11 results about "Costunolide" patented technology

The invention relates to the field of biological medicine, in particular to a carrier-free nanoparticle which is formed by self-assembly of cyclosporine A and costunolide through intermolecular weak interaction. The invention also provides a preparation method of the traditional Chinese medicine composition and application of the traditional Chinese medicine composition in preparation of medicines for treating xerophthalmia. The carrier-free nano eye drops based on the synergistic effect of Chinese and western medicines are used for anti-inflammatory treatment of the xerophthalmia, a new strategy is provided for precise diagnosis and treatment of the xerophthalmia, the problems of single target spot, limited curative effect and the like in traditional treatment are solved, and more efficient inflammation control is expected to be achieved. While the curative effect is improved, the tolerance risk caused by long-term use is reduced, double optimization of the curative effect and safety is realized, and the limitation of traditional single drug treatment is broken through. By adopting the carrier-free nano preparation, the delivery efficiency of the medicine on the ocular surface is effectively improved, the bioavailability is enhanced, powerful support is provided for improving the curative effect of the medicine, and the carrier limitation bottleneck is broken through.

The invention discloses an application of costunolide in preparation of a medicine for treating and / or preventing a non-alcoholic fatty liver disease. It is found that costunolide can activate an Nrf2-ARE signal channel of a body, liver cell lipid metabolism abnormality is effectively improved from the molecular level, and meanwhile the pathological influence of oxidative damage on liver tissue is remarkably relieved. Experimental data show that the compound has a remarkable intervention effect on NAFLD, a scientific basis is provided for development of a novel liver disease treatment agent due to the unique dual regulation and control mechanism of the compound, particularly, the compound shows an important development prospect in the field of clinical intervention of metabolism-related liver injury, and an innovative solution is provided for NAFLD lacking a special-effect therapy at present.

The invention discloses an esophageal cancer targeting nano-tablet based on a traditional Chinese medicine composition and a preparation method of the esophageal cancer targeting nano-tablet. The targeted nano tablet is prepared from the following refined extracts: a rhizoma paridis total saponin extract, a pseudobulbus cremastrae seu pleiones colchicine derivative extract, a panax notoginseng total saponin extract, a carthamin yellow extract, a thunberg fritillary bulb total alkaloid extract, frankincense-myrrh compound volatile oil, a resin extract and an astragaloside IV extract. The nano-carrier comprises a nano-carrier, a seaweed-laminarin composite extract, a processed rhizoma pinelliae total alkaloid extract and costus root volatile oil, and the costus root volatile oil serves as one of targeting ligands to be used for modifying the nano-carrier. The targeting property is strong: the dual-targeting ligand (costunolide-TOPK affinity peptide) on the surface of the nano-carrier can actively recognize and combine with a specific receptor of esophageal cancer cells, and meanwhile, due to the size (about 100-200 nanometers) of the carrier, the carrier is easy to enrich in tumor tissues through enhanced permeation and retention (EPR) effect, so that the modernization upgrading of the idea of'channel guiding medicine 'is realized.

The application discloses a dehydrocostus lactone derivative, a preparation method and medical application thereof, and belongs to the technical field of chemical synthesis. The dehydrocostus lactone derivative is shown as a general formula I. The compound has certain inhibiting effect on HBsAg and HBeAg, can be used for preparing anti-HBV drugs, and provides more efficient and safe candidate drug molecules for clinical anti-HBV treatment.

This invention provides the application of costunolide in the preparation of a drug for preventing posterior capsule opacification. Costunolide effectively reduces posterior capsule opacification after extracapsular lens extraction (ECLE) and exhibits significant anti-inflammatory and anti-fibrotic effects in both in vitro and in vivo models. Mechanistic studies have identified matrix metalloproteinase 8 (MMP8) as a key downstream effector of costunolide, confirming that costunolide inhibits MMP8 expression, thereby blocking the transformation of lens epithelial cells (LECs) into mesenchymal cells and subsequent fibrotic processes. This lays a solid foundation for developing targeted therapies for posterior cataract, a common surgical complication.

The invention relates to the field of biological medicine, in particular to AS vulnerable plaque treatment nanoparticles and a preparation method and application thereof.The nanoparticles comprise hollow mesoporous manganese dioxide nanospheres, and the manganese dioxide nanospheres are loaded with 5 alpha-hydroxycostus acid and perfluoropentane; the manganese dioxide nanosphere is coated with an M2 type macrophage-liposome hybrid membrane, and VLA-4 is expressed on the M2 type macrophage-liposome hybrid membrane. By means of the scheme, normalization of new vessels in plaques is achieved, then the plaques are stabilized, and the problem that treatment cannot be conducted from the perspective of normalization of the new vessels in the prior art is solved.

A fructus cannabis intestine-moistening pill high performance liquid chromatography fingerprint establishment method relates to the field of medicine, and comprises the following steps: weighing fructus cannabis intestine-moistening pill medicinal material powder, adding methanol, plugging, weighing, soaking, carrying out ultrasonic extraction, cooling, weighing, complementing the weight loss, uniformly shaking, and filtering to obtain a test solution; the method comprises the following steps: weighing an emodin reference substance, a rhein reference substance, a chrysophanol reference substance, a hesperidin reference substance, a costunolide reference substance, a dehydrocostunolide reference substance and a paeoniflorin reference substance, adding methanol to prepare a mixed reference substance solution, and filtering to obtain a reference substance solution; sucking the test sample solution and the reference substance solution, injecting the test sample solution and the reference substance solution into a high performance liquid chromatograph, measuring and recording a chromatogram, importing detection results of the test sample solution and the reference substance solution into fingerprint spectrum software, and generating a reference fingerprint spectrum through data matching. The quality of the fructus cannabis intestine moistening pill can be effectively represented, the quality of the medicine can be comprehensively monitored, and the method has the advantages of being high in stability, high in precision and good in reproducibility.

The invention relates to the technical field of organic synthesis, in particular to a method for asymmetrically and semi-synthesizing parsnip lactone or an expanded ring derivative of parsnip lactone. According to the method, through a series of chemical reactions, including a ring closing addition reaction (RCM), an asymmetric alkenyl substitution reaction (AAS) and a ring opening ring closing addition reaction (ROM / RCM), a natural and rich precursor compound costunolide is converted into parsnilolactone or an expanded ring derivative thereof. The method has the characteristics of high efficiency, good selectivity and large-scale production, can provide possibility for large-scale synthesis of the parsnip lactone and the ring-expanded derivative thereof, is widely applied to the fields of drug discovery and treatment, and particularly has important potential in development of antiviral and anticancer drugs.

The invention discloses a nucleic acid-small molecule non-covalent compound as well as a preparation method and application thereof. The method for constructing the nucleic acid-small molecule non-covalent compound based on calculation virtual screening guidance is provided for the first time, and a natural active compound capable of forming the compound with framework nucleic acid with a stable three-dimensional structure through non-covalent binding is rapidly screened out through molecular docking; a trace thermophoresis technology verifies that the prediction method is high in accuracy, and a plurality of nucleic acid-small molecule non-covalent complexes including costunolide-framework nucleic acid complexes are successfully constructed. The method does not need chemical modification on drugs or nucleic acids, and is high in universality. The nucleic acid-small molecule non-covalent complex obtained according to the method disclosed by the invention, especially COS-FNA, shows excellent kidney targeting property and ultrahigh treatment efficacy in a kidney disease model, and provides a brand new universal platform for development of kidney targeting drugs.

The invention discloses alantolactone spliced oxazinane spirooxindole 3, which is specifically prepared by the following steps: refluxing various substituted isatin, alantolactone and proline in an organic solvent, and carrying out 1, 3-dipole 3 + 2 cycloaddition reaction to generate an intermediate, thereby obtaining the alantolactone spliced oxazinane spirooxindole 3. Then nitrogen atoms in the intermediate are subjected to nitrogen oxidation and rearrangement reaction under the action of an oxidizing agent m-chloroperoxybenzoic acid, the final product alantolactone spliced oxazinane spirooxindole 3 is generated, and the skeleton compound can provide a compound source for biological activity screening and has important application value for medicine screening and pharmaceutical industry. The method is simple and easy to operate, raw materials are cheap and easy to obtain, the method can be carried out in various organic solvents, and the method also has good air stability, wide applicability and good compatibility for various substituent groups. And the skeleton compound has a tumor growth inhibition activity effect on human lung adenocarcinoma cells (A549).

The invention provides a novel eudecane-guaiane sesquiterpene dimer as shown in a structural formula as well as a pharmaceutical composition, a preparation method and application thereof, and belongs to the technical field of medicines. The preparation method provided by the invention comprises the following steps: by taking 6 different structures of cinemanane lactone as raw materials, carrying out Diels-Alder reaction / deprotection on the raw materials and guaiane dienes to prepare 6 cinemanane-guaiane sesquiterpene dimers, and further carrying out structural modification to obtain 6 derivatives; or preparing a germacane-guaiane dimer by taking costunolide as a raw material, and further performing intramolecular cyclization to obtain 15 eudecane-guaiane sesquiterpene dimers. The eudecane-guaiane sesquiterpene dimer provided by the invention has inhibitory activity on human hepatoma cell lines HepG2, Huh7 and SK-Hep-1, can form a pharmaceutical composition with a pharmaceutically acceptable carrier, and can be used for preparing anti-hepatoma drugs.