Antiplasmodial activity of (I-3,II-3)-biflavonoids and other constituents from Ormocarpum kirkii

Dhooghe, Liene; Maregesi, Sheila M.; Mincheva, Irena; Ferreira, Daneel; Marais, Jannie P.J.; Lemière, Filip; Matheeussen, An; Cos, Paul; Maes, Louis; Vlietinck, A. J.; Apers, Sandra; Pieters, Luc

doi:10.1016/j.phytochem.2010.02.005

Cited by 48 publications

(43 citation statements)

References 26 publications

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“…In addition, compounds 1, 2 and 5 exhibited AChE inhibitory activity with minimum inhibitory requirement values of 100, 50 and 1000 ng, respectively (Table 1). Compound 2 has been reported antimalarial against P. falciparum and cytotoxic against MRC-5 with IC 50 values of 2.18 and 8.13 mg/mL, respectively (Dhooghe et al 2010 Figure 1. Structures of isolated compounds 1 -10.…”

Section: Resultsmentioning

confidence: 99%

Chemical constituents and biological activities from roots ofEnkleia siamensis

Rajachan

Kanokmedhakul

Nasomjai

et al. 2013

Natural Product Research

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Chemical investigation from roots of Enkleia siamensis (Kurz) Nervling resulted in the isolation of 10 compounds. Their structures were established on the basis of 1D and 2D NMR spectroscopic data as linobiflavonoid (1), chamaejasmin (2), 7-O-β-D-glucopyranosylchamaejasmin (3), ormocarpin (4), (-)-wikstromol (5), matairesinol (6), (+)-lariciresinol (7), umbelliferone (8), daphnoretin (9) and carthamidin (10). Compounds 2 and 8 showed cytotoxicity against KB, MCF-7 and NCI-H187 cancer cell lines. Compounds 1, 2 and 5 showed weak minimum inhibitory requirements to acetylcholinesterase with values ranging from 50 to 1000 ng. In addition, compound 2 exhibited antimalarial activity against Plasmodium falciparum with an IC50 value of 2.32 μg/mL.

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Section: Resultsmentioning

confidence: 99%

Chemical constituents and biological activities from roots ofEnkleia siamensis

Rajachan

Kanokmedhakul

Nasomjai

et al. 2013

Natural Product Research

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“…Numerous studies have been reported wide varieties of pharmacological activities of polyphenols and flavonoids, including antiplasmodial activity [24,25]. Antiplasmodial activity has been reported for some biflavonoids primarily (I-30, II-8)-biflavones, in which a high number of methoxy substituents were associated with high activity [26]. This group enhances the lipophilicity of the substance, improving its incorporation into cells [27].…”

Section: Discussionmentioning

confidence: 99%

In vitro antiplasmodial activity of Withania frutescens —Solanaceae

Bouzidi

Bakrim

Mahiou

et al. 2017

European Journal of Integrative Medicine

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A B S T R A C TIntroduction: Drugs resistant Plasmodium falciparum is a recurring issue that threatens public health. New anti-plasmodial drugs are needed to overcome this problem. The aim of this study was to characterize in vitro an-tiplasmodial activity of Withania frutescens (Solanaceae) against chloroquine-resistant Plasmodium falciparum strain. Methods: The in vitro antiplasmodial activity of leaves and roots extracts from Withania frutescens was performed in 96 well plates and preliminary phytochemical analysis was performed for the active fractions. The toxicity of the plant extract against CHO (Chinese Hamster Ovary) cells was assessed using the tetrazolium salt MTT col-orimetric assay. The selectivity index (SI) was calculated as the ratio between the cytotoxic and antiparasitic activities. Results: The methanol extract of W. frutescens leaves showed a good antiplasmodial activity (CC 50 18.1 μg/ml). Furthermore, ethyl acetate and butanol fractions showed promising in vitro antiplasmodial activity with a se-lectivity index of 3.1 and 2.4, respectively. The roots of W. frutescens were found to be inactive with a CC 50 value > 80 μg/ml. Conclusion: The antiplasmodial activity of W. frutescens may in part be attributed to the presence of polyphenolic and flavonoid compounds. Based on our results, ethyl acetate and butanol leaves fractions could be considered as a promising source for the development of putative antiplasmodial drugs.

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“…For the trans-isomers of dihydroflavone, the thermodynamically more stable conformation was when 2-H was axial and 3-H was equatorial, and therefore the absolute configuration had to be either (2R, 3S) or (2S, 3R) [9]. Moreover, for 1, a negative n → π ⁎ "cotton effects" at high wavelength (309 nm, Δε − 14.25) by CD spectrum indicated a 2R configuration [10], so the configurations of C-2/C-3 were deduced to be (2R, 3S). Besides, the two parts of the structure of 1 had the same units, rather than antipode for each other (their 1 H-and 13 C-NMR signals were overlapped and the [α] D 19 was not zero), so the two units had the same absolute configurations of (2R, 3S) and (2″R, 3″S) at C-2/C-3 and C-2″/C-3″.…”

Section: Cytotoxic Assaymentioning

confidence: 99%