Quinoline-2-carboxylic acid isolated from Ephedra pachyclada and its structural derivatives show inhibitory effects against α-glucosidase and α-amylase

• Published in: Applied biological chemistry Vol. 57; no. 4; pp. 441 - 444
• Main Authors: Lee, Hwa-Won, Yang, Ji-Yeon, Lee, Hoi-Seon
• Format: Journal Article
• Language: English
• Published: Seoul The Korean Society for Applied Biological Chemistry 01.08.2014; Springer Nature B.V; 한국응용생명화학회
• Subjects: Acarbose; Acids; Amylases; Applied Microbiology; Bioactive compounds; Biological activity; Biological Techniques; Bioorganic Chemistry; Carboxyl group; Carboxylic acids; Chemistry; Chemistry and Materials Science; Chloroform; Derivatives; Diabetes mellitus; Ephedra; Glucosidase; Quinoline; α-Amylase; α-Glucosidase; 농학; quinoline-2-carboxylic acid; α-glucosidase; α-amylase; antidiabetic activity
• ISSN: 1738-2203; 2468-0834; 2234-344X; 2468-0842
• DOI: 10.1007/s13765-014-4156-3

The aim of present study was to isolate a bioactive compound from the chloroform fraction of Ephedra pachyclada stems and to evaluate antidiabetic activities against α-glucosidase and α-amylase. According to various chromatographic and spectroscopic analyses, the bioactive compound of E. pachyclada was identified as quinoline-2-carboxylic acid. Based on the IC 50 values of quinoline-2-carboxylic acid derivatives against α-glucosidase and α-amylase, quinoline-2-carboxylic acid (9.1 and 15.5 μg/mL) exhibited potent inhibitory activities, followed by quinoline-3-carboxylic acid (10.6 and 31.4 μg/mL), quinoline-4-carboxylic acid (60.2 and 152.4 μg/mL), and acarbose (66.5 and 180.6 μg/mL) against α-glucosidase and α-amylase, respectively. However, quinoline-2-carboxaldehyde, quinoline-3-carboxaldehyde, and quinoline-4-carboxaldehyde showed no inhibitory activities. Antidiabetic activity depended on the existence of a carboxyl group on quinoline for activities against α-glucosidase and α-amylase. Therefore, E. pachyclada and quinoline-2-carboxylic acid derivatives could be suitable as alternative synthetic antidiabetic agents.