Anticholinesterase activity of coumarin derivatives isolated from the roots of Heptaptera cilicica

Alzheimer's disease is characterized by memory loss, problems with language, disorientation of time and place, poor or decreased judgment, problems with abstract thinking, misplacing things, changes in mood or behavior, changes in personality, and loss of initiative [1]. Plants contain active compounds have become new sources to investigate for the pharmaceutical industry. Numerous plants have been used to treat neurodegenerative diseases [2]. The genus Heptaptera (Apiaceae) is represented in Turkey from four species [3]. These species were known to be rich in coumarin derivatives [4 – 6] and have acetylcholinesterase inhibitory activity [7]. In this study, the chloroform extract of the roots of Heptaptera cilicica (Boiss. & Bal.) Tutin and the isolated compounds were investigated in terms of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory effects by Ellman method [8]. According to the results, chloroform extract of H. cilicica roots showed 31 and 64% inhibition against AChE and BuChE at 50 µg/ml. Among the isolated coumarin derivatives, the most potent compound was prunate which exhibited significantly high inhibitory potency against AChE (IC₅₀= 1.88 ± 0.072µM) and BuChE (IC₅₀= 0.29 ± 0.426µM) as compared with the reference compound, galantamine hydrobromide (IC₅₀= 0.22 ± 0.062µM for AChE and IC₅₀= 0.15 ± 0.187µM for BuChE).

Keywords: Heptaptera cilicica (Boiss. & Bal.) Tutin, Apiaceae, coumarin, AChE, BuChE.

References:

[1] Topcu G, Kusman T. Lamiaceae family plants as a potential anticholinesterase source in the treatment of Alzheimer's Disease. Bezmialem Science 2014; 1: 1 – 25

[2] Adewusi EA, Moodley N, Steenkamp V. Medicinal plants with cholinesterase inhibitory activity: A review. Afr J Biotechnol 2010; 9: 8257 – 8276

[3] Herrnstadt I, Heyn CC. Heptaptera Marg. & Reuter. In: Davis PH, editors. Flora of Turkey and the East Aegean Islands. University Press: Edinburgh, 1972, 388 – 390

[4] Appendino G, Özen HÇ, Tagliapietra S, Cisero M. Coumarins from Heptaptera anisoptera. Phytochemistry 1992; 31: 3211 – 3213

[5] Appendino G, Özen HÇ, Nano GM, Cisero M. Sesquiterpene coumarin ethers from the genus Heptaptera. Phytochemistry 1992; 31: 4223 – 4226

[6] Appendino G, Özen HC, Jakupovic J. A sesquiterpene coumarin ether and a coniferyl ester from Heptaptera anisoptera. Fitoterapia 1993; LXIV(6): 505 – 506

[7] Şenol FZ, Yilmaz G, Şener B, Koyuncu M, Orhan I. Preliminary screening of acetylcholinesterase inhibitory and antioxidant activities of Anatolian Heptaptera species. Pharm Biol 2010; 48: 337 – 341

[8] Ellman GL, Courtney D, Andies V, Featherstone RM. A new and rapid colorimetric determination of acetylcholinesterase activity. Biochem Pharmacol 1961; 7: 88 – 95