scholarly journals Prenylated Isoflavanones from the Stem Bark of Erythrina poeppigiana (Leguminosae) and its Antimalarial Properties

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Tati Herlina ◽  
Anderson Arnold Aloanis ◽  
Dikdik Kurnia ◽  
Desi Harneti ◽  
Rani Maharani ◽  
...  
Keyword(s):  
Methanol Extract ◽  
Ethyl Acetate Extract ◽  
Antimalarial Activity ◽  
Stem Bark ◽  
In Vitro Bioassay ◽  
Erythrina Poeppigiana ◽  
Antimalarial Agents ◽  
Bioassay Guided Fractionation ◽  
Promising Source

During the course of our continuous search for novel antimalarial compounds derived from the Indonesian Erythrina plants, the methanol extract of the stem bark of Erythrina poeppigiana demonstrated significant antimalarial activity against Plasmodium falciparum parasites, in vitro. Bioassay-guided fractionation of the ethyl acetate extract resulted in the isolation of three known platyisoflavanone (1), erypogein D (2), and sophoraisoflavanone A (3). Compounds 1–3 showed strong antimalarial activity against 3D7 strain of P. falciparum with IC50 values of 0.52, 0.36, and 3.65μM, respectively. This result indicates that stem bark of E. poeppigiana is a promising source of antimalarial agents, and merits further investigation.

scholarly journals Antimalarial Activity ofCroton macrostachyusStem Bark Extracts againstPlasmodium berghei In Vivo

2018 ◽  
Vol 2018 ◽  
pp. 1-6 ◽  
Author(s):  
Jackie K. Obey ◽  
Moses M. Ngeiywa ◽  
Paul Kiprono ◽  
Sabah Omar ◽  
Atte von Wright ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Methanol Extract ◽  
Ethyl Acetate Extract ◽  
Antimalarial Activity ◽  
Stem Bark ◽  
Significant Suppression ◽  
Innovative Drug ◽  
Croton Macrostachyus ◽  
Different Doses

There is an increasing need for innovative drug and prophylaxis discovery against malaria. The aim of the present study was to testin vivoantiplasmodial activity ofCroton macrostachyusH. (Euphorbiaceae) stem bark extracts from Kenyan folkloric medicine. Inbred Balb/c mice were inoculated with erythrocytes parasitized withPlasmodium berghei(ANKA). Different doses (500, 250, and 100 mg/kg) ofC. macrostachyusethyl acetate, methanol, aqueous, and isobutanol extracts were administrated either after inoculation (Peters’ 4-day suppressive test) or before inoculation (chemoprotective test) of the parasitized erythrocytes. All the extracts showed significant suppression of parasitemia compared to control (p<0.001): for the ethyl acetate extract in the range of 58–82%, for the methanol extract in the range of 27–68%, for the aqueous extract in the range of 24–72%, and for the isobutanol extract in the range of 61–80%. Chemoprotective effect was significant (p<0.001) and the suppression caused by the ethyl acetate extract was between 74 and 100%, by the methanol extract between 57 and 83%, and by the isobutanol extract between 86–92%. The study showed that it is possible to inhibit the growth of the parasites by various stem bark extracts ofC. macrostachyusin Balb/c mice supporting the folkloric use of the plant against malaria.

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 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 Potent In Vitro Antimalarial Activity of Metacycloprodigiosin Isolated from Streptomycesspectabilis BCC 4785

2002 ◽  
Vol 46 (4) ◽  
pp. 1112-1113 ◽  
Author(s):  
Masahiko Isaka ◽  
Amonlaya Jaturapat ◽  
Jarin Kramyu ◽  
Morakot Tanticharoen ◽  
Yodhathai Thebtaranonth
Keyword(s):  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Fermentation Broth ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Antimalarial Agents ◽  
Bioassay Guided Fractionation

ABSTRACT Bioassay-guided fractionation of the extract from the fermentation broth of Streptomyces spectabilis BCC 4785 led to the isolation of three principle antimalarial agents, metacycloprodigiosin, bafilomycin A1, and spectinabilin. Metacycloprodigiosin exhibited potent in vitro activity against Plasmodium falciparum K1, with a 50% inhibitory concentration of 0.0050 ± 0.0010 μg/ml, while its cytotoxicity was much weaker.

Discovery of 3-Cinnamamido-N-Substituted Benzamides as Potential Antimalarial Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Haicheng Liu ◽  
Yushi Futamura ◽  
Honghai Wu ◽  
Aki Ishiyama ◽  
Taotao Zhang ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Antimalarial Activity ◽  
In Vitro Assays ◽  
Compound Library ◽  
Antimalarial Agents ◽  
Phenotypic Screen ◽  
Ic50 Values ◽  
Substituted Benzamides

Background: Malaria is one of the most devastating parasitic diseases, yet the discovery of antimalarial agents remains profoundly challenging. Very few new antimalarials have been developed in the past 50 years, while the emergence of drug-resistance continues to appear. Objective: This study focuses on the discovery, design, synthesis, and antimalarial evaluation of 3-cinnamamido-N-substituted benzamides. Method: In this study, a screening of our compound library was carried out against the multidrug-sensitive Plasmodium falciparum 3D7 strain. Derivatives of the hit were designed, synthesized and tested against P. falciparum 3D7 and the in vivo antimalarial activity of the most active compounds was evaluated using the method of Peters’ 4-day suppressive test. Results: The retrieved hit compound 1 containing a 3-cinnamamido-N-substituted benzamide skeleton showed moderate antimalarial activity (IC50 = 1.20 µM) for the first time. A series of derivatives were then synthesized through a simple four-step workflow, and half of them exhibited slightly better antimalarial effect than the precursor 1 during the subsequent in vitro assays. Additionally, compounds 11, 23, 30 and 31 displayed potent activity with IC50 values of approximately 0.1 µM, and weak cytotoxicity against mammalian cells. However, in vivo antimalarial activity is not effective which might be ascribed to the poor solubility of these compounds. Conclusion: In this study, phenotypic screen of our compound library resulted in the first report of 3-cinnamamide framework with antimalarial activity and 40 derivatives were then designed and synthesized. Subsequent structure-activity studies showed that compounds 11, 23, 30 and 31 exhibited the most potent and selective activity against P. falciparum 3D7 strain with IC50 values around 0.1 µM. Our work herein sets another example of phenotypic screen-based drug discovery, leading to potentially promising candidates of novel antimalarial agents once given further optimization.

scholarly journals SYNTHESIS AND ANTIMALARIAL ACTIVITY OF SOME NEW 3-PHENYL-2-THIOXOTHIAZOLIDIN-4-ONE DERIVATIVES

2017 ◽  
Vol 9 (3) ◽  
pp. 58
Author(s):  
Mehul Zaveri ◽  
Neha Kawathekar
Keyword(s):  
Antimalarial Activity ◽  
Research Work ◽  
Aromatic Aldehydes ◽  
Maximum Activity ◽  
Spectroscopic Techniques ◽  
Activity Data ◽  
Antimalarial Agents ◽  
Ic50 Values ◽  
Current Therapies

Objective: Current therapies to treat P. falciparum malaria are heavily reliant on artemisinin-based combinations. However, resistance to artemisinin has recently been identified, and resistance to key artemisinin partner drugs is already widespread. Therefore, there is an urgent need for new antimalarial drugs with improved attributes over older therapies. The objective of this research work is to synthesize new antimalarial agents more effective against clinically relevant malarial strains.Methods: In present work, a series of ten 3-phenyl-2-thioxothiazolidin-4-one (MF1-MF10) derivatives, were synthesized by Knoevenagel condensation of N-phenyl rhodanine (I1) with substituted aromatic or hetro aromatic aldehydes using microwave irradiation. N-phenyl rhodanine (I1) was synthesized by a conventional reaction involving methyl-2-mercaptoacetate (1) and phenyl Isothiocyanates in presence of triethylamine. All the synthesized compounds were characterized by various spectroscopic techniques and evaluated for in-vitro antimalarial activity by microdilution technique against resistance strains of Plasmodium falciparum.Results: The antimalarial activity data showed that six compounds (MF1, MF3, MF4, MF5, MF7 and MF8) exhibited IC50 values ranging from 1.0-1.30 µg/ml, three compounds (MF2, MF6 and MF10) displayed IC50 values in the range of 0.9-1.0 µg/ml. Compound MF9 showed most significant result with maximum activity (IC50 = 0.85µg/ml).Conclusion: The antimalarial activity results revealed that compound MF9 possess potent activity and could be identified as a promising lead for further investigation.

scholarly journals Anti-fungal activities of constituents from Uvaria scheffleri and Artabotrys brachypetalus

2006 ◽  
Vol 51 (1) ◽  
pp. 79-86 ◽  
Author(s):  
A.C. Odebode ◽  
S.A. Jonker ◽  
C.C. Joseph ◽  
S.W. Wachira
Keyword(s):  
Fusarium Solani ◽  
Radial Growth ◽  
Fungal Pathogens ◽  
Dry Weight ◽  
Stem Bark ◽  
Inhibitory Effect ◽  
In Vitro Bioassay ◽  
Botryodiplodia Theobromae ◽  
Anti Fungal

The anti-fungal activity of schefflone, a mixture of dimmer, 3,5 dimethoxy carvacrol and annonaceous acetogenin, extracted from stem-bark and root of Uvaria scheffleri and Artabotrys bruchypetalus against Fusarium solani, Botryodiplodia theobromae, Asperillus niger and Aspergillus flavus was determined. An in-vitro bioassay showed that the minimum inhibitory effect of the compounds to the fungal pathogens occurred at 200 ppm in both radial growth and mycelia dry weight measurements. Acetogenin from A brachypetalus had a very strong anti-fungal effect on all the test fungi. The effects of the compounds were more pronounced on F solani than on the other. The bioassay methods also play a significant role in the sensitivity of the samples on the pathogens. .

scholarly journals Antiplasmodial and Cytotoxic Cytochalasins from an Endophytic Fungus, Nemania sp. UM10M, Isolated from a Diseased Torreya taxifolia Leaf

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 777 ◽  
Author(s):  
Mallika Kumarihamy ◽  
Daneel Ferreira ◽  
Edward Croom ◽  
Rajnish Sahu ◽  
Babu Tekwani ◽  
...  
Keyword(s):  
Mouse Model ◽  
Solid Tumor ◽  
Endophytic Fungus ◽  
Antimalarial Activity ◽  
Vero Cells ◽  
Antiplasmodial Activity ◽  
Etoac Extract ◽  
Bioassay Guided Fractionation

Bioassay-guided fractionation of an EtOAc extract of the broth of the endophytic fungus Nemania sp. UM10M (Xylariaceae) isolated from a diseased Torreya taxifolia leaf afforded three known cytochalasins, 19,20-epoxycytochalasins C (1) and D (2), and 18-deoxy-19,20-epoxy-cytochalasin C (3). All three compounds showed potent in vitro antiplasmodial activity and phytotoxicity with no cytotoxicity to Vero cells. These compounds exhibited moderate to weak cytotoxicity to some of the cell lines of a panel of solid tumor (SK-MEL, KB, BT-549, and SK-OV-3) and kidney epithelial cells (LLC-PK11). Evaluation of in vivo antimalarial activity of 19,20-epoxycytochalasin C (1) in a mouse model at 100 mg/kg dose showed that this compound had weak suppressive antiplasmodial activity and was toxic to animals.

scholarly journals Antimalarial Activity of Ethyl Acetate Extract and Fraction of Bidens pilosa against Plasmodium berghei (ANKA)

2020 ◽  
Vol 2020 ◽  
pp. 1-8 ◽  
Author(s):  
Noumedem Anangmo Christelle Nadia ◽  
Yamssi Cédric ◽  
Simeni Njonnou Sylvain Raoul ◽  
Ngongang Ouankou Christian ◽  
Mounvera Abdel Azizi ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Crude Extract ◽  
Plasmodium Berghei ◽  
Ethyl Acetate Extract ◽  
Antimalarial Activity ◽  
Hematological Parameters ◽  
Control Group ◽  
Bidens Pilosa

Background. Malaria is one of the most critical diseases causing about 219 million cases worldwide in developing countries. The spread and development of resistance against chemical antimalarial drugs is one of the major problems associated with malaria control. The present study was to investigate the antimalarial efficacy of ethyl acetate extract and one fraction of Bidens pilosa in vivo in order to support the usage of this plant by traditional healers to treat malaria. Methods. The extracts were prepared by maceration of B. pilosa leaf powder in ethyl acetate. The liquid filtrate of the extract and the best in vitro antiplasmodial fraction using HPLC were concentrated and evaporated using a rotavapor under vacuum to dryness. The antimalarial activity of B. pilosa plant products were evaluated in vivo against Plasmodium berghei infected mice according to the Peter and Rane test. The antimalarial efficacy of the a selected crude extract (ethyl acetate extract) was evaluated at 125, 250, and 500 mg/kg, while a selected fraction from ethyl acetate extract (fraction 12) was evaluated at 62.5 and 125 mg/kg. Blood from experimental animals was collected to assess hematological parameters. Results. The crude extract of ethyl acetate and fraction 12 demonstrated 100% in vivo parasite suppressive activity at doses of 500 mg/kg and 125 mg/kg, respectively, for the crude extract and fraction 12. The mice treated with 250 and 500 mg/kg had their parasitemia (intraerythrocytic phase of P. Berghei) drop considerably, disappearing by the 8th day in mice receiving 500 mg/kg. The ethyl acetate extract of B. pilosa, fraction 12 showed an even higher antiplasmodial activity. By the 5th day of the experiment, the treatment led to a modification of hematological parameters in mice. The chloroquine (5 mg/kg), fraction 12 (125 mg/kg), and the crude extract (500 mg/kg) groups all survived the 30 days of the experiment, while the negative control group registered 100% of the deaths. Conclusion. This study scientifically supports the use of Bidens pilosa leaves in the traditional treatment of malaria. However, the mode of action and in vivo toxicity of the plant still need to be assessed.

scholarly journals Synthesis and Antimalarial Activities of Cyclen 4-Aminoquinoline Analogs

2009 ◽  
Vol 53 (4) ◽  
pp. 1320-1324 ◽  
Author(s):  
M. O. Faruk Khan ◽  
Mark S. Levi ◽  
Babu L. Tekwani ◽  
Shabana I. Khan ◽  
Eiichi Kimura ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
High Selectivity ◽  
Antimalarial Activity ◽  
New Class ◽  
Antimalarial Agents ◽  
Sensitive Clone ◽  
Resistant Strains ◽  
Incorporation Assay

ABSTRACT In an attempt to augment the efficacy of 7-chloro 4-aminoquinoline analogs and also to overcome resistance to antimalarial agents, we synthesized three cyclen (1,4,7,10-tetraazacyclododecane) analogs of chloroquine [a bisquinoline derivative, 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline HBr, and a 7-chloro-4-(1,4,7,10-tetraaza-cyclododec-1-yl)-quinoline-Zn2+ complex]. The bisquinoline displays the most potent in vitro and in vivo antimalarial activities. It displays 50% inhibitory concentrations (IC50s) of 7.5 nM against the D6 (chloroquine-sensitive) clone of Plasmodium falciparum and 19.2 nM against the W2 (chloroquine-resistant) clone, which are comparable to those of artemisinin (10.6 and 5.0 nM, respectively) and lower than those of chloroquine (10.7 and 87.2 nM, respectively), without any evidence of cytotoxicity to mammalian cells, indicating a high selectivity index (>1,333 against D6 clone and >521 against W2 clone). Potent antimalarial activities of the bisquinoline against chloroquine- and mefloquine-resistant strains of P. falciparum were also confirmed by in vitro [3H]hypoxanthine incorporation assay. The in vivo antimalarial activity of the bisquinoline, as determined in P. berghei-infected mice, is comparable to that of chloroquine (50% effective dose, ≤1.1 mg/kg when given orally); no apparent toxicity has been observed up to the highest dose tested (3 × 30 mg/kg). The bisquinoline inhibits in vitro hemozoin (β-hematin) formation with an IC50 of 1.1 μM, which is about 10-fold more potent than chloroquine (IC50 9.5 μM). Overall, this article describes the discovery of a new class of cyclen 4-aminoquinoline analogs as potent antimalarial drugs.

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