scholarly journals Biological and Phytochemical Investigations on Caesalpinia benthamiana, a Plant Traditionally Used as Antimalarial in Guinea

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Jean Loua ◽  
Mohamed Sahar Traore ◽  
Aissata Camara ◽  
Mamadou Aliou Balde ◽  
Louis Maes ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Methanolic Extract ◽  
Moderate Activity ◽  
Good Activity ◽  
Phytochemical Screening ◽  
Antiprotozoal Activity ◽  
Trypanosoma Brucei Brucei ◽  
Leaf Extracts ◽  
Bioassay Guided Fractionation

Caesalpinia benthamiana is widely used as antimalarial in Guinean traditional medicine. Leaf extracts of the plant were tested for their in vitro antiprotozoal activity against Trypanosoma brucei brucei and T. cruzi and the chloroquine-sensitive Ghana strain of Plasmodium falciparum along with their cytotoxicity on MRC-5 cells. The methanolic extract showed the strongest antiprotozoal activity against P. falciparum (IC50 4 μg/ml), a good activity against T. brucei (IC50 13 μg/ml), and a moderate activity against T. cruzi (IC50 31 μg/ml) along with an IC50 on human MRC-5 cells of 32 μg/ml. Bioassay-guided fractionation from the methanolic extract led to antiplasmodially active subfractions. A prospective, placebo-controlled ethnotherapeutic trial assessed the antimalarial effectiveness and tolerability of C. benthamiana syrup administered orally to children with uncomplicated malaria as compared with chloroquine syrup. Phytochemical screening of the leaf extracts indicated the presence of flavonoids, terpenoids, tannins, saponins, and iridoids.

scholarly journals Triterpenic Acids and Flavonoids from Satureja parvifolia. Evaluation of their Antiprotozoal Activity

2006 ◽  
Vol 61 (3-4) ◽  
pp. 189-192 ◽  
Author(s):  
Catalina van Baren ◽  
Ivie Anao ◽  
Paola Di Leo Lira ◽  
Silvia Debenedetti ◽  
Peter Houghton ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Moderate Activity ◽  
Antiprotozoal Activity ◽  
Active Components ◽  
Trypanosoma Brucei Rhodesiense ◽  
Meoh Extract ◽  
Triterpenic Acids ◽  
Bioassay Guided Fractionation ◽  
Low Cytotoxicity ◽  
First Time

Bioassay-guided fractionation of a Satureja parvifolia MeOH extract led to the isolation of eriodictyol, luteolin and ursolic and oleanolic acids as its active components against Plasmodium falciparum K1. This is the first time these compounds are reported as constituents of S. parvifolia. Ursolic acid showed an IC50 of 4.9 μg/ml, luteolin 6.4 μg/ml, oleanolic acid 9.3 μg/ml and eriodictyol 17.2 μg/ml. Antiplasmodial activity of eriodictyol and luteolin is reported here for the first time. Besides, the four compounds showed activity against P. falciparum 3D7 strain and Trypanosoma brucei rhodesiense. Eriodictyol showed moderate activity on all the parasites but was the most selective compound as a result of its rather low cytotoxicity (IC50 174.2 μg/ml) on the mammalian KB cell line.

scholarly journals Evaluation of theIn VitroAntiplasmodial, Antileishmanial, and Antitrypanosomal Activity of Medicinal Plants Used in Saudi and Yemeni Traditional Medicine

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Ramzi A. Mothana ◽  
Nawal M. Al-Musayeib ◽  
Mohamed F. Al-Ajmi ◽  
Paul Cos ◽  
Louis Maes
Keyword(s):  
Medicinal Plants ◽  
High Selectivity ◽  
Moderate Activity ◽  
Good Activity ◽  
Antiprotozoal Activity ◽  
Traditional Use ◽  
Active Constituents ◽  
Intracellular Amastigotes ◽  
Antitrypanosomal Activity

The antiplasmodial, antileishmanial, and antitrypanosomal activity of twenty-five medicinal plants distributed in Saudi Arabia and Yemen was evaluated. The plants were extracted with methanol and screenedin vitroagainst erythrocytic schizonts ofPlasmodium falciparum, intracellular amastigotes ofLeishmania infantumandTrypanosoma cruzi, and free trypomastigotes ofT. brucei. To assess selectivity, cytotoxicity was determined on MRC-5 cells. Criteria for activity were anIC50<10 μg/mL and high selectivity (SI). Seven plants showed interesting antiprotozoal activity in one or more models. Extracts ofCaralluma penicillataandAcalypha ciliatashowed fairly good activity againstP. falciparumwith IC50of 6.7 and 10.8 μg/mL and adequate selectivity (SI>9.6and>5.9). Interesting activity againstL. infantumwas obtained withVerbascum bottae(IC50of 3.2 μg/mL, SI 10.2) andSolanum glabratum(IC508.1 μg/mL, SI 3.4). The extracts ofC. penicillata, Leucas virgata, Loranthus regularis, andV. bottaeexhibited moderate activity againstT. brucei(IC508.5, 8.1, 8.3, and 2.3 μg/mL;SI>7.6, 7.7, 4.3, and>14.1). These results partly support the traditional use of some of the selected medicinal plants and warrant further investigations into the putative active constituents.

scholarly journals Molecular identification of Trypanosoma brucei brucei and in vitro anti-trypanosomal activity of different parts of methanolic extract of Senna occidentalis

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Zainab Aliyu Alhafiz ◽  
Mohammed Sani Abdulsalami ◽  
Mohammed Auwal Ibrahim ◽  
Timothy Bulus ◽  
Ahmed Babangida Suleiman
Keyword(s):  
Trypanosoma Brucei ◽  
Molecular Identification ◽  
Methanolic Extract ◽  
Trypanosoma Brucei Brucei ◽  
Different Parts

scholarly journals Synthesis of 1H-3-{4-[(3-Dimethylaminopropyl)aminomethyl]phenyl}-2-phenylindole and Evaluation of Its Antiprotozoal Activity

Molbank ◽  
10.3390/m1060 ◽  
2019 ◽  
Vol 2019 (2) ◽  
pp. M1060 ◽  
Author(s):  
Jean Guillon ◽  
Clotilde Boudot ◽  
Anita Cohen ◽  
Solène Savrimoutou ◽  
Sandra Rubio ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Leishmania Donovani ◽  
Structure Characterization ◽  
Antiprotozoal Activity ◽  
Protozoan Parasites ◽  
Trypanosoma Brucei Brucei ◽  
Antiparasitic Activity ◽  
Ic50 Values

1H-3-{4-[(3-Dimethylaminopropyl)aminomethyl]phenyl}-2-phenylindole was synthesized via a multi-step pathway starting from 2-iodoaniline. Structure characterization of this new indole compound was achieved by 1H-NMR, 13C-NMR and ESI-MS spectral analysis. The title compound was screened in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani and Trypanosoma brucei brucei). Biological results showed antiparasitic activity with IC50 values in the μM range.

Phytochemical analysis and salivary amylase inhibition activities of Carica papaya leaf and Garcinia mangostana pericarp extracts and partially purified fractions

2017 ◽  
Vol 6 (1) ◽  
pp. 34
Author(s):  
Michael Russelle Alvarez ◽  
Paolo Robert Bueno ◽  
Raymond Oliver Cruz ◽  
Richard Macapulay ◽  
Francis Jayson Vallesfin ◽  
...  
Keyword(s):  
Crude Extract ◽  
Carica Papaya ◽  
Uv Light ◽  
Digestive Enzyme ◽  
Phytochemical Analysis ◽  
Phytochemical Screening ◽  
Salivary Amylase ◽  
Garcinia Mangostana ◽  
Leaf Extracts

Plant-derived digestive enzyme inhibitors particularly those targeted to carbohydrate metabolism has been the focus of recent studies as natural supplements for weight control and diabetes. The present study explores the salivary amylase inhibition activity of Garcinia mangostana (Linn.) pericarp extracts and Carica papaya (Linn.) leaf extracts and fractions, as well as perform phytochemical screening and quantification, and thin layer – and high performance liquid chromatographic profiling. ­Results show that crude extracts and purified fractions were able to inhibit salivary amylase, with C. papaya fraction 1 being the most active at 30.89% inhibition. Phytochemical screening of all extracts tested ­positive for tannins, glycosides, phenolics, flavonoids and alkaloids. Quantification of phenolics showed that extracts contained high levels of phenolics, with C. papaya crude extract having the highest content with 219.0±12.7 mg GAE/g extract followed by G. mangostana crude extract with 247.1±18.0 mg GAE/g extract. Quantification of total flavonoids also showed C. papaya crude extract to contain the highest content with 55.12±0.679 mg QE/g extract. All extracts contained negligible alkaloid content, though. HPLC and TLC profiling showed several peaks and bands, when viewed in 210 nm and UV light, respectively. These results demonstrate in vitro the salivary amylase inhibitory activity of both plants and their potential as antidiabetic drug candidates; however, further studies need to be done, like isolation and structure elucidation of active components and toxicity assays. Keywords: Amylase inhibition, phytochemical quantification, Carica papaya, Garcinia mangostana

scholarly journals Unusual derivatives from Hypericum scabrum

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Sara Soroury ◽  
Mostafa Alilou ◽  
Thomas Gelbrich ◽  
Marzieh Tabefam ◽  
Ombeline Danton ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
2D Nmr ◽  
Moderate Activity ◽  
Trypanosoma Brucei Rhodesiense ◽  
L6 Cells ◽  
Aerial Parts ◽  
Hypericum Scabrum ◽  
New Compounds ◽  
Absolute Structure

AbstractThree new compounds (1–3) with unusual skeletons were isolated from the n-hexane extract of the air-dried aerial parts of Hypericum scabrum. Compound 1 represents the first example of an esterified polycyclic polyprenylated acylphloroglucinol that features a unique tricyclo-[4.3.1.11,4]-undecane skeleton. Compound 2 is a fairly simple MPAP, but with an unexpected cycloheptane ring decorated with prenyl substituents, and compound 3 has an unusual 5,5-spiroketal lactone core. Their structures were determined by extensive spectroscopic and spectrometric techniques (1D and 2D NMR, HRESI-TOFMS). Absolute configurations were established by ECD calculations, and the absolute structure of 2 was confirmed by a single crystal determination. Plausible biogenetic pathways of compounds 1–3 were also proposed. The in vitro antiprotozoal activity of the compounds against Trypanosoma brucei rhodesiense and Plasmodium falciparum and cytotoxicity against rat myoblast (L6) cells were determined. Compound 1 showed a moderate activity against T. brucei and P. falciparum, with IC50 values of 3.07 and 2.25 μM, respectively.

scholarly journals FRACTIONATION OF THE N-HEXANE EXTRACT OF GARCINIA BANCANA MIQ. (MANGGIS HUTAN) LEAVES AND ITS ANTIOXIDANT ACTIVITY BASED ON 1,1-DIPHENYL-2- PICRYLHYDRAZYL AND FERRIC REDUCING ANTIOXIDANT POWER ASSAYS

2018 ◽  
Vol 10 (1) ◽  
pp. 407
Author(s):  
Dewi Kumala Putri ◽  
Berna Elya ◽  
Nuraini Puspitasari
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Hexane Extract ◽  
Phytochemical Screening ◽  
Active Fraction ◽  
Leaf Extracts ◽  
Antioxidant Power ◽  
Dpph Method ◽  
Ferric Reducing Antioxidant Power

Objective: To assess the antioxidant activity from another part of the plant, in this study, leaf extracts in n-hexane were fractionated.Methods: Ten fractions were obtained and tested in vitro for antioxidant activity using two methods, 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferricreducing antioxidant power (FRAP), to identify the most active fraction.Results: The IC50 of the most active fraction was 36.24 μg/mL using the DPPH method, and the EC50 was 39.54 μg/mL using the FRAP method. Themost active fraction was also shown to contain terpenoids.Conclusion: The most active fraction of an n-hexane extract of the leaves of Gacinia bancana Miq., which was tested by both DPPH and FRAP methodshad antioxidant activities with IC50 and EC50 values of 36.2482 μg/mL and 39.5442 μg/mL, respectively. Phytochemical screening showed that activefraction contains terpenoids.

scholarly journals Cross-Resistance to Nitro Drugs and Implications for Treatment of Human African Trypanosomiasis

2010 ◽  
Vol 54 (7) ◽  
pp. 2893-2900 ◽  
Author(s):  
Antoaneta Y. Sokolova ◽  
Susan Wyllie ◽  
Stephen Patterson ◽  
Sandra L. Oza ◽  
Kevin D. Read ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
Parent Drug ◽  
Cross Resistance ◽  
Pharmacokinetic Studies ◽  
African Trypanosomiasis ◽  
Trypanosoma Brucei Brucei ◽  
Resistant Lines

ABSTRACT The success of nifurtimox-eflornithine combination therapy (NECT) for the treatment of human African trypanosomiasis (HAT) has renewed interest in the potential of nitro drugs as chemotherapeutics. In order to study the implications of the more widespread use of nitro drugs against these parasites, we examined the in vivo and in vitro resistance potentials of nifurtimox and fexinidazole and its metabolites. Following selection in vitro by exposure to increasing concentrations of nifurtimox, Trypanosoma brucei brucei nifurtimox-resistant clones designated NfxR1 and NfxR2 were generated. Both cell lines were found to be 8-fold less sensitive to nifurtimox than parental cells and demonstrated cross-resistance to a number of other nitro drugs, most notably the clinical trial candidate fexinidazole (∼27-fold more resistant than parental cells). Studies of mice confirmed that the generation of nifurtimox resistance in these parasites did not compromise virulence, and NfxR1 remained resistant to both nifurtimox and fexinidazole in vivo. In the case of fexinidazole, drug metabolism and pharmacokinetic studies indicate that the parent drug is rapidly metabolized to the sulfoxide and sulfone form of this compound. These metabolites retained trypanocidal activity but were less effective in nifurtimox-resistant lines. Significantly, trypanosomes selected for resistance to fexinidazole were 10-fold more resistant to nifurtimox than parental cells. This reciprocal cross-resistance has important implications for the therapeutic use of nifurtimox in a clinical setting and highlights a potential danger in the use of fexinidazole as a monotherapy.

Sign in / Sign up

Export Citation Format

Share Document