60 results about "Hep G2" patented technology

The invention relates to the medicine technical field, in particular to saponin compounds of Siraitic acid IIB and Siraitic acid IIC which are extracted and separated from fructus momordicae roots, a method for preparing the same and application thereof in an anti-tumor medicine. The molecular formulas of the two compounds are C40H60O14 and C41H62O15 respectively. By various modern spectral analysis, particularly the application of advanced two-dimensional nuclear magnetic resonance spectrum to comprehensive analysis, the chemical structures of the two compounds are determined. In vitro anti-tumor tests show that the compound Siraitic acid IIB can obviously inhibit lung cancer cells A-549 and liver cancer cells Hep-G2, and the compound Siraitic acid IIC can also obviously inhibit liver cancer cells Hep-G2. The invention provides lead compound for research on a new anti-tumor medicine, and has essential values in comprehensively developing and utilizing fructus momordicae resources.

The invention relates to a phenothiazine compound and a preparation method thereof. The invention further relates the application of the phenothiazine compound in anti-cancer drug preparation and anti-cancer drugs using the compound as the effective component. The phenothiazine compound has the advantages that the compound with broad-spectrum anti-cancer effect is obtained by modifying phenothiazine ternary interlink parent nucleuses, synthesizing method is simple, and high yield is achieved; the phenothiazine compound has certain restraining effect on human breast cancer cells line MCF-7 and human hepatoma cell line Hep-G2, and a new thought is provided to new drugs satisfying clinic requirements.

The invention relates to assessment and fermentation of marine actinomycete WBF9 that is used for producing anti-tumor compound and the separation and purification of the anti-tumor compound and the cytotoxic activity, and pertains to the microscopic organisms medicine filed. Bacterial strain WBF9, which is streptomyces griseorubens that is separated from the sea for the first time, is identified as one of the new bacterial strains of streptomyces griseorubens by traditionally classification and 16SrDNA genetic analysis. Culture medium (glucose: 1 percent, potato: 15 percent, yeast powder: 0.6 percent, calcium chloride: 0.12 percent and natural seawater, pH value 7.2) is applied by the bacterial strain for fermentation, and the compound extracted from the fermentation liquor, which has strong anti-tumor activity and identified as Norharmane by MS and NMR technique, is the first compound that is acquired by separating marine actinomycete. According to the MTT method, the compound is found to have cytotoxicity against four tumor cells: KB, BGC 803, Hep G2 and SGC 7901, and is a potential anti-tumor medicine.

The invention relates to a chlorin and artesunate compound with photosensitive and sound-sensitive activity as well as a preparation method and an application of the compound and belongs to the technical field of chemical medicines. The chlorin and artesunate compound with photosensitive and sound-sensitive activity has different degrees of inhibition effects on human hepatoma cells Hep G2 in in-vitro anti-tumor activity evaluation. The photoactivity and ultrasonic activity are both higher than that of chlorin e6 and artesunate which are used as positive controls. The compound can be used for preparing a photosensitizer and a sound-sensitive agent in photodynamic therapy and sonodynamic therapy methods for tumor therapy.

The invention relates to a hydrophilic chlorin photo-sensitive and sono-sensitive agent with long wavelength and a preparation method and an application thereof, and belongs to the field of chemical medicine. The compound is represented as the following formula described in the description. The compound of hydrophilic chlorin photo-sensitive and sono-sensitive agent with long wavelength has inhibition effects in different degrees on human liver cancer cell Hep G2 in anticancer activity evaluation in vitro. The ratio of photoactivity to dark activity and the ratio of sono-activity to dark activity are much higher than that of hemoporphyrinmonomethyl ether as a positive contrast. The hydrophilic chlorin photo-sensitive and sono-sensitive agent with long wavelength has advantages of low toxicity, high efficiency, treatment wavelength moving towards long wave region and the like. The compound in the invention can be used as an excellent photosensitizer and an excellent sonosensitizer for photodynamic and sonodynamic therapy of tumors.

The invention relates to a method for verifying and fermenting polar marine ray fungi AFN1007 producing antitumor active substance, and the research on the antitumor activity of the zymotic fluid thereof, belonging to the microbial medicine field. The strain AFN1007 is verified to be a novel kind of Streptomyces by the traditional classification and the analysis of 16S rDNA gene of the AFN1007. The compositions of a culture medium by percentage are: 1 percent of soybean flour, 1 percent of tragantine, 0.1 percent of KNO3, 0.05 percent of MgSO4, 0.001 percent of FeSO4, 0.05 percent of NaCl and natural seawater with a pH value between 7.2 and 7.4. The strain is fermented by using the culture medium. The MTT method shows that the zymotic fluid has strong antitumor action on four tumor cells of KB, BGC 803, Hep G2 and Hela and an antitumor compound with a novel structure is expected to be found in the zymotic fluid.

The invention relates to the fields of marine organism and medical technology, and provides an aaptamine alkaloid compound which is obtained by extraction, separation and purification from marine Aaptos aaptos produced in sea areas nearby the Paracel Islands, wherein the chemical structure of the alkaloid compound is as shown in the formula (I) (in the specification). In-vitro activity tests prove that the alkaloid compound has remarkable inhibitory activity on various different tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal carcinoma cells KB, human liver cancer cells Hep G2 and human colon cancer cells HT-29, and the alkaloid compound can be used for preparing anti-tumor medicines.

The invention discloses a compound Chinese actinidia root Chinese medicinal composition and a preparation method and application thereof, belonging to the technical field of traditional Chinese medicines. The Chinese medicinal composition is characterized by comprising the following traditional Chinese medicines in parts by weight: 40-80 parts of Chinese actinidia root, 20-40 parts of salvia chinensis, 20-40 parts of herba scutellariae barbatae, 20-40 parts of herba oldenlandiae and 20-40 parts of giant knotweed. The compound Chinese actinidia root Chinese medicinal composition has remarkable proliferation inhibition effects on various cancer cells such as a hepatoma cell line Hep-G2, a lung cancer cell line NCI-H460, a gastric cancer cell line MGC-803, a breast cancer cell line MCF-7, a colon cancer cell line HCT-116 and the like, and can be used for reducing physical and psychological pains of a cancer patient in the chemo-treatment process and solving the problems of difficult and expensive administration.

The invention discloses a vitamin D oxime derivative and a synthetic method and an application thereof. The method comprises the following steps: carrying out an oximation reaction between a compound I and hydroxylamine hydrochloride, thereby obtaining two A cyclic oxime derivatives such as (Z)-3-oxime vitamin D2 and (E)-3-oxime vitamin D2 of the vitamin D2 of different configurations; and enabling a compound 1.2 to react with methoxylamine hydrochloride, thereby obtaining two A cyclic oxime ether derivatives such as (Z)-3-methyl oxime ester vitamin D2 and (E)-3-methyl oxime ester vitamin D2 of the vitamin D2 of different configurations. The four vitamin D oxime derivatives have good effects of inhibiting human hepatoma cells Hep G2 and human breast cancer cells MCF-7 and have potential medicinal values.

This invention characterizes the selective apoptotic activity of specially prepared Alpha 2-HS glycoprotein and fragments thereof. Specifically, Alpha 2-HS glycoprotein which has been overloaded with zinc, as well as fragnents thereof, selectively induce apoptosis in HT-29 (colon cancer), LNCaP (prostate cancer) and Hep G2 (hepatoma) cells while having no effect on CCD 18 Co (normal colon) cells.

The invention discloses a 3-benzimidazole-6, 7-piperonylcyclo-2(1H)-quinolinone-zinc complex and a preparation method and application thereof. The preparation method of the complex mainly comprises: putting a compound shown in the formulas (II) and zinc chloride into an organic solvent, adjusting pH of the system to 5-7 and performing a coordination reaction process under heating or no heating toobtain a desired product. Compared with the common antitumor drug cisplatin, the complex has higher inhibitory activity to human liver cancer cells Hep G2 and lower toxicity to normal cells and is expected to be used for preparation of antitumor drugs. The structure of the complex is shown in the formula (I). The raw material for preparation of the complex is shown in the formulas (II).

The invention relates to the technical field of marine organisms and medicines and provides an aaptamine alkaloid compound extracted, separated and purified from a marine animal aaptos originating from surrounding waters of the Xisha Islands. The chemical structure of the aaptamine alkaloid compound is shown in a formula (I) as shown in the specification. In-vitro activity tests prove that the compound has obvious inhibitory activity on various tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal cancer cells KB, human liver cancers Hep G2, human colon cancer cells HT-29 and the like and can be used for preparing antitumor medicines.

The invention discloses a cobalt (II) complex of quinolinone derivative, and a synthesis method and application thereof. The synthesis method of the quinolinone cobalt complex comprises the following steps: weighing cobaltous chloride and a ligand 3-(1H-benzimidazolyl-2-yl)-6-methyl-2(1H)-quinolinone according to the stoichiometric proportion, dissolving in a polar solvent, and carrying out complexing reaction. The research of the in-vitro antitumor activity indicates that the complex has certain proliferation inhibition activity for human cervical cancer cell Hela229, human stomach cancer cell MGC-803, human liver cancer cell strain Hep G2 and BEL-7404 cell strain, and has the maximum activity for human liver cancer cell strain Hep G2. The quinolinone cobalt complex is disclosed as the following formula (I).

The invention relates to the fields of marine organism and medical technology, and provides an aaptamine alkaloid compound which is obtained by extraction, separation and purification from marine Aaptos aaptos produced in sea areas nearby the Paracel Islands, wherein the chemical structure of the alkaloid compound is as shown in the formula (I) (in the specification). In-vitro activity tests prove that the alkaloid compound has remarkable inhibitory activity on various different tumor cells such as human acute leukemic cells HL60, human chronic leukemic cells K562, human breast cancer cells MCF-7, human nasopharyngeal carcinoma cells KB, human liver cancer cells Hep G2 and human colon cancer cells HT-29, and the alkaloid compound can be used for preparing anti-tumor medicines.

The invention belongs to the field of organic chemical synthesis, and discloses cyclobutyl-1-enamine compounds, a preparation method thereof and application of the cyclobutyl-1-enamine compounds in antiviral and antitumor drugs. The compound has a structure of a general formula (I), and EWG is selected from alkyl or aryl substituted sulfonyl; r is selected from alkyl, alkoxy, halogen and nitryl. The preparation method comprises the following steps: heating an alkyne amide raw material to a molten state under thermal driving, and carrying out [2 + 2] cycloaddition reaction among molecules to obtain the polysubstituted cyclobutyl-1-enamine compound. The method has the advantages of easily available raw materials, simple steps, no catalyst, no solvent, high yield and the like. The compound has anti-SARS-CoV-2, 5637, Hela, SW480, Hep G2, A549 and MCF-7 activity, and has a good application prospect in the aspect of treating novel coronavirus, bladder cancer, cervical cancer, colon cancer, liver cancer, lung cancer and breast cancer. (I).

The invention relates to a new carbazole alkaloid represented by the formula (1), and also relates to a preparation method thereof and applications thereof. The alkaloid is characterized in that: crude extracts of an organic solvent of Antipathes dichotcma (Pallas) are extracted with ethyl acetate or chloroform after being suspended on water, an ethyl acetate layer or a chloroform layer is collected for carrying out the normal pressure silica gel column chromatography, the thin-layer chromatography is used for tracing and combination, and a chloroform-acetone solvent system in a volume ratio of 9:1 is used for elution, the collected Rf value is about 0.5 to 0.7, and compositions of ultraviolet absorption exist under the wavelength of 254nm of an ultraviolet lamp, a crude product is gained, and a pure product is obtained through the further purification. The carbazole alkaloid can be used for preparing medicines treating gastric cancers, liver cancers and anti-herpes simplex virus, and has the half inhibition concentration IC50 of 67.38mu g / mL and 73.65mu g / mL respectively to human gastric adenocarcinoma cell line SGC-7901 and human hepatoma cell Hep G2; and the IC50 value of the anti-herpes simplex HSV-I virus is 30.68mu g / mL.

The invention discloses a vitamin D2 glucoside analogue, a synthesis and an application thereof. According to the invention, vitamin D2 is taken as a raw material, vitamin D2 fragment alcohol is prepared through an oxidation reduction reaction, and then vitamin D2 and its fragment alcohol are respectively taken as raw materials for synthesizing structural analogues of a and b. The synthesis method has the advantage of easily available raw materials, mild reaction condition, simple operation, and high yield, the novel synthesized vitamin D2 glucoside analogue has good inhibition capability to human liver cancer cell Hep G2 and human breast cancer cell MCF-7, and has latent medicinal value.

The present invention relates to the application of saliva combined with lactobacillus in the preparation of a drug for treating obesity, and belongs to the field of biomedicine technology. The present invention provides the application of saliva combined with lactobacillus XA-1416 in the preparation of a drug for preventing and / or treating obesity, or preventing and / or treating obesity-related diseases. This strain can inhibit the weight gain of mice with obesity model induced by high-fat diet, reduce the blood lipid level of mice with obesity model induced by high-fat diet, improve the liver damage index of mice with obesity model induced by high-fat diet, reduce the area of ​​white fat cells in mice with obesity model induced by high-fat diet, promote the conversion of intestinal conjugated bile acid to free bile acid in mice with obesity model induced by high-fat diet, increase the level of intestinal FXR antagonist in mice with obesity model induced by high-fat diet, improve the intestinal flora imbalance of mice with obesity model induced by high-fat diet, inhibit fat accumulation in Hep G2 model, and inhibit differentiation into adipocytes in 3T3-L1 model.

The invention provides a method for extracting an antineoplastic active component from Armillaria luteo-virens. The method comprises the following steps: grinding Armillaria luteo-virens fruiting body into a powder and extracting with ethyl acetate; fetching a supernatant and carrying out one-dimension liquid phase separation: adopting a Silica normal-phase silica gel column and binary organic phases including A phase n-hexane and B phase ethanol, and carrying out gradient elution with concentration of the B phase being 0-75%; collecting 10-14 min eluant and carrying out two-dimension liquid phase separation by the elution mode of isocratic elution with concentration of the B phase being 4-8%; and collecting 6-8 min eluant and carrying out three-dimensional liquid phase separation by the elution mode of isocratic elution with concentration of the B phase being 2-3%, and collecting 7.5-12 min eluant and drying by evaporation so as to obtain a target product. According to the method, separation and purification are carried out by high performance liquid chromatography. Repeatability is high, preparation quantity is large, and operation is simple and time-saving. It is found through experiments that the compound has an inhibitory effect on Hep-g2. Thus, the compound has an anti-cancer drug developing potential and provides theoretical foundation for research and development of new drugs.

The invention relates to a medicine with a remarkable anti-hepatitis B effect. A structure of the medicine is shown as a formula 1 as shown in the specification. A compound which is low in toxicity has a great inhibition effect on HBsAg and HBeAg secreted by Hep G2.2.15 cells in vitro and has a therapeutic index remarkably higher than lamivudine, thereby being suitable for serving as the medicinefor hepatitis B treatment.

The invention discloses a compound Chinese actinidia root Chinese medicinal composition and a preparation method and application thereof, belonging to the technical field of traditional Chinese medicines. The Chinese medicinal composition is characterized by comprising the following traditional Chinese medicines in parts by weight: 40-80 parts of Chinese actinidia root, 20-40 parts of salvia chinensis, 20-40 parts of herba scutellariae barbatae, 20-40 parts of herba oldenlandiae and 20-40 parts of giant knotweed. The compound Chinese actinidia root Chinese medicinal composition has remarkableproliferation inhibition effects on various cancer cells such as a hepatoma cell line Hep-G2, a lung cancer cell line NCI-H460, a gastric cancer cell line MGC-803, a breast cancer cell line MCF-7, a colon cancer cell line HCT-116 and the like, and can be used for reducing physical and psychological pains of a cancer patient in the chemo-treatment process and solving the problems of difficult and expensive administration.

The present invention discloses an application of an oxamide compound in the preparation of an anti-liver cancer drug. The oxamide compound is N-(4,5,6,7-tetrahydro-1H-indazole-5-)-N'-(4-(p-tolyl)phenyl)oxamide, and the molecular formula is C 22 H 22 N4O3, with a molecular weight of 390.44 and a structural formula as shown in Formula (I), investigated the effect of N-(4,5,6,7-tetrahydro-1H-indazole-5-)-N'-(4-(p-tolyl)phenyl)oxalamide on the proliferation of liver cancer cells. The results showed that N-(4,5,6,7-tetrahydro-1H-indazole-5-)-N'-(4-(p-tolyl)phenyl)oxalamide exhibited significant anti-proliferation activity against human liver cancer cells (Hep G2, Hep 3B, PLC / PRF / 5, and Huh7), while exhibiting low toxicity against normal human liver cells (LX-2). This suggests that it possesses strong anti-liver cancer activity and excellent cell selectivity. Therefore, it is expected to be used in the preparation of anti-liver cancer drugs.

The invention discloses an ursolic acid pyrimidine amide derivative as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis and medicinal chemistry. The structural formula of the ursolic acid pyrimidine amide derivative is as shown in formula I. The preparation of the ursolic acid pyrimidine amide derivative comprises the following steps: oxidizing C-3 hydroxyl on an ursolic acid A ring into carbonyl, reacting with benzaldehyde with different substituent groups to obtain a benzylidene ursolic acid derivative, and reacting with different amines under the action of DCC / HOBt to generate an amide group, and reacting the ursolic acid amide derivative with guanidine hydrochloride in an alkaline environment to obtain the finished compound. The compound has a remarkable inhibition effect on human lung cancer cells A549, human breast cancer cells MCF-7, human cervical cancer cells HeLa and human hepatoma cell lines Hep G2, shows low toxicity on human normal hepatic epithelial cells Ges-1, and has the potential of developing and preparing antitumor drugs.

The invention provides a composition containing orlistat and dihydropyrimidine compounds. The specific definition of the dihydropyrimidine compounds is shown in the specification. The in-vitro test result indicates that the orlistat and dihydropyrimidine compounds can generate a synergistic inhibiting action on HBV (hepatitis B virus) DNA (deoxyribonucleic acid) replication in Hep G2.2.15 cells within the mol ratio range (the combined drug index CI is less than 1).

The invention provides neutral sea cucumber polysaccharide for resisting type II diabetes mellitus as well as a preparation method and application thereof, and the preparation method comprises the following steps: grinding light dry sea cucumber, performing protease enzymolysis, performing anion exchange column separation to obtain sea cucumber polysaccharide, and evaluating the anti-diabetes activity of the sea cucumber polysaccharide through insulin-resistant Hep G2 cells. The activity and activity of the sea cucumber neutral polysaccharide obtained by the method are reported for the first time, the glucose uptake capability of insulin-resistant Hep G2 cells can be remarkably improved, and due to the starch-like structure, the sea cucumber neutral polysaccharide can be used as an active substance and an auxiliary stabilizer in the preparation tabletting process.

The invention discloses a small-molecule heterocyclic dimer for tumor treatment and its use. The small-molecule heterocyclic dimer has the following structure: Experiments have shown that the small-molecule heterocyclic dimer of the present invention has a broad tumor-inhibiting spectrum and strong anti-tumor activity, and is effective against human cervical cancer cells HeLa and human liver cancer cells Hep G2. , IC of human breast cancer cell MCF-7, human pharyngeal squamous cell carcinoma cell FaDu, human non-small cell lung cancer cell A549 50 reaching the μM level, much higher than the control drug ligustrazine, while the IC on human breast cells MCF 10A 50 higher than that of tumor cells, showing the characteristics of high efficiency and low toxicity. The small molecule heterocyclic dimer of the present invention has potential application value in the development of antitumor drugs.

The invention discloses a vitamin D2 glucoside analogue, a synthesis and an application thereof. According to the invention, vitamin D2 is taken as a raw material, vitamin D2 fragment alcohol is prepared through an oxidation reduction reaction, and then vitamin D2 and its fragment alcohol are respectively taken as raw materials for synthesizing structural analogues of a and b. The synthesis method has the advantage of easily available raw materials, mild reaction condition, simple operation, and high yield, the novel synthesized vitamin D2 glucoside analogue has good inhibition capability to human liver cancer cell Hep G2 and human breast cancer cell MCF-7, and has latent medicinal value.

The invention discloses an indole quinone derivative of ursolic acid, a preparation method and application thereof, and belongs to the technical fields of organic synthesis and medicinal chemistry. The general structural formula of this ursolic acid indole quinone base derivative is shown in formula (I): the ursolic acid indole quinone base derivative of the present invention has significant antitumor activity, and pharmacological experiments show that it has Cervical cancer cell line HeLa, breast cancer cell line MCF‑7 and liver cancer cell line HepG2 have significant inhibitory effects, and have the potential to develop anti-tumor drugs.

The invention discloses synthesis and antitumor activity research of a novel drug small molecular formula (1) containing an indole structure, wherein R is as follows: 5-acetylvaleric acid is used as a starting raw material, then Fischer reaction, methylation reaction and hydrolysis reaction are performed to obtain 4-(5-(tert-butyl)-1, 2-dimethyl-1H-indole-3-yl) butyric acid, and the 4-(5-(tert-butyl)-1, 2-dimethyl-1H-indole-3-yl) butyric acid is used as a raw material. The compound is coupled with different amine compounds to obtain a target compound. A target compound is subjected to a CCK-8 experiment, and a conclusion is obtained that the target compound 6f and 5-fluorouracil are tested at the concentration of 20 [mu] M within 6a-6 h, and it can be known that the compound 6f has the best inhibition effect on A549 cells, Hela cells and A549 cells. IC50 value calculation is carried out on a target compound under various concentrations, the IC50 value of 6c to Hep G2 cells is minimum and the inhibition effect is best, and the IC50 value of 6f to A549 cells and Hela cells is minimum and the inhibition effect is best.