Article
Biochemistry & Molecular Biology
Thibaut Barbier, Alexia Barbry, Jeremy Magand, Cedric Badiou, Floriane Davy, Anne Baudouin, Yves Queneau, Oana Dumitrescu, Gerard Lina, Laurent Soulere
Summary: In this study, new series of compounds were synthesized by combining the benzo[b]thiophene nucleus and the acylhydrazone functional group for screening against Staphylococcus aureus. Among the compounds tested, (E)-6-chloro-N'-(pyridin-2-ylmethylene)benzo[b]thiophene-2-carbohydrazide (II.b) showed promising antimicrobial activity with a minimal inhibitory concentration of 4 μg/mL against S. aureus strains, including clinically isolated strains resistant to methicillin and daptomycin.
Article
Microbiology
Mohamad Hamad, Farah Al-Marzooq, Vunnam Srinivasulu, Hany A. Omar, Ashna Sulaiman, Dana M. Zaher, Gorka Orive, Taleb H. Al-Tel
Summary: We report the discovery of a new class of potent antimicrobial compounds effective against Gram-positive bacteria, including MRSA. These compounds exhibit low minimum inhibitory concentrations and rapid killing ability, without inducing bacterial resistance. Furthermore, they show minimal toxicity to human red blood cells. The study suggests that these small molecules hold promise as new antibacterial agents against MRSA infections.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Chemistry, Medicinal
Onanong Vorasin, Khanchyd Momphanao, Praewpan Katrun, Chutima Kuhakarn, Chutima Jiarpinitnun
Summary: The study identified a range of potential antibacterial vinyl sulfone derivatives, with nitrile-substituted vinyl phenyl sulfones showing the strongest activity and potentially functioning through sulfhydryl conjugation. Additionally, these compounds could also affect host cell adhesion, suggesting promising therapeutic potential for S. aureus and MRSA.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Mayara A. R. Garcia, Reinaldo S. Theodoro, Janaina C. O. Sardi, Mariana B. Santos, Gabriela M. Ayusso, Fernando R. Pavan, Alan R. Costa, Lucas M. Santa Cruz, Pedro L. Rosalen, Luis O. Regasini
Summary: The designed and synthesized 4-bromo-3'-aminochalcone (5f) demonstrated potent antibacterial activity against methicillin-susceptible and methicillin-resistant Staphylococcus aureus, with potential for biofilm reduction and new applications as an antibacterial agent.
BIOORGANIC CHEMISTRY
(2021)
Article
Infectious Diseases
Helio S. Sader, Cecilia G. Carvalhaes, Rodrigo E. Mendes
Summary: The study evaluated the antimicrobial activity of Ceftaroline against Staphylococcus aureus isolated from patients with infective endocarditis. Ceftaroline demonstrated potent in vitro activity against a large collection of S. aureus isolates recovered from patients with bloodstream infections, including IE. Ceftaroline susceptibility rates were higher in North America and LATAM-APAC compared to Europe.
INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES
(2021)
Article
Biochemistry & Molecular Biology
Chunling Wei, Peiwu Cui, Xiangqian Liu
Summary: Antibacterial resistance is a serious global health problem, and scientists are focusing on developing new antibacterial drugs from natural products. This study investigated the antibacterial activity and mechanism of madecassic acid (MA), a compound isolated from Chinese medicine. It was found that MA had inhibitory effects on eight pathogenic bacteria, with a minimum inhibitory concentration of 31.25μg/mL for Staphylococcus aureus.
Article
Chemistry, Multidisciplinary
Vinicius C. Rocha, Rayssa A. Cajas, Allan I. Andrade-de-Siqueira, Roberto B. P. Almeida, Julia Godoy-Silva, Marina M. Goncalves, Joao Henrique G. Lago, Josue de Moraes
Summary: This study identifies dehydrodieugenol B from the Brazilian Nectandra leucantha plant as a potential treatment for schistosomiasis, showing superior efficacy compared to praziquantel in early stage infections.
Article
Biochemistry & Molecular Biology
Yunxing Fu, Chunqing Leng, Yuan Fan, Xia Ma, Xianghui Li, Xuefei Wang, Zhenghuan Guo, Xiujun Wang, Ruofeng Shang
Summary: DPTM, a new pleuromutilin derivative, showed potent antibacterial activity against MRSA and promoted wound healing in a murine skin infection model. It also decreased the secretion of inflammatory cytokines IL-6 and TNF-alpha in plasma. These results highlight the potential of DPTM as a novel antibacterial agent.
Article
Microbiology
Min Ju, Thushinari Joseph, Nopakorn Hansanant, Mengxin Geng, McKinley Williams, Andrew Cothrell, Andrew Riley Buhrow, Frank Austin, Leif Smith
Summary: The Mu1140 analogs, K2A and R13A, have shown superior efficacy in treating MRSA infections compared to native Mu1140 or vancomycin. These analogs bind to the cell wall precursor lipid II, block cell wall synthesis, and disrupt bacterial membranes. They may provide a future alternative for treating serious Gram-positive bacterial infections.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Chemistry, Medicinal
Yu Deng, Yang Zhang, Xiao-Hu Chen, Cheng-Hong Li
Summary: Growing antibiotic resistance has created an urgent need for new antibiotics. The synthesis of novel pleuromutilin derivatives with a 4(3H)-quinazolinone scaffold or its analogues was reported. Furthermore, structure-activity relationship studies revealed the importance of substituted positions on the scaffold for improving antibacterial activity. Compound 23 showed the best in vitro antibacterial activity against MRSA and low cytotoxicity to cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Infectious Diseases
Katarzyna Kosznik-Kwasnicka, Natalia Kazmierczak, Lidia Piechowicz
Summary: Biofilms are complex structures composed of bacterial cells embedded in extracellular polymeric substances (EPS). They are difficult to eradicate and bacteriophages have shown to penetrate the matrix and reach the bacterial cells. However, biofilm regrowth and phage-resistant bacteria are concerns. The combination of staphylococcal phages and lactoferrin, a protein with anti-biofilm properties, accelerates the anti-biofilm effect and prevents biofilm re-growth, showing potential use in medical settings for biofilm eradication procedures.
Article
Nanoscience & Nanotechnology
Yujie Gao, Yuanhao Dong, Yubin Cao, Wenlong Huang, Chenhao Yu, Shangyan Sui, Anchun Mo, Qiang Peng
Summary: The study found that graphene oxide (GO) has superior antibacterial performance against methicillin-resistant Staphylococcus aureus (MRSA) at low concentrations and exhibits dose-dependent anti-MRSA effect. The GO-MRSA interaction provides fundamental support for antibacterial mechanisms, including cleavage and encapsulation effects. In conclusion, GO nanosheets may be a promising antimicrobial agent against MRSA.
JOURNAL OF BIOMEDICAL NANOTECHNOLOGY
(2021)
Article
Chemistry, Organic
Fan Yang, Bao-Jun Su, Ya-Jie Hu, Jin-Long Liu, Hua Li, Ya-Qi Wang, Hai-Bing Liao, Dong Liang
Summary: Novel cycloneolignane enantiomers and related neolignanes were isolated from Piper hancei stems, showing significant inhibitory effects on nitric oxide secretion and downregulation of inflammatory gene expression in BV-2 microglial cells.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Viktoria Rungelrath, Frank R. DeLeo
Summary: Staphylococcus aureus is a major cause of bacterial infections worldwide, with resistance to antibiotics and the ability to evade host defenses. Research has identified certain virulence molecules of S. aureus as therapeutic targets. Treatment options for methicillin-resistant S. aureus are limited, highlighting the need for further research to develop new therapies.
ANTIOXIDANTS & REDOX SIGNALING
(2021)
Article
Agricultural Engineering
Jingwen Sun, Yu Xie, Zhiyuan Chen, Yipin Fan, Yunfeng Liu, Qi Gao, Jianqiang Li, Jingwen Bai, Yu Yang
Summary: Magnolia officinalis root extract was found to inhibit the growth of MRSA by damaging its cell wall and membrane. The study also showed that the extract interfered with MRSA's carbohydrate metabolism by binding to the mannose transporter (ManP). These findings suggest that ManP could be a potential target for combating MRSA infections.
INDUSTRIAL CROPS AND PRODUCTS
(2023)
Article
Polymer Science
Giovanna Amaral Filipe, Victoria Akemi Itakura Silveira, Marcelly Chue Goncalves, Rayanne R. Beltrame Machado, Celso Vataro Nakamura, Cristiani Baldo, Suzana Mali, Renata Katsuko Takayama Kobayashi, Maria Antonia P. Colabone Celligoi
Summary: This study aims to develop biodegradable films based on cassava starch, pullulan, and sophorolipids for the treatment of skin infections. By adding sophorolipids and citric acid, the properties of the films were modified, resulting in antimicrobial effects. The results of the study show that these films can inhibit the growth of common skin pathogens.
Article
Polymer Science
Flavia Amanda Pedroso de Morais, Ana Carolina Vieira De Oliveira, Rodolfo Bento Balbinot, Danielle Lazarin-Bidoia, Tania Ueda-Nakamura, Sueli de Oliveira Silva, Katieli da Silva Souza Campanholi, Ranulfo Combuca da Silva Junior, Renato Sonchini Goncalves, Wilker Caetano, Celso Vataru Nakamura
Summary: Biotin, spermine, and folic acid were covalently linked to the F127 copolymer to form a drug delivery system for treating B16F10 cells with HY-loaded PDT. Spectroscopy and spectrophotometric techniques were used to analyze the chemical structures and binders quantification. The hydrophobicity of the binders was found to affect the physicochemical parameters such as critical micelle concentration, critical micelle temperature, size, polydispersity, and zeta potential. The modification with spermine resulted in less changes in the physical and chemical parameters of the micelles.
Article
Biochemistry & Molecular Biology
Elisa Parcero Hernandes, Danielle Lazarin-Bidoia, Raquel Dosciatti Bini, Celso Vataru Nakamura, Luiz Fernando Cotica, Sueli De Oliveira Silva Lautenschlager
Summary: In this study, the in vitro effects of iron-oxide magnetic nanoparticles conjugated with the antitumor drug doxorubicin on human breast cancer cells were evaluated. The results showed that these nanoparticles induced cellular redox imbalance and oxidative stress, leading to DNA damage, lipid peroxidation, cell membrane disruption, and loss of mitochondria potential in MCF-7 cells. The association of iron-oxide nanoparticles and doxorubicin may be a potential candidate for anticancer therapy.
Article
Biochemistry & Molecular Biology
Regina G. G. Dare, Elayaraja Kolanthai, Craig J. J. Neal, Yifei Fu, Sudipta Seal, Celso V. V. Nakamura, Sueli O. S. Lautenschlager
Summary: Exposure to ultraviolet radiation can cause photodamage to cellular macromolecules, leading to photoaging and photocarcinogenesis. Cerium oxide nanoparticles (CNPs) exhibit antioxidant activity due to their enzyme-like properties. This study aimed to synthesize CNPs associated with tannic acid (TA) and investigate their photoprotective effects in UVB-exposed L929 fibroblasts.
Article
Biochemistry & Molecular Biology
Aline Pinto Zani, Caroline Pinto Zani, Zia Ud Din, Edson Rodrigues-Filho, Tania Ueda-Nakamura, Francielle Pelegrin Garcia, Sueli de Oliveira Silva, Celso Vataru Nakamura
Summary: In this study, a new synthetic compound A3K2A3 was found to have anti-tumor activity against cervical cancer cells. The potential mechanism of action includes regulation of redox balance, damage to cell membrane and DNA, and inhibition of cell division leading to apoptosis. These findings suggest that A3K2A3 could be a promising alternative for the treatment of cervical cancer.
Article
Virology
Thalita Zago Oliveira, Dyenefer Pereira Fonseca, Andre Henrique dos Santos, Thays Rosa da Silva, Danielle Lazarin-Bidoia, Zia Ud Din, Benedito Prado Dias Filho, Celso Vataru Nakamura, Edson Rodrigues-Filho, Tania Ueda-Nakamura
Summary: We report the in vitro anti-HSV-1 activity of two dibenzylideneketone compounds, DBK1 and DBK2, for the first time. DBK1 demonstrated virucidal activity and caused morphological changes in the HSV-1 envelope. DBK2 reduced HSV-1 plaque size in vitro. The DBKs are promising anti-HSV-1 candidates due to their low toxicity and ability to exert an antiviral effect at the early stages of HSV-1-host cell interaction.
ARCHIVES OF VIROLOGY
(2023)
Article
Biochemistry & Molecular Biology
Alex Graca Contato, Vanessa Kaplum, Debora Botura Scariot, Francielle Pelegrin Garcia, Hugo Falzirolli, Fabio Vandresen, Tania Ueda-Nakamura, Sueli de Oliveira Silva, Cleuza Conceicao da Silva, Celso Vataru Nakamura
Summary: Leishmaniasis is a tropical disease that affects approximately 1.3 million people annually. Current treatments for this disease have dangerous side effects. This study discovered that a limonene-acylthiosemicarbazide compound (ATZ-S-04) shows promising antiproliferative activity against Leishmania parasites and affects their morphology.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Biochemistry & Molecular Biology
Caroline Pinto Zani, Aline Pinto Zani, Cristiane Melissa Thomazini, Karina Miyuki Retamiro, Aline Rufino de Oliveira, Debora Lais Goncalves, Maria Helena Sarragiotto, Francielle Pelegrin Garcia, Sueli de Oliveira Silva, Celso Vataru Nakamura, Tania Ueda-Nakamura
Summary: In this study, the cytotoxic potential and mechanism of action of a compound called BCP-1 were analyzed in breast cancer cells and non-tumor breast cells. The results showed that BCP-1 inhibited cancer cell proliferation, induced cell cycle arrest and oxidative stress, and activated apoptosis and autophagy pathways. BCP-1 also demonstrated antimetastatic potential.
Review
Chemistry, Medicinal
Naiara Cassia Gancedo, Raquel Isolani, Natalia Castelhano de Oliveira, Celso Vataru Nakamura, Daniela Cristina de Medeiros Araujo, Andreia Cristina Conegero Sanches, Fernanda Stumpf Tonin, Fernando Fernandez-Llimos, Danielly Chierrito, Joao Carlos Palazzo de Mello
Summary: This study aimed to synthesize the anticancer and anti-proliferative potential of Limonium species through a systematic review. The results indicate that Limonium species have the potential to be a source of new potential cytotoxic and anticancer agents. However, further research and improved experimental designs are needed to better understand the mechanism of action of these compounds.
Article
Integrative & Complementary Medicine
Carla Maria Mariano Fernandez, Sirlene Adriana Kleinubing, Thaysa Ksiaskiewcz Karam, Fabiana Brusco Lorenzetti, Carolina Trevisolli Palomo, Byanca Pereira Moreira de Oliveira, Odinei Hess Goncalves, Zilda Cristiani Gazim, Mariza Barion Romagnolo, Katiany Rizzieri Caleffi-Ferracioli, Regiane Bertin de Lima Scodro, Marli Miriam de Souza Lima, Tania Ueda Nakamura, Celso Vataru Nakamura, Benedito Prado Dias Filho
Summary: The present study aimed to develop and characterize solid lipid nanoparticles (SLN-CEPc) and chitosan-coated solid lipid nanoparticles (C-SLN-CEPc) loaded with crude extract of Piper corcovadensis roots. Both formulations showed high encapsulation efficiency, formed a monodispersed system with small and spherical particles, and exhibited promising antimycobacterial activity against Mycobacterium tuberculosis H37Rv. The cytotoxicity testing on Vero cells also indicated low toxicity. The study suggests the potential of nanoencapsulation for the development of new products.
BOLETIN LATINOAMERICANO Y DEL CARIBE DE PLANTAS MEDICINALES Y AROMATICAS
(2023)
Article
Biochemistry & Molecular Biology
Flavia Amanda Pedroso de Morais, Rodolfo Bento Balbinot, Amanda Beatriz Kawano Bakoshi, Danielle Lazarin-Bidoia, Katieli da Silva Souza Campanholi, Ranulfo Combuca da Silva Junior, Renato Sonchini Goncalves, Tania Ueda-Nakamura, Sueli de Oliveira Silva, Wilker Caetano, Celso Vataru Nakamura
Summary: The study developed biomodified coated-lipid vesicles with the photosensitizer hypericin (HY) incorporated. The results demonstrated good stability, low tendency to form complexes with proteins, and promising photodynamic potential. These nanosystems hold potential for future therapeutic and diagnostic applications.
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
(2023)
Article
Chemistry, Medicinal
Jose Rivaldo dos Santos Filho, Rodolfo Bento Balbinot, Celso Vataru Nakamura, Juliana Cristina Castro, Everton da Silva Santos, Jose Eduardo Goncalves, Giani Andrea Linde, Nelson Barros Colauto, Regina Aparecida Correia Goncalves, Arildo Jose Braz de Oliveira
Summary: This study aims to investigate the antileishmanial activity of lipid fractions from mushrooms against Leishmania amazonensis and found that the lipid crude extract and fractions have inhibitory effects on the parasite and are more selective towards the host cells. These results provide a significant basis for further research on the potential use of these fractions in the treatment of leishmaniasis.
REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY
(2023)