title: 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.
authors.affiliation: Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.|Faculty of Fisheries and Marine Science, Sam Ratulangi University, Kampus Bahu, Manado, 95115, Indonesia.
authors.forename: Wilmar
authors.initials: W
authors.lastname: Maarisit
authors.affiliation: Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan. yamazaki@tohoku-mpu.ac.jp.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Yamazaki
authors.affiliation: Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.
authors.forename: Syu-Ichi
authors.initials: SI
authors.lastname: Kanno
authors.affiliation: Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.
authors.forename: Ayako
authors.initials: A
authors.lastname: Tomizawa
authors.affiliation: Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.|College of Marine Sciences, Gyeongsang National University, Tongyeong, Gyeongnam, 650-160, Korea.
authors.forename: Jong-Soo
authors.initials: JS
authors.lastname: Lee
authors.affiliation: Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.
authors.forename: Michio
authors.initials: M
authors.lastname: Namikoshi
mesh_terms: D048690:Fruiting Bodies, Fungal / Q000737:chemistry*; D006027:Glycosides / Q000737:chemistry*; D006801:Humans; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D014315:Triterpenes / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D006027:Glycosides; D014315:Triterpenes; C514277:cucurbitane; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
keywords: (24E)-3,4-Seco-cucurbita-4,24-diene-3,26,29-trioic acid; Inhibitor; Protein tyrosine phosphatase 1B; Russula lepida; Seco-cucurbitane triterpene