Panaxadiol compound as well as preparation method and medical application thereof
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A technology of panaxadiol and pharmaceutical preparations, applied in the field of biomedicine, can solve problems such as incomplete cure, achieve good neuroprotective effect, mild reaction conditions, and simple operation
Active Publication Date: 2022-08-05
YANBIAN UNIV
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[0003] Although there are clinically available anti-Alzheimer's drugs, their effects are only able to alleviate the symptoms of early patients and improve memory ability, but cannot completely cure or prevent the serious disease
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Embodiment 1
[0023] 1) 6 mmol p-nitrophenyl chloroformate in dichloromethane solution (6 mmol / 10 mL) was slowly added to 1 mmol panaxadiol in dichloromethane solution (1 mmol / 1 mL) under ice bath , then 2 mmol of N,N-lutidine (DMAP) and 3 mmol of triethylamine were added, and the reaction was carried out overnight at room temperature;
[0024] 2) After the completion of the reaction, purify by silica gel chromatography to obtain Intermediate A with a yield of 93%;
[0025] 3) Take 1 mmol of Intermediate A and 5 mmol of methylpiperazine into 3 mL of ethanol, and react at room temperature for 8 h;
[0026] 4) After the reaction is completed, ethyl acetate is added for extraction, washed with saturated brine, suction filtered, dried, and subjected to column chromatography to obtain compound Q4.
[0027] The resulting compounds are named:
[0028] (3 S ,5 R ,8 R ,9 R ,10 R ,12 R ,13 R ,14 R ,17 S )-12-hydroxy-4,4,8,10,14-pentamethyl-17-(( R )-2,6,6-trimethyltetrahydro-2 H -pyran-2...
Embodiment 2
[0035] Pharmaceutical composition: 1000 tablets each containing 100 mg of active ingredient Formulation: 100 g of the present compound Q4, 2 g of hydroxypropyl methylcellulose, 10 g of wheat starch, 100 g of sucrose, 6 g of magnesium stearate ; The dose to be used should be adapted to the nature and severity of the disease, the route of administration and the age and weight of the patient. The daily dose varies from 0.1 mg to 1.0 g and can be administered in one or several doses.
[0036] The medical use of the compounds of the present invention is further demonstrated by the following tests:
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Abstract
The invention discloses a panoxadiol compound as well as a preparation method and medical application thereof, and relates to a novel compound with anti-Alzheimer's disease activity, the panoxadiol compound is structurally modified and optimized on the basis of a natural product panoxadiol, the physicochemical property of the panoxadiol compound is improved, the pharmacological activity of the panoxadiol compound is improved, and the druggability of the panoxadiol compound is enhanced. The preparation method of the panoxadiol compound provided by the invention has the advantages that the reaction condition is mild, the reaction process is simple to operate, and the used reagent is cheap and easy to obtain. The prepared novel panoxadiol derivative has the effect similar to that of panoxadiol, MTT experimental research shows that the protection effect of the compound Q4 on A beta 25-35 induced nerves is stronger than that of panoxadiol and positive control donepezil, and the compound Q4 does not show cytotoxicity to PC12 when the concentration is 7.5-120 mu M, and can be applied to preparation of Alzheimer's disease drugs.
Description
technical field [0001] The invention discloses a panaxadiol compound, which is a new compound; the invention also provides a preparation method and medical application of the compound, belonging to the technical field of biomedicine. Background technique [0002] Alzheimer's disease was first discovered and reported by German physician Eros Alzheimer in 1906. AD is the most common neurodegenerative disease, accounting for approximately 70% of cases and one of the leading causes of human death. According to the latest official statistics released by WHO in 2020, there are currently more than 55 million people diagnosed with dementia in the world, and the overall number of patients is increasing at a rate of nearly 10 million cases per year, with an average of one person suffering from dementia every three seconds. It is estimated that by 2050, the number of people living with dementia in the world will reach 139 million. [0003] Although there are anti-Alzheimer's disease ...
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