49 results about "Brefeldin A" patented technology

The invention provides brefeldin A ester derivatives having antitumor activity and their preparation method and use. The brefeldin A ester derivatives have structures shown in the structural general formula (I). The brefeldin A ester derivatives have high effects on esophagus cancer, lung cancer, kidney cancer, colorectal cancer and prostatic cancer and have an in-vitro detection effective inhibition rate of 80%. The preparation method of the brefeldin A ester derivatives has simple processes and can be operated easily.

The invention discloses brefeldin A ester derivatives, and preparation and application thereof. The brefeldin A ester derivative compounds have antioxidation activity and antitumor activity, wherein the brefeldin A ester derivative compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable antioxidation effect and can remove DPPH, ABTS and super oxygen free radical (O2<->), and the compound (I-7) has better removal effect on DPPH, ABTS and super oxygen free radical (O2<->) than vitamin E; and the compound disclosed as Formula (I-1), (I-3), (I-5) or (I-7) has favorable inhibition activity for human lung cancer cells A549. Therefore, the result shows that the derivatives have wide application prospects in the drug development system, provide a new and broader idea for synthesizing and screening BFA (brefeldin A) derivative drugs and provide a more efficient way for treating related diseases.

The invention relates to the technical field of microbes, and concretely relates to a new plant endophytic fungus and its application in the preparation of brefeldin A (BFA). The plant endophytic fungus is Eupenicillium brefeldianum F4a, and is preserved in China Center for Type Culture Collection on Dec. 18, 2012 with the preservation number of CCTCC M2012531. The Eupenicillium brefeldianum F4a can generate high content BFA, and the highest fermentation output reaches 1.9g/L. The invention also provides a method for preparing the highly pure BFA through HP20 solid phase extraction and rapid silica gel column chromatography or a pure crystallization technology. The method has the advantages of low production cost, great reduction of treatment and pollution of organic matters, and good industrial prospect. The BFA prepared in the invention has antifungal and insecticidal activity, and is an ideal veterinary or agricultural candidate drug.

The invention relates to Brefeldin A-producing bacteria, a preparation method, a method for preparing the brefeldin A by fermentation and the application thereof. The Brefeldin A-producing bacteria has the advantages of easy selection, cultivation and storage, low cost, simple process, short preparation period, high yield, no usage of toxic raw material, less organic solvent, thorough guarantee of medicine resource, potential of mass production and favorable economic and social benefits, contributes to the maintenance of ecological balance and the protection of natural resources. The fermentation product of the invention, of which the main component is THSG, develops novel medical application, the Brefeldin A has high safety, low toxicity, stable property, stronger pharmacological action, simple preparation process, high yield and considerably wide range of application, is multipurpose, and can provide a novel source for medicines for preventing, diagnosing, detecting, protecting, curing and researching antimycotic, antiviral and antineoplastic diseases and the directly related diseases.

The invention relates to the field of medicinal chemistry, and relates to derivatives obtained by simultaneous modification on 4-site and 7-site of brefeldin A. Particularly, the invention relates to 4,7-site difurazan NO donor substituted brefeldin A derivatives, and a preparation method of the derivatives and uses of the derivatives in preparing antineoplastic drugs. The brefeldin A derivatives are as shown by a general formula I or II, shown in the description, wherein m and n are respectively integers within the range of 1 to 8.

The present invention discloses compounds for the treatment of cancer and its application. These compounds comprises one of the following compound: Ammonium pyrrolidinedithiocarbamate Bay 11-7085 BIO Brefeldin A (+)-Butaclamol Calcimycin Calmidazoliur chloride Chelerythrine chloride CK2 Inhibitor 2 CGP-74514A hydrochloride CGS-12066A meleate Dequalinium dichloride Dihydroouabain Diphenyleneiodonium chloride Emetine dihydrochloride hydrate GR 127935 hydrochloride Nifedipine 6-Nitroso-1,2-benzopyrone Palmitoyl-DL-Carnitine chloride Parthenolide PD 169316 1,10-Phenanthroline monohydrate 4-Phenyl-3-furoxancarbonitrile Prazosin hydrochloride Protoporphyrin IX disodium Quinacrine dihydrochloride Quabain Retinoic acid p-hydroxyanilide Rottlerin Sanguinarine chloride Tetraethylthium disulfide and SU 9516. The invention also provides new uses of these compounds, compounds such as for the preparation of the treatment of cancer, inhibit cancer cell, cancer stem cell growth and provides a new pharmaceutical composition for treating cancers

The invention discloses a brefeldin A glycosylated derivative shown in a formula (I) and a preparation method and application thereof. The invention provides a novel brefeldin A glycosylated derivative; the water solubility of the brefeldin A glycosylated derivative is enhanced; the tumor inhibiting activity of the brefeldin A is retained; in-vitro detection shows that the effective inhibition rate to cancer cells such as a human esophagus cancer and the like can be up to 80%; the preparation method of the preferred brefeldin A glycosylated derivative is obtained by optimizing the conditions of a compound (II), (img file='DDA0000451154560000011.TIF' wi='776' he='307'/), in the formula (I), R is pentose, hexose, amino hexose or hexose acid.

The invention discloses brefeldin A (BFA) and a derivative and application thereof. The brefeldin A has the extremely high anti-HIV latency activity, and the series compound is obtained through a static culture fermentation method and chemical modification. The brefeldin A and the derivative thereof are of a structure shown as a formula (I) (please see the formula in the description), wherein R1-R5 represent H, OH, CH3, OCH3 and (OCH3)2 or OCOCH3 respectively, and R6 represents CH3. The brefeldin A and the derivative thereof can serve as anti-HIV latency drugs and can be applied to preparation of a drug for treating an AIDS jointly with an antiretroviral drug, when the brefeldin A and the derivative thereof are jointly applied with the antiretroviral drug, the brefeldin A and the derivative thereof can enable latent HIVs in infected cells to be expressed, have the effect of intervening HIV latency and can clear the activated and infection-latent cells to accelerate clearance of a latent virus storage, and the wide application prospect is achieved.

The invention belongs to the technical filed of microbes, and concretely relates to Penicillium ochrochloron and its application in the preparation of brefeldin A. A technical problem to be solved in the invention is providing a new choice for production of BFA through biological fermentation. A bacterial strain produced in the invention is Penicillium ochrochloron SWUKD4.211, and has a preservation number of CCTCC M2015022. The invention also provides a method for producing the BFA by adopting Penicillium ochrochloron fermentation. The BFA production ability of the bacterial strain obtained through the method can reach 356.0mg/L, and the method provides a new choice for the production of the BFA, provides a precisou strain for biological pharmacy, and has great application values.

Polyethylene glycol-brefeldin A ester derivatives are provided. Structures of the derivatives are shown as a formula I, a formula II, a formula III or a formula IV. Applications of the novel compounds in preparation of medicines for treating and preventing liver cancer, lung cancer, breast cancer, kidney cancer, cancer of colon and prostatic cancer are also provided.

The invention belongs to the field of natural medicine and medicinal chemistry, and relates to a preparation method and uses of a class of brefeldin A derivative containing chlormethine linked at site4 and having antitumor activity, wherein the brefeldin A derivative containing chlormethine linked at site 4, and the pharmaceutically acceptable salt have a structure represented by the following general formula I, and n is defined in the claim and specification.

The invention discloses a brefeldin A combined anti-cancer compound medicine, aims to provide a brefeldin A combined anti-cancer compound medicine which has low using concentration and small toxic and side effects and has an excellent treatment effect on tumors, in particular prostatic cancer, and belongs to the technical field of medicines. According to the technical key points, the medicine is prepared from brefeldin A combined with taxane drugs.

The invention belongs to the field of natural medicine and medicinal chemistry, and relates to a preparation method and uses of a class of brefeldin A derivative containing chlormethine linked at site4 and site 7 and having antitumor activity, wherein the brefeldin A derivative containing chlormethine linked at site 4 and site 7, and the pharmaceutically acceptable salt have a structure represented by the following general formula I, and n is defined in the claim and specification.

Peripherally administered Brefeldin A and its analogs and derivatives are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal issues.

Belonging to the technical field of T lymphocyte receptors, the invention provides a method for non-therapeutic purpose restoration of the immune function of infiltrating T lymphocytes. The method includes: mixing an immune function impaired infiltrating T lymphocyte solution with a blocking agent to obtain a blocking agent-containing solution, wherein the blocking agent includes an anti-Tim-3 blocking antibody and/or an anti-PD-1 blocking antibody; mixing the blocking agent-containing solution with an anti-CD3 antibody and an anti-CD28 antibody, and then performing cultivation to obtain a culture; and mixing the culture with Brefeldin A, and performing incubation to obtain immune function restored infiltrating T lymphocytes. The method provided by the invention can restore the immune function of immune function impaired infiltrating T lymphocytes.

The invention relates to the field of medicinal chemistry, and in particular, relates to an application of a brefeldin A ester derivative in the aspect of inhibiting tumor proliferation activity; the brefeldin A ester derivative can be used for preventing or treating hyperproliferative diseases, and the structure of the brefeldin A ester derivative is represented by a formula (I). Hyperproliferative diseases comprise liver cancer, leukemia, breast cancer, colonic adenocarcinoma, gastric cancer, lung cancer, Bartter's esophagus cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymph cancer, kidney cancer, brain cancer, nerve cancer, nasopharynx cancer, oral cancer and colorectal cancer, so that the brefeldin A ester derivative has the potential of being developed into a novel antitumor drug.