667 results about "Diterpene" patented technology

Several diterpene glycosides (e.g., rubusoside, rebaudioside, steviol monoside and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, and celecoxib. The use of the diterpene glycoside rubusoside increased solubility in all tested compounds. The diterpene glycosides are a naturally occurring class of water solubility-enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries. Aqueous solutions by using rubusoside to increase the solubility of otherwise insoluble drugs will have several new routes of administration. In addition, aqueous solutions of therapeutic compounds with rubusoside were shown to retain the known pharmacological activity of the compounds.

Enhanced methods have been discovered, using either sonication or homogenization followed by increased temperature and pressure, to solubilize compounds using diterpene glycosides and to produce a powder form of the compound-solubilizer complex than can be reconstituted in water. Without the diterpene glycoside, the compounds were insoluble or sparingly soluble in water, including some fat-insoluble vitamins. Water solutions of these compounds were made using a diterpene glycoside solubilizer, for example, rubusoside. The compound-solubilizer complex was then dehydrated to a stable powder that could then be reconstituted with water. A reconstituted drug-solubilizer complex (curcumin-rubusoside) was shown to be effective on reconstitution. In addition, the diterpene glycoside, rubusoside, was shown to be an inhibitor of permeability glycoprotein (P-gp), and will thus increase gastrointestinal absorption of certain drugs administered with rubusoside.

The present invention provides isolated or essentially pure diterpenoic tetrahydropyran, such as steviol-19-glucuronide, steviol, stevioside and rebaudioside processes for obtaining the same and methods for obtaining stable pharmaceutically acceptable salts of the same for use of such compounds or compositions in a treatment of cardiovascular disorders or vascular disease or for the manufacture of medicaments to treat a condition of a cardiovascular disorder or vascular disease.

The present invention relates generally to chemical agents useful in the treatment and prophylaxis of infection by pathogenic or potentially pathogenic entities, or entities capable of opportunistic infection in mammals, including humans and primates, non-mammalian animals and avian species. More particularly, the present invention provides a chemical agent of the macrocyclic diterpene family obtainable from a member of the Euphorbiaceae family of plants or botanical or horticultural relatives thereof or derivatives or chemical analogues or chemically synthetic forms of the agents for use in the treatment or prophylaxis of infection by pathogenic entities in mammalian, animal and avian subjects. The present invention further contemplates a method for the prophylaxis and / or treatment in mammalian, animal or avian subjects of infection or potential infection by pathogenic entities by the topical or systemic administration of a macrocyclic diterpene obtainable from a member of the Euphorbiaceae family of plants or their botanical or horticultural derivatives or a derivative, chemical analogue or chemically synthetic form of the agent. The chemical agent of the present invention may be in the form of a purified compound, mixture of compounds, a precursor form of one or more of the compounds capable of chemical transformation into a therapeutically active agent or in the form of a chemical fraction, sub-fraction, preparation or extract of the plant.

The invention discloses a rosinyl bis-quaternary ammonium surfactant, the general molecular formula of which is as follows. In the formula, R is a rosinyl ricyclic diterpene structure, X is Br or I, and n is larger than or equal to 1 and smaller than or equal to 10. The invention also discloses a method for preparing the compound: firstly, dehydroabietic acid or disproportionated rosin is adopted to prepare rosinyl tertiary amine, and then the rosinyl tertiary amine and saturated dihalide are prepared into the rosinyl bis-quaternary ammonium surfactant through quaternization. The synthesis of the rosinyl tertiary amine comprises the following steps: the dehydroabietic acid or the disproportionated rosin is converted into active acyl chloride intermediate, and then the acyl chloride intermediate and N,N-dimethyl ethanolamine are prepared into the rosinyl tertiary amine in the presence of the triethylamine which is used as the acid-binding agent. The rosinyl tertiary amine and the saturated dihalide are reacted in the solvent isopropyl alcohol, and then vacuum drying is performed after filtration. The prepared surface active agent has good surface activity performance; the raw material is inexpensive and easy to obtain, and can be biodegraded; the synthetic method is assisted with microwave, the reaction time is short, and the product purity is high.

Cosmetic or dermopharmaceutical compositions containing, in a dermatologically acceptable carrier, at least one diterpene among: cafestol, kahweol and chemical derivatives are useful for slimming treatments including prevent and / or treat cellulite or orange peel and / or to refine contours of the face, skin firming, to reduce the steatomery of the thighs, to decrease the volume / fatty overload of the spare tire at the hips, to reduce “love handles”, both on men and women.

A raw green coffee bean extraction method and coffee extract end product. The method produces a coffee extract end product which contains antioxidants (phenolic compounds), diterpenes (having detoxification properties), has greater bioavailability and greater ability to quench oxidative stress in comparison to existing polyphenol extracts.

A pressure-sensitive adhesive, comprising a polymer (A), which is formed by polymerization of a radical polymerizable monomer, contains carboxyl groups, and has a glass transition temperature within a range from −80 to 0° C. and a weight average molecular weight within a range from 500,000 to 1,500,000, a tricyclic diterpene carboxylic acid (B), and a curing agent (C) capable of reacting with a carboxyl group, wherein the total acid value of the combination of the polymer (A) and the tricyclic diterpene carboxylic acid (B) is within a range from 5 to 50 (mgKOH / g).

The invention concerns a method for producing terpenes of interest in plants having glandular trichomes, as well as plants useful for producing said terpenes of interest. Said plants comprise a sequence encoding a heterologous terpene synthase under the control of a promoter enabling it to be specifically expressed in the trichomes. Moreover, the pathway for producing endogenous diterpenes is preferably blocked in the trichomes of the plants, to increase the flow in the heterologous pathway. The secretion of heterologous terpenes is spontaneous resulting in easy collection. The present invention also concerns plants exhibiting a blocked production of a compound having antibiotic properties at the surface of leaves exhibiting enhanced efficiency of transformation by a bacterium.

The invention relates to C19-diterpenoid alkaloid which has cardiotonic and hart failure-resistance activities and is shown in the formula I, pharmaceutically acceptable salts of the C19-diterpenoid alkaloid, preparation methods of the C19-diterpenoid alkaloid and the salts, and medicines containing the C19-diterpenoid alkaloid and the salts, as well as application of the C19-diterpenoid alkaloid and the salts as medicines with cardiotonic and hart failure-resistance effects. In the formula I, R1 is hydrogen, hydroxyl or methoxyl; R2 is hydrogen or methyl; and R3, R4 and R5 represent hydrogen or hydroxyl.

Aqueous solutions of diterpenes such as Forskolin, its congeners, analogs and derivatives, up to approximately 6% concentration, are prepared using suitably substituted cyclodextrin as a solubilizing agents. In the absence of cyclodextrin, some diterpenes such as Forskolin are soluble in water only to concentrations of about 0.001%. Such aqueous solutions find applications in topical and systemic use, as pharmaceutical, cosmeceutical, nutraceutical preparations containing diterpenes such as Forskolin and congeners.

The present invention is directed to a unicellular organism system, such as a yeast, for producing geranylgeranyl pyrophosphate and a diterpene in vivo. The yeast cell preferably comprises an inducible nucleic acid sequence encoding geranylgeranyl pyrophosphate synthase, an inducible nucleic acid sequence encoding a soluble form of HMG-CoA reductase, a nucleic acid sequence of an allele that confers an increase in sterol metabolic flux and, in the diterpene-producing cell, a diterpene synthase.

A chemical agent of the diterpene family obtained from a member of the Euphorbiaceae family of plants for use in the treatment of prophylaxis of prostate cancer or a related cancer or condition.

The invention discloses a rosinyl sulphonate gemini surfactant, the general structure thereof is shown in the right formula, R represents rosinyl tricyclic diterpene group and is an integer less than or equal to 1 and greater than or equal to 5. The preparation method is as follows: nucleophilic reaction is carried out on dehydro-abietylamine or disproportionated rosin and dibromoalkane to obtain an active intermediate N, N'-didehydro-abietylamine base alpha, omega-diamine which is then used to react with 2-bromoethyl sodium sulfonate to obtain the rosinyl sulphonate gemini surfactant. The surfactant prepared by the invention has better water solubility, very high surface activity and ability of reducing oil / water interfacial tension, excellent solubilization, salt-resistance, anti-deposition and wetting properties for oil, cheap and accessible raw materials and low toxicity, and is biodegradable.

The invention discloses a method for synthesizing a novel tetracyclic diterpene compound from stevioside, which is cost-efficient and feasible. The compound is represented by a general formula (I), wherein the definitions of R1, R2, X, Y are shown in the specification. The invention discloses a potential application value of the compound in the aspects of anti-tumor and anti-inflammation and a detailed preparation method of the compound as well as physical data of Fourier transform infrared spectroscopy (FT-IR), hydrogen nuclear magnetic resonance spectroscopy (1 HNMR), mass spectrometry (MS) and the like.

The present invention relates to useful diterpenes and pharmaceutical compositions containing them of the formula:for use in the treatment of cardiovascular and inflammatory diseases and for cancers susceptible to an NF-κB inhibitor and an endothelin receptor inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.

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 discloses a diterpenoid compound and the preparing method and application thereof. The diterpenoid compound is obtained by using aralia melanocarpa roots as the raw material through extractum extraction, organic solvent extraction, column chromatography on silica gel and high pressure liquid chromatography separation. The molecular formula of the diterpenoid compound is C20H30O3. The name of the diterpenoid compound is 14-oxygen-ent-8(9),15-(14-oxo-ent-pimara-8(9),15-diene-19-oic acid). The structural formula is as shown in the specification. According to the preparing method, aralia melanocarpa roots are used as the raw material, and extractum extraction, organic solvent extraction, column chromatography on silica gel and high pressure liquid chromatography separation are conducted to generate the diterpenoid compound. The diterpenoid compound can be applied to preparation of anti-inflammatory drugs for prevention and / or treatment. The diterpenoid compound is subjected to in-vitro anti-inflammatory activity testing, and experimental results show a good lipopolysaccharide (LPS) restraining effect and a good effect of inducting pulmonary alveolar macrophages (RAW264.7) to generate NO. A new compound or lead compound with high application value can be provided for the medical industry.

This invention relates to a method for preparing roinyl diterpene modified alpha-aminophosphate, and its anti-tumor application. The method comprises: reacting roinyl amine diterpenoid with substituted benzaldehyde and phosphite at a mol ratio of 1 :( 1-1.05) :( 1-1.1) by solvent synthesis, one-pot synthesis or solvent-free synthesis. The inroduction of roinyl diterpene into aminophosphate can largely improve the liposolubility and bioactivity of the compound. R1 structure comes from natural product rosin, thus has low toxicity.

Single-phase microemulsions, comprising a solvent, a surfactant blend and a carrier fluid, are effective spacer fluids for use during cementing operations. The solvent may be selected from the group consisting of monoterpenes, diterpenes, and alkyl or aryl esters of short-chain alcohols. The surfactant blend comprises a water-wetting surfactant or nonionic surfactant, a co-surfactant and an oil-solubilizing surfactant. The carrier fluid is aqueous. The solvent and surfactant blend are combined with the carrier fluid to produce the well-treatment microemulsion.

The present invention relates generally to chemical agents useful in the treatment and prophylaxis of inflammatory conditions or in the amelioration of symptoms resulting from or facilitated by an inflammatory condition in a mammalian animal including human and primate, non-mammalian animal and avian species. More particularly, the present invention provides a chemical agent of the macrocyclic diterpene family obtaining from a member of the Euphorbiaceae family of plants or botanical or horticultural relatives thereof or derivatives or chemical analogues or chemically synthetic forms of the agents for use in the treatment or prophylaxis of an inflammatory condition or in the amelioration of symptoms resulting from or facilitated by an inflammatory condition in a mammal, animal or avian species. The present invention further contemplates a method for the prophylaxis or treatment of mammalian, animal or avian subjects for inflammatory conditions including chronic or transitory inflammatory conditions or for ameliorating. the symptoms of an inflammatory condition by the topical or systemic administration of a macrocyclic diterpene obtainable from a member of the Euphorbiaceae family or botanical or horticultural relatives thereof or a derivative, chemical analogue or chemically synthetic form of the agent. The chemical agent of the present invention may be in the form of a purified compound, mixture of compounds, a precursor form of one or more of the compounds capable of chemical transformation into a therapeutically active agent or be in the form of a chemical fraction, sub-fraction or preparation or extract of the plant.

Disclosed herein are sweetener compositions comprising at least one sweetener and at least one sweetness enhancer chosen from terpenes (such as sesquiterpenes, diterpenes, and triterpenes), flavonoids, amino acids, proteins, polyols, other known natural sweeteners (such as cinnamaldehydes, selligueians, hematoxylins), secodammarane glycosides, and analogues thereof, wherein the at least one sweetness enhancer is present in the composition in an amount at or below the sweetness detection threshold level of the sweetness ehancer, and the at least one sweetener and the at least one sweetness enhancer are different. Also disclosed herein are methods for enhancing sweetness of a composition, comprising combining at least one sweetener and at least one sweetness enhancer chosen from terpenes (such as sesquiterpenes, diterpenes, and triterpenes), flavonoids, amino acids, proteins, polyols, other known natural sweeteners (such as cinnamaldehydes, selligueians, hematoxylins), secodammarane glycosides, and analogues thereof, wherein the at least one sweetness enhancer is present in the composition in an amount at or below the sweetness detection threshold level of the at least one sweetness enhancer, and the at least one sweetener and the at least one sweetness enhancer are different.

The invention discloses a CYP450 (Cytochrome P450) gene participating in tanshinone biosynthesis and a coded product as well as application thereof, and belongs to the field of medicinal plant genetic engineering. The gene is firstly obtained through cloning from salvia miltiorrhiza bunge, is a key enzyme gene for a biosynthesis pathway of a tanshinone compound and is a key step of catalyzing miltiradiene to ferruginol. The CYP76Q1 gene provided by the invention has a nucleotide sequence shown by SEQ ID NO. 1. Protein coded by the gene has an amino acid residue sequence shown by SEQ ID No. 2 in a sequence table and protein with the same activity as that of the amino acid residue sequence shown by the SEQ ID No. 2 and derived from the SEQ ID No. 2. The CYP76Q1 gene provided by the invention is closely associated with biosynthesis of the tanshinone compound, has great theoretical and actual significance to regulating and producing a plant diterpene compound and improving the content of the diterpene active ingredient tanshinone in the salvia miltiorrhiza bunge through a biotechnology, contributes to quality improvement of the salvia miltiorrhiza bunge medicinal material and variety selection, also has the capacity of producing ferruginol monomer with pharmacological activity by constructing engineering bacteria using the gene, and has excellent application prospect.

The invention relates to the field of pesticides, in particular to application of a diterpene alkaloid compound serving as a secondary metabolite of a seaweed endophytic fungus. The diterpene alkaloid compound serving as the secondary metabolite of the seaweed endophytic fungus has insecticidal effect and is shown as a formula (I). The natural diterpene alkaloid compound is obtained by extractingand separating yeast of Aspergillus oryzae cf-2 fungus separated from ocean red alga heterosiphonia; and by insecticidal activity experiments, the fatality rate of artemia is 74.2 percent when the diterpene alkaloid compound is 100 micrograms per milliliter.

The invention relates to tripterygium wilfordii diterpenes lactone derivates represented by the formula (1), optical isomers thereof and pharmaceutically acceptable salts and hydrate thereof, wherein C5 and C6 are combined by C-C or C=C bind; P and Q represent hydrogen, oxygen, hydroxyl, halogen, sulfhydryl, C1-C6 alkoxyl, C1-C6 alkylamino radical, or C1-C6 alksulfhydryl combined on positions C5 or C6 respectively when C5 and C6 are combined by C-C bind; and C14XY is combined at the position C14 with the structure shown in the view, and W and Z represent oxygen, hydroxyl, halogen, sulfhydryl, C1-C6 alkoxyl, C1-C6 alkylamino radical, or C1-C6 alksulfhydryl combined on positions C12 or C13 respectively, '-'combined with X, Y, Z, W, P and Q represent '' '' or '' ''. The invention further relates to a synthetic method thereof and the applications on preparing the medicine for treating hypertrophic tumor.

Compositions comprising an effective amount of a curcuminoid species and an effective amount of a diterpene lactone species, a triterpene species or derivatives thereof that have a synergistic effect on specific inhibition of inducible COX-2 activity and have minimal effect on COX-1 activity are disclosed. Methods of using the compositions for providing synergistic anti-inflammatory effects are also disclosed.

A method of inhibiting excitotoxicity by indirectly activating α4β2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of α7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate α4β2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis.

The invention relates to a method used for extracting cembrenediols from tobacco inflorescence. The method comprises following steps: 1, an organic solvent is adopted to extraction and condensation so as to obtain a tobacco flower surface glandular hair secreta crude extract; 2, the crude extract is subjected to solvent precipitation so as to remove higher alkanes, and pigments are removed with active carbon so as to obtain a tobacco diterpene extract product, wherein the tobacco diterpene extract product possesses broad-spectrum inhibition effect on plant pathogenic fungi, and especially excellent inhibition effect on apple rot; 3, the tobacco diterpene extract product is subjected to silica gel column chromatography successively so as to obtain two main diterpene compounds alpha-4,8,13-cembratriene-1,3-diol, and beta-4,8,13-cembratriene-1,3-diol with antitumor activity, neuroprotective agent activity, and bacteriostatic activity. Waste tobacco inflorescence is taken as the raw material, so that utilization of waste resources is realized; extraction step is simplified greatly, and cost is reduced; and product yield and purity are high.