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Procyanidin Oligomers from Japanese Quince (Chaenomeles japonica) Fruit Inhibit Activity of MMP-2 and MMP-9 Metalloproteinases

机译:日本木瓜果实中的花青素低聚物抑制MMP-2和MMP-9金属蛋白酶的活性

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摘要

The influence of procyanidin extract from Japanese quince fruit on the activities of matrix metalloproteinases MMP-2 and MMP-9 secreted to culture medium by human peripheral blood mononuclear cells (PBMC) and by human leukemia HL-60 cells was investigated by gelatin zymography. The extract proved to be an effective inhibitor of the enzymes activities (for MMP-2 and MMP-9 secreted by PBMC IC50 = 16-19 mug extract/mL and 22-25 mug extract/mL, respectively). To identify the most effective components of the extract it was fractionated by means of column chromatography on TSKgel Toyopearl HW-40 (S) bed. The obtained fractions were analyzed by TLC, HPLC, and MALDI-TOF MS. Their antioxidant activity was measured as cation radicals ABTS*+ scavenging efficiency. The fractions VIII-XIV containing oligomers from trimer to hexamer (and probably higher oligomers) appeared to be the most effective inhibitors of MMP-2 and MMP-9 activity (IC50 value close to 4.6 mug total polyphenols/mL). To the best of our knowledge, it is the first report on gelatinase-inhibitory activity of Japanese quince fruit polyphenol extract. We conclude that polyphenols from Japanese quince can be used in cancer chemoprevention, although further studies are needed to elucidate the mechanisms underlying their biological activities. Keywords: Polyphenols; procyanidin oligomers; Japanese quince (Chaenomeles japonica); MMP-2; MMP-9; HL-60.
机译:用明胶酶谱法研究了木瓜果中原花青素提取物对人外周血单个核细胞(PBMC)和白血病HL-60细胞分泌的基质金属蛋白酶MMP-2和MMP-9活性的影响。提取物被证明是有效的酶活性抑制剂(PBMC IC50分泌的MMP-2和MMP-9分别为16-19杯提取物/ mL和22-25杯提取物/ mL)。为了鉴定提取物中最有效的成分,在TSKgel Toyopearl HW-40(S)床上通过柱色谱法对其进行分级分离。通过TLC,HPLC和MALDI-TOF MS分析获得的级分。测定它们的抗氧化活性,作为阳离子自由基ABTS * +清除效率。从三聚体到六聚体的低聚体VIII-XIV馏分(可能还有更高的低聚体)似乎是最有效的MMP-2和MMP-9活性抑制剂(IC50值接近4.6杯总多酚/ mL)。据我们所知,这是日本木瓜果多酚提取物对明胶酶抑制活性的首次报道。我们得出结论,虽然需要进一步研究阐明其生物活性的基础,但日本木瓜的多酚可用于癌症的化学预防。关键字:多酚;原花青素低聚物;日本木瓜(木瓜); MMP-2; MMP-9; HL-60。

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