CN116549427A - New use of hydroxycitric acid for treating cholelithiasis and cholecystitis induced by cholelithiasis - Google Patents
New use of hydroxycitric acid for treating cholelithiasis and cholecystitis induced by cholelithiasis Download PDFInfo
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- CN116549427A CN116549427A CN202310607581.4A CN202310607581A CN116549427A CN 116549427 A CN116549427 A CN 116549427A CN 202310607581 A CN202310607581 A CN 202310607581A CN 116549427 A CN116549427 A CN 116549427A
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- hydroxycitric acid
- cholelithiasis
- cholecystitis
- hydroxycitric
- induced
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- ZMJBYMUCKBYSCP-UHFFFAOYSA-N Hydroxycitric acid Chemical compound OC(=O)C(O)C(O)(C(O)=O)CC(O)=O ZMJBYMUCKBYSCP-UHFFFAOYSA-N 0.000 title claims abstract description 34
- 229940089491 hydroxycitric acid Drugs 0.000 title claims abstract description 24
- 201000001352 cholecystitis Diseases 0.000 title claims abstract description 10
- 201000001883 cholelithiasis Diseases 0.000 title claims description 19
- 239000003814 drug Substances 0.000 claims abstract description 11
- VYYWVGGAJXBBCA-YIRLFHOGSA-K tripotassium;(1s,2s)-1,2-dihydroxypropane-1,2,3-tricarboxylate Chemical compound [K+].[K+].[K+].[O-]C(=O)[C@@H](O)[C@](O)(C([O-])=O)CC([O-])=O VYYWVGGAJXBBCA-YIRLFHOGSA-K 0.000 claims description 8
- RVEPHTVUPANNSH-UHFFFAOYSA-H tricalcium;1,2-dihydroxypropane-1,2,3-tricarboxylate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]C(=O)C(O)C(O)(C([O-])=O)CC([O-])=O.[O-]C(=O)C(O)C(O)(C([O-])=O)CC([O-])=O RVEPHTVUPANNSH-UHFFFAOYSA-H 0.000 claims description 7
- 150000002596 lactones Chemical class 0.000 claims description 6
- IRBQOWGQMRVZMV-UHFFFAOYSA-K trisodium;1,2-dihydroxypropane-1,2,3-tricarboxylate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C(O)C(O)(C([O-])=O)CC([O-])=O IRBQOWGQMRVZMV-UHFFFAOYSA-K 0.000 claims description 3
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000001130 gallstones Diseases 0.000 abstract description 13
- 230000000694 effects Effects 0.000 abstract description 8
- 238000002474 experimental method Methods 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 5
- 201000010099 disease Diseases 0.000 abstract description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 3
- 241001465754 Metazoa Species 0.000 abstract description 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 28
- 235000012000 cholesterol Nutrition 0.000 description 14
- 210000000232 gallbladder Anatomy 0.000 description 8
- 238000002360 preparation method Methods 0.000 description 8
- 239000003925 fat Substances 0.000 description 7
- 241000699670 Mus sp. Species 0.000 description 6
- 239000004575 stone Substances 0.000 description 6
- 108010023302 HDL Cholesterol Proteins 0.000 description 5
- 108010028554 LDL Cholesterol Proteins 0.000 description 5
- 238000008050 Total Bilirubin Reagent Methods 0.000 description 5
- 230000015572 biosynthetic process Effects 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 5
- 208000000913 Kidney Calculi Diseases 0.000 description 4
- 206010029148 Nephrolithiasis Diseases 0.000 description 4
- 239000013078 crystal Substances 0.000 description 4
- 239000012046 mixed solvent Substances 0.000 description 4
- VUFVEQXOJPZCFT-UHFFFAOYSA-L C(CC(O)(C(=O)[O-])CC(=O)[O-])(=O)OO.[Na+].[Na+] Chemical compound C(CC(O)(C(=O)[O-])CC(=O)[O-])(=O)OO.[Na+].[Na+] VUFVEQXOJPZCFT-UHFFFAOYSA-L 0.000 description 3
- 238000011740 C57BL/6 mouse Methods 0.000 description 3
- 210000000941 bile Anatomy 0.000 description 3
- 239000000306 component Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 238000000465 moulding Methods 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- PFHZIWAVXDSFTB-CVYQJGLWSA-N (+)-garcinia acid Chemical compound OC(=O)[C@H]1OC(=O)C[C@@]1(O)C(O)=O PFHZIWAVXDSFTB-CVYQJGLWSA-N 0.000 description 2
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 description 2
- 239000003613 bile acid Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 235000005911 diet Nutrition 0.000 description 2
- 230000037213 diet Effects 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- 239000011521 glass Substances 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 230000003908 liver function Effects 0.000 description 2
- 238000010172 mouse model Methods 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 210000002700 urine Anatomy 0.000 description 2
- BHQCQFFYRZLCQQ-UHFFFAOYSA-N (3alpha,5alpha,7alpha,12alpha)-3,7,12-trihydroxy-cholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 BHQCQFFYRZLCQQ-UHFFFAOYSA-N 0.000 description 1
- SHCSOTQTAIXSJZ-UHFFFAOYSA-N 1,1,2-trihydroxypropane-1,2,3-tricarboxylic acid Chemical class OC(=O)CC(O)(C(O)=O)C(O)(O)C(O)=O SHCSOTQTAIXSJZ-UHFFFAOYSA-N 0.000 description 1
- 208000004845 Cholecystolithiasis Diseases 0.000 description 1
- 239000004380 Cholic acid Substances 0.000 description 1
- 208000003322 Coinfection Diseases 0.000 description 1
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 1
- 229920002556 Polyethylene Glycol 300 Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 108010021119 Trichosanthin Proteins 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 208000038016 acute inflammation Diseases 0.000 description 1
- 230000006022 acute inflammation Effects 0.000 description 1
- 230000003044 adaptive effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- QXDMQSPYEZFLGF-UHFFFAOYSA-L calcium oxalate Chemical compound [Ca+2].[O-]C(=O)C([O-])=O QXDMQSPYEZFLGF-UHFFFAOYSA-L 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 description 1
- 235000019416 cholic acid Nutrition 0.000 description 1
- 229960002471 cholic acid Drugs 0.000 description 1
- 208000037976 chronic inflammation Diseases 0.000 description 1
- 230000006020 chronic inflammation Effects 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 230000008602 contraction Effects 0.000 description 1
- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 description 1
- 235000018823 dietary intake Nutrition 0.000 description 1
- 235000012041 food component Nutrition 0.000 description 1
- 239000005428 food component Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 235000004213 low-fat Nutrition 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- IGHGOYDCVRUTSU-UHFFFAOYSA-M sodium;2-hydroxypropane-1,2,3-tricarboxylic acid;hydroxide Chemical compound [OH-].[Na+].OC(=O)CC(O)(C(O)=O)CC(O)=O IGHGOYDCVRUTSU-UHFFFAOYSA-M 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
The invention belongs to the technical field of biological medicines, and particularly relates to a novel application of hydroxycitric acid in treating gall-stone and cholecystitis induced by the gall-stone. Animal modeling experiments prove that the hydroxycitric acid and the derivatives thereof have statistically effective treatment effects on calculus and cholecystitis induced by the calculus or related diseases, and have good application prospects.
Description
Technical Field
The invention belongs to the technical field of biological medicines, and particularly relates to a novel application of hydroxycitric acid in treating gall-stone and cholecystitis induced by the gall-stone.
Background
Cholelithiasis is one of the common and multiple diseases in clinical gastroenterology, and can stimulate the mucosa of the gallbladder after stones are formed in the gallbladder, so that not only can chronic inflammation of the gallbladder be caused, but also secondary infection can be caused after stones are embedded in the neck or duct of the gallbladder, and acute inflammation of the gallbladder is caused.
Cholelithiasis can be classified into cholesterol-based calculus, cholelithiasis-pigment-based calculus explained and mixed calculus; wherein at least 80% of the gall stones are cholesterol-based stones; the cause of gall stones is not single and is the result of the combined actions of environment, heredity and personal life style; however, the direct cause of gall stones is mostly insufficient secretion of bile, and is insufficient to dissolve cholesterol.
The formation of kidney stones and the formation process of kidney stones are caused by the fact that the concentration of stone-forming substances in urine is increased or the solubility is reduced due to certain factors, the urine is supersaturated, crystals are precipitated, and the crystals locally grow and accumulate, so that the stones are finally formed.
Hydroxycitric acid can help dissolve calcium oxalate (main component of kidney stones), and has effects of preventing and treating kidney stones; however, there is no description of the related treatment of hydroxycitric gallstones.
CN1082354C hydroxycitric acid concentrate and method of preparation disclose that hydroxycitric acid has an effect of inhibiting the synthesis of fats and cholesterol. It appears that in principle, inhibition of fat absorption and cholesterol synthesis may improve gallstones; however, according to the research of "Effect of the invention, the diet of low fat and low cholesterol for a long period of time is found to be less than that of gall stones, which are not only lost but also more serious, by virtue of the diet of" FPixley et al, brMedJ (ClinResed) 1985 "," Gallstoneformationduring weight-reductiondieting.RALiddle, RBGoldstein, JSaxton.ArchInternMed1989."," Thermofectloaddegingallstone formation of the invention-induced rapid weight loss "," RLGebhardset al, hepatology1996 ".
The study of Effectofvariousfoodingcallbladdrempty, LMarciniet al EurJCrinNutr 2013 shows that fat is the most effective food component that stimulates gallbladder contraction and promotes gallbladder emptying. That is, dietary intake of cholesterol is not an important factor in causing gallstones.
Disclosure of Invention
The invention aims to provide a novel application of hydroxycitric acid for treating gall stones and cholecystitis induced by the stones.
The invention discloses application of hydroxycitric acid and derivatives thereof in preparing medicines for treating gall-stone and/or cholecystitis.
Specifically, the hydroxycitric acid and the derivative thereof are at least one of the following components:
hydroxycitric acid, hydroxycitric lactone, and hydroxycitric acid salt.
More specifically, the hydroxycitrate includes sodium hydroxycitrate, potassium hydroxycitrate, calcium hydroxycitrate.
The medicine for the application can be a specific preparation form prepared from the hydroxycitric acid and derivatives thereof and pharmaceutically acceptable auxiliary materials by adopting a conventional preparation process, and the preparation form is not limited, and can be a preparation form prepared from the trichosanthin, including but not limited to tablets, capsules and granules.
The preparation method of the medicine for the application is not limited, and can be any preparation process which can be adopted in the pharmaceutical field.
The medicine for the application can mainly adopt an oral administration method according to the self characteristics, and the preparation formulation of the medicine can be tablets, granules, capsules, soft capsules, oral liquid, suspension and the like.
Animal modeling experiments prove that the hydroxycitric acid and the derivatives thereof have statistically effective treatment effects on cholecystitis or related diseases induced by stones, and meanwhile, the safety experiments also prove that the hydroxycitric acid and the derivatives thereof have good safety and definite application prospect.
Drawings
The invention will be further described with reference to the drawings and examples.
FIG. 1 is a structural formula of 2-hydroxycitric acid.
FIG. 2 is a structural formula of hydroxycitric lactone.
FIG. 3 is a structural formula of potassium hydroxycitrate.
FIG. 4 is a photograph of a model set of cholesterol crystallized pellets of an example.
Detailed Description
The present invention will be described in further detail with reference to the following examples, which are not intended to limit the present invention, but are merely illustrative of the present invention. The experimental methods used in the following examples are not specifically described, but the experimental methods in which specific conditions are not specified in the examples are generally carried out under conventional conditions, and the materials, reagents, etc. used in the following examples are commercially available unless otherwise specified.
In specific embodiments, steps, material selections, numerical parameters that are not described in detail are all routine selections in the art, or any prior art that is presently disclosed.
EXAMPLE influence of monohydroxy citric acid on C57BL/6 mouse gall bladder stones
1. Modeling and intervention method
SPF class C57BL/6 mice, 60 males, 7-8 weeks. After quarantine is qualified, the random classification is divided into 5 groups: normal group 12, model group 48. Model mice were fed with high fat, high calories, high cholesterol (15.0% fat, 1.0% cholesterol, 0.5% cholic acid) and normal mice were fed with normal feed. After molding for 1 month, 8 mice were randomly selected from the model group, 2 mice were randomly selected from the normal group, bile was collected in a glass test tube by dissecting and collecting gall bladder, the color was observed, a portion of the bile sample was sampled and put on a glass plate for smear, and observed under a high power microscope, a large amount of cholesterol crystal particles were found under the microscope of the model group, the crystal particles were not found in the normal group, and the molding was confirmed to be successful.
Model mice were randomly assigned to model control, experimental low, medium, and high dose groups, 10 mice/group. After 1 week of adaptive feeding, normal mice were fed normal feed, and the remaining mice were given high fat, high calorie, high cholesterol (15.0% fat, 1.0% cholesterol, 0.5% bile acid) feed for 4 weeks for modeling. The drug intervention is performed during molding, the drug administration method and the drug dosage are performed according to the pre-experimental dosage of the subject group, and the drug administration is performed for 4 weeks, 1 time a day.
Mixed solvent: 10% dmso (dimethyl sulfoxide) +40% peg300 (polyethylene glycol;
polyethylenglycol 300) +5% Tween-80 (Tween 80) +45% Saline (physiological saline)
Medicament: and (3) dissolving the hydroxycitric acid by using a mixed solvent.
The administration mode is as follows: gastric lavage, once per day:
the dosage is as follows:
model control group: 15mg/kg mixed solvent
Experimental low dose group: 2.5mg/kg hydroxycitric acid
Dose group in experiment: 5mg/kg hydroxycitric acid
Experimental high dose group: 10mg/kg hydroxycitric acid
Wherein the residual amounts of the low, medium and high dose groups are supplemented to 15mg/kg by using the mixed solvent.
2. Specimen collection
After 8 weeks, blood was collected and the concentrations of Total Bile Acid (TBA), total Cholesterol (TC), triglyceride (TG), total Bilirubin (TBiL), low-density lipoprotein cholesterol (LDL-C) and high-density lipoprotein cholesterol (HDL-C) were measured as shown in Table 1.
TABLE 1 Effect of hydroxycitric acid on liver function index in miceN＝10)
| Group of | Dosage of | TBA | TBiL | TC | TG | HDL-C | LDL-C |
| mg/Kg | μmol/L | μmol/L | μmol/L | μmol/L | μmol/L | μmol/L | |
| N | / | 18.16±5.37 | 4.79±0.52 | 2.08±0.16 | 1.00±0.08 | 0.65±0.12 | 0.43±0.11 |
| M | / | 193.28±11.97 N | 104.61±18.12 N | 5.71±0.41 N | 2.36±0.14 N | 2.03±0.21 N | 1.32±0.24 N |
| Low | 2.5 | 136.12±12.81 M | 3.81±0.31 M | 4.65±0.38 M | 2.32±0.22 M | 1.32±0.22 M | 1.01±0.22 M |
| Mid | 5 | 96.68±14.13 M | 3.25±0.26 M | 3.75±0.32 M | 1.78±0.24 M | 1.15±0.19 M | 0.82±0.20 M |
| Hig | 10 | 73.12±19.21 M | 2.21±0.21 M | 2.98±0.29 M | 1.33±0.18 M | 0.97±0.16 M | 0.68±18 M |
In table 1, N groups are normal groups, M groups are model control groups, low groups are experimental Low dose groups, mid groups are experimental medium dose groups, hig are experimental high dose groups.
In the table 1, the contents of the components, N represents P < 0.05 compared to N groups; M represents P < 0.05 compared to group M;
as shown in Table 1, the experimental groups showed a statistically different decrease in TBA, TG, TC, TBiL, LDL-C, HDL-C compared to the model control group, demonstrating the therapeutic effect of hydroxycitric acid.
Example Effect of dihydroxycitric acid derivatives on C57BL/6 mouse gall bladder stones
In order to investigate the quality effect of hydroxycitric acid derivatives on cholecystolithiasis, the potential medical value of various hydroxycitric acid derivatives was tested in the same manner as in example one, specifically:
hydroxycitric acid lactone [ CAS546-43-0]
Hydroxy sodium citrate [ CAS6132-04-3]
Potassium hydroxycitrate [ CAS866-84-2]
Calcium hydroxycitrate [ CAS814-80-2]
The grouping is as follows:
A-Low 2.5mg/kg hydroxycitric lactone
A-Mid 5mg/kg hydroxycitric lactone
A-Hig 10mg/kg hydroxycitric lactone
B-Low 2.5mg/kg sodium hydroxy citrate
B-Mid 5mg/kg sodium hydroxy citrate
B-Hig 10mg/kg sodium hydroxy citrate
C-Low 2.5mg/kg Potassium hydroxycitrate
C-Mid 5mg/kg potassium hydroxycitrate
C-Hig 10mg/kg Potassium hydroxycitrate
D-Low 2.5mg/kg calcium hydroxycitrate
D-Mid 5mg/kg calcium hydroxycitrate
D-Hig 10mg/kg calcium hydroxycitrate
The remainder was the same as in example one, and the results are shown in Table 2.
TABLE 2 influence of hydroxycitric acid derivatives on liver function index in miceN＝10)
| Group of | Dosage of | TBA | TBiL | TC | TG | HDL-C | LDL-C |
| mg/Kg | μmol/L | μmol/L | μmol/L | μmol/L | μmol/L | μmol/L | |
| N | / | 18.16±5.37 | 4.79±0.52 | 2.08±0.16 | 1.00±0.08 | 0.65±0.12 | 0.43±0.11 |
| M | / | 193.28±11.97 N | 104.61±18.12 N | 5.71±0.41 N | 2.36±0.14 N | 2.03±0.21 N | 1.32±0.24 N |
| A-Low | 2.5 | 115.70±10.89 M | 3.24±0.26 M | 3.99±0.30 M | 1.99±0.22 | 1.14±0.21 | 0.87±0.21 |
| A-Mid | 5 | 82.18±11.91 M | 2.76±0.22 M | 3.19±0.26 M | 1.59±0.23 | 0.91±0.19 | 0.69±0.22 |
| A-Hig | 10 | 62.15±16.33 M | 1.88±0.18 M | 2.58±0.24 M | 1.28±0.19 | 0.74±0.17 | 0.56±0.20 |
| B-Low | 2.5 | 140.44±14.67 M | 4.03±0.33 M | 4.91±0.37 M | 2.45±0.24 | 1.40±0.19 | 1.07±0.18 |
| B-Mid | 5 | 99.41±14.98 M | 3.35±0.27 M | 3.89±0.32 M | 1.94±0.19 | 1.11±0.20 | 0.84±0.21 |
| B-Hig | 10 | 76.11±20.26 M | 2.29±0.22 M | 3.12±0.30 M | 1.55±0.22 | 0.89±0.17 | 0.68±0.18 |
| C-Low | 2.5 | 149.73±15.94 M | 4.22±0.34 M | 5.27±0.40 M | 2.62±0.22 | 1.50±0.20 | 1.14±0.22 |
| C-Mid | 5 | 106.35±15.96 M | 3.58±0.29 M | 4.24±0.35 M | 2.11±0.19 | 1.21±0.22 | 0.92±0.21 |
| C-Hig | 10 | 81.01±21.36 M | 2.45±0.23 M | 3.38±0.32 M | 1.68±0.19 | 0.96±0.19 | 0.73±0.18 |
| D-Low | 2.5 | 126.05±11.77 M | 3.56±0.29 M | 4.38±0.33 M | 2.18±0.21 | 1.25±0.19 | 0.95±0.20 |
| D-Mid | 5 | 89.36±13.03 M | 3.00±0.24 M | 3.47±0.29 M | 1.73±0.18 | 0.99±0.20 | 0.75±0.17 |
| D-Hig | 10 | 67.39±17.69 M | 2.06±0.20 M | 2.73±0.26 M | 1.36±0.15 | 0.78±0.16 | 0.59±0.16 |
In the table 2 of the description of the present invention, N represents P < 0.05 compared to N groups; M represents P < 0.05 compared to group M;
from table 2, it can be seen that the therapeutic effect ratio: hydroxycitric acid lactone > calcium hydroxycitrate > sodium hydroxycitrate > potassium hydroxycitrate. But any group has a statistically significant therapeutic effect.
The foregoing detailed description is directed to one of the possible embodiments of the present invention, which is not intended to limit the scope of the invention, but is to be accorded the full scope of all such equivalents and modifications so as not to depart from the scope of the invention.
Claims (4)
1. Application of hydroxycitric acid and its derivatives in preparing medicine for treating cholelithiasis and/or cholecystitis is provided.
2. The use according to claim 1, wherein the hydroxycitric acid and derivatives thereof are at least one of the following components:
hydroxycitric acid, hydroxycitric lactone, and hydroxycitric acid salt.
3. The use according to claim 2, wherein the hydroxycitrate comprises sodium hydroxycitrate, potassium hydroxycitrate, calcium hydroxycitrate.
4. The use according to claim 1, further comprising a pharmaceutically acceptable adjuvant.
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20010099460A (en) * | 2001-09-29 | 2001-11-09 | 서석춘 | Cholesterol stones in bile ducts using herbal ingredients |
| CN103284145A (en) * | 2013-04-28 | 2013-09-11 | 臧鸿飞 | Combination beverage for discharging internal light hepatic calculus |
| US20150297545A1 (en) * | 2014-02-06 | 2015-10-22 | University Of Houston System | Organic acids as agents to dissolve calcium minerals in pathological calcification and uses thereof |
| CN105055579A (en) * | 2015-09-11 | 2015-11-18 | 吉林大学 | Compound traditional Chinese medicine composition for treating urolithiasis and preparation method thereof |
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- 2023-05-26 CN CN202310607581.4A patent/CN116549427B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20010099460A (en) * | 2001-09-29 | 2001-11-09 | 서석춘 | Cholesterol stones in bile ducts using herbal ingredients |
| CN103284145A (en) * | 2013-04-28 | 2013-09-11 | 臧鸿飞 | Combination beverage for discharging internal light hepatic calculus |
| US20150297545A1 (en) * | 2014-02-06 | 2015-10-22 | University Of Houston System | Organic acids as agents to dissolve calcium minerals in pathological calcification and uses thereof |
| CN105055579A (en) * | 2015-09-11 | 2015-11-18 | 吉林大学 | Compound traditional Chinese medicine composition for treating urolithiasis and preparation method thereof |
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| Title |
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| 郑建仙: "《常见病联合用药手册》", 中国医药科技出版社, pages: 242 - 243 * |
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