scholarly journals Aktivitas Antimalaria Daun Erythrina variegata

2018 ◽  
Vol 10 (1) ◽  
pp. 36
Author(s):  
Tati Herlina ◽  
Unang Supratman ◽  
Anas Subarnas ◽  
Supriyatna Sutardjo ◽  
Noor Rain Abdullah
Keyword(s):  
Plasmodium Falciparum ◽  
Lactate Dehydrogenase ◽  
Column Chromatography ◽  
Active Compound ◽  
Resistant Strain ◽  
Methanol Extract ◽  
Antimalarial Activity ◽  
Antimalarial Agents ◽  
Erythrina Variegata

The leaves of Erythrina variegata (Leguminosae) used tradisional plant of an antimalarial. In the course of our continuing search for novel an antimalarial compound from Erythrina plants, the methanol extract of the leaves ofE. variegata showed significant antimalarial activity in vitro toward Plasmodium falciparum in vitro using the lactate dehydrogenase (LDH) method. The methanol extract of the leaves of E. variegata showed against bothstrains of parasite with IC50of 6.8 ?g/ml against K1 and > 60 ?g/ml against 3D7, respectively. The methanol extract of the leaves of E. variegata was separated by using bioassay-guide fractionation. The n-buthanol fraction yieldedthe most activity, exhibiting equipotency against both strains of parasite with IC50of 5.1 ?g/ml against K1 and 13.5 ?g/ml against 3D7, respectively. Furthermore, by using the antimalarial activity to follow separation, the n-buthanol fraction was separated by combination of column chromatography to yield an active compound. The active compound showed antimalarial activity against both strains of parasite used with IC50 of 4.3 ?g/ml against K1 and 23.5 ?g/ml against 3D7, respectively. Its inhibition of the resistant strain (K1) was also much better compared to its inhibition of the sensitive strain (3D7), indicated that the leaves of E. variegata to be potential as antimalarial agents, but its lower potency compared to artemisinin and chloroquin.

scholarly journals ANTI-MALARIAL COMPOUND FROM THE STEM BARK OF Erythrina variegata

2010 ◽  
Vol 9 (2) ◽  
pp. 308-311 ◽  
Author(s):  
Tati Herlina ◽  
Unang Supratman ◽  
M. S. Soedjanaatmadja ◽  
Anas Subarnas ◽  
Supriyatna Sutardjo ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Ethyl Acetate ◽  
Active Compound ◽  
Chemical Structure ◽  
Methanol Extract ◽  
Ethyl Acetate Fraction ◽  
Stem Bark ◽  
Erythrina Variegata ◽  
Ldh Assay

During the course of our continuing search for novel anti-malarial compounds from Indonesian plants, the methanol extract of the bark of E. variegata showed significant anti-malarial activity toward Plasmodium falciparum in vitro using the lactate dehydrogenase (LDH) assay. The methanol extract of the bark of E. variegata  was separated by using bioassay-guide fractionation. The ethyl acetate fraction showed the most activity, exhibiting equipotency against both strains of parasite with IC50 of 23.8 µg/mL against 3D7 and 9.3 µg/mL against K1. Furthermore, by using the anti-malarial activity to follow separation, the ethyl acetate fraction was separated by combination of column chromatography to yield an active compound. The chemical structure of active compound was determined on the basis of spectroscopic evidences and comparison with those previously reported and identified as an isoflavonoid, warangalone. The warangalone showed anti-malarial activity against both strains of parasite used with IC50 of 4.8 µg/mL against 3D7 and 3.7 µg/mL against K1.   Keywords: Antimalarial, Erythrina variegata, warangalone

scholarly journals Synthesis, antimalarial activity evaluation and molecular docking studies of some novel dispiro-1,2,4,5-tetraoxanes

2015 ◽  
Vol 10 (4) ◽  
pp. 917 ◽  
Author(s):  
Mukesh Kumar Kumawat ◽  
Dipak Chetia
Keyword(s):  
Plasmodium Falciparum ◽  
Molecular Docking ◽  
Resistant Strain ◽  
Antimalarial Activity ◽  
Binding Pocket ◽  
Docking Studies ◽  
Spectroscopic Techniques ◽  
Molecular Docking Studies ◽  
Activity Screening

<p class="Abstract">Seven novel dispiro-1,2,4,5-tetraoxane derivatives were synthesized and characterized by a number of analytical and spectroscopic techniques. The molecules were subsequently screened for in vitro antimalarial activity against chloroquine resistant strain of <em>Plasmodium falciparum</em> (RKL-9). At antimalarial activity screening, two compounds, namely 5d (MIC = 15.6 µg/mL or 64.5 µM) and 5f (MIC = 15.6 µg/mL or 54.6 µM) were found to be about 1.5 times more potent against chloroquine resistant strain-RKL-9 compared to chloroquine (MIC = 25.0 µg/mL or 78.3 µM). Molecular docking studies of potent ligands were also performed in cysteine protease binding pocket residues of falcipain-2 as a target protein.</p><p> </p>

scholarly journals A Novel Series of [1,2,4]Triazolo[4,3-a]Pyridine Sulfonamides as Potential Antimalarial Agents: In Silico Studies, Synthesis and In Vitro Evaluation

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4485
Author(s):  
Veronika R. Karpina ◽  
Svitlana S. Kovalenko ◽  
Sergiy M. Kovalenko ◽  
Oleksandr G. Drushlyak ◽  
Natalya D. Bunyatyan ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Molecular Docking ◽  
Virtual Screening ◽  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Virtual Library ◽  
Antimalarial Agents ◽  
Starting Point ◽  
In Silico Studies

For the development of new and potent antimalarial drugs, we designed the virtual library with three points of randomization of novel [1,2,4]triazolo[4,3-a]pyridines bearing a sulfonamide fragment. The library of 1561 compounds has been investigated by both virtual screening and molecular docking methods using falcipain-2 as a target enzyme. 25 chosen hits were synthesized and evaluated for their antimalarial activity in vitro against Plasmodium falciparum. 3-Ethyl-N-(3-fluorobenzyl)-N-(4-methoxyphenyl)-[1,2,4]triazolo[4,3-a]pyridine-6-sulfonamide and 2-(3-chlorobenzyl)-8-(piperidin-1-ylsulfonyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one showed in vitro good antimalarial activity with inhibitory concentration IC50 = 2.24 and 4.98 μM, respectively. This new series of compounds may serve as a starting point for future antimalarial drug discovery programs.

scholarly journals Aktivitas Penghambatan Ekstrak Etanol Daun Cassia Spectabilis Terhadap Pertumbuhan Plasmodium falciparum dan Plasmodium berghei

2017 ◽  
Vol 3 (1) ◽  
pp. 17 ◽  
Author(s):  
Wiwied Ekasari ◽  
Nindya Tresiana ◽  
Suciati Iryani ◽  
Tutik Sri Wahyuni ◽  
Heny Arwaty
Keyword(s):  
Plasmodium Falciparum ◽  
Methanol Extract ◽  
Antimalarial Activity ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
In Vivo Test ◽  
Ic50 Value ◽  
Cassia Spectabilis

Background: Antimalarial screening against nine species of the genus Cassia showed that the methanol extract of leaves Cassia spectabilis have the highest activity. Since it will be used as a traditional medicine, hence it is needed further studies of antimalarial activity of these plants by choosing a safer solvent, namely ethanol. Objective: In vitro anti-malarial activity against Plasmodium falciparum was conducted using the method of Trager and Jensen. Methods: The serial solution tested were: 100, 10, 1,  0.1 and 0.01 µg/ mL, while the in vivo test was performed based on Peter’s test (The days suppressive test) that using P. berghei (strain ANKA) infected mice. Results: The results showed that ethanolic extract of C. spectabilis leaves has inhibitory activity against P. falciparum with IC50 value of 12.52 µg/ mL and against P. berghei with ED50 value of 131.5 mg/kg body weight. Conclusions: A further study to see the potential of ethanol extract from C. Spectabilis leaves as anti-malaria is warranted. 

scholarly journals In Vitro Activity of Lumefantrine (Benflumetol) against Clinical Isolates of Plasmodium falciparum in Yaoundé, Cameroon

1998 ◽  
Vol 42 (9) ◽  
pp. 2347-2351 ◽  
Author(s):  
Leonardo K. Basco ◽  
Jean Bickii ◽  
Pascal Ringwald
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Geometric Mean ◽  
Vitro Activity ◽  
Clinical Isolates ◽  
Cross Resistance ◽  
In Vitro Activity ◽  
Antimalarial Agents ◽  
Fluorene Derivative

ABSTRACT The in vitro antimalarial activity of the new Chinese synthetic drug, lumefantrine, also known as benflumetol (a fluorene derivative belonging to the aminoalcohol class), was determined by an isotopic microtest against 61 fresh clinical isolates of Plasmodium falciparum and compared with that of other established antimalarial agents. The geometric mean 50% inhibitory concentration of lumefantrine was 11.9 nmol/liter (95% confidence intervals, 10.4 to 13.6 nmol/liter; range, 3.3 to 25.6 nmol/liter). The in vitro activities of lumefantrine against the chloroquine-sensitive and the chloroquine-resistant isolates did not differ (P > 0.05). There was a significant positive correlation of responses between lumefantrine and two other aminoalcohols studied, mefloquine (r = 0.688) and halofantrine (r = 0.677), and between lumefantrine and artesunate (r = 0.420), suggesting a potential for in vitro cross-resistance. Our data suggest high in vitro activity of lumefantrine, comparable to that of mefloquine, and are in agreement with the promising results of preliminary clinical trials.

scholarly journals Chemical and Bioactivity Evaluation of the Bark of Neonauclea purpurea

2012 ◽  
Vol 7 (2) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Netiya Karaket ◽  
Kanyaratt Supaibulwatana ◽  
Supatsara Ounsuk ◽  
Valérie Bultel-Poncé ◽  
Van Cuong Pham ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Traditional Medicine ◽  
Resistant Strain ◽  
Antimalarial Activity ◽  
Indole Alkaloids ◽  
Vero Cells ◽  
Stem Bark ◽  
Meoh Extract ◽  
Bioassay Guided Fractionation

Bioassay-guided fractionation of the MeOH extract from the stem bark of Neonauclea purpurea used in traditional medicine, resulted in the isolation of 2 indole alkaloids, cadambine (1) and α-dihydrocadambine (2), as well as a quinolic compound, 2,6-dimethoxy-1,4-benzoquinone (3). Antimalarial activity evaluation showed that compounds 2 and 3 exhibited mild in vitro antimalarial activity against Plasmodium falciparum, the chloroquine-resistant strain K1 with IC50 values of 6.6 and 11.3 μM, respectively. Compounds 1 and 2 showed no cytotoxicity to monkey (Vero) cells, but compound 3 showed weak cytotoxicity with an IC50 value of 1.19 μM.

scholarly journals Optimization of Xanthones for Antimalarial Activity: the 3,6-Bis-ω-Diethylaminoalkoxyxanthone Series

2002 ◽  
Vol 46 (1) ◽  
pp. 144-150 ◽  
Author(s):  
Jane Xu Kelly ◽  
Rolf Winter ◽  
David H. Peyton ◽  
David J. Hinrichs ◽  
Michael Riscoe
Keyword(s):  
Plasmodium Falciparum ◽  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Multidrug Resistant ◽  
Food Vacuole ◽  
Ionic Interactions ◽  
Side Chains ◽  
Antimalarial Agents ◽  
Unique Manner

ABSTRACT Hydroxyxanthones have been identified as novel antimalarial agents. The compounds are believed to exert their activity by complexation to heme and inhibition of hemozoin formation. Modification of the xanthone structure was pursued to improve their antimalarial activity. Attachment of R-groups bearing protonatable nitrogen atoms was conducted to enhance heme affinity through ionic interactions with the propionate side chains of the metalloporphyrin and to facilitate drug accumulation in the parasite food vacuole. A series of 3,6-bis-ω-diethylaminoalkoxyxanthones with side chains ranging from 2 to 8 carbon atoms were prepared and evaluated. Measurement of heme affinity for each of the derivatives revealed a strong correlation (R 2 = 0.97) between affinity and antimalarial potency. The two most active compounds in the series contained 5- and 6-carbon side chains and exhibited low nanomolar 50% inhibitory concentration (IC50) values against strains of chloroquine-susceptible and multidrug-resistant Plasmodium falciparum in vitro. Both of these xanthones exhibit stronger heme affinity (8.26 × 105 and 9.02 × 105 M−1, respectively) than either chloroquine or quinine under similar conditions and appear to complex heme in a unique manner.

scholarly journals Aktivitas Penghambatan Ekstrak Etanol Daun Cassia Spectabilis Terhadap Pertumbuhan Plasmodium falciparum dan Plasmodium berghei

2017 ◽  
Vol 3 (1) ◽  
pp. 17
Author(s):  
Wiwied Ekasari ◽  
Nindya Tresiana ◽  
Suciati Iryani ◽  
Tutik Sri Wahyuni ◽  
Heny Arwaty
Keyword(s):  
Plasmodium Falciparum ◽  
Methanol Extract ◽  
Antimalarial Activity ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
In Vivo Test ◽  
Ic50 Value ◽  
Cassia Spectabilis

Background: Antimalarial screening against nine species of the genus Cassia showed that the methanol extract of leaves Cassia spectabilis have the highest activity. Since it will be used as a traditional medicine, hence it is needed further studies of antimalarial activity of these plants by choosing a safer solvent, namely ethanol. Objective: In vitro anti-malarial activity against Plasmodium falciparum was conducted using the method of Trager and Jensen. Methods: The serial solution tested were: 100, 10, 1,  0.1 and 0.01 µg/ mL, while the in vivo test was performed based on Peter’s test (The days suppressive test) that using P. berghei (strain ANKA) infected mice. Results: The results showed that ethanolic extract of C. spectabilis leaves has inhibitory activity against P. falciparum with IC50 value of 12.52 µg/ mL and against P. berghei with ED50 value of 131.5 mg/kg body weight. Conclusions: A further study to see the potential of ethanol extract from C. Spectabilis leaves as anti-malaria is warranted. 

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