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

• Main Authors: Piret Saar-Reismaa (Author), Olga Bragina (Author), Maria Kuhtinskaja (Author), Indrek Reile (Author), Pille-Riin Laanet (Author), Maria Kulp (Author), Merike Vaher (Author)
• Format: Book
• Published: MDPI AG, 2022-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/ph15010087; 1424-8247
• Keywords: <i>Dipsacus fullonum</i> L.; <i>Borrelia burgdorferi</i>; antibacterial activity; bis-iridoids; sylvestrosides; cytotoxicity; Medicine; R; Pharmacy and materia medica; RS1-441
• Source: Pharmaceuticals, Vol 15, Iss 1, p 87 (2022)

Lyme disease (LD) is a tick-borne bacterial disease that is caused by <i>Borrelia burgdorferi</i>. Although acute LD is treated with antibiotics, it can develop into relapsing chronic form caused by latent forms of <i>B. burgdorferi</i>. This leads to the search for phytochemicals against resistant LD. Therefore, this study aimed to evaluate the activity of <i>Dipsacus fullonum</i> L. leaves extract (DE) and its fractions against stationary phase <i>B. burgdorferi</i> in vitro. DE showed high activity against stationary phase <i>B. burgdorferi</i> (residual viability 19.8 ± 4.7%); however, it exhibited a noticeable cytotoxicity on NIH cells (viability 20.2 ± 5.2%). The iridoid-glycoside fraction showed a remarkable anti-<i>Borrelia</i> effect and reduced cytotoxicity. The iridoid-glycoside fraction was, therefore, further purified and showed to contain two main bioactives-sylvestrosides III and IV, that showed a considerable anti-<i>Borrelia</i> activity being the least toxic to murine fibroblast NIH/3T3 cells. Moreover, the concentration of sylvestrosides was about 15% of DE, endorsing the feasibility of purification of the compounds from <i>D. fullonum</i> L. leaves.