Verbascoside, synthetic derivatives and other glycosides from Argentinian native plant species as potential antitumoral agents

Abstract

A phytochemical study was performed on three native plant species from the central-western zone of Argentina: Buddleja cordobensis Grisebach, Baccharis salicina Torr. & A. Gray and Nepeta cataria L. We could obtain verbascoside (1) from B. cordobensis. From N. cataria we could obtain 1, 5, 9-epi-deoxyloganic acid (2) L. Finally, we could isolate 2--(L-rhamnopyranosyl)-3-angeloyloxy-15-acetyloxy-7,13( 14)-E-dienent-labdane (3) and 2--(L-rhamnopyranosyl)-3--angeloyloxy-15-hydroxy-7,13( 14)-E-dien-ent-labdane (4) from B. salicina. Moreover, three derivatives from 1, and one semi-synthetic derivative from 2, were prepared. PCR reaction was used to analyse the activity against DNA polymerase, and cell culture to determine cytotoxicity and antitumoral activity. Verbascoside (1) was strongly active in the nanomolar scale (IC 50 = 356 nM) against DNA polymerization. Moreover, verbascoside was also strongly active in the nanomolar scale against human melanoma cell line (IC 50 = 256 nM) and human colorectal cell line (IC 50 = 320 nM). Furthermore, derivatives 6 and 7 were cytotoxic against both cancer cell lines.

Synthesis of Structurally Related Coumarin Derivatives as Antiproliferative Agents

“…The HEK 293 cell line was used as non-tumoral control. All cells were incubated at 37 °C in a 5% CO 2 atmosphere and cultured in DMEM media supplemented with 10% fetal bovine serum (FBS), penicillin (10 μg/mL), and streptomycin (100 μg/mL) …”

“…All cells were incubated at 37 °C in a 5% CO 2 atmosphere and cultured in DMEM media supplemented with 10% fetal bovine serum (FBS), penicillin (10 μg/mL), and streptomycin (100 μg/mL). 28 4.3.2. Tumoral Cell Proliferation.…”

The Anti-Tumor Efficacy of Verbascoside on Ovarian Cancer via Facilitating CCN1-AKT/NF-κB Pathway-Mediated M1 Macrophage Polarization

“…VB has recently received considerable attention owing to its significant clinical value, including antioxidative, antiinflammatory, antibacterial, and antifungal properties (8)(9)(10)(11)(12). Moreover, VB also possesses anti-tumour activity against various cancers, such as glioblastoma, prostate cancer, and breast cancer (13)(14)(15)(16)(17). For example, VB has an anti-tumour role in breast cancer by suppressing cell proliferation (16).…”

Formulation of a Phenol-Rich Extract from Unripe Olives (Olea europaea L.) in Microemulsion to Improve Its Solubility and Intestinal Permeability

“…Oleuropein showed potential antioxidant, anti-inflammatory, anti-atherogenic, anti-cancer, anti-viral, anti-aging, and neuroprotective properties [ 10 , 15 , 16 , 17 ]. Verbascoside, also known as acteoside or kusaginin [ 18 ], is a bio-active molecule well-known for its antioxidant, anti-inflammatory, antibacterial, antifungal, potential anticancer, and anti-tuberculosis properties [ 18 , 19 , 20 , 21 , 22 , 23 ]. In a recent study, ligstroside showed beneficial effects against Alzheimer’s disease and the capability in expanding the lifespan and enhancing the cognitive function of aged mice in vivo [ 24 ].…”