title: Synthesis and biological evaluation of Hederacolchiside A1 derivatives as anticancer agents.
abstract: Modification of Hederacolchiside A1 (HA1) on 28-COOH gave a series of novel triterpenoid saponin compounds containing ester or amide group. Comparing with natural product HA1, several derivatives showed decreased toxicity in the mice acute toxicity trial and increased the anticancer activity in vitro. Especially compound 1 exhibited the strongest antiproliferative activities against human cancer cell lines tested (IC50=1.1-4.6μM) and potent tumor inhibition rate in vivo (46.8%).
authors: National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
authors: Yuanying
authors: Y
authors: Fang
authors: College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, 818 Xingwan Road, Nanchang 330004, China.
authors: Zunhua
authors: Z
authors: Yang
authors: National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
authors: Hui
authors: H
authors: Ouyang
authors: National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
authors: Rikang
authors: R
authors: Wang
authors: National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
authors: Jun
authors: J
authors: Li
authors: National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
authors: Hesong
authors: H
authors: Huang
authors: National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
authors: Yi
authors: Y
authors: Jin
authors: National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, 56 Yangming Road, Nanchang 330006, China.
authors: Yulin
authors: Y
authors: Feng
authors: College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, 818 Xingwan Road, Nanchang 330004, China.
authors: Shilin
authors: S
authors: Yang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D012503:Saponins / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D012503:Saponins; C467827:hederacolchisid A1
keywords: Anticancer activity; Derivatives; Hederacolchiside A(1); Triterpenoid saponins