35 results about "Elemene" patented technology

The invention belongs to the technical field of biological medicines, and discloses application of beta-elemonic acid or derivatives thereof or pharmaceutically acceptable salts thereof in preparation of medicines for preventing and / or treating polycystic ovarian syndrome (PCOS). The beta-elemonic acid is screened from a medicinal and edible library, and experiments prove that the beta-elemonic acid can remarkably improve the PCOS ovarian form and the number of mature follicles, normalize the disordered estrus cycle, remarkably improve the serum hormone level and further remarkably improve the sugar tolerance, insulin tolerance and weight of PCOS. The beta-elemonic acid disclosed by the invention is a compound based on homology of medicine and food, can be used as a medicine as well as a natural ingredient of food, is relatively low in toxicity, ensures the safety after long-term use, is relatively low in safety evaluation cost of a relatively brand-new synthetic compound, and can be applied to development and preparation of a medicine or a lead compound thereof for preventing and / or treating PCOS, or a health care product.

The invention discloses a saccharomyces cerevisiae recombinant strain based on a uracil metabolism gene URA3 as well as a construction method and application of the saccharomyces cerevisiae recombinant strain. The construction method comprises the following steps: taking saccharomyces cerevisiae rich in farnesyl pyrophosphate as an original strain, introducing a uracil metabolism gene URA3, synchronously overexpressing a ribosome biosynthetic gene UTP10 and an iron metabolism gene FIT3, and utilizing the uracil metabolism gene URA3 to express up-regulation correlation with the ribosome biosynthetic gene UTP10 and the iron metabolism gene FIT3, so as to obtain the farnesyl pyrophosphate-rich saccharomyces cerevisiae. The metabolic flux of the terpenoids is enhanced, and the saccharomyces cerevisiae recombinant strain for efficiently producing the terpenoids is constructed. According to the method, a metabolic network of yeast is systematically optimized, and combined regulation and control on precursor flux distribution, protein translation capability and metal ion steady state are realized, so that the microbial synthesis efficiency of sesquiterpenoids such as patchouli alcohol and beta-elemene is remarkably improved.

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).

The application discloses a elemene colon-targeting nano-capsule and a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations, and comprises a core and a pH-sensitive enteric polymer coated on the surface of the core, wherein the core comprises elemene and a self-nanoemulsifying lipid material, and the self-nanoemulsifying lipid material comprises an oil phase, an emulsifier and a co-emulsifier. The nano-capsule has small particle size, uniform dispersion, a clear capsule structure, high drug loading and high encapsulation efficiency, can protect the drug from being released in advance in the stomach and small intestine, and can be effectively delivered to the colon. Animal experiments show that the nano-capsule releases the drug in the form of nanoemulsion in simulated colon fluid, can significantly inhibit the tumor growth of in-situ tumor-bearing mice, has good biological safety, and significantly improves the anti-colorectal cancer therapeutic effect of the drug.

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 present invention discloses an engineered bacterium for producing β-elemene and its application. The recombinant bacterium provided by the present invention expresses genes for enzymes related to the IPP and DMAPP biosynthesis pathways, as well as farnesyl pyrophosphate synthase, and a mutant of the lettuce-derived germarene A synthase gene in the host Escherichia coli BL21(DE3)star. The recombinant bacterium can obtain a germarene A precursor after IPTG induction in SBMSN medium, and then generate β-elemene after high-temperature conversion. The time-to-yield reaches the highest level reported to date, providing a useful strain for the biosynthesis of β-elemene.

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 relates to the field of biochemical engineering, and discloses a post-treatment method for producing beta-elemene through liquid-liquid two-phase fermentation by using a solid drying agent, which comprises the following steps: adding 1-5% W / V of solid drying agent into an emulsion layer after fermentation to carry out step-by-step demulsification, and combining stirring and centrifugal operation, so that the recovery rate of an n-dodecane layer is increased to 79.7-81.6%; the yield of the target product beta-elemene is obviously improved. The method is suitable for the scale of shake flasks and fermentation tanks, has the advantages of simplicity in operation, low cost, high efficiency and the like, and provides an effective technical scheme for industrially producing beta-elemene raw material medicines by adopting microorganisms.

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 belongs to the technical field of quality control of traditional Chinese medicines, and relates to a thin-layer chromatography identification method and application of bighead atractylodes rhizome and an extract thereof. The invention provides two thin-layer identification methods, one thin-layer identification method takes four components such as atractylenolide I, atractylenolide II, atractylenolide III and beta-eudesmol in bighead atractylodes rhizome as index components, and the other thin-layer identification method takes three components such as atractylenone, geranene B and beta-elemene in bighead atractylodes rhizome as index components. The two methods can be used for rapidly and accurately identifying the rhizoma atractylodis macrocephalae medicinal material, the rhizoma atractylodis macrocephalae volatile oil, the volatile oil clathrate and the rhizoma atractylodis macrocephalae clathrate related preparations, are mild in condition and easy to operate, are favorable for comprehensively improving the quality control level of rhizoma atractylodis macrocephalae related products, provide feasible reference for innovation and research and development related to rhizoma atractylodis macrocephalae in each stage, and have important industrial value.

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 present invention discloses a 13-heterocyclic-β-elemene nitric oxide donor derivative, its preparation, and use. The present invention provides a 13-heterocyclic-β-elemene nitric oxide donor derivative having a structure as shown in general formula (I), or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof. The derivative of the present invention surpasses previous β-elemene nitric oxide donor derivatives in design strategy by introducing a nitrogen-containing ring structure and an NO donor that enhance antitumor activity in vivo. This significantly improves the physicochemical properties of the β-elemene nucleus and can be used to treat leukemia, among other diseases for which effective therapeutic agents are currently lacking. #imgabs0#

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.

A terpenoid synthase for producing germacrene A and application thereof.The present application relates to a germacrene A synthase AarTPS34 gene and its coding product and application.The AarTPS34 gene is cloned from folium artemisiae argyi, and the AarTPS34 gene is a key enzyme gene for synthesizing germacrene A, a sesquiterpenoid compound, which is obtained from artemisia for the first time.The experiment proves that the AarTPS34 protein of the present application can catalyze the precursor material farnesyl pyrophosphate (FPP) to generate the sesquiterpenoid compound germacrene A, and germacrene A is a synthetic precursor of anticancer active ingredient beta-elemene, and the research on germacrene A has important theoretical and practical significance for improving the quality of folium artemisiae argyi and producing plant monoterpene compounds.

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 invention relates to the technical field of quality standards and detection of traditional Chinese medicine prescriptions, in particular to a method for establishing a fingerprint spectrum of volatile components of a caulis spatholobi traditional Chinese medicine compound and the fingerprint spectrum of the caulis spatholobi traditional Chinese medicine compound. The invention discloses a method for establishing a fingerprint spectrum of volatile components of a caulis spatholobi traditional Chinese medicine compound, germacrone, curcumenol, beta-elemene and curdione are used as reference substances, the fingerprint spectrum is established through gas chromatography-mass spectrometry, and the fingerprint spectrum has 24 common peaks. The fingerprint spectrum of the volatile components of the caulis spatholobi traditional Chinese medicine compound has the advantages of being good in stability, high in precision, good in repeatability and the like, the volatile components of the caulis spatholobi traditional Chinese medicine compound can be accurately analyzed, and a new method is provided for comprehensively and objectively evaluating the quality of the volatile components of the caulis spatholobi traditional Chinese medicine compound.

The invention discloses recombinant Escherichia coli for improving the GMA titer through protein scaffold cascade pathway key enzymes IspA and GAS and application of the recombinant Escherichia coli. A fusion protein is expressed in the recombinant Escherichia coli and is obtained by cascading four peptide binding modules with the pathway key enzymes IspA and GAS respectively, the four peptide binding modules are respectively connected to the N end of the IspA and the C end of the GAS through connecting peptides, and the four peptide binding modules are SpyCatcher, SpyTag, SnoopCatcher and SnoopTag; the four peptide binding modules form a stable enzyme cascade assembly through specific covalent interaction, so that spatial close-range cascade catalysis of IspA and GAS is realized, the synthesis efficiency of germacene A is improved, and finally, germacene A is converted into beta-elemene through Cope rearrangement. According to the method disclosed by the invention, glycerol is used as a carbon source, efficient synthesis of germacene A is realized through IPTG induction and in-situ extraction, and Cope rearrangement of germacene A is driven under a high-temperature condition to be converted into beta-elemene. Through verification of a shake flask and a fermentation tank, the yield of beta-elemene reaches 7.2 g / L and 31.2 g / L respectively, and the product yield and the substrate utilization rate are increased.

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 discloses a recombinant *Escherichia coli* strain that synergistically enhances the synthesis efficiency of β-elemene based on liquid-liquid phase separation, temporal regulation, and dynamic multi-enzyme assembly, and its application in β-elemene biosynthesis. In the recombinant *E. coli* strain, a stable covalent dual-enzyme complex of IspA and GAS is first constructed using a SnoopTag / SnoopCatcher system, and the upstream key enzyme IDI is further introduced. Simultaneously, the RGGRGG repeat sequence, capable of forming membrane-free droplets, is used as a phase separation scaffold, with an SH3 ligand fused to its N-terminus. The SH3 domain is then linked to the C-terminus of both the IspA-GAS enzyme complex and IDI. Through the specific interaction of the SH3 ligand / SH3 domain, the key enzyme is directionally recruited and spatially enriched into the aggregates. A temporal regulation strategy is also introduced: the expression of the IspA-GAS enzyme complex and IDI is first induced by IPTG, followed by delayed induction of RGGRGG aggregate expression, thus recruiting the already formed enzyme complex into the aggregates. This invention not only reduces the amount of glycerol used and improves the glycerol conversion rate, but also increases the yield of β-elemene.

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 present invention discloses a strain and method for producing β-elemene, and belongs to the field of bioengineering technology. The present invention constructs a recombinant cell expressing farnesol kinase, farnesyl phosphate kinase, polyphosphate kinase 2, and a combination of recombinant cells of germarene A synthase, and utilizes the recombinant cell or the combination of recombinant cells to catalyze farnesol to synthesize β-elemene. The substrate of the present invention is cheap, easily available, and the present invention can obtain 17g / L β-elemene by adding 20g / L farnesol reaction for 24h. Therefore, the present invention has good industrial application prospects and is conducive to the large-scale production of β-elemene.

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.