Article
Pharmacology & Pharmacy
Shirleide Santos Nunes, Juliana de Oliveira Silva, Renata Salgado Fernandes, Sued Eustaquio Mendes Miranda, Elaine Amaral Leite, Marcelo Alexandre de Farias, Rodrigo Villares Portugal, Geovanni Dantas Cassali, Danyelle M. Townsend, Monica Cristina Oliveira, Andre Luis Branco de Barros
Summary: PEGylated liposomes are widely studied as drug delivery systems, but their interaction with cells may be hindered by the addition of PEG. This study compared the characteristics and drug delivery capabilities of PEGylated and non-PEGylated liposomes. The results showed that non-PEGylated liposomes had better cellular uptake and were more effective in controlling tumor growth.
Article
Chemistry, Medicinal
Xiaqiu Qiu, Yuanqing Li, Bin Yu, Jie Ren, Huidan Huang, Min Wang, Hong Ding, Zhiyu Li, Jubo Wang, Jinlei Bian
Summary: CDK9 inhibitor BAY-1143572 converted into PROTACs leads to degradation of CDK9 in acute myeloid leukemia cells, with the most potent molecule B03 showing enhanced antiproliferative activity. This enhanced activity is mediated by increased kinase inhibitory activity and apoptosis induction levels. B03 can also induce CDK9 degradation in vivo, indicating its potential as a therapeutic strategy in acute myeloid leukemia.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Rosanna Mallamaci, Maria Annunziata M. Capozzi, Cosimo Cardellicchio
Summary: Two aminobenzylnaphthols, synthesized with the Betti reaction, were investigated as antiproliferative agents against adenocarcinoma human colorectal (Caco-2) and human neuroblastoma (SH-SY5Y) cell lines. One molecule showed better antiproliferative activity after 24 hours of incubation, while the other was more effective after 72 hours. These results suggest that both compounds have potential biological activity.
APPLIED SCIENCES-BASEL
(2022)
Article
Pharmacology & Pharmacy
Zixu Liu, Wei Chu, Qianhe Sun, Linxuan Zhao, Xinyi Tan, Yu Zhang, Tian Yin, Haibing He, Jingxin Gou, Xing Tang
Summary: A novel hybrid nano-carrier system composed of micelles encapsulated within PEGylated liposomes was developed to combine the unique strengths of each component for combined delivery of GEM and CDDP. The hybrid liposomes showed enhanced cellular uptake and decreased IC50 value in vitro, as well as improved pharmacokinetic properties and antitumor efficacy in vivo. This study demonstrated the potential of the micelle-containing PEGylated hybrid liposomes for synergistic chemotherapy with GEM and CDDP.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Medicine, Research & Experimental
Javier Fernandez, Blanca Silvan, Rodrigo Entrialgo-Cadierno, Claudio J. Villar, Raffaele Capasso, Jose Antonio Uranga, Felipe Lombo, Raquel Abalo
Summary: Flavonoids, with diverse pharmacological properties, show potential effects against cancer cells, especially xanthohumol displaying the best antitumor activity, even surpassing 5-FU. Some flavonoids, like apigenin and luteolin, may have a synergistic effect when combined with 5-FU, offering promising treatment options for CRC.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Chemistry, Multidisciplinary
Alexei N. Izmest'ev, Galina A. Gazieva, Lada V. Anikina, Sergey A. Pukhov, Valentina A. Karnoukhova, Natalya G. Kolotyrkina, Angelina N. Kravchenko
Summary: Two novel series of compounds were synthesized and evaluated for their antiproliferative activity, with one compound showing high potency with very low GI(50) values against a subset of cancer cell lines among 60 tested.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Bin Wang, Youcai Liu, Lejing Zhang, Yajuan Wang, Zhaoxi Li, Xin Chen
Summary: In this paper, a series of novel compounds were designed as selective histone deacetylase 6 inhibitors. Compound 8f showed high inhibitory activity and selectivity, as well as good antiproliferative activity against multiple tumor cells.
Article
Biochemistry & Molecular Biology
Laura Gallego-Yerga, Andrea Jazmin Chiliquinga, Rafael Pelaez
Summary: Increasing awareness of the structure of microtubules has driven research on targeting tubulin for novel chemotherapies, particularly for glioblastoma multiforme (GBM) cells. Optimization of potently anti-tubulin drugs with improved pharmacokinetic properties is challenging, but the use of ensemble pharmacophore screening has led to the development of a new tetrazole-based tubulin inhibitor. This inhibitor demonstrated remarkable antimitotic effects against various cancer cells, especially GBM cells, with high selectivity and overcome the limitations typically associated with tubulin binding agents.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Domenico Nuzzo, Miriana Scordino, Antonino Scurria, Costanza Giardina, Francesco Giordano, Francesco Meneguzzo, Giuseppa Mudo, Mario Pagliaro, Pasquale Picone, Alessandro Attanzio, Stefania Raimondo, Rosaria Ciriminna, Valentina Di Liberto
Summary: IntegroPectin from grapefruit shows strong antioxidant and antiproliferative effects, making it a potential therapeutic agent for oxidative stress-associated brain disorders and cancer. Further studies on its molecular mechanisms are urgently needed to fully explore its therapeutic and preventive potential.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Tingting Liang, Xiaomin Zhou, Lu Lu, Haiyang Dong, Yanan Zhang, Yungen Xu, Jianguo Qi, Yahong Zhang, Jianhong Wang
Summary: Colchicine binding site inhibitors have great potential for treating tumors. Tetrahydro-quinoxaline derivatives designed in this study showed promising antitumor activities, with compound 11a being the most potent candidate.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Alexandros-Dimitrios C. Magklaras, Christina N. N. Banti, Sotiris K. K. Hadjikakou
Summary: The antiproliferative activity of three clinically used antibiotics (CIP·HCl, PEN·Na, and TC·HCl) was studied through DNA inhibition mechanisms using ex vivo, in silico, and in vitro methods. The binding interactions of the antibiotics with DNA were determined through UV-Vis spectra and viscosity measurements, and their binding constants (K-b) were calculated. Docking studies were performed to explain the ex vivo results. The in vitro antiproliferative activity of the antibiotics was evaluated against MCF-7 cells, and the toxicity was tested against MRC-5 cells. TC·HCl and CIP·HCl exhibited significant antiproliferative activity and low toxicity despite their low binding affinity to DNA or different mode of interaction.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Pharmacology & Pharmacy
Zixu Liu, Linxuan Zhao, Xinyi Tan, Zixuan Wu, Ning Zhou, Nan Dong, Yu Zhang, Tian Yin, Haibing He, Jingxin Gou, Xing Tang, Song Gao
Summary: In this study, a novel nanocarrier, NLEH, was developed to improve the encapsulation efficiency, sterilization stability, and antitumor activity of norcantharidin (NCTD). NLEH exhibited higher encapsulation efficiency and better sterilization stability compared to NCTD liposomes and NCTD emulsions. Furthermore, NLEH showed improved therapeutic effects by promoting absorption, prolonging blood circulation, enhancing tumor-targeting accumulation, improving tumor penetration, and increasing antitumor immunity.
EXPERT OPINION ON DRUG DELIVERY
(2022)
Article
Chemistry, Multidisciplinary
Marwa F. Ahmed, Atiah H. Almalki
Summary: New thiosemicarbazone derivatives were synthesized and evaluated for their anticancer activity, with compounds IIIa, IIIe, and IIIh showing promising results. Compound IIIa exhibited potent inhibitory activity against ribonucleotide reductase and induced apoptosis through activating the intrinsic apoptotic pathway.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Paulina Strugala, Anna Urbaniak, Patryk Kurys, Aleksandra Wloch, Teresa Kral, Maciej Ugorski, Martin Hof, Janina Gabrielska
Summary: The study examined the antioxidant and cytotoxic activities of purple potato ethanolic extract of the Blue Congo variety (BCE), demonstrating its ability to protect lipid membranes against peroxidation and inhibit the growth of colon cancer cells.
Article
Biochemistry & Molecular Biology
Fu-Li Xie, Zhi-Tong Huang, Lan Bai, Jian-Wei Zhu, Hui-Hua Xu, Qing-Qin Long, Qi-Feng Guo, Yong Wu, Si-Hong Liu
Summary: Two iridium (III) polypyridine complexes were synthesized and encapsulated in liposomes, showing high cytotoxicity against cancer cells while having no significant toxicity towards non-cancer cells. The complexes inhibit cell proliferation, induce cell cycle arrest, and affect mitochondrial function and ROS levels, suggesting a potential mechanism of action through ROS-mediated mitochondrial dysfunction and activation of PI3K/AKT signaling pathways in cancer cells.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Maddalena Sguizzato, Elisabetta Esposito, Rita Cortesi
Summary: Skin disorders can be treated with topical drug applications utilizing lipid-based nanosystems, including liposomes, ethosomes, transferosomes, solid lipid nanoparticles, and more. These nanosystems offer efficient delivery of drugs, potentially reducing side effects, and have the ability to administer antioxidant molecules topically. More research is needed to understand the interaction between lipid-based nanosystems and the skin, but highlighting their possibilities could benefit the scientific community.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Andrea Alogna, Valentina Gentili, Claudio Trapella, Supandeep Singh Hallan, Maddalena Sguizzato, Giovanni Strazzabosco, Mercedes Fernandez, Rita Cortesi, Roberta Rizzo, Daria Bortolotti
Summary: Liposomes have been utilized in various fields due to their versatility and easy production. This study evaluated the use of liposomes as a vehicle for delivering active components from snail mucus, showing promising effects on wound healing reconstitution. Specifically, the HC-loaded liposomes demonstrated superior cell monolayer reconstruction compared to untreated and HC-treated samples, indicating a novel delivery strategy for the HelixComplex mucus.
Article
Pharmacology & Pharmacy
Maddalena Sguizzato, Francesca Ferrara, Paolo Mariani, Alessia Pepe, Rita Cortesi, Nicolas Huang, Fanny Simeliere, Paola Boldrini, Anna Baldisserotto, Giuseppe Valacchi, Elisabetta Esposito
Summary: This study described a formulative research for the development of vesicular systems for mangiferin based on phosphatidylcholine and the block copolymer pluronic, and compared their effect on mangiferin transdermal administration. The results showed that multilamellar vesicles retain mangiferin drugs more effectively than unilamellar ones, and the protective effect exerted by Plurethosomes and transethosomes suggests their possible application in enhancing cutaneous antioxidant defense.
Article
Pharmacology & Pharmacy
Mariaconcetta Sicurella, Maddalena Sguizzato, Rita Cortesi, Nicolas Huang, Fanny Simeliere, Leda Montesi, Peggy Marconi, Elisabetta Esposito
Summary: This study investigated smart semisolid forms based on phosphatidylcholine and Pluronic for delivering mangiferin to treat HSV-1 infections. Results showed that mangiferin could be efficiently included in all types of gels and that the Pluronic organogel exhibited strong control over drug diffusion.
Article
Cell Biology
Enrica Cappellozza, Federico Boschi, Maddalena Sguizzato, Elisabetta Esposito, Rita Cortesi, Manuela Malatesta, Laura Calderan
Summary: The investigation of drug delivery systems and their absorption in the body can be simplified by using bio-imaging techniques. However, the high autofluorescence of the skin makes it difficult to detect the fluorescence signal from administered fluorophores. This study developed a method to analyze the fluorescence of skin samples and distinguish the signal from administered fluorescent molecules. The results showed that solid lipid nanoparticles with polymer are a suitable drug delivery system for transcutaneous administration.
EUROPEAN JOURNAL OF HISTOCHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Mariaconcetta Sicurella, Maddalena Sguizzato, Paolo Mariani, Alessia Pepe, Anna Baldisserotto, Raissa Buzzi, Nicolas Huang, Fanny Simeliere, Sam Burholt, Peggy Marconi, Elisabetta Esposito
Summary: This study designed and evaluated gel formulations of quercetin and mangiferin for the treatment of HSV-1 infection. The physical-chemical characteristics and diffusion kinetics of the gels were studied and evaluated, with the poloxamer-based gel showing better stability of polyphenol activity. In addition, the virucidal effect of quercetin and mangiferin loaded in the gels against HSV-1 was assessed.
Article
Instruments & Instrumentation
Maddalena Sguizzato, Markus Drechsler, Anna Baldisserotto, Rita Cortesi, Elisabetta Esposito
Summary: The study investigated the use of monoolein aqueous dispersions (MADs) as delivery systems for antioxidant molecules AP and AT. Results showed that MAD-AP and MAD-AT exhibited good performance in terms of size and antioxidant activity. The study demonstrated that MADs could be potentially used as effective delivery systems for antioxidant supplementation in dietary or cosmetic fields.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2022)
Editorial Material
Biochemistry & Molecular Biology
Elisabetta Esposito
Article
Pharmacology & Pharmacy
Francesca Ferrara, Mascia Benedusi, Maddalena Sguizzato, Rita Cortesi, Anna Baldisserotto, Raissa Buzzi, Giuseppe Valacchi, Elisabetta Esposito
Summary: This study aimed to design ethosomes and transethosomes for topical administration of quercetin. The results showed that both phosphatidylcholine concentration and quercetin affected the vesicle size. Transethosomes produced by the highest amount of phosphatidylcholine exhibited control over quercetin entrapment capacity, antioxidant activity, and size stability. In vitro permeation studies revealed enhanced quercetin permeation with transethosomes compared to ethosomes. Additionally, scratch wound and migration assays suggested the potential of quercetin-loaded transethosomes as an adjuvant strategy for skin conditions.
Article
Biochemistry & Molecular Biology
Francesca Ferrara, Mascia Benedusi, Franco Cervellati, Maddalena Sguizzato, Leda Montesi, Agnese Bondi, Markus Drechsler, Walter Pula, Giuseppe Valacchi, Elisabetta Esposito
Summary: In this study, transethosomes were explored as potential delivery systems for dimethyl fumarate. Formulative studies were conducted to investigate the effects of various compositions on the morphology and drug entrapment capacity of vesicles. Results showed that certain formulations were able to effectively improve wound healing and control drug release, indicating their potential application in wound treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Elisabetta Esposito, Laura Calderan, Andrea Galvan, Enrica Cappellozza, Markus Drechsler, Paolo Mariani, Alessia Pepe, Maddalena Sguizzato, Enrico Vigato, Edoardo Dalla Pozza, Manuela Malatesta
Summary: This study investigated the transdermal fate of ethosomes and transethosomes on human skin. The results showed that the vesicle penetration capability was influenced by their physical-chemical features, with different vesicles reaching different levels of the skin. This offers potential for tailored transdermal drug delivery based on specific cutaneous pathologies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Mariaconcetta Sicurella, Walter Pula, Karolina Musial, Katarzyna Cieslik-Boczula, Maddalena Sguizzato, Agnese Bondi, Markus Drechsler, Leda Montesi, Elisabetta Esposito, Peggy Marconi
Summary: This study investigated the use of an ethosome gel loaded with dimethyl fumarate as a potential treatment for HSV-1 infections. The study evaluated the effect of drug concentration on size distribution and stability of ethosomes and demonstrated the antiviral activity of the gel. The results showed that the gel effectively reduced viral growth and was safe for use on the skin.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Polymer Science
Denise Bellotti, Maria D'Accolti, Walter Pula, Nicolas Huang, Fanny Simeliere, Elisabetta Caselli, Elisabetta Esposito, Maurizio Remelli
Summary: In this study, a formulation suitable for the administration of calcitermin on vaginal mucosa was developed for the treatment of fungal infections. The rheological behavior, erosion, and leakage of different gel formulations were compared, and the selected gel was loaded with calcitermin. The calcitermin-loaded gel showed improved release kinetics and enhanced anticandidal activity.
