Farnesylation of the activated RAS oncogene product by protein farnesyltransferase (FTase) is a critical step for its oncogenic function. Bioassay-guided purification of Ferula asafoetida (Umbelliferae) extract led to the isolation of the coumarin-derived sesquiterpene galbanic acid (1) as an active principal for FTase inhibitory activity, together with the four structurally related sesquiterpenes karatavicinol (2), umbelliprenin (3), farnesiferol B (4), and farnesiferol C (5). The 50 % inhibitory concentration (IC (50)) of 1 against FTase in an enzyme-based assay was calculated as 2.5 µM. Compound 1 also demonstrated potent inhibition of the proliferation of oncogenic RAS-transformed NIH3T3/Hras-F in a dose-dependent manner. The IC (50) value of 1 on the proliferation of oncogenic RAS-transformed NIH3T3/Hras-F cells was calculated as 16.2 µM, whereas its IC (50) value on control vector-transfected normal RAS-containing NIH3T3/ZIPneo cells was 58.5 µM.
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http://dx.doi.org/10.1055/s-0030-1250049 | DOI Listing |
Adv Biomed Res
November 2024
Molecular and Cell Biology Research Center, Faculty of Medicine, Mazandaran University of Medical Sciences, Sari, Iran.
Background: Non-alcoholic fatty liver disease is related to lipid accumulation and inflammation. Considering the role of lipin-1 and lipin-2 in fat homeostasis and inflammation, this study aimed to explore the effect of galbanic acid (Gal) and resveratrol (RSV) on alterations in the gene expression levels and protein abundance of lipin-1 and lipin-2 in HepG2 liver cells lipid-enriched with palmitate (Pal).
Materials And Methods: HepG2 cells were subjected to different amounts of Gal and RSV for 24 hours in the presence of Pal to induce lipid accumulation.
Bioorg Chem
September 2024
Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran; Diabetes Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran. Electronic address:
α-Glucosidase inhibitory activity of galbanic acid and its new amide derivatives 3a-n were investigated. Galbanic acid and compounds 3a-n showed excellent anti-α-glucosidase activity with IC values ranging from 0.3 ± 0.
View Article and Find Full Text PDFArch Physiol Biochem
December 2024
Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran.
Introduction: Sirtuin1 (SIRT1) plays a crucial role in the pathophysiology of non-alcoholic fatty liver disease. We investigated the mechanistic role of galbanic acid (Gal) as a regulator of SIRT1 and .
Methods: HepG2 cells were treated with Gal in the presence or absence of EX-527, a SIRT1-specific inhibitor, for 24 h.
Naunyn Schmiedebergs Arch Pharmacol
August 2024
Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
High mortality rate of melanoma is due to the metastasis of malignant cells. Galbanic acid (GBA) is a natural sesquiterpene coumarin with valuable pharmaceutical activities. Our study aimed to investigate whether GBA can affect the migration, invasion, and adhesion of melanoma cells.
View Article and Find Full Text PDFPathol Res Pract
August 2023
Department of Human Genetics, McGill University, Montreal, Canada; Victor Philip Dahdaleh Institute of Genomic Medicine at McGill University, Montreal, Canada; Department of Biochemistry and Clinical Laboratories, Faculty of Medicine, Tabriz University of Medical Sciences, Tabriz, Iran. Electronic address:
Galbanic acid (GBA), as a natural compound has potential anticancer properties. It has been documented that GBA shows promising therapeutic potential against various types of cancer, including breast, lung, colon, liver, and prostate cancer. Several mechanisms involve im anti-tumor effects of GBA include apoptosis induction, cell cycle arrest, inhibition of angiogenesis, suppression of metastasis, and modulation of immune responses.
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