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Three structurally related sets of hydroisobenzofuran analogs of sclerophytin A were prepared in three or four steps from (S)-(+)-carvone via an aldol-cycloaldol sequence. The most potent members of each set of analogs exhibited IC(50)'s of 1-3 microM in growth inhibitory assays against KB3 cells. The NCI 60-cell line 5-dose assay for analog 6h revealed a GI(50)=0.148 microM and LC(50)=9.36 microM for the RPMI-8226 leukemia cell line, and a GI(50)=0.552 microM and LC(50)=26.8 microM for the HOP-92 non-small cell lung cancer cell line.
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http://dx.doi.org/10.1016/j.bmcl.2009.10.079 | DOI Listing |
VDAC, the most abundant protein in the outer mitochondrial membrane, plays a central role in mitochondrial physiology. Its oligomerization has been contemplated to be involved in critical processes such as mtDNA release and apoptosis, yet the underlying molecular mechanisms remain poorly defined. VBIT-4, a small molecule widely used as a VDAC1 oligomerization inhibitor, has seen extensive applications over the past five years without proper mechanistic characterization.
View Article and Find Full Text PDFPhysiol Res
July 2025
Department of Pharmacology, Pharmacy Faculty, Cukurova University, Adana, Republic of Türkiye.
The activation of Calcium-Sensing Receptors (CaSRs) reduces detrusor activity in bladder tissues. Also, hydrogen sulfide (H2S) produces in bladder tissue and regulates the bladder smooth muscles tone. However, there is no evidence of the interaction between CaSRs and H2S in bladder tissue.
View Article and Find Full Text PDFPhysiol Res
March 2025
Department of Radiology, Suining Central Hospital, Suining, Sichuan Province, China.
To explore the effects and underlying mechanisms of Mdivi-1 on three common clinical models of acute kidney injury (AKI). Three common AKI cell models were constructed, classified into the control group (human renal tubular epithelial cells [HK-2] cells), the Iohexol group (HK-2 cells treated with Iohexol), the Genta group (HK-2 cells treated with Gentamicin), and the Cis group (HK-2 cells treated with Cisplatin). To explore the optimal protective concentration of Mdivi-1 for each AKI cell model, the experimental design consisted of the following seven groups: the control group (HK-2 cells cultured in medium), three injury groups (HK-2 cells subjected to Iohexol, Gentamicin, or Cisplatin), and the corresponding protection groups (with a certain concentration of Mdivi-1 added to each injury group).
View Article and Find Full Text PDFPhysiol Res
March 2025
Department of Pharmacology, Pharmacy Faculty, Cukurova University, Adana, Republic of Türkiye.
Hydrogen sulfide (H2S) is a gas neurotransmitter that is synthesized in various mammalian tissues including vascular tissues and regulates vascular tone. The aim of this study is to investigate whether the endogenous L-cysteine/H2S pathway is impaired due to aging and endothelial denudation in mouse isolated thoracic aorta. For this purpose, young (3-4 months) and old (23-25 months) mice were used in the experiments.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
December 2024
Faculty of Chemistry and Chemical Engineering, Babeş-Bolyai University, 11 Arany Janos str., 400028 Cluj-Napoca, Romania. Electronic address:
Novel (N-arylamino)phenothiazinium dyes containing meta-substituted-arylamine auxochrome units were successfully obtained by applying a sonochemical protocol designed for a more efficient energy usage in the preparation of methylene blue (MB) analogues. Single crystal X-ray diffraction analysis revealed the spatial arrangement in aggregated crystalline state of (N-(meta-bromoaryl)amino)phenothiazinium dye with minor variances induced by the nature of the halogenide counterion (iodide or chloride). The optical UV-vis properties of the novel (N-arylamino)phenothiazinium dyes were comparable to those of the parent MB, with the longest wavelength absorption maxima situated in the visible range (640-680 nm), large molar extinction coefficients (log ε = 4.
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