阅读说明：本技术 波尔定碱或其盐在制备降低血尿酸水平、防治尿酸性肾病的药品中的用途 (Application of boldine or its salt in preparing medicine for reducing blood uric acid level and preventing and treating uric acid nephropathy ) 是由 马良 付平 于 2019-12-02 设计创作，主要内容包括：本发明涉及波尔定碱或其盐在制备降低血尿酸水平、防治尿酸性肾病的药品中的用途,属于医药领域。一方面,本发明提供了波尔定碱或其盐在制备降低血尿酸水平的药品或保健品中的用途。另一方面,本发明还提供了波尔定碱或其盐在制备预防和/或治疗尿酸性肾病的药品中的用途。动物实验证明,波尔定碱能够大幅降低血尿酸水平,同时改善高尿酸血症小鼠肾小管扩张、坏死以及肾纤维化的程度。本发明的应用能够为临床治疗高尿酸血症及其导致的高尿酸肾病提供新的用药选择。(The invention relates to an application of boldine or salt thereof in preparing a medicine for reducing the level of uric acid and preventing and treating uric acid nephropathy, belonging to the field of medicines. In one aspect, the invention provides the use of boldine or a salt thereof in the manufacture of a medicament or health product for reducing the level of uric acid in blood. In another aspect, the invention also provides the use of boldine or its salt in the preparation of a medicament for the prevention and/or treatment of uric acid nephropathy. Animal experiments prove that the boldine can greatly reduce the blood uric acid level and improve the degree of the hyperuricemia mouse renal tubule dilatation, necrosis and renal fibrosis. The application of the invention can provide a new drug selection for clinical treatment of hyperuricemia and hyperuricemia nephropathy caused by the hyperuricemia.)

1. Use of boldine or its salt in preparing medicine or health product for reducing blood uric acid level is provided.

2. Use of boldine or its salt in preparing medicine for preventing and/or treating uric acid nephropathy.

3. Use according to claim 2, characterized in that: the drug reduces blood creatinine levels.

4. Use according to claim 2, characterized in that: the medicine reduces the blood uric acid level.

5. Use according to claim 2, characterized in that: the medicine reduces the urinary protein creatinine ratio.

6. Use according to claim 2, characterized in that: the medicament improves tubular dilation and/or necrosis.

7. Use according to claim 2, characterized in that: the medicament reduces the number of renal inflammatory cells.

8. Use according to claim 2, characterized in that: the medicine can improve renal fibrosis.

9. Use according to any one of claims 1 to 8, characterized in that: the medicine or health care product is a preparation prepared by taking the boldine or the salt thereof as an active ingredient and adding acceptable auxiliary materials or auxiliary ingredients.

10. Use according to claim 9, characterized in that: the preparation is an oral preparation or an injection preparation.

Technical Field

The invention relates to an application of boldine or salt thereof in preparing a medicine for reducing the level of uric acid and preventing and treating uric acid nephropathy, belonging to the field of medicines.

Background

Hyperuricemia refers to non-daily measurement of fasting serum uric acid levels of greater than or equal to 416 μmol/L (7mg/dl) in men and equal to 357 μmol/L (6mg/dl) in women under normal purine diet. In recent years, numerous studies at home and abroad prove that hyperuricemia is closely related to the occurrence and development of gout, cardiovascular diseases, metabolic syndrome, hypertension and kidney diseases. Hyperuricemia is a significant cause of increased prevalence of Chronic Kidney Disease (CKD) and is an independent risk factor for CKD progression. Studies have shown that lowering the level of uric acid in the blood can delay the progression of renal disease. Treating hyperuricemia, preventing and correcting hyperuricemia, lowering blood uric acid level and preventing urate from depositing in kidney.

Boldine base (Boldine), chemical name 2, 9-dihydroxy-1, 10-dimethoxy aporphine, has the following structural formula:

prior studies have shown that boldine can inhibit low density lipoprotein oxidation in vitro and Atherosclerosis in vivo, prevent lipid peroxidation and cytochrome P4502E1 inactivation in human liver microsomes, and prevent some diseases caused by oxidation of mitochondria (see: Santanam N, Penumetcha M, Speisky H, et al. A novel alkaline antioxidant, binder and synthetic antioxidant, reduced form of RU486, inhibition of oxidation of LDL-control and alkaline adsorption in vivo LDLR- () microorganism [ J. Atherosclerosis,2004,173(2): 203. 210.). In addition, boldine is also an anticancer drug that is widely used in some areas.

However, reports on the effects of the boldine in reducing uric acid and preventing and treating the uric acid nephropathy are not found so far.

Disclosure of Invention

The present invention is directed to solving at least one of the problems of the prior art. Therefore, the invention aims to provide the application of the boldine or the salt thereof in preparing medicines or health care products for reducing the level of hematuria. Another object of the present invention is to provide a use of boldine or a salt thereof for the preparation of a medicament for the prevention and/or treatment of uric acid nephropathy.

The invention provides an application of boldine or salt thereof in preparing a medicine or health-care product for reducing the level of hematuria acid.

The invention provides an application of boldine or salt thereof in preparing a medicine for preventing and/or treating uric acid nephropathy.

Further, the pharmaceutical product reduces blood creatinine levels.

Further, the drug lowers blood uric acid levels.

Further, the drug lowers the urinary protein creatinine ratio.

Further, the drug improves tubular dilation and/or necrosis.

Further, the medicament reduces the number of renal inflammatory cells.

Further, the medicine improves renal fibrosis.

Furthermore, the medicine or the health care product is a preparation prepared by taking the boldine or the salt thereof as an active ingredient and adding acceptable auxiliary materials or auxiliary ingredients.

Further, the preparation is an oral preparation or an injection preparation.

In the present invention, the salt of the boldine base refers to an acid and/or base salt of the boldine base with an inorganic acid and/or base, an organic acid and/or base, and also includes a zwitterionic salt (inner salt), and also includes a quaternary ammonium salt such as an alkylammonium salt. The salt according to the invention may be, for example, the hydrochloride, sulfate, citrate, benzenesulfonate, hydrobromide, hydrofluoride, phosphate, acetate, propionate, succinate, oxalate, malate, succinate, fumarate, maleate, tartrate or trifluoroacetate salt of boldine.

The invention provides application of boldine or salt thereof in preparing a medicine for reducing the level of uric acid and preventing and treating uric acid nephropathy. Animal experiments prove that the boldine can greatly reduce the blood uric acid level and improve the degree of the hyperuricemia mouse renal tubule dilatation, necrosis and renal fibrosis. The application of the invention can provide a new drug selection for clinical treatment of hyperuricemia and hyperuricemia nephropathy caused by the hyperuricemia.

Drawings

FIG. 1 is a graph showing the results of measurement of the blood uric acid level of a mouse in example 1;

FIG. 2 is a graph showing the results of measurement of the serum creatinine level of the mouse in example 1;

FIG. 3 is a graph showing the results of measurement of the ratio of mouse urine protein to creatinine in example 1;

FIG. 4 is a PAS staining pattern of mouse kidney tissue in example 1;

FIG. 5 is a graph of MASSON staining of mouse kidney in example 1.

Detailed Description

The scheme of the invention will be explained with reference to the examples. It will be appreciated by those skilled in the art that the following examples are illustrative of the invention only and should not be taken as limiting the scope of the invention. The examples, where specific techniques or conditions are not indicated, are to be construed according to the techniques or conditions described in the literature in the art or according to the product specifications. The reagents or instruments used are not indicated by the manufacturer, and are all conventional products commercially available.