Cytotoxicity of gypsogenic acid isolated from Gypsophila trichotoma

Abstract

Background:Gypsophila trichotoma Wend. (Caryophyllaceae) is a medicinal plant which is protected in Bulgaria by the Biodiversity Law. Previous studies have showed the presence of triterpene saponins, sterols, flavonoids, triterpens, etc.Objective:Gypsogenic acid, isolated from Gypsophila trichotoma roots, was evaluated for cytotoxic activity.Materials and Methods:The structure of the compound was elucidated by spectral methods. The cell survival fraction was determined by the MTT dye reduction assay, performed with some modifications.Results:Gypsogenic acid was tested in a panel of human tumor cell lines and was found to inhibit the proliferation of malignant cells. It was active against leukemic cells with lymphoid (SKW-3 and BV-173) or myeloid phenotype (HL-60, K-562, and LAMA-84), as well as against the EJ bladder carcinoma cell line. Bcr-Abl expressing myeloid cells (LAMA-84 and especially K-562) displayed lower sensitivity. HL-60/Dox cells were less sensitive to gypsogenic acid than the parent cell line, which shows that gypsogenic acid is probably a substrate of MRP-1.

Natural and Semisynthetic Pentacyclic Triterpenes for Chronic Myeloid Leukemia Therapy: Reality, Challenges and Perspectives

“…An interesting comparison might be made between the oleananes gypsogenin ( 5 ) and gypsogenic acid ( 6 ), whose only difference is the group on C‐4: an aldehyde and a carboxylic acid, respectively (Figure 2). Gypsogenin has presented a 24‐hour IC 50 of 12.67 μM against K562, [39] which contrasts greatly with the 72‐hour IC 50 values found for gypsogenic acid of 227.6 μM for K562 and 121.2 μM for LAMA‐84 cell [40] . This important difference in activity needs confirmation with additional studies using the same test conditions.…”

“…However, it is adequate to imagine that the group at C‐4 might play a decisive role for antileukemic activity. Furthermore, compared with cell lines of other types of leukemia, it has been shown that these Ph+ lines, K562 and LAMA‐84, have presented decreased sensitivity to gypsogenic acid [40] …”

Antitumor activity of the combination of artemisinin and epirubicin in human leukemia cells

“…A slightly modified version of MTT assay was performed to determine the cell survival fraction. 18 Exponentially growing HL-60 and HL-60/Dox cells were seeded into 96well plates. The cells were treated with the indicated drugs in 3-5 different concentrations, and the cell viability was determined after 72 hours of incubation, adding MTT (10 mg/ml).…”

Production of Δ7-Sterols from In Vitro Root Cultures of Endangered Gypsophila trichotoma

“…The population of the taxon has decreased as a result of the reduction of its distribution. G. trichotoma has been proved to have high anti-inflammatory, antiviral, antibacterial, antioxidant, and hepatoprotective properties [1]. Phytochemical examination revealed the presence of triterpene saponins, flavonoids, sterols, triterpenes and volatiles [2].…”