138 results about "Terpenoid Indole Alkaloids" patented technology

The present invention relates to spray dried hydrophobic phytochemical (i.e., yohimbine and ibogaine) compositions, a process for making such compositions and a method of using such compositions for, e.g., the promotion of weight loss. Typically, the hydrophobic dietary compositions of the present invention exhibit enhanced absorptivity when taken orally.

The present invention pertains to a composition comprising Ibogaine, an indole alkaloid, its active salts and its principal metabolite noribogaine, a demethylated form of ibogaine, for the treatment of hepatitis C and hepatitis C related complications, administered in single or multiple dose regimens effective to reduce somatic complaints, liver enzyme values and viral load caused by chronic hepatitis C in patients, and methods of using the same.

The invention discloses application of a class of indole alkaloids to preparation of a marine biofouling prevention coating material. The (E)-3-(1H-imidazole-4-yimethylene)-6-(1H-indl-3-ylmethyl)-2,5-piperazinediol (figured in formula 1), the meleagrin (figured in formula 2), the glandicoline B (figured in formula 3), the 11alpha-methoxyroquefortine C (figured in formula 4), the fumiquinazoline D (figured in formula 5), the cyclotryprostatins B (figured in formula 6) and the fumiquinozaline G (figured in formula 7), which are provided by the invention, have marine biofouling prevention activity and can be used for preparing the marine biofouling prevention coating material; if the compounds permeate or diffuse into film forming natural resin, polyethylene ethyl acetate copolymer and other polymers such as hydrolyzable, soluble or insoluble resin in an independent or combined way to prepare the marine biofouling prevention coating material, the marine biofouling prevention coating material can release sufficient effective components to a surface to achieve an antifouling function; and as the compounds are natural active ingredients, are hard to dissolve in water but easy to dissolve low-polarity organic solvents such as chloroform and ethyl acetate, and have favorable oleophilic properties, the components can be applied to preparing the marine antifouling agents in an independent or combined way and have a favorable application prospect.

Indole alkaloid derivatives having an opioid receptor agonistic effect, their synthesis, and therapeutic compositions containing these derivatives, and methods of treating conditions with these compounds and therapeutic compositions, are provided.

The invention discloses a process for preparing Cinobufacini freeze dried injection, which is prepared from indole alkaloid significant part extracted from dried toad peels and medicinal adjuvant through freeze drying, the Cinobufacini significant part is prepared through warm water extraction, centrifuging, and ultrafiltration purification.

The invention relates to the field of anti-tumor drugs, and specifically discloses an indole alkaloid adduct, and a preparation method and an application thereof in preparing an anti-tumor drug. The indole alkaloid adduct has a structure shown as a formula I, wherein R is formed in the way that an indole alkaloid is subjected to hydrazinolysis and the hydrazinolysis product is bonded with hydrazine group. The indole alkaloid adduct can significantly reduce toxicity to normal cells and in-vivo toxicity and inhibit in-vitro proliferation of various tumor cell lines and the growth of tumor in the nude mouse bearing the tumor.

The invention provides a method for measuring the contents of indole alkaloids in cinobufagin alcohol precipitation liquid. The alcohol precipitation method is a key unit operation in the production process of cinobufagin injection and a quick and effective content analysis method aiming at the alcohol precipitation process is especially important. The method comprises the following steps of: collecting a representative alcohol precipitation liquid sample as a correction set; measuring the contents of the indole alkaloids by adopting ultraviolet visible spectrophotometry and scanning a near-infrared original spectrum chart of the bisindole alkaloids at the same time; selecting a proper spectrum preprocessing method, a modeling spectrum section and a main factor number; and constructing a near-infrared quantitative correction model of the indole alkaloid of the alcohol precipitation liquid sample and quickly measuring the content of the cinobufagin alcohol precipitation liquid sample with the unknown content by using a chemometric method. The invention has the advantages of quickness, no damage and accuracy, can effectively solve the problems of lacking of quality monitoring and batch difference in the alcohol precipitation process and provides a new idea and means for quality control of the traditional Chinese medicine process.

The invention discloses a 3, 3'-disubstituted 3-pyrrole oxoindole compound and an asymmetric synthetic method thereof and belongs to the fields of organic chemistry and medicines. The structure of the compound takes the 3, 3'-disubstituted 3-pyrrole oxoindole compound as a framework, and the type of indole alkaloid is enriched so as to provide a sufficient compound source for screening pharmaceutical activity. Meanwhile, a synthetic method of the compound is provided. The asymmetric synthetic method comprises the following steps: dissolving 3-pyrrole oxoindole, an electrophilic reagent and a chiral catalyst in an organic solvent; carrying out a reaction at (-20)-25 DEG C; after reaction, separating and purifying to obtain the compound. The method is mild in reaction condition, easy in obtaining of raw materials and catalyst, free from metal residues, simple to operate, high in yield and further high in stereoselectivity.

The invention relates to indole alkaloid formalardeemin shown in a chemical structural formula ((-)-5-N-formalardeemin), pharmaceutically acceptable salts of the same, and application of the indole alkaloid formalardeemin serving as an anti-tumor medicament in curing malignant tumors of human beings. The indole alkaloid formalardeemin serving as an anti-tumor medicament can not only inhibit the growth of malignant tumors directly, but also can be used as a chemosensitizer when used together with other anti-tumor medicaments such as doxorubicine, vincristine and the like to achieve the effect of effectively killing tumor cells by reversing the multi-drug resistance of the tumor cells. More significantly, compared with the indole alkaloid formalardeemin serving as a tumor cell growth inhibitor directly, the indole alkaloid formalardeemin serving as the chemosensitizer has a better effect, so the indole alkaloid formalardeemin has important clinical application prospect.

A method for modulating in a cell the expression of one or more genes involved in the biosynthesis of a metabolite or a precursor for this metabolite by inserting into a cell a nucleotide sequence coding for a transcription factor comprising an AP2 DNA-binding domain, and/or by modifying the expression of a nucleotide sequence coding for such a transcription factor already present in the cell is provided. The method is useful for enhancing the biosynthesis of secondary metabolites in plants such as alkaloids including terpenoid indole alkaloids. Also provided is a method for enhancing stress tolerance in plants by the use of such transcription factors.

The invention relates to the field of traditional Chinese medicine extraction and separation, in particular to two indole new alkaloid compounds extracted, separated and identified from purslane, andan extraction and separation method and application thereof.The molecular formulas of the two new indole alkaloid compounds separated from purslane medicinal materials are respectively C17H13NO4 and C18H15NO5, and are respectively named as oleraindole A and oleraindole B.The invention also provides theextraction and separation method of the two new alkaloid compounds, which comprises the followingsteps of: sequentially adopting water decoction and extraction, silica gel column chromatography, polyamide column chromatography, ODS medium pressure column, and Sephadex LH-20 purification and liquid phase separation to preparethe two new alkaloid compounds. The structure of thetwo new alkaloid compounds is determined by ultraviolet, infrared, mass spectrum, hydrogen spectrum, carbon spectrum and two-dimensional nuclear magnetic spectrum analysis.The two indole new alkaloid compounds extracted from the purslane have anti-inflammatory, anti-tumor and nerve protection effects, and the salt orderivative of thetwo indole new alkaloid compounds can be used as a leading substance for synthesizing other compounds, as well as raw materials for new drug development and pharmacological activityresearch, and can be used for preparing anti-inflammatory, anti-tumor and nerve protection drugs.

The invention provides a kind of indole alkaloids possessing a 1,2,4-oxadiazole fragment, and a preparation method and application thereof. The structure of the indole alkaloids is shown as a formula I, and in the formula I, A, R and n are defined as the specification and the claims. The indole alkaloids are novel in structure, the synthetic route is simple in operation, the yield is high, the safety is good, and the indole alkaloids possess obvious protection effect on beta-amyloid protein, hydrogen peroxide and oxygen-glucose deprivation induced nerve cell damage, and are applicable to prepare medicines for preventing and/or treating nervous system degenerative diseases.

The invention relates to a drug of indole alkaloid, and particularly relates to application of rhynchophylline in preparation of adrug with an anxiolytic effect and an antidepressant effect. The drug disclosed by the invention is composed of the rhynchophylline and pharmaceutical acceptable auxiliary materials, wherein the content of the rhynchophylline is 1-99.5%. The drug disclosed by the invention is oral preparations and can be tablets, capsules or the like.

The present invention relates to the field of plant secondary metabolites, particularly terpenoid indole alkaloids. More particularly the present invention relates to the production of the anti-cancer metabolites vincristine and vinblastine. The invention provides novel polynucleotide sequences derived from Catharanthus roseus and the use of said polynucleotide sequences to stimulate the production of vinblastine and/or vincristine in plants of Catharanthus roseus and plant cell lines derived thereof. The invention further relates to recombinant plants, plant cells, tissue and organ cultures obtainable by the process of the invention.

The invention belongs to the technical field of medicine, and provides activities and structure of new indole alkaloid compounds 1-10 derived from insect symbiotic bacterium Chaetomium globosum secondary metabolite and also provides a separation purification preparation method and related activities of compounds pillworm chaetoglobosins E and H with favorable antitumor activity. The structural formula is disclosed as (I). The invention provides an alternative compound for developing new antitumor drugs, and has very important meanings for development and utilization of medicinal insect symbiotic bacterium resources.

This invention discloses chemical structure and extraction method of indole alkaloids including flabelliform dine (EF-14) from Ervatamia flabelliformis Tsiang. This invention also discloses the application of the indole alkaloids and their salts for manufacturing analgsics, drugs or food for treating opioid dependence.

The invention discloses a quinoline-aspidospermine bi-indole alkaloid compound. The quinoline-aspidospermine bi-indole alkaloid compound has the structural formulas shown in a formula I and a formulaII (please see the specification for the formula I and the formula II), wherein R1-R4 are correspondingly selected from hydrogen, hydroxy, methoxyl, ethyoxyl, acetyl, alkyl hydrocarbon and halogen. The experiment proves that the compound has the anti-inflammatory activity, the compound provides a lead compound for development of an anti-inflammatory preparation, and development and utilization ofplant medicinal resources are facilitated.

Most atitumor drugs clinically applied at present have the disadvantages of unsatisfactory curative effect and high toxicity. The invention provides a tetracyclic indole alkaloid imidazolisopropylacetyltheaninecarbobenzoxypyridoindole, and a preparation method and an application thereof. In the physiologic pH environment, the imidazolisopropylacetyltheaninecarbobenzoxypyridoindole can form a nanostructure which can be adsorbed by tumor cells, and the nanostructure of the imidazolisopropylacetyltheaninecarbobenzoxypyridoindole inhibits the tumor cell proliferation in vitro, and enters the tumor cells to induce the excess autophagy of the tumor cells in order to cause rupture death because of accumulation of autophagosomes in the tumor cells. The imidazolisopropylacetyltheaninecarbobenzoxypyridoindole is a nanometer antitumor agent having a brand new action mechanism, and has a broad clinic application prospect.

The invention belongs to the technical field of medicine, and relates to a sowbug symbiotic bacterium of chaetomium globosum and application thereof to the preparation of indole alkaloid compounds with the antitumor effects. The invention provides activity and structures of new indole alkaloid compounds 1 to 10 from the secondary metabolites of the chaetomium globosum, and provides a separation purification preparation method and structure identification of the new compounds. The chaetomium globosum provided by the invention is preserved in CCTCC (China Center for Type Culture Collection), andhas the strain preservation number being CCCC M2016343. The preservation time is June 23, 2016; the preservation address is Wuhan University, Wuhan, China. The invention provides backup compounds fordeveloping the novel anti-tumor medicine, and has the important significance on the development and utilization of medical insect symbiotic bacterium resources.

The biosynthesis of fungal bicyclo[2.2.2]diazaoctane indole alkaloids with a wide spectrum of biological activities have attracted increasing interest. Their intriguing mode of assembly has long been proposed to feature a non-ribosomal peptide synthetase, a presumed intramolecular Diels-Alderase, a variant number of prenyltransferases, and a series of oxidases responsible for the diverse tailoring modifications of their cyclodipeptide-based structural core. Until recently, the details of these biosynthetic pathways have remained largely unknown due to lack of information on the fungal derived biosynthetic gene clusters. Herein, we report a comparative analysis of four natural product metabolic systems of a select group of bicyclo[2.2.2]diazaoctane indole alkaloids including (+)/(−)-notoamide, paraherquamide and malbrancheamide, in which we propose an enzyme for each step in the biosynthetic pathway based on deep annotation and on-going biochemical studies.

The invention provides a preparing method of a compound brucea javanicaseed oil liposome freeze-dried powder, and belongs to the technical field of traditional Chinese medicine preparation. The preparing method is characterized by comprising the following steps: 1) weighing soybean phospholipids, cholesterol, vitamin E and brucea javanicaseed oil, dissolving by ethanol, and taking as an oil phase; 2) measuring a toad venom aqueous extract, adding mannitol and sucrose, and adding distilled water to as an aqueous phase; 3) injecting the oil phase into the aqueous phase, and extruding by a micropore filter membrane to obtain a suspension; 4) filling a penicillin bottle with the suspension, carrying out freeze drying, and thus obtaining the compound brucea javanicaseed oil liposome freeze-dried powder. The preparation method of the compound brucea javanicaseed oil liposome freeze-dried powder adopts the brucea javanicaseed oil and toad venom for combined application, the average encapsulation rate of the prepared liposome freeze-dried powder is 91.90%, the average content of indole alkaloids is 5.19*10<-3> mg.g<-1>, the average content of oleic acid is 79.08 mg.g<-1>, the average content of linoleic acid is 50.41 mg.g<-1>, the antitumor effect is good, and toxic and side effects are small.

The invention discloses a method for generating 3-substituted-2-indolone compounds by use of a Knoevenagel condensation reaction with aromatic aldehydes and indol-2-ones as substrates and lipase as a catalyst. The 3-substituted-2-indolone compounds are important intermediates for synthesizing indole alkaloids, and meanwhile, and have wide pharmacological and physiological activity. According to the method, the product yield is 87.8-94.2%; the method is mild in reaction conditions, simple to operate, low in production cost, high in yield, wide in substrate spectrum and low in environmental pollution.