50 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 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.

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).

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 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 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 present invention provides an indole alkaloid compound in Folium Isatidis and an extraction and separation method and application thereof, and belongs to the fields of extraction and separation of traditional Chinese medicine, phytochemistry and pharmaceutical technology. The present invention provides an indole alkaloid compound extracted from Folium Isatidis, and its chemical structural formula is shown in formula (II) or formula (III), wherein formula (II) is named 4-hydroxyindole-3-acetonitrile, and formula (III) is named 3-acetamido-indolesulfonamide; and the present invention also provides a simple and rapid extraction and separation method for the compound. The extraction and separation process of the present invention is simple to operate, easy to control, and suitable for industrial production; the obtained indole alkaloid compound has anti-inflammatory and anti-tumor effects, and has good application prospects in the preparation of anti-inflammatory and therapeutic drugs for gastric cancer, liver cancer and lung cancer.

The invention discloses a method for preparing a 3-carboxylic acid compound through an efficient synthesis route by taking a simple and easily prepared brominated substrate as a starting raw material. Compared with the prior art, the route provided by the invention has the following remarkable advantages: high-activity iodide used in a traditional method is avoided, and the raw material preparation difficulty is reduced; a'one-pot method 'reaction is adopted, so that the operation steps are simplified, and the separation and purification processes of an intermediate product are reduced; reaction conditions are mild, the catalyst is small in dosage, cheap and easy to obtain, and the production cost is reduced; the yield of the derivative is high, the atom economy is good, and the method is suitable for large-scale production. In addition, the indole alkaloid derivative synthesized by the method has potential physiological activity, and an important material basis is provided for related drug development and biological activity research.

A novel hexahydropyrroloindole alkaloid extracted from wolfberry fruit can effectively solve the problems of extracting and preparing novel hexahydropyrroloindole alkaloid A from wolfberry fruit and realizing its application in preparing drugs for preventing and treating type 2 diabetes. The dried wolfberry fruit is heated under reflux for extraction, concentrated, and applied to a macroporous adsorption resin column. The product is eluted with water, ethanol, and acetone in sequence. The ethanol fraction is concentrated under reduced pressure, extracted, mixed with silica gel, gradient eluted, the same fractions are combined, the target component is eluted, mixed with silica gel, gradient eluted, the fractions within the retention time are collected, concentrated, and dried. The application of the prepared novel hexahydropyrroloindole alkaloid A in preparing drugs for preventing and treating type 2 diabetes can significantly promote glucose consumption in insulin-resistant HepG2 cells, improve glucose uptake capacity, promote glycogen synthesis, and enhance the activities of key glycolytic enzymes hexokinase and pyruvate kinase. The development and application prospects are broad and the economic and social benefits are significant.

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.

The invention relates to application of indole alkaloids in preparation of ferroptosis inhibitors. The indole alkaloid has a structure as shown in a formula (I): # imgabs0 #, wherein R1, R2 and R3 are independently H, C1-6 alkyl, C1-6 alkoxy or C1-6 carboxylic ester. The specific indole alkaloid disclosed by the invention has a remarkable inhibition effect on ferroptosis of neuronal cells, is low in cytotoxicity, and can be used for preparing medicines for treating and / or preventing neurodegenerative diseases and ischemic cerebral apoplexy caused by ferroptosis.

Antimicrobial systems with naturally derived ingredients and compositions comprising them are described. The systems have a first ingredient comprising an indole alkaloid and a second natural ingredient that includes a beta carboline alkaloid where the systems and compositions provide superior antimicrobial benefits.

An indole alkaloid, specifically the alkaloid (3S,3aR,8aS)-3-butyl-5-hydroxy-3,3a,8a-trimethyl-3,3a,8,8a-tetrahydro-2H-furo[2,3-b]indole-2-one, with the generic name Andranone, as an antineoplastic agent against neoplastic cells of colon cancer, breast cancer, leukaemia, central nervous system cancer, prostate cancer, lung cancer and cervical cancer.