Application of agarotetrol in preparation of medicine for treating vascular dementia diseases
A technology for vascular dementia and agarwood tetraol, applied in the field of medicine, can solve the problems such as no reports of agarwood tetraol, and achieve the effects of no toxic side effects, convenient use, and behavioral improvement.
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Embodiment 1
[0021] The preparation of agaratetrol (PFC24):
[0022] Dried Chinese medicine Agarwood (2.9kg) was pulverized, 90% ethanol (10L) was ultrasonically extracted at 60°C for 30min, repeated 5 times, and the extract was concentrated to obtain extract (459.3g). The extract was then suspended in 1L of water, extracted five times with equal volumes of petroleum ether and ethyl acetate, and the solvent was recovered to obtain petroleum ether extraction fraction (0.7g) and ethyl acetate extraction fraction (374.8g).
[0023] Mix the sample with an equal amount of 80-100 mesh silica gel for the ethyl acetate extraction part, divide the section through normal phase silica gel column chromatography, and first use petroleum ether-ethyl acetate mixed solvent (50:1, 30:1, 20:1, 10:1, 5:1, 3:1, 2:1, 1:1, 0:1, v / v) for gradient elution, on the same column, followed by gradient elution with ethyl acetate-methanol Off (5:1, 3:1, 2:1, 1:1, 0:1, v / v). Ethyl acetate-methanol elution (5:1, 3:1, v / ...
Embodiment 2
[0025] Spectral data of agarotetrol (PFC24): colorless solid, CAS registration number 69809-22-9, molecular formula C 17 h 18 o 6 ;[α] D 18 -17.9 (c 0.20, MeOH); 1 H NMR (methanol-d 4 ,500MHz)δ H 7.24 (5H, m, H-2′~6′), 6.13 (1H, s, H-3), 4.73 (1H, d, J=4.0Hz, H-5), 4.55 (1H, d, J= 7.4Hz, H-8), 4.03(1H,dd,J=7.4,2.4Hz,H-7),4.00(1H,dd,J=4.9,2.4Hz,H-6),3.04(2H,t, J=7.8Hz,H 2 -7′),2.94(2H,m,H 2 -8'); 13 C NMR (methanol-d 4 ,126MH Z )δ C 182.0 (C, C-4), 171.2 (C, C-2), 165.4 (C, C-8a), 141.2 (C, C-1′), 129.6 (CH, C-3′, C-5′ ), 129.4 (CH, C-2′, C-6′), 127.4 (CH, C-4′), 121.8 (CH, C-4a), 114.1 (CH, C-3), 74.0 (CH, C -6),72.4(CH,C-7),70.1(CH,C-8),66.7(CH,C-5),36.3(CH 2 ,C-8′),33.7(CH 2 , C-7′). Its spectral data is consistent with literature [Yoshii E, Koizumi T, Oribe T, Takeuchi F, Kubo K. The structure of agarotetrol, a novel highlyoxygenated chromone from agarwood (jinko). Tetrahedron Letters, 1978, 19, 3921-3924], chemical structural formula figure 1 shown.
Embodiment 3
[0027] Acute toxicity test of PFC24 in mice.
[0028] 1. Experimental materials
[0029] (1) Experimental reagents: PFC24, physiological saline.
[0030] (2) Equipment: electronic balance, syringe, gavage needle.
[0031] (3) Grouping of experimental animals: 1) Fasting for 12 hours before administration, age of mice: 7-9 weeks, observation for one week after the first dose administration. 2) 30 Kunming rats, half male and half female, 6 rats in each group of normal group, 10mg / kg group, 20mg / kg group, 50mg / kg group, and 100mg / kg group, fasted for 12h before administration, age of rats: 7 ~9 weeks, observe for one week after the first dose.
[0032] 2. Experimental steps
[0033] (1) Experiment preparation stage: Compound concentration 5mg / mL (0.4-0.5mL / 20g, based on 0.4mL / 20g is calculated as the maximum amount of gavage) physiological saline was prepared as a solvent, and the control group was not administered.
[0034] (2) Formal experiment: administration was performe...
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