Euplotin C is a sesquiterpene of marine origin endowed with significant anti-microbial and anti-tumor properties. Despite the promising functional profile, its progress as a novel drug candidate has failed so far, due to its scarce solubility and poor stability in aqueous media, such as biological fluids. Therefore, overcoming these limits is an intriguing challenge for the scientific community. In this work, we synthesized β-cyclodextrin-based nanosponges and investigated their use as colloidal carriers for stably complex euplotin C. Results obtained proved the ability of the carrier to include the natural compound, showing remarkable values of both loading efficiency and capacity. Moreover, it also allowed us to preserve the chemical structure of the loaded compound, which was recovered unaltered once extracted from the complex. Therefore, the use of β-cyclodextrin-based nanosponges represents a viable option to vehiculate euplotin C, thus opening up its possible use as pharmacologically active compound.
Modern society is reviving the practice of aromatherapy, and lavender is reported to be the most worldwide purchased plant for essential oils (EO) extraction. Since odors can modulate cognitive functions acting through specific neuroanatomical pathways, lavender EO inhalation can enhance cognition. Taking into account EO quality and diffusion devices, we conducted a systematic review on the effects of lavender EO inhalation on arousal, attention and memory in healthy subjects. Starting from this new multidisciplinary perspective, cognitive effects were revised to link outcomes to effective and reproducible aromatherapy protocols. A systematic search on MEDLINE database using Cognitive Atlas and plant authenticity-related keywords was performed. Among the 806 articles yielded, 11 articles met eligibility criteria. Subjects administered with lavender EO displayed arousal decrease and sustained attention increase. Puzzling results were obtained regarding memory. Lack of EO quality assessment and high heterogeneity in inhalation protocols did not allow assessing whether different EO composition differently modulates cognition and whether placebo or expectancy effect can be discerned from EO effect itself. However, GABAergic pathway modulation exerted by linalool, a major lavender EO constituent, explains arousal reduction and sustained attention enhancement. In conclusion, aromatherapy can be an innovative, practical and non-invasive tool to prevent cognitive lapses.
Developing fit-to-purpose analytical screening methods for plant marker constituents by simple and affordable techniques represents a constant and important request from the current transformation chain of plant products. In this work, methods developed on classical thin-layer chromatography (TLC) and overpressured layer chromatography (OPLC) have been applied on some of the most valuable commercial plant products, such as star anise (Illicium verum Hook. f.) essential oil and extracts, common thyme (Thymus vulgaris L.) and sweet fennel (Foeniculum vulgare Mill.) essential oils and acerola fruit (Malpighia punicifolia L.) hydroalcoholic extracts, to evaluate OPLC potentiality in comparison with TLC performances in the detection of some characteristic constituents. OPLC provided higher performance with respect to TLC in all experiments performed due to higher selectivity demonstrated on all the tested marker compounds except for flavonoids in acerola extracts. Considering the usage of planar chromatography in the quality control of plant derivatives, the present paper shows how the OPLC protocols were both highly time- and solvent-saving in comparison with classical TLC.
Modern society is reviving the practice of aromatherapy, and lavender is reported being the most worldwide purchased plant for essential oil (EO) extraction. Since recent studies reported cognitive enhancing effects of lavender besides the hypno-inducing effects, a literature review is needed. Considering EO quality and diffusion devices, we conducted a systematic review on the effects of lavender EO inhalation on arousal, attention and memory in healthy subjects. Starting from this new multidisciplinary perspective, cognitive effects were reviewed to link outcomes to effective and reproducible protocols. A systematic search on MEDLINE, ERIC, PsycInfo, Google Scholar, and Scopus databases using Cognitive Atlas and plant-related keywords was conducted. Among the 1,203 articles yielded, 11 met eligibility criteria. Subjects administered with lavender EO displayed arousal decrease and sustained attention increase. Controversial results emerged regarding memory. Lack of EO quality assessment and protocols heterogeneity did not allow assessing whether different EO composition differentially modulates cognition and whether placebo effect can be discerned from EO effect itself. However, GABAergic pathway modulation exerted by linalool, a major lavender EO constituent, might explain cognitive functions empowerment. We speculate aromatherapy could be a burgeoning cognition enhancing tool, although further investigation is required to reach robust conclusions.
Among natural chemicals used as cancer chemo-preventive and/or chemotherapeutic agents, saponins represent one of the most promising and interesting family of compounds. In this work, we aimed to elucidate the biological effects on human cells of six saponin fractions (SFs) obtained from in vitro cultures of Astragalus verrucosus Moris, a poorly characterized species. Interestingly, SF (3) showed a strongly inhibitory effect on the proliferation of human colon adenocarcinoma cell line (HCT116) via activation of a p53-dependent apoptotic pathway. In addition, SF (3) and the other SFs did not display genotoxic activity in human peripheral lymphocytes.
Hypericum perforatum L. (Guttiferae) (St. John’s wort) is a well-known traditional medicinal plant that has been used for centuries for the treatment of several diseases, such as skin lesions, eczema, burns and microbial, inflammatory and psychological disorders [1,2]. The crude extract of H. perforatum is now widely used in Europe as a drug for the treatment of depression [3]. Proven photodynamic, antiviral, antiretroviral, and antitumoral activities of Hypericum extracts also suggests using of this plant in Acquired Immune Deficiency Syndrome (AIDS) and cancer treatments [4].
Among natural chemicals used as cancer chemo-preventive and/or chemotherapeutic agents, saponins represent one of the most promising and interesting family of compounds. In this work, we aimed to elucidate the biological effects on human cells of six saponin fractions (SFs) obtained from in vitro cultures of Astragalus verrucosus Moris, a poorly characterized species. Interestingly, SF ( 3 ) showed a strongly inhibitory effect on the proliferation of human colon adenocarcinoma cell line (HCT116) via activation of a p53-dependent apoptotic pathway. In addition, SF ( 3 ) and the other SFs did not display genotoxic activity in human peripheral lymphocytes.
The genus Hypericum (Guttiferae) is one of the most representative species in temperate zones and Turkey is one of the most important Mediterranean sites. Due to the increasing commercial value of Hyperici herba (Hypericum perforatum), many wild Turkish Hypericum species have received currently a considerable renewed interest as potential substitutes of the well-established H. perforatum crops for their similar content in the standardization bioactives (hypericins, hyperforins, and flavonoids). The present paper reported the volatile fingerprints of three selected wild Turkish Hypericum species recently characterized as H. perforatum bioactive-like profiles but lacking of the requested well-established usage in the EU market. In this context, the volatile constituents of the three-selected Hypericum spp. were investigated as additional discriminating markers to enhance the likelihood that this adulterating plant raw material will be detected before it is incorporated into finished H. perforatum products.
Glioblastoma multiforme (GBM) is an aggressive brain tumour with high resistance to radio- and chemotherapy. As such, increasing attention has focused on developing new therapeutic strategies to improve treatment responses. Recently, attention has been shifted to natural compounds that are able to halt tumour development. Among them, carnosol (CAR), a phenolic diterpene present in rosemary, has become a promising molecule that is able to prevent certain types of solid cancer. However, no data are available on the effects of CAR in GBM. Here, CAR activity decreased the proliferation of different human glioblastoma cell lines, particularly cells that express wild type p53. The p53 pathway is involved in the control of apoptosis and is often impaired in GBM. Notably, CAR, through the dissociation of p53 from its endogenous inhibitor MDM2, was able to increase the intracellular p53 levels in GBM cells. Accordingly, functional reactivation of p53 was demonstrated by the stimulation of p53 target genes’ transcription, the induction of apoptosis and cell cycle blockade. Most importantly, CAR produced synergistic effects with temozolomide (TMZ) and reduced the restoration of the tumour cells’ proliferation after drug removal. Thus, for the first time, these data highlighted the potential use of the diterpene in the sensitization of GBM cells to chemotherapy through a direct re-activation of p53 pathway. Furthermore, progress has been made in delineating the biochemical mechanisms underlying the pro-apoptotic effects of this molecule.
Salvia wagneriana Polak is a tropical species native to Central America, well adapted to grow in the Mediterranean basin for garden decoration. Micropropagation has been assessed from axillary shoots of adult plants using a Murashige and Skoog basal medium, with the addition of 1.33-μM 6-benzylaminopurine for shoot proliferation; the subsequent rooting phase occurred in plant growth regulator-free medium. The plants were successfully acclimatised with high survival frequency. Hairy roots were induced after co-cultivation of leaf lamina and petiole fragments with Agrobacterium rhizogenes and confirmed by PCR. The establishment and proliferation of the selected HRD3 line were obtained in hormone-free liquid medium and the production of rosmarinic acid (RA) was evaluated after elicitation. The analysis of RA was performed by LC-ESI-DAD-MS in the hydroalcoholic extracts. The addition of casein hydrolysate increased the RA production, whereas no enrichment was observed after the elicitation with jasmonic acid.
The aroma fingerprints of seven endemic Sardinian populations of Genista species (Genista bocchierii, Genista arbusensis, Genista cadasonensis, Genista corsica, Genista morisii, Genista pichisermolliana, Genista sulcitana) were defined for the first time in order to investigate the relationship between their chemotaxonomic classification and discriminating volatiles. It is the first time that the inter-species compositional variations of non-terpenoidic constituents and target volatiles such as linalool, limonene, 2,6-nonadienal, 2-pentylfuran, (E)-2-(2-pentenyl)-furan, ß-caryophyllene and caryophyllene oxide were related by Principal Components Analysis to the actual chemotaxonomic classification of the selected Sardinian Genista species. Although they are not considered marketable aromatic plants, these original results have shown the potential role of volatiles not only as new further important chemotaxonomic markers of Genista species, but also as potential ecological factors in the chemodiversity of some endemic Mediterranean Genista or, more in general, in vegetation changes and reforestation processes.
Turkish Hypericum origanifolium Willd has been recently considered for its hypericin and phenolic content as a potential substitute of the well-established EU market position Hypericum perforatum. However, a complete phytochemical characterization of H. origanifolium has not carried out yet in order to assert its potential industrial value. The present paper represents the first attempt to define the aromatic fingerprint of a representative wild Turkish H. origanifolium Willd. population. In addition, its volatiles were studied as potential discriminating constituents between H. perforatum and H. origanifolium with a similar hypericin and phenolic composition.
Exposure to stressful environmental conditions can induce severe metabolic variations in basil (Ocimum basilicum) aroma. The aromatic profiles of Dark Opal and Red Rubim varieties (in vivo plants, in vitro shoots, callus, and suspension cultures) were investigated for the first time. The established calli represented the most interesting miniaturised aromatic plant systems, as they were able to emit many typical basil volatiles with very low amounts of phenylpropanoids (1–2%). The hydrocarbon monoterpenes and oxygenated volatiles emitted from calli of both varieties were greatly and conversely affected by UV-C and UV-B, in comparison with the non-irradiated samples. As calli of both varieties still maintained very low levels of phenylpropanoids even after UV elicitation, they might be regarded not only as efficient in vitro plant models to study volatile compounds under UV stress conditions, but also as safe aromatic biomass in comparison with in vivo basil plants.
The volatile constituents of the rare species of Hypericum, namely Hypericum pruinatum (as one population) and Hypericum aviculariifolium subp. depilatum var. depilatum (endemic, as two populations namely 'Gümüş' and 'Yeniköy') growing wild in the mountainous parts of Northern Turkey were studied for the first time. The essential oils (EOs) were extracted by hydrodistillation of the air-dried aerial parts and analysed by GC-FID and GC-MS. A total of 56, 49 and 50 EO components representing 98.2%, 96.9% and 99.4% of the total composition were identified respectively from one population for H. pruinatum and two populations for Hypericum aviculariifolium subp. depilatum var. depilatum. GC-MS profiles showed significant compositional variations not only between the two Turkish species, but also between the two populations of the same species highlighting the importance of genetic factors affecting secondary metabolite profile.
A series of new room temperature ionic liquids based on N-alkyl-N-methylmorpholinium cations (the alkyl chain ranging from ethyl to nonyl) and a hydrophilic anion (dicyanamide), a mostly unexplored class of room temperature ionic liquids (RTILs), has been synthesized and characterized. Selected physico-chemical properties (density, viscosity and ionic conductivity) have been measured and the salts' propensity to organize into ionic clusters has been explored. The inspection of their Walden plots and electrospray ionization spectra strongly prompts for the occurrence of clustering phenomena, especially for salts bearing long alkyl chains. This structural organization has been confirmed using X-ray scattering techniques and the existence of a high degree of intermediate range order has been detected, as fingerprinted by distinct diffraction features at low Q. These evidences are rationalized in terms of a structural model where, similarly to other RTILs, the alkyl chains tend to segregate from the charged moieties.
Curcuma longa L. (turmeric) is one of the most important spice and safe food additives. Its main constituents, curcuminoids, showed anti-inflammatory, antitumor and antioxidant effects. In the present work, an in vitro propagation method was developed to achieve selected plant organs with quantified curcuminoid content. In vitro plants were obtained from sprouting buds as primary explants. The major curcuminoid constituents, such as curcumin (CUR), demethoxycurcumin (DEM), and bis-demethoxycurcumin (bis-DEM) were examined in different organs by LC-DAD-ESI-MS. A significant production of curcumin (more than 260 microg g(-1) fresh weight) was obtained from in vitro microrhizomes, especially grown in a Murashige and Skoog medium (MS) supplemented with kinetin (0.1 mg L((-1)), alpha-naphthaleneacetic acid (NAA, 1 mg L(-1)), sucrose (6%), agar (5%) and activated charcoal (0.1%). The analyzed microrhizomes showed reduced amounts of DEM and bis-DEM in comparison with CUR levels. In addition a shoot culture line was suitable to biosynthesize curcuminoids, in a ratio very similar to that identified in the fresh rhizomes of parent plants. This study represents the first direct quantification of curcuminoids in turmeric in vitro shoots and microrhizomes to be used in dietary supplements.
The essential oils (EOs) and static headspaces (HSs) of in vitro plantlets and callus of Mentha x piperita were characterized by GC-MS analysis. Leaves were used as explants to induce in vitro plant material. The EO yields of the in vitro biomass were much lower (0.1% v/w) than those of the parent plants (2% v/w). Many typical mint volatiles were emitted by the in vitro production, but the callus and in vitro plantelet EOs were characterized by the lack of both pulegone and menthofuran. This was an important difference between in vitro and in vivo plant material as huge amounts of pulegone and menthofuran may jeopardise the safety of mint essential oil. Regarding the other characteristic volatiles, menthone was present in reduced amounts (2%) in the in vitro plantlets and was not detected in the callus, even if it represented the main constituent of the stem and leaf EOs obtained from the cultivated mint (26% leaves; 33% stems). The M. piperita callus was characterized by menthol (9%) and menthone (2%), while the in vitro plantlet EO showed lower amounts of both these compounds in favour of piperitenone oxide (45%). Therefore, the established callus and in vitro plantlets showed peculiar aromatic profiles characterized by the lack of pulegone and menthofuran which have to be monitored in the mint oil for their toxicity.