Article
Chemistry, Organic
Riko Minami, Tsubasa Kasai, Keisuke Murata, Haruhiko Fuwa
Summary: In this study, a convergent total synthesis of (+)-muricatetrocin B, a tetrahydrofuran-containing acetogenin with potent and selective cytotoxicity against HT-29 human colon adenocarcinoma cell line, was achieved in 13 steps. The synthesis is highlighted by a late-stage sequential olefin cross-metathesis/Hartung-Mukaiyama cyclization for the assembly of the 2,5-trans-substituted tetrahydrofuran ring.
Article
Pharmacology & Pharmacy
Natsuki Kubota-Ishida, Takashi Matsuhira, Chizuko Kaji, Chika Kikuchi, Yuji Tabata
Summary: The study compared the effects of a novel PDE4 inhibitor, AA6216, with crisaborole on skin inflammation, showing that AA6216 is a more potent inhibitor of PDE4 and of cytokine production. In mouse models of dermatitis, AA6216 significantly suppressed skin inflammation, suggesting its potential as a novel and effective topical therapeutic agent for the treatment of dermatitis including AD.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Yani Arhab, Karim Bessaa, Houda Abla, Meryem Aydin, Renaud Rahier, Arnaud Comte, Leyre Brizuela, Saida Mebarek, Florent Perret, Mickael Cherrier, Abdelkarim Abousalham, Alexandre Noiriel
Summary: This study investigates the impact of structural modifications of PLD inhibitors on enzyme activity and aims to identify new potent inhibitors of eukaryotic PLDs. Vanadate was found to be the most potent inhibitor among all, with an IC50 of around 58 μM. Screening a chemical library of 3120 compounds helped optimize the screening process and paved the way for the discovery of new potent inhibitors.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Food Science & Technology
A. A. Echenique-Martinez, D. G. Rodriguez-Sanchez, R. Troncoso-Rojas, C. Hernandez-Brenes, L. E. Robles-Ozuna, L. C. Montoya-Ballesteros
Summary: This study investigated the antifungal effect of a crude avocado seed extract enriched with acetogenins against the causal agent of grey rot in strawberries. Avosafe (R) at a concentration of 7,500 mg/L directly affected the stationary phase of the developing fungus and significantly inhibited conidial germination. The results suggest that Avosafe (R) could be a potential natural fungistatic agent against Botrytis cinerea in processed food products.
INTERNATIONAL FOOD RESEARCH JOURNAL
(2021)
Article
Multidisciplinary Sciences
Yulong Wei, Lesan Yan, Lijun Luo, Tao Gui, Biang Jang, Ahmad Amirshaghaghi, Tianyan You, Andrew Tsourkas, Ling Qin, Zhiliang Cheng
Summary: The study found that the enzyme sPLA(2) increases in OA cartilage tissues, and inhibiting its activity could be an effective treatment strategy. By incorporating an sPLA(2) inhibitor into micelles, it improved drug delivery within the joints and showed promising potential as a therapeutic agent for OA.
Article
Biochemistry & Molecular Biology
Tassia R. Costa, Aleff F. Francisco, Fabio F. Cardoso, Leandro S. Moreira-Dill, Carlos A. H. Fernandes, Antoniel A. S. Gomes, Cesar L. S. Guimaraes, Silvana Marcussi, Paulo S. Pereira, Hamine C. Oliveira, Marcos R. M. Fontes, Saulo L. Silva, Juliana P. Zuliani, Andreimar M. Soares
Summary: Snakebite envenoming is a major health crisis in many tropical regions, prompting the need for new solutions. This study highlights gallic acid as an effective inhibitor of snake venom myotoxicity, proposing a new mechanism of action and potential as an antivenom compound.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Dermatology
Kim Papp, Jacek C. Szepietowski, Leon Kircik, Darryl Toth, Lawrence F. Eichenfield, Donald Y. M. Leung, Seth B. Forman, May E. Venturanza, Kang Sun, Michael E. Kuligowski, Eric L. Simpson
Summary: The study evaluated the efficacy and safety of RUX cream in patients with AD, showing significant effects on reducing itch and improving skin inflammation, with superior efficacy compared to vehicle cream and good tolerability.
JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Angelina Subeska, Jan Althaus, Theresa Hake, Walburga Hanekamp, Dominik Bettenworth, Dennis Mulac, Klaus Langer, Matthias Lehr
Summary: This passage describes the potent potential of Indole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 as anti-inflammatory drugs, but only very low plasma concentrations could be achieved through oral administration in animal experiments. To optimize the metabolic stability, structural modifications were made but did not result in higher plasma concentrations. Cellular permeation assays revealed that these substances were good substrates for gastrointestinal efflux transporters, explaining their poor oral absorption.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Angelina Subeska, Merlin Ekodo Voundi, Walburga Hanekamp, Dennis Mulac, Klaus Langer, Matthias Lehr
Summary: Cytosolic phospholipase A(2)alpha (cPLA(2)alpha) is an interesting target for new anti-inflammatory drug development. The metabolic stability and permeability of potent inhibitors can be improved by introducing alkyl substituents or increasing rigidity near the ketone group. The polar ketone group is a decisive factor in the reverse transport of molecules, and its removal significantly increases permeability. However, these structural variations may lead to a decrease in the inhibitory potency against cPLA(2)alpha.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Multidisciplinary Sciences
Jennifer R. Shelley, Brian J. McHugh, Jimi Wills, Julia R. Dorin, Richard Weller, David J. Clarke, Donald J. Davidson
Summary: The human skin barrier is impaired in inflammatory skin diseases, and Staphylococcus aureus contributes to further barrier impairment. Previous studies have shown that the host defence peptide HBD2 can prevent damage caused by the extracellular protease V8 secreted by S. aureus. This study examines the mechanism of HBD2-mediated barrier protection in vitro.
SCIENTIFIC REPORTS
(2023)
Article
Dermatology
Jonathan I. I. Silverberg, Lars E. E. French, Richard B. B. Warren, Bruce Strober, Kim Kjoller, Morten O. A. Sommer, Philippe Andres, Jakob Felding, Anne Weiss, Deniz Tutkunkardas, Tine Skak-Nielsen, Emma Guttman
Summary: This study examined the PDE4 enzymatic activity and anti-inflammatory effects of orismilast in vitro, ex vivo, and in vivo. The results showed that orismilast selectively and potently inhibited PDE4 and demonstrated broad-spectrum anti-inflammatory activity. These findings support the clinical development of oral orismilast as a novel treatment option for chronic inflammatory skin diseases.
JOURNAL OF THE EUROPEAN ACADEMY OF DERMATOLOGY AND VENEREOLOGY
(2023)
Article
Plant Sciences
Onkar Nath, Stephen J. Fletcher, Alice Hayward, Lindsay M. Shaw, Ardashir Kharabian Masouleh, Agnelo Furtado, Robert J. Henry, Neena Mitter
Summary: The study presents a chromosome-level genome assembly of the commercial avocado cultivar Hass, offering valuable insights into the genetic characteristics and biosynthetic pathways of avocados. Analysis of the genome revealed specific features of heptose biosynthesis in avocados and highlighted the importance of endoglucanase genes in fruit ripening. The genome also identified unique genes in avocado and related species, providing a foundation for the development of elite avocado varieties in the future.
HORTICULTURE RESEARCH
(2022)
Article
Cell Biology
Dong Woo Kang, Won Chan Hwang, Yu Na Noh, Youra Kang, Younghoon Jang, Jung-Ae Kim, Do Sik Min
Summary: Phospholipase D1 (PLD1) is identified as a transcriptional target of histone deacetylase (HDAC) inhibitors and contributes to drug resistance in GBM. Inhibiting PLD1 can enhance the efficacy of HDAC inhibitors in treating GBM.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Gaku Tsuji, Kazuhiko Yamamura, Koji Kawamura, Makiko Kido-Nakahara, Takamichi Ito, Takeshi Nakahara
Summary: Atopic dermatitis (AD) is a chronic inflammatory skin disease with a complex pathogenesis involving skin barrier dysfunction, type II immune response, and pruritus. Advances in understanding the immunological mechanisms of AD have identified multiple novel therapeutic targets. New biologic agents targeting various cytokines and pathways are being developed for systemic and topical therapy, including JAK inhibitors, histamine H4 receptor antagonists, and microbiome modulation. This review provides insights into the current and future directions of novel therapies for AD and highlights their mechanisms of action and efficacy, supporting the advancement of precision medicine in the treatment of AD.
Review
Pharmacology & Pharmacy
Helena Iznardo, Esther Roe, Esther Serra-Baldrich, Lluis Puig
Summary: Abrocitinib, a selective JAK1 inhibitor, has been approved for the treatment of moderate-to-severe atopic dermatitis in adults. It has shown efficacy and safety in clinical trials involving both children and adults, and in comparison with dupilumab. The expected response rates for abrocitinib at week 12 are 62.9% for the 200 mg dose and 43.0% for the 100 mg dose. Abrocitinib has a faster effect in relieving itch compared to dupilumab. Caution is necessary when using abrocitinib due to its incomplete target selectivity, and additional screening and monitoring may be required.
Article
Biology
P. J. J. Trojan, M. S. Bohatch-Junior, M. F. Otuki, F. Souza-Fonseca-Guimaraes, P. V. Svidnicki, V. Nogaroto, D. Fernandes, E. A. Krum, G. M. Favero
BRAZILIAN JOURNAL OF BIOLOGY
(2016)
Article
Plant Sciences
Daniel Augusto Gasparin Bueno Mendes, Bruna da Silva Soley, Arthur da Silveira Prudente, Graziela Sponchiado, Barbara Guerreira Alpande Ferreira, Matheus Correa dos Santos, Amanda Sobreiro Modesto de Andrade, Clarissa de Medeiros Amorim, Tania Mari Belle Bresolin, Christiane Meyre-Silva, Katia Christina Zuffellato-Ribas, Jamil Assreuy, Michel Fleith Otuki, Daniela de Almeida Cabrini
Article
Cell Biology
Muryel Carvalho Goncalves, Veronica Vargas Horewicz, Debora Denardin Luckemeyer, Arthur Silveira Prudente, Jamil Assreuy
Article
Plant Sciences
Cintia Delai da Silva Horinouchi, Daniel Augusto Gasparin Bueno Mendes, Stefanie Nolte, Priscilla Salles de Brito, Bruna da Silva Soley, Giovani Marino Favero, Valdir Alves Facundo, Adair Roberto Soares Santos, Daniela de Almeida Cabrini, Michel Fleith Otuki
JOURNAL OF ETHNOPHARMACOLOGY
(2017)
Editorial Material
Medicine, General & Internal
Rosa Camila Lucchetta, Bruno Salgado Riveros, Roberto Pontarolo, Rosana Bento Radominski, Michel Fleith Otuki, Fernando Fernandez-Llimos, Cassyano Januario Correr
REVISTA DA ASSOCIACAO MEDICA BRASILEIRA
(2017)
Article
Medicine, Research & Experimental
Priscila Lucia Pawloski, Camila Guimaraes Moreira, Cintia Delai Silva Horinouchi, Daniel Fernandes, Luiz Renato Olchanheski Junior, Willian Machado, Daniela Almeida Cabrini, Michele Dietrich, Raba Paludo, Michel Fleith Otuki
BIOMEDICINE & PHARMACOTHERAPY
(2018)
Article
Medicine, Research & Experimental
Ana Paula Prestes, Willian Moreira Machado, Junior Garcia Oliveira, Luiz Renato Olchanheski, Fabio Andre Santos, Gustavo Ferreira Alves, Arthur Silveira Prudente, Michel Fleith Otuki, Katia Sabrina Paludo, Regina Sordi, Daniel Fernandes
Article
Pharmacology & Pharmacy
Maira Macedo Noroes, Larissa Gonzaga Santos, Elaine Cristina Gavioli, Vanessa de Paula Soares Rachetti, Michel Fleith Otuki, Daniela de Almeida Cabrini, Arthur da Silveira Prudente, Janiana Raiza Jentsch Matias Oliveira, Muryel de Carvalho Goncalves, Juliano Ferreira, Delia Preti, Francesco De Logu, Romina Nassini, Eunice Andre
EUROPEAN JOURNAL OF PHARMACOLOGY
(2019)
Article
Neurosciences
Marcella Amorim Ferreira, Debora Denardin Luckemeyer, Sergio Jose Macedo-Junior, Roberta Giusti Schran, Ana Merian Silva, Arthur Silveira Prudente, Raquel Tonello, Juliano Ferreira
Summary: Central sensitization, a characteristic of difficult to treat painful conditions, involves calcium influx in nociceptive neurons, with the Cav2.1, Cav2.2, and now the Cav2.3 voltage-gated calcium channels playing key roles. Inhibition of Cav2.3 has shown to partially reverse secondary hyperalgesia in a mouse model, especially in female mice, indicating its potential as a molecular target for CS. Additionally, the role of sexual differences in painful conditions needs more attention and exploration in clinically relevant pain models.
Article
Neurosciences
Cinder Faith Cohen, Arthur Silveira Prudente, Temugin Berta, Sang Hoon Lee
Summary: The study revealed the crucial role of TRPC4 in pain and migraine, with the TRPC4 antagonist ML204 showing promising effects in reducing migraine-like behaviors induced by nitroglycerin and lowering CGRP levels in mice. These findings suggest TRPC4 as a potential target for novel clinical treatments for migraineurs.
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2021)
Article
Medicine, Research & Experimental
Arthur S. Prudente, Graziela Sponchiado, Daniel A. G. B. Mendes, Bruna S. Soley, Daniela A. Cabrini, Michel F. Otuki
BIOMEDICINE & PHARMACOTHERAPY
(2017)
Article
Medicine, General & Internal
Rosa Camila Lucchetta, Bruno Salgado Riveros, Roberto Pontarolo, Rosana Bento Radominski, Michel Fleith Otuki, Fernando Fernandez-Llimos, Cassyano Januario Correr
Article
Chemistry, Medicinal
Amanda M. Slomp, Sandra M. W. Barreira, Luise Z. B. Carrenho, Camila C. Vandresen, Ingrid F. Zattoni, Stephanie M. S. Lo, Juliana C. C. Dallagnol, Diogo R. B. Ducatti, Alexandre Orsato, M. Eugenia R. Duarte, Miguel D. Noseda, Michel F. Otuki, Alan G. Goncalves
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2017)
