Anti-cancer agents in Saudi Arabian herbals revealed by automated high-content imaging

Abstract

Natural products have been used for medical applications since ancient times. Commonly, natural products are structurally complex chemical compounds that efficiently interact with their biological targets, making them useful drug candidates in cancer therapy. Here, we used cell-based phenotypic profiling and image-based high-content screening to study the mode of action and potential cellular targets of plants historically used in Saudi Arabia’s traditional medicine. We compared the cytological profiles of fractions taken from Juniperus phoenicea (Arar), Anastatica hierochuntica (Kaff Maryam), and Citrullus colocynthis (Hanzal) with a set of reference compounds with established modes of action. Cluster analyses of the cytological profiles of the tested compounds suggested that these plants contain possible topoisomerase inhibitors that could be effective in cancer treatment. Using histone H2AX phosphorylation as a marker for DNA damage, we discovered that some of the compounds induced double-strand DNA breaks. Furthermore, chemical analysis of the active fraction isolated from Juniperus phoenicea revealed possible anti-cancer compounds. Our results demonstrate the usefulness of cell-based phenotypic screening of natural products to reveal their biological activities.

Anastatica hierochuntica (L.) methanolic and aqueous extracts exert antiproliferative effects through the induction of apoptosis in MCF-7 breast cancer cells

“…Limited literature is available regarding the antiproliferative activity of A. hierochuntica plant extracts on mammalian cell lines ( Ali et al, 2014 , Abou-Elella et al, 2016 , Mohammed et al, 2015 ). Detailed studies related to the anticancer activity of A. hierochuntica is limited to its anti-melanogenesis ( Nakashima et al, 2010 ) and anti-cervical cancer activities ( Hajjar et al, 2017 ), using the methanolic extract of the whole plant. No information about the plant parts with possible antitumor properties against BC, is currently available.…”

New Advances in Fast Methods of 2D NMR Experiments

“…The authors of this study have reported an accuracy of 1-2%, an average precision of 3%, which is believed to be better than those previously achieved with different approaches [95]. This approach is also used in acquiring R1 longitudinal relaxation rates [4].…”

“…More importantly, NMR has the ability to evaluate information about the environment of each atom and their neighbor's nuclei (both through space and through bond), allowing researchers to differentiate the unique magnetic environments of the same nuclei in different positions of a single molecule. Thus, NMR spectroscopy is extensively used for the identification and in the structural elucidation in a wide Nuclear Magnetic Resonance 2 range of applications in gas [2,3], liquid [4][5][6][7][8][9][10][11][12][13][14][15][16], and solid-state samples [17][18][19][20][21][22][23][24][25][26][27][28]. Nowadays, NMR spectroscopy is one of the most important analytical tools that has been used in several fields.…”

NMR as a “Gold Standard” Method in Drug Design and Discovery

“…The available literature [ 32 , 33 , 34 , 36 ] highlights the practicality of NMR in drug design studies. For these reasons, NMR spectroscopy is highly sought after in drug development [ 37 , 38 , 39 , 40 , 41 ], for both molecule identification [ 11 , 13 , 14 , 18 , 42 , 43 , 44 , 45 , 46 ] and structural elucidation [ 15 , 16 , 17 , 45 , 47 , 48 , 49 , 50 , 51 ]. NMR has been successfully applied in stereochemistry [ 52 , 53 , 54 , 55 , 56 ] and isomer determination [ 57 , 58 , 59 , 60 , 61 ], in drug-protein interactions studies [ 62 , 63 , 64 ], and in the evaluation of drug toxicity [ 65 , 66 , 67 , 68 ].…”