31 results about "Cyclic depsipeptide" patented technology

The invention relates to the technical field of biological medicine, in particular to application of cyclic dipeptide to improvement or treatment of dyslipidemia related diseases. According to the present invention, the research results show that the cyclo (glycerol-casein) dipeptide has good safety and cholesterol lowering activity, and can reduce mouse serum total cholesterol, low density lipoprotein cholesterol, increase serum high density lipoprotein cholesterol, reduce the content of liver total cholesterol, reduce liver fat accumulation, and slow down the weight increase of mice. The cyclic (glycerol-casein) dipeptide can realize the effect of lowering cholesterol by regulating intestinal flora. The cyclic (glycerol-tyrosine) dipeptide is derived from probiotics, food and medicines, belongs to food-borne cyclic dipeptide, and is high in safety and small in toxic and side effects. The cyclo (glycerol-casein) dipeptide is expected to be developed into a class of innovative medicines and health-care foods with the effect of reducing cholesterol, and has a very good application prospect. The invention also provides the cyclic (sweet-tyrosine) dipeptide and a health food and a pharmaceutical composition containing the cyclic (sweet-tyrosine) dipeptide.

The invention discloses a diketopiperazine heterodimer as well as a biosynthesis method and application thereof, and belongs to the technical field of bioengineering. The biosynthesis method of the diketopiperazine heterodimer comprises the following steps: S1, culturing a recombinant cell containing P450 dimerization enzyme or a mutant thereof, and performing induced expression to obtain a whole-cell culture; and S2, adding a cyclic dipeptide substrate containing tryptophan into the whole-cell culture, carrying out a catalytic reaction, and separating and purifying the obtained product to obtain the diketopiperazine heterodimer. According to the invention, the P450 dimerization enzyme or the mutant thereof is used for catalyzing the biosynthesis of the tryptophan-containing diketopiperazine into the diketopiperazine heterodimer with different regioselectivity / stereoselectivity, the biosynthesis method is green and environment-friendly, the efficiency is high, and the variety of the diketopiperazine heterodimer is greatly expanded.

The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

The invention discloses a peptide with an anti-photoaging effect as well as a preparation method and application of the peptide. The cyclic dipeptide cyclo (LO) and the linear dipeptide LO disclosed by the invention can be used for remarkably inhibiting the activity of MMP-1 and efficiently blocking collagen degradation. In addition, the cyclic dipeptide and the linear dipeptide have no cytotoxic effect when being co-cultured with fibroblasts, so that the cyclic dipeptide and the linear dipeptide have no stimulation and side effects on cells, and are high in safety and good in stability. The cyclic dipeptide and the linear dipeptide disclosed by the invention can resist UVA (Ultraviolet A) damage, have a promoting effect on cell proliferation activity after UVA irradiation and have an anti-aging effect on cells after UVA irradiation. The two peptides disclosed by the invention can be used for preparing medicines or cosmetics for resisting light aging, resisting aging, beautifying and protecting skin. The peptide fragment disclosed by the invention has a good application prospect in the fields of medicines, cosmetics and the like.

The invention discloses preparation of p-methyl peptide and application of the p-methyl peptide in agriculture, and relates to the field of preparation of p-methyl peptide and application of the p-methyl peptide in plants, and the preparation method comprises the following steps: step 1, feeding and device building: adding a preset amount of L-alanine and ethylene glycol into a 250mL single-mouth round-bottom flask. As a natural cyclic dipeptide, the p-methyl peptide shows an excellent environment-friendly characteristic in plant stress resistance application. Compared with a traditional method depending on chemical fertilizers and pesticides, the method has the advantages that the method is non-toxic and harmless, soil hardening and water eutrophication caused by excessive use of the chemical fertilizers are avoided, quality safety of agricultural products is not affected as pesticide residues exceed the standard, and damage to non-target organisms and damage to ecological balance are avoided; the problem of environmental pollution caused by a traditional method is avoided from the source, and powerful support is provided for agricultural ecological environmental protection.

This invention provides the application of a cyclic dipeptide in inhibiting the TRPV1 protein, wherein the cyclic dipeptide is a cyclic (D-leucine-L-proline) dipeptide. This invention also relates to the application of the cyclic dipeptide in the preparation of topical skin agents or pharmaceuticals with TRPV1 protein inhibitory activity, wherein the topical skin agent is selected from: creams, lotions, gels, toners, serums, masks, eye creams, aerosol cleansing foams, sprays, shower gels, or facial cleansers.

The invention belongs to the technical field of gene engineering, and particularly relates to an NRPS gene, a vector and construction and preparation of a high-yield cyclic dipeptide compound recombinant strain of the NRPS gene. According to the invention, an NRPS core gene is excavated from a sea squirt-derived fungus Diapothesp.SYSU-MS4722, a recombinant strain is constructed by using the gene and using Aspergillus oryzae as a heterologous expression host, the cyclic dipeptide natural product cyclo (Phe-Ala) is successfully separated, and the yield can reach 110 mg / L, which is increased by 20 times compared with the yield of cyclo (Phe-Ala) in reported marine bacteria Pseudomonasputida. Therefore, the aspergillus oryzae recombinant strain disclosed by the invention can be used for efficiently preparing the cyclic dipeptide compound cyclo (Phe-Ala) and has an important application value.

The invention relates to a pyridazinic acid unit-containing cyclic ester peptide compound, a preparation method thereof, a pharmaceutical composition containing the compound, application of the compound in preparation of a medicine for inducing rupture and death of a tumor cell membrane, and application of the compound in preparation of a medicine for activating tumor immune response, and particularly relates to a pyridazinic acid unit-containing cyclic ester peptide compound and a pharmaceutical composition containing the pyridazinic acid unit-containing cyclic ester peptide compound. The invention also relates to application of the compound in preparation of medicines for treating diseases related to cell death in organisms.

The invention discloses an application of cyclic dipeptide in preparation of drugs for treating diseases related to damage of calcium-sensitive receptors, the dipeptide can directly activate CaSR activity of damaged organ cells in a targeted manner, and can enter the cells to promote expression of CaSR upstream genes, so that the related diseases caused by damage of CaSR are effectively reversed. Animal experiments prove that Cyclo (L-Pro-L-Trp) can effectively improve the symptoms of hypocalcemia, intestinal tract calcium absorption damage, parathyroid hormone excessive secretion, osteoporosis and the like caused by CaSR damage, and non-target organ toxicity is controllable (liver and kidney function indexes are not obviously changed). Cell experiments prove that Cyclo (L-Pro-L-Trp) can effectively activate CaSR of parathyroid gland main cells and intestinal epithelial cells and various calcium ion internal flow channels and promote proliferation of the parathyroid gland main cells and the intestinal epithelial cells.

The application relates to a DPPBA-assisted proline-based cyclic dipeptide homogeneous synthesis method and biological activity application, and belongs to the technical field of organic synthesis. The application utilizes the auxiliary precipitation of DPPBA as a carrier to perform solution homogeneous coupling reaction and Fmoc removal strategy with equivalent amounts of protected amino acids, and optimizes and simplifies the preparation method of proline-based cyclic dipeptides and derivatives and the biological activity application of proline-based cyclic dipeptides.

A fungicidal composition comprising a component A comprising a cyclic depsipeptide Aureobasidin A or a stereoisomer thereof, and a component B comprising a bacterium Bacillus amyloliquefaciens. A method of controlling or preventing phytopathogenic diseases or phytopathogenic fungi on a plant or on propagation material thereof, the method comprising applying the composition to the plant, locus thereof, or propagation material thereof. A use of the composition as a fungicide.

The application discloses an Aspergillus strain and application of a cyclic depsipeptide compound of the Aspergillus strain, and belongs to the technical field of microorganisms.The strain is Aspergillus sp BTBU20212048, and the preservation number is CGMCC NO.40328.The application further discloses application of the Aspergillus strain, and a cyclic depsipeptide compound is obtained through fermentation, extraction, separation and chromatography.The cyclic depsipeptide compound is stable in structure, has inhibiting effect on Candida albicans, and has a minimum inhibiting concentration of 200 μg / mL; and when the compound is used in combination with rapamycin, the minimum inhibiting concentrations of the two can be reduced.

The invention discloses a method for extracting cyclic dipeptide from mussels, the extracted cyclic dipeptide and application of the cyclic dipeptide, and belongs to the technical field of food science and engineering. According to the method disclosed by the invention, the problems that the content of cyclic dipeptide in a natural matrix is low, the separation efficiency is poor and a high-purity monomer is difficult to obtain in the prior art are solved through a synergistic purification strategy of double-enzyme step-by-step enzymolysis, organic solvent extraction and binary / ternary silica gel column gradient elution. The method is stable in process, good in reproducibility and high in extraction purity. Cell experiments prove that the obtained cyclic dipeptide (especially cyclic (proline-leucine)) has remarkable antioxidant and anti-aging activity, and a technical support and an experimental basis are provided for developing marine-derived functional foods and health-care products.

The invention provides application of cyclic dipeptide to regulation of cytokines and preparation of anti-inflammatory soothing cosmetics, and belongs to the technical field of cosmetics. In a cell factor network participating in the inflammation process, key media such as TNF-alpha, IL-1beta, IL-6 and IL-10 play an important role in the skin level, and the cyclo (glycine-L-proline) dipeptide can regulate release of the cell factors or limit the effect of the cell factors, so that the cyclo (glycine-L-proline) dipeptide can have anti-inflammatory and soothing effects. According to the cosmetic disclosed by the invention, the cyclic dipeptide is added, so that the anti-inflammatory and soothing effects of the cosmetic can be greatly improved, at least one effect of reducing erythema, reducing percutaneous water loss, relieving stabbing pain and reducing an after-sun erythema index is realized, and the cosmetic disclosed by the invention can be suitable for sensitive skin.

A fungicidal composition comprising a component A comprising a cyclic depsipeptide Aureobasidin A or a stereoisomer thereof, and a component B comprising thymol. A method of controlling or preventing phytopathogenic diseases or phytopathogenic fungi on a plant or on propagation material thereof, the method comprising applying the composition to the plant, locus thereof, or propagation material thereof. A use of the composition as a fungicide.

The present invention addresses the problem of providing a new means for imparting tolerance to environmental stress such as salt stress, particularly providing a means for imparting tolerance to environmental stress to plants by using a cyclic cyclodipeptide that is a 2,5-diketopiperazine derivative.　The present invention provides: a plant environmental stress tolerance enhancer composed of a cyclodipeptide that contains phenylalanine and / or leucine, and / or a salt of said cyclodipeptide; a composition for imparting tolerance to environmental stress to plants, the composition containing the aforementioned enhancer; and a seed containing the aforementioned composition on the surface and / or in the interior thereof.

The invention discloses a Liupao tea quality evaluation method, which comprises: carrying out solvent extraction on a Liupao tea sample, and carrying out centrifugal filtration to prepare a test sample solution; carrying out gradient elution separation on components in the test solution, and carrying out positive ion mode detection by adopting mass spectrometry to obtain original data containing primary mass spectrometry and secondary mass spectrometry; and deconvolving the original data into an abf format file, uploading the abf format file to MS-DIAL software, performing normalization processing to form an mgf format file and a peak area table, and representing the generated chemical nodes through a GNPS online analysis platform. 249 flavonoid compounds, 16 polypeptide compounds and 5 cyclic dipeptide derivatives are rapidly found and identified, and flavor and active substances in Liupao tea are rapidly and comprehensively analyzed.

Disclosed herein include methods, compositions, and kits suitable for use in preventing, slowing the progression of or treating obesity and weight controlling. The method can comprise administering to a subject a composition comprising a neurokinin 1 receptor (NK1R) antagonist (e.g., aprepitant) and a cyclic dipeptide (e.g., cyclo(His-Pro)).

This invention belongs to the field of bioactive peptides, specifically relating to the application of a cyclic dipeptide in promoting the growth of *Lactobacillus plantarum*. This invention provides an active cyclic dipeptide, Cyclo(Leu-Pro), which promotes the growth of *Lactobacillus plantarum*, shortens the lag phase of *Lactobacillus plantarum* in harsh environments, accelerates its growth rate, and enhances the stress resistance of *Lactobacillus plantarum*.

The invention relates to the technical field of microorganisms, and discloses a putrefying bacterium bacteriostasis determination method of a piperazine derivative, which comprises the following steps: S1, taking endophyte bacillus coagulans of cultured pseudosciaena crocea as a research object, obtaining 9 cyclic dipeptide small molecule compounds from 30L of fermentation liquor of the endophyte bacillus coagulans, the cyclic (proline-valine) has bacteriostatic activity, the cyclic (proline-valine) has bacteriostatic activity, and the cyclic (proline-valine) has bacteriostatic activity; performing structural modification screening by taking a piperazine ring as a parent nucleus; s2, screening a solvent, washing and activating the cultured three bacteria to obtain a bacterial suspension, and culturing and observing the bacterial suspension; s3, determining the maximum solubility of the compound by using a dynamic method; s4, completing a compound sensitivity experiment in a sterile environment; and S5, determining the minimum inhibitory concentration by using a broth dilution method. The research on the antibacterial structure-function relationship of the diketopiperazine compound further finds that the 1-Boc-4 (piperidine-4-yl)-piperazine and the 1-cyclopropyl methyl piperazine have good antibacterial activity on the three indicator bacteria, and have the potential value of being developed into preservatives and preservatives.

The invention provides an application of natural cyclic dipeptides in preparation of a radiation-induced oral mucositis treatment preparation, and relates to the technical field of biological medicine.In the embodiment of the invention, network pharmacology and molecular docking show that key natural component cyclic dipeptides such as cyclo-(pro-tyr), cyclo-(phe-pro) and cyclo (L-Pro-L-Val) of periplaneta americana are combined with key targets such as AKT1, GAPDH and IL1beta, and therefore the radiation-induced oral mucositis treatment preparation is obtained. Tissue inflammatory response in RTOM is inhibited through NF-kappa B, PI3K / AKT and other pathways, cell apoptosis is reduced, infection is resisted to relieve tissue damage, and tissue healing is promoted by promoting cell proliferation and migration. And a theoretical basis is provided for application of the natural cyclic dipeptide in preparation of a radiation-induced oral mucositis treatment preparation.

The invention belongs to the technical field of natural medicine development, and relates to preparation of I-IV cyclic dipeptide compounds and application of the I-IV cyclic dipeptide compounds in antibacterial medicine development. According to the invention, cyclic dipeptide compounds with antibacterial activity are separated from a crude extract of fungus Hormonema dematioids, and the cyclic dipeptide compounds are respectively a compound cyclic (D-isoleucine-D-valine) dipeptide (I), a compound cyclic (D-alanine-D-valine) dipeptide (II), a compound cyclic (L-proline-glycine) dipeptide (III) and a compound cyclic (D-alanine-D-phenylalanine) dipeptide (IV). An antibacterial test proves that the compound has a remarkable inhibiting effect on human pathogenic bacteria staphylococcus aureus, and the cyclic dipeptide compound can be used as a pharmaceutical active component for preparing antibacterial drugs, especially drugs for treating diseases caused by staphylococcus aureus infection. # imgabs0 #

A fungicidal composition comprising a component A comprising a cyclic depsipeptide Aureobasidin A or a stereoisomer thereof, and a component B comprising kasugamycin or natamycin. A method of controlling or preventing phytopathogenic diseases or phytopathogenic fungi on a plant or on propagation material thereof, the method comprising applying the composition to the plant, locus thereof, or propagation material thereof. A use of the composition as a fungicide.

The present application provides the use of a cyclic dipeptide to improve barrier moisturization repair, the cyclic dipeptide is selected from the group consisting of: cyclic (L-leucine-L-proline) dipeptide, cyclic (D-leucine-L-proline) dipeptide or a combination thereof. The improved barrier moisturization repair of the present application is achieved by promoting the expression of skin barrier-related factors FLG, AQP3, LOR and / or IVL. The present application also relates to the use of a cyclic dipeptide in the preparation of a skin external preparation having the effect of improving barrier moisturization repair, the skin external preparation is selected from the group consisting of: a face cream, a lotion, a gel, a toner, an essence, a mask, an eye cream, an aerosol cleaning foam, a spray, a shower gel, or a facial cleanser.

The invention discloses a peach disease-resistant fresh-keeping coating based on pectin-coated cyclic dipeptide as well as a preparation method and application of the peach disease-resistant fresh-keeping coating. The cyclo (tyrosine-proline) is disclosed for the first time, can significantly inhibit the growth of the botryodispora cacao hypha, is high in biological safety, is prepared into a novel high-safety and high-efficiency disease-resistant fresh-keeping coating in a pectin coating manner, and has the application prospect of replacing traditional chemical pesticide for prevention and treatment.

This invention discloses the use of cyclic dipeptides in the preparation of drugs for the prevention / treatment of metabolism-related inflammatory diseases, belonging to the field of biomedical technology. The cyclic dipeptide has the following structural formula and molecular formula C1. 18 H 18 N2O2, with a molecular weight of 294.35 Da, is an ADCY7 inhibitor. It inhibits ADCY7 protein expression by binding to ADCY7, thereby playing a role in the prevention / treatment of diseases such as fatty liver associated with metabolic dysfunction. It is composed of natural amino acids, has good biocompatibility, low immunogenicity, and few toxic side effects, and has good safety. It overcomes the defect of easy degradation in vivo of traditional linear peptide drugs and has broad prospects for the development of indications.