23 results about "Cucurbitacins" patented technology

The invention discloses application of cucurbitacine I in preparation of cisplatin sensitization drugs for treating ovarian cancer, and belongs to the technical field of sensitization drugs for tumor chemotherapy. CuI and CDDP have a good synergistic tumor inhibition effect on ovarian cancer, CuI may directly act on EGFR and can be combined with CDDP to significantly inhibit phosphorylation of EGFR and downstream STAT3 protein thereof, induce DNA damage and ROS accumulation, amplify a pyroptosis effect, increase release of TAAs and DAMPs, promote DC maturation and promote infiltration of CD8 + T cells and memory T cells in TIME in vivo, so that the tumor inhibition effect on ovarian cancer is improved. The expression of an inhibitory costimulatory molecule PD-1 in CD8 + T cells is reduced, the whole body immune effect is activated, and the TIME of the ovarian cancer is remarkably improved. The combined treatment strategy of CuI-CDDP controls the progress of ovarian cancer from a dual mechanism of directly inhibiting tumor cells and promoting anti-tumor immune activation.

The invention provides a Hemsleya chinensis cytochrome oxidase HcCYP87D19 gene, and the sequence of the gene is shown in SEQ NO: 1. This invention constructs a transgenic Saccharomyces cerevisiae engineering bacteria co-transfected with Hemsleya cathayensis cytochrome oxidase HcCYP87D19 and HcCYP81Q58, the bacteria can produce a variety of cucurbitacin intermediates including 11-Carbonyl-cucurbita-5,23-diene-3β,16a,20,25-tetrol (6), 11-Carbonyl-cucurbita-5,23-diene-3β,16α,20,23-tetrol (6b), 11-Carbonyl-cucurbita-5,23-diene-16α,20,25-triol-3-one (6a), 11-Carbonyl-cucurbita-5,24-diene-16α,20,23-triol-3-one (6c), it provides a source for cucurbitacin production.

This invention discloses an anti-hepatitis active composition, its preparation method, and its application. The anti-hepatitis active composition, by mass percentage, comprises 70.3±0.4% cucurbitacin B, 26.1±0.2% isocucurbitacin B, and 3.6±0.3% cucurbitacin E. Using widely available sunflower seed shells as raw material, this invention obtains a high-purity, quality-controllable anti-hepatitis active composition by optimizing the extraction solvent, eluent composition, and chromatographic detection methods, ensuring the uniformity and controllability of TCs quality. Compared with cucurbitacin tablets, the anti-hepatitis active composition of this invention has a higher median lethal dose (LD50) and a NOAEL of 15 mg / kg BW, exhibiting higher safety.

The present application relates to a composition for inhibiting melanin production, its application, and a whitening method. The composition comprises active ingredients and excipients, wherein the active ingredients include one or more combinations of cucurbitacin B, mulberry root C, and hypocrellin A. Experimental verification demonstrates that any monomer of cucurbitacin B, mulberry root C, or hypocrellin A, or any combination thereof, exhibits significant inhibition of mushroom tyrosinase activity, inhibits tyrosinase activity in B16F10 cells, and inhibits melanin production in B16F10 cells, with low cytotoxicity. Application of the composition in cosmetic or pharmaceutical formulations can effectively whiten and combat melasma.

The invention relates to the technical field of plant genetic engineering and molecular breeding, in particular to application of CmBt and CmBr genes in regulation and control of bitter taste of muskmelon fruits. Physical interaction exists between muskmelon fruit bitter taste regulation factors CmBt and CmBr proteins, and expression of a bitter taste synthesis key gene CmBi is synergistically activated; the CmbtCmbr double mutants are constructed through a gene editing technology, it is proved that double-gene knockout has a synergistic effect, and the content of cucurbitacine B in all tissue of muskmelon can be more remarkably reduced; field trials show that under induction of forchlorfenuron, bitter taste of fruits of the CmbtCmbr double mutant completely disappears, the effect of the CmbtCmbr double mutant is remarkably superior to that of a single-gene mutant, and quality characters such as fruit weight and sugar degree are not negatively influenced; effective gene resources and germplasm materials are provided for solving the industrial problem that fruits become bitter due to the fact that plant growth regulators are used in muskmelon production.

This invention relates to the application of cucurbitacin Q1 in the preparation of drugs for treating gliomas, belonging to the field of biomedical technology. The cucurbitacin Q1 of this invention has a significant inhibitory effect on glioma cell activity. It can inhibit the protein expression of JAK1, JAK2, and STAT4 by regulating the JAK-STAT signaling pathway, and block the phosphorylation activation of STAT3 protein, thus weakening downstream signal transduction in this pathway. Simultaneously, it can also exert an anti-tumor effect by regulating the phosphorylation level of related proteins in the PI3K-AKT signaling pathway. The cucurbitacin Q1 of this invention not only significantly inhibits the proliferation, invasion, and migration of glioma cells, but also significantly increases the apoptosis rate of glioma cells.

The present application relates to the field of bioengineering, and particularly provides a epimerase Epi20 gene, the sequence of the gene is shown as SEQ NO:1, the enzyme can effectively utilize cucurbitacin 6a to synthesize cucurbitacin 6d, and provides a source for cucurbitacin production.

The invention discloses application of cucurbitacin B in preparation of a medicine for treating or preventing bombyx mori nuclear polyhedrosis virus. The research shows that the terpenoid cucurbitacin B can effectively inhibit replication of the bombyx mori nuclear polyhedrosis virus (BmNPV) in bombyx mori cells and bombyx mori bodies; the cucurbitacin B can be used for inhibiting the replication of the virus in bombyx mori cells and bombyx mori bodies through proper concentration and drug adding time, a new thought is provided for prevention of bombyx mori BmNPV infection, and a foundation is laid for prevention and treatment of virus infection in sericulture production.

The invention relates to a method for constructing a trichosanthes kirilowii maxim medicinal material fingerprint spectrum and determining the content of trichosanthes kirilowii maxim index components. The method comprises the following steps: taking a trichosanthes kirilowii maxim medicinal material to prepare a test solution; taking rutin, chrysoeriol and cucurbitacine D to prepare a reference substance solution; respectively injecting the test solution and the reference solution into a liquid chromatograph-mass spectrometer, obtaining a fingerprint spectrum of the trichosanthes kirilowii maxim medicinal material according to the liquid chromatograph-mass spectrometer, establishing a UHPLC-QQQ-MS quantitative detection method, and determining the content of the index components in the trichosanthes kirilowii maxim medicinal material in an MRM mode. According to the method for constructing the snakegourd fruit medicinal material fingerprint spectrum and measuring the content, provided by the invention, the evaluation standard of snakegourd fruits is comprehensively improved, and the effectiveness of the snakegourd fruit medicinal material in clinical use is ensured.

The present invention provides a cucurbitacin compound, its preparation method, and application, belonging to the field of pharmaceutical chemistry. The cucurbitacin compound represented by Formula I is extracted and isolated from Scrophularia purpurogenum. This furanocoumarin compound can inhibit the phosphorylation of STAT3 in triple-negative breast cancer cells and further affect the expression of downstream apoptosis-related proteins PARP and Caspase3, promoting apoptosis in triple-negative breast cancer cells, thereby inhibiting the growth of triple-negative breast cancer. It has broad application prospects in the preparation of drugs for the prevention and / or treatment of triple-negative breast cancer. #imgabs0# Formula I.

The invention relates to the technical field of medicines, and discloses application of cucurbitacine compounds in preparation of a medicine for treating herpes virus infection. Particularly, the cucurbitacine I, the cucurbitacine IIA and the cucurbitacine B effectively inhibit HSV-1 infection in Vero cells while maintaining corresponding cell viability, and the cucurbitacine I, the cucurbitacine IIA and the cucurbitacine B have a wide effective dose window and better patent medicine potential. According to the invention, the effect of the cucurbitacine compound in prevention and treatment of herpes virus infection is found for the first time, and the cucurbitacine compound is expected to become a low-toxicity and high-efficiency medicine and is applied to the medicine for treating herpes virus infection.

Provided are methods of modifying a cucurbitacine biosynthetic pathway by inhibiting cucurbitacine biosynthetic pathway enzymes in plants and plant cells, the production of plants and plant cells of the family Cucurbitacine having modified cucurbitacine and cucurbitacine derivatives, the plants and plant cells thus modified, and propagation thereof, and compositions comprising the modified plants and plant cells.

The present application relates to the technical field of biological medicine, and specifically discloses a small-molecule coupling compound targeting ASGPR, which has the following general formula: wherein X is a small-molecule ligand with the ability to target ASGPR; and Y is a derivative of cucurbitacin B. . The small-molecule coupling compound can be used in the preparation of a drug targeting ASGPR and having the functions of precise chemotherapy and radiotherapy sensitization. The small-molecule coupling compound prepared by the present application can achieve precise killing of liver cancer cells; the water solubility of cucurbitacin B is improved after coupling; the small-molecule coupling compound integrates precise chemotherapy and radiotherapy sensitization, and can significantly enhance the cancer-killing effect in combination with low-dose radiotherapy; and the small-molecule coupling compound has no obvious systemic toxicity and is well tolerated by patients.

The invention discloses application of cucurbitacine B (abbreviated as CuB) in preparation of drugs for relieving pulmonary fibrosis progress, and particularly relates to application of CuB in regulation and control of M2 macrophage polarization by inhibiting PI3K / AKT signaling pathways, by exploring the mechanism, a new therapeutic approach can be found for pulmonary fibrosis PF, theoretical and experimental foundations are provided for pathogenesis of PF and novel drug research and development, and the application of the cucurbitacine B in regulation and control of M2 macrophage polarization by inhibiting PI3K / AKT signaling pathways is developed. The method can be extended to provide a modern experimental basis for traditional Chinese medicine treatment of PF, research on the disease formation mechanism of PF and CuB drug targets is expected to promote theoretical development of subjects, meet clinical practical requirements, fill the theoretical blank and further promote industry development in the field of PF research, and the method has great social and economic benefits and application and popularization prospects.

This invention discloses the application of cucurbitacin B in the preparation of drugs for the treatment or prevention of silkworm nucleopolyhedrovirus. The research of this invention shows that the terpene compound cucurbitacin B can effectively inhibit the replication of silkworm nucleopolyhedrovirus (BmNPV) in silkworm cells and within the silkworm. By using appropriate concentrations and drug addition times, cucurbitacin B can inhibit the replication of the virus in silkworm cells and within the silkworm, providing a new approach for the prevention of BmNPV infection in silkworms and laying the foundation for the prevention and control of viral infections in sericulture.

The invention provides a composition which is composed of cucurbitacine A and gemcitabine. The invention further provides application of the composition in preparation of anti-pancreatic cancer drugs. The composition has the capacity of inhibiting clone formation of pancreatic cancer, inducing apoptosis of pancreatic cancer and / or inhibiting tumor progress. According to the invention, cucurbitacin A and gemcitabine are combined for use, gemcitabine can be synergistically sensitized to inhibit pancreatic cancer tumor activity, pancreatic tumor cells are inhibited, and toxicity of drugs to normal cells is reduced.

The application discloses a cucurbitacin B derivative A2, a preparation method and application thereof, and the structural formula of the cucurbitacin B derivative A2 is provided. 50 The cucurbitacin B derivative A2 provided by the application has a strong inhibitory effect on the proliferation activity of a human non-small cell lung cancer cell line A549, and the IC value is only 0.009 muM, which is increased by nearly 10 times than the inhibitory activity of cucurbitacin B on the proliferation of A549, and the toxicity to normal cells L02 is reduced by nearly 10 times, and the selectivity coefficient is increased by nearly 100 times than cucurbitacin. The xenograft mouse experiment result is consistent with the cell result, and can be used as a candidate drug for treating human non-small cell lung cancer; the preparation method has the advantages of rich raw material source, mild reaction condition, convenient operation in reaction process, cheap and easily obtained reagent, low toxicity or non-toxicity, low cost and suitability for industrial production.

The invention relates to the technical field of medicines for treating hand-foot syndrome and breast cancer, in particular to a composition for preventing and / or treating hand-foot syndrome (HFS) and synergistically resisting breast cancer as well as a preparation method and application of the composition. The composition comprises CuB-DOX (at) Lip, the CuB is cucurbitacine B, the DOX is doxorubicin, and the Lip is liposome. The mass ratio of CuB to DOX is 1: 5. The preparation method comprises the following steps: 1, preparing CuB-loaded lipidosome by using a film dispersion method; and 2, preparing the liposome CuB-DOX-coated Lip co-loaded with the two drugs by using an ammonium sulfate gradient method. In-vitro experiments prove that the combined application of the two medicines has the effect of treating the breast cancer. In-vivo experiments show that the compound has an obvious targeting effect. Meanwhile, the tumor growth inhibition effect of the CuB-DOX-coated Lip is obviously higher than that of a free drug group and a DOX-coated Lip group. Compared with a DOX-coated Lip group, IL-6 in a mouse in the CuB-DOX-coated Lip group is remarkably reduced, and IL-10 in the mouse in the CuB-DOX-coated Lip group is remarkably increased, which indicates that the CuB-DOX-coated Lip effectively inhibits inflammatory response in the mouse, so that the effect of preventing HFS is achieved.

The present invention discloses the use of an RNA-binding protein inhibitor in the preparation of a drug for inhibiting the replication of hepatitis B virus, wherein the RNA-binding protein is insulin-like growth factor 2 mRNA-binding protein 1. The present invention for the first time confirms that the host factor insulin-like growth factor 2 mRNA-binding protein 1 can promote the replication of hepatitis B virus, and this promoting effect is achieved by insulin-like growth factor 2 mRNA-binding protein 1 recognizing and binding to the m6A modification on hepatitis B virus RNA and increasing its stability. Therefore, the present invention provides a new target for anti-hepatitis B virus. Anti-hepatitis B virus effects can be exerted by targeting and inhibiting the expression of insulin-like growth factor 2 mRNA-binding protein 1 or using cucurbitacin B to inhibit the binding of insulin-like growth factor 2 mRNA-binding protein 1 to hepatitis B virus RNA, thereby providing new ideas for the research and development of new anti-hepatitis B virus drugs.

The present invention belongs to the field of biopharmaceutical technology, and specifically relates to a method and application for preparing cucurbitacin B derivatives by strong acid dehydration and peroxyacid oxidation. The present invention utilizes strong acid to catalyze the dehydration of cucurbitacin B and peroxyacid to oxidize the carbon-carbon double bond of cucurbitacin B, provides a variety of structural modification methods for cucurbitacin B, and synthesizes a series of novel cucurbitacin B derivatives. Subsequently, by using human breast cancer MCF-7 cells and human kidney epithelial HEK-293 cells to verify its proliferation inhibition effect and specificity, it was found that the anti-tumor activity of the compound was retained, and the selectivity index was improved compared to cucurbitacin B, which is worthy of further study.

The invention belongs to the field of biomedical engineering, and particularly provides application of a compound II as a proteasome inhibitor, the compound II is cucurbitacin E, the CAS number of the compound II is 18444-66-1, and the compound II is a natural small molecule compound. Experiments prove that cucurbitacin E can obviously inhibit the proteasome function and is a novel proteasome inhibitor. The proteasome inhibitor screened by the invention may become a new generation of proteasome inhibitor which is better in effect, stronger in specificity, smaller in side effect and also plays a role in solid tumors; the proteasome inhibitor can be finally used for preparing drugs for inhibiting tumor cell proliferation and / or inducing tumor cell death, and has important drug and medical clinical values.

Diabetes (DM) is a group of metabolic disorders characterized by chronic hyperglycemia, possibly accompanied by lipemia and obesity. These conditions drive insulin resistance and increase cardiovascular risk. Cucurbita moschata having a chemical name contains a variety of carotenoids, flavonoids, L-arginine, and cucurbitacine, which are biologically active compounds known to humans with a variety of therapeutic effects including anti-inflammatory, anti-oxidation, and health-promoting properties. The present disclosure proposes a white pumpkin powder (WPP)-based composition to improve glucose uptake, accelerate lipid metabolism, and lead to weight loss. In-vitro experiments carried out on human liver HepG2 cells indicate that glucose uptake and insulin sensitivity are remarkably improved, lipid in liver cells is reduced, and the influence on adipogenesis as a weight loss marker is increased. Furthermore, based on the outcome of the disclosure, the proposed WPP composition has the ability to be used at its optimal dose as an effective potential natural therapeutic agent for managing diabetes, dyslipidemia and obesity.

The invention discloses a nano-structure liposome and a preparation method thereof, and belongs to the technical field of liposome. The preparation method of the nanostructured liposome comprises the following steps: taking an oil phase and a water phase as raw materials to react to obtain the nanostructured liposome, the oil phase is prepared from glycerin monostearate, medium chain triglyceride, polyethylene glycol stearate, polyoxyethylene 35 castor oil, cucurbitacine B and cell-penetrating peptide TAT; the water phase comprises a glucose solution and Tween 80. The cucurbitacine B is applied to the aspect of anti-cancer chemotherapy drugs, solves the technical problem of poor bioavailability of the existing cucurbitacine B, and has the characteristics of good biocompatibility, low toxicity and good absorbability.