title: Protein tyrosine phosphatase 1B (PTP1B) inhibitory constituents from the aerial parts of Tradescantia spathacea Sw.
abstract: Inhibitors of protein tyrosine phosphatase 1B (PTP1B) are promising agents for the treatment of type 2 diabetes and obesity. The bioactivity-guided isolation led to the separation of two new compounds, (±)-tradescantin (13) and tradescantoside (16), along with fourteen known compounds (1-12, 14, and 15) from the aerial parts of Tradescantia spathacea Sw. (Commelinaceae). Their chemical structures were elucidated by spectroscopic methods as well as by comparing with those reported in the literature. The isolated compounds (1-16) were then examined for their inhibitory activity toward PTP1B. The results indicated that compounds 2, 6, 8, and 12 possessed potent inhibition with IC50 values of 7.82±0.79, 6.80±0.89, 4.55±0.92, and 6.38±0.14 μM, respectively. Kinetic study of compounds 2, 6, 8, 12, 13, and 16 was conducted and the structure-activity relationships of the isolated compounds (1-16) were also discussed herein. To the best of our knowledge, all the isolates were separated for the first time from this plant.
authors: College of Pharmacy, Catholic University of Daegu, Gyeongsan 712-702, Republic of Korea; Faculty of Pharmacy, Hue University of Medicine and Pharmacy, Hue University, Hue City, Viet Nam.
authors: Quoc Hung
authors: QH
authors: Vo
authors: College of Pharmacy, Catholic University of Daegu, Gyeongsan 712-702, Republic of Korea.
authors: Phi Hung
authors: PH
authors: Nguyen
authors: College of Pharmacy, Catholic University of Daegu, Gyeongsan 712-702, Republic of Korea.
authors: Bing Tian
authors: BT
authors: Zhao
authors: Department of Food Science & Nutrition, Pukyong National University, Busan 608-737, Republic of Korea.
authors: Md Yousof
authors: MY
authors: Ali
authors: Department of Food Science & Nutrition, Pukyong National University, Busan 608-737, Republic of Korea.
authors: Jae Soo
authors: JS
authors: Choi
authors: College of Pharmacy, Catholic University of Daegu, Gyeongsan 712-702, Republic of Korea. Electronic address: bsmin@cu.ac.kr.
authors: Byung Sun
authors: BS
authors: Min
authors: Faculty of Pharmacy, Hue University of Medicine and Pharmacy, Hue University, Hue City, Viet Nam.
authors: Thi Hoai
authors: TH
authors: Nguyen
authors: College of Pharmacy, Catholic University of Daegu, Gyeongsan 712-702, Republic of Korea. Electronic address: woomh@cu.ac.kr.
authors: Mi Hee
authors: MH
authors: Woo
mesh_terms: D002109:Caffeic Acids / Q000737:chemistry / Q000302:isolation & purification; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification; D005960:Glucosides / Q000737:chemistry / Q000302:isolation & purification; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010654:Phenylbutyrates / Q000737:chemistry / Q000302:isolation & purification; D035261:Plant Components, Aerial / Q000737:chemistry; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D034823:Tradescantia / Q000737:chemistry*
chemical_list: D002109:Caffeic Acids; D004791:Enzyme Inhibitors; D005960:Glucosides; D010654:Phenylbutyrates; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
keywords: PTP1B inhibitors; Tradescantia spathacea Sw.; Tradescantin; Tradescantoside; Type 2 diabetes