68results about How to "Good cell membrane permeability" patented technology

The invention provides a fluorescence dye using fluorescein as matrix, and a preparation method and application thereof. The fluorescence dye using fluorescein as maternal has the structure in general formula I. The fluorescence dye is used for biological dyeing, and simultaneously one of the dyes is applied to external and internal detections of cysteine, and meanwhile is applied to in vivo detection and other fields. The compound has a certain level of water-solubility, and simultaneously has good cell membrane permeability. The compound of the present invention simultaneously has novel spectrum characteristics, and the fluorescein derivative dyes with good properties are applied to the aspect of the fluorescence imaging.

The invention discloses an application of naphthyl derivatives used as targeted pH fluorescent probes for mitochondria, and specifically discloses targeted marking of 1- methyl-4-[2-(6-hydroxyl-2-naphthalene)- vinyl]-pyridium (HNEP<+>) in the mitochondria of living cells, and an application thereof in pH detection. The derivatives are excited at a wavelength of 390nm, and achieve maximum fluorescence emission at a wavelength of 586nm. The fluorescence intensity at a wavelength of 586nm is gradually weakened with the rising of the pH value from 5.00 to 11.50 in a phosphate buffer system. The pKa value is 8.8, and the linear range of the pH value is 7.8-10.0 and suitable for detection for the mitochondria in an alkaline environment (with a pH value of 8.0). In addition, the probes have an ultra-large Stokes displacement (196nm), and are high in selectivity and water solubility, low in toxicity and beneficial to fluorescence imaging study in the cells. A colocalization experiment in the cells and a pH adjustment experiment for the mitochondria prove that the probes are capable of realizing specific targeted marking for the mitochondria, and capable of detecting the change of the pH value in the mitochondria with high sensitivity.

The invention discloses a pseuoginsenoside F11 phospholipid complex as well as a preparation method and application of the pseuoginsenoside F11 phospholipid complex and belongs to the field of pharmaceutic preparations. The preparation method of the pseuoginsenoside F11 phospholipid complex comprises the following steps of: dispersing phospholipid in a hydrophilic carrier solution with a certain concentration, then adding pseuoginsenoside F11 to obtain a mixture, and then grinding the mixture into a suspension solution with the particle size being smaller than 1000nm, wherein the medicine, namely the pseuoginsenoside F11 and the phospholipid mutually act to form a phospholipid compound. The pharmaceutic liposolubility of the prepared phospholipid compound is increased, the permeability of the prepared phospholipid compound on cell membranes is increased, and therefore the bioavailability of the pseuoginsenoside F11 is greatly improved; the phospholipid compound can be prepared into quick-release pellets; and the activity of the prepared pseuoginsenoside F11 quick-release pellets is remarkably improved. No organic solvent is used in the preparation process, so that the environmental pollution is avoided and the production safety is improved.

The present inventors have found that when screening for cyclic peptide compounds that can specifically bind to a target molecule, the use of a library including cyclic peptide compounds having a long side chain in the cyclic portion can improve the hit rate for cyclic peptide compounds that can specifically bind to the target molecule. Meanwhile, the present inventors have found that tryptophan and tyrosine residues, which have conventionally been used in oral low molecular-weight pharmaceuticals and are amino acid residues having an indole skeleton or a hydroxyphenyl group, are not suitable for peptides intended to attain high membrane permeability.

The invention relates to novel binder-drug conjugates (ADCs) having improved properties, to active metabolites of these ADCs and to processes for their preparation. The present invention furthermore relates to the use of these conjugates for the treatment and / or prevention of diseases and to the use of these conjugates for preparing medicaments for treatment and / or prevention of diseases, in particular hyperproliferative and / or angiogenic disorders such as, for example, cancer diseases.

The invention discloses a polypeptide for carrying out targeting on mitochondria, and a preparation method and application of the polypeptide. The polypeptide is briefly recorded as MTPs. The polypeptide, which is prepared by the scheme of the invention, for carrying out the targeting on the mitochondria has a simple in synthesis method, and the obtained polypeptide can specifically carry out targeting on the cell mitochondria, is almost non-toxic to cells, has good cell membrane penetration characteristics, can be conveniently subjected to further multifunctional derivative modification, and provides a potential delivery tool for preparation of mitochondrial targeting drugs.

The invention provides a green fluorescence cyanine dye, which has a structural general formula I shown in the specification, wherein in the formula, X is C(CH3)2, O, S or Se; R1 and R2 are independently selected form H, C1-18 alkyl groups, OR6, C1-6 alkyl group OR6 or halogen respectively; R3 is N(R5)(R7); R4 is selected from C1-18 alkyl groups, benzyl groups and substituted benzyl groups; the substituted benzyl groups are arbitrarily substituted by the following groups: C1-18 alkyl groups, CN, COOH, NH2, NO2, OH, SH, C1-6 alkoxy groups, C1-6 alkyl amino groups, C1-6 acylamino groups, halogen or C1-6 halogenated alkyl groups; R5 and R7 are independently selected from H or C1-18 alkyl groups respectively; R6 is H or C1-18 alkyl groups; and Y is negative ions. The fluorescence dye can be used for DNA (Deoxyribonucleic Acid) quantitative detection and biological dyeing, and is applied to the fields of nucleic acid marking, blood cell analysis, clinic medical diagnosis, immune analysis detection and the like.