9 results about "Micafungin" patented technology

The invention discloses a recombinant genetically engineered bacterium for producing a micafungin precursor FR901379 and an application of the recombinant genetically engineered bacterium. The recombinant genetically engineered bacterium for producing the micafungin precursor FR901379 is obtained by performing overexpression on an epigenetic modification factor in a phomopsis sheathing genome and performing screening to obtain the recombinant genetically engineered bacterium for producing the micafungin precursor FR901379. The epigenetic modification factor comprises a histone methyltransferase (Dot 1), a histone methyltransferase (Set2) or a histone deacetylase (Rpd3). The yield of FR901379 produced by the engineering strain is increased by 40% compared with that of an original strain. The method disclosed by the invention has the characteristics of simplicity and convenience in operation, high transformation efficiency and good genetic stability.

The invention discloses an application of micafungin in preparation of a medicine for inhibiting fungi, and an application of micafungin and trifloxystrobin combined medicine in preparation of a medicine for inhibiting fungi, especially an inhibition effect on magnaporthe oryzae. Research finds that micafungin has an inhibition effect on magnaporthe oryzae. Micafungin and trifloxystrobin are combined for use and have a synergistic effect, so that the drug resistance of the trifloxystrobin drug-resistant magnaporthe oryzae can be overcome, and the antibacterial effect on the magnaporthe oryzae is improved. Research finds that micafungin has a broad-spectrum antifungal effect and also has an inhibition effect on botrytis cinerea, fusarium moniliforme, linseed fungus and other fungi besides the inhibition effect on magnaporthe oryzae.

The invention discloses a preparation method and application of a 1-(2-((3-methoxy-2-(6-methoxyquinoline-3-yl)-3-oxoethyl) amino)-2-oxoethyl) piperidine-4-formamide compound. The structure of the compound is shown as a general formula 1, wherein R in the formula is various substituted aromatic rings, thiazole, naphthalene rings, aliphatic chains and the like. An enzyme inhibition activity experiment result shows that part of the compounds have a relatively strong inhibition effect on chitin synthetase and also have a relatively strong inhibition effect on fungi such as candida albicans, aspergillus flavus, cryptococcus neoformans and aspergillus fumigatus. A drug resistance activity test result shows that part of the compounds have certain inhibitory activity on variant thalli such as fluconazole-resistant candida albicans, fluconazole-resistant cryptococcus neoformans and micafungin-resistant candida albicans, and have the potential of coping with the drug resistance problem. The compounds are simple and cheap in preparation raw materials and simple and convenient in synthesis method, and can be used as lead compounds for designing antifungal drugs.

The application discloses application of micafungin in preparation of a medicine for inhibiting fungi, and application of combination of micafungin and trifloxystrobin in preparation of the medicine for inhibiting fungi, especially for inhibiting Magnaporthe grisea. It is found by the application that micafungin has an inhibiting effect on Magnaporthe grisea. The combination of micafungin and trifloxystrobin has a synergistic effect, can overcome the drug resistance of Magnaporthe grisea with trifloxystrobin resistance, and improve the antibacterial effect on Magnaporthe grisea. It is found by the application that micafungin has a broad-spectrum antifungal effect, and has an inhibiting effect on other fungi such as Botrytis cinerea, Vibrio cholerae and Aspergillus niger in addition to Magnaporthe grisea.

The invention relates to the technical field of biological medicine, in particular to an antifungal pharmaceutical composition based on a (1, 3)-beta-D-glucan synthase inhibitor. In-vitro experiment results show that the antibacterial peptide LL-37 and (1, 3)-beta-D-glucan synthase inhibitors (caspofungin, micafungin, anidulafungin and iremifungin) are combined for use to achieve the effect of synergistically inhibiting candida albicans, candida auricula, candida tropicalis, candida glabrata, candida parapsilosis and candida krusei, so that the antibacterial peptide LL-37 can be combined with the (1, 3)-beta-D-glucan synthase inhibitors (caspofungin, micafungin, anidulafungin and iremifungin) to achieve the effect of inhibiting the (1, 3)-beta-D-glucan synthase inhibitors). And 3) preparing the antifungal drug by combining the 1, 2, 4, 5, 6, 7, 8, 8, 9, 10- However, the antibacterial peptide LL-37 is easily degraded by in-vivo protease, so that the expression of the antibacterial peptide LL-37 in an organism is up-regulated by adopting an antibacterial peptide LL-37 expression accelerant, and the antibacterial peptide LL-37 and a (1, 3)-beta-D-glucan synthetase inhibitor are synergistically antibacterial in the organism.

The invention discloses application of a quasi-kinesization modification inhibitor in preparation of a medicine for preventing and / or treating vascular calcification of chronic kidney diseases. The micafungin serving as a metalloid modification inhibitor inhibits osteogenic transdifferentiation of vascular smooth muscle cells, reduces the expression of an osteogenic factor RUNX2 and increases the expression of a contraction marker alpha-SMA of the vascular smooth muscle cells. Meanwhile, calcium salt deposition of vascular smooth muscle cells is remarkably inhibited. It is found for the first time that micafungin can play a role in protecting CKD vascular calcification independent of the antifungal effect of micafungin. The discovery provides a new hope for prevention and treatment of CKD vascular calcification.

Provided are a novel echinocandin drug impurity compound, a preparation method therefor, and the use thereof. Compared with the structure of drug micafungin, the echinocandin drug impurity compound has one more hydrophobic acyl side chain. The method comprises first dissolving a side chain active ester in a solvent, adding a basic catalyst, and then adding an appropriate amount of a FR179642 compound for reaction. The provided high-purity echinocandin drug impurity can be applied to quality control of the echinocandin drug as a reference standard for establishing analysis methods.

The present application relates to the technical field of biological medicine, in particular to an antifungal drug composition based on (1,3)-beta-D-glucan synthase inhibitor and application thereof. In vivo and in vitro experiments prove that the combination of endogenous antibacterial peptide LL-37 and (1,3)-beta-D-glucan synthase inhibitor (such as caspofungin, micafungin, anidulafungin, rezafungin and albaconazole) shows significant synergistic inhibitory effect on multiple drug-resistant pathogenic fungi such as Candida albicans and Candida auris. Since free antibacterial peptides are easily degraded by proteases, the present application is based on the synergistic killing mechanism of breaking the network barrier of fungal cell wall and assisting endogenous defense peptide to target cell membrane, and ingeniously uses the "antibacterial peptide LL-37 expression promoter" to actively up-regulate the synthesis of host natural peptides, which provides a new drug regimen for clinical treatment of deep fungal infection.

An aqueous pharmaceutical composition suitable for parenteral administration and having enhanced storage stability includes between about 0.1 mg / mL and about 40 mg / mL micafungin; (ii) between about 0.1 mM and 400 mM buffering agent; and (iii) between about 0 mg / mL and about 500 mg / mL tonicity adjusting agent, wherein the pH of the composition is between about 3.0 and 7.0, for example, between about 3.5 and 7.0.