs, preparation method and applications thereof

The invention relates to multi-substituted pyrido sulfur nitrogen 7-membered ring derivatives represented by a general formula I-1, wherein the derivatives have wide anti-tumor activities. In vitro cell test results show that the compounds provide good inhibition effects for multiple human tumor cell lines, wherein the human tumor cell lines comprise human leukemia cell line OP-1, human colon carcinoma cell line HT29, human lung cancer cell line H460, paclitaxel resistant human lung cancer cell line H460TaxR, adriamycin resistant human breast cancer cell line MCF-7 / Adr and the like. According to the present invention, pharmaceutical auxiliary materials can be mixed with the compounds of the present invention independently or mixtures of the compounds and effective components of other anti-tumor drugs to prepare pharmaceutical formulations for treatments of various tumor diseases. The compounds represented by the I-1 are prepared by carrying out condensation and oxidation on compounds represented by a formula I-2 and R7COZ (Z is OH or halogen).
Owner:CHANGCHUN DISCOVERY SCI

Kit for left colonic carcinoma detection

The invention discloses a kit for left colonic carcinoma detection. The kit comprises an aptamer capable of detecting KLK6 protein and can be used for screening left colonic carcinoma. The kit has the advantages of being high in sensitivity, low in cost and suitable for large-scale screening.
Owner:汉氏联合(天津)干细胞研究院有限公司

Preparation method of folic acid modified Pluronic P85 copolymer and application of folic acid modified Pluronic P85 copolymer in 5-fluorouracil nano drug

The invention relates to the technical field of biological medicines, firstly provides a folic acid modified Pluronic P85 copolymer and also relates to a preparation method of a 5-fluorouracil anti-cancer nano drug. Experiments show that the 5-fluorouracil nano drug prepared by adopting the folic acid modified Pluronic P85 copolymer can be used for obviously inhibiting tumour cell growth; meanwhile, in a mouse colonic carcinoma hepatic metastasis model, formation of colonic carcinoma liver metastases can be obviously reduced, and lifetime of a mouse can be obviously prolonged, so that the folic acid modified Pluronic P85 copolymer has a good effect on resisting colonic carcinoma hepatic metastasis, and the 5-fluorouracil anti-cancer nano drug is hopeful to be an anti-tumour drug with a clinical application prospect.
Owner:SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY

Application of Aurora-B kinase and Survivin in preparation of colorectal cancer diagnosis kit

InactiveCN110261612AMaterial analysisAurora B kinaseLarge Intestine Carcinoma
The present invention relates to the field of diagnosis and treatment of the colorectal cancer, and in particular to the use of aurora-B kinase and survivin in the diagnosis of the colorectal cancer. The invention aims to provide application of Aurora B and Survivin in preparation of a colorectal cancer diagnosis kit. Expression of nuclear Aurora B and cytoplasmic Survivin are involved in lymph node metastasis of the colon cancer, and both nuclear Aurora B and cytoplasmic Survivin are closely related to lymph node metastasis of the colon cancer. Nuclear Aurora B and cytoplasmic Survivin are diagnostic markers and therapeutic targets for colorectal cancer.
Owner:GUILIN MEDICAL UNIVERSITY

EpCAM gene humanized mouse tumor cell model as well as construction method and use thereof

The invention belongs to the fields of genetic engineering and genetic modification of mouse cells, and particularly relates to an EpCAM gene humanized mouse tumor cell model as well as a constructionmethod and application thereof. A mouse EpCAM gene is knocked out by virtue of a CRISPR technique, and meanwhile, the humanized EpCAM gene is inserted into a mouse colon cancer cell CT26 through lentivirus infection. The EpCAM gene humanized mouse tumor cell model can be used for evaluating antibody tumor pesticide effect and has important guiding significance to clinic effects of developed drugs. Meanwhile, the EpCAM gene humanized mouse tumor cell model is an ideal mouse tumor cell model for evaluating the safety of anti-EpCAM antibody drugs and can be used for carrying out preclinical in-vivo evaluation on toxicological immunocell therapies of EpCAM antibody drugs and EpCAM-CAR T, EpCAM-CAR NK, so that a market blank is filled up.
Owner:NANJING BIOHENG BIOTECH CO LTD

A kind of camptothecin colon positioning drug release pellet and preparation method thereof

The invention belongs to the field of pharmaceutical preparations, and in particular relates to a colonic positioning drug release pellet of camptothecin and a preparation method thereof. First of all, the present invention provides a camptothecin nanoemulsion / pellet with colon-positioned drug release. The preparation of camptothecin into a nanoemulsion can improve the solubility of camptothecin, and further preparation into a concentrated nanoemulsion / pellet can be used to improve the solubility of camptothecin. The drug-loaded amount is doubled, and the drug-loaded nanoemulsion can be positioned and released in the colon. Camptothecin can be directly absorbed in the form of nanoemulsion, which avoids the problem of the opening of its lactone ring, and increases the solubility of camptothecin. It can smoothly cross the aqueous barrier on the surface of the colon and be taken up by colon cancer tissue, which enhances the curative effect and reduces the toxicity, and has great application value.
Owner:兰州市食品药品检验检测研究院 +1

Application of Chaofengcao Extract in the Preparation of Tumor Cell Multidrug Resistance Reversal Agent

The invention discloses an application of a cynanchum ascyrifolium extract in the preparation of tumor cell multidrug resistance reversal agents. The cynanchum ascyrifolium extract reverses the drug-resistant actions of human gastric tumor multidrug resistance cells, human colonic carcinoma multidrug resistance cells and human lung carcinoma multidrug resistance cells on clinical commonly used drugs such as taxol, adriamycin, 5-fluorouracil and cis-platinum. The cynanchum ascyrifolium extract disclosed by the invention is simple and convenient in preparation method, is combined with antitumor drugs to be applied to clinical application and has wide application prospects, and the curative effect of chemotherapy is improved.
Owner:QINGDAO UNIV

Product of Maillard reaction of tryptophan and glucose and its preparation method and application

ActiveCN102516234AOrganic active ingredientsOrganic chemistryMaillard reactionAdenoid cystic carcinoma
The invention discloses a product of the Maillard reaction of tryptophan and glucose and its preparation method and application. The invention also discloses a pharmaceutical composition for treating tumors. The pharmaceutical composition for treating tumors contains an effective dose of the product of the Maillard reaction of tryptophan and glucose and pharmaceutically acceptable carriers. A result of the research shows that the product of the Maillard reaction of tryptophan and glucose has strong cell targeted killing effects on a human cervical carcinoma cell line, a human colon cancer cell line, a human mucoepidermoid carcinoma cell line, an adenoid cystic carcinoma cell line, a lymphoma cell line, a breast cancer cell line and a lung cancer cell line, and does not produce apoptosis induction effects on common cells. The pharmaceutical composition which is utilized for treating tumors and is prepared from tryptophan has low toxicity, high efficiency and an important meaning in the filed of antitumor drug development.
Owner:HARBIN MEDICAL UNIVERSITY

Method and a Compound for Preventing Mammalian Cancer Cell Proliferation and for Treating Cancer

InactiveUS20210030673A1Prevent proliferationImproved suppression mammalian cancer cell proliferationPharmaceutical delivery mechanismEther/acetal active ingredientsProstate cancer cellBetulonic acid
A composition and a method for use in suppressing growth and / or proliferation of cancer cells in vivo and in vitro is provided. The composition includes an alcoholic lignan extract prepared from coniferous species optionally in combination with betulonic acid or betulinic acid. The composition inhibits growth and / or proliferation of at least prostate and melanoma cancer cells in vitro. Combination of the alcoholic lignan extract and betulonic or betulinic acid has a synergic effect specifically in inhibition of melanoma and prostate cancer cell proliferation and toxicity. Oral daily administration of the composition decreases or in some cases abolishes tumors of patients with breast cancer, brain cancer or colon cancer. The composition is suitable for use in cancer treatment in pet animals as well.
Owner:GRANULA

5-aryl nicotinamide LSD1/HDAC double-target inhibitor and preparation method and application thereof

The invention relates to a 5-aryl nicotinamide LSD1 / HDAC double-target inhibitor and a preparation method and application thereof in preparation of antitumor drugs, and belongs to the technical field of medicinal chemistry. The compound has the following general formula shown in the specification, wherein R1 is preferably OH, CH3 and H; and R2 is preferably OH, OCH3, F, CN, H and CH3. The compound has relatively strong inhibitory activity to LSD1 and HDAC1, and the IC50 of most compounds to HDAC1 is less than 10 nM, which is superior to that of a positive drug SAHA. The in-vitro anti-tumor activity IC50 of a plurality of compounds on a human colon cancer HCT-116 cell strain, a human gastric cancer MGC-803 cell strain and human leukemia THP-1, MOLT-4 and MV4: 11 cell strains is less than 1.0 mu M, and the in-vitro anti-tumor activity of the compound I-4 on THP-1 is 6 times that of SAHA. The compound provides a basis for research and development of LSD1 / HDAC double-target inhibitor drugs.
Owner:XINXIANG MEDICAL UNIV
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