title: The cytotoxic activities of cardiac glycosides from Streptocaulon juventas and the structure-activity relationships.
abstract: A series of cardiac glycosides were isolated and identified from the anti-tumor fraction of the root of Streptocaulon juventas in previous studies. In the present research, the cytotoxic activities of the 43 cardiac glycosides on three cell lines, human lung A549 adenocarcinoma cell, large cell lung cancer NCI-H460 cell and normal human fetal lung fibroblast MRC-5 cell, were evaluated in vitro. Most of the tested compounds showed potent inhibitory activities toward the three cell lines. Then, the structure-activity relationships were discussed in detail. It was indicated that hydroxyl and acetyl groups at C-16 increased the activity, whereas hydroxyl group at C-1 and C-5 can both increase and decrease the activity. Two glucosyl groups which were connected by C1'→C6' showed better inhibitory activity against cancer cell lines, while the C1'→C4' connection showed stronger inhibitory activity against the normal cell line. Also, this is the first report that the activities of these compounds exhibited different variation trends between A549 and NCI-H460 cell lines, which indicated that these compounds could selectively inhibit the cell growth. The results would lay a foundation for further research on new anti-tumor drug development.
authors.affiliation: Development and Utilization Key Laboratory of Northeast Plant Materials, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Rui
authors.initials: R
authors.lastname: Xue
authors.affiliation: Development and Utilization Key Laboratory of Northeast Plant Materials, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Na
authors.initials: N
authors.lastname: Han
authors.affiliation: Development and Utilization Key Laboratory of Northeast Plant Materials, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Chun
authors.initials: C
authors.lastname: Ye
authors.affiliation: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Lihui
authors.initials: L
authors.lastname: Wang
authors.affiliation: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Jingyu
authors.initials: J
authors.lastname: Yang
authors.affiliation: The People's Liberation Army 463 Hospital, Shenyang 110042, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Development and Utilization Key Laboratory of Northeast Plant Materials, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address: yinjun2002@yahoo.com.
authors.forename: Jun
authors.initials: J
authors.lastname: Yin
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D029062:Apocynaceae / Q000737:chemistry*; D002301:Cardiac Glycosides / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D015394:Molecular Structure; D018517:Plant Roots / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D002301:Cardiac Glycosides
keywords: A549; Anti-tumor activity; Cardiac glycosides; MRC-5; NCI-H460; Streptocaulon juventas