22 results about "Elemene" patented technology

The invention belongs to the technical field of medicines, and particularly relates to a beta-elemene tryptophan methyl ester derivative and application thereof in preparation of antitumor drugs. According to the beta-elemene tryptophan methyl ester derivative with the structure as shown in the formula (I), on the basis of maintaining a beta-elemene structural framework, a tryptophan methyl ester group is introduced to the 13th site of beta-elemene, and unsubstituted C3-7 heterocycloalkyl, substituted C3-7 heterocycloalkyl, unsubstituted C5-11 hetero-spirocycloalkyl or substituted C5-11 hetero-spirocycloalkyl is introduced to the 14th site of beta-elemene, so that the beta-elemene tryptophan methyl ester derivative with the structure as shown in the formula (I) is obtained. The water solubility and the pharmacokinetic property of the compound are effectively improved. Experimental results show that the anti-tumor activity of the beta-elemene tryptophan methyl ester derivative with the structure as shown in the formula (I) provided by the invention is obviously enhanced compared with that of beta-elemene. Formula (I).

Disclosed are a 14-chloro-β-elemene nitric oxide donor derivative and a preparation method and use thereof in the preparation of anti-tumor drugs. The 14-chloro-β-elemene nitric oxide donor derivative has a general formula shown in formula (I): in formula (I): R1 represents a linear or cyclic alcohol amine structure containing nitrogen and oxygen atoms; and each of R2 and R3 is independently selected from the group consisting of C1-10 alkyl, C3-12 cycloalkyl, C6-12 aryl, 5- to 10-membered cyclic heteroaryl, C2-10 alkenyl, C2-10 alkynyl, and C2-10 alkoxy.

The invention provides the synthetase of the (-)-gemmarene A and the preparation method of the synthetase, and the synthesis of the (+)-beta-elemene is effectively realized.

This invention belongs to the field of pharmaceutical technology, specifically relating to a series of novel Procaspase-3 activators and their application in the preparation of various malignant tumor drugs. One novel Procaspase-3 activator is a compound of Formula 1 and its salt. The β-elemene-structured Procaspase-3 activator described in this invention aims to activate the activity of Procaspase-3, which is highly expressed in various tumor cells, and induce tumor cell apoptosis restart. These new compounds exhibit stronger physiological activity and stability.

The application discloses a hydrophobic temperature-sensitive mesoporous silica drug delivery system and a preparation method and application thereof, and the drug delivery system takes copper sulfide nanoparticles as a core, takes amino-modified hydrophobic mesoporous silica as a shell, and is coated with a surface coating of a temperature-sensitive polymer PEG-p(AAm-co-AN), wherein the hydrophobic mesoporous silica is prepared from silane coupling agent A151 containing a carbon-carbon double bond and a silicon source TEOS; the drug delivery system has photothermal effect and upper critical solution temperature responsiveness, can load a large amount of hydrophobic drugs such as beta-elemene, and can realize controllable release under 980nm near-infrared light irradiation. The phase transition temperature of the delivery system is 43 DEG C, so that the combination of photothermal therapy and chemotherapy can be realized while the drug release is controlled, so as to achieve more effective tumor inhibition. In addition, the preparation method is simple and has wide application prospect.

This invention relates to the field of antitumor drug technology, and discloses a cervical cancer treatment composition based on β-elemene and its preparation method. The composition comprises β-elemene, dimethyl sulfoxide (DMSO), and a diluent matrix; wherein the final concentration of β-elemene is 10 μg / mL to 50 μg / mL, and the volume percentage of DMSO is constant at 0.4% to 0.6%. The preparation method includes preparing a stock solution and preparing the final product. By dynamically adjusting the volume of DMSO added, the total amount of solvent in the composition at different drug concentrations remains constant, thus establishing a strict single-variable evaluation system for in vitro drug delivery. This invention effectively eliminates the cytotoxicity additive interference caused by fluctuations in the amount of solubilizer in conventional drug delivery systems, prevents the aggregation and precipitation of poorly soluble components in the aqueous phase, and can objectively and accurately reflect the true pharmacological activity of β-elemene in inhibiting cervical cancer cells and inducing ferroptosis.

The invention relates to the fields of biochemical engineering, synthetic biology and biological medicine, in particular to a gemmarene A synthetase mutant, a fusion protein, an engineering strain and application. According to the invention, the GASX-L1H2H3V436LH4 with the highest catalytic activity is successfully obtained by means of point mutation and structural domain substitution; compared with wild type LTC2 and HaGAS1, the enzyme has the advantages that the catalytic activity is obviously improved, the fusion protein HaGAS1GGGSERG20 is constructed through a flexible linker, and the beta-elemene synthesis efficiency is further improved; on the basis, by strengthening a cytoplasm MVA pathway and constructing a peroxisome MVA pathway, intracellular precursor substances and acetyl coenzyme A are fully utilized, and the yield of elemene is further increased; on the basis, genes related to grease metabolism are screened to find overexpressed TGL4, and the shake flask yield of elemene is further increased.

The invention discloses a fertilizer for curcuma zedoary and a fertilization method, belongs to the technical field of plant fertilization, and solves the problem of how to increase the content of elemene in the curcuma zedoary. Comprising the following steps: S1, preparing a fertilizer for fertilizing curcuma zedoary in advance; s2, when curcuma zedoary seed stems are planted, base fertilizer is applied to gaps between the adjacent seed stems, soil covering and ridging are carried out, and enzyme liquid fertilizer is sprayed; s3, topdressing is conducted on the curcuma zedoary, topdressing is conducted three times, and when topdressing is conducted each time, corresponding enzyme liquid fertilizer is sprayed. By standardizing curcuma zedoary planting and scientifically fertilizing, the yield of curcuma zedoary is increased, and more high-quality raw materials are provided for elemene extraction, so that the yield of elemene is increased; the fertilizer obtained through a proper proportion promotes growth of curcuma zedoary and improves the yield and quality of curcuma zedoary. The curcuma zedoary is subjected to three times of additional fertilization, corresponding enzyme liquid fertilizer is sprayed during each time of additional fertilization, and the yield of the curcuma zedoary is increased by reasonably matching fertilization.

The invention relates to a beta-elemene concentrated preparation for injection, which has the characteristics of simple process, environmental friendliness, suitability for industrialization, lower cost and the like. The concentrated preparation for beta-elemene injection is prepared from the following components: beta-elemene, soybean oil, polyethylene glycol 15 hydroxystearate, egg yolk lecithin, polysorbate and the balance of absolute ethyl alcohol.

The invention discloses application of TRPV1, NUDT9 and MT-ND5 as targets in preparation and screening of drugs for treating brain glioma, and belongs to the technical field of biology. According to the application disclosed by the invention, experiments prove that the expression of NUDT9 and MT-ND5 in brain glioma cells is knocked down, the proliferation of the brain glioma cells is reduced, TRPV1 in the brain glioma cells is knocked down, the proliferation of the brain glioma cells is promoted, the expression of NUDT9 and MT-ND5 in the brain glioma cells is reduced by beta-elemene, and the beta-elemene has the effect of inhibiting tumor growth; the application prospect of the TRPV1, the NUDT9 and the MT-ND5 serving as the target spot in screening the medicine for treating the brain glioma is shown. According to the application disclosed by the invention, the condition that the beta-elemene and the TMZ are combined to enhance DNA damage accumulation through a synergistic effect, continuously activate a cell apoptosis pathway and increase the sensitivity of glioma cells to the TMZ is determined for the first time, so that the curative effect is improved, and the toxicity is reduced.

The invention provides recombinant yarrowia lipolytica for producing beta-elemene in a subcellular compartment and a construction method and application of the recombinant yarrowia lipolytica, and belongs to the field of bioengineering. The recombinant yarrowia lipolytica is prepared by taking yarrowia lipolytica as an original strain, performing localization expression on a germacene A synthase coding gene in a liposome through a liposome localization signal Oleosin, and knocking out a peroxisome biogenic factor 10 in a yarrowia lipolytica genome, so as to obtain the recombinant yarrowia lipolytica. And inserting into a 3-hydroxy-3-methylglutaryl CoA reductase expression cassette, a farnesyl pyrophosphate synthase expression cassette, an isopentenyl pyrophosphate isomerase expression cassette, a diacylglycerol acyltransferase expression cassette and a sterol acyltransferase expression cassette to obtain the recombinant expression vector. The recombinant yarrowia lipolytica disclosed by the invention can be used for efficiently producing beta-elemene.

The application relates to the technical field of biological medicine manufacturing, and discloses a controlled-release type preparation composition for realizing ovary function recovery, which comprises a core active unit, a moisturizing slow-release unit and a plant extract component. The core active unit is an anisotropic core-shell structure microcapsule with asymmetric charge distribution, which is composed of chitosan, polyglutamic acid and an internal compound, and a layer of outwardly radiating carboxyl brush-shaped molecular chain is distributed on the surface of the core active unit. The moisturizing slow-release unit comprises a polymer skeleton formed by rosmarinic acid and hyaluronic acid, and the polymer skeleton internally occludes elemene. The application utilizes a kinetic restriction mechanism to construct an anisotropic surface layer topology, avoids mucus protein adsorption, induces anti-inflammatory immune regulation by physically adapting mucosal receptors, the moisturizing slow-release unit firstly constructs a physical barrier to repair damage, and the core active unit is used to realize component graded controlled release.

The invention relates to the technical field of microorganisms, in particular to a method for improving quality and insect resistance of purple perilla through inoculation of arbuscular mycorrhizal fungi, which is characterized in that the arbuscular mycorrhizal fungi are rhizosporium endophyllum, and insects are beet armyworms. The arbuscular mycorrhizal fungi are inoculated, so that the growth of the aboveground part and the underground part of the purple perilla is remarkably promoted, and the biomass of the purple perilla is improved; accumulation of linalool, perillyl alcohol, perillaldehyde, elemene, ocimene and limonene in the perilla leaves can be promoted, and the quality of the perilla is improved; the content of defense secondary metabolites such as flavone and tannin of the perilla leaf and the activity of defense enzymes such as polyphenol oxidase and phenylalanine ammonialyase can be improved, and the resistance of the perilla leaf to beet armyworms is improved. After the arbuscular mycorrhizal fungi inoculated perilla leaves are eaten, the growth and development of the beet armyworms are inhibited, and the beet armyworms show that the weight and the body length are reduced, and the developmental duration is prolonged.

The application belongs to the technical field of pharmaceutical chemistry synthesis, and relates to a PAC-1 analogue based on a beta-elemene piperazine structure and application thereof in preparation of an antitumor drug. The PAC-1 analogue based on the beta-elemene piperazine structure is a compound as shown in formula I and a salt. The Procaspase-3 activator with the beta-elemene piperazine structure is used for developing the Procaspase-3 which can be activated in various tumor cells and can induce tumor cell apoptosis restart. The derivatives have stronger physiological activity and stability.

This invention relates to an oral microemulsion containing elemene, its preparation method, and its uses. The microemulsion has a simple formulation, high drug loading capacity, good stability, and a simple preparation process, making it suitable for the prevention and treatment of gastric diseases, especially gastric cancer.

The application discloses a chamomile beta-elemene synthesis enzyme gene McTPS5 and application thereof. The beta-elemene synthesis enzyme gene McTPS5 is cloned from chamomile, the full-length cDNA sequence of the gene is shown as SEQ ID NO:1, the coding sequence is shown as SEQ ID NO:2, and the amino acid sequence coded by the gene is shown as SEQ ID NO:3. The exogenous recombinant protein of the McTPS5 gene is prepared, and after reaction in a catalytic substrate, the sesquiterpene beta-elemene can be generated, and the beta-elemene can be prepared. Meanwhile, the McTPS5 is transferred into a plant expression vector, and by exogenous transformation of plant materials, the beta-elemene plant or the transgenic material containing the sesquiterpene beta-elemene synthesis enzyme gene can be cultivated.

This invention discloses terpenoid compounds with anticancer activity and their preparation methods, belonging to the field of biotechnology. The invention employs a chemical-enzymatic method, first chemically synthesizing the natural substrate analog 7-O-FPP, and then using the sesquiterpene synthase TmS for in vitro catalysis to obtain three oxygen-containing sesquiterpene products. MTT activity assays showed that the three compounds exhibited significant anticancer activity against gastric cancer SGC7901, lung cancer NCI-H1975, cervical cancer HeLa, and esophageal squamous cell carcinoma KYSE-150 cells. Compounds 1 and 3 showed anticancer activity against various cancer cell lines. 50 The concentration of compounds below 1 μg / mL showed significantly superior activity compared to the clinical drug β-elemene; compound 2 exhibited higher activity against lung cancer cells and low toxicity to normal MRC-5 cells. This invention provides an efficient method for preparing novel terpenoid compounds, and the resulting compounds offer high-quality lead molecules for the development of new anticancer drugs, demonstrating promising application prospects.

The application belongs to the technical field of biological medicine, and discloses application of beta-elemene acid or a derivative or a pharmaceutically acceptable salt thereof in preparation of a medicine for preventing and / or treating polycystic ovary syndrome (PCOS). The beta-elemene acid is screened from a medicinal and edible homology library, and experiments prove that the beta-elemene acid can significantly improve the ovary morphology and mature follicle quantity of PCOS, normalize the estrous cycle, significantly improve the serum hormone level, and also significantly improve the glucose tolerance, insulin tolerance and body weight of PCOS. The beta-elemene acid of the application is a compound based on medicinal and edible homology, which can be used as a medicine and also as a natural ingredient of food, has low toxicity, is safe in long-term use, has low cost of safety evaluation of a relatively new synthetic compound, and can be applied to development and preparation of a medicine for preventing and / or treating PCOS or a lead compound thereof.

The invention discloses a method for detecting the content of active ingredients in magnolia wufengensis volatile oil, and belongs to the field of quality control of traditional Chinese medicines. A gas chromatograph is adopted to be equipped with a hydrogen flame ionization detector (GC-FID), a chromatographic column is Agilent VF-17 ms, carrier gas is helium, and the flow velocity is 0.8 mL / min; temperature programming; and carrying out quantitative analysis by adopting an external standard method. The GC method for simultaneously determining the content of the five active ingredients (beta-elemene, ethyl palmitate, ethyl linoleate, ethyl linolenate and squalene) in the magnolia wufengensis volatile oil is established for the first time, the method is economical, accurate and good in repeatability, and scientific basis and technical support are provided for quality control and standardized evaluation of the magnolia wufengensis volatile oil.

This invention provides a novel use of Atractylodes macrocephala essential oil for the prevention and treatment of hair loss and alopecia areata. The characteristic components of the Atractylodes macrocephala essential oil include: atractylenolide I, atractylenolide II, atractylenolide III, atractylone, β-elemene, hesperidin, and isohesperidin. The invention also provides a method for preparing essential oil compositions, pharmaceutical formulations, and uses for the prevention and treatment of hair loss and alopecia areata. This method reduces bitterness and the first-pass effect in the liver, resulting in more stable blood drug concentrations and improved patient compliance. Compared to existing methods, it has advantages such as better efficacy and no toxic side effects. Developing health products and pharmaceuticals for the prevention and treatment of hair loss and alopecia areata based on this method has great potential.

This invention relates to the field of microbial technology, specifically disclosing a recombinant yeast strain and its application in the fermentation production of β-elemene. Compared to the original yeast strain, the recombinant yeast strain of this invention expresses farnesyl diphosphate synthase ERG20, lettuce-derived sesquiterpene synthase LsLTC2, and rose-derived bifunctional farnesyl diphosphate synthase RrFPS, and expresses IDI1, ERG13, ERG8, ERG10, ERG12, MVD1, and tHMGR in peroxisomes. Preferably, the expression level of squalene synthase ERG9 in the cell matrix is ​​further downregulated, ERG10, ERG13, and IDI1 are overexpressed, and XFPK, PTA, POXB, and ACS are expressed. The recombinant yeast strain of this invention can efficiently produce β-elemene, providing a more effective method for the industrial production of β-elemene.

The invention provides application of beta-elemene in preparation of a medicine for treating and / or preventing enteritis, relates to the technical field of biomedicine, and is technically characterized by providing application of beta-elemene in preparation of a medicine for treating and / or preventing enteritis. The research reveals a brand new action mechanism of beta-elemene in the aspect of preventing radiation-induced enteritis for the first time. The natural product acts on two targets of intestinal microbiome and host cells at the same time through an original'start-fuel 'strategy, and shows unique treatment advantages. Specifically, the beta-elemene can be used for specifically enriching probiotics lactobacillus gadolinii and increasing the yield of lactic acid in intestinal tracts, and epithelial cells are protected from radiation damage by virtue of a synergistic relationship between the beta-elemene and the lactic acid, so that a complete signal channel from microbial metabolites to host cell protection is broken through. The double-boundary regulation and control mechanism breaks through a traditional single-target treatment mode, and a brand new normal form is provided for microbiome targeted therapy.