Background: Curcumin, the active ingredient of turmeric, has a remarkable antitumor activity against various cancers, including glioblastoma. However, it has poor absorption and low bioavailability; thus, to cross the blood-brain barrier and reach tumor tissue, it needs to be transferred to tumor site by special drug delivery systems, such as nanoparticles.
Objective: We aimed to evaluate the antitumor activity of curcumin on glioblastoma tissue in the rat glioma-2 (RG2) tumor model when it is loaded on poly(lactic-co-glycolic acid)-1,2-distearoyl-glycerol-3-phospho-ethanolamine-N-[methoxy (polyethylene glycol)-2000] ammonium salt (PLGA-DSPE-PEG) hybrid nanoparticles.
Methods: Glioblastoma was induced in 42 adult female Wistar rats (250-300g) by RG2 tumor model. The curcumin-loaded nanoparticles were injected by intravenous (n=6) or intratumoral route (n=6). There were five control groups, each containing six rats. First control group was not applied any treatment. The remaining four control groups were given empty nanoparticles or curcumin alone by intravenous or intratumoral route, respectively. The change in tumor volume was assessed by magnetic resonance imaging and histopathology before and 5days after drug injections.
Results: Tumor size decreased significantly after 5days of intratumoral injection of curcumin-loaded nanoparticle (from 66.6±44.6 to 34.9±21.7mm, p=0.028), whereas it significantly increased in nontreated control group (from 33.9±21.3 to 123.7±41.1mm, p=0.036) and did not significantly change in other groups (p>0.05 for all).
Conclusion: In this in vivo experimental model, intratumoral administration of curcumin-loaded PLGA-DSPE-PEG hybrid nanoparticles was effective against glioblastoma. Curcumine-loaded nanoparticles may have potential application in chemotherapy of glioblastoma.
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http://dx.doi.org/10.1016/j.msec.2017.03.292 | DOI Listing |
Chem Biodivers
January 2025
Gannan Medical University, Depatment of Medicinal Chemistry, Gannan Medical University, 341000, Ganzhou, CHINA.
Extracting natural active ingredients from plants is an effective way to develop and screen modern drugs. Psoralea corylifolia is a leguminous plant whose seeds have long been used as a Traditional Chinese Medicine to treat psoriasis, rheumatism, dermatitis, and other diseases. To date, several main compounds, including coumarins, flavonoids, monoterpene phenols, and benzofurans, have been identified from the seeds of Psoralea corylifolia.
View Article and Find Full Text PDFJ Exp Med
March 2025
Center for Immune-Related Diseases at Shanghai Institute of Immunology, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
Activation of CD8+ T cells necessitates rapid metabolic reprogramming to fulfill the substantial biosynthetic demands of effector functions. However, the posttranscriptional mechanisms underpinning this process remain obscure. The transfer RNA (tRNA) N1-methyladenine (m1A) modification, essential for tRNA stability and protein translation, has an undefined physiological function in CD8+ T cells, particularly in antitumor responses.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Institute of Natural Sciences and Mathematics, Ural Federal University, 51 Lenina Ave., 620000 Ekaterinburg, Russian Federation.
The labile tautomerism of -unsubstituted 5-acyl-4-pyridones, which exist in the form of 4-pyridone or 4-hydroxypyridine depending on the solvent, has been demonstrated. This equilibrium determines the reactivity of pyridones and their ability to undergo substitution reactions of the OH group. A regioselective and convenient method for the construction of functionalized pyrazolo[4,3-]pyridines (30-93%) based on the intramolecular amination reaction of 4-pyridones with hydrazines has been developed.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Catalysis Laboratory, School of Chemistry, University of Hyderabad, Hyderabad-500 046, India.
Simple and sustainable three- and four-step sequences of di-OH-protection/mono-OMe-deprotection/OrgRC and di-OH-protection/mono-OMe-deprotection/OrgRC/OMe-deprotection protocols were developed to construct biologically active natural products of irisoquin, irisoquin A, irisoquin D, irisoquin F, sorgoleone-364, embelin, rapanone, 5--methylembelin, 5--methylrapanone and their analogues from the commercially available 2,5-dihydroxy-1,4-benzoquinone, aliphatic aldehydes and Hantzsch ester (1,4-DHP) in very good to excellent yields by using organocatalytic reductive coupling (OrgRC) as key reaction. Many of these natural compounds exhibited a broad spectrum of biological activities including antioxidant, anti-inflammatory, anticonvulsant, anxiolytic, analgesic, anthelmintic, antitumor, antibacterial, and antifertility properties. At the same time, simple and readily available 2,5-dihydroxy-1,4-benzoquinone was transformed into a functionally rich library of 2,5-dihydroxy-3,6-dialkyl-1,4-benzoquinones in very good yields by using sequential OrgRC followed by deprotection reactions and resulting natural/unnatural products would be excellent targets for investigation to show their biological activities compared to known natural products.
View Article and Find Full Text PDFJ Cell Mol Med
February 2025
Department of Chemotherapy, Jiangxi Cancer Hospital, Nanchang, Jiangxi, China.
Tumour cells possess a multitude of chemoresistance mechanisms, which could plausibly contribute to the ineffectiveness of chemotherapy. O-methylguanine-DNA methyltransferase (MGMT) is an important effector protein associated with Temozolomide (TMZ) resistance in various tumours. To some extent, the expression level of MGMT determines the sensitivity of cells to TMZ, but the mechanism of its expression regulation has not been fully elucidated.
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