14 results about "Butylphthalide" patented technology

The invention discloses an aromatic alkylamine ferroptosis inhibitor based on a butylphthalide structure and a preparation method and application thereof. The chemical structural formula of the ferroptosis inhibitor is shown as a formula 1 or a formula 2. The ferroptosis inhibitor can inhibit ferroptosis caused by a ferroptosis inducer and can reduce the level of active oxygen in cells. Nerve injury caused by cerebral ischemia reperfusion can be relieved, and symptoms of neurological diseases such as Alzheimer's disease and Parkinson's disease can be relieved; compared with a ferroptosis inhibitor Ferrostatin-1, the aryl alkyl amine compound disclosed by the invention has better metabolic stability and is suitable for in-vivo drug effect evaluation. Therefore, the novel aryl alkyl amine compound provided by the invention has a very good application value in treatment of neurological diseases related to ferroptosis.

This invention discloses butylphthalide nanoparticles, comprising: a layered double hydroxide and butylphthalide, wherein the butylphthalide is loaded onto the layered double hydroxide. This invention also discloses a method for preparing the above-mentioned butylphthalide nanoparticles, comprising the following steps: mixing the layered double hydroxide, butylphthalide, and water, adsorbing, separating the solid and liquid phases, and drying to obtain butylphthalide nanoparticles. This invention further discloses the application of the above-mentioned butylphthalide nanoparticles in the preparation of drugs for treating acute renal ischemia-reperfusion injury. This invention also discloses a drug for treating acute renal ischemia-reperfusion injury, comprising: the above-mentioned butylphthalide nanoparticles and pharmaceutically acceptable excipients. The butylphthalide nanoparticles of this invention have high drug loading capacity, good stability, and can target and activate the PI3K-AKT signaling pathway, effectively inhibit HK-2 cell apoptosis and oxidative stress, restore mitochondrial function, and improve renal ischemia-reperfusion injury.

Disclosed are an aromatic alkylamine ferroptosis inhibitor based on a butylphthalide structure, a preparation method therefor, and an application thereof. The chemical structural formula of the ferroptosis inhibitor is as shown in formula (1) or formula (2). The ferroptosis inhibitor is capable of inhibiting ferroptosis caused by a ferroptosis inducer, and reduces the level of intracellular reactive oxygen species. The ferroptosis inhibitor reduces neurological damage caused by cerebral ischemia-reperfusion, and alleviates symptoms of neurological disorders such as Alzheimer's disease and Parkinson's disease. Compared to the ferroptosis inhibitor Ferrostatin-1, the arylalkylamine compound exhibits better metabolic stability and is suitable for in-vivo efficacy evaluation. Therefore, the novel arylalkylamine compound provided by the present invention demonstrates great application value in the treatment of ferroptosis-related neurological disorders.

The invention provides a method for extracting phthalide chemical components in angelica sinensis, which comprises the following steps of: firstly, shearing and emulsifying the angelica sinensis at a high speed, carrying out high-speed shearing and extraction by using petroleum ether and ethyl acetate as extraction solvents, and recovering the solvents from the extract under reduced pressure through a rotary evaporator to obtain angelica sinensis essential oil; wherein the extracted essential oil contains senkyunolide A, ligustilide and butylphthalide. Aiming at the characteristics that the phthalide component in the angelica volatile oil is thermally unstable and is easy to oxidize, the phthalide component in the angelica volatile oil can be rapidly extracted under a low-temperature condition by combining a petroleum ether-ethyl acetate solution system with a high-speed shearing, dispersing and emulsifying technology, and the activity of the angelica volatile oil can be better maintained. The method has the characteristics of low temperature, simplicity in operation, short time and low cost.

The application provides a triazole compound for protecting brain tissue and a preparation method thereof, and belongs to the technical field of biological medicines, and provides a triazole compound as shown in formula (I) and chiral isomers, enantiomers, diastereoisomers, geometric isomers, free forms or pharmaceutically acceptable salts, hydrates, solvates or esters thereof; and also provides a preparation method thereof; compared with the prior art, the application combines the internal ester ring-opening product of butylphthalide and ligustrazine through triazole to synthesize a novel triazole compound which can be used for protecting brain tissue; the preparation method of the triazole compound is simple and the raw materials are easy to obtain; the triazole compound has better biological activity and brain tissue protection effect than butylphthalide / ligustrazine, and has significant protection activity on a SH-SY5Y cell damage model.

The application relates to the field of drug chemical synthesis, in particular to a synthesis process of a butylphthalide derivative. The synthesis method of the butylphthalide derivative comprises the following steps: butylphthalide and lithium aluminum hydride are mixed in tetrahydrofuran, reacted with tert-butyl dimethyl chlorosilane, then reacted with acid and tetrabutylammonium fluoride trihydrate, esterified with 2-morinol or a derivative thereof after oxidation, and purified to obtain the butylphthalide derivative. The synthesis method has the characteristics of mild conditions, simple operation, fewer side reactions, high selectivity, better industrial adaptability of the prepared butylphthalide derivative, and high purity of the finished product.

The invention discloses application of butylphthalide in preparation of a medicine for preventing and treating obesity-related acute pancreatitis, and belongs to the technical field of medicines. The invention discloses application of butylphthalide in treatment of obesity-related acute pancreatitis. Pancreatic necrosis, systemic inflammation and distant organ injury caused by obesity-related acute pancreatitis can be remarkably improved. Wherein after intervention of butylphthalide, pathological scores of lung, kidney and pancreas are obviously reduced by 73.08%, 70.00% and 59.26%; the expression level of the pancreatitis marker is obviously reduced and is reduced by 53.80% compared with that of a model group; the expression levels of proinflammatory factors IL-1beta, IL-6 and TNF-alpha in serum are obviously reduced, and are respectively reduced by 69.45%, 78.80% and 67.64% compared with a model group.

The invention discloses a pharmaceutical composition and application thereof, the pharmaceutical composition comprises butylphthalide and Ceridutinib, and the mass ratio of butylphthalide to Ceridutinib is (1000: 1)-(1: 1000). The pharmaceutical composition disclosed by the invention has a good effect on treating cerebrovascular diseases, butylphthalide and Ceridutinib show a synergistic effect, an excellent curative effect is favorably obtained, the dosage of the medicine is reduced, and the clinical medication safety is favorably improved.

This invention belongs to the field of chemical pharmaceutical technology, specifically disclosing a method for preparing butylphthalide. In the method provided by this invention, crude 2-(α-hydroxypentyl)benzoic acid, obtained by the condensation reaction of o-formylbenzoic acid and an organometallic reagent, is subjected to alkali treatment, and the pH is adjusted to 3.8-4. The crude 2-(α-hydroxypentyl)benzoic acid is then separated and purified to obtain 2-(α-hydroxypentyl)benzoic acid and a filtrate. The pH of the filtrate is adjusted to 1.8-2, and o-formylbenzoic acid is separated and purified. The o-formylbenzoic acid is then used in the above condensation reaction to perform a ring-closing reaction on 2-(α-hydroxypentyl)benzoic acid, yielding butylphthalide. This invention, through reasonable experimental process design, provides a method for preparing butylphthalide with high yield, high purity, low energy consumption, and a simple process.

The present application relates to a butylphthalide impurity compound, a preparation method and use thereof. The impurity compound of the present application is similar to butylphthalide in structure, but has no significant effect on the secretion of TNF-alpha of LPS-induced mouse primary microglial cells; instead, the impurity compound has significant neurotoxicity on mouse brain neuroblastoma cell line (Neuro-2a), and can significantly inhibit the length of Neuro-2a nerve cell axon and the number of cells with axon. The content of peroxidized impurities has an effect on the treatment of butylphthalide composition on nerve function damage of tMCAO model rats, and the higher the content of peroxidized impurities, the greater the degree of nerve function damage. Limiting the impurity compound of the present application in the quality control of butylphthalide is beneficial to the quality control of butylphthalide drugs, and can ensure the effectiveness, safety and quality control of the drugs.

This invention relates to a butylphthalide cationic nanoemulsion, its preparation method, and its application, belonging to the field of pharmaceutical technology. The butylphthalide cationic nanoemulsion comprises an oil phase, an aqueous phase, butylphthalide, an emulsifier, a co-emulsifier, an osmotic pressure regulator, and a cationic surfactant. The butylphthalide content in the nanoemulsion is 0.30%–2.50% by mass. The average particle size of the butylphthalide cationic nanoemulsion is 80–200 nm, the polydispersity index is 0.070–0.200, and the zeta potential is 20–30 mV. This invention solves the problems of poor water solubility and low stability of butylphthalide by preparing it into a nanoemulsion formulation; furthermore, by administering it via nasal administration, it meets the need for rapid neuroprotection in ischemic stroke.

The application discloses a sulfide prodrug combination based on butylphthalide as a carrier, which has the structure shown in the following formula I. The butylphthalide prodrug can increase the curative effect of drugs and reduce the toxic side effects.

The application discloses a kind of pharmaceutical composition and its application, the pharmaceutical composition includes butylphthalide and sedutin, the mass ratio of butylphthalide and sedutin is 1000:1~1:1000.The effect of the pharmaceutical composition of the application in treating cerebrovascular disease is good, butylphthalide and sedutin show synergistic effect, which helps to obtain excellent curative effect, and reduce drug dosage, which helps to improve the safety of clinical drug use.

This invention provides an environmentally friendly method for preparing the active pharmaceutical ingredient butylphthalide. Using butylphthalide as a raw material and water as a solvent, the active pharmaceutical ingredient butylphthalide is prepared in a simple, environmentally friendly one-pot process via hydrolysis with sodium hydroxide solution, acidification with sulfuric acid solution, and reductive lactone formation catalyzed by an iridium catalyst. After simple extraction, drying, and concentration, a product with a purity greater than 99% according to 1H NMR spectroscopy and a yield greater than 90% is obtained. The synthetic method provided by this invention features concise reaction conditions and steps, simple operation, is environmentally friendly, has high synthesis efficiency, and facilitates separation and purification. It has promising industrial applications and plays a positive role in organic synthesis, pharmaceutical production, and fine chemicals.