49 results about "Altertoxin III" patented technology

The invention discloses nitrogen substitution podophyllum type derivatives with antitumor activity and a preparation method and application thereof. The nitrogen substitution podophyllum type derivatives (as formula V) with fine antitumor activity are prepared by introducing 1-(3-amino propyl) imidazole, benzimidazole, 2-thienylmethylamine or trihydroxymethyl aminomethane to C ring 4-position activated by 4-demethylation surface podophyllotoxin. The nitrogen substitution podophyllum type derivatives can act on tumor cells with multiple paths and multiple target points, and accordingly better antitumor curative effect is achieved. Antitumor activity of the derivatives is evidently increased compared with that of the 4-demethylation surface podophyllotoxin. The derivatives can be prepared into antitumor drugs to apply to antitumor therapies.

The invention discloses a sulfur-substituted podophyllum derivative, and a synthetic method and application thereof. Through sulfur substitution reaction, 2-mercapto-1,3,4-thiadiazole or 3-mercapto-1,2,4-triazole is respectively introduced into a C-4 site of podophyllotoxin or 4'-demethyl-epipodophyllotoxin so as to obtain the sulfur-substituted podophyllum derivative represented by a formula (V). Cell apoptosis test results of in-vitro BGC823, HepG2 and A549 tumor cell strains show that sulfur-substituted podophyllum derivative has good anti-tumor activity, high safety and low toxicity and can be prepared into clinical anticancer medicines.

The invention discloses a 4-amino oxadiazole epipodophyllotoxin derivative and a preparation method and application thereof. The 4-amino oxadiazole epipodophyllotoxin derivative has a structure shown as a Formula (1), wherein R1 represents hydrogen or methyl, and R2 represents hydrogen, alkyl, aryl, heteroaryl or heteroaryl alkyl. The derivative is prepared according to the following steps of: firstly, subjecting podophyllotoxin serving as a raw material to azido reaction, reduction, addition and elimination to obtain isothiocyanate epipodophyllotoxin; secondly, reacting an isothiocyanate epipodophyllotoxin intermediate with a hydrazide compound to obtain a thiosemicarbazide derivative; and finally, subjecting to cyclization, and thus obtaining a corresponding 4-amino oxadiazole derivative. The preparation method is simple and is easy to operate. Initial in-vitro screening tests show that the toxicity of the derivative on normal cells is obviously reduced, meanwhile, certain compounds have better anti-tumor activity, and high-efficiency and low-toxicity anti-tumor drugs can be expected to be prepared.

A chimeric toxin is disclosed comprising a peptide ligand specifically targeting neurons involved in pain processing; and a clostridial neurotoxin light chain, wherein the ligand is linked to the light chain. The methods of preparing such chimeric toxin and the method of using the chimeric toxin to regulate pain transmission are also disclosed.

The invention belongs to the technical field of chemical pharmacy, and particularly relates to podophyllotoxin derivatives and application of the podophyllotoxin derivatives in aspect of tumor suppression. Corresponding compound is obtained through a synthesis technology, and activity studies on antitumor in vitro show that the podophyllotoxin derivatives have strong inhibitory activity to tumor cell strains.

The invention relates to the technical field of biologic pharmacy, and discloses a method for removing pertussis component pilin 2/3 endotoxin. The method comprises the steps that after bordetella pertussis is fermented and cultured, thalli are centrifugally collected, thalli are extracted through a urea phosphate buffer solution, a supernate is centrifugally collected, and PEG-8000 and ammonium sulfate are used for performing precipitation; precipitates are extracted by the phosphate buffer solution, then, a supernate is centrifugally collected, a Q-Sepharose chromatographic column is adoptedfor processing, and a phosphate buffer solution containing sodium chloride is adopted for eluting the Fim 2/3 component. By combining PEG8000 precipitating, ammonia sulfate precipitating and Q-Sepharose chromatographic column processing are combined, endotoxin in pilin 2/3 is removed through repeated means, on the premise of not introducing allogenic materials, the effective ingredient Fim 2/3 biologic activity and recycling rate are kept, and meanwhile the endotoxin in Fim 2/3 can be removed to 10 EU/mg or lower.

A novel composition for regenerating a cartilage has been demanded, which can achieve a good effect of regenerating a hyaline cartilage that is a nearly normal cartilage without requiring the use of any transplanted cell. The present invention provides a composition for regenerating a cartilage, wherein (a) a monovalent metal salt of low endotoxin alginic acid and (b) SDF-1 are used in combination.

The invention discloses an otobain compound, a preparation method therefor and application thereof. The compound has a structure shown in formula I. The preparation method is that piperonal is protected by 1,3-propanedithiol, reacts with 2-(5H)-furanone, and is subjected to cyclizing, deprotection, reduction and acylation reaction synthesis to obtain the otobain compound. The otobain compound adopts the piperonal which is cheap and easy to get as the raw material, is obtained through a simple and easy method, has good anti-neoplasm activity, is lower toxicity to normal cells compared to podophyllotoxin medicine, and has less side effects.The otobain compound can be clinically applied in manners of oral taking, intravenous injection, intramuscular injection and the like. Formula I:(img file='DDA0000691317640000011.TIF' wi='431' he='627' /)

The invention discloses a pharmaceutical composition of acetolide acetate and its medical application. The pharmaceutical composition of acetolide acetate provided by the invention contains acetolide acetate and a kind of The obtained natural product compound (I) with a novel structure, alanorelin acetate and compound (I) acting alone can reduce the content of serum transaminase, bilirubin and urea nitrogen in animals with liver damage, alleviate jaundice and renal dysfunction, And can reduce plasma endotoxin content; when alanorelin acetate and compound (I) act in combination, the pharmacological effect is more obvious, can be developed into the medicine for the treatment of acute liver failure, has outstanding substantive characteristics compared with the prior art and significant progress.

The invention discloses a compound of a single sugar cluster and a heterozygous sugar cluster, which are shown in formula (I), wherein the definition of a substituent group in the compound of the formula (I) is disclosed in detail in the specification. In addition, the invention also discloses a preparation method and a pharmaceutical composition of the compound. The compound has adhesion resistance and a protecting function on endotoxic shock.

The invention belongs to the technical field of medicines, and relates to Biliatresone separated and purified from plants, as well as a preparation method, medicinal composition and application thereof. The Biliatresone further comprises cis-trans-isomer, enantiomer, diastereoisomer, raceme, solvate, hydrate or pharmaceutically acceptable salt and ester. Bioactivity experimental tests indicate that the compound can be used for remarkably inhibiting zebrafish larvae from gallbladder dysplasia, and prove that the compound Biliatresone has bioactivity, can be further used as biliary epithelia-philic medicines for studying biliary atresia inducing animal models.

The present invention discloses an anilino-substituted podophyllin derivative having antitumor activity, method for preparation thereof, and use thereof. By means of anilino reactions, the present invention introduces 4-chloro-3-methylaniline, 3-fluoro-4-methoxyaniline, 4,4′-diaminodiphenylmethane, o-anisidine, 4-chloro-2-aminoanisole, anthranilonitrile, 2,6-dichloro-4-aminophenol, N,N-dimethylamino meta-aniline, 2-ethyl-5-nitroaniline, 2 2′-diaminodiphenylsulfide, or 2-aminobenzotrifluoride into position 4 of the active C-ring of podophyllotoxin or 4′-demethylepipodophyllotoxin to obtain the aniline-substituted podophyllotoxin derivative shown in formula (V); by means of multi-pathway and multi-target effects on tumor cells, said derivative has significantly increased antitumor activity, and can be prepared as an antineoplastic drug and applied in clinical antitumor therapy.

The invention discloses a veterinary drug composition. The veterinary drug composition is prepared from the following raw materials, by weight, 400-500 parts of glucose oxidase, 200-300 parts of bacillus, 50-100 parts of cysteine, 50-75 parts of methionine, 100-150 parts of glutathione and 1-5 parts of selenium yeast. The invention also provides the preparing method and application of the composition. With coordinated components, the invented composition of veterinary drug plays a role of synergistic effect in the aspect of prevention against osomycosis and/or mycotoxin poisoning in livestocks, providing a new choose for feed additives and veterinary drugs.

The invention discloses a detection method for preparing a spiny platinum-coated gold nanorod chiral dimer for DNA damage and belongs to the technical field of analytical chemistry and the technical field of food security. The method comprises the steps of (1) synthesis of a gold nanorod; (2) synthesis of a spiny platinum-coated gold nanorod; (3) surface-oriented nucleic acid functionalization of the spiny platinum-coated gold nanorod; (4) establishment of a spiny platinum-coated gold nanorod chiral dimer; (5) pre-damage of biotoxin to a DNA; and (6) detection of the DNA damage by using the spiny platinum-coated gold nanorod chiral dimer. A plasma chiral spectroscopy signal can be successfully applied to the field of biosensing detection. The spiny platinum-coated gold nanorod chiral dimer assembled by using a nucleic acid generates a circular dichromatic spectrum signal of a visible light/near-infrared region, thereby being applied to detection of the DNA damage through biotoxin and metabolites thereof.

The invention discloses a series of new 4alpha-acyloxy-2'(2',6'),2alpha-polyhalogenated podophyllotoxin derivatives and a preparation method thereof. The chemical general formula of the series of 4alpha-acyloxy-2'(2',6'),2alpha-polyhalogenated podophyllotoxin derivatives is shown in the specification, wherein X is Cl, Y is H, or X and Y are Cl, or X is Br and Y is H. The preparation method comprises the following steps: performing E-cyclohalogenation, C-4 hydroxy protection, C-2alpha-chloro, and C-4 deprotection on podophyllotoxin used as a raw material so as to obtain 2'(2',6'),2alpha-polyhalogenated podophyllotoxin, and finally reacting DMAP/DCC or BF3.Et2O used as a esterification reagent C-4-OH with 11 carboxylic acids so as to obtain the 4alpha-acyloxy-2'(2',6'),2alpha-polyhalogenated podophyllotoxin derivatives, wherein the C-cycloacrylated product is produced in accompanying when the BF3.Et2O is used as the esterification reagent. The test shows that the 4alpha-acyloxy-2'(2',6'),2alpha-polyhalogenated podophyllotoxin derivatives have good insecticidal activity which is partially higher than that of the podophyllotoxin, wherein the insecticidal activities of a plurality of compounds are higher than that of commercial botanical pesticide toosendanin, and a botanical insecticide with high efficiency and low toxicity can be hopefully prepared from the 4alpha-acyloxy-2'(2',6'),2alpha-polyhalogenated podophyllotoxin derivatives.

Embodiments of the invention are directed to a composition comprising a recombinant protein in soluble form wherein said recombinant protein comprises a portion of the Clostridium difficile toxin B sequence that comprises an epitope for anti-toxin B antibody. Other embodiments of the invention are directed to the generation of antibodies using peptide fragments of C. difficile toxin B.

The invention discloses new application of prostaglandin compounds. The prostaglandin compounds are shown as a formula I and can be used for preparing medicaments for relieving and/or treating vivo toxin accumulation and/or improving skin conditions, wherein R1 is hydrogen atom, C1-C4 straight-chain or branched-chain alkyl, phenyl and any pharmaceutically acceptable salt such as sodium salt, potassium salt, ammonium salt and the like; 13th and 14th sites are carbon-carbon single bond or double bonds; and R2 and R3 express the same or different halogen atoms respectively.

The invention discloses application of long-chain neurotoxin (alpha-cobratoxin, alpha-CbTX) of cobra in preparation of a muscarine type M4 receptor activator. The neurotoxin has the function of reducing pain through activating M4 receptor-dependent T type calcium current, and the muscarine type M4 receptor activator containing the long-chain neurotoxin of the cobra can be established to perform the application of clinical analgesia.