29 results about "Isoamoenylin" patented technology

The invention discloses an icaritin derivative, a composition and application, the structural formula of the icaritin derivative is as follows: in the structural formula, R1 is independently selected from hydrogen, hydroxyl and C1-C3 alkoxy; r2 is independently selected from hydrogen, an isopentenyl group, an isoamyl group and a Mannich base; r3 is independently selected from hydrogen, hydroxyl or OR3 ', R3 'is selected from rhamnosyl, rhamnose-(2-> 1)-glucosyl, rhamnose-(3-> 1)-glucosyl, propynyl and triazole groups substituted by alcoholic hydroxyl, benzyl and glycosyl; r4 is independently selected from a hydroxyl group or OR4 ', and R4' is selected from a propynyl group, a glucosyl group, and an alcoholic hydroxyl group, a benzyl group and a glycosyl substituted triazole group; r5 is independently selected from hydrogen, isopentenyl and Mannich base; mannich base is selected from N (CH3) 2 and N (CH2CH3) 2, R6 is independently selected from hydroxyl and OR6 ', and R6' is selected from hydrogen, rhamnosyl, rhamnose-(2-> 1)-xylosyl and rhamnose-(2-> 1)-rhamnosyl.The icaritin derivative provides a new direction for treatment of sarcopenia.

This invention provides a chalcone isopentenyltransferase gene. GiPT16 This invention relates to the GiPT16 protein, amplification primer set, and applications, belonging to the field of biogenetics technology. It is based on *Glycyrrhiza inflata* (GiPT16 protein, amplification primer set, and applications). Glycyrrhiza inflata Using whole-genome sequencing data and a reverse genetics strategy, the key aromatic isopentenyltransferase GiPT16, involved in the isopentenylation modification of chalcone active ingredients, was successfully identified and functionally characterized. This enzyme was confirmed to specifically catalyze the biosynthesis of psoralen and glycyrrhizin C using DMAPP as a donor. It is the first chalcone isopentenyltransferase characterized in *Glycyrrhiza inflata*, filling a gap in the study of key enzymes in the chalcone isopentenylation metabolic pathway of this species and providing important evidence for further elucidating the molecular mechanisms of quality formation in *Glycyrrhiza inflata* medicinal materials.

The invention relates to application of isopentenyl transferase FnPT1, and belongs to the technical field of enzymology. The isopentenyl transferase FnPT1 screened and verified in the invention is different from most of reported flavonoid isopentenyl transferases, the isopentenyl transferase FnPT1 can catalyze the isopentenyl modification reaction of a larger substrate of flavone glycoside, and the isopentenyl transferase FnPT1 has the potential to be applied to the synthetic biology of the flavone glycoside. The important application value is realized.

This invention belongs to the field of synthetic biology and microbial engineering, and discloses a chemical-biological method for preparing the isopentenyl bibenzyl compound 2-isopentenyl-3,3',4',5-tetrahydroxybibenzyl (NPB-1575) which has anti-ischemic stroke activity. The specific disclosed method includes: (1) chemically synthesizing the substrate dihydropiperidine; (2) constructing an engineered Escherichia coli strain based on the isopentenyl utilization pathway, co-expressing hydroxyethylthiazol kinase, isopentenyl phosphokinase, isopentenyl pyrophosphate isomerase and specific isopentenyl transferase, and efficiently synthesizing the isopentenyl donor; (3) using this strain to catalyze dihydropiperidine in whole cells, the yield in a 200L fermenter can reach 2.54g / L, which is nearly 40 times higher than the existing method; (4) obtaining NPB-1575 with a purity >98.5% by macroporous adsorption resin and normal / reversed phase chromatography and recrystallization. This method uses readily available raw materials, involves simple steps, is environmentally friendly, and yields high purity, laying the foundation for the development of NPB-1575 as a new drug for ischemic stroke and showing significant application potential.

The application discloses a process for preparing 3-methyl-2-buten-1-al diisopentyl acetal by continuous reaction rectification. The process comprises the following steps: reacting and rectifying isopentenyl alcohol and isopentenyl aldehyde in a reaction rectification tower to prepare 3-methyl-2-buten-1-al diisopentyl acetal, characterized in that the content of 2-methyl-3-buten-2-al in the liquid phase of the third to fifth trays of the reaction rectification tower from bottom to top is less than or equal to 1 wt%. By the continuous reaction rectification process, the device can be stably operated for more than 7200 hours, and the economic benefit of the enterprise can be remarkably improved.

The application provides a fusariobutenolide derivative 4''-O-isopentenyl fusariobutenolide C, and a structural formula of the compound is provided.The 4''-O-isopentenyl fusariobutenolide C can significantly inhibit the growth of seven human routine pathogenic bacteria in antibacterial activity testing, and the MIC is 8.6-28.3 μg / mL, and the antibacterial effect on one strain of human drug-resistant pathogenic bacteria, methicillin-resistant Staphylococcus aureus, is significant, and the MIC is 16.8 μg / mL, and the 4''-O-isopentenyl fusariobutenolide C can be applied to preparation of antibacterial drug precursors, and lays a material foundation for next-step biological medicine development and application of antibacterial components.

The invention discloses a preparation method of all-trans-farnesol through a three-enzyme cascade reaction. The invention firstly provides a mutant of farnesyl pyrophosphate synthase, and the amino acid sequence of the mutant is shown as SEQ ID No.3. Compared with a wild type, the mutant is applied to enzyme catalytic synthesis of farnesol, so that the conversion rate of a gold product is remarkably improved. The invention also provides a three-enzyme cascade reaction preparation method of farnesol, which comprises the following steps: in the same reaction system, dimethyl allyl diphosphate is used as a substrate; according to the method, isopentenyl diphosphate isomerase, farnesyl pyrophosphate synthase or a mutant thereof and farnesyl pyrophosphatase are used as catalytic enzymes for enzymatic reaction to prepare all-trans-farnesyl alcohol. According to the invention, in a single reaction system, three key enzymes are combined for application, so that continuous catalysis, high-efficiency and high-selectivity preparation of all-trans-farnesol is realized, process steps are simplified, and a new way is provided for green and efficient preparation of farnesol.

The invention discloses a medical application of an isopentenyl flavonoid compound or an aryl naphthalene lignan compound in podophyllum hexandrum. The isopentenyl flavone compound and the aryl naphthalene lignan compound can obviously inhibit proliferation of FLS cells induced by TNF-alpha, and show anti-RA activity in a rat RA model induced by a complete Freund's adjuvant; the isopentenyl flavonoid compound can play an anti-RA effect by inhibiting JAK1, inhibit phosphorylation of proteins such as PLC-gamma, p38 and JNK in FLS cells induced by TNF-alpha, inhibit NF-kappa B intracellular expression, and inhibit a JAK1 downstream signal channel at the cellular level; the aryl naphthalene lignan compound can play an anti-RA effect by inhibiting TNF-alpha, inhibit expression of RIP-1 and TRAF2 / 4 / 5 in FLS cells induced by TNF-alpha, inhibit expression in NF-kB nucleus, and inhibit a TNF-alpha downstream signal channel at the cellular level.

The invention discloses an isopentenyl transferase and an application of the isopentenyl transferase in synthesis of bakuchiol. Specifically, recombinant saccharomyces cerevisiae for expressing the isopentenyl transferase is constructed, the isopentenyl transferase CcPT6 from fructus psoraleae is obtained through screening, the isopentenyl transferase CcPT6 can catalyze an isopentenylation reaction of a coumaric acid substrate to generate bakuchiol, and the activity of the isopentenyl transferase CcPT6 is higher than that of a reported sequence BAK36. The CcPT7 is obtained by truncating 54 amino acids at the N end of the CcPT6, the catalytic activity is improved by 74%, and the activity of the CcPT7 is higher than that of a reported BAK36 mutant. In addition, the invention also provides a recombinant saccharomyces cerevisiae and yarrowia lipolytica engineering strain for integrally expressing the isopentenyl transferase CcPT6 or CcPT7, so that the artificial biosynthesis of the bakuchiol is realized. The discovery of the isopentenyl transferase and the construction of the recombinant engineering strain have important meanings for promoting the biosynthesis of the bakuchiol.

The invention discloses an oxygen isopentenyl transferase participating in synthesis of sesquiterpene coumarin and an application of the oxygen isopentenyl transferase. Belongs to the technical field of gene engineering. The invention discloses an open reading frame sequence of a Xinjiang ferula oxygen isopentenyl transferase FsPT9 gene and an amino acid sequence coded by the Xinjiang ferula oxygen isopentenyl transferase FsPT9 gene. The FsPT9 gene is obtained by screening and cloning based on combined analysis of multi-omics data of ferula sinkiang, a yeast expression vector is constructed, and a catalytic mechanism of the FsPT9 is identified in vitro by taking 7-hydroxycoumarin and farnesyl pyrophosphate as substrates. A yeast heterologous expression system proves that the FsPT9 can catalyze 7-hydroxycoumarin and farnesyl pyrophosphoric acid to generate umbelliferone. The invention discloses a key enzyme for initial synthesis of sesquiterpene coumarin for the first time, and the key enzyme is an oxygen isopentenyl transferase which is reported for the first time and is used for catalyzing three isopentenyl units at the same time, so that theoretical guidance is provided for synthesis and transformation of pharmacodynamic substances of asafetida sesquiterpene coumarin.

The application discloses a synthetic method of natural product Moracin N and belongs to the technical field of organic synthesis. The application takes an aldehyde containing a benzene ring as a starting raw material, introduces an isopentenyl group on the benzene ring through a Friedel-Crafts reaction, connects a hydroxyl protecting group to a No. 4 position hydroxyl group of the benzene ring to obtain an intermediate II, then uses a phosphorus ylide reagent to prepare the intermediate II into gem-dibromo olefin to obtain an intermediate III, then under the catalysis of a base and a copper catalyst, the gem-dibromo vinyl group is coupled with an ortho hydroxyl group to form a benzofuran ring to obtain an intermediate IV, then 3,5-dihydroxy bromobenzene is introduced to the right side of the benzofuran ring of the intermediate IV through a Suzuki-Miyaura reaction to obtain an intermediate VI, and finally the hydroxyl protecting group of the intermediate VI is removed to obtain Moracin N. The synthetic route of the application is simple, the reaction condition is mild, the safety is high, the required raw material is cheap and easy to obtain, the total cost is low, and the application is suitable for industrialized preparation.

The invention discloses a compound with T-type calcium channel inhibitory activity, a composition and application and a screening method thereof, and belongs to the technical field of medical chemistry and biological medicine. The compound takes a 6-isopentenyl isomer of parvacol as a parent nucleus, has excellent inhibitory activity and selectivity through structural optimization design and virtual screening, can improve DHT-induced hair follicle function inhibition or regulate scalp microenvironment calcium steady state, and has a good application prospect. The compound can be used for preparing Cav3 family T-type calcium channel inhibitors and medicines for preventing alopecia and / or promoting hair growth. The compound can be prepared into a solution, a gel, a cream or a liposome in vitro preparation. The compound disclosed by the invention not only has the effects of preventing alopecia, promoting hair growth and the like, but also reduces the risk of skin sensitization and reactivity, and improves the stability and process accessibility of an external preparation.

This invention discloses a protein with O-isopentenyltransferase activity, related biomaterials, and applications, belonging to the field of biotechnology. This invention screened and cloned an O-isopentenyltransferase gene (GlOPT), which can be used to prepare O-isopentenyltransferase. Experiments have confirmed that this O-isopentenyltransferase can catalyze the in vitro conversion of 8-hydroxybergamot lactone to arugulatin; catalyze the conversion of bergamotol to isoimperatorin; and catalyze the conversion of xanthotoxin to imperatorin. This provides technical support for the production of isopentenyl furanocoumarin-like active ingredients from arugula, lays the foundation for research on the biosynthetic pathways of coumarin compounds, and has significant theoretical and practical implications.

This invention relates to isopentenyl flavonoids, their preparation methods, and applications, belonging to the field of natural product chemistry. Specifically, it involves the separation of five isopentenyl flavonoids—daphengiratriprenylone D, (3"'R)-daphnegiravone F, (3"'S)-daphnegiravone F, daphnegiravone E, and daphnegiralin H—from *Daphne giraldii* Nitsche, a plant in the Thymelaeaceae family, using silica gel column chromatography, macroporous resin chromatography, ODS column chromatography, and HPLC. Their inhibitory activity against HepG2 and Hep3B cells was tested. Ultimately, it was found that these compounds exert their antitumor effect by inhibiting the growth activity of tumor cells. The preparation method of this invention is simple, reproducible, and yields high-purity compounds with significant antitumor activity.

The invention discloses a method for extracting isopentenyl flavonoid compounds from black mulberries, which adopts an ultrasonic-assisted ionic liquid extraction method and comprises the following steps: crushing the black mulberries, mixing the crushed black mulberries with ionic liquid, soaking the mixed black mulberries, and carrying out ultrasonic extraction. Compared with a traditional water extraction method, the total content of the extracted isopentenyl flavonoid compounds sanggenone D and sanggenone C is increased by about 3.00 times. Meanwhile, the extraction method is green, efficient and energy-saving, and avoids environmental pollution to a greater extent.

The application relates to application of an isopentenyl transferase FnPT1 and belongs to the technical field of enzymology. The isopentenyl transferase FnPT1 screened and verified by the application is different from most reported flavonoid isopentenyl transferases, the isopentenyl transferase FnPT1 can catalyze isopentenyl modification reaction of flavonoid glycoside which is a relatively large substrate, the isopentenyl transferase FnPT1 has potential application in flavonoid glycoside synthetic biology, and has important application value.

The invention relates to a preparation method of a natural product icaritin. The method comprises the following steps: performing MOM protection on a compound 1 to obtain an intermediate compound 2, reacting with p-methoxybenzaldehyde to obtain an intermediate compound 3, and reacting under alkaline catalysis to obtain a compound 4; removing MOM protection in an acidic environment to obtain 5, and reacting 5 with an isopentenyl derivative under the catalysis of Lewis acid to obtain icaritin 6; according to the method, synthesis steps are remarkably shortened, most of existing routes need about ten steps, and the route provided by the invention can realize synthesis of icaritin only through five-step reaction; through reasonable route design, introduction of isopentenyl is innovatively carried out in the last step, so that side reactions are reduced, and the purification difficulty is reduced.

The present application relates to a kind of isoprenyl-alpha-pyrone dimer Hypericumonates D-F and its preparation method and application, belong to the field of medicinal chemistry, the isoprenyl-alpha-pyrone dimer Hypericumonates D-F is first extracted from the leaves and branches of Hypericum monogynum Isolation, its structural formula is D-F formula.Compounds D-E has significant inhibitory effect on the NO production in mouse microglial cells (BV-2 cells) induced by lipopolysaccharide (LPS), and its activity is stronger than that of positive drug minocycline, with the potential application in the field of neuroinflammatory drugs, the present application simultaneously relates to a kind of pharmaceutical composition, it includes above-mentioned isoprenyl-alpha-pyrone dimer Hypericumonates D-F, and pharmaceutically acceptable adjuvant, it has the efficacy of anti-neuroinflammation.

The invention discloses a protein with O-isopentenyl transferase activity, a related biological material and application, and belongs to the technical field of biology. According to the invention, an O-isopentenyl transferase gene (GlOPT) is screened and cloned, and the O-isopentenyl transferase can be prepared by using the gene. Experiments prove that the O-isopentenyl transferase can be used for catalyzing 8-hydroxybergamolactone in vitro to generate glehnia littoralis; the bergamot phenol is catalyzed to generate isoimperatorin; and the xanthotoxol is catalyzed to generate imperatorin. Technical support is provided for production of glehnia littoralis isopentenyl furocoumarin active ingredients, a foundation is laid for research on a biosynthesis route of coumarin compounds, and the method has important theoretical and practical significance.

The invention provides a method for selectively synthesizing an isopentenyl phenolic compound, relates to the technical field of a preparation method of the isopentenyl phenolic compound, and particularly relates to a novel method for highly selectively converting a phenolic compound and an allyl alcohol compound into the isopentenyl phenolic compound by taking lewis acid and hexafluorophosphate as a composite catalyst. On one hand, the hexafluorophosphate and the lewis acid cooperate to activate the allyl alcohol compound, so that the oxygen alkylation side reaction is remarkably inhibited, the carbon alkylation product is specifically generated, and the yield of the target product is high; meanwhile, the catalyst dosage is small, conditions are mild, reaction is rapid, and the principle of green chemistry is better met; and on the other hand, the preparation method disclosed by the invention is wide in applicable substrate range, and the substrate is easy to obtain.

The invention provides an isopentenyl phenol compound and a preparation method and application thereof.The structural formula of the isopentenyl phenol compound is a formula A or a formula B. The isopentenyl phenol compound is obtained through separation from shiitake mushrooms, has no non-specific toxicity to T cells, B cells and keratinocytes, can effectively inhibit proliferation activity of the T cells, the B cells and the keratinocytes, and has a good application prospect. The compound also has antioxidant activity, can be used for preparing drugs for resisting autoimmune diseases, such as psoriasis, can inhibit the development of psoriasis from multiple ways, and has a multi-target synergistic effect mechanism.

To provide a fibroblast growth factor-5 production inhibitor having excellent fibroblast growth factor-5 production inhibitory action and high safety.SOLUTION: The fibroblast growth factor-5 (FGF-5) production inhibitor includes at least one selected from the group consisting of pinobanksin, pinocembrin, quercetin, rutin, isoquercetin, genistein, 6-prenylnaringenin, isosakuranetin, and biochanin A.SELECTED DRAWING: None

Isopentenyl flavonoid enantiomer compounds are extracted from Epimedium sagittatum and their preparation method and application. The preparation method comprises the following steps: crushing the Epimedium sagittatum to prepare a paste, suspending the paste with water, extracting the paste with petroleum ether, dichloromethane, ethyl acetate and n-butanol respectively to obtain extracts of various parts, performing gradient elution separation by silica gel column chromatography, combining similar parts according to the color development results of thin layer chromatography (TLC) to obtain multiple polar segments; chromatographing the target polar segment and performing gradient elution to obtain multiple components, then combining similar components through thin layer chromatography (TLC) spot plate absorption to obtain multiple sub-components; eluting and purifying the target sub-components, collecting fractions with different retention times, and drying to obtain four compounds respectively. The four compounds have a significant inhibitory effect on the cell viability of human breast cancer MCF-7 cells and have anti-breast cancer activity. The four compounds can be used in the preparation of drugs for treating breast cancer, with huge social and economic benefits.

The invention provides a boric acid ester cross-linking type high-temperature stable polycarboxylic acid pumping agent and a preparation process of the boric acid ester cross-linking type high-temperature stable polycarboxylic acid pumping agent. The pumping agent is prepared from the following components in parts by weight: 45 to 60 parts of isopentenyl polyoxyethylene ether, 15 to 20 parts of allyl polyoxyethylene ether, 18 to 22 parts of acrylic acid, 4 to 6 parts of 2-acrylamide-2-methylpropanesulfonic acid, 3 to 5 parts of N-vinyl pyrrolidone, 2 to 3 parts of maleic anhydride, 5 to 7 parts of 3-acrylamido phenylboronic acid, 5 to 7 parts of boric acid ester dynamic cross-linking agent, 1.5 to 2.5 parts of KH550 modified nano ZnO and 0.9 to 1.2 parts of initiator. 0.4-0.6 part of a chain transfer agent, 10-15 parts of a phosphate buffer solution and 210-250 parts of deionized water. The prepared pumping agent has the comprehensive advantages of high-temperature stability, excellent water-retaining property and dispersibility, segregation resistance, high strength and the like.

The invention belongs to the technical field of medicines, and discloses quinoid chalcones with an A ring having an isopentenyl group and an anti-diabetes application thereof. The compound provided by the invention has a structure shown in a general formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method comprises the following steps: (1) synthesizing 3, 5-dihydroxy-2-acetyl-6, 6-diisopentenyl cyclohexane-2, 4-dienone, (2) synthesizing a quinone chalcone compound with an A ring having an isopentenyl group, and (3) synthesizing a quinoid chalcone compound with an A ring having an isopentenyl group. And (3) synthesizing a dimer compound with an A ring having isopentenyl and quinoid chalcone bridged by methylene. The compound provided by the invention is simple in preparation method and has a remarkable anti-diabetic effect. # imgabs0 #

The invention relates to the technical field of medicines, and discloses a quinonoid chalcone dimer compound with an A ring having an isopentenyl group and an anti-tumor application of the quinonoid chalcone dimer compound. The compound provided by the invention has a structure shown in a general formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method comprises the following steps: (1) synthesizing 3, 5-dihydroxy-2-acetyl-6, 6-diisopentenyl cyclohexane-2, 4-dienone, (2) synthesizing a quinone chalcone compound with an A ring having an isopentenyl group, and (3) synthesizing a quinoid chalcone compound with an A ring having an isopentenyl group. And (3) synthesizing the quinoid chalcone dimer compound with an A ring having an isopentenyl group. The compound provided by the invention is simple in preparation method and shows relatively good anti-tumor activity. # imgabs0 #

The invention belongs to the technical field of genetic engineering and enzymology, and particularly relates to isopentenyl transferase and application thereof to preparation of isopentenyl isoflavone. The isopentenyl transferase FoPT2 with the amino acid sequence shown as SEQ ID NO.2 is verified for the first time to show catalytic activity on 6 isoflavone compounds (genistein, dihydrogenistein, biochanin A, calycosin, genistin and 3 ', 4', 7-trihydroxy isoflavone), 21 isopentenyl products are generated in total, the structures of 10 products are analyzed, and 3 products are synthesized for the first time. The isopentenylation modification comprises 13 kinds of mono-isopentenylation (C- / O-connection) and 8 kinds of diisopentenylation (C-O connection / C-C connection), modification sites comprise C-6, 7-O, C-8, 4 '-O and the like, and wide regioselectivity is shown. By optimizing reaction conditions, the catalytic efficiency of FoPT2 is improved, the preparation of isopentenyl isoflavone with various structures is facilitated, and a new possibility is provided for isopentenyl isoflavone products.

The invention provides a chalcone isopentenyl transferase gene GiPT16, a GiPT16 protein, an amplification primer group and application, and belongs to the technical field of biological genes. The key aromatic isopentenyl transferase GiPT16, which participates in isopentenylation modification of chalcone active ingredients, is successfully mined and functionally identified by adopting a reverse genetics strategy on the basis of whole genome sequencing data of Glycyrrhiza inflata (Glycyrrhiza inflata). The chalcone isopentenyl transferase is proved to be capable of specifically catalyzing biosynthesis of psoralen B and licochalcone C by taking DMAPP as a donor, is the first represented chalcone isopentenyl transferase in glycyrrhiza inflate, fills the blank of key enzyme research of the species in a chalcone isopentenyl metabolic pathway, and has a wide application prospect. An important basis is provided for deeply analyzing a molecular mechanism formed by the quality of the glycyrrhiza inflate medicinal material.

The application belongs to the technical field of enzyme engineering, and discloses a high-activity isopentenyl phosphate kinase mutant and application thereof. H274P The high-activity isopentenyl phosphate kinase mutant is AtIPK H274P , wherein the amino acid at position 274 of the wild-type AtIPK is mutated from histidine H to proline P. S47A,L124A SmDAGK S47A,L124A can constitute an efficient isopentenol utilization pathway which can effectively convert prenol into DMAPP. By using the pathway, an engineering strain with improved isopentenyl modification ability can be constructed, and the strain has more advantages compared with a traditional engineering strain based on a mevalonate pathway.