48 results about "Sesquiterpene lactone" patented technology

The invention provides an application of a gemmarane type sesquiterpene lactone compound in preparation of an antitumor drug. The gemmarane type sesquiterpene lactone compound disclosed by the invention has a relatively strong inhibition effect on proliferation of tumor cells, especially leukemia cells, and is more particularly most sensitive to human erythroleukocyte leukemia cells (HEL).

The invention discloses a guaiane type sesquiterpene lactone quasi-natural product as well as a preparation method and application of the guaiane type sesquiterpene lactone quasi-natural product. The quasi-natural product and the derivative thereof are prepared by taking (R)-Carvone as an initial raw material through a chemical synthesis method. Experiments show that the guaiane type sesquiterpene lactone compound prepared by the invention has the effect of inhibiting red blood cell hemolysis, can be used as a candidate drug molecule for preventing and / or treating NLRP3 inflammasome related diseases, and has the potential of being developed into related anti-inflammatory drugs.

The present invention discloses an amino acid sesquiterpene lactone compound 11β,13-dihydro-13-prolyl-lactucin, which has anti-inflammatory activity, expands the source of anti-inflammatory drugs, and takes a step further in the study of active monomer components in chicory.

The invention discloses an application of a sesquiterpene lactone compound in preparation of a medicine for enhancing a radiation therapy effect, and belongs to the technical field of biomedicine.The elephantopus tomentosus monomer EM-2 in a formula (I) enhances G2 / M phase retardation caused by ionizing radiation by inhibiting a signal channel caused by the ionizing radiation, so that the sensitivity of the radiation therapy is remarkably improved. Experimental results show that the compound combined with radiotherapy can reduce the expression of a cell proliferation marker Ki67, reverse ionizing radiation induced p-AKT activation, and further enhance the anti-tumor effect of radiotherapy. The compound has a good proliferation inhibition effect on cervical cancer cells, and has low toxicity on normal human skin fibroblast HSF cells. On the other hand, EM-2 can be combined with AKT protein in a targeted mode to inhibit a PI3K / AKT signal transduction pathway activated by radiotherapy, meanwhile, protective autophagy activated after radiotherapy is inhibited, and the sensitivity of ionizing radiation to cervical cancer cells is improved.

The invention discloses a high-efficiency targeted anti-hepatic fibrosis oral nano drug delivery system and a preparation method thereof. According to the system, a sesquiterpene lactone component, namely lettuce lactone (LC), in Xinjiang traditional liver protection medicinal material cichorium glandulosum is used as a medicine core, and although the lettuce lactone has a good anti-fibrosis effect, the lettuce lactone (LC) has the problems of poor water solubility, high first-pass metabolism and the like. Therefore, 18 beta-glycyrrhetinic acid modified silicon-based hybrid micelles (LC-FS-G) are studied and constructed, the liver targeting property of glycyrrhetinic acid and a silicon-based cross-linked structure are utilized to enhance the stability, and drug release is responded in a glutathione (GSH) high expression environment by virtue of a disulfide bond. The particle size of the obtained micelle is uniform (27.83 nm), the encapsulation efficiency reaches 95.05%, and the drug loading rate is 10.62%. The system is slowly released in gastric juice (48h release lt); 50%), and the gt can be quickly released in a high GSH environment (36h release gt; 87%), and the liver fibrosis process can be reversed by regulating and controlling a TGF-beta / Smad pathway. According to the strategy, physicochemical and metabolic restrictions of LC are overcome, and a new way with high efficiency and low toxicity is provided for oral nano targeted therapy of hepatic fibrosis.

The invention discloses a 1, 10-split ring type guaiane sesquiterpene lactone quasi-natural product as well as a preparation method and application of the 1, 10-split ring type guaiane sesquiterpene lactone quasi-natural product. The quasi-natural product and the derivative thereof are prepared by taking (R)-Carvone as a raw material through a chemical synthesis method. Experiments show that the 1, 10-split ring type guaiane sesquiterpene lactone compound prepared by the invention has the effect of inhibiting red blood cell hemolysis, can be used as a candidate drug molecule for preventing and / or treating NLRP3 inflammasome related diseases, and has the potential of being developed into related anti-inflammatory drugs.

The present invention discloses a sesquiterpene lactone compound, its preparation, and application. The compound is isolated from the plant Lepidoptera of the genus Lepidoptera in the Asteraceae family and obtained through solvent extraction, silica gel column chromatography, ODS column chromatography, and liquid chromatography separation. Experimental results demonstrate that the sesquiterpene lactone compound provided by the present invention can significantly inhibit the proliferation of glioma cells, induce apoptosis in glioma cells, and alter mitochondrial membrane potential in cells. Therefore, the compound is a candidate anti-glioma drug.

The invention relates to the technical field of biological medicine, in particular to centipeda minima extracellular vesicle nose drops and a preparation method and application thereof.The centipeda minima extracellular vesicle nose drops comprise active ingredients, plant extracellular vesicles (Cm-EVs) derived from centipeda minima, the concentration of the plant extracellular vesicles (Cm-EVs) is 1 * 10 < 10 >-5 * 10 < 11 > particles / ml; the key active substances are as follows: the content of the Cm-EVs naturally encapsulated sesquiterpene lactone compound centipederin is more than or equal to 50 micrograms per milliliter (detected by HPLC-MS); the pharmaceutical auxiliary materials comprise 0.05 to 0.2 percent (w / v) of sodium hyaluronate, 0.8 to 1.0 percent (w / v) of NaCl and 0.005 to 0.02 percent (v / v) of polysorbate 80; the method has the beneficial effects that the targeted enrichment capability is realized: mucous membrane adhesion is enhanced through surface pectin protein, and the nasal cavity residence time is prolonged to 6 hours (the free medicine is less than 1 hour); the nano-scale particle size (80-200nm) can efficiently penetrate through the mucous layer, and the nasal mucosa drug concentration reaches 20 times of the plasma concentration (rat pharmacokinetic data); the long-acting slow-release property is as follows: the active ingredients are protected by the lipid bilayer, the cumulative release rate of the centipederin within 72 hours reaches 82%, and the free medicine can be completely released within 24 hours.

The invention provides dimerized guaiane sesquiterpene lactone 1-25 shown in a structural formula as well as a pharmaceutical composition, a preparation method and application thereof, and belongs to the technical field of medicines. The preparation method disclosed by the invention comprises the following steps: carrying out Diels-Alder reaction / deprotection on guaiane diene and divinyl ketone, so as to obtain the dimerization guaiane sesquiterpene lactone 1 to 25. The dimerized guaiane sesquiterpene lactone has inhibitory activity on human hepatoma cell lines HepG2, Huh7 and SK-Hep-1, and the compound 17 can significantly inhibit growth of transplanted tumors in nude mice, can form a pharmaceutical composition with a pharmaceutically acceptable carrier, and can be used for preparing anti-hepatoma drugs.

The invention belongs to the technical field of cosmetics, and discloses application of sesquiterpene lactone compounds in whitening. The invention finds that the arnica lactone D and artemisinin have related whitening effects for the first time, specifically, the arnica lactone D and artemisinin are capable of inhibiting melanogenesis and tyrosinase activity, good in inhibition effect, low in onset concentration and non-irritant to red blood cells, so that the arnica lactone D and artemisinin have certain safety, also have relatively good anti-inflammatory activity, can improve hyperpigmentation after inflammation, and can be used for preventing and treating inflammation. The method has great potential in the fields related to cosmetics.

This document discloses a method for generating intermediates in the total synthesis of (+)-daunoglobin or its derivatives, and the total synthesis of (+)-daunoglobin or its derivatives. This document also discloses methods for forming compounds of formula XIV and XV, wherein compounds of formula XIV and XV are as defined in the specification.

The present invention belongs to the field of biomedicine and specifically discloses the use of a sesquiterpene lactone compound from Yemazhui in the preparation of a drug for treating polycystic ovary syndrome. The use of the sesquiterpene lactone compound from Yemazhui in the preparation of a drug for treating polycystic ovary syndrome disclosed in the invention has the following beneficial effects: 1. For the first time, the sesquiterpene lactone compound from Yemazhui was applied to a mouse model of polycystic ovary syndrome. Related experiments demonstrated that the sesquiterpene lactone compound from Yemazhui alleviated polycystic ovary syndrome symptoms and inhibited ovarian and systemic inflammation; 2. The sesquiterpene lactone compound from Yemazhui has been clinically used, has a single component, and is safe and reliable, facilitating clinical application and promotion.

The invention discloses an eudecane type sesquiterpene lactone TBB chlorambucil heterocomplex and application thereof, the derivative is a compound TBB-DJ, and the structural formula of the derivative is as shown in the formula TBB-DJ. Experimental results show that the compound TBB-DJ has a remarkable inhibition effect on proliferation activity and migration ability of liver cancer cells, and shows a unique anti-hepatocellular carcinoma effect of the compound TBB-DJ. Therefore, the compound TBB-DJ has an important application prospect in research and development of anti-hepatocellular carcinoma drugs.

This application discloses the use of artesunate in the preparation of drugs for enhancing the therapeutic effect of PARP inhibitors, belonging to the field of biomedical technology. The artesunate described in this application is a sesquiterpene lactone derivative extracted from the traditional Chinese medicine Artemisia annua. It has an inhibitory effect on the proliferation of BRCA wild-type ovarian cancer cells and low toxicity to normal human ovarian epithelial cells. This application's research found that artesunate can enhance the DNA damage and apoptosis induced by PARP inhibitors (such as olaparib, niraparib, and rucaparib), and improve the sensitivity of PARP inhibitors to BRCA wild-type ovarian cancer.

The present invention relates to a process for recovering sesquiterpene lactones using non-ionic polymer resin adsorption.

The present invention provides a sesquiterpene lactone derivative with anti-inflammatory and anticancer activity, as well as a preparation method and use thereof. Specifically, the present invention provides a compound represented by the following formula I, or a hydrate, solvate, stereoisomer, racemate, or pharmaceutically acceptable salt or prodrug thereof, wherein R1 and R2 are as defined herein. Compound I is an NF-κB inhibitor. Therefore, the compounds of the present invention can be used to treat or prevent NF-κB-mediated diseases, disorders, and conditions, such as cancer and inflammation.

The invention relates to the field of medicinal chemistry, relates to a guaiane sesquiterpene lactone compound as well as a preparation method and application thereof, and in particular relates to a guaiane sesquiterpene lactone compound which is a compound 1 to a compound 8, a preparation method of the guaiane sesquiterpene lactone compound and medical application of the guaiane sesquiterpene lactone compound in preparation of medicines for preventing or treating inflammatory diseases. Furthermore, two compounds (a compound 5 and a compound 8) with remarkable anti-inflammatory activity are rapidly screened by using an LPS-induced RAW264.7 cell inflammation model, the structure is novel, the synthesis method is simple and convenient, and an excellent anti-inflammatory effect is shown in an in-vitro model. Compared with the existing anti-inflammatory drugs, the compound has the potential of becoming a new generation of anti-inflammatory drugs, and can be used as a lead compound to develop a novel anti-inflammatory drug.

The invention discloses a sesquiterpene lactone compound as well as a preparation method and application thereof, and relates to the technical field of pesticides. According to the invention, three sesquiterpene lactone compounds are obtained by extracting, separating and purifying overground parts of tithonia diversifolia. According to the present invention, the prepared sesquiterpene lactone compound tithonin A can effectively prevent and control the plant virus ToBRFV, the ToBRFV inhibition effect of the sesquiterpene lactone compound tithonin A is superior to the broad-spectrum bactericide ningnanmycin to a certain extent, the prevention and control effect is good, and the alpha-OH is the main functional group after the sesquiterpene lactone compound tithonin A is compared with the similar compounds.

The invention discloses an eudecane type sesquiterpene lactone TBA dimethylamine adduct, namely a compound TBA-DMA, and the structural formula of the compound TBA-DMA is as shown in the formula TBA-DMA. Experimental results show that the compound TBA-DMA has a remarkable inhibiting effect on proliferation activity of liver cancer cells, the targeting effect on the liver cancer cells is more selective than that on normal cells, the specific anti-tumor effect of the compound TBA-DMA is shown, and damage of anti-cancer drugs to the normal liver cells can be reduced. Therefore, the compound can be used as a candidate molecule for the development of anti-cancer drugs, and particularly has an important application prospect in the research and development of anti-hepatocellular carcinoma (HCC) drugs.

The present invention discloses a hirsutinolide-type sesquiterpene lactone having anti-prostate cancer activity, a preparation method and an application thereof, wherein the hirsutinolide-type sesquiterpene lactone has a compound represented by formula (I); wherein R1 is selected from C 1～10 The hirsutinolide-type sesquiterpene lactone provided by the present invention has significant anti-prostate cancer cell proliferation activity, and its IC 50 Low value.

The application discloses a marine-derived compound Cpd-8 and application thereof in preparation of a medicine for resisting TNF-induced cell death. Through screening of an extract library of marine-derived sponge symbiotic fungi of a research group, a small-molecule inhibitor with a novel structure is obtained, which can resist TNF-induced cell death, and specifically, the marine-derived sesquiterpene lactone nitrobenzene analogue Cpd-8 and a pharmaceutically acceptable salt thereof. The compound can inhibit TNF-induced cell death and formation of a complex II in a signal pathway, thereby exerting an anti-cell death activity. In-vitro cell experiment results show that the compound of the application can significantly inhibit TNF-induced cell death. In-vivo animal experiment results show that the compound of the application can inhibit TNF-alpha / D-GaIN (D-galactosamine)-induced acute liver injury, and significantly prolong the survival period of mice.

The invention discloses a natural sesquiterpene lactone compound and application thereof in preparation of a medicine for treating or preventing inflammatory diseases, and the structural formula of the natural sesquiterpene lactone compound is shown as campetolide A (1) and campetolide B. According to the natural sesquiterpene lactone compound, the new compounds campetolide A (1) and campetolide B (2) are extracted from branches and leaves of golden camellia, and the two compounds are found to have a remarkable inhibiting effect on NO generation; the compound can be used for preparing an NO production inhibitor, has a good application prospect in preparation of drugs for treating or preventing NO-mediated inflammatory diseases including immune system inflammation, respiratory system inflammation, digestive system inflammation and the like, and can be used as a lead compound for preparing drugs or drugs for treating or preventing NO-mediated inflammatory diseases.

The invention discloses an eucalyptol type sesquiterpene lactone TBA and TBB nitrogen mustard derivative as well as a preparation method and application thereof. The structural formulas of the eucalyptol type sesquiterpene lactone TBA and TBB nitrogen mustard derivative are respectively shown as a formula TBA-DJ-1-3 and a formula TBB-DJ-1-3. Cytotoxicity tests show that the nitrogen mustard derivatives can inhibit the proliferation activity of liver cancer cells, particularly, the proliferation inhibition effect of the compound TBA-DJ-2 on HepG2 cancer cells is remarkably better than that of a parent body, and the nitrogen mustard derivatives can be used for clinically preparing anti-liver cancer drugs.

The invention discloses an application of sesquiterpene lactone CJ shown as a formula I in preparation of a medicine for preventing and treating hepatic fibrosis, and relates to the technical field of biological medicines, and the sesquiterpene lactone CJ can obviously protect the liver from CCl4-induced injury and effectively improve hepatic fibrosis symptoms. The action mechanism is that HSP90AA1 is regulated in a targeted manner to inhibit an NLRP3 / caspase-1 signal channel, so that pyroptotic death of hepatocytes is generated. In addition, the sesquiterpene lactone CJ also shows a remarkable improvement effect in an LX-2 cell inflammation model induced by TGF-beta1. The callistephus chinensis extract sesquiterpene lactone CJ provided by the invention has a remarkable effect in the aspect of preventing and treating CCl4-induced hepatic fibrosis.

The invention belongs to the technical field of medicines, and particularly relates to a composition containing oncolytic viruses and application of the composition in the field of preparation of antitumor drugs. In order to solve the problem that the anti-tumor effect is poor when an oncolytic virus is independently used, the invention provides an anti-tumor interferon inhibitor and oncolytic virus composition, the active ingredients of the composition comprise an interferon inhibitor (a gemarane type sesquiterpene lactone compound EM-2) and an oncolytic virus VSV delta51 which are active ingredients with a synergistic effect, in the preparation of anti-tumor drugs, a remarkable anti-tumor effect can be achieved through combined use. It is found for the first time that the gemmarane type sesquiterpene lactone compound can be used as an interferon inhibitor and can be used as an anti-tumor synergist or a drug resistance reversal agent of oncolytic viruses, the anti-tumor effectiveness of the oncolytic viruses is remarkably improved by inhibiting interferon signal channels, and the gemmarane type sesquiterpene lactone compound has important application value and wide clinical transformation prospects and is worthy of popularization and application. And a new direction is expected to be provided for clinical treatment of tumors.

The present application relates to a kind of guaiane type sesquiterpene lactone compounds and preparation method and purposes, the guaiane type sesquiterpene lactone compound is from the whole grass of thousand leaf achillea ( Yarrow ​ L.) Is extracted using organic solvent, extraction, then by normal phase silica gel column chromatography, low pressure fast preparation chromatography and two to three methods in semi-preparative high performance liquid chromatography Separation, obtain two new guaiane type sesquiterpene lactone monomer compounds, by high resolution mass spectrometry and nuclear magnetic resonance spectroscopy etc. Method determines two compounds as new guaiane type sesquiterpene lactone compound, and its structure identification is carried out.In addition, the two guaiane type sesquiterpene lactone compounds are determined by microglial cell BV2 to the related activity determination of treating neuroinflammation, and the results show that: the guaiane type sesquiterpene lactone compound can treat neuroinflammation, can be used for anti-neuroinflammatory drug.

The invention discloses a camellia chrysantha terpenoid, an extraction method thereof and application of the camellia chrysantha terpenoid in preparation of an ACL inhibitor, and belongs to the field of biological medicine, and the terpenoid (the structure is shown in the following formula 1 and formula 2) is separated from branches and leaves of camellia camellia plant camellia chrysantha of the theaceae family, the compound 1 is guaiane type sesquiterpene lactone, and the compound 2 is guaiane type sesquiterpene lactone. And the compound 2 is an ursane type triterpenoid compound. Multiple in-vitro activity tests show that the two terpenoids have significant ATP-citrate lyase inhibitory activity, and can be applied to preparation of drugs for preventing, delaying or treating ACL-mediated glucose and lipid metabolism disorders and other related diseases. The compound provided by the invention can also provide a lead compound for research and development of novel drugs for diseases related to glucose and lipid metabolism disorders.

The application discloses a saussurea involucrata sesquiterpene lactone compound for promoting expression of antioxidant enzyme CAT in cells and application thereof, and is compounds 1-7. The compound is obtained by extraction and separation from aerial parts of saussurea involucrata, is safe and reliable in source, meets the safety requirement for biological use, and has the effects of promoting expression of antioxidant enzyme CAT in cells and significantly reversing up-regulation of MDA caused by H2O2, and has the effects of anti-aging and anti-oxidation.

The present application relates to the technical field of natural product extraction, and particularly relates to application of a sesquiterpene lactam compound separated from honeysuckle to preparation of an antiviral drug and a separation method thereof.The present application has the beneficial effect that a novel sesquiterpene lactam compound is separated from honeysuckle for the first time, the separation and purification method is simple, and after activity testing, it is found that the compound has certain antibacterial activity and has potential medicinal value.