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提取物对 mPRα 的拮抗活性。

The antagonistic activity of extracts on mPRα.

机构信息

Integrated Bioscience Section, Graduate School of Science and Technology, National University Corporation, Shizuoka University, Shizuoka, Japan.

Biological Science Course, Graduate School of Science, Shizuoka University, Shizuoka, Japan.

出版信息

Nat Prod Res. 2023 Jun;37(11):1872-1876. doi: 10.1080/14786419.2022.2120873. Epub 2022 Sep 6.

DOI:10.1080/14786419.2022.2120873
PMID:36067477
Abstract

The current study attempted to evaluate the antagonistic activity of compounds isolated and purified from the marine algae during cultivation. The compounds were collected on a filter, concentrated on ODS columns and separated by HPLC. Two peaks that showed competitive progesterone binding activity with membrane progesterone receptor α (mPRα) were purified. Their physiological activity was further uncovered by and oocyte maturation and ovulation-inducing assays using zebrafish. The compounds inhibited the induction of oocyte maturation and ovulation. Moreover, the results showed that the compounds have antagonistic activity against mPRα. The purified compounds with antagonistic activity against mPRα would be considered as new pharmaceutical candidate.

摘要

本研究旨在评估在培养过程中从海洋藻类中分离和纯化的化合物的拮抗活性。将化合物收集在过滤器上,用 ODS 柱浓缩,然后通过 HPLC 分离。纯化了两个显示与膜孕激素受体α(mPRα)竞争孕激素结合活性的峰。通过使用斑马鱼的 和 卵母细胞成熟和排卵诱导测定进一步揭示了它们的生理活性。这些化合物抑制了卵母细胞成熟和排卵的诱导。此外,结果表明这些化合物对 mPRα 具有拮抗活性。具有拮抗 mPRα 活性的纯化化合物将被视为新的药物候选物。

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