131 results about "Pharmacologic effects" patented technology

The present invention relates to a novel pomalidomide derivative that exhibits improved pharmacological effects compared to pomalidomide, and is used to treat brain diseases. The novel pomalidomide derivative developed in the present invention has excellent binding ability to cereblon, is almost non-cytotoxic, has low possibility of teratogenic side effects, and can regulate TNF-α expression, as well as suppress oxidative stress and has excellent in vivo pharmacokinetic stability, and shows excellent effects of improving the decrease in motor ability, which is a symptom of Parkinson's disease, and increasing the expression of tyrosine hydroxylase, which is decreased in Parkinson's disease, and can be used for the prevention or treatment of brain diseases such as Parkinson's disease.

The application discloses a bacteriostatic and acne-removing microemulsion containing plant extracts and a preparation method thereof. The bacteriostatic and acne-removing microemulsion contains a microemulsion loaded with quercetin alone, a microemulsion loaded with sasanquasapernin alone, and a microemulsion loaded with quercetin and sasanquasapernin simultaneously. The bacteriostatic and acne-removing microemulsion containing plant extracts prepared by the application not only solves the problems of stickiness of camellia oil and poor solubility of quercetin, but also has a synergistic inhibitory effect on propionibacterium acnes, achieves the same high-efficiency bacteriostatic effect with a lower drug concentration, saves drug cost, reduces drug irritation, and expands the application of quercetin and sasanquasapernin in the cosmetic and pharmaceutical fields due to the rich pharmacological effect of the plant extracts, low side effect and safety. The microemulsion system prepared by the application is clear, transparent, uniform and stable, the preparation process is simple, the required energy is low, the cost is low, and the system is beneficial to commercial production.

The invention relates to the technical field of traditional Chinese medicine compositions, in particular to a traditional Chinese medicine composition for relieving acute kidney injury and a preparation method thereof.The traditional Chinese medicine composition comprises honeysuckle-derived exosome-like nano-vesicles (HELNVs), and the particle size distribution of the HELNVs is 68.06-164.20 nm. Firstly, the HELNVs retain various bioactive components of honeysuckle, and the HELNVs retain various bioactive components of the honeysuckle; the components can play a stronger pharmacological role through a synergistic effect; secondly, due to the nanoscale particle size (68.06-164.20 nm), the HELNVs can better penetrate through a biological barrier, and the targeting property and the bioavailability are improved; thirdly, the natural source and exosome-like structure of the HELNVs may endow the HELNVs with unique cell affinity, which is beneficial to the interaction of the HELNVs with target cells; finally, the HELNVs are used as a natural nano-carrier, so that the HELNVs have better safety.

The invention relates to the technical field of health-care food, in particular to a freckle-removing and whitening traditional Chinese medicine composition, a preparation method thereof and freckle-removing and whitening nourishment. Effective components of the freckle-removing and whitening traditional Chinese medicine composition are prepared from the following raw materials in parts by weight: 2-6 parts of peach kernels, 1-5 parts of Chinese wolfberry fruits, 1-5 parts of longan aril, 1-5 parts of Chinese dates, 1-4 parts of lily bulbs, 0.5-4 parts of mulberries, 0.2-2.5 parts of poria cocos and 0.1-0.6 part of double-petal red roses. The freckle-removing and whitening traditional Chinese medicine composition has the effect of accelerating melanin dissolution so as to achieve the good effects of removing freckles and whitening the skin color. Meanwhile, the freckle-removing and whitening traditional Chinese medicine composition disclosed by the invention is good in safety, edible, capable of exerting the pharmacological action and synergistic interaction of all the components and multiple in benefits.

The invention discloses a tetrandrine ferulate and its application in the preparation of a medicament for treating pulmonary fibrosis. The pharmacological effects of tetrandrine and ferulic acid, as well as those after salification, are studied. It is found that both have an anti-pulmonary fibrosis effect, and the two can be used in combination to synergistically exert a more excellent anti-pulmonary fibrosis efficacy. At the same time, the solubility of tetrandrine can also be increased. This has not been reported in existing literature. The tetrandrine ferulate of the present invention has lower cytotoxicity, and the cell viability of normal human liver cells LO-2 and human embryonic fibroblasts MRC-5 is higher than that of tetrandrine, which alleviates the burden of liver and lungs to a certain extent and has good safety.

The application discloses application of total flavones of chrysanthemum morifolium ramat and metabolites thereof in preparation of uric acid-lowering or liver and kidney protecting drugs or health care products. The total flavones of chrysanthemum morifolium ramat contain various flavone compounds. In a hyperuricemia model mouse, the total flavones of chrysanthemum morifolium ramat can significantly reduce blood uric acid level, and has a significant protective effect on liver and kidney, and the effect is achieved by inhibiting the activity and expression of xanthine oxidase and adenosine deaminase in the liver, and regulating the expression of uric acid related transporters in the kidney. Meanwhile, metabolites of the total flavones of chrysanthemum morifolium ramat, luteolin-7-O-glucuronide and apigenin-7-O-glucuronide, can also play a pharmacological role in the mouse body. In vitro experiments and mouse primary hepatocytes further prove that luteolin-7-O-glucuronide and apigenin-7-O-glucuronide have an inhibiting effect on the activity and expression level of xanthine oxidase. The application widens the application range of traditional Chinese medicinal materials, and provides a new direction for development of efficient and low-toxic uric acid-lowering and anti-gout drugs or health care products.

The invention discloses a traditional Chinese medicine compound screening method based on machine learning, and relates to the technical field of biological medicine.According to the traditional Chinese medicine compound screening method, multi-source traditional Chinese medicine compound spleen tonifying related component data are collected and integrated, a data set containing information such as components, medicine effects and indications is constructed, and follow-up model training is supported; utilizing machine learning to train a compound screening model, identifying drug effect related components, predicting effective parts of traditional Chinese medicinal materials of the components, and revealing contribution of the components to the drug effect; structural characteristics of chemical components are extracted, potential pharmacological effects of the chemical components are analyzed, and drug effect and toxicity analysis is supported; and a pharmacodynamic index set is constructed to evaluate the effect, toxicity and timeliness of the components, and support is provided for pharmacodynamic optimization. Animal experiments are combined to verify the synergistic effect among the components, so that the model prediction accuracy is ensured. The proportion of the compound components is adjusted according to the experimental result to maximize the drug effect and reduce the side effect to meet the requirements of different patients.

The present invention discloses a method for extracting effective active ingredients from Buddleja buddhist flower and its application. The method comprises the following steps: first subjecting the crushed Buddleja buddhist flower to ethanol reflux extraction and concentration, and then extracting the obtained Buddleja buddhist flower alcohol extract with petroleum ether, ethyl acetate, and n-butanol respectively. The remaining aqueous phase is concentrated under reduced pressure, purified by a D101 macroporous resin column, and the target product obtained after drying is structurally identified as a verbascoside monomer compound. The method of the present invention can better control the quality standards of Buddleja buddhist flower and pave the way for a more in-depth study of its pharmacological effects by effectively separating the verbascoside compounds from the Buddleja buddhist flower, thereby laying the foundation for the clinical development of new drugs with anti-tumor, antioxidant, and immunomodulatory activities.

The present invention discloses a liquid formulation of L-serine or a pharmaceutically acceptable salt thereof and a method for preparing the same. Specifically, the present invention relates to a liquid formulation and a method for preparing the same, wherein the liquid formulation comprises a high concentration of L-serine or a pharmaceutically acceptable salt thereof, has excellent stability and safety, and exhibits excellent pharmacological effects.

The invention relates to the field of pharmaceutical preparations, and discloses a compound preparation composition containing olopatadine and brimonidine for a nasal cavity and a preparation method of the compound preparation composition. The compound preparation composition for the nasal cavity is prepared from the following components in percentage by weight: 0.01 to 0.5 percent of olopatadine and 0.01 to 0.5 percent of brimonidine. According to the compound preparation composition, olopatadine and brimonidine are combined for use, the curative effect is remarkably improved compared with single-drug treatment, a good synergistic interaction effect is shown, multiple pharmacological effects are achieved through one-time drug administration, and drug use convenience and long-term treatment compliance are greatly improved.

The invention discloses application of traditional Chinese medicine monomer poplar bud flavin (including homologues thereof and extracts / mixtures containing the same) in preparation of drugs for treating nerve injury diseases and a preparation method of the drugs for treating the nerve injury diseases. The pharmacological action mechanism of the monomer poplar bud flavin is deeply explored, and animal model application effect verification proves that the monomer poplar bud flavin (including homologues thereof and extracts / mixtures containing the homologues) can obviously improve core symptoms of cerebral apoplexy, autism, Alzheimer's disease and depression models, is high in safety, and can be used for preparing a medicine for treating cerebral apoplexy, autism, Alzheimer's disease and depression models. The invention also develops a medicine for treating cerebral apoplexy, autism, Alzheimer's disease and depression, which takes the poplatin as a core component (including homologues of the poplatin and extracts / mixtures containing the poplatin), and is expected to provide new research results and application schemes for treatment of nerve injury diseases such as cerebral apoplexy, autism, Alzheimer's disease, depression and the like. The important significance is realized on improving the treatment effect.

According to the application of the dipsacus asper saponin VI in regulating and controlling the differentiation of the surface stem cells, the brand new pharmacological action of the dipsacus asper saponin VI in targeted promotion of the differentiation of the epidermal stem cells is found for the first time, the cognitive limitation of the prior art is broken through, a brand new target spot and direction are provided for research and development of innovative drugs for wound repair, and the application of the dipsacus asper saponin VI in regulating and controlling the differentiation of the epidermal stem cells is realized. A medicine containing teasel saponin VI is adopted, epidermal stem cells are taken as a core target, wound reepithelialization is accelerated by promoting directional differentiation of the epidermal stem cells, the mechanism is clear, the targeting property is high, a core link capable of directly hitting wound healing is adopted, epidermal stem cell differentiation is regulated in a targeted manner, and meanwhile, the medicine has the synergistic effects of resisting inflammation and promoting angiogenesis; the obvious application potential is realized on refractory wounds such as diabetic feet and pressure sores.

Disclosed are a novel crystal form of tegoprazan sulfonic acid salt and a method of preparing a pharmaceutical composition containing the same. More specifically, disclosed are a novel crystal form of tegoprazan sulfonic acid salt, which greatly improves raw material stability, non-hygroscopicity and solubility, and exhibits pharmacological effects comparable to conventional tegoprazan free base forms, and a method of preparing the same. The novel crystal form of tegoprazan sulfonic acid salt has excellent raw material stability, non-hygroscopicity, and solubility and is thus useful for the development of a novel tegoprazan formulation.

The invention discloses phthalide compounds as well as a preparation method and application thereof. The phthalide compounds comprise a compound 1 and a compound 2 as well as a preparation method and application thereof. The two compounds are separated and purified from the ethyl acetate extract of the traditional Chinese medicine ligusticum wallichii for the first time. An in-vitro biological activity test shows that the two compounds have obvious inhibitory activity on xanthine oxidase, which indicates that the two compounds can be used as novel potential candidate drugs for treating hyperuricemia and gout. The embodiment of the invention provides a preparation method, structural identification and pharmacological action of the two phthalide compounds, and provides a new strategy for treatment of hyperuricemia and gout diseases.

The invention relates to the technical field of mastopathy drugs, in particular to a traditional Chinese medicine composition, a preparation method thereof and application of the traditional Chinese medicine composition in treatment of breast cancer. The traditional Chinese medicine composition is prepared from the following raw materials: radix astragali, cortex moutan, cortex cinnamomi, radix sophorae flavescentis, semen plantaginis, herba ephedrae, rhizoma chuanxiong, spica prunellae, fructus cnidii, semen cuscutae, radix angelicae sinensis, wine-processed fructus ligustri lucidi, radix rehmanniae preparata, rhizoma atractylodis The traditional Chinese medicine composition is reasonable in compatibility of various raw materials, can generate a synergistic effect, has a good treatment effect on breast cancer, treats both symptoms and root causes, combines purgation and tonification, can strengthen the body resistance to eliminate pathogenic factors, reduces toxicity and improves the effect, has a definite drug effect, reduces the possibility of tumor metastasis, enhances the immunity of the organism, and improves the living quality and survival rate of patients. According to the limited preparation method, active ingredients in the medicinal materials can be extracted to the maximum extent, pharmacological action is promoted to be played, the ingredients are natural, side effects are small, and wide application prospects are achieved.

The present invention discloses a natural raw material synergistic blood pressure lowering health-care tea drink and a preparation method thereof, and relates to the technical field of health-care tea drinks, the raw materials comprise, by weight, 50 parts of radix glehniae, 20 parts of radix angelicae and 20 parts of fructus psoraleae, and the auxiliary materials comprise, by weight, 3 parts of sodium benzoate, 3 parts of sodium cyclamate, 2 parts of chitosan, 2 parts of xanthan gum, 0.1 part of lemon yellow and 0.1 part of carmine. According to the blood pressure-reducing health-care tea drink with natural raw materials synergistic interaction, the synergistic interaction among the raw materials is realized through the matching effect among the radix glehniae, the fructus psoraleae and the radix angelicae, the radix glehniae has the effects of reducing blood pressure and blood fat, improving digestion, improving sleep and the like, and the radix angelicae has the effects of reducing blood pressure, relieving exterior syndrome, dispelling wind, relieving pain, eliminating dampness, arresting leucorrhea, diminishing swelling, expelling pus and the like; the psoralen has pharmacological effects of strengthening heart, resisting osteoporosis, resisting tumors, resisting oxidation, protecting nerves and the like, and the active component methoxysarin is extracted and added into the tea drink, so that the tea drink can efficiently reduce blood pressure and improve blood circulation.

This invention provides a novel application of IdeS, which is used to prepare products addressing photoaging of the skin. These products include skincare products and pharmaceuticals for the prevention and / or treatment of photoaging. The pharmaceuticals are in the form of ointments, and the skincare products are used as adjunct treatments for preventing and treating photoaging. IdeS treatment significantly improves the extensive erythema, wrinkles, desquamation, inflammation, and thickened stratum corneum observed in photoaging model mice. It has been developed as a novel biological therapeutic drug with strong pharmacological effects, few side effects, and avoidance of allergic reactions, thus providing a basis for the clinical treatment of photoaging and photodamage.

The present invention relates to a liposome composition for oral administration, the composition comprising a GLP-1 analog. The liposome according to the present invention has both excellent encapsulation efficiency and encapsulation content of the GLP-1 analog drug, and the prepared liposome composition resists digestive enzymes in the gastrointestinal tract and does not easily degrade when administered orally, thus having excellent stability, and has a high absorption rate in the body, and thus exhibits excellent pharmacological effects.

The invention provides application of Laetanine in preparation of a medicine for preventing and / or treating gastric ulcer, and belongs to the technical field of biological medicine. The medicine prepared from the Laetanine has the effects of relieving gastric ulcer pain, reducing the pH value of gastric juice and reducing the ET-1 content in plasma at the same time. Research confirms that the Lapanine can enable the pH value of gastric juice of a rat to tend to a normal value, increase the contents of PGE2 and T-SOD in plasma and reduce the contents of ET-1, TNF-alpha and IL-6 in the plasma, that is, the Lapanine has the effects of relieving gastric ulcer pain, reducing the pH value of the gastric juice and reducing the content of ET-1 in the plasma at the same time, the specific pharmacological action of the Lapanine in gastric ulcer is further confirmed, and a foundation is laid for clinical use.

The invention provides a component separation method of a xanthoceras sorbifolia bunge tea leaf dichloromethane extract. Comprising the following steps: step 1, preparing materials and equipment; step 2, extracting and separating: weighing shiny-leaved yellowhorn tea leaf powder, heating, refluxing and extracting by using an ethanol solution, combining extracting solutions, and concentrating under reduced pressure to obtain a total extract; extracting with dichloromethane, concentrating under reduced pressure to obtain 26.1 g of dichloromethane, dissolving the residual methanol extract with 70% methanol water, filtering, performing preparative liquid chromatography, and eluting; 3, through separation and analysis, the four compounds are determined to be quercitrin, quercetin, myricetin and rutin respectively. According to separation results, the xanthoceras sorbifolia bunge tea contains more flavonoid components, and the flavonoid components have the effects of resisting inflammation, resisting oxidation, reducing blood fat and the like and are important components for playing pharmacological effects of the xanthoceras sorbifolia bunge tea.

The invention discloses an application of fennel volatile oil in a medicine for treating pressure sores. The fennel volatile oil is used as a unique active component for preparing the medicine for treating the pressure sores. Through deep research on the pharmacological action of the fennel volatile oil and the treatment effect on a pressure sore animal model, it is proved that the fennel volatile oil can effectively promote healing of pressure sores, and a safer and more effective treatment choice can be provided for pressure sore patients.

The present application relates to tetrahydroprotoberberine THPB derivatives, and particularly relates to application of a tetrahydroprotoberberine THPB derivative GP10 in preparation of a medicine for improving or treating epilepsy and neuroinflammation; the new candidate compound GP10 discovered by the present application has significant anti-epilepsy activity, not only expands the pharmacological effect spectrum of THPBs, but also provides a new strategy for research and development of anti-epilepsy drugs or auxiliary treatment drugs. Meanwhile, the present application research proves that GP10 can interfere with the structure of DAMP molecules, affect the combination of DAMP molecules and PRR and the downstream signal transduction, and the mechanism is verified through in-vivo and in-vitro experiments, which provides a new theoretical basis and thought for development of anti-inflammatory drugs.

The present invention relates to a sustained-release pharmaceutical composition using a GLP-1 receptor agonist. Specifically, microparticles comprising semaglutide are prepared using a 5-hydroxydopamine-modified self-crosslinkable hyaluronic acid derivative (SAMH) as a carrier, and the semaglutide is gradually released over a long period of time upon injection into the body, thereby providing excellent effects on blood glucose control and weight management. The sustained-release pharmaceutical composition according to the present invention maintains a low viscosity before administration to the human body, thus being easily administered by injection, and is self-crosslinked and hydrogelated after administration to the human body, and thus can maintain the pharmacological effect of the semaglutide for a long period of time with only a single administration.

Provided is a novel compound that is useful as an antiviral drug, exhibits strong drug efficacy in low dosages, can be used safely, and has reverse transcriptase inhibitory activity. This compound is expressed by formula (I) (wherein ring A is (i-a) or (i-b) (where R1 represents a halogen or the like, R2 represents a halogen or the like, R3 represents hydrogen or the like, L represents –O– or the like, R4 represents hydrogen or the like, ring B represents an optionally substituted five-membered or six-membered aromatic heterocycle ring or the like, and n represents an integer of 1-3), and Z is (Z) (where each R6 independently represents a halogen or the like, and m represents an integer of 0-2)).

The invention belongs to the field of organic synthesis, and relates to preparation of organic germanium compounds, in particular to a visible light induced germanium alkylation synthesis method. According to the method, germane hydride and a hypervalent iodine reagent are taken as starting raw materials, and under the catalytic action of a photocatalyst 9, 10-phenanthrenequinone, a series of alkynyl, alkenyl, nitrile and phenyl germanes are synthesized. The reaction has the advantages of environmental friendliness, mild conditions, simplicity and convenience in operation, high atom / step economy, wide substrate application range and the like. By applying the method, the germanium-based post-modification of the drug molecule derivative can be realized, and a convenient means is provided for constructing an organic germanium compound which is unique in structure and has potential biological activity and pharmacological action.

The invention discloses a Chinese herbal medicine pain-relieving formula and a preparation process thereof, relates to the technical field of traditional Chinese medicines, and solves the technical problems of complex formula, slow effect taking speed and single dosage form in the existing technical scheme. The Chinese herbal medicine pain-relieving formula comprises the following raw materials in parts by weight: 1 part of radix tinosporae, 1 part of sinomenium acutum, 1 part of radix tinosporae and 1 part of sinomenium acutum. The preparation method comprises the following steps: cleaning the raw material medicines of tinospora cordifolia and sinomenium acutum, and removing impurities; carrying out drying treatment on the pretreated raw material medicines; mixing the dried raw material medicines, and crushing into fine powder; the formula provided by the invention is refined, the pharmacological action of each component is clear, and the tinospora cordifolia clears away heat and toxic materials and relieves swelling Sinomenium acutum dispels wind, eliminates dampness, promotes qi circulation and dredges The two medicines are combined to clear heat without damaging yang and promote the circulation of qi without consuming vital energy and act together, so that the dual effects of clearing heat, removing toxicity, promoting the circulation of qi and dredging collaterals are realized; the invention provides a plurality of dosage form choices, so that the formula can flexibly adapt to the requirements of different disease courses, different scenes and different patient groups.

Application of total monoterpene glycosides of Paeonia veitchii Lynch and analysis method for active ingredients in total monoterpene glycosides of Paeonia veitchii Lynch. For the first time, the UPLC-MS / MS technology is adopted in the present invention to establish the fingerprint of total monoterpene glycosides of Paeonia veitchii Lynch from 11 batches of different producing areas, laying a foundation for revealing the effective ingredient group of total monoterpene glycosides of Paeonia veitchii Lynch. Five compounds with muscle-building effects mainly composed of total monoterpene glycosides of Paeonia veitchii Lynch are determined in the present invention, including 4 monoterpene glycoside compounds, and one belongs to the isomer of benzoylpaeoniflorin. Application of total monoterpene glycosides of Paeonia veitchii Lynch in preparing animal feed or medicine for increasing muscle. The present invention establishes a fingerprint-pharmacodynamic correlation model of total monoterpene glycosides of Paeonia veitchii Lynch. While establishing the quality evaluation standard for muscle-building effects based on the fingerprint of the effective part of total monoterpene glycosides of Paeonia veitchii Lynch, it also provides a new idea for screening active ingredients of other pharmacological effects of Paeonia veitchii Lynch. The present invention lays a theoretical foundation for the development of muscle-building foods for fitness people and provides new resources for the development of animal feed additives in animal husbandry.

The invention discloses a novel plant toothpaste preparation method and a product traceable information code manufacturing method. The novel plant toothpaste preparation method comprises the following steps: 1, taking plant straws, plant branches, plant leaves, plant cores, plant rhizomes, plant fruits, peels and shells thereof and the like as abrasive raw materials of toothpaste; for example, sugarcane, corn stalks, corncobs, coconut peels and shells and the like can be used as abrasive raw materials, so that the novel plant toothpaste is harmless to human bodies, reduces tooth wear, protects tooth health, and has pharmacological effects of refreshing, diminishing inflammation, relieving pain, cleaning, whitening and the like of Chinese herbal medicines; 2, a product traceable information code manufacturing method of the novel plant toothpaste comprises the following steps: performing mathematical hybrid operation on unified codes, geographic information, weather information, toothpaste types, production dates, manufacturer brand codes, production batch information and the like of products to generate a hybrid digital code, a bar code, a two-dimensional code and the like; and a unique code which is printed on a packaging carrier of the toothpaste and serves as product traceability.

The invention discloses a gemfibrozil deuterated derivative as shown in a formula (I) as well as a preparation method and application thereof, and belongs to the field of organic and pharmaceutical synthesis. The method is simple in preparation process and low in cost. The gemfibrozil deuterated derivative synthesized by the method has the advantages of high purity and high deuterated rate. The invention also discloses an application of the gemfibrozil deuterated derivative in treatment of hyperlipidemia. The pharmacological action of the gemfibrozil deuterated derivative disclosed by the invention is obviously improved, and toxic metabolites of the gemfibrozil deuterated derivative are obviously reduced.

The invention discloses a compound traditional Chinese medicine preparation for improving tumor immunity and resisting tumors, belongs to the technical field of anti-tumor traditional Chinese medicines, and discloses a compound traditional Chinese medicine preparation for improving tumor immunity and resisting tumors. The traditional Chinese medicine composition comprises the following components in parts by weight: 10-25 parts of ginseng, 15-18 parts of selfheal, 12-18 parts of seaweed, 12-19 parts of astragalus membranaceus, 10-16 parts of angelica sinensis, 18-30 parts of oldenlandia diffusa, 10-15 parts of fleece-flower root, 10-14 parts of poria cocos, 10-16 parts of thunberg fritillary bulb, 8-14 parts of pseudobulbus cremastrae seu pleiones and 8-17 parts of curcuma zedoary. Through the specific pharmacological action, growth and proliferation of thyroid tumor cells are inhibited, the development speed of tumors can be slowed down, the malignancy degree of the tumors can be reduced, apoptosis of the thyroid tumor cells can be induced, and the number of the tumor cells can be effectively reduced by inducing apoptosis of the tumor cells, so that the anti-tumor purpose is achieved.