57results about How to "Suppressed expression level" patented technology

The invention provides a sequence of microRNA like siRNA (msiRNA) aiming at a hepatitis B virus (HBV) S gene and a secondary structure of msiRNA. The sequence is a nucleotide sequence of msiHBs. After co-transfecting HepG2 and Huh7 cells, the msiRNA and a reporter HBV replicating plasmid pHY106+wta can inhibit expression of HBsAg and HBeAg. After transfecting the HepG2.2.15 cell, the msiHBs can also effectively inhibit the expression levels of HBsAg and HBeAg and the load of the HBV in the supernatant. Besides, the msiRNA also has the immunostimulatory activity and can activate innate immunity via a Toll like receptor pathway. Therefore, the msiRNA has double activities of inhibition of HBV gene expression as well as replication and immunostimulation and can be applied to preparation of drugs for treating HBV chronic infection.

Provided is a pharmaceutical composition for the treatment and prevention of alcoholic liver diseases, including cilostazol as an active ingredient. Cilostazol inhibits expression levels of TNF-α and FAS (fatty acid synthase) gene in a concentration-dependent manner, and also significantly inhibits the activity of caspase-3. Accordingly, cilostazol shows superior effects for the treatment or prevention of alcoholic liver diseases, in particular, alcoholic hepatitis compared to pentoxifylline which is conventionally used as a therapeutic agent for the treatment for alcoholic hepatitis. Thus, cilostazol is suitable for use as a drug for the treatment or prevention of alcoholic hepatitis.

The invention provides an application of ART (artesunate) as an anti-leukemia-tumor drug and relates to the field of medical health. ART is taken as a chemotherapeutic drug with targeted inhibition of STAT3 for leukemia tumor. Expression level of STAT3 can be inhibited rapidly and effectively, so that leukemia treatment is realized, ART has a strong inhibition effect on THP-1 cell proliferation and can induce THP-1 apoptosis, and the fact that ART can remarkably reduce protein level of STAT3 and activate Caspase8 and Caspase3 protein simultaneously to induce apoptosis is further proved. Intraperitoneal injection of ART into a THP-1 cell transplantation tumor mouse model discovers that ART can obviously inhibit tumor growth and down-regulate the expression level of STAT3 in tumor tissue. Experiments prove that ART plays an anti-tumor effect on THP-1 by down-regulating expression of STAT3 and activating apoptotic proteins Caspase8 and Caspase3 simultaneously.

The invention relates to a retroviral recombinant capable of efficiently expressing siRNA targeting the ATP binding region of BCRP/ABCG2 gene, which belongs to the field of genetic engineering. Retroviral recombinants are recombined with retroviral RNAi expression system and oligonucleotide fragments, and are packaged by viral packaging cells. The invention is mainly applied to the drug resistance reversal of the breast cancer resistance protein.

Disclosed are compounds of Formula (I):

or a salt thereof, wherein: Z is CR₆R₆ or C═O; Ring A is:

and R₁, R₂, R₃, R₄, R₅, m, and n are defined herein. Also disclosed are methods of using such compounds to inhibit Helios protein, and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.

The invention belongs to the field of biomedicine and functional food, and particularly relates to a method for rapidly preparing linseed polysaccharide with antiviral and immunomodulatory activities.The method for rapidly preparing linseed polysaccharide with the antiviral and immunomodulatory activities comprises the following steps: 1) separation of linseed hulls and kernels; 2) extraction oflinseed polysaccharide; 3) deproteinization and alcohol precipitation; 4) column chromatography purification. The method for preparing linseed polysaccharide FHP-2 is simple, efficient and rapid, andcan be popularized as a general process for preparing linseed polysaccharide, and the novel linseed polysaccharide FHP-2 has anti-hepatitis B virus and immunomodulatory activities and has the potential to be developed into novel drugs and functional food additives.

The invention belongs to the technical field of pharmacy, and relates to an application of a dendrobium nobile water extract in treating type 2 diabetes mellitus, in particular to regulation of insulin resistance and triglyceride synthesis of a dry dendrobium water extract and a fresh dendrobium water extract in a high-sugar state. Experimental results prove that the dendrobium nobile water extract prepared by the invention can obviously inhibit the expression level of mRNA of fatty acid binding protein, improve the peripheral insulin resistance, protect the pancreatic beta cell function, increase insulin sensitivity, obviously inhibit the expression level of diacylglycerol acyltransferase mRNA, reduce the TG biosynthesis, improve the sensitivity of the body to insulin and leptin, increasethe mRNA expression level of sterol regulatory element-binding protein 1, and effectively regulate the triglyceride biosynthesis so as to achieve inhibition of type 2 diabetes mellitus from multipleaspects. Therefore, the dendrobium nobile water extract disclosed by the invention can be used for treating type 2 diabetes mellitus and has a good development prospect in the aspect of treating type2 diabetes mellitus.

The invention provides application of a gold complex in preparation of a medicine for preventing and/or treating multiple sclerosis, and belongs to the technical field of biological medicine. The gold complex has good biological safety, and can inhibit the activity of pro-inflammatory cytokine receptor related tyrosine kinase JAK1 in immune cells, regulate the differentiation of young CD4 + T cells to Th17 cells, inhibit the expression level of inflammatory factors, and prevent and treat multiple sclerosis. The gold complex molecule can prevent or treat mouse EAE, the prevention effect is up to 2/3, and the obvious mouse EAE treatment effect is shown. Gold complex molecules can enter immune cells of a central nervous system of an EAE mouse through in-vivo metabolism, and by inhibiting the activity of cell JAK1, differentiation of young CD4 + T cells to Th17 cells and secretion of IL-17 inflammatory factors are inhibited, but the activity of the immune cells is not affected.

The invention discloses application of African swine fever virus D205R and D345L genes, and particularly relates to application of the African swine fever virus D205R and D345L genes in preparation of an African swine fever virus vaccine. The African swine fever virus D205R and D345L genes can significantly inhibit virus infection induced interferon expression, and inhibit interferon stimulation gene ISGs expression. Through dual-luciferase reporter gene system detection, the invention finds that through comparison, sendai-virus-induced interferon promoter activity and interferon stimulation response element (ISRE) activity can be inhibited through expression of the D205R and D345L genes. The fluorescent quantitative PCR test finds that the expression of the D205R and D345L genes can significantly inhibit the mRNA expression level of I-type interferon IFNbeta induced by Sendai virus infection, and inhibit the expression level of interferon stimulating genes ISG15 and OASL playing an antiviral function; and in conclusion, two kinds of African swine fever virus proteins with the function of inhibiting host cell antiviral innate immune response are identified, and a new choice is provided for preparing an African swine fever virus gene deletion vaccine.

The present invention discloses a class of shRNAs used for inhibiting replication of African swine fever viruses. The shRNAs contain two shRNA sequences such as SEQ ID NO.1 and SEQ ID NO.2. The present invention also provides a use of the aforementioned shRNAs in inhibiting the replication of the African swine fever viruses. The present invention also provides a recombinant expression vector containing the aforementioned shRNAs, and an adeno-associated virus (AAV) and a preparation method thereof. The provided shRNAs and recombinant AAV can be used to prepare drugs for preventing and/or treating African swine fever virus infection, such as therapeutic vaccines and can also effectively inhibit the replication and infection of the African swine fever viruses, and the preparation process is simple and conducive to large-scale production and promotion and application.

The invention relates to application of a protein SPINK7 in preparation of a medicine for promoting healing of an excessive-inflammation wounded area. According to the application, an excessive inflammatory reaction of a wounded area of skin can be effectively inhibited, healing of wounded areas, particularly a diabetes wounded area is promoted, a way is provided for promoting healing of chronic inflammatory wounded areas, particularly the diabetes wounded area, and thus, the application has a good application prospect.

The invention provides a histamine receptor inhibitor and derivatives thereof in the preparation of anti-Zika virus drugs. The histamine receptor inhibitor is preferably one or more of mebhydrolin napadisylate, ketotifen fumarate, flunarizine hydrochloride, cyproheptadinehydrochloride, JNJ-7777120, desloratadine, brompheniramine maleate, brompheniramine maleate, chlorpheniramine maleate and cetirizine hydrochloride. The invention brings forward for the first time that the histamine receptor inhibitor and its derivatives have clear anti-Zika virus effect and can significantly inhibit the expression level of Zika virus protein and Zika virus RNA. The invention also screens out histamine receptor inhibitors with better inhibitory effect on Zika virus, including mebhydrolin napadisylate, cyproheptadinehydrochloride, JNJ-7777120, desloratadine, etc., whose inhibition effect on Zika virus at a concentration of 10 uM is equivalent to inhibition effect of ribavirin at a concentration of 40 uM.The histamine receptor inhibitor and the derivatives can be used as good candidate drugs for anti-Zika virus drugs.

The invention belongs to the technical field of pharmacy, and relates to application of a fresh dendrobe aqueous extract in preparation of drugs for treating metabolic diseases. The invention particularly relates to adjustment of fatty acid and triglyceride synthesis by a fresh dendrobe aqueous extract. Experimental results prove that the fresh dendrobe aqueous extract prepared by the invention can obviously inhibit the mRNA expression level of sterol regulatory element binding protein 1, diacylglycerol acyltransferase and microsome triacylglycerol transporter, and effectively regulate the biosynthesis of triglyceride; and the fresh dendrobe aqueous extract can obviously inhibit the mRNA expression levels of acetyl-CoA carboxylase, fatty acid synthase and stearoyl-CoA desaturase, and effectively regulate fatty acid synthesis; and the fresh dendrobe aqueous extract can inhibit the mRNA expression level of the FABP4, improve the peripheral insulin resistance, protect pancreatic beta cellfunctions, and improve the sensitivity of insulin, thereby inhibiting the metabolic diseases related to the FABP4; and therefore, the fresh dendrobe aqueous extract prepared by the method can be usedas the drug for treating the metabolic diseases.

The invention relates to the field of molecular genetics and biomedicines, in particular to a shRNA for specifically reducing human Aurora-A gene expression and application of the shRNA. The invention provides hairpin interference RNA (ribonucleic acid) for specifically reducing human Aurora-A gene expression, shown by SEQIDNO. 1; an aimed target sequence is the 995th-1015th bit of human Aurora-AmRNA, shown by SEQIDNO. 2; the shRNA can be sheared in vivo or in vitro to form siRNA shown by SEQIDNO. 4 and SEQIDNO. 5; the invention further provides a DNA (deoxyribonucleic acid) oligonucleotide chain for coading the shRNA, shown by SEQIDNO. 3, and a plasmid including the DNA oligonucleotide chain shown by SEQIDNO. 3. According to the invention, after medicines of Aurora-A-shRNA interference carriers transfect human esophageal cancer cells EC9706, an mRNA transcriptional level and a protein expression level of Aurora-A genes in cells are significantly reduced so as to significantly reduce invasiveness of esophageal cancer cells and prompt apoptosis of esophageal cancer cells irradiated and induced by UV (ultra violet), thereby overcoming the defect that the siRNA chemically synthetized in vitro has short acting time, and providing a new way for developing novel antitumor drugs.

The invention discloses a new use for an ER (estrogen receptor) antagonist, wherein the new use is an application in preparation for a medicine used for treating the paclitaxel resistance of tumour cells, the tumour is breast cancer, and the ER antagonist is ER antagonist ICI182,780. Experiment confirms that the high-level expression of ER (estrogen receptor) is an important related index of the medicine resistance of breast cancer cells; the ER antagonist has the advantages of inhibiting the expression level of ER protein and blocking the influence of estrogen on the occurrence and development of breast cancer; and the new use for the ER antagonist exerts good function of reversing the medicine resistance of tumour in paclitaxel-resistant breast cancer cell model, and has wide application prospect in medicine used for treating the paclitaxel resistance of human breast cancer.

The invention relates to a PDGFR-beta gene expression inhibitor. The inhibitor contains at least one of an mPG molecule and an mPG molecule modified with a cell delivery carrier. The PDGFR-beta gene expression inhibitor contains at least one of mPG molecules and mPG molecules modified with a cell delivery carrier, delivery of the mPG molecules in cells is achieved, PDGFR-beta notch G-quadruplex can be specifically recognized and stabilized in the cells through the mPG molecules, and therefore gene expression of the PDGFR-beta gene expression inhibitor can be regulated in the cells. The expression level of the gene is inhibited.

The invention discloses a novel biomarker for early abortion diagnosis, and particularly relates to a method for diagnosing, predicting and/or monitoring early abortion by hsa-miR-29a-3p and application of hsa-miR-29a-3p. According to the invention, hsa-miR-29a-3p is proposed as a marker for early pregnancy embryo implantation and bad pregnancy outcome for the first time, and then the regulation effect of hsa-miR-29a-3p on decidualization is proved by using an in-vitro endometrial stromal cell decidualization model. The temporal-spatial expression specificity based on the marker has wide clinical diagnosis and prediction application prospects. According to the specific expression of the hsa-miR-29a-3p in different pregnancy periods and in decidua tissues of early abortion, the early abortion of pregnancy can be effectively predicted and diagnosed.

The invention discloses an inhibitor for knocking down circXPO1 and application of the inhibitor in preparation of a medicine for treating glioma. At present, the research reports that the expression of circXPO1 is related to osteosarcoma, lung adenocarcinoma and prostate cancer, and the related effect of circXPO1 on malignant glioma is not reported. According to the invention, a pair of shRNAs is designed according to the splicing site of circXPO1, and the shRNAs can significantly inhibit the expression level of circXPO1 and can inhibit the activity, proliferation and migration of glioma.

The invention discloses a preparation method and application of an oral microsphere carrying a small molecular nucleic acid drug. The preparation method comprises the following steps of: step 1, preparing a cationized konjac polysaccharide solution, and adding a small molecular nucleic acid drug solution to obtain a stable nano nucleic acid drug; step 2, preparing a biodegradable carrier solution,mixing the nano nucleic acid drug in the biodegradable carrier solution as an internal phase, generating liquid drops under the shearing action of an immiscible external phase fluid by adopting a microfluidic device, and polymerizing or curing to obtain the microsphere carrying the nano nucleic acid drug; and step 3, loading a preset amount of Eudragit colon-soluble aqueous dispersion coating liquid into coating equipment, and coating the microsphere carrying the nano nucleic acid drug by using the coating equipment to obtain the oral microsphere carrying the small molecular nucleic acid drug. The preparation method disclosed by the invention has the advantages of being flexible, low in cost, simple and easy to operate, safe and reliable, capable of effectively improving the bioavailability and targeting property of the small molecular nucleic acid drug, and the like.