In this study, we aimed to investigate the potential relationship between gossypol-induced cytotoxicity of human promyelocytic leukemia cell line (HL-60) leukemic cells and intracellular serine/threonine protein phosphatase (PP) dynamics and human telomerase reverse transcriptase (hTERT) activity. Gossypol was found to be cytotoxic in HL-60 cells with the IC(50) dose of 4.5 microM. The combination of gossypol and okadaic acid in IC(50) doses revealed the increased cytotoxicity in a time-dependent manner. Treatment of cells with gossypol has shown significant decrease in PP2A activity. The expression of the PP2A catalytic subunit was downregulated in gossypol-treated cells with 24 hours' intervals. hTERT mRNA levels were gradually decreased. In conclusion, during gossypol-induced cytotoxicity, intracellular activity and expression of PP2A was decreased as well as the activity of hTERT. The variation of hTERT activity in gossypol-treated HL-60 cells may be the potential reason for the phosphatase interaction during the gossypol treatment of leukemic cells resulting in cellular cytotoxicity.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1179/102453309X12583347113771 | DOI Listing |
Chem Biodivers
January 2025
Naval Medical University, Phytochemistry, No.325 Guohe Road, Not Available, 200433, Shanghai, CHINA.
One new Sesquiterpene wikstromicrol (1), one new lignan (7R, 8S, 8'S)-9-acetoxyl (-)-isolariciresinol (8), and twelve known compounds were isolated from the branches and leaves of Wikstroemia micrantha. The structures of new compounds were elucidated by extensive interpretation of spectroscopic data and quantum chemical calculations of ECD spectra. The bioactivity assay showed that compounds 6 and 7 had weak cytotoxicity against MCF-7, HCT-116, and HL-60 cell lines with IC50 values ranging from 33.
View Article and Find Full Text PDFChem Biol Drug Des
January 2025
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Target cyclooxygenase 2 (COX-2) and 5-lipoxygenase (5-LOX) inhibitors; 5-([2,5-Dihydroxybenzyl]amino)salicylamides (Compounds 1-11) were examined for potential anticancer activity, with a trial to assess the underlying possible mechanisms. Compounds were assessed at a single dose against 60 cancer cell lines panel and those with the highest activity were tested in the five-dose assay. COMPARE analysis was conducted to explore potential mechanisms underlying their biological activity.
View Article and Find Full Text PDFRSC Adv
January 2025
Key Laboratory of Functional Molecules Analysis and Biotransformation of Universities in Yunnan Province, Yunnan Characteristic Plant Extraction Laboratory, School of Chemical Science and Technology, School of Medicine, Yunnan University Kunming Yunnan 650500 PR China
The natural products of 2,5-diketopiperazines have attracted considerable attention due to their potent pharmacological activities. Guided by genome mining techniques, five albonoursin analogues, designated as albocandins A-E (1-5), were isolated from sp. YINM00030, an actinomycete sourced from the rhizosphere soil of medicinal plants.
View Article and Find Full Text PDFFitoterapia
January 2025
Key Laboratory for Forest Resources Conservation and Utilization in the Southwest Mountains of China, Ministry of Education, Southwest Forestry University, Kunming 650224, China; Yunnan Provincial Key Laboratory for Conservation and Utilization of In-forest Resource, Southwest Forestry University, Yunnan Kunming, 650224, China. Electronic address:
Two new tropolone-bearing sesquiterpenoids (1-2), two new dolabrane-type diterpenoids (3-4) along with eight known compounds as ionone-type sesquiterpenoid (5), oleanane triterpenoid (6), vanillin and its derivative (7-8), neolignan (9), two lignans (10-11), flavanonol glycoside (12) were isolated from whole plants of Croton lauioides Radcl.-Sm. & Govaerts.
View Article and Find Full Text PDFMolecules
December 2024
Department of Chemistry, University of the Pacific, 3601 Pacific Avenue, Stockton, CA 95211, USA.
In the field of drug development, the quest for novel compounds that bind to DNA with high affinity and specificity never ends. In the present work, we report the newest development in this field, namely, triplex DNA-specific binding ligands based on the 5-substituted flavone scaffold in our lab. Biophysical studies showed that the newly synthesized flavone derivatives (depending on the side chains) bind to triplex DNA with binding affinities better than or similar to 5-substituted 3,3',4',7-tetramethoxyflavonoids.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!