67results about How to "Improve tumor inhibition" patented technology

The invention discloses an antibody coupling drug targeting on EGFR, a preparation method thereof and uses thereof. The antibody-conjugated drug targeting EGFR is named LR004-VC-MMAE consisting of anantibody, a cytotoxic drug and a linker, wherein the antibody drug conjugate has a structure represented by the formula I, wherein mAb is an LR004 monoclonal antibody, n=2-8. The novel antibody-conjugated drug LR004-VC-MMAE can not only target EGFR antigen, but also has strong cytotoxicity to tumor cells. Compared with LR004 itself, it did not affect the affinity, endocytosis and targeting of theantibody, and better retained its biological function. Compared to LR004, the antitumor effect of LR004-VC-MMAE antibody-conjugated drug is significantly improved, and the tumor disappeared. Comparedto LR004, LR004-VC-MMAE antibody-conjugated total antibody showed longer half-life, slower clearance rate, lower concentration of free MMAE in plasma, shorter half-life and faster clearance rate, which is conducive to reduce toxicity.

The invention relates to a tumor specific killer cell preparation and a preparation method thereof. A specific killer cell is a mixture of DC (Dendritic Cell) vaccine, and CIK (Cytokine Induced Killer) and CTL (Cytotoxic Lymphocyte) cells. The preparation contains thymopentin; the preparation is mixed with the killer cells so as to have the effect of obviously improving the treatment effect.

The invention discloses a fermented composition of multiple probiotics and composite medicinal and edible fungi, and a preparation method and an application thereof. According to the invention, a composite polysaccharide extract is obtained by enzymolysis and extraction of various medicinal and edible fungi by using compound enzymes, and the extract is subjected to symbiotic fermentation by using multiple intestinal probiotics, such that a fermented composition is obtained. The invention also relates to an application of the fermented composition in preparing health-care products used for preventing and treating tumors. The medicinal and edible fungi adopted by the invention are any three or more than three selected from lucid ganoderma, agaricus blazei murill, shiitake, and flammulina velutipes. The fungi are subjected to crushing, soaking, and enzymolysis; and bifidobacterium and lactobacillus are added for fermentation. Through symbiotic fermentation with the intestinal probiotics, the molecular weight of medicinal and edible fungi composite polysaccharide is substantially reduced, tumor cell inhibiting activity is substantially improved, and inhibition effect is substantially improved.

The invention provides a nanoemulsion of ginsenoside, its preparation method and application. The ginsenoside emulsion provided by the invention contains ginsenoside, water, oil, an isotonic agent and a surfactant, and may also contain a stabilizer. The emulsion provided by the invention does not contain organic solvents and solubilizers with toxic and side effects, so it is non-allergic and has small side effects; and the content of active ingredients in the oil phase of the nanoemulsion provided by the invention is relatively high, which meets the high clinical efficacy requirements. At the same time, the emulsion can also change the distribution of saponins in the human body, improve the bioavailability of the drug, and can make the ginsenosides concentrate in the tumor site in the body, so as to improve the antitumor effect of the compound.

The invention discloses folate-conjugated polyethylene glycol monostearate, and a preparation method and application thereof. The folate-conjugated polyethylene glycol monostearate has a structure shown as below, wherein n equals to 45-136. The preparation method of the folate-conjugated polyethylene glycol monostearate comprises the following steps: weighing folic acid and triethylamine; adding dimethylsulfoxide for dissolution; adding dicyclohexylcarbodiimide and N-hydroxy succinimide; stirring at room temperature by avoiding light; standing for overnight; filtering to remove by-products; then adding polyethylene glycol monostearate; heating to dissolve; reacting overnight to obtain a coarse product; placing the coarse product in a dialysis bag; dialyzing with water; and conducting freeze-drying to obtain the folate-conjugated polyethylene glycol monostearate. The folate-conjugated polyethylene glycol monostearate can be applied to preparation of a folic acid modified antitumor drug delivery system, improve drug targeting, efficacy and pharmacokinetics, and reduce toxicity.

A slow-release hormone-type anticancer medicine features that its active anticancer component is wrapped by the slow-release auxiliary to prepare the slow-release implant or injection. Said slow-release injection is composed of slow-release microballs and solvent divided into ordinary one and special one containing the suspending aid chosen from carboxymethyl cellulose sodium and mannitol.

The invention relates to the field of pharmaceutical preparations and traditional Chinese medicine preparations and discloses a nano liposome containing a traditional Chinese medicine effective component timosaponin AIII. A preparation method of the nano liposome comprises the following steps: (1) mixing a timosaponin AIII solution and a film material solution; removing a solvent and moisture to obtain a lipid thin film; (2) adding a phosphate buffering solution and hydrating to obtain a timosaponin AIII liposome rough suspension solution; (3) carrying out ultrasonic treatment or high-pressure homogenization treatment at 40 DEG C to 60 DEG C to obtain the timosaponin AIII nano liposome. The timosaponin AIII nano liposome can be used for preparing a medicine for inhibiting tumor cell proliferation and has a good application prospect.

The invention belongs to the technical field of medicines, and provides a sialic acid lipid derivative which can be used for modifying a particle preparation and a preparation method and application thereof. The structural general formula of the sialic acid lipid derivative is as shown in the specification, wherein R1 is an H atom or C1-C6 alkyl; R2 is H, (CH2) m or C2-C6 alkenyl, and m =1-17; when X is an H atom or an O atom, R3 is (CH2) n or cholesteryl, and n = 1-17; when X is a carbonyl group, R3 is a C12-C24 alkoxy group, a C12-C24 alkyl substituted amino group or cholesteryl; and R4 is -OH, -NHCOCH3 or -NHCOCH2OH. The sialic acid lipid derivative disclosed by the invention can be used for modifying a particle preparation and realizing different treatment or diagnosis purposes according to the properties of the medicine. Especially in the anti-tumor aspect, the sialic acid lipid derivative can endow a particle preparation with excellent tumor targeting ability to improve the tumorinhibition effect.

A slow-release anticancer medicine containing hormone component for preparing the slow-release implant or slow-release injection is composed of the active anticancer component chosen from hormone-type anticancer medicine and its synergist, and the medicinal additive chosen from polylactic acid, the copolymer of polyoxyacetic acid and hydroxyacetic acid, ethene-vinyl acetate copolymer and polifeprosan.

A traditional Chinese medicinal preparation for treating malignant tumors is prepared by using 10-20g of Radix Astragali, 5-15 parts of ginseng, 10-25g of Spica Prunellae, 2-5g of licorice root, 20-25g of Rhizoma Curcumae, 25-30g of Barbed Skullcap Herb, 5-10g of dried toad, 15-20g of Radix Ranunculi Ternati, 20-25g of Polyporus Umbellatus, 20-25g of Cornu Bubali and 25-30g of Agrimonia eupatoria. The traditional Chinese medicinal preparation for treating malignant tumors has the advantages of low cost and good curative effect.

The invention pertains to pharmacy field, comprising connecting two polypeptides of different functions with a carrier molecule of polyethylene glycol(PEG). One polipeptide thereof is a cell adhesive peptide with a seaquence of Glu-Ile-Leu-Asp-Val, and the other polipepetide thereof is an antitumor oligopeptide with a seaquence of Tyr-X-Glu-Pro-Gly-Pro-Y-Ala,in which X is Leu or Ile, and Y is Thr or Ser. The synthesized hybrid molecule is called guiding double functional antitumor polypeptide, possessing a suppression function for tumour cell growth and transfer, and can be used in antitumor pharmacy.

An anticancer sustained-release implant is characterized in that active anticancer ingredient is wrapped into pharmaceutical excipient to be made into the sustained-released implant or sustained injection. The active anticancer ingredient is the combination of anti-metabolism anticancer medicine and synergistic agent thereof. The synergistic agent is made from mustine drug and/or antimitotic drug and/or plant alkaloids. The pharmaceutical excipient is made from polylactic acid, copolymer of polyglycolic acid and glycolic acid, ethylene-vinyl acetate copolymer, FAD: sebacic acid (SA) copolymer and/or polifeprosan, etc. The sustained-release injection is composed of sustained release microspheres and menstruum, and the menstruum is classified into common menstruum and special menstruum with suspending agent. The suspending agent is made from sodium carboxymethyl cellulose, mannite, etc. and is used for suspending active anticancer ingredients or sustained-release gains or microspheres containing active anticancer ingredients so as to facilitate injection. Partial tumor placement or sustained-release agent injection can reduce medicine systemic toxicity effect as well as can selectively increase medicine concentration at partial tumor to enhance the curative effect of non-operative treatments such as chemotherapeutic drug, radiation therapy, etc.

Provided are an improved EGFR antibody or a functional segment thereof, comprising an engineered heavy chain and light chain. Specifically, the antibody is an engineered whole human-source monoclonal antibody. Also provided is a method for manufacturing said whole human-source antibody and usage of the antibody in the manufacture of medicines used for the treatment of tumors.

A magnetic nano-Ni medicine with high target performance for suppressing the cells of tumor, especially the malignant tumor, is prepared through preparing the solution of the single-dispersing Ni nanoparticles with functionalized surface, ultrasonic stirring, adding it in the solution of quercetin or other medicine able to suppress the cells of tumor, and slight stirring.

The invention particularly relates to a quercetin-low molecular heparin-paclitaxel conjugate as well as a preparation method and application thereof. Quercetin and paclitaxel have good anti-tumor activity, but the quercetin and the paclitaxel are poor in water solubility and low in bioavailability, so that the clinical application condition is not ideal. The invention provides a paclitaxel-low molecular heparin-quercetin conjugate. Low-molecular heparin sodium is taken as a skeleton and the paclitaxel and the quercetin are connected through covalent bonds. As an anti-tumor active component, the conjugate effectively improves the defect of poor solubility of the paclitaxel and the quercetin. The conjugate obtained according to the preparation method basically does not destroy the active structures of the paclitaxel and the quercetin, well retains the pharmacological activity of the paclitaxel and the quercetin, is applied to anti-tumor drugs, is expected to achieve the treatment effectof the paclitaxel and the quercetin, and has important clinical treatment significance.

The invention belongs to the field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition for treating colon cancer. The traditional Chinese medicinecomprises the following main active ingredients in parts by weight: 2-4 parts of radix astragali, 0.5-1 part of herba epimedii, 1-1.5 parts of radix paeoniae rubra, 0.5-1 part of rhizoma curcumae, 1.5-3 parts of rhizoma smilacis glabrae and 0.5-1.5 parts of fried rhizoma atractylodis macrocephalae. The invention further provides a preparation method and application of the traditional Chinese medicine composition for treating colon cancer. Experiments of colon cancer tumor-bearing mice show that when the traditional Chinese medicine composition for treating colon cancer is combined with chemotherapeutics for application, although the tumor inhibition effect of the chemotherapeutics is not obviously enhanced, the survival time of the mice can be obviously prolonged, the weight loss caused bythe chemotherapeutics is relieved, the T lymphocyte level of the mice is improved, particularly, the levels of CD4 <+> T lymphocytes and CD8 <+> T lymphocytes are remarkably improved, indicating thatthe traditional Chinese medicine composition for treating the colon cancer can improve the body immunity of a patient suffering from the colon cancer, the living quality of the patient is improved, and the survival time of the patient is prolonged.

A sustained-release steroid preparation with antitumor effect is provided, which is characterized in that an antitumor component is coated inside pharmaceutically-acceptable adjuvant to make a sustained-release implant or sustained-release injection. The antitumor component is an antitumor steroid drug or synergists thereof. The antitumor steroid drug is selected from chlormethine drugs and/or antimitotic drugs and/or plant alkaloids. The pharmaceutically-acceptable adjuvant is selected from polylactic acid-polyglycolic acid-hydroxyacetic acid copolymer, ethylene-vinyl acetate copolymer and/or polifeprosan. The sustained-release injection contains sustained-release microspheres and solvents, wherein the solvents include common solvents and special solvents containing a suspending agent, wherein the suspending agent is selected from sodium carboxymethylcellulose, mannitol and the like and used to suspend sustained-release granules or microspheres, thereby facilitating injection. The sustained-release preparation is administered by local delivery in the tumor site or injection, which can not only reduce systemic toxicity but also selectively increase local drug concentration in the tumor site and enhance the therapeutic effect of nonoperative treatment such as drug therapy and radiotherapy.

The invention discloses a single-chain antibody of a target EGFR dimerized interface and application of the antibody. Fusion protein contains an amino acid sequence in which heavy-chain variable-region protein, connecting peptide and light-chain variable-region protein are sequentially connected with one another from 5' to 3', wherein the amino acid sequence of the heavy-chain variable-region protein is shown as SEQ ID NO:1, and the amino acid sequence of the light-chain variable-region protein is shown as SEQ ID NO:3. Genes of the single-chain antibody of the target EGFR dimerized interface and Pichia pastoris engineering bacteria are constructed and optimized, and the single-chain antibody is obtained through fermentation and separation purification, that is to say that the single-chainantibody of the target EGFR dimerized interface is prepared efficiently and successfully by means of a genetic engineering technology. The antibody is low in relative molecular mass, high in penetrability, more excellent in tumor inhibition effect during solid tumor treatment and capable of effectively inhibiting abnormal expression of EGFR to prevent the proliferation and growth of tumor cells; afoundation is laid for later development of novel inhibitors of the EGFR, and the antibody has a high application value.

The invention relates to novel usage of an astragalus mongholicus and flavone extract, in particular to application of the astragalus mongholicus and flavone extract in preparation of chemotherapy drugs for laryngocarcinoma. The chemotherapy drugs are composed of an ethanol extract of astragalus mongholicus and cisplatin, and the mass ratio of the ethanol extract of the astragalus mongholicus to the cisplatin is not less than 6:1. The laryngocarcinoma is the second largest respiratory high-incidence tumor after lung cancers, and is highly prevalent in northern China, an I type recommended drugfor the laryngocarcinoma chemotherapy is the cisplatin, and the dose-dependent nephrotoxicity of the cisplatin greatly limits its clinical application. The extract enhances the tumor suppressing ability, and the astragalus mongholicus and the flavone have a good protective effect on the kidney damage caused by the cisplatin.

The anticancer implant features the effective anticancer component coated inside the supplementary material to form slow released implant or slow released injection. The effective anticancer component is the composition of anticancer antimetabolite and its synergist. The synergist is selected from nitrogen mustard medicine, karyokinesis resisting medicine and/or plant alkaloid. The medicinal supplementary material is PLA, PLGA, EVAc, etc or their composition; the slow released injection consists of slow released microballoon and solvent; the solvent is common solvent or special solvent containing suspending agent; and the suspending agent is sodium carboxymethyl cellulose, mannitol, etc. Implanting or injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.

Disclosed are a corresponding-kaurane type diterpene derivative and application in preparation of antitumor drugs thereof. The structure of the corresponding-kaurane type diterpene derivative is as shown in formula (I); a preparation method of the compound shown in the formula (I) comprises the following steps that 1, Isoforretin A and DMAP are dissolved in dichloromethane, triethylamine is added,the temperature is maintained between 0 DEC G-5 DEC G and acetyl chloride is added dropwisely, and the temperature of reaction liquid is increased to 20 DEC G-25 DEC G and stirring reaction is conducted after the dropwise adding is completed; 2, saturated sodium bicarbonate aqueous solution is added into the reaction liquid to quench the reaction after it is detected by TLC that the reaction is conducted completely, a water layer is extracted by the dichloromethane for three times, an organic layer is combined, the organic layer is washed by dilute hydrochloric acid for three times, and threelayers are washed by saturated saline solution. The organic layer is collected, dried by magnesium sulfate anhydrous, filtered and concentrated to obtain crude products. The crude products are purified by flash silica gel column chromatography to obtain target products in the formula (I) as pure products.

The invention provides a novel polymer-bonded tumor vascular blocker. The invention is characterized in that an ethanolamine modified amino acid block copolymer poly(ethylene glycol)-b-poly(L-asparticacid) and a small molecule vascular blocker DMXAA are bonded to obtain a novel polymer-bonded medicine. A polymer main body in the novel bonded medicine is polyamino acid with excellent biocompatibility and good degradability, and a poly(ethylene glycol)hydrophilic segment protects the stability of nanoparticles in blood circulation; the DMXAA group in the bonded medicine promotes spontaneous assembly of the polymer-bonded medicine into stable nanoparticles in an aqueous solution due to an own strong Pi-Pi stacking effect and an own strong hydrophobic action. The polymer-bonded medicine is simple in technology, is easily produced on a large scale, is good in biocompatibility and stability, has the characteristic of slow release, is accumulated and stays on a tumor site for a long time, and has the advantage of long-term destruction to tumor blood vessels. The invention further provides a preparation method of the polymer-bonded medicine. The polymer-bonded medicine has a very good application prospect in the field of tumor therapy.

The invention discloses an anti-human EGFR antibody drug conjugate as well as a preparation method and an application thereof. The anti-human EGFR antibody drug conjugate has a structure as shown in a formula I which is described in the specification. According to the invention, the anti-human EGFR antibody drug conjugate targeting EGFR and mainly used for solid tumor treatment is constructed by coupling an SCT-200 fully humanized monoclonal antibody with Linker-MMAE through a chemical method of reducing disulfide bonds between antibody chains. Compared with SCT-200, the novel antibody drug conjugate SCT-200-Linker-MMAE provided by the invention has the advantages that the affinity, endocytosis activity and targeting property of the antibody are not influenced, the biological function of the antibody is better reserved, the activity is obviously improved compared with SCT-200, the expression of related proteins in the tumor apoptosis process can be obviously inhibited, and the tumor inhibition effect is greatly enhanced.

The invention especially relates to a chlorogenic acid acylate capable of improving bioavailability of chlorogenic acid and application of the chlorogenic acid acylate with a structural formula as described in the specification in preparation of drugs used for treating tumors, belonging to the field of biological medicine. The chlorogenic acid acylate provided by the invention can improve the in-vivo bioavailability of chlorogenic acid, thereby overcome the problem of low absorptivity of chlorogenic acid in oral administration due to influence of intestinal florae and substantially improving the inhibition effect of chlorogenic acid on tumors.