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

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

JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA ◽

10.20473/jfiki.v3i12016.17-21 ◽

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

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Antimalaria Activity of Cassia spectabilis DC Leaf and Its Inhibition Effect in Heme Detoxification

10.21203/rs.2.22061/v1 ◽

2020 ◽

Author(s):

Wiwied - Ekasari ◽

Dewi Resty Basuki ◽

Heny - Arwati ◽

Tutik Sri Wahy

Keyword(s):

Antimalarial Activity ◽

Ethanol Extract ◽

Ic50 Value ◽

Cassia Spectabilis ◽

In Vivo Testing ◽

Chloroquine Diphosphate ◽

Better Than

Abstract Background In previous studies, Cassia spectabilis DC leaf has shown a good antimalarial activity. Therefore, this study is a follow-up study of leaf activity and mechanism of C. spectabilis DC as an antimalarial. Methods In vitro antimalarial activity testing using P. falciparum which was done with bioassay guide isolation in order to obtain the active compound. In vivo testing towards infected P. berghei mice was conducted to determine the effects of antimalarial prophylaxis and antimalarial activity in combination with artesunate. Whereas, heme detoxification inhibition testing as one of the antimalarial mechanisms was carried out using the Basilico method. Results The results showed that active antimalarial isolate obtained from C. spectabilis DC leaf had a structural pattern that was identical to (-)-7-hydroxyspectaline. Prophylactic test on infected P. berghei mice obtained the highest dose of inhibition percentage of 90% ethanol extract of C. spectabilis DC leaf was 68.61% while positive (doxycycline) control at 100 mg kg-1 was 73.54%. In antimalarial testing in combination with artesunate, it was found that administering 150 mg kg-1 (three times a day) of C. spectabilis DC (D0 − D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate with 99.18% and 92.88% inhibition percentage. For the inhibitory activity of heme detoxification from ethanol extract 90%, C. spectabilis DC leaf had IC50 value of 0.375 mg mL-1 which was better than chloroquine diphosphate. Conclusion These results showed that C. spectabilis DC leaves possesses potent antimalarial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.

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Various Parts of Helianthus annuus Plants as New Sources of Antimalarial Drugs

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2019/7390385 ◽

2019 ◽

Vol 2019 ◽

pp. 1-7

Author(s):

Wiwied Ekasari ◽

Dwi Widya Pratiwi ◽

Zelmira Amanda ◽

Suciati ◽

Aty Widyawaruyanti ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Helianthus Annuus ◽

Antimalarial Activity ◽

Ethanol Extract ◽

The Other ◽

Antimalarial Agent ◽

A Value ◽

Ethanol Extracts

Background. Each part of H. annuus plants is traditionally used as medicinal remedies for several diseases, including malaria. Antimalarial activity of the leaf and the seed has already been observed; however, there is no report about antimalarial activity of the other parts of H. annuus plants. In this study, we assess in vitro and in vivo antimalarial activity of each part of the plants and its mechanism as antimalarial agent against inhibition of heme detoxification. Objective. To investigate the antimalarial activity of various parts of H. annuus. Methods. Various parts of the H. annuus plant were tested for in vitro antimalarial activity against Plasmodium falciparum 3D7 strain (chloroquine-sensitive), in vivo antimalarial activity against P. berghei using Peters’ 4-day suppressive test in BALB/c mice, curative and prophylaxis assay, and inhibition of heme detoxification by evaluating β-hematin level. Results. Ethanol extract of the roots showed the highest antimalarial activity, followed by ethanol extract of leaves, with IC50 values of 2.3 ± 1.4 and 4.3 ± 2.2 μg/mL, respectively and the percentage inhibition of P. berghei of 63.6 ± 8.0 and 59.3 ± 13.2 at a dose of 100 mg/kg, respectively. Ethanol extract of roots produced an ED50 value of 10.6 ± 0.2 mg/kg in the curative test and showed an inhibition of 79.2% at a dose of 400 mg/kg in the prophylactic assay. In inhibition of heme detoxification assay, root and leaf ethanol extracts yielded a lower IC50 value than positive (chloroquine) control with a value of 0.4 ± 0.0 and 0.5 ± 0.0 mg/mL, respectively. Conclusion. There were promising results of the ethanol extracts of root of H. annuus as a new source for the development of a new plant-based antimalarial agent.

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Antiplasmodial activity of Ethanolic extract of Cassia spectabilis DC leaf and its inhibition effect in Heme detoxification

BMC Complementary Medicine and Therapies ◽

10.1186/s12906-021-03239-9 ◽

2021 ◽

Vol 21 (1) ◽

Author(s):

Wiwied Ekasari ◽

Dewi Resty Basuki ◽

Heny Arwati ◽

Tutik Sri Wahyuni

Keyword(s):

Ethanolic Extract ◽

Positive Control ◽

Antiplasmodial Activity ◽

In Vivo Test ◽

Cassia Spectabilis ◽

Chloroquine Diphosphate ◽

Better Than

Abstract Background In previous studies, Cassia spectabilis DC leaf has shown a good antiplasmodial activity. Therefore, this study is a follow-up study of the extract of leaf of C. spectabilis DC on its in vitro and in vivo antiplasmodial activity and mechanism as an antimalarial. Methods The extract was fractionated, sub-fractionated and isolated to obtain the purified compound. In vitro antiplasmodial activity test against Plasmodium falciparum to find out the active compound. In vivo test against P. berghei ANKA-infected mice was conducted to determine prophylactic activity and antiplasmodial activity either alone or in combination with artesunate. The inhibition of heme detoxification test as one of the antimalarial mechanisms was carried out using the Basilico method. Results The results showed that active antimalarial compound isolated from C. spectabilis DC leaf had a structural pattern that was identical to (−)-7-hydroxycassine. Prophylactic test of 90% ethanolic extract of C. spectabilis DC leaf alone against P. berghei ANKA-infected mice obtained the highest percentage inhibition was 68.61%, while positive control (doxycycline 13 mg/kg) was 73.54%. In combination with artesunate, 150 mg/kg three times a day of C. spectabilis DC (D0-D2) + artesunate (D2) was better than the standard combination of amodiaquine + artesunate where the inhibition percentages were 99.18 and 92.88%, respectively. The IC50 of the extract for the inhibitory activity of heme detoxification was 0.375 mg/ml which was better than chloroquine diphosphate (0.682 mg/ml). Conclusion C. spectabilis DC leaf possessed potent antiplasmodial activity and may offer a potential agent for effective and affordable antimalarial phytomedicine.

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Chenopodium ambrosioides L. essential oil and ethanol extract on control of canine Ancylostoma spp.

Semina Ciências Agrárias ◽

10.5433/1679-0359.2017v38n4p1947 ◽

2017 ◽

Vol 38 (4) ◽

pp. 1947 ◽

Cited By ~ 2

Author(s):

Jessica Nascimento Moraes Monteiro ◽

Anderson Barros Archanjo ◽

Gabriela Porfirio Passos ◽

Adilson Vidal Costa ◽

Lenir Cardoso Porfirio ◽

...

Keyword(s):

Essential Oil ◽

Ethanolic Extract ◽

Ethanol Extract ◽

Gastrointestinal Nematodes ◽

Active Principle ◽

Chenopodium Ambrosioides ◽

In Vivo Test ◽

Vitro Effect

The use of Chenopodium ambrosioides L. has shown to be promising in the management of gastrointestinal nematodes. The objective of this study was to quantitate the yield and characterize the chemical composition of the essential oil of C. ambrosioides, as well as to evaluate the in vitro effect of the ethanolic extract and the essential oil in L3 of Ancylostoma spp. and the in vivo effect(s) of the essential oil in dogs. The effects of the ethanol extract and essential oil on Ancylostoma spp. were evaluated in vitro by exposing larvae to the extract at concentrations ranging from 0.005 g mL-1 to 0.2 g mL-1 and to essential oil at concentrations of 50, 100, and 150 ?L mL-1. For the in vivo test, 26 healthy dogs, naturally infected by Ancylostoma spp., were divided into three groups: F1 - cookies were administered without active principle; F2 - herbal cookies containing 37.5 ?L g-1 essential oil of C. ambrosioides L.; F3 - cookies plus a commercial formulation containing febantel, pyrantel, praziquantel, and ivermectin. Complete blood counts and serum biochemistry for AST, ALT, AF, urea, creatinine, total protein, and albumin were performed. The yield of the essential oil was 0.3% m v-1, and its major components included ?-terpinene (1.24%), p-cymene (4.83%), and ascaridol Z (87%) and E (5.04%) isomers. The concentrations of C. ambrosioides L. ethanol extract used were ineffective against Ancylostoma spp. larvae. The essential oil at a concentration of 150 ?L mL-1 was effective against L3 larvae. In the in vivo study in dogs, the herbal cookies containing C. ambrosioides L essential oil reduced the number of eggs per gram of feces.

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Stage-dependent effect of deferoxamine on growth of Plasmodium falciparum in vitro

Blood ◽

10.1182/blood.v76.6.1250.1250 ◽

1990 ◽

Vol 76 (6) ◽

pp. 1250-1255 ◽

Cited By ~ 36

Author(s):

S Whitehead ◽

TE Peto

Keyword(s):

Plasmodium Falciparum ◽

Growth Inhibition ◽

Antimalarial Activity ◽

Clinical Malaria ◽

Inhibitory Effect ◽

Parasite Development ◽

And Control ◽

Speed Of Onset

Abstract Deferoxamine (DF) has antimalarial activity that can be demonstrated in vitro and in vivo. This study is designed to examine the speed of onset and stage dependency of growth inhibition by DF and to determine whether its antimalarial activity is cytostatic or cytocidal. Growth inhibition was assessed by suppression of hypoxanthine incorporation and differences in morphologic appearance between treated and control parasites. Using synchronized in vitro cultures of Plasmodium falciparum, growth inhibition by DF was detected within a single parasite cycle. Ring and nonpigmented trophozoite stages were sensitive to the inhibitory effect of DF but cytostatic antimalarial activity was suggested by evidence of parasite recovery in later cycles. However, profound growth inhibition, with no evidence of subsequent recovery, occurred when pigmented trophozoites and early schizonts were exposed to DF. At this stage in parasite development, the activity of DF was cytocidal and furthermore, the critical period of exposure may be as short as 6 hours. These observations suggest that iron chelators may have a role in the treatment of clinical malaria.

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Antimalarial activity of betulinic acid and derivatives in vitro against Plasmodium falciparum and in vivo in P. berghei-infected mice

Parasitology Research ◽

10.1007/s00436-009-1394-0 ◽

2009 ◽

Vol 105 (1) ◽

pp. 275-279 ◽

Cited By ~ 46

Author(s):

Matheus Santos de Sá ◽

José Fernando Oliveira Costa ◽

Antoniana Ursine Krettli ◽

Mariano Gustavo Zalis ◽

Gabriela Lemos de Azevedo Maia ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Betulinic Acid ◽

Antimalarial Activity

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In vivo Neurological, Analgesic and In vitro Antioxidant and Cytotoxic Activities of Ethanolic Extract of Leaf and Stem Bark of Wedelia chinensis

Bangladesh Pharmaceutical Journal ◽

10.3329/bpj.v22i1.40021 ◽

2019 ◽

Vol 22 (1) ◽

pp. 18-26

Author(s):

Sayema Khanum ◽

Md Shahid Sarwar ◽

Mohammad Safiqul Islam

Keyword(s):

Body Weight ◽

Oral Administration ◽

Radical Scavenging ◽

Ethanolic Extract ◽

Ethanol Extract ◽

Pharmaceutical Journal ◽

Stem Bark ◽

Cytotoxic Activities

Wedelia chinensis is a widely used anti-inflammatory and hepatoprotective medicinal plant in Bangladesh. In this study, analgesic, neurological, antioxidant and cytotoxic activities of the ethanolic extract of leaf and stem bark of W. chinensis were investigated. Oral administration of the ethanolic extract of W. chinensis (200- and 300-mg/kg body weight) was investigated on animal model for neurological activity using open field test and hole cross test. Acetic acid induced writhing method was used to assess the analgesic activity. DPPH (1,1-diphenyl, 2-picryl hydrazyl) radical scavenging assay was used for determining the antioxidant activity, while brine shrimp lethality bioassay was used for investigating cytotoxicity. The ethanol extract of the plant produced significant reduction (P<0.05) of locomotion in both doses (200- and 300-mg/kg body weight) indicating pronounced neurological activity. Oral administration of alcoholic leaves and stem extracts significantly (p < 0.05) inhibited writhing response in mice. The percentage of scavenging of DPPH free radical was found to be concentration dependent with IC50 value of 44.10 ± 0.65 and 38.96 ± 0.50 μg/ml for leaves and stem extracts, respectively. Our findings indicate that W. chinensis may be a source of natural antioxidant with potent analgesic, neurological and cytotoxic activities. Bangladesh Pharmaceutical Journal 22(1): 18-26, 2019

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Computational Chemogenomics Drug Repositioning Strategy Enables the Discovery of Epirubicin as a New Repurposed Hit for Plasmodium falciparum and P. vivax

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.02041-19 ◽

2020 ◽

Vol 64 (9) ◽

Author(s):

Letícia Tiburcio Ferreira ◽

Juliana Rodrigues ◽

Gustavo Capatti Cassiano ◽

Tatyana Almeida Tavella ◽

Kaira Cristina Peralis Tomaz ◽

...

Keyword(s):

Plasmodium Falciparum ◽

In Silico ◽

Antimalarial Activity ◽

Drug Repositioning ◽

Dna Gyrase ◽

Plasmodium Yoelii ◽

Computer Assisted ◽

Content Type

ABSTRACT Widespread resistance against antimalarial drugs thwarts current efforts for controlling the disease and urges the discovery of new effective treatments. Drug repositioning is increasingly becoming an attractive strategy since it can reduce costs, risks, and time-to-market. Herein, we have used this strategy to identify novel antimalarial hits. We used a comparative in silico chemogenomics approach to select Plasmodium falciparum and Plasmodium vivax proteins as potential drug targets and analyzed them using a computer-assisted drug repositioning pipeline to identify approved drugs with potential antimalarial activity. Among the seven drugs identified as promising antimalarial candidates, the anthracycline epirubicin was selected for further experimental validation. Epirubicin was shown to be potent in vitro against sensitive and multidrug-resistant P. falciparum strains and P. vivax field isolates in the nanomolar range, as well as being effective against an in vivo murine model of Plasmodium yoelii. Transmission-blocking activity was observed for epirubicin in vitro and in vivo. Finally, using yeast-based haploinsufficiency chemical genomic profiling, we aimed to get insights into the mechanism of action of epirubicin. Beyond the target predicted in silico (a DNA gyrase in the apicoplast), functional assays suggested a GlcNac-1-P-transferase (GPT) enzyme as a potential target. Docking calculations predicted the binding mode of epirubicin with DNA gyrase and GPT proteins. Epirubicin is originally an antitumoral agent and presents associated toxicity. However, its antiplasmodial activity against not only P. falciparum but also P. vivax in different stages of the parasite life cycle supports the use of this drug as a scaffold for hit-to-lead optimization in malaria drug discovery.

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Antiplasmodial Quinones from the Rhizomes of Kniphofia Foliosa

Natural Product Communications ◽

10.1177/1934578x1300800920 ◽

2013 ◽

Vol 8 (9) ◽

pp. 1934578X1300800 ◽

Cited By ~ 1

Author(s):

Martha Induli ◽

Meron Gebru ◽

Negera Abdissa ◽

Hosea Akala ◽

Ingrid Wekesa ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Methyl Ether ◽

Spectroscopic Data ◽

Antimalarial Activity ◽

In Vivo Assay

Extracts of the rhizomes of Kniphofia foliosa exhibited antiplasmodial activities against the chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plasmodium falciparum with IC50 values of 3–5 μg/mL. A phenyloxanthrone, named 10-acetonylknipholone cyclooxanthrone (1) and an anthraquinone-anthrone dimer, chryslandicin 10-methyl ether (2), were isolated from the rhizomes, along with known quinones, including the rare phenylanthraquinone dimers, joziknipholones A and B. The structures of these compounds were determined based on spectroscopic data. This is the second report on the occurrence of the dimeric phenylanthraquinones in nature. In an in vitro antiplasmodial assay of the isolated compounds, activity was observed for phenylanthraquinones, anthraquinone-anthrone dimers and dimeric phenylanthraquinones, with joziknipholone A being the most active. The new compound, 10-acetonylknipholone cyclooxanthrone, also showed anti-plasmodial activity. In an in vivo assay, knipholone anthrone displayed marginal antimalarial activity.

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