Karavilagenin C derivatives as antimalarials

Ramalhete, Cátia; Lopes, Dinora; Molnár, Joséph; Mulhovo, Silva; Rosário, Virgílio Estólio do; Ferreira, Maria José U.

doi:10.1016/j.bmc.2010.11.015

Cited by 27 publications

(40 citation statements)

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“…This is most likely due to the incomplete suppression of parasitemia, rapid metabolism and or excretion of terpenoid Furthermore, from the in vivo results herein (Table 1) and the in vitro antiplasmodial results for the esters of karavilagenin C [22,25], it appears that the number of carbon atoms in the acyl groups affects the antimalarial activity.…”

Section: Biologymentioning

confidence: 67%

“…Using criteria for in vitro antimalarial activity adopted by Batista et al [24], most of these compounds and semi-synthetic derivatives exhibited excellent/good inhibitory effects (IC50 ≤ 1 µM/IC50 = 1 -20 µM) against blood schizonts of chloroquine-sensitive and resistant strains of P. falciparum [21][22][23]. Some of these terpenoids exhibited promising in vitro activity against liver stages of P. berghei Vincke and Lips infections, emphasizing their dual-stage antimalarial activity [23,25].…”

Section: Introductionmentioning

confidence: 97%

“…balsamina led to the isolation of several cucurbitane triterpenoids [19][20][21][22][23]. Using criteria for in vitro antimalarial activity adopted by Batista et al [24], most of these compounds and semi-synthetic derivatives exhibited excellent/good inhibitory effects (IC50 ≤ 1 µM/IC50 = 1 -20 µM) against blood schizonts of chloroquine-sensitive and resistant strains of P. falciparum [21][22][23].…”

Section: Introductionmentioning

confidence: 98%

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In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents

Silva

Ramalhete

Nogueira

et al. 2015

European Journal of Medicinal Chemistry

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Section: Biologymentioning

confidence: 67%

Section: Introductionmentioning

confidence: 97%

Section: Introductionmentioning

confidence: 98%

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In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents

Silva

Ramalhete

Nogueira

et al. 2015

European Journal of Medicinal Chemistry

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“…Despite the wide ethnomedical use of T. elegans as an antimalarial remedy (Bandeira et al, 2001), this is the first study to document its significant antiplasmodial activity. Studies conducted by Ramalhete et al, 2008 revealed moderate or no significant activity of polar leaf extracts from the same plant species. Nevertheless, studies conducted on indole alkaloids from a closely related species, T. sessilifolia, showed some good antiplasmodial activity (Girardot et al, 2012), which could explain the observed bioactivity.…”

Section: Resultsmentioning

confidence: 97%

In vitro antiplasmodial screening of ethnopharmacologically selected South African plant species used for the treatment of malaria

Bapela

Meyer

Kaiser

2014

Journal of Ethnopharmacology

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Abstract:Ethnopharmacological relevance: The investigated plant species are traditionally used by Venda people of South Africa, in the treatment of malaria and associated symptoms.Aim of the study: To evaluate the in vitro antiplasmodial efficacy and cytotoxic properties of indigenous medicinal plants used by Venda people against malaria. Materials and methods:In vitro antiplasmodial activity and cytotoxic properties were evaluated on twenty indigenous plant species. Ground plant material was extracted in dichloromethane: 50% methanol (1:1). Antiplasmodial activity was evaluated against the chloroquine-sensitive strain of Plasmodium falciparum (NF54). The cytotoxicity of the plant extracts were assessed against mammalian L-6 rat skeletal myoblast cells. The selectivity index (SI) values were then calculated.Results: Of the 43 plant extracts evaluated, 10 exhibited pronounced antiplasmodial activity (IC 50 ≤ 5μg/ml) with good therapeutic indices (SI ≥ 10). Lipophilic plant extracts were relatively more potent than polar extracts. Tabernaemontana elegans Stapf. (Apocynaceae) and Vangueria infausta Burch. subsp. infausta (Rubiaceae) extracts displayed significant antiplasmodial activity (IC 50 < 2 μg/ml). Conclusion:Findings of this study partly support the ethnomedical use of the investigated plant species by Venda people as antimalarial remedies. The study also highlights some of the knowledge gaps that require further phytochemical studies on the specified plant species.

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“…Although the isolation of an active principle was not carried out, it is likely that the molecule presenting the highest antiplasmodial activity is a triterpene, since compounds of this class have several studies reporting its antiplasmodial activities (NOGUEIRA;LOPES, 2011;RAMALHETE et al, 2011;RAMALHETE et al, 2014) and this chemical class seems to be the most abundant in species of the genus Combretum (DAWE et al, 2013) and in the species C. leprosum (FACUNDO et al, 1993;FACUNDO et al, 2008). Triterpenes that were isolated from the genus Combretum also showed activities against another microorganisms, like fungi (BISOLI et al, 2008), bacteria (ANGEH et al, 2007a;ANGEH et al, 2007b;SONGCA, RAMURAFHI;OLUWAFEMI, 2013), viruses (ASRES;BUCAR, 2005) and other species of parasites (TELES et al, 2011;HAAVIKO et al, 2014).…”

Section: Resultsmentioning

confidence: 99%

In Vitro Antiplasmodial Activity of Flower Extracts From Combretum Leprosum Mart (Mofumbo)

Passarini

Medeiros

Meneguetti

et al. 2016

CeN

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Malaria is the cause of hundreds of thousands of deaths per year, besides putting billions of people at risk of developing disease. When it comes to its therapy, the drugs used currently are losing its efficacy due to increase in the frequency of resistant strains of the parasite, highlighting the importance for the search of new classes of molecules presenting antiplasmodial activity. In the present work, the antiplasmodial activities of five extracts (crude, hexane, chloroform, ethyl acetate and methanol) from the flowers of Combretum leprosum are assessed. The method employed for obtaining the extracts was silica gel column chromatography, and the techniques used for the analysis of antiplasmodial activity (IC 50 ) and citotoxicity (MLD 50 ) were ELISA and MTT respectively, where a selectivity index was calculated after the obtaining of these two values. The extract presenting the highest antiplasmodial activity was the chloroform extract (IC 50 = 3.97 µg/mL), however, this extract also presented the higher cytotoxicity (MLD 50 = 18.12 µg/mL), and therefore the extract presenting the best overall activity was the methanolic extract (IS = 18.97 IntrodutionOver 3 billion people are estimated to be at risk of being infected with malaria and therefore developing disease, and according to latest estimates, hundreds of thousands of deaths caused by it occurred in each year of this millennium (WHO, 2014). The world region that suffers the heaviest burden is Africa, where the great majority of cases of malaria occur, mainly in children under the age of five (WHO, 2014). The disease is caused by parasitic protozoa of the genus Plasmodium, of which five species are known to infect humans: P. falciparum, P. vivax, P. malariae, P. ovale, and P. knowlesi (COX, 2010). The parasite life cycle begins when a female mosquito of Anopheles genus bites a human and releases the sporozoites from its salivary glands to the dermis, where they reach the avascular tissue and then a percentage of them migrates and enters the blood vessels, making their way to the liver, where they undergo cellular modifications and perform rounds of asexual replication (ALY; VAUGHAN; KAPPE, 2009).After leaving the liver, the parasite begins other cycles of asexual replication inside red blood cells, using molecules and cellular structures of the host cells to survive, grow and reproduce, generating thousands of merozoites and causing the characteristic symptoms of the disease (TILLEY; DIXON; KIRK, 2011). When it comes to its chemotherapy, most of the cases of uncomplicated malaria are treated currently by the use of ACT's drugs, although is already known that these drugs are losing its efficacy due to the increase in frequency of resistant strains (VISSER; VUGT; GROBUSCH, 2014), which highlights the importance for the search of new molecules bearing antiplasmodial activity.Plants have been used during millennia by humanity, and pharmacological studies of medicinal plants yielded useful molecules in the treatment of various diseases, includ...

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Karavilagenin C derivatives as antimalarials

Cited by 27 publications

References 27 publications

In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents

In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents

In vitro antiplasmodial screening of ethnopharmacologically selected South African plant species used for the treatment of malaria

In Vitro Antiplasmodial Activity of Flower Extracts From Combretum Leprosum Mart (Mofumbo)

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