Article
Biochemistry & Molecular Biology
Eisuke Kato, Ai Tsuruma, Ayaka Amishima, Hiroshi Satoh
Summary: Young barley leaf extract (YB) has pancreatic lipase inhibitory activity, which reduces lipid absorption and exhibits antiobesity effects. Fructose-bisphosphate aldolase in YB serves as a proteinous lipase inhibitor, showing characteristic inhibition at a low concentration of 16 ng/mL.
BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Peiyi Jin, Linzhou Chen, Jinjian Zhong, Tiefeng Yuan, Lin Gan, Jilong Huang, Liping Wang, Huajun Fan, Chen Lin
Summary: This study identified and named the major lipase inhibitory components in Dioscoreae nipponica, namely protodioscin, protogracillin, dioscin, and gracillin. The study also confirmed that dioscin and gracillin were the main inhibitors based on stability tests. This method not only revealed the lipase inhibitory components in Dioscoreae nipponica, but also provided an effective approach for hierarchical screening of lipase inhibitors from natural plants.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemistry & Molecular Biology
Claudia Sciacca, Nunzio Cardullo, Luana Pulvirenti, Antonella Di Francesco, Vera Muccilli
Summary: Obesity is a complex disease associated with excessive body fat and is considered a risk factor for various pathologies. Pancreatic lipase (PL) plays a crucial role in fat digestion and its inhibition is being explored as a potential treatment for obesity. In this study, a library of new compounds inspired by natural neolignans was synthesized and evaluated for their inhibitory activity against PL. Several synthetic compounds showed better inhibitory activity compared to the natural neolignans, highlighting their potential as more effective PL inhibitors.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Ravindra Patil, Samadhan Patil, Vijay Maheshwari, Mohini Patil
Summary: The study demonstrates the inhibitory effect of pentacyclic triterpenoids (PIT) on pancreatic lipase (PL), indicating their potential as a natural PL inhibitor in the treatment of obesity. The isolated PTT was identified as lupeol, and the endophytic isolate was identified as Colletotrichum gigasporum, showing promise as a valuable bioresource for obesity treatment.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Nutrition & Dietetics
Yongqi Tian, Cuicui Liu, Shaoyun Wang, Ming Du, Beiwei Zhu
Summary: Obesity is a serious public health problem and requires the discovery of highly safe and effective PLIs. In this study, a method using magnetic nanoparticles was established to rapidly fish out potential PLIs, resulting in the identification of two new PLIs. These peptides can stably bind to the PL active site and have inhibitory effects on PL.
FRONTIERS IN NUTRITION
(2022)
Article
Biochemistry & Molecular Biology
Jinfang Xu, Pengkun Cao, Zhiyu Fan, Xujing Luo, Gangqiang Yang, Tingli Qu, Jianping Gao
Summary: In this study, a magnetic core-shell metal-organic frameworks composite was fabricated as a support for the covalent immobilization of porcine pancreatic lipase (PPL). The resulting composite exhibited high loading capacity and relative activity recovery, and PPL showed enhanced tolerance to temperature and pH after immobilization. Ligand fishing was performed using the composite, resulting in the identification of eight lipase inhibitors. This method provides a feasible, selective, and effective platform for discovering enzyme inhibitors from natural products.
Article
Biochemistry & Molecular Biology
Sunil Kumar Singh, Sandeep Kumar, Navin Viswakarma, Daniel R. Principe, Subhasis Das, Gautam Sondarva, Rakesh Sathish Nair, Piush Srivastava, Subhash C. Sinha, Paul J. Grippo, Gregory R. J. Thatcher, Basabi Rana, Ajay Rana
Summary: Research shows that MAP4K4 promotes pancreatic cancer by phosphorylating MLK3, and the MAP4K4-specific inhibitor GNE-495 can block pancreatic cancer cell growth and extend survival in animal models.
Article
Pharmacology & Pharmacy
Bilal Ahmad, Emily P. Friar, Emerald Taylor, Muhammad Sufyan Vohra, Christopher J. Serpell, Michelle D. Garrett, Jason Siau Ee Loo, Isabel Lim Fong, Eng Hwa Wong
Summary: In this study, the anti-obesity effects of two flavones (PMF and TMF) were evaluated through inhibition of pancreatic lipase and inhibition of adipogenesis. Both flavones competitively inhibited pancreatic lipase activity and reduced lipid accumulation in adipocytes. They also downregulated the expression of adipogenic and lipogenic genes and upregulated the expression of lipolytic genes. Overall, PMF was found to be a more potent inhibitor of both pancreatic lipase activity and adipogenesis compared to TMF. These findings suggest that PMF and TMF have anti-obesity activities and should be further investigated.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Jingyi Jian, Jiaming Yuan, Yu Fan, Jincai Wang, Tingting Zhang, Jeroen Kool, Zhengjin Jiang
Summary: A screening platform for pancreatic lipase inhibitors was established by combining magnetic beads-based ligand fishing and high-resolution bioassay profiling, allowing rapid and accurate screening of bioactive components from complex natural products.
Article
Integrative & Complementary Medicine
Larissa Junqueira Gatto, Gustavo Rezende Bellei de Oliveira, Katlin Suellen Rech, Paula Francislaine Moura, Caroline Gribner, Francis Jose Zortea Merino, Suelen Avila, Josiane de Fatima Gaspari Dias, Obdulio Gomes Miguel, Marilis Dallarmi Miguel
Summary: The study found that EBF (IC50: 3.21 mu g/mL) and FFA (IC50: 1.14 mu g/mL) of Myrcia hatschbachii showed stronger inhibitory activity against alpha-glucosidase compared to acarbose (IC50: 193.65 mu g/mL); they exhibited inhibitory effects on pancreatic lipase, antioxidant potential, and presence of gallic and ellagic acids in FFA.
BOLETIN LATINOAMERICANO Y DEL CARIBE DE PLANTAS MEDICINALES Y AROMATICAS
(2021)
Article
Gastroenterology & Hepatology
Shalini G. Hegde, Sindhu Kashyap, Sarita Devi, Prasanna Kumar, A. John Michael Raj, Anura Kurpad
Summary: This study aimed to investigate the prevalence of exocrine pancreatic insufficiency (EPI) in children with acute pancreatitis (AP) and evaluate the diagnostic ability of a breath test. The study found that 66.7% of AP children in the sample had EPI during admission, and the condition persisted during follow-up. The 4-hour breath test showed good diagnostic ability for detecting EPI in children.
Article
Chemistry, Inorganic & Nuclear
Tongshun An, Chenwei Liu, Yanzhao Yin, Xiao-Feng Wu, Zhiping Yin
Summary: A general method for the synthesis of benzoxazin-4-ones using a palladium and silver co-catalyzed system has been developed. The method employs benzotriazoles as substrates and Cr(CO)(6) as a solid carbonyl source, and proceeds through a ring-opening/denitrogenative/carbonylation cascade reaction to yield the desired products. This protocol eliminates the need for toxic CO gas and specialized equipment, and can also be applied to the late-stage functionalization of uricosuric agent probenecid-derived substrates.
Article
Biochemical Research Methods
Sihua Quan, Mengyi Wen, Ping Xu, Chu Chu, Hui Zhang, Kai Yang, Shengqiang Tong
Summary: This study aims to efficiently screen pancreatic lipase inhibitors in Rheum palmatum using affinity ultrafiltration-high-performance liquid chromatography (AUF-HPLC) combined with high-resolution inhibition profiling (HRIP). Several new potent pancreatic lipase inhibitors were discovered in this study.
PHYTOCHEMICAL ANALYSIS
(2023)
Article
Biochemistry & Molecular Biology
Xuan Li, Sayo Morita, Hiroaki Yamada, Keita Koga, Wakana Ota, Toma Furuta, Atsushi Yamatsu, Mujo Kim
Summary: Pancreatic lipase is crucial in the digestion of dietary fat, and modulating its activity is a strategy to combat obesity. Orlistat is currently the only approved pancreatic lipase inhibitor for obesity treatment, but its side effects limit its tolerability. This study identified free linoleic acid and oleic acid as potent inhibitors of pancreatic lipase, with potential for weight management.
Article
Nutrition & Dietetics
Xuan Li, Hiroaki Yamada, Sayo Morita, Yusuke Yamashita, Youngil Kim, Takashi Kometani, Nikesh Narang, Toma Furuta, Mujo Kim
Summary: A study found that the ethanolic extract of sesame meal is a potent pancreatic lipase inhibitor, and it can significantly reduce postprandial triglyceride concentration and improve lipidemic profile. In a crossover trial, treatment with the sesame meal extract showed significant improvement in postprandial blood indicators after high dietary fat intake in healthy individuals. This suggests the significant potential of free linoleic acid and oleic acid and natural products rich in these compounds for managing obesity and related conditions.
Article
Food Science & Technology
Nadia S. R. S. Mota, Maicon R. Kviecinski, Rodrigo C. Zeferino, Daniela A. de Oliveira, Lizandra C. Bretanha, Sandra R. S. Ferreira, Gustavo A. Micke, Danilo Wilhelm Filho, Rozangela C. Pedrosa, Fabiana Ourique
FOOD AND CHEMICAL TOXICOLOGY
(2018)
Article
Nutrition & Dietetics
Isabela Machado Barbosa David, Flavia de Souza Fernandes, Juliana Barreto dos Santos Silva Ferreira, Daniela Dero Ludtke, Daniel Fernandes Martins, Franciane Bobinski, Thiago Bezerra Gaspar Carvalho da Silva, Luiza Daux Buffon, Maria Biatriz Rodrigues Kopper, Gustavo Silveira da Silva, Rodrigo Costa Zeferino, Rozangela Curi Pedrosa, Maicon Roberto Kviecinski
NUTRITION RESEARCH
(2019)
Article
Oncology
Rodrigo C. Zeferino, Nadia S. R. S. Mota, Valdelucia M. A. S. Grinevicius, Karina B. Filipe, Paola M. Sulis, Fatima R. M. B. Silva, Danilo W. Filho, Claus T. Pich, Rozangela C. Pedrosa
INVESTIGATIONAL NEW DRUGS
(2020)
Article
Environmental Sciences
Renan R. dos Santos, Erica C. Rosa, Thiago Rosa, Eduardo A. Ferreira, Eliana F. Gris, Rosangela V. de Andrade, Angelica A. Amato
INTERNATIONAL JOURNAL OF ENVIRONMENTAL RESEARCH AND PUBLIC HEALTH
(2019)
Article
Food Science & Technology
Valdelucia M. A. S. Grinevicius, Katia S. Andrade, Nadia S. R. S. Mota, Lizandra C. Bretanha, Karina B. Felipe, Sandra R. S. Ferreira, Rozangela C. Pedrosa
FOOD AND CHEMICAL TOXICOLOGY
(2019)
Article
Oncology
Jean C. Benassi, Flavio A. R. Barbosa, Valdelucia M. A. S. Grinevicius, Fabiana Ourique, Daniela Coelho, Karina B. Felipe, Antonio L. Braga, Danilo W. Filho, Rozangela C. Pedrosa
Summary: This study evaluated the cytotoxic and antiproliferative potential of Se-DHPM on cancer cells, with 49H showing selective cytotoxicity to HepG2 cells and inducing apoptosis. Molecular assays revealed interactions between 49H and DNA, impacting DNA structure and cell cycle regulation.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2021)
Review
Genetics & Heredity
Caroline Fratelli, Jhon Siqueira, Calliandra Silva, Eduardo Ferreira, Izabel Silva
Article
Biochemistry & Molecular Biology
Jean C. Benassi, Flavio A. R. Barbosa, Graziani Candiotto, Valdelucia M. A. S. Grinevicius, Danilo Wilhelm Filho, Antonio L. Braga, Rozangela C. Pedrosa
Summary: The study evaluated the cytotoxic and antiproliferative potential of new dihydropyrimidinone-derived selenoesters compounds against breast cancer cells, with 49A and 49F compounds showing the highest cytotoxicity for MCF-7 cells and selectivity for non-tumor cells. Compound 49F demonstrated antiproliferative potential by reducing colony formation. Molecular assays indicated different interactions with CT-DNA, with compound 49A causing hyperchromism and 49F causing hypochromism, while docking and molecular dynamics simulations suggested both compounds act as minor groove ligands stabilized by hydrogen bonds and hydrophobic interactions, with 49A being more energetically favorable. Despite some ADMET violations for 49F, overall results suggest it as a promising leader compound with anti-tumor potential for breast cancer.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Aline Aita Naime, Flavio Augusto Rocha Barbosa, Diones Caeran Bueno, Rozangela Curi Pedrosa, Romulo Faria Santos Canto, Dirleise Colle, Antonio Luiz Braga, Marcelo Farina
Summary: The study focused on the temporal events mediating the prevention of ferroptosis and found that the protective effects of anti-ferroptotic agents were reduced when delivered at time-points characterized by increased lipoperoxidation. Direct antioxidant efficacy was not significantly associated with cytoprotective effects.
FREE RADICAL RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Giovanna Oliveira de Brito, Bruna Cabral Reis, Eduardo A. Ferreira, Nilton T. Vilela Junqueira, Livia C. L. Sa-Barreto, Fulvio Mattivi, Urska Vrhovsek, Eliana Fortes Gris
Summary: Tapereba peel extract exhibits significant phenolic compound content and antioxidant activity, with high retention of phenolic compounds when microencapsulated with chitosan. This study provides valuable insights into the composition and stability of tapereba peel extract.
Article
Cardiac & Cardiovascular Systems
Marianne Lucena da Silva, Ivo Vieira de Sousa Neto, Alexandra C. G. B. de Lima, Fabricio Barin, Otavio de Toledo Nobrega, Rita de Cassia Marqueti, Graziella F. B. Cipriano, Joao Luiz Quagliotti Durigan, Eduardo Antonio Ferreira, Martim Bottaro, Ross Arena, Larry P. Cahalin, Jose Alberto Neder, Gerson Cipriano Junior
Summary: This study investigated the effects of home-based low-frequency electrical stimulation (LFES) on plasma cytokines profile, oxidative stress biomarkers, metalloproteinases (MMPs) activity, and exercise performance in heart failure (HF) patients. The results showed that LFES increased active-MMP2 activity and decreased active-MMP9 activity, but did not elicit changes in cytokines, oxidative stress biomarkers, or exercise performance.
JOURNAL OF CARDIOVASCULAR DEVELOPMENT AND DISEASE
(2022)
Article
Health Care Sciences & Services
Joao de Sousa Pinheiro Barbosa, Leonardo Costa Pereira, Marileusa Dosolina Chiarello, Kerolyn Ramos Garcia, Giovanna Oliveira de Brito, Eliana Fortes Gris, Margo Gomes de Oliveira Karnikowski
Summary: This study analyzed the use of legal and illegal drugs by elderly individuals who received psychosocial assistance in the Federal District of Brazil. The majority of elderly users were male, with a higher consumption rate of illegal substances compared to legal ones. The elderly used drugs for a long period of time but had low adherence to treatment, with alcohol being the most prevalent psychoactive substance.
Article
Biochemistry & Molecular Biology
Daniela Coelho dos Santos, Jamal Rafique, Sumbal Saba, Gabriela M. Almeida, Tamila Siminski, Cynthia Padua, Danilo W. Filho, Ariane Zamoner, Antonio L. Braga, Rozangela C. Pedrosa, Fabiana Ourique
Summary: This study demonstrated the antitumor mechanism of selenylated imidazo[1,2-a]pyridine compound IP-Se-06 against HepG2 cells, showing high cytotoxicity and selectivity, as well as inhibition of cell proliferation, induction of apoptosis, and interference with cell cycle proteins and DNA fragmentation, both in vitro and in vivo.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2021)