Antineoplastic pharmaceutical composition and application thereof
A technology of anti-tumor drugs and compositions, applied in the field of medicine, to achieve the effects of convenient operation, reduced toxicity, and reduced damage
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Embodiment 1
[0038] Embodiment 1: the preparation method of oridonin
[0039] Dried the aboveground part (9kg) of Rubescens japonicus, refluxed and extracted with 10 times the amount of 95% ethanol solution for 3 times, each time for 2 hours, and recovered the obtained ethanol extract until it had no alcohol smell to obtain the extract. The extract was dissolved in water, degreased with an equal volume of petroleum ether, and then extracted with an equal volume of ethyl acetate to obtain 180 g of ethyl acetate layer extract. Afterwards, the ethyl acetate layer extract was separated by silica gel column chromatography, and dichloromethane and methanol were used in volumes of 100:0, 100:1, 100:2, 100:3, 100:5, 100:7, and 100:10. By continuous elution, the crude product of oridonin was obtained, and white needle crystals (3g) were obtained by recrystallization.
[0040] The white needle crystals (MeOH) were positive for the reaction of vanillin-concentrated sulfuric acid. Combined with 1H a...
Embodiment 2
[0047] Example 2: Molecular docking
[0048] 1 Experimental method
[0049] Molecular docking of Rubescensin A and EGFR was carried out using Autodock4.23 molecular docking software, and the binding free energy of Rubescensin A and EGFR was obtained.
[0050] 2 Experimental results
[0051] Depend on figure 1 It can be seen that Rubescensin A binds to Lys721 and Asp831 of EGFR in the form of hydrogen bonds, and binds to Val702, Leu694 and Leu820 in the form of hydrophobic bonds. The binding free energy of oridonin A to EGFR is -8.34kcal / mol, and its binding site is the intracellular ATP binding site of EGFR (Cell, 2006, 125:1137-1149). Normally, the binding free energy predicted by Autodock reaches -9kcal / mol, which means that the affinity can reach the nM level. The molecular docking research results combined with the previous experimental research results suggest that Rubescensin A has a strong binding ability to EGFR.
Embodiment 3
[0052] Example 3: The growth inhibitory effect of cetuximab combined with oridonin on human laryngeal squamous cell carcinoma HEp-2 cells and Tu212 cells
[0053] 1 Experimental method
[0054] (1) MTT assay for cell proliferation: HEp-2 and Tu212 cells were inoculated in RPMI-1640 medium containing 10% fetal bovine serum, 1×105 U / L penicillin and 100 g / L streptomycin, in a 5% CO2 incubator , cultured at 37°C. HEp-2 and Tu212 cells in the logarithmic growth phase were seeded in 96-well plates at 3×104 and 5×104 cells per well, respectively. After culturing for 24 hours, cetuximab at concentrations of 0, 1, 10, and 100 μg / mL and 0, 12, 24, and 36 μM oridonin were added. Three replicate wells were set up for each group, and a negative control was set up at the same time. Place in a 5% CO2 incubator at 37°C for 24 and 48 hours. Add 100 μL of 5 mg / mL MTT to each well, and after culturing for 2.5 hours, carefully discard the culture medium in the well, add 150 μL of DMSO to eac...
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