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antiplasmodial activity

In Vivo Efficacy and Metabolism of the Antimalarial Cycleanine and Improved In Vitro Antiplasmodial Activity of Semisynthetic Analogues

October 30, 2021 - 12:39 -- Open Access
Uche FI, Guo X, Okokon J, Ullah I, Horrocks P, Boateng J, Huang C, Li WW
Antimicrob Agents Chemother. 2021 Jan 20;65(2):e01995-20

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine [compound 1], isochondodendrine [compound 2], and 2'-norcocsuline [compound 3]) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semisynthetic analogues (compounds 4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR green 1 fluorescence assay.

NOT Open Access | In vitro antiplasmodial activity, targeted LC-MS metabolite profiling, and identification of major natural products in the bioactive extracts of Palicourea and Psychotria species from the Amazonia and Atlantic Forest biomes, Brazil

September 7, 2021 - 15:32 -- NOT Open Access
Gontijo DC, do Nascimento MFA, Rody HVS, Magalhães RA, Margalho LF, Brandão GC, de Oliveira AB
Metabolomics. 2021 Sep 4;17(9):81

To assess the antiplasmodial activity of 24 extracts from Palicourea and Psychotria genera, along with the targeted LC–MS metabolite profiling, as well as identification of the main metabolites in the bioactive extracts.

Growth, secondary metabolite production, and in vitro antiplasmodial activity of Sonchus arvensis L. callus under dolomite [CaMg(CO3)2] treatment

August 25, 2021 - 16:02 -- Open Access
Wahyuni DK, Rahayu S, Zaidan AH, Ekasari W, Prasongsuk S, Purnobasuki H
PLoS One. 2021 Aug 20;16(8):e0254804

Malaria is still a global health problem. Plasmodium is a single-cell protozoan parasite that causes malaria and is transmitted to humans through the female Anopheles mosquito. The previous study showed that Sonchus arvensis L. callus has antiplasmodial activity. Several treatments are needed for callus quality improvement for antimalarial compound production. This study aimed to examine the effect of dolomite [CaMg(CO3)2] on growth (morpho-anatomical structure and biomass), secondary metabolite production, and in vitro antiplasmodial activity of S. arvensis L. callus.

NOT Open Access | Chemical constituents of two Cameroonian medicinal plants: Sida rhombifolia L. and Sida acuta Burm. f. (Malvaceae) and their antiplasmodial activity

June 16, 2021 - 09:42 -- NOT Open Access
Kamdoum BC, Simo I, Ngadjui BT, et al.
Nat Prod Res. 2021 Jun 14:1-8

An extensive phytochemical investigation of the EtOH/H2O (7:3) extracts of Sida rhombifolia L. and Sida acuta Burm. f., yielded a previously undescribed ceramide named rhombifoliamide (1) and a xylitol dimer (2), naturally isolated here for the first time, as well as the thirteen known compounds viz, oleanolic acid (3), β-amyrin glucoside (4), ursolic acid (5), β-sitosterol glucoside (6), tiliroside (7), 1,6-dihydroxyxanthone (8), a mixture of stigmasterol (9) and β-sitosterol (10), cryptolepine (11), 20-Hydroxyecdysone (12), (E)-suberenol (13), thamnosmonin (14) and xanthyletin (15).

Violacein-Induced Chaperone System Collapse Underlies Multistage Antiplasmodial Activity

April 13, 2021 - 13:07 -- Open Access
Tavella TA, da Silva NSM, Maranhão Costa FT, et al.
ACS Infect Dis. 2021 Apr 9;7(4):759-776

Antimalarial drugs with novel modes of action and wide therapeutic potential are needed to pave the way for malaria eradication. Violacein is a natural compound known for its biological activity against cancer cells and several pathogens, including the malaria parasite, Plasmodium falciparum (Pf). Herein, using chemical genomic profiling (CGP), we found that violacein affects protein homeostasis. Mechanistically, violacein binds Pf chaperones, PfHsp90 and PfHsp70-1, compromising the latter's ATPase and chaperone activities.

NOT Open Access | In vitro and in vivo antiplasmodial activity of novel quinoline derivative compounds by molecular hybridization

April 6, 2021 - 13:54 -- NOT Open Access
Marinho JA, Martins Guimarães DS, Abramo C, et al.
Eur J Med Chem. 2021 Apr 5;215:113271

Chloroquine (CQ) has been the main treatment for malaria in regions where there are no resistant strains. Molecular hybridization techniques have been used as a tool in the search for new drugs and was implemented in the present study in an attempt to produce compound candidates to treat malarial infections by CQ-resistant strains. Two groups of molecules were produced from the 4-aminoquinoline ring in conjugation to hydrazones (HQ) and imines (IQ).

Antiplasmodial activity of Ethanolic extract of Cassia spectabilis DC leaf and its inhibition effect in Heme detoxification

February 23, 2021 - 12:50 -- Open Access
Ekasari W, Basuki DR, Arwati H, Wahyuni TS
BMC Complement Med Ther. 2021 Feb 19;21(1):71

In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial.

Potential repurposing of four FDA approved compounds with antiplasmodial activity identified through proteome scale computational drug discovery and in vitro assay

January 19, 2021 - 15:59 -- Open Access
Diallo BN, Swart T, Hoppe HC, Tastan Bishop Ö, Lobb K
Sci Rep. 2021 Jan 14;11(1):1413

Malaria elimination can benefit from time and cost-efficient approaches for antimalarials such as drug repurposing. In this work, 796 DrugBank compounds were screened against 36 Plasmodium falciparum targets using QuickVina-W. Hits were selected after rescoring using GRaph Interaction Matching (GRIM) and ligand efficiency metrics: surface efficiency index (SEI), binding efficiency index (BEI) and lipophilic efficiency (LipE).

Synthesis and Antiplasmodial Activity of Novel Bioinspired Imidazolidinedione Derivatives

January 7, 2021 - 10:41 -- Open Access
Jaromin A, Czopek A, Parapini S, Basilico N, Misiak E, Gubernator J, Zagórska A
Biomolecules. 2020 Dec 29;11(1):E33

Malaria is an enormous threat to public health, due to the emergence of Plasmodium falciparum resistance to widely-used antimalarials, such as chloroquine (CQ). Current antimalarial drugs are aromatic heterocyclic derivatives, most often containing a basic component with an added alkyl chain in their chemical structure. While these drugs are effective, they have many side effects. This paper presents the synthesis and preliminary physicochemical characterisation of novel bioinspired imidazolidinedione derivatives, where the imidazolidinedione core was linked via the alkylene chain and the basic piperazine component to the bicyclic system.

Novel Harmicines with Improved Potency against Plasmodium

September 29, 2020 - 13:19 -- Open Access
Marinović M, Perković I, Rajić Z, et al.
Molecules. 2020 Sep 23;25(19):E4376

Harmicines represent hybrid compounds composed of β-carboline alkaloid harmine and cinnamic acid derivatives (CADs). In this paper we report the synthesis of amide-type harmicines and the evaluation of their biological activity. N-harmicines 5a-f and O-harmicines 6a-h were prepared by a straightforward synthetic procedure, from harmine-based amines and CADs using standard coupling conditions, 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo [4,5-b]pyridinium 3-oxid hexafluorophosphate (HATU) and N,N-diisopropylethylamine (DIEA).


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