Article
Biochemistry & Molecular Biology
C. A. Marquezin, C. M. A. de Oliveira, F. Vandresen, E. L. Duarte, M. T. Lamy, C. C. Vequi-Suplicy
Summary: 2-TSC, a potential drug, impacts membrane structure, with higher solubility in lipids and ethanol, displaying different structures. As a fluorescence quencher, it influences fluidization and organization of the bilayer.
CHEMISTRY AND PHYSICS OF LIPIDS
(2021)
Article
Biochemistry & Molecular Biology
Monika Hreusova, Vojtech Novohradsky, Lenka Markova, Hana Kostrhunova, Ivan Potocnak, Viktor Brabec, Jana Kasparkova
Summary: In this study, a gallium(III) complex with cloxyquin ligands is found to effectively inhibit the proliferation of rhabdomyosarcoma cells, a type of aggressive and difficult-to-treat cancer in children. The complex exhibits selective toxicity towards cancer cells compared to noncancerous fibroblasts. It induces ferroptosis in rhabdomyosarcoma cells through interference with iron metabolism, and is capable of killing both bulk and stem cells. This is the first non-iron metal compound shown to induce ferroptosis in cancer cells.
BIOINORGANIC CHEMISTRY AND APPLICATIONS
(2022)
Article
Multidisciplinary Sciences
Mahbub Alam, Mohammed Nurul Abser, Ajoy Kumer, Md Mosharef Hossain Bhuiyan, Parul Akter, Md Emdad Hossain, Unesco Chakma
Summary: The thiosemicarbazones and their derivatives were synthesized and characterized, and their drug likeness and bioavailability properties were evaluated. Quantum calculations and docking studies were performed to assess the binding affinity of these compounds against human pathogenic bacteria and fungi. The synthesized derivatives showed higher affinity than standard drugs, and in-vitro tests confirmed their antimicrobial activity against certain pathogens.
Article
Engineering, Mechanical
Huan Yang, Yuanshun Tan
Summary: This study develops a stochastic impulsive PCa model to analyze the elimination of androgen-dependent and androgen-independent cancer cells under noise interference with ADT and immunotherapy. The research illustrates that high-intensity noise perturbation can inhibit the development of PCa and theoretically and numerically verifies that frequent vaccination can improve the survival time of patients undergoing ADT.
NONLINEAR DYNAMICS
(2021)
Article
Oncology
Xinyue Yang, Yang Lu, Qin Kuang, Yong Wu, Xin Tan, Jizhong Lan, Zhe Qiang, Tao Feng
Summary: Prostate cancer is a common malignancy among men, but current therapies have limitations. This study established a co-culture system of prostate cancer cell lines and human embryonic stem cells (hESCs) to investigate the antitumor activity of the co-culture supernatant (Co-Sp). The Co-Sp showed concentration-dependent inhibition of prostate cancer cell viability, colony formation, and induced cell cycle arrest. It also promoted apoptosis and inhibited cell migration and invasion. In vivo experiments confirmed the inhibitory effect of Co-Sp on tumor growth. Mechanistic studies revealed the involvement of various proteins and signaling pathways in the antitumor activity of Co-Sp. These findings suggest a new way to utilize hESCs in cancer therapy and contribute to the development of stem cell-based treatments.
FRONTIERS IN ONCOLOGY
(2023)
Article
Engineering, Environmental
Abdul Rehman, Elena Russell, Faisal Saleem, Farhan Javed, Sajjad Ahmad, Valentine C. Eze, Adam Harvey
Summary: This study focused on the synthesis of trans-limonene bis-epoxide (trans-LBE) and investigated the effects of reaction temperature, mole ratio, and reaction time on the yield. The results showed that a 97% yield of trans-LBE could be achieved at 60 degrees Celsius after 5 minutes of reaction time with a 1:2 mole ratio of (R)-(+)-limonene to NBS.
JOURNAL OF ENVIRONMENTAL CHEMICAL ENGINEERING
(2021)
Article
Chemistry, Inorganic & Nuclear
Yasmim G. Goncalves, Amanda B. Becceneri, Angelica E. Graminha, Victor M. Miranda, Rafaella R. Rios, Francisco Rinaldi-Neto, Monica S. Costa, Ana C. R. Goncalves, Victor M. Deflon, Kelly A. G. Yoneyama, Pedro I. S. Maia, Eduardo F. Franca, Marcia R. Cominetti, Roberto S. Silva, Gustavo Von Poelhsitz
Summary: This article describes the synthesis, physicochemical characterization, and in vitro antitumor assays of four novel ruthenium(II) complexes. The results demonstrate that these complexes have potential in vitro antitumor activity and contribute to further studies in medicinal inorganic chemistry.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Multidisciplinary
Esteban Rodriguez-Arce, Eric Gavrilov, Ximena Alvite, Nazia Nayeem, Ignacio E. Leon, Michelle C. Neary, Lucia Otero, Dinorah Gambino, Claudio Olea Azar, Maria Contel
Summary: This work reports the synthesis and stability study of four gold(I) [AuClL] compounds containing chloro and biologically active protonated thiosemicarbazones based on 5-nitrofuryl (L=HSTC). The cytotoxicity of these compounds was evaluated against cancer cell lines, and one compound showed significant antimigratory and anti-angiogenic properties on a renal cancer cell line (Caki-1), along with preferential accumulation in the cell nuclei. Its mode of action seems to involve interaction with DNA and induction of apoptosis.
Article
Chemistry, Medicinal
Nguyen Thi Kim Giang, Nguyen Dinh Thanh, Tran Ha Quyen, Doan Thi Huong, Vu Ngoc Toan, Hoang Thi Kim Van
Summary: Several substituted isatin N-(2,3,4,6-tetra-O-acetyl-beta-D-glucopyranosyl)thiosemicarbazones were synthesized and evaluated for their antibacterial and antifungal activity. Compound 6h exhibited the highest inhibitory activity against Staphylococcus aureus, and docking studies suggested that it inhibited the DNA Gyrase enzyme in S. aureus.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Luis Fernando Mendez-Lopez, Pierluigi Caboni, Eder Arredondo-Espinoza, Juan J. J. Carrizales-Castillo, Isaias Balderas-Renteria, Maria del Rayo Camacho-Corona
Summary: Bioassay-guided fractionation of a CHCl3-MeOH extract from Cissus trifoliata stems identified an active fraction against PC3 prostate cancer cells, containing various natural compounds. Exposure of PC3 cells to resveratrol induced significant changes in numerous genes, leading to inhibition of cell proliferation.
Article
Oncology
Huiying Cheng, Sijie Tang, Xueqi Lian, Hong Meng, Xiang Gu, Jiajia Jiang, Xiaohua Li
Summary: DNA methylation, mediated by DNA methyltransferase, affects gene expression and plays a role in malignant diseases. The classic inhibitor 5-Aza inhibits tumor cell proliferation and induces cell cycle arrest. It increases tumor suppressive proteins and transcription factors, while decreasing oncogene expression. These results suggest potential clinical applications in prostate cancer treatment.
Article
Biochemistry & Molecular Biology
Mahendiran Dharmasivam, Mahan Gholam Azad, Rizwana Afroz, Vera Richardson, Patric J. Jansson, Des R. Richardson
Summary: This study demonstrates the potent and broad anti-proliferative activity of Dp44mT and particularly DpC, and is important for establishing optimized combinations with standard chemotherapies.
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
(2022)
Article
Chemistry, Medicinal
Irina I. Khan, Saida S. Karshieva, Darina V. Sokolova, Tatiana S. Spirina, Vladimir A. Zolottsev, Alexandra S. Latysheva, Natalia Y. Anisimova, Marina V. Komarova, Marina N. Yakunina, Tatiana A. Nitetskaya, Alexander Y. Misharin, Vadim S. Pokrovsky
Summary: The study aimed to investigate the mechanisms of action of alsevirone in prostate cancer, showing significant antitumor activity through CYP17A1 inhibition, apoptosis induction, and reduction in testosterone levels. Alsevirone demonstrated higher cytotoxicity compared to abiraterone, with a notable reduction in tumor growth in vivo.
ARCHIV DER PHARMAZIE
(2022)
Article
Chemistry, Inorganic & Nuclear
Niloufar Abbaszadeh, Negar Jaahbin, Ayda Pouraei, Fatemeh Mehraban, Mohammad Hedayati, Amitis Majlesi, Fatemeh Akbari, Seyed Ataollah Sadat Shandiz, Ali Salehzadeh
Summary: The study successfully synthesized nickel oxide nanoparticles functionalized with glutamic acid and conjugated with thiosemicarbazide (NiO@Glu/TSC), demonstrating significant growth inhibition of human breast cancer cells (MCF-7). Compared to normal cells (HEK293), MCF-7 cells showed a higher sensitivity to these nanoparticles.
JOURNAL OF CLUSTER SCIENCE
(2022)
Article
Cell Biology
Vanessa P. Rocha, Samir P. C. Campos, Caroline A. Barros, Pablo Trindade, Leticia R. Q. Souza, Triciana G. Silva, Etel R. P. Gimba, Anderson J. Teodoro, Rafael B. Goncalves
Summary: Bovine lactoferrin (bLf) induces cell death and morphological changes in the human prostate cancer cell line DU-145, along with G(1)-phase arrest, caspase 3/7 activation, and increased oxidative stress.
OXIDATIVE MEDICINE AND CELLULAR LONGEVITY
(2022)
Article
Chemistry, Applied
Mariana R. Passos de Souza, Anderson V. G. Ramos, Josiane A. Monteiro de Oliveira, Marcia R. P. Cabral, Eloisa G. Sampiron, Regiane B. de Lima Scodro, Mary Ann Foglio, Ana Lucia T. G. Ruiz, Marta R. B. do Carmo, Maria H. Sarragiotto, Debora C. Baldoqui
Summary: The chemical investigation of Chromolaena palmaris expanded the phytochemical composition knowledge of the genus by discovering 25 compounds, including a phytoprostane, flavonoids, phenolic acids, and a caffeoyl-glucoside derivative. The plant showed cytotoxicity towards human cancer cell lines and antimicrobial activity against Mycobacterium tuberculosis, with some compounds exhibiting potential for further drug development.
NATURAL PRODUCT RESEARCH
(2022)
Article
Chemistry, Applied
Luciana Bitencourt de Souza, Sirlene Valerio Tinti, Ilza Maria de Oliveira Sousa, Ilio Montanari Jr, Jose Luiz da Costa, Joao Ernesto de Carvalho, Mary Ann Foglio, Ana Lucia Tasca Gois Ruiz
Summary: This study evaluated the anti-proliferative potential of ethanolic extract and fractions from Mentha aquatica L aerial parts. F2 fraction showed potent and irreversible anti-proliferative effects without inducing cell cycle arrest in human tumor and non-tumor cell lines. However, storage conditions need to be optimized to enhance F2 stability for further research.
NATURAL PRODUCT RESEARCH
(2022)
Article
Chemistry, Applied
Ilza Maria de Oliveira Sousa, Gerardo Alvarez Rivera, Diana Pinto, Nubia de Cassia Almeida Queiroz, Veronica Isabel Correia Bastos, Lucia Elaine O. Braga, Josman Dantas Palmeira, Helena Amaral, Helena Maria Neto Ferreira, Helena Cristina Correia Oliveira, Fernando J. Mendes Goncalves, Ana Lucia T. G. Ruiz, Elena Ibanez, Beatriz P. P. Oliveira, Mary A. Foglio
Summary: The study investigated the effects of N-2 atmosphere on the spray-drying process of Fridericia chica plant extract, showing that different drying atmospheres can affect compound content but not pharmacological activity; the extract promotes cell migration and exhibits antimicrobial activity.
NATURAL PRODUCT RESEARCH
(2022)
Article
Toxicology
Thania Rios Rossi Lima, Estela de Oliveira Lima, Jeany Delafiori, Rodrigo Ramos Catharino, Joao Lauro Viana de Camargo, Lilian Cristina Pereira
Summary: This study demonstrates that Diuron and its metabolites have toxic effects on the mitochondrial function of rat bladder urothelium, leading to cellular damage and death.
TOXICOLOGY MECHANISMS AND METHODS
(2022)
Article
Immunology
Lucia Elaine de Oliveira Braga, Gisele Goulart da Silva, Ilza Maria de Oliveira Sousa, Ellen Cristina Souza de Oliveira, Michele Pedroza Jorge, Karin Maia Monteiro, Tamires Carolina Sedano, Mary Ann Foglio, Ana Lucia Tasca Gois Ruiz
Summary: The study evaluated the therapeutic potential of Mentha aquatica essential oil to treat gastrointestinal disorders. The essential oil showed a strong gastroprotective effect on peptic ulcers, reducing gastric secretion and acidity. It also exhibited anti-inflammatory properties in a model of induced gastrointestinal lesions.
INFLAMMOPHARMACOLOGY
(2022)
Article
Chemistry, Applied
Rogerio Jose Machado Junior, Julia C. Camilli, Rosanna Tarkany Basting, Patricia Maria Wiziacki Zago, Ilza Maria de Oliveira Sousa, Kaio Eduardo Buglio, Ana Lucia T. G. Ruiz, Paulo Roberto Nogueira Carvalho, Joao Ernesto de Carvalho, Sara T. O. Saad, Mary Ann Foglio
Summary: This study reports the in vitro cytoprotective synergistic effect of the combination of F. chica extract and enriched geranylgeraniol on keratinocytes exposed to zoledronic acid. The combination treatment significantly increased cell viability and reversed the effects of zoledronic acid on the cells. This study provides valuable data for potential treatment of MRONJ.
NATURAL PRODUCT RESEARCH
(2023)
Article
Biochemical Research Methods
Jeany Delafiori, Alessandra V. de S. Faria, Arthur N. de Oliveira, Geovana M. Sales, Flavia Luisa Dias-Audibert, Rodrigo R. . Catharino
Summary: Zika virus infection induces metabolic alterations in prostate cells, especially in glycerolipids, fatty acids, and acylcarnitines. This may be related to viral exploitation of cellular resources and increased oxidative stress metabolites.
JOURNAL OF PROTEOME RESEARCH
(2023)
Article
Biology
Mariana Alves Sobreiro, Adriana Della Torre, Maria Elisa Melo Branco de Araujo, Paula Renata Bueno Campos Canella, Joao Ernesto de Carvalho, Patricia de Oliveira Carvalho, Ana Lucia Tasca Gois Ruiz
Summary: The bioavailability of glucoside flavonoids is affected by the nature of the sugar, with glucosides being absorbed faster than rhamnoglucosides. Enzymatic hydrolysis is a strategy to enhance bioavailability. This study evaluated the kinetic parameters of hesperidinase-mediated hydrolysis of rutin and found that hydrolyzed rutin derivatives showed anti-proliferative and anti-mutagenic effects, making it a promising raw material for food supplements.
Article
Chemistry, Applied
Eveleny Tirsa Vaca Meza, Jorge Vasquez-Kool, Noe Ildefonso Costilla Sanchez, Amandio Vieira, Rodney Alexandre Ferreira Rodrigues, Adilson Sartoratto, Angela del Pilar Flores Granados, Carmen Luisa Marin Tello, Ana Lucia Tasca Gois Ruiz
Summary: This study evaluated the chemical composition and anti-proliferative activity of essential oils (EOs) from seven medicinal plants in Cachicadan, La Libertad Region, Peru. Gas chromatography-mass spectrometry analysis identified limonene and linalool as the common components in all EOs. The EO from Tagetes minuta leaves showed irreversible cytostatic effects against MCF-7 human breast tumor cells.
NATURAL PRODUCT RESEARCH
(2023)
Article
Food Science & Technology
Gisele Goulart da Silva, Lucia Elaine de Oliveira Braga, Ellen Cristina Souza de Oliveira, Joao Ernesto de Carvalho, Josy Goldoni Lazarini, Pedro Luiz Rosalen, Ana Paula Dionisio, Ana Lucia Tasca Gois Ruiz
Summary: The standardized extract (CAE) obtained from cashew apple bagasse shows potential beneficial effects on ulcerative colitis. CAE is more effective in delaying disease progression but cannot prevent or inhibit the disease. The concentration of carotenoids in CAE may not be sufficient, and there may be an antagonistic relationship between carotenoids and anacardic acids.
Article
Chemistry, Inorganic & Nuclear
Amanda A. Silva, Silmara C. L. Frajacomo, Allefe B. Cruz, Kaio Eduardo Buglio, Daniele Daiane Affonso, Marcelo Cecconi Portes, Ana Lucia T. G. Ruiz, Joao Ernesto de Carvalho, Wilton R. Lustri, Douglas H. Pereira, Ana M. da Costa Ferreira, Pedro P. Corbi
Summary: This study focuses on the synthesis, characterization, and antiproliferative activity of naproxen (Nap)-based complexes of copper(II) and platinum(II). The strategy involves combining bioactive ligands and metals to search for new and improved antiproliferative agents. The copper complex (Cu-Nap) has a binuclear paddle-wheel structure, while the platinum complex (Pt-Nap) has a square planar cis-[Pt(Nap)(2)(DMSO)(2)] isomer. Both complexes were inactive against bacteria but showed different activity against tumor cells.
Article
Biochemistry & Molecular Biology
Ana Carolina de Aguiar, Gustavo Araujo Pereira, Claudia Silva da Costa Ribeiro, Marcos Nogueira Eberlin, Lana Pereira Soares, Ana Lucia Tasca Gois Ruiz, Glaucia Maria Pastore, Julian Martinez
Summary: Capsiate and phenolics in different forms of BRS Moema peppers were analyzed and quantified using UHPLC-ESI-MS/MS. The peppers were found to contain significant amounts of capsiate and phenolic compounds, with esterified phenolics being the main fraction. The phenolic fractions demonstrated high antioxidant capacity, but the correlation between phenolic compounds and antioxidant activity suggested the presence of other bioactive or phenolic compounds contributing to the overall phenolic content.
Article
Chemistry, Applied
Beatriz P. Moreno, Francielli A. Pereira, Aline A. R. Andrade, Marcia R. P. Cabral, Alana C. Battistella, Tatiana S. Tiuman, Mary A. Foglio, Ana L. T. G. Ruiz, Marta Regina Barrotto do Carmo, Maria Helena Sarragiotto, Debora Cristina Baldoqui
Summary: This study investigated the chemical composition of Pterocaulon angustifolium, a native plant from Brazil, and identified multiple compounds, including various coumarins. The study found that P. angustifolium exhibits antiproliferative, antioxidant, antimicrobial, and cholinesterase inhibitory activities.
NATURAL PRODUCT RESEARCH
(2023)
Article
Multidisciplinary Sciences
Luciane A. N. Nesello, Adriana Campos, Andrea Rebello, Francielli T. Motta, Luisa N. B. Mariano, Fatima C. Buzzi, Ana Lucia T. G. Ruiz, Joao Ernesto De Carvalho, Valdir Cechinel-Filho, Luisa M. Silva
Summary: This study evaluated the biological activities of Abuta selloana extracts, which showed antiulcer, analgesic, and cytotoxic activities. Phytochemical analysis revealed the presence of phenolic compounds in the extracts. The leaves of this plant may be a promising source of compounds with cytotoxic potential, and the whole plant could contain bioactive compounds associated with gastroprotective and analgesic properties.
ANAIS DA ACADEMIA BRASILEIRA DE CIENCIAS
(2022)
Article
Pharmacology & Pharmacy
Adriana Muniz Massocatto, Nyessia Fernanda de Souza Silva, Caroline Calixto Kazama, Michele Dal Bem Pires, Orlando Seiko Takemura, Ezilda Jacomassi, Ana Lucia Tasca Gois Ruiz, Antonio Laverde Junior
Summary: Pereskia aculeata and P. grandifolia have shown antioxidant, anticholinesterase, molluscicidal, cytotoxic, and antiproliferative properties. This research highlights the potential of these species as sustainable sources of nutraceutical compounds.
PHARMACEUTICAL SCIENCES
(2022)
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)
