2015Journal of Applied Pharmaceutical ScienceOpen access

Cytotoxic Triterpenes and Sterols from Pipturus arborescens (Link) C.B. Rob.

Mariquit M. M. De Los Reyes, Glenn G. Oyong, Virgilio Jr., Vincent Ng, Chien‐Chang Shen, Consolacion Y. Ragasa

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Abstract

The triterpenes, squalene (1), friedelin (2) and a mixture of ursolic acid (3a) and oleanolic acid (3b) in a 2:3 ratio, and a mixture of β-sitosterol (4a) and stigmasterol (4b) in a 2:1 ratio, obtained from the dichloromethane extract of Pipturus arborescens (Link) C.B. Rob., were evaluated for their anti-proliferative activities against three human cancer cell lines, breast (MCF-7) and colon (HT-29 and HCT-116), and a normal cell line, human dermal fibroblast-neonatal (HDFn) using the in vitro PrestoBlue ® cell viability assay.The HCT-116 cell line was most susceptible to the compounds and mixtures tested.Triterpene 1 was most cytotoxic against HCT-116 and MCF-7 with IC50 values of 4.21 and 5.92 μg/mL, respectively.Triterpene 2 and the mixture of 3a and 3b were highly anti-proliferative against HCT-116 cells (IC50 of 1.22 and 1.66 μg/mL, respectively) and moderately inhibitory against MCF-7 cells (IC50 of 16.51 and 23.97 μg/mL, respectively).The mixture of 4a and 4b exhibited high cytotoxicity against HCT-116 cells (IC50 of 1.14 μg/mL).Compounds 1-4b showed the least activity against HT-29 cells (IC50 of 11.97 to 52.52 μg/mL).Cytotoxic effect was not observed against HDFn cells (>100 μg/mL).Comparing the effects of 1-4b on the two colon cancer cell lines, the IC50 values of 1-4b against HCT-116 were lower than those of HT-29.

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The triterpenes, squalene (1), friedelin (2) and a mixture of ursolic acid (3a) and oleanolic acid (3b) in a 2:3 ratio, and a mixture of β-sitosterol (4a) and stigmasterol (4b) in a 2:1 ratio, obtained from the dichloromethane extract of Pipturus arborescens (Link) C.B. Rob., were evaluated for their anti-proliferative activities against three human cancer cell lines, breast (MCF-7) and colon (HT-29 and HCT-116), and a normal cell line, human dermal fibroblast-neonatal (HDFn) using the in vitro PrestoBlue ® cell viability assay.The HCT-116 cell line was most susceptible to the compounds and mixtures tested.Triterpene 1 was most cytotoxic against HCT-116 and MCF-7 with IC50 values of 4.21 and 5.92 μg/mL, respectively.Triterpene 2 and the mixture of 3a and 3b were highly anti-proliferative against HCT-116 cells (IC50 of 1.22 and 1.66 μg/mL, respectively) and moderately inhibitory against MCF-7 cells (IC50 of 16.51 and 23.97 μg/mL, respectively).The mixture of 4a and 4b exhibited high cytotoxicity against HCT-116 cells (IC50 of 1.14 μg/mL).Compounds 1-4b showed the least activity against HT-29 cells (IC50 of 11.97 to 52.52 μg/mL).Cytotoxic effect was not observed against HDFn cells (>100 μg/mL).Comparing the effects of 1-4b on the two colon cancer cell lines, the IC50 values of 1-4b against HCT-116 were lower than those of HT-29.

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Available abstract

The triterpenes, squalene (1), friedelin (2) and a mixture of ursolic acid (3a) and oleanolic acid (3b) in a 2:3 ratio, and a mixture of β-sitosterol (4a) and stigmasterol (4b) in a 2:1 ratio, obtained from the dichloromethane extract of Pipturus arborescens (Link) C.B. Rob., were evaluated for their anti-proliferative activities against three human cancer cell lines, breast (MCF-7) and colon (HT-29 and HCT-116), and a normal cell line, human dermal fibroblast-neonatal (HDFn) using the in vitro PrestoBlue ® cell viability assay.The HCT-116 cell line was most susceptible to the compounds and mixtures tested.Triterpene 1 was most cytotoxic against HCT-116 and MCF-7 with IC50 values of 4.21 and 5.92 μg/mL, respectively.Triterpene 2 and the mixture of 3a and 3b were highly anti-proliferative against HCT-116 cells (IC50 of 1.22 and 1.66 μg/mL, respectively) and moderately inhibitory against MCF-7 cells (IC50 of 16.51 and 23.97 μg/mL, respectively).The mixture of 4a and 4b exhibited high cytotoxicity against HCT-116 cells (IC50 of 1.14 μg/mL).Compounds 1-4b showed the least activity against HT-29 cells (IC50 of 11.97 to 52.52 μg/mL).Cytotoxic effect was not observed against HDFn cells (>100 μg/mL).Comparing the effects of 1-4b on the two colon cancer cell lines, the IC50 values of 1-4b against HCT-116 were lower than those of HT-29.

Key concepts: Terpene, Gentianaceae, Traditional medicine, Chemistry, Stereochemistry, Biology, Botany, Medicine

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