Marco Filice

• PhD Pharmaceutical Chemistry
• Principal Investigator at Complutense University of Madrid

The current search for more effective and milder cancer treatments has led to the development of a wide variety of multifunctional nanoplatforms that are designed to both diagnose and treat cancer. In this study, the optimization of the synthesis of theranostic materials based on mesoporous silica nanoparticles (MSNs) functionalized with different...

Background and Aims Targeting epigenetic mechanisms offer a potential breakthrough in addressing kidney diseases. Thus, inhibition of the bromodomain and extra-terminal (BET) domain proteins using the small molecule inhibitor JQ1, has shown promise in preclinical models of acute kidney injury (AKI) and chronic kidney disease (CKD). However, clinica...

Nanostructured materials possess promising potential for cancer therapy through precise adjustment of their functionalization and physicochemical attributes. This study primarily focuses on the synthesis and characterization of mesoporous silica nanoparticles (MSN) that are functionalized with titanocene dichloride (a therapeutic agent) and one of...

Nanoscale materials have demonstrated a very high potential in anticancer therapy by properly adjusting their functionalization and physicochemical properties. Herein, we report the synthesis of some novel vanadocene-loaded silica-based nanomaterials incorporating four different S-containing amino acids (penicillamine, methionine, captopril, and cy...

The pharmacological activity of organotin(IV) complexes in cancer therapy is well recognized but their large applicability is hampered by their poor water solubility. Hence, carbon dots, in particular nitrogen‐doped graphene quantum dots (NGQDs), may be a promising alternative for the efficient delivery of organotin(IV) compounds as they have a sub...

Five different silica nanoparticles functionalized with vitamin B12, a derivative of coumarin found in green plants and a minimum content of an organotin(IV) fragment (1-MSN-Sn, 2-MSN-Sn, 2-SBA-Sn, 2-FSPm-Sn and 2-FSPs-Sn), were identified as excellent anticancer agents against triple negative breast cancer, one of the most diagnosed and aggressive...

(1) Background: Early response after acute myocardial infarction (AMI) prevents extensive cardiac necrosis, in which inflammation resolution, including expression of anti-inflammatory interleukin-10 (IL-10), may play a key role. (2) Methods: We synthesized NIL10, a micelle-based nanoparticle, to target IL-10 receptor in mice and pigs subjected to A...

Background: Rapid screening and accurate diagnosis of acute myocardial infarction are critical to reduce the progression of myocardial necrosis, in which proteolytic degradation of myocardial extracellular matrix plays a major role. In previous studies, we found that targeting the extracellular matrix metalloprotease inducer (EMMPRIN) by injecting...

A new series of theranostic silica materials based on fibrous silica particles acting as nanocarriers of two different cytotoxic agents, namely, chlorambucil and an organotin metallodrug have been prepared and structurally characterized. Besides the combined therapeutic activity, these platforms have been decorated with a targeting molecule (folic...

Ag2S nanoparticles are near-infrared (NIR) probes providing emission in a specific spectral range (~1200 nm), and superparamagnetic iron oxide nanoparticles (SPION) are colloidal systems able to respond to an external magnetic field. A disadvantage of Ag2S NPs is the attenuated luminescent properties are reduced in aqueous media and human fluids. C...

Rationale: Early response after acute myocardial infarction (AMI) is crucial to prevent extensive cardiac necrosis. Interleukin-10 (IL-10) is a key antiinflammatory cytokine, whose expression is closely associated with macrophage polarization towards inflammation resolution. Results: We synthesized NIL10, a micelle-based nanoparticle conjugated to...

In recent years, nanotechnology and biocatalysis have undergone awesome improvements, finally bringing a great revolution in different scientific areas. In this sense, working at the interface of materials engineering and biological sciences, the research branch of nanobiocatalys has emerged and demonstrated its wide application scope. As a represe...

Inorganic materials can provide a set of tools to decontaminate solid, liquid or air containing viral particles. The use of disinfectants can be limited or not practical in scenarios where continuous cleaning is not feasible. Physicochemical differences between viruses raise the need for effective formulations for all kind of viruses. In the presen...

The treatment of skin wounds poses significant clinical challenges, including the risk of bacterial infection. In particular due to its antimicrobial and tissue regeneration abilities chitosan (a polymeric biomaterial obtained by the deacetylation of chitin) has received extensive attention for its effectiveness in promoting skin wound repair. On t...

Cancer is the second leading cause of death in the world, which is why it is so important to make an early and very precise diagnosis to obtain a good prognosis. Thanks to the combination of several imaging modalities in the form of the multimodal molecular imaging (MI) strategy, a great advance has been made in early diagnosis, in more targeted an...

List of contributors for the Book named "Magnetic Nanoparticle-Based Hybrid Materials" by Woodhead Publishing Series in Electronic and Optical Materials, 2021, Pages xv-xxi.

Biosensors based on two-dimensional (2D) nanomaterials could make analytical results available within a few minutes at the patient bedside or physician office, at low cost and with a very low limit of detection. The nano-sized nature of nanomaterials and their unique chemical and electrical properties can improve patient care by making the sensors...

As cancer remains one of the leading causes of death, its accurate diagnosis at a very early stage is an important goal to obtain the best possible prognosis. By integrating complementary modalities, multimodal molecular imaging has improved the ability to diagnose early, guide therapy, and predict outcomes of cancer treatment. Toward this end, mag...

Applied nanotechnology has experienced tremendous advance over the last decade. In this study, the efficient synthesis of highly stable palladium-nanoparticles (PdNPs) biohybrids based on the application of an enzyme, which induces in situ the generation of spherical nanoparticles on the protein network, has been described. A heterogeneous material...

The Front Cover shows that the supported enzyme naringinase on a laminar zeolite is able to produce citrus flavonoids of important pharmacologic activities from citrus wastes, and in addition, the same enzymatic catalytic system is used for debittering citrus juices. In their Communication, J. M. Carceller et al. explain that naringine, a glycoside...

Enzyme‐powered micro/nanomotors have myriads of potential applications in various areas. To efficiently reach those applications, it is necessary and critical to understand the fundamental aspects affecting the motion dynamics. Herein, we explored the impact of enzyme orientation on the performance of lipase‐powered nanomotors by tuning the lipase...

The impact of enzyme orientation on the performance of lipase‐powered nanomotors was explored and analysed, indicating that hydrophobic interaction is the best strategy for immobilizing lipase to provide high‐efficiency catalysis. This results in a high‐efficiency enhanced Brownian motion, which would be vital in promoting the future applications o...

The crude naringinase from Penicillium decumbens and a purified naringinase with high α‐L‐rhamnosidase activity could be covalently immobilized on two‐dimensional zeolite ITQ‐2 after surface modification with glutaraldehyde. The influence of pH and temperature on the enzyme activity (in free and immobilized forms) as well as the thermal stability w...

The synthesis, characterization and cytotoxic activity against different cancer cell lines of various mesoporous silica-based materials containing folate targeting moieties and a cytotoxic fragment based on a triphenyltin(IV) derivative have been studied. Two different mesoporous nanostructured silica systems have been used: firstly, micronic silic...

Functional properties of each enzyme strictly depend on immobilization protocol used for linking enzyme and carrier. Different strategies were applied to prepare the immobilized derivatives of Rhizomucor miehei lipase (RML) and chemically aminated RML (NH2-RML). Both RML and NH2-RML forms were covalently immobilized on glyoxyl sepharose (Gx-RML and...

Three different multifunctional nanosystems based on the tethering onto mesoporous silica nanoparticles (MSN) of different fragments such as an organotin-based cytotoxic compound Ph3Sn{SCH2CH2CH2Si(OMe)3} (MSN-AP-Sn), a folate fragment (MSN-AP-FA-Sn), and an enzyme-responsive peptide able to release the metallodrug only inside cancer cells (MSN-AP-...

Magnetic resonance imaging (MRI) is the most powerful technique for non-invasive diagnosis of human diseases and disorders. Properly designed contrast agents can be accumulated in the damaged zone and be internalized by cells, becoming interesting cellular MRI probes for disease tracking and monitoring. However, this approach is sometimes limited b...

Endothelial dysfunction plays a central role in the pathophysiology of pulmonary arterial hypertension (PAH). MicroRNAs (miRNAs) are small single-strand and non-coding RNAs that negatively regulate gene function by binding to the 3′-untranslated region (3′-UTR) of specific mRNAs. microRNA-1 (miR-1) is upregulated in plasma from idiopathic PAH patie...

Production of citrus flavonoids prunin and naringenin was performed selectively through the enzyme hydrolysis of naringin, a flavonoid glycoside abundant in grapefruit wastes. To produce the monoglycoside flavonoid, prunin, crude naringinase from Penicillium decumbens was purified by a single purification step resulting in an enzyme with high α-rha...

Lack of endothelial nitric oxide causes endothelial dysfunction and circulating monocyte infiltration, contributing to systemic atheroma plaque formation in arterial territories. Among the different inflammatory products, macrophage-derived foam cells and smooth muscle cells synthesize matrix metalloproteinases (MMPs), playing a pivotal role in ear...

In the recent years, targeted cancer theranosis -the concomitant therapeutic treatment and selective visualization of cancerous tissue- has become a powerful strategy to improve patient prognosis. In this context, targeted multimodal molecular imaging -the combination of different imaging modalities overcoming their individual limitations- has attr...

Functionalized magnetite nanoparticles (FMNPs) and functionalized mesoporous silica nanoparticles (FMSNs) were synthesized by the conjugation of magnetite and mesoporous silica with the small and fluorogenic benzothiazole ligand, that is, 2(2-hydroxyphenyl)benzothiazole (hpbtz). The synthesized fluorescent nanoparticles were characterized by FTIR,...

The immobilization of biocatalysts on magnetic nanomaterial surface is a very attractive alternative to achieve enzyme nanoderivatives with highly improved properties. The combination between the careful tailoring of nanocarrier surfaces and the site-specific chemical modification of biomacromolecules is a crucial parameter to finely modulate the c...

Fusarium verticillioides lipases were purified in a “cascade” method using octadecyl Sepabeads and octyl Sepharose resins, which led to the isolation of two proteins with lipolytic activities. Lip 1 was purified after octyl Sepharose adsorption presenting 30.3 kDa and, Lip 2 presented 68.0 kDa after octadecyl adsorption. These immobilization proces...

Nowadays, thanks to the successful discoveries in the biomedical field achieved in the last two decades, a deeper understanding about the complexity of mechanistic aspects of different pathological processes has been obtained. As a consequence, even the standard therapeutic protocols have undergone a vast redesign. In fact, the awareness about the...

The use of enzymes in food processing represents a historically well-established approach that gets its deepest roots in thousands of years BC. In fact, even in an unconscious way, the mankind always applied enzyme-based bioprocesses for example in beer brewing, bread baking, and cheese and wine making. Nevertheless, throughout the centuries, proce...

The authors would like to add the following sentence to the “Acknowledgments” section of their article [1]:[...]

In this study, trypsin (Enzyme Comission 3.4.21.4) was immobilized in a low cost, lignocellulosic support (corn cob powder—CCP) with the goal of obtaining peptides with bioactive potential from cheese whey. The pretreated support was activated with glyoxyl groups, glutaraldehyde and IDA-glyoxyl. The immobilization yields of the derivatives were hig...

In this study, trypsin (Enzyme Comission 3.4.21.4) was immobilized in a low cost, lignocellulosic support (corn cob powder—CCP) with the goal of obtaining peptides with bioactive potential from cheese whey. The pretreated support was activated with glyoxyl groups, glutaraldehyde and IDA-glyoxyl. The immobilization yields of the derivatives were hig...

This review compiles the most recent advances described in literature on the preparation of noble metal nanoparticles induced by biological entities. The use of different free or substituted carbohydrates, peptides, proteins, microorganisms or plants have been successfully applied as a new green concept in the development of innovative strategies t...

Palladium nanoparticles enzyme aggregate (PANEA) were prepared from Candida antarctica B lipase and palladium salt by precipitation and subsequent in situ Pd nanoparticle formation. This heterogeneous catalyst was successfully used for the Suzuki-Miyaura cross-coupling reaction between bromobenzene with different phenylboronic acid derivatives unde...

Soluble lipase from Thermomyces lanuginosa (TLL) was dramatically hyper-activated by a cationic surfactant, cetyltrimethylammonium bromide (CTAB). The greatest hyperactivation (above 340-fold) was observed with 0.005% CTAB. In addition to that, very high hyperactivation was also observed with much higher concentrations of surfactant (100-fold in th...

The aldol reactions catalyzed by aldolases are an important tool in the synthesis of different products or building blocks. However, despite its advantages, aldolases, as enzymes, have some troubles as their low activity against synthetic substrates or the low stability, doing difficult their application. There are different tools to improve the pr...

A p-nitrophenylphosphonate palladiumpincerwas synthesized and selectively inserted by ir-reversible attachment on the catalytic serineofdif-ferent commercial lipases with good to excellentyields in most cases.Among all, lipase from Candidaantarctica B(CAL-B) was the best modified enzyme.Theartificial metalloenzymeCAL-B-palladium (Pd)catalyst was su...

A solid-phase strategy using lipase as biomolecular scaffold to produce large amount of Cu2+-metalloenzyme is here proposed. The application of this protocol on different 3D cavities of the enzyme allows creating a heterogeneous artificial metallolipase showing chimeric catalytic activity. The artificial catalyst was assessed in cycloaddition and c...

The preparation and performance of a suitable chimeric biosensor based on antibodies (Abs) immobilized on lipase-coated magnetic particles by means of a standing orienting strategy are presented. This novel system is based on hydrophobic magnetic particles coated with modified lipase molecules able to orient and further immobilize different Abs in...

In this paper a series of 2-iminomethoxyethyl mannose-based mono- and disaccharides have been synthesized by chemoenzymatic approach and used in coupling reactions with ε-amino groups of lysine residues in a model protein (ribonuclease A, RNase A) to give semisynthetic neoglycoconjugates. In order to study the influence of structure of the glycans...

The activity of several commercial and genetically engineered lipases, already immobilized on octyl-Sepharose, in aqueous solutions containing ionic liquids (ILs) in a molar concentration of 0.01 mol L-1 was investigated. Strong variations in the hydrolytic activity values were found depending on the lipase, the ionic liquid and the substrate used....

Cascade reactions are an emerging technology in organic chemistry, introducing elegance and efficiency to synthetic strategies. This Review provides an overview of the novel and recent achievements in cascade processes catalyzed by bionanostructures. The examples here selected demonstrate the advances related to the application of heterogeneous nan...

One important parameter for the application of lipase catalysts in chemical industries is the specific activity displayed towards natural or unnatural substrates. Different strategies to enhance the lipase activity have been described. The immobilization of lipases on hydrophobic supports by interfacial adsorption at low ionic strength permitted th...

The reaction of transesterification between oils (e.g., olive oil) and ascorbic acid in polar anhydrous media (e.g., tert-amyl alcohol) catalyzed by immobilized lipases for the preparation of natural liposoluble antioxidants (e.g., ascorbyl oleate) was studied. Three commercial lipases were tested: Candida antarctica B lipase (CALB), Thermomyces la...

The straightforward synthesis of novel enzyme-metalNP nanobiohybrids in aqueous medium was developed. These new nanobiohybrids were excellent multivalent catalysts combining both activities in various sets of synthetic reactions even at ultra-low concentrations (ppb amount).

Enantiomerically pure product synthesis plays a key role in production of pharmaceuticals. The application of biocatalytic approaches represents a convenient and sustainable way for this purpose. The enormous potential of enzymes for the transformation of synthetic chemicals with high chemo-, regio- and enantioselectivity is on increasing awareness...

This Communication presents the development of a novel strategy for the easy conjugation of biomolecules to hydrophobic magnetic microparticles via reversible coating with previously functionalized lipase molecules. First, the ability of lipase to be strongly adsorbed onto hydrophobic surfaces was exploited for the stabilization of microparticles i...

Carbohydrates are complex and structurally diverse compounds in nature with key roles in a broad range of life processes including signal transduction, carcinogenesis and immune responses. Many natural products contain oligosaccharides that are vital for their biological activity. Despite ongoing challenges, tremendous progresses have been made in...

This protocol describes the regioselective deprotection of single hydroxyls in peracetylated monosaccharides and disaccharides by enzymatic or chemoenzymatic strategies. The introduction of a one-pot enzymatic step by using immobilized biocatalysts obviates the requirement to carry out tedious workups and time-consuming purifications. By using this...

An efficient chemoselective method for the creation of semisynthetic lipases by site-specific incorporation of tailor-made peptides on the lipase-lid site was developed. These new enzymes showed excellent improved specificity and regio- or enantioselectivity in different biotransformations.

The design of new strategies for improving the catalytic activity of lipases in their application on non-natural substrates is in great demand due to their biotechnological applications. This perspective illustrates the power of technologies, such as the immobilization of enzymes on nanomaterials and the site-specific chemical modification of enzym...

Carbohydrates are key molecules in nature with multiple roles in biological processes. Specifically the biological function of the glycosylated part is of great importance in natural products. In many cases carbohydrate-containing molecules are structurally diverse and this heterogeneity makes the isolation of sufficient amounts of the organic mole...

In this work peracetylated lactose and related compounds have been tested as advanced intermediate substrates in enzymatic deprotections catalyzed by acetyl xylan esterase (AXE) from Bacillus pumilus. In particular, we present a simple and efficient enzymatic procedure to obtain products bearing only one free primary hydroxy group in the C6′ positi...

Asymmetric hydrolysis of dimethyl 3-phenylglutarate (1) by immovilized LipBL preparations. (TIFF)

Enantioselective hydrolysis of 2-O-butyroil mandelic acid (5) by immovilized LipBL preparations. (TIFF)

MALDI-TOF Peptide Mass Fingerprinting (PMF) spectrum. The PMF analysis was carried out on fragments of lipase LipBL obtained through trypsin digestion. The sequence coverage of these fragments is shown underlined. (TIFF)

Similarity values of amino acid sequences for LipBL and homologue proteins (DOC)

Enantioselective hydrolysis of methyl mandelate (4) by immovilized LipBL preparations. (TIFF)

Enantioselective hydrolysis of 4-phenyl-2-hydroxyethylbutyrate (7) by immovilized LipBL preparations. (TIFF)

Background: Among extremophiles, halophiles are defined as microorganisms adapted to live and thrive in diverse extreme saline environments. These extremophilic microorganisms constitute the source of a number of hydrolases with great biotechnological applications. The interest to use extremozymes from halophiles in industrial applications is thei...

The influence of additives on the activity of different covalently and site-specific chemically modified immobilized preparations of a lipase from Geobacillus thermocatenulatus (BTL2) was investigated with a view to obtain a very high active biocatalyst. Non-ionic surfactant and co-solvents at different concentration range were applied. The CNBr-BT...

Rhizomucor miehei lipase (RML) is greatly hyperactivated (around 20- to 25-fold toward small substrates) in the presence of sucrose laurate. Hyperactivation appears to be an intramolecular process because it is very similar for soluble enzymes and covalently immobilized derivatives. The hyperactivated enzyme was immobilized (in the presence of sucr...

Lipase B from Candida antarctica (CAL-B) has been site-directedly modified by the introduction of a trans,trans-hexadiene moiety onto lipase molecules, identified by MALDI-TOF. This modification on CAL-B permitted its immobilization on Q-Sepharose supports in excellent yields (>95%) when native lipase was not immobilized at pH 7 and 25 °C. After th...

Organic cosolvents may improve the properties of lipases (e.g., selectivity); however, organic cosolvents also promote the desorption of the enzyme from its hydrophobic supports. In this study, adsorbed lipase molecules were cross-linked with polyfunctional polymers, such as aldehyde-dextrans, to prevent this desorption. The desorption of adsorbed...

Staphylococcus warneri strain EX17 produces three lipases with different molecular weights of 28, 30, and 45 kDa. The 45 kDa fraction (SWL-45) has been purified from crude protein extracts by one chromatographic step based on the selective adsorption of this lipase by interfacial activation on different hydrophobic supports at low ionic strength. T...

Partial acylation of only one primary hydroxyl group of glycerol generates a chiral center at position 2. Rhizomucor miehei lipase (RML) catalyzes the kinetically controlled transesterification of different aromatic carboxylic acids methyl esters with glycerol. High synthetic yields of glyceryl esters (around 70-80%) were obtained even in the prese...

The activity of a lipase from Geobacillus thermocatenulatus (BTL2) can be greatly improved by site-directed chemical modification of a single external Cys64. This residue is placed in the proximity of the region where the lid is allocated when the lipase exhibits its open and active form. Thiol group of Cys64 was modified by thiol-disulfide exchang...

The addition of small amount of different ionic liquids modified the activity and regioselectivity of different immobilized preparations of R. miehei lipase catalyzing the hydrolysis of hexa-O-acetyl lactal in aqueous media. ILs with [emim] as cation and different anions were first evaluated affecting in a different manner depending on the immobili...