87 results about "Andrographolide derivatives" patented technology

The invention relates to an andrographolide derivative, which has the structure as shown in a general formula I: wherein, R1, R2 and R3 are the same or different hydrogen, substituted or non-substituted organic acid radical, inorganic acid radical, alkyl, aryl or heteroaryl, while at least one of R1, R2 and R3 is R-lipoic acid or S-lipoic acid or the mixture of R-lipoic acid and S-lipoic acid or the corresponding dihydrolipoic acid or acetylcysteine radical of R-lipoic acid or S-lipoic acid; the derivative has good anti-tumor effect, and the derivative can cause apoptosis of tumor cells, directly eliminate gram positive bacteria, staphylococcus aureus and sensitivities MRSA5676 and MRSA5677, inhibit the QS system of gram negative bacteria and pseudomonas aeruginosa and inhibit and damage the formation of the bio-film of pseudomonas aeruginosa; the product has prominent hypoplycemic effect and is suitable for the preparation of the medicines that can cure cancers, inflammations, diabetes mellitus and bacterial and viral infection.

The present invention relates to carbon glycoside compound, and is especially 15-(14-deoxy-11, 12-dehydro)-andrographolide carbon glycoside derivative and its preparation process. The preparation process includes dewatering andrographolide as precursor compound, epoxidation and other reaction to obtain serial andrographolide derivatives; dissolving the derivatives and beta- carbon glycoside ketone in organic solvent and condensation reaction at certain temperature in the presence of catalyst for certain time. The derivative is significant in developing andrographolide.

The invention belongs to the technical field of medicines, discloses applications of andrographolide derivatives in preparation of medicines preventing and treating hepatic fibrosis, and relates to 15-benzylidene-14-deoxy-11,12-dehydroandrographolide derivatives and 3,19 esterified compounds thereof. Experiments prove that the compounds significantly inhibit human hepatic stellate cell LX-2 metastasis and activation, significantly reduce the fibrosis level of hepatic tissues of rats affected with hepatic fibrosis, reduce contents of extracellular matrix protein (ECM) related components, significantly reduce the level of immune inflammation correlation factors of rats affected with hepatic fibrosis, effectively inhibit immuno-inflammatory responses, inhibit hepatic stellate cell activation in hepatic tissues, and promote collagen degradation. The compounds are used as active components for preparing the anti-hepatic fibrosis medicines, and are efficient and low in toxicity, thus providing a novel medicine route for hepatic fibrosis treatment and prevention, and expanding the optional range of clinical medicine application. The compounds and the applications have good development prospects.

The invention discloses a compound and medical acceptable salt with general formula (I) and making method and their drug agent, which possesses better COX-2 expressive inhibiting and TNF-alpha inhibiting and IL-6 inhibiting action.

The invention discloses the medical application of a 15-methylene replaced andrographolide derivant as shown in general formula 1, more particularly relates to the application thereof in preparing anti-hepatitis B virus drugs, pertaining to the pharmaceutical chemistry field. HepG2.2.15 cells are used for detecting the secretory volumes of HBsAg and HBeAg and the HBV DNA level related to viral particles in the supernatant liquid of a nutrient solution, and the result shows that the 15-methylene replaced andrographolide derivant has good in-vitro anti-HBV effect. The 15-methylene replaced andrographolide derivant has better development and application prospect by being applied in preparing drugs used for treating and preventing Hepatitis B.

The invention belongs to the technical field of medicine, discloses the application of andrographolide derivative in preparation antineoplastic agents, and relates to 15-benzyl subunit -14-deoxy-11,12-dehydrogenation andrographolide derivative and 3,19 esters thereof. The experience shows that the chemical compounds have the remarkable effects of restraining cancer cell cloning and forming and resisting migration of cancer cell and human vascular endothelial; and the chemical compounds show stronger effects of restraining tumor growth, antimetastasis and antiangiogenic in a mice transplanting tumour animal model. The chemical compounds are used as activity components for preparing antineoplastic agents, have the advantages of high efficient and low toxicity. the invention provides a new drug way for curing and preventing transfer of the tumour, expands selection range of clinical pharmacy, and is significant to taking full advantage of plant resources of the common andrographis herb.

The present invention provides a methods and compositions for treating a host afflicted with a viral infection, particularly a Flaviviridae infection, including hepatitis C infection, comprising administering an effective antiviral amount of a derivative of andrographolide alone or in combination or alternation with another antiviral compound.

The invention belongs to the technical field of medicinal chemistry, and discloses application of andrographolide C15 substituted series derivatives to the preparation of a medicine for resisting hepatitis B. HepG2.2.15 cells are used for detecting the secretion amount of hepatitis B surface antigen (HBsAg) in culture solution supernatant, a large number of andrographolide derivative compounds are screened, and compounds which have high hepatitis B virus (HBV) resistance are optimally selected and have a structure shown in a general formula 1; and the compounds have high HBV-resistant activity, high efficiency and low toxicity and are taken as active ingredients to be used for preparing a medicine for resisting viral hepatitis B, and a new medicine is provided for treating hepatitis, so that the selectable range of clinical medicines is expanded.

The invention relates to an andrographolide derivative the structure of which is shown in a formula (I) or (II) and a stereoisomer, a stereomer, a tautomer, a solvate, a polymorph, a metabolin, ester, a pharmaceutically acceptable salt or a prodrug of the derivative. The andrographolide compound provided by the invention has the advantages of good solubility, high purity and good antipyretic property; and the andrographolide compound is especially suitable to be used as an effective component for preparing antipyretic, anti-inflammatory and antimicrobial medicaments.

The invention relates to applications of andrographolide derivatives A1-4, B1-2, C1-2 and D1-13 in preparing anti-HIV medicines.

The invention relates to a method for preparing andrographolide derivatives, and a preparation thereof. The preparation is a salt which consists of Kalii Dethydroandrographolidi Succinas and Adamantanes and has the effect of synergistic interaction. The curative effect of the preparation is better than that of the independent use of Kalii Dethydroandrographolidi Succinas and Adamantanes.

The invention discloses a new water-soluble andrographolide derivative, salt and a preparation method thereof and medical application of the derivative comprising the salt and pharmaceutical composition. The invention also discloses an inhibiting action of andrographolide derivative to macrophage secretion NO induced by LPS, antibacterial action and inhibiting action to pinna swelling induced by xylene, can be used for preparing treating drugs for anti-inflammatory, antibacterial, antivirus and anticancer and can be used for preparing drugs for treating infectious shock, septicemia, inflammatory bowel disease, rheumatoid arthritis and juvenile rheumatoid arthritis.

The invention discloses the application of an andrographolide C15 substitution derivative in manufacturing an anti-hepatitis drug, which belongs to the technical field of pharmaceutical chemistry. According to the invention, MDBK (mardin-darby bovine kidney cells) and BVDV (bovine viral diarrhea virus) are utilized to study the inhibitory action of the compound on cytopathic effect caused by the virus through an external screening model. Through the screening of a large number of andrographolide derivatives, the compound with a structure of general formula 1 is found to significantly inhibit MDBK cytopathic effect caused by the BVDV; the andrographolide C15 substitution derivative has high efficiency and low toxicity, thereby being used for manufacturing medicaments for treating and preventing hepatitis and having good prospect in development and application. The general formula 1 is shown in the description.

The invention discloses an andrographolide derivative nitric oxide donor compound as well as a preparation method and an application thereof. The derivative has a structure expressed by a formula (I), wherein R1 refers to hydrogen, organic acid radical, inorganic acid radical, alkyl, aryl or heteroaryl, R2 refers to hydrogen, organic acid radical, inorganic acid radical, alkyl, aryl or heteroaryl, R3 refers to hydrogen, organic acid radical, inorganic acid radical, alkyl, aryl or heteroaryl, and at least one of R1, R2 and R3 is a functional group capable of releasing nitric oxide or an organic acid radical substituted by nitroxide group. The andrographolide derivative nitric oxide donor compound can be used for preparing medicaments for treating diabetes, medicaments for treating cardiovascular diseases, antimicrobial medicaments and antiviral medicaments. The medicaments can be prepared to tablets, capsules, granules, fine granules, powder, pills, patches, oral liquid or injection.

The invention discloses an andrographolide derivative and a preparation method and application thereof, belongs to the technical field of medicines, and relates to a novel compound with respiratory virus activity resistance, an isomer of the compound or salt capable of being accepted pharmaceutically, a medicine composition containing the compound, a preparation method of the medicine composition and application of the compound in the medicine for treating and / or preventing infections caused by respiratory viruses. The compound and the isomer of the compound or the sat capable of being accepted pharmaceutically are shown in the general formula (I), wherein R1, R2 and R3 are specified in the patent claim and the specification.

The invention provides a novel antiviral andrographolide derivative and a preparation method and application thereof. The novel antiviral andrographolide derivative, non-toxic pharmaceutically acceptable salts and compositions thereof have good application prospects in aspects such as infection resistance, virus resistance, inflammation diminishment and antipyretic analgesics. The derivative has high water solubility and high oral bioavailability. According to the novel antiviral andrographolide derivative, the andrographolide serves as a raw material, the preparation process is simple, the cost is low, and industrial production can be performed.

The invention relates to a defervescence anti-inflammatory and anti-infection medicine with immunization function, a preparation and an application thereof. Andrographolidume derivant is andrographolidume sodium bisulfite hydrate, and the molecular formula of the andrographolidume sodium bisulfite hydrate is C20H29O7SNa.nH2O, wherein n is equal to a number between 0.88 and 3.5. The derivant has better water solubility and better storage stability, and is suitable to prepare treatment or prevention medicines for reducing fever and relieving internal heat of fever, resisting bacteria and diminishing inflammation, resisting virus and allaying fever, and adjusting immunologic function.

We describe for the first time that andrographolide dirivatives such as DDAG effectively reduced OVA-induced inflammatory cell recruitment into BAL fluid, IL-4, IL-5, IL-13 and eotaxin production, serum IgE synthesis, pulmonary eosinophilia, mucus hypersecretion and AHR in a mouse asthma model potentially via inhibition of NF-kappa B activity. Moreover, low dose of DDAG and glucocorticoid combination treatment synergistically attenuate inflammation in mouse asthma model. These findings support a therapeutic value for DDAG in the treatment of asthma.

The invention discloses an andrographolide derivative and a preparation method and application thereof. The derivative has a structure expressed by the formula (1), wherein R1 is C1 to C11 chain hydrocarbon or C1 to C11 chain hydrocarbon with terminals substituted by ternary to heptabasic ring groups; and R2 and R3 are hydrogen, organic acid radical, inorganic acid radical, alkyl or acryl. The andrographolide derivative can be made into tablets, capsules, granules, fine granules, powder, pills, patches, oral liquid or injection.

The invention discloses an andrographolidume composition and application thereof. The composition consists of a component I and a component II according to a molar ratio of between 1:10 and 10:1, wherein the component I is at least one of andrographolidume, andrographolidume derivatives and pharmaceutically acceptable salts of the andrographolidume derivatives, and the component II is at least one of lipoic acid and dihydrolipoic acid. The composition can be prepared into anticancer, anti-inflammatory, antibacterial, antivirus or hypoglycemic medicaments.

The present invention relates to novel derivatives of Andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of Andrographolide have the general formula (I)The andrographolide derivatives represented by general formula (I) are useful for treating cancer, HSV, HIV, psoriasis, restonosis, atherosclerosis, other cardiovascular disorders, and can be used as antiviral, antimalarial, antibacterial, hepatoprotective, and immunomodulating agents and for treatment of other metabolic disorders.

The invention discloses the application of a 15-methylene replaced andrographolide derivant as shown in general formula 1 in preparing anti-inflammatory, antipyretics and analgetics drugs, pertaining to the pharmaceutical chemistry field. Mice auricular swelling induced by dimethylbenzene, cotton ball granuloma of mice, hyperpyrexia of rats induced by yeast, mouse hot-plate test, writhing test of mice and other models are used for testifying that the 15-methylene replaced andrographolide derivant has anti-inflammatory, antipyretic and analgetic functions. Compared with andrographolide, the 15-methylene replaced andrographolide derivant has better anti-inflammatory, antipyretic and analgetic functions, and the research result of mouse acute toxicity test shows that the toxicity of the 15-methylene replaced andrographolide derivant is very slight. The 15-methylene replaced andrographolide derivant has relatively good application prospect by being applied to the development of anti-inflammatory, antipyretics and analgetics drugs.

The invention discloses a compound and medical acceptable salt with general formula (I) and making method and their drug agent, which possesses better COX-2 expressive inhibiting and TNF-alpha inhibiting and IL-6 inhibiting action.

The invention discloses indole andrographolide, ramification of the indole andrographolide and a preparing method and medical application of the ramification, and belongs to the field of medicinal chemistry. The structure general formulas of the ramification of the indole andrographolide are shown in (I) and (II) in the specification, R1 represents hydrogen, substituent or non-substituent C1-8 aliphatic series acyl, substituent or non-substituent aromatic acyl and silylation, R2 and R4 represent hydrogen, substituent or non-substituent C1-8 aliphatic series acyl, substituent or non-substituent aromatic acyl and silylation or double bond delta 14, 15 generated through the elimination reaction of 14 bit or 15 bit, and R3 represents hydrogen, substituent or non-substituent C1-8 aliphatic series acyl and substituent or non-substituent aromatic acyl. The invention further discloses the preparing method of the indole andrographolide and medical application of the ramification in preparing antineoplastic drugs.

The invention discloses a 19-carboxyl andrographolide derivative, a preparation method and medicinal application thereof, belonging to the field of medicinal chemistry. The 19-carboxyl andrographolide derivative has a structure general formula shown in 1, wherein R1 is substituted or unsubstituted C1-8 aliphatic acyls, and substituted or unsubstituted benzoyl; R2 is hydrogen, substituted or unsubstituted C1-8 aliphatic acyls, and substituted or unsubstituted benzoyl; and R3 is hydrogen, substituted or unsubstituted C1-8 aliphatic acyls, and substituted or unsubstituted phenyl. The invention also discloses a preparation method of the 19-carboxyl andrographolide derivative and application of the 19-carboxyl andrographolide derivative to preparation of anti-tumor drugs.

The invention relates to water-soluble andrographolide derivatives, a preparation method thereof and application on medicine, and particularly, relates to water-soluble andrographolide derivatives shown in the general formula I and a mixer thereof, as well as the use of the water-soluble andrographolide derivatives and the mixer on antiphlogistic, antifebrile, antibacterial and other medicines, and the definitions of all substituent groups in the general formula are the same as those in the specification.

The invention belongs to the technical field of medicines and relates to 14-deoxy-14,15-didehydro andrographolide derivatives (1-3) shown in a general formula (I), and a medicine composition of the derivatives, a preparation method and application of the derivatives and the medicine composition of the derivatives to preparation of medicines for resisting hepatitis B.

The invention relates to a pharmaceutical composition with andrographolide derivatives as active components, and a preparation method thereof. The andrographolide derivatives can be mixed with oil and emulsifying agent and made into emulsion for treating diseases due to excessive nitric oxide formation. The andrographolide derivatives have the following general formula, wherein R1 and R2 are selected from acetyl, hydroxy, alkyl, aryl, ceteroary, aralkyl, heteroaralkyl, alkyloyl group, alkenyloyl group, aroyl and heteroaroyl, or R1 and R2 are substituted by isopropylidene, and R3 is selected from Hydrogen or halogen.

The invention discloses a pharmaceutical composition containing andrographolide and a use of the pharmaceutical composition, and relates to a drug containing common andrographis herb, belonging to the technical field of medicines. The pharmaceutical composition containing andrographolide comprises the following components in parts by mass: 95-100 parts of andrographolide, 0-5 parts of andrographolide derivatives and the balance of pharmaceutically acceptable carriers. The pharmaceutical composition containing andrographolide disclosed by the invention has the effects of resisting bacteria, diminishing inflammation, resisting viruses, bringing down a fever, regulating the immunity and resisting tumors, can be used for restraining synthesis, release and inflammatory activity of the prostaglandin, and is mainly used for treating diseases such as bacillary dysentery, viral pneumonia, viral upper respiratory tract infection and acute tonsillitis.

The invention discloses oxidized andrographolide, a preparation method and application in enhancing of in-vivo killing capacity of CIK (cytokine induced killer) cells. The oxidized andrographolide isa product of which the hydroxyl at the C18 site of the andrographolide is oxidized. The preparation method comprises the following steps of S1, culturing of bacterial strain; S2, converting of microorganisms; S3, extracting of converted product; S4, high-speed reverse purifying, wherein the ion liquid with effective concentration is added into the fermenting culture medium in step S1. The invention discloses an andrographolide derivative, and the andrographolide derivative is an oxidized product of the andrographolide; the andrographolide derivative is prepared by a microorganism conversion method. The oxidized andrographolide can enhance the in-vivo killing capacity of CIK cells on tumors.