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antiplasmodial activity

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).

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
Bhatt V, Kumari S, Upadhyay P, Agrawal P, Anmol, Sahal D, Sharma U
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
Igoli NP, Al-Tannak NF, Ezenyi IC, Gray AI, Igoli JO
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
Vanaerschot M, Murithi JM, Fidock DA, et al.
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.

NOT Open Access | Antimalarial diterpenoids from Vitex rotundifolia: Isolation, structure elucidation, and in vitro antiplasmodial activity

July 13, 2020 - 15:47 -- NOT Open Access
Kim YA, Latif A, Kong CS, Seo Y, Dalal SR, Cassera MB, Kingston DGI
Bioorg Chem. 2020 Jul;100:103925

Vitex rotundifolia is an important medicinal plant frequently employed in traditional medicines for the treatment of various ailments. Although this plant species has been under exploration for its constituents by various research groups including our own group, no reports were found regarding the antimalarial potential of this plant or of its purified phytochemicals. Phytochemical investigation of this plant yielded three new (1-3) and five known (4-8) diterpenoids.

Antiplasmodial activity of Cocos nucifera leaves in Plasmodium berghei-infected mice

June 8, 2020 - 15:05 -- Open Access
Tayler NM, De Jesús R, Spadafora R, Coronado LM, Spadafora C
J Parasit Dis. 2020 Jun; 44(2):305-313

Plasmodium falciparum (P. falciparum) malaria presents serious public health problems worldwide. The parasite´s resistance to antimalarial drugs has proven to be a significant hurdle in the search for effective treatments against the disease. For this reason, the study of natural products to find new antimalarials remains a crucial step in the fight against malaria. In this study, we aimed to study the in vivo performance of the decoction of C. nucifera leaves in P. berghei-infected mice. We analyzed the effectiveness of different routes of administration and the acute toxicity of the extract.

Antiplasmodial Activity of p-Substituted Benzyl Thiazinoquinone Derivatives and Their Potential against Parasitic Infections

April 6, 2020 - 14:52 -- Open Access
Casertano M, Menna M, Fattorusso C, Basilico N, Parapini S, Persico M, Imperatore C.
Molecules. 2020 Mar 27;25(7). pii: E1530

Malaria is a life-threatening disease and, what is more, the resistance to available antimalarial drugs is a recurring problem. The resistance of Plasmodium falciparum malaria parasites to previous generations of medicines has undermined malaria control efforts and reversed gains in child survival.

NOT Open Access | HPLC-DAD-SPE-NMR isolation of tetracyclic spiro-alkaloids with antiplasmodial activity from the seeds of Erythrina latissima

April 6, 2020 - 08:20 -- NOT Open Access
Zarev Y, Foubert K, Cos P, Maes L, Elgorashi E, Apers S, Ionkova I, Pieters L
Nat Prod Res. 2020 Apr;34(7):1037-1040

Seven tetracyclic spiro-alkaloids, i.e. glucoerysodine (1), erysodine (2), epi-erythratidine (3), erysovine (4), erythratidine (5), erysotrine (6) and erythraline (7) were isolated from the seeds of Erythrina latissima by means of conventional separation methods and HPLC-DAD-SPE-NMR. Their structures were elucidated by spectroscopic means.

The gender-related variability in the pharmacokinetics and antiplasmodial activity of naphthoquine in rodents

February 17, 2020 - 14:31 -- Open Access
Yuewu Xie, Huixiang Liu, Yanhong Sun and Jie Xing
Malaria Journal 2020 19:71, 13 February 2020

Naphthoquine (NQ) is a suitable partner anti-malarial for the artemisinin-based combination therapy (ACT), which is recommended to be taken orally as a single-dose regimen. The metabolism of NQ was mainly mediated by CYP2D6, which is well-known to show gender-specific differences in its expression. In spite of its clinical use, there is limited information on the pharmacokinetics of NQ, and no data are available for females. In this study, the effect of gender on the pharmacokinetics and antiplasmodial efficacy of NQ in rodents was evaluated. The underlying factors leading to the potential gender difference, i.e., plasma protein binding and metabolic clearance, were also evaluated.

Antiplasmodial Activity of Nitroaromatic Compounds: Correlation with Their Reduction Potential and Inhibitory Action on Plasmodium falciparum Glutathione Reductase

December 23, 2019 - 14:39 -- Open Access
Marozienė A, Lesanavičius M, Davioud-Charvet E, Aliverti A, Grellier P, Šarlauskas J, Čėnas N
Molecules 2019, 24(24), 4509, pii: E4509.

With the aim to clarify the mechanism(s) of action of nitroaromatic compounds against the malaria parasite Plasmodium falciparum, we examined the single-electron reduction by P. falciparum ferredoxin:NADP+ oxidoreductase (PfFNR) of a series of nitrofurans and nitrobenzenes (n = 23), and their ability to inhibit P. falciparum glutathione reductase (PfGR). The reactivity of nitroaromatics in PfFNR-catalyzed reactions increased with their single-electron reduction midpoint potential (E17).


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