146 results about "Diterpene" patented technology

The invention relates to the technical field of medicines, in particular to application of lasiokaurin and cis-platinum combined medicine in preparation of a medicine for treating liver cancer. As a diterpenoid compound, lasiokaurin shows significant potential in the anti-cancer field. However, in medical research and clinical application at present, related reports about combined use of lasiokaurin and a classical anti-cancer drug cis-platinum for treating liver cancer do not exist. Based on the current research situation, the invention creatively provides the application of the lasiokaurin and cis-platinum combined medicine in the aspect of preparing the liver cancer treatment medicine. In-depth study finds that lasiokaurin and cis-platinum can generate a synergistic effect and jointly play a strong anti-tumor role, and a brand new way is opened up for treatment of liver cancer.

The present application relates to the technical field of microbial medicine, and particularly to a preparation method and application of indole diterpenoid compounds. Specifically, the extract of plant endophytic fungus F4a after solid fermentation culture is separated and purified to obtain indole diterpenoid compounds; the plant endophytic fungus F4a is a strain with the preservation number CCTCC NO: M 2012531. The indole diterpenoid compounds provided by the present application have significant antifeedant, insecticidal and hypotensive activities, and they can be used as ideal candidate compounds of antifeedants, insecticides or hypoglycemic drugs. The compounds can be produced through fungal fermentation, and the preparation method is simple, efficient and high in product purity. The present application has good application prospect.

The invention discloses a polyfunctional rosin-based reactive diluent. The structural formula of the polyfunctional rosin-based reactive diluent is shown as a formula (I) or a formula (II). The polyfunctional rosin-based reactive diluent has a rigid tricyclic diterpenoid structure of rosin, is small in molecular weight and low in viscosity, can be used for preparing an ultraviolet curing material, has excellent hardness and scratch resistance after light curing and film forming, and is simple in preparation method, low in cost and suitable for industrial production. And a polycarboxylic acid functional group is efficiently constructed under a mild condition.

The application relates to the medical technical field, in particular to application of neoline in treatment of Parkinson's disease. 19 The C 19 The type-II diterpene alkaloid neoline can significantly improve movement disorder in a MPTP-induced Parkinson's disease model mouse, the drug efficacy is equivalent to that of the positive drug madopar, the effective dose is much lower than that of the positive drug, the administration mode is oral administration, drug compliance and use convenience are good, and the neoline can be used for development of anti-Parkinson's disease drugs.

The present disclosure provides a P450 cytochrome enzyme for andrographolide synthesis and its application, belonging to the field of bioengineering. The present disclosure uses Saccharomyces cerevisiae CEN.PK2-1D as a host, and implements knockout of ROX1 and GAL80 genes on the genome, and integrative expression of GGPP synthase encoding gene and CPS diterpene synthase encoding gene at ROX1 site; and implements free expression of ApCPR and CYP71A8 and CYP71D10 both with truncated signal peptides, successfully constructing recombinant S. cerevisiae, and achieving de novo synthesis of 3,15,19-Trihydroxy-8(17),13-ent-labdadiene-16-oic acid. Compared with the blank, a response value of a product peak reaches 1.9*106, and this strategy provides necessary reference for analyzing biosynthetic pathway of andrographolide and using metabolic engineering to synthesize andrographolide and related derivatives thereof.

The application discloses application of an NtBCP gene in synthesis of cembranoid diterpenoids in tobacco and improvement of tobacco germplasm resources and belongs to the technical field of tobacco genetic engineering. The application proves through experiments that the NtBCP gene is specifically expressed in tobacco trichome stalk cells and is highly related to metabolism of cembranoid diterpenoids in tobacco, and the nucleotide sequence of the NtBCP gene is shown as SEQ ID NO. 1. Further through overexpression technology, the application finds that after overexpression of the NtBCP gene in cultivated tobacco, the obtained transgenic tobacco has obviously increased cembranoid diterpenoids compared with normal control plants. The application can provide a new strategy and path for genetic engineering breeding of tobacco or cultivation of new varieties of other crops.

The present invention refers to a method for the preparation of a compound according to formula (45), its enantiomers, diastereomers, a racemic mixture, and the pharmaceutically acceptable salts thereof. Furthermore the invention refers to a compound of formula (45) prepared by said method for use in treatment of neurodegenerative disorders and to pharmaceutical compositions.

The invention relates to the technical field of medicines, in particular to a composition with ingenane diterpenoid compounds as chemotherapeutic drug sensitizers and application of the composition. The chemotherapeutic drug sensitizer and the composition thereof provided by the invention can be used as the chemotherapeutic drug sensitizer, especially the sensitizer of breast cancer treatment drugs, and can be used for increasing the sensitivity of breast cancer cells to the chemotherapeutic drugs by inhibiting CHK1 (Ser345) phosphorylation so as to realize sensitization and provide a new treatment strategy for treating breast cancer.

The application belongs to the field of genetic engineering and biosynthesis, and particularly relates to biosynthesis of a class of diterpenoids. The application provides genes having a key role in the formation of a 5-8-5 tricyclic mother nucleus and a five-membered heterocyclic ring in biosynthesis of the class of diterpenoids, which are respectively named as PrcA and PrcB and polypeptides encoded by the genes, expression of PrcA and PrcB is carried out through a heterologous expression system of Aspergillus oryzae, and five diterpenoids with novel structures and anti-metabolic related fatty liver disease activity are obtained. The application provides application of the polypeptides in biosynthesis of the class of diterpenoids, and enriches a diterpenoid library, thereby providing lead compound resources for discovering new anti-metabolic related fatty liver disease medicinal raw materials.

This invention discloses an isosporanoid diterpenoid compound, its pharmaceutical composition, its preparation method, and its application, relating to the field of pharmaceutical technology. This invention is the first to extract the isosporanoid diterpenoid compound 3-epi-kravanhin A from the stems and leaves of *Amomum villosum*, and the structure of this isosporanoid diterpenoid is a novel compound reported for the first time. The isosporanoid diterpenoid compound 3-epi-kravanhin A isolated from the stems and leaves of *Amomum villosum* exhibits significant GLP-1 secretion-promoting and DPP-4-inhibiting activities. Experiments show that compound 3-epi-kravanhin A has hypoglycemic and weight-loss effects.

The invention relates to the technical field of medicines, in particular to an enantiomer-atesane type diterpenoid compound as well as a preparation method and an application of the enantiomer-atesane type diterpenoid compound. The enantiomer-atesane diterpenoid compound disclosed by the invention is derived from plants, has anti-tumor activity, has cytotoxicity to human leukemia cells, human liver cancer cells and human cervical cancer cells, and is relatively good in inhibitory activity. Wherein the compound 3 has the best effect, the IC50 values of the compound 3 to three human tumor cells are 7.5 + / -1.2 micromole per liter, 9.8 + / -1.0 micromole per liter and 10.1 + / -0.9 micromole per liter respectively, and the activity of the compound 3 is equivalent to that of a positive control drug mitomycin. Particularly, the compound 3 also has good cytotoxicity to drug-resistant liver cancer cells (Huh7-LR cells), and the IC50 value of the compound 3 is 9.6 + / -1.1 micromole per liter. The compound 3 shows huge potential as a lead compound by virtue of the novel chemical structure and potent cytotoxicity shown in various cell lines.

The invention belongs to the field of marine natural products, and relates to indole diterpene alkaloid and application thereof as an antibacterial agent. The indole diterpenoid alkaloid compound 1 has a strong cell proliferation inhibition effect, and the IC50 value of the indole diterpenoid alkaloid compound 1 on a human gastric cancer cell strain SGC-7901 is 19.16 [mu] g / mL; and the IC50 value on a human hepatoma cell line HepG2 is 6.27 mu g / mL. The IC50 of the positive drug cis-platinum to SGC-7901 and the IC50 of the positive drug cis-platinum to HepG2 are 3.56 mu g / mL and 1.99 mu g / mL respectively. The structure of the compound 1 is shown in the specification.

Disclosed is a preparation method for cannflavin compounds. The preparation method has the advantages of cheap and easily available raw materials, few reaction steps, short production period, simple operation, etc. The method comprises: firstly, condensing 4′-hydroxy-3′-methoxyacetophenone and diethyl carbonate (DEC) under an alkaline condition to obtain 4′-hydroxy-3′-methoxybenzoyl acetate; reacting 1,3,5-trihydroxybenzene with bromo-isoamylene under an alkaline condition to obtain 2-isopentenyl-1,3,5-trihydroxybenzene; and finally, condensing 4′-hydroxy-3′-methoxybenzoyl acetate and 2-isopentenyl-1,3,5-trihydroxybenzene at a high temperature to produce cannflavin B and / or isocannflavin B, and then subjecting same to separation and purification to obtain pure cannflavin B and pure isocannflavin B.

This invention relates to the field of biosynthesis technology, and particularly to engineered yeast strains and their application in the total fermentation production of steviol glycosides. This invention utilizes site-directed mutagenesis to mutate wild-type kaurenoic acid 13-hydroxylase, obtaining the G481L / Q159L mutant. This mutant is then applied to the production of steviol or steviol glycosides, constructing a steviol or steviol glycoside synthesis pathway in the *Saccharomyces cerevisiae* host to achieve efficient production of steviol or steviol glycosides. Simultaneously, by enhancing the level of diterpene precursor synthesis genes in chassis cells (MVA pathway, acetyl-CoA, GGPP, transport proteins, UDPG pathway), the yield of steviol glycosides is further increased, reducing costs for industrial production.

The invention provides a cassane diterpenoid compound and an application of the cassane diterpenoid compound in preparation of an anti-neuroinflammation medicine. Six novel cassane diterpenoid compounds are separated from mysorethorn, and a preparation method of the six compounds is provided. According to the present invention, the inhibition effect of lipopolysaccharide (LPS)-induced BV-2 microglial cells on NO production is determined, and the six compounds have anti-neuroinflammatory activity, and particularly, the compounds 4 and 5 have good anti-inflammatory effect compared with other compounds, and have the potential of anti-neuroinflammatory drug preparation.

The application discloses a lycoctine type diterpenoid alkaloid compound and a preparation method and application thereof. 20 The diterpenoid alkaloid compound Carmaloidline E shows significant antidepressant activity in a mouse behavioral despair model experiment, is obviously superior to fluoxetine as a positive medicine, and can be used for developing antidepressant drugs.

The invention discloses euphorbia macrocarpa diterpene compounds as well as an extraction method and application thereof, belongs to the field of traditional Chinese medicine extraction, and particularly relates to euphorbia macrocarpa diterpene compounds which are separated from euphorbia macrocarpa and have structural formulas shown as (I), (II) and (III), isomers of the compounds and pharmaceutically acceptable salts of the compounds. The compound has an inhibitory effect on NO in RAW264.7 cells induced by LPS (lipopolysaccharide), or a pharmaceutical composition containing the compound can be used for preparing anti-inflammatory drugs, and groups in the compound are described in the claims and the specification.

The invention discloses a 5 / 8 / 5 chitosan clostridium diterpenoid compound, a biosynthetic gene cluster and application of the biosynthetic gene cluster, and relates to the technical field of biological medicines. A 5 / 8 / 5 chitin type diterpenoid biosynthetic gene cluster Thm in trichoderma harzianum is identified through a genome mining system, chitin diterpenoid compounds with diversified structures are obtained by means of heterologous expression, the obtained compounds are subjected to anti-thrombotic activity comprehensive evaluation, and the result shows that the compounds 6 and 31 can obviously inhibit vascular thrombosis, the compound 6 has a remarkable inhibition effect on collagen-induced platelet aggregation, and the compound 31 has a better inhibition capability on thrombin-induced platelet activation. The compounds 6 and 31 show powerful antithrombotic effects in artery, vein and pulmonary artery thrombosis models, so that powerful technical support is provided for development of antithrombotic drugs.

This invention belongs to the field of natural product chemistry, and relates to characteristic vibsane-type diterpenoids with a seven-membered ring skeleton from *Viburnum awabuki*, or their salts, as well as their preparation methods and applications. Specifically, this invention relates to 15 vibsane-type diterpenoids with a seven-membered ring skeleton extracted and isolated from the dried leaves of *Viburnum awabuki*, a plant in the Viburnaceae family. The vibsane-type diterpenoids were isolated by silica gel column chromatography, HP20 macroporous resin column chromatography, ODS column chromatography, and HPLC. The antitumor activity of these compounds was investigated by testing their inhibitory effects on three tumor cell lines: HepG2, A549, and MCF-7.

To provide protein kinase C (PKC) modulating compounds and methods of treating a subject with cancer using the compounds.SOLUTION: There are provided tricyclic compounds, such as K101-C1301 compounds shown below or pharmaceutically acceptable salts thereof, tautomers thereof, or stereoisomers thereof.SELECTED DRAWING: Figure 1

The invention relates to the technical field of medicines, and discloses a novel light cuspidine type diterpenoid alkaloid compound and application of the novel light cuspidine type diterpenoid alkaloid compound. According to the present invention, the novel C20 selaginine type diterpenoid alkaloids such as the Carmaloidline C, the Carmaloidline D and the Aconialoidline C, which are provided by the present invention, all have significant analgesic effects; wherein the analgesic activity of the Carmaloidline C is the strongest, is superior to that of the positive drug morphine and is obviously superior to that of the positive drug ibuprofen, and the analgesic activity of the Carmaloidline D and the analgesic activity of the Aponiloidline C are superior to that of the positive drug ibuprofen. The medicines can be used for developing analgesic medicines for various acute or chronic pains.

This invention discloses a novel C20-type diterpenoid alkaloid compound, its preparation method, and its applications. The molecular formula of the C20-type diterpenoid alkaloid compound is C... 29 H 36 N2O2. This invention, through systematic and in-depth research on the chemical composition of Delphinium spp., uses the whole herb of Delphinium spp. as raw material. Through alcohol extraction, silica gel column chromatography, and preparative liquid chromatography purification, multi-spectral data analysis shows that a new C20 diterpenoid alkaloid compound was isolated from Delphinium spp. This compound is a novel compound reported for the first time. Antitumor activity studies have shown that this C20 diterpenoid alkaloid compound has good inhibitory activity against colon adenocarcinoma cells and can be used to develop plant-derived antitumor drugs.

The invention relates to a halogenated kaurane diterpenoid compound, and belongs to the technical field of natural product chemistry and medicinal chemistry. In the prior art, separation and purification of halogenated kaurane diterpenoid compounds from pteris semipinnata plants have the problems of low efficiency and insufficient purity, and deep research and application of the active ingredients are restricted. The novel compound is successfully obtained from a pteris semipinnata ethanol or methanol extract through systematic extraction and a multi-step chromatographic separation technology, the chemical structure of the novel compound is confirmed to be 16R-17-chloroethyl-1 beta-hydroxy-ent-kauran-19-acid through nuclear magnetic resonance and high-resolution mass spectrometry, and the structural formula is shown in the specification. The compound shows proliferation inhibition activity on K562 leukemia cells, A549 lung cancer cells, MDA-MB-231 breast cancer cells, SW480 colon cancer cells and human lung cancer paclitaxel drug-resistant strains A549 / Taxo in an in-vitro experiment, so that the compound can be used for preparing antitumor drugs.

The invention belongs to the field of marine natural pharmaceutical chemistry, and particularly provides a marine fungus-derived diterpenes diterpenoid compound as well as a preparation method and application thereof. According to the present invention, the diterpenes diterpenes compound is obtained from the marine fungus Penicillium brasilianum HBU-136, and the chemical structural formula of the marine fungus-derived diterpenes diterpenes compound is represented by the formula I, wherein the chemical structural formula of the marine fungus-derived diterpenes diterpenes compound is represented by the formula I, and the chemical structural formula of the marine fungus-derived diterpenes diterpenes compound is represented by the formula II; experiments prove that the compound has strong inhibitory activity on human gastric cancer cells (MGC-803, AGS and HGC-27), pulmonary epithelial cancer cells (A-549), liver cancer cells (HepG2) and colon cancer cells (SW-620), can be used as an antitumor drug, and has a wide application prospect.

The present application provides use of a diterpene compound derivative or a salt thereof in the preparation of a medicine for preventing and treating atopic dermatitis. The micromolecular diterpene compound derivative or the salt thereof has a remarkable effect of preventing and treating atopic dermatitis, shows a good prevention and treatment effect on a mouse AD model induced by OXA or MC903, can inhibit the increase of skin lesion score, the thickening of ear thickness, the aggravation of ear swelling and the increase of mast cells in mouse lesion, and also can reduce the IgE concentration of serum and improve the itching degree, indicating that the compound can be used for preventing and treating atopic dermatitis, thereby providing a new prevention and treatment thought and an effective medicine for treatment of atopic dermatitis.

The application provides a labdan-type diterpene glycoside extracted from Yunnan linaloe, and a use thereof, and belongs to the technical field of natural medicinal chemistry. The labdan-type diterpene glycoside is a compound shown in formula I or a salt thereof. The compound has good inhibitory activity on triple-negative breast cancer cells, and is expected to be used for preparing a drug for preventing and / or treating triple-negative breast cancer, and has a good application prospect.

The invention discloses a saccharomyces cerevisiae genetic engineering strain and application thereof. Based on a chassis strain SquMC13 with high squalene productivity, a sclareol synthesis route is modularly reconstructed, precursor carbon flow distribution is dynamically regulated and controlled, cell wall and membrane system steady states are adjusted, membrane lipid composition is adjusted, a cell cycle is intervened, and a product efflux system is enhanced, so that the problem of cytotoxicity caused by product accumulation is relieved to a certain extent. According to the invention, a plurality of saccharomyces cerevisiae engineering strains with high yield of sclareol are constructed, including Scl14, Scl24, Scl31, Scl38, Scl71 and Scl75, the result of the strain Scl75 is most prominent, the yield of sclareol fermented by a 250 mL shake flask is up to 4.1 g / L, efficient, stable and green biosynthesis of sclareol is realized, and a new strategy and theoretical basis are provided for microbial preparation of complex diterpenoid compounds.

The invention relates to the technical field of traditional Chinese medicines, and provides a traditional Chinese medicine effective part composition for treating atopic dermatitis, a preparation as well as a preparation method and application thereof. The composition comprises a flavonoid extract of pimpinella thellungiana, an alkaloid extract of cortex dictamni, a saponin extract of fructus kochiae, a triterpenic acid extract of selfheal, a flavonoid extract of scutellaria baicalensis, a diterpenic acid extract of golden larch bark, a polysaccharide extract of angelica sinensis, a monoterpenoid glycoside extract of radix paeoniae alba, an alkaloid extract of cortex phellodendri and a coumarin extract of fructus cnidii. A sophora flavescens alkaloid extract and a honeysuckle phenylpropanoid extract; the traditional Chinese medicine preparation comprises the composition and auxiliary materials. The invention also discloses application of the composition and the preparation in preparation of medicines for treating atopic dermatitis. The medicinal preparation obtained by the invention can relieve pruritus, relieve inflammatory response, improve dry skin and relieve skin injury, thereby treating atopic dermatitis.

The invention discloses an improved molasses culture medium and an application method of the improved molasses culture medium in increasing the yield of bird nest alkane diterpenoid high-activity compounds, and relates to the technical field of microbial fermentation. The invention aims to solve the problems of long production period, low product yield, large batch difference and difficulty in large-scale and process control when a solid culture medium is used for static fermentation in the existing production method. The method comprises the following steps: inoculating 0.1-0.5% of black egg nest fungus into a flat plate solid culture medium for culture, and then transferring into a liquid seed culture medium for shake culture to obtain a seed solution; inoculating the seed liquid into a fermentation tank filled with an improved molasses culture medium for deep fermentation to obtain fermentation liquid; mycelia are separated from the fermentation liquor, and a product rich in the bird nest alkane diterpenoids is obtained through washing, quick freezing, drying, smashing, extracting and concentrating. The invention can obtain the improved molasses culture medium and the application method of the molasses culture medium in increasing the yield of the bird's nest alkane diterpenoid high-activity compounds.

The application discloses a daphne-type diterpenoid compound Wikstdaphnein A, a preparation method and application thereof. The monomer compound is obtained by repeatedly separating and purifying the ethyl acetate part extract of Daphne fedtschenkoi by using various separation fillers and separation technologies. The relative configuration and absolute configuration of the monomer compound are identified by using a spectrum method and a calculation chemistry method, and the molecular formula and structural formula are deduced. Further in-vitro cell activity researches show that the new compound Wikstdaphnein A separated and identified from the ethyl acetate extract of Daphne fedtschenkoi has good inhibitory activity on melanoma cells. The application is helpful for the development and utilization of natural compounds of Daphne fedtschenkoi.