A compound with the effect of drastic purgation and water excretion, and a preparation method and application thereof

Abstract

The application discloses a compound with the function of purgation and water excretion, which has a chemical structural formula as shown in formula (I). The compound is a new natural product of tetracyclic triterpenes, has good fat solubility and chemical stability, can be conveniently extracted from the rhizome of the herbal medicine Alisma orientale and prepared into an oral or injection dosage form. The application further provides a preparation method and application of the compound. The compound can obviously inhibit the increase of the abdominal volume and the weight of ascites of mice in a dose-dependent manner, and is a new water excretion drug with great potential.

Description

Technical Field

[0001] This invention belongs to the field of medicine and relates to a new medicinal tetracyclic triterpenoid natural product, more specifically, to the structure of hygroscopic lecithin, its extraction method and application. Background Technology

[0002] Ascites is an abnormal accumulation of fluid in the abdominal cavity caused by various factors. Its formation is a complex process involving multiple organs and systems. The main causes include: cirrhosis leading to portal hypertension and hypoalbuminemia, which is the most common cause of ascites formation; congestive heart failure, pericarditis, etc., leading to obstruction of venous return and causing ascites; nephrotic syndrome leading to obstruction of body fluid and excretion, resulting in ascites; tumors such as ovarian cancer and colon cancer compressing lymphatic vessels, leading to obstruction of lymphatic return and ascites; tuberculous peritonitis, inflammatory bowel disease, etc., leading to increased permeability of peritoneal vessels and ascites; malnutrition, especially hypoalbuminemia, leading to leakage of fluid into the abdominal cavity and ascites; and other causes such as trauma, acute pancreatitis, and connective tissue diseases.

[0003] Ascites poses several health risks to patients, including: ① Direct impact on the body: Ascites can cause abdominal distension and pain, and in severe cases, even difficulty breathing, affecting the patient's mobility and daily life. ② Increased burden on the circulatory system: After ascites forms, the large amount of fluid entering the abdominal cavity concentrates the blood, reduces effective circulating blood volume, increases blood viscosity, and slows blood flow, potentially causing hypotension or shock. ③ Kidney damage: Ascites contains a large amount of nutrients and albumin; significant protein loss can worsen hypoalbuminemia and further alter the distribution of blood volume in the circulatory system, damaging the kidneys. ④ Increased risk of infection: The presence of ascites easily leads to bacterial infections in the abdominal cavity, especially during paracentesis or drainage, which can easily cause secondary infections and lead to peritonitis. ⑤ Increased burden on the liver: The formation of ascites exacerbates hepatic ischemia and hypoxia, intensifying hepatocyte necrosis. Especially in patients with cirrhosis, the presence of ascites usually indicates that the liver has entered a decompensated stage. ⑥ Other complications: Such as hepatic encephalopathy and ruptured esophageal and gastric varices, which can endanger the patient's life.

[0004] Timely and symptomatic treatment of ascites promotes drainage from the abdominal cavity, alleviating patient suffering, preventing complications, and benefiting the patient's health. Common treatments for ascites include salt restriction, sodium excretion, and diuresis. For refractory and tension ascites, methods such as drainage, albumin infusion, transjugular intrahepatic portosystemic shunt, and liver transplantation may be used; however, the efficacy of these methods is not ideal. Traditional Chinese medicine employs a "strong purgative" approach, using classic herbs such as Euphorbia kansui, Euphorbia pekinensis, and Croton tiglium, which can rapidly drain the fluid from the intestines, demonstrating significant clinical efficacy and highlighting the unique characteristics of traditional Chinese medicine. However, a problem exists: these Euphorbiaceae herbs have relatively high toxicity, and their effective purgative components and mechanisms are unclear, warranting further investigation.

[0005] Begonia limprichtii Irmscher is a traditional Chinese medicine found in southwestern my country. It is a perennial herb belonging to the Begoniaceae family and is used to treat injuries from falls, rheumatic pain, and sore throat. It has a good safety profile, but its chemical composition and drainage properties have not yet been reported. Summary of the Invention

[0006] One objective of this invention is to address the above-mentioned technical problems by providing a small molecule compound with a novel structure and strong purgative and diuretic effects as a new option for ascites drainage drug treatment.

[0007] To achieve the above-mentioned objectives, the present invention provides the following technical solution:

[0008] In a first aspect, the present invention provides a compound having a strong water-repellent effect, having a chemical structural formula as shown in formula (I):

[0009]

[0010] The aforementioned compound, named cucurbitacin, contains thirty carbon atoms in its parent nucleus and is a typical tetracyclic triterpenoid. Its structural characteristic is that the angular methyl group 19-CH3 is attached to C-9, rather than the common C-10 of triterpenoids, thus belonging to the cucurbitacin class. However, it lacks the hydroxyl substitution common in cucurbitacins at C-16, making it a rare 16-dehydroxylated cucurbitacin with a novel structure that has not been previously reported. The cucurbitacin monomer is a white powder, sparingly soluble in water but readily soluble in organic solvents such as methanol, ethanol, ethyl acetate, and chloroform, with a bitter taste. Stability studies show that the content remains unchanged after 12 months at room temperature, and its properties show no alteration. Even after 6 months of accelerated testing at 40℃ and 75% relative humidity, no significant changes were observed in its physicochemical properties. This demonstrates its excellent chemical stability, providing convenient conditions for the production, transportation, and storage of the preparation.

[0011] In a second aspect, the present invention provides a pharmaceutical composition comprising the compounds described herein.

[0012] Preferably, the pharmaceutical composition further includes a pharmaceutically acceptable carrier and / or excipients.

[0013] Thirdly, the present invention provides a method for preparing the compound of the present invention, comprising the following steps:

[0014] a. Take the dried rhizomes of *Liriope muscari*, crush them, extract them with an organic solvent, filter them, concentrate them, and obtain a fluid extract;

[0015] b. Add the fluid extract to water, stir, filter, wash with water, dry, and obtain a precipitate;

[0016] c. Separate the precipitate by silica gel column chromatography, eluting with a petroleum ether-ethyl acetate gradient;

[0017] d. Detect column chromatography fractions, combine, concentrate, and obtain the compound.

[0018] Preferably, the organic solvent mentioned in step a can be any one or a mixture of organic solvents such as methanol, ethanol, ethyl acetate, acetone, chloroform, and petroleum ether, such as a mixture of petroleum ether and ethyl acetate (volume ratio 2:1). Methanol or ethanol, a lower alcohol, is preferred, and pharmaceutical-grade alcohol, i.e., aqueous ethanol (e.g., aqueous ethanol with a volume fraction of 75%-85%), is more suitable to meet the requirements of relevant regulations, cost, safety, and environmental protection in pharmaceutical production. The extraction method can be percolation, reflux, maceration, microwave extraction, or supercritical fluid extraction, with reflux being preferred.

[0019] The weight-to-volume ratio of water lily to organic solvent is 1g:3-5mL, preferably 1g:4mL.

[0020] Preferably, step b is a water sedimentation process, in which the amount of water added is 5 to 15 times the weight of the extract, preferably 10 times. The extract is stirred at room temperature or under heating to fully dissolve and suspend the extract. Then it is cooled, allowed to stand, filtered, and the precipitate is washed with water in small amounts several times.

[0021] Preferably, the column chromatography in step c can be repeated until the target analyte of the desired purity is obtained.

[0022] Preferably, in step d, the column chromatography fraction is detected by thin-layer chromatography or liquid chromatography.

[0023] More preferably, the thin-layer chromatography is conventional silica gel thin-layer chromatography, the developing solvent is petroleum ether-ethyl acetate (3:1) or chloroform-methanol (98:2); the color development method is iodine fuming.

[0024] More preferably, the liquid chromatography method uses a conventional C18 reversed-phase silica gel column; the mobile phase is methanol-0.1% formic acid (50:50 to 100:0) gradient elution; and the detection wavelength is 237 nm.

[0025] The preparation method of this invention has a short extraction route, simple operation, regenerable column chromatography packing material, low cost, and is feasible for large-scale production.

[0026] Fourthly, the present invention provides the use of the compounds or pharmaceutical compositions described herein in the preparation of drugs for draining ascites.

[0027] The evaluation of the ascites drainage efficacy of cypermethrin showed that mice inoculated with H22 mouse liver cancer cells experienced significant abdominal enlargement, while oral administration of cypermethrin (10–40 mg / kg) resulted in a greater reduction in abdominal swelling. -1 ·d -1 It can significantly inhibit the increase in abdominal volume and ascites weight in mice in a dose-dependent manner; at the same time, it was observed that the mice in the drug group had increased defecation frequency, loose stools, and obvious diarrhea, similar to "drastic purging of water".

[0028] Preferably, the compound is formulated into a pharmaceutically acceptable dosage form in monomeric form or as a plant extract containing it.

[0029] Preferably, the dosage form comprises a pharmaceutically acceptable carrier and / or excipients.

[0030] The monomer of hyacinthin or plant extracts containing hyacinthin are formulated into a variety of pharmaceutically acceptable dosage forms to meet the diverse needs of clinical use. These dosage forms include tablets, hard capsules, soft capsules, granules, pellets, ointments, and injections. Pharmaceutically acceptable carriers, excipients, or additives required for the formulation include commonly used pharmaceutical diluents and absorbents such as starch, dextrin, calcium sulfate, lactose, mannitol, sucrose, sodium chloride, glucose, calcium carbonate, kaolin, microcrystalline cellulose, aluminum silicate, calcium hydrogen phosphate, and light magnesium oxide; commonly used pharmaceutical wetting agents and binders such as water, glycerin, polyethylene glycol, ethanol, propanol, starch paste, dextrin, syrup, honey, glucose solution, gum arabic paste, gelatin paste, sodium carboxymethyl cellulose, shellac, methyl cellulose, potassium phosphate, and polyvinylpyrrolidone; and commonly used pharmaceutical disintegrants such as dried starch, alginate, agar powder, brown algae starch, and carbon. Sodium bicarbonate, citric acid, calcium carbonate, polyoxyethylene, sorbitol fatty acid esters, sodium dodecyl sulfonate, methylcellulose, ethylcellulose, etc.; disintegration inhibitors, such as sucrose, tristearate, cocoa butter, hydrogenated oil, etc.; lubricants, such as talc, silica, corn starch, stearates, boric acid, liquid paraffin, polyethylene glycol, etc.; pharmaceutically commonly used cosolvents, such as ethanol, propylene glycol, polyethylene glycol, polysorbate 80, lecithin, urea, sodium benzoate, sodium salicylate, nicotinamide, cyclodextrin, soybean oil, etc.; pharmaceutically acceptable carriers or excipients will not be listed in detail, and those skilled in the art can make specific selections based on their general knowledge.

[0031] Compared with existing ascites-draining drugs, the water-draining agent of the present invention has the following advantages:

[0032] (1) Draining lotus extract is a novel small molecule component with a structure type completely different from existing drainage drugs, and may contain different targets and mechanisms of action.

[0033] (2) The effect of draining ascites with water-reducing lotus seed extract is similar to the traditional Chinese medicine treatment of "drastic purging and water expulsion", which promotes the rapid expulsion of accumulated fluid from the intestines and has a significant therapeutic effect.

[0034] (3) The original plant has a long history of use as a folk herbal medicine and has no obvious toxic side effects, indicating that the lycopodium clavatum has good clinical safety.

[0035] (4) The original plant is a herbaceous plant of the genus Begonia Linn., which is similar to the common begonia flower varieties in horticulture. It can be artificially propagated and planted on a large scale to meet the demand for raw materials in large-scale production.

[0036] (5) The preparation process of water hyacin is simple, and high-purity monomers can be obtained at low cost;

[0037] (6) The lipophilic compound is highly lipophilic, has good solubility, and is easily absorbed orally;

[0038] (7) The physicochemical properties of the water-repellent compound are stable and it has a long shelf life.

[0039] In summary, the present invention has a novel structure of water-draining lotus seed extract, and has outstanding advantages such as high efficiency, novel mechanism, and stability. The raw materials are readily available and the cost is low, making it a new drug with great development potential for draining ascites. Attached Figure Description

[0040] Figure 1 This is the mass spectrum of hygroscopic methyl hydroxylamine.

[0041] Figure 2 This is the hydrogen nuclear magnetic resonance spectrum of hygroscopic methyl methacrylate (HMR).

[0042] Figure 3 This is the carbon NMR spectrum of lysimachia christinae.

[0043] Figure 4 This is the liquid chromatogram of hygroscopic methyl methionine.

[0044] Figure 5 This is the ultraviolet spectrum of hygroscopic methyl hydroxylamine.

[0045] Figure 6 This is a pharmacodynamic diagram of lysimachia christinae in treating ascites in mice, where A is a comparison of mouse appearance; B is a comparison of mouse weight; and C is a comparison of mouse abdominal circumference. Detailed Implementation

[0046] The technical solution of the present invention will be further described below with reference to the accompanying drawings and specific embodiments. Unless otherwise specified, the instruments or reagents used in the embodiments are all conventional instruments or reagents in the art and are conventional products that can be purchased from the market. Unless otherwise specified, the specific experimental operations involved in the text are all understandable or known to those skilled in the art based on their common knowledge or conventional technical means, and will not be described in detail here.

[0047] Example 1: Extraction, separation and structural determination of hygroscopic glycoside A

[0048] 1. Example 1 of extraction and separation of hygroscopic glycoside A:

[0049] (1) Take 300g of dried rhizome of Begonia limprichtii Irmscher (purchased from the herbal medicine market in Leshan City, Sichuan Province), crush it into coarse powder, put it in a round-bottom flask, add 1.2L of methanol, reflux for 1 hour, cool, and filter; extract the residue twice more in the same way; combine the three extracts, concentrate under reduced pressure, and obtain 65g of extract.

[0050] (2) Pour the extract into 650mL of water, heat it in an 80℃ water bath, stir it quickly to fully dissolve, disperse and suspend the extract, then cool it, let it stand for 1 hour, filter it, wash the filter cake several times with a small amount of water, dry it, and obtain 33g of precipitated powder.

[0051] (3) Take 20g of precipitated powder, dissolve it in 60mL of methanol, mix it into silica gel, dry it, and pack it into a silica gel column (silica gel specification 200-300 mesh). Elute with a gradient of petroleum ether-ethyl acetate (10:0 to 0:10). Collect a total of 80 fractions (Fr1-80). Check each fraction with silica gel thin layer, develop with petroleum ether-ethyl acetate (volume ratio 3:1), and develop with iodine fuming. The results show that Fr15-Fr18 contain the same single main spot. Combine and concentrate to obtain 1.8g of white powder (PSY-2).

[0052] Its purity was determined by liquid chromatography. Chromatographic conditions: ODS column (150×4.6, 5μm), methanol-0.1% formic acid (50:50 to 100:0) gradient elution, detection wavelength 237nm, flow rate 1mL / min.

[0053] The results are as follows Figure 4 As shown, the chromatogram displays a single main peak with a purity >98%.

[0054] 2. Structural determination:

[0055] PSY-2 is a white powder. UVλmax: 237, 266(sh)nm ( Figure 5 );ESI-TOF-MSm / z:541.3140[M+H] + 558.3440[M+NH4] + 563.3001[M+Na] + (Calculated value C) 32 H 44 O7,540.308704)( Figure 1)。

[0056] 1 H-NMR(400MHz,CDCl3)δppm:1.03(3H,s,H-18),1.09(3H,s,H-19),1.15(3H,s,H-29),1.25(3H,s,H-28),1.36(3H,s,H-30),1.44(3H,s,H-21),1.54(3H,s,H-26),1.58(3H,s,H-27),2.03(3H,s,Ac),5.76(1H,m,H-6),5.94(1H,d,J=2.4Hz,H-1),6.41(1H,d,J=15.6Hz,H-23),7.12(1H,d,J=15.6Hz,H-24),3.49(1H,br s,H-10),3.13(1H,d,J=14.4Hz,H12b),2.74(1H,d,J=14.4Hz,H12a),2.33(1H,m,H-7a),2.03(1H,m,H-7b),2.04(1H,m,H-8),0.9~1.7(5H,m,H-15,16,17)( Figure 2 )。

[0057] 13 C-NMR(100MHz,CDCl3)δppm:114.98(C-1),144.49(C-2),198.76(C-3),47.50(C-4),136.65(C-5),120.94(C-6),23.54(C-7),41.56(C-8),48.85(C-9),34.77(C-10),213.54(C-11),48.63(C-12),50.32(C-13),48.30(C-14),34.08(C-15),20.92(C-16),49.04(C-17),18.98(C-18),19.94(C-19),78.81(C-20),23.97(C-21),201.58(C-22),118.90(C-23),153.33(C-24),79.07(C-25),26.73(C-26),25.94(C-27),27.98(C-28),20.19(C-29),17.58(C-30),21.89(Ac),169.78(Ac)( Figure 3 )。

[0058] Using two-dimensional spectral analysis such as HSQC and HMBC and referring to relevant literature (Magnetic Resonance In Chemistry 2005; 43:489-491), the above spectral data were completely assigned, and PSY-2 was identified as a new cucurbitacin, named cypermethrin.

[0059] The molecular formula of PSY-2 (a type of hygroscopic compound) is C2. 32 H 44 O7, with a molecular weight of 540, has the following molecular structure as shown in formula (I).

[0060]

[0061] The systematic name of this hygroscopic acetone is: (6R,E)-6-hydroxy-6-((9R,10R,13R,14S,17S)-2-hydroxy-4,4,9,13,14-pentamethyl-3,11-dioxo-4,7,8,9,10,11,12,13,14,15,16,17-dodecylhydro-3H-cyclopenta[a]phenanthrene-17-yl)-2-methyl-5-oxohept-3-en-2-yl acetate ((6R,E)-6-hydroxy-6-( (9R,10R,13R,14S,17S)-2-hydroxy-4,4,9,13,14-pentamethyl-3,11-dioxo-4,7,8,9,10,11,12,13, 14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl)-2-methyl-5-oxohept-3-en-2-yl acetate).

[0062] 3. Example 2 of extraction and separation of hygroscopic glycoside A:

[0063] (1) Take 100g of dried water lily, crush it into coarse powder, put it in a round bottom flask, add 500mL of 80% v / v ethanol, reflux for 1 hour, cool and filter; extract the residue twice more in the same way; combine the three extracts, concentrate under reduced pressure to obtain 22g of extract.

[0064] (2) Pour the extract into 330mL of water, heat it in an 80℃ water bath, stir it quickly to fully dissolve, disperse and suspend the extract, then cool it, let it stand for 1 hour, filter it, wash the filter cake several times with a small amount of water, dry it, and obtain 13g of precipitated powder.

[0065] (3) Take 10g of precipitated powder, dissolve it in 30mL of methanol, mix it into silica gel, dry it, pack it into a silica gel column (silica gel specification 200-300 mesh), and elute it with a gradient of petroleum ether-ethyl acetate (10:0-0:10); check each fraction with silica gel thin layer, develop it with petroleum ether-ethyl acetate (3:1), develop it with iodine fuming, combine it, concentrate it, and obtain 1.2g of light yellow powder.

[0066] (4) Dissolve the powder in 5 ml of methanol, mix with silica gel, dry, pack into a silica gel column (silica gel specification 200-300 mesh), and elute with a gradient of petroleum ether-ethyl acetate (10:0-0:10); combine with silica gel thin-layer chromatography, concentrate, and obtain 0.7 g of white powder.

[0067] 4. Example 3 of extraction and separation of hygroscopic glycoside A:

[0068] (1) Take 100g of dried water lily, crush it into coarse powder, put it in a round bottom flask, add 300mL of ethyl acetate, reflux for 1 hour, cool and filter; extract the residue twice more in the same way; combine the three extracts, concentrate under reduced pressure to obtain 13g of extract.

[0069] (2) Pour the extract into 65mL of water, heat it in an 80℃ water bath, stir it quickly to fully dissolve, disperse and suspend the extract, then cool it, let it stand for 1 hour, filter it, wash the filter cake several times with a small amount of water, dry it, and obtain 11g of precipitated powder.

[0070] (3) Take 10g of precipitated powder, dissolve it in 30mL of methanol, mix it into silica gel, dry it, pack it into a silica gel column (silica gel specification 200-300 mesh), and elute it with a gradient of petroleum ether-ethyl acetate (10:0-0:10); check each fraction with silica gel thin layer, develop it with petroleum ether-ethyl acetate (volume ratio 3:1), develop it with iodine fuming, combine them, concentrate it, and obtain 0.9g of white powder.

[0071] 5. Example 4 of extraction and separation of hygroscopic glycoside A:

[0072] (1) Take 100g of dried water lily, crush it into coarse powder, put it in a round bottom flask, add 350mL of petroleum ether-ethyl acetate (volume ratio 2:1), reflux for 1 hour, cool, and filter; extract the residue twice more in the same way; combine the three extracts, concentrate under reduced pressure to obtain 12g of extract.

[0073] (2) Pour the extract into 90mL of water, heat it in an 80℃ water bath, stir it quickly to fully dissolve, disperse and suspend the extract, then cool it, let it stand for 1 hour, filter it, wash the filter cake several times with a small amount of water, dry it, and obtain 11g of precipitated powder.

[0074] (3) Take 10g of precipitated powder, dissolve it in 30mL of methanol, mix it into silica gel, dry it, pack it into a silica gel column (silica gel specification 200-300 mesh), and elute it with a gradient of petroleum ether-ethyl acetate (10:0-0:10); check each fraction with silica gel thin layer, develop it with petroleum ether-ethyl acetate (volume ratio 3:1), develop it with iodine fuming, combine the fractions, concentrate it, and obtain 1.0g of white powder.

[0075] Chemical structure identification showed that the products obtained through the extraction and separation examples 2-4 above were identical to PSY-2.

[0076] Example 2: The efficacy of hygroscopic lecithin

[0077] 1. Experimental Method:

[0078] BALB / c mice were intraperitoneally injected with H22 mouse liver cancer cells diluted in 200 μL PBS (2 × 10⁻⁶). 6 (number / animal). After 7 days, ascites cells were recollected and resuspended in PBS to 2.67 × 10⁻⁶. 7 / mL. Subsequently, each mouse was intraperitoneally injected with H22 cells diluted in 200 μL PBS (2 × 10⁹ / mL). 6 (Number of cells / mouse). Mice inoculated with cells were administered the drug by gavage (once daily), and changes in ascites volume were observed.

[0079] BALB / c mice were randomly divided into 5 groups:

[0080] (1) Normal group;

[0081] (2) Model group: H22;

[0082] (3) Low-dose PSY-2 group: H22 + PSY-2 (10 mg·kg) -1 ·d -1 );

[0083] (4) Medium-dose group of PSY-2: H22 + PSY-2 (20 mg·kg) -1 ·d -1 );

[0084] (5) High-dose PSY-2 group: H22 + PSY-2 (40 mg·kg) -1 ·d -1 ).

[0085] 2. Observation indicators:

[0086] Over 12 days, the mouse weight and abdominal circumference were measured and recorded.

[0087] 3. Experimental Results:

[0088] Mice inoculated with H22 cells showed significant abdominal enlargement, while mice administered PSY-2 by gavage showed significantly inhibited abdominal enlargement. Figure 6 , A), and showed a dose-dependent relationship.

[0089] Meanwhile, the measured changes in mouse body weight and abdominal circumference also showed the same trend: the body weight and abdominal circumference of mice inoculated with H22 cells increased significantly within 12 days, while the increase in body weight and abdominal circumference of mice treated with PSY-2 drugs was significantly inhibited. Figure 6 (B, C).

[0090] Meanwhile, it was observed that the mice in the drug-treated group experienced significant diarrhea, with increased frequency of defecation and loose stools, suggesting that ascites was mainly excreted through the intestines, exhibiting the characteristics of "drastic purging and water expulsion" in traditional Chinese medicine.

[0091] Example 3: Preparation of Hydrangea Acid Tablets

[0092] Take 50g of hymenoplasmin and mix it with 1900g of a mixture of lactose and starch (lactose to starch weight ratio of 3:2, filler) in a granulator. First, mix at low speed (about 100-200r / min) for 5-10 minutes to ensure the active ingredient is evenly dispersed in the filler. Then, add 50mL of a 5% hydroxypropyl methylcellulose (binder) aqueous solution and continue mixing at medium speed (about 300-400r / min) for 10-15 minutes to form a soft mass. Granulate the mass through an 80-mesh sieve, dry it to control the moisture content at 2%-5%, and then granulate it through a 100-mesh sieve. Finally, mix it thoroughly with 40g of sodium carboxymethyl starch (disintegrant) and 10g of magnesium stearate (lubricant). Place the mixture in the hopper of a tablet press and compress it into 10,000 tablets, each containing 5mg of hymenoplasmin.

[0093] Example 4: Preparation of Ligusticum striatum capsules

[0094] Take 50g of hyacinthin and place it in a mixer with 1800g of a mixture of microcrystalline cellulose and lactose (microcrystalline cellulose to lactose weight ratio of 2:1, filler). Mix at 25 rpm for 10 minutes. Add 50mL of a 5% hydroxypropyl methylcellulose aqueous solution (binder) and continue mixing for 15 minutes to form a soft mass. Granulate the mass through an 80-mesh sieve, dry it to control the moisture content at 2%-5%, and then granulate it through a 100-mesh sieve. Place the granules in a mixer with 50g of crospovidone (disintegrant) and 10g of magnesium stearate (lubricant) and mix at 20 rpm for 20 minutes. Fill the mixture into capsules using a capsule filling machine to make 10,000 capsules, each containing 5mg of hyacinthin.

[0095] Example 5: Preparation of Hydrangea Acid Injection

[0096] Take 50g of hymenoplasmin and place it in a clean container. Add 5L of PEG-400 and stir until fully dissolved. Dilute with water for injection to 50L. Filter through a 0.22μm microporous membrane. Under aseptic conditions, quantitatively fill 10,000 ampoules with 5mL of the filtrate. Sterilize the filled ampoules by moist heat at 121℃ for 20 minutes. Each 5mL ampoule contains 5mg of hymenoplasmin.

[0097] The above description is merely a preferred embodiment of the present invention and is not intended to limit the present invention in any way. Therefore, any simple modifications, equivalent changes, and alterations made to the above embodiments based on the technical essence of the present invention without departing from the scope of the present invention shall still fall within the scope of the present invention.

Claims

1. A compound having a strong purgative and water-repellent effect, characterized in that, It has the chemical structural formula shown in formula (I):

2. A pharmaceutical composition, characterized in that, Includes the compound described in claim 1.

3. The pharmaceutical composition according to claim 2, characterized in that, The pharmaceutical composition also includes a pharmaceutically acceptable carrier and / or excipients.

4. A method for preparing the compound of claim 1, characterized in that, Includes the following steps: a. Take the dried rhizomes of *Liriope muscari*, crush them, extract them with an organic solvent, filter them, concentrate them, and obtain a fluid extract; b. Add the fluid extract to water, stir, filter, wash with water, dry, and obtain a precipitate; c. Separate the precipitate by silica gel column chromatography, eluting with a petroleum ether-ethyl acetate gradient of 10:0 to 0:

10. d. Detect column chromatography fractions, combine, concentrate, and obtain the compound.

5. The method according to claim 4, characterized in that, The organic solvent is any one or more of methanol, ethanol, ethyl acetate, acetone, chloroform, and petroleum ether.

6. The method according to claim 4, characterized in that, The ratio of water lily to organic solvent is 1g:3-5mL.

7. The method according to claim 4, characterized in that, In step d, the column chromatography fraction is detected by thin-layer chromatography or liquid chromatography.

8. The use of the compound of claim 1 or the pharmaceutical composition of claim 2 in the preparation of a drug for draining ascites.

9. The application according to claim 8, characterized in that, The compound is formulated into a pharmaceutically acceptable dosage form in either monomeric form or as a plant extract containing it.

10. The application according to claim 9, characterized in that, The dosage form contains a pharmaceutically acceptable carrier and / or excipients.

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