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Phytochem Anal ; 33(4): 612-618, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35243708

RESUMEN

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), α-glucosidase, and α-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 (Ki ) values were calculated to determine in vitro enzyme inhibition effects. RESULTS: Tomentosin was isolated in high yield (0.64%). The IC50 and Ki 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. 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 α-glucosidase and α-amylase. These results suggested that tomentosin has α-glucosidase and α-amylase inhibitor potential.


Asunto(s)
Inula , Sesquiterpenos , Acetilcolinesterasa , Butirilcolinesterasa , Anhidrasa Carbónica II , Cromatografía Liquida , Etanol , Inula/química , Lactonas/farmacología , Cloruro de Metileno , Extractos Vegetales/farmacología , Sesquiterpenos/farmacología , Espectrometría de Masas en Tándem , alfa-Amilasas , alfa-Glucosidasas
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