1323 results about "Antitumor activity" patented technology

The invention relates to the field of natural products, in particular to a dimer compound of guaiane type sesquiterpenes and uric acid as well as an extraction and separation method and application of the dimer compound. According to the invention, a new dimer compound of guaiane type sesquiterpene and uric acid is extracted and separated from carpesium abrotanoides in Guizhou, and it is found that the dimer compound has relatively strong anti-tumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharynx cancer, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an optional scheme for broad-spectrum anti-cancer drugs. Moreover, in human prostate cancer cells PC3, human cervical cancer cells Hela, human liver cancer cells HepG2 and human glioma cells U87 which are resistant to paclitaxel, the compound also shows strong anti-cancer activity, which indicates that the compound has the potential of treating patients resistant to paclitaxel.

The invention discloses application of camellia nitidissima exosome-like nano-vesicles in preparation of antitumor drugs, and belongs to the technical field of biological medicines. The exosome-like nano-vesicles are extracted from golden camellia for the first time, and the exosome-like nano-vesicles are proved to have remarkable anti-tumor activity.

The invention discloses a compound with anti-tumor activity. The compound has a chemical structural formula as shown in a formula (I). The compound belongs to a novel tetracyclic triterpenoid natural product, has good fat solubility and chemical stability, and can be conveniently extracted from the rhizome of a herbal medicine Polygala fallax Hemsl. And prepared into an oral or injection form. The invention also provides a preparation method and application of the compound. The compound provided by the invention can obviously inhibit the growth of mouse lung cancer and reduce the volume and weight of tumor, and can be used for treating tumor diseases.

The invention discloses erianin PROTACs as well as a preparation method and application thereof, the structural formula of the erianin PROTACs is # imgabs0 #, E3 Ligand is pomalidomide, and Linker is an alkane chain or a PEG chain. The erianin PROTACs disclosed by the invention are superior to the prior art in the aspects of target protein degradation efficiency, anti-tumor activity, innovativeness, application prospect and the like, and show remarkable technical progress and practical value.

The invention provides a gamma delta T cell preparation as well as a preparation method and application thereof, and belongs to the technical field of T cells. The liposome is prepared from the following raw materials in parts by weight: 15-20 parts of modified gamma delta T cell liposome, 1-3 parts of cell stimulating factors and 4-7 parts of culture medium freeze-dried powder, the modified gamma delta T cell lipidosome is prepared by embedding gamma delta T cells through lipidosome, coupling with acetylenic bond modified chitosan, and further mixing with MFAP4 protein and b4GALT1 protein. The culture medium freeze-dried powder is prepared by freeze-drying the culture medium in the engineering culture process of gamma delta T cells, and the cell stimulating factors are resveratrol and quercitrin. According to the gamma delta T cell preparation prepared by the invention, the survival ability and resistance of gamma delta T cells are improved, the anti-tumor activity of the gamma delta T cells is improved, and the gamma delta T cell preparation has relatively good antioxidant and anti-inflammatory effects, reduces the inhibition of inflammation on an immune system and has a very good treatment effect on pancreatic ductal adenocarcinoma.

The invention provides an AS01 derivative adjuvant, a preparation method thereof and application of the AS01 derivative adjuvant in preparation of vaccines or anti-tumor drugs, and belongs to the technical field of biological drugs or products. The AS01 derivative adjuvant is prepared from the following components in parts by mass: 0.5 to 1.0 part of cholesterol, 2.0 to 4.0 parts of dioleoyl lecithin and at least one of the following components in parts by mass: 0.1 to 0.2 part of monophosphoryl lipid A, 0.1 to 0.2 part of QS-21, 0.36 to 0.72 part of 3M-052, 0.4 to 0.8 part of muramyl dipeptide and 0.2 to 0.4 part of oligodeoxynucleotide. According to the AS01 derived adjuvant, a novel synergistic adjuvant system is developed by integrating various immunomodulators, so that the immunogenicity of a vaccine is enhanced. The HPV vaccine is prepared on the basis of the AS01 derived adjuvant, so that the immunogenicity can be enhanced, and good anti-tumor activity can be achieved. Therefore, the invention provides a new strategy for immunotherapy of HPV-related tumors.

The invention discloses an enantiokaurane compound with antitumor activity as well as a preparation method and application of the enantiokaurane compound. According to the present invention, chemical components of Western African plant I.trichantha tubers are deeply studied, and a variety of chromatographic separation methods such as macroporous resin, silica gel resin, medium pressure preparation-MCI column, gel normal pressure column and semi-preparative high performance liquid chromatography are combined to separate to obtain one enantiokaurane new compound Trichanthone B; experiments show that the compound obtained through separation has a good inhibition effect on an MIA PaCa-2 pancreatic cancer cell line and an A549 lung cancer cell line, and IC50 of the compound on the MIA PaCa-2 pancreatic cancer cell line reaches a nanomole level; the effect of the compound is stronger than that of positive drugs 5-fluorouracil and carboplatin, and the compound has the potential of being developed into new drugs for resisting pancreatic cancer and lung cancer.

The invention relates to a turtle-derived cyclic peptide compound with an anti-tumor effect and a preparation method thereof. The preparation method comprises the following steps: crushing tortoise plastron, adding water for reflux extraction, filtering, concentrating and drying to obtain tortoise-shell glue; dissolving the obtained tortoise-shell gelatin in water, adding protease for enzymolysis, and centrifuging after enzyme deactivation to take supernate; carrying out graded filtration on the obtained supernate and collecting components; and separating and purifying the collected components to obtain the cyclic peptide. The obtained compound has remarkable anti-tumor activity and has a good application prospect in preparation of anti-tumor drugs.

The invention discloses an anti-tumor medicine composition combined with a PARG inhibitor and application. Through natural product library screening and CCK-8 experiments, it is found that PARG knockout gastric cancer cells show significantly enhanced sensitivity to ginsenoside CK. Further clone formation experimental analysis shows that PARG knockout significantly enhances the inhibitory effect of ginsenoside CK on gastric cancer cell proliferation. In in-vivo experiments, a CDX model is utilized to verify that PARG knockout can significantly enhance the anti-tumor activity of ginsenoside CK on gastric cancer. The discovery provides an important experimental basis for clinical application of PARG as a gastric cancer treatment target and ginsenoside CK as a potential treatment drug. The research finds that the PARG inhibitor and ginsenoside CK are combined to achieve a better killing effect on other various cancer cells, and it is indicated that improvement of the effect is broad-spectrum.

The invention discloses poplar and phellinus igniarius polysaccharide SVP-1 as well as a preparation method and application thereof, and belongs to the field of biological medicines. The poplar phellinus igniarius polysaccharide SVP-1 provided by the invention has remarkable anti-tumor activity, and can effectively inhibit proliferation, invasion and migration of tumor cells so as to block malignant progression of tumors. The structure is clear, the preparation method is controllable, the stability and biological activity of polysaccharide components are ensured, and a reliable basis is provided for development of antitumor drugs. When the traditional Chinese medicine composition is used together with radiotherapy and chemotherapy medicines, a synergistic effect can be achieved, the sensitivity of tumors to treatment can be improved, the toxic and side effects of radiotherapy and chemotherapy can be relieved, and the effects of reducing toxicity and increasing efficiency are achieved. According to the combined treatment strategy, the curative effect of the existing tumor therapy can be remarkably improved, meanwhile, adverse reactions are reduced, and a new optimization scheme is provided for clinical tumor treatment.

The present invention relates to a hetero (aromatic) ring-substituted cyclic diamine compound, the preparation thereof and the use thereof in the preparation of a drug for treating and / or preventing tumors. The structural formula of the compound is as shown in (I). The compound has a significant inhibitory effect on the growth of cells of tumors such as leukemia, lymphoma, breast cancer, melanoma, ovarian cancer, colorectal cancer, cervical cancer, lung cancer, prostate cancer, esophageal cancer, glioma, kidney cancer, nasopharyngeal carcinoma, liver cancer, gastric cancer and pancreatic cancer. Compared with the prior art, the compound of the present invention has a broad-spectrum anti-tumor activity, has a good effect on inhibiting tumors, and has an effect of degrading PD-L1 proteins, and is thus a PD-L1 immunomodulator.

The invention belongs to the field of biological medicine, and relates to an anti-EGFR monoclonal antibody, a bispecific antibody thereof, a pharmaceutical composition and application. Specifically, the invention relates to an anti-EGFR antibody or an antigen binding fragment thereof. The invention also relates to an anti-EGFR (Epidermal Growth Factor Receptor) and anti-MET (Methyl The anti-EGFR monoclonal antibody and the bispecific antibody provided by the invention both have good anti-tumor activity.

The invention provides a pyrrolidone dihydroisoxazole compound as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis. Specifically, under the catalytic action of Lewis base, beta-oxoacrylamide and 4-nitroisoxazole serve as raw materials, and the pyrrolidone dihydroisoxazole compound is synthesized through a one-step method. Beta-oxoacrylamide and 4-nitroisoxazole which are simple and easy to obtain are adopted as starting raw materials, dearomatization [3 + 2]-cycloaddition reaction is carried out under the catalysis of Lewis base, the pyrrolidone dihydroisoxazole compound is synthesized, the method is easy and convenient to operate and mild in reaction condition, the used reagents and raw materials are economical and easy to obtain, and the method is suitable for industrial production. The target product yield is high, the substrate application range is wide, and the in-vitro anti-tumor activity is good.

The invention belongs to the field of chemical medicines, and particularly relates to a combined medicine for preventing and / or treating prostatic cancer, application of the combined medicine and a medicine composition. The combined medicine disclosed by the invention comprises immune cells with enhanced infiltration degree and a galectin-1 inhibitor; the immune cells with enhanced infiltration degree are natural killer (NK) cells with TTTY15-USP9Y chimera RNA knocked out, the infiltration degree and anti-tumor activity of the NK cells in a prostate cancer microenvironment can be improved, and the activated NK cells have a stronger killing effect on tumor cells in vitro. The immune cells with enhanced infiltration degree and the galectin-1 inhibitor are combined for use, so that the composition shows a synergistic effect in treatment of prostatic cancer, and has a wide application prospect.

The invention provides lucid ganoderma oligopeptide with an anti-tumor effect and a preparation method thereof. The three oligopeptides are separated and purified from the ganoderma lucidum for the first time, and the oligopeptides have broad-spectrum anti-tumor activity, can effectively inhibit tumor cell proliferation, have good biological compatibility and have great application prospects.

The invention discloses an engineered NK cell and a preparation method thereof. The antitumor activity of the NK cell is enhanced through synergistic modification of a fusion polypeptide and an anti-TIGIT monoclonal antibody. The amino acid sequence of the fusion polypeptide is shown as SEQ ID NO.1. The fusion polypeptide can specifically target tumor cells and activate the proliferation and killing functions of NK cells. And the anti-TIGIT monoclonal antibody further relieves the immunosuppression by blocking a TIGIT-CD155 signal channel. In-vitro experiments show that the killing rate of the combined modified NK cell on various solid tumors is obviously higher than that of the traditional CAR-NK cell. A PDX model shows that the engineered NK cells significantly inhibit tumor growth and enhance NK cell infiltration in a tumor microenvironment. The invention provides a new strategy with high efficiency and low toxicity for immunotherapy of solid tumors.

The invention discloses a preparation method and application of roasted barley and malt polysaccharide with an anti-cancer effect. The roasted barley malt polysaccharide is a neutral heteropolysaccharide which mainly takes-> 3)-beta-D-Glcp-(1-> and->-beta-D-Glcp-(1->) as main chains, branches exist at O-3 / O-4 positions, and the branch chains are mainly composed of-> 4)-beta-D-Xylp-(1->,-> 3, 4)-beta-D-Xylp-(1-> and alpha-D-Glcp-(1->. The monosaccharide composition comprises arabinose, glucose and xylose in a molar mass ratio of 1.86: 33.43: 1.00, and the molecular weight is 23.81 kDa. In-vitro activity experiments prove that the roasted barley malt polysaccharide disclosed by the invention has a remarkable inhibition effect on proliferation of liver cancer cells, lung cancer cells, breast cancer cells and colorectal cancer cells, particularly on the liver cancer cells, and shows outstanding anti-tumor activity, so that the roasted barley malt polysaccharide is expected to be developed and applied in the fields of foods, health-care products or medicines.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dammarane sapogenin-isatin derivative and application thereof in anti-tumor treatment. The dammarane sapogenin-isatin conjugate is constructed by taking dammarane sapogenin as a mother nucleus, deriving the dammarane sapogenin and chloroacetic acid and then introducing an indolone structural unit, and R1, R2 and R3 are as described in the claims and the specification. According to the invention, isatin fragments and ginsenoside are coupled for the first time, the anti-tumor activity of the compounds is systematically evaluated, and the action mechanism research of the compounds in colorectal cancer and other tumors is further developed. Results show that the obtained compound has relatively good anti-tumor efficacy, tumor cell selectivity, relatively low toxicity and relatively high bioavailability, and shows good patent medicine potential and wide market prospects.

The invention provides a new anti-tumor ganoderma lucidum variety, a related product as well as a preparation method and application of the new anti-tumor ganoderma lucidum variety, and belongs to the field of new ganoderma lucidum varieties. The new variety of ganoderma lucidum provided by the invention is classified and named as Ganoderma sichuanense Xianzhi No.13, and is preserved in the China Center for Type Culture Collection (CCTCC) on October 25, 2024, and the preservation number is CCTCC NO: M 20242347. Compared with the existing ganoderma lucidum variety, the new ganoderma lucidum variety provided by the invention has higher yield and higher content of effective components and anti-cancer active components, and the extract of the ganoderma lucidum has good anti-tumor activity.

The invention relates to the technical field of antitumor drugs, in particular to a Ru (II) complex and a preparation method and application thereof, and the Ru (II) complex has a structure as shown in a formula I. The Ru (II) complex synthesized by the method disclosed by the invention not only has relatively high cytotoxicity, but also has good photodynamic antitumor activity. After the complex is illuminated, the efficiency of the complex entering cells in an active transportation mode can be accelerated, mitochondria and endoplasmic reticulum are targeted at the same time, mitochondrial membrane potential decline and endoplasmic reticulum stress are caused to form a dual organelle damage effect, immunogenic cell death is caused, the tumor microenvironment is adjusted, and the tumor cell immunogenicity is improved. The enrichment of dendritic cells (DCs) in tumor cells is realized, the chemotactic activity of effector T cells is improved, the proportion of CD4 < + > and Foxp3 < + > cell populations is reduced, and finally the anti-tumor immune response is activated. Meanwhile, the complex provided by the invention can also induce the cell to generate pan apoptosis, retard the cell cycle in the G2 / M period and enhance the effect of the complex in inhibiting tumor proliferation.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 2-aminopyrimidine compound, application thereof and an antitumor drug. The 2-aminopyrimidine compound provided by the invention has a structure as shown in a formula (I). According to the invention, 2-aminopyrimidine is used as a mother nucleus structure, and a series of 2-aminopyrimidine compounds are successfully constructed by accurately introducing a biologically active imidazole, thiazole or oxazole nitrogen-containing heterocyclic ring fragment at the 5 # site of 2-aminopyrimidine; systematic in-vitro anti-tumor activity evaluation proves that the 2-aminopyrimidine compound with the structure as shown in the formula (I) provided by the invention shows remarkable inhibitory activity on various tumor cell lines, and the activity of part of the compound is even superior to that of a clinical control drug. The structural diversity of 2-aminopyrimidine compounds is enriched, valuable lead compounds are provided for developing novel efficient antitumor drugs, and the 2-aminopyrimidine compounds have important scientific significance and clinical transformation potential. # imgabs0 #

The invention discloses an artemisinin derivative nano assembly with anti-tumor activity and a preparation method and application thereof. The nano assembly is formed by self-assembling artemisinin derivatives through intermolecular force and modifying the artemisinin derivatives with a PEG modifier; the artemisinin derivative is artesunate or dihydroartemisinin of which the side chain is binary acid or saturated fatty alcohol or unsaturated fatty alcohol; the mass ratio of the artemisinin derivative to the PEG modifier is (10: 90)-(90: 10), so that the technical effects of high drug loading capacity, good stability, low toxic and side effects and the like are realized, the urgent demand on high-efficiency and low-toxicity preparations in clinic is met, a new strategy is provided for the assembly of homotype synergistic drug nanoparticles, and the application prospect is broad. An effective nano platform is provided for developing a carrier-free nano assembly and a high-efficiency and low-toxicity nano preparation.

The invention relates to a hydroxamic acid derivative of benzimidazole as well as a preparation method and application of the hydroxamic acid derivative. Specifically disclosed are a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a stereoisomer thereof. The hydroxamic acid derivative of benzimidazole is novel in structure, has good inhibitory activity on HDAC and / or PARP, and further shows good anti-tumor activity.

The invention discloses an exosome engineered targeted drug delivery system and a preparation method and application thereof, and belongs to the field of biomedices.The exosome engineered targeted drug delivery system is prepared by mixing and reacting surface modified exosome and pH response type drug controlled release nanoparticles; the pH response type drug controlled release nanoparticles react with the surface modified exosome through a click chemical reaction; the surface of the membrane of which the surface is modified with the exosome is modified with a maleimide group and an azide group; the novel nano-drug has pH responsiveness; the click chemical reaction is thiol-ene click reaction. Bifunctional groups (MAL and N3) are directionally grafted on the surface of an exosome membrane, uniform drug particles are prepared in combination with a micro-fluidic technology, an efficient bimodal targeting drug delivery system is successfully constructed, and remarkable technical advantages are shown in the aspects of improving targeting precision, enhancing antitumor activity, controlling drug release, inhibiting tumor metastasis and the like; and a new technical approach is provided for precise treatment of adenoid cystic carcinoma.

The invention discloses a benzoyl phenylurea selenium analogue, a preparation method and application thereof, and a pharmaceutical composition containing the benzoyl phenylurea selenium analogue, and belongs to the technical field of chemical synthesis and medicines. The benzoyl phenylurea selenium analogue has a remarkable inhibition effect on tubulin polymerization, has remarkable anti-tumor activity and has high application value in the cancer treatment process, raw materials for preparing the benzoyl phenylurea selenium analogue are easy to obtain, preparation conditions are mild, and the preparation method is simple and convenient.

The invention relates to an STING gene knockout TIL capable of enhancing anti-tumor activity and a preparation method and application of the TIL, in particular to a genetically engineered immune cell, and an STING gene in the genetically engineered immune cell is silenced or down-regulated. The ferroptosis resistance of the immune cell provided by the invention is remarkably enhanced, the immune cell can be better infiltrated into a tumor microenvironment, and the immune cell has a remarkable anti-tumor effect.

The present invention relates to a polypeptide-drug conjugate that binds to IL4Ra and a use thereof, and provides: a polypeptide comprising a ligand that specifically binds to IL4Ra and a temperature-responsive disordered domain; and a polypeptide-drug conjugate in which a cytotoxic drug is bound to the polypeptide. More specifically, the polypeptide, in which an IL4RA-binding ligand and a temperature-responsive disordered domain are repetitively linked, exhibits high selectivity in binding to IL4Ra, and the polypeptide-drug conjugate, in which a cytotoxic drug is bound to the polypeptide, demonstrates significantly enhanced cancer cell-killing efficacy and anti-tumor activity compared to unbound drugs or conventional anticancer agents, and has been confirmed to suppress drug resistance in cancer cells that are resistant to the anticancer agent temozolomide. Accordingly, the polypeptide-drug conjugate can be provided as an effective anticancer therapeutic agent for the treatment of tumors overexpressing IL4Ra and as a pharmaceutical composition for inhibiting drug resistance in cancer cells exhibiting resistance to anticancer drugs.

The invention relates to the field of biological medicine, and discloses application of a GADD34 inhibitor in preparation of a medicine for enhancing CAR-T cell tumor treatment. The invention provides an innovative strategy for inhibiting CAR-T cell depletion through targeted regulation and control of an endoplasmic reticulum stress pathway to solve the problems that in an existing CAR-T therapy, the anti-tumor activity is reduced, and the solid tumor treatment effect is insufficient due to T cell depletion. Researches find that an IRE1-XBP1 pathway is used as a core signal axis of endoplasmic reticulum stress, and excessive activation of the IRE1-XBP1 pathway can drive CAR-T cell depletion related phenotypes (such as PD-1 / LAG-3 up regulation and cytokine secretion reduction). Screening experiments show that inhibiting the upstream regulatory factor GADD34 of the IRE1 not only can effectively reduce the IRE1-XBP1 signal intensity, but also can cooperatively relieve the endoplasmic reticulum stress pressure by regulating protein translation recovery, so that the CAR-T cell steady state is more comprehensively maintained. Therefore, the GADD34 inhibitor can provide a new way for enhancing CAR-T cell tumor treatment.

The invention discloses a carbamoyl-substituted diarylethene derivative as well as a preparation method and application thereof, and the preparation method comprises the following steps: reacting R-substituted 3-bromo-2-hydroxybenzaldehyde with an arylmethyl triphenylphosphonium bromide compound or an aryl acetic acid compound to obtain an intermediate A; then the intermediate A and cuprous cyanide are subjected to a heating reaction in N, N-dimethylformamide and nitrogen atmosphere, and an intermediate B is obtained; and finally, heating the intermediate B, acetaldoxime and indium trichloride in toluene for reaction to obtain the carbamoyl-substituted diarylethene derivative. The carbamoyl-substituted diarylethene derivative disclosed by the invention has a remarkable effect in an in-vitro anti-tumor activity test, particularly has excellent anti-proliferation ability to human BRCA mutant tumor cells, and can be used for preparing medicines for treating PARP-1 activity abnormity related diseases. The synthesis route is simple, the cost is low, and large-scale implementation is facilitated.

The invention belongs to the technical field of biology, and discloses a bioactive peptide which is a micromolecular anti-tumor bioactive peptide derived from sea cucumber, and the amino acid sequence of the bioactive peptide is FNPDTFD. Sephadex G-15 gel chromatography and mass spectrometry technologies are used for separating, purifying and structurally identifying the sea cucumber flower enzymolysis peptide, so that the small molecule peptide with a potential anti-tumor effect is obtained. A cell viability experiment verifies that the small molecule peptide can selectively inhibit the proliferation of EGFR mutant non-small cell lung cancer cells. Besides, molecular docking and protein immunoblotting results show that the peptide can be combined with EGFR mutant protein, and the activation of a downstream Akt / mTOR signal channel is inhibited by targeting the EGFR mutant protein, so that the biological activity of resisting the non-small cell lung cancer is exerted. The bioactive peptide not only has the potential of being developed into a new generation of EGFR targeting antitumor drugs, but also has wide application prospects in the field of functional health food. The preparation process is simple, and is suitable for industrial production and market popularization and application.