Artatrovirenols A-B as well as pharmaceutical composition, preparation method and application of artatrovirenols A-B
A technique of artemisinol and medicine, applied in the field of medicine, can solve the problems of no report of the pharmaceutical composition, no report of the application of liver cancer drugs of the pharmaceutical composition and the like
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Embodiment 1
[0025] Preparation of compound 1-2:
[0026]Take the dried aerial part of Artemisia annua, crush it with 10 times the amount of 90% ethanol for cold soaking and extraction twice, combine the ethanol extracts and concentrate under reduced pressure until there is no alcohol smell to obtain the ethanol extract, disperse the extract in water, and wash with acetic acid Ethyl was extracted 3 times to obtain the ethyl acetate extraction fraction, which was subjected to silica gel column chromatography, and acetone-petroleum ether (10:90, 30:70, 50:50, v / v) and acetone were used for gradient Eluted to get 3 fractions Fr.1~Fr.3; Fr.2 was obtained by silica gel column chromatography (ethyl acetate-petroleum ether, 10:90, 20:80, 40:60, 100:0, v / v) 4 components Fr.2-1~Fr.2-4; Fr.2-2 were chromatographed by medium pressure MCICHP 20P column, water-methanol (50:50,30:70,10:90,0:100) Gradient elution obtained 4 fractions Fr.2-2-1~Fr.2-2-4; Fr.2-2-1 was subjected to silica gel column chromat...
Embodiment 2
[0057] In the previous work of the present invention, it was found that the 90% ethanol extract of the dry aerial part of Artemisia annua had certain cytotoxic activity to three strains of liver cancer cells (HepG 2, Huh7, SMMC-7721), and further isolated 2 pairs of Three liver cancer cell lines have cytotoxic activity of sesquiterpenoids, Artatrovirenols A-B (Artatrovirenols A-B, 1-2).
[0058] Cytotoxic activity of compounds 1-2 against liver cancer cell lines.
[0059] 1. Materials and Methods
[0060] 1.1 Materials
[0061] Liver cancer cell lines (HepG2, Huh7 and SMMC-7721) were purchased from Shanghai Ji Ning Biotechnology Co., Ltd.; medium (Dulbecco's Modified Eagle Medium, DMEM) was purchased from Thermo Fisher Scientific (Suzhou, China); serum (fetal bovine serum, FBS ) was purchased from Life Technologies (NY, USA); RPMI-1640 was purchased from ThermoFisher Biochemical Products (Beijing, China).
[0062] 1.2 Instruments
[0063] Flex Station 3 desktop multifuncti...
preparation Embodiment 1-7
[0080] In the following preparation examples, conventional reagents are selected, and the preparations are prepared according to existing conventional methods. This application example only reflects that at least one of the compounds 1-2 of the present invention can be prepared into different preparations. For specific reagents and The operation is not specifically limited:
[0081] 1. With at least one of the compounds 1-2 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 ~5mg / mL.
[0082] 2. After at least one of the compounds 1-2 prepared in Example 1 is dissolved in DMSO, it is dissolved in sterile water for injection, stirred to dissolve it, filtered with a sterile suction filter funnel, and then sterile purified. filtered, divided into ampoules, freeze-dried at low temperature and sealed aseptically to obtain a...
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