Article
Biochemistry & Molecular Biology
Henoc del Rosario, Ester Saavedra, Ignacio Brouard, Daniel Gonzalez-Santana, Celina Garcia, Elena Spinola-Lasso, Carlos Tabraue, Jose Quintana, Francisco Estevez
Summary: Synthetic flavonoids with new substitution patterns show potential as anticancer drugs. In this study, twelve chalcones were synthesized and their antiproliferative effects on human tumour cells were evaluated. The most cytotoxic chalcones contained a furoyl substituent linked by an ester or an amide through the 2'-hydroxy or the 2'-amino group of the chalcone skeleton. The synthetic chalcone 2'-furoyloxy-4-methoxychalcone (FMC) displayed higher potency than the antineoplastic agent etoposide and had less toxicity on normal blood cells. The mechanism of action involved cell cycle arrest, induction of apoptosis, and inhibition of tubulin polymerization, and depended on the generation of reactive oxygen species.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Congjun Xu, Zhanghong Xiao, Jing Wang, Hualu Lai, Tao Zhang, Zilin Guan, Meng Xia, Meixu Chen, Lingling Ren, Yuanfeng He, Yuqi Gao, Chunshun Zhao
Summary: Through stepwise structure optimization, a potent and selective ferroptosis inducer targeting GPX4 was developed, showing significant induction of ferroptosis at cellular level and restrained tumor growth in a mouse xenograft model without obvious toxicity.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Physical
Suresh Kumar, Bhavna Saroha, Gourav Kumar, Ekta Lathwal, Sanjeev Kumar, Badri Parshad, Meena Kumari, Naveen Kumar, Mabel M. Mphahlele-Makgwane, Peter R. Makgwane
Summary: The dynamic growth in green organic synthetic methodologies for diverse heterocyclic scaffolds has substantially contributed to the field of medicinal chemistry. The use of hybrid metal nanocatalysts is a benign strategy for ensuring the advancement of modern synthetic chemistry and adhering to the principles of green chemistry. This review will summarize different metal nanocatalysts for the efficient green synthesis of various heterocycles.
Review
Biochemistry & Molecular Biology
Anna-Maria Lazaratos, Matthew G. Annis, Peter M. Siegel
Summary: GPNMB plays an immunosuppressive role in cancer by promoting tumor growth and metastasis, and its expression is associated with poor prognosis. It regulates cancer progression by restraining immune responses.
Article
Plant Sciences
Huanhuan Xu, Yanping Lan, Jiayi Xing, Yi Li, Lecheng Liu, Yongqin Wang
Summary: This study elucidates the function of chalcone isomerase genes in Allium fistulosum and provides new insights into improving the synthesis efficiency of naringenin.
FRONTIERS IN PLANT SCIENCE
(2022)
Article
Chemistry, Medicinal
Fatma Fouad Hagar, Samar H. Abbas, Dalia Abdelhamid, Hesham A. M. Gomaa, Bahaa G. M. Youssif, Mohamed Abdel-Aziz
Summary: A series of new 1,3,4-oxadiazole-chalcone/benzimidazole hybrids were synthesized and investigated for their antiproliferative activities. Compounds 9g-i and their oxygen isosteres, 10f-h, exhibited promising antiproliferative activities with IC50 values ranging from 0.80 to 2.27 μM.
ARCHIV DER PHARMAZIE
(2023)
Review
Oncology
Cemre Ucaryilmaz Metin, Gulnihal Ozcan
Summary: Hypoxia plays a crucial role in the heterogeneity of tumors, and HIF-1 alpha reinforces cancer hallmarks and enhances the aggressiveness of cancer cells in hypoxic niches. However, the understanding of the role of HIF-1 alpha in gastric cancer is limited, highlighting the need for further research.
Article
Immunology
Niura Madalena Bila, Caroline Barcelos Costa-Orlandi, Carolina Orlando Vaso, Jean Lucas Carvalho Bonatti, Leticia Ribeiro de Assis, Luis Octavio Regasini, Carla Raquel Fontana, Ana Marisa Fusco-Almeida, Maria Jose Soares Mendes-Giannini
Summary: The study evaluated the efficacy of 2-hydroxychalcone in anti-dermatophytic and anti-biofilm activity, demonstrating its inhibitory effects on early-stage and mature biofilms and enhanced efficacy under photodynamic therapy. Furthermore, 2-hydroxychalcone targets ergosterol, promotes the generation of reactive oxygen species, and induces fungal cell death by apoptosis and necrosis.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Mohammad Murwih Alidmat, Melati Khairuddean, Naziera Mohammad Norman, Anis Nasihah Mohamed Asri, Mohd Hisyam Mohd Suhaimi, Garima Sharma
Summary: This study synthesized several compounds with anti-malarial activity using the Claisen-Schmidt condensation method, with one compound showing significant anti-proliferative effects against Plasmodium parasites. Molecular docking analysis revealed the potential mechanism of action for these compounds.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Moran Sun, Minghua Yuan, Yingying Kang, Jinling Qin, Yixin Zhang, Yongtao Duan, Longfei Wang, Yongfang Yao
Summary: alpha-Fluorinated chalcones were synthesized and tested for their inhibitory effects on human cancer cell growth. The most potent compound, 4c, demonstrated selective toxicity against cancer cells and disrupted microtubule networks, leading to cell cycle arrest and apoptosis. Furthermore, compound 4c inhibited angiogenesis and metastasis of cancer cells. Overall, chalcone hybrid 4c is a promising anti-cancer agent targeting tubulin assembly.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biotechnology & Applied Microbiology
Hong Wang, Guoxin Jing, Jintong Niu, Li Yang, Youyuan Li, Yi Gao, Huichao Wang, Xiaorong Xu, Yechang Qian, Shilong Wang
Summary: The study introduces a novel supramolecular photosensitizer LDH@ZnPc, capable of triggering pyroptosis while possessing mitochondria anchoring ability, effectively enhancing the antitumor immunity in photodynamic therapy.
JOURNAL OF NANOBIOTECHNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Amal Kamal Abdel-Aziz, Eman M. E. Dokla, Khaled A. M. Abouzid, Saverio Minucci
Summary: This study discovered a novel endoplasmic reticulum (ER) inducer, EMD37, which exhibited potent anticancer activity against NCI-60 cancer cell lines. Genome-wide transcriptome profiling and drug signature mining revealed that EMD37 promoted ER stress and unfolded protein response (UPR) mechanisms. Additionally, EMD37 inhibited mTOR signaling and induced G2/M cell cycle arrest and apoptosis in human cancer cells.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Peng-Chao Huo, Xiao-Qing Guan, Peng Liu, Yun-Qing Song, Meng-Ru Sun, Rong-Jing He, Li-Wei Zou, Li-Juan Xue, Jin-Hui Shi, Nan Zhang, Zhi-Guo Liu, Guang-Bo Ge
Summary: In this study, a series of indanone-chalcone hybrids were designed and synthesized to find potent and highly selective hCES2A inhibitors. Among them, B7 showed the most potent inhibition on hCES2A and excellent specificity. These compounds are potential candidates for the development of novel anti-diarrhea agents to ameliorate irinotecan-induced intestinal toxicity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Environmental Sciences
Mrinal Kashyap, Kanchan Samadhiya, Atreyee Ghosh, Vishal Anand, Hyunju Lee, Naomi Sawamoto, Atsushi Ogura, Yoshio Ohshita, Parasharam M. Shirage, Kiran Bala
Summary: The research focuses on the intracellular biosynthesis of Ag/AgCl nanohybrids in microalgae, Scenedesmus sp., and its effects on cell growth and lipid profile. The study found that the total lipid content of cells remained static during the biosynthesis of Ag/AgCl nanoparticles, and the FAME profile improved. Tests showed that the synthesized nanoparticles exhibited antibacterial efficiency.
ENVIRONMENTAL RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Dongjuan Si, Huijuan Luo, Xiaomeng Zhang, Kundi Yang, Hongmei Wen, Wei Li, Jian Liu
Summary: Inhibition of p53-MDM2 interactions is a promising strategy for cancer treatment. The unsaturated pyrrolidone compound 4h showed good binding affinity with MDM2 and demonstrated excellent antitumor activity by inducing cell cycle arrest and apoptosis. This compound has potential as a novel antitumor agent.
BIOORGANIC CHEMISTRY
(2021)
Article
Neurosciences
Pallavi B. McElroy, Li-Ping Liang, Brian J. Day, Manisha Patel
EXPERIMENTAL NEUROLOGY
(2017)
Article
Biochemistry & Molecular Biology
Pallavi B. McElroy, Ashwini Sri Hari, Brian J. Day, Manisha Patel
JOURNAL OF BIOLOGICAL CHEMISTRY
(2017)
Article
Respiratory System
Brian J. Day, Jie Huang, Briana Q. Barkes, May Gillespie, Li Li, Lisa A. Maier
Article
Biochemistry & Molecular Biology
Jennifer N. Pearson-Smith, Li-Ping Liang, Shane D. Rowley, Brian J. Day, Manisha Patel
NEUROCHEMICAL RESEARCH
(2017)
Article
Toxicology
Reena Berman, Gregory P. Downey, Azzeddine Dakhama, Brian J. Day, Hong Wei Chu
TOXICOLOGICAL SCIENCES
(2018)
Article
Biochemistry & Molecular Biology
Li-Ping Liang, Jennifer N. Pearson-Smith, Jie Huang, Brian J. Day, Manisha Patel
Review
Pharmacology & Pharmacy
Brian J. Day
BIOCHEMICAL PHARMACOLOGY
(2019)
Article
Biochemistry & Molecular Biology
Brian J. Day, Preston E. Bratcher, Joshua D. Chandler, Matthew B. Kilgore, Elysia Min, John J. LiPuma, Robert J. Hondal, David P. Nichols
FREE RADICAL BIOLOGY AND MEDICINE
(2020)
Article
Pharmacology & Pharmacy
Li-Ping Liang, Ruth Fulton, Erica L. Bradshaw-Pierce, Jennifer Pearson-Smith, Brian J. Day, Manisha Patel
Summary: In this study, metalloporphyrin catalytic antioxidants AEOL11207 and AEOL11114 showed significant neuroprotective effects against 6-OHDA-induced neurotoxicity in a rat model of Parkinson disease. The compounds demonstrated gastrointestinal absorption, high plasma concentrations, and ability to penetrate the blood-brain barrier, indicating their potential for disease modification in PD.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2021)
Article
Toxicology
Reena Berman, Elysia Min, Jie Huang, Katrina Kopf, Gregory P. Downey, Kent Riemondy, Harry A. Smith, Cecile S. Rose, Max A. Seibold, Hong Wei Chu, Brian J. Day
Summary: Upon returning from deployment to Afghanistan, a substantial number of U.S. military personnel report symptoms of deploymentrelated lung disease (DRLD) believed to be caused by prolonged inhalation of toxic desert particulate matter. This study using a mouse model demonstrated that inhalation of airborne particulate matter during deployment may prime airways to be more responsive to allergen exposure after returning home, potentially due to dysregulated immune responses.
TOXICOLOGICAL SCIENCES
(2021)
Review
Chemistry, Medicinal
Reena Berman, Cecile S. Rose, Gregory P. Downey, Brian J. Day, Hong Wei Chu
Summary: Approximately 3 million US military personnel and contractors were deployed to Southwest Asia and Afghanistan over the past two decades, and many developed persistent respiratory symptoms upon returning to the US, referred to as deployment-related lung diseases (DRLD). Exposures to high levels of particulate matter are a major factor contributing to DRLD, activating lung immune and structural cells to initiate various cell signaling pathways. Understanding how airborne exposures during deployment contribute to DRLD may help identify effective targets for alleviating respiratory diseases and improving quality of life for veterans and active duty military personnel.
CHEMICAL RESEARCH IN TOXICOLOGY
(2021)
Article
Toxicology
Niccolette Schaunaman, Taylor Crue, Diana Cervantes, Kelly Schweitzer, Harrison Robbins, Brian J. Day, Mari Numata, Irina Petrache, Hong Wei Chu
Summary: This study investigated the effects of electronic cigarette vapor on human distal airway epithelial responses to influenza A virus infection. The results showed that pre-exposure to e-vapor increased the pro-inflammatory response in human distal airways, independently of the severity of cell injury during viral infection.
ARCHIVES OF TOXICOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Brian J. Day, Elysia Min, Jie Huang, Chris Stanley
Summary: The innate immune response to infection can lead to inflammation and oxidative damage, and most anti-inflammatory and antioxidant therapies may further suppress the immune response. This study found that using thiocyanate as the counter anion for cationic manganese porphyrin catalytic antioxidants can enhance their antioxidant spectrum and supplement innate immunity.
Article
Biochemistry & Molecular Biology
Hina Agraval, Taylor Crue, Niccolette Schaunaman, Mari Numata, Brian J. Day, Hong Wei Chu
Summary: The use of electronic cigarettes (ECs) is common among adolescents and young adults, but their limited knowledge about the detrimental effects on lung health is concerning. This study aimed to investigate the effects of ECs on viral infection and the release of TNF-related apoptosis-inducing ligand (TRAIL) in human lung slices. The results suggest that EC exposure amplifies viral infection and TRAIL release, highlighting the importance of appropriate TRAIL levels in controlling viral infection in EC users.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Immunology
Shaan Gellatly, Nicole Pavelka, Taylor Crue, Kelly S. Schweitzer, Brian J. Day, Elysia Min, Mari Numata, Dennis R. Voelker, April Scruggs, Irina Petrache, Hong Wei Chu
JOURNAL OF INFLAMMATION RESEARCH
(2020)