17 results about "Cytochalasin" patented technology

The invention provides cytochalasin based on soil fungi Xylaria sp. Y01 and application of the cytochalasin, and belongs to the technical field of medicinal chemistry. According to the invention, 27 kinds of cytochalains are separated from a soil fungus Xylaria sp. Y01, wherein the 27 kinds of cytochalains comprise 13 kinds of newly discovered compounds. It is explored whether these compounds have an inhibitory effect on the release of pro-inflammatory cytokines. The result shows that the compound 22 shows a remarkable anti-inflammatory effect on RAW264.7 cells by up-regulating the expression of SOCS3. Therefore, the compound 22 is expected to become a potential candidate drug for developing drugs for treating inflammatory diseases.

The invention relates to a microbial metabolite and an application technology of the microbial metabolite in the field of drug research, in particular to a cytochalasin compound as well as a preparation method and application of the cytochalasin compound. The cytochalasin compound is a compound 1 and a compound 2 as shown in a formula I, the molecular formula of the compound 1 is C29H35NO4, and the structural formula of the compound 1 is 1 in the formula I, and the molecular formula of the compound 2 is C29H37NO3, and the structural formula of the compound 2 is 2 in the formula I. The invention further discloses a preparation method of the cytochalasin compound. Experimental results show that the two compounds show anti-tumor activity on various tumor cell lines, can effectively inhibit cell proliferation, and have the potential of serving as a cell proliferation inhibitor or an anti-tumor preparation. Compared with traditional chemical synthesis, the preparation of the target compound is achieved through the microbial fermentation technology, and the method has the advantages of being simple in operation process, short in production period, low in cost and the like, is suitable for large-scale production and has important application prospects. Formula I

The invention discloses a synthetic method of a cytochalasin compound curtalasin B. The synthetic method comprises the following steps: reacting a compound 22 with dimethyl ketone peroxide in a solvent at the temperature of-35 to-20 DEG C to generate a compound 23; reacting the compound 23 with boron trifluoride diethyl etherate in a solvent at-78 to 5 DEG C to obtain a compound 24; reacting the compound 24 with vanadyl acetylacetonate and tert-butyl hydroperoxide in a solvent at 15-35 DEG C to obtain a compound 25; dissolving the compound 25 in toluene, adding tri-pentafluorophenyl boron at room temperature, heating to 80 DEG C, and reacting to obtain a compound 26; and dissolving the compound 26 in absolute methanol, adding anhydrous potassium carbonate at 0-35 DEG C, and reacting at room temperature to obtain the curtalasin B. The invention further discloses a preparation method of the curtalasin B. The method is simple to operate, simple in post-treatment, low in product separation and purification cost and high in synthesis efficiency; most of the used reagents are commercially obtained, are low in price and do not need special treatment.

The application discloses a method for fermentatively producing Aspochalasin D and belongs to the technical field of microorganisms and fermentation. The method is characterized in that the liquid fermentation conditions of Aspergillus flavipes are optimized, and a mutant strain ΔaspoA::OEaspoG strain is obtained through aspoA gene knockout and aspoG gene overexpression. The fermentative production of Aspochalasin D by using the method can make the yield of Aspochalasin D reach 812.1 mg / L. The cell relaxation Aspochalasin D obtained through the fermentation of the mutant strain of Aspergillus flavipes has various activities such as antibacterial activity and anticancer activity, and can be applied to the agricultural and pharmaceutical industries.

The invention relates to the field of organic chemical synthesis, in particular to a synthesis method of Curtaxasin A, an intermediate of Curtaxasin A and a synthesis method of Curtaxasin A. The preparation method comprises the following steps: taking cytochalasin D as an initial raw material, carrying out deacetylation reaction and epoxidation reaction to prepare an intermediate II as shown in a formula II, and carrying out trans-ring epoxy ring opening and alpha-ketol rearrangement reaction on the intermediate II to obtain Curtaxasin A. Reagents used in the method are cheap and easy to obtain, operation is easy, the total yield can reach 56%, the method is a simple, efficient and environment-friendly synthetic route of the cytochalasin A, a first way is opened up for chemical synthesis of the antifungal cytochalasin A, and the method has important significance in the field of medicine.

The invention discloses a cytochalasin compound with an anti-tumor effect as well as a preparation method and application of the cytochalasin compound. The compound disclosed by the invention is derived from a fermentation product of a cynanchum chinense endophytic fungus Aspergilusizukae RD-16. The compound disclosed by the invention has the advantages that the compound can be used for preparing the cynanchum chinense endophytic fungus; the compound has remarkable cytotoxic activity to various tumor cells and almost has no toxicity to normal colonic epithelial cells. Meanwhile, the compound also has an effect of inhibiting angiogenesis. A Western Blot experiment result proves that the compound activates the expression of tumor cell autophagy related protein by inhibiting a PI3K-AKT-mTOR signal channel and induces tumor cells to generate autophagy; on the other hand, by inhibiting expression of angiogenesis related protein p-VEGFR2, tumor angiogenesis is blocked, and the anti-tumor effect is synergistically enhanced through multiple paths. The compound has potential application in preparation of novel anti-tumor drugs, and provides scientific basis for research and development of novel anti-tumor drugs.

The invention discloses two novel cytochalasin compounds with activity of inhibiting methicillin-resistant staphylococcus aureus (MRSA) and application of the cytochalasin compounds. The invention provides a compound shown as a formula (I) or a compound shown as a formula (II). The compound shown in the formula (I) is named as a compound Aizuchalasin A. The invention further discloses a preparation method of the compound. The compound shown in the formula (II) is named as a compound Aizuchlaasin B. The formula (I) is shown in the description. The compound A and the compound B of the Aizuchalasin have the activity of inhibiting methicillin-resistant staphylococcus aureus. The invention provides a lead compound for developing a new anti-MRSA medicine, and has great value for treating MRSA infection.

The invention relates to the technical field of medical chemistry, and particularly discloses a cytochalasin compound boerelasin L with a novel skeleton type, which is separated from Boeremia exigua of Fritillaria hupehensis. Specifically, the invention relates to an application of the compound in preparation of drugs with significant inhibitory activity on NO inflammatory effect, by establishing an LPS-induced RAW264.7 cell inflammation model, the result shows that the compound has significant anti-inflammatory activity (IC50 = 8.56 [mu] M) and has no cytotoxicity, and by means of ELISA and Western Blot methods, it is found that the compound can down-regulate expression of iNOS and COX-2 and inhibit secretion of inflammatory factors IL-6 and TNF-alpha, so that the compound can be applied to preparation of drugs with significant inhibitory activity on NO inflammatory effect. The cytochalasin compound provided by the invention realizes dose-dependent inhibition of LPS-induced NO generation, and has excellent safety and patent medicine potential at the same time.

The invention relates to the technical field of medical chemistry, particularly discloses cytochalasin C containing sulfone molecules and separated from endophytic fungi Boeremia exigua of Fritillaria hupehensis and application potential of the cytochalasin C in preparation of anti-inflammatory drugs, and more particularly discloses application of the cytochalasin C in preparation of drugs with remarkable inhibitory activity on NO inflammatory effect. The cytochalasin containing the sulfone molecules shows better anti-inflammatory activity, and the IC50 value of the cytochalasin containing the sulfone molecules is 17.99 [mu] M. The compound has the advantage of efficient anti-inflammation, and NO generated by LPS stimulation can be inhibited.

The invention belongs to the technical field of shellfish genetic breeding, and particularly relates to a cultivation method of triploid offspring seeds for promoting growth of mytilus coruscus. According to the cultivation method, when the proportion of first polar bodies in fertilized eggs of mytilus coruscus accounts for 35%-40% of the total fertilized eggs, a cytochalasin B (CB) solution induces the fertilized eggs of mytilus coruscus, and then incubation and development are carried out. According to the mytilus coruscus triploid offspring seeds cultivated through the cultivation method, the triploid rate can reach 84%, the growth rate is improved by 30%-40% compared with that of diploid, larvae enter an attachment metamorphosis stage in advance, the seedling cultivation cost is greatly reduced, and a new direction is provided for industrialization development of mytilus coruscus.

The invention discloses an application of a mitochondria-rich cell disintegration body in treatment of myocardial ischemia reperfusion injury. The invention provides an application of a mitochondrial-rich cell disintegration body in preparation of a product for preventing and / or treating myocardial ischemia-reperfusion injury. The cell disintegration body is extracted from mitochondrial donor cells treated by cytochalasin D. The invention further provides a preparation method of the mitochondrial-rich cell disintegration body. The mitochondrial-rich cell disintegration body has ultrahigh mitochondrial loading capacity and functional activity and excellent in-vivo and in-vitro stability; the functional mitochondria can be efficiently delivered to a heart injury area, the myocardial protection effect is achieved by activating an endothelial cell autophagy pathway, the heart function is remarkably improved, the infarct area is reduced, and the good clinical application prospect is achieved.

The invention discloses an extracellular vesicle preparation rich in mitochondria as well as a preparation method and application of the extracellular vesicle preparation. According to the invention, stem cells are stimulated by resveratrol, so that the mitochondrial content in cells is increased; then, the stem cells are treated with cytochalasin B, and the extracellular vesicle preparation rich in mitochondria is prepared through a series of centrifugation. According to the extracellular vesicle preparation provided by the invention, the damage of mitochondria in the preparation process is effectively reduced, the yield of extracellular vesicles is improved, the mitochondria with a complete mitochondrial structure and biological activity is efficiently enriched, and the stability and effectiveness of the mitochondria in disease treatment are ensured. The extracellular vesicles provided by the invention can efficiently deliver healthy mitochondria to damaged cells, improve disease symptoms and provide a safe and efficient treatment means for diseases related to mitochondrial dysfunction.

The application discloses a construction method of aneuploid ovarian cancer cell model. The construction method of the aneuploid ovarian cancer cell model comprises the following steps: co-culturing cytochalasin D and ovarian cancer cells in a first culture medium to obtain the aneuploid ovarian cancer cell model. The cytochalasin D is used to induce the ovarian cancer cells, which can induce the diploid and near-diploid ovarian cancer cells into aneuploid ovarian cancer cells. After the aneuploid ovarian cancer cells are inoculated into nude mice, the nude mice have tumorigenicity, still maintain a high proportion of aneuploid ovarian cancer cells, and can be used for researching the occurrence and development mechanism of ovarian cancer and tumor intervention, and can also be used for researching the curative effect of a drug for treating ovarian cancer in vitro, in vivo and in clinic, and providing new test materials for researching the occurrence, development, drug resistance, metastasis and biomarker of ovarian cancer.

The invention discloses a preparation method of lactam alkaloid self-leucaena leucocephala and an application of the lactam alkaloid self-leucaena leucocephala in preparation of The antitumor active substance Cytochalasin J with high potential activity is extracted, separated and prepared from a leucaena leucocephala plant pod material, the leucaena leucocephala plant material is rich in source, extraction and preparation are easy to operate, and pharmacological experiments show that the compound Cytochalasin J has remarkable activity of inhibiting growth of central nervous system tumor cells SF-268 and breast cancer cells MCF-7 in vitro, and can be used for preparing antitumor drugs. Moreover, the monomeric compound is stable and easy to store, so that the compound has the potential of being developed and used for preparing corresponding anti-tumor drugs, or has the potential of application and development as a lead compound for developing effective low-toxicity anti-tumor drugs. Formula (1).

The application discloses a kind of based on de-nucleated stem cell's promoting repair microvesicle and its preparation method and application, including the following steps: using cytochalasin B to de-nucleate stem cell, using Percoll centrifugation or vortex method separates the stem cell cytoplast of de-nucleated stem cell, using extrusion device with filter membrane repeatedly extruding, namely de-nucleated stem cell microvesicle.The method in the application removes the nucleus of stem cell while retaining the key protein and RNA of stem cell to play the function of promoting repair, reduces the risk of dangerous gene transfer.Moreover, based on extrusion method can effectively control the particle size distribution of microvesicle, and based on the size of filter membrane pore size, the size of the prepared microvesicle is flexibly adjusted, and has significant therapeutic effect in tissue damage and the like.

The present application relates to the technical field of cell imaging, and particularly relates to a method for observing the surface structure of the nucleus of a cell. The method comprises nuclear-cytoplasmic separation and observation of the nucleus. The nuclear-cytoplasmic separation comprises cell pretreatment and centrifugal separation of cytoplasm and nucleus. The cell pretreatment comprises placing the cell in a culture medium comprising nocodazole and cytochalasin B for 1.5-3 hours; the culture medium comprises, in terms of weight parts, 0.1-0.5 parts of nocodazole and 2-10 parts of cytochalasin B. The present application provides a nuclear-cytoplasmic separation method for treating cells with nocodazole and cytochalasin B, which can quickly obtain the nucleus while improving the problems of nucleus shrinkage and collapse, and completely preserving the structure of the nucleus, which has important value in the field of observing the surface ultrastructure of the nucleus.

The application provides a preparation method of high-yield high-temperature-resistant homologous triploid Argopecten irradias, and the Argopecten irradias parent shellfish with high-temperature-resistant characteristics is screened through a molecular marker assisted breeding technology; after the parent shellfish is induced to spawn, the fertilized eggs are treated by using cytochalasin B to induce the generation of homologous triploidy, and the cleavage rate, the hatching rate, the metamorphosis rate and the triploid larva rate are comprehensively considered, so that the high-efficiency induction of the homologous triploid of the hermaphrodite shellfish is realized. The SNP site most significantly related to the high-temperature-resistant performance of the Argopecten irradias is identified through whole genome association analysis, a high-temperature-resistant molecular marker is developed, and the individual with the high-temperature-resistant genotype is screened for spawning and fertilization. The triploid larva obtained through the method has a faster growth and development speed than the common diploid larva, and the artificial breeding cost can be greatly reduced.