Antiplasmodial Activity, Cytotoxicity and  Structure-Activity Relationship Study of Cyclopeptide Alkaloids

Tuenter, Emmy; Segers, Karen; Kang, Kyo Bin; Viaene, Johan; Sung, Sang Hyun; Cos, Paul; Maes, Louis; Heyden, Yvan Vander; Pieters, Luc

doi:10.3390/molecules22020224

Cited by 24 publications

(16 citation statements)

References 17 publications

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“…The plant extracts were assayed against Plasmodium falciparum chloroquine-sensitive (FCB), P. falciparum chloroquine-resistant (W2), and a P. falciparum field isolate (coded CAM06, obtained from local patients) strains using the lactate dehydrogenase (pLDH) method previously described by [22] and modified by [23, 24]. Parasites were cultured in vitro according to the method of [25].…”

Section: Methodsmentioning

confidence: 99%

Antimalarial Efficacy and Toxicological Assessment of Extracts of Some Ghanaian Medicinal Plants

Laryea

Borquaye

2019

Journal of Parasitology Research

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The economic costs associated with morbidity and mortality due to malaria and malaria associated complications in many sub-Saharan countries and other malaria endemic regions of the world are huge. Reports of emergence of parasite resistance to current malaria drugs have complicated malaria treatment and require the development of new therapeutic agents. The folkloric use of medicinal plants for the management of malaria is well documented. This work evaluated the antiplasmodial activities and toxicity of some medicinal plants used to treat malaria and malaria-like symptoms in Ghana. Plant extracts were obtained by cold maceration in 70% ethanol. Antiplasmodial efficacies were assessed in vitro against 3 strains of Plasmodium falciparum strains (FCM, W2, and CAM06) and in vivo via the 4-day suppressive test in Plasmodium berghei infected mice. Cytotoxicity and acute toxicity were assessed in mammalian cells and mice, respectively. All extracts were active against at least one of the Plasmodium falciparum strains in in vitro evaluations with IC50’s in the range of 4–116 μg/mL, whereas Bidens pilosa extracts, with a chemosuppression rate of 75%, was the most active plant in the in vivo experiments. All plant extracts displayed very weak to no cytotoxicity against the mammalian cell line used and exhibited very good selectivity towards the Plasmodium parasites. Syzygium guineense and Parinari congensis extracts were the most toxic in the acute toxicity tests. Altogether, the results indicate that the medicinal plants do possess impressive antiplasmodial properties and provide scientific basis for their use in traditional herbal medicine.

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Section: Methodsmentioning

confidence: 99%

Antimalarial Efficacy and Toxicological Assessment of Extracts of Some Ghanaian Medicinal Plants

Laryea

Borquaye

2019

Journal of Parasitology Research

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“…Further, two aporphine alkaloids and other compounds were isolated from Xylopia sericea leaves. One of the aporphine alkaloids, anonaine (55)…”

Section: Aporphine and Morphinandienone Alkaloidsmentioning

confidence: 99%

“…e ring system consists of a hydroxystyrylamine moiety, an amino acid, and a β-hydroxy amino acid; attached to the ring is a side chain, comprised of one or two more amino acid moieties [55]. e structures of the cyclopeptide alkaloids from plants that possess antimalarial activity are shown in Figure 10.…”

Section: Protoberberine Alkaloidsmentioning

confidence: 99%

Alkaloids from Plants with Antimalarial Activity: A Review of Recent Studies

Uzor

2020

Evidence-Based Complementary and Alternative Medicine

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Malaria is one of the major health problems in developing countries. The disease kills a large number of people every year and also affects financial status of many countries. Resistance of the plasmodium parasite, the causative agent, to the existing drugs, including chloroquine, mefloquine, and artemisinin based combination therapy (ACT), is a serious global issue in malaria treatment and control. This warrants an urgent quest for novel compounds, particularly from natural sources such as medicinal plants. Alkaloids have over the years been recognized as important phytoconstituents with interesting biological properties. In fact, the first successful antimalarial drug was quinine, an alkaloid, which was extracted from Cinchona tree. In the present review work, the alkaloids isolated and reported recently (2013 till 2019) to possess antimalarial activity are presented. Several classes of alkaloids, including terpenoidal, indole, bisindole, quinolone, and isoquinoline alkaloids, were identified with a promising antimalarial activity. It is hoped that the reports of the review work will spur further research into the structural modification and/or development of the interesting compounds as novel antimalarial drugs.

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“…Preliminary SAR studies indicated that the 13-membered ring cyclopeptide alkaloids were generally more active than the 14 and 15 membered analogues. Also, a methoxy group on the styrylamine moiety was more favourable for antiplasmodial activity than a hydroxy group [281, 282].…”

Section: Macrocyclesmentioning

confidence: 99%

Antiplasmodial natural products: an update

Tajuddeen

Heerden

2019

Malar J

122

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BackgroundMalaria remains a significant public health challenge in regions of the world where it is endemic. An unprecedented decline in malaria incidences was recorded during the last decade due to the availability of effective control interventions, such as the deployment of artemisinin-based combination therapy and insecticide-treated nets. However, according to the World Health Organization, malaria is staging a comeback, in part due to the development of drug resistance. Therefore, there is an urgent need to discover new anti-malarial drugs. This article reviews the literature on natural products with antiplasmodial activity that was reported between 2010 and 2017.MethodsRelevant literature was sourced by searching the major scientific databases, including Web of Science, ScienceDirect, Scopus, SciFinder, Pubmed, and Google Scholar, using appropriate keyword combinations.Results and DiscussionA total of 1524 compounds from 397 relevant references, assayed against at least one strain of Plasmodium, were reported in the period under review. Out of these, 39% were described as new natural products, and 29% of the compounds had IC50 ≤ 3.0 µM against at least one strain of Plasmodium. Several of these compounds have the potential to be developed into viable anti-malarial drugs. Also, some of these compounds could play a role in malaria eradication by targeting gametocytes. However, the research into natural products with potential for blocking the transmission of malaria is still in its infancy stage and needs to be vigorously pursued.

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Antiplasmodial Activity, Cytotoxicity and Structure-Activity Relationship Study of Cyclopeptide Alkaloids

Cited by 24 publications

References 17 publications

Antimalarial Efficacy and Toxicological Assessment of Extracts of Some Ghanaian Medicinal Plants

Antimalarial Efficacy and Toxicological Assessment of Extracts of Some Ghanaian Medicinal Plants

Alkaloids from Plants with Antimalarial Activity: A Review of Recent Studies

Antiplasmodial natural products: an update

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