The 3<sup>rd</sup> International Conference on Drug Discovery & Therapy: Dubai, February 7 - 11, 2011

Process Chemistry and Drug Manufacturing (Track)

PTP1B Active constituents from Helichrysum arenarium (L.) Moench

Haji Akber Aisa
Xinjiang Key Laboratory of Plant Resources and Natural Products Chemistry, Xinjiang Technological Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China

Abstract:

Helichrysum arenarium (L.) Moech (Compositae), a commonly used Uyghur medicine, is mainly distributed in Xinjinag, central Asia, and Europe. It has the functions of diuretic, choleretic, hepatoprotective, anti-viral, and antioxidant properties, and is habitually used for the treatment of cholecystitis, gallstone and diabetes mellitus. In order to clarify the antidiabetic bioactive components of this medicinal plant, studies on the chemical constituents of this plant were conducted. Seven compounds were isolated from 70% EtOH extract of H. arenarium, and their structures were identified by comprehensive spectroscopic analysis as 6-(4-methoxystyryl)-4-hydroxy-2H-pyran-2-one (1), kaempferol (2), astragalin (3), naringenin (4), apigenin (5), 7-geranyloxycoumarin (6), and sucrose (7), among which, compounds 1, 3, 6 were firstly isolated from this plant. All compounds were assayed on protein tyrosine hosphatase 1B (PTP1B) activities, and compound 1 showed high inhibitory effect on PTP1B with an IC50 value of 13.06 μg/mL, which supplied scientific basis for the further exploration in the treatment of diabetes mellitus.

Key word: Helichrysum arenarium, Chemical constituents, Bioactivity, PTP1B