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 Medjournal_title
Journal of natural medicinesauthors
Maarisit W,Yamazaki H,Kanno SI,Tomizawa A,Lee JS,Namikoshi Mdoi
10.1007/s11418-016-1061-6subject
Has Abstractpub_date
2017-01-01 00:00:00pages
334-337issue
1eissn
1340-3443issn
1861-0293pii
10.1007/s11418-016-1061-6journal_volume
71pub_type
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