Dihydroxydibenzo[b,f][1,5]dioxocine compound, and preparation method, pharmaceutical composition and application thereof
A technology of dihydroxydiphenyl and dioxa, which is applied in the field of chemistry and can solve the problems of limited application and effect of cancer chemical drug treatment, poor selectivity, and drug resistance of cancer cells.
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Embodiment 1
[0083] Example 1: Compound 3-ethoxy-10-formyl-9-hydroxy-4,7-dimethyl-6,12-dioxo-6,12-dihydroxydibenzo [b,f][1,5]Dioxocane-1-carboxylic acid extraction, separation and structure identification.
[0084] 1. Extraction and Isolation from Lichen Plants
[0085] Step (1): Naturally dry lichen hongxue tea, crush it, extract with ethanol with a volume concentration of 60%-70% as the extraction solvent, and concentrate the extract to obtain a paste-like AMH primary extract
[0086] Step (2), mix the initial AMH extract and distilled water at a volume ratio of 1:1 to obtain the first suspension; then mix the first suspension with ethanol or absolute ethanol with a volume concentration of 95% to ethanol The final volume concentration is greater than 80%. After shaking, let it stand for alcohol precipitation, separate the ethanol extract from the upper layer, and concentrate the ethanol extract to obtain the paste-like primary anticancer efficacy part AMH-A;
[0087] Step (3), mix AMH-...
Embodiment 2
[0101] Example 2: Compound 3-ethoxy-10-formyl-9-hydroxy-4,7-dimethyl-6,12-dioxo-6,12-dihydroxydibenzo Biological experimental results of [b,f][1,5]dioxocane-1-carboxylic acid's antitumor effect, combined antitumor effect, toxicological safety and antitumor mechanism
[0102] The following are some specific experimental examples to illustrate the formula (1) compound 3-ethoxy-10-formyl-9-hydroxyl-4,7-dimethyl-6,12-dioxo-6,12- Dihydroxydibenzo[b,f][1,5]dioxocane-1-carboxylic acid (indicated by A in the chart below, the same below) has significant, selective, cell-targeted anti-tumor effects , as well as the combined anti-tumor effect with clinical anti-tumor drugs, its toxicological safety and anti-tumor mechanism.
[0103] 1. The effect of compound A on inhibiting and killing human cancer cells in vitro:
[0104] In vitro anti-tumor test method: Compound A is dissolved in analytically pure DMSO, and the final concentration is 0, 1, 2, 4, 8, 16 µg / ml (or 0, 2.5, 5, 10, 20, 30,...
Embodiment 3
[0142] Example 3: Compound 3-ethoxy-10-formyl-9-hydroxy-4,7-dimethyl-6,12-dioxo-6,12-dihydroxydibenzo [b,f][1,5]dioxocane-1-carboxylic acid anticancer mechanism
[0143] 1. Promote the apoptosis of cancer cells
[0144] Using Western Blot detection, it was found that compound A of formula (1) can significantly promote the formation of CleavedPARP, a marker of cancer cell apoptosis, and the results are shown in Figure 22 .
[0145] 2. Effects on the growth cycle of cancer cells
[0146] Experimental method: after liver cancer cell HepG2 was treated with compound A of formula (1) for 48 hours, the cell cycle and apoptosis were detected by flow cytometry (FACS). The results are shown in Table 5.
[0147] Results: Compound A of formula (1) can significantly affect the differentiation and cycle of cancer cells, arrest cells in G1 phase, and reduce cells in S phase during division.
[0148] Table 3. Effects on cell cycle (FCM, HepG2)
[0149]
[0150] 3. Effect on gene exp...
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