163results about How to "Antiproliferative activity" patented technology

The invention discloses a gRNA (guide ribonucleic acid) sequence. The sequence can be used for DNA (deoxyribonucleic acid) sequence edition by using a hepatitis B virus genome S gene conserved region site as a target sequence, can successfully destroy the HBV (hepatitis B virus) cccDNA and integrated-state HBV DNA in a HBV stable cell model and an HBV hydrodynamic mouse model, and obtains obvious effects on inhibiting HBV replication and expression. The invention also discloses application of the CRISPR-Cas9 system containing the gRNA sequence in preparing drugs for treating hepatitis B.

The present application describes a method of treating prostate cancer, melanoma or hepatic cancer in a subject in need thereof, the method comprising administering to said subject a therapeutically effective amount of the heterocyclic compound represented by Formula I or its pharmaceutically acceptable salt:

The invention discloses a quinoline and quinazoline derivative I, a preparation method, an intermediate C, composition and an application. The preparation method comprises two methods, wherein the first method comprises steps as follows: 1, a compound A and a compound B react in a solvent under the action of alkali 1 to obtain a compound C; and 2, the product C obtained in the step 1 reacts with a compound D under the action of alkali 2; and the second comprises step as follows: the compound A and a compound E react in the solvent under the action of the alkali 1. The invention further provides the application of the compound represented in formula I or medicine composition in preparation of an EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor, an A431 or H1975 cell proliferation inhibitor or medicine for preventing or treating tumor diseases. The provided compound has better antitumor activity.

The invention discloses application of glacial water in preparation of an externally applied agent for the skin and a glacial water-containing externally applied agent for the skin. It is found for the first time that glacial water can obviously promote propagation of fibroblasts, improve synthesis of fibroblast collagen I and elastin laminin of the skin and substantially inhibit propagation activity of human epidermal melanocytes (HEM-m) and formation of melanin. Glacial water is used as one or more selected from the group consisting of an anti-aging active component, a whitening active component and a moisture-retaining component of the externally applied agent for the skin; so the glacial water-containing externally applied agent for the skin is natural and safe and is capable of improving skin elasticity, resisting crease, repairing impaired skin, reducing hyperpigmentation and whitening the skin.

The invention relates to secalonic acid H derived from penicillium oxalicum and application of the secalonic acid H for preparing a medicine for preventing human colon cancer. The compound has a function of inhibiting human colon cancer cell proliferation. The structural formula of the secalonic acid H is as shown in the specification. Through fermentation culture of Penicillium oxalicum IBPT-6, a fermented substance is prepared, and the compound is separated and purified from the fermented substance. Tests show that the compound has relatively high anti-tumor activity upon human colon cancer cells HCT116. The compound can be used for preventing human colon cancer cell proliferation inhibition medicines or anti-tumor medicines for studying human colon cancer.

The invention provides a beta-elemene halide, a preparation method therefor and an application of the beta-elemene halide. Specifically, the invention provides a preparation method for a compound witha structure represented by a formula I shown in the description, wherein each group is as defined in the description. The invention further provides a compound with a structure represented by a formula II shown in the description (each group is as defined in the description), a pharmaceutical composition containing the compound represented by the formula II, the compounds and isotope derivatives,chiral isomers, allosteric isomers, different salts, prodrug, preparations and the like of these compounds. The compounds can serve as intermediates and be used for preparing derivatives of elemene and treating various diseases capable of being treated by the elemene, including lung cancer, mammary cancer, liver cancer, and the like.

The invention relates to a bisbenzimidazole bicarbazole compound, in particular to applications of the bisbenzimidazole bicarbazole compound in a specific binding nucleic acid G-quadruplex structure and an anti-tumor drug. The bisbenzimidazole bicarbazole compound and a nucleic acid sample to be detected are incubated in a buffer solution with a pH (Potential of Hydrogen) value of 6-8; an absorption peak of an ultraviolet-visible absorption spectrum within the range of 390-440nm is obviously enhance through observation; or whether a fluorescence spectrum has a fluorescence peak between within the range of 430-540 is observed to detect whether the nucleic acid sample to be detected is nucleic acid in the G-quadruplex structure. The bisbenzimidazole bicarbazole compound is added into a culture solution containing tumor cells as a drug, cultured together with the tumor cells, and used for inhibiting tumor cell proliferation, or the bisbenzimidazole bicarbazole compound is used for inhibiting the tumor cell proliferation as a most active ingredient of the drug. A method has the advantages of simplicity, quickness and cheapness.

The invention relates to polyphenols substances, a synthesis method thereof and the use thereof, in particular to a flavonoid derivative, a preparation method thereof and the use thereof, and solves the problem that the conventional natural flavonoids compounds are difficult to extract and obtain and cannot be widely used. The structural formula (I) of an intermediate and the structural formula (II) of a final product are shown below, wherein R1, R2 and R3 are respectively selected from hydrogen, C1-C8 alkyl, halogen, nitro, C1-C8 alkoxy and amino; and R1, R2 and / or R3 can be fused with a benzene ring to form a substituted or unsubstituted fused ring compound; R4 and R5 are respectively selected from C1-C8 alkyl, C1-C8 alkoxy and alkylene; R may be H, methoxy-methoxy or methoxy; and b ring is a benzene ring or a heterocyclic compound. The derivative can be used for preparing medicaments for resisting tumors and cardiovascular and cerebrovascular diseases and inhibitors of protein tyrosine kinases, opens up a new way for preparing the medicaments and brings a new breakthrough to the medicament field; and the synthesis method has the advantages of mild condition and convenient operation.

The invention discloses a class of compounds with antitumor activity. The structural formula is as follows: In the formula, R is one or two substituents of ethynyl, chlorine, fluorine, trifluoromethyl and 3-fluorobenzyloxy; X is O or NH; Y is CH2 or CO (carbonyl); Z is H or methoxy; n=5 or 6. The salicylic amide compounds in the structural formula are synthesized from 5-nitrosalicylic acid or 4-methoxysalicylic acid and aniline derivatives through amidation, reduction, and reaction with monoethyl pimelic acid chloride. . The compound has a novel structure and the synthesis method is easy to realize. The anti-tumor activity test showed that it has inhibitory effect on the growth of human liver cancer cells (HepG-2), human colon cancer (SW 480) and human prostate cancer cells (PC3), and the activity of most compounds is stronger than that of gefitinib. The use of preparing anti-tumor drug preparations.

The invention discloses an application of an ingenane diterpene compound in preparation of antitumor drug. The ingenane diterpene compound is one or more of the ingenane diterpene compound shown in a formula (1). The ingenane diterpene compound can obviously inhibit the propagation activity of breast cancer cells, compared with a traditional tumor therapeutic method, tumor inhibitory effect is good, toxic and side effects are little, targeting property is strong, the ingenane diterpene compound has no damage to normal cells, security can be guaranteed at maximum degree, the ingenane diterpene compound provides a latent novel medicine development purpose for treating breast cancer, and can be a further research as an anti-breast cancer candidate medicine.

The invention belongs to the field of medicaments and particularly relates to inoscavin A as a monomeric component in the phellinus as well as a preparation method and an application of the inoscavin A. The preparation method of the inoscavin A comprises the following steps of: (1) grinding the phellinus serving as a herbal medicine, and carrying out reflux extraction by ethanol; (2) extracting the ethanol extract by petroleum ether, and removing the petroleum ether; (3) extracting the extract by methylene dichloride, taking the ethylene dichloride layer, and drying to obtain the methylene dichloride extract; and (4) dissolving the extract into a flowing phase, carrying out high-speed counter-current chromatography, receiving and merging the flows, and recovering the solvent to obtain dried powder. Due to the adoption of the technical scheme, the compound of the inoscavin A as a monomeric component in the phellinus can be prepared in batch. The experiments in vitro prove that the compound has lung cancer tumor cell inhibition activity and liver cancer tumor cell proliferation activity. The experiments in vivo prove that the compound has the efficacy of diminishing inflammation and regulating immunity and can take effect together with the medicament for tumor chemotherapy so that the medicinal effect of the compound in vitro and vivo can be studied further.

The invention provides an aromatic heterocyclic amide substituted diarylurea compound, a preparation method and application thereof. The structural formula of the compound is shown as the specification, wherein Ar is a pyridine heterocycle containing pivaloyl amino or methylamine carbonyl, R1 and R2 are trifluoromethyl, trifluoromethoxy or halogen, R2 can also be alkoxy with a tertiary amine group substituted end and a carbon atom number of 2-3, and the alkoxy is connected to the para-position of urea through the O atom. The compound can be prepared by three-step organic synthesis reaction, and the method has the advantages of easy operation of the reaction process, easily available raw materials, mild reaction conditions, cheap reagents and the like, and is suitable for large-scale production by pharmaceutical enterprises. The compound has good inhibitory activity on VEGFR-2 kinase, also can inhibit the proliferation activity of tumor cells, and can be used for preparation of antitumor drugs and VEGFR-2 kinase activity inhibition drugs, thus having good application prospects and scientific research value.

The invention relates to secalonic acid I originated from penicillium oxalicum and an application thereof in the preparation of drugs for preventing human esophagus cancer. Secalonic acid can inhibit the proliferation of human esophagus cancer cells. The structure of secalonic acid is represented in the description. Penicillium oxalicum IBPT-6 is cultured through fermentation to obtain the fermentation product; and secalonic acid is separated from the fermentation product and then purified. The experiment results show that secalonic acid can well inhibit the activity of human esophagus cancer cell EC9706. Secalonic acid can be used to prepare drugs for inhibiting the proliferation of human esophagus cancer cells and antitumor drugs, and can also be applied to the research on human esophagus cancer.

The invention discloses an andrographolide-19-amide derivative, a preparation method and its use in medicine, which belongs to the pharmaceutical chemistry field. According to the invention, a structural general formula of the andrographolide-19-amide derivative is shown as (A): R1 and R2 are hydrogen, substituted or non-substituted C1-C8 aliphatic acyl, substituted or non-substituted aromatic acyl; and R3 and R4 are hydrogen, substituted or non-substituted C1-C8 alkyl, substituted or non-substituted aromatic group. The invention also discloses the preparation method of the andrographolide-19-amide derivative and an application of the andrographolide-19-amide derivative for preparing antitumor drugs.

The invention relates to an oil control composition, which is prepared from octanoyl glycine, nicotinamide, inositol, sophorolipid fermentation liquor and a laminaria saccharina extract. The oil control composition prepared from the nicotinamide, the inositol, the octanoyl glycine, the laminaria saccharina extract and the sophorolipid fermentation liquor adjusts oil secretion on the basis of moisture retention, and establishes a three-dimensional balance oil control technology aiming at inhibition for the activity of three target points, i.e., lipase, 5 alpha-reductase and sebum flow regulation.

The present invention belongs to the technical field of medicine, and discloses a cordycepin nanometer liposome, a preparation method, and antitumor activity applications thereof. The cordycepin is easily degraded in vivo so as to deactivate. According to the present invention, the in vitro and in vivo antitumor activity results of the product show that the cordycepin liposome provides significant inhibition effects on liver cancers, and the in vivo activity of the cordycepin is well retained through the liposome dosage form; the cordycepin liposome difficultly achieves the high encapsulation rate through the existing preparation method; the cordycepin nanometer liposome of the present invention comprises cordycepsin, phospholipid, cholesterol, a surfactant, and an antioxidants; and the preparation method combines a pH gradient method and a reverse evaporation method, wherein the cordycepin nanometer liposome obtained through the preparation method has characteristics of high encapsulation rate (more than or equal to 90%), uniform particle size, and good stability.

The invention relates to secalonic acid I derived from penicillium oxalicum and application of the secalonic acid I for preparing a medicine for preventing human colon cancer. The compound has a function of inhibiting human colon cancer cell proliferation. The structural formula of the secalonic acid I is as shown in the specification. Through fermentation culture of Penicillium oxalicum IBPT-6, a fermented substance is prepared, and the compound is separated and purified from the fermented substance. Tests show that the compound has relatively high anti-tumor activity upon human colon cancer cells HCT116. The compound can be used for preventing human colon cancer cell proliferation inhibition medicines or anti-tumor medicines for studying human colon cancer.

The invention discloses a recombinant human endostatin protein with different amino acid structures, a method for preparing the recombinant human endostatin protein and application thereof. Amino acid sequences of a recombinant human endostatin protein 1 are shown as SEQ ID NO.1, and amino acid sequences of a recombinant human endostatin protein 2 are shown as SEQ ID NO.2. The recombinant human endostatin protein, the method and the application have the advantages that the two types of recombinant proteins are active in the aspects of inhibiting the proliferation activity of vascular endothelial cells under the induction actions of basic fibroblast growth factors (bFGF) and inhibiting the angiogenesis activity of chick chorioallantoic membranes (CAM) and are easy to enter the vascular endothelial cells and vascular endothelial cells of the chick chorioallantoic membranes, and transmembrane effects of the recombinant human endostatin protein and the structural stability of N ends can be obviously improved; effects of directly inhibiting tumor cell growth can be realized, effects of inhibiting generation of neonatal vascular endothelial cells can be effectively realized, and the recombinant human endostatin protein can be used for treating various diseases, including solid tumor, retinal diseases due to diabetes mellitus and rheumatoid arthritis, due to angiogenesis.

The invention discloses a plant extract preparation for preventing astriction of senile. The ingredients and weigh shares are: 30-40 shares of senna extract, 30-40 shares of aloe extract, 20-30 shares of areca nut extract, 304 shares of oryzanol, 20-30 shares of calcium lactate, and proper amount of accessories. The invention uses the active ingredients in natural plants scientifically and naturally, pointing to the reason of senile astriction, carries on further treatment and prevention, and solves the problem of astriction in cell parallel. Because the active ingredients of the preparation are from the extract of natural plant, and it has target direction performance, it has no toxin and side effects.

The invention provides 2,9-bis-styryl substituted phenanthroline compounds specifically combined with G-tetrastrobila-structure nucleic acid and a preparation method thereof, and application of the 2,9-bis-styryl substituted phenanthroline compounds in tumor resistance. The structural formula is disclosed as Formula I. The compounds disclosed as Formula I can quickly judge whether the sample to be detected is G-tetrastrobila-structure nucleic acid by ultraviolet-visible absorption spectrum or fluorescence spectrum. The drug effect test proves that the compounds disclosed as Formula I in vitro have strong inhibiting actions on multiple tumor cell strains. The 2,9-bis-styryl substituted phenanthroline compounds can be used for preparing anticancer drugs.

The invention belongs to the technical field of medicines, and relates to a diaryl pyrazole compound, and a preparation method and a purpose thereof. Specifically, the invention relates to the compound and the compound as a tumor cell proliferation inhibitor in preparing antitumor medicines. The compound has a structural formula represented as the following, wherein R1-R8 and X are defined as in the specifications.

The invention provides an application of a TIGIT-ECD recombinant protein in resisting allogeneic immunological rejection. The amino acid sequence of the recombinant protein TIGIT-ECD is shown as SEQ ID NO:1. The nucleotide sequence coding the recombinant protein TIGIT-ECD is shown as SEQ ID NO:2. The recombinant protein is capable of effectively regulating macrophage polarization by activating a TIGIT-CD155 signal path, and contributes to inducing allogeneic graft tolerance. Therefore, the recombinant protein TIGIT-ECD can serve as a graft rejective reaction inhibitor, and can also be appliedto preparing drugs for preventing and treating the graft rejective reaction.

The invention relates to the technical field of a horse placenta extract and a pharmaceutical application thereof, specifically to a horse placenta water-soluble protein extract with bioactivity, a preparation method and an application thereof. According to the present invention, during an extraction process, a phosphate buffer solution with a pH value close to a physiological pH value and an osmotic pressure close to a physiological osmotic pressure is adopted as an extraction solvent so as to maintain activity of active substances in a horse placenta to the maximal degree; with the horse placenta extract, activity of normal lymphocytes can be significantly enhanced, proliferation activity of T-lymphocytes and B-lymphocytes induced by ConA and LPS can be significantly inhibited, and killing activity of NK cells on PC-3 cancer cells can be significantly enhanced, such that adjustment effects are provided for immune functions to a certain degree; and with the horse placenta extract, oxidative damage of skin fibroblasts due to H2O2 can be significantly inhibited, cell viability can be improved, MDA content in cells can be reduced, enzyme activities of SOD and GPx can be improved, apoptosis rate can be reduced, and DNA damage can be inhibited, such that a certain protection effect is provided for oxidative damage.

The invention provides 2,4,6-trisubstituted pyridino[3, 4-d]pyrimidine compounds, salts thereof and application and belongs to the technical field of anti-cancer drugs. The compounds are novel in structure and easy in synthesis, have inhibiting activity to epidermal growth factor receptor (EGFR) tyrosine kinase, have obvious inhibiting activity to EGFR of a single mutant (L858R) and double mutants (L858R / T790M), have obvious in-vivo and in-vitro anti-tumor activity and can be applied to the treatment of EGFR mutation related cancers, the synthesis raw materials are readily available, and the synthesis method is easy to achieve.

The invention discloses a 5-hydroxy-2'-nitroaurone or 5-hydroxy-4'-nitroaurone derivatives and application thereof, wherein the derivatives are a compound represented as the formula (I), an isomer or a pharmaceutically acceptable salt thereof. The compound is excellent in inhibition activity on endothelial cells and tumor cells comprising A549, Bel-74021 and MCF-7, and is excellent in inhibition effects on migration and invasion of the tumor cell A549.

The invention relates to a method for preparing two isoflavone compounds and application of resisting tumor and plant germ. The method adopts the secondary metabolite of the endogenic fungus YT2-02 from sponge and derris to produce the two isoflavone structural compounds. Bioactivity tests prove that the two isoflavone structural compounds can be used as cell proliferation inhibitors or plant germ resisting agents.

The invention relates to the technical field of medicine chemistry, in particular to a heteroaromatic ring compound with a thiosemicarbazone structure unit and a preparation method and application ofthe compound. The heteroaromatic ring compound with the thiosemicarbazone structure unit is chelated with metal ions in gastric cancer cells to form a stable complex, and accordingly the proliferationactivity of the gastric cancer cells MGC803 is inhibited. It is proved through a result of an embodiment that compared with a compound 3-AP, the heteroaromatic ring compound with the thiosemicarbazone structure unit has good proliferation inhibition activity on the gastric cancer cells MGC803.

The invention relates to a preparation method and application of penicillium citrinum-derived penicitrinine A. The compound has the effect of restraining human nasopharyngeal carcinoma cell proliferation. The structural formula of the compound is shown in the description. According to the invention, through fermenting culture of penicillium citrinum IBPT-5, a fermentation product is obtained, and then the compound is separated and purified from the fermentation product. Experiment results confirm that the compound has better antitumor activity on human nasopharyngeal carcinoma cells such as CNE-1 and CNE-2. The penicillium citrinum-derived penicitrinine A can be applied to preparation of human nasopharyngeal carcinoma cell proliferation inhibition drugs or antitumor drugs to be used for research on human nasopharyngeal carcinoma.

The invention discloses applications of 4-4' isomerized secalonic acid D derived from Penicillium oxalicum in colon cancer. According to the present invention, the compound isomerization is rare 4-4'linkage and is different from the 2-2' linkage of the known secalonic acid D; and the experiment results prove that the polyphenol-based compound has good inhibitory activity against colon cancer cells, can be used for preparing colon cancer cell proliferation inhibiting drugs or anti-colon cancer drugs, and can be used for antitumor research.

The invention discloses a transformed CRISPR / SaCas9 (clustered regularly interspaced short palindromic repeat / streptococcus pyogenes Cas9) system targeting at hepatitis B virus and application of thesystem. According to designing principles of gRNA (guide ribonucleic acid) of CRISPR and conservative regions of HBV (hepatitis B virus) sequences of different genotypes, three gRNAs are screened andconstructed on a PX601expression vector, meanwhile, different specific liver promoters are selected and combined with an enhancer of an HBV genome, and two promoter combinations are screened to transform the expression vector PX601. When the rRNA guided CRISPR transformation system is applied to cell models and mouse models, expression and replication of hepatitis B virus genes can be effectivelyinhibited while liver tissue expression specificity of SaCas9 is remarkably improved. The system is easy to operate, high in security and high in HBV replication. The transformed CRISPR / SaCas9 systemhas the potential of being a novel treatment medicine for treating hepatitis B virus.