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Application of resveratrol in preparing anti-SARS-CoV-2 (severe acute respiratory syndrome-coronavirus-2) medicine

A technology of resveratrol and sars-cov-2, which is applied in the field of medicinal chemistry, can solve the problems of no more than 10%, enhance the stability of insoluble drug solutions, and have no clarity, achieve high drug loading, and improve the surface Effect of charge, high solubility

Inactive Publication Date: 2020-06-02
南京大渊医美生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, limited to the principle of cyclodextrin inclusion, RES molecules and cyclodextrin can only theoretically exist in a molar ratio of 1:1, but in practice, because the inclusion efficiency of cyclodextrin is generally lower than 100 %, so the molar content of cyclodextrin is generally higher than that of RES
This has brought about an obvious problem: since the molecular weight of cyclodextrin is much higher than that of RES, the solid content of RES in the final RES clathrate is limited to a low level, generally not higher than 10%. That is to say, in order to promote the solubilization of RES, nearly 90% of substances without any physiological activity have to be added, which is not an efficient loading method
However, according to our research, in the existing research on the three-phase material formed by drug + solid dispersion + cyclodextrin, there is no clear effective means to enhance the solution stability of poorly soluble drugs

Method used

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  • Application of resveratrol in preparing anti-SARS-CoV-2 (severe acute respiratory syndrome-coronavirus-2) medicine
  • Application of resveratrol in preparing anti-SARS-CoV-2 (severe acute respiratory syndrome-coronavirus-2) medicine
  • Application of resveratrol in preparing anti-SARS-CoV-2 (severe acute respiratory syndrome-coronavirus-2) medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1: protein structure preparation

[0050] Obtain the newly analyzed complex crystal structure of the new coronavirus 3CL protease from the PDB protein structure database (Protein Data Bank, PDB) (ID: 6LU7), delete the water molecules and small molecular compounds in it, and leave the protein structure to obtain SARS - Three-dimensional high-resolution crystal structure of CoV-2 coronavirus 3CL hydrolase (Mpro).

[0051] We used the published conformation of the hydrolase unique to the new coronavirus itself (this hydrolase is different from the hydrolase of previous viruses such as SARS), combined with the molecular conformation of RES, to simulate docking, and found that RES can be in the hydrolase. Key sites form effective docking. Therefore, RES may be able to be used against novel coronaviruses.

[0052] Small Molecule Compound Docking

[0053] Use the MGL Tools software package to process the protein structure, add hydrogen, add Kollman charges, add Ga...

Embodiment 2

[0059] The problem to be solved is that we hope to increase the water solubility of RES in order to improve its solubility in water and increase the killing effect on coronaviruses. Therefore, we tried the solubility after using several auxiliary materials and RES to form complexes alone, and found that several auxiliary materials were better for increasing the solubility of RES. This step is actually used to screen which material is better for solubilizing RES and maintaining solution stability.

[0060] For the comparison of single-factor solubilization techniques (percentages are mass fractions), the prescriptions are shown in Table 1.

[0061] Table 1 Comparison of single-factor solubilization technology prescriptions

[0062]

[0063]

[0064] According to the prescription, weigh each substance in proportion to obtain a mixture with a total mass of M. The mass concentration of weighing 30 times that of M is 98% ethanol, the mixture is dissolved in the ethanol, hea...

Embodiment 3

[0072] We use the two materials with better solubilization effect screened in Example 2, namely HP-β-CD or HPMCAS-M to make a binary complex, that is, to form RES-HP-β-CD or RES-HPMCAS -M, the main purpose of this step is to judge which material has a better RES "capacity" by increasing the RES content, that is, which material can hold more RES, which is mainly used to consider the preparation of high solid content RES is set. The method is: according to the prescription listed in Table 3, in the mode of A+B or A+C, each substance is weighed in proportion to obtain a mixture with a total mass of M. The mass concentration of weighing 30 times that of M is 98% ethanol, the mixture is dissolved in the ethanol, heated to 50° C. and stirred to dissolve to form a clear and transparent solution, and the organic solvent is quickly volatilized and removed by a vacuum rotary evaporator to obtain White powdery solid product. RES solid content climbing test (percentage is mass fraction)...

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Abstract

The invention belongs to the field of medicine chemicals and in particular relates to application of resveratrol in preparing an anti-SARS-CoV-2 (severe acute respiratory syndrome-coronavirus-2) medicine. According to the application, in-vitro cell level experiments show that a prepared novel high-solubility quick-release RES (resveratrol) preparation has a certain inhibition function on SARS-CoV-2, the inhibition function is prior to that of RES which is independently used, and possibility of clinical use can be achieved. In the preparation, super-saturation formation modes are concluded intothree principles in mutual combination and mutual synergism, that is, the RES is formed at an amorphous molecular state by using a water-soluble high polymer material, a part of the RES at the molecular state is wrapped by using cyclodextrin and is distributed to the surface of the water-soluble high polymer material, and charges on the surface of a medicine-high polymer material complex are improved by using surfactants such as phospholipid and sodium cholate.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the application of resveratrol in the preparation of anti-SARS-CoV-2 virus drugs. Background technique [0002] Since SARS-CoV-2 is a new strain of coronavirus that has never been found in humans before, there is currently no specific treatment for the disease caused by the new coronavirus. At present, many research groups at home and abroad are focusing on finding chemical drugs or active ingredients of traditional Chinese medicine that may have a therapeutic effect on SARS-CoV-2, but there is no definite conclusion yet. [0003] Resveratrol (Resveratrol, RES) is a natural polyphenolic substance with strong biological activity, mainly derived from grapes, knotweed, peanuts, mulberries and other plants. Existing findings show that RES has a variety of pharmacological effects, including anti-tumor, cardiovascular protection, blood lipid lowering, anti-bacterial and anti-infla...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61K47/24A61K47/28A61K47/38A61K47/69A61K9/20A61K9/16A61K9/48A61P31/14A61P11/00
CPCA61K9/1617A61K9/1652A61K9/2013A61K9/2054A61K9/4858A61K9/4866A61K31/05A61K47/6951A61P11/00A61P31/14
Inventor 王台虎黄和赵万洲
Owner 南京大渊医美生物技术有限公司
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