33 results about "Enzymes levels" patented technology

The invention discloses a coelenterazine analog and a preparing method and application thereof. The coelenterazine analog has the general structure formula (I) shown in the description, wherein R1, R2 and R3 in the formula are different substituents. According to application of the compound as a bioluminescence substrate, the existence and quantity (including the enzyme level, the cell level and the animal level) of coelenterazine luciferase can be detected with bioluminescence, and the in vitro, cell and in vivo distribution imaging of luciferase can be detected; the compound can serve as a report signal to detect the pharmacologic action and the toxic effect of medicine on the enzyme level, the cell level and the animal level under the existence of luciferase.

Methods are provided for controlling metabolic flux rate in a cell-free system comprising a complex set of enzymes, to produce a desired product of a pathway of interest. In the methods of the invention, measurements of metabolic performance parameters are taken by continuous monitoring or intermittent monitoring. Based on the metabolic performance parameters, the system is modified by one or more steps comprising: (i) altering enzyme levels in the cell-free system; (ii) altering feed rate of a substrate that controls redox flux or carbon flux to the cell-free system; (iii) altering O₂ addition to the cell-free system; (iv) controlling efficiency of electron transport system by altering leakage across a membrane; wherein enzymes present in the pathway of interest catalyze production of a desired product.

The invention relates to an amide derivative and a purpose thereof. The invention discloses an N-(4-substiguted aminoacyl phenyl)-5-substited furan-2-formamide compound and tests the activity of the compound for inhibiting falcipain-2 in experiment of enzyme level in vitro, and the result indicates that the compound has strong inhibitory activity to falcipain- 2. Therefore, the N-(4-substiguted aminoacyl phenyl)-5-substited furan-2-formamide compound provided in the invention can act as cysteine protease (falcipain-2) inhibitor in food vacuole of plasmodium to stop further proliferation of plasmodium in a host.

The invention relates to a substituted benzene alkyl amides compound, i.e. 4-(N-substituted amino-sulfonyl) benzene alkyl amide compound and a usage thereof. The inventor makes comprehensive use of CADD and SPR experiment based on Biacore, finds the substituted benzene alkyl amides compound and applies a reasonable drug design method to modify the structure of the substituted benzene alkyl amides compound so as to finally obtain the 4-(N-substituted amino-sulfonyl) benzene alkyl amide compound; after tests, the obtained 4-(N-substituted amino-sulfonyl) benzene alkyl amide compound inhibits the activity of falcipain-2 in in-vitro enzyme level experimental tests; and the result shows that the 4-(N-substituted amino-sulfonyl) benzene alkyl amide compound has strong falcipain-2 activity inhibiting capability and can be used for preparing medicaments for treating malaria caused by plasmodium.

The invention discloses a naphthenic-base mono substituted amino fluorescein compound as well as a preparation method and application thereof. The naphthenic-base mono substituted amino fluorescein compound has a structural general formula (described in the specification) or a free form thereof, wherein n is 0-9, and m is 1-9; when n is equal to m, R is mono substituted groups such as a hydrogen group, methyl, ethyl, propyl and halogen; and when n is not equal to m, R is the hydrogen group. The naphthenic-base mono substituted amino fluorescein compound can be used for detecting distribution and imaging of luciferase in vitro, cells and vivo by detecting the presence and quantity (including enzyme level, cellular level and animal level) of the luciferase by virtue of bioluminescence, can be also used for detecting distribution and imaging of ATP in vitro, cells and vivo by detecting the presence and quantity (including enzyme level, cellular level and animal level) of ATP and can be used for detecting pharmacological action of a medicine in enzyme level, cellular level and animal level as a report signal in the presence of luciferase, ATP and Mg<2+>.

The invention relates to an in-vitro model construction method for predicting toxicity of a compound upon fatty liver diseases. The method comprises the following steps: culturing different liver cells under a two-dimensional or three-dimensional condition, and culturing a fat converted liver cell in-vitro culture model by using a culture medium with a free fatty acid component. By adopting the in-vitro culture system, a growth micro environment in a liver cell can be simulated, the morphology and the function of the liver cell can be maintained for a long time, a cytochrome enzyme level is approximate to that in vivo, and the model has typical characteristics of fat converted liver cells, is capable of replacing fatty liver animal models, and achieving toxicology metabolism detection or pharmacodynamics study on a compound in long-term action on fat converted liver tissue in vitro.

The invention relates to a Chinese composition and a preparation method thereof. The Chinese composition is prepared from the following components in part by weight: 100 to 400 parts of bupleurum, 50 to 300 parts of lucid ganoderma, 50 to 400 parts of root of red-rooted salvia and 100 to 450 parts of Chinese magnoliavine fruit. The Chinese composition has the effects of clearing away heat and toxic material, promoting urination and expelling toxin, protecting liver and decreasing enzyme level, promoting blood circulation and removing blood stasis, tonifying spleen and removing dampness through diuresis, recovering normal liver function, completely clearing viruses and the like.

The invention discloses a compound A8 used as a histone transmethylase NSD3 activity inhibitor and a medicine purpose thereof. The compound A8 has a chemical structure shown as a formula I in description, and the chemical name is 6-amino-9-(2-(p-tolyloxy)ethyl)-9H-purine-8-thiol. The medicine purpose refers to the preparation of anti-tumor medicine by using at least one of the compound A8 or hydrates, pharmaceutically acceptable salt, dynamic isomers, stereoisomers and precursor compounds as active ingredients. Experiments show that the compound A8 can effectively inhibit the NSD3 enzyme activity; the enzyme level IC50 value is 0.69+/-0.06mumol/L; the growth and proliferation of a non-small-cell lung cancer cell line H460 can be obviously inhibited. The compound has the effect of inhibiting the tumor cell proliferation, is hopeful to being used as an active ingredient for preparing the anti-tumor medicine and has medicine prospects.

The invention provides C-6 site modified NanoLuc type analogues and a preparation method and application thereof. The C-6 site modified NanoLuc type analogues have a structure as shown in a formula Iwhich is described in the specification. In the formula I, R1 is selected from a group consisting of a 4-fluorophenyl group, a 4-chlorphenyl group, a 4-bromophenyl group, a 3-fluoro-4-aminophenyl group, a thienyl group, a furyl group, a 5-methylfuryl group, a naphth-2-yl group, a benzofuryl group, a 4-methylphenyl group, a 3,5-dimethylphenyl group, a 4-hydroxymethylphenyl group, a 4-methoxyphenylgroup and a 4-mercaptophenyl group. The analogues can be used as a bioluminescent substrate for researching protein-protein and protein-ligand interactions, monitoring protein stability and bioluminescence resonance energy transfer and the like. The invention provides application of the analogues to in-vitro, cellular and in-vivo distribution imaging under the action of NanoLuc luciferase in virtue of bioluminescence and application of the analogues as a report signal to detect the pharmacological action and toxic action of a drug at an enzyme level, a cellular level and an animal level in thepresence of NanoLuc luciferase.

The invention provides a medicine for inhibiting Marek's disease virus replication, which comprises a deubiquitinating enzyme UL36 inhibitor and a medicine for preventing or resisting Marek's disease. The deubiquitinating enzyme UL36 inhibitor DUBs-IN-1 and the derivative thereof are screened out for the first time through an enzyme activity experiment for inhibiting virus encoding, a drug toxicity experiment on a CEF cell level, a virus CPE inhibition experiment and a chicken Marek's disease model experiment, the activity of UL36 can be inhibited on an enzyme level, replication of Marek's disease viruses can be inhibited on a cell level, and the Marek's disease tumor growth and visceral hemorrhage can be inhibited on the animal level, has the advantages of extremely strong effect and small dosage, and can be widely applied to production practice of Marek's disease prevention in poultry industry as an anti-MD drug.

The present invention provides nucleic acid and amino acid sequences of acetyl CoA synthetase (ACS), plastidic pyruvate dehydrogenase (pPDH), ATP citrate lyase (ACL), Arabidopsis pyruvate decarboxylase (PDC), and Arabidopsis aldehyde dehydrogenase (ALDH), specifically ALDH-2 and ALDH-4. The present invention also provides a recombinant vector comprising a nucleic acid sequence encoding one of the aforementioned enzymes, an antisense sequence thereto or a ribozyme therefor, a cell transformed with such a vector, antibodies to the enzymes, a plant cell, a plant tissue, a plant organ or a plant in which the level of an enzyme has been altered, and a method of producing such a plant cell, plant tissue, plant organ or plant. Desirably, alteration of the level of enzyme results in an alteration of the level of acetyl CoA in the plant cell, plant tissue, plant organ or plant. In addition, the present invention provides a recombinant vector comprising an antisense sequence of a nucleic acid sequence encoding pyruvate decarboxylase (PDC), the E1alpha subunit of pPDH, the E1beta subunit of pPDH, the E2 subunit of pPDH, mitochondrial pyruvate dehydrogenase (mtPDH) or aldehyde dehydrogenase (ALDH) or a ribozyme that can cleave an RNA molecule encoding PDC, E1alpha pPDH, E1beta pPDH, E2 pPDH, mtPDH or ALDH.

The invention relates to an application of flavonoid products in preparation of a drug for treating cancer and an inhibitor. The flavonoid products are myricetin, a dihydroxylation form of myricetin or a dihydroxylation form of quercetin, and an Mg<2+> preparation is used during application. The bioactive range of natural flavonoid on the enzyme level is extended, and a road is paved for developing flavonoid assisted targeted cancer treatment. Besides, great research space exists in researching the function of myricetin on 5'-ribozyme family and combination of myricetin with other drugs to target DDR (DNA damage response) for cancer treatment.

The invention discloses a coelenterazine-h-based deuterated compound and a preparation method and application thereof, the chemical structural formula is as follows, wherein R1 is phenyl or deuterated phenyl, R2 is hydrogen or deuterium, R3 is hydrogen or deuterium, R4 is hydrogen or deuterium, R5 is hydrogen or deuterium, R6 is hydrogen or deuterium, and at least one of R1-R6 is a deuterated group. According to the application of the deuterated compound as a bioluminescent substrate, the in-vivo and in-vitro distribution condition of luciferase can be monitored. The bioluminescence intensity of the deuterated substance of coelenterazine-h is superior to that ofthe coelenterazine-h at the enzyme level, the cell level and the animal level . Meanwhile, the preparation method of the deuterated compound of coelenterazine-h, provided by the invention, is simple, classical in reaction steps, high in operability and low in cost, and has a good practical value.

The invention discloses an in-vitro composition method for evaluating a hair growing/hair loss prevention effect. The in-vitro composition method comprises the following steps: S1, analyzing a 5alphareductase inhibition level; S2, carrying out cell effect analysis: analyzing cytotoxicity, a cell proliferation capability and an anti-oxidization capability; S3, analyzing angiogenesis; S4, evaluating a result and predicating. The in-vitro composition method disclosed by the invention is used for screening functionalized cosmetic raw materials through various biology methods and through a combined enzyme level test, a cell test and a tissue level test; a testing system is simple and low in price; special equipment is not needed; a detection is rapid, flexible and universal. The in-vitro composition method can be used for qualitatively and evaluating effects of hair growing raw materials; the method disclosed by the invention also can be used for replacing live animals and human volunteersand is used for screening and detecting the toxicity and effects of the hair growing and hair loss prevention raw materials.

The invention discloses a cydonia oblonga-ocimum basilicum total flavonoid composition and application thereof in atherosclerosis. The cydonia oblonga-ocimum basilicum total flavonoid composition comprises the following components in parts by weight: 1-3 parts of cydonia oblonga total flavonoid and 1-3 parts of ocimum basilicum total flavonoid. A test of the cydonia oblonga-ocimum basilicum totalflavonoid composition for atherosclerotic rats shows that: the cydonia oblonga-ocimum basilicum total flavonoid composition can effectively reduce blood fat and blood vessel injury factor level, increase antioxidant enzyme level, improve organism oxidation resistance, reduce oxide formation, increase blood vessel protection factor level, effectively protect blood vessel, improve liver function andprevent lipid metabolism disorder. The synergistic effect of the cydonia oblonga-ocimum basilicum total flavonoid composition improves the curative effect on atherosclerosis, and further provides a theoretical basis for preventing and treating atherosclerosis.

A C1 compound as histone methyltransferase NSD3 activity inhibitor and its pharmaceutical use are disclose. C1 has that chemical structure represent by formula I chemical name: 6-Amino-9-(2-(o-Tolyloxy) ethyl)-9H-Purine-8-Thiol; At least one of that compound C1 or its hydrate, pharmaceutically acceptable salt, tautomers, stereoisomer. And precursor compounds are used as an active ingredient in thepreparation of an anti-tumor drug. Experiments show that the compound C1 of the invention can effectively inhibit the NSD3 enzyme activity. And the IC50 value of the enzyme level is 14.63 +- 3. 85 [mu]mol/L. And the compound C1 has good NSD3 enzyme inhibition effect. As an effective inhibitor of an important tumor target NSD3, the compound of the invention is expected to be used as an active ingredient for preparing an antineoplastic drug. And has a pharmaceutical prospect.

The present invention provides a pediatric myocarditis treating formula, wherein the components comprise, by weight, 10 g of honeysuckle, 10 g of raw milkvetch root, 6 g of cyrtomium fortunei, 6 g of atractylodes macrocephala, 10 g of saposhnikovia divaricata, 6 g of atractylodes lancea, 10 g of agastache rugosa, and 10 g of adenophora stricta miq. According to the present invention, the pediatric myocarditis treating formula is suitable for treatment of a variety of pediatric myocarditis caused by viruses, the effect is good, the cardiac muscle of the pediatric myocarditis patients can be nourished and the cardiac function can be improved through the formula, the pediatric myocarditis pathological change development can be effectively prevented, the myocardial enzyme level of the pediatric patients can be significantly improved, and various indexes of the body can be effectively promoted to achieve the normal levels.

A B6 compound as histone methyltransferase NSD3 activity inhibitor and its pharmaceutical use are disclosed. B6 has a chemical structure represented by formula I. Chemical name: 6-Amino-9-(2-(4-Isopropoxyphenoxy) ethyl)-9H-Purine-8-Thiol; At least one of that compound B6 or its hydrate, pharmaceutically acceptable salt, tautomer, stereoisomer. And precursor compound is used as an active ingredientfor preparing an antineoplastic drug. Experiments show that the compound B6 of the invention can effectively inhibit the NSD3 enzyme activity. And the IC50 value of the enzyme level is 0.82 +- 0.17 [mu]mol/L, and significantly inhibited the growth and proliferation of non-small cell lung cancer cell line H460. The compound of the invention has the effect of inhibiting tumor cell proliferation, and is expected to be used as an active ingredient for preparing an anti-tumor drug. And has pharmaceutical prospect.