Isolation of dihydrobenzofuran derivatives from ethnomedicinal species polygonum barbatum as anticancer compounds
文献类型：期刊论文
| 作者 | Farooq, Umar1,2; Naz, Sadia1; Shams, Afshan3; Raza, Yasir4; Ahmed, Ayaz3; Rashid, Umer1; Sadiq, Abdul5,6 |
| 刊名 | Biological research
 |
| 出版日期 | 2019-01-07 |
| 卷号 | 52页码:12 |
| 关键词 | Dihydrobenzofuran Polygonum barbatum Ethnomedicine Oral and lungs carcinoma Antiangiogenesis Anticancer |
| ISSN号 | 0716-9760 |
| DOI | 10.1186/s40659-018-0209-0 |
| 通讯作者 | Farooq, umar(umarf@cuiatd.edu.pk) ; Rashid, umer() ; Sadiq, abdul() |
| 英文摘要 | Backgroundethnomedicinally, 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.methodsthe 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.resultsthree 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 48.520.95 and 53.24 +/- 1.49 against oral cancer cells as compared to standard drug (ic50=97.76 +/- 3.44m). 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 48h treatment. in antiangiogenesis assay, compounds 1, 2 and 3 exhibited ic50 values of 8.2 +/- 1.1, 13.4 +/- 1.1 and 57.7 +/- 0.3m 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. |
| WOS关键词 | ANTITUMOR |
| WOS研究方向 | Life Sciences & Biomedicine - Other Topics |
| WOS类目 | Biology |
| 语种 | 英语 |
| WOS记录号 | WOS:000455007500001 |
| 出版者 | SOC BIOLGIA CHILE |
| URI标识 | http://www.irgrid.ac.cn/handle/1471x/2372920 |
| 专题 | 大连化学物理研究所 |
| 通讯作者 | Farooq, Umar; Rashid, Umer; Sadiq, Abdul |
| 作者单位 | 1.COMSATS Univ Islamabad, Dept Chem, Abbottabad Campus, Abbottabad 22060, Pakistan 2.Chinese Acad Sci, Inst Chem, State Key Lab Mol React Dynam, Beijing Natl Lab Mol Sci, Beijing 100190, Peoples R China 3.Univ Karachi, Int Ctr Chem & Biol Sci, Dr Panjwani Ctr Mol Med & Drug Res, Karachi, Pakistan 4.Univ Karachi, Dept Microbiol, Karachi, Pakistan 5.Univ Malakand, Dept Pharm, Chakdara 18000, KP, Pakistan 6.Jacobs Univ Bremen, Fac Hlth, Dept Life Sci & Chem, D-28759 Bremen, Germany |
| 推荐引用方式 GB/T 7714 | Farooq, Umar,Naz, Sadia,Shams, Afshan,et al. Isolation of dihydrobenzofuran derivatives from ethnomedicinal species polygonum barbatum as anticancer compounds[J]. Biological research,2019,52:12. |
| APA | Farooq, Umar.,Naz, Sadia.,Shams, Afshan.,Raza, Yasir.,Ahmed, Ayaz.,...&Sadiq, Abdul.(2019).Isolation of dihydrobenzofuran derivatives from ethnomedicinal species polygonum barbatum as anticancer compounds.Biological research,52,12. |
| MLA | Farooq, Umar,et al."Isolation of dihydrobenzofuran derivatives from ethnomedicinal species polygonum barbatum as anticancer compounds".Biological research 52(2019):12. |
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来源：大连化学物理研究所
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