Antiviral influenza treatments and hemorrhage ‐related adverse events in the United States Food and Drug Administration Adverse Event Reporting System (FAERS) database
ConclusionIn this study, some signals for GI hemorrhage were observed, particularly for peramivir and baloxavir marboxil. Further investigation is warranted to better understand and evaluate the potential risks of GI hemorrhage associated with antiviral treatments for influenza. (Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy)
Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy - April 25, 2024 Category: Drugs & Pharmacology Authors: Jyotirmoy Sarker, Emir Carkovic, Karolina Ptaszek, Todd A. Lee Tags: RESEARCH ARTICLE Source Type: research

Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity
CONCLUSION: The rupestonic acid L-ephedrine ester (A) and rupestonic acid L-ephedrine complex (B) were synthesized and characterized using 1H NMR and 13C NMR. Moreover, their purity was determined by HPLC. Both compounds A and B exhibited more potent activities against the strains of A/PR/8/34 (H1N1) and A/FM/1/47 (H1N1) than rupestonic acid. Compound A can be regarded as a very promising lead compound for the development of anti-influenza inhibitors. Based on these results, more rupestonic acid derivatives will be designed and synthesized in the future for the development of anti-influenza inhibitors.PMID:38623973 | DOI:1...
Source: Current Pharmaceutical Design - April 16, 2024 Category: Drugs & Pharmacology Authors: Jianping Yong Canzhong Lu Source Type: research

Synthesis of Rupestonic Acid L-Ephedrine Derivatives with Preliminary In vitro Anti-influenza Viral Activity
CONCLUSION: The rupestonic acid L-ephedrine ester (A) and rupestonic acid L-ephedrine complex (B) were synthesized and characterized using 1H NMR and 13C NMR. Moreover, their purity was determined by HPLC. Both compounds A and B exhibited more potent activities against the strains of A/PR/8/34 (H1N1) and A/FM/1/47 (H1N1) than rupestonic acid. Compound A can be regarded as a very promising lead compound for the development of anti-influenza inhibitors. Based on these results, more rupestonic acid derivatives will be designed and synthesized in the future for the development of anti-influenza inhibitors.PMID:38623973 | DOI:1...
Source: Current Pharmaceutical Design - April 16, 2024 Category: Drugs & Pharmacology Authors: Jianping Yong Canzhong Lu Source Type: research

Viruses, Vol. 16, Pages 388: Impact of the H274Y Substitution on N1, N4, N5, and N8 Neuraminidase Enzymatic Properties and Expression in Reverse Genetic Influenza A Viruses
In conclusion, the H274Y-NA substitution of different group-1-NAs systematically reduced their affinity for MUNANA substrate without a significant impact on NA Vm. The impact of the H274Y-NA substitution on viral NA expression was different according to the studied NA. (Source: Viruses)
Source: Viruses - March 1, 2024 Category: Virology Authors: Alexandre Gaymard Caroline Picard Guilhem Vazzoler Pascale Massin Emilie Frobert Murielle Sabatier Mendy Barthelemy Martine Valette Mich èle Ottmann Jean-S ébastien Casalegno Bruno Lina Vanessa Escuret Tags: Communication Source Type: research

Viruses, Vol. 15, Pages 2366: Antiviral Activity of Probenecid and Oseltamivir on Influenza Virus Replication
In this study, we evaluated the efficacy of the neuraminidase inhibitor, oseltamivir, against probenecid, which targets the host cells and is less likely to engender resistance. Our results show that probenecid has superior antiviral efficacy compared to oseltamivir in both in vitro replication assays and in vivo mouse models of influenza infection. (Source: Viruses)
Source: Viruses - November 30, 2023 Category: Virology Authors: Jackelyn Murray David E. Martin Fred D. Sancilio Ralph A. Tripp Tags: Article Source Type: research

GSE247870 Targeting SOX13 inhibits the assembly of respiratory chain supercomplexes to overcome ferroptosis-resistance in gastric cancer
Contributors : Mingzhe Ma ; Hui YangSeries Type : Genome binding/occupancy profiling by high throughput sequencingOrganism : Homo sapiensTherapeutic resistance represents a bottleneck to treatment in advanced gastric cancer (GC). Ferroptosis is an iron-dependent form of non-apoptotic cell death and is associated with anti-cancer therapeutic efficacy. Further investigations are required to clarify the underlying mechanisms. Ferroptosis-resistant GC cell lines were constructed. Dysregulated mRNAs between ferroptosis-resistant and parental cell lines were identified. The expression of SOX13/SCAF1 was manipulated in GC cell ...
Source: GEO: Gene Expression Omnibus - November 17, 2023 Category: Genetics & Stem Cells Tags: Genome binding/occupancy profiling by high throughput sequencing Homo sapiens Source Type: research

Visualizing intracellular sialidase activity of influenza A virus neuraminidase using a fluorescence imaging probe
In this study, we established a protocol to visualize the sialidase activity of intracellular NA at the Golgi of influenza A virus-infected cells using BTP9-Neu5Ac. Furthermore, we employed this fluorescence imaging protocol to elucidate the intracellular inhibition of laninamivir octanoate, an anti-influenza drug. At approximately 7h after infection, newly synthesized viral NAs localized at the Golgi. Using our developed protocol, we successfully histochemically stained the sialidase activity of intracellular viral NAs localized at the Golgi. Importantly, we observed that laninamivir octanoate effectively inhibited the in...
Source: Journal of Virological Methods - November 1, 2023 Category: Virology Authors: Koki Amano Yuuki Kurebayashi Tadanobu Takahashi Yutaka Narimichi Tadamune Otsubo Kiyoshi Ikeda Akira Minami Hideyuki Takeuchi Source Type: research

Visualizing intracellular sialidase activity of influenza A virus neuraminidase using a fluorescence imaging probe
In this study, we established a protocol to visualize the sialidase activity of intracellular NA at the Golgi of influenza A virus-infected cells using BTP9-Neu5Ac. Furthermore, we employed this fluorescence imaging protocol to elucidate the intracellular inhibition of laninamivir octanoate, an anti-influenza drug. At approximately 7h after infection, newly synthesized viral NAs localized at the Golgi. Using our developed protocol, we successfully histochemically stained the sialidase activity of intracellular viral NAs localized at the Golgi. Importantly, we observed that laninamivir octanoate effectively inhibited the in...
Source: Journal of Virological Methods - November 1, 2023 Category: Virology Authors: Koki Amano Yuuki Kurebayashi Tadanobu Takahashi Yutaka Narimichi Tadamune Otsubo Kiyoshi Ikeda Akira Minami Hideyuki Takeuchi Source Type: research

Visualizing intracellular sialidase activity of influenza A virus neuraminidase using a fluorescence imaging probe
In this study, we established a protocol to visualize the sialidase activity of intracellular NA at the Golgi of influenza A virus-infected cells using BTP9-Neu5Ac. Furthermore, we employed this fluorescence imaging protocol to elucidate the intracellular inhibition of laninamivir octanoate, an anti-influenza drug. At approximately 7 h after infection, newly synthesized viral NAs localized at the Golgi. Using our developed protocol, we successfully histochemically stained the sialidase activity of intracellular viral NAs localized at the Golgi. Importantly, we observed that laninamivir octanoate effectively inhibited the i...
Source: Journal of Virological Methods - November 1, 2023 Category: Virology Authors: Koki Amano Yuuki Kurebayashi Tadanobu Takahashi Yutaka Narimichi Tadamune Otsubo Kiyoshi Ikeda Akira Minami Hideyuki Takeuchi Source Type: research

Visualizing intracellular sialidase activity of influenza A virus neuraminidase using a fluorescence imaging probe
In this study, we established a protocol to visualize the sialidase activity of intracellular NA at the Golgi of influenza A virus-infected cells using BTP9-Neu5Ac. Furthermore, we employed this fluorescence imaging protocol to elucidate the intracellular inhibition of laninamivir octanoate, an anti-influenza drug. At approximately 7 h after infection, newly synthesized viral NAs localized at the Golgi. Using our developed protocol, we successfully histochemically stained the sialidase activity of intracellular viral NAs localized at the Golgi. Importantly, we observed that laninamivir octanoate effectively inhibited the i...
Source: Journal of Virological Methods - November 1, 2023 Category: Virology Authors: Koki Amano Yuuki Kurebayashi Tadanobu Takahashi Yutaka Narimichi Tadamune Otsubo Kiyoshi Ikeda Akira Minami Hideyuki Takeuchi Source Type: research

Neuraminidase inhibition improves endothelial function in diabetic mice
Am J Physiol Heart Circ Physiol. 2023 Oct 6. doi: 10.1152/ajpheart.00337.2023. Online ahead of print.ABSTRACTNeuraminidases cleave sialic acids from glycocalyx structures and plasma neuraminidase activity is elevated in type 2 diabetes (T2D). Therefore, we hypothesize circulating neuraminidase degrades the endothelial glycocalyx and diminishes flow-mediated dilation (FMD), while its inhibition restores shear mechanosensation and endothelial function in T2D settings. We found that compared with controls, T2D subjects have higher plasma neuraminidase activity, reduced plasma nitrite concentrations, and diminished FMD. Ex viv...
Source: American Journal of Physiology. Heart and Circulatory Physiology - October 6, 2023 Category: Physiology Authors: Christopher A Foote Francisco I Ramirez-Perez James A Smith Thaysa Ghiarone Mariana Morales-Quinones Neil J McMillan Marc A Augenreich Gavin Power Katherine Burr Annayya Aroor Shawn B Bender Camila Manrique-Acevedo Jaume Padilla Luis A Martinez-Lemus Source Type: research

Neuraminidase inhibition improves endothelial function in diabetic mice
Am J Physiol Heart Circ Physiol. 2023 Oct 6. doi: 10.1152/ajpheart.00337.2023. Online ahead of print.ABSTRACTNeuraminidases cleave sialic acids from glycocalyx structures and plasma neuraminidase activity is elevated in type 2 diabetes (T2D). Therefore, we hypothesize circulating neuraminidase degrades the endothelial glycocalyx and diminishes flow-mediated dilation (FMD), while its inhibition restores shear mechanosensation and endothelial function in T2D settings. We found that compared with controls, T2D subjects have higher plasma neuraminidase activity, reduced plasma nitrite concentrations, and diminished FMD. Ex viv...
Source: American Journal of Physiology. Heart and Circulatory Physiology - October 6, 2023 Category: Physiology Authors: Christopher A Foote Francisco I Ramirez-Perez James A Smith Thaysa Ghiarone Mariana Morales-Quinones Neil J McMillan Marc A Augenreich Gavin Power Katherine Burr Annayya Aroor Shawn B Bender Camila Manrique-Acevedo Jaume Padilla Luis A Martinez-Lemus Source Type: research

Neuraminidase inhibition improves endothelial function in diabetic mice
Am J Physiol Heart Circ Physiol. 2023 Oct 6. doi: 10.1152/ajpheart.00337.2023. Online ahead of print.ABSTRACTNeuraminidases cleave sialic acids from glycocalyx structures and plasma neuraminidase activity is elevated in type 2 diabetes (T2D). Therefore, we hypothesize circulating neuraminidase degrades the endothelial glycocalyx and diminishes flow-mediated dilation (FMD), while its inhibition restores shear mechanosensation and endothelial function in T2D settings. We found that compared with controls, T2D subjects have higher plasma neuraminidase activity, reduced plasma nitrite concentrations, and diminished FMD. Ex viv...
Source: American Journal of Physiology. Heart and Circulatory Physiology - October 6, 2023 Category: Physiology Authors: Christopher A Foote Francisco I Ramirez-Perez James A Smith Thaysa Ghiarone Mariana Morales-Quinones Neil J McMillan Marc A Augenreich Gavin Power Katherine Burr Annayya Aroor Shawn B Bender Camila Manrique-Acevedo Jaume Padilla Luis A Martinez-Lemus Source Type: research

Neuraminidase inhibition improves endothelial function in diabetic mice
Am J Physiol Heart Circ Physiol. 2023 Oct 6. doi: 10.1152/ajpheart.00337.2023. Online ahead of print.ABSTRACTNeuraminidases cleave sialic acids from glycocalyx structures and plasma neuraminidase activity is elevated in type 2 diabetes (T2D). Therefore, we hypothesize circulating neuraminidase degrades the endothelial glycocalyx and diminishes flow-mediated dilation (FMD), while its inhibition restores shear mechanosensation and endothelial function in T2D settings. We found that compared with controls, T2D subjects have higher plasma neuraminidase activity, reduced plasma nitrite concentrations, and diminished FMD. Ex viv...
Source: American Journal of Physiology. Heart and Circulatory Physiology - October 6, 2023 Category: Physiology Authors: Christopher A Foote Francisco I Ramirez-Perez James A Smith Thaysa Ghiarone Mariana Morales-Quinones Neil J McMillan Marc A Augenreich Gavin Power Katherine Burr Annayya Aroor Shawn B Bender Camila Manrique-Acevedo Jaume Padilla Luis A Martinez-Lemus Source Type: research

Neuraminidase inhibition improves endothelial function in diabetic mice
Am J Physiol Heart Circ Physiol. 2023 Oct 6. doi: 10.1152/ajpheart.00337.2023. Online ahead of print.ABSTRACTNeuraminidases cleave sialic acids from glycocalyx structures and plasma neuraminidase activity is elevated in type 2 diabetes (T2D). Therefore, we hypothesize circulating neuraminidase degrades the endothelial glycocalyx and diminishes flow-mediated dilation (FMD), while its inhibition restores shear mechanosensation and endothelial function in T2D settings. We found that compared with controls, T2D subjects have higher plasma neuraminidase activity, reduced plasma nitrite concentrations, and diminished FMD. Ex viv...
Source: American Journal of Physiology. Heart and Circulatory Physiology - October 6, 2023 Category: Physiology Authors: Christopher A Foote Francisco I Ramirez-Perez James A Smith Thaysa Ghiarone Mariana Morales-Quinones Neil J McMillan Marc A Augenreich Gavin Power Katherine Burr Annayya Aroor Shawn B Bender Camila Manrique-Acevedo Jaume Padilla Luis A Martinez-Lemus Source Type: research