TY - JOUR
T1 - Anti-cancer agents in Saudi Arabian herbals revealed by automated high-content imaging
AU - Hajjar, Dina A.
AU - Kremb, Stephan Georg
AU - Sioud, Salim
AU - Emwas, Abdul-Hamid M.
AU - Voolstra, Christian R.
AU - Ravasi, Timothy
N1 - KAUST Repository Item: Exported on 2020-10-01
Acknowledgements: We thank Najeh Kharbatia, staff scientist, King Abdullah of Science and Technology (KAUST) Analytical Core Lab. We also thank Dr. Amal Aldhebiani (Assistant Professor of Plant Taxonomy in the Biological Sciences Department at King Abdulaziz University, Jeddah Saudi Arabia) for taxonomic plant identifications. The project was funded by: King Abdullah of Science and Technology (KAUST).
PY - 2017/6/13
Y1 - 2017/6/13
N2 - 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.
AB - 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.
UR - http://hdl.handle.net/10754/625051
UR - http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0177316
UR - http://www.scopus.com/inward/record.url?scp=85020725736&partnerID=8YFLogxK
U2 - 10.1371/journal.pone.0177316
DO - 10.1371/journal.pone.0177316
M3 - Article
C2 - 28609451
SN - 1932-6203
VL - 12
SP - e0177316
JO - PLOS ONE
JF - PLOS ONE
IS - 6
ER -
