42 results about "Aporphine" patented technology

Described is a new class of small molecule inhibitors of amyloid beta protein (Abeta) aggregation, based on apomorphine. These molecules target the nucleation phase of Abeta self-assembly and interfere effectively with aggregation of Abeta 1-40 into amyloid fibrils in vitro as determined by transmission electron microscopy, Thioflavin T (ThT) fluorescence, and velocity sedimentation. Structure-activity studies using apomorphine analogues demonstrate that 10,11-dihydroxy substitutions of the D ring are preferred for the inhibitory effectiveness of these aporphines, and that methylation of these hydroxyl groups reduces their inhibitory potency. The ability of these small molecules to inhibit Abeta amyloid fibril formation appears to be linked to their ability to undergo auto-oxidation in solution, implicating an auto-oxidation product as the active Abeta inhibitor. Sedimentation velocity and electron microscopy studies demonstrate that apomorphine and analogues facilitate oligomerization of Abeta into short nonfibrillar soluble assemblies, but inhibit Abeta fibrillization.

The invention discloses total alkaloid extract extracted from lotus leaf and its preparation method. The extract mainly comprises nuciferine, N-demethylnuciferine, O-demethyl nuciferine, oxopurpureine, nuciferine, tulipiferine, N-demethyl armepavine, 2-hydroxy-1-methoxy aporphine, armepavine, N-methyl isococlaurine, N-methyl coclaurine, dehydronuciferine, dehydronuciferine and its derivant, etc. The extractcan be extracted through one or more of methods of solvent-extraction, solvent extraction, ion exchange resin process, macroporous adsorbent resins method, extraction by supercritical fluid, column chromatography, and liquid-liquid countercurrent distribution chromatography. The total amount of different kinds of alkaloids in the extract is 5-100% (w/w), wherein nuciferine content occupies 5-100% (w/w).

The invention discloses an apo-phenanthrene and application of apo-phenanthrene oxide biological alkaline, which is characterized by the following: treating self-immune disease through inhibiting the proliferation of T, B lymph cell; avoiding host-resistance disease or allergic disease due to marrow transplantation.

The present invention discloses novel pharmaceutically acceptable salts of aporphine compounds and carboxyl-group containing agents. Also, the present invention discloses methods for preparing the pharmaceutically acceptable salts. These pharmaceutically acceptable salts are suitable for use in treating and/or preventing hyperglycemic disease and/or several oxidative stress related diseases.

The invention relates to a lotus leaf extract, a monomer component and application thereof. An active monomer component of the extract is aporphine alkaloid and comprises 2-hydroxy-1-methoxy-aporphine, nuciferine and N-nornuciferine. The lotus leaf extract and the monomer component have good inhibition to acetylcholinesterase, and can be developed into medicaments for treating the diseases such as Alzheimer's disease, glaucoma, asthenic bulbar paralysis, intestinal obstruction and the like.

The invention discloses application of aporphine alkaloid, oxoaporphine alkaloid and derivatives thereof in preparing antibacterial medicines. The invention provides a new medical usage and develops a new application field for the known aporphine alkaloid, the oxoaporphine alkaloid, the derivatives thereof and pharmaceutically acceptable salts thereof. The compounds, such as the aporphine alkaloid, the oxoaporphine alkaloid, the derivatives thereof and the pharmaceutically acceptable salts thereof, have remarkable antibacterial activity for staphylococcus aureus and methcillin-resistant staphylococcus aureus, and the invention provides a new compound for seeking for a new antibacterial medicine.

Methods and engineered yeast cells for generating a benzylisoquinoline alkaloid product are provided herein. A method comprises providing engineered yeast cells and a feedstock to a reactor. In the reactor, the engineered yeast cells are subjected to fermentation by incubating the engineered yeast cells for a time period to produce a solution comprising the BIA product and cellular material. The solution comprises not more than one class of molecule selected from the group of protoberberine, morphinan, isopavine, aporphine, and benzylisoquinoline. Additionally, at least one separation unit is used to separate the BIA product from the cellular material to provide the product stream comprising the BIA product.

The invention belongs to the technical field of pharmacy and in particular relates to a usage of an oxidized aporphine derivative and a composition thereof. The invention discovers that the oxidized aporphine derivative can effectively inhibit the tumor proliferation and that when the oxidized aporphine derivative is used together with antitumor drugs to cure tumor, the synergy can be achieved, the cure effect can be enhanced, and the amount of the antitumor drugs in use can be reduced, thereby obviously reducing the toxic and side effects of the antitumor drugs.

New aporphine derivatives are disclosed which have formula (I) and the physiologically acceptable salts thereof. Said derivatives may be used for the treatment of Parkinson's disease, hemicrania, restless legs syndrome (RLS), sexual dysfunction in men and women, hyperprolactemia and psychotic disorders, and/or evaluation of Parkinson's disease. Processes for the preparation of such derivatives are also disclosed.

The invention relates to an aporphine compound represented by general formula (I) or stereoisomer thereof, pharmaceutically acceptable salt or pharmaceutically acceptable solvate and medical application thereof. The compound can be used for preventing or treating diseases related with serotonin 1A receptors, wherein the diseases comprise central nervous system diseases, in particular schizophrenia, depression and movement disorder caused by Parkinson's resistant medicament. The invention also relates to a medicinal composition comprising the compound.

The invention discloses an aporphine type alkaloid and a preparation method thereof. The compound is 8-acetamido-isocorydine, which is prepared through the nucleophilic substitution reactions between 8-amino-isocorydine, and the chemical structure formula of the compound is represented in the description. Through a Kunming white mouse tumor xenograft model, the results show that the provided alkaloid has a strong effect on inhibiting the tumor growth in body and has a good antitumor activity.

The invention discloses a toner and a preparation method thereof. The toner is prepared from the following raw materials in parts by weight: 2-6 parts of ginseng, 4-8 parts of Chinese angelica, 3-7 parts of mint, 4-8 parts of rose, 5-9 parts of ethyl alcohol and 100-120 parts of Dendrobium officinale water extract. The preparation method comprises the steps of mixing, soaking and obtaining a finished product. The toner disclosed by the invention has the function of moisturizing, and also has the effects of secondary cleaning and deep moisturizing; a large number of effective constituents are contained in the toner, so that the skin of a long-time user can be tender and fine, ruddy and bright; a large number of effective constituents such as polysaccharide, alkaloid, amino acids, trace elements and aporphines compounds are contained in the main constituent Dendrobium officinale water extract of the whole toner, so that the toner can play roles in strengthening the skin, preventing senility and wrinkles and invigorating the circulation of blood.

The invention discloses a preparation method of Pollyalthia laui Merr roots. The preparation method comprises the following steps: wetting dry powder of Pollyalthia laui Merr roots with lye and adding a solvent for extracting; and filtering and concentrating the extracting solution at reduced pressure to obtain a total extract, adding water for suspending, extracting by using chloroform, and recycling under reduced pressure to obtain a chloroform extracting part which is the lipophilic total alkaloids part of the Pollyalthia laui Merr roots. The lipophilic total alkaloids part comprises four carbazole alkaloids, three aporphine alkaloids and an amide alkaloid. The extract prepared by the method disclosed by the invention is high in yield, simple in process flow, low in cost and suitable for preparation on a large scale, has good broad spectrum anti-tumor activity and can be applied to medicines for preventing and treating tumors.

The invention relates to a non-catechol aporphine compound as well as a pharmaceutic composition and application thereof, in particular to a non-catechol aporphine compound shown as a general formula (I) or a stereoisomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate and medical application thereof. The compound can be used for preventing or treating diseases related with serotonin 1A receptors, comprising central nervous system diseases, particularly schizophrenia, depressions and dyskinesia caused by medicaments for resisting parkinson's diseases. The invention also relates to the medical composition containing the compound.

The present invention discloses a dicranostigma leptopodum (maxim) fedde alkaloid effective part preparation method, wherein the dicranostigma leptopodum (maxim) fedde alkaloid effective part obtained through chemical steps is a brownish-black powdery solid, and comprises aporphine alkaloid, morphinane alkaloid, protopine alkaloid, protoberberine alkaloid and isoquinoline alkaloid. According to the present invention, with the method, the concentration of the active compound can be effectively improved, the drug taking dose can be lowered, and the pharmacological activity of the dicranostigma leptopodum (maxim) fedde alkaloid can be significantly improved.

The invention discloses a new oxidized iso-aporphine alkaloid derivative-4,6-dis-(2-pyridyl)-5,6-dihydro-4H-1,5-diaza-benzo[de]cyclopentane[b]-8-anthranone(PPCA for short), a synthetic method and an application. The PPCA synthetic method comprises the following steps: weighting 1-nitrogen-5-bromobenzanthrone and 2-(aminomethyl)pyridine, taking 1-nitrogen-5-bromobenzanthrone for dissolving in n-amyl alcohol, adding the weighted 2-(aminomethyl)pyridine and performing backflow reaction at the temperature of 140-180 DEG C, cooling, performing pumping filtration, washing the filter residue, and drying to obtain the oxidized iso-aporphine alkaloid derivative. The invention investigates the oxidized iso-aporphine alkaloid derivative has inhibition activity on the propagation of various human tumor cell strains such as HepG2, MGC80-3, SK-OV-3 and T-24, the result shows that the oxidized iso-aporphine alkaloid derivative has obvious external antineoplastic activity and has good latent medicinal value. A structural formula of PPCA is shown in a following formula.