Aromatase inhibitor high-throughput screening model based on fluorescence detection principle

An aromatase, high-throughput technology, applied in the field of pharmacology, can solve the problems of time-consuming and laborious, high experimental conditions, and difficulty in high-throughput screening.
CN103149186AInactive Publication Date: 2013-06-12CHINA PHARM UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CHINA PHARM UNIV
Publication Date
2013-06-12
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to aromatase inhibitory activity high-throughput screening realized by means of a homogeneous time-resolved fluorescence technique. By detecting the fluorescence intensity ratio (665nm / 610nm) of an excitation light irradiated reaction system and performing formula conversion, the inhibitory activity of a to-be-detected sample on aromatase can be determined. By means of high-throughput screening new model, the harm of a radioligand binding principle-based experimental method to laboratory personnel and environment can be avoided. And the high-throughput screening model provided in the invention has the advantages of high efficiency, rapidity, accuracy, and inexpensiveness.
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Description

technical field

[0001] The invention belongs to the field of pharmacology. A high-throughput screening model of aromatase inhibitors in vitro is constructed by using a homogeneous time-resolved fluorescence detection technology, which is used for high-throughput detection of aromatase inhibitory activity of test samples. Background technique

[0002] Steroid A-ring aromatase mainly exists in ovary and placenta, but also in other tissues, such as brain, adrenal gland, testis, bone marrow, fat, skin, muscle and some tumor tissues. Aromatase takes androgen as a substrate, and with the participation of oxygen and NADPH, undergoes two hydroxylations at the 19-position of the substrate, and finally aromatizes the A ring to generate estrogen products. Inhibition or inactivation of aromatase activity can lead to a decrease in estrogen levels in the body, thereby interfering with estrogen-related physiological processes such as ovulation, implantation, etc., and can also cause estrog...

Claims

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