Santamanactone derivatives and pharmaceutical composition thereof, preparation method and application thereof
A technology of santamanide and derivatives, which is applied in the direction of drug combination, application, and pharmaceutical formula, and can solve the problems of no pharmaceutical composition, no liver fibrosis without drug composition, no santamanide derivatives, etc.
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Embodiment 1
[0020] The preparation of santamanactone derivatives of the present invention:
[0021] One. The synthesis of monoesterification santamanolactone (compound 1-18):
[0022] At room temperature, the corresponding acid (0.16 mmol) was dissolved in 1 mL of dichloromethane and added to a 10 mL round-bottomed flask, and 28 μL of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide ( EDCI, 0.16 mmol), 1 mg p-dimethylaminopyridine (DMAP, 0.02 mmol), 20 mg santamanide (0.08 mmol). After reacting for 2 h, 5% HCl aqueous solution was added to quench the reaction, dichloromethane (3 mL) was extracted three times, the organic phases were combined, dried over anhydrous sodium sulfate, concentrated under reduced pressure to remove the solvent, and then subjected to silica gel column chromatography, and acetone-petroleum ether (10 :90, v / v) elution.
[0023] 1-O-octanoylsantamane lactone (compound 1) structural data:
[0024] Molecular formula: C 23 h 35 o 4
[0025] Molecular weight: 374.52 ...
Embodiment 2
[0173] Cytotoxic activity of santamanide derivatives 1-21 against the human hepatic stellate cell line HSC-LX2.
[0174] 1. Materials and Methods
[0175] 1.1 Materials
[0176] Human hepatic stellate cells line LX2 (HSC-LX2) was purchased from Shanghai Ji Ning Biotechnology Co., Ltd.; RPMI-1640 medium and fetal bovine serum were purchased from Gibco BRL (NY, USA); MTT was purchased from Guangzhou Saiguo Biotechnology Co., Ltd.
[0177] 1.2 Instruments
[0178] Flex Station 3 desktop multifunctional microplate reader (Bio-RAD 680, USA); analytical balance (AG135, Metler Toledo, China); incubator (DHP-9082, Shanghai).
[0179] 1.3 Experimental process
[0180] MTT method was used to measure the toxic activity of samples on HSC-LX2 cells. HSC-LX2 cells were cultured in RPMI-1640 medium containing 10% fetal bovine serum. Cells grown in logarithmic phase were taken at 1×10 4 Inoculate in a 96-well plate at the density of each well, and replace the maintenance solution with ...
preparation Embodiment 1-7
[0189] In the following preparation examples, conventional reagents are selected, and preparations are prepared according to existing conventional methods. This application example only reflects that at least one of the compounds 1-21 of the present invention can be prepared into different preparations. For specific reagents and The operation is not specifically limited:
[0190] 1. With at least one of the compounds 1-21 prepared in Example 1, after dissolving with DMSO, add water for injection according to a conventional method, fine filter, potting and sterilizing to make an injection, the concentration of the injection is 0.5 -5 mg / mL.
[0191] 2. After dissolving at least one of the compounds 1-21 prepared in Example 1 with DMSO, dissolve it in sterile water for injection, stir to dissolve it, filter it with a sterile suction filter funnel, and then sterilize it. filtered, divided into ampoules, freeze-dried at low temperature and sealed aseptically to obtain a powder inje...
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