Inhibitory Effect of Extracts from Three Uyghur Medicine on the Protein Tyrosine Phosphatase 1B Activity

Abstract

Abstract:

Protein tyrosine phosphatase-1B is one of new drug targets against insulin sensitizer. In this study, we investigated the inhibitory effect of petroleumether extracts from 3 Uygur herbs, including Ziziphora Clinopodioides Lam., Helichrysum arenarium (Linn.) Moench, and Ver-nohia anthelmintica (L.) willd, on the PTP1B activity and the mode of inhibition. The results showed that recombinant PTP1B was highly expressed by the prokaryotic expression system and its molecular weigh was 40.8 kDa. Three extracts showed different inhibitory effects on the PTP1B activity, with IC₅₀ values of 20.2 μg/mL, 12.65 μg/mL, and 9.7 μg/mL, respectively. The enzyme kinetic studies revealed non-competitive type of inhibition, competitive type of inhibition, and mixed competitive type of inhibition with the inhibitory constants (K_i) of 0.275 μg/mL, 1.245 μg/mL, and 0.192 μg/mL, respectively. The study will provide support for further exploration and utilization of Uygur herbs.

Key words: Uygur herbs, PTP1B, inhibition, prokaryotic expression system

LIU He-Pei, DOU Jun, MA Ji, XIN Xue-Lei, ZHAO Hai-Qing, AISA Haji Akber. Inhibitory Effect of Extracts from Three Uyghur Medicine on the Protein Tyrosine Phosphatase 1B Activity[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2011, 23(1): 142-145.

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