A5049092095- Malaria Research and Control
- Synthesis and biological activity
- Computational Drug Discovery Methods
- Click Chemistry and Applications
- Crystallization and Solubility Studies
- Synthesis and Biological Evaluation
- X-ray Diffraction in Crystallography
- Natural product bioactivities and synthesis
- Natural Compounds in Disease Treatment
- SARS-CoV-2 and COVID-19 Research
- Boron Compounds in Chemistry
- Boron and Carbon Nanomaterials Research
- Mosquito-borne diseases and control
- Synthesis and Catalytic Reactions
- Bioactive natural compounds
- Traditional and Medicinal Uses of Annonaceae
- Insect and Pesticide Research
- HIV/AIDS drug development and treatment
- Drug Transport and Resistance Mechanisms
- Synthesis and Characterization of Heterocyclic Compounds
- Bioactive Compounds and Antitumor Agents
- Cancer therapeutics and mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Research on Leishmaniasis Studies
- Autophagy in Disease and Therapy
Macau University of Science and Technology
2016-2025
University of Macau
2020-2024
Quality Research
2023
University of Milano-Bicocca
2013-2019
University of Milan
2008-2015
Mylan (Switzerland)
2015
Institute of Molecular Science and Technologies
2007-2012
The outbreak of coronavirus (SARS-CoV-2) disease caused more than 100,000,000 people get infected and over 2,200,000 being killed worldwide. However, the current developed vaccines or drugs may be not effective in preventing pandemic COVID-19 due to mutations severe side effects newly vaccines. Chinese herbal medicines their active components play important antiviral activities. Corilagin exhibited effect on human immunodeficiency virus (HIV), hepatitis C (HCV) Epstein-Barr (EBV). whether it...
Managing malaria. Malaria is responsible for two million deaths per year particularly in developing countries, therefore there great need the development of cost effective treatment. The synthesis a library trisubstituted triazines with potent antimalarial vitro activity reported. Among them, five products may be developed as potential leads search new drugs against plasmodial chloroquine-resistant strains.
Abstract The antimalarial drug methylene blue (MB) affects the redox behaviour of parasite flavin‐dependent disulfide reductases such as glutathione reductase (GR) that control oxidative stress in malaria parasite. reduced flavin adenine dinucleotide cofactor FADH 2 initiates reduction to leucomethylene (LMB), which is oxidised by oxygen generate reactive species (ROS) and MB. MB then acts a subversive substrate for NADPH normally required regenerate enzyme function. synergism between...
Abstract Artemisinins are proposed to act in the malaria parasite cytosol by oxidizing dihydroflavin cofactors of redox‐active flavoenzymes, and under aerobic conditions inducing their autoxidation. Perturbation redox homeostasis coupled with generation reactive oxygen species (ROS) ensues. Ascorbic acid–methylene blue (MB), N ‐benzyl‐1,4‐dihydronicotinamide (BNAH)–MB, BNAH–lumiflavine, BNAH–riboflavin (RF), NADPH–FAD– E. coli flavin reductase (Fre) systems at pH 7.4 generate leucomethylene...
Abstract Twenty six peroxides belonging to bridged 1,2,4,5‐tetraoxanes, 1,2,4‐trioxolanes (ozonides), and tricyclic monoperoxides were evaluated for their in vitro antimalarial activity against Plasmodium falciparum (3D7) cytotoxic activities immortalized human normal fibroblast (CCD19Lu), liver (LO 2 ), lung (BEAS‐2B) cell lines as well (HepG2) (A549) cancer‐cell lines. Synthetic ozonides shown have the highest cytotoxicity on HepG2 (IC 50 =0.19–0.59 μ m some of these compounds selectively...
This article discloses a new horizon for the application of peroxides in medical chemistry. Stable cyclic are demonstrated to have cytotoxic activity against cancer cells; addition mechanism action is proposed. Synthetic bridged 1,2,4,5-tetraoxanes and ozonides were effective HepG2 cells some selectively targeted liver (the selectivity indexes compounds 11 b 12 8 5, respectively). In cases, tetraoxanes more selective than paclitaxel, artemisinin, artesunic acid. Annexin V flow-cytometry...
Leishmaniasis is a neglected tropical disease, and there an emerging need for the development of effective drugs to treat it. To identify novel compounds with antileishmanial properties, series functionalized spiro[indoline-3,2'-pyrrolidin]-2-one/spiro[indoline-3,3'-pyrrolizin]-2-one 23a-f, 24a-f, 25a-g were prepared from natural-product-inspired pharmaceutically privileged bioactive sub-structures, i.e., isatins 20a-h, various substituted chalcones 21a-f, 22a-c amino acids, via 1,3-dipolar...
In this report, we discuss the synthesis of modified betulin through chemical derivatization a natural compound. The compound was fully characterized by proton (1H), carbon-13 (13C), heteronuclear single quantum coherence (HSQC) and distortionless enhancement polarization transfer (DEPT) NMR elemental analysis. We investigated optical properties ultraviolet (UV) Fourier-transform infrared (FTIR) spectroscopy.
Honey is a natural product of ethnopharmacology widely used worldwide and in the fast-changing world science technology. Packed with rich chemical compositions, this traditional nutrient has been indicated for variety new uses. In paper, different varieties honey nutritional value multidimensional use are comprehensively discussed their antibacterial, antiviral, anticancer, anti-inflammatory, antiparasitic effects. addition, effects promoting wound healing, regulating oxidative stress,...
Conjugated polymers (CPs) continue to revolutionize the landscape of materials science with their unique electrical, optical, and mechanical properties [...]
Forty‐five aminoperoxides belonging to bridged azaozonides, N‐substituted and tricyclic were evaluated for in vitro antimalarial activity against Plasmodium falciparum (3D7) cytotoxicity immortalized human normal liver (LO2) lung (BEAS‐2B) cell lines, as well (HepG2) (A549) cancer lines. Seven azaozonides exhibited high the chloroquine‐sensitive 3D7 strain of P. falciparum, with IC50 < 1 µM. The lead compound 22 showed = 0.07 µM selectivity index 1428. Most generally non‐cytotoxic both...
Abstract Flavin adenine dinucleotide (FAD) is reduced by NADPH– E. coli flavin reductase (Fre) to FADH 2 in aqueous buffer at pH 7.4 under argon. Under the same conditions, turn cleanly reduces antimalarial drug methylene blue (MB) leucomethylene blue. The latter rapidly re‐oxidized artemisinins, thus supporting proposal that MB exerts its activity, and synergizes action of interfering with redox cycling involving NADPH reduction cofactors parasite disulfide reductases. Direct treatment...
Cancers illustrating resistance towards apoptosis is one of the main factors causing clinical failure conventional chemotherapy. Innovative therapeutic methods which can overcome non-apoptotic phenotype are needed. The AMP-activated protein kinase (AMPK) central regulator cellular energy homeostasis, metabolism, and autophagy. Our previous study showed that identified natural AMPK activator able to apoptosis-resistant cancer via autophagic cell death. Therefore, an ideal pharmaceutical...
Bridged aminoperoxides, for the first time, were investigated in vitro antimalarial activity against chloroquine-resistant Plasmodium falciparum strain K1 and their cytotoxic activities immortalized human normal liver (LO2) lung (BEAS-2B) cell lines as well (HepG2) (A549) cancer lines. Aminoperoxides exhibit good cytotoxicity A549 line. Synthetic ozonides shown to have high P. falciparum. A cyclic voltammetry study of peroxides was performed, most compounds did not show a direct correlation...
Due to their extended p-orbital delocalization, conjugated polymers absorb light in the range of visible–NIR frequencies. We attempt exploit this property create materials that compete with inorganic semiconductors photovoltaic and light-emitting materials. Beyond competing for applications photonic devices, organic compounds, polymers, small molecules have also been biomedical like phototherapy biodetection. Recent research on has focused bioapplications based absorbed energy conversions...
Drug resistance of non-small cell lung cancer (NSCLC) is highly correlated to the mutation epidermal growth factor receptor (EGFR). Although EGFR tyrosine kinase inhibitors (TKIs) are available clinically, molecular complexity NSCLC has made it necessary search for alternative therapeutic approaches overcome drug NSCLC. In present study, we identified a triterpene molecule derived from herbal plant Tripterygium wilfordii, celastrol, as novel autophagy inducer. We demonstrate that celastrol...
Host cell invasion by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is mediated the interaction of viral spike protein (S) with human angiotensin-converting enzyme (ACE2) through receptor-binding domain (RBD). In this work, computational and experimental techniques were combined to screen antimalarial compounds from different chemical classes, aim identifying small molecules interfering RBD-ACE2 and, consequently, invasion. Docking studies showed that interfere same region...