61 results about "Aromatase" patented technology

The invention discloses an application of a long-chain fatty acid derivative shown as formula 5 or plant extracts containing the same in preparing preparations to inhibit the activity of aromatizing enzyme and in preparing pharmaceutical compositions to prevent or treat prostatoplasia diseases. The application opens up a new application field for the compound and also provides a new way for preventing and treating the diseases in the field.

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating estrogen receptor activity in a cell or patient or treating an estrogen receptor-mediated disorder, particularly breast and other cancers, in a patient in need thereof by administering an effective amount of compound of the invention thereto.

Compositions and methods for the use of inhibitory nucleic acids, for example small inhibitory ribonucleic acids (siRNA), to adjust, manipulate, prevent, inhibit, interfere, or block the androgen signal transduction pathway in a host cell, for example in a host's hair cell are provided. Aspects of the disclosure provide compositions and methods for interfering with the androgen signal transduction pathway by down regulating the expression of proteins involved in the androgen signal transduction pathway. Exemplary gene targets encoding proteins involved in the androgen signal transduction pathway include but are not limited to isozymes I and II of 5-α reductase, the androgen receptor, aromatase, 3-α-hydroxysteroiddehydrogenase, 3-β-hydroxysteroiddehydrogenase , 3-β-hydroxysteroiddehydrogenase-4-5-isomerase, 17-β-hydroxysteroidoxidoreductase, and steroid sulfatase. In some aspects, the inhibitory nucleic acids, for example siRNAs, interfere with the expression of targeted genes by preventing, reducing, or inhibiting the translation of mRNA transcribed from the targeted gene.

The invention provides a miRNA biomarker for diagnosis of polycystic ovarian syndromes.The miRNA biomarker is miR27a.Research shows that miR27a promotes apoptosis of granular cells, inhibits generation of aromatase, makes female hormones in granular cells disproportionate and leads to ovulation failures to cause polycystic ovarian syndromes.By inducing a mouse polycystic ovarian syndrome model with DHT, it is found that miR27a is highly expressed in the mouse polycystic ovarian syndrome model, and the effect of miR27a and target genes thereof in nosogenesis of polycystic ovarian syndromes is verified.miR27a can serve as a biomarker for polycystic ovarian syndromes, and a theoretical basis is provided for clinical pharmacy.

The present invention relates to the competence of oocytes for uterine implantation and development into living individuals. The invention more particularly relates to markers that are detected and measured in granulosa cells collected along with the oocytes during oocyte aspiration as it is done in assisted reproduction techniques. Markers include cytochrome P450 aromatase (CYP19A1), cell division cycle 42 (CDC42), 3-β-hydroxysteroid dehydrogenase 1 (3βHSD1), serpm peptidase inhibitor clade E member 2 (SERPINE 2), and adrenodoxm (ADX) that are detected and measured, using RT-PCR.

The invention discloses a medicinal composition, which comprises two or three of a, b and c, wherein a is long-chain fatty acid compounds of a formula I or plant extract containing the same; b is flavonoid compounds of a formula II or plant extract containing the same; and c is the following alkaloid compounds or plant extract containing the same: N1,N5,N10-tri-(E / Z)-coumaroyl spermidine, 1-O-(beta-D-glucose)-(2S, 3S, 4R)-2N-[(2'R)-2'-hydroxytetracosenoicacid]-octadecylene-3,4-diol, putrescine and indol-3-acetic acid. The medicinal composition of the invention can be used for preparing aromatizing enzyme inhibitor, 5alpha reductase inhibitor, alpha1-adrenergic receptor antagonist, cyclooxygenase-2 inhibitor, prostate-specific antigen (PSA) secretion inhibitor, anti-inflammation medicamentor medicament for resisting prostatic hyperplasia, prostatitis or prostatic cancer.

The invention discloses a kit and method for detecting CYP19A1 gene polymorphism by a pyrophosphoric acid sequencing method. The kit is used for examining the CYP19A1 gene polymorphism, particularly rs4646 (G is greater than T) single nucleotide polymorphism. The kit comprises primers shown as SEQ ID NO. 2-4. According to the kit, accurate, quick and high-flux detection of the CYP19A1 gene polymorphism can be realized, so that individual administration for realizing safe, rational and effective suppression on primer aromatase of the kit is achieved.

The present invention relates to compounds useful for measuring aromatase activity. The invention further provides methods for measuring aromatase activity and for screening test agents which modulate aromatase activity. A kit is also provided for use in such screening methods.

The invention relates to the field of medicinal chemistry and in particular relates to 4-imidazolyl quinoline and quinazoline ketone aromatizing enzyme inhibitors. The invention further discloses a preparation method and pharmacological activity of the inhibitors, a medicinal composition containing the compounds as well as the medical application of the inhibitors, in particular the medical application of the inhibitors in preventing or treating estrogen maintaining diseases such as breast cancers, endometrial cancers, female sexual precocity, gynecomastia and the like.

The invention relates to a pharmaceutical composition, particularly to a pharmaceutical composition with antitumor activity. The pharmaceutical composition with antitumor activity comprises 5,6-dimethylxanthenone-4-acetic acid (DMXAA) or an pharmaceutically acceptable salt or ester thereof and one drug component selected from glycopeptide antibiotics, actinomycins, mitomycins, glucoside antibiotics, Colchicum alkaloid, elemenes, aromatic enzyme inhibitors, LH-RH receptor antagonists, animal antitumor drugs and somatostatin analogues. The synergic composition has better antitumor activity. More specifically, the invention provides an application of the composition in treating tumors.

Provided are methods for determining level of bioactive testosterone in a biological sample. In one aspect, aromatase enzyme is utilized to convert free, bio-available testosterone into estradiol and the amount of estradiol is measured before and after the addition of enzyme. The difference in measurements provides the amount of bioactive testosterone in the sample. In another aspect, a competitor of testosterone binding to SHBG is utilized to displace testosterone bound to SHBG. Measurements of total testosterone in the sample before addition of competitor and afterwards are taken, such that the delta reflects the amount of testosterone that was bound on SHBG.

The invention discloses two sterol derivatives, a separation and extraction method thereof and an application thereof in preventing and treating prostatoplasia diseases. The two sterol derivatives are compounds 24-methylene cholesterol linoleate and cycloeucalenol linoleate shown as formula 1 and formula 2. The compounds which are not reported have the function of inhibiting the activity of aromatizing enzyme. The invention also discloses an application of the two sterol derivatives in preparing preparations to inhibit the activity of aromatizing enzyme and in preparing pharmaceutical compositions to prevent or treat prostatoplasia diseases.

The present invention relates to cell-based assays involving the estrogen receptor and / or aromatase. The assays use assay cells that are transfected with linear cassettes containing the ESR1 or the CYP19A1 gene of interest and measure the effect of mutations on the activity of the estrogen receptor and / or aromatase, and on their response to inhibitors.

The invention discloses a sugar alcohol ester of long-chain fatty acids, namely a linolenic acid sorbitol ester which is a compound shown as formula 1, and a preparation method thereof. The compound which is not reported has higher aromatizing enzyme inhabitation activity than free fatty acids. The invention also discloses applications of the sugar alcohol ester of long-chain fatty acids or plant extract containing the same in preparing preparations to inhibit the activity of aromatizing enzyme and in preparing pharmaceutical compositions to prevent and treat prostatoplasia diseases.

The present invention provides a cell activation agent, a collagen production accelerator, a whitening agent, an antioxidant, an anti-inflammatory agent, an aromatase activity accelerator, a protease activity accelerator, a skin external preparation, and food, which all contain an extract of Hibiscus makinoi.

The invention discloses a method for detecting estrogen in the environment, which comprises the following steps of: connecting a luciferase reporter gene vector with a rockfish aromatase gene pituitary specific promoter, constructing a reporter plasmid, co-transfecting a U251-MG cell to the reporter plasmid, a goldfish estrogen acceptor expression plasmid and an actin plasmid, stimulating the transfected U251-MG cell by using a sample to be tested, and detecting estrogen in the sample by detecting the activity of luciferase. The detection method provided by the invention has good repeatability, high sensitivity and reliable detection result, is simple and convenient to operate and can be widely applied to estrogen detection in the environment.

The present invention is directed to an aromatase activating agent containing a plant selected from among mulberry bark, ginseng, cucumber, and phellodendron bark; or chlorella; or an extract of any of these ingredients. The aromatase activating agent of the present invention is highly safe to the human body, and useful as a drug or cosmetic composition for prevention, amelioration, or treatment of various lesions caused by estrogen deficiency.

The present invention is directed to an aromatase activating agent containing a plant selected from among mulberry bark, ginseng, cucumber, and phellodendron bark; or chlorella; or an extract of any of these ingredients. The aromatase activating agent of the present invention is highly safe to the human body, and useful as a drug or cosmetic composition for prevention, amelioration, or treatment of various lesions caused by estrogen deficiency.

The present invention relates to novel uses of a steroid compound, which specifically binds to the androgen receptor (AR) but which is not metabolized by aromatase to a process for their preparation, to pharmaceutical compositions containing them, and to the use of said compounds for the prophylaxis and / or treatment of hormone-dependent or hormone receptor regulated cancers in mammals.

The invention discloses a polyhydroxy long-chain fatty acid, namely a 10, 11, 12-trihydroxy heptadecadienoic acid which is a compound shown as formula 1, and a separation and extraction method thereof. The compound which is not reported has high aromatizing enzyme inhabitation activity. The invention also discloses applications of the polyhydroxy long-chain fatty acid or plant extracts containing the same in preparing preparations to inhibit the activity of aromatizing enzyme and in preparing pharmaceutical compositions to prevent and treat prostatoplasia diseases.

A method of increasing expression of the aromatase gene by treating a cell population with an effective amount of an aromatase activator containing an extract of Iris florentina, where the effective amount ranges from 0.0001 to 1% by weight based on the total weight of the aromatase activator on a dry basis.

The invention discloses construction and application of recombinant saccharomyces cerevisiae for synthesizing carmine acid, and belongs to the technical field of gene engineering and biological engineering. The method comprises the following steps of heterologously expressing OKS of cyclase zhuI, aromatase zhuJ and Octaketide synthase 1, C-glucosyltransferase UGT2, monooxygenase aptC and 4'-phosphopantetheine transferase npgA in saccharomyces cerevisiae, thereby obtaining the recombinant saccharomyces cerevisiae capable of synthesizing the carmine acid. The recombinant saccharomyces cerevisiaecan be used for synthesizing carmine acid by taking acetyl-CoA and malonyl-CoA synthesized on the basis of the recombinant saccharomyces cerevisiae as precursors, so that the recombinant saccharomyces cerevisiae plays an important role in the fields of cosmetics, textiles and foods.

Four new analogues, 17β-hydroxy-7α,17α-dimethylestr-4,6-diene-3-one (2), 11β,17β-dihydroxy-7α, 17α-dimethyl-estra-1,3,5-triene-3-one (3), 3α,10β,17β-trihydroxy-7α,17α-dimethyl-5α-estrane (4), and 17β-hydroxy-7α,17α-dimethyl-5α-estrane-3,6-dione (5) of anabolic drug mibolerone (1) were synthesized. Derivatives 2 (IC50=3.83 ±0.3 μM) and 3 (IC50=4.24 ±0.2 μM) were identified as potent anti-inflammatory agents against T-cell proliferation. Derivative 4 (IC50=28.5 ±0.07 μM) showed a potent anti-inflammatory activity against TNF-α production. In addition, compounds 1 (IC50=46.0 ±2.4 μM), 2 (IC50=54.4 ±0.3 μM), 3 (IC50=49.1 ±0.4 μM), 4 (IC50=58.0 ±0.1 μM) and 5 (IC50=52.7 ±0.3 μM) showed a remarkable anti-inflammatory activity against NO⋅ production. Metabolite 4 (IC50=0.072 ±0.001 μM) showed a potent inhibitory activity against human placental aromatase. Compound 1 (IC50=24.19 ±2.1 μg / mL) was found to be cytotoxic against BJ normal cell line, while metabolites 2-5 were identified as non-cytotoxic.

Implementation is directed to selectively inhibiting estrogen production and providing estrogenic effects in a human body. A dietary supplement includes a processed Morinda citrifolia product that is used to inhibit aromatase or aromatase enzymes that function to convert androgens to estrogens, inhibit receptors from binding with estrogen, and reduce and / or regulate estrogen production, as well as reduce the amount of estrogen produced within the body and regulating such production. The dietary supplement further provides estrogenic effects. The present invention methods and compositions effectively function to treat estrogen-dependent cancers, and particularly inhibit, destroy, and reverse the effects of of estrogen-dependent cancerous tumors through the introduction into the body (e.g. ingesting) a safe, pre-determined dosage of a naturaceutical composition formulated with or comprising one or more processed Morinda citrifolia products for a safe, pre-determined duration.

The present invention provides a medicine compound including the following raw materials with the weight portions such as 18 to 30 portions of prepared rehmannia rhizome, 9 to 12 portions of cornus dogwood fruit, 8 to 16 portions of Chinese yam, 9 to 12 portions of medlar, 8 to 16 portions of field dodder and 8 to 16 portions of deerhorn glue, and the purpose in preparing the medicine for delaying vaginal aging. The medicine is an active medicine for strengthening external gonad tissue aromatase and a medicine for increasing vaginal blood supply. The medicine is a medicine for preventing or / and curing senile vaginitis. Under a specific diagnosis standard, the medicine provided by the present invention has definite efficacy. The medicine has the advantages of same efficacy on delaying vaginal aging, few raw materials, wide sources, effective cost saving due to selection of raw materials, no effect on the level of serum estrogen after long-term administration, no proliferation on endometrium and safety. The present invention provides a new choice for clinically curing senile vaginitis, in particular preventing senile vaginitis or recurrence of senile vaginitis.

The invention discloses an oxygen-bridged bicyclo-heptene sulfonate compound containing five-membered nitrogen heterocycle and application of the oxygen-bridged bicyclo-heptene sulfonate compound in preparation of anti-breast cancer drugs, and belongs to the technical field of medicines. According to the invention, a furan derivative containing a five-membered nitrogen heterocyclic ring and an ethylene sulfonate derivative are used as raw materials, a catalyst is not needed, and the oxygen-bridged bicyclo-heptene compound containing the five-membered nitrogen heterocyclic ring is prepared by one step through a Diels-Alder reaction. The compound provided by the invention can well inhibit MCF-7 cells, also has good inhibitory activity on drug-resistant breast cancer cells LCC2, can well inhibit aromatase, and has an application prospect in breast cancer treatment.

The invention relates to a composition for treating prostatic diseases and a preparation method thereof. The composition comprises the following components in parts by mass: 30 to 50 parts of theaflavin, 15 to 25 parts of herba dianthi superbi and 5 to 15 parts of herba dianthi chinensis. The preparation method comprises the following steps: S1: selecting materials; S2: adding the materials; S3: mixing powder; S4: mixing the powder again. The composition provided by the invention can be used for treating prostatic chronic inflammations and is used for treating diseases including prostatic hyperplasia, frequent micturition, dysuria, urgent urination, incomplete micturition, unsmooth and discontinuous micturition, urine leakage, heavy urine odor, micturition difficulty, hematuresis and the like; the composition has the effects of inhibiting the generation of DHT (Double Hydrogen Testosterone), balancing hormone in bodies, inhibiting aromatase, cleaning free radicals and reducing combination of sex hormone and protein.