# Constituents of Indonesian medicinal plant averrhoa bilimbi and Their Cytochrome P450 3A4 and 2D6 Inhibitory Activities
> Auw L.

URL kanonis: https://discover.unhas.ac.id/publications/constituents-of-indonesian-medicinal-plant-averrhoa-bilimbi-and-their-cytochrome
Jurnal / Konferensi: Natural Product Communications
Tahun terbit: 2015
DOI: https://doi.org/10.1177/1934578x1501000116
ISSN: 1934578X
Kuartil SJR: Q3
Citations: 5

## Authors
- Auw L.

## Abstract
As constituents of Averrhoa bilimbi leaves we identified three new compounds (1-3) together with 12 known ones (4-15); their inhibitory activities on cytochrome P450 3A4 (CYP3A4) and 2D6 (CYP2D6) were examined. Among the isolated compounds, the mixture of 1 and 2, and compounds 4 and 9 showed strong inhibition on CYP3A4, but mild or no inhibition on CYP2D6. These compounds revealed the characteristics of 1) time- and concentration-dependent inhibition, 2) requirement of NADPH for the inhibition, 3) no protection by nucleophiles, and 4) suppression of the inhibition by competitive inhibitor. Thus, they are suggested to be mechanism-based inactivators of CYP3A4 and CYP2D6. The kinetic parameters for the inactivation (k(inact) and K(I)) were 0.19 min(-1) and 36.7 μM for the mixture of 1 and 2, 0.126 min(-1) and 10.5 μM for 4, and 0.29 min(-1) and 23.4 μM for 9.

## Keywords
- CYP3A4
- Chemistry
- Stereochemistry
- Inhibitory postsynaptic potential
- Cytochrome P450
- CYP2D6
- Enzyme
- Biochemistry
- Biology
- Neuroscience

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Sumber: Discover Unhas — RIMS Universitas Hasanuddin.
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