In vitro antiplasmodial activity of indole alkaloids from the stem bark of Geissospermum vellosii

Mbeunkui, Flaubert; Grace, Mary H.; Lategan, Carmen; Smith, Peter J.; Raskin, Ilya; Lila, Mary Ann

doi:10.1016/j.jep.2011.11.036

Cited by 54 publications

(39 citation statements)

References 25 publications

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“…In addition, 1,2,3-triazole-tethered ␤-lactam and 7-chloroquinoline bifunctional hybrids were synthesized and showed reasonable antimalarial activities, with IC 50 values ranging from 1. (24,25). A series of novel ketoenamine chalcone-chloroquine-based hybrids were synthesized, and compounds 25 and 27 each showed 99.9% in vivo suppression of parasitemia at a dosage of 100 mg/ kg/day by the oral route (26).…”

Section: Discussionmentioning

confidence: 99%

Enhanced Antimalarial Activity by a Novel Artemether-Lumefantrine Lipid Emulsion for Parenteral Administration

Zhao

et al. 2014

Antimicrob Agents Chemother

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dArtemether and lumefantrine (also known as benflumetol) are difficult to formulate for parenteral administration because of their low aqueous solubility. Cremophor EL as an emulsion excipient has been shown to cause serious side effects. This study reports a method of preparation and the therapeutic efficacies of novel lipid emulsion (LE) delivery systems with artemether, lumefantrine, or artemether in combination with lumefantrine, for parenteral administration. Their physical and chemical stabilities were also evaluated. Furthermore, the in vivo antimalarial activities of the lipid emulsions developed were tested in Plasmodium berghei-infected mice. Artemether, lumefantrine, or artemether in combination with lumefantrine was encapsulated in an oil phase, and the in vivo performance was assessed by comparison with artesunate for injection. It was found that the lumefantrine lipid emulsion (LUM-LE) and artemether-lumefantrine lipid emulsion (ARM-LUM-LE-3) (1:6) began to decrease the parasitemia levels after only 3 days, and the parasitemia inhibition was 90% at doses of 0.32 and 0.27 mg/kg, respectively, with immediate antimalarial effects greater than those of the positive-control group and constant antimalarial effects over 30 days. LUM-LE and ARM-LUM-LE-3 demonstrated the best performance in terms of chemical and physical stabilities and antiplasmodial efficacy, with a mean particle size of 150 nm, and they have many favorable properties for parenteral administration, such as biocompatibility, physical stability, and ease of preparation. Malaria is one of the most significant causes of morbidity and death worldwide. Every year, nearly one million deaths result from malaria infection, with about 85% occurring among children under 5 years of age. Indeed, one patient dies from malaria every 36 s (1).Artemisinin and its derivatives are the most important antimalarial drugs; the chemical structures of the four artemisinin compounds and lumefantrine (also known as benflumetol) are presented in Fig. 1. Artemisinin is an effective antimalarial drug isolated from the Chinese herbal medicine Artemisia annua L. It has a special sesquiterpene lactone with a peroxy group. In malaria parasites, artemisinin can be activated by intraparasitic heme iron, which catalyzes cleavage of the endoperoxide (2). Due to its unique structure and antimalarial mechanism, artemisinin has excellent antimalarial activity with low toxicity; therefore, artemisinin-based combination therapy (ACT) is recommended as the first-line strategy to treat malaria (3). After the introduction of ACT interventions, morbidity and mortality rates associated with malaria were decreased in several parts of the world (4). However, antimalarial resistance would probably be increased after longterm application of artemisinin alone. WHO reformed the malaria treatment policy in February 2004, proposing to stop the use of single antimalarial drugs (e.g., artemisinin and quinine) and promoting the use of ACTs. Recently, combination therapies such as artemether in co...

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Section: Discussionmentioning

confidence: 99%

Enhanced Antimalarial Activity by a Novel Artemether-Lumefantrine Lipid Emulsion for Parenteral Administration

Zhao

et al. 2014

Antimicrob Agents Chemother

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“…3F [20]. Compound 4 was identified as geissoschizone [31] based on the comprehensive 2D NMR analysis (Suppl . Tables 1 and 2).…”

Section: Analysis and Identification Of Alkaloidsmentioning

confidence: 99%

Isolation and structural elucidation of indole alkaloids from Geissospermum vellosii by mass spectrometry

Mbeunkui¹,

Grace²,

Lila³

2012

Journal of Chromatography B

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“…Mbeunkui et al (2012) 28 showed the alkaloids geissolosimine, geissospermine, geissoschizoline and vellosiminol, isolated from crude methanolic extract of G. vellosii, had antiplasmodial activity in vitro antiplasmodial activity against the chloroquine-sensitive strain of Plasmodium falciparum, and showed the highest activity for geissolosimine and a weak activity for vellosiminol.…”

Section: S-susceptible (Zone Of Bacterial Inhibition In Mm)mentioning

confidence: 99%

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2012

IJPSR

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The main cause of increasing of infectious diseases cases is due to multidrugresistant microorganisms emergence, particularly Pseudomonas aeruginosa and Staphylococcus aureus, responsible for most of hospital-acquired infections and millions deaths related. Despite development of new antibiotics, control of these microorganisms is not always successful. Several plant extracts have demonstrated antimicrobial effects and may be used as an alternative therapy for these infections. Aiming to evaluate antibacterial activity of extracts from Eleutherine plicata (marupazinho), Geissospermum vellosii (pau-pereira) and Portulaca pilosa (amor crescido) against multidrugresistant bacteria, samples of Oxacillin-Resistant Staphylococcus aureus (ORSA) and multidrug-resistant P. aeruginosa (MDR P. aeruginosa) isolated from human clinical processes were tested. The antibacterial activity was determined by disk diffusion method and minimum inhibitory concentration (MIC) by microdilution method. Extracts and fractions were tested at concentrations of 500, 250, 125, 62.5, 31.2 and 16.2 µg/mL dissolved in DMSO 10%. E.

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In vitro antiplasmodial activity of indole alkaloids from the stem bark of Geissospermum vellosii

Cited by 54 publications

References 25 publications

Enhanced Antimalarial Activity by a Novel Artemether-Lumefantrine Lipid Emulsion for Parenteral Administration

Enhanced Antimalarial Activity by a Novel Artemether-Lumefantrine Lipid Emulsion for Parenteral Administration

Isolation and structural elucidation of indole alkaloids from Geissospermum vellosii by mass spectrometry

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