Article
Microbiology
Karthik Ramalingam, Sonali Gangwar, Deep Chandra Balodi, Apeksha Anand, Shailendra Yadav, Subhasish Biswas, Anil Kumar Karunakaran Sasikala, Kailash Chand Gupta, Sanjay Batra, Neena Goyal
Summary: Chemotherapy is crucial for controlling visceral leishmaniasis, but current regimens have drawbacks. This study identified compound 3c as the lead candidate for treating VL, showing the best in vivo antileishmanial efficacy.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Biochemical Research Methods
Subhadip Saha, Shubham Vashishtha, Bishwajit Kundu, Monidipa Ghosh
Summary: The study utilizes bioinformatics and immunology to design a multi-epitope vaccine for the prevention and treatment of visceral leishmaniasis. The vaccine shows high affinity and potential effectiveness in a global population. Successful cloning and optimization of the vaccine's nucleic acid sequence have also been achieved.
BMC BIOINFORMATICS
(2022)
Article
Multidisciplinary Sciences
Helen Ashwin, Jovana Sadlova, Barbora Vojtkova, Tomas Becvar, Patrick Lypaczewski, Eli Schwartz, Elizabeth Greensted, Katrien Van Bocxlaer, Marion Pasin, Kai S. Lipinski, Vivak Parkash, Greg Matlashewski, Alison M. Layton, Charles J. Lacey, Charles L. Jaffe, Petr Volf, Paul M. Kaye
Summary: Leishmaniasis is considered a vaccine-preventable disease, but costs and uncertainty hinder progress in vaccine development. Controlled human infection models offer a way to speed up vaccine development and gain better understanding of disease pathogenesis.
NATURE COMMUNICATIONS
(2021)
Article
Parasitology
Hasna Riyal, Tiago R. Ferreira, Andrea Paun, Kashinath Ghosh, Nilakshi Samaranayake, David L. Sacks, Nadira D. Karunaweera
Summary: Leishmaniasis, caused by Leishmania parasites and transmitted by sand flies, has many different species that can cause disease in humans and animals. Recent research has found evidence of genetic exchange and hybridization in L. donovani parasites within the sand fly vector, Phlebotomus argentipes. This discovery provides new insight into the mechanisms for the diversity of clinical manifestations in humans affected by L. donovani.
Article
Biochemistry & Molecular Biology
Ahmed H. E. Hassan, Waleed A. Bayoumi, Selwan M. El-Sayed, Trong-Nhat Phan, Yeon Ju Kim, Chae Hyeon Lee, Soo Bin Cho, Taegeun Oh, Gyeongpyo Ham, Kazem Mahmoud, Joo Hwan No, Yong Sup Lee
Summary: A series of chromone-peptidyl hybrids was synthesized and repurposed for the identification of potential antileishmanial compounds against visceral leishmaniasis. Compounds 7c, 7n, and 7h showed potential IC50 values (9.8, 10, and 12 μM, respectively) comparable to erufosine but lower potency than miltefosine. Cytotoxicity assessment using human THP-1 cells revealed that compounds 7c and 7n were non-cytotoxic up to 100 μM, while erufosine and miltefosine exhibited cytotoxicity. In silico studies identified specific substituents on the chromone-peptidyl hybrids as crucial for binding to LdCALP. These findings suggest that compounds 7c and 7n could be potential non-cytotoxic antileishmanial agents for the development of treatment against visceral leishmaniasis.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Antonio Lipa Castro, Sebastien Pomel, Catherine Cailleau, Natalie Fournier, Indira Dennemont, Philippe M. Loiseau, Gillian Barratt
Summary: This article describes the in-vivo evaluation of AmB-loaded, lipid-based cochleate systems designed for the oral route. The study found that cochleate formulations based on Lipoid PSP70 show promising antiparasitic activity for the treatment of visceral leishmaniasis.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Public, Environmental & Occupational Health
Santhi John Tharakan, Dincy C. Peter, Rajiv Karthik, Vedantam Rupa, Winsley Rose, Meera Thomas, Malathi Manuel, Priscilla Rupali, Susanne Pulimood, Sitara Swarna Rao Ajjampur
Summary: This study reports on 52 suspected cases of cutaneous and mucosal leishmaniasis in a tertiary care setting in southern India from 2008 to 2018. Of the 12 confirmed cases, seven had mucocutaneous leishmaniasis, two had cutaneous leishmaniasis, and three had post-kala-azar dermal leishmaniasis. The emerging trend of atypical MCL caused by L. donovani variants highlights the importance of a high index of suspicion combined with PCR-based diagnostics for accurate diagnosis of different manifestations of leishmaniasis.
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE
(2021)
Review
Biology
Pedro Cecilio, Anabela Cordeiro-da-Silva, Fabiano Oliveira
Summary: This review discusses various aspects of sand flies as vectors of Leishmania parasites, including their basic biology, ecology, and interactions with the parasites. It highlights the need to study the vectors as well as the diseases and etiological agents.
COMMUNICATIONS BIOLOGY
(2022)
Review
Parasitology
Malgorzata Anna Domagalska, Michael P. Barrett, Jean-Claude Dujardin
Summary: Treatment failure (TF), particularly in leishmaniasis, is a major concern in the management of parasitic diseases. It is unclear whether drug resistance (DR), measured by in vitro drug susceptibility assays, is the sole contributor to TF. This article addresses three key questions to clarify the relationship between TF and DR.
TRENDS IN PARASITOLOGY
(2023)
Article
Infectious Diseases
Pamornsri Sriwongpan, Supalert Nedsuwan, Jidapa Manomat, Sakarn Charoensakulchai, Kittiphat Lacharojana, Jamnong Sankwan, Natheeporn Kobpungton, Taweesak Sriwongpun, Saovanee Leelayoova, Mathirut Mungthin, Suradej Siripattanapipong, Toon Ruang-areerate, Tawee Naaglor, Theethach Eamchotchawalit, Phunlerd Piyaraj
Summary: This study is the first community-based investigation in Thailand that examines the prevalence and associated risk factors of Leishmania infection among immunocompetent individuals. It highlights the urgent need for effective interventions to prevent and control the disease in endemic areas.
PLOS NEGLECTED TROPICAL DISEASES
(2021)
Review
Microbiology
Carolina Ferreira, Jerome Estaquier, Ricardo Silvestre
Summary: Leishmania manipulates host metabolic pathways to evade the immune response, facilitating long-term survival and altering the metabolism of infected macrophages, which is linked to infection resistance. Studying the interactions between metabolism and innate immune cell function holds promise for therapeutic or prophylactic interventions.
CURRENT OPINION IN MICROBIOLOGY
(2021)
Article
Biology
Madhu Puri, Harsimran Kaur Brar, Nimisha Mittal, Evanka Madan, Rajesh Srinivasan, Kapil Rawat, Srija Moulik, Mitali Chatterjee, Sai Siva Gorthi, Rohini Muthuswami, Rentala Madhubala
Summary: L. donovani is a parasite causing visceral leishmaniasis, and the portable LAMP device developed in this study can detect and amplify its DNA with high sensitivity, specificity, and accuracy, potentially serving as a reliable point-of-care diagnostic and prognostic tool for Leishmania infections in the future.
JOURNAL OF BIOSCIENCES
(2021)
Article
Mathematics, Interdisciplinary Applications
Yi Zhao, Amir Khan, Usa Wannasingha Humphries, Rahat Zarin, Majid Khan, Abdullahi Yusuf
Summary: This paper investigates the most dangerous form of leishmaniasis, visceral leishmaniasis, and establishes the existence and uniqueness of solutions for the fractional leishmania epidemic model using fixed point theorems. The basic properties and stability of the model are studied, and numerical solutions are found using Newton polynomial and Adams-Bashforth methods.
FRACTALS-COMPLEX GEOMETRY PATTERNS AND SCALING IN NATURE AND SOCIETY
(2022)
Article
Immunology
Siddharth Sankar Singh, Shashi Bhushan Chauhan, Susanna S. S. Ng, Dillon Corvino, Fabian de Labastida Rivera, Jessica A. Engel, Nic Waddell, Pamela Mukhopadhay, Rebecca L. Johnston, Lambros T. Koufariotis, Susanne Nylen, Om Prakash Singh, Christian R. Engwerda, Rajiv Kumar, Shyam Sundar
Summary: This study identified increased expression of AREG in CD4(+) T cells from individuals with asymptomatic L. donovani infection, suggesting the presence of an ongoing inflammatory response and highlighting the potential role of AREG in preventing inflammation-induced tissue damage and subsequent disease in asymptomatic individuals.
CLINICAL & TRANSLATIONAL IMMUNOLOGY
(2022)
Article
Parasitology
Kanok Preativatanyou, Komson Chinwirunsirisup, Atchara Phumee, Pathamet Khositharattanakool, Sakone Sunantaraporn, Padet Siriyasatien, Jerome Depaquit
Summary: Autochthonous leishmaniasis in Thailand has become a public health concern, with an increasing number of new clinical cases. A study in southern Thailand found Asian new leishmaniasis and visceral leishmaniasis transmitted by sand flies, as well as a suspected novel trypanosoma species. These findings contribute to a better understanding of the transmission of leishmaniasis and the establishment of effective prevention and control measures.
Article
Hematology
Ava Diarra, Nicolas Duployez, Elise Fournier, Claude Preudhomme, Valerie Coiteux, Leonardo Magro, Bruno Quesnel, Mael Heiblig, Pierre Sujobert, Fiorenza Barraco, Marie Balsat, Quentin Scanvion, Eric Hachulla, David Launay, Ibrahim Yakoub-Agha, Louis Terriou
Summary: VEXAS syndrome is caused by somatic mutations in the UBA1 gene. Patients with VEXAS syndrome often display late-onset autoinflammatory symptoms and hematologic abnormalities. Allogeneic hematopoietic stem cell transplantation (ASCT) has shown promising outcomes in some patients, but further clinical trials are needed to determine its efficacy and place in the treatment arsenal for VEXAS syndrome.
Article
Immunology
Sarah Stabler, Catherine Lamblin, Sacha Gaillard, Nicolas Just, Mirela Mihailescu, Nathalie Viget, Thierno Sy Ndiaye, Arnaud Dzeing Ella, Guillaume Brunin, Pierre Weyrich, Anne Prevotat, Cecile Chenivesse, Olivier Le Rouzic, Geoffrey Mortuaire, Fanny Vuotto, Karine Faure, Amelie Leurs, Frederic Wallet, Caroline Loiez, Marie Titecat, Remi R. Le Guern, Eric Hachulla, Sebastien Sanges, Etienne N. Nicolas, Louis Terriou, David Launay, Benjamin Lopez, Mathilde Bahuaud, Frederic Batteux, Sylvain Dubucquoi, Cyrielle Gesquiere-Lasselin, Myriam Labalette, Guillaume Lefevre
Summary: This study aimed to evaluate a systematic research strategy for the diagnosis of specific polysaccharide antibody deficiency (SPAD) in adults with unexplained bacterial infections. The results showed that SPAD is the most common immunodeficiency in adults with recurrent and/or severe bacterial infections, and should be screened in these patients.
CLINICAL INFECTIOUS DISEASES
(2023)
Correction
Immunology
Sebastien Sanges, Nicolas Germain, Stephane Vignes, David Seguy, Sarah Stabler, Nicolas Etienne, Louis Terriou, David Launay, Eric Hachulla, Damien Huglo, Sylvain Dubucquoi, Myriam Labalette, Guillaume Lefevre
JOURNAL OF CLINICAL IMMUNOLOGY
(2023)
Article
Rheumatology
Yann Nguyen, Cecile M. Yelnik, Nathalie Morel, Romain Paule, Romain Stammler, Leo Placais, Karim Sacre, Bertrand Godeau, Helene Maillard, David Launay, Sandrine Morell-Dubois, Anastasia Dupre, Guillaume Lefevre, Cecile Devloo, Virginie Dufrost, Ygal Benhamou, Herve Levesque, Gaelle Leroux, Jean-Charles Piette, Luc Mouthon, Eric Hachulla, Marc Lambert, Veronique Le Guern, Nathalie Costedoat-Chalumeau
Summary: This study used unsupervised clustering analysis to identify four homogeneous phenotypic subgroups among APS patients, primarily involving venous, arterial, SLE or other autoimmune disease-associated, and arterial microthrombotic phenotypes. These findings may be explained by heterogeneous pathophysiological mechanisms.
Article
Rheumatology
Sebastien Sanges, Lisa Rice, Ly Tu, Eleanor Valenzi, Jean-Luc Cracowski, David Montani, Julio C. Mantero, Camille Ternynck, Guillemette Marot, Andreea M. Bujor, Eric Hachulla, David Launay, Marc Humbert, Christophe Guignabert, Robert Lafyatis
Summary: This study examined the serum proteome of patients with systemic sclerosis-associated pulmonary arterial hypertension (SSc-PAH) and identified two proteins that were significantly correlated with pulmonary vascular resistance (PVR), potentially providing biomarkers for earlier diagnosis and treatment.
ANNALS OF THE RHEUMATIC DISEASES
(2023)
Review
Respiratory System
J. Le Pavec, D. Launay, V. Cottin, M. Reynaud-Gaubert
REVUE DES MALADIES RESPIRATOIRES
(2023)
Article
Rheumatology
Benjamin Chaigne, Kevin Chevalier, Athenais Boucly, Christian Agard, Antoine Baudet, Arnaud Bourdin, Celine Chabanne, Vincent Cottin, Pierre Fesler, Francois Goupil, Patrick Jego, David Launay, Herve Levesque, Arnaud Maurac, Shirine Mohamed, Cecile Tromeur, Laurence Rottat, Olivier Sitbon, Marc Humbert, Luc Mouthon
Summary: Objective of this study was to describe PAH in well-characterized MCTD patients. Results showed that pericarditis, polyarthritis, thrombocytopenia, ILD and anti-Sm antibodies were independent predictive factors of PAH in MCTD. Survival rates of MCTD-PAH patients did not differ from SLE-PAH and SSc-PAH patients. Tobacco exposure was an independent predictor of mortality in MCTD-PAH.
Article
Medicine, General & Internal
Aurore Collet, Christophe Zawadzki, Emmanuelle Jeanpierre, Caroline Kitel, Sylvain Dubucquoi, Eric Hachulla, Sophie Susen, David Launay
Summary: Systemic sclerosis (SSc) is associated with endothelial activation and fibrosis. Non-O blood group is linked to higher risk of thrombosis, fibrosis and autoimmune diseases. The distribution of ABO groups in SSc patients is similar to the general population, but non-O groups are associated with inflammation and endothelial activation, and a slightly higher frequency of pulmonary and vascular complications in SSc.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Medicine, General & Internal
D. Launay, L. Bouillet, I. Boccon-Gibod, B. Trumbic, D. Gobert, O. Fain
Summary: Hereditary angioedema is a rare disease characterized by recurrent attacks of noninflammatory edema. It can be life-threatening and significantly affect quality of life. The usual treatments for mast cell-mediated angioedema do not work for this condition. Treatment options include selective B2 bradykinin receptor antagonist or C1 inhibitor concentrate for severe attacks, and the use of attenuated androgen or C1 inhibitor concentrate for short-term prophylaxis. Recently available kallikrein inhibitors are an important advancement in long-term prophylaxis of hereditary angioedema attacks.
REVUE DE MEDECINE INTERNE
(2023)
Review
Medicine, General & Internal
T. Penet, M. R. Pokeerbux, S. Morell-Dubois, S. Sanges, H. Maillard, E. Ledoult, M. Lambert, C. Yelnik, V. Sobanski, D. Launay, E. Hachulla, M. M. Farhat
Summary: This study presents two cases of giant-cell arteritis with coronaritis and provides a review on this complication.
REVUE DE MEDECINE INTERNE
(2023)
Article
Immunology
Bijay Kumar Jha, Sanjay Varikuti, Chaitenya Verma, Rahul Shivahare, Nicholas Bishop, Gregory P. Dos Santos, Jacquelyn McDonald, Aakash Sur, Peter J. Myler, Sergio Schenkman, Abhay R. Satoskar, Bradford S. McGwire
Summary: A parasite mutant with depleted expression of Cyp19 was generated and found to be unable to replicate and cause clinical disease in host cells or mice. Immunization studies using the mutant parasite line showed that it can effectively prevent death from acute disease. These results suggest that parasite Cyp19 may be a candidate for drug targeting and the mutant parasite line warrants further immunization studies for prevention of Chagas disease.
Article
Health Care Sciences & Services
Quentin Ducrocq, Laurence Guedon-Moreau, David Launay, Louis Terriou, Sandrine Morell-Dubois, Helene Maillard, Guillaume Lefevre, Vincent Sobanski, Marc Lambert, Cecile Yelnik, Meryem-Maud Farhat, Maria Jose Garcia Fernandez, Eric Hachulla, Sebastien Sanges
Summary: Rare disease referral centres face challenges in clinical expertise and research activities, which can be overcome with telemedicine. Tele-expertise could generate a potential weekly income of EUR 500, while teleconsultations can address the limitation of frequent visits in research activities. Telemedicine has become a conventional follow-up modality for patients with rare diseases.
Article
Environmental Sciences
Madjid Djouina, Christophe Waxin, Segolene Caboche, Karine Lecointe, Alexander Steimle, Delphine Beury, Mahesh S. Desai, David Hot, Laurent Dubuquoy, David Launay, Cecile Vignal, Mathilde Body-Malapel
Summary: Oral exposure to DON mycotoxin exacerbates the development of enteritis and colitis-associated colorectal cancer in mice, even at low doses. The results suggest that DON, at concentrations currently tolerated in the human diet, could promote the development of intestinal inflammatory diseases and colorectal cancer.
SCIENCE OF THE TOTAL ENVIRONMENT
(2023)
Article
Rheumatology
Amelie Nicolas, Sylvie Leroy, Luc Mouthon, Yurdagul Uzunhan, Vincent Cottin, Arsene Mekinian, Viviane Queyrel, Eric Hachulla, Benoit Gachet, David Launay, Nihal Martis
Summary: This study provides an overview of the diagnostic approaches, follow-up, and treatment strategies used in France for the management of SSc-associated ILD. The results highlight the heterogeneity and gaps in current clinical practices, calling for improvement and standardization.
THERAPEUTIC ADVANCES IN MUSCULOSKELETAL DISEASE
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Antoine Dupont, Vincent Koether, Julien Labreuche, Paul Felloni, Thierry Perez, Pascal de Groote, Jacques Remy, Alain Duhamel, Eric Hachulla, David Launay, Martine Remy-Jardin
Summary: Dual-energy CT lung perfusion provides complementary information in systemic sclerosis patients, depicting perfusion changes in patients with normal or minimally infiltrated lung parenchyma.
EUROPEAN RADIOLOGY
(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)