Beta-sitosterol derivative as well as preparation method and application thereof
A technology of β-sitosterol and its derivatives, which is applied in the field of β-sitosterol derivatives and its preparation, can solve the problem of the solubility of β-sitosterol and the specific combination of β-sitosterol derivatives and avidin to construct nanoparticles, etc. problems, to achieve good clinical application prospects, convenient blood vessel administration, and convenient preparation of pharmaceutical dosage forms
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Embodiment 1
[0036] Embodiment 1 Preparation of β-sitosterol derivatives (B-BS) of the present invention
[0037] Dissolve β-sitosterol (0.15mmol) in 60ml of DMSO, under the action of dehydrating agent DCC (3.0mmol) and catalyst DMAP (3.0mmol), stir at 0°C for 6h; then add β-sitosterol at a molar ratio of 1:3 For biotin (B), raise the temperature from the ice bath to room temperature 25°C, and stir overnight in the dark. Concentrate the filtrate, recrystallize with glacial ether or isopropanol, purify by chromatography or preparative liquid phase, and freeze-dry to obtain the β-sitosterol derivative B-BS (yield is about 48%). The ion peak identified by mass spectrometry [M+H ] + For: 642.1.
[0038] 1 HNMR (400MHz, DMSO): The characteristic peaks of biotin: 10.76-10.82 (NH, 2H, broad peak), 4.47-4.65 (2C-H, 2H), 2.80-3.10 (CH 2 , 2H), 3.24(CH, 1H), 2.32(CH 2 , 2H), 1.23-1.68 (3CH 2 , 6H); The characteristic peak of β-sitosterol: 0.85-0.88 (4CH 3 , 12H), 0.99-1.03 (CH 3 , 3H), 1.08-...
Embodiment 2
[0042] Preparation of embodiment 2β-sitosterol derivative avidin nanoparticles
[0043] Get the β-sitosterol derivative (B-BS) that is equivalent to β-sitosterol 5g and prepare through embodiment 1, be dissolved in a small amount of DMSO or ethanol earlier, dilute with water for injection then, add sodium chloride 1.0g, then Add equimolar avidin (the assembly of B-BS and avidin can be assembled according to various molar ratios of 1-4:1, such as figure 2 shown), stir evenly at room temperature to obtain composite β-sitosterol derivative avidin nanoparticles, characterized by transmission electron microscopy, its nanometer size is about 25nm (such as image 3 shown).
Embodiment 3
[0044] The preparation of embodiment 3β sitosterol derivatives injection
[0045] Take the β-sitosterol derivative (B-BS) prepared by Example 1 in an amount equal to 30 g of β-sitosterol, dissolve it in water for injection, add 5.0 g of sodium chloride and stir evenly, dilute hydrochloric acid to adjust the pH=5.0, and then add 0.5% activated carbon for injection, keep the temperature at 60°C for 30 minutes, after decarbonization, add water for injection to the filtrate to 1000ml, filter through a 0.22μm sterile filter membrane, pack 2ml / branch into glass curved neck ampoules, melt seal, and circulate at 100°C Steam damp heat sterilization for 40 minutes, and then label and store.
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