Anti-human hepatoma Hep-G2 proliferative, apoptotic, and antimutagenic activity of tagitinin C from Tithonia diversifolia leaves

Tagitinin C, a major sesquiterpenoid, was isolated from the leaves of Tithonia diversifolia. The high morbidity and mortality rate of hepatoma in Taiwan motivated our interest in the investigation of tagitinin C’s mechanism against the human hepatocellular carcinoma. The methanolic extract of leaves...

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Bibliographic Details
Published in:Journal of natural medicines 2013, Vol.67 (1), p.98-106
Main Authors: Liao, May-Hua, Tsai, Yuan-Nuan, Yang, Chi-Yu, Juang, Chi-Long, Lee, Ming-Yi, Chang, Li-Hsueh, Wen, Hsiao-Chuan
Format: Article
Language:English
Subjects:
Animals
antimutagenic activity
Antimutagenic Agents - chemistry
Antimutagenic Agents - pharmacology
Antimutagenic Agents - therapeutic use
apoptosis
Apoptosis - drug effects
Asteraceae - chemistry
Biomedical and Life Sciences
Biomedicine
caspases
Complementary & Alternative Medicine
cytotoxicity
Female
Hep G2 Cells
hepatoma
Humans
inhibitory concentration 50
interphase
leaves
Medicinal Chemistry
Mice
Mice, Inbred BALB C
Mice, Nude
morbidity
mortality
Original Paper
Pharmacology/Toxicology
Pharmacy
Plant Extracts - chemistry
Plant Extracts - pharmacology
Plant Extracts - therapeutic use
Plant Leaves - chemistry
Plant Sciences
population growth
Sesquiterpenes - chemistry
Sesquiterpenes - pharmacology
Sesquiterpenes - therapeutic use
Tithonia diversifolia
Xenograft Model Antitumor Assays
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Summary:Tagitinin C, a major sesquiterpenoid, was isolated from the leaves of Tithonia diversifolia. The high morbidity and mortality rate of hepatoma in Taiwan motivated our interest in the investigation of tagitinin C’s mechanism against the human hepatocellular carcinoma. The methanolic extract of leaves of T. diversifolia (TDM) and tagitinin C were found to have cytotoxic activities against human hepatoma Hep-G2 cells in the MTT assay with IC₅₀ values of 40.0 ± 2.0 and 2.0 ± 0.1 μg/mL, respectively. This compound induced population increase in the sub-G₁ phase and S phase arrest. Treatment with tagitinin C isolated from TDM resulted in activation of both caspase 3 and caspase 8 which suggested that the antiproliferative effect of this compound was caspase-dependent apoptosis. Magnetic resonance techniques indicated that the tumorigenisity of xenografts derived from Hep-G2 cells was retarded by the delivery of tagitinin C (15 μg/mouse/day) relative to the control counterparts.
ISSN:1340-3443
1861-0293
DOI:10.1007/s11418-012-0652-0