AI Article Synopsis
- Four new steroidal alkaloids were identified from the plant Pachysandra procumbens using a method that tested their ability to inhibit a specific binding site related to estrogens.
- Compounds 1-7 and 9 showed strong activity in inhibiting this estrogen binding site, with compounds 3, 5, and 9 enhancing tamoxifen's antiestrogen effects in lab cells.
- The structure of the new compounds was determined using various spectral analysis techniques.
Article Abstract
Four novel steroidal alkaloids, (+)-(20S)-20-(dimethylamino)-3-(3'alpha-isopropyl)-lactam-5alpha-+ ++preg n-2-en-4-one (1), (+)-(20S)-20-(dimethylamino)-16alpha-hydroxy-3-(3'alpha-isopropyl) -la ctam-5alpha-pregn-2-en-4-one (2), (+)-(20S)-3-(benzoylamino)-20-(dimethylamino)-5alpha-pregn-2-en-++ +4beta -yl acetate (3), and (+)-(20S)-2alpha-hydroxy-20-(dimethylamino)-3beta-phthalimido-5 alpha- pregnan-4beta-yl acetate (4), as well as five known compounds, (-)-pachyaximine A (5), (+)-spiropachysine (6), (+)-axillaridine A (7), (+)-epipachysamine D (8), and (+)-pachysamine B (9), were isolated from Pachysandra procumbens, using a bioassay-guided fractionation based on inhibition of 3H-tamoxifen binding at the antiestrogen binding site (AEBS). Compounds 1-7 and 9 demonstrated significant activity as AEBS-inhibitory agents, and compounds 3, 5 and 9 were found to potentiate significantly the antiestrogenic effect mediated by tamoxifen in cultured Ishikawa cells. The structure elucidation of compounds 1-4 was carried out by spectral data interpretation.
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Article Synopsis
- Four new steroidal alkaloids were identified from the plant Pachysandra procumbens using a method that tested their ability to inhibit a specific binding site related to estrogens.
- Compounds 1-7 and 9 showed strong activity in inhibiting this estrogen binding site, with compounds 3, 5, and 9 enhancing tamoxifen's antiestrogen effects in lab cells.
- The structure of the new compounds was determined using various spectral analysis techniques.
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