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

Abstract

Lyme disease (LD) is a tick-borne bacterial disease that is caused by Borrelia burgdorferi. Although acute LD is treated with antibiotics, it can develop into relapsing chronic form caused by latent forms of B. burgdorferi. This leads to the search for phytochemicals against resistant LD. Therefore, this study aimed to evaluate the activity of Dipsacus fullonum L. leaves extract (DE) and its fractions against stationary phase B. burgdorferi in vitro. DE showed high activity against stationary phase B. burgdorferi (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-Borrelia 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-Borrelia 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 D. fullonum L. leaves.

Phytochemical Screening and Antioxidant Activity of Selected Estonian Galium Species

“…Plants are a natural source of active compounds, phytochemicals, many of which with favourable bioactivity for humans. Analytical investigation allows for the determination of the phytochemical composition and confirmation of specific therapeutic properties of the plants already acknowledged for their potential by ethnomedicine [ 1 , 2 , 3 , 4 , 5 ]. The Galium L. genus, comprising about 667 species found worldwide, over a third of which can be found in Europe, includes several species that have been used in traditional medicine to alleviate a variety of ailments [ 6 , 7 ].…”

Dipsacus and Scabiosa Species—The Source of Specialized Metabolites with High Biological Relevance: A Review

“…Another species of Dipsacus is D. fullonum L., commonly known as teasel or wild teasel [33,34]. Traditionally, D. fullonum has been used to treat Lyme disease [35] and eye infections in cattle [36].…”

“…Some representatives of Dipsacus and Scabiosa biosynthesize chemical compounds of various classes, mainly triterpenoid derivatives (Table 2) [5][6][7]12,21,22,27,40,48,49,51,65,66,81,82,[88][89][90][91][92][93][94][95][96], which possess a variety of bioactivities. In addition, iridoids [6,7,13,22,27,33,34,65,66,75,78,84,89,[92][93][94][95][96][97][98][99][100] (Table 3), phenolic acids [6,24,27,29,…”

“…The presence of iridoid glycosides including loganin and loganic acid was widespread in the roots or leaves of Dipsacus spp. [6,22,27,33,34,65,66,89,92,93,[95][96][97]99] and flowers of S. atropurpurea subsp. maritima [7,84] (Table 3).…”

A Review on the Molecular Mechanisms of Action of Natural Products in Preventing Bone Diseases

“…In humans, the potential impacts of dietary proteins on the reduction of BDs was recently highlighted [ 23 ] and supported by two systematic reviews and meta-analyses studies conducted independently, which collectively reported that dietary protein intake improved femoral neck and total hip BMD, showed improvements on the lumbar spine, and significantly reduced cases of hip fractures [ 24 , 25 ]. In previous reviews, the pro-osteoanabolic and anti-osteocatabolic properties of extracts from different plant species were thoroughly discussed [ 26 , 27 , 28 , 29 ], motivating several new studies on the application of herbal materials in halting bone resorption in vitro and in vivo [ 30 , 31 , 32 , 33 , 34 , 35 , 36 ]. In this review, we aim to discuss the cellular and molecular mechanisms behind the health-promoting benefits of selected plant-derived and purely characterized NPs.…”