Contents lists available at ScienceDirect Acta Tropica journal homepage: www.elsevier.com/locate/actatropica Phytochemical profiling, antioxidant and anticancer activities of Gastrocotyle hispida growing in Saudi Arabia Abdelaaty A. Shahat a,c, ⁎ , Syed Hidayathulla a , Azmat A. Khan b , Amer M. Alanazi b , Osaid T. Al Meanazel b , Ali S. Alqahtani a , Mansour S. Alsaid a , Ahmed A. Hussein d a Pharmacognosy Department, Saudi Arabia b Pharmaceutical Chemistry Department, College of Pharmacy, King Saud University, PO Box 2457, Riyadh, 11451, Saudi Arabia c Phytochemistry Dept., National Research Centre, 33 El Bohouth St. (former El Tahrirst.) Dokki, P. O. 12622, Giza, Egypt d Chemistry Department, Cape Peninsula University of Technology, P.O. Box 1906, Bellville 7535, South Africa ARTICLE INFO Keywords: Anticancer Gastrocotyle hispida MTT Antioxidant ABSTRACT The present study aimed at isolation the phytocompounds from the aerial parts of Gastrocotyle hispida and to evaluate its antioxidant and anticancer potential using in vitro assay. Gastrocotyle hispida is belonging to the family Boraginaceae used as a refreshing drink like tea. The decoction of the leaves is diuretic and is used in the treatment of rheumatism. Phytochemical study of a methanol extract yielded five known compounds viz: β- sitosterol (GH-1), β-sitosterol 3-glucoside (GH-2), 1-O-β-glucopyranosyl-1,4-dihydroxy-2-prenylbenzene (GH- 3), 6-Hydroxy-2,2-dimethyl-3-chrom (GH-4) and rosmarinic acid (GH-5). Total phenolic and flavonoid contents were calculated for the extract and fractions, the methanolic extract contained the highest content of total flavonoids (178 mg/g, expressed as quercetin equivalents) and total polyphenol (98.4 mg/g, expressed as gallic acid equivalent). Compounds were isolated by using column chromatography. In vitro, antioxidant activity of the extract and isolated compounds was investigated by DPPH and ABTS radical scavenging assays. The four different cell lines HepG2 (Liver), HEK-293 (Kidney) MCF-7 (Breast) and MDA-MB 231 (Breast) were used against the compounds. The isolated compounds showed dose-dependent free radical scavenging property in all tested models with the IC 50 values of 10.2 μg/mL rosmarinic acid (GH-5), 52.1 μg/mL β-sitosterol (GH-1) and 85 μg/mL for β-sitosterol 3-glucoside (GH-2). The β-sitosterol (GH-1) showed significant activity against HepG2 and HEK 293 cell lines. Rosmarinic acid (GH-5) possesses potent anticancer activity against breast cancer cells (MCF7) with the IC 50 value of 4.2 μg/mL. It can be concluded that Gastrocotyle hispida has potential antioxidant, anticancer activities and further used as an anticancer agent. 1. Introduction Cancer is one of the most life-threatening diseases, with more than 100 different types occurring due to some molecular changes within the cell. It is the third leading cause of death worldwide following cardio- vascular and infectious diseases. (Shaikh et al., 2014). Cancer is a major public health burden in both developed and developing countries. Ac- cording to WHO, cancer is one of the leading causes of death world- wide, which accounted for 7.6 million deaths (around 13%) of the world’s population annually. Furthermore, WHO estimated that the worldwide deaths are likely to rise to over 11 million in 2030 (Dai and Mumper, 2010). The limited success of the currently used clinical therapies including radiation, chemotherapy, immunomodulation, and surgery in treating cancer, as evident by the high morbidity and mortality rates, indicates that there is an imperative need of new cancer management (Bhandari, 2015). Due to lack of effective drugs, cost of chemotherapeutic agents, and the side effects of anticancer drugs, cancer can be a cause of death. Therefore, efforts are still being made to search for effective naturally occurring anticarcinogens that would prevent, slow, or reverse cancer development. Medicinal plants have a special place in the management of cancer. It is estimated that plant- derived compounds in one or the other way constitute more than 50% of anticancer agents (Karayil, 2016). The National Cancer Institute collected about 35,000 plant samples from 20 countries and has screened around 114,000 extracts for an- ticancer activity. It was estimated that 14 cancer drugs of the top 35 drugs in year 2000 based on worldwide sales were natural products and natural product derivatives. Thus, it is urgent to find more and more https://doi.org/10.1016/j.actatropica.2019.01.013 Received 6 February 2018; Received in revised form 15 January 2019; Accepted 15 January 2019 ⁎ Corresponding author at: Pharmacognosy Department, College of Pharmacy, King Saud University, Riyadh, 11451, Saudi Arabia. E-mail address: ashahat@ksu.edu.sa (A.A. Shahat). Acta Tropica 191 (2019) 243–247 Available online 16 January 2019 0001-706X/ © 2019 Elsevier B.V. All rights reserved. T