scholarly journals Antiprotozoal Nor-Triterpene Alkaloids from Buxus sempervirens L.

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 696
Author(s):  
Lara U. Szabó ◽  
Marcel Kaiser ◽  
Pascal Mäser ◽  
Thomas J. Schmidt
Keyword(s):  
Causative Agent ◽  
Mammalian Cells ◽  
Sleeping Sickness ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
East African ◽  
Trypanosoma Brucei Rhodesiense ◽  
Buxus Sempervirens ◽  
Life Threatening

Malaria and human African trypanosomiasis (HAT; sleeping sickness) are life-threatening tropical diseases caused by protozoan parasites. Due to limited therapeutic options, there is a compelling need for new antiprotozoal agents. In a previous study, O-tigloylcyclovirobuxeine-B was recovered from a B. sempervirens L. (common box; Buxaceae) leaf extract by bioactivity-guided isolation. This nor-cycloartane alkaloid was identified as possessing strong and selective in vitro activity against the causative agent of malaria tropica, Plasmodium falciparum (Pf). The purpose of this study is the isolation of additional alkaloids from B. sempervirens L. to search for further related compounds with strong antiprotozoal activity. In conclusion, 25 alkaloids were obtained from B. sempervirens L., including eight new natural products and one compound first described for this plant. The structure elucidation was accomplished by UHPLC/+ESI-QqTOF-MS/MS and NMR spectroscopy. The isolated alkaloids were tested against Pf and Trypanosoma brucei rhodesiense (Tbr), the causative agent of East African sleeping sickness. To assess their selectivity, cytotoxicity against mammalian cells (L6 cell line) was tested as well. Several of the compounds displayed promising in vitro activity against the pathogens in a sub-micromolar range with concurrent high selectivity indices (SI). Consequently, various alkaloids from B. sempervirens L. have the potential to serve as a novel antiprotozoal lead structure.

scholarly journals Antiprotozoal Activity of Turkish Origanum onites Essential Oil and Its Components

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4421 ◽  
Author(s):  
Tasdemir ◽  
Kaiser ◽  
Demirci ◽  
Demirci ◽  
Baser
Keyword(s):  
Gas Chromatography ◽  
Essential Oil ◽  
Mammalian Cells ◽  
Leishmania Donovani ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Flame Ionization ◽  
Main Component ◽  
Origanum Onites

Essential oil of Origanum species is well known for antimicrobial activity, but only a few have been evaluated in narrow spectrum antiprotozoal assays. Herein, we assessed the antiprotozoal potential of Turkish Origanum onites L. oil and its major constituents against a panel of parasitic protozoa. The essential oil was obtained by hydrodistillation from the dried herbal parts of O. onites and analyzed by Gas Chromatography-Flame Ionization Detector (GC-FID) and Gas Chromatography coupled with Mass Spectrometry (GC-MS). The in vitro activity of the oil and its major components were evaluated against Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani, and Plasmodium falciparum. The main component of the oil was identified as carvacrol (70.6%), followed by linalool (9.7%), p-cymene (7%), γ-terpinene (2.1%), and thymol (1.8%). The oil showed significant in vitro activity against T. b. rhodesiense (IC50 180 ng/mL), and moderate antileishmanial and antiplasmodial effects, without toxicity to mammalian cells. Carvacrol, thymol, and 10 additional abundant oil constituents were tested against the same panel; carvacrol and thymol retained the oil’s in vitro antiparasitic potency. In the T. b. brucei mouse model, thymol, but not carvacrol, extended the mean survival of animals. This study indicates the potential of the essential oil of O. onites and its constituents in the treatment of protozoal infections.

scholarly journals In Vitro Activity of the Antifungal Plant Defensin RsAFP2 against Candida Isolates and Its In Vivo Efficacy in Prophylactic Murine Models of Candidiasis

2008 ◽  
Vol 52 (12) ◽  
pp. 4522-4525 ◽  
Author(s):  
Patricia M. Tavares ◽  
Karin Thevissen ◽  
Bruno P. A. Cammue ◽  
Isabelle E. J. A. François ◽  
Eliana Barreto-Bergter ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Mammalian Cells ◽  
Vitro Activity ◽  
Murine Models ◽  
In Vitro Activity ◽  
Plant Defensin ◽  
In Vivo Efficacy

ABSTRACT We show that RsAFP2, a plant defensin that interacts with fungal glucosylceramides, is active against Candida albicans, inhibits to a lesser extent other Candida species, and is nontoxic to mammalian cells. Moreover, glucosylceramide levels in Candida species correlate with RsAFP2 sensitivity. We found RsAFP2 prophylactically effective against murine candidiasis.

scholarly journals Niclosamide Is Active In Vitro against Mycetoma Pathogens

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 4005
Author(s):  
Abdelhalim B. Mahmoud ◽  
Shereen Abd Algaffar ◽  
Wendy van de Sande ◽  
Sami Khalid ◽  
Marcel Kaiser ◽  
...  
Keyword(s):  
Nitro Group ◽  
Causative Agent ◽  
Drug Repurposing ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Minimal Inhibitory Concentrations ◽  
Redox Active ◽  
Causative Agents ◽  
Madurella Mycetomatis

Redox-active drugs are the mainstay of parasite chemotherapy. To assess their repurposing potential for eumycetoma, we have tested a set of nitroheterocycles and peroxides in vitro against two isolates of Madurella mycetomatis, the main causative agent of eumycetoma in Sudan. All the tested compounds were inactive except for niclosamide, which had minimal inhibitory concentrations of around 1 µg/mL. Further tests with niclosamide and niclosamide ethanolamine demonstrated in vitro activity not only against M. mycetomatis but also against Actinomadura spp., causative agents of actinomycetoma, with minimal inhibitory concentrations below 1 µg/mL. The experimental compound MMV665807, a related salicylanilide without a nitro group, was as active as niclosamide, indicating that the antimycetomal action of niclosamide is independent of its redox chemistry (which is in agreement with the complete lack of activity in all other nitroheterocyclic drugs tested). Based on these results, we propose to further evaluate the salicylanilides, niclosamidein particular, as drug repurposing candidates for mycetoma.

Searching for new drugs for Chagas diseases: triazole analogs display high in vitro activity against Trypanosoma cruzi and low toxicity toward mammalian cells

2018 ◽  
Vol 50 (2) ◽  
pp. 81-91 ◽  
Author(s):  
Robson Xavier Faria ◽  
Daniel Tadeu Gomes Gonzaga ◽  
Paulo Anastácio Furtado Pacheco ◽  
André Luis Almeida Souza ◽  
Vitor Francisco Ferreira ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Mammalian Cells ◽  
New Drugs ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Low Toxicity

The alkaloid fraction from Buxus sempervirens leaves shows strong in vitro activity against Plasmodium falciparum

Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
JB Althaus ◽  
G Jerz ◽  
P Winterhalter ◽  
M Kaiser ◽  
R Brun ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Buxus Sempervirens ◽  
Alkaloid Fraction

Role of Single-Electron Oxidation Potential and Lipophilicity in the Antiplasmodial in vitro Activity of Polyphenols: Comparison to Mammalian Cells

2008 ◽  
Vol 63 (5-6) ◽  
pp. 445-450 ◽  
Author(s):  
Philippe Grellier ◽  
Aušra Nemeikaitė-Čėnienė ◽  
Jonas Šarlauskas ◽  
Narimantas Čėnas
Keyword(s):  
Mammalian Cell ◽  
Mammalian Cells ◽  
Oxidation Potential ◽  
Vitro Activity ◽  
Antiplasmodial Activity ◽  
Cell Cytotoxicity ◽  
In Vitro Activity ◽  
Positive Dependence

In spite of extensive studies, the structure-activity relationships in the action of polyphenols against the malaria parasite Plasmodium falciparum are poorly understood so far. As the mammalian cell cytotoxicity of polyphenols shows a negative dependence on the potential of the phenoxyl radical/phenol redox couple (E27 ), due to the involvement of prooxidant events, and a positive dependence on the octanol/water distribution coefficient at pH 7.0 (log D), we examined the role of these parameters in their antiplasmodial in vitro activity. We found that the concentrations of hydroxybenzenes causing 50% inhibition of the growth of P. falciparum strain FcB1 (IC50) are described by the regression log IC50 (μm) = 0.36 + 1.81 E27 (V) - 0.10 log D [n = 11, r2 = 0.760, F(2.8) = 12.03]. The IC50 values of flavonoids (n = 5), comprising a separate less active series, did not depend on their E27 values, 0.33 V- 0.75 V. These findings were similar to the mammalian cell cytotoxicity data. However, the mammalian cell cytotoxicity of hydroxybenzenes showed more pronounced dependence on their E27 values [Δlog CL50 /ΔE27 = (6.9-5.1) V-1, where CL50 is the compound concentration for 50% cell survival] than on their antiplasmodial activity. Although it is unclear whether the prooxidant action is the main factor in the antiplasmodial action of polyphenols or not, our data showed that the ease of their oxidation (decrease in E27 ) may enhance their activity. On the other hand, the different sensitivity of the mammalian cell cytotoxicity and the antiplasmodial activity of the hydroxybenzenes to their E27 values implied that compounds with high oxidation potential may be used as relatively efficient antiplasmodial agents with low mammalian cell cytotoxicity.

In Vitro Activity of Phytocannabinoids from High Potency Cannabis sativa

Planta Medica ◽  
2012 ◽  
Vol 78 (05) ◽  
Author(s):  
A Husni ◽  
S Ross ◽  
O Dale ◽  
C Gemelli ◽  
G Ma ◽  
...  
Keyword(s):  
Cannabis Sativa ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
High Potency
Sign in / Sign up

Export Citation Format

Share Document