Anticancer Effect of the Iridoid Glycoside Fraction from Dipsacus fullonum L. Leaves

Abstract

Species of Dipsacus have been widely used in folk medicine for their neuroprotective, antiosteoporotic, antioxidative, anticomplementary, and antibacterial activities. However, there has been but a limited amount of research on the anticancer effect of one of the most popular representatives of this genus, D. fullonum. Also, the cytotoxic activity has not yet been investigated of the constituents of D. fullonum leaves. The purpose of this study was to evaluate the cytotoxic activity of the bis-iridoid glycosides isolated from D. fullonum leaves against murine fibroblast NIH/3T3, mouse melanoma B16F10, HeLa human cervical cancer, human breast cancer MCF7 and MDB-MB-231 cells. The bis-iridoids, obtained by chromatographic fractionation of the extract of D. fullonum leaves, were characterized by thin-layer chromatography and high-performance liquid chromatography-mass spectrometry (HPLC-MS)/MS analysis. The cytotoxicity of the iridoid fraction was evaluated by WST-1 assay, and the number of dead cells was determined by the propidium iodide test. HPLC-MS/MS analysis showed the isolated bis-iridoid fraction to consist mainly of sylvestroside III and/or sylvestroside IV. This fraction was applied to cell cultures and kept for 48 and 72 hours. The results demonstrated that the iridoid glycosides had a differential ability to induce cell death in normal and cancer cells. The study confirmed that the bis-iridoids extracted from D. fullonum leaves had a selective cytotoxic effect on human breast cancer cell lines MCF7 and MDB-MD-231, while their cytotoxic effect on noncancer cells was low.

Extraction and Fractionation of Bioactives from Dipsacus fullonum L. Leaves and Evaluation of Their Anti-Borrelia Activity

“…Based on the WST-1 assay results, the cytotoxicity arose from polyphenols as the NP7 fraction had a viability of 54.7 ± 9.2%. These results correlate with those of our previous studies on iridoid fractions having a 63.3 ± 13.7% viability [18]. The detailed results of the statistical comparison test are given in Supplementary Materials File S1.…”

“…A similar fraction produced and tested previously by our group has shown activity against the selective cytotoxic effect on human breast cancer cell lines MCF7 and MDB-MD-231 [18]. Fraction NP5 contained mainly loganic acid, which also exhibited anti-Borrelia activity, similarly to iridoids from fraction NP2.…”

“…It has also been demonstrated that the composition of the leaves significantly differs from that of the root [16], demonstrating good antioxidant and antimicrobial activities [16,17]. Moreover, our research group's investigations have established the in vivo effectiveness of teasel leaves extracts against several cancer strains [18]. The current study aimed to continue our research group's earlier investigations on D. fullonum L. leaves [18,19] by elucidating, fractionating, identifying and quantifying the content of D. fullonum L. bioactives (iridoids and polyphenolics) to evaluate their anti-Borrelia activity against stationary phase Borrelia burgdorferi.…”

“…Moreover, our research group's investigations have established the in vivo effectiveness of teasel leaves extracts against several cancer strains [18]. The current study aimed to continue our research group's earlier investigations on D. fullonum L. leaves [18,19] by elucidating, fractionating, identifying and quantifying the content of D. fullonum L. bioactives (iridoids and polyphenolics) to evaluate their anti-Borrelia activity against stationary phase Borrelia burgdorferi. Additionally, the composition of the more promising fractions was identified and quantified together with their antioxidative capacity, anti-Borrelia activity and cytotoxicity evaluated.…”

Phytochemical Screening and Antioxidant Activity of Selected Estonian Galium Species

“…Studies of medicinal plants have demonstrated that the health-promoting properties and therapeutically beneficial qualities can often be attributed to specific polyphenols or iridoids, two of the most prevalent groups of bioactives in many plant extracts, and in the representatives of the Galium genus [ 9 , 11 , 16 , 17 ]. Polyphenols are the most abundant secondary metabolites in plants, notably characterised by their potent antioxidant properties [ 18 ].…”