247results about How to "Has inhibitory activity" patented technology

The invention provides a bufogenin derivative of the following general formula I or a pharmaceutically-acceptable salt, a preparation method thereof, a pharmaceutical composition containing the derivative, and applications of the bufogenin derivative and the pharmaceutical composition. The bufogenin derivative has inhibitory activity on various human tumor cell lines and can be used as an anticancer drug against malignant tumors.

The invention relates to a new process for preparing animal protolysate containing high calcium with complex enzyme hydrolysized chicken bone mud, which is characterized in that it comprises the following steps: disintegrating chicken bone ultramicroly to make bone mud, formulating bone mud suspending solution, heating under 80-100 Deg .C for 20-30 minutes, cooling to temperature proper for enzyme reaction, regulating pH value, adding complex enzyme for reacting for a certain time, then heating to 85-90 Deg. C and keeping for 10-20 minutes for sterilization, and getting product which is concentration of sepia, semitransparent or stramineous powder. The invention resolves problems of odour of raw material and bitter caused by enzymolysis, the product most of which is short peptide and free amino acid can be adsorbed easily by human body which increase comprehensive utilization ratio of product, and the product possess certain action for inhibiting angiotonin zymose.

The invention relates to a bufalin derivative having a structure represented as a general formula I, wherein R is selected from one of the following structure groups as shown in the specification, or pharmaceutically acceptable salt, as well as a preparation method, a pharmaceutical composition and application of the derivative. The bufalin derivative has an activity on inhibiting tumor cell lines, and can be used as a medicine for treating malignant tumors.

The invention relates to a 5-substituted methylpyrrolidine-2, 4-diketone compound and the use thereof. The structure of the 5-substituted methylpyrrolidine-2, 4-diketone compound is shown in a general formula (I), wherein R1, R2 and R3 are defined as the specification. The compound with the structure shown in the general formula (I) belongs to the technical field of applying compound to pesticide and can be used for preparing phytocide.

The invention relates to fields of insecticides and fungal inhibitors, and concretely relates to an alga bromosesquiterpene compound, a preparation thereof and an application thereof. The concrete structural formula of the compound is represented by formula (I). The preparation method of the compound comprises the following steps: drying and crushing red alga Laurencia composita, and extracting with an organic solvent to obtain crude extracts; and carrying out silica gel column chromatography on the crude extracts, carrying out gradient elution, and separating and purifying components obtained through gradient elution with an eluent volume ratio of 15-10:1 to obtain the target compound (I). Results of insecticidal activity experiments of the bromosesquiterpene compound obtained in the invention show that the lethality of 100mug / ml of the compound to artemia is 87.7%, the median lethal concentration is 37.0mug / ml, and the compound simultaneously has a good antifungal activity.

The invention relates to a lactobacillus and in particular relates to a low-temperature resistant lactobacillus with ACE (angiotensin converting enzyme) inhibitory activity. The low-temperature resistant lactobacillus with the ACE inhibitory activity is lactobacillus plantarum I1 which is preserved in the China general microbiological culture collection center of which the preservation address is No.3, No1. yard, Beichen west road, Chaoyang District of Beijing, the preservation data is September 18th, 2012, and the preservation number is CGMCC No.6575; the lactobacillus plantarum I1 has the ACE inhibitory rate being 66%, can tolerate 6% of NaCl and 100mg / kg of nitrite, and can fast generate acid; the growing temperature of the lactobacillus plantarum I1 is 4-40 DEG C, and is suitable for low-temperature fermentation; and the low-temperature resistant lactobacillus has obvious protease activity and lipase activity, can not generate mucus, has an obvious antibacterial effect on staphylococcus aureus and colon bacillus, and can be used as a meat product leavening agent strain under a low-temperature condition.

The invention relates to a technology for preparing thermally stable slowly digestible starch, belonging to the technical field of preparation of slowly digestible starch in food processing. Ordinary starch is quickly digestible starch, and a thermally stable slowly digestible starch product can be obtained through the following processes (enzymolysis, tea polyphenol adding and spray drying): adding 20-50g of water to 1kg of starch raw material to blend into a 2-5 percent starch suspension, adding pullulanase (the addition is 1-5U / g) at 50 DEG C with a pH value of 5.0, and carrying out enzymolysis for 4-10h; adding 20-80g of tea polyphenol, mixing, heating to 100 DEG C for enzyme inactivating for 125n and cooling to room temperature; homogenizing by a high-voltage homogenizer under 20MPa, and drying into powder by using a spray dryer (the air inlet temperature is 160-200 DEG C, and the air outlet temperature is 80-100 DEG C); and packaging to obtain the slowly digestible starch product.

The invention relates to 4'-amino-4'-dehydroxyl-oleandrin and 4'-amino-4'-dehydroxyl-odoroside A and use thereof. The invention provides a compound represented by the following general formula I shown in the description or pharmaceutically acceptable salts thereof, a preparation method therefor, a pharmaceutical composition containing the compound represented by the following general formula I shown in the description or pharmaceutically acceptable salts thereof and use thereof. The compound has inhibitory activity to the propagation of humanized tumor cell lines and can serve as a drug for treating malignant tumors.

The invention discloses pyrazolo[3,4-d]pyrimidone compounds and application thereof in preparation of a phosphodiesterase IX inhibitor. The structure of the compounds is shown as a formula (1); in the formula, when R' is 2-chlorophenyl, R refers to phenyl, substituted phenyl, benzyl, substituted benzyl, 3-methylpyridine, 1-phenylethyl, diphenylmethyl or CHCH3CONHR1, wherein R1 refers to phenyl ormethyl, methoxyl, ethoxyl, isopropoxy, methylthio, NHCOCH3 or NCH3CH3 substituted phenyl; when R' is phenyl, R refers to CHCH3CONHR2, wherein R2 refers to methoxyl or ethoxyl substituted phenyl; and when R' is methyl, R refers to 4-methoxy-benzyl, diphenylmethyl or N-(2-amino-cyclohexyl)-4-methoxy-benzenesulfonamide. The pyrazolo[3,4-d]pyrimidone compounds have activity of inhibiting phosphodiesterase IX, can serve as the phosphodiesterase IX inhibitor, can be used for preparing the phosphodiesterase IX inhibitor, and have wide application prospect. The compounds are shown as the formula (1).

The invention relates to hydroxyl phosphate amino acid ester derivatives of Brefeldin A, a preparation method thereof, and an application thereof. The invention relates to a fungal metabolite. The derivatives comprises (+)-Brefeldin A-4,7-dihydroxyl phosphate amino acid ester, (+)-Brefeldin A-4-hydroxyl phosphate amino acid ester, and (+)-Brefeldin A-7-hydroxyl phosphate amino acid ester. According to the invention, Brefeldin A hydroxyl phosphate amino acid ester derivatives with high bioactivity, good dissolubility, and good bioavailability are synthesized. The derivatives are simple to prepare, and the cost is low. The derivatives are advantaged in novel structure, relatively stable structure, and substantial inhibitive activities against tumor cell proliferation. Compared with the original medicine (+)-Brefeldin A, the derivatives are advantaged in good dissolubility and long half-life period. The Brefeldin A hydroxyl phosphate amino acid ester derivatives can be applied in the preparations of anticancer medicines.

A compound of the formula (I) wherein Z<4>, Z<5> and Z<9> each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; R is a group of the formula (II) (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.

The invention relates to novel benzanthracene cyclic compounds and a preparation method and use thereof. The benzanthracene cyclic compounds have the structure shown in a general formula I or II. The compounds can be used as topoisomerase inhibitors for preparing anti-tumor, cell growth-resistant, antibacterial and antimalarial medicaments. The invention also relates to a method for preparing the compounds. In the formula I, C1' and C3' have an S structure simultaneously, and in the formula II, C1' and C3' have an R structure simultaneously.

A streptomyces strain, and anti-kidney-cancer applications of piericidin metabolites thereof are disclosed. The streptomyces strain is streptomyces sp.HBERC-58855, and is deposited in the China Center for Type Culture Collection, in Wuhan University, Wuhan, China on April 20, 2017. The accession number of the streptomyces sp.HBERC-58855 is CCTCC NO:M 2017186. The 16sRNA nucleotide sequence of the streptomyces sp.HBERC-58855 is shown as SEQ ID NO:1. Piericidin compounds including piericidin A, piericidin A2, piericidin C2, IT-143-A, IT-143-B and piericidin s3a are extracted from the streptomyces sp.HBERC-58855 through fermentation for the first time, and are applied in preparation of anti-kidney-cancer medicines. Candidate compounds are provided for development of novel anti-kidney-cancer medicines. The streptomyces and the piericidin compounds are of great significance for marine microorganism medicine resource development.

The invention discloses a use of 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives in preparation of a drug for prevention or treatment on cerebral hemorrhage. Through a self-created computer-assisted drug molecule design program and virtual screening, it is shown that the 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound and its derivatives have a ROCK1 protein inhibitory activity and can be used for treating cerebral hemorrhage. Through further biological activity detection of the screened 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound, it is shown that the screened 4,7-dihydrotetrazyl[1,5-alpha]pyrimidine compound has an obvious ROCK1 protein inhibitory activity and has good prevention and treatment effects in an atorvastatin-induced zebra fish cerebral hemorrhage model.

The invention relates to the technical field of a medicine, and particularly relates to two diterpenoid compounds libertellenone G and libertellenone H with antineoplastic activities extracted from secondary metabolite of arctic curvularia molecular genus. The chemical structural formulas are shown in the specification. The invention also provides a preparation method of the diterpenoid compounds, and application of the diterpenoid compounds in preparation of an antitumor drug.

The invention provides an application of compounds Pyrrocidines in preparation of an anti-tuberculosis drug, namely, an application of the compounds Pyrrocidines, derivatives of the compound Pyrrocidines or pharmaceutically acceptable salts of the compounds Pyrrocidines as tyrosine phosphatase inhibitors or in preparation of the tyrosine phosphatase inhibitors. The compounds 19-O-methyl-pyrrrocidine B and pyrrrocidine B have inhibitory activity on mycobacterium tuberculosis tyrosine phosphatase B, and IC50 of the compounds is 3.9 mu M and 75.5 mu M respectively. The compounds can effectively inhibit dephosphorylation activity of the mycobacterium tuberculosis tyrosine phosphatase B and has the clinical application potential for tuberculosis treatment; besides, the compounds Pyrrocidines are natural-metabolism active micro-molecular products separated from microorganisms and can be produced through chemical synthesis and large-scale fermentation separation, the sources are abundant, the production cost is low, and the possibility of medicine preparation is high.

The invention discloses an application of radix acanthopanacis trifoliate extract in inhibiting alpha-glucosidase. The radix acanthopanacis trifoliate extract is extracted and concentrated by ethanol and then extracted respectively by petroleum ether, ethylacetate and normal butanol. The radix acanthopanacis trifoliate extract is identified to have 9 terpenoids. The invention also discloses an alpha-glucosidase inhibitor, and the alpha-glucosidase inhibitor comprises radix acanthopanacis trifoliate extract as well as one or more additives acceptable on the medicine. The experiment shows that the extract of radix acanthopanacis trifoliate leaves, stalks and roots has inhibitory activity for the alpha-glucosidase; in 9 terpenoids of the radix acanthopanacis trifoliate extract, the compound 6 has best activity for inhibiting the alpha-glucosidase, which is far higher than a reference product acarbose.

The invention discloses a pyrrolidine[3,4-d]pyrimidine derivative and a preparation method and an application thereof. The pyrrolidine[3,4-d]pyrimidine derivative is an inhibitor of a type I insulin-like growth factor receptor (IGF-1R), and has a good IGF-1R inhibiting function and a good cancer cell proliferation inhibiting function, so that the pyrrolidine[3,4-d]pyrimidine derivative can be taken as a therapeutic agent for treating tumors and relevant diseases.

The invention relates to 2-(thiazol-2-yl)imino-5-(benzylidene)thiazolidin-4-one shown as formulas I, II, III or IV or a mixture thereof, wherein R1 is selected from hydrogen, C1-C2 alkyl or C3-C4 straight-chain or branched chain alkyl, R2 is selected from hydrogen, C1-C2 alkyl or C3-C4 straight-chain or branched chain alkyl, X1-X5 are selected from hydrogen, C1-C2 alkyl, C3-C4 straight-chain or branched chain alkyl, nitro, amino or NHCOR, and R is selected from hydrogen, C1-C2 alkyl or C3-C4 straight-chain or branched chain alkyl. Applications of the 2-(thiazol-2-yl)imino-5-benzal thiazoline-4-one or the mixture thereof in preparation of neuraminidase inhibitors are also disclosed.

The invention relates to the technical field of biomedicine, in particular relates to a royal jelly polypeptide and application thereof. According to the invention, intestinal tract enzyme is extracted from a queen bee larva in vivo, and an in vivo enzymolysis environment of queen bee is simulated to carry out enzymolysis on royal jelly so as to obtain 1-3kDa of royal jelly polypeptide. The royal jelly polypeptide can be used for preparing an A beta inhibitor.

A strain of low temperature tolerant lactic acid bacteria with ACE inhibitory activity, which involves a strain of lactic acid bacteria. The low-temperature resistant lactic acid bacterium with ACE inhibitory activity is Lactobacillus plantarum I1, which is preserved in the General Microbiology Center of China Microbiological Culture Collection Management Committee. The preservation address is No. 3, No. 1 Beichen West Road, Chaoyang District, Beijing, and the preservation date is 2012 On September 18, 2009, the deposit number was CGMCCNo.6575. Bacterial strain I1 in the present invention has an ACE inhibition rate of 66%, can tolerate 6% NaCl and 100mg / kg of nitrite and can rapidly produce acid; its growth temperature is 4-40°C, and is suitable for low-temperature fermentation; It has significant protease activity, lipase activity, does not produce mucus, has obvious antibacterial effect on Staphylococcus aureus and Escherichia coli, and can be used as a starter strain for meat products under low temperature conditions.

An anticancer 17-hydroxy-steroid lactone medicine for treating lung cancer, breast cancer, liver cancer, leukemia, etc is disclosed. Its advantages are simple preparing process and high suppression activity to A-549, MCF-7, BEL-7402 and P388.

The invention relates to a gallbladder wood leaf composition containing strictosamide and a preparation thereof. The gallbladder wood leaf composition containing the strictosamide is characterized in that the composition is applied in the preparation of medicament for clearing heat and eliminating phlegm and relieving cough and asthma, and or is applied in the preparation of medicines used for treating expectoration, cough with dyspnea and irritability asthma; the composition is composed of alkaloid and flavonoid extracted from gallbladder wood leaf through combination, and the alkaloid contains strictosamide, 10-hydroxy-strictosamide and short snakeroot glucoside; and the flavonoid contains kaempferol-3-O-rutinoside and rutin. The invention also discloses a preparation of the composition. The gallbladder wood leaf composition provided by the invention has the advantages that the active ingredient is definite, and the gallbladder wood leaf composition has notable curative effects.

A pyrimidone derivative represented by formula (I) or a salt thereof: wherein: Y represents two hydrogen atoms, a sulphur atom, an oxygen atom; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted by a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R3 represents a phenyl-group, a phenyl-CH2- group, a C1-6 alkyl-O-C(O)- group, a phenyl-C(O)- group, a 5-10 membered heterocyclic group, a phenyl-CH2-O-C(O)- group, a -C(O)-5-10 membered heterocyclic group, these groups being optionnally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkoxy group, a C1-6 alkylsulfonyl group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-12 dialkylamino-group, an acetoxy group, an aminosulfonyl group; R4 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1-6 alkyl group; m represents 0 to 2, in the form of a free base or of an addition salt with an acid.

The invention relates to bromophenol amino thiourea compounds (I-IV), and compositions and applications thereof, and also relates to a preparation method of the compounds. The chemical structure formula of the compounds is represented in the description. In the chemical structural formula, R1, R2, R3, R4, R5 and R6 are one or two of H, Br, OH, and OCH3. For the compound (I), R1 and R2 are Br; R3 and R4 are OCH3; and R5 and R6 are H. For the compound (II), R1 R2, and R5 are Br; R3 and R4 are OCH3; and R6 is H. For the compound (III), R1 and R2 are Br; R3 and R4 are OH; R5 is H; and R6 is phenyl. For the compound (IV), R1 and R2 are Br; R3 and R4 are OH; and R5 and R5 are H. The invention also relates to a composition containing at least one compound mentioned above or salts formed by a physiologically acceptable inorganic acid / organic acid and the compounds. The invention further relates to a dosage form of the composition, and the dosage form can be tablet, capsule, injection solution, suppository, patch, powder, suspension, and the like.

The present invention relates to 4-aminopyrazolo[3,4-d]pyrimidinylazabicyclo derivatives and pharmaceutical compositions containing the same, wherein the 4-aminopyrazolo[3,4-d]pyrimidinylazabicyclo derivatives and pharmaceutical compositions containing them not only have BTK inhibitory activity but also has remarkably high selectivity for the inhibitory activity of BTK vs. ITK, and thereby can beusefully used for the prevention or treatment of autoimmune diseases or cancers as BTK inhibitors.

The invention discloses an indole derivative with a 1, 2, 4-oxadiazole structure, which has antibacterial activity, a preparation method thereof and application thereof in preparation of antibacterial medicines, belonging to the technical field of medicine synthesis. The compound has the structure as shown in the general formula I, wherein when an A ring is an aromatic ring, R1 and R2 are ortho-positions, meta-positions and para-substituted groups on the aromatic ring; and when the an A ring is a non-aromatic ring, both the R1 and R2 are hydrogen. The compound disclosed by the invention is a novel alkaloid compound which is synthesized for the first time; and the compound has certain inhibitory activity on methicillin-resistant staphylococcus aureus (MRSA), which is found for the first time in synthetic compound in vitro model testing experiments, and therefore, the compound has potential application prospects in preparation of antibacterial medicines and treatment of bacterial infection.

The invention discloses a preparing method of a peroxy-ergosterol compound. The preparing method comprises the steps of smashing blocks of poria cocos, conducting reflux extraction 3-5 times, recycling an extracting solution to obtain extract, adding water to disperse the extract, and using ethyl acetate to conduct extraction 5-10 times to obtain a crude extract; using dynamic axial industrially-prepared chromatography to separate the crude extract to obtain a relatively pure product of peroxy-ergosterol; recrystallizing the obtained relatively pure product of peroxy-ergosterol to obtain peroxy-ergosterol of which the purity is larger than 98%. The invention further discloses application of the peroxy-ergosterol compound in preparing a drug for resisting herpes simple virus I. The multiplication of HSV-I in cells can be inhibited, the multiplication of the virus can be 100% inhibited when the concentration of peroxy-ergosterol is 40.12Mug / mL, and the selection index of peroxy-ergosterol in HSV-I is 7.5. As is shown, peroxy-ergosterol can be applied to preparing the drug for resisting the herpes simplex virus-I(HSV-I).

The present invention relates to a compound with 1,6-methylene-[10]-annulene basic skeleton. Said invention provides its structure formula. Said compound has the activity for inhibiting tumor cell, can be used for developing new anti-tumor medicine for curing cancer of lung, mammary cancer, liver cancer and leukemia, etc.