The United Graduate School of Agricultural Sciences, Kagoshima University, 1-21-24 Korimoto, Kagoshima 890-0065, Japan.
Graduate School of Agriculture, Forestry and Fisheries, Kagoshima University, Kagoshima 890-0065, Japan.
Molecules. 2024 May 3;29(9):2119. doi: 10.3390/molecules29092119.
Many liqueurs, including spirits infused with botanicals, are crafted not only for their taste and flavor but also for potential medicinal benefits. However, the scientific evidence supporting their medicinal effects remains limited. This study aims to verify in vitro anticancer activity and bioactive compounds in shochu spirits infused with Cordyceps militaris, a Chinese medicine. The results revealed that a bioactive fraction was eluted from the spirit extract with 40% ethanol. The infusion time impacted the inhibitory effect of the spirit extract on the proliferation of colon cancer-derived cell line HCT-116 cells, and a 21-day infusion showed the strongest inhibitory effect. Furthermore, the spirit extract was separated into four fractions, A-D, by high-performance liquid chromatography (HPLC), and Fractions B, C, and D, but not A, exerted the effects of proliferation inhibition and apoptotic induction of HCT-116 cells and HL-60 cells. Furthermore, Fractions B, C, and D were, respectively, identified as adenosine, cordycepin, and N-(2-hydroxyethyl)-adenosine (HEA) by comprehensive chemical analyses, including proton nuclear magnetic resonance (H-NMR), Fourier transform infrared spectroscopy (FT-IR), and electrospray ionization mass spectrometry (ESI-MS). To better understand the bioactivity mechanisms of cordycepin and HEA, the agonist and antagonist tests of the A3 adenosine receptor (A3AR) were performed. Cell viability was suppressed by cordycepin, and HEA was restored by the A3AR antagonist MR1523, suggesting that cordycepin and HEA possibly acted as agonists to activate A3ARs to inhibit cell proliferation. Molecular docking simulations revealed that both adenosine and cordycepin bound to the same pocket site of A3ARs, while HEA exhibited a different binding pattern, supporting a possible explanation for the difference in their bioactivity. Taken together, the present study demonstrated that cordycepin and HEA were major bioactive ingredients in Cordyceps militaries-infused sweet potato shochu spirits, which contributed to the in vitro anticancer activity.
许多利口酒，包括用植物制成的烈酒，不仅因其口感和风味而酿造，还可能具有潜在的药用功效。然而，支持其药用功效的科学证据仍然有限。本研究旨在验证一种以蛹虫草为药材的烧酒的体外抗癌活性和生物活性化合物。结果表明，用 40%乙醇从烧酒提取物中洗脱得到一个生物活性馏分。浸泡时间影响烧酒提取物对结肠癌细胞系 HCT-116 细胞增殖的抑制作用，21 天浸泡的抑制作用最强。此外，烧酒提取物通过高效液相色谱（HPLC）分离成四个馏分，A-D，B、C 和 D 馏分，但不是 A 馏分，对 HCT-116 细胞和 HL-60 细胞的增殖抑制和诱导凋亡作用。此外，通过质子核磁共振（H-NMR）、傅里叶变换红外光谱（FT-IR）和电喷雾电离质谱（ESI-MS）等综合化学分析，分别鉴定 B、C 和 D 馏分为腺苷、蛹虫草素和 N-(2-羟乙基)-腺苷（HEA）。为了更好地了解蛹虫草素和 HEA 的生物活性机制，进行了 A3 腺苷受体（A3AR）激动剂和拮抗剂测试。蛹虫草素抑制细胞活力，A3AR 拮抗剂 MR1523 恢复 HEA，表明蛹虫草素和 HEA 可能作为激动剂激活 A3AR 以抑制细胞增殖。分子对接模拟表明，腺苷和蛹虫草素都结合到 A3ARs 的相同口袋部位，而 HEA 则表现出不同的结合模式，这可能解释了它们生物活性的差异。综上所述，本研究表明，蛹虫草素和 HEA 是蛹虫草烧酒的主要生物活性成分，对体外抗癌活性有贡献。
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