葛根素衍生物及其醫學用途
The invention relates to a novel application of puerarin and derivates thereof in the pharmaceutical field. The puerarin and the derivates thereof have a COX-2-selective inhibition effect, are safe in use without toxic side effect, and have notable effectiveness. The puerarin and the derivates thereof can be used to prevent and cure osteoarthritis, rheumatic arthritis, rheumatoid arthritis, urarthritis, hepatitis, conjunctivis, myocarditis, secondary inflammations caused by tumor and diabetes, itai itai diseases caused by cold or trauma, and other difficult and baffling diseases.
Inventor: Albert Sun-chi Chan | Shi Lin Chen | Yueming Li | Dajian Yang
Priority Number: CN100572374C
IPC Current: C07D031134 | A61K0031352 | A61K00317048 | A61P000306 | C07H001707
Assignee Applicant: Hong Kong Jockey Club Inst Chinese Medic
Title: Puerarin derivatives and their medical uses | Puerarin derivative and its medical use
Usefulness: Puerarin derivatives and their medical uses | Puerarin derivative and its medical use
Summary: (I) are useful to treat myocardial ischemia and for modulating blood lipid levels, dilating coronary and cerebral arteries, reducing oxygen consumption of cardiomyocytes, improving microcirculation and preventing aggregation of blood platelets. The method is useful for enhancing the bioavailability of (I) (all claimed). The ability of (I) to treat myocardial ischemia was tested in rats by inducing acute myocardial ischemia by injection of posterior pituitary extract and treatment with varying concentrations of (I) with propranolol as a positive control. T-wave amplitude variation was measured post-injection by ECG and compared with untreated controls. For animals treated with 1.28 g/kg hexa-acetylpuerarin 15 seconds post injection, T-wave amplitude was 29.09 ± 16.50 μV, compared with 105.23 ± 33.09 μV for the untreated control and 18.51 ± 9.26 μV for the positive control.
Novelty: New puerarin derivatives, useful e.g. to treat myocardial ischemia, modulate blood lipid levels, dilating coronary and cerebral arteries and reduce oxygen consumption of cardiomyocytes
化工/材料
化工/材料應用
楊大堅
李月明
陳士林
陳新滋
中國內地
