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Year : 2017  |  Volume : 13  |  Issue : 50  |  Page : 289-293

Antiproliferative activity of Haematoxylum brasiletto H. Karst

1 Laboratory of Chemistry of Natural Products, School of Chemical and Biological Sciences, Guerrero State University, Chilpancingo, Guerrero, Mexico
2 Department of Natural Products, Institute of Chemistry, Mexico National Autonomous University (UNAM), Ciudad de, México
3 School of Regional Development Sciences, Guerrero State University, Acapulco, Guerrero, Mexico
4 Department of Chemical and Biological Sciences, Sonora State University, Blvd. Luis Donaldo Colosio esq. Rosales s/n Col. Centro, Hermosillo, Sonora, Mexico
5 National Institute of Cancerology, Tlalpan, Ciudad de México, Mexico

Correspondence Address:
R E Robles-Zepeda
Department of Chemical and Biological Sciences, Sonora State University, Blvd. Luis Donaldo Colosio esq. Rosales s/n Col. Centro, Hermosillo, Sonora
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Source of Support: None, Conflict of Interest: None

DOI: 10.4103/pm.pm_466_16

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Background: Haematoxylum brasiletto is a tree that grows in Central America, commonly known as “Palo de Brasil,” which is used in the traditional medicine for the treatment of cancer and gastric ulcers. Objective: The aim of this study was to isolate the compounds responsible for antiproliferative activity of H. brasiletto. Materials and Methods: A bioassay-guided fractionation of ethanol extract of H. brasiletto was performed using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide cell proliferation assay to measure the antiproliferative activity on six human cancer cell lines (A549, LS180, HeLa, SiHa, MDA-MB-231, and NCI-H1299) and one human noncancer cell line (ARPE-19). The ethanol extract was partitioned with hexane, dichloromethane, and ethyl acetate. The active dichloromethane fraction was fractioned by silica-column chromatography, and active subfractions were separated using preparative-thin layer chromatography. The chemical structure of an isolated compound was elucidated with different chemical and spectroscopic methods. Results: The flavonoid brazilin (1) was isolated from the heartwood of H. brasiletto. The measurement of antiproliferative activity showed that brazilin can inhibit the growth of SiHa, MDA-MB-231, A549, and NCI-H1299 cell lines by 50% at doses of 44.3, 48.7, 45.4, and 48.7 μM, respectively. Furthermore, the flavonoid showed a high antiproliferative activity on LS 180 and HeLa with IC50 values of 62.2 and 71.9 μM, respectively. Brazilin also exhibited a high antiproliferative activity on the human noncancer cell line ARPE-19 with an IC50 value of 37.9 μM. Conclusions: Brazilin: (6aS,11bR)-7,11b-Dihidro-6H-indeno[2,1-c] cromeno-3,6a, 9,10-tetrol was isolated; this compound demonstrated antiproliferative activity against several human cancer cell lines. This work demonstrated that brazilin, a flavonoid isolated and characterized of H. brasiletto, has antiproliferative activity against cancer cell lines. Abbreviations used: MTT: [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium]; FBS: Fetal bovine serum; TLC: Thin layer chromatography.

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