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Chemical constituents from the roots of Kadsura coccinea with their protein tyrosine phosphatase 1B and acetylcholinesterase inhibitory activities

Archives of Pharmacal Research 2020년 43권 2호 p.204 ~ 213
우미희 ( Woo Mi-Hee ) - Daegu Catholic University College of Pharmacy

 ( Nguyen Duc Hung ) - Daegu Catholic University College of Pharmacy
최재수 ( Choi Jae-Sue ) - Pukyong National University Department of Food and Life Science
 ( Park Se-Eun ) - Pukyong National University Department of Food and Life Science
 ( Thuong Phuong Thien ) - National Institute of Medicinal Materials Department of Herbal Analysis and Standardization
민병순 ( Min Byung-Sun ) - Daegu Catholic University College of Pharmacy
 ( Le Duc Dat ) - Ton Duc Thang University Faculty of Pharmacy

Abstract


Kadsura coccinea (Lem.) A. C. Smith has been used as a tonic, decongestant, and digestive agent. The roots are also employed in traditional medicine to treat chronic enteritis, acute gastritis, duodenal ulcers, rheumatic pain in bone, and traumatic injuries. In the present study, we have described the biological evaluation of constituents from the roots of K. coccinea with PTP1B and AChE inhibitory activities for the first time in literature. A new compound (1), kadcoccilactone T, and 24 known ones (2?25) were isolated and identified using spectroscopic methods. All the isolates were examined for PTP1B and AChE inhibitory activities. Compounds 4 and 8 expressed strong PTP1B inhibition with IC50 values of 1.57?±?0.11 and 3.99?±?1.08 μM, respectively. Apparently, these compounds were further studied for PTP1B enzyme kinetic analysis. The result indicated that compounds 4 and 8 exhibited mixed-type inhibition with the Κi values of 4.97 and 3.26 μM, respectively.

키워드

Kadsura coccinea; Nortriterpenoids; PTP1B; AChE
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