Currently available treatments for acute myeloid leukemia exhibit side effects that limit their use, with primary and secondary resistance as persistent issues. While edible mushrooms possess nutritional value, they are also an excellent source of bioactive compounds that may have the potential to treat multiple disease states. The aim of the present study was to investigate the in vitro inhibitory effects of chromatographic fractions from the methanol extract of Cantharellus cibarius in a human acute myeloid leukemia (AML) cell line MV4-11. The mushrooms were purchased from a grocery store, the fruiting bodies were triturated and then extracted with 99.9% methanol to generate a crude extract. This crude extract was then redissolved in methanol, filtered over cotton to remove insoluble solids, and then fractionated over Sephadex® LH-20. Each fraction was dried and then analyzed by reverse-phase HPLC. A typical UV wavelength was selected for the detection of possible anticancer compounds in C. cibarius based on the major chromophores in main fungal anticancer agents reported. Based on chromatographic profiles, specific fractions that might contain potential anticancer agents were combined, and the inhibitory activity of the combined fractions was assessed against the MV4-11 leukemia cell line. Data confirmed that one combined fraction LH-20F-IV showed the greatest degree of in vitro inhibitory activity against the selected cell line. Fast determination of the potential anticancer compound containing fraction was completed through the application of reported chemoinformatics on HPLC detection of possible chromophores in potential anticancer agents, in combination with cellular bioassays.
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http://dx.doi.org/10.1615/IntJMedMushrooms.2024055328 | DOI Listing |
Biochem Pharmacol
December 2024
Zhongshan Hospital Institute of Clinical Science, Shanghai Medical College, Fudan University, Shanghai 200032, China. Electronic address:
B-cell lymphoma extra large (BCL-X) is an important anti-apoptotic protein of BCL-2 family. It is frequently overexpressed in various hematologic and solid tumors, often positively correlated with chemotherapy resistance in tumors. However, the clinical development of the small molecule BCL-X inhibitor ABT-263 has been challenged on account of its on-target and dose-limiting toxicity.
View Article and Find Full Text PDFBioorg Med Chem Lett
December 2024
Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi 710032, China. Electronic address:
FLT3-ITD and TKD mutants play a central role in acute myeloid leukemia (AML), making FLT3 an attractive target for AML treatment. To discover next-generation FLT3 inhibitors and gather additional structure-activity relationship (SAR) information, we performed structural modifications of G-749 (denfivontinib) utilizing structure simplification and scaffold hopping strategies. Among these derivatives, MY-10 exhibited the most potent and selective inhibition of MV4-11 cell proliferation, demonstrating potent inhibitory activity against FLT3-ITD (IC = 6.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Department of Neurosurgery, China-Japan Union Hospital of Jilin University, Changchun, 130033, China. Electronic address:
Targeting XPO1 inhibition has emerged as a promising therapeutic strategy in cancer treatment. Despite the numerous XPO1 inhibitors reported to date, no XPO1 degraders have been disclosed. In this study, we reported the design, synthesis and biological characterization of small-molecule XPO1 degraders based upon the proteolysis targeting chimera (PROTAC), marking the first public disclosure of XPO1 degraders.
View Article and Find Full Text PDFLeuk Res
December 2024
Endocrinology Department, The Third People's Hospital of Henan Province, China. Electronic address:
Objective: The primary methods for defining the prognostic risk of AML patients are cytogenetic and molecular analysis at the time of diagnosis. However, the prognosis of intermediate-risk patients is still not well assessed for biomarkers. The main objective of this meta-analysis is to evaluate the relationship between circRNAs and AML prognosis, to provide a theoretical basis for finding effective prognostic indicators in intermediate-risk patients, and to provide an important scientific basis for the development or revision of WHO practice guidelines and ELN risk classification, and to highlight the importance of continuing to focus on and evaluate the prognostic impact of circRNAs on AML in future studies.
View Article and Find Full Text PDFCell Mol Biol (Noisy-le-grand)
November 2024
Betül-Ziya Eren Genome and Stem Cell Center, Erciyes University, Kayseri, Türkiye.
Homeobox (HOX) transcript antisense RNA (HOTAIR) and HOX genes are reported to be more expressed in various cancers in humans in recent studies. The role of HOTAIR and HOXD genes in acute myeloid leukemia (AML) and chronic myeloid leukemia (CML) is not well known. In this study, expression levels of HOXD8, HOXD9 and HOXD11 from HOXD gene family and HOTAIR were determined from peripheral blood samples of 30 AML and 30 CML patients and 20 healthy volunteers by quantitative Real Time PCR.
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