Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa.
BACKGROUND: Natural 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 ac...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
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Public Library of Science (PLoS)
2011-01-01
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| Series: | PLoS ONE |
| Online Access: | http://europepmc.org/articles/PMC3112233?pdf=render |
| _version_ | 1818313705207627776 |
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| author | Ouchen Wang Sujun Liu Jiawei Zou Liting Lu Lin Chen Sunquan Qiu He Li Xincheng Lu |
| author_facet | Ouchen Wang Sujun Liu Jiawei Zou Liting Lu Lin Chen Sunquan Qiu He Li Xincheng Lu |
| author_sort | Ouchen Wang |
| collection | DOAJ |
| description | BACKGROUND: Natural 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 FINDINGS: THA 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. CONCLUSION: The 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. |
| first_indexed | 2024-12-13T08:37:59Z |
| format | Article |
| id | doaj.art-ffa443b0030e4e568ad4213f4cf8fd7d |
| institution | Directory Open Access Journal |
| issn | 1932-6203 |
| language | English |
| last_indexed | 2024-12-13T08:37:59Z |
| publishDate | 2011-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj.art-ffa443b0030e4e568ad4213f4cf8fd7d2022-12-21T23:53:36ZengPublic Library of Science (PLoS)PLoS ONE1932-62032011-01-0166e2113010.1371/journal.pone.0021130Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa.Ouchen WangSujun LiuJiawei ZouLiting LuLin ChenSunquan QiuHe LiXincheng LuBACKGROUND: Natural 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 FINDINGS: THA 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. CONCLUSION: The 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.http://europepmc.org/articles/PMC3112233?pdf=render |
| spellingShingle | Ouchen Wang Sujun Liu Jiawei Zou Liting Lu Lin Chen Sunquan Qiu He Li Xincheng Lu Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa. PLoS ONE |
| title | Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa. |
| title_full | Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa. |
| title_fullStr | Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa. |
| title_full_unstemmed | Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa. |
| title_short | Anticancer activity of 2α, 3α, 19β, 23β-Tetrahydroxyurs-12-en-28-oic acid (THA), a novel triterpenoid isolated from Sinojackia sarcocarpa. |
| title_sort | anticancer activity of 2α 3α 19β 23β tetrahydroxyurs 12 en 28 oic acid tha a novel triterpenoid isolated from sinojackia sarcocarpa |
| url | http://europepmc.org/articles/PMC3112233?pdf=render |
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