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Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

ABSTRACT: Elephantopus scaber is an ethnomedicinal plant used by the Zhuang people in Southwest China to treat headaches, colds, diarrhea, hepatitis, and bronchitis. A new ? -truxinate derivative, ethyl, methyl 3,4,3',4'-tetrahydroxy- ? -truxinate (1), was isolated from the ethyl acetate extract of the entire plant, along with 4 known compounds. The antioxidant activity of these 5 compounds was determined by ABTS radical scavenging assay. Compound 1 was also tested for its cytotoxicity effect against HepG2 by MTT assay (IC50 = 60? ? M), and its potential anti-inflammatory, antibiotic, and antitumor bioactivities were predicted using target fishing method software.

SUBMITTER: Wang J

PROVIDER: S-EPMC4055671 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature

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Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

Wang Jianjun J Li Ping P Li Baosai B Guo Zhiyong Z Kennelly Edward J EJ Long Chunlin C

Evidence-based complementary and alternative medicine : eCAM 20140519

Elephantopus scaber is an ethnomedicinal plant used by the Zhuang people in Southwest China to treat headaches, colds, diarrhea, hepatitis, and bronchitis. A new δ -truxinate derivative, ethyl, methyl 3,4,3',4'-tetrahydroxy- δ -truxinate (1), was isolated from the ethyl acetate extract of the entire plant, along with 4 known compounds. The antioxidant activity of these 5 compounds was determined by ABTS radical scavenging assay. Compound 1 was also tested for its cytotoxicity effect against HepG ...[more]

PMID: 24963325

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Project description:BACKGROUND:Ethnomedicinally, the family Polygonaceae is famous for the management of cancer. Various species of this family have been reported with anticancer potentials. This study was designed to isolate anticancer compounds from ethnomedicinally important species Polygonum barbatum. METHODS:The column chromatography was used for the isolation of compounds from the solvent fraction of P. barbatum. The characterization of isolated compounds was performed by various spectroscopic techniques like UV, IR, mass spectrometry and 1D-2D NMR spectroscopy. Keeping in view the ethnomedicinal importance of the family, genus and species of P. barbatum, the isolated compounds (1-3) were screened for anticancer potentials against oral cancer (CAL-27) and lungs cancer (NCI H460) cell lines using MTT assay. Active compound was further investigated for apoptosis by using morphological changes and flow cytometry analysis. In vivo anti-angiogenic study of the isolated compounds was also carried using chorioallantoic membrane assay. Docking studies were carried out to explore the mechanism of anticancer activity. RESULTS:Three dihydrobenzofuran derivatives (1-3) have been isolated from the ethyl acetate fraction of P. barbatum. The structures of isolated compounds were elucidated as methyl (2S,3S)-2-(3,4-dimethoxyphenyl)-4-((E)-3-ethoxy-3-oxoprop-1-en-1-yl)-7-methoxy-2,3-dihydrobenzo-furan-3-carboxylate (1), (E)-3-((2S,3S)-2-(3,4-dimethoxyphenyl)-7-methoxy-3-(methoxy carbonyl)-2,3-dihydrobenzofuran-4-yl)acrylic acid (2) and (2S,3S)-4-((E)-2-carboxyvinyl)-2-(3,4-dimethoxyphenyl)-7-hydroxy-2,3-dihydrobenzofuran-3-carboxylic acid (3). The compound 1 was found to be more potent with IC50 of 48.52?±?0.95 and 53.24?±?1.49 against oral cancer cells as compared to standard drug (IC50?=?97.76?±?3.44 ?M). Both compound also inhibited lung cancer cells but at higher concentrations. Morphological and flow cytometry analysis further confirms that compound 1 induces apoptosis after 24 to 48 h treatment. In antiangiogenesis assay, compounds 1, 2 and 3 exhibited IC50 values of 8.2?±?1.1, 13.4?±?1.1 and 57.7?±?0.3 ?M respectively. The docking studies revealed that the compounds under study have the potential to target the DNA and thymidylate synthase (TS). CONCLUSION:Based on its overwhelming potency against the tested cell lines and in angiogenesis assay, compound 1 can be further evaluated mechanistically and can be developed as anticancer drug candidate.

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Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

Publications

Bioactivities of Compounds from Elephantopus scaber, an Ethnomedicinal Plant from Southwest China.

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