Application of mogroside V in preparation of anti-renal fibrosis medicine

Monk fruit saponin V, through multi-target synergistic action, solves the problem of large toxic side effects of existing anti-renal fibrosis drugs, significantly improves renal function and inhibits fibrosis progression, providing a new approach for natural drugs in the treatment of renal fibrosis, and is suitable for the preparation of renal protection products in various dosage forms.

CN120919147APending Publication Date: 2025-11-11GUANGDONG PHARMA UNIV
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Patent Information

Application Number
CN202511167138.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-08-20
Publication Date
2025-11-11

AI Technical Summary

Technical Problem

Existing anti-renal fibrosis drugs have significant toxic side effects and incomplete treatment, and current technologies have failed to effectively utilize the role of natural drugs in renal fibrosis.

Method used

Using mogroside V as the active ingredient, we develop drugs or health products for the preparation of anti-renal fibrosis. Through multi-target and multi-pathway synergistic effects, we utilize its anti-fibrotic effect in renal fibrosis, including the preparation of drugs for the prevention and/or treatment of obstructive nephropathy, renal fibrosis, and renal fibrosis secondary to urinary tract obstruction.

Benefits of technology

Monk fruit saponin V significantly improves renal function, reduces serum creatinine and blood urea nitrogen levels, inhibits the expression of renal fibrosis markers, and reduces collagen deposition. It is safe, effective, and has no side effects, making it suitable for preparing renal protection products in different dosage forms to meet clinical treatment and daily health care needs.

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Abstract

The invention discloses application of mogroside V in preparation of an anti-renal fibrosis medicine, and belongs to the technical field of biological medicines. Experiments prove that the mogroside V can obviously improve the renal function of a mouse with renal fibrosis, and the serum creatinine and blood urea nitrogen levels are obviously reduced. Meanwhile, the compound can be used for effectively inhibiting the expression of fibrosis markers alpha-SMA and Fibronectin in renal tissues, and delaying the fibrosis process by up-regulating the expression level of an epithelial-mesenchymal transition marker E-cadherin. In addition, the mogroside V can also significantly reduce collagen deposition in kidney tissues, and plays a role in treating renal fibrosis. The traditional Chinese medicine composition has the advantages of safety, effectiveness, no side effect, good taste and the like when being used for preparing the anti-renal fibrosis medicine.
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Description

Technical Field

[0001] This invention belongs to the field of biomedical technology, specifically relating to the application of mogroside V in the preparation of anti-renal fibrosis drugs. Background Technology

[0002] Renal fibrosis is the core pathological process in the progression of chronic kidney disease (CKD) to end-stage renal disease (ESRD). It is characterized by myofibroblast activation and migration, tubular epithelial-mesenchymal transition (EMT), and excessive deposition of extracellular matrix (ECM), ultimately leading to irreversible loss of renal function. Key pathological changes include glomerular sclerosis, tubulointerstitial fibrosis, and renal scarring.

[0003] Besides renal fibrosis, organ fibrosis also includes liver fibrosis and pulmonary fibrosis, but the pathological manifestations, mechanisms, and regulatory pathways of fibrosis differ significantly among different organs. For example, the core driving factor of liver fibrosis is the activation of hepatic stellate cells (HSCs), while renal fibrosis mainly involves mechanisms such as the proliferation of renal interstitial fibroblasts, podocyte injury, and epithelial-mesenchymal transition (EMT). Furthermore, the weights of signaling pathways such as TGF-β1 / Smads and AngII / CTGF vary in different organ fibrosis cases. Therefore, even if a drug shows good efficacy in other organ fibrosis, it cannot be directly inferred that it has the same efficacy in renal fibrosis without rigorous kidney-specific experimental verification.

[0004] Currently, first-line treatments for renal fibrosis, such as angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs), can only slow down but not stop the fibrosis process, and have side effects such as hyperkalemia.

[0005] With a better understanding of disease mechanisms and the advancement of modern science, the medical field has realized that relying solely on single-target drugs is insufficient for a complex disease caused by the combined effects of multiple genetic and environmental factors.

[0006] Traditional Chinese medicine (TCM), based on the principle of "treating the symptoms as the root cause" and minimizing toxic side effects, is gradually gaining popularity. The synergistic effect of multiple targets and pathways is a key characteristic of TCM treatment. This approach can be more rational and effective for complex, chronic, multifactorial diseases like renal fibrosis, making natural Chinese herbal medicines a crucial direction for drug research and development in the treatment of renal fibrosis.

[0007] Monk fruit (Swingle) is a perennial vine mainly cultivated in southern China. Traditional Chinese medicine considers it to be sweet and cool in nature, entering the lung and large intestine meridians. It is a natural sweetener, and regular consumption is beneficial to health. The Chinese Pharmacopoeia records that it "clears heat and moistens the lungs, lubricates the intestines and promotes bowel movements, used for dry cough due to lung heat, sore throat and loss of voice, and constipation due to intestinal dryness." It is one of the first batch of medicinal and edible materials in my country.

[0008] Monk fruit is rich in nutrients, and about 46 triterpenoid glycosides can be isolated from it, mainly including mogrosides I, III, IV, and V. Among them, mogroside V is the most abundant and has been the subject of the most extensive research.

[0009] Monk fruit saponin V is an amphiphilic cucurbitane tetracyclic triterpenoid saponin composed of hydrophobic glycosidic bonds and five hydrophilic sugar groups, with the molecular formula C2. 60 H 102 O 29 Its relative molecular mass is 1287.43, CAS number is 88901-36-4, and its chemical structure is shown below. Figure 1 Saponin A is the main sweet component in monk fruit, and its sweetness is about 300 times that of sucrose. It has been reported that monk fruit saponin V has a wide range of pharmacological and biological activities. However, its role in renal fibrosis has not yet been reported. Summary of the Invention

[0010] The present invention aims to solve at least one of the technical problems existing in the prior art. To this end, the present invention proposes the application of mogroside V in the preparation of anti-renal fibrosis drugs.

[0011] To achieve the above objectives, the present invention adopts the following technical solution:

[0012] This invention provides the use of mogroside V in any of the following:

[0013] (a1) Prepare drugs or health products for the prevention and / or treatment of obstructive nephropathy;

[0014] (a2) Prepare drugs or health products for the prevention and / or treatment of renal fibrosis;

[0015] (a3) Prepare drugs or health products for the prevention and / or treatment of renal fibrosis secondary to urinary tract obstruction;

[0016] (a4) Prepare medicines or health products for the prevention and / or treatment of other acute or chronic kidney diseases presenting as renal interstitial fibrosis.

[0017] In some embodiments, the obstructive nephropathy includes mechanical obstruction, dynamic obstruction, or extrinsic compressive obstruction; the mechanical obstruction includes obstruction caused by stones, tumors, inflammation, or congenital malformations.

[0018] In some embodiments, the drug or health product further includes pharmaceutically or health-product-acceptable excipients, such as pharmaceutically acceptable carriers and / or pharmaceutical carriers.

[0019] In some embodiments, the pharmaceutically acceptable carrier may be any one or more of buffers, emulsifiers, suspending agents, stabilizers, preservatives, excipients, fillers, coagulants, blending agents, surfactants, dispersants, and defoamers.

[0020] In some embodiments, the filler includes, but is not limited to, one or more of microcrystalline cellulose, pregelatinized starch, hydroxypropyl cellulose, and polyethylene glycol.

[0021] In some embodiments, the pharmaceutical carrier includes any one or more of microcapsules, liposomes, nanoparticles, and polymers.

[0022] In some embodiments, the excipients acceptable for the health product include at least one of sweeteners, acidulants, anti-caking agents, and gliding agents.

[0023] In some embodiments, mogroside V is the sole active ingredient in the drug or health product.

[0024] In some embodiments, the drug further includes one or more active ingredients or activators, which are other traditional Chinese medicinal materials (such as Scutellaria baicalensis, Salvia miltiorrhiza, etc.) or chemical drugs with anti-fibrotic effects.

[0025] In some embodiments, the dosage form of the drug includes tablets, capsules, granules, pills, oral liquids, injections, sprays, or lozenges.

[0026] In some embodiments, the drug is administered orally.

[0027] In some embodiments, the purity of mogroside V used as a raw material in the drug or health product is 1-99%.

[0028] In some embodiments, the purity of mogroside V used as a raw material in the drug or health product is greater than or equal to 98%.

[0029] In summary, compared with the prior art, the present invention achieves the following technical effects:

[0030] This invention provides the application of mogroside V in the preparation of anti-renal fibrosis drugs, expands the treatment options for monomeric drugs in renal fibrosis, provides a theoretical basis for finding new natural drug targets for the prevention and treatment of renal fibrosis, and offers a new approach for further research and clinical translation in nephrology.

[0031] This invention experimentally verified that mogroside V can significantly improve renal function in mice with renal fibrosis, as evidenced by a significant decrease in serum creatinine and blood urea nitrogen levels. Simultaneously, this component can effectively inhibit the expression of fibrosis markers α-SMA and Fibronectin in renal tissue, and delay the fibrosis process by upregulating the expression level of E-cadherin, an epithelial-mesenchymal transition (EMT) marker. Furthermore, mogroside V can significantly reduce collagen deposition in renal tissue, thus exhibiting a therapeutic effect on renal fibrosis. Its use in the preparation of anti-renal fibrosis drugs has advantages such as safety, efficacy, no side effects, and pleasant taste.

[0032] Developing monk fruit saponin V or its combinations into kidney-protective products in different dosage forms can meet the dual needs of clinical treatment and daily health care, and has broad market application prospects. Attached Figure Description

[0033] Figure 1 This is the network pharmacological analysis result of mogroside V and renal fibrosis in this invention; Figure 1 A is the chemical structural formula of mogroside V; Figure 1 B represents the use of the Venn diagram online website to merge and intersect mogro saponin V with disease-related targets, resulting in 292 duplicate targets. Figure 1 C represents the regulatory network of "drug-target-disease"; Figure 1 D represents the main biological processes, cellular components, and related molecular functions involved in the treatment of renal fibrosis with mogroside V. Figure 1 E represents the top ten core pathways involved in the KEGG enrichment analysis.

[0034] Figure 2 Monk fruit saponin V improves renal morphological changes in a C57 / BL6 mouse UUO model; Figure 2 A shows a photograph of the ligated kidney of each group of mice after the 7-day experiment. Figure 2 B represents the weight of the kidney on the ligated side; data are expressed as mean ± SD, ns: no significance, *p<0.05, **p<0.01, ***p<0.001, ****p<0.001, and statistical analysis was performed using a standard t-test.

[0035] Figure 3 Effects of monk fruit saponin V on serum creatinine and blood urea nitrogen in UUO model mice Figure 3 A represents the serum creatinine levels in UUO mice. Figure 3 B represents the serum urea nitrogen results of UUO mice. Data are presented as mean ± SD, where ns: not significant, *p<0.05, **p<0.01, ***p<0.001, ****p<0.001, and standard t-tests were used for statistical analysis.

[0036] Figure 4 Effects of monk fruit saponin V on renal tissue pathology in UUO renal fibrosis mice; Figure 4 A shows the Masson staining pattern and the quantitative analysis results of the positive area area in the staining results; Figure 4 B shows the Sirius red staining pattern and the quantitative analysis results of the positive area in the staining results. Data are presented as mean ± SD, where ns: not significant, *p<0.05, **p<0.01, ***p<0.001, ****p<0.001.

[0037] Figure 5 Effects of mogroside V on the expression of fibrosis markers in mouse kidney tissue; Figure 5 A represents the results of Western blot analysis of mouse kidney tissue after the 7-day experiment. Figure 5 B represents the statistical analysis of the results of the Western blot experiment. Figure 5 C represents the qRT-PCR results of mouse kidney tissue after 7 days of experimentation. Data are presented as mean ± SD, where ns: not significant, *p<0.05, **p<0.01, ***p<0.001, ****p<0.001, and standard t-tests were used for statistical analysis.

[0038] Figure 6 Effects of monk fruit saponin V on α-SMA expression in mouse kidney tissue; Figure 6 A represents the immunohistochemical staining results of the renal tubular interstitial region in the UUO group. Figure 6 B represents the quantitative analysis results of the positive area in the immunohistochemical staining results. Data are presented as mean ± SD, where ns: not significant, *p<0.05, **p<0.01, ***p<0.001, ****p<0.001, and standard t-tests were used for statistical analysis. Detailed Implementation

[0039] To further illustrate the technical means and effects of the present invention in achieving its intended purpose, the following detailed description of the specific implementation methods, structures, features, and effects of the present invention, in conjunction with the accompanying drawings and preferred embodiments, is provided below.

[0040] This invention aims to provide a novel use for mogroside V, a natural active ingredient with anti-renal fibrosis effects and minimal toxic side effects. Specifically, the inventors have discovered a natural organic compound, mogroside V, which has been experimentally proven to have anti-fibrotic effects and can be used to prevent and treat fibrotic diseases, especially renal fibrosis caused by unilateral ureteral obstruction (UUO). This provides a new solution to the problems of significant toxic side effects and incomplete treatment of existing anti-renal fibrosis drugs.

[0041] Through mouse experiments, the inventors discovered that: mogroside V can alleviate kidney lesions induced by UUO surgery in mice; mogroside V can reduce collagen deposition in the kidneys of UUO mice; and mogroside V has a significant anti-renal fibrosis effect and is not prone to recurrence after treatment.

[0042] This invention first analyzed the Swiss Target Prediction, PharmMapper, and Batman databases, identifying 382 targets related to mogroside V. Then, it screened and analyzed the Disgenet and GeneCards databases, identifying 7085 target genes closely related to renal fibrosis. Finally, the Venn diagram online website was used to merge drug-disease related targets and take the intersection, resulting in 292 duplicate targets. Figure 1 B). Using Cyctoscape software, these intersecting targets were visualized to create a regulatory network of "drug-target-disease". Figure 1 C), revealing the potential relationship between mogroside V and renal fibrosis.

[0043] Secondly, using the DAVID online database, GO and KEGG analyses were performed on the 292 key targets obtained to investigate the biological functions, molecular mechanisms, and pathways involved by mogroside V in treating renal fibrosis. In the GO analysis, the top ten significantly enriched terms in biological processes (BP), cellular components (CC), and molecular functions (MF) were identified. GO enrichment results showed that the biological processes mainly involved in mogroside V's treatment of renal fibrosis included the response to hypoxia, glutathione metabolism, and protein phosphorylation; GO-CC was mainly enriched in the cytoplasm and cell membrane; and molecular functions were mainly concentrated in fatty acid binding, steroid binding, ferrous ion binding, ATP binding, and glutathione peroxidase activity. Figure 1 D). The top ten core pathways involved in KEGG enrichment analysis include, for example... Figure 1 As shown in E.

[0044] This invention provides the application of mogroside V in the preparation of anti-renal fibrosis drugs. Mogroside V expands the treatment options for monomeric drugs in renal fibrosis, opening up new avenues for the development of anti-renal fibrosis drugs. In particular, mogroside V can significantly reduce serum creatinine and blood urea nitrogen levels in mice with renal fibrosis, thus achieving a therapeutic effect on renal fibrosis.

[0045] In this invention, the content of mogroside V in the anti-renal fibrosis drug is preferably 1-99%. In this invention, the purity of the mogroside V raw material used in the anti-renal fibrosis drug is greater than 98%. This invention does not have special requirements for the source of mogroside V; any source well-known to those skilled in the art is acceptable. The structural formula of mogroside V is as follows: Figure 1 As shown in A, the molecular formula is C. 60 H 102 O 29 The CAS number is 88901-36-4.

[0046] The present invention does not have any special limitation on the source of the mogroside V, and any mogroside V that can meet the above purity requirements can be used.

[0047] In this invention, the dosage form of the drug includes, but is not limited to, tablets, capsules, granules, sprays, injections, lozenges, pills, oral liquids, and microspheres.

[0048] This invention selects appropriate pharmaceutical excipients and determines their dosage and preparation method according to the specific requirements of the drug dosage form, without making any special limitations.

[0049] To further illustrate the present invention, the technical solutions provided by the present invention will be described in detail below with reference to the embodiments and accompanying drawings, but they should not be construed as limiting the scope of protection of the present invention.

[0050] Example

[0051] Unilateral ureteral ligation (UUO) is a stable and well-established classic animal model for studying renal fibrosis. It involves surgically ligating the left ureter in mice to simulate the process of renal interstitial fibrosis caused by urinary tract obstruction. Because it accelerates renal tubular damage caused by mechanical obstruction of the urinary system, it leads to excessive production of reactive oxygen species in the kidney, resulting in irreversible kidney damage. Its characteristics are similar to human renal fibrosis, almost perfectly replicating the same fibrotic events in humans.

[0052] Experimental mice were randomly divided into four groups: sham operation group (Sham), model group (UUO), mogroside V treatment group (50 mg / kg, UUO + MV 50), and mogroside V treatment group (100 mg / kg, UUO + MV 100), with seven mice in each group. Before unilateral ureteral ligation, mice received mogroside V treatment for three consecutive days. To facilitate accurate weighing of all mice and calculation of the required anesthesia dose, mice were fasted for 24 hours preoperatively but allowed free access to water, and received the medication continuously for seven days postoperatively.

[0053] Surgical Procedure: ① Hair Removal: Apply a small amount of hair removal cream to a sterile cotton swab and gently wipe away hair in a circular motion on the left side of the mouse's back; ② Anesthesia: Inject sodium pentobarbital into the mouse's peritoneal cavity at a dose of 50 mg / kg; ③ Ureter Ligation: Place the mouse on its left side and fix it on a temperature-controlled plate at approximately 37°C; then precisely locate the left dorsal side of the mouse and carefully make a tiny incision using surgical forceps. Through this incision, the left kidney can be clearly exposed. Next, carefully dissect the tissue connecting to the ureter. At the upper proximal part of the ureter, about one-third of the length of the entire duct, a ligation is made using silk thread. About 1 cm below this ligation point, a second ligation is made. Then, the ureter is gently cut between the two ligation points with scissors to prevent retrograde infection. ④ Suturing: First, suture the peritoneum and then suture the lateral skin. At the same time, thoroughly disinfect the skin area around the wound to prevent infection. ⑤ Place the mouse on a 37°C heating pad and wait for it to wake up from anesthesia. After the mouse wakes up, transfer it to an IVC cage for feeding.

[0054] The entire process was performed under aseptic conditions. The UUO group was treated with mogroside V via gavage for three days before surgery and for seven consecutive days after surgery; the Sham and UUO groups received PBS via gavage as a control. During the treatment period, the mice were weighed daily to observe their growth.

[0055] The following tests were performed on various indicators in each group of mice:

[0056] Test Example 1

[0057] In the examples, the ligated kidney of each group of mice was photographed after 7 days of experimentation. Figure 2 A) and weight statistics of the ligated kidney ( Figure 2 B). The results showed that treatment with mogroside V reduced renal structural damage in mice to varying degrees; the left kidney weight in the mogroside V treatment group was significantly lower than that in the untreated group, and this difference became more significant with increasing dosage. Figure 2 B, ns: meaningless, *p<0.05, **p<0.01, ***p<0.001, ****p<0.001).

[0058] Serological tests were performed on mice in each group after the 7-day experiment in the examples. The results are as follows: Figure 3 As shown.

[0059] Depend on Figure 3 It can be seen that the serum creatinine in UUO mice ( Figure 3 A) and blood urea nitrogen ( Figure 3 B) The significant decrease after treatment with mogroside V indicates that mogroside V has a good therapeutic effect on renal fibrosis.

[0060] Test Example 2

[0061] Masson staining was performed on the kidneys of mice at the end of the 7-day experiment in this example. Figure 4 A) and Sirius red staining ( Figure 4 B) Observe the deposition of collagen fibers in the kidney tissue of mice and quantitatively analyze the area of ​​positive regions in the staining results. The results showed that compared with the UUO group, the area of ​​collagen fibers in the kidneys of mice treated with mogroside V was significantly reduced (masson staining showed blue areas of collagen fibers, and Sirius red staining showed bright red areas of collagen fibers), indicating a reduction in the degree of fibrosis.

[0062] Morphological analysis of fibrotic tissue (based on) Figure 4 A&4B)

[0063] 1. Masson staining ( Figure 4 A)

[0064] (1) Sham surgery group

[0065] Renal tubules: regular in shape, with tightly packed epithelial cells, pink cytoplasm, and an intact basement membrane (light blue thread-like);

[0066] Interstitial region: Only a very small amount of blue collagen fibers (normal connective tissue component) are observed.

[0067] (2) UUO group

[0068] Renal tubules: extensive atrophy / dilation, flattening of epithelial cells (reduction of pink area), partial disintegration of tubular structures;

[0069] Interstitial fibrosis: Diffuse deposition of large amounts of dark blue collagen fibers, forming coarse cords or sheet-like areas (indicated by arrows);

[0070] Inflammatory infiltration: Lymphocyte aggregation can be seen in the interstitium.

[0071] (3) Monk fruit saponin V treatment group

[0072] Renal tubular structure: The degree of atrophy has decreased, and the morphology of some tubules is close to normal;

[0073] Collagen deposition: The area of ​​the blue region is significantly reduced, and the residual collagen is distributed in a fine network (vs. the dense deposition of the UUO group).

[0074] 2. Sirius red staining ( Figure 4 B)

[0075] Staining characteristics:

[0076] Type I collagen (mature fibers): bright red, arranged in large bundles (dominated by UUO group);

[0077] Other tissue components, such as cytoplasm, are pale pink or colorless, forming a striking contrast with the red-stained collagen fibers, making it easy to distinguish different tissue structures.

[0078] Test Example 3

[0079] Observations of mice after the 7-day experiment in the sham-operated group showed that both kidneys were of uniform size, normal in shape, reddish-brown in color, with smooth and intact capsules, relatively elastic, easy to cut, and with a clear boundary between the cortex and medulla. In the surgical group, the obstructed kidney (left side) was significantly larger than the normal kidney (right side), with unequal size. The obstructed kidney was a pale pink color, with an uneven capsule, and connective tissue adhesions around it, making it difficult to separate. The kidney elasticity was weakened, and there was greater resistance when cutting. At the same time, a yellowish-brown fluid flowed out. After cutting, the renal cortex and medulla were blurred, the renal cortex was thinned, and there was varying degrees of dilation of the renal pelvis and calyces. Among the groups, the UUO group showed significantly more severe obstruction. The drug-treated group showed less obstructed urine and less renal structural damage than the UUO group.

[0080] Test Example 4

[0081] H&E pathological staining was performed on mice after the 7-day experiment in the example. Compared with sham-operated mice, UUO mice induced renal fibrosis with inflammatory cell infiltration, varying degrees of vascular collapse, glomerular atrophy, renal tubular dilation, and renal tubular epithelial cell detachment into the lumen and lumen destruction.

[0082] Test Example 5

[0083] Western blotting was performed on mouse kidney tissues after the 7-day experiment to detect the expression levels of fibrosis-related markers. The results showed that mogroside V reduced the expression of α-SMA and Fibronectin in the kidneys, while increasing the expression of E-cadherin (e.g., ...). Figure 5 A and Figure 5 (as shown in B).

[0084] qRT-PCR results showed that mogroside V could reduce the expression levels of α-SMA and fibrinectin in the kidney tissue of UUO mice at the mRNA level, and upregulate the expression of E-cadherin (e.g., Figure 5 (As shown in C), this is consistent with changes in protein expression levels.

[0085] Renal interstitial fibroblasts and myofibroblasts are the main causes of excessive ECM production. α-Smooth muscle actin (α-SMA) is a molecular marker of myofibroblasts; therefore, α-SMA levels are directly proportional to the degree of fibrosis. Immunohistochemical staining showed significantly increased α-SMA expression in the tubulointerstitial region of the UUO group, staining a brownish-red color. Figure 6 A). In the groups treated with mogroside V at 50 mg / kg and 100 mg / kg, the α-SMA positive areas were reduced, and the staining intensity decreased. Quantitative analysis of the α-SMA positive area showed that it was 21.79% and 15.48% respectively, compared to 27.3% for UUO positive areas. Mogroside V intervention significantly inhibited the upregulation of α-SMA expression and alleviated UUO-induced renal fibrosis. Figure 6 B, ns: meaningless, *p<0.05, **p<0.01, ***p<0.001, ****p<0.001).

[0086] As can be seen from the above examples and test cases, monk fruit saponin V has a significant therapeutic effect on renal fibrosis.

[0087] Because the UUO animal model can simulate the progression of acute kidney injury to fibrosis caused by mechanical urinary tract obstruction (such as stones or tumor compression), its pathological features (such as TGF-β / Smad pathway activation, inflammatory cell infiltration, and ECM deposition) are highly similar to those of human obstructive nephropathy. Monk fruit saponin V can improve renal morphology and function in UUO mice, reduce renal collagen deposition and fibrotic protein (α-SMA, Fibronectin) expression, and upregulate E-cadherin protein levels. It significantly inhibited the progression of renal interstitial fibrosis in the UUO model, suggesting its potential for prevention and / or treatment of acute kidney injury and secondary fibrosis caused by urinary tract obstruction.

[0088] Since monk fruit saponin V is derived from monk fruit (Siraitia grosvenorii), and according to the regulations of the National Health Commission of the People's Republic of China, monk fruit is listed as one of the first batch of medicinal and edible herbs, it can be used both as a medicinal herb and as food. Therefore, using monk fruit saponin V can effectively overcome the toxic side effects of current first-line treatments for renal fibrosis and can be used to prepare drugs or health products for the prevention and / or treatment of other acute or chronic kidney diseases manifested as renal interstitial fibrosis.

[0089] Developing monk fruit saponin V or its combinations into kidney-protective products in different dosage forms can meet the dual needs of clinical treatment and daily health care, and has broad market application prospects.

[0090] The above description is merely a preferred embodiment of the present invention and is not intended to limit the present invention in any way. Although the present invention has been disclosed above with reference to preferred embodiments, it is not intended to limit the present invention. Any person skilled in the art can make some modifications or alterations to the above-disclosed technical content to create equivalent embodiments without departing from the scope of the present invention. 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. The application of mogroside V in any of the following, characterized in that, include: (a1) Prepare drugs or health products for the prevention and / or treatment of obstructive nephropathy; (a2) Prepare drugs or health products for the prevention and / or treatment of renal fibrosis; (a3) Prepare drugs or health products for the prevention and / or treatment of renal fibrosis secondary to urinary tract obstruction; (a4) Prepare medicines or health products for the prevention and / or treatment of other acute or chronic kidney diseases presenting as renal interstitial fibrosis.

2. The application according to claim 1, characterized in that, The obstructive nephropathy includes mechanical obstruction, dynamic obstruction, or extrinsic compressive obstruction; the mechanical obstruction includes obstruction caused by stones, tumors, inflammation, or congenital malformations.

3. The application according to claim 1, characterized in that, The drug or health product also includes pharmaceutically or health product-acceptable excipients.

4. The application according to any one of claims 1-3, characterized in that, The drug or health product in which monk fruit saponin V is the only active ingredient.

5. The application according to any one of claims 1-3, characterized in that, The drug also includes one or more active ingredients or activators, which are other traditional Chinese medicinal materials or chemical drugs with anti-fibrotic effects.

6. The application according to claim 1, characterized in that, The dosage forms of the drug include tablets, capsules, granules, pills, oral liquids, injections, sprays, or lozenges.

7. The application according to claim 1, characterized in that, The drug can be administered orally.

8. The application according to claim 1, characterized in that, The purity of mogroside V used as a raw material in the aforementioned medicine or health product is 1-99%.

9. The application according to claim 7, characterized in that, The purity of mogroside V used as a raw material in the drug or health product is greater than or equal to 98%.

Citation Information

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