Background: Malaria is one of the most important life-threatening infectious diseases in the tropics. In spite of the effectiveness of artemisinin-based combination therapy, reports on reduced sensitivity of the parasite to artemisinin in Cambodia and Thailand warrants screening for new potential antimalarial drugs for future use. Ghanaian herbalists claim that has antimalarial activity. Therefore, antiplasmodial activity, cytotoxic effects, and antioxidant and phytochemical properties of leaf extract were investigated in this study.
Methodology/principal Findings: Aqueous, 70% hydroethanolic and ethyl acetate leaf extracts were prepared using standard procedures. Antiplasmodial activity was assessed by using chloroquine-sensitive malaria parasite strain NF54. The SYBR® Green and tetrazolium-based calorimetric assays were used to measure parasite growth inhibition and cytotoxicity, respectively, after extract treatment. Total antioxidant activity was evaluated using a free radical scavenging assay. Results obtained showed that extracts protected red blood cells against mediated damage. Fifty percent inhibitory concentration (IC) values were 24.0±1.08 g/ml, 22.5±0.12 g/ml, and 9.5±0.69 g/ml for aqueous, hydroethanolic, and ethyl acetate extracts, respectively. Flavonoids, tannins, and saponins were present in the hydroethanolic extract, whereas only the latter was observed in the aqueous extract. Aqueous and hydroethanolic extracts showed stronger antioxidant activities compared to the ethyl acetate extract.
Conclusions/significance: The extracts of have antiplasmodial properties and low toxicities to human red blood cells. The extracts could be developed as useful alternatives to antimalarial drugs. These results support claims of the herbalists that decoctions of are useful antimalarial agents.
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http://dx.doi.org/10.1155/2019/6976298 | DOI Listing |
Mini Rev Med Chem
January 2025
Department of Physiology and Pharmacology Vittorio Erspamer, Sapienza University of Rome, 00161, Rome, Italy.
Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides.
View Article and Find Full Text PDFChem Asian J
January 2025
Birla Institute of Technology and Science - Pilani Campus: Birla Institute of Technology & Science Pilani, Pharmacy, BITS Pilani, Pilani campus, Vidya Vihar, 333031, Pilani, INDIA.
In this study, we built on the known inhibitory potential of diaminoquinazolines (DAQs) against different stages of Plasmodium development and designed a convenient two-step synthesis to combine DAQ with the primaquine (PQ) pharmacophore. The PQ-DAQ hybrids displayed potent in vitro activities in the low nanomolar range (IC50 of 135.20-398.
View Article and Find Full Text PDFMolecules
December 2024
Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovačića 1, 10000 Zagreb, Croatia.
As the resistance of to the existing antimalarials increases, there is a crucial need to expand the antimalarial drug pipeline. We recently identified potent antimalarial compounds, namely harmiquins, hybrids derived from the β-carboline alkaloid harmine and 4-amino-7-chloroquinoline, a key structural motif of chloroquine (CQ). To further explore the structure-activity relationship, we synthesised 13 novel hybrid compounds at the position -9 of the β-carboline ring and evaluated their efficacy in vitro against 3D7 and Dd2 strains (CQ sensitive and multi-drug resistant, respectively).
View Article and Find Full Text PDFInt J Nanomedicine
January 2025
Affiliated Hospital, Qinghai University, Xining, Qinghai, People's Republic of China.
Background: Acacetin (AC) is a flavonoid compound with antiperoxidant, anti-inflammatory, and antiplasmodial activity. However, the solubility of AC is poor and nano acacetin (Nano AC) was synthesized. The intestinal mucosal barrier is impaired in sepsis rats, and the protective effects and mechanism of AC and Nano AC on the intestinal mucosal barrier are unclear.
View Article and Find Full Text PDFAppl Sci (Basel)
January 2024
Department of Microbiology and Medical Zoology, University of Puerto Rico School of Medicine, San Juan 00921, Puerto Rico.
Gracilioether M () and 11,12-dihydrogracilioether M (), two polyketides with a [2(5H)-furanylidene]ethanoate moiety, along with known plakortone G () and its new naturally occurring derivative 9,10-dihydroplakortone G (), were isolated from the Caribbean marine sponge . The structures and absolute configuration of , , and were characterized by analysis of HRESIMS and NMR spectroscopic data, chemical derivatization, and side-by-side comparisons with published NMR data of related analogs. Compounds and and a mixture of and were evaluated for cytotoxicity against MCF-7 human breast cancer cells.
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