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The present study was designed to synthesize and evaluate ursolic acid hybrid compounds against glioma cells. Initial screening revealed that most of the synthesized compounds displayed better inhibitory effect on glioma cell proliferation compared to parent ursolic acid. The mechanism of inhibitory effect of the most potent compound 6d on glioma cells was investigated in detail. Treatment with compound 6d significantly (p < 0.001) reduced U251 and C6 cell proliferation at 48 h. The growth of U251 and C6 glioma cells was reduced to minimum level (17 and 21%) on treatment with 10 μM concentration of compound 6d. Treatment of the U251 cells with 10 μM concentration of compound 6d caused a significant (p < 0.05) inhibition of cAMP level. In U251 cell cultures treatment with compound 6d at 10 μM concentration enhanced proportion of apoptotic cells to 69.32% compared to 2.34% in the control cultures. The compound 6d treatment of U251 cells for 48 h caused arrest of cell cycle in the G0/G1 phase with consequent decrease of cell population in G2/M and S phases. The results from TEM showed that compound 6d treatment of U251 cells for 48 h caused blebbing of the cell membranes, chromatin condensation, appearance of foamy cytoplasmic material and autophagic vacuoles. The results from SEM revealed that compound 6d treatment of U251 cells caused a marked inhibition of microvilli and extensions on the cell surfaces. Thus present study demonstrates that compound 6d inhibits glioma cell growth, induces apoptosis and arrest cell cycle through metabolic pathway down-regulation. Therefore, compound 6d can be evaluated further for the treatment of glioma.
This article was published in the following journal.
Name: European journal of medicinal chemistry
Ursolic Acid Exhibits Potent Anticancer Effects in Human Metastatic Melanoma Cancer Cells (SK-MEL-24) via Apoptosis Induction, Inhibition of Cell Migration and Invasion, Cell Cycle Arrest, and Inhibition of Mitogen-Activated Protein Kinase (MAPK)/ERK Signaling Pathway.
BACKGROUND Ursolic acid is an important bioactive triterpenoid that has been reported to be of tremendous pharmacological importance. However, the anticancer potential of ursolic acid has not been exa...
To investigate the influences of long non-coding ribonucleic acid (lncRNA) small nucleolar RNA host gene 20 (SNHG20) on proliferation and apoptosis of glioma cells, and further explore the mechanis...
MicroRNAs are involved in the regulation of tumor formation. A previous study suggested that miR-10a promotes glioma cell migration and invasion. However, the effect of miR-10a on the proliferation of...
Ursolic acid (UA) as a natural ursane-triterpenoid has rich pharmacological activities. We have found that it possesses aggregation properties and could self-assemble into organogels. Based on the agg...
In addition to the known antitumour effects of ursolic acid (UA), increasing evidence indicates that this molecule plays a role in cardiac protection. In this study, the effects of ursolic acid on the...
This is an open-label, active treatment trial to determine the pharmacokinetics of orally administered ursolic acid and to assess the potential efficacy and safety of ursolic acid in subje...
This phase I trial studies the side effects and best dose of ascorbic acid when given together with bevacizumab in treating patients with high grade glioma that has come back (recurrent). ...
This phase I trial studies the side effects and best dose of memory-enriched T cells in treating patients with grade II-IV glioma that has come back or does not respond to treatment. Memor...
Cellceutix has developed Kevetrin (thioureidobutyronitrile), belonging to an anti-proliferative p53 activator pharmacological class, for the treatment of cancer. Nonclinical studies have d...
Currently, treatment with a specific anti-epileptic drug mainly depends on the physicians' preference, as there are no studiessupporting the use of one specific anticonvulsant in glioma pa...
A pentacyclic triterpene that occurs widely in many PLANTS as the free acid or the aglycone for many SAPONINS. It is biosynthesized from lupane. It can rearrange to the isomer, ursolic acid, or be oxidized to taraxasterol and amyrin.
A plant genus of the family VALERIANACEAE. Members contain ursolic acid and oleanolic acid glycosides, sulfapatrinosides (triterpenoid glycosides), and patriscabrol (iridolactone).
A plant genus in the family CAPRIFOLIACEAE. The common name derives from its traditional use for menstrual cramps. It is a source of viburnine, valerianic acid, vibsanin, and ursolic acid. Note that true cranberry is VACCINIUM MACROCARPON.
A fatty acid-binding protein expressed by ASTROCYTES during CENTRAL NERVOUS SYSTEM development, and by MALIGNANT GLIOMA cells. It is also expressed by ASTROCYTES in response to injury or ISCHEMIA, and may function in repair of the MYELIN SHEATH.
Endocrine cells which secrete GASTRIN, a peptide that induces GASTRIC ACID secretion. They are found predominantly in the GASTRIC GLANDS of PYLORIC ANTRUM in the STOMACH, but can also be found in the DUODENUM, nervous and other tissues.