New alkaloids from Cryptolepis sanguinolenta

Cimanga, K.; Bruyne, Tess De; Pieters, Luc; Claeys, Magda; Vlietinck, A. J.

doi:10.1016/0040-4039(96)00112-8

Cited by 188 publications

(124 citation statements)

References 3 publications

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“…Cryptolepine was isolated from Cryptolepis sanguino-lenta [24]. Neocryptolepine (as well as 2-C1-, 2-Br-and 2 methoxyneocryptolepine) was obtained by organic synthesis as previously described [25].…”

Section: Compoundsmentioning

confidence: 99%

Interactions of cryptolepine and neocryptolepine with unusual DNA structures

et al. 2003

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1 These authors contributed equally to this work. AbstractCryptolepine, the main alkaloid present in the roots of Cryptolepis sanguinolenta, presents a large spectrum of biological properties. It has been reported to behave like a DNA intercalator with a preference for GC-rich sequences. In this study, dialysis competition assay and mass spectrometry experiments were used to determine the affinity of cryptolepine and neocryptolepine for DNA structures among duplexes, triplexes, quadruplexes and single strands. Our data confirm that cryptolepine and neocryptolepine prefer GC over AT-rich duplex sequences, but also recognize triplex and quadruplex structures. These compounds are weak telomerase inhibitors and exhibit a significant preference for triplexes over quadruplexes or duplexes.

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Section: Compoundsmentioning

confidence: 99%

Interactions of cryptolepine and neocryptolepine with unusual DNA structures

et al. 2003

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“…Crude extracts of C. sanguinolenta and their fractions, as well as indoquinoline alkaloids isolated from the plant, have been shown to have activity against Plasmodium falciparum both in vitro and in vivo. [9][10][11][12][13] In addition to studies indicating anti-plasmodial effect, extracts of C. sanguinolenta have been shown to have anti-microbial activity 3,6,[14][15][16][17][18][19][20][21] , to be anti-hyperglycaemic 22,23 and antiinflammatory. 24 A preliminary study of the clinical efficacy of an aqueous extract of C. sanguinolenta as an anti-malarial preparation had been carried out which indicated the efficacy of the extract against falciparum malaria.…”

Section: Introductionmentioning

confidence: 99%

Clinical efficacy of a tea-bag formulation of Cryptolepis sanguinolenta root in the treatment of acute uncomplicated falciparum malaria

Bugyei¹,

Boye²,

Addy³

2011

Ghana Medical Journal

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SUMMARYObjective: To evaluate the clinical efficacy and safety of a tea bag formulation of the root of C. sanguinolenta Design: This is a prospective descriptive open trial. Setting: Patients were recruited from Korle-Bu, Mamprobi and Dansoman Polyclinics. Subjects: Forty-four subjects with uncomplicated malaria were recruited for the study. Method: Patients presented with clinical symptoms of malaria. Laboratory investigations conducted included malaria parasite counts, haematological indices and biochemical tests which were obtained before, during and after a 5-day treatment period, up to Day 28 posttreatment. All patients in the study were symptomatic with significant parasitaemia. Patients were given one teabag three times a day, that is, morning, noon and night, for five days of treatment. Results: Fifty percent of the patients were cleared of their P. falciparum parasitaemia by 72 hours, and all by Day 7. Presenting symptoms of fever, chills, nausea and vomiting cleared rapidly, all by Day 3, but resolution of haematological and biochemical abnormalities associated with malaria was generally slow, a feature seen in malaria post-treatment. The overall cure rate was 93.5% due to two cases of recrudescence on Days 21 and 28. The laboratory findings did not suggest any toxicity. Conclusion: On the basis of fever clearance and disappearance of parasitaemia by Day 7, the formulation has been shown to be non-toxic and highly effective in the treatment of acute uncomplicated malaria.

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“…SCHLTR. (Asclepiadaceae) have been used as scaffolds for drug discovery, since this plant is used as a traditional herbal medicine in West and Central Africa 12,13) (Fig. 1).…”

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confidence: 99%

Synthesis and in Vitro Testing of Antimalarial Activity of Non-natural-Type Neocryptolepines: Structure–Activity Relationship Study of 2,11- and 9,11-Disubstituted 6-Methylindolo[2,3-b]quinolines

et al. 2013

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This report describes the synthesis and in vitro anti-malarial evaluations of certain C2 or C8 and C11-disubstituted 6-methyl-5H-indolo[2,3-b]quinoline (neocryptolepine congener) derivatives. To attain higher activities, the structure-activity relationship (SAR) studies were conducted by varying the kind of alkylamino or ω-aminoalkylamino stubstituents at C11 and with Cl at the C2 position, or CO 2 Me at the C9 position. The anti-malarial activities of the tested compounds were significantly increased compared to the 11-non(alkylamino) derivatives. The 3-aminopropylamino group at C11 was further modified to urea and thiourea, which improved the cytotoxicity against normal cells. The best results were achieved with compounds 8 and 9d against the NF54 strain with the IC 50 /SI values as of 86 nM/20 and 317 nM/370, respectively. Furthermore, the compounds were tested for β-haematin inhibition. Twelve were found to have IC 50 values below 100 µM and a linear correlation between the β-haematin inhibition and cell growth inhibition in the NF54 strain was found for those derivatives with basic amino side chains. A second correlation was identified between the NF54 activity and physico-chemical factors related to solvation and polarity.

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New alkaloids from Cryptolepis sanguinolenta

Cited by 188 publications

References 3 publications

Interactions of cryptolepine and neocryptolepine with unusual DNA structures

Interactions of cryptolepine and neocryptolepine with unusual DNA structures

Clinical efficacy of a tea-bag formulation of <i>Cryptolepis sanguinolenta</i> root in the treatment of acute uncomplicated falciparum malaria

Synthesis and <i>in Vitro</i> Testing of Antimalarial Activity of Non-natural-Type Neocryptolepines: Structure–Activity Relationship Study of 2,11- and 9,11-Disubstituted 6-Methylindolo[2,3-<i>b</i>]quinolines

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