Article
Biochemistry & Molecular Biology
Abdullah G. Al-Sehemi, Mehboobali Pannipara, Rishikesh S. Parulekar, Omkar Patil, Prafulla B. Choudhari, M. S. Bhatia, P. K. Zubaidha, Yasinalli Tamboli
Summary: The main protease (M-pro) of the novel coronavirus is a crucial target for drug development, with potential inhibition of the virus through nitric oxide. Further molecular docking and simulation studies are needed to validate the effectiveness of potential inhibitors.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Biochemistry & Molecular Biology
Abdullah G. Al-Sehemi, Rishikesh S. Parulekar, Mehboobali Pannipara, Manzur P. P. Ali, Pudukulathan K. Zubaidha, Manish S. Bhatia, Tapan Kumar Mohanta, Ahmed Al-Harrasi
Summary: This study utilized in silico screening method and the 3D structure of SARS-CoV-2 M-pro protein to discover potential inhibitor candidates and investigate their interactions with the substrate binding pocket. The findings suggest that certain furoxan derivatives can serve as both NO donor and SARS-CoV-2 M-pro protein inhibitors, offering a dual mechanism of action for the treatment of SARS-CoV-2.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Alexandra D. Voloshina, Anastasiia S. Sapunova, Natalia V. Kulik, Mayya G. Belenok, Irina Yu Strobykina, Anna P. Lyubina, Syumbelya K. Gumerova, Vladimir E. Kataev
Summary: The study found that several ammonium derivatives of diterpenoids steviol and isosteviol exhibited high antibacterial activity against MRSA strains and cytotoxic effects on cancer cell lines. It also showed potential anticancer effects on MCF-7 cells while causing minimal harm to normal cells, indicating promising scaffolds for the development of new antibacterial drugs and anticancer agents targeting mitochondria.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Sin -Min Li, Jia-Yu Chou, Shuo-En Tsai, Ching-Chun Tseng, Cheng-Yen Chung, Wei-Zheng Zeng, Yu-Pei Hu, Naoto Uramaru, Guan-Jhong Huang, Fung-Fuh Wong
Summary: An efficient synthesis method was developed for furoxan/1,2,4-triazole hybrids 5a-k from methyl 5-(halomethyl)-1-aryl-1H-1,2,4-triazole-3-carboxylates 1 through two-steps reaction including hydrolyzation and esterification. The newly synthesized compounds were evaluated for their exogenous NO release ability, in vitro and in vivo anti-inflammatory activity, and in silico predictions. Compound 5f showed extraordinary COX-2 inhibition and selectivity, as well as better inhibition of cytokine and gastric safety compared to Indomethacin. Molecular modeling and in silico predictions identified compound 5f as a potential anti-inflammatory agent with comparable effects to Celecoxib.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Federica Sodano, Elena Gazzano, Barbara Rolando, Elisabetta Marini, Loretta Lazzarato, Roberta Fruttero, Chiara Riganti, Alberto Gasco
Summary: This study investigated a set of hybrid compounds with different nitric oxide (NO) releasing capacities, composed of 3-R-substituted furoxan moieties linked to a mitochondrial probe, rhodamine B. Strong electron-withdrawing groups at the 3-position of the furoxan showed high cytotoxicity likely due to their high NO-releasing properties and ability to inhibit cellular proteins by covalent binding. The most interesting product was identified as the rhodamine hybrid containing 3-SO2C6H5 substituted furoxan moiety, showing high cytotoxicity over the entire concentration range tested.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Pedro Olim, Renato B. Pereira, Maria Jose G. Fernandes, Carolina M. Natal, Jose R. A. Coelho, A. Gil Fortes, M. Sameiro T. Goncalves, David M. Pereira
Summary: Natural products have been identified as a promising source of novel anticancer drugs. This study synthesized and tested over 20 semisynthetic derivatives of compounds belonging to different chemical classes, and found that two derivatives of 6-hydroxyflavanone displayed enhanced cytotoxicity against gastric adenocarcinoma and lung carcinoma cells. These derivatives exhibited selective anticancer activity and induced apoptosis.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Applied
Bulat F. Garifullin, Irina Yu Strobykina, Leysan R. Khabibulina, Anastasiya S. Sapunova, Aleksandra D. Voloshina, Radmila R. Sharipova, Bulat Khairutdinov, Yuriy F. Zuev, Vladimir E. Kataev
Summary: Conjugates of diterpenoid isosteviol and N-acetyl-D-glucosamine were synthesized and found to exhibit cytotoxicity against several human cancer cell lines, with two compounds showing selective cytotoxicity against M-Hela cells through induction of apoptosis.
NATURAL PRODUCT RESEARCH
(2021)
Article
Chemistry, Medicinal
Liwaliding Maihesuti, Hongwei Gao, Qi Wang, Jianguo Cao, Haji Akber Aisa, Guozheng Huang
Summary: The study achieved the chemical conversion of silybin to hydnocarpin and siliandrin, synthesized 45 new amide derivatives, and demonstrated the anti-proliferative activity of some compounds against cancer cells.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Xiaoping Zhao, Ziyang Chen, Ning Lin, Jingzhi Ma
Summary: In this study, a regio-selective and local modification strategy was performed on the reducing end of cellulose nanocrystals (CNC) with the grafting of long-chain poly(ethylene oxide) (PEO) to produce the end-grafted nanocrystals (CNC-eg-PEO). Through thiol-ene click reaction, the terminal allyl-PEO was covalently attached on the modified nanocrystal possessing the reactive thiol groups, maintaining surface chemistry and enhancing redisperstion stability. The CNC-eg-PEO showed low cytotoxicity to ATCC cell lines HFF and CAL-27, suggesting its potential for biomedical applications.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Engineering, Environmental
Meijiao Zhou, Jinhua Li, Mine Du, Jun Wang, Han Yeong Kaw, Lizhong Zhu, Wei Wang
Summary: In this study, it was found that halobenzoquinones (HBQs) can be metabolized by reacting with glutathione (GSH) to form various glutathionylated conjugates (SG-HBQs), and SG-MeO-HBQs were identified as the primary metabolites significantly correlated with the unusual cytotoxicity variation of HBQs. This metabolic pathway can enhance toxicity and provide new insights into the toxicity and metabolic mechanism of HBQs.
ENVIRONMENTAL SCIENCE & TECHNOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Teerapich Kasemsuk, Natthiya Saehlim, Patcharee Arsakhant, Gunya Sittithumcharee, Seiji Okada, Rungnapha Saeeng
Summary: A novel series of acanthoic acid analogues containing triazole moiety were synthesized, with 3d exhibiting the strongest cytotoxic activity. Computational studies showed that 3d has high binding energy with CDK-2 and EGFR protein kinases, indicating its potential as an anticancer agent.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Beatriz Salesa, Patricia Ferrus-Manzano, Alberto Tunon-Molina, Alba Cano-Vicent, Marcelo Assis, Juan Andres, Angel Serrano-Aroca
Summary: Gold nanoparticles (AuNPs) are promising for biomedical applications due to their excellent biosafety. However, their cytotoxicity in human HaCaT cells is time-dependent, and concentrations above 300 μg/mL show toxic activity. Low concentrations of AuNPs do not exhibit significant proliferative or antiviral activity, and gene expression is not modified after exposure to AuNPs for 24 hours. These results indicate that AuNPs are stable inactive materials suitable for biomedical and clinical applications.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Review
Food Science & Technology
Yezhi Fu, Evelyn Jiang, Yuan Yao
Summary: This review provides an overview of starch composition, structure, and properties, as well as the structural tailoring methods to overcome functional limitations and expand starch applications. The interactions of starch with lipids, polysaccharides, and phenolics are also discussed. Additionally, current progress in porous starch and starch-based nanoparticles is described, including the use of new techniques such as CRISPR-Cas9 and emulsion-assisted approaches.
ANNUAL REVIEW OF FOOD SCIENCE AND TECHNOLOGY
(2022)
Article
Engineering, Electrical & Electronic
A. L. Kozlovskiy, K. Egizbek, B. A. Prmantayeva, M. V. Zdorovets, K. K. Kadyrzhanov
Summary: This work focuses on evaluating the doping of Fe3O4 nanoparticles with gadolinium and neodymium to obtain nanocomposites of GdFeO3/Fe2O3 and NdFeO3/Fe2O3 types, and determining their efficiency in purifying aqueous media by absorbing manganese. The synthesized nanocomposites showed higher absorption efficiency for manganese ions and greater stability compared to undoped hematite nanoparticles.
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN ELECTRONICS
(2021)
Article
Materials Science, Coatings & Films
Ping Li, Junyu Qian, Wentai Zhang, Christine Schille, Ernst Schweizer, Alexander Heiss, Ulrich E. Klotz, Lutz Scheideler, Guojiang Wan, Jurgen Geis-Gerstorfer
Summary: The study investigated the effect of sandblasting surface treatment with two different sizes of Al2O3 particles on the degradation rates of zinc and its alloys. The results showed that the sandblasting treatment significantly increased the degradation rates, but the particle size was associated with cytotoxicity effects.
SURFACE & COATINGS TECHNOLOGY
(2021)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
