Application of polyguluronic acid sulfate in the preparation of anti-hepatitis B virus medicine
A technology of guluronic acid sulfate and hepatitis B virus, which is applied in the field of marine drugs, can solve the problems of many adverse reactions, easy relapse after drug withdrawal, virus mutation and drug resistance, etc., and achieve enhanced production and secretion, enhanced Innate immunity, effects of suppressed expression
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Examples
Embodiment 1
[0030] Embodiment 1, structure and physicochemical property analysis of polyguluronic acid sulfate
[0031] The acid degradation method adopted in the present invention prepares and separates polyguluronic acid from seaweed polysaccharide alginate, and then obtains polyguluronic acid sulfate after sulfation reaction (recorded in the patent ZL 200310105718.9 that polyguluronic acid The preparation method of glucuronic acid sulfate PGS).
[0032] The molecular skeleton of the polyguluronic acid sulfate ester of the present invention is composed of α-L-guluronic acid connected by 1→4, and C in the sugar residue 2 and C 3 bits have at least one SO 3 Na, the content of sulfate is 20%~40%; the weight average molecular weight of polyguluronic acid sulfate is 2 kDa~20 kDa; its general molecular formula can be expressed as [C 12 h 16-m o 12 Na 2 ·(SO 3 Na) m ] n , where m=1~4, n=5~30.
[0033] The carbon NMR spectrum of polyguluronic acid sulfate is as follows figure 1 Shown...
Embodiment 2
[0036] Embodiment 2, the anti-hepatitis B virus effect of polyguluronic acid sulfate PGS in vitro
[0037] 1) Evaluation of the effect of PGS on inhibiting the expression of HBsAg and HBeAg at the cellular level
[0038] Using the HepG2.2.15 cell line (provided by the School of Medicine, Ocean University of China) as a cell model, ELISA kits and thiazolium blue (MTT) colorimetry were used to detect the inhibition of polyguluronic acid sulfate PGS on the expression of HBsAg and HBeAg Effect and cytotoxicity, and calculate the half toxic concentration CC 50 value. Positive control drug selection lamivudine.
[0039] Experimental results such as image 3 and Figure 4 shown. Such as image 3 As shown, PGS (30-250 µg / mL) has no obvious inhibitory activity on the proliferation of HepG2.2.15 cells, and the maximum non-toxic concentration is 250 µg / mL after PGS acts on the cells for 6 days. After 6 and 9 days of PGS, CC 50 The values were 931 µg / mL and 891 µg / mL, respective...
Embodiment 3
[0047] Embodiment 3, the action mechanism of PGS anti-hepatitis B virus in vitro
[0048] 1) Effect of PGS on the expression and secretion of interferon β (IFNβ)
[0049] The effect of PGS on the expression of cytokines and antiviral proteins (such as IFNβ) in HepG2.2.15 cells was evaluated by ELISA method. After HepG2.2.15 cells were treated with different concentrations of PGS (50, 100, 200 and 400 μg / mL) for 6 days, the supernatant was changed every 3 days, and the supernatant and cells were collected on the 6th day. The IFN-β in the cell culture supernatant and cell lysate was determined according to the instructions of the ELISA kit.
[0050] Experimental results such as Figure 6 As shown, compared with the control group, after treatment with different concentrations of PGS (100, 200 and 400 µg / mL), the expression of IFN-β in the cells was significantly increased (P Figure 6 A). At the same time, when the concentration reached 400 µg / mL, PGS significantly increased th...
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Abstract
Description
Claims
Application Information
- IPC
- A61K31/737; A61P31/20; A61P35/00
- CPC
- A61K31/737
- Inventors
- 赵峡; 王伟