Clinical trials have shown temozolomide to be an effective agent for treatment of malignant melanoma. In order to investigate its suitability for delivery via the skin, a series of temozolomide esters was synthesized as prodrugs. In vitro assays demonstrated temozolomide, temozolomide acid and the hexyl ester equi-effective against selected cancer cell lines. The susceptibility of the esters to enzyme hydrolysis and their effectiveness for application to the skin were investigated. The esters effectively diffuse through rat skin and the hexyl ester demonstrated profound potency for penetrating through skin. Topical application of 5% (w/v) hexyl ester in DMSO solution on a mouse model demonstrated a significant inhibition of tumor growth. These results suggest that temozolomide esters could be an effective alternative to temozolomide in the treatment of skin cancer.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.canlet.2005.11.029 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Differences in the Quality Components of Wuyi Rock Tea and Huizhou Rock Tea.
Foods
December 2024
College of Horticulture, South China Agricultural University, Guangzhou 510642, China.
Different origins and qualities can lead to differences in the taste and aroma of tea; however, the impacts of origin and quality on the taste and aroma characteristics of Wuyi rock tea and Huizhou rock tea have rarely been studied. In this study, high-performance liquid chromatography (HPLC), gas chromatography-mass spectrometry (GC-MS), and sensory evaluation methods were used to compare the quality components of Wuyi rock tea and Huizhou rock tea. The sensory evaluation showed that they each have their own characteristics, but the overall acceptability of Wuyi rock tea is ahead of Huizhou rock tea ( < 0.
View Article and Find Full Text PDFFirst Evidence of Novel Organothiophosphate Esters as Prevalent New Pollutants in Dust from Automotive Repair Shops Discovered by High-Resolution Mass Spectrometry.
Environ Sci Technol
December 2024
Shandong Key Laboratory of Environmental Processes and Health, School of Environmental Science and Engineering, Shandong University, Qingdao 266237, China.
The occurrence of organophosphorus compounds has garnered global concern due to their widespread production and potential environmental risks. Limited structural information has hindered a comprehensive understanding of their composition. By characteristic fragmentation-based nontarget analysis, the occurrence and composition of organothiophosphate esters (OTPEs), which are antiwear additives in lubricant oils that have received little attention previously, were investigated in dust from automotive repair shops and surrounding buildings.
View Article and Find Full Text PDFUnveiling the Larvicidal Potential of Golpar ( Desf. ex Fisch.) Essential Oil and Its Main Constituents on and Mosquito Vectors.
Plants (Basel)
October 2024
Chemistry Interdisciplinary Project (ChIP), School of Pharmacy, University of Camerino, Via Madonna delle Carceri, 62032 Camerino, Italy.
Article Synopsis
- * The EO was found to have significant insecticidal properties, mainly due to its components hexyl butyrate and octyl acetate, demonstrating lethal concentrations (LC) against various mosquito larvae.
- * Importantly, the EO and its components displayed low toxicity to human cells, indicating potential for safe use in developing larvicides.
Article Synopsis
- This study analyzed the aroma components of 38 different plum varieties at three maturity stages using advanced techniques (HS-SPME-GC-MS) to identify and quantify 138 aromatic compounds.
- Thirteen main aroma compounds were found to be dominant, and statistical methods revealed 24 key aroma components that can distinguish plums based on their ripening stages.
- The research highlighted significant differences in aroma profiles between early- and late-maturing plums, indicating their potential use as indicators for identifying and differentiating plum germplasm.
Exploring the use of gull eggs as bioindicators of phthalate esters exposure.
Environ Res
December 2024
Department of Environmental Chemistry, IDAEA-CSIC, Jordi Girona 18-26, 08034, Barcelona, Catalonia, Spain. Electronic address:
Plastic pollution and associated plasticizers are a global threat affecting aquatic environments. Phthalates are among the most used plasticizers that can impact on fauna due to their endocrine-disrupting properties. The aim of this study was to investigate the use of eggs of Audouin's gull (Larus audouinii) and yellow-legged gull (Larus michahellis) as biomonitors of phthalate exposure.
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!