70 results about "Indole alkaloid" patented technology

The invention relates to the technical field of indole alkaloid compounds, in particular to indole pleurotus nebrodensis alkali A, a preparation method thereof and application of the indole pleurotus nebrodensis alkali A to preparation of drugs for preventing and resisting tumors. Pleurotus nebrodensis sporocarp is smashed, ethyl alcohol is added, heating reflux preparation and concentration are conducted, obtained pleurotus nebrodensis total extract is dispersed into suspension with water, and then the suspension is placed in a drying oven to be dried to obtain the indole pleurotus nebrodensis alkali A. The indole pleurotus nebrodensis alkali A is obtained. The method comprises the following steps: sequentially extracting with petroleum ether, dichloromethane and ethyl acetate, concentrating an extracting solution to obtain ethyl acetate part extract, carrying out gradient elution separation on the ethyl acetate part extract by silica gel column chromatography, carrying out gradient elution on the obtained third fraction by high performance liquid chromatography, purifying and separating, and collecting eluate to obtain the indole pleurotus nebrodensis alkali A at 16.3 minutes. The indole pleurotus nebrodensis alkali A is disclosed for the first time, and it is found through in-vitro antitumor pharmacodynamic experiments that the indole pleurotus nebrodensis alkali A has a certain inhibition effect on human HGC-27 gastric cancer cells, so that the indole pleurotus nebrodensis alkali A can be used for preparing drugs for preventing and resisting gastric cancer.

The invention relates to a novel hexahydropyrroloindole alkaloid extracted from fructus lycii, which can effectively solve the problems of extracting and preparing the novel hexahydropyrroloindole alkaloid A from the fructus lycii and realizing the application of the novel hexahydropyrroloindole alkaloid A in preparation of medicines for preventing and treating type 2 diabetes mellitus. The novel hexahydropyrroloindole alkaloid A is prepared by the following steps: sequentially eluting with water, ethanol and acetone, carrying out reduced pressure concentration on an ethanol part, extracting, stirring a sample with silica gel, carrying out gradient elution, merging the same fractions, eluting a target component, stirring the sample with silica gel, carrying out gradient elution, collecting fractions within retention time, concentrating and drying, thereby obtaining the novel hexahydropyrroloindole alkaloid A in the preparation of the medicine for preventing and treating the type 2 diabetes mellitus and the application of the novel hexahydropyrroloindole alkaloid A in the preparation of the medicine for preventing and treating the type 2 diabetes mellitus. Glucose consumption in insulin-resistant HepG2 cells can be remarkably promoted, glucose uptake capacity is improved, glycogen synthesis is promoted, activity of glycolysis key enzymes hexokinase and pyruvate kinase is enhanced, development and application prospects are wide, and economic and social benefits are remarkable.

The invention relates to the discovery of a biosynthetic gene cluster of an alkaloid, namely, exopoid C, and the biosynthetic gene cluster of the exopoid. A biosynthetic gene cluster exo of an exopoid compound is obtained from a fungus Penicillium sp.HDN14-431 through genome mining, the gene cluster comprises a heme-dependent oxidase gene exoA which is composed of indole dioxygenase and a cytochrome b5 structural domain, a cytochrome P450 enzyme gene exoB and an isopentenyl transferase gene exoC which is composed of indole dioxygenase and a cytochrome b5 structural domain, and the cytochrome P450 enzyme gene exoB and the isopentenyl transferase gene exoC are used as biosynthetic genes of the exopoid compound. All genes in a gene cluster are expressed through an aspergillus nidulans heterologous expression system, two isopentenyl indole alkaloids are obtained in total, and a compound I is a new compound exopoid C. And the compound II, namely the exopoid, is a known compound. The biosynthesis pathway of the compound is reported for the first time.

The invention discloses a method for synchronously, efficiently and directionally preparing indirubin and tryptanthrin by using a blue grass raw material, which comprises the following steps: pretreating blue grass to obtain blue grass powder or slurry; adding water into the blue grass powder or slurry, then adding a precursor substance, and carrying out ultrasonic or microwave treatment; according to different target products, static conversion or dynamic conversion can be carried out, or static conversion or dynamic conversion is carried out after microorganisms producing cellulase and oxygenase are inoculated, and the products are subjected to post-treatment such as drying and grinding. The method is simple to operate, high in processing efficiency, flexible in product scheme, low in production cost and suitable for large-scale production. The content of the indole alkaloid in the obtained material rich in the indole alkaloid is 1%-10%; the yield of indirubin reaches 5.64 mg / g, which is 21.7 times that of the traditional process; and the tryptanthrin yield reaches 7.68 mg / g, which is 10.8 times that of the traditional process.

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%.

Provided are indole alkaloid compounds in a noni enzyme, wherein the structural formula is shown in the following formula:Provided is a preparation method of the above-mentioned compound and application of the indole alkaloid compound in the noni enzyme in the preparation of an α-glucosidase inhibitor. The indole alkaloid compound in the noni enzyme provided by the invention has a simple preparation process, low cost and abundant raw material sources.

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 als 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.

This invention belongs to the technical field of chemical drug synthesis, specifically relating to an indole alkaloid compound, its preparation method, and its application. The indole alkaloid compound, whose structural formula is shown in Formula I, is synthesized from 7-bromoindole and a boric acid ester as starting materials. The preparation process is simple and easy, and the resulting indole alkaloid compound or a pharmaceutically acceptable salt thereof exhibits highly effective targeted inhibition of STEAP1, inhibiting STEAP1 at both the protein and cellular levels and demonstrating potent anti-proliferative effects against prostate cancer cells in animals.

The invention discloses a method for preparing isopentenyl indole alkaloid Debromolustramine B. The isopentenyl indole alkaloid Debromolustramine B belongs to the technical field of organic synthesis, an o-bromo aniline aldehyde compound is used as an initial raw material, and on the basis of novel chiral p-toluene sulfinyl guidance, cheap copper catalysis amido alpha-position arylation and 3, 3-dimethyl allyl bromide cyclization reaction, the isopentenyl indole alkaloid Debromolustramine B is synthesized, and the isopentenyl indole alkaloid Debromolustramine B is obtained. According to the present invention, the key aryl quaternary carbon chiral center in the isopentenyl indole alkaloid Debomolustramine B is constructed, and the isopentenyl indole alkaloid Debomolustramine B with the butyrylcholine esterase inhibition activity is prepared through the subsequent series of chemical conversion, such that the material basis is provided for the further research of the natural product Debomolustramine B and the analogue thereof. The method has the advantages that the reaction conditions are mild, the cheap metal copper is used as the catalyst, the synthesis route is short, the energy consumption is low, the environmental protection is facilitated, and the large-scale chiral preparation of the isopentenyl indole alkaloid Debromofloutramine B is facilitated; the method also has the characteristics of relatively good atom economy and high product yield.

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 present disclosure provides compounds of Formula (I) or (II). The provided compounds may be useful as anti-microbial agents (e.g. antiplasmodial agents). The present disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating or preventing a disease).

Antimicrobial systems having naturally derived components and compositions containing them are described, the systems having a first component comprising an indole alkaloid and a second naturally derived component comprising a phenolic acid, and the systems and compositions provide superior antimicrobial benefits.

The invention provides a toad skin extract, a traditional Chinese medicine composition, a traditional Chinese medicine gel ointment, a preparation method and application, and belongs to the technical field of traditional Chinese medicine extraction and traditional Chinese medicine preparations. The preparation method of the toad skin extract comprises the following steps: mixing dried toad skin with an ethanol solution, performing reflux extraction to obtain a toad skin extracting solution, performing centrifugation to obtain supernate, and performing concentration and drying to obtain the toad skin extract. According to the preparation method, the content of bufalin, cinobufagin, resibufogenin and indole alkaloid extracted from the toad skin is increased, the preparation method is stable and feasible, and the prepared toad skin extract can inhibit bacteria. The traditional Chinese medicine gel ointment is easy to coat, smooth and bright in ointment body, good in skin following performance and uncovering and pasting performance, free of residues in stripping, good in adhesiveness, excellent in overall quality and good in reproducibility, has the effects of diminishing swelling and treating acne, is free of acute toxicity, does not cause the conditions of skin erythema and edema, is free of irritation to skin and is high in safety.

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 invention discloses a monoterpenoid indole alkaloid derivative for improving a memory cognition function and a preparation method and application thereof, and relates to the field of pharmacy. The monoterpenoid indole alkaloid derivative comprises a monoterpenoid indole alkaloid compound with a structure as shown in a general formula I, or pharmaceutically acceptable salt or stereoisomer or prodrug molecule of the monoterpenoid indole alkaloid compound. According to the present invention, it is found for the first time that the prepared monoterpene indole alkaloid derivative can regulate and control the growth and differentiation of nerve cells, and can increase the synthesis of new proteins by inhibiting eukaryotic elongation factor 2 kinase (eEF2K) so as to enhance the growth of neurite and promote the maturation of neurons. Experimental results prove that the prepared monoterpenoid indole alkaloid derivative has application prospects in improving neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease and the like), Down's syndrome and senescence-related memory cognitive impairment. # imgabs0 #

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 present invention relates to the technical field of antifungal treatment, specifically to the application of monoterpene indole alkaloids in the preparation of antifungal drugs. The results show that the monoterpene indole alkaloids provided by the present invention have significant antibacterial activity against fungi, providing a new idea for the preparation of antifungal drugs.

The invention discloses an indole alkaloid compound as well as a preparation method and application thereof. Belongs to the technical field of microbial pesticides. The invention provides a molecular structure of an indole alkaloid compound, a preparation related microorganism and a preparation method of the indole alkaloid compound. According to the indole alkaloid compound provided by the invention, the structural characteristics such as a structural framework and a ring forming mode are different from those of known indole alkaloid compounds. The related indole alkaloid compound is produced by fermenting a strain Aspergillus japonicus TE-739D, and is easy to carry out large-scale fermentation production; the preparation method provided by the invention can be used for rapidly and accurately preparing the indole alkaloid compound. It is found for the first time that the indole alkaloid compound has bacteriostatic activity on drug-resistant botrytis cinerea, can significantly inhibit the growth of the drug-resistant botrytis cinerea, and can be used as a lead compound or a novel biopesticide component for inhibiting the drug-resistant botrytis cinerea.

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.

To expand use of (-)-Neoechinulin A produced also by Aspergillus genus and Eurotium genus, indole alkaloid that is secondary metabolite of marine fungus, used for molding dried bonito flakes.SOLUTION: Degranulation inhibition (-)-Neoechinulin A. It can also be used for food additives. It was confirmed that (-)-Neoechinulin A does not affect the activation of Lyn, a non-receptor tyrosine kinase located upstream of degranulation signal, and suppresses the phosphorylation of Syk, a non-receptor tyrosine kinase downstream. A decrease in phosphorylation levels of Akt, a serine / threonine kinase, was also confirmed. These results suggest that (-)-Neoechinulin A inhibits extracellular Ca2+ influx and suppresses degranulation by downregulating the Syk and Akt signaling pathways.SELECTED DRAWING: Figure 4

The present invention relates to microorganisms for producing monoterpene indole al-kaloids (MIAs) and derivatives thereof de novo, including halogenated MIAs and halo-genated derivatives thereof. Also provided herein are methods for producing MIAs and derivatives thereof de novo, in particular halogenated MIAs and derivatives thereof, in a 5 microorganism, as well as useful nucleic acids, vectors and host cells for performing the present methods.

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.

Described herein are polypeptides encoding enzymes for the synthesis of monoterpene indole alkaloids. For example, the polypeptide comprises or consists of the sequence of SEQ ID NO: 1-65, or a variant thereof having at least 80% sequence identity to SEQ ID NO: 1-65, or a fragment of the polypeptide, or the variant thereof.

The present invention relates to indole alkaloids from Brucea javanica, their preparation methods, and applications, belonging to the field of pharmaceutical technology. Specifically, the invention relates to two indole alkaloid derivatives extracted and isolated from Brucea javanica, a plant of the genus Simarthaceae. These derivatives exhibit excellent anti-tumor activity. The preparation method of the present invention is simple and easy to implement, has good reproducibility, and is of high purity. #imgabs0#

The invention discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method of the steroid-indole alkaloid hybrid dimer compound and application of the steroid-indole alkaloid hybrid dimer compound in preparation of an anti-tumor chemotherapeutic drug sensitizer. The steroid indole diketopiperazine alkaloid hybrid compound is prepared from a fungus Aspergillus sp.EGF15-0-3 rice culture medium for the first time; the compound is a novel skeleton compound found for the first time in nature. It is found for the first time that the heterocomplex has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. The chemosensitization activity of the heterocomplex on the tumor chemotherapeutic drug topotecan TPT is found for the first time, drug source molecules and data support are provided for developing a novel natural anti-tumor combined inhibitor, and the heterocomplex has important significance on development and utilization of marine aspergillus fungus resources.