Article
Microbiology
Yaoguang Zhang, Jian Chen, Hao Pan, Xiaojiang Ma, Li Jiang, Qian Zhu, Huanyu Wu, Zhenyu Wang
Summary: In this study, a triplex real-time quantitative PCR assay was developed for the simultaneous differential detection of three protozoan parasites in the human intestinal tract. The assay showed high sensitivity, specificity, and repeatability, and demonstrated good practical application value in fecal samples from patients with diarrhea.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Public, Environmental & Occupational Health
Tanja E. Peters, Benno Kreuels, Marylyn M. Addo, Egbert Tannich, Camilla Rothe
Summary: This study analyzed 339 cases of returning travellers with confirmed giardiasis between 2007 and 2016 in Hamburg, Germany, finding a significantly higher risk of treatment failure with metronidazole for patients returning from South Asia. Second-line treatment regimens showed inconsistency and unsatisfactory results, suggesting a need for reevaluation of treatment strategies for giardiasis. Prospective trials are urgently needed to assess new first-line treatment options and improve second-line treatment strategies.
TRAVEL MEDICINE AND INFECTIOUS DISEASE
(2021)
Review
Biochemistry & Molecular Biology
Antonio Moreno-Herrera, Sandra Cortez-Maya, Virgilio Bocanegra-Garcia, Bimal Krishna Banik, Gildardo Rivera
Summary: Parasitic infections caused by various protozoa affect millions of people worldwide annually, with limited pharmacological treatments. Developing new and more effective drugs could be crucial in improving therapy outcomes for parasitic diseases.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Somayeh Behrouz, Mohammad Navid Soltani Rad, Zahra Ganji, Marzieh Behrouz, Elham Zarenezhad, Mahmoud Agholi
Summary: This study describes the design, synthesis, and evaluation of new propargylamine derivatives containing a 2-methyl-5-nitroimidazole core. The propargylamines were efficiently synthesized through a three-component reaction and their antigiardial activity was investigated. Compound 2b exhibited potent antigiardial activity. In addition, in silico analysis was performed to assess the physicochemical properties and docking interactions of the compounds.
Article
Infectious Diseases
Amber N. Barnes, Anu Davaasuren, Uyanga Baasandavga, Paul M. Lantos, Battsetseg Gonchigoo, Gregory C. Gray
Summary: The study found that zoonotic enteric parasites Cryptosporidium spp. and Giardia duodenalis are present in human, animal, fly, and water samples in different regions of Mongolia. Risk factors for parasite exposure include drinking water source, access to indoor handwashing site, rural location, and animal ownership. Public health efforts should focus on water, sanitation and hygiene measures, and One Health collaboration between human and animal health sectors.
PLOS NEGLECTED TROPICAL DISEASES
(2021)
Article
Immunology
Xia Li, Meng Feng, Yanqing Zhao, Yuhan Zhang, Ruixue Zhou, Hang Zhou, Zhen Pang, Hiroshi Tachibana, Xunjia Cheng
Summary: Macrophages play a crucial role in combating amoebiasis by releasing pro-inflammatory cytokines in response to infection. Entamoeba histolytica can activate the NLRP3 inflammasome through secretion of peroxiredoxins during interaction with host cells, potentially offering a novel therapeutic approach for this global threat.
FRONTIERS IN IMMUNOLOGY
(2021)
Article
Chemistry, Medicinal
Maritza Velasquez-Torres, Jose Guadalupe Trujillo-Ferrara, Marycarmen Godinez-Victoria, Rosa Adriana Jarillo-Luna, Victor Tsutsumi, Virginia Sanchez-Monroy, Araceli Posadas-Mondragon, Roberto Issac Cuevas-Hernandez, Jose Angel Santiago-Cruz, Judith Pacheco-Yepez
Summary: This study demonstrates for the first time the in vitro and in silico anti-amoebic activity of riluzole, showing that it reduces the viability of Entamoeba histolytica and induces cell death. It also suggests that riluzole has a higher affinity than metronidazole for the antioxidant enzymes of the parasite. Further research should be conducted to confirm the anti-amoebic effects of riluzole in vivo.
Article
Multidisciplinary Sciences
Caterine Potes-Morales, Maria del Pilar Crespo-Ortiz
Summary: The study aimed to determine the prevalence of intestinal parasites in a young adult population and their pets. The results showed a high prevalence of parasitism and polyparasitism among university students, suggesting exposure to parasite-infected animals and contaminated environments. Pets were also found to be carriers of parasitic infections.
Article
Microbiology
Elena Chiappini, Teresa Paba, Matilde Bestetti, Luisa Galli
Summary: Parasitic infections are prevalent in internationally adopted children, and an accurate evaluation protocol is needed.
Article
Microbiology
Alejandro Dashti, Henar Alonso, Cristina Escolar-Minana, Pamela C. Koster, Begona Bailo, David Carmena, David Gonzalez-Barrio
Summary: Thorough independent assessment of the diagnostic performance of novel diagnostic assays is essential. In this study, the VIASURE Cryptosporidium, Giardia, & E. histolytica real-time PCR assay was evaluated for its performance in detecting and identifying enteric protozoan parasites. The assay demonstrated good performance for routine testing in clinical microbiological laboratories.
MICROBIOLOGY SPECTRUM
(2022)
Article
Biotechnology & Applied Microbiology
Abhishek Mewara, Sandhya Khunger, Chayan Sharma, Sivanantham Krishnamoorthi, Shreya Singh, Rakesh Yadav, Sumeeta Khurana, Rakesh Sehgal
Summary: We developed a rapid mLAMP assay for early detection of common intestinal parasites-Entamoeba histolytica and Giardia duodenalis. The assay has a fast reaction time and excellent sensitivity and specificity.
LETTERS IN APPLIED MICROBIOLOGY
(2023)
Article
Multidisciplinary Sciences
Aldian Amaruddin, Jan Pieter R. Koopman, Munawir Muhammad, Kaatje Lenaerts, Hans M. H. van Eijk, Eric A. T. Brienen, Anoecim R. Geelen, Lisette van Lieshout, Sitti Wahyuni, Ed J. Kuijper, Romy D. Zwittink, Firdaus Hamid, Erliyani Sartono, Maria Yazdanbakhsh
Summary: Intestinal helminths are highly prevalent in low-SES children in Indonesia and can contribute to poor health outcomes by affecting the gut microbiome and gut barrier function. Treatment with albendazole can reduce helminth infections and improve gut permeability, but only in children without helminth infections.
SCIENTIFIC REPORTS
(2022)
Article
Microbiology
Laura Morales-Luna, Abigail Gonzalez-Valdez, Beatriz Hernandez-Ochoa, Roberto Arreguin-Espinosa, Daniel Ortega-Cuellar, Rosa Angelica Castillo-Rodriguez, Victor Martinez-Rosas, Noemi Cardenas-Rodriguez, Sergio Enriquez-Flores, Luis Miguel Canseco-avila, Veronica Perez de la Cruz, Fernando Gomez-Chavez, Saul Gomez-Manzo
Summary: Giardia lamblia is a early divergent single-celled eukaryotic parasite, and its fused enzyme G6PD::6PGL is a bifunctional enzyme that catalyzes the first two steps of the PPP with higher efficiency than individual proteins. The final metabolites of the catalytic reaction of G6PD::6PGL are identified as 6-phosphoglucono-delta-lactone and 6-phosphogluconate. Therefore, G6PD::6PGL is a potential drug target for the rational synthesis of novel anti-Giardia drugs.
Article
Biochemistry & Molecular Biology
Tamara Smutna, Alena Dohnalkova, Robert Sutak, Ravi Kumar Narayanasamy, Jan Tachezy, Ivan Hrdy
Summary: This study discovered a previously unknown hydrogenase in the cytosol of T. vaginalis, which can use cytochrome b5 as an electron acceptor. Trichomonads with overexpressed cytosolic hydrogenase showed decreased hydrogen excretion and increased excretion of methylated alcohols, suggesting that the cytosolic hydrogenase uses hydrogen gas as a source of reducing power for cytoplasmic reactions.
Article
Microbiology
Shun-Xian Zhang, David Carmena, Cristina Ballesteros, Chun-Li Yang, Jia-Xu Chen, Yan-Hong Chu, Ying-Fang Yu, Xiu-Ping Wu, Li-Guang Tian, Emmanuel Serrano
Summary: The study found that in Tengchong City, Yunnan Province, infection rates of Cryptosporidium spp., Entamoeba histolytica, Giardia duodenalis, and Blastocystis sp. were relatively high, but most infections were asymptomatic, and co-infections were usually purely random.
Article
Engineering, Chemical
Sadaf Aiman Khan, Marut Jain, Kamal Kishore Pant, Zyta Maria Ziora, Mark A. T. Blaskovich
Summary: Methylparaben (MeP) is a serious water pollutant in cosmetic industry effluents, but a hybrid catalyst of silver nanoparticles on reduced graphene oxide (rGO/AgNPs) fabricated using a green reducing agent showed significantly enhanced photocatalytic degradation efficiency of MeP. The conditions influencing the degradation kinetics were comprehensively studied using response surface methodology. The nanocomposite exhibited high stability and potential for multiple cycles of use, providing new insights into the development of low-cost photocatalysts for cosmetic wastewater treatment.
INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Ramar Perumal Samy, Stephen P. P. Mackessy, Alagarmalai Jeyasankar, Mano Ranjana Ponraj, Octavio Luiz Franco, Matthew A. A. Cooper, Matheswaran Kandasamy, Tapan Kumar Mohanta, Jebasingh Bhagavathsingh, Sakthivel Vaiyapuri
Summary: PaTx-II, an active component from the venom of the Mulga Snake, showed potent antimicrobial activity and promoted wound healing.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biotechnology & Applied Microbiology
Mark S. Butler, Ian R. Henderson, Robert J. Capon, Mark A. T. Blaskovich
Summary: The global need for new antibacterial drugs to combat drug-resistant bacterial infections is receiving significant attention, leading to numerous funding, policy, and legislative initiatives to support antibacterial research and development. This review assesses the impact of these programs by analyzing the clinical development of various types of antibacterial drugs and the number of drug approvals in recent years. The findings show an increasing number of early-stage candidates and a presence of novel antibacterial compounds, particularly targeting Gram-negative bacteria.
JOURNAL OF ANTIBIOTICS
(2023)
Article
Chemistry, Multidisciplinary
Anton A. Galochkin, Vladimir V. Baranov, Karl A. Hansford, Louise I. M. Friberg, Elena D. Strel'tzova, Egor S. Lipatov, Yulia V. Nelyubina, Angelina N. Kravchenko
Summary: A synthetic method for the preparation of selenoglycolurils was reported, where unsubstituted, 1-substituted, and 1,3-disubstituted thioglycolurils were transformed into isothiouronium salts through S-methylation with MeI (Step 1), followed by selenation with in situ generated NaHSe (Step 2). The selenoglycolurils showed potent antifungal activity against Candida albicans and Cryptococcus neoformans (MIC 0.25-0.125 μg/mL) without causing toxicity to mammalian cells, highlighting the unique role of organoselenium compounds as novel antifungal agents.
Review
Chemistry, Multidisciplinary
Angelo Frei, Anthony D. D. Verderosa, Alysha G. G. Elliott, Johannes Zuegg, Mark A. T. Blaskovich
Summary: Metal ions have antimicrobial activity and are considered as potential new antibiotics. Metal complexes can also be used for antimicrobial photodynamic therapy and radionuclide diagnosis of bacterial infections.
NATURE REVIEWS CHEMISTRY
(2023)
Article
Biology
Bing Zhang, Wanida Phetsang, M. Rhia L. Stone, Sanjaya Kc, Mark S. S. Butler, Matthew A. A. Cooper, Alysha G. G. Elliott, Urszula Lapinska, Margaritis Voliotis, Krasimira Tsaneva-Atanasova, Stefano Pagliara, Mark A. T. Blaskovich
Summary: Antimicrobial resistance is a critical concern for human health, and this study presents the development of vancomycin fluorescent probes that can be used for detecting and visualizing Gram-positive bacteria as well as for measuring outer membrane permeabilization in Gram-negative bacteria. The probes were synthesized by modifying vancomycin with an azide substituent, enabling it to undergo copper-catalyzed azide-alkyne cycloaddition reactions. The probes exhibited similar antibacterial profiles to the parent vancomycin antibiotic and were versatile tools for various detection and imaging techniques.
COMMUNICATIONS BIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Annick van Niekerk, M. Cassiem Joseph, Angela Kavanagh, Hue Dinh, Andrew J. Swarts, Selwyn F. Mapolie, Johannes Zuegg, Amy K. Cain, Alysha G. Elliott, Mark A. T. Blaskovich, Angelo Frei
Summary: Infections associated with antibiotic resistance (AMR) are projected to become the leading cause of death in the coming decades due to over-prescription of antibiotics and a lack of new drug development. A community-driven initiative, Community for Open Antimicrobial Drug Discovery (CO-ADD), has identified metal-based drugs as a potential and untapped source for combating AMR. Testing of 18 palladium (Pd) and ruthenium (Ru) complexes has revealed that Pd complexes, particularly Pd1, exhibit potent antifungal activity against Candida glabrata. Furthermore, in-vivo studies in Galleria mellonella larvae have demonstrated the non-toxic nature of these compounds.
Article
Chemistry, Physical
Joanna Bojarska, Martin Breza, Milan Remko, Ye Yuan, Zyta M. Ziora, Tsun-Thai Chai, Izabela D. Madura, Krzysztof Kaczmarek, Mark A. T. Blaskovich, Wojciech M. Wolf
Summary: A supramolecular behavior of a newly synthesized compound and a library of tetrazole-based H-bonding synthons were studied by X-ray crystallography and computational techniques. The supramolecular assembly was controlled by various interactions, including O...H, N...H, C...H, and pi-stacking interactions. The 3D topologies of the supramolecular architectures were visualized and dispersion forces played a crucial role. Quantum-chemical treatment revealed the chemical activity and stability of the compound. These findings provide valuable information for the design of therapeutic agents containing tetrazole motifs.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Plant Sciences
Rachel Chen, Scott A. Minns, John A. Kalaitzis, Mark S. Butler, Maira Rosin, Daniel Vuong, Soo Sum Lean, Yit-Heng Chooi, Ernest Lacey, Andrew M. Piggott
Summary: Researchers discovered TuronicinA (1) from Streptomyces sp. MST-123921 in soil, which showed potent antimicrobial activity against fungi and bacteria without cytotoxicity to human cells.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Chemistry, Medicinal
Nhan T. Pham, Joana Alves, Fiona A. Sargison, Reiko Cullum, Jan Wildenhain, William Fenical, Mark S. Butler, David A. Mead, Brendan M. Duggan, J. Ross Fitzgerald, James J. La Clair, Manfred Auer
Summary: Antimicrobial resistance is a global public health threat, and finding new therapeutics to treat infections caused by multi-drug resistant bacteria is urgent. This study presents a fluorescence imaging assay to monitor macrophage infection by S. aureus, which can help identify potential antibiotics. The assay combined with nanoscaled chemical analyses led to the discovery of a new active rifamycin analogue. This finding offers a promising approach for identifying antimicrobial compounds with intracellular activity in macrophages.
ACS INFECTIOUS DISEASES
(2023)
Review
Biochemistry & Molecular Biology
Angela A. Salim, Mark S. Butler, Mark A. T. Blaskovich, Ian R. Henderson, Robert J. Capon
Summary: This review summarizes all natural products (500 compounds, including 17 semi-synthetic derivatives) reported in the primary literature up to December 2022 that have been shown to inhibit the egg hatching, motility, larval development, and/or survival of helminths (nematodes, flukes, and tapeworms). These parasites infect and harm the health, welfare, productivity, and lives of commercial livestock, companion animals, and other valuable, endangered, and exotic animals. The review focuses on chemical structures, source organisms, and anthelmintic properties, including the target species, animal hosts, and potency measures used in bioassays.
NATURAL PRODUCT REPORTS
(2023)
Review
Biochemistry & Molecular Biology
Beth Rayner, Anthony D. Verderosa, Vito Ferro, Mark A. T. Blaskovich
Summary: Antimicrobial resistance poses a global threat due to the rise of multi-drug resistant bacteria and the lack of new antibiotics. The 'Trojan horse' approach, which uses bacteria's iron transport system to deliver antibiotics, shows promise in combating this issue. The use of siderophore antibiotic conjugates, such as cefiderocol, has proven to be effective against resistant bacteria. This review discusses recent advancements in these conjugates and the challenges in their design for more efficacious therapies.
RSC MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Alice Yuan, Hayley Fong, Jennifer V. Nguyen, Sophia Nguyen, Payton Norman, Reiko Cullum, William Fenical, Anjan Debnath
Summary: A study found that oligomycin D, a metabolite derived from marine microbes, exhibits high potency in inhibiting Naegleria fowleri, a free-living ameba that causes brain infection. Oligomycin D was found to be more potent than traditional drugs and showed fast-acting properties. Additionally, a natural peptide leucinostatin was identified as another potent compound against N. fowleri.
ACS INFECTIOUS DISEASES
(2023)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)