Isolation of narciprimine from Cyrtanthus contractus (Amaryllidaceae) and evaluation of its acetylcholinesterase inhibitory activity

Nair, Jerald J.; Aremu, Adeyemi O.; Staden, J. Van

doi:10.1016/j.jep.2011.07.028

Cited by 48 publications

(52 citation statements)

References 26 publications

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“…A dataset containing 36 newly synthesized compounds collected from recent literature [80][81][82] and 50 decoys which were not included in the training and test set was used as an external test set. Prediction performances of the nine models are shown in Table 3.…”

Section: External Test Setmentioning

confidence: 99%

Classification of Acetylcholinesterase Inhibitors and Decoys by a Support Vector Machine

Wang¹,

Hu²,

Wang³

et al. 2012

CCHTS

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Acetylcholinesterase has long been considered as a target for Alzheimer disease therapy. In this work, several classification models were built for the purpose of distinguishing acetylcholinesterase inhibitors (AChEIs) and decoys. Each molecule was initially represented by 211 ADRIANA.Code and 334 MOE descriptors. Correlation analysis, F-score and attribute selection methods in Weka were used to find the best reduced set of descriptors, respectively. Additionally, models were built using a Support Vector Machine and evaluated by 5-, 10-fold and leave-one-out cross-validation. The best model gave a Matthews Correlation Coefficient (MCC) of 0.99 and a prediction accuracy (Q) of 99.66% for the test set. The best model also gave good result on an external test set of 86 compounds (Q=96.51%, MCC=0.93). The descriptors selected by our models suggest that H-bond and hydrophobicity interactions are important for the classification of AChEIs and decoys.

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Section: External Test Setmentioning

confidence: 99%

Classification of Acetylcholinesterase Inhibitors and Decoys by a Support Vector Machine

Wang¹,

Hu²,

Wang³

et al. 2012

CCHTS

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“…Pancratistatin is another alkaloid obtained from this family that has shown potent and cell line specific antiproliferative properties (Jensen et al, 2011;Nair and van Staden, 2013). Some other plants in this family, such as Boophone disticha and Cyclamen purpurascens have displayed novel, broad spectrum antibacterial activity (Cheesman et al, 2012) and may contain antibacterial agents which could be used in the treatment of typhoid fevers and urogenital infections respectively (Nkanwen et al, 2009) of the abundant alkaloids obtained from the family Amaryllidaceae are hypothesized to be responsible for various medicinal properties of the family (Chattopadhyay et al, 1983;Boger and Wolkenberg, 2000;Koorbanally et al, 2000;Nair et al, 2000;Elgorashi et al, 2003a;;Osorio et al, 2010;Cheesman et al, 2012;Refaat et al, 2012a, 2012b, 2012c, 2013a, 2013bJin, 2013 and have shown cardiovascular activity (Mugabo et al, 2001;Andraws et al, 2005;Burger et al, 2009;Rostoff et al, 2010;Jayakumar and Sheu, 2011;Nair et al, 2011;Mugabo et al, 2012). Previously, we have reported positive inotropic effect, with no chronotropic effect (Mugabo et al, 2001) and negative inotropic and chronotropic effects with crude extracts of the bulbs of Crinum macowanii and hippadine respectively, in isolated perfused rat hearts.…”

Section: Introductionmentioning

confidence: 99%

Effects of hippadine on the blood pressure and heart rate in male spontaneously hypertensive Wistar rats

Mugabo

Philander

Raji

et al. 2014

Journal of Ethnopharmacology

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“…Statistically, more than 500 different kinds of Amaryllidaceae alkaloids (AAs) have been isolated from the medicinal plants of the family Amaryllidaceae123. Owing to the diverse pharmacological activities, such as anticancer, antimalaria, antifungal, neuroprotective effects, acetylcholinesterase and butyrylcholinesterase-inhibitory activity4567, these alkaloids have attracted a great deal of attentions in modern medical societies.…”

mentioning

confidence: 99%

Antiproliferative activities of Amaryllidaceae alkaloids from Lycoris radiata targeting DNA topoisomerase I

Chen

Tian

et al. 2016

Sci Rep

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Crude Amaryllidaceae alkaloids (AAs) extracted from Lycoris radiata are reported to exhibit significant anti-cancer activity. However, the specific alkaloids responsible for the pharmacodynamic activity and their targets still remain elusive. In this context, we strived to combine affinity ultrafiltration with topoisomerase I (Top I) as a target enzyme aiming to fish out specific bioactive AAs from Lycoris radiata. 11 AAs from Lycoris radiata were thus screened out, among which hippeastrine (peak 5) with the highest Enrichment factor (EF) against Top I exhibited good dose-dependent inhibition with IC50 at 7.25 ± 0.20 μg/mL comparable to camptothecin (positive control) at 6.72 ± 0.23 μg/mL. The molecular docking simulation further indicated the inhibitory mechanism between Top I and hippeastrine. The in vitro antiproliferation assays finally revealed that hippeastrine strongly inhibited the proliferation of HT-29 and Hep G2 cells in an intuitive dose-dependent manner with the IC50 values at 3.98 ± 0.29 μg/mL and 11.85 ± 0.20 μg/mL, respectively, and also induced significant cellular morphological changes, which further validated our screening method and the potent antineoplastic effects. Collectively, these results suggested that hippeastrine could be a very promising anticancer candidate for the therapy of cancer in the near future.

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Isolation of narciprimine from Cyrtanthus contractus (Amaryllidaceae) and evaluation of its acetylcholinesterase inhibitory activity

Cited by 48 publications

References 26 publications

Classification of Acetylcholinesterase Inhibitors and Decoys by a Support Vector Machine

Classification of Acetylcholinesterase Inhibitors and Decoys by a Support Vector Machine

Effects of hippadine on the blood pressure and heart rate in male spontaneously hypertensive Wistar rats

Antiproliferative activities of Amaryllidaceae alkaloids from Lycoris radiata targeting DNA topoisomerase I

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