Abietane type diterpenoid compound with anti-tumor effect, preparation method, pharmaceutical composition and application
An anti-tumor effect, rosinane technology, applied in the direction of anti-tumor drugs, drug combinations, medical preparations containing active ingredients, etc.
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Embodiment 1
[0037] A rosin-type diiterpene compound having an anti-tumor effect, chemical name is 12,16-epoxy-17 (15 → 16) - shifted-3, 5, 8, 12-rosettene tetrane-7, 11, 14-triketone, rosin-type diiterpene compound BracTeatum A, as shown in the following formula I:
[0038]
[0039] 1. Physicochemical properties test of the above compound BracTeatum A.
[0040] 1.1 Molecular Structure Determination
[0041] The nuclear magnetic resonance unit used for Bruker Avance III 500 nuclear magnetic resonance instrument manufactured by Bruker, using deuterated CDCl 3 (Deuterated chloroform) reagent, the hydrogen-proof and carbon spectrum data from the resultatum A obtained from the resulting rosin-type diiterpene compound is shown in Table 1 below. figure 1 , 2 Indicated.
[0042] Table 1 Hydrogens of BracTeatum A 1 H-NMR (500MHz) and carbon spectrum 13 C-NMR (125MHz) data
[0043]
[0044] Note: The chemical displacement is denoted; S means a single peak; m represents a multi-peak; DD represents...
Embodiment 2
[0050] The preparation method of rosin-type diiterpene compound BracTeatum A in Example 1, including the following steps:
[0051] (1) Crushing the wind-dried branches of 9kg of the gossy, then dipped at 70 ° C in ethanol in the volume fraction of 90%, each dip, 5 hours, ethanol added to the branches of the boss The fragmented mass is 10 mL / g, the insoluble material is filtered and the filtrate is combined, and then the temperature is 0.08 MPa, the temperature is 45 ° C under reduced pressure to dry the extract 630g;
[0052] (2) The resulting dipper and water are mixed with a mass ratio of 1: 2 to a suspension, and the equivalent acetate is extracted 3 times, combined with the extract, at a vacuum degree of 0.08 MPa, and the temperature is 45 ° C low temperature. EtOAc EtOAc EtOAc EtOAc
[0053] (3) EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc elut eluting Each gradient elution volume is 10: 1, 5: 1, 3: 1, 1: 1, 1: 3, 1: 5 and 1: 10, the volume ...
Embodiment 3
[0057] The preparation method of rosin-type diiterpene compound BracTeatum A in Example 1, including the following steps:
[0058] (1) Crushing the wind-dried branches of 9kg of the gossip, then dipped at 75 ° C in ethanol in the volume fraction of 80%, each extravasive 6 hours, the addition of ethanol is added to the branches of the boss The debris mass is 12mL / g, the insoluble material is filtered and the filtrate is mixed, and then the temperature is 0.07 MPa, and the temperature is 50 ° C under reduced pressure and evaporated.
[0059] (2) The resulting dipper and water are mixed by mass 1: 1, and the equivalent acetate is extracted 3 times, combined with the extract, at a vacuum degree of 0.07 MPa, and the temperature is 50 ° C low temperature EtOAc EtOAc EtOAc
[0060] (3) EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc elut eluting The gradient elution volume is 9.9.:1, 4.9: 1, 2.9: 1, 0.9: 1, 1: 0.9, 1: 4.9 and 1: 9.9, the volume ratio of th...
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