Patent classifications
C07H15/06
ALGAL BOTANICAL EXTRACTS RICH IN EICOSAPENTAENOIC ACID AS TRI/DIGLYCERIDE CONJUGATE
Botanical extracts are provided, which comprise ethanol extracts of Nannochloropsis algae having between 10 wt % and 50 wt % polar lipids and between 45 wt % and 60 wt % fatty acids, wherein the fatty acids comprise more than 10 wt % of eicosapentaenoic acid (EPA) as triglyceride conjugates and/or diglyceride conjugates, and less than 15 wt % EPA as free fatty acids. EPA level may reach up to 90 wt %, and the botanical extract may be fluid at room temperature. Growth conditions are configured, adjusted and monitored to promote EPA formation in the cell vacuoles, resulting in a high proportion of EPA as tri/di-glyceride conjugates, as well as in a high concentration of ?-3 fatty acids, which merely requires gentle extraction procedures to reach the final products, thereby maintaining the biochemical of the compounds without excessive modifications.
ALGAL BOTANICAL EXTRACTS RICH IN EICOSAPENTAENOIC ACID AS TRI/DIGLYCERIDE CONJUGATE
Botanical extracts are provided, which comprise ethanol extracts of Nannochloropsis algae having between 10 wt % and 50 wt % polar lipids and between 45 wt % and 60 wt % fatty acids, wherein the fatty acids comprise more than 10 wt % of eicosapentaenoic acid (EPA) as triglyceride conjugates and/or diglyceride conjugates, and less than 15 wt % EPA as free fatty acids. EPA level may reach up to 90 wt %, and the botanical extract may be fluid at room temperature. Growth conditions are configured, adjusted and monitored to promote EPA formation in the cell vacuoles, resulting in a high proportion of EPA as tri/di-glyceride conjugates, as well as in a high concentration of ?-3 fatty acids, which merely requires gentle extraction procedures to reach the final products, thereby maintaining the biochemical of the compounds without excessive modifications.
HEXA-LACTOSIDE-TRIAZANONANE TRIACETIC ACID (NOTA) DERIVATIVE, METHOD FOR RADIOLABELING HEXA-LACTOSIDE POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENT FOR LIVER RECEPTOR WITH GA-68, AND HEXA-LACTOSIDE PET IMAGING AGENT FOR LIVER RECEPTOR
The present invention provides a hexa-lactoside-triazanonane triacetic acid (NOTA) derivative, a method for radiolabeling a hexa-lactoside positron emission tomography (PET) imaging agent for a liver receptor with Ga-68, and a hexa-lactoside PET imaging agent for a liver receptor. The hexa-lactoside-NOTA derivative is a conjugate of six chains of lactose with NOTA obtained by conjugating hexa-lactoside to a chelating agent p-thiocyanate-benzyl-triazanonane diacetic acid-glutamic acid in the presence of triethyl amine/dimethyl formamide as a solvent. The radiolabeling method comprises labeling with Ga-68 at room temperature. According to the present invention, the labeling effect is stable, the labeling efficiency of the labeled product is greater than 95%, the labeled product is highly stable and the radiochemical purity is still greater than 90% after 4 hours.
HEXA-LACTOSIDE-TRIAZANONANE TRIACETIC ACID (NOTA) DERIVATIVE, METHOD FOR RADIOLABELING HEXA-LACTOSIDE POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENT FOR LIVER RECEPTOR WITH GA-68, AND HEXA-LACTOSIDE PET IMAGING AGENT FOR LIVER RECEPTOR
The present invention provides a hexa-lactoside-triazanonane triacetic acid (NOTA) derivative, a method for radiolabeling a hexa-lactoside positron emission tomography (PET) imaging agent for a liver receptor with Ga-68, and a hexa-lactoside PET imaging agent for a liver receptor. The hexa-lactoside-NOTA derivative is a conjugate of six chains of lactose with NOTA obtained by conjugating hexa-lactoside to a chelating agent p-thiocyanate-benzyl-triazanonane diacetic acid-glutamic acid in the presence of triethyl amine/dimethyl formamide as a solvent. The radiolabeling method comprises labeling with Ga-68 at room temperature. According to the present invention, the labeling effect is stable, the labeling efficiency of the labeled product is greater than 95%, the labeled product is highly stable and the radiochemical purity is still greater than 90% after 4 hours.
Glycolipids and pharmaceutical compositions thereof for use in therapy
The invention may provide, in part, compounds for use as antiproliferative, chemotherapeutic, antiviral, cell sensitizing or adjuvant agents, and pharmaceutical compositions including the compounds. The compounds may be for use in treating diseases and disorders related to cell proliferation such as cancer, or in treating diseases and disorders which are linked to aberrant control of protein synthesis, such as cancer, viral infection, muscle wasting, autistic spectrum disorders, Alzheimer's disease, Huntingdon's disease and Parkinson's disease.
Glycolipids and pharmaceutical compositions thereof for use in therapy
The invention may provide, in part, compounds for use as antiproliferative, chemotherapeutic, antiviral, cell sensitizing or adjuvant agents, and pharmaceutical compositions including the compounds. The compounds may be for use in treating diseases and disorders related to cell proliferation such as cancer, or in treating diseases and disorders which are linked to aberrant control of protein synthesis, such as cancer, viral infection, muscle wasting, autistic spectrum disorders, Alzheimer's disease, Huntingdon's disease and Parkinson's disease.
Rhamnolipid Esters As Nonionic Surfactants For Cosmetic Use
The invention provides ester derivatives of rhamnolipids, formulations comprising these, and the use thereof.
Rhamnolipid Esters As Nonionic Surfactants For Cosmetic Use
The invention provides ester derivatives of rhamnolipids, formulations comprising these, and the use thereof.
SPHINGAMIDE COMPOUNDS AND METHODS FOR BINDING iNKT CELLS
The compounds, compositions and methods provided herein antagonize, inhibit, decrease, reduce, suppress, or disrupt CD1d-mediated, iNKT cell-mediated, and/or iNKT cell TCR-mediated immune signaling. The sphingamide compounds were rationally designed based upon 3D structural considerations in relation to the structures of each of CD1d, the iNKT cell TCR, and the ternary complex CD1d-a-GalCer analog lipids-TCR. More specifically, the addition of an amide in the phytosphingosine tail of a derivative of -GalCer led to a non-conserved binding with CD1d, a conserved binding with the iNKT cell TCR, and an antagonist-like phenotype.
Chemical Synthesis Method of Plesiomonas Shigelloides Serotype O51 O-antigen Oligosaccharide
The present disclosure discloses the chemical synthesis method of the Plesiomonas shigelloides serotype O51 O-antigen oligosaccharide, belonging to the field of chemistry. Source-abundant D-glucose, L-fucose, D-glucosamine and the like are used as raw materials to prepare three glycosylation building blocks, the synthetic route composed of 11 reaction modules is designed, and through the optimization of protecting group and the optimization of the time of introducing functional group, the preparation of the target oligosaccharide chain is successfully achieved. The oligosaccharide chain prepared in the present disclosure has the advantages of cheap and easy-to-get raw materials, and simple and easy-to-repeat preparation method. The present disclosure will have good application prospects in the aspects of development of new drugs and vaccines of Plesiomonas shigelloides, and the like.