37results about How to "Concentration dependent" patented technology

The invention discloses a liver-targeted platinum-loaded nanometer prodrug for treating liver cancers and a preparation method thereof. The liver-targeted platinum-loaded nanometer prodrug is prepared by taking sodium alginate with the good biocompatibility as a framework to be modified with glycyrrhetinic acid (GA) with a liver cancer cell targeting capacity and a tetravalent platinum compound (PtCl2(OH)2(NH3)2) through a self-assembly technique. In-vitro drug releasing and cytotoxicity tests prove that the platinum-loaded drug nanoparticles have the good blood stability and the intracellular slow-release effect and also have the tumor cell killing capacity. The nanometer prodrug is expected to be used for targeting treatment on the liver cancers and has a good application prospect in the biomedical field.

The invention discloses a brain targeted medicine lipidosome preparation as well as a preparation method and an application thereof. The brain targeted medicine lipidosome which has an enhancement effect is prepared by taking oligopeptide with arginine residues as a target molecule and by using a thin film hydration method and a three-bottle method, and the technical problems that a conventional lipidosome preparation cannot penetrate through blood brain barrier and has no brain targeting are solved. The galenic pharmacy observation shows that the encapsulation efficiency and the particle size of the brain targeted medicine lipidosome preparation disclosed by the invention meet the medicine requirements, and compared with ordinary lipidosome, the brain targeted medicine lipidosome disclosed by the invention is good in acid sensitivity and good in stability in serum, and has in-vitro cell medicine effect and in-vivo mouse glioma medicine effect which are higher than those of long circulation Doxorubicin lipidosome.

The invention discloses a transmembrane peptide-mediated antisense antibacterial agent which comprises popliteal lymph node assay (PLNA) 787; and the PLNA 787 is formed by connecting transmembrane peptide (KFF) 3K and LNA 787 by cysteine-(4-(N-maleimide methyl)-1- cyclohexidine actidione)-hexane and is prepared by a solid phase synthesis method. The transmembrane peptide-mediated antisense antibacterial agent takes bacteria curing gene as a target spot, has the advantages of being high in specificity, efficient, low in toxicity, safe and the like, has remarkable inhibition effect on the growth of drug-resistant bacteria, and especially has remarkable antagonism on the growth of methicillin-resistant staphylococcus aureus.

The invention relates to the technical field of medicines, in particular to a preparation method of a lignan compound in sabia parviflora and an application thereof, and further provides an application of the lignan compound in preparation of medicines or health care products for preventing and treating fatty liver injury. The pharmacological studies show that the compound provided by the invention can significantly reduce a large amount of cell apoptosis caused by FFA treatment of LO2 cells, can reduce the cell apoptosis rate caused by FFA when the concentration of the compound is greater than 2.5 [mu]g / ml, and has concentration dependence; meanwhile, when the concentration of the compound is greater than 2.5 [mu]g / ml, the content of Albumin can be up-regulated; the activity of AST and ALT is weakened, and the content of TG is reduced, so that the compound has a protective effect on FFA-induced liver normal cell damage, and is expected to be developed into a new medicine or health care product for preventing and treating fatty liver injury diseases.

The invention relates to sulphated compound microalgae polysaccharide. The sulphated compound microalgae polysaccharide is prepared by mixing sulphated chlorella polysaccharide and sulphated spirulinaon the base of the ratio of 1 to 16-16 to 1. The sulphated compound microalgae polysaccharide is capable of effectively inhibiting in-vitro proliferation of tumor cells, and is high in water solubility, so that the sulphated compound microalgae polysaccharide can play a role in vitro and is capable of inhibiting the growth of tumor.

The invention relates to the technical field of medicines, in particular to an application of Cynanoside H in preparation of a drug for preventing and treating a breast cancer. A pharmacological studyshows that Cynanoside H inhibits MDA-MB-231 cell proliferation through inducing S-phase cycle arrest, reverses epithelial-mesenchymal transition to inhibit MDA-MB-231 cell migration and invasion, plays a role in preventing and treating the breast cancer, especially triple-negative breast cancer, and provides a new idea for research and development of the drug for preventing and / or treating the breast cancer.

The invention discloses a Bacillus sphaericus parasporal crystal protein preparation method and application thereof. Wild type Bacillus sphaericus IAB 872 is cultured, and ultrasonic treatment, lysozyme treatment, DTT (dithiothreitol) treatment and compound cardiografin treatment are performed to improve the yield and activity of soluble crystal proteins, thereby obtaining high-effect soluble crystal proteins as many as possible. The Bacillus sphaericus parasporal crystal proteins have a certain inhibiting effect on human malignant tumor cells, and can be used for the preparation of antitumor drugs. The inhibition of the Bacillus sphaericus parasporal crystal proteins on the proliferation of human tumor cells includes the inhibition on tumor cells, the influence on apoptosis promotion of tumor cells, the influence on G2 / M phase of cells and the arrest of cells in G2 / M phase.

The invention discloses application of aripiprazole in preparation of an antineoplastic drug. According to the application, it is found for the first time that the aripiprazole can inhibit the proliferative activity of colorectal cancer cells, reduce the clone formation number of the colorectal cancer cells, and inhibit growth of tumors of colorectal cancer. The colorectal cancer proliferative activity inhibiting effect of the aripiprazole is more remarkable along with the increase of the concentration of the aripiprazole and prolonging of the medication time, and has concentration dependencyon the cycle arrest function and in-vivo inhibiting function on the colorectal cancer cells. Meanwhile, the aripiprazole is a drug ratified by FDA for sale; compared with new medicine development, thecost is low, no obvious toxic or side effect exists, the aripiprazole is used for assisting in treatment of colorectal cancer, and a new drug source can be provided for adjuvant therapy of cancer.

The invention discloses application and salvianolic acid B and analogues of the salvianolic acid B in preparing anti-HPV-viral-infection medicine, and belongs to the field of biomedicine. The inventordiscovers that the salvianolic acid B and the analogues, such as myricetin and dihydromyricetin, of the salvianolic acid B for the first time through researches, the salvianolic acid b and the analogues of the salvianolic acid B have good anti-HPV-viral-infection activity and can effectively block adhering of HPV viruses to target cells, and then HPV viral infection is inhibited. Experiments prove that the salvianolic acid B and capsid protein of the viruses can be directly bound, and adhesion of antagonism viruses to the target cells achieves an anti-virus effect. The salvianolic acid B actsin the early stage that the viruses enter the cells, and can also act in the middle stage and the later stage that the viruses enter the cells. The effects are better than medicine only acting on theearly stage that the viruses enter the cells in the prior art. The salvianolic acid B is harmless to the human body in a concentration range where the salvianolic acid B can achieve the anti-virus function. It is very likely that the salvianolic acid B is developed into a novel microbicide for preventing and treating HPV and other sexually transmitted viral infection.

According to the invention, a panaxadiol triterpenoid saponin compound containing seven new compounds is separated from Panax notoginseng leaves by utilizing various separation methods comprising normal-phase and reverse-phase silica gel column chromatography, macroporous adsorption resin column chromatography, gel column chromatography, preparative high performance liquid chromatography and the like. Activity determination experiments show that the seven new compounds have anti-inflammatory activity, and a material foundation is laid for further pharmacological activity screening and clinicalresearch and development of anti-inflammatory drugs with exact curative effects and small toxic and side effects in the future.

The invention relates to a traditional Chinese medicine compound composition with taxus chinensis as a monarch drug and the application of the traditional Chinese medicine compound composition. The invention provides a traditional Chinese medicine compound composition with taxus chinensis as a monarch drug and the application of the traditional Chinese medicine compound composition. The traditional Chinese medicine compound composition with the taxus chinensis as the monarch drug comprises taxus chinensis, fructus ligustri lucidi, ganoderma lucidum, sculellaria barbata and dandelion. The traditional Chinese medicine compound composition provided by the invention is applied to the preparation of an anti-tumor drug. According to the invention, different concentrations of drug-containing serums show a good proliferation inhibition effect on tumor cells and have concentration dependence. In an in-vivo experiment, a traditional Chinese medicine compound of the traditional Chinese medicine compound composition provided by the invention shows a good growth inhibition effect on a tumor cell nude-mouse transplanted tumor model, and the tumor-inhibiting rate of the high-dose group of the traditional Chinese medicine compound is 50.8 percent. The traditional Chinese medicine compound composition provided by the invention is applied to the anti-tumor field.

The invention relates to the field of polysaccharide separation and purification methods and application, in particular to an acidic brasenia schreberi polysaccharide and a separation and purification method and application thereof. The method comprises the following steps: firstly preparing crude polysaccharide, then deproteinizing, separating by adopting a DEAE-52 cellulose column to obtain the high-purity acidic brasenia schreberi polysaccharide BSP-5, and carrying out structure identification on the polysaccharide by virtue of methods such as infrared spectroscopic analysis, ultraviolet full-wavelength scanning, high performance liquid chromatography monosaccharide composition analysis, gel permeation chromatography molecular weight determination and the like. The results show that the polysaccharide is alpha-configuration pyranose with uniform properties, is composed of D-mannose, D-galactose, D-xylose and L-fucose in a molar ratio of 0.08: 1.39: 1: 0.23, is an acidic heteropolysaccharide, and has an average molecular weight of 119.5 KD. In-vitro anti-oxidation and anti-tumor experiment results show that the separated and purified acid brasenia schreberi polysaccharide has relatively strong anti-oxidation effect and anti-tumor biological activity.

The invention discloses an application of caffeic acid to prepare an anti-HPV-virus-infection medicine, and belongs to the biomedical field. Through research, it is first found by the inventor that caffeic acid has good anti-HPV-virus-infection activity and can effectively block adhesion of HPV viruses to target cells, so that HPV virus infection is inhibited. It is proved by experiments that caffeic acid can directly combine with capsid protein of viruses and antagonize adhesion of viruses to target cells, thereby achieving the anti-virus effect. Caffeic acid acts in an early stage when viruses enter cells and acts in medium and later stages after virus entrance. The anti-HPV-virus-infection medicine has an effect superior than that of a medicine that only acts in an early stage when viruses enter cells in the prior art. At the same time, caffeic acid is harmless to the human body in a concentration range, during which caffeic acid has an anti-virus function, and is high in use valueand good in safety. Caffeic acid has likely possibility of becoming a new microbicide for next-generation prevention and treatment of infection of sexual transmission viruses, such as HPV.

The invention discloses an application of a bifid pregnane-type steroid compound in the preparation of a medicine for resisting erythroleukemia, and belongs to the technical field of biology and medicine and pharmacy. The bifid pregnane-type steroid compound disclosed by the invention is C21 steroid saponin BW18. MTT assay shows that the BW18 at different concentrations could inhibit the cell viability of HEL and is concentration dependent. The results of a flow cytometer and Western blot show that the BW18 induces the G2 phase cycle block of HEL cells by up-regulating P27 and down-regulatingthe expression of c-Myc, cyclin E1, CDK1 and CDK2 cycle-related proteins, regulates the expression of differentiation-related genes of erythroid and megakaryocyte lines, promotes the differentiation of cells to erythroid and megakaryocyte lines, thus inhibits the development of erythroleukemia. The BW18 can be used as a potential small molecule for treating the erythroleukemia, and provides a research basis for the development of the medicine for treating the erythroleukemia.

The invention discloses a benzoheterocycle substituted phenanthridine quaternary ammonium salt derivative and a preparation method and application thereof, the benzoheterocycle substituted phenanthridine quaternary ammonium salt derivative has a structure shown as a formula (I), wherein R1 is selected from benzoheterocycle, substituted benzoheterocycle and aromatic heterocycle; R2 is selected from hydrogen, alkyl, cycloalkyl, heteroalkyl, alkoxy, halogen, cyano, amino, dimethylamino, nitryl, trifluoromethyl, trifluoromethoxy, acetamido and hydroxyl; x is halogen or benzenesulfonic acid anion. The derivative provided by the invention is completely different from a traditional 3-methoxybenzamide (3-MBA) mother nucleus in structure and has physicochemical properties different from those of the 3-MBA mother nucleus, and experiments show that the derivative has an effect of inhibiting FtsZ, can be used as an FtsZ inhibitor and can also be used as a bacteriostatic agent.

The invention provides application of lung cough in preparation of a product for preventing and treating breast cancer, and belongs to the technical field of biological pharmacy. It is found for the first time that lung force cough can effectively treat breast cancer, and the lung force cough has the effects of inhibiting the activity of breast cancer cells, inhibiting proliferation of the breast cancer cells, promoting apoptosis of the breast cancer cells and changing the morphology of the breast cancer cells, so that the effect of treating the breast cancer is achieved. The lung cough inhibits proliferation of breast cancer cells, has concentration dependence, has obvious influence on the human breast cancer cell cycle, and can retard the breast cancer cell cycle in the S phase, and the higher the drug concentration is, the more obvious the retardation is.

The invention discloses a polypeptide specifically binding to CD123 protein, a polypeptide complex, a co-delivery system and a preparation method and application thereof. The general formula for the arrangement of amino acids in the polypeptide is X 1 ‑DYDTR‑X 2 ‑QGTD‑X 3 ‑G‑X 4 ‑DFRRISD‑X 5 ; Can bind to CD123 positive cells and inhibit the development of leukemia; the polypeptide complex can increase the number of binding of the polypeptide to CD123 positive cells, and a single drug can inhibit the development of leukemia and prolong the survival period of leukemia mice; the co-delivery system can Loading chemotherapeutic drugs for tumor treatment reduces the toxicity of chemotherapeutic drugs to normal cells.

The invention relates to the technical field of medicines, in particular to a preparation method of a lignan compound in sabia parviflora and an application thereof, and further provides an application of the lignan compound in preparation of medicines or health care products for preventing and treating fatty liver injury. The pharmacological studies show that the compound provided by the invention can significantly reduce a large amount of cell apoptosis caused by FFA treatment of LO2 cells, can reduce the cell apoptosis rate caused by FFA when the concentration of the compound is greater than 2.5 [mu]g / ml, and has concentration dependence; meanwhile, when the concentration of the compound is greater than 2.5 [mu]g / ml, the content of Albumin can be up-regulated; the activity of AST and ALT is weakened, and the content of TG is reduced, so that the compound has a protective effect on FFA-induced liver normal cell damage, and is expected to be developed into a new medicine or health care product for preventing and treating fatty liver injury diseases.

The invention relates to the field of traditional Chinese medicine and discloses new application of herba miscanthi sacchariflori and an antitumor drug. The invention provides the new application of the herba miscanthi sacchariflori in preparing a drug with an anti-tumor effect. According to the invention, by adopting a qPCR experiment, the action mechanism of the qPCR experiment is clarified from a gene level, and the experiment shows that the extract of the herba miscanthi sacchariflori can up-regulate the NFKB2 gene obviously and down-regulate the expression of EGFR and WNT7B genes obviously, and inhibit the tumor cell activity in a range of 50 to 400mug / ml and shows that the herba miscanthi sacchariflori has anti-tumor activity.

The invention discloses a liver-targeted platinum-loaded nanometer prodrug for treating liver cancers and a preparation method thereof. The liver-targeted platinum-loaded nanometer prodrug is prepared by taking sodium alginate with the good biocompatibility as a framework to be modified with glycyrrhetinic acid (GA) with a liver cancer cell targeting capacity and a tetravalent platinum compound (PtCl2(OH)2(NH3)2) through a self-assembly technique. In-vitro drug releasing and cytotoxicity tests prove that the platinum-loaded drug nanoparticles have the good blood stability and the intracellular slow-release effect and also have the tumor cell killing capacity. The nanometer prodrug is expected to be used for targeting treatment on the liver cancers and has a good application prospect in the biomedical field.

The invention discloses an application of polyketone compounds pestalpolyol A as a drug for treating the alzheimer disease. A caenorhabditis elegans model CL4176 of the alzheimer disease is taken as aresearch target, a commercial medicine galanthamine of the alzheimer disease is taken as positive control, and small molecule compounds capable of effectively inhibiting caenorhabditis elegans CL4176paralysis can be effectively screened from a large quantity of natural products or artificially synthesized compounds. A paralysis experiment result proves that compared with the positive control galanthamine, the added polyketone compounds pestalpolyol A with the same concentration have a better effect on inhibiting caenorhabditis elegans paralysis, the inhibition function has concentration dependence in the concentration range of 100 mu M, and the cytotoxicity is smaller.

The invention belongs to the technical field of pharmaceutical compounds, and relates to an aromatic heterocycle substituted acridine quaternary ammonium salt derivative and a preparation method and application thereof, the aromatic heterocycle substituted acridine quaternary ammonium salt derivative has a structure as shown in a formula (I): wherein R1 is selected from aromatic heterocycle and substituted aromatic heterocycle ; and X is halogen or benzenesulfonic acid anion. The invention provides the aromatic heterocycle substituted acridine quaternary ammonium salt derivatives and the preparation method and application thereof, the aromatic heterocycle substituted acridine quaternary ammonium salt derivatives are designed and synthesized by simplifying the structure, intercepting effective fragments in sanguinarine and berberine, and splicing the effective fragments with aromatic heterocycle pharmacophores. The unique antibacterial effect is expected to be exerted through a dual antibacterial mechanism of inhibiting bacterial FtsZ and bacterial biofilm.

The invention discloses a transmembrane peptide-mediated antisense antibacterial agent which comprises popliteal lymph node assay (PLNA) 787; and the PLNA 787 is formed by connecting transmembrane peptide (KFF) 3K and LNA 787 by cysteine-(4-(N-maleimide methyl)-1- cyclohexidine actidione)-hexane and is prepared by a solid phase synthesis method. The transmembrane peptide-mediated antisense antibacterial agent takes bacteria curing gene as a target spot, has the advantages of being high in specificity, efficient, low in toxicity, safe and the like, has remarkable inhibition effect on the growth of drug-resistant bacteria, and especially has remarkable antagonism on the growth of methicillin-resistant staphylococcus aureus.

The present invention utilizes a variety of separation means, including forward and reverse phase silica gel column chromatography, macroporous adsorption resin column chromatography, gel column chromatography and preparation of high performance liquid chromatography, etc., and obtains 7 leaves of Panax notoginseng Panaxadiol-type triterpene saponins including new compounds. These 7 new compounds have been shown to have anti-inflammatory activity by activity assay, which has laid a material foundation for further pharmacological activity screening and clinical research to develop anti-inflammatory drugs with definite curative effect and less toxic and side effects.

The invention discloses application of trilobatin to preparation of anti-HIV virus infection medicines. According to researches, the trilobatin has broad-spectrum anti-HIV-1 activity and low cytotoxicity, and a possible mechanism includes that the trilobatin is capable of specifically targeting at a gp41 N-terminal repeat sequence area to further inhibit HIV entering. The trilobatin is expected tobe developed into excellent anti-HIV small molecule entering inhabitants.

The invention relates to the field of traditional Chinese medicine and discloses new application of herba miscanthi sacchariflori and an antitumor drug. The invention provides the new application of the herba miscanthi sacchariflori in preparing a drug with an anti-tumor effect. According to the invention, by adopting a qPCR experiment, the action mechanism of the qPCR experiment is clarified from a gene level, and the experiment shows that the extract of the herba miscanthi sacchariflori can up-regulate the NFKB2 gene obviously and down-regulate the expression of EGFR and WNT7B genes obviously, and inhibit the tumor cell activity in a range of 50 to 400mug / ml and shows that the herba miscanthi sacchariflori has anti-tumor activity.

The invention discloses a Bacillus sphaericus parasporal crystal protein preparation method and application thereof. Wild type Bacillus sphaericus IAB 872 is cultured, and ultrasonic treatment, lysozyme treatment, DTT (dithiothreitol) treatment and compound cardiografin treatment are performed to improve the yield and activity of soluble crystal proteins, thereby obtaining high-effect soluble crystal proteins as many as possible. The Bacillus sphaericus parasporal crystal proteins have a certain inhibiting effect on human malignant tumor cells, and can be used for the preparation of antitumor drugs. The inhibition of the Bacillus sphaericus parasporal crystal proteins on the proliferation of human tumor cells includes the inhibition on tumor cells, the influence on apoptosis promotion of tumor cells, the influence on G2 / M phase of cells and the arrest of cells in G2 / M phase.

The invention provides application of Jinxiaocapsule in preparation of anti-breast cancer drugs, and relates to the technical field of biological pharmacy. The application specifically relates to preparation of a medicinal preparation for inhibiting the activity of breast cancer cells, inhibiting the proliferation of the breast cancer cells and promoting the apoptosis of the breast cancer cells. The invention provides a pharmaceutical preparation for treating breast cancer. It is confirmed by the invention that the Jin-sensitive capsule can inhibit the activity of MDA-MB-231 cells, MDA-MB-468 cells and 4T1 cells, and has concentration dependence; the proliferation of MDA-MB-231 and MDA-MB-468 cells can be inhibited, and the concentration and time dependence is realized; the cell morphology of MDA-MB-231 and MDA-MB-468 can be changed, and the cell morphology of the influence on the apoptosis of human breast cancer cells MDA-MB-231 and MDA-MB-468 is obvious; and the cycle of human breast cancer cells MDA-MB-231 and MDA-MB-468 is retarded in the S period. And the Jinfei capsule is a clinical compound medicine and can be directly applied to a human body, and clinical safety evaluation is not needed.

The invention discloses a preparation method of dammarane saponin and application of the dammarane saponin in preparation of hypoglycemic and anti-inflammatory drugs and health products. The dammaranesaponin is prepared by the following operation steps of: S1, taking 10kg of dried cyclocarya paliurus leaves, adding a 75% ethanol aqueous solution, sequentially heating, refluxing and extracting for3 times for 3 hours, 2 hours and 2 hours respectively, combining filtrates, and recovering ethanol under reduced pressure to obtain 2.10kg of extract; and S2, taking and suspending 1.5kg of the extract in 20L of water, performing adsorption by using a D101 macroporous adsorption resin chromatographic column, performing washing by using water, and performing eluting by using 30% and 95% ethanol torespectively obtain 250g of 30% ethanol eluate and 625.0g of 95% ethanol eluate which are used as cyclocarya paliurus leaf extracts rich in dammarane triterpenoid saponin. Most of dammarane triterpenoid saponin compounds provided by the invention can inhibit alpha-glycosidase and inhibit release of nitric oxide in lipopolysaccharide-induced RAW264.7 cells, show good hypoglycemic and anti-inflammatory activity, have concentration dependence, and can be used for developing hypoglycemic and anti-inflammatory related drugs and health products.