作者: Coelho, Eduardo Antonio Ferraz ; Roatt, Bruno Mendes ; Pereira, Isabela Amorim Gonçalves ; de Freitas, Camila Simões ; Soyer, Tauane Gonçalves ; Chávez-Fumagalli, Miguel Angel ; de Paula Costa, Guilherme ; Ludolf, Fernanda ; Ramos, Fernanda Fonseca ; Bandeira Câmara, Raquel Soares ; de Sousa Vieira Tavares, Grasiele ; Vale, Danniele Luciana ; Martins, Vívian Tamietti ; Pimenta, Breno Luiz ; Galdino, Alexsandro Sobreira ; Lage, Daniela Pagliara ; de Jesus, Marcelo Moreira

ABSTRACTThe treatment for visceral leishmaniasis (VL) causes toxicity in patients, entails high cost and/or leads to the emergence of resistant strains. No human vaccine exists, and diagnosis presents problems related to the sensitivity or specificity of the tests. Here, we tested two phage clones, B1 and D11, which were shown to be protective against Leishmania infantum infection in a murine model as immunotherapeutics to treat mice infected with this parasite species. The phages were used alone or with amphotericin B (AmpB), while other mice received saline, AmpB, a wild‐type phage (WTP) or WTP/AmpB. Results showed that the B1/AmpB and D11/AmpB combinations induced polarised Th1‐type cellular and humoral responses, which were primed by high levels of parasite‐specific IFN‐γ, IL‐12, TNF‐α, nitrite and IgG2a antibodies, which reflected in significant reductions in the parasite load in distinct organs of the animals when analyses were performed 1 and 30 days after the treatments. Reduced organic toxicity was also found in these animals, as compared with the controls. In conclusion, preliminary data suggest the potential of the B1/AmpB and D11/AmpB combinations as immunotherapeutics against L. infantum infection.

2024-03-01·Bioorganic Chemistry

Rational design and synthesis of triazene-amonafide derivatives as novel potential antitumor agents causing oxidative damage towards DNA through intercalation mode

Article

作者: Gao, Yun-Fei ; Xia, Ya-Mu ; Sun, Ping ; Zhang, Xue ; Zhang, Jia-Yin ; Gao, Wei-Wei ; Liang, Chen ; Yu, Ri-Lei ; Xu, Na ; Zhang, Qi-Ming

In this work, we rationally designed and synthesized two novel triazene-amonafide derivatives 2-(2-(diisopropylamino)ethyl)-5-(3,3-dimethyltriaz-1-en-1-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione (D-11) and 5-(3,3-diethyltriaz-1-en-1-yl)-2-(2-(diisopropylamino)ethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione (D-12) as potential antitumor agents. The DNA damage induced by the intercalation mode of D-11 (D-12) towards DNA was electrochemically detected through the construction of efficient biosensors. The consecutive processes of reversible redox of naphthylimide ring and irreversible oxidation of triazene moiety were elucidated on the surface of glassy carbon electrode (GCE) by CV, SWV, and DPV methods. Electrochemical biosensors were obtained through the immobilization of ctDNA, G-quadruplexes, poly(dG), and poly(dA), respectively, on the clean surface of GCE. After the incubation of biosensors with D-11 or D-12, the peaks of dGuo and dAdo decreased prominently, and the peak of 8-oxoGua appeared at +0.50 V, suggesting that the interaction between D-11 (D-12) and DNA could result in the oxidative damage of guanine. Unexpected, the as-prepared DNA biosensor possessed satisfactory anti-interference property and good practicability in real samples. UV-vis and fluorescence spectra, and gel electrophoresis assays were employed to further confirm the intercalation mode of D-11 (D-12) towards DNA base pairs. Moreover, D-11 was proved to exhibit stronger anti-proliferation activity than mitionafide and amonafide against both A549 and HeLa cell lines.

2023-11-01·The European Physical Journal E

D11 and small angle neutron scattering: a paradigm of ILL

Article

作者: White, John

AbstractThis paper describes some of the early events in the 50 year success of D11. That, and the Institut Laue Langevin are linked by an attitude that embraces both instrument renewal and new areas of science. The neutron sources proved to be reliable and serviceable, the neutron guides and guide hall have been a great benefit, and the user concept has led to a strengthening international community of diverse and good science and to new instruments clamouring for funding in a growing facility. Designs were perfected and the second wind (Deuxième Souffle) funded the outflow from which a second strong phase has evolved.Graphical Abstract

100 项与 D-0011 相关的药物交易

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