42 results about "Aporphine" patented technology

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 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 present invention discloses novel aporphine derivatives. Also, the present invention discloses that these novel aporphine derivatives can be used for treating oxidative stress induced diseases such as cardiovascular disease, diabetes, aging, Alzheimer's disease, kidney disease, cancer or brain ischemic disease etc.

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 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 cobalt (II) metal complex taking an oxidized iso-aporphine ramification as a ligand as well as a synthetic method and application thereof. The cobalt (II) metal complex is obtained by dissolving 4,6-bis-(2-pyridyl)-5,6-dihydro-4H-1,5-diaza-benzo [de] cyclopentane [b]-8-anthracenone and cobalt chloride hexahydrate (II) into a polar solvent and then carrying out complexing reaction through mixing and can be particularly synthesized through a solution method or a solvothermal method. The inventor discovers that the cobalt (II) metal complex disclosed by the invention has in-vitro antitumor activity outstandingly higher than that of the ligand by observing the proliferation inhibition activity of the cobalt (II) metal complex on multiple human tumor cell strains; in addition, an in-vivo tumor inhibition experiment of a nude mouse bearing the tumor shows that PPCA-Co(II) has good tumor inhibition effect on a nude mouse model of a human hepatocarcinoma cell BEL-7402. The structural formula of the cobalt (II) metal complex is as shown in the specification.

Described is a new class of small molecule inhibitors of amyloid β protein (Aβ) aggregation, based on apomorphine. These molecules target the nucleation phase of Aβ self-assembly and interfere effectively with aggregation of Aβ 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 Aβ amyloid fibril formation appears to be linked to their ability to undergo auto-oxidation in solution, implicating an auto-oxidation product as the active Aβ inhibitor. Sedimentation velocity and electron microscopy studies demonstrate that apomorphine and analogues facilitate oligomerization of Aβ into short nonfibrillar soluble assemblies, but inhibit Aβ fibrillization.

The invention discloses a highly active oxoaporphinoid-rhodium (III) complex, and synthetic methods and an application thereof. The complex can be synthesized through adopting three different methods. The three synthetic methods gradually become simple from complex, and are completely different from present synthetic methods of oxoaporphinoid-metal complxes. The inhibition effect of a ligand OGC, an oxoglaucine-rhodium (III) complex and the complex disclosed in the invention on various tumor cell strains and in vivo tumor inhibition of the complex disclosed in the invention are investigated in the invention, and results show that complex disclosed in the invention has substantially enhanced in vitro and in vivo antitumor activity, and has far higher antitumor activity than the ligand OGC and the oxoglaucine-rhodium (III) complex. The structural formula of the highly active oxoaporphinoid-rhodium (III) complex is represented by formula (I) shown in the description.

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 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.