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LC-MS Fingerprint Profile, Chemical Study and Antitumor Activity of Roots from Kielmeyera coriacea (Calophyllaceae)

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LC-MS Fingerprint Profile, Chemical Study and Antitumor Activity of Roots from Kielmeyera coriacea (Calophyllaceae)

Bryna T. A. F. Gama1, Eliângela C. C. Costa1, Lucília Kato1, Rosy I. M. De A. Ribeiro2, Kamilla M. Dos Santos2, Lucas S. Azevedo2, Afif F. Monteiro3, Vanessa G. Pasqualotto Severino1.

1 Universidade Federal de Goiás, Instituto de Química, Goiânia/GO, Brazil.
2 Universidade Federal de São João Del-Rei, Campus Centro-Oeste Dona Lindu, Divinópolis/MG, Brazil.
3 Universidade Estadual Paulista Júlio de Mesquita Filho, Araraquara/SP, Brazil.
*[email protected]

The Cerrado is the second largest plant formation in Brazil. It is a region with an unique biological richness, presenting about 10 thousand plants1. In view of this biodiversity, it is highlighted the Kielmeyera genus and K. coriacea species, native to the Brazilian Cerrado, popularly known as pau-santo. It has been reported that plants of the Kielmeyera have potential for the treatment and/or control of diseases such as schistosomiasis, leishmaniasis, malaria, cancer, infections2,3. In addition, this genus is widely used in folk medicine. However, there is no study about roots from K. coriacea. In this context, a LC-MS fingerprint profile and chemical study of the ethanolic extract of roots (EER) from K. coriacea were carried out, in order to identify the secondary metabolites present in the species. It was also done to evaluate its cytotoxic potential against HeLa cells that are related to colon cancer of the uterus. The EER was subjected to liquid-liquid extraction obtaining the hexane (FH), ethyl acetate (FAE) and hydroalcoholic (FHA) fractions. The FAE was chromatographed and the 3-hydroxy-2,4-dimethoxyxanthone was isolated. Furthermore, the chromatographic process of FH and FAE fractions afforded subfractions, which were submitted to the LC-MS chemical fingerprint. EER, fractions, eight subfractions and isolated compound were submitted to a colorimetric test for cell viability assessment (IC50) using the MTT test. The results indicated that the EER, FH and FAE fractions presented cytotoxic activity against HeLa cells, with an IC50 of 5.0 μg mL-1, 2.8 μg mL-1 and 2.9 μg mL-1, respectively. Of the eight subfractions, four presented IC50, in the concentrations tested, and through the fingerprint it was possible to identify substances possibly responsible for the expressive biological results (Table 1). The isolated compound was not active against the cancer cell. According to the literature, hexane extract from K. coriacea root bark was cytotoxic to cells MDA-MB-435, HCT-8, HL-60, and SF-2954 and from it δ-tocotrienol was isolated, the same compound identified in subfraction FAE-2.4.3 in this research. Thus, this study made it possible to identify and correlate the secondary metabolites present in the K. coriacea roots with their promising cytotoxic activity, contributing to the chemical and biological knowledge of the species.

Table 1: IC50 values of the plant´s subfractions and compounds identified by LC-MS
Subfraction IC50 (µg mL-1) Identified compound
FAE-2.4.3* 3.5 quercetin-3-O-glucoside and δ-tocotrienol
FAE-4.4* 3.3 acylphoroglucinol
FAE-2.7.3* 2.7 4-hydroxy-2,3-methylenedioxixanthone and 3-hydroxy-1,2-dimethoxyxanthone
FH-10 0.9 lupeol, acylphoroglucinol and quercitrin
Legend: *subfraction from the ethyl acetate fraction; FH-10: subfraction from the hexane fraction

[1] Marinho, et al. Afroforest Syst, 88: 767-778, 2014.
[2] Coqueiro, et al. Journal of Natural Products, 79:470-476, 2016.
[3] Zagoto, et al. Journal of Ethnopharmacology, 105:47-54, 2006.
[4] De Mesquita, et al. Bioorganic & Medicinal Chemistry, 19:623-630, 2011.