The structure-activity relations of [His(7)]-corazonin were studied using two different bioassay systems; i.e. inhibitory effect on spinning rate in the silkworm, Bombyx mori, and darkening response in albino nymphs of the migratory locust, Locusta migratoria. Deletion of the N-terminus, shortening of the peptide and single amino acid substitutions reduced activity in a similar manner except for the minimum effective dose in the two insects. The results also revealed that the residues at position 1, 3 and 5 were particularly important for biological activity. Despite the different physiological affects, the two insect species exhibited similar structure-activity relationships, suggesting that they might have similar receptor systems.
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http://dx.doi.org/10.1016/s0196-9781(03)00169-4 | DOI Listing |
Drug Des Devel Ther
January 2025
Department of Hepatobiliary Surgery, Jingzhou Hospital Affiliated to Yangtze University, Jingzhou, Hubei, People's Republic of China.
Introduction: Oxidative stress is an important cause of acetaminophen (APAP)-induced liver injury (AILI). Sakuranetin (Sak) is an antitoxin from the cherry flavonoid plant with good antioxidant effects. However, whether sakuranetine has a protective effect on APAP-induced liver injury is not clear.
View Article and Find Full Text PDFHeliyon
January 2025
Department of Chemical Sciences, Faculty of Science and Technology, Universiti Kebangsaan Malaysia (UKM), 46300, Bangi, Selangor, Malaysia.
The Fabaceae family, particularly genus , is renowned for significant medicinal properties. These plants have been used as natural remedies to address various health issues and are rich in flavonoids. Therefore, this review aimed to provide a comprehensive overview of antibacterial activity, structure-activity relationship, especially against drug-resistance and mode of action for flavonoids isolated from .
View Article and Find Full Text PDFDrug Des Devel Ther
January 2025
Department of Anesthesiology, The Affiliated Hospital of Qingdao University, Qingdao, People's Republic of China.
Introduction: The mechanism of remimazolam, a benzodiazepine that activates γ-aminobutyric acid a (GABAa) receptors, in cerebral ischemia/reperfusion (I/R) injury is not well understood. Therefore, we explored whether remimazolam activates protein kinase B (AKT)/glycogen synthase kinase-3β (GSK-3β)/nuclear factor erythroid 2-related factor 2 (NRF2) to attenuate brain I/R injury in transcerebral I/R-injured rats and transoxygenic glucose deprivation/reperfusion (OGD/R)-injured SY5Y cells.
Material And Methods: Remimazolam was added at the beginning of cell and rat reperfusion, and the PI3K/AKT inhibitor LY294002 was added to inhibit the AKT/GSK-3β/NRF2 pathway 24 h before cellular OGD/R treatment and 30 min before rat brain I/R treatment.
Angew Chem Int Ed Engl
January 2025
Sun Yat-Sen University, School of Chemistry, 135 Xingang West, 510275, Guangzhou, CHINA.
Integrating enzymes with reticular frameworks offers promising avenues for access to functionally tailorable biocatalysis. This Minireview explores recent advances in enzyme-reticular frameworks hybrid biocomposites, focusing on the utilization of porous reticular frameworks, including metal-organic frameworks, covalent-organic frameworks, and hydrogen-bonded organic frameworks, to regulate the reactivity of an enzyme encapsulated inside mainly by pore infiltration and in situ encapsulation strategies. We highlight how pore engineering and host-guest interfacial interactions within reticular frameworks create tailored microenvironments that substantially impact the mass transfer and enzyme's conformation, leading to biocatalytic rate enhancement, or imparting enzyme with non-native biocatalytic functions including substrate-selectivity and new activity.
View Article and Find Full Text PDFis a common, waterborne gastrointestinal parasite that causes diarrheal disease worldwide. Currently there are no effective therapeutics to treat cryptosporidiosis in at-risk populations. Since natural products are a known source of anti-parasitic compounds, we screened a library of extracts and pure natural product compounds isolated from bacteria and fungi collected from subterranean environments for activity against .
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