Abstract: Nanocomplex for targeted repairing of neurovascular lesion. The nanocomplex comprises a lipid, an apolipoprotein and a targeted peptide, the targeted peptide formed by covalently linking, through a bridge structure, a nanocarrier linking end and a peptide chain targeting RAGE, which specifically binds to cerebrovascular lesion site. Based on AD and the high expression of RAGE in cerebrovascular and brain parenchyma in diabetic encephalopathy, the nanocomplex, as modified by the targeted peptide, can mainly bind, in a targeted manner, to cerebrovascular endothelium by linking the targeted peptide, to repair vascular endothelial cells, promote removal of AB plaque near blood vessels, and repair cerebrovascular and neurovascular unit components such as microglial cells, astrocytes and neurons. Ameliorating cognitive impairment is achieved by combined repairing of multiple components and restoring cerebrovascular functions and cerebral blood flow.

Abstract: Disclosed is a nanocomplex, a preparation method therefor, and a use thereof. The nanocomplex comprises 0-60% a protein drug, 0.03-15% hyaluronic acid, 0.8-20% protamine, 35-95% lipid components, and 2.5-40% a apolipoprotein and/or a mimetic peptide thereof; the lipid components comprise an electrically neutral lipid and an anionic lipid; and the total amount of hyaluronic acid and protamine is 0.03-15%. The nanocomplex of the present invention provides a general-type carrier for protein drugs having different physicochemical properties (such as molecular weights of 10-255 KDa and PIs of 4-11), implements highly efficient intracellular, in vivo, and even in-brain delivery, utilized technology is universal in nature, and said invention can effectively solve the current problem of insufficient in vivo and in vitro transport of protein drugs (comprising a protein drug exceeding the molecular weight and PI of an embodiment).

Abstract: An isolated stearoyl amino acid salt of formula (II) or formula (III) is provided, wherein M in the formula (II) is K+, Na+, or NH4+; and M2+ in the formula (III) is Ba2+, Ca2+, or Mg2+. Also provided are compositions containing the isolated stearoyl amino acid salt and methods of using the isolated stearoyl amino acid salt and composition to treat a disorder, such as cerebral ischemia, stroke, Alzheimer's disease, and Parkinson's disease.

Abstract: The present invention discloses a reconstituted lipoprotein modified by monosialoteterahexosyl ganglioside, an application in preparing a drug carrier thereof, and an application in preparing a drug for treating or preventing a disease associated with A? deposition thereof. Specifically, the present invention discloses an application of an appropriate amount of monosialoteterahexosyl ganglioside in modifying the reconstituted lipoprotein to increase an affinity of the reconstituted lipoprotein with amyloid ?-protein (A?), and facilitating clearance of A?. Meanwhile, the reconstituted lipoprotein modified by monosialoteterahexosyl ganglioside is used as a multi-mode nano carrier for preventing and treating central nervous system diseases, and particularly Alzheimer's disease.

Abstract: A stearoyl amino acid salt having a structural formula of the general formula (I), wherein R1 is H or an aromatic base capable of being substituted by one or more substituents, or a C1-4 straight chain or an alkyl with a branched chain, the substituent being an alcoholic hydroxyl group or a phenolic hydroxyl group; and R2 is a C11-25 saturated or unsaturated aliphatic group. Also provided are methods of preparing the stearoyl amino acid salt, and methods of using the stearoyl amino acid salt. Compared to a prototype drug stearoyl amino acid, the stearoyl amino acid salt described herein has excellent physicochemical properties, good stability, high relative bioavailability, a strong drug effect and a high safety factor. It is thus expected to become a candidate for clinical treatment of neurodegenerative diseases and acute brain injury, and a clinical drug for weight loss, thus having broad application prospects.

Abstract: A stearoyl amino acid salt having a structural formula of the general formula (I), wherein R1 is H or an aromatic base capable of being substituted by one or more substituents, or a C1-4 straight chain or an alkyl with a branched chain, the substituent being an alcoholic hydroxyl group or a phenolic hydroxyl group; and R2 is a C11-25 saturated or unsaturated aliphatic group. Also provided are methods of preparing the stearoyl amino acid salt, and methods of using the stearoyl amino acid salt. Compared to a prototype drug stearoyl amino acid, the stearoyl amino acid salt described herein has excellent physicochemical properties, good stability, high relative bioavailability, a strong drug effect and a high safety factor. It is thus expected to become a candidate for clinical treatment of neurodegenerative diseases and acute brain injury, and a clinical drug for weight loss, thus having broad application prospects.

Abstract: The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (?)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (?)-meptazinol compounds were synthesized, from the starting material (?)-meptazinol, successively by N-demethylation forming (?)-nor-meptazinol and then by acylation with ?,?-alkanediacyl dihalides or alkylation with ?,?-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A? aggregation test demonstrated that the bivalent (?)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both AChE and A? aggregation. The most potent compound inhibited both AChE and BChE at nM level, which was 10000 and 1500 times more potent than (?)-MEP hydrochloride, respectively.

Abstract: The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (?)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (?)-meptazinol compounds were synthesized, from the starting material (?)-meptazinol, successively by N-demethylation forming (?)-nor-meptazinol and then by acylation with ?,?-alkanediacyl dihalides or alkylation with ?,?-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A? aggregation test demonstrated that the bivalent (?)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both ACHE and A? aggregation. The most potent compound inhibited both ACHE and BCHE at nM level, which was 10000 and 1500 times more potent than (?)-MEP hydrochloride, respectively.