133 results about "Diterpenoid degradation" patented technology

The diterpenic labdane 3-[2-[decahydro-6-hydroxy-5-(hydroxymethyl)-5,ha-dimethyl-2-methylene-1-naphthalenyl]ethylidene]-dihydro-4-hydroxy-2(3h)-furanone, chemically diagrammed as inhibits the synthesis of pro-inflammatory cytokines, activates the PPAR-gamma receptor and diminishes nuclear factor kappa B. The compound is useful to treat auto-immune diseases, for organ and tissue transplantation, and to treat immunodeficiency (e.g., AIDS).

The invention discloses a gene for generating related diterpene synthase together with a tanshinone compound as well as an encoding product and an application thereof. The gene is named as the tanshin ent-kaurene synthase gene (SmKSL) and is obtained from tanshin by cloning and adopting a gene chip technology, and as for the sequence, see to SEQ ID No.1. The protein encoded by the SmKSL is the protein provided with an aminoacid residue sequence with SEQ ID No.2 or is the protein derived via the SEQ ID No. 2 by replacement, deletion or addition of one or more aminoacid residues for the aminoacid residue sequence with SEQ ID No.2 and provided with the same activity with the aminoacid residue sequence with SEQ ID No.2. The SmKSL is a key enzyme gene in a tanshin diterpene secondary metabolic pathway, the genetic expression is closely related with the generation of the tanshinone compounds, for example, tanshinone IIA, and the invention has important theoretical and practical significances for adjusting and producing plant diterpenoid compounds and cultivating the excellent medical new plant variety.

The invention provides a plurality of labdane diterpenoid compounds and derivatives thereof, which can be used for preparing pharmaceutical composition for preventing or treating neurodegenerative diseases. The invention also provides an arborvitae seed extract, the arborvitae seed extract contains one or more labdane diterpenoid compounds and the derivatives, and can be used for preparing pharmaceutical composition for preventing or treating neurodegenerative diseases.

The invention discloses a callicarpa nudiflora extract with an anti-inflammatory effect. The callicarpa nudiflora extract contains 24%-36% of flavonoid compound, 0.8%-3% of phenethyl alcohol glycoside and 15%-27% of diterpenoid compound. The obtained callicarpa nudiflora extract has high anti-inflammatory activity.

The invention belongs to the field of traditional Chinese medicine production, and relates to 1-alkylated daphnane diterpene and application thereof to preparation of anti-HIV drugs. 1-alkylated daphnane diterpene is a compound extracted from S. chamaejasme of the Stellera genus; tests prove that 1-alkylated daphnane diterpene is remarkable in anti-HIV activity, and the EC50 value is lower than 0.001 [mu]M; 1-alkylated daphnane diterpene is relatively low in cytotoxicity, and the CC50 value is higher than 11 [mu]M; compared with a positive control drug zidovudine, 1-alkylated daphnane diterpene has more obvious advantages; the 1-alkylated daphnane diterpene compound can serve as an active ingredient for preparation of the anti-HIV drugs.

The invention relates to a novel ingenane-type diterpenoid (1) and a tiglic alkane-type diterpenoid (2) obtained by separating from euphorbia stracheyi, and two ingenane-type diterpenoids (3, 4) obtained by separating from ewuphorbia wallichii, as well as a preparation method of the same, and an application of the ingenane-type diterpenoid (1) and a tiglic alkane-type diterpenoid (2) in preparation for anti-tumour medicines. In-vitro anti-tumour active screening indicates that the compounds disclosed by the invention are obvious in the effect of inhibiting tumour cell proliferative activity, and are capable of being combined with pharmaceutically acceptable carriers to prepare clinically acceptable medicine dosage forms for treating various cancers. The invention provides lead compounds for researching novel anti-tumour medicines, and has an important value in development and utilization for the resources of medicinal plants.

The present invention relates to the field of medicine technology, and in particular relates to six novel-structured diterpene compounds of Lobophytumin A, Lobophytumin B, Lobophytumin C, Lobophytumin D, Lobophytumin E and Lobophytumin F, which are separated from Lobophytum cristatum Tixier-Durivault of Genus Lobophytum, and a preparation method and application thereof to preparation of medicament for treating type II diabetes mellitus. The structural formulas of the Lobophytumin A, Lobophytumin B, Lobophytumin C, Lobophytumin D, Lobophytumin E and Lobophytumin F are as follows. According to biological activity test, the compounds can be used as a protein tyrosine phosphatase 1B (PTP1B) inhibitor and an insulin sensitizer for preparation of medicaments for treating type II diabetes mellitus, obesity and complications thereof.

The invention discloses a wedelia trilobata anti-tumor extract and preparation and application methods thereof. The wedelia trilobata anti-tumor extract is prepared by adding solvent into wedelia trilobata powder for extraction, filtering and decompression-concentrating extracted liquor to obtain a total extract, mixing the total extract with water into a suspension, performing extraction sequentially through petroleum ether and ethyl acetate and performing decompressed recovery to obtain a petroleum ether solution, an ethyl acetate solution and a aqueous solution, wherein the petroleum ether solution contains one eudesmene type sesquiterpene lactone, five enantiotopic kaurane type diterpenoid compounds, two oleanane type triterpenes, one cycloartane type triterpene, one sterol compound, two dipeptide compounds and one caffeate compound. The prepared wedelia trilobata anti-tumor extract is high in yield, simple in technical process, low in cost and applicable to large-scale preparation, and meanwhile, has broad-spectrum anti-tumor activity and can serve as an active component applied to tumor control and treatment drugs.

The invention relates to the technical field of a medicine, and particularly relates to two diterpenoid compounds libertellenone G and libertellenone H with antineoplastic activities extracted from secondary metabolite of arctic curvularia molecular genus. The chemical structural formulas are shown in the specification. The invention also provides a preparation method of the diterpenoid compounds, and application of the diterpenoid compounds in preparation of an antitumor drug.

The present invention relates to technical field of medicine, and relates to the use of diterpenoid compounds of glaucocalyxin A, glaucocalyxin B, glaucocalyxin C, glaucocalyxin D, glaucocalyxin E and glaucocalyxin F in Isodon japonica (Burm f) Hara var glaucocalyx (Max) Hara for preparing anti-cancer medicine. The invention adopts an MTT method for executing cytotoxicity experiment. The result shows that the glaucocalyxin A, glaucocalyxin B, glaucocalyxin C, glaucocalyxin D, glaucocalyxin E and glaucocalyxin F all have remarkable cytotoxicity respectively thereby can be used for preparing the anti-cancer medicine. The invention provides a new source for preparing anti-cancer medicine.

The invention relates to a plant cell culture technology, in particular to a method for biosynthesizing abietane diterpenoid compounds by using cephalotaxus fortune culture cells. The method comprises the following steps of: placing cephalotaxus fortune cells in a common culture medium, and culturing, wherein50 to 150g of the cells are inoculated in each liter of wet weight of the culture medium; and adding an inducer at the final concentration of 10 to 2,000 mu M and 50 to 200g of adsorbent into each liter of culture medium at the initial stage of cell exponential growth, wherein the inducer is an abiological inducer or fungal elicitor. The method is a biosynthesis method and is stable and environment-friendly; and products are completely adsorbed onto the adsorbent, so that the operation process of separation and purification is greatly simplified, the cost is reduced and industrial production is easy to realize. Meanwhile, seven abietane diterpenoid compounds comprising a new compound are synthesized. The abietane diterpenoid compounds have high bioactivity, and are important lead compounds, and the technology has important commercial application prospect.

The present invention discloses a novel diterpenoid compound separated from the Antrodia camphorate fruiting body, more particularly, a compound with the following structural formula (see the chemical formula), and the medically acceptable salt, solvent compound, hydrate or compound of the same biological activity or the derivative and so on. The present invention also discloses the application of the novel compound in the neural protection and the composition of the medicine with the compound as the active ingredient.

The invention discloses an application of an ingenane diterpene compound in preparation of antitumor drug. The ingenane diterpene compound is one or more of the ingenane diterpene compound shown in a formula (1). The ingenane diterpene compound can obviously inhibit the propagation activity of breast cancer cells, compared with a traditional tumor therapeutic method, tumor inhibitory effect is good, toxic and side effects are little, targeting property is strong, the ingenane diterpene compound has no damage to normal cells, security can be guaranteed at maximum degree, the ingenane diterpene compound provides a latent novel medicine development purpose for treating breast cancer, and can be a further research as an anti-breast cancer candidate medicine.

The invention discloses a tripterygium wilfordii diterpene synthase TwGES1 and an encoding gene and application thereof. Twges1 genes are obtained through cloning from tripterygium wilfordii suspension cells; and the genes are key enzyme genes obtained through synthesis of diterpene components from tripterygium wilfordii. Experiments prove that TwGES1 proteins can catalyze GGPP to form geranyl linalool ((E, E)-geranyl linalool), can catalyze FPP to form nerolidol ((E)-nerolidol), not only have important significance on biological synthesis of such diterpene compounds as triptolide in the tripterygium wilfordii and but also have important theoretical and practical significance on adjustment and production of plant diterpene compounds and cultivation of high-quality tripterygium wilfordii.

The diterpenic labdane 3-[2-[decahydro-6-hydroxy-5-(hydroxymethyl)-5,ha-dimethyl-2-methylene-1-naphthalenyl]ethylidene]-dihydro-4-hydroxy-2(3h)-furanone, chemically diagrammed asinhibits the synthesis of pro-inflammatory cytokines, activates the PPAR-gamma receptor and diminishes nuclear factor kappa B.The compound is useful to treat auto-immune diseases, for organ and tissue transplantation, and to treat immunodeficiency (e.g., AIDS).

The invention relates to a preparation method of antioxidant plant insulating oil and belongs to the technical field of insulating oil. The antioxidant plant insulating oil is prepared by adding beta-cyclodextrin embedded sage essential oil microcapsules, sage essential oil contains diterpenoid compounds such as carnosic acid and carnosol which can effectively remove oxygen ions, protect the plantinsulating oil from damage and inhibit the peroxidation effect of lipid at the same time, and an aqueous or alcohol extract of plant sage leaves is an effective antioxidant and an effective free radical scavenger. The antioxidant plant insulating oil is prepared by adding lipophilic silica nanoparticles, and the silica nanoparticles can absorb active oxygen generated during aging of the plant insulating oil, effectively inhibit the oxidation process of plant insulating oil ester molecules, improve the oxidation resistance of the plant insulating oil and the ability to adsorb the active oxygenand effectively adsorb the beta-cyclodextrin embedded sage essential oil microcapsules to avoid the phenomenon of agglomeration of the microcapsules.

The invention belongs to the technical field of medicines and particularly relates to a callicarpa nudiflora extract or a diterpene compound separated from an overground part of callicarpa nudiflora and medical application of pharmaceutical composition prepared from the callicarpa nudiflora extract and the diterpene compound to preparation of medicines for treating gliomas. According to in-vitro tests, the callicarpa nudiflora extract and the diterpene compound can play a role in inhibition of human brain malignant spongioblastoma U251 cells by inhibition of cell proliferation and induction of cell apoptosis and can be used for development of the medicines for treating the gliomas.

The invention discloses application of xerophilusin B in preparation of products for inhibiting tumor growth. The xerophilusin B can be applied to preparation of products with the following functions: (1) preventing or treating tumors and (2) inhibiting proliferation of tumor cells, wherein the chemical structural formula of the xerophilusin B is as shown in a formula I in the specification. Therefore, in consideration of constant discovery of various novel compounds in plectranthus plants and remarkable effects discovered in tumor treatment and researches, along with gradually further researches on compound ingredients extracted from plectranthus plants, diterpenoid compounds represented by the xerophilusin B can bring a novel approach for tumor treatment.

The invention discloses a diterpenoid compound. A preparation method comprises the following steps: A, degreasing Chinese azalea flower with dichloromethane once or more than once, then carrying out filtration and collecting filter residue; B, extracting the Chinese azalea flower with alcohol or an alcohol solution once or more than once, then carrying out filtration, collecting a filtrate and then carrying out pressure-reduced concentration and drying so as to obtain alcohol extract; C, adding water into the alcohol extract, degreasing the alcohol extract with petroleum ether again, carrying out extraction with ethyl acetate after degreasing, extracting the obtained ethyl acetate extraction liquid with a saturated aqueous sodium bicarbonate solution and evaporating an ethyl acetate phase to dryness to obtain crude ethyl acetate extract; and D, separating and purifying the crude ethyl acetate extract by using column chromatography to obtain the purified diterpenoid compound. The diterpenoid compound provided by the invention has a strong inhibitory effect on colon cancer cells (HT-29 and HCT-8), liver cancer cells (Bcl-7402), small cell lung cancer (A549) and / or breast cancer (MCF-7).

A composition based on labdane-diterpenoids that provides better photo protection against both UV A and UV B radiations in the HaCaT human keratinocyte cell lines is disclosed. The composition comprises 8,13-epoxy-1α,6β,7β,9α-tetrahydroxylabd-14-en-11-one alone and in combination with 6β-acetoxy-8,13-epoxy-1α,7β,9α-trihydroxylabd-14-en-11-one and / or 7β-acetoxy-8,13-epoxy-1α,6β,9α-trihydroxylabd-14-en-11-one. The composition protects the cells of the skin from harmful UV A and UV B rays through synergistic mechanisms with utility as a safe long-term cosmetic solution for preventing UV-induced skin damage and to induce sunless tanning. Additionally, the composition enhances melanogenesis in B16F1 mouse melanoma cells acting as tanning inducers / accelerators both in the presence or absence of sunlight. Elevation of melanogenesis confers additional protection against UV-induced skin damage.

The invention provides pinus koraiensis needle essential oil as well as an extraction method and application thereof in a bacteriostatic culture medium, which belongs to the technical field of plant essential oil extraction. The pinus koraiensis needle essential oil comprises free amino acid and a compound, wherein the content of the free amino acid is 244.44 mg / kg; and calculating at the mass ofthe pinus koraiensis needle essential oil as 100 percent, the compound accounts for 97.92 percent, wherein olefins account for 87.97 percent, alcohols account for 3.7 percent, esters account for 5.77percent, oxides account for 0.24 percent, ketones account for 0.14 percent, and the diterpenes compound accounts for 0.1 percent. The pinus koraiensis needle essential oil obtained by adopting the extraction method contains 46 compounds, so that compared with the existing report, the types of the compounds in the pinus koraiensis needle essential oil can be greatly increased. The pinus koraiensisneedle essential oil is used as a sterilizing agent to be added into the culture medium, so that the bacteria infection rate of the culture medium can be reduced.

The invention relates to recombinant expression of terpenoid synthase enzymes and geranylgeranyl diphosphate synthase (GGPPS) enzymes in cells and the production of diterpenoids.

The invention provides a crystal form of a compound as shown in the formula II. The crystal form belongs to an orthorhombic crystal system; the space group is P212121; the crystal cell parameters are as shown in the specification, wherein alpha is equal to 90.00 DEG, beta is equal to 99.00 DEG, and gamma is equal to 90.00 DEG; Z is equal to 4; the crystal cell volume is as shown in the specification. The invention also provides a preparation method and application of the crystal form. The compound with the crystal form in the formula II, which is separated from leonurus japonicus, has a certain inhibiting effect on platelet aggregation and has a better effect than clopidogrel bisulfate as an anti-platelet aggregation drug under the same concentration (0.1mM), so that a new choice is provided for developing a novel natural anti-platelet aggregation drug.

The invention relates to eight new cassane diterpenoid compounds separated from the seed of a leguminous Caesalpinia L. plant Caesalpinia minax Hance through a phytochemical extraction separating process, cytotoxicity of the compounds on the gastric gland cancer, the lung cancer, the liver cancer and the breast cancer, and an application of the compounds in the clinic prevention and treatment of tumors.

3,4-open-ring helianthemum diterpenoid type compounds, a preparing method thereof and applications of the compounds are disclosed. The structure formulas of the compounds are shown as formulas I and II. The compounds are used for preparation of medicines or healthcare products for inhibiting inflammation, and for preventing and / or treating gynecologic inflammation and acute infectious hepatitis.

The invention provides an abietane type diterpenoid compound with blood lipid lowering activity as well as a preparation method and application of the abietane type diterpenoids compound. Particularly, the compound provided by the invention has a structure shown as the formula I in the description, wherein the definition of all radicals is described in the description. The compound provided by the invention has the activity of increasing low-density lipoprotein intake in vivo or in vitro, and has the potential of being used as novel blood lipid lowering medicine.

The invention relates to the technical field of medicine and the application of diterpene compounds, including glaucocalyxin B, glaucocalyxin C, glaucocalyxin D, glaucocalyxin E and glaucocalyxin F in rabdosia japonica, to preparation of anti-hepatitis virus medicines. The invention performs anti-hepatitis B surface antigen and hepatitis B core antigen experiments of diterpene compounds including glaucocalyxin B, glaucocalyxin C, glaucocalyxin D, glaucocalyxin E and glaucocalyxin F by a hepatitis B surface antigen (HBsAg) diagnostic kit and a hepatitis B core antigen (HBeAg) diagnostic kit. The result shows that these compounds have obvious anti-hepatitis B virus activity, thus, these compound can be used for preparation of anti-hepatitis B virus medicines.

The invention relates to a diterpene compound extracted and separated from the traditional Chinese medicine Siberia chinensis, a preparation method and an application thereof. The diterpenoids include all compounds with the following general structural formula; The preparation method of the diterpenoid compound comprises the following steps: pulverizing the weed grass, extracting with an organic solvent, degreasing, and separating and purifying by column chromatography. The diterpenoid compound exhibits a growth inhibitory effect on various microorganisms, especially methicillin-resistant Staphylococcus aureus (MRSA) and fungi, and is a class of compounds with application prospects. When preparing antimicrobial drugs, the diterpenoids can be used alone or in combination to prepare tablets, injections, capsules, granules, powders, suppositories, ointments, sprays, gels, lotions, and films , liniment, foam and other dosage forms. The invention has the advantages of simple preparation, low cost and high production efficiency, and is very suitable for industrialized production.

The invention relates to a medicinal diterpenoid compound separated from dried aerial parts of Callicarpa nudiflora and a preparation method of the compound. The diterpenoid compound is reported for the first time, adopts a novel structure, and can be obtained through extraction from the dried aerial parts of the Callicarpa nudiflora, separation and purification. In-vitro tests prove that the compound plays a role in inhibiting human brain glioblastoma U251 cells by inhibiting cell proliferation and inducing cell apoptosis and can be developed into drugs for treating neuroglioma.

The invention discloses a diterpene position extract of Siegesbeckia orientalis L., wherein the content of diterpene compounds in the extract is at least 40%, the content of kirenol is at least 7%. The invention also provides the process for preparing the extract and its use in preparing medicament for the treatment of rheumatism and rheumatoid diseases.