37results about How to "Concentration dependent" patented technology

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 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 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.

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 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 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 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 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.

The present invention relates to the field of medical technology, in particular to the application of Cynanoside H in the preparation of drugs for the prevention and treatment of breast cancer. Pharmacological studies have shown that Cynanoside H inhibits the proliferation of MDA-MB-231 cells by inducing S-phase cycle arrest; It can inhibit the migration and invasion of MDA-MB-231 cells, play a role in the prevention and treatment of breast cancer, especially triple-negative breast cancer, and provide new ideas for the development of drugs for the prevention and / or treatment of breast cancer.