Treatment of ErbB2-overexpressing BT474 and MDA-MB-453 breast cancer cells with 1 to 10 μmol/L betulinic acid inhibited cell growth, induced apoptosis, downregulated specificity protein (Sp) transcription factors Sp1, Sp3, and Sp4, and decreased expression of ErbB2. Individual or combined knockdown of Sp1, Sp3, Sp4 by RNA interference also decreased expression of ErbB2 and this response was because of repression of YY1, an Sp-regulated gene. Betulinic acid-dependent repression of Sp1, Sp3, Sp4, and Sp-regulated genes was due, in part, to induction of the Sp repressor ZBTB10 and downregulation of microRNA-27a (miR-27a), which constitutively inhibits ZBTB10 expression, and we show for the first time that the effects of betulinic acid on the miR-27a:ZBTB10-Sp transcription factor axis were cannabinoid 1 (CB1) and CB2 receptor-dependent, thus identifying a new cellular target for this anticancer agent.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4924623 | PMC |
| http://dx.doi.org/10.1158/1535-7163.MCT-12-0026 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Betulinic acid mitigates lipopolysaccharide-induced intestinal injury of weaned piglets through modulation of the mitochondrial quality control.
Int Immunopharmacol
January 2025
Hunan Engineering Research Center of Livestock and Poultry Health Care, College of Veterinary Medicine, Hunan Agricultural University, Changsha 410128, China. Electronic address:
Intestinal injury of weaned piglets often leads to reduced immunity, diarrhea and growth retardation, resulting in significant economic losses to agriculture. Betulinic acid (BA) is a natural plant-derived active ingredient with multiple pharmacological activities including immune modulation and anti-inflammatory. This study was aimed to investigate the potential mechanism that BA as a feed additive mitigated lipopolysaccharide (LPS)-induced intestinal injury in piglets.
View Article and Find Full Text PDFAssessing the efficacy of iso-mukaadial acetate and betulinic acid against selected Plasmodium falciparum glycolytic pathway proteins: in silico and in vitro studies.
BMC Chem
January 2025
Department of Biochemistry, University of Johannesburg, Auckland Park Campus, Cnr Kingsway Avenue and University Road, Auckland, Park, PO Box 524, Johannesburg, 2006, South Africa.
Malaria is the extensive health concern in sub-Saharan Africa, with Plasmodium falciparum being the most lethal strain. The continued emergence of drug-resistant P. falciparum advocates for the development of new antimalarials.
View Article and Find Full Text PDFWeekly administration of betulinic acid prevents development of chronic renal failure from acute renal failure in folic acid-induced mouse model of kidney injury.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Division of Pharmacology and Toxicology, ICAR-Indian Veterinary Research Institute, Izatnagar, 243 122, India.
Betulinic acid (BA) has been shown to exhibit various pharmacological activities and it has shown the protective effect on acute renal failure (ARF) and chronic renal failure (CRF); however, no reports are available on its effect on ARF-CRF transition. Therefore, we aimed to investigate the effects of BA on ARF-CRF transition. A single dose of 250 mg/kg body weight (BW) intraperitoneal injection of folic acid was given in mice for inducing ARF-CRF transition (injury group; I) on day 1.
View Article and Find Full Text PDFMonophthalates of betulinic acid and related pentacyclic triterpenes inhibit efficiently the SOS-mediated nucleotide exchange and impact PI3K/AKT signaling in oncogenic K-RAS4B proteins.
RSC Adv
January 2025
University of Wuppertal, School of Mathematics and Natural Sciences Gaussstrasse 2042119 Wuppertal Germany
Betulinic acid and other herbal pentacyclic triterpenes have attracted interest in cancer research as these natural products induce apoptosis and suppress tumor progression. However, the molecular basis of the antitumor effect is still unknown. Here we show that monophthalates of betulinic acid and related triterpenes inhibit GDP/GTP exchange in oncogenic K-RAS4B proteins the PI3K/AKT downstream cascade.
View Article and Find Full Text PDFOptimization of betulinic and ursolic acids and phenolics extraction from endemic Rosa pisiformis using Box-Behnken design in relation to cytotoxic activities.
Sci Rep
January 2025
Section of Botany, Department of Biology, Science Faculty, Ege University, Bornova, İzmir, Turkey.
Despite its important pharmacological bioactivities, betulinic acid is still primarily obtained through extraction from heartwood and bark or synthesized synthetically, with less than 3% efficiency. Our endemic rose species, Rosa pisiformis (Christ.) D.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!