Some antimalarial agents in use typically bear basic side chains as ligands. Such ligands were attached to the amino substituent of a bridgehead atom of already antiprotozoal active 3-azabicyclo[3.2.2]nonanes. Structure verification was done by NMR measurements. The new compounds were tested for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum K 1 (multiresistant) and Trypanosoma brucei rhodesiense as well as for their cytotoxicity against L6 cells. Their activities are compared to those of already prepared compounds and structure-activity relationships are discussed.
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http://dx.doi.org/10.1007/s12272-014-0523-1 | DOI Listing |
Nat Commun
January 2025
School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-Sen University, Shenzhen, China.
Hypoxic tumors present a significant challenge in cancer therapy due to their ability to adaptation in low-oxygen environments, which supports tumor survival and resistance to treatment. Enhanced mitophagy, the selective degradation of mitochondria by autophagy, is a crucial mechanism that helps sustain cellular homeostasis in hypoxic tumors. In this study, we develop an azocalix[4]arene-modified supramolecular albumin nanoparticle, that co-delivers hydroxychloroquine and a mitochondria-targeting photosensitizer, designed to induce cascaded oxidative stress by regulating mitophagy for the treatment of hypoxic tumors.
View Article and Find Full Text PDFInt J Rheum Dis
January 2025
The First Affiliated Hospital of Anhui University of Chinese Medicine, Hefei, Anhui, China.
Background: N6-methyladenosine (m6A) is one of the most conserved internal RNA modifications, which has been implicated in many biological processes, such as apoptosis and proliferation. Wilms tumor 1-associating protein (WTAP), as a key component of m6A methylation, is a nuclear protein that has been associated with the regulation of proliferation and apoptosis. Rheumatoid arthritis (RA), a systemic, infiltrating autoimmune disease, is characterized by synovial hyperplasia.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Department of Health Sciences, Institute of Research for Food Safety and Health (IRC-FSH), University "Magna Graecia" of Catanzaro, 88100 Catanzaro, Italy.
In this manuscript, the effects of two extracts from were tested: (a) an extract titrated to 49.7% of andrographolide and obtained from leaves of the plant: (b) the pure andrographolide titrated to 99%. The extracts were dissolved in 1-butanol and tested on tumor lines (MCF7 and SH-SY5Y) and the non-tumor line (Huvec) to understand the effects on cell proliferation.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Anesthesiology & Perioperative Medicine, Mayo Clinic, Rochester, MN 55905, USA.
Aging disrupts multiple homeostatic processes, including autophagy, a cellular process for the recycling and degradation of defective cytoplasmic structures. Acute treatment with the autophagy inhibitor chloroquine blunts the maximal forces generated by the diaphragm muscle, but the mechanisms underlying neuromuscular dysfunction in old age remain poorly understood. We hypothesized that chloroquine treatment increases the presynaptic retention of the styryl dye FM 4-64 following high-frequency nerve stimulation, consistent with the accumulation of unprocessed bulk endosomes.
View Article and Find Full Text PDFMolecules
January 2025
Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, 142432 Chernogolovka, Russia.
Artemisinin is a sesquiterpene lactone derived from the plant L., renowned for its antimalarial activity. Based on this compound, various derivatives and analogues have been obtained that exhibit diverse biological activities, including clinically approved drugs.
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