Dichlorochromone compound with helicobacter pylori inhibition activity and preparation method and application thereof

Abstract

The invention provides a dichlorochromone compound with helicobacter pylori inhibition activity as well as a preparation method and application thereof, and belongs to the field of natural medicines. A compound 1 and a compound 2 are separated from agilawood produced from aquilaria sinensis' Hooke No.1 ', the compound 1 is (5R, 6R, 7S, 8R)-5, 8-dichloro-6, 7-dihydroxy-2-[2-(4-methoxy) ethyl]-5, 6, 7, 8-tetrahydrochromone, and the compound 2 is (5R, 6R, 7S, 8R)-5, 8-dichloro-6, 7-dihydroxy-2-[2-(4-methoxy) ethyl]-5, 6, 7, 8-tetrahydrochromone. The compound 2 is (5R, 6R, 7S, 8R)-5, 8-dichloro-6, 7-dihydroxy-2-(2-phenethyl)-5, 6, 7, 8-tetrahydrochromone; the two compounds can effectively inhibit the activity of helicobacter pylori, and have wide development and application prospects in preparation of related drugs or health care products for inhibiting excessive generation of helicobacter pylori.

Description

Technical Field

[0001] The invention belongs to the technical field of natural product separation, and in particular relates to two new compounds and preparation methods and applications thereof. Background Art

[0002] Chronic gastritis is a common disease of the digestive system, and its pathological changes are mainly manifested as chronic inflammation of the gastric mucosa. According to the results published by the World Health Organization, the global incidence of gastric diseases is as high as 80%, among which chronic gastritis is the most common, accounting for 50% of the total number of gastric diseases. The incidence of gastric diseases in my country is higher than the global level, among which chronic gastritis accounts for a higher proportion of the overall gastric diseases than the global level, about 50% to 80%, which has a great impact on people's lives and work. Long-term prolongation of this disease will also lead to the occurrence of gastric cancer. Relevant studies have shown that 80% to 95% of patients with chronic gastritis have Helicobacter pylori infection in the gastric mucosa. Helicobacter pylori (Hp) infection is the most important pathogenic factor of gastritis and the most important and controllable risk factor for preventing gastric cancer. Almost all Hp patients with current infection have varying degrees of gastric mucosal inflammation. Therefore, finding natural, safe and efficient Helicobacter pylori inhibitors has become one of the research hotspots.

[0003] Agarwood is a wood formed by the accumulated resin secreted by plants of the genus Aquilaria or Gyrinops in the family Thymelaeaceae after being damaged by the outside world. Agarwood is known as the "king of incense". It has the effects of promoting qi and relieving pain, warming the middle and stopping vomiting, and relieving asthma. It is used for chest and abdominal distension and pain, stomach cold, vomiting and hiccups, and kidney deficiency, qi reversal and asthma. It is a precious traditional Chinese medicine commonly used in clinical Chinese medicine to treat stomach diseases. The main characteristic components of agarwood are sesquiterpenes and 2-(2-phenylethyl) chromone compounds, which have pharmacological effects such as anti-inflammatory, antibacterial, anti-gastric ulcer, promoting gastrointestinal motility, and anti-tumor. Summary of the invention

[0004] The object of the present invention is to provide a new compound extracted from 'Reke No. 1' white aquilaria sinensis.

[0005] The object of the present invention is to provide a method for extracting, separating and purifying a new compound extracted from 'Reke No. 1' Aquilaria sinensis.

[0006] Another purpose of this study is to provide new compounds in Reke No. 1's white agarwood that have significant inhibitory effects on the activity of Helicobacter pylori and further develop the value of agarwood.

[0007] Based on the above purpose, the molecular formula of compound 1 is C 18 H 18 Cl 2 O 5, Compound 1: (5R, 6R, 7S, 8R)-5,8-dichloro-6,7-dihydroxy-2-[2-(4-methoxy)ethyl]-5,6,7,8-tetrahydrochromone; having the structure shown below:

[0008]

[0009] The molecular formula of compound 2 is C 17 H 16 Cl 2 O 4 , Compound 2: (5R,6R,7S,8R)-5,8-dichloro-6,7-dihydroxy-2-(2-phenylethyl)-5,6,7,8-tetrahydrochromone;

[0010] Has the following structure:

[0011]

[0012] The present invention provides a method for preparing the new compound having the activity of inhibiting Helicobacter pylori described in the above technical solution, comprising the following steps:

[0013] (1) Extraction and crude separation of 'Reke No. 1' Aquilaria sinensis sample

[0014] The 'Reke No. 1' white agarwood sample was naturally dried in the shade, crushed into coarse powder, and then extracted 5-7 times with 8 times / time 95% v / v methanol under heating reflux, and all extracts were combined and concentrated under reduced pressure until there was no alcohol taste to obtain an alcohol extract. The alcohol extract was suspended with 1 times the weight of distilled water as the aqueous phase, and extracted with petroleum ether, ethyl acetate, and n-butanol in sequence using a liquid-liquid extraction method. The ratio of the organic phase to the aqueous phase was 3:2 (v / v). After reduced pressure concentration, three extraction parts of petroleum ether, ethyl acetate, and n-butanol were obtained, and the ethyl acetate part was recorded as part A.

[0015] (2) Separation and purification of ethyl acetate fraction

[0016] The ethyl acetate fraction was dissolved with a small amount of methanol, and 1.4-1.5 times of 60-80 mesh silica gel was taken for sample mixing. Vacuum column chromatography was used, and gradient elution was first performed with 30:1, 10:1, 5:1, 2:1 (v / v) of petroleum ether-ethyl acetate as the elution system, and then eluted with 80:1, 50:1, 25:1, 15:1, 10:1, 5:1, 2:1, 1:1, 0:1 (v / v) as the chloroform-methanol elution system. The fraction was analyzed and detected by thin layer chromatography, and 16 fractions A1 to A16 were obtained by merging.

[0017] (3) A10 fraction sample separation

[0018] The A10 fraction sample was separated by RP-18 column chromatography, with a system gradient elution of 3:7, 2:3, 1:1, 3:2, 7:3, 4:1, 9:1, 1:0 (v / v) methanol-distilled water, and 22 fractions A10-1 to A10-22 were obtained by TLC detection and HPLC analysis. The A10-17 fraction was then eluted by Sephadex LH-20 gel column with chloroform-methanol (1:1, v / v), and 8 fractions A10-17-1 to A10-17-8 were obtained by thin layer chromatography analysis. A10-17-6 was further eluted with chloroform-methanol (200:1→0:1, v / v) on a silica gel column. The specific volume ratio of chloroform-methanol for gradient elution was 200:1, 100:1, 80:1, 50:1, 25:1, 10:1, 0:1. After thin layer chromatography analysis, six fractions A10-17-6-1 to A10-17-6-6 were obtained. A10-17-6-4 was purified by semi-preparative high performance liquid chromatography (C 18 Column; acetonitrile-water = 28:72, v / v; flow rate 4.0 mL / min; UV detection wavelength 210 / 254 nm) was used for elution to obtain compound 1 and compound 2.

[0019] The present invention evaluates the activity of inhibiting Helicobacter pylori by MIC and MBC assays, and the results show that both Compound 1 and Compound 2 can effectively inhibit the production of Helicobacter pylori.

[0020] Based on this, the present invention provides the use of the above compound or the compound prepared by the above preparation method for inhibiting the activity of Helicobacter pylori.

[0021] The present invention provides the use of the compound or the compound prepared by the preparation method as an inhibitor of Helicobacter pylori activity.

[0022] An inhibitor for inhibiting the activity of Helicobacter pylori, comprising compound 1 and / or compound 2.

[0023] The present invention provides the use of the above compound or the compound prepared by the above preparation method in preparing a drug for treating and / or alleviating the activity of Helicobacter pylori.

[0024] The present invention provides the use of the above compound or the compound prepared by the above preparation method in preparing a health product for alleviating the activity of Helicobacter pylori.

[0025] Furthermore, the Helicobacter pylori infection includes one or more of stomach problems such as chronic gastritis, atrophic gastritis, and gastric ulcer.

[0026] The present invention provides a drug for treating and / or inhibiting the activity of Helicobacter pylori, comprising compound 1 or / and compound 2, and a pharmaceutically acceptable adjuvant;

[0027] The present invention provides a health product for inhibiting the activity of Helicobacter pylori, comprising compound 1 or / and compound 2, and an adjuvant acceptable to the health product.

[0028] Furthermore, the dosage form of the medicine or health product is tablets, capsules, powder injections or suspensions.

[0029] Compared with the prior art, the present invention has the following beneficial effects:

[0030] The present invention provides compound 1 (C 18 H 18 Cl 2 O 5 ), compound 2 (C 17 H 16 Cl 2 O 4 ) is a tetrahydrochromone with a novel structure, which is a new compound, has the activity of inhibiting Helicobacter pylori, and can be used to treat or alleviate diseases related to Helicobacter pylori. The present invention evaluates the inhibition of Helicobacter pylori production by MIC and MBC determination methods, and compound 1 and compound 2 can inhibit the growth of Helicobacter pylori. Therefore, it is shown that the above-mentioned compounds can be used to prepare medicines for treating and / or inhibiting the activity of Helicobacter pylori, or for preparing health products for inhibiting the activity of Helicobacter pylori. BRIEF DESCRIPTION OF THE DRAWINGS

[0031] Figure 1 is the compound 1 prepared in Example 1 1 H NMR spectrum;

[0032] Figure 2 is the compound 1 prepared in Example 1 13 C NMR spectrum;

[0033] Figure 3 is the DEPT spectrum of compound 1 prepared in Example 1;

[0034] Figure 4 is the HSQC spectrum of compound 1 prepared in Example 1;

[0035] Figure 5 is the compound 1 prepared in Example 1 1 H- 1 H COSY spectrum;

[0036] Figure 6 is the HMBC spectrum of compound 1 prepared in Example 1;

[0037] Figure 7 is the ROESY spectrum of compound 1 prepared in Example 1;

[0038] Figure 8 is the HRESIMS spectrum of compound 1 prepared in Example 1;

[0039] Fig. 9 is the compound 2 prepared in Example 1 1 H NMR spectrum;

[0040] Fig.10 is the compound 2 prepared in Example 1 13 C NMR spectrum;

[0041] Fig.11 is the DEPT spectrum of compound 2 prepared in Example 1;

[0042] Fig.12 is the HSQC spectrum of compound 2 prepared in Example 1;

[0043] Fig.13 is the compound 2 prepared in Example 1 1 H- 1 H COSY spectrum;

[0044] Fig.14 is the HMBC spectrum of compound 2 prepared in Example 1;

[0045] Fig.15 is the ROESY spectrum of compound 2 prepared in Example 1;

[0046] Fig.16 It is the HRESIMS spectrum of compound 2 prepared in Example 1. DETAILED DESCRIPTION

[0047] In order to better understand the technical content of the present invention, specific embodiments are provided below to further illustrate the present invention.

[0048] Unless otherwise specified, the experimental methods used in the embodiments of the present invention are all conventional methods.

[0049] Unless otherwise specified, the materials, reagents, etc. used in the embodiments of the present invention can be obtained from commercial sources.

[0050] Example 1

[0051] 1.1 Instruments and reagents

[0052] Bruker AV-500 superconducting nuclear magnetic resonance spectrometer (Bruker, Switzerland); Autospec300 mass spectrometer (VG, UK); analytical high performance liquid chromatograph (Agilent, USA); semi-preparative high performance liquid chromatograph (Agilent, USA); N-1000 (2L) vertical rotary evaporator and CA-1111 cooling water circulation device (Shanghai Ailang Instrument Co., Ltd.); SHZ-D (Ⅲ) circulating vacuum pump (Shanghai Longtuo Instrument Equipment Co., Ltd.); AS220.R2 1 / 10,000 electronic scale (RADWAG Wagi Elektroniczne); Sephadex LH-20 gel (Merck Co., Ltd.); C 18 Reverse phase silica gel (20-45 μm, Fuji Silysia Chemical Ltd, Japan); Cosmosil C 18 Chromatographic column (10.0ID×250.0mm, Nacalai tesque Company) CosmosilπNAP chromatographic column (10.0ID×250.0mm, Nacalai tesque Company); silica gel for column chromatography and thin layer chromatography silica gel plate (Qingdao Ocean Chemical Plant); deuterated reagents and chromatographic methanol (Merck Company, Germany); 95% ethanol, methanol, ethyl acetate, chloroform, petroleum ether, acetone and other commonly used organic reagents (Tianjin Komiao, Tianjin Fuchen, Guangzhou Guanghua and other companies).

[0053] 1.2 Preparation and structural identification of compounds

[0054] The 'Reke No. 1' agarwood sample (1.98 kg) was collected from Pingding Town, Huazhou City, Guangdong Province in December 2016. It was identified as Aquilaria sinensis (Lour.) Spreng. by Researcher Dai Haofu from the Institute of Tropical Biotechnology, Chinese Academy of Tropical Agricultural Sciences. The voucher specimen (No. RK1CL202308) is preserved in the Institute of Tropical Biotechnology, Chinese Academy of Tropical Agricultural Sciences.

[0055] The preparation method of the compound comprises the following steps:

[0056] 1) Extraction and crude separation of 'Reke 1' Aquilaria sinensis sample

[0057] The agarwood sample (1.98 kg) of 'Reke No. 1' white woody product was naturally dried in the shade, crushed into coarse powder, and then extracted 5-7 times with 8 times / time 95% v / v methanol under heating reflux, and all extracts were combined and concentrated under reduced pressure until there was no alcohol taste, and an alcohol extract (244.8 g) was obtained. The alcohol extract was suspended with 1 times the weight of distilled water as the aqueous phase, and extracted with petroleum ether, ethyl acetate, and n-butanol in sequence by liquid-liquid extraction method, with the ratio of organic phase to aqueous phase being 3:2 (v / v), and three extraction parts of petroleum ether, ethyl acetate, and n-butanol were obtained by reduced pressure concentration, and the ethyl acetate part was recorded as part A.

[0058] 2) Separation and purification of ethyl acetate fraction

[0059] The ethyl acetate fraction (202.8 g) was dissolved in a small amount of methanol, and 1.4-1.5 times of 60-80 mesh silica gel was used for sample mixing. Vacuum column chromatography was used, and gradient elution was first performed with 30:1, 10:1, 5:1, 2:1 (v / v) of petroleum ether-ethyl acetate as the elution system, and then eluted with 80:1, 50:1, 25:1, 15:1, 10:1, 5:1, 2:1, 1:1, 0:1 (v / v) as the chloroform-methanol elution system. Each gradient elution was 5 column volumes, and one column volume was 2 L. The fractions were analyzed and detected by thin layer chromatography, and 16 fractions A1 to A16 were obtained by merging.

[0060] 3) A10 fraction sample separation

[0061] The A10 fraction sample was separated by RP-18 column chromatography with a system gradient elution of 3:7, 2:3, 1:1, 3:2, 7:3, 4:1, 9:1, 1:0 (v / v) methanol-distilled water, each gradient elution was 15 column volumes, and one column volume was 120 mL. After TLC detection and HPLC analysis, a total of 22 fractions, A10-1 to A10-22, were obtained.

[0062] The A10-17 fraction was then eluted through a Sephadex LH-20 gel column with 400 mL of chloroform:methanol (1:1, v / v), and detected by thin layer chromatography. A total of 8 fractions, A10-17-1 to A10-17-8, were obtained by combining.

[0063] A10-17-6 was further eluted through a silica gel column with chloroform-methanol (200:1→0:1, v / v). The specific gradient elution volume ratios were 200:1, 100:1, 80:1, 50:1, 25:1, 10:1, 0:1. Each concentration was eluted with 4 column volumes, and one column volume was 50 mL. The residue was analyzed and detected by thin layer chromatography, and a total of 6 fractions, A10-17-6-1 to A10-17-6-6, were obtained by merging.

[0064] A10-17-6-4 was purified by semi-preparative HPLC (C 18 Column; acetonitrile / water, 28:72, v / v; flow rate 4.0 mL / min; UV detection wavelength 210 / 254 nm) was used to elute compound 1 (5.3 mg, t R 57.0min) and compound 2 (7.7mg, t R 61.5min).

[0065] The structure of compound 1 is shown below:

[0066]

[0067] The structure of compound 1 prepared in Example 1 was identified, and the test results were as follows: Figures 1 to 8 , high resolution mass spectrum of the compound m / z 385.0599[M+H] + , molecular formula is C 18 H 18 Cl 2 O 5 Compound 1 H(500MHz) and 13 C (125MHz) NMR data are shown in Table 1:

[0068] The structure of compound 2 is shown below:

[0069]

[0070] The structure of compound 2 prepared in Example 1 was identified. Figures 9 to 16 , high resolution mass spectrum of the compound m / z 355.0497[M+H] + , molecular formula is C 17 H 16 Cl 2 O 4 Compound 1 H(500MHz) and 13 C (125MHz) NMR data are shown in Table 1:

[0071] Table 1 Compounds 1 H and 13 C NMR data (δ in ppm, J in Hz, in DMSO-d 6 )

[0072]

[0073]

[0074] Example 2 Determination of the activity of the compound in inhibiting Helicobacter pylori

[0075] The frozen Helicobacter pylori strains were thawed at room temperature, and the bacterial solution was inoculated on solid plate medium for recovery. 2 , 10% CO 2 , 85% N 2 , inverted in an incubator at 37°C for 5 to 7 days. Scrape the cultured colonies and culture them in liquid culture medium for 4 to 5 days. Take the cultured Hp bacterial solution, dilute and mix with liquid culture medium (BHI), and adjust the bacterial solution concentration to 1×10 8 CFU / mL. The compounds were dissolved in DMSO and the initial screening drug concentration was set at 100 μmol·L -1 The anti-Hp activity of all compounds was tested at this concentration. The microdilution method was used to test the antibacterial rate, and the inhibitory concentration was greater than 100 μmol·L -1 The compound concentration was adjusted to 3.125-100 μmol·L by serial dilution method. -1 , the final volume is 200μL / well. Clarithromycin (CLA) was used as the positive drug, BHI and DMSO were used as blank controls, and each experimental group was repeated 3 times. The 96-well plate was placed at 37°C, microaerobic, and shaken at 150 rpm for 48 hours. The absorbance was measured at 600nm using an ELISA reader. Combined with the turbidity in the wells, the MIC was the lowest concentration at which no bacterial growth was observed; the MBC was the lowest concentration that could kill bacteria in the culture medium.

[0076] OD 600 The value reflects the bacterial concentration and is calculated according to the following formula:

[0077] Inhibition rate (%) = (OD 600 Control bacterial solution-OD 600 Treated bacterial solution) / OD 600 Control bacterial solution ×100.

[0078] Table 2 Results of the inhibitory activity of compounds against Helicobacter pylori

[0079]

[0080] a Positive control, *P<0.05vs positive control group, *P<0.01vs positive control

[0081] It can be seen from the above examples that the present invention has discovered a new class of compounds with the activity of inhibiting Helicobacter pylori; the compound is derived from the agarwood produced by the white agarwood of 'Reke No. 1', and has good application prospects in the development of drugs or health products to solve the problem of gastritis caused by Helicobacter pylori infection.

[0082] The above is only a preferred embodiment of the present invention. It should be pointed out that a person skilled in the art can make several improvements and modifications without departing from the principle of the present invention. These improvements and modifications should also be regarded as within the scope of protection of the present invention.

Claims

1. A dichlorochromone compound, characterized in that: The dichlorochromone compound is compound 1 or compound 2, and compound 1 has a structure shown in the following formula (1): Compound 2 has the structure shown in the following formula (2):

2. The method for preparing the dichlorochromone compound according to claim 1, characterized in that: The steps include: (1) extracting and crudely separating the Aquilaria sinensis sample to prepare the ethyl acetate fraction; (2) separating and purifying the ethyl acetate fraction to obtain 16 fractions A1 to A16; (3) Separate the A10 fraction sample to obtain the target compound.

3. The method for preparing the dichlorochromone compounds according to claim 1, characterized in that: The white aucklandia is 'Reke No. 1' white aucklandia.

4. The method for preparing dichlorochromone compounds according to claim 2, characterized in that: The steps include: (1) Extraction and crude separation of 'Reke No. 1' Aquilaria sinensis sample The sample of 'Reke No. 1' Aquilaria sinensis was naturally dried in the shade, crushed into coarse powder, and then extracted with 95% v / v methanol under heating and reflux. All the extracts were combined and concentrated under reduced pressure until there was no alcohol taste, thereby obtaining an alcohol extract. The alcohol extract was suspended with 1 times the weight of distilled water as the aqueous phase, and extracted with petroleum ether, ethyl acetate and n-butanol in sequence by liquid-liquid extraction method, and concentrated under reduced pressure to obtain three extraction fractions of petroleum ether, ethyl acetate and n-butanol, and the ethyl acetate fraction was recorded as fraction A; (2) Separation and purification of ethyl acetate fraction The ethyl acetate fraction was dissolved with methanol, and the silica gel was mixed with the sample, and vacuum column chromatography was performed, first with petroleum ether-ethyl acetate as the elution system with a volume ratio of 30:1, 10:1, 5:1, 2:1 for gradient elution, and then with chloroform-methanol as the elution system with a volume ratio of 80:1, 50:1, 25:1, 15:1, 10:1, 5:1, 2:1, 1:1, 0:1 to obtain 16 fractions A1 to A16; (3) A10 fraction sample separation The A10 fraction sample was separated by RP-18 column chromatography, with methanol-distilled water in a volume ratio of 3:7, 2:3, 1:1, 3:2, 7:3, 4:1, 9:1, 1:0 as the system gradient elution, and combined after TLC detection and HPLC analysis to obtain 22 fractions from A10-1 to A10-22; the A10-17 fraction was then eluted through a Sephadex LH-20 gel column with chloroform:methanol in a volume ratio of 1:1 to obtain 8 fractions from A10-17-1 to A10-17-8; A10-17-6 was further eluted through a silica gel column with a chloroform-methanol volume ratio of 200:1 to 0:1 for gradient elution, to obtain 6 fractions from A10-17-6-1 to A10-17-6-6; A10-17-6-4 was eluted by semi-preparative high performance liquid chromatography to obtain the target compound.

5. The method for preparing dichlorochromone compounds according to claim 4, characterized in that: The steps include: (1) Extraction and crude separation of 'Reke No. 1' Aquilaria sinensis sample The 'Reke No. 1' agarwood sample was naturally dried in the shade, crushed into coarse powder, and then extracted with 8 times / time 95% v / v methanol under heating reflux for 5-7 times, all the extracts were combined, and concentrated under reduced pressure until there was no alcohol taste, to obtain an alcohol extract; the alcohol extract was suspended with 1 times the weight of distilled water as the aqueous phase, and extracted with petroleum ether, ethyl acetate, and n-butanol in sequence by liquid-liquid extraction method, with the volume ratio of organic phase to aqueous phase being 3:2, and three extraction parts of petroleum ether, ethyl acetate, and n-butanol were obtained by reduced pressure concentration, and the ethyl acetate part was recorded as part A; (2) Separation and purification of ethyl acetate fraction The ethyl acetate fraction was dissolved in methanol, and 1.4-1.5 times of 60-80 mesh silica gel was mixed with the sample, and vacuum column chromatography was performed, firstly using petroleum ether-ethyl acetate as an elution system with a volume ratio of 30:1, 10:1, 5:1, 2:1 for gradient elution, and then using a chloroform-methanol elution system with a volume ratio of 80:1, 50:1, 25:1, 15:1, 10:1, 5:1, 2:1, 1:1, 0:1 for elution, and thin layer chromatography was performed to analyze and detect, and 16 fractions A1 to A16 were obtained by merging; (3) A10 fraction sample separation The A10 fraction sample was separated by RP-18 column chromatography, with a volume ratio of 3:7, 2:3, 1:1, 3:2, 7:3, 4:1, 9:1, 1:0 of ​​methanol-distilled water as the system gradient elution, and 22 fractions A10-1 to A10-22 were obtained by TLC detection and HPLC analysis. The A10-17 fraction was then separated by Sephadex chromatography. The LH-20 gel column was eluted with chloroform-methanol in a volume ratio of 1:1, and the mixture was analyzed and detected by thin layer chromatography to obtain 8 fractions, A10-17-1 to A10-17-8; A10-17-6 was further eluted with a gradient of chloroform-methanol in a volume ratio of 200:1, 100:1, 80:1, 50:1, 25:1, 10:1, and 0:1 by silica gel column, and 6 fractions, A10-17-6-1 to A10-17-6-6, were obtained by thin layer chromatography analysis and detection; A10-17-6-4 was eluted by semi-preparative high performance liquid chromatography to obtain compounds 1 and 2, wherein the semi-preparative high performance liquid chromatography used C 18 Column; acetonitrile-water with a volume ratio of 28:72; flow rate 4.0 mL / min; UV detection wavelength 210 / 254 nm.

6. Use of the compound according to claim 1 or the compound prepared by the preparation method according to claim 2 in preparing an inhibitor for inhibiting the activity of Helicobacter pylori.

7. Use of the compound according to claim 1 or the compound prepared by the preparation method according to claim 2 in preparing a medicament for treating and / or alleviating diseases associated with Helicobacter pylori production, or in preparing a health product for alleviating diseases associated with Helicobacter pylori production.

8. The use according to claim 7, characterized in that: The Helicobacter pylori-related diseases include chronic gastritis, atrophic gastritis, and gastric ulcer.

9. A medicine or health product for inhibiting the production of Helicobacter pylori, comprising the compound according to claim 1 or the compound prepared by the preparation method according to claim 2 and pharmaceutically or health-care-product acceptable excipients.

10. The medicine or health product for inhibiting the production of Helicobacter pylori according to claim 9, characterized in that: The dosage form is tablet, capsule, powder injection or suspension.

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