35results about How to "High anticancer activity" patented technology

The preparation method comprises the following steps: degreasing polygonatum cyrtonema leaf superfine powder, sequentially carrying out ultrasonic-assisted enzymolysis treatment on cellulase, xylanase, high-temperature-resistant alpha-amylase, papain and saccharifying enzyme, and carrying out alcohol precipitation, dialysis and vacuum freeze drying treatment to obtain the polygonatum cyrtonema leaf polysaccharide. The polygonatum cyrtonema leaf enzyme extraction crude polysaccharide is obtained; and separating the enzyme-extracted crude polysaccharide through a cellulose column, and purifying through a sephadex column to obtain the polygonatum cyrtonema leaf enzyme-extracted polysaccharide. Polysaccharide in polygonatum cyrtonema leaves is extracted through ultrasonic-assisted compound enzyme, single pure polysaccharide is obtained through alcohol precipitation, dialysis, cellulose column chromatography and gel column chromatography, and the purity can reach 99.86%; the obtained enzyme extraction polysaccharide has good anti-cancer activity, can significantly inhibit proliferation of breast cancer cells and colorectal cancer cells, has the characteristics of good biocompatibility, strong specificity, low toxic and side effects and the like, and has wide application prospects.

The present invention relates to a curcumin 2-chloroadenine derivative compound or a stereoisomer, a deuterated substance, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a cocrystal thereof.

The invention belongs to the technical field of drug carriers, and particularly discloses a preparation method and application of a closed-loop feedback-regulation nano drug delivery system.The preparation method comprises the following steps that a starting material containing a reversible molecular library is provided, and the reversible molecular library is prepared in a buffer salt system; under thermodynamic control, adding anti-cancer drug molecules and guest molecules into the starting material; through a reversible covalent reaction process, molecules in an initial material spontaneously form a self-assembled nano-carrier containing drug molecules under the combined action of the drug molecules and guest molecules. According to the preparation method and application of the closed-loop feedback-regulation nano drug delivery system, reversible covalent reaction, closed-loop feedback-regulation and self-assembly technologies are combined, spontaneous construction of a nano carrier is achieved, and the nano carrier is endowed with excellent drug loading capacity, stability and environmental responsiveness.

The invention provides a tumor targeted nano drug delivery system and a preparation method and application thereof, the tumor targeted nano drug delivery system comprises a PD-L1 monoclonal antibody, radix pseudostellariae cyclic peptide B and an mPEG-PLGA-NH2 nano carrier, the radix pseudostellariae cyclic peptide B is encapsulated in the mPEG-PLGA-NH2 nano carrier, and the outer surface of the mPEG-PLGA-NH2 nano carrier is modified with the PD-L1 monoclonal antibody. The tumor-targeted nano drug delivery system has good anti-cancer activity and biocompatibility, has longer circulation time and higher bioavailability, is obviously superior to free drugs in the aspects of tumor resistance and immunoregulation, and is expected to be applied to preparation of tumor-targeted drugs, especially gastric cancer-targeted drugs.

The invention discloses a bispecific antibody targeting CD3 and PD-L1 and an application of the bispecific antibody. The bispecific antibody comprises a first antigen binding region, a second antigen binding region and an Fc part, the Fc part comprises a first Fc peptide fragment and a second Fc peptide fragment; the first antigen binding region comprises an scFv fragment and a binding protein of a first molecule or a fragment thereof, the binding protein of the first molecule or the fragment thereof is connected with the N end of the scFv fragment, and the C end of the scFv fragment is connected with the N end of the first Fc peptide fragment; the second antigen binding region comprises a binding protein of a second molecule or a fragment thereof, and the binding protein of the second molecule or the fragment thereof is connected with the N end of the second Fc peptide fragment; the first molecule and the second molecule are PD-L1, and the scFv fragment has CD3 binding activity. The bispecific antibody disclosed by the invention is good in safety, high in anti-cancer activity and high in clinical application and drug development value.

The invention provides an application of ginkgetin in enhancing VS4718 or ponatinib in resisting the progress of esophageal squamous cell carcinoma. It is found that ginkgo biflavone can enhance the growth and invasion inhibition effect of VS4718 or ponatinib on esophageal squamous carcinoma cells; ginkgo biflavone is used for enhancing the inhibition effect of VS4718 or ponatinib on glycolipid metabolism of tumor cells, and the ginkgo biflavone is respectively combined with VS4718 or ponatinib to generate a synergistic anti-cancer effect.

The invention discloses a preparation method and application of a tris (2-methyl-2-phenylpropyl) stann-3, 5-dichlorosalicylate complex, and the tris (2-methyl-2-phenylpropyl) stann-3, 5-dichlorosalicylate complex is a complex # imgabs0 # with the following structural formula (I). The invention also discloses a preparation method of the tris (2-methyl-2-phenylpropyl) stann-3, 5-dichlorosalicylate complex and an application of the tris (2-methyl-2-phenylpropyl) stann-3, 5-dichlorosalicylate complex in preparation of antitumor drugs.

The invention discloses a 12-nitrogen substituted matrine ester derivative, a preparation method and an application thereof, and relates to the technical field of development and application of natural product derivatives of medicinal chemistry. Aiming at the disadvantages of the natural product matrine, such as low bioavailability, poor activity and large dosage, which limit its wide application, the invention hydrolyzes matrine and prepares matrine ester, and then replaces and transforms the 12-nitrogen substituted matrine ester derivatives to prepare a series of 12-nitrogen substituted matrine ester derivatives. Anti-tumor activity experiments show that the derivatives have good anti-cancer activity, and in particular have good inhibitory function on liver cancer and lung cancer cells.

The invention relates to tripterine-luteolin-based self-assembled nanoparticles as well as a preparation method and application thereof, and belongs to the field of biological medicines. Compared with single tripterine, the tripterygium wilfordii derivative nano-particles provided by the invention have a stronger inhibition effect on tumor cells and lower toxicity, and have a good application prospect in the development of antitumor drugs.

The present invention discloses a metal complex tailed with a TDO inhibitor, and its preparation method and application. The preparation method of the metal complex tailed with a TDO inhibitor of the present invention is specifically as follows: in a light-proof and inert gas environment, a metal dimer precursor and a dechlorinating agent are added to anhydrous methanol, refluxed and stirred at 60°C for 0.2 to 72 hours, and filtered after the reaction; an immune checkpoint TDO inhibitor ligand is added to the filtrate, and the reaction is carried out in an anaerobic environment. After the reaction is complete, an anion salt is added thereto, the solution is filtered and concentrated, and then frozen. After freezing, centrifugation is performed to obtain a crude product, which is purified by column chromatography to obtain a metal complex. The aryl / cyclopentadienyl metal complex of the present invention can be well positioned in the nucleus of cancer cells, induce cell necrosis, lead to immunogenic cell death, and inhibit the expression of immune checkpoint TDO, thereby achieving good anticancer activity, ICD induction activity and immune checkpoint TDO inhibition activity.

The invention relates to a novel CRS fragment peptide with immunological enhancement activity and application of the novel CRS fragment peptide. More specifically, the present invention relates to a novel peptide consisting of the amino acid sequence of SEQ ID NO: 2 or an amino acid sequence having 95% or higher sequence homology thereto and a vaccine adjuvant, their use as a cancer therapeutic agent and an antiviral composition. The peptides disclosed herein are CRS fragment peptides disclosed herein for the first time, exhibiting anticancer activity, immunological enhancement and antiviral activity.

The invention discloses a preparation method and application of a bis [tri (2-methyl-2-phenylpropyl) tin] 5-sulfosalicylate complex. The bis [tri (2-methyl-2-phenylpropyl) tin] 5-sulfosalicylate complex is a complex # imgabs0 # with the following structural formula (I). The invention further discloses a preparation method of the bis [tri (2-methyl-2-phenylpropyl) tin] 5-sulfosalicylate complex and application of the bis [tri (2-methyl-2-phenylpropyl) tin] 5-sulfosalicylate complex in preparation of antitumor drugs.

The invention discloses a preparation method and application of a bis (tricyclohexyltin) 5-sulfosalicylate complex. The bis (tricyclohexyltin) 5-sulfosalicylate complex is a complex # imgabs0 # with a structural formula (I) as shown in the specification. The invention also discloses a preparation method of the bis (tricyclohexyltin) 5-sulfosalicylate complex and application of the bis (tricyclohexyltin) 5-sulfosalicylate complex in preparation of antitumor drugs.

The invention discloses a preparation method and application of a tricyclohexyltin 2-hydroxy-3-naphthoic acid ester complex. The tricyclohexyltin 2-hydroxy-3-naphthoic acid ester complex is a complex # imgabs0 # with the following structural formula (I). The invention further discloses a preparation method of the tricyclohexyltin 2-hydroxy-3-naphthoic acid ester complex and application of the tricyclohexyltin 2-hydroxy-3-naphthoic acid ester complex in preparation of antitumor drugs.

The present invention relates to a cytohormone fusion protein comprising a cytohormone domain that can specifically induce an immune cell targeting domain and proliferation and / or activation of immune cells. Specifically, the present invention relates to a fusion protein that specifically delivers a cytohormone (e.g., IL-2 or IL-15) to a depleted immune cell (e.g., a depleted T cell) within a tumor, thereby inducing and enhancing the activation of the immune cell. The fusion protein according to the present invention can selectively deliver a cytohormone that promotes the proliferation or activation of immune cells to effector T cells or the like in a tumor microenvironment, thereby inducing a strong immune enhancement and anti-cancer response in a tumor. Moreover, through the unique structure of the cytohormone action domain, systemic toxicity and even side effects caused by the cytohormone can be obviously reduced.

The invention belongs to the field of electrochemistry and green synthesis, and particularly relates to a preparation method and application of quinoxalinone substituted by cyanoalkyl at the C3 position. The preparation method comprises the following steps: by taking quinoxalinone and acrylonitrile as reaction raw materials, adding an electrolyte, an organic solvent and an additive, and carrying out electrolytic reaction to obtain the C3-position cyanoalkyl substituted quinoxalinone. The method for electrolytically synthesizing the C3-position cyanoalkyl substituted quinoxalinone is reported for the first time, acrylonitrile which is low in price and easy to obtain serves as an alkyl source, pre-activation of a substrate is not needed, operation is easy, cost is low, the atom utilization rate is high, participation of a chemical redox reagent is not needed, the reaction temperature is room temperature, and the method is suitable for industrial production. The C3-position cyanoalkyl substituted quinoxalinone can be efficiently and greenly synthesized; the quinoxalinone substituted by cyanoalkyl at the C3 position has good anti-cancer activity, can be used for preparing anti-cancer drugs, and has important application value.

The invention relates to a polysaccharide-assisted tea extract as well as a preparation method and application thereof. Fresh tea leaves are soaked with an aloe polysaccharide solution, tea leaves obtained through filtration are dried in the sun to obtain dry tea leaves, then the dry tea leaves are soaked with filtrate obtained through filtration again and then filtered, the tea leaves are subjected to pure water soaking and high-temperature and high-pressure treatment to obtain tea leaf liquid, and the tea leaf liquid is subjected to concentration, pure water hydrolysis and high-temperature and high-pressure treatment to obtain hydrolyzed tea leaf liquid. And mixing the filtrate obtained by filtering the hydrolyzed tea liquid with the filtrate obtained in the previous step, filtering, concentrating and drying. The ethanol aqueous solution can dissolve soluble substances of the aloe polysaccharide, and insoluble impurities are removed in the subsequent filtering step. According to the method, effective substances of the tea leaves are extracted under the assistance of the polysaccharide, the EGCG content in the tea leaves can be greatly increased, and the anticancer activity of the tea extract is improved through the synergistic effect of the aloe polysaccharide and active substances in the tea extract.

The application belongs to the technical fields of medicinal chemistry and antitumor drugs, and discloses a polypeptide with anticancer activity, a preparation method and application thereof. The polypeptide is a Bathiapeptide F analogue containing a thiazole or dithiazole skeleton, and the molecular structure of the polypeptide contains independently changeable amino acid residue or peptide residue substituents. The application designs and synthesizes a new polypeptide analogue containing a thiazole or dithiazole skeleton by taking Bathiapeptide F as a parent structure. The preparation method includes the steps of amination reaction, sulfuration reaction, thiazole ring formation reaction, amide condensation reaction, ester hydrolysis, and removal of an amino protecting group. Experimental results show that the polypeptide has obvious inhibitory effect on Huh7 liver cancer cells, MDA-MB-231 breast cancer cells and A375 melanoma cells, and can be used for preparing anticancer drugs, and has good drug development prospects.

The present invention relates to a novel compound, a pharmaceutical composition for preventing or treating resistant cancer comprising the novel compound or a pharmaceutically acceptable salt thereof, and use thereof. When the composition of the present invention is administered together with an anticancer agent, it can exhibit an excellent anticancer effect.

The invention discloses a semi-sandwich structure iridium ferrocene pyridine complex, a preparation method thereof and an anti-cancer application thereof. Its structural formula is shown in formula (I), R is methyl, phenyl or biphenyl, and the double bond is in cis and trans configurations. By testing the growth inhibition rate of the target complex on human alveolar basal epithelial cancer cells, cervical cancer cells and normal human lung epithelial cells, and comparing them, it is found that the target complex exhibits good anti-cancer activity, confirming the synergistic anti-cancer effect of ferrocene and metal iridium complexes. The substituent R is changed from methyl→phenyl→biphenyl, and the activity of the complex is effectively improved, confirming that improving the electron donation ability of the ligand is conducive to improving the anti-cancer activity of such complexes. In addition, the trans-configuration complex also shows higher activity. The target complex can accumulate in the lysosome in A549 cells and cause lysosome damage, thereby causing cancer cell death. The complex shows a certain selectivity between normal cells and cancer cells.

The application discloses a preparation method of diterpenoid compounds and application thereof. Ten diterpenoid compounds are separated from Euphorbia fischeriana, including six kinds of atisine type diterpenoid compounds, two kinds of gansuine type diterpenoid compounds, one kind of taxodine type diterpenoid compound and one kind of sequirine type diterpenoid compound. The diterpenoid compounds have the effect of promoting apoptosis of SW1990 pancreatic cancer cells, wherein the anticancer activity of compounds 1, 3 and 9 is better than that of positive drug paclitaxel, and the compounds can be used as leading compounds of anti-pancreatic cancer drugs, and also provide a basis and a new idea for extraction and medicinal research of the diterpenoid compounds.

This invention belongs to the field of pharmaceutical technology, specifically relating to a tetravalent platinum complex based on cinnamic acid, its preparation method, and its application. This invention is the first to introduce a cinnamic acid group into the structure of a tetravalent platinum complex, designing and synthesizing a series of novel platinum-based anticancer prodrugs, namely cinnamic acid-platinum (IV) complexes. Biological evaluation shows that these complexes exhibit stronger anticancer activity than classic divalent platinum drugs and good selectivity for cancer cells, demonstrating the potential of highly effective, low-toxicity, and drug-resistant novel anticancer drugs.

The invention discloses a preparation method and application of a tricyclohexyltin 1-hydroxy-2-naphthoic acid ester complex. The tricyclohexyltin 1-hydroxy-2-naphthoic acid ester complex is a complex # imgabs0 # with the following structural formula (I). The invention further discloses a preparation method of the tricyclohexyltin 1-hydroxy-2-naphthoic acid ester complex and application of the tricyclohexyltin 1-hydroxy-2-naphthoic acid ester complex in preparation of antitumor drugs.

The present invention discloses a compound with anti-tumor activity, which has the following structural formula: The present invention also provides a method for preparing a compound with anti-tumor activity, wherein the carboxyl group on the first amino acid at the C-terminus of the CS-piscidin polypeptide is connected to the amino group of the side chain of the Cyclo-RGDfk polypeptide to obtain the CS-RGD polypeptide; the amino group on the first amino acid at the N-terminus of the CS-RGD polypeptide is connected to the carboxyl group on myristic acid to obtain the Myr-CS polypeptide. The present invention also provides the use of a compound with anti-tumor activity in the preparation of an anti-tumor drug. The Myr-CS polypeptide of the present invention has stronger targeting to cancer cells such as leukemia cells and ovarian cancer cells, exhibits good anti-tumor effects, has low toxicity to normal cells, and has higher drug safety.

This invention belongs to the field of pharmaceutical research technology, specifically relating to a marine cyclic peptide, its synthesis method, and its uses. The structural formula of the marine cyclic peptide is shown in Formula I. Compared with natural Galaxamide, the Galaxamide analog containing D-leucine provided by this invention exhibits a greater inhibitory effect on human cancer cells, and the more D-leucines introduced, the stronger the anticancer activity. Simultaneously, by replacing one of the L-leucines in Galaxamide with other amino acids, the synthesized Galaxamide derivative is more effective than natural Galaxamide and has the potential to inhibit the proliferation of human cancer cell lines HepG2, U87, and MCF-7.

The present invention relates to an anti-tumor adenovirus and an anti-cancer composition comprising the same. The double-stranded small interfering ribonucleic acid (siRNA) of the present invention promotes the killing of cancer cells by simultaneously inhibiting the expression of a first nucleic acid and a second nucleic acid, and has an anti-cancer activity that is significantly better than treating individual small interfering ribonucleic acids (siRNA) together, and has the effect of synergistically improving the cancer cell killing efficacy during the combined treatment with an anti-cancer agent. The adenovirus comprising an expression cassette encoding a short hairpin ribonucleic acid (shRNA) for expressing an anti-tumor adenovirus and a human telomerase reverse transcriptase (hTERT) promoter has the effect of avoiding the immune response in the body to specifically deliver to cancer cells and achieve systemic treatment, can achieve local delivery, has excellent selectivity, and can present a significant anti-cancer effect through minimally invasive treatment, and can be effectively used as an anti-cancer composition or anti-cancer adjuvant for various cancers.

The present invention provides a rhein-piperazine-furanone hybrid and a preparation method and application thereof, and relates to the technical field of rhein pharmaceutical chemistry. The present invention first prepares compound 4, and then reacts with an acyl chloride intermediate 3 of rhein 1 or diacerein 2. N The rhein-piperazine-furanone hybrid 5 is obtained by the acylation reaction, the synthesis route is simple, the by-products are few, the product separation and purification operation is simple, and the reaction yield is above 48%. The rhein-piperazine-furanone hybrid 5 prepared by the present invention has strong toxicity to various cancer cells and low toxicity to normal cells, and has excellent anticancer activity and selectivity.

The present invention discloses a lonidamine-modified organic compound, and also discloses a cyclometallic complex based on the organic compound, and a preparation method and application thereof. The organic compound of the present invention is obtained by chemically modifying the carboxylic acid group of lonidamine, and has good anti-tumor, antibacterial and anti-inflammatory activities. The cyclometallic complex obtained based on the organic compound can solve the problems of poor lipid solubility and large dosage of lonidamine when it is used as an anti-tumor drug or an anti-tumor drug component, and can also solve the problems of cisplatin tolerance and adverse side effects produced by tumor cells when the simple cyclometallic complex is used as an anti-tumor drug or an anti-tumor drug component. In addition, the cyclometallic complex of the present invention can also be used as a glycolysis inhibitor or an energy metabolism inhibitor to stimulate immune function.

The invention relates to a series of 2, 4-diarylaminopyrimidine analogues and a preparation method and application thereof, belongs to the technical field of medicines, and relates to a series of 2, 4-diarylaminopyrimidine analogues and preparation and application thereof, the series of 2, 4-diarylaminopyrimidine analogues have a structure as shown in a formula I, and R1-R7 are as shown in the specification. The invention also comprises pharmaceutically acceptable salts of the 2, 4-diarylaminopyrimidine analogue, and a pharmaceutical composition containing the 2, 4-diarylaminopyrimidine analogue or the pharmaceutically acceptable salts of the 2, 4-diarylaminopyrimidine analogue as an active ingredient. The 2, 4-diarylaminopyrimidine analogue or the medicinal salt thereof disclosed by the invention has better anticancer activity, and the preparation method is simple, feasible and easy to operate. # imgabs0 #

The invention relates to a preparation method and application of a methylthiazole derivative with anti-hepatoma activity, and belongs to the technical field of synthesis of medicines. On the basis of a 2-[3-cyano-4-(2-isobutoxy)-phenyl]-4-methylthiazole-5-formic acid structure, terminal alkyne is introduced to the structure, then a click reaction and an azide compound react to obtain a plurality of compounds with novel structures, and activity tests in anti-tumor, anti-inflammatory and anti-oxidation aspects show that the compound has a broad application prospect. The obtained compound has obvious anti-cancer activity and provides huge application value for research and development of anti-cancer drugs.