Papers by Antonio Vassallo
Pharmaceutics
Many substances in plant extracts are known for their biological activities. These substances act... more Many substances in plant extracts are known for their biological activities. These substances act in different ways, exerting overall protective effects against many diseases, especially skin disorders. However, plant extracts’ health benefits are often limited by low bioavailability. To overcome these limitations, drug delivery systems can be employed. In this study, we evaluated the antioxidant power of an ethanolic extract from Myrtus communis L. (myrtle) berries through colorimetric tests (DPPH and FRAP). The antioxidant activity was also verified by using fibroblast cell culture through cellular Reactive Oxygen Species (ROS) levels measurements. Moreover, the myrtle extract was formulated in phospholipid vesicles to improve its bioavailability and applicability. Myrtle liposomes were characterized by size, surface charge, storage stability, and entrapment efficiency; visualized by using cryo-TEM images; and assayed for cytocompatibility and anti-ROS activity. Our results sugges...
Antioxidants
Antioxidant compounds with health benefits can be found in food processing residues, such as grap... more Antioxidant compounds with health benefits can be found in food processing residues, such as grape pomace. In this study, antioxidants were identified and quantified in an extract obtained from Graciano red grape pomace via a green process. The antioxidant activity of the extract was assessed by the DPPH and FRAP tests, and the phenolic content by the Folin–Ciocalteu test. Furthermore, nanotechnologies were employed to produce a safe and effective formulation that would exploit the antioxidant potential of the extract for skin applications. Anthocyanins, flavan-3-ols and flavanols were the main constituents of the grape pomace extract. Phospholipid vesicles, namely liposomes, were prepared and characterized. Cryo-TEM images showed that the extract-loaded liposomes were predominantly spherical/elongated, small, unilamellar vesicles. Light scattering results revealed that the liposomes were small (~100 nm), homogeneously dispersed, and stable during storage. The non-toxicity of the li...
Pharmaceutics
Food extract’s biological effect and its improvement using nanotechnologies is one of the challen... more Food extract’s biological effect and its improvement using nanotechnologies is one of the challenges of the last and the future decades; for this reason, the antioxidant effect of scarlet eggplant extract liposomal incorporation was investigated. Scarlet eggplant (Solanum aethiopicum L.) is a member of the Solanaceae family, and it is one of the most consumed vegetables in tropical Africa and south of Italy. This study investigated the antioxidant activity and the phytochemical composition of S. aethiopicum grown in the Basilicata Region for the first time. The whole fruit, peel, and pulp were subjected to ethanolic exhaustive maceration extraction, and all extracts were investigated. The HPLC-DAD analysis revealed the presence of ten phenolic compounds, including hydroxycinnamic acids, flavanones, flavanols, and four carotenoids (one xanthophyll and three carotenes). The peel extract was the most promising, active, and the richest in specialized metabolites; hence, it was tested on...
Among all the plant species examined, together with the food products that derive from it, coffee... more Among all the plant species examined, together with the food products that derive from it, coffee has a reputation that over the course of history has had a rather controversial evolution: some episodes are emblematic of the mistrust that, in the first decades of its diffusion in Europe and in the World, accompanied the drink. Coffee is obtained by infusing the powder obtained by grinding the toasted seeds of some species of tropical shrubs belonging to the genus Coffea, practiced through various techniques; although there are over 100 species, those used for food consumption are very few, and almost all of the market is aimed at only two of them: Coffea arabica and Coffea canephora, better known commercially (but improperly) with the name of Robusta. Today it can be said that the antioxidant activity of coffee, intended both as a vegetable and as a drink, has been known for some time and has been evaluated through different methods; various studies have shown that the high content of polyphenols in coffee plays an important role in its strong antioxidant action. Since 1997, the year in which the first works on this activity were presented, the concern about the potential risks related to coffee intake has rapidly diminished and a line of research has originated aimed at evaluating its therapeutic effects, especially chemopreventive, antidiabetic and anticarginogenic effects. It was immediately proposed that, at the head of the wide family of active polyphenolic compounds, there were chlorogenic acids, whose remarkable ability to prevent oxidative cell damage was immediately determined.
Nanomaterials, 2020
Hydroxycitrate (HCA), a main organic acid component of the fruit rind of Garcinia cambogia, is a ... more Hydroxycitrate (HCA), a main organic acid component of the fruit rind of Garcinia cambogia, is a natural citrate analog that can inhibit the ATP citrate lyase (ACLY) enzyme with a consequent reduction of inflammatory mediators (i.e., nitric oxide (NO), reactive oxygen species (ROS), and prostaglandin E2 (PGE2)) levels. Therefore, HCA has been proposed as a novel means to prevent, treat, and ameliorate conditions involving inflammation. However, HCA presents a low membrane permeability, and a large quantity is required to have a biological effect. To overcome this problem, HCA was formulated in liposomes in this work, and the enhancement of HCA cell availability along with the reduction in the amount required to downregulate NO, ROS, and PGE2 in macrophages were assessed. The liposomes were small in size (~60 nm), monodispersed, negatively charged (−50 mV), and stable on storage. The in vitro results showed that the liposomal encapsulation increased by approximately 4 times the intra...
The present study was designed to characterize the phenolic compounds of Thymus serpyllum L. and ... more The present study was designed to characterize the phenolic compounds of Thymus serpyllum L. and Hypericum perforatum L. The extraction process was carried out through the use of a Kumagawa extractor. The solvents (hexane, diethyl ether, acetate ethyl and methanol) were chosen in order of increasing polarity. The methanol soluble fractions were analyzed by liquid chromatography–mass spectrometry (LC-MS). High performance liquid chromatography/electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS) method was used for the phenolic compounds analysis. 14 phenolic compounds were identified in the Thymus serpyllum L., five of which were phenolic acids, nine flavan-3ols. Moreover, this methodology allowed the separation of up to 14 constituents in methanolic Hypericum perforatum L. extract, covering various classes of plant secondary metabolites, namely hydroxycinnamic acids, flavanols including flavonol glycosides and flavonol aglyca, biflavone and a naphthodianthrone.
Cosmetics, 2021
In recent years, there has been considerable interest in using microalgal lipids in the food, che... more In recent years, there has been considerable interest in using microalgal lipids in the food, chemical, pharmaceutical, and cosmetic industries. Several microalgal species can accumulate appreciable lipid quantities and therefore are characterized as oleaginous. In cosmetic formulations, lipids and their derivatives are one of the main ingredients. Different lipid classes are great moisturizing, emollient, and softening agents, work as surfactants and emulsifiers, give consistence to products, are color and fragrance carriers, act as preservatives to maintain products integrity, and can be part of the molecules delivery system. In the past, chemicals have been widely used but today’s market and customers’ demands are oriented towards natural products. Microalgae are an extraordinary source of lipids and other many bioactive molecules. Scientists’ attention to microalgae cultivation for their industrial application is increasing. For the high costs associated, commercialization of mi...
Antioxidants, 2021
The peppers of the Capsicum species are exploited in many fields, as flavoring agents in food ind... more The peppers of the Capsicum species are exploited in many fields, as flavoring agents in food industry, or as decorative and therapeutic plants. Peppers show a diversified phytochemical content responsible for different biological activities. Synergic activity exerted by high levels of antioxidant compounds is responsible for their important anti-inflammatory property. A methanolic extract was obtained from a new pepper genotype and tested for anti-inflammatory activity. The extract was incorporated into phospholipid vesicles to increase the bioavailability of its bioactive components. Two types of phospholipid vesicles were produced, conventional liposomes and Penetration Enhancer containing Vesicles (PEVs). They were tested in human monoblastic leukemia U937 cell line, showing no cytotoxic effect. The intracellular reactive oxygen species (ROS) and nitric oxide (NO) levels were measured to value the in vitro efficacy of the vesicles in regulating inflammatory responses. Liposomal ...
Antioxidants, 2020
Overproduction of oxidants in the human body is responsible for oxidative stress, which is associ... more Overproduction of oxidants in the human body is responsible for oxidative stress, which is associated with several diseases. High intake of vegetables and fruits can reduce the risk of chronic diseases, as they are sources of bioactive compounds capable of contrasting the free radical effects involved in cancer, obesity, diabetes, and neurodegenerative and cardiovascular diseases. Capsicum annuum L. cv Senise is a sweet pepper that is grown in the Basilicata region (Italy). It is an important source of polyphenols, carotenoids, and capsinoids and can play a key role in human health. In this study, an ethanol extract was obtained from C. annuum dried peppers and the analysis of the phytochemical composition was performed by LC-ESI/LTQ Orbitrap/MS. The extract was incorporated into liposomes, which showed small size (~80 nm), good homogeneity, negative surface charge, and good stability in storage. The biological activity of the extract was evaluated in the human hepatoma (HepG2) cell...
Evidence-Based Complementary and Alternative Medicine, 2020
The prevalence of nosocomial infections due to multidrug resistant (MDR) bacterial strains is ass... more The prevalence of nosocomial infections due to multidrug resistant (MDR) bacterial strains is associated with high morbidity and mortality. Folk medicine and ethnopharmacological data can provide a broad range of plants with promising antimicrobial activity. Triphala, an Ayurvedic formula composed of three different plants: Terminalia chebula Retz., Terminalia bellirica (Gaertn.) Roxb. (Combretaceae), and Phyllanthus emblica L. (Phyllanthaceae), is used widely for various microbial infections. Various extraction techniques were applied in the extraction of the biologically active constituents of Triphala in order to compare their efficiency. Microwave-assisted extraction (MAE) was shown to be the most efficient method based on yield, extraction time, and selectivity. The Triphala hydroalcoholic extract (TAE) has been chemically characterized with spectroscopic and chromatographic techniques. Triphala hydroalcoholic extract was evaluated alone or with carvacrol. Different drug formul...
Pharmaceutics, 2020
The purpose of this study was to improve the knowledge on Hura crepitans L., a plant belonging to... more The purpose of this study was to improve the knowledge on Hura crepitans L., a plant belonging to the Euphorbiaceae family that, on the one hand, is known to be toxic, but on the other, is a source of polyphenols with health-promoting effects. Different green extraction methods were applied, varying solvent, temperature, and duration of extraction, which can influence the phytochemical profile and biological activity of plant extracts, and the extracts were fully characterized. Aqueous extracts exhibited a superior antioxidant activity, as indicated by different spectrophotometric tests, and were cytoprotective to HepG2 cells used as model cells. Liquid chromatography–mass spectrometry analyses were performed to identify the secondary metabolites involved in these effects and demonstrated that solvent, duration, and temperature indeed influenced the extraction of polyphenols. Furthermore, the most promising extract, in terms of antioxidant potential, was incorporated into liposomes ...
Molecules, 2020
Acute myeloid leukemia (AML) is among the top four malignancies in Saudi nationals, and it is the... more Acute myeloid leukemia (AML) is among the top four malignancies in Saudi nationals, and it is the top leukemia subtype worldwide. Resistance to available AML drugs requires the identification of new targets and agents. Hsp90 is one of the emerging important targets in AML, which has a central role in the regulation of apoptosis and cell proliferation through client proteins including the growth factor receptors and cyclin dependent kinases. The objective of the first part of this study is to investigate the putative Hsp90 inhibition activity of three novel previously synthesized quinazolines, which showed HL60 cytotoxicity and VEGFR2 and EGFR kinases inhibition activities. Using surface plasmon resonance, compound 1 (HAA2020) showed better Hsp90 inhibition compared to 17-AAG, and a docking study revealed that it fits nicely into the ATPase site. The objective of the second part is to maximize the anti-leukemic activity of HAA2020, which was combined with each of the eleven standard ...
Molecules, 2020
Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease characterized by the produ... more Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease characterized by the production of inflammatory factors. In order to overcome the side effects of currently used anti-inflammatory drugs, several attempts have been made to identify natural products capable of relieving RA symptoms. In this work, a herbal preparation consisting of propolis, pomegranate peel, and Aglianico grape pomace (PPP) extracts (4:1:1) was designed and evaluated for its effect on a murine collagen-induced arthritis (CIA) model. Firstly, the chemical contents of four different Italian propolis collected in the Campania region (Italy) were here reported for the first time. LC-MS analyses showed the presence of 38 constituents, identified in all propolis extracts, belonging to flavonoids and phenolic acids classes. The Pietradefusi extract was the richest one and thus was selected to design the PPP preparation for the in vivo assay. Our results highlight the impact of PPP on RA onset and progre...
Natural Product Communications, 2015
A new phenolic compound, 6′- O-sulfonyl-salidroside (1), together with fifteen known compounds, w... more A new phenolic compound, 6′- O-sulfonyl-salidroside (1), together with fifteen known compounds, were isolated from the all parts of Limonium pruinosum. Their structures were elucidated by 1D and 2D NMR experiments including 1D TOCSY, DQF-COSY, HSQC and HMBC spectroscopy, as well as ESIMS analysis. The antioxidant activity of the extracts and all isolated compounds was evaluated by DPPH test.
Natural Product Communications, 2016
Two new sesquiterpenes, 8α-(4-hydroxymethacryloyl)-14-acetoxy-salonitenolide (1) and 8α-(2-hydrox... more Two new sesquiterpenes, 8α-(4-hydroxymethacryloyl)-14-acetoxy-salonitenolide (1) and 8α-(2-hydroxymethyl 2-butenoyl)-14-acetoxy-salonitenolide (2), together with five known sesquiterpenes were isolated from the leaves of Vernonia nigritiana Oliv. & Hiern. Their structural characterization was obtained on the basis of extensive NMR spectroscopic and mass spectrometric studies.
Natural Product Communications, 2008
Three new oleanane saponins (1–3), together with four known ones (4–7), were isolated from the ae... more Three new oleanane saponins (1–3), together with four known ones (4–7), were isolated from the aerial parts of Polyscias guilfoylei. Their structures were elucidated by 1D and 2D NMR experiments, including 1D TOCSY, DQF-COSY, ROESY, HSQC, and HMBC spectroscopy, as well as ESIMS analysis. The antiproliferative activity of all compounds was evaluated using three murine and human cancer cell lines; J774.A1, HEK-293, and WEHI-164. All the compounds were inactive except for 3β- O-[β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl]-echinocystic acid 28-[ O-β-D-glucopyranosyl-(1→6) O-β-D-glucopyranosyl] ester (3), which was active against all the cell lines.
Natural Product Communications, 2012
Four new oleanane saponins (1-4), together with three known saponins, were isolated from the aeri... more Four new oleanane saponins (1-4), together with three known saponins, were isolated from the aerial parts of Dizygotheca elegantissima R. Vig. & Guillaumin. Their structures were elucidated by 1D and 2D NMR experiments including 1D TOCSY, DQF-COSY, HSQC, and HMBC spectroscopy, as well as ESIMS analysis. The antiproliferative activity of all isolated compounds was evaluated.
Natural Product Communications, 2009
One new flavonoid glycoside, 3-O-kaempferol 4-O-(galloyl)-β-D-glucoside, one new bergenin derivat... more One new flavonoid glycoside, 3-O-kaempferol 4-O-(galloyl)-β-D-glucoside, one new bergenin derivative, 11-0-caffeoylbergenin, along with other known flavonoids and phenolic derivatives, were isolated from the leaves of Securinega virosa. Their structures were established on the basis of detailed spectral analysis. In vitro biological analysis of the isolated compounds showed that they were able to quench DPPH radicals and had a direct scavenging activity on superoxide anion. Kaempferol 3-O-(4-galloyl)-β-D-glucopyranoside (1), 11-0-caffeoylbergenin (2), and glucogallin (6) exhibited the highest antioxidant capacity, being also able to modulate hydroxyl radical formation more efficiently than the other compounds, acting as direct hydroxyl radical scavengers and chelating iron.
Pharmaceuticals (Basel, Switzerland), Jan 22, 2018
The aim of the present study was the development of a "smart bandage" for the topical a... more The aim of the present study was the development of a "smart bandage" for the topical administration of diclofenac, in the treatment of localized painful and inflammatory conditions, incorporating Molecularly Imprinted Polymers (MIPs) for the controlled release of this anti-inflammatory drug. For this purpose, MIP spherical particles were synthesized by precipitation polymerization, loaded with the therapeutic agent and incorporated into the bandage surface. Batch adsorption binding studies were performed to investigate the adsorption isotherms and kinetics and the selective recognition abilities of the synthesized MIP. In vitro diffusion studies were also carried out using Franz cells and the obtained results were reported as percentage of the diffused dose, cumulative amount of diffused drug, steady-state drug flux and permeability coefficient. Moreover, the biocompatibility of the developed device was evaluated using the EPISKIN™ model. The Scatchard analysis indicated ...
Evidence-based complementary and alternative medicine : eCAM, 2018
is a genus of flowering plants belonging to Asteraceae family. This genus is mainly represented b... more is a genus of flowering plants belonging to Asteraceae family. This genus is mainly represented by the (All.) Nyman ex Soldano, the milky thistle, a plant of Mediterranean origin. is consumed as a monofloral boar thistle honey. Chromatography separation of CHCl and BuOH extracts of aerial parts of led to isolation of 18 pure compounds. Their structures were elucidated by 1D-and 2D-NMR spectroscopy and confirmed by mass spectrometry analysis. Sinapic aldehyde, abietin, chlorogenic acid, neochlorogenic acid, 8-hydroxypinoresinol, 9-hydroxypinoresinol, pinoresinol, 4-ketopinoresinol, nortrachelogenin, and -guaiacylglycerol---4'-dihydroconiferyl alcohol were isolated from CHCl extract, while luteolin 4'--glucuronide, naringenin7--neohesperidoside, kaempferol-3---L-rhamnopyranosyl-(1→6)--D-glucopyranoside, apigenin-7---L-rhamnopyranosyl-(1→6)--D-glucopyranoside, quercitrin, quercetin-3---L-rhamnopyranosyl-(1→6)--D-glucopyranoside, ciwujiatone, and nortrachelogenin-4,4'-di---D...
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Papers by Antonio Vassallo