Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates

ZHOU Yu; HU Li-na; LUO Jian-fei; YU Shi-chong; WU Qiu-ye

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Objective To synthetize and conduct PTP1B inhibitory activity experiment of series of novel mangiferin derivates. Methods Different benzyl groups were introduced to mangiferin framework by nucleophilic substitution reaction. All the compounds were screened against protein tyrosine phosphatase 1B(PTP1B)with the colorimetrie assay. Results Eight compounds were synthesized and all the compounds exhibited PTP1B inhibitory activity to some extent. Conclusions Derivates of mangiferin remarkably enhanced the activity compared with mangiferin itself. In addition, the benzylated derivates with chloro atom had better inhibitory activity than other substitution groups. Furthermore,the para position of the benzyl was a better place for introducing substituent than meta and ortho position.

Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates

1. NO. 82 Hospital of PLA, Huaian 223001,China

2. Department of Organic Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China

Received Date: 2011-01-06

Rev Recd Date: 2011-03-10

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Abstract: Objective To synthetize and conduct PTP1B inhibitory activity experiment of series of novel mangiferin derivates. Methods Different benzyl groups were introduced to mangiferin framework by nucleophilic substitution reaction. All the compounds were screened against protein tyrosine phosphatase 1B(PTP1B)with the colorimetrie assay. Results Eight compounds were synthesized and all the compounds exhibited PTP1B inhibitory activity to some extent. Conclusions Derivates of mangiferin remarkably enhanced the activity compared with mangiferin itself. In addition, the benzylated derivates with chloro atom had better inhibitory activity than other substitution groups. Furthermore,the para position of the benzyl was a better place for introducing substituent than meta and ortho position.

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Synthesis and PTP1B activity of enzyme inhibition of mangiferin derivates

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