Preparation method and application of an ivy saponin STING pathway inhibitor
By synthesizing STING pathway inhibitor derivatives through chemical modification of ivy saponins and aromatic compounds, the problems of high protein consumption, high cost and complex target identification in existing technologies have been solved, realizing the preparation of STING pathway inhibitors in a highly efficient and economical manner, and enhancing the efficiency and purity of drug development.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- BEIJING UNIV OF CHINESE MEDICINE
- Filing Date
- 2024-12-04
- Publication Date
- 2026-06-05
AI Technical Summary
Existing technologies for studying hederone saponin STING pathway inhibitors suffer from problems such as high protein consumption, high cost, complex target identification, and limitations of in vitro models, which affect research efficiency and accuracy.
By chemically modifying ivy saponins and aromatic compounds, and employing reflux reaction, thin-layer chromatography monitoring, and silica gel column chromatography, a highly efficient STING pathway inhibitor derivative was synthesized, simplifying the preparation process and improving purity.
It reduced experimental costs, improved drug development efficiency and yield, enhanced STING pathway inhibitory activity, and provided new drug candidates for the treatment of related diseases.
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Figure CN122145542A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of biomedical technology, specifically to a method for preparing and applying an inhibitor of the hederone saponin STING pathway. Background Technology
[0002] The innate immune response recognizes pathogen-associated pattern molecules (PAMPs) through pattern recognition receptors, promoting the expression of cytokines such as type I interferon (IFN-I), and plays a key role in the body's defense against pathogens. The cGAS-STING pathway, as an important immune regulatory mechanism, is closely related to various inflammatory processes and autoimmune diseases due to its abnormal activation. Hederogenin, as a natural pentacyclic triterpenoid compound, has a variety of pharmacological activities. Previous studies have found that it can effectively inhibit the STING signaling pathway, but the inhibitory activity is weak. Therefore, the development of highly efficient and specific STING pathway inhibitors is of great significance.
[0003] While existing technologies for studying the STING pathway inhibitory activity of hederonegenin employ methods such as chemical modification, molecular docking, and cell models, they still suffer from several significant drawbacks. First, the large amount of protein consumed is a significant issue. To verify the interaction between hederonegenin and STING protein, large quantities of purified STING protein are required, increasing experimental costs and potentially leading to material shortages. Second, high cost is another major limitation. From chemical modification to molecular docking and cell model experiments, each step requires expensive reagents and equipment, keeping research costs high and limiting widespread application. Furthermore, the complexity of target identification is a pressing issue. Due to the complexity of signaling pathways in vivo, identifying the precise target of hederonegenin requires tedious experimental verification and data analysis, increasing experimental difficulty and potentially affecting the accuracy of results. Finally, the limitations of in vitro models are a major bottleneck. While cell models can simulate the in vivo environment to some extent, they cannot fully replicate the complexity of real organisms, potentially leading to biased results that require further verification in animal models or human experiments. Summary of the Invention
[0004] The purpose of this invention is to synthesize derivatives with high efficiency in inhibiting STING pathway activity by chemically modifying hederogenin for the treatment of immune and inflammation-related diseases. This invention proposes a method for preparing and applying hederogenin STING pathway inhibitors.
[0005] The technical solution of the present invention to solve the above-mentioned technical problems is as follows:
[0006] A method for preparing an inhibitor of the hederaponin STING pathway includes the following steps:
[0007] S10. Take an appropriate amount of ivy saponin and aromatic compounds, add N,N-dimethylformamide as a reaction solvent, and add an appropriate amount of K2CO3.
[0008] S20. Stir the reaction under reflux for a certain period of time, and monitor the reaction progress by thin-layer chromatography until the reaction is complete.
[0009] S30. After the reaction is complete, N,N-dimethylformamide is evaporated to dryness under reduced pressure, the residue is dissolved in dichloromethane, and then extracted and washed successively with deionized water and saturated brine.
[0010] S40. Collect the organic layer, dry it with anhydrous sodium sulfate, filter it, and evaporate it under reduced pressure to obtain the crude product.
[0011] S50. The crude product is separated and purified by silica gel column chromatography to obtain the target compound, namely the STING pathway inhibitor derivative.
[0012] Based on the above technical solution, the present invention can be further improved as follows.
[0013] Furthermore, the aromatic compound is benzyl bromide.
[0014] Furthermore, in step S10, the concentrations of both hederaponin and aromatic compounds are 1 mM, and the volume of N,N-dimethylformamide (DMF) is 15 mL.
[0015] Furthermore, in step S20, the temperature of the heating reflux is 85°C, and the reaction time is 4 hours.
[0016] Furthermore, in step S30, the silica gel column chromatography is Flash silica gel column chromatography, and the target compound obtained is a white solid with a yield of 88%.
[0017] Furthermore, the structure of the compound was confirmed by proton NMR spectroscopy, carbon NMR spectroscopy, and high-resolution mass spectrometry.
[0018] An application of an ivy saponin STING pathway inhibitor, wherein the derivative is used to inhibit the expression of IFN-β, and its STING pathway inhibitory activity is screened at the cellular level by constructing a luciferase reporter gene model, and its STING pathway inhibitory activity is characterized by the effect of the derivative on the expression level of IFN-β, a downstream molecule of the STING pathway.
[0019] Compared with the prior art, the technical solution of this application has the following beneficial technical effects:
[0020] This invention provides a more economical and efficient preparation method. Through chemical synthesis, ivy saponins are combined with aromatic compounds to generate a series of novel STING pathway inhibitor derivatives. This method not only reduces the reliance on large-scale purification of STING protein, thus lowering experimental costs, but also enhances the STING pathway inhibitory activity of ivy saponins through chemical modification, improving drug development efficiency. Secondly, this invention employs thin-layer chromatography (TLC) to monitor the reaction process, ensuring complete and controllable reaction. This technical feature not only improves the accuracy of the preparation process but also helps optimize reaction conditions, further reducing costs and increasing yield. Precise control of reaction time avoids unnecessary waste of raw materials and energy consumption. Furthermore, this invention uses silica gel column chromatography for separation when preparing STING pathway inhibitor derivatives. Purification, a key technical feature, not only simplifies the preparation process but also improves the purity and quality of the product. Silica gel column chromatography effectively removes impurities and unreacted raw materials, resulting in a higher purity target compound. This facilitates subsequent drug activity evaluation and preclinical studies, providing strong support for drug development and application. Furthermore, the preparation method of this invention is not only suitable for laboratory-scale research but also has the potential for industrial production. By optimizing reaction conditions and purification processes, large-scale production of high-quality STING pathway inhibitor derivatives can be achieved. This helps reduce drug production costs, improve drug accessibility and cost-effectiveness, and provide more options for the treatment of related diseases. In summary, this method not only improves drug preparation efficiency and purity but also reduces experimental and production costs, providing new drug candidates and development pathways for the treatment of STING pathway-related diseases. Attached Figure Description
[0021] Figure 1 This is a flowchart of a method for preparing an inhibitor of the STING pathway of ivy saponin.
[0022] Figure 2 This is a schematic diagram of the general formula 1 of the present invention. Detailed Implementation
[0023] The technical solutions of the embodiments of the present invention will be clearly and completely described below with reference to the accompanying drawings. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention.
[0024] A method for preparing an inhibitor of the hederaponin STING pathway includes the following steps:
[0025] S10. Take an appropriate amount of ivy saponin and aromatic compound, add N,N-dimethylformamide as a reaction solvent, and add an appropriate amount of K2CO3. The aromatic compound is benzyl bromide. In step S10, the concentration of ivy saponin and aromatic compound is 1mM, and the volume of N,N-dimethylformamide (DMF) is 15mL.
[0026] S20. Stir the reaction under reflux for a certain period of time, and monitor the reaction progress by thin-layer chromatography until the reaction is complete. In step S20, the reflux temperature is 85°C and the reaction time is 4 hours.
[0027] S30. After the reaction is complete, N,N-dimethylformamide is evaporated to dryness under reduced pressure, the residue is dissolved in dichloromethane, and then extracted and washed with deionized water and saturated brine in sequence. In step S30, the silica gel column chromatography is Flash silica gel column chromatography. The target compound obtained is a white solid with a yield of 88%.
[0028] S40. Collect the organic layer, dry it with anhydrous sodium sulfate, filter it, and evaporate it under reduced pressure to obtain the crude product.
[0029] S50. The crude product is separated and purified by silica gel column chromatography to obtain the target compound, namely the STING pathway inhibitor derivative.
[0030] The structure of the compound was confirmed by proton NMR, carbon NMR, and high-resolution mass spectrometry.
[0031] An application of an ivy saponin STING pathway inhibitor, in which the derivative is used to inhibit the expression of IFN-β, was investigated. By constructing a luciferase reporter gene model, the inhibitory activity of the derivative on the STING pathway was screened at the cellular level. The inhibitory activity of the derivative on the expression level of IFN-β, a downstream molecule of the STING pathway, was characterized by its effect on the STING pathway.
[0032] Example 1
[0033] Accurately weigh 1 mM HE and 1 mM benzyl bromide, add 15 mL N,N-dimethylformamide (DMF) as the reaction solvent, add an appropriate amount of K2CO3, and stir the mixture under reflux at 85 °C for 4 h. Monitor the reaction by TLC, and use cerium sulfate staining to develop the HE derivative. Stop the reaction after it is complete. Evaporate the DMF to dryness under reduced pressure, dissolve it in dichloromethane (DCM), extract and wash twice with deionized water, and extract and wash once with saturated brine. Collect the organic layer, dry the organic layer with an appropriate amount of anhydrous sodium sulfate, filter, evaporate to dryness under reduced pressure, mix with silica gel, and separate the compound by Flash silica gel column chromatography. White solid; yield 88%;
[0034] After successfully preparing the hederaponin STING pathway inhibitor derivative, nuclear magnetic resonance (NMR) spectroscopy was performed to verify its structure and confirm its purity. 1 H NMR) and carbon nuclear magnetic resonance (NMR) 13 Analysis was performed using both 12C NMR and high-resolution mass spectrometry (HRMS). 1 In the 1H NMR spectrum (400 MHz, solvent: CDCl3), the singlet (s) at a chemical shift (δ) of 0.61 ppm corresponds to three hydrogen atoms (H-25), which is a methyl group on the ivy saponin backbone. The doublet (dd) at 2.83 ppm corresponds to one hydrogen atom (H-18), with J values of 17.0 and 5.0 Hz, indicating that this hydrogen atom is located on two adjacent carbon atoms in different chemical environments. The doublets (d) at 3.42 and 3.71 ppm each correspond to one hydrogen atom (H-23), with a J value of 13.0 Hz, reflecting that the two hydrogen atoms on H-23 have different chemical shifts due to steric hindrance or the influence of the chemical environment. The multiplet (m) at 3.63 ppm corresponds to one hydrogen atom (H-3), which is a methylene or methine group on the ivy saponin backbone. The doublet (d) at 5.04 and 5.09 ppm each corresponds to one hydrogen atom, which are two hydrogen atoms on the benzyl bromide moiety (Bn-CH2), with a J value of 15.5 Hz, indicating that they are in the trans configuration. The multiplet (m) at 5.28 ppm corresponds to one hydrogen atom (H-12), which is an alkene hydrogen atom on the ivy saponin skeleton. The multiplet (m) at 7.32 ppm corresponds to five hydrogen atoms (H-Ar), which are hydrogen atoms on the benzyl bromide moiety benzene ring.
[0035] exist 13In the CNMR (100 MHz, CDCl3 solvent) spectrum, the carbon atoms and their functional groups corresponding to each chemical shift were confirmed, including multiple methyl, methylene, methine, and quaternary carbon atoms on the ivy saponin backbone, as well as carbon atoms on the benzyl bromide moiety of the benzene ring. In particular, the chemical shift at 66.1 ppm corresponds to C-23 and Bn-CH2, further confirming that the benzyl bromide moiety has been successfully attached to the ivy saponin backbone. The chemical shift at 72.3 ppm corresponds to C-3, a key carbon atom on the ivy saponin backbone. The chemical shift at 122.6 ppm corresponds to C-12, an alkene carbon atom on the ivy saponin backbone. The carbon atoms on the benzene ring correspond to 128.1 ppm (appearing twice, indicating two symmetrical substituent positions on the benzene ring), 128.6 ppm (appearing once, indicating one asymmetrical substituent position on the benzene ring), and 136.6 ppm (corresponding to the carbon atom on the benzene ring bonded to bromine). Finally, the chemical shift at 177.6 ppm corresponds to C-28, which is a carboxyl carbon atom on the ivy saponin skeleton (although it may have been esterified or converted to other forms during preparation).
[0036] Furthermore, high-resolution mass spectrometry (HRMS) analysis confirmed the structure of this derivative. The observed mass-to-charge ratio (m / z) was 563.4079, which is consistent with the theoretically calculated mass-to-charge ratio ([M+H]+563.4079, for the molecular formula C) 37 H 54 The O4 (the theoretical mass of which is 562.4022 plus the mass of one hydrogen ion) matches perfectly, further confirming the structure and purity of the derivative.
[0037] In summary, the structure of the hederone saponin STING pathway inhibitor derivative was successfully verified and its purity was confirmed through nuclear magnetic resonance and high-resolution mass spectrometry analysis, providing a solid foundation for subsequent bioactivity evaluation and clinical application.
[0038] Example 2
[0039] Using 0.3 mM of the compound from Example 1 as the starting material, 0.6 mM of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDCI) and 0.15 mM of 4-dimethylaminopyridine (DMAP) were used as the condensing agent and catalyst for the esterification reaction, respectively, in reaction with 0.9 mM of 5-nitro-2-furanic acid. The reaction was carried out in dichloromethane (DCM) solvent for more than 12 hours, and the reaction progress was monitored by thin-layer chromatography (TLC) until the reaction was confirmed to be complete. Subsequently, the reaction system underwent a series of post-treatment steps, including extraction and washing with deionized water and saturated brine, drying of the organic layer, filtration, evaporation under reduced pressure, and mixing with silica gel. Finally, the target compound was obtained by Flash silica gel column chromatography. The compound was a white solid with a yield of 42% and a melting point in the range of 112.3-114.8 °C.
[0040] To verify the structure of compound 3a, a 1H NMR spectrum was performed. 1 H NMR) and carbon nuclear magnetic resonance (NMR) 13 Analysis was performed using CNMR and high-resolution mass spectrometry (HRMS). 1 In the 1H NMR (400MHz, DMSO-d6 solvent) spectrum, multiple chemical shifts (δ) corresponding to hydrogen atom signals were observed. For example, the singlet (s) at 0.56 ppm corresponds to three hydrogen atoms (H-25), which is a methyl group on the compound skeleton. The doublet (dd) at 2.83 ppm corresponds to one hydrogen atom (H-18), with J values of 17.0 and 4.0 Hz, indicating that this hydrogen atom is located on adjacent carbon atoms in two different chemical environments. The doublets (d) at 4.08 and 4.13 ppm each correspond to one hydrogen atom (H-23), with a J value of 14.5 Hz, reflecting that the two hydrogen atoms on H-23 have different chemical shifts due to steric hindrance or the influence of the chemical environment. The doublet (dd) at 4.94 ppm corresponds to one hydrogen atom (H-3), with J values of 14.0 and 6.5 Hz, indicating that H-3 is located in a more complex chemical environment. The doublets (d) at 5.01 and 5.06 ppm each correspond to one hydrogen atom, which are two hydrogen atoms on the benzyl bromide moiety (Bn-CH2), with a J value of 15.5 Hz, indicating that they are in the trans configuration. The multiplet (m) at 5.20 ppm corresponds to one hydrogen atom (H-12), which is an alkene hydrogen atom on the compound skeleton. The multiplet (m) at 7.33 ppm corresponds to five hydrogen atoms (H-Ar), which are hydrogen atoms on the benzyl bromide benzene ring. In addition, multiplets were observed at 7.57 ppm and 7.77 ppm, corresponding to two hydrogen atoms (H-3′,3″ and H-4′,4″), respectively. These hydrogen atoms may originate from the furan ring moiety formed after the reaction with 5-nitro-2-furanic acid.
[0041] exist 13 In the C10 NMR spectrum (100 MHz, solvent CDCl3-d1), multiple chemical shifts corresponding to carbon atom signals were observed. These signals included multiple methyl, methylene, methine, and quaternary carbon atoms on the compound skeleton, as well as carbon atoms in the benzyl bromide moiety and the furan ring moiety. In particular, the chemical shifts at 65.3 ppm and 66.3 ppm corresponded to C-23 and Bn-CH2, respectively, which further confirmed that the benzyl bromide moiety had been successfully attached to the compound skeleton. The chemical shift at 76.5 ppm corresponded to C-3, a key carbon atom on the compound skeleton. The carbon atoms in the furan ring moiety corresponded to chemical shifts of 112.9 ppm (C-4″, 4″′), 119.9 ppm, and 120.0 ppm (C-3″, 3″′). In addition, chemical shifts of 156.2 and 156.3 ppm were observed corresponding to the carbon atom attached to the ester group (C-COOR), and a chemical shift of 176.3 ppm corresponding to the carboxyl carbon atom (C-28).
[0042] Finally, high-resolution mass spectrometry (HRMS) analysis also confirmed the structure of the compound. The observed mass-to-charge ratio (m / z) was 841.5835, which is consistent with the theoretically calculated mass-to-charge ratio ([M+H]+841.5835, for the molecular formula C) 47 H 56 N2O 12 The theoretical mass (840.3833 plus the mass of one hydrogen ion) is a perfect match, further confirming the structure and purity of the compound.
[0043] In summary, the structure of compound 3a was successfully verified and its purity was confirmed through nuclear magnetic resonance and high-resolution mass spectrometry analysis, providing a solid foundation for subsequent bioactivity evaluation and potential drug development.
[0044] Example 3
[0045] In the experiment, 0.3 mM of the compound from Example 1 was accurately weighed as the starting material. For the esterification reaction, 0.6 mM of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDCI) was added as a condensing agent, and 0.15 mM of 4-dimethylaminopyridine (DMAP) was added as a catalyst. Simultaneously, 0.3 mM of 5-nitro-2-furanic acid was added dropwise to ensure a smooth reaction. The entire reaction system used dichloromethane (DCM) as a solvent and was stirred at room temperature for over 12 hours. The reaction progress was monitored by thin-layer chromatography (TLC), and the reaction was stopped once complete.
[0046] After the reaction was completed, the reaction system underwent post-treatment. First, the reaction mixture was extracted and washed twice with deionized water to remove water-soluble impurities. Next, it was extracted and washed again with saturated brine to further purify the product. Subsequently, the organic layer was collected and dried with an appropriate amount of anhydrous sodium sulfate to remove residual water. After filtration and evaporation under reduced pressure, the resulting solid product was mixed with silica gel for subsequent Flash silica gel column chromatography. Through this step, the target compound 3a was successfully separated from the reaction mixture as a white solid with a yield of 41% and a melting point ranging from 76.6 to 79.1 °C.
[0047] To verify the structure of compound 3a, a 1H NMR spectrum was performed. 1 H NMR) and carbon nuclear magnetic resonance (NMR) 13 Analysis was performed using CNMR and high-resolution mass spectrometry (HRMS). 1 In the 1H NMR (400MHz, DMSO-d6) spectrum, multiple chemical shifts (δ) corresponding to hydrogen atom signals were observed. For example, the singlet (s) at 0.53 ppm corresponds to three hydrogen atoms (H-25), which is a methyl group on the compound skeleton. The doublet (dd) at 2.81 ppm corresponds to one hydrogen atom (H-18), with J values of 17.0 and 6.0 Hz, indicating that this hydrogen atom is located on two adjacent carbon atoms in different chemical environments. The multiplet (m) at 3.40 ppm corresponds to one hydrogen atom (H-3), which is a methine methyl group on the compound skeleton. The doublets (d) at 4.06 and 4.22 ppm each correspond to one hydrogen atom (H-23), with J values of 14.0 and 13.5 Hz, respectively, reflecting that the two hydrogen atoms on H-23 have different chemical shifts due to steric hindrance or the influence of the chemical environment. The doublets (d) at 5.00 and 5.04 ppm each correspond to one hydrogen atom, which are two hydrogen atoms on the benzyl bromide moiety (Bn-CH2), with a J value of 15.5 Hz, indicating that they are in the trans configuration. The multiplet (m) at 5.19 ppm corresponds to one hydrogen atom (H-12), which is an alkene hydrogen atom on the compound skeleton. The multiplet (m) at 7.33 ppm corresponds to five hydrogen atoms (H-Ar), which are hydrogen atoms on the benzyl bromide benzene ring. In addition, doublets were observed at 7.53 ppm and 7.77 ppm, each corresponding to one hydrogen atom (H-3′ and H-4′), which are from the furan ring moiety formed after the reaction with 5-nitro-2-furanic acid.
[0048] exist 13In the C10 NMR (100 MHz, DMSO-d6) spectrum, multiple chemical shifts corresponding to carbon atom signals were observed. These signals included multiple methyl, methylene, methine, and quaternary carbon atoms on the compound skeleton, as well as carbon atoms in the benzyl bromide moiety and the furan ring moiety. In particular, the chemical shifts at 65.2 ppm and 66.9 ppm corresponded to C-23 and Bn-CH2, respectively, further confirming that the benzyl bromide moiety had been successfully attached to the compound skeleton. The chemical shift at 76.5 ppm corresponded to C-3, a key carbon atom on the compound skeleton. The carbon atoms in the furan ring moiety corresponded to chemical shifts such as 113.0 ppm (C-4″) and 119.5 ppm (C-3″). In addition, chemical shifts of 156.3 and 156.5 ppm were observed corresponding to the carbon atom attached to the ester group (C-COOR), and a chemical shift of 176.3 ppm corresponding to the carboxyl carbon atom (C-28).
[0049] Finally, high-resolution mass spectrometry (HRMS) analysis also confirmed the structure of the compound. The observed mass-to-charge ratio (m / z) was 702.4000, which is consistent with the theoretically calculated mass-to-charge ratio ([M+H]+702.4000, for the molecular formula C) 42 H 55 The mass of NO8 (the theoretical mass is 701.3928 plus the mass of one hydrogen ion) matches perfectly, further confirming the structure and purity of the compound.
[0050] In summary, the structure of the compound was successfully verified and its purity was confirmed through analysis using nuclear magnetic resonance and high-resolution mass spectrometry, providing a solid foundation for subsequent bioactivity evaluation and potential drug development.
[0051] The present invention also includes compounds of general formula 1 or pharmaceutically acceptable salts thereof, such as Figure 2 As shown:
[0052] General Formula 1;
[0053] R1 is selected from hydrogen or aryl;
[0054] R2 is selected from hydrogen, furan group, and thiophene group;
[0055] R3 is selected from hydrogen, furan group, and thiophene group.
[0056] It should be noted that, in this document, relational terms such as "first" and "second" are used only to distinguish one entity or operation from another, and do not necessarily require or imply any such actual relationship or order between these entities or operations. Furthermore, the terms "comprising," "including," or any other variations thereof are intended to cover non-exclusive inclusion, such that a process, method, article, or apparatus that comprises a list of elements includes not only those elements but also other elements not expressly listed, or elements inherent to such a process, method, article, or apparatus. Without further limitations, an element defined by the phrase "comprising one..." does not exclude the presence of other identical elements in the process, method, article, or apparatus that includes said element.
[0057] Although embodiments of the invention have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made to these embodiments without departing from the principles and spirit of the invention, the scope of which is defined by the appended claims and their equivalents.
Claims
1. A method for preparing an inhibitor of the hederaponin STING pathway, characterized in that, Includes the following steps: S10. Take an appropriate amount of ivy saponin and aromatic compounds, add N,N-dimethylformamide as a reaction solvent, and add an appropriate amount of K2CO3. S20. Stir the reaction under reflux for a certain period of time, and monitor the reaction progress by thin-layer chromatography until the reaction is complete. S30. After the reaction is complete, N,N-dimethylformamide is evaporated to dryness under reduced pressure, the residue is dissolved in dichloromethane, and then extracted and washed successively with deionized water and saturated brine. S40. Collect the organic layer, dry it with anhydrous sodium sulfate, filter it, and evaporate it under reduced pressure to obtain the crude product. S50. The crude product is separated and purified by silica gel column chromatography to obtain the target compound, namely the STING pathway inhibitor derivative.
2. The method for preparing an inhibitor of the hederaponin STING pathway according to claim 1, characterized in that, The aromatic compound is benzyl bromide.
3. The method for preparing an inhibitor of the hederaponin-STING pathway according to claim 1, characterized in that, In step S10, the concentrations of both hederaponin and aromatic compounds are 1 mM, and the volume of N,N-dimethylformamide (DMF) is 15 mL.
4. The method for preparing an inhibitor of the hederaponin-STING pathway according to claim 1, characterized in that, In step S20, the temperature of the heating reflux is 85°C, and the reaction time is 4 hours.
5. The method for preparing an hederaponin STING pathway inhibitor according to claim 1, characterized in that, In step S30, the silica gel column chromatography is Flash silica gel column chromatography, and the target compound obtained is a white solid with a yield of 88%.
6. A method for preparing an hederaponin STING pathway inhibitor according to any one of claims 1 to 5, characterized in that, The structure of the compound was confirmed by proton NMR, carbon NMR, and high-resolution mass spectrometry.
7. The application of the hederaponin STING pathway inhibitor prepared according to claim 1, characterized in that, The derivative is used to inhibit the expression of IFN-β. By constructing a luciferase reporter gene model, its STING pathway inhibitory activity was screened at the cellular level. The effect of the derivative on the expression level of IFN-β, a downstream molecule of the STING pathway, was used to characterize its STING pathway inhibitory activity.