Faculty of Pharmacy, Ağrı İbrahim Çeçen University, Agri, Türkiye.
Central Research and Application Laboratory, Ağrı İbrahim Çeçen University, Agri, Türkiye.
Phytochem Anal. 2022 Jun;33(4):612-618. doi: 10.1002/pca.3114. Epub 2022 Mar 4.
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.
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), α-glucosidase, and α-amylase enzymes.
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 (IC ) and inhibition constant (K ) values were calculated to determine in vitro enzyme inhibition effects.
Tomentosin was isolated in high yield (0.64%). The IC and K values for tomentosin were calculated as 5.00 ± 0.19 (r = 0.9688) and 4.62 ± 0.10 μM for hCAI, 5.40 ± 0.26 (r = 0.9677) and 5.22 ± 0.31 μM for hCAII, 6.75 ± 0.208 (r = 0.9891) and 3.75 ± 0.27 μM for AChE, 6.67 ± 0.307 (r = 0.9820) and 0.51 ± 0.11 μM for BChE, 26.61 ± 0.236 (r = 0.9815) and 2.61 ± 0.71 μM for α-glucosidase and 26.89 ± 1.54 μM (r = 0.9670) for α-amylase, respectively.
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 α-glucosidase and α-amylase. These results suggested that tomentosin has α-glucosidase and α-amylase inhibitor potential.
土木香内酯是旋覆花(Inula viscosa(L.))的特征成分,是一种具有抗癌作用的重要倍半萜内酯。获得纯土木香内酯的方法不足以进行抗癌药物研究。
本研究旨在开发一种从土木香中高产量分离土木香内酯的特定方法。还旨在研究土木香内酯对人碳酸酐酶 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。
通过特定的柱色谱法纯化土木香内酯。通过液相色谱-串联质谱(LC-MS/MS)测定土木香二氯甲烷、索氏提取二氯甲烷、乙醇和乙醇提取物中土木香内酯的含量。计算半最大抑制浓度(IC )和抑制常数(K )值以确定体外酶抑制作用。
土木香内酯以高产率(0.64%)分离。土木香内酯的 IC 和 K 值分别计算为 5.00 ± 0.19(r = 0.9688)和 4.62 ± 0.10 μM 用于 hCAI、5.40 ± 0.26(r = 0.9677)和 5.22 ± 0.31 μM 用于 hCAII、6.75 ± 0.208(r = 0.9891)和 3.75 ± 0.27 μM 用于 AChE、6.67 ± 0.307(r = 0.9820)和 0.51 ± 0.11 μM 用于 BChE、26.61 ± 0.236(r = 0.9815)和 2.61 ± 0.71 μM 用于α-葡萄糖苷酶和 26.89 ± 1.54 μM(r = 0.9670)用于α-淀粉酶。
与阳性对照相比,土木香内酯从土木香的糊状提取物中以高产率分离,结果表明土木香内酯对 hCAI、hCAII、AChE 和 BChE 的抑制作用较弱,但对α-葡萄糖苷酶和α-淀粉酶的抑制作用非常有效。这些结果表明土木香内酯具有α-葡萄糖苷酶和α-淀粉酶抑制剂的潜力。