The MeOH/CHCl (1:1) extracts of the roots and leaves of and showed potent antitrypanosomal activity during preliminary screening on . Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B () and beilschmiedol C (), and one new phenylalkene obscurene A () together with twelve known compounds (-). In addition, four new derivatives (-) were synthesized from compound . Their structures were elucidated based on their NMR and MS data. Compounds , , and were isolated for the first time from the genus. Additionally, the NMR data of compound are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against and the chloroquine-resistant strain in vitro, respectively. From the tested compounds, the mixture of new compounds and exhibited the most potent antitrypanosomal activity in vitro with IC value of 4.91 μM.
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http://dx.doi.org/10.3390/molecules25122862 | DOI Listing |
Org Lett
January 2025
Department of Chemistry, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama, Kanagawa 223-8522, Japan.
Human African trypanosomiasis (HAT) is one of the most lethal of the neglected tropical diseases. While the discovery of a novel antitrypanosomal drug is highly desired, the creation of a superior lead compound is challenging. Herein we report ukabamide (), which was isolated from a marine sp.
View Article and Find Full Text PDFInt J Parasitol Drugs Drug Resist
January 2025
Laboratory of Microbiology, Parasitology and Hygiene, Infla-Med Centre of Excellence, University of Antwerp, 2610, Wilrijk, Belgium. Electronic address:
Surra and Dourine are widespread diseases caused by two protozoan parasites Trypanosoma brucei evansi and Trypanosoma brucei equiperdum, respectively. A wide range of animals including camels, horses, cattle and buffaloes are susceptible to infection. These diseases pose a significant socio-economic burden, primarily due to the limited therapeutic options and the complications associated with toxicity and drug resistance, making disease management particularly challenging.
View Article and Find Full Text PDFPhytochemistry
March 2025
Centre for Natural and Human Sciences, Federal University of ABC, Santo Andre, SP, 09280-560, Brazil. Electronic address:
As part of our continuous study on the Annonaceae species Porcelia macrocarpa, in the present work, eight chemically related 2-alkyl-3-hydroxy-4-methyl-γ-lactones (1-8) were isolated. Their structures were characterised by NMR, MS, and VCD. Their antitrypanosomal activity was evaluated in vitro against intracellular amastigotes with EC values ranged from 13.
View Article and Find Full Text PDFChemMedChem
November 2024
Laboratório de Síntese e Química Medicinal (LASQUIM)., Faculdade de Ciências Farmacêuticas, Alimentos e Nutrição, Universidade Federal de Mato Grosso do Sul (UFMS), Avenida Costa e Silva, s/n, Bairro Universitário, Campo Grande, Mato Grosso do Sul, CEP 79070-900, Brazil.
A series of 2-nitroimidazole-1,2,3-triazole sulfonamide hybrid analogs were designed using medicinal chemistry approaches, such as bioisosterism, molecular hybridization, Topliss tree decision, and Craig plot. A total of 24 compounds were synthesized via click chemistry in satisfactory yields. Overall, analogs 15 a-x exhibited relevant in vitro anti-trypanosomatid activity against amastigote forms of T.
View Article and Find Full Text PDFPLoS One
November 2024
Research and Laboratories Sector, National Drug and Cosmetic Control Laboratories (NDCCL), Saudi Food and Drug Authority, Riyadh, Saudi Arabia.
Recently, the growth in the consumption of functional foods with potential nutritional and health benefits revealed rapid progress in phytochemical analysis to assure quality and profile the chemical composition. Bee propolis, a gummy exudate produced in beehives after harvesting from different plant species and showed to contain bioactive secondary metabolites with biological importance. The main goal of the current study is to profile the chemical composition of red propolis samples from the Brazilian stingless bee Tetragonula biroi for the first time using HPLC-UV-ELSD and NMR analysis for assignment of the abundant metabolites' classes as well as extraction and isolation of the major compounds.
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