Shanghai Jiao Tong University

Other

Fudan University

Hongzhuan Chen

Hao Wang

Qian Zhang

Yang Lu

Xinghai Wang

Jianhua Liu

Shuangqi Tang

Meiyan Lu

Zhuibai Qiu

Qingxiang Song

Gan Jiang

Qiong Xie

Xiaoling Gao

Zheng Xia

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 Aβ 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. The nanocomplex has a disease repair effect and can carry drugs, which are delivered to cerebrovascular lesion site.

Nano complex for targeted repairing of neurovascular lesion, and preparation and use thereof

A stearoyl amino acid salt having a structural formula of the general formula (I), wherein Ris H or an aromatic base capable of being substituted by one or more substituents, or a Cstraight chain or an alkyl with a branched chain, the substituent being an alcoholic hydroxyl group or a phenolic hydroxyl group; and Ris a Csaturated 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. 

Stearoyl amino acid salt and preparation method and application thereof

The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (&#x2212;)-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 (&#x2212;)-meptazinol compounds were synthesized, from the starting material (&#x2212;)-meptazinol, successively by N-demethylation forming (&#x2212;)-nor-meptazinol and then by acylation with &#x3b1;,&#x3c9;-alkanediacyl dihalides or alkylation with &#x3b1;,&#x3c9;-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A&#x3b2; aggregation test demonstrated that the bivalent (&#x2212;)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both AChE and A&#x3b2; aggregation. The most potent compound inhibited both AChE and BChE at nM level, which was 10000 and 1500 times more potent than (&#x2212;)-MEP hydrochloride, respectively. It inhibited AChE-induced A&#x3b2; aggregation by a factor of 2 compared with propidium.

Bivalent (&#x2212;)-meptazinol compounds and/or their salts, and their preparation and futilization

Growing community of inventors

Shanghai, China

Hongzhuan Chen