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A bioactivity-guided separation strategy was used to identify novel antistroke compounds from (L.) R. Br., a medicinal plant. As a result, 4 undescribed compounds (, , and ) and 13 known compounds, including 1 new natural product (), were isolated from The structures of these compounds were elucidated through comprehensive spectroscopic techniques, such as 1D/2D nuclear magnetic resonance (NMR) spectroscopy, high-resolution electrospray ionization mass spectrometry (HRESIMS), and quantum chemical calculations. An oxygen-glucose deprivation/reoxygenation (OGD/R)-injured rat pheochromocytoma (PC12) cell model was used to evaluate the antistroke effects of the isolates. Compounds , , , and provided varying degrees of protection against OGD/R injury in the PC12 cells at concentrations of 12.5, 25, and 50 µM. Among the tested compounds, compound demonstrated the most potent neuroprotective effect, which was equivalent to that of the positive control drug (edaravone). Then, transcriptomic and bioinformatics analyses were conducted to reveal the regulatory effect of compound on gene expression. In addition, quantitative real-time PCR (qPCR) was performed to verify the results of the transcriptomic and bioinformatics analyses. These results suggest that the in vitro antistroke effect of compound may be associated with the regulation of the gene. Thus, compound is a promising candidate for the development of novel antistroke drugs derived from natural products, and this topic should be further studied.
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http://dx.doi.org/10.3390/molecules29184389 | DOI Listing |
Bioorg Chem
August 2025
School of Chemistry and Chemical Engineering, Nanjing University of Science & Technology, Nanjing 210094, China. Electronic address:
The emerging recognition of ferroptosis as a pathophysiological nexus in cerebrovascular accidents has unveiled a critical therapeutic exigency for developing novel ferroptosis-targeted therapeutic agents to mitigate stroke-induced neuronal degeneration and dysfunction. The evolutionary-endowed chemical diversity of phytochemicals has emerged as a cornerstone in rational drug design paradigms, serving as indispensable molecular repositories for expediting the development of innovative pharmacotherapeutics with enhanced target specificity and mechanistic novelty. Herein, the screening of polyketides compounds (1-40) derived from Ophiobolus cirsii LZU-1509, which includes 27 underexplored compounds and 13 known polyketides, has identified a potent ferroptosis inhibitor, compound 15, displaying the excellent capacity to rescue ischemic stroke in vitro and in vivo.
View Article and Find Full Text PDFJ Med Chem
April 2025
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China.
Ischemic stroke, a major cause of disability and death worldwide, lacks effective treatments due to the complexity of brain ischemia/reperfusion (I/R) injury. The transient receptor potential melastatin 2 (TRPM2) channel is a promising therapeutic target. In this study, an extracellular TRPM2 inhibitor with an indolizine scaffold was identified through chemical library screening.
View Article and Find Full Text PDFMetabolites
March 2025
Jinfo Mountain Forestry Ecosystem of Chongqing Observation and Research Station, Chongqing Institute of Medicinal Plant Cultivation, Chongqing 408435, China.
Musk is a widely used traditional Chinese medicine derived from musk deer that has the pharmacological effects of "activating blood dredging collateral" and "consciousness-restoring resuscitation". Its volatile compounds (VCs) play a key role in these effects, especially in the treatment of stroke. However, there have been no comprehensive studies on the differences in the VCs of these different musks.
View Article and Find Full Text PDFMolecules
September 2024
Institute of Translational Medicine, Medical College, Yangzhou University, Yangzhou 225009, China.
A bioactivity-guided separation strategy was used to identify novel antistroke compounds from (L.) R. Br.
View Article and Find Full Text PDFDrug Deliv Transl Res
May 2025
Department of Pharmaceutics and Drug Manufacturing, Faculty of Pharmacy, Modern University for Technology and Information, Cairo, Egypt.
Candesartan (CDN) is a useful anti-stroke medication because it lowers blood pressure, inflammation, oxidative stress, angiogenesis and apoptosis. However, CDN has limited efficacy due to its low solubility and poor bioavailability. This study set out to develop nasal pH-responsive in situ hydrogel of CDN-loaded invasomes a (PRHCLI) for enhancing CDN's release, penetration, bioavailability, and effectiveness as a possible treatment for stroke.
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