A new specific method for isolation of tomentosin with a high yield from Inula viscosa (L.) and determination of its bioactivities
A new specific method for isolation of tomentosin with a high yield from Inula viscosa (L.) and determination of its bioactivities
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DOI：
10.1002/pca.3114
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发表时间：
2022-03-04
影响因子：
3.3
通讯作者：
Cakir, Ahmet
中科院分区：
文献类型：
--
作者：
Aydin, Tuba;Saglamtas, Ruya;Cakir, Ahmet
简介 毛毛素是旋覆花 (Inula viscosa (L.)) 的特征成分，是一种重要的倍半萜内酯，具有抗癌作用。获得纯毛毛素的方法不足以用于抗癌药物研究。目的本研究旨在开发一种从 I. viscosa 中高产分离绒毛素的具体方法。它还旨在研究毛妥菌素对人碳酸酐酶 I (hCAI)、人碳酸酐酶 II (hCAII)、乙酰胆碱酯酶 (AChE)、丁酰胆碱酯酶 (BChE)、α-葡萄糖苷酶和 α-淀粉酶的抑制作用。材料和方法 毛毛素通过特定的柱层析方法纯化。采用液相色谱-串联质谱法(LC-MS/MS)测定粘毛苋提取物二氯甲烷、二氯甲烷索氏法、乙醇和乙醇索氏法提取物中绒毛素的含量。计算半数最大抑制浓度（IC50）和抑制常数（K-i）值以确定体外酶抑制效果。结果毛毛素的分离得率较高（0.64%）。绒毛菌素的 IC50 和 K-i 值计算为：hCAI 为 5.00 +/- 0.19 (r = 0.9688) 和 4.62 +/- 0.10 μM，hCAII 为 5.40 +/- 0.26 (r = 0.9677) 和 5.22 +/- 0.31 μM，hCAII 为 6.75 +/- 0.208 AChE 为 (r = 0.9891) 和 3.75 +/- 0.27 mu M，BChE 为 6.67 +/- 0.307 (r = 0.9820) 和 0.51 +/- 0.11 mu M，BChE 为 26.61 +/- 0.236 (r = 0.9815) 和 2.61 +/- 0.71 mu M α-葡萄糖苷酶和 α-淀粉酶分别为 26.89 +/- 1.54 mu M (r = 0.9670)。结论 与阳性对照相比，从粘毛花糊状提取物中分离得到高产率的毛毛素，确定毛毛素对 hCAI、hCAII、AChE 和 BChE 的作用较弱，但对 α-葡萄糖苷酶和 α-淀粉酶的作用完全有效。这些结果表明毛毛素具有 α-葡萄糖苷酶和 α-淀粉酶抑制剂的潜力。
Introduction Tomentosin, the characteristic component of Inula viscosa (L.) is an important sesquiterpene lactone with anticarcinogenic effects. Methods of obtaining pure tomentosin are not sufficient for anticancer drug research. Objectives This study aims to develop a specific method to isolate tomentosin from I. viscosa with high yield. It also aims to investigate the inhibitory effects of tomentosin on human carbonic anhydrase I (hCAI), human carbonic anhydrase II (hCAII), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), alpha-glucosidase, and alpha-amylase enzymes. Material and methods Tomentosin was purified by a specific column chromatography method. The content of tomentosin in dichloromethane, dichloromethane by Soxhlet method, ethanol and ethanol by Soxhlet method extracts of I. viscosa was determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Half maximal inhibitory concentration (IC50) and inhibition constant (K-i) values were calculated to determine in vitro enzyme inhibition effects. Results Tomentosin was isolated in high yield (0.64%). The IC50 and K-i values for tomentosin were calculated as 5.00 +/- 0.19 (r = 0.9688) and 4.62 +/- 0.10 mu M for hCAI, 5.40 +/- 0.26 (r = 0.9677) and 5.22 +/- 0.31 mu M for hCAII, 6.75 +/- 0.208 (r = 0.9891) and 3.75 +/- 0.27 mu M for AChE, 6.67 +/- 0.307 (r = 0.9820) and 0.51 +/- 0.11 mu M for BChE, 26.61 +/- 0.236 (r = 0.9815) and 2.61 +/- 0.71 mu M for alpha-glucosidase and 26.89 +/- 1.54 mu M (r = 0.9670) for alpha-amylase, respectively. Conclusion Tomentosin was isolated in high yield from the paste-like extract of I. viscosa compared to the positive controls, it was determined that tomentosin was weakly effective against hCAI, hCAII, AChE and BChE, but thoroughly effective against alpha-glucosidase and alpha-amylase. These results suggested that tomentosin has alpha-glucosidase and alpha-amylase inhibitor potential.