Sesquiterpene in wild mugwort and its pharmaceutical composition and its preparation method and application
A sesquiterpene and composition technology, applied in the direction of drug combination, pharmaceutical formula, medical preparations containing active ingredients, etc., can solve the problem that there is no anti-hepatic fibrosis drug of compound 1-13 and its pharmaceutical composition
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Embodiment 1
[0023] Preparation of Compound 1-13:
[0024]The dry aerial part of Artemisia chinensis is crushed, extracted by cold soaking with 95% ethanol twice, each time for 4 days, the ethanol extracts are combined, and the ethanol extract is recovered under reduced pressure. The extract was dispersed in water and extracted with ethyl acetate, then concentrated to the ethyl acetate extract. Then the ethyl acetate extract was subjected to silica gel column chromatography with ethyl acetate-petroleum ether (0:100, 5:95, 10:90, 20:80, 40:60 and 100:0) as the eluent gradient Elution gave six fractions of Fr.A-Fr.F. Fraction Fr.C was subjected to silica gel column chromatography (acetone-petroleum ether, 5:95, 10:90 and 20:80) to obtain three fractions Fr.C1-Fr.C3. Fraction Fr.C1 was subjected to MCI gelCHP 20P column chromatography (water-methanol, 10:90 and 0:100) and semi-preparative HPLC (water-acetonitrile, 30:70) to obtain compound 13 (12 mg). Fraction Fr.C2 was subjected to MCI ge...
Embodiment 2
[0162] Cytotoxic activity of compounds 1-13 against HSC-LX2.
[0163] 1. Materials and Methods
[0164] 1.1 Materials
[0165] 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.
[0166] 1.2 Instruments
[0167] Flex Station 3 desktop multifunctional microplate reader (Bio-RAD 680, the United States); analytical balance (AG135, Metler Toledo, China); incubator (DHP-9082, Shanghai).
[0168] 1.3 Experimental process
[0169] 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 the culture medium containing differe...
preparation Embodiment 1-7
[0179] 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 1-13 of the present invention can be prepared into different preparations. For specific reagents and The operation is not specifically limited:
[0180] 1. With at least one of the compounds 1-13 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.
[0181] 2. After dissolving at least one of the compounds 1-13 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 in...
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