title: Promising anti-diabetic potential of capillin and capillinol isolated from Artemisia capillaris.
abstract: Caffeoylquinic acids, flavonoids, and coumarins isolated from Artemisia capillaris have recently emerged as therapeutic candidates for diabetes and diabetic complications; however, there have been very few studies of the anti-diabetic potential of polyacetylenes. In the present study, we investigated the anti-diabetic potential of two polyacetylenes isolated from A. capillaris, namely capillin and capillinol by investigating their ability to inhibit α-glucosidase, protein tyrosine phosphatase 1B (PTP1B), and rat lens aldose reductase (RLAR). Capillin displayed potent inhibitory activity against α-glucosidase, PTP1B, and RLAR, while capillinol showed moderate inhibitory activity against α-glucosidase and PTP1B at the concentrations tested. In addition, a kinetic study revealed that capillin inhibited α-glucosidase and RLAR in a noncompetitive manner, while inhibited PTP1B in a mixed-type manner. Capillinol inhibited α-glucosidase and PTP1B in a mixed-type manner. Docking simulations of these compounds demonstrated negative binding energies and close proximity to residues in the binding pocket of PTP1B, indicating that these polyacetylenes have a high affinity and tight binding capacity for the active site of the enzyme. Furthermore, capillin dose-dependently inhibited peroxynitrite (ONOO(-))-mediated tyrosine nitration. The results clearly demonstrate the promising potential of capillin and capillinol as therapeutic interventions for the management of diabetes as well as diabetes-associated complications.
authors.affiliation: Department of Pharmacy, Mawlana Bhashani Science and Technology University, Santosh, Tangail, 1902, Bangladesh.
authors.forename: Md Nurul
authors.initials: MN
authors.lastname: Islam
authors.affiliation: Angiogenesis & Chinese Medicine Laboratory, Department of Pharmacology, University of Cambridge, Cambridge, UK.
authors.forename: Ran Joo
authors.initials: RJ
authors.lastname: Choi
authors.affiliation: Department of Food Science and Human Nutrition, Chonbuk National University, Jeonju, 561-756, Republic of Korea. jungha@jbnu.ac.kr.
authors.forename: Hyun Ah
authors.initials: HA
authors.lastname: Jung
authors.affiliation: Korean BioInformation Center (KOBIC), Daejeon, 305-806, Republic of Korea.
authors.forename: Sang Ho
authors.initials: SH
authors.lastname: Oh
authors.affiliation: Department of Food and Life Science, Pukyong National University, Busan, 608-737, Republic of Korea. choijs@pknu.ac.kr.
authors.forename: Jae Sue
authors.initials: JS
authors.lastname: Choi
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors; D000480:Alkynes / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D019306:Artemisia / Q000737:chemistry*; D053280:Diynes / Q000302:isolation & purification / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology; D000441:Hexanols / Q000302:isolation & purification / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000302:isolation & purification / Q000494:pharmacology; D007908:Lens, Crystalline / Q000201:enzymology; D062105:Molecular Docking Simulation; D030421:Peroxynitrous Acid / Q000037:antagonists & inhibitors; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors; D051381:Rats
chemical_list: D000480:Alkynes; D053280:Diynes; D065089:Glycoside Hydrolase Inhibitors; D000441:Hexanols; D007004:Hypoglycemic Agents; C000618315:capillinol; D030421:Peroxynitrous Acid; C065814:capillin; D000449:Aldehyde Reductase; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1
keywords: Aldose reductase; Anti-diabetic; Capillin; Capillinol; Protein tyrosine phosphatase 1B; α-Glucosidase