Abstract
BackgroundNatural products represent an important source for agents of cancer prevention and cancer treatment. More than 60% of conventional anticancer drugs are derived from natural sources, particularly from plant-derived materials. In this study, 2α, 3α, 19β, 23β-tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid from the leaves of Sinojackia sarcocarpa, was isolated, and its anticancer activity was investigated both in vitro and in vivo.Principal FindingsTHA possessed potent tumor selected toxicity in vitro. It exhibited significantly higher cytotoxicity to the cancer cell lines A2780 and HepG2 than to IOSE144 and QSG7701, two noncancerous cell lines derived from ovary epithelium and liver, respectively. Moreover, THA showed a dose-dependent inhibitory effect on A2780 ovary tumor growth in vivo in nude mice. THA induced a dose-dependent apoptosis and G2/M cell cycle arrest in A2780 and HepG2 cells. The THA-induced cell cycle arrest was accompanied by a downregulation of Cdc2. The apoptosis induced by THA was evident by induction of DNA fragmentation, release of cytoplasmic Cytochrome c from mitochondria, activation of caspases, downregulation of Bcl-2 and upregulation of Bax.ConclusionThe primary data indicated that THA exhibit a high toxicity toward two cancer cells than their respective non-cancerous counterparts and has a significant anticancer activity both in vitro and in vivo. Thus, THA and/or its derivatives may have great potential in the prevention and treatment of human ovary tumors and other malignancies.
Highlights
Natural products represent a rich reservoir for anticancer compounds [1,2]
The primary data indicated that tetrahydroxyurs-12-en-28-oic acid (THA) exhibit a high toxicity toward two cancer cells than their respective noncancerous counterparts and has a significant anticancer activity both in vitro and in vivo
IC20, IC50, and IC80 were the concentrations of drug that inhibit growth by 20%, 50%, and 80%, respectively, relative to the control. doi:10.1371/journal.pone.0021130.t001
Summary
Natural products represent a rich reservoir for anticancer compounds [1,2]. Over sixty percent of currently used anticancer drugs are derived from natural sources such as plants, marine organisms and microorganisms [3,4]. Triterpenoids are structurally diverse organic compounds of more than 20,000 naturally occurring variants that share a basic triterpenoid moiety [7,8]. These compounds are ubiquitously distributed throughout the plant kingdom and have many biological activities. Triterpenoids have been implicated in a wide range of biological pathways or processes including nuclear factor-kappaB signalling, apoptosis, transcription, angiogenesis, and tumor metastasis [14,15,16]. These compounds are potential candidates for anticancer agents. 2a, 3a, 19b, 23b-tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid from the leaves of Sinojackia sarcocarpa, was isolated, and its anticancer activity was investigated both in vitro and in vivo
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