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

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

  • J Nat Med. 2017 Jan;71(1):334-337. doi: 10.1007/s11418-016-1061-6.
Wilmar Maarisit 1 2,  Hiroyuki Yamazaki 3,  Syu-Ichi Kanno 1,  Ayako Tomizawa 1,  Jong-Soo Lee 1 4,  Michio Namikoshi 1
Affiliations

Affiliations

  • 1 Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan.
  • 2 Faculty of Fisheries and Marine Science, Sam Ratulangi University, Kampus Bahu, Manado, 95115, Indonesia.
  • 3 Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, Sendai, 981-8558, Japan. yamazaki@tohoku-mpu.ac.jp.
  • 4 College of Marine Sciences, Gyeongsang National University, Tongyeong, Gyeongnam, 650-160, Korea.
PMID: 27866320 DOI: 10.1007/s11418-016-1061-6
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.

Keywords

(24E)-3,4-Seco-cucurbita-4,24-diene-3,26,29-trioic acid; Inhibitor; Protein tyrosine phosphatase 1B; Russula lepida; Seco-cucurbitane triterpene.

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