Application of sulfydryl derivative in preparation of weight-losing product
By using thiol derivatives such as dithiol succinic acid and trimerthiocyanic acid to prepare weight loss products, the problems of limited types of existing weight loss drugs and poor results in lifestyle intervention therapy have been solved, and significant weight loss effects have been achieved.
Patent Information
- Application Number
- CN202510689860.9
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-05-27
- Publication Date
- 2025-07-11
AI Technical Summary
There are limited types of weight loss drugs and adverse reactions. The existing lifestyle intervention therapy is difficult to effectively lose weight, and there is a huge clinical need.
Thiodo derivatives such as dithiopolysuccinic acid and trimerthiocyanic acid are used as active ingredients of weight loss products to prepare medicines or health products, including fillers, binders and other auxiliary materials. The dosage form is granules or injections.
Through animal experiments, thiol derivatives significantly inhibit weight gain and effectively alleviate obesity, especially for simple or secondary obesity.
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Figure CN120284936A_ABST
Abstract
Description
Technical Field
[0001] The invention belongs to the field of medical technology, and particularly relates to the application of thiol derivatives in the preparation of weight loss products. Background Art
[0002] There are many causes of overweight and obesity, including genetic and environmental factors, changes in metabolism and endocrine function, bad living and eating habits, and mental and psychological factors. Studies have found that obesity can not only induce chronic diseases, including cardiovascular disease, diabetes, insulin resistance, and metabolic syndrome, but also increase the risk of cancer. Therefore, weight loss treatment has become an urgent problem that needs to be solved.
[0003] Lifestyle intervention therapy dominated by diet and exercise is a more recommended method, but for many people, lifestyle changes are very difficult, and this method is not always effective. The use of drugs is one of the necessary options for weight loss. The American Endocrine Society Guidelines (Pharmacological Management of Obesity: An Endocrine Society Clinical Practice Guideline) point out that if the weight loss is ≥5% within 3 months after using the drug, it is recommended to continue taking the drug. However, at present in Europe and China, the only weight loss drug approved for marketing by the drug regulatory authorities is orlistat. The types of weight loss drugs approved for marketing by the US drug regulatory authorities are also very limited, and there are many adverse reactions. Some drugs for treating other diseases also have a certain role in assisting weight loss, such as the hypoglycemic drug metformin, SGLT2 inhibitors, anti-epileptic drugs zonisamide, topiramate, etc., but they often have limited efficacy. At present, there is still a huge clinical demand for new weight loss drugs.
[0004] Thiol derivatives are a class of organic molecules with thiol (-SH) functional groups. Thiol plays an important role in chemical reactions. It can participate in the formation of disulfide bonds and form complexes with metal ions. It has the characteristics of reducing and oxygen absorbing properties. Common thiol derivatives include cysteine, glutathione and thioredoxin. These compounds play important physiological roles in organisms. For example, cysteine participates in intracellular redox reactions and protein stability, glutathione is a natural detoxifier, and thioredoxin is widely used in medicine and cosmetics. In addition, thiol derivatives can also participate in drug synthesis and have potential pharmacological effects. Summary of the invention
[0005] The present invention aims at the problems existing in the prior art and provides the application of thiol derivatives in the preparation of weight loss products.
[0006] To achieve the above purpose, the technical solution adopted by the present invention is as follows: Use of a mercapto derivative in the preparation of a weight loss product, wherein the mercapto derivative is selected from one or more of 2,3-dimercaptopropionic acid, dimercaptopropanesulfonic acid, dimercaptosuccinic acid, dimercaprol, trithiocyanuric acid, and salts or esters of the above compounds.
[0007] Preferably, the mercapto derivative is selected from one of 2,3-dimercaptopropionic acid, dimercaptosuccinic acid, trithiocyanuric acid, and salts or esters of the above compounds.
[0008] More preferably, the mercapto derivative is selected from one of dimercaptosuccinic acid, trithiocyanuric acid, and salts or esters of the above compounds.
[0009] Preferably, the mercapto derivative is the only active ingredient or one of the active ingredients in the weight loss product.
[0010] Preferably, the weight loss refers to non-drug-induced obesity.
[0011] More preferably, the obesity is simple obesity or secondary obesity.
[0012] Preferably, the product is a drug or a health product.
[0013] Preferably, the product further comprises excipients acceptable in drugs or health products.
[0014] Preferably, the excipients include at least one of fillers, binders, wetting agents, disintegrants, absorption promoters, surfactants, adsorption carriers, lubricants, and flavoring agents.
[0015] Preferably, the dosage form of the product is pills, oral liquids, granules, tablets, capsules, injections, or ointments.
[0016] More preferably, the dosage form of the product is granules or injections.
[0017] Compared with the prior art, the present invention has the following beneficial effects: Through animal experiments, the present invention detected the body weights of mice and fully verified that mercapto derivatives, especially dimercaptosuccinic acid and trithiocyanuric acid, have a significant weight loss effect and can effectively inhibit weight gain. Description of the Drawings
[0018] Figure 1 It is a graph of the body weights of mice in the normal control group and the model group before drug administration intervention.
[0019] Figure 2 It is a graph of the body weights of mice in each group during drug administration intervention from Day 0 to Day 29.
[0020] Figure 3 It is a graph of the body weights of mice in each group on Day 29 of drug administration intervention.
[0021] Figure 1 and Figure 3 In the table, compared with the normal control group, * indicates P < 0.05, **** indicates P < 0.0001; compared with the model group, # indicates P < 0.05. DETAILED DESCRIPTION
[0022] It is worth noting that the raw materials used in the present invention are all common commercially available products. Among them, dithiosuccinic acid, batch number 240901, was purchased from Shanghai SPH Ruier Pharmaceutical Co., Ltd.; thiocyanic acid, purity 95%, was purchased from Aladdin; high-fat feed, item number D12492, was purchased from Research Diets.
[0023] Example 1. Research objects: Succinic acid and thiocyanic acid.
[0024] Among them, take 250 mg of dimercaptosuccinic acid and add it to 41.67 mL of normal saline to prepare a 6 mg / mL dimercaptosuccinic acid solution, and store it in the dark; take 200 mg of thiocyanate and add it to 50 mL of normal saline to prepare a 4 mg / mL dimercaptosuccinic acid solution, and keep it aside.
[0025] 2. Experimental animals: 24 3-week-old C57BL / 6 mice, half male and half female, were purchased from Jiangsu Jicui Yaokang Biotechnology Co., Ltd., with the experimental animal production license number: SCXK (Su) 2023-0009. All mice were placed in a breeding room with a temperature control of 20-26°C and a relative humidity of 40-70%, and were allowed to eat and drink freely.
[0026] 3. Animal model establishment: C57BL / 6 mice were continuously fed a high-fat diet for 8 weeks. During this period, the mice were allowed to eat and drink freely. The weight changes of the mice were closely monitored. At the end of the 8th week, the weight of the mice was about 20% higher than that of the mice on a normal diet. The obesity model was successfully established. The mice were weighed once a week during the modeling period.
[0027] 4. Experimental grouping and administration: C57BL / 6 mice were divided into a normal control group, a model group, a dimercaptosuccinic acid group, and a thiocyanate group, a total of 4 groups, 6 mice in each group. Except for the normal control group mice fed with ordinary feed, the mice in the other groups were fed with a high-fat diet to establish an obesity model. After the model was successfully established, the mice in the dimercaptosuccinic acid group were given 30 mg / kg dimercaptosuccinic acid, and the mice in the thiocyanate group were given 20 mg / kg thiocyanate, once a day, by gavage at a volume of 5 mL / kg; the mice in the normal control group were gavaged with an equal volume of normal saline for 4 weeks. The mice were weighed every 2 days during the administration period.
[0028] 5. Statistical analysis: The body weight of mice was measured using a precision electronic scale every week, and the average value was calculated. Statistical analysis was performed using SPSS 19.0. The independent samples t-test was used to compare the differences between the two groups; one-way ANOVA was used for multiple groups. The significance level was set at α = 0.05.
[0029] 6. Experimental results: The experimental results are shown as follows. Figures 1-3 As can be seen from Figure 1 , before the administration intervention, the body weight of the normal control group was 27.94 g, while that of the model group reached 36.04 g. The initial body weight of the normal control group was significantly lower than that of the model group (P < 0.0001), indicating successful modeling.
[0030] As can be seen from Figure 2 , on Day 7 of the administration intervention, the body weight of the dimercaptosuccinic acid group began to be significantly lower than that of the model group. After that, it fluctuated, but on Days 19 - 29 of the intervention, the body weight was significantly lower than that of the model group; while for the trithiocyanuric acid group, the body weight on Days 11 - 29 of the administration intervention was significantly lower than that of the model group, and there was no significant difference between the two groups.
[0031] As can be seen from Figure 3 , on Day 29 of the administration intervention, although the body weights of the mice in the model group, dimercaptosuccinic acid group, and trithiocyanuric acid group were all higher than those in the normal control group, the body weights of the mice in the dimercaptosuccinic acid group and trithiocyanuric acid group were significantly lower than that of the model group (P < 0.05), indicating that both dimercaptosuccinic acid and trithiocyanuric acid can significantly alleviate the weight gain of obese mice.
[0032] Finally, it should be noted that the above content is only used to illustrate the technical solution of the present invention, rather than limiting the protection scope of the present invention. Any simple modification or equivalent replacement of the technical solution of the present invention by those of ordinary skill in the art shall not depart from the essence and scope of the technical solution of the present invention.
Claims
1. Use of a mercapto derivative in the preparation of a weight loss product, characterized in that, The mercapto derivative is selected from one or more of 2,3-dimercaptopropionic acid, dimercaptopropanesulfonic acid, dimercaptosuccinic acid, dimercaprol, trithiocyanuric acid, and salts or esters of the above compounds.
2. The application according to claim 1, wherein The mercapto derivative is selected from one of 2,3-dimercaptopropionic acid, dimercaptosuccinic acid, trithiocyanuric acid, and salts or esters of the above compounds.
3. The application according to claim 2, characterized in that, The mercapto derivative is selected from one of dimercaptosuccinic acid, trithiocyanuric acid, and salts or esters of the above compounds.
4. The application according to claim 1, wherein The mercapto derivative is the only active ingredient or one of the active ingredients in the weight loss product.
5. The application according to claim 1, characterized in that, The weight loss refers to non-drug obesity, and the obesity is simple obesity or secondary obesity.
6. The application according to claim 1, characterized in that The product is a drug or a health product.
7. The application according to claim 6, wherein The product further includes excipients acceptable in drugs or health products.
8. The application according to claim 7, characterized in that, The excipients include at least one of fillers, binders, wetting agents, disintegrants, absorption promoters, surfactants, adsorption carriers, lubricants, and flavoring agents.
9. The application according to claim 1, wherein The dosage form of the product is pills, oral liquids, granules, tablets, capsules, injections, or ointments.
10. The application according to claim 9, wherein The dosage form of the product is granules or injections.