Preparation and application of alpha-glucosidase induced and released NO donor
A technology of glucosidase and glucose, which is applied in the preparation of sugar derivatives, medical preparations of non-active ingredients, sugar derivatives, etc., can solve problems such as lowering blood pressure, achieve the effect of improving oral availability and realizing intelligent response
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Embodiment 1
[0054] Example 1: Small molecule α-glucosidase induces the release of NO donor synthesis method, the synthesis route is as follows:
[0055]
[0056] Step 1: Dissolve compound a (1.0eq.) and compound b (2eq.) of formula 1 in dry DCM, add BF under argon protection 3 .Et 2 O (3eq.), reflux reaction at 45°C for 48h; after the reaction is completed, add an appropriate amount of saturated NaHCO 3 After quenching the reaction, after extraction, drying, filtration, and spin-drying, the crude product was separated and purified by silica gel column chromatography to obtain the target compound c, which was a compound with a structure such as formula 5. Compound c was a yellow oil with a yield of 40 %-60%.
[0057] Step 2: Dissolve compound c (1.0eq.), NBS (1.5eq.) and initiator BPO (0.1eq.) in CCl 4 , Heated to reflux at 78°C for 6h under the protection of argon. After the reaction is completed, cooling, filtering, and spin-drying of the filtrate give the crude product, which is se...
Embodiment 2
[0075] Example 2: Macromolecule α-glucosidase induces the release of NO donor synthesis method, the synthesis route is as follows:
[0076]
[0077] Step 1: Dissolve compound a (1.0eq.) and compound b (2eq.) of formula 1 in dry DCM, add BF under argon protection 3 .Et 2 O (3eq.), reflux reaction at 45°C for 48h; after the reaction is completed, add an appropriate amount of saturated NaHCO 3 After quenching the reaction, after extraction, drying, filtration, and spin-drying, the crude product was separated and purified by silica gel column chromatography to obtain the target compound c, which was a compound with a structure such as formula 5. Compound c was a yellow oil with a yield of 40 %-60%.
[0078] Step 2: Dissolve compound c (1.0eq.), NBS (1.5eq.) and initiator BPO (0.1eq.) in CCl 4 , Heated to reflux at 78°C for 6h under the protection of argon. After the reaction is completed, cooling, filtering, and spin-drying of the filtrate give the crude product, which is s...
Embodiment 3
[0083] Example 3: Effect of NO Donor Drugs on Oral Absorption of P-gp Substrate Drugs
[0084] The α-glucosidase prepared in Example 1 or 2 induces the release of NO donor drug and doxorubicin, paclitaxel, and camptothecin anticancer drugs are administered to mice at the same time, and a blank comparison experiment is performed at the same time. Through ICR mice Pharmacokinetic experiments were conducted to study the effect of α-glucosidase-induced release of NO donors on the oral availability of the drug. The result is as Figure 1-3 As shown, the results show that NO donor drugs can significantly increase the oral bioavailability of doxorubicin and increase its effective time; paclitaxel and camptothecin may be due to the low oral bioavailability, and the NO donor for the above two drugs Oral bioavailability has little effect.
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