407 results about "Dose dependence" patented technology

The invention relates to a new class of compounds, which are 1-phenylalcoxy-2-β-phenylethyl derivatives, as P-glycoprotein (P-GP) inhibitors. These compounds are useful in drug resistance events. They have been shown able to inhibit in a dose-dependent manner Glycoprotein-P (P-gp) activity in cell lines in which the expression of said glycoprotein is very high, like Caco-2 (human colon cancer) cells and MCF7/Adr (adriamycin-resistant human breast carcinoma) cells. The invention also relates to methods of production and the utilization of such compounds as medicaments useful in the treatment of states linked to the difficulty for some drugs to cross the blood-brain barrier (BBB) and generally within the context of the problems of drug resistance induced by chemotherapy agents.

Compositions and methods for the treatment of drug-induced long QT syndrome and other cardiac channelopathies are disclosed herein. The compositions and methods of the present invention comprise binding one or more QT prolonging drugs with a liposome prior to parenteral (intravenous or subcutaneous) administration, or administration of an empty liposome prior to or concomitantly with therapeutic agents known to have a high risk of QT prolongation, or immediately following an envenomation. The results presented show an abrogation of the adverse effects of QT prolonging drugs in a dose-dependent manner by the compositions of the present invention.

The invention discloses the application of celastrol in the preparation of the medicine for treating cancer expressing CIP2A protein. The celastrol of the invention has the characteristics of having no obvious down regulation CIP2A protein with the cell line particularity, reducing the expressing of oncoprotein in lung cancer, liver cancer, breast cancer and gastric cancer with time and dose pendence, causing oncoprotein C-Myc steadied by CIP2A to generate corresponding retrogradation, displaying remarkable cytotoxic activity in the cell of lung cancer and liver cancer, and having effective function of anti-tumor proliferation in the transplant model of tumor of nude mice lung cancer. The celastrol has a wide application prospect in treating lung cancer, head and neck squamous cell carcinoma, carcinoma of colon, gastric cancer, liver cancer, breast cancer and other cancer expressing CIP2A oncoprotein.

The invention relates to medicine. The inventive method for treating human diseases associated with an increased deoxyribonucleic acid content in extracellular spaces of tissues and organs, consists in orally injecting a DNA ferment in a quantity of 20 000-500 000 Kunz units in a day per 1 kg of the body mass. The single dose of the inventive medicinal preparation for treating human diseases associated with an increased deoxyribonucleic acid content in extracellular spaces of tissues and organs comprises 20 000-500 000 Kunz units of the DNAse ferment. The oral administration of the above-mentioned important doses of the preparation only allows the catalytically significant amount of DNAse to be absorbed into the systemic circulation in such a way that the dose-dependent treating effect thereof is exhibited.

G. vaginalis infection, a major cause of bacterial vaginosis (BV), is associated with biofilm formation. The present invention relates to treatment of G. vaginalis infections and BV with DNase. DNase reduces biofilm formation and increases biofilm breakdown, both in a dose dependent manner. The present invention further relates to treating BV and G. vaginalis infections with a combination of DNase and an antibiotic known to treat these diseases.

The invention provides methods and compositions for treating a tissue disorder in a subject by parenterally administering a solution of aminolevulinic acid (ALA) or a derivative thereof that is not greater than 1.0 percent by weight into a local subcutaneous or dermal region of the subject; and administering high fluence light to said bodily area to produce a phototoxic species in said local region, thereby treating a tissue disorder in the subject.

The invention discloses the application of koumine to the preparation of medicines for treating chronic pains and belongs to the application of gelsemium alkaloid monomer. The analgesic experiments of the koumine on chronic pains of animals prove that the koumine has potent dose-dependent analgesic effect, the analgesic potency is superior to that of the classical antipyretic-analgesic and anti-inflammatory drugs which are aspirin and indomethacin, the therapeutic index of the koumine is much higher than that of the total alkaloids of gelsemium, the koumine possibly has no tolerance, no addiction and little side effect, which indicates that the koumine has potent and low-toxicity analgesic effect, the mechanism of action of the koumine is possibly different from those of clinically common opium analgesics or aspirin analgesics, the koumine and the pharmaceutically acceptable salt thereof have the application of preparing of the medicines for treating chronic pains and have no serious disadvantages of the clinically common analgesics and can be developed into a novel analgesic which has potent analgesic effect in treating chronic pains such as inflammatory pain, neuropathic pain, cancer pain and the like, has no tolerance and addiction and little side effect, thus the koumine has bright industrialization prospect.

The invention discloses novel growth hormone releasing hormone analog peptides and an application thereof in preparing medicines for treating infertility. Experiments discover that 2D, 2E or 2F peptide has obviously high hypophysis GH releasing activity and hypophysis hormone releasing specificity. Tested by the conjugation reaction of an in-vitro GHRH dimer peptide and a hypophysis GHRH receptor, 2D, 2E and 2F dimer peptides have extremely high hypophysis receptor binding activity, wherein the 2F dimer peptide has the maximum binding activity. With the 2F peptide as the representative, infertility model treatment finds out that, compared with a normal saline group and a pure cyclophosphamide control group, in the 2F dimer peptide group, the spermatocytes and the spermatogonia in the seminiferous tubules are obviously increased, the seminiferous tubule cells are arranged in order and large in volume, the cavities of the seminiferous tubules are reduced and even disappear, and dose dependency is shown. All the facts indicate that the GHRH peptides with the 2F peptide as the representative have an obvious effect of stimulating the proliferation and the maturation of spermatogonia/oogonia, thereby promoting reproduction; and as a result, the novel growth hormone releasing hormone analog peptides can be applied to medicines for treating infertility.

Leptin was previously demonstrated to exert potent immune modulatory properties in several immune mediated disorders. The aim of the study was to determine leptin's anti-tumor effect in a murine model of human hepatocellular carcinoma (HCC). In vivo, Athymic T cell deficient (nude) mice transplanted with 1×10⁶ human Hep3B cells, followed by administration of two daily intraperitoneal doses of 0.5 mg/gram leptin for 6 weeks. Leptin administration induced a significant reduction in tumor size and improved survival in nude mice. Histologically, tumors of leptin-administered mice featured increased inflammatory exudate in interphase areas. Leptin-induced tumor suppression was associated with a significant increase in peripheral natural killer (NK) cell number. Splenocytes from leptin-treated mice featured decreased expression of CIS mRNA. To determine which lymphocyte subset is a prerequisite for the anti tumor effect of leptin, T&B cell deficient (Scid) mice and T,B& NK deficient (Scid-Beige) mice were subcutaneously implanted with Hep3B tumor cells, with and without the daily intraperitoneal administration of 0.5 mg/gram leptin for 6 weeks. SCID mice featured leptin-associated tumor suppression similar to those of nude mice. In contrast, NK-deficient SCID-Beige mice developed larger tumors. To further establish natural killer cell's central role in mediation of leptin's anti-tumor effect, NK cells were incubated in vitro with increasing doses of leptin, demonstrating a dose-dependent increase in cytotoxic activity. Incubation of leptin with hepatoma cell line was found to induce a dose-dependent reduction in hepatoma cell proliferation, suggesting an additive direct anti-tumor effect. Further synergism in inhibition of hepatoma cell proliferation in vitro was achieved following addition of natural killer cells. HCC cells expressed leptin receptor mRNA, while addition of leptin induced increased mRMA expression of STAT2 and SOCS1 on tumor cell lines. Leptin administration induces a significant suppression of human HCC. This effect is mediated by induction of natural killer cell proliferation and activation, and by direct inhibition of tumor growth. Decreased natural killer cell expression of inhibitory CIS protein and over expression of the anti-proliferative STAT2 and SOCS1 proteins in HCC lines may underline both anti cancerous effects of leptin.

The invention discloses a series drugs for resisting novel coronavirus SARS-CoV-2 and application thereof. In-vitro cell test results show that compounds disclosed in the invention can significantly inhibit infection of SARS-CoV-2 on normal cells, have an inhibition effect on novel coronavirus SARS-CoV-2 at a cellular level, can significantly reduce the virus titer of novel coronavirus in cells and inhibit proliferation of the novel coronavirus in cells, and has dose dependence. Therefore, the compounds can be used as inhibitors for novel coronavirus SARS-CoV-2, and has the potential of treating COVID-19 pneumonia caused by infection of a human body with the coronavirus SARS-CoV-2 or other diseases caused by infection of animals with the coronavirus SARS-CoV-2.

The invention discloses an application of polysaccharide extract of Artemisia argyi, which inhibits mouse transplanting Heps tumor and Eac tumor to improve the activity of mouse NK cell. The extract possesses obvious reinforced immune function, which is dependent on dose.

The invention discloses a radix scutellariae total flavonoids aglycon extract, also a preparation method of radix scutellariae total flavonoids aglycon extract and functions of treating and resisting renal fibrosis. Content of total flavonoids aglycons in the radix scutellariae total flavonoids aglycon extract is 45-70%. The extract is mainly composed of scutellarein, wogonin, oroxylin A and other aglycons. The preparation method of the extract is as follows: crushing radix scutellariae roots, screening by a No. 1 screen; adding 1-5 times amount of water, uniformly stirring, keeping temperature for enzymolysis at 32-40 DEG C for 5-9 hours, baking under vacuum at 60 DEG C, adding 2-8 times amount of ethyl acetate, continuously extracting for 6-10 hours, depressurizing, recycling solvent, thus obtaining total flavonoids aglycon extract. The extract can obviously relieve renal fibrosis symptoms when irrigated into a mouse stomach with renal fibrosis caused by mercuric chloride moulding and when a group of mice having the extract is compared with group of mice without having the extract. Results suggest that the total flavonoids aglycon extract has a dose dependence in preventing renal fibrosis.

This invention relates to embodiment to a molecular beacon, methods and kits for the detection of expression of p21(Waf1/Cip1), in response to chemotherapy. Specifically, the introduction of a phosphorothioate-modified p21-beacon by transfection in human tumor cells yields increased signal in a dose dependent manner.

The invention discloses a method for testing the biological activity of recombination insulinotropic hormone (Exendin-4) and relative application. Wherein, it comprises: using Exendin-4 to activate the cell to make cAMP excrete; the cAMP of cell will be increased quickly; using enzyme immunity method to test the cAMP content in the supernate of cracked cell and the cAmp content has dosage dependency in the supernate of cracked cell, to calculate the biological activity of Exendin-4, while the test cell is RIN-5F cell. The invention can be used to control the quality of recombination insulinotropic hormone (Exendin-4). The invention uses enzyme immunity method to test the biological activity, with simple process, less waste, high accuracy and better safety.

The invention relates to application of stephanine and hydrochloride thereof in the field of medicine, namely the stephanine or cepharanthine hydrochlofide is taken as an effective ingredient to prepare an anti-hepatitis B virus drug. The research shows that: the median toxic concentration (TC50) of the CH to cells is 2.09mu g.ml; and the CH can inhibit the synthesis of HBV DNA in the cells (P is less than 0.01) and is dose-dependent, the inhibition ratio of the CH to the HBV DNA in supernatant fluids of the cells is more than 50 percent when the dose is more than 0.5mu g.mL, IC50 of the CH is 0.324mu g.mL, the therapeutic index TI is equal to 6.45 (the TI is more than 2.0 and less than 10.0), and the CH has stronger effect of inhibiting the synthesis of the HBV DNA and is an effective low-toxicity drug. The invention develops novel pharmaceutical application of the stephanine and the hydrochloride of the stephanine, has the advantages of rich source of preparation raw materials, low cost, small toxic side effect, and simple preparation technology, can be prepared into oral dosage forms, injection dosage forms, tablets and the like, and has convenient use.

The invention discloses application of Lunasin polypeptide in the aspect of preparing substance with weight-reducing activity. Lunasin is substance with weight-reducing activity and is prepared by inhibiting differentiation of mouse preadipocyte (3T3-L1) through a PPAR gamma passage. The application includes: using an MTT method to detect influence, on 3T3-L1 adipocyte activity, of Lunasin at different dosages; detecting inhibiting effect, on adipocyte differentiation, of Lunasin at different dosages. Compared with current study conditions of Lunasin, the application has the advantages that the application shows that Lunasin can inhibit differentiation of insulin-induced 3T3-L1 cells, reduce accumulation of lipid droplets in lipid and inhibit mRNA expression of PPAR gamma, Lunasin presents dosage dependence, and effect of Lunasin with dosage higher than 50ug/mL is better than that of rosiglitazone of 5ug/mL; the application shows that Lunasin has potential weight-reducing effect.

The disclosure provides new compounds and compositions thereof, and methods for treating or ameliorating a disorder relating to CDG-Ia. In particular, the disclosure provides benzoisothiazolone inhibitors of PMI, which have been synthesized and their ability to drive glycosylation has been demonstrated. The disclosure provides two synthetic routes for these compounds, including a new copper-catalyzed N-arylation reaction amenable to parallel derivitization. The disclosed compounds represent potent inhibitors of PMI, and their dose-dependent efficacy in cell-based models of glycosylation have been demonstrated. In addition, the disclosed compounds are selective over PMM and therefore, are useful in treating or ameliorating a disorder relating to CDG-Ia.

The invention belongs to the medicinal field, in particular to a new application of Gardenia. The technological problem needed to be solved is to provide the new medicinal application of the Gardenia, namely the application in preparing medicines for curing vascular dementia. Proved by experiments, after the inventor adopts a permanent bilateral common carotid artery ligation method and establishes animal models of the vascular dementia and cures the animal models for a month by giving different dosages of geniposide and positive control drug, the inventor carries out behavior and pathological observation for observing the influence of behavior and pathological brain tissue and related biochemical parameters of the geniposide on dementia rats. The inventor finds out that the geniposide with different dosages has functions of improving and recovering cognitive dysfunction of the vascular dementia rats and the rats have dose-dependency, wherein, the geniposide with medium and high dosages has the function of curing the dementia close to donepezil. Therefore, the Gardenia or the geniposide can be adopted for curing the vascular dementia.

The invention to insecticide with folium and atractylodes extract as active ingredients. The insecticide is composed of folium and atractylodes extract and organic dissolvent. The volume ratio of folium extract and atractylodes extract is 1:(2-10). The concentration of the mixture of folium and atractylodes extract in the organic dissolvent is 0.3v/v%-12.0v/v%. The insecticide has a kill effect over national standard B level, evident dose dependence, and good helminthicide.

A system, method and apparatus is disclosed, comprising a biomathetical model for optimizing cognitive performance in the face of sleep deprivation that integrates novel and nonobvious biomathematical models for quantifying performance impairment for both chronic sleep restriction and total sleep deprivation; the dose-dependent effects of caffeine on human vigilance; and the pheonotypical response of a particular user to caffeine dosing, chronic sleep restriction and total sleep deprivation in user-friendly software application which itself may be part of a networked system.

The invention discloses a preparation method of sargassum oligosaccharide. The preparation method comprises the steps that fine polysaccharide obtained through degreasing and deproteinizing of sargassum is taken as a raw material, ultrasonic treatment is utilized, alginate lyase, mannase, xylanase and pectinase are sequentially added to perform enzymolysis on the polysaccharide, the polysaccharide which is not degraded fully is removed through an ethyl alcohol sedimentation method, supernate is centrifuged and screened by a molecular sieve to obtain retained matter, freeze drying is performed, and the sargassum oligosaccharide is prepared. The prepared sargassum oligosaccharide has the high inhibitory activity on alpha-glucosidase, the IC50 value is 4.82 mg/mL, the dose dependency is presented, and meanwhile the obvious promoting effect on glucose consumption of insulin-resistant HepG2 cells is achieved. According to the preparation method, the non-specific commercial enzymes are adopted, the process route is simple and reasonable, the method is suitable for industrialization, the preparation amount of the hypoglycemic active oligosaccharide is increased, and meanwhile the enzyme consumption and production cost are reduced; the method is an effective method for preparing the sargassum oligosaccharide and can be applied to hypoglycemic drugs, health care products and food.