Kartogenin cartilage delivery material based on epsilon-polylysine as well as preparation method and kit thereof
A technology of polylysine and polylysine hydrochloride, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, bone diseases, etc., can solve the problem that it is difficult to really improve KGN intervention in arthritis biological Utilization etc.
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Embodiment 1
[0050] This embodiment provides a Kartogenin cartilage delivery material based on ε-polylysine, which has a structure such as formula (I):
[0051]
[0052] Among them, R is:
[0053]
[0054] R 1 for:
[0055]
[0056] Among them, p and q are the collection of positive integers and 0, and 0≤p≤50, 0≤q≤20;
[0057] R 2 for: -H or
[0058]
[0059]
[0060] In a preferred embodiment, in formula (I), n is a positive integer, and 5≤n≤200.
[0061] In a preferred embodiment, in formula (I), a, b, and c are a set of positive integers and 0, and a≥0, and at least one of b and c is not 0.
[0062] In a preferred embodiment, in formula (I), a+b+c=n.
Embodiment 2
[0064] This embodiment provides the preparation method of the ε-polylysine-based Kartogenin cartilage delivery material having the structure of formula (I) when c=0 in the above-mentioned embodiment 1:
[0065] Accurately weigh 0.317g (1mmol) KGN and 0.26g (1.2mmol) 4-(4,6-dimethoxytriazin-2-yl)-4-methylmorpholine hydrochloride (DMTMM), fully dissolve In 15mL of DMF, stirred at 25°C for 2 hours; then, under the conditions of 5Pa and 60°C, the organic solvent DMF was evaporated, and the obtained solid powder was dissolved in 2mL of dichloromethane, and separated by column chromatography. The separation conditions were: : 200-300-mesh column chromatography silica gel, the eluent is a mixed solvent of dichloromethane / petroleum ether with a volume ratio of 1:2, and the yellow powder active intermediate with the structure of formula (II) is obtained.
[0066]
[0067] Accurately weigh 1g (the molar weight of the amino group is about 6.1mmol) of ε-polylysine hydrochloride (the de...
Embodiment 3
[0071] This example provides the preparation method of the epsilon-polylysine-based Kartogenin cartilage delivery material having the structure of formula (I) when a=0.6, b=0.2, and c=0.2 in the above-mentioned embodiment 1:
[0072] Kartogenin (0.32g, 0.1mmol), PEG polymer represented by formula (III) (p=5, q=1, 0.36g, 0.12mmol), dicyclohexylcarbodiimide (0.25g, 0.12mmol) and 4-dimethylaminopyridine (0.15g, 0.12mmol) were dissolved in anhydrous dichloromethane, stirred at 25°C for 25 hours; Compound 0.5g, yield 80%;
[0073]
[0074] Accurately weigh 1 g of polylysine hydrochloride (the molar weight of the amino group is about 6.1 mmol), dissolve it in 50 mL of water / N'N-dimethylformamide with a volume ratio of 1:1, and use 2M NaOH The pH of the solution was adjusted to between 8-9; then 0.56g (1.22mmol) of compound (II) and 1.4g (2.44mmol) of compound (IV) were added, and stirred at room temperature for 30 hours; then 50mL was added to the reaction solution to Ionized w...
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