Review
Biochemistry & Molecular Biology
Feyisayo O. Adepoju, Kingsley C. Duru, Erguang Li, Elena G. Kovaleva, Mikhail V. Tsurkan
Summary: Betulin is a natural triterpene with potential wound healing properties. It has protective effects against various diseases such as cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It can modify multiple pharmacological targets and has anti-inflammatory activity on signaling pathways like MAPK, NF-kappa B, and Nrf2.
Review
Neurosciences
Yizhen Jiang, Xiangwen Tang, Peng Deng, Chao Jiang, Yuqing He, Dingjun Hao, Hao Yang
Summary: Neurological diseases have a significant impact on public health and patient's quality of life. Understanding the unique pathological characteristics and underlying molecular mechanisms of each disease is crucial for effective treatment. Fisetin, a flavonoid derived from natural medicinal plants, shows promising neuroprotective effects and reverses cognitive abnormalities through its multifaceted biological activity and therapeutic mechanisms.
MOLECULAR NEUROBIOLOGY
(2023)
Review
Pharmacology & Pharmacy
Syed Shams Ul Hassan, Saptadip Samanta, Raju Dash, Tomasz M. Karpinski, Emran Habibi, Abdul Sadiq, Amirhossin Ahmadi, Simona Bungau
Summary: Fisetin, a flavonoid compound, exhibits potent antioxidant properties and protects cells against oxidative stress, reducing the risk of neuroinflammation and neurodegenerative diseases.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Environmental Sciences
Rajan Kumar, Rakesh Kumar, Navneet Khurana, Sachin Kumar Singh, Shelly Khurana, Surajpal Verma, Neha Sharma, Manish Vyas, Kamal Dua, Rubiya Khursheed, Ankit Awasthi, Sukriti Vishwas
Summary: In this study, a self-nanoemulsifying drug delivery system (SNEDDS) of fisetin, a polyphenolic flavonoid, was developed to enhance its solubility and bioavailability. The SNEDDS formulation significantly improved the rotenone-induced behavioral changes in rats compared to naive fisetin, indicating its potential as an anti-Parkinsonian agent.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2022)
Article
Chemistry, Physical
Wencheng Xia, Feng Wu, Soni Jaiswal, Yijiang Li, Yaoli Peng, Guangyuan Xie
Summary: The study demonstrated that a compound collector consisting of coal tar and diesel can effectively enhance the floatability of low rank coal by modifying the chemical and physical properties of coal surface. The compound collector increased the hydrophobicity of the coal surface, generated more flocs, and accelerated the rupture of liquid film between coal particle and bubble, resulting in improved coal floatability compared to diesel alone.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2021)
Article
Chemistry, Medicinal
Ina Poehner, Antonio Quotadamo, Joanna Panecka-Hofman, Rosaria Luciani, Matteo Santucci, Pasquale Linciano, Giacomo Landi, Flavio Di Pisa, Lucia Dello Iacono, Cecilia Pozzi, Stefano Mangani, Sheraz Gul, Gesa Witt, Bernhard Ellinger, Maria Kuzikov, Nuno Santarem, Anabela Cordeiro-da-Silva, Maria P. Costi, Alberto Venturelli, Rebecca C. Wade
Summary: In this study, a systematic and multidisciplinary approach was used to develop selective antiparasitic compounds. Through computational fragment-based design and crystallographic structure determination, compounds with activity against multiple targets were obtained. Additionally, the combination of polypharmacology design and parasite-specific optimization led to the discovery of compounds effective against T. brucei brucei.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Neurosciences
Rosa Savino, Anna Nunzia Polito, Gabriella Marsala, Antonio Ventriglio, Melanie Di Salvatore, Maria Ida De Stefano, Anna Valenzano, Luigi Marinaccio, Antonello Bellomo, Giuseppe Cibelli, Marcellino Monda, Vincenzo Monda, Antonietta Messina, Rita Polito, Marco Carotenuto, Giovanni Messina
Summary: Agomelatine (AGM) is a new atypical antidepressant that is exclusively prescribed for treating depression in adults. It belongs to the class of melatonin agonists and selective serotonin antagonists (MASS), acting as an agonist for melatonin receptors MT1 and MT2 and as an antagonist for 5-HT2C/5-HT2B receptors. AGM helps to resynchronize disrupted circadian rhythms and improves sleep patterns. Its antagonism on serotonin receptors increases the availability of norepinephrine and dopamine in the prefrontal cortex, leading to its antidepressant and nootropic effects. However, the use of AGM in the pediatric population and its efficacy in neurological developmental disorders like ADHD and ASD have not been extensively studied. This review aims to explore the potential role of AGM in these disorders, highlighting its ability to modulate neurotransmission and promote neuronal plasticity.
Article
Chemistry, Medicinal
Ina Poehner, Antonio Quotadamo, Joanna Panecka-Hofman, Rosaria Luciani, Matteo Santucci, Pasquale Linciano, Giacomo Landi, Flavio Di Pisa, Lucia Dello Iacono, Cecilia Pozzi, Stefano Mangani, Sheraz Gul, Gesa Witt, Bernhard Ellinger, Maria Kuzikov, Nuno Santarem, Anabela Cordeiro-da-Silva, Maria P. Costi, Alberto Venturelli, Rebecca C. Wade
Summary: This study presents a systematic, multidisciplinary approach to the development of selective antiparasitic compounds with multiple targets. The approach combines computational fragment-based design and crystallographic structure determination to derive a structure-activity relationship for multitarget inhibition. The optimized compounds show promising inhibition against various parasitic targets while minimizing toxicity.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Jun Xie, Haigang Du, Shanle Chen, Xiangke Sun, Lin Xin
Summary: The compound modification of surfactants and acetic acid has been found to lead to the transformation of pore shape and affect a wider pore size range in coal samples. Anionic and cationic surfactants can increase hydrophilicity and promote the connection of larger pores, while non-ionic surfactants reduce hydrophilicity, increase porosity, promote connection of pores, and simplify pore structure. Non-ionic surfactants are found to be more conducive to coal seam pore reconstruction compared to anionic and cationic surfactants.
Article
Biochemistry & Molecular Biology
Su-Hwan Kim, Chang-Ki Huh
Summary: The goal of this study was to provide basic data for the development of functional food and health materials from Rhus verniciflua seeds. The researchers isolated and purified an antioxidative compound from the seeds using solvent fractionation and column chromatography, and identified it as fisetin.
Article
Chemistry, Inorganic & Nuclear
Ming Jiang, Juzheng Zhang, Shihang Xu, Yanping Li, Wenjuan Li, Hong Liang, Feng Yang
Summary: In this study, a series of indium compounds were designed and synthesized as potential anticancer agents, and one particular compound showed high cytotoxicity against cisplatin-resistant cells. It exerted its effects through multiple targets, including blocking the cell cycle, inducing apoptosis, inhibiting telomerase, and exhibiting anti-metastatic activity.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Medicinal
Alessandro Papa, Ilaria Cursaro, Luca Pozzetti, Chiara Contri, Martina Cappello, Silvia Pasquini, Gabriele Carullo, Anna Ramunno, Sandra Gemma, Katia Varani, Stefania Butini, Giuseppe Campiani, Fabrizio Vincenzi
Summary: This study aimed to develop multitarget inhibitors for the endocannabinoid system and epigenetic machinery to achieve synergistic therapeutic effects in oxidative stress-related conditions. The first-in-class FAAH-HDAC multitarget inhibitors were designed, synthesized, and evaluated for their neuroprotective properties. Compound 4h showed balanced inhibitory activity against the selected targets and outperformed the standard antioxidant in vitro.
ARCHIV DER PHARMAZIE
(2023)
Article
Cell Biology
Yuting Meng, Qiong Zhang, Kaihang Wang, Xujun Zhang, Rongwei Yang, Kefan Bi, Wenbiao Chen, Hongyan Diao
Summary: The study found significant differences in m6A profiles between severe and mild COVID-19 patients, with RBM15 being a major m6A methyltransferase positively correlated with disease severity. By elevating m6A modifications of multitarget genes, RBM15 regulates host immune response to SARS-CoV-2, indicating its potential as a target for COVID-19 treatment.
CELL DEATH & DISEASE
(2021)
Article
Cell Biology
Peng Zhang, Jian Cui
Summary: It is well established that inflammatory reactions and oxidative stress play a crucial role in the pathogenesis of cerebral ischemia-reperfusion. Fisetin, a flavonoid compound, has been shown to have antioxidant and anti-inflammatory effects in various diseases. This study investigated the neuroprotective effects of fisetin in brain injuries caused by cerebral ischemia-reperfusion, as well as its potential role in modulating NF-kappa B signaling. The results demonstrated that fisetin effectively protected against cell injury, suppressed inflammatory cytokines, and reduced oxidative stress in a dose-dependent manner, ultimately leading to improved outcomes in ischemia-reperfusion injury.
Article
Biochemistry & Molecular Biology
Xiaodong Xu, Yimin Ding, Junbin Jin, Chengjie Xu, Wenyi Hu, Songtao Wu, Guoping Ding, Rui Cheng, Liping Cao, Shengnan Jia
Summary: This study demonstrates the significance of CDK1-STAT3 signaling in maintaining the cancer stemness of PDAC and suggests that targeting this axis with inhibitors like fisetin could be a potential therapeutic strategy to overcome drug resistance and eliminate PDAC.
CELL AND BIOSCIENCE
(2023)