22 results about "Indole alkaloid" patented technology

The invention provides a planting method for promoting synthesis of camptothecin and derivatives thereof from nothapodytes pittosporoides. The planting method comprises the following steps: planting a plurality of nothapodytes pittosporoides trees in a planting field; organic fertilizer is applied to the multiple planted nothapodytes pittosporoides trees every first preset time; the planted nothapodytes pittosporoides trees are soaked with cold water for several days, and temperature and water stress is carried out; removing the nothapodytes nothapodytes which do not survive after water stress; introducing microorganisms every second preset time to adjust rhizosphere microorganisms of the nothapodytes pittosporoides trees so as to carry out microorganism stress; watering is stopped in autumn, so that the survival nothapodytes nothapodytes trees are subjected to sunlight stress, and the survival nothapodytes nothapodytes trees enter the sunlight stress period; in the sunlight stress period, synthesis of terpene indole alkaloid of rhizosphere microorganisms is activated, and synthesis of camptothecin and derivatives of camptothecin from nothapodytes pittosporoides is promoted; wherein except for the sunlight stress period, the environment temperature of the planting field is kept at 5 DEG C or above, and the environment humidity is kept at 63%-78%.

The application discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method thereof and application of the compound in preparation of an antitumor chemotherapy drug sensitizer, and first prepares the steroid-indole diketopiperazine alkaloid hybrid compound from a fungus Aspergillus sp. EGF15-0-3 rice culture medium. The compound is a new skeleton compound first discovered in nature. It is first discovered that the hybrid compound has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. It is first discovered that the hybrid compound has chemotherapy sensitization activity on a tumor chemotherapy drug topotecan TPT, which provides a drug source molecule and data support for development of a new natural antitumor combination inhibitor, and has important significance for development and utilization of marine Aspergillus sp. fungus resources.

The invention discloses a biphenyl-diketopiperazine indole alkaloid hybrid compound, which is separated from a fermentation product of a strain Aspergillus candidus HNNU0546, and has a skeleton molecule formed by hybridizing rare diketopiperazine indole alkaloid with biphenyl molecules through an isopentenylation branch chain, and the biphenyl compound can obviously inhibit the activity of crop disease fungi.

The application discloses a synthesis method and application of an indole alkaloid derivative. The method uses 5-aminoindole or 6-aminoindole as a substrate, reacts with acyl chloride or carboxylic acid to obtain an intermediate, and then reacts with Hydroxyclavatol to obtain a Penindolone (PND) derivative of the application. The method has the advantages of easy availability of raw materials, short reaction time, few steps involved, simple post-treatment and the like. The indole alkaloid PND derivative prepared by the method has good anti-influenza virus activity and wide application prospect.

The invention belongs to the field of organic chemical synthesis, and relates to a method for synthesizing a natural product Pyrroloazocine indole alkaloid skeleton. According to the method, a commercially available compound 1 and phenylhydrazine are taken as synthesis starting points, and a [2.2. 2] bridge ring system is constructed through key Fischer indole synthesis, Stille coupling reaction and intermolecular Diels-Alder reaction. The preparation method comprises the following steps: carrying out a cyclopropanation reaction mediated by carbene, carrying out a Ley-Griffith oxidation reaction, and carrying out a Beckmann rearrangement and an intramolecular SN2 cyclization cascade reaction so as to realize the construction of the core skeleton of the Pyrroloazocine indole alkaloid. According to the method, a material basis can be provided for activity testing of the Pyrroloazocine indole alkaloid and the analogue thereof, and a thought is provided for synthesis route design of more complex cage-shaped indole alkaloid basic frameworks.

The invention provides a preparation method of a natural product indole alkaloid TMC-205, which comprises the following steps: introducing-COCF3 to the 3-site of indole, hydrolyzing-COCF3 to generate TMC-205 or introducing-CHO to the 3-site of indole, and then introducing-CHO to the 3-site to carry out two lines of Pinnick oxidation to generate TMC-205, by establishing an intermediate, the selectivity is high, the side reaction is extremely few, the problem of low yield caused by direct introduction of carboxyl is solved, and the preparation method is suitable for industrial production. According to the present invention, the method can achieve the quantitative and efficient conversion into the carboxyl group, the use of the high toxicity, the high flammability and the expensive reagent in the traditional method is avoided, and in the key step of constructing the core isoprene structure, the 6-bromoindole with the simple structure is innovatively adopted to directly carry out the Heck-dehydration reaction, such that the potential side reaction is effectively reduced, and the cost is reduced; therefore, the product yield is remarkably improved, and the method is suitable for industrial large-scale production.

The invention discloses a monoterpene indole alkaloid compound as well as a preparation method and application thereof, and belongs to the technical field of medicines. The monoterpene indole alkaloid compound disclosed by the invention is separated from ervatamia palmata, has remarkable activity for repairing podocyte injury under the hypoxia condition, and can be used for preparing a medicine for treating chronic renal injury under the hypoxia condition. The traditional Chinese medicine composition has relatively high economic benefits aiming at the current situation of non-hypoxia chronic kidney injury specific medicines.

The application discloses application of an indole alkaloid compound and derivatives in preparation of anti-liver cancer drugs and belongs to the technical field of biological medicines. A structural formula of the indole alkaloid compound is shown in the following formula: the indole alkaloid compound in the application is separated from a medicinal plant Ampelopsis megalophylla Planch, and a series of derivatives (salts) are obtained through derivation or chemical preparation, the compounds can inhibit the effect of HepG 2 human liver cancer cells, and have the drug development potential for preventing or treating liver cancer.

The invention relates to the technical field of indole alkaloid synthesis, and discloses a low-cost short-path indole alkaloid synthesis method, which comprises: mixing o-nitrobenzene acetaldehyde, a substituted amine compound and an active methylene compound according to a molar ratio of 1: (1.0-1.5): (1.0-1.2), adding a catalyst, an alkali and a solvent, carrying out a stirring reaction for 2-6 h at a temperature of 40-80 DEG C, and carrying out filtration, washing and drying to obtain the indole alkaloid. Performing post-treatment to obtain a nitro-substituted indole precursor; and mixing the nitro-substituted indole precursor with a reducing reagent according to a molar ratio of 1: (2.0-3.0), carrying out a reaction at 60-80 DEG C for 2-3 h, and carrying out post-treatment to obtain the indole alkaloid. The synthesis method is short in path, low in cost, mild in condition and suitable for industrial production.

The application discloses an indole alkaloid compound, a preparation method and application thereof in preparation of a medicine for treating chronic kidney disease, and the structure of the indole alkaloid compound is shown as formula I. The new indole alkaloid compound is extracted from fruits of a plant for the first time, the compound can significantly reverse the increase of alpha-smooth muscle actin, type I collagen and vimentin expression in HK-2 cells induced by TGF-beta, and the compound shown as formula I has a drug development potential for preventing or treating chronic kidney disease, in particular, anti-kidney fibrosis, at a concentration of 10 muM.

Disclosed is yeast cells having peroxisomally localized GPP synthase and a peroxisomally localized enzyme that converts GPP into a monoterpenoids, cannabinoids, monoterpene indole alkaloids and prenylated aromatic compounds; or a precursor therefore, which yeast cells are capable of producing improved amounts of monoterpenoids, cannabinoids, monoterpene indole alkaloids and prenylated aromatic compounds, compared with the same yeast cells where the GPP synthase and the enzyme that converts GPP are located in the cytoplasm. Further disclosed is the use of the yeast cell for producing monoterpenoids, cannabinoids, monoterpene indole alkaloids and prenylated aromatic compounds.

This invention belongs to the field of pharmaceutical technology, specifically relating to a class of sarpagine-type indole alkaloid derivatives, their preparation methods, and applications. The structural formula of this class of compounds is shown in formula (I). They exhibit good antitumor activity, low toxicity to normal cells, and are safe, effective, and low-toxicity candidate antitumor drugs.

The invention discloses a monoterpenoid indole alkaloid compound as well as a preparation method and application thereof. The monoterpenoid indole alkaloid compound has a structure as shown in any one of formulas I to XII. The invention discloses a monoterpenoid indole alkaloid compound found from a medicinal plant gossypium hirsutum, and provides an extraction and separation method, a structure identification method and an anti-inflammatory effect application of the monoterpenoid indole alkaloid compound. The monoterpenoid indole alkaloid compounds 1, 4 and 8 provided by the invention have obvious activity of inhibiting release of LPS-induced RAW264.7 macrophage NO, which proves that the prepared monoterpenoid indole alkaloid compounds have good anti-inflammatory activity and can be used for preparing natural anti-inflammatory drugs.

This invention discloses a mutant of PjTA-R6 transaminase, its construction method, and its applications. Using schizosphingine, a key precursor of large-volume monoterpene indole alkaloids, as the target for reductive amination, this invention rationally designs the PjTA-R6 transaminase through a global free energy optimization strategy, obtaining 10 mutants with significantly higher catalytic efficiencies than the original PjTA-R6 transaminase. Recombinant *E. coli* strains based on these mutants are then constructed, resulting in a substantial improvement in reductive amination catalytic efficiency. The PjTA-R6 L164E / L57F mutant provided by this invention achieves a 99% conversion rate of schizosphingine to bacamargine via whole-cell reductive amination, a 46% increase compared to the original strain. The PjTA-R6 transaminase mutant provided by this invention exhibits significant catalytic efficiency, offering a powerful tool enzyme for overcoming the industrial bottleneck of transaminase catalysis of large-volume substrates, and possesses broad application prospects.

The invention provides an asymmetric preparation method of bisindole alkaloid (S)-6 ''-Debromohaamacanthin A. The method comprises the following steps: carrying out ester group reduction reaction on a compound 1 and lithium aluminum hydride to obtain a compound 2; carrying out azide substitution reaction on the compound 2, 1, 8-diazabicyclo [5.4. 0] undec-7-ene and diphenyl azide phosphate to obtain a compound 3; performing hydrolysis reaction on the compound 2 and a hydrochloric acid solution to obtain a compound 4; the preparation method comprises the following steps: mixing 6-bromoindole with oxalyl chloride to obtain an acyl chloride compound reaction solution; then carrying out acyl chloride substitution reaction on the compound 4, an acyl chloride compound reaction solution and triethylamine to obtain a compound 5; and carrying out Staudinger reduction reaction on the compound 5 and triphenylphosphine, so as to obtain the bisindole alkaloid (S)-6 ''-Debromohaamacanthin A. The invention further discloses a preparation method of the bisindole alkaloid (S)-6''-Debromohaamacanthin A. The invention further provides application, and the target product is used for preparing anti-tumor drugs. The synthetic route is unique in design, mild in reaction condition, high in catalytic efficiency, short in route, few in side reaction and simple and convenient to operate. According to the method, the problems that the source of the natural product (S)-6 ''-Debromohaamacanthin A is limited and the extraction rate is low can be solved.

The anti-tumor pharmaceutical composition derived from the marine symbiotic bacteria comprises an active component A, an active component B and a medicinal carrier, the active component A is indole alkaloid separated from fermentation liquor of the marine symbiotic bacteria Streptomyces sp.M2021-03, and the molecular formula of the indole alkaloid is H21NO4; the active ingredient B is a polyketone compound separated from a fermentation solution of marine symbiotic bacteria Pseudomonas sp.M2021-07, and the molecular formula of the polyketone compound is C24H30O6; the medicinal carrier is a composite carrier of poloxamer 188 and beta-cyclodextrin in a mass ratio of 1: 2. The active component A (indole alkaloid) blocks mitotic division by inhibiting tumor cell microtubule polymerization, the active component B (polyketone compound) can down-regulate VEGF expression and inhibit angiogenesis, and the inhibition rates of MCF-7 and A549 cells are respectively increased by 40% and 35% compared with those of a single component when the two components are combined.

This invention belongs to the field of extraction and separation of traditional Chinese medicine, specifically relating to a method for the extraction and separation of indole alkaloids and its application. The compound is named oleraindolinpyrro, with the molecular formula C2. 12 H 14 N₂O₃, with the structural formula shown in formula (I). This invention employs ethanol reflux extraction, ODS column chromatography, Sephadex LH-20 gel column chromatography, and high-performance liquid chromatography to isolate this compound from Portulaca oleracea with a purity exceeding 96%. Pharmacological experiments show that this compound significantly inhibits the release of IL-1β and TNF-α from LPS-induced RAW264.7 macrophages, exhibiting anti-inflammatory activity. The method of this invention is simple, environmentally friendly, and produces high purity; the obtained compound can be used to prepare anti-inflammatory drugs or as a lead compound for research.

The invention discloses indole alkaloid natural product derivatives for treating drug-resistant small cell lung cancer as well as a preparation method and application of the indole alkaloid natural product derivatives. According to the method, a benzophenone diphenol derivative intermediate which is simple and easy to prepare reacts with indole to obtain the indole alkaloid natural product derivative; the method has the advantages of easily available raw materials, simple post-treatment and the like; the indole alkaloid natural product derivative prepared by the invention has good in-vivo and in-vitro small cell lung cancer drug-resistant cell activity, and has a wide application prospect.

The invention discloses tryptamine indole alkaloid as well as a preparation method and application thereof. The tryptamine indole alkaloid, the derivatives thereof, the organic and inorganic acid salts, the pharmaceutical composition containing the compounds and the plant extract can effectively treat or prevent diseases with pathological characteristics of lysosomal pathway disorders, including but not limited to anxiety, depression, neurodegenerative diseases, autoimmune diseases and the like, by adjusting TFEB. The tryptamine indole alkaloid can also be used as an IDO and MAOA inhibitor to improve diseases closely related to IDO and MAOA, including but not limited to depression, neurodegenerative diseases, autoimmune diseases and the like.

The application provides a full synthesis method of Ervitsine, and the full synthesis method of the indole alkaloid Ervitsine is prepared by using a halogenated furan as a raw material through an organic full synthesis method. The full synthesis method of the indole alkaloid Ervitsine provided by the application has the advantages of cheap and easily available raw materials, mild reaction conditions, short steps, high total yield, low production cost and good prospects for industrial production.

A compound represented by formula (I) and a preparation method thereof, and a pharmaceutically acceptable salt thereof, a metabolic precursor thereof, a metabolite thereof, an isomer thereof or a prodrug thereof; experiments show that the indole alkaloid not only promotes axon growth of peripheral sensory neurons, improves the nerve conduction velocity and anesthesia symptom of diabetic rats, but also promotes healing of foot ulcer wounds of diabetic rats, thus having good therapeutic effects on diabetic complication peripheral neuropathy and diabetic feet; they also show that the indole alkaloid also obviously reduces a degree of pulmonary fibrosis induced by bleomycin in mice, and plays a role in protecting lung tissues.