RRC ID 62062
Author Kitagawa N, Morikawa T, Motai C, Ninomiya K, Okugawa S, Nishida A, Yoshikawa M, Muraoka O.
Title The Antiproliferative Effect of Chakasaponins I and II, Floratheasaponin A, and Epigallocatechin 3-O-Gallate Isolated from Camellia sinensis on Human Digestive Tract Carcinoma Cell Lines.
Journal Int J Mol Sci
Abstract Acylated oleanane-type triterpene saponins, namely chakasaponins I (1) and II (2), floratheasaponin A (3), and their analogs, together with catechins-including (-)-epigallocatechin 3-O-gallate (4), flavonoids, and caffeine-have been isolated as characteristic functional constituents from the extracts of "tea flower", the flower buds of Camellia sinensis (Theaceae), which have common components with that of the leaf part. These isolates exhibited antiproliferative activities against human digestive tract carcinoma HSC-2, HSC-4, MKN-45, and Caco-2 cells. The antiproliferative activities of the saponins (1-3, IC50 = 4.4-14.1, 6.2-18.2, 4.5-17.3, and 19.3-40.6 µM, respectively) were more potent than those of catechins, flavonoids, and caffeine. To characterize the mechanisms of action of principal saponin constituents 1-3, a flow cytometric analysis using annexin-V/7-aminoactinomycin D (7-AAD) double staining in HSC-2 cells was performed. The percentage of apoptotic cells increased in a concentration-dependent manner. DNA fragmentation and caspase-3/7 activation were also detected after 48 h. These results suggested that antiproliferative activities of 1-3 induce apoptotic cell death via activation of caspase-3/7.
Volume 17(12)
Published 2016-11-26
DOI 10.3390/ijms17121979
PII ijms17121979
PMID 27898032
PMC PMC5187779
MeSH Camellia sinensis / chemistry* Caspase 3 / metabolism Caspase 7 / metabolism Catechin / analogs & derivatives* Catechin / pharmacology Cell Cycle / drug effects Cell Line, Tumor Cell Survival / drug effects DNA Fragmentation / drug effects Flowers / chemistry Humans Oleanolic Acid / analogs & derivatives* Oleanolic Acid / pharmacology Plant Extracts / chemistry Plant Extracts / pharmacology* Saponins / pharmacology*
IF 4.556
Human and Animal Cells HSC-4(RCB1902) MKN45(RCB1001) CACO-2(RCB0988)