Abstract

Passion fruit seed extract (PFSE), a product rich in stilbenes such as piceatannol and scirpusin B, has various physiological effects. It is unclear whether PFSE and its stilbene derivatives inhibit cancer cell proliferation via human glyoxalase I (GLO I), the rate-limiting enzyme for detoxification of methylglyoxal. We examined the anticancer effects of PFSE in two types of human cancer cell lines with different GLO I expression levels, NCI–H522 cells (highly-expressed GLO I) and HCT116 cells (lowly-expressed GLO I). PFSE and its stilbenes inhibited GLO I activity. In addition, PFSE and its stilbenes supressed the cancer cell proliferation of NCI–H522 cells more than HCT116 cells. These observations suggest that PFSE can provide a novel anticancer strategy for prevention and treatment.

Highlights

  • Cancer is one of the primary causes of death worldwide; its incidence is increasing

  • The IC50 values of piceatannol and scirpusin B were calculated to be 0.75 μM, and 4.2 μM, respectively; and the IC50 of the piceatannol equivalent of Passion fruit seed extract (PFSE) was 0.38 μM. These findings suggest that piceatannol and scirpusin B are the primary contributors to PFSE's inhibitory effect on glyoxalase I (GLO I)

  • To investigate whether PFSE and stilbenes are effective at suppressing the growth of cells that have different GLO I expression levels, we evaluated the antiproliferative effects of PFSE, piceatannol, and scirpusin B on NCI–H522 cells and HCT116 cells

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Summary

Introduction

Cancer is one of the primary causes of death worldwide; its incidence is increasing. whereas colorectal cancer is the major cause of cancer death in developed countries, lung cancer is the leading cause of cancer death among males in all countries [1]. Sustained mild suppression of tumors by food constituents such as flavonoids is desired [3,4]. Methylglyoxal (MG) is a byproduct of tumor-specific aerobic glycolysis [5]. It is highly reactive with proteins and DNA/RNA, and is believed to induce apoptosis in tumor cells [6]. Many human tumors, including those of the colon and lungs, reportedly have increased GLO I activity [7,8]. The GLO I enzyme is believed to be a potential therapeutic target for inducing cancer cell apoptosis. It has been reported that phenylpropanoids such as natural polyphenols represented by flavonoids have GLO I inhibitory activity [9]. The GLO I inhibitory activity of compounds having a stilbene structure is hardly known

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