Protein tyrosine phosphatase 1B inhibitory properties of seco-cucurbitane triterpenes obtained from fruiting bodies of Russula lepida.

Abstract:

:The known seco-cucurbitane triterpene, (24E)-3,4-seco-cucurbita-4,24-diene-3,26,29-trioic acid (1), has been isolated as a potent protein tyrosine phosphatase (PTP) 1B inhibitor together with a new analogue, (24E)-3,4-seco-cucurbita-4,24-diene-3-hydroxy-26,29-dioic acid (2), from the fruiting bodies of Russula lepida. Further evaluation of their biological properties against PTPs revealed that compound 1 inhibited T-cell PTP activity similarly to PTP1B and exhibited moderate selectivity against PTP1B over vaccinia H-1-related phosphatase. Moreover, the in vitro growth inhibitory effects of 1 and 2 against three human cancer cell lines were examined in order to evaluate cell-based efficacy. However, neither 1 nor 2 enhanced insulin-stimulated p-Akt levels at non-cytotoxic concentrations.

journal_name

J Nat Med

authors

Maarisit W,Yamazaki H,Kanno SI,Tomizawa A,Lee JS,Namikoshi M

doi

10.1007/s11418-016-1061-6

subject

Has Abstract

pub_date

2017-01-01 00:00:00

pages

334-337

issue

1

eissn

1340-3443

issn

1861-0293

pii

10.1007/s11418-016-1061-6

journal_volume

71

pub_type

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