Cholinesterase Inhibiting and Antiplasmodial Steroidal Alkaloids from Sarcococca hookeriana

Devkota, Krishna Prasad; Lenta, Bruno Ndjakou; Choudhary, M. Iqbal; Naz, Qamar; Boyom, Fabrice Fekam; Rosenthal, Philip; Sewald, Norbert

doi:10.1248/cpb.55.1397

Cited by 43 publications

(45 citation statements)

References 19 publications

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“…The pharmacological action of this plant is reported as antibacterial, antitumor, antiulcer and acetylcholine esterase inhibitory 46 and hypotensive [46][47][48] , respiratory disorders, gastrointestinal, liver diseases, syphilis, fever, inflammation, rheumatism 49 , ganglionblocking 50 , Alzheimers disease 48 , antileishmanial and antiplasmodial [51][52] . The plant species is known to possess a major source of sarcosine, saracodine and pachyaximine-A [53][54] .…”

Section: Ethnopharmacological Activitiesmentioning

confidence: 99%

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2017

IJPSR

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Indian medicinal plants and traditional knowledge have been an integral part of our lifestyle since ages and now became an important source for natural product research (NPR) and development. Due to its knowing ability and applications, this knowledge has long been used as a thriving source for discovery of new drug molecules. This study was conducted under the routine drug development program of the Institute with the aim to explore the first-hand ethnobotanical information of 4 important plants i.e. Artemisia nilagirica, Lyonia ovalifolia, Sarcococca saligna and Taraxacum officinale and to correlate their possible applications in future research and developmental activities. The reported information was collected from 86 informants (villagers and herbal practitioners) of Nainital, Almora and Bageshwar districts of Uttarakhand Himalaya, during 2014-2016. The popularity of individual plant species for their ethnopharmacological uses was calculated as percent citation (PC) and cross verified through other informants of studied areas as well as the literature reported for their modern therapeutic applications.

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Section: Ethnopharmacological Activitiesmentioning

confidence: 99%

Untitled

2017

IJPSR

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“…In addition, steroids may participate in growth regulation, proliferation and cell death (Devkota et al, 2007;Freilich et al, 2000;Pabón et al, 2002) and redox mechanisms (Pabón et al, 2009). These compounds could participate in a conjugated addition of nucleophilic amino acid residues present in target enzymes such as cysteine proteases on leishmania (Mottram et al, 2004) in a Michael type mechanism.…”

Section: Extract /Compound 1 2 3 4 5 (Diosgenonementioning

confidence: 99%

Antiprotozoal activity and cytotoxicity of extracts from Solanum arboreum and S. ovalifolium (Solanaceae)

LondoÃ±o¹,

Cardona²,

Álzate³

et al. 2016

J. Med. Plants Res.

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Leishmaniasis, Chagas and Malaria are a major health problem in Latin America. Medicinal plants constitute viable alternatives to conventional medicine in many developing countries. Several Solanum species have shown antimicrobial activity, specifically, Solanum nudum has shown in vitro antimalarial activity. Based on the aforementioned, we determined the antiprotozoal activity and cytotoxicity of alcoholic and non-alcoholic extracts from Solanum arboreum and Solanum ovalifolium. Extracts were obtained by percolation with solvents of different polarity: hexane, dichloromethane, ethyl acetate and ethanol. All extracts were evaluated in vitro for antiprotozoal activity against Leishmania panamensis, Trypanosome cruzi and Plasmodium falciparum. Cytotoxicity was also evaluated. In vitro screening showed that dichloromethane (D2) and ethanol (Et2) extracts of S. arboreum were the most active against all three protozoa tested here (EC 50 = 1.2 and 4.6 µg/ml against L. panamensis, 13.3 and 2.7 µg/ml against T. cruzi and 3.0 and 2.9 µg/ml against P. falciparum, respectively). These extract were cytotoxic against human U-937 macrophages (6.1 and 4.4 µg/ml, respectively). Additional studies on toxicity using other cell lines are needed. The activity of the Et2 extract is probably due to the presence of polar compounds such as saponins, flavonoids and coumarins. The activity of D2 extract is probably due to the presence of steroids such as diosgenone. These extracts have potential as a source of compounds for the development of new antiprotozoal therapeutical alternatives and therefore further studies are needed to evaluate and validate the use of the extracts as phytotherapeutics.

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“…The reaction mixture was slowly treated with 5% aq NH 4 Cl (20 mL) and extracted with three  20 mL portions of DCM. The combined organic extract was washed with water (20 mL) and brine (20 mL (8). Diosgenone (2, 50 mg, 0.12 mmol, 1 eq.)…”

Section: Chemical Transformationsmentioning

confidence: 99%

“…Only a few reports concerning antiplasmodial activity of steroids could be found in the literature, in spite of the fact that some steroidal alkaloids are active against malaria [8]. S. nudum steroidal compounds' antiplasmodial activity and their lack of mutagenicity, clastogenicity [9,10] and cytotoxicity [11] have substantiated this plant's potential use in anti-malarial medication and encouraged attempts to search for new pharmacophores and more active compounds than diosgenone.…”

Section: Introductionmentioning

confidence: 99%

Diosgenone Synthesis, Anti-Malarial Activity and QSAR of Analogues of This Natural Product

et al. 2013

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Solanum nudum Dunal steroids have been reported as being antimalarial compounds; however, their concentration in plants is low, meaning that the species could be threatened by over-harvesting for this purpose. Swern oxidation was used for hemisynthesis of diosgenone (one of the most active steroidal sapogenin diosgenin compounds). Eighteen structural analogues were prepared; three of them were found to be more active than diosgenone (IC 50 27.9 μM vs. 10.1 μM, 2.9 μM and 11.3 μM). The presence of a 4-en-3-one grouping in the A-ring of the compounds seems to be indispensable for antiplasmodial activity; progesterone (having the same functional group in the steroid A-ring) has also displayed antiplasmodial activity. Quantitative correlations between molecular structure and bioactivity were thus explored in diosgenone and several derivatives using well-established 3D-QSAR techniques. The models showed that combining electrostatic (70%) and steric (30%) fields can explain most variance regarding OPEN ACCESSMolecules 2013, 18 3357 compound activity. Malarial parasitemia in mice became reduced by oral administration of two diosgenone derivatives.

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Cholinesterase Inhibiting and Antiplasmodial Steroidal Alkaloids from Sarcococca hookeriana

Cited by 43 publications

References 19 publications

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Antiprotozoal activity and cytotoxicity of extracts from Solanum arboreum and S. ovalifolium (Solanaceae)

Diosgenone Synthesis, Anti-Malarial Activity and QSAR of Analogues of This Natural Product

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