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antiplasmodial activity

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
Author(s): 
Kamdoum BC, Simo I, Ngadjui BT, et al.
Reference: 
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
Author(s): 
Tavella TA, da Silva NSM, Maranhão Costa FT, et al.
Reference: 
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
Author(s): 
Marinho JA, Martins Guimarães DS, Abramo C, et al.
Reference: 
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
Author(s): 
Ekasari W, Basuki DR, Arwati H, Wahyuni TS
Reference: 
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
Author(s): 
Diallo BN, Swart T, Hoppe HC, Tastan Bishop Ö, Lobb K
Reference: 
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
Author(s): 
Jaromin A, Czopek A, Parapini S, Basilico N, Misiak E, Gubernator J, Zagórska A
Reference: 
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
Author(s): 
Marinović M, Perković I, Rajić Z, et al.
Reference: 
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).

NOT Open Access | Chemical profiling and quantification of potential active constituents responsible for the antiplasmodial activity of Cissampelos pareira

July 30, 2020 - 13:59 -- NOT Open Access
Author(s): 
Bhatt V, Kumari S, Upadhyay P, Agrawal P, Anmol, Sahal D, Sharma U
Reference: 
J Ethnopharmacol. 2020 Jul 26:113185

Cissampelos pareira is used traditionally in India as a remedy for the treatment of various diseases including malaria but the active ingredients responsible for antiplasmodial activity have not yet been investigated.

NOT Open Access | Antiplasmodial activity of a novel diarylheptanoid from Siphonochilus aethiopicus

July 27, 2020 - 15:08 -- NOT Open Access
Author(s): 
Igoli NP, Al-Tannak NF, Ezenyi IC, Gray AI, Igoli JO
Reference: 
Nat Prod Res. 2020 Jul 27:1-8

The Nigerian and South African varieties of Siphonochilus aethiopicus were examined for their phytochemical constituents. The ethyl acetate extract of the rhizomes of the South African variety yielded a novel diarylheptanoid, 2,3-diacetoxy-7-(3'',4''-dihydroxy-5''-methoxyphenyl)-1-(4'-hydroxy-3'-methoxyphenyl)-5-heptene and the flavonoid 3,7-dimethoxyquercetin. From the hexane extract of the Nigerian variety, siphonochilone and another flavonoid, 3,4',7-trimethylkaempferol were isolated.

Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity

July 21, 2020 - 12:14 -- Open Access
Author(s): 
Vanaerschot M, Murithi JM, Fidock DA, et al.
Reference: 
Cell Chem Biol. 2020 Jul 16; 27(7):806-816.e8

The search for antimalarial chemotypes with modes of action unrelated to existing drugs has intensified with the recent failure of first-line therapies across Southeast Asia. Here, we show that the trisubstituted imidazole MMV030084 potently inhibits hepatocyte invasion by Plasmodium sporozoites, merozoite egress from asexual blood stage schizonts, and male gamete exflagellation.

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