In Vitro Antimalarial Activity and Toxicity of Helianthus annuus L. Leaf Extract against Plasmodium falciparum

Background: Malaria is one of the public health problems in Indonesia. The morbidity rate is still quite high, especially in the eastern part of Indonesia. Objective: This study aimed to determine the inhibitory activity of the leaf extracts of Helianthus annuus L. against Plasmodium falciparum strain 3D7 as well as the cytotoxicity of the extracts. Methods: The leaves of H. annuus were extracted by the maceration method with n-hexane, chloroform, and ethanol 96% to increase polarity. The antimalarial assay was performed by using Trager and Jensen method, and the cytotoxicity test was carried out by the MTT method. Results: The results of antimalarial study showed that the chloroform extract had IC50 value of 0.002 µg/mL and CC50value of 138.03 µg/mL, 96% ethanol extract had an IC50 value of 0.02 µg/mL and CC50 value of 617.81 µg/mL, and n-hexane extract had an IC50 value of 1.29 µg/mL and CC50 value of 104.89 µg/mL. The selectivity index (SI) values of the chloroform, ethanolic, and n-hexane extracts were calculated and obtained 69,015.00, 30,890.50, and 81.31, respectively. Conclusion: To conclude, the chloroform extract of H. annuus L. leaf gave strong antimalarial activity against P. falciparum strain 3D7 without any cytotoxicity; therefore, H. annuus L. leaf can be a good candidate for the development of an antimalarial drug.

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Inhibition of Heme Polymerization Invitro Assay Of Extract of Sirih Leaf (Piper betle Linn.) and Sun Flower Leaves (Helianthus annuus L.)

Indonesian Journal of Pharmaceutical Science and Technology ◽

10.24198/ijpst.v7i1.25319 ◽

2020 ◽

Vol 7 (1) ◽

pp. 22 ◽

Cited By ~ 1

Author(s):

Ami Tjitraresmi ◽

Moelyono Moektiwardoyo ◽

Yasmiwar Susilawati

Keyword(s):

Helianthus Annuus ◽

Antimalarial Activity ◽

Antimalarial Drugs ◽

Piper Betle ◽

Phytochemical Screening ◽

Helianthus Annuus L ◽

Betel Leaf ◽

The People ◽

Ic50 Values

Malaria is a disease that occurs in tropical countries like Indonesia. The incidence of malaria in the world is still quite high and the occurrence of cases of Plasmodium resistance to antimalarial drugs and the widespread of resistance have prompted researchers to look for new antimalarial drugs, especially from natural materials. Betel leaf (Piper betle Linn.) And sunflower leaf (Helianthus annuus L.) have long been used by the people of Indonesia as an antimalarial drug. The purpose of this study was to determine antimalarial activity through inhibition of heme polymerization and determine secondary metabolite compounds by phytochemical screening from betel leaves and sunflower leaves. The heme polymerization inhibition activity assay was carried out by the in-vitro method using a microplate reader at 415 nm and 630 nm wavelengths. IC50 values of betel leaf extract and sunflower leaf were 178.67 μg/ml and 160.10 μg/ml, respectively. Phytochemical screening results from betel leaf showed the presence of flavonoids, polyphenols, tannins, quinones, saponins, and monoterpenoids-sesquiterpenoids, while sunflower leaves contain alkaloids, polyphenols, flavonoids, steroids and monoterpenoids-sesquiterpenoids.Keywords: Piper betle Linn., Helianthus annuus L., Malaria, Heme Polymerization

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A new protoberberine alkaloid from Meconopsis simplicifolia (D. Don) Walpers with potent antimalarial activity against a multidrug resistant Plasmodium falciparum strain

Journal of Ethnopharmacology ◽

10.1016/j.jep.2013.09.052 ◽

2013 ◽

Vol 150 (3) ◽

pp. 953-959 ◽

Cited By ~ 17

Author(s):

Phurpa Wangchuk ◽

Paul A. Keller ◽

Stephen G. Pyne ◽

Wilford Lie ◽

Anthony C. Willis ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Antimalarial Activity ◽

Multidrug Resistant ◽

Falciparum Strain ◽

Protoberberine Alkaloid

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Skrining Aktivitas Antimalaria Beberapa Tanaman Indonesia Hasil Eksplorasi Dari Hutan Raya Cangar, Batu-Malang, Jawa Timur

JURNAL FARMASI DAN ILMU KEFARMASIAN INDONESIA ◽

10.20473/jfiki.v3i12016.7-11 ◽

2017 ◽

Vol 3 (1) ◽

pp. 7

Author(s):

Achmad Fuad Hafid ◽

Nike Puliansari ◽

Nur Suci Lestari ◽

Lidya Tumewu ◽

Abdul Rahman ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Eucalyptus Globulus ◽

Antimalarial Activity ◽

Probit Analysis ◽

National Forest ◽

Parasitic Disease ◽

Antimalarial Therapy ◽

Ic50 Value ◽

Stem Extract

Background: Malaria is the most important parasitic disease. Malaria control which depends on specific chemotherapy now complicated by resistance of Plasmodium falciparum to most commonly available antimalarial drug. Such situation has heralded the need for alternative antimalarial therapy. Objective: This research aim was to find new antimalarial candidates from some Indonesia plants collected from Cangar National Forest, Batu-Malang, East Java. Methods: Eleven samples of leaves and stem extracts were screened against Plasmodium falciparum 3D7 culture which maintained in RPMI-1640 Medium. Samples tested in concentration of 0.01, 0.1, 1, 10 and 100 µg/ml. Probit analysis was used to determine IC50. Results: In vitro antimalarial activity revealed that only three crude extracts samples from Fraxinus griffithi stem extract, Piper sulcatum leaves extract and Eucalyptus globulus stem extract had good antimalarial activity with IC50 value of 0.33, 0.20 and 0.55 µg/ml, respectively. Conclusions: Fraxinus griffithi stem extract, Piper sulcatum leaves extract and Eucalyptus globulus stem extract might be a good candidate for antimalarial natural product resources.

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Antiplasmodial activity of faloak bark (Sterculia quadrifida, R.Br.) extract from East Nusa Tenggara, Indonesia

Indonesian Journal of Pharmacology and Therapy ◽

10.22146/ijpther.1975 ◽

2021 ◽

Vol 2 (2) ◽

Author(s):

Priska Ernestina Tenda ◽

Maria Hilaria ◽

Arba Pramundita Ramadani

Keyword(s):

Antimalarial Activity ◽

Ethanolic Extract ◽

Antiplasmodial Activity ◽

Current Development ◽

Antimalarial Drug Resistance ◽

Falciparum Strain ◽

Ic50 Value ◽

Endemic Medicinal Plant ◽

The Relationship

The current development of antimalarial drug resistance encourages researchers to discover and develop novel antimalarials. One of its alternatives for antimalarial discovery is using medicinal plants remembering the success of artemisinin. Sterculia quardrifida R. Br. bark, locally name as faloak, is an endemic medicinal plant from East Nusa Tenggara that has been used traditionally to treat malaria. However, its antimalarial activity has not been investigated, yet. This study was aimed to evaluate the antiplasmodial activity of ethanolic extract of faloak bark against Plasmodium falciparum in vitro. Using FCR-3 P. falciparum strain, the ethanolic extract was evaluated on various concentration (1, 10, 50, and 100 μg/mL, respectively). The IC50 value was determined by the relationship between concentration and percentage of growth inhibition. The result showed that the percentage of inhibition of P. falciparum was concentration dependent, higher concentration resulting on higher percentage of inhibition with the IC50 42.399 ± 9.517 μg/mL. It can be concluded that the ethanolic extract of faloak bark have moderate antiplasmodial activity against P. falciparum in vitro.

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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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A polyphenol, pyrogallol changes the acidic pH of the digestive vacuole of Plasmodium falciparum

Life Sciences, Medicine and Biomedicine ◽

10.28916/lsmb.5.1.2021.82 ◽

2021 ◽

Vol 5 (1) ◽

Author(s):

Nur Saidatul Aqilah Ja’afar ◽

Nik Nor Imam Nik Mat Zin ◽

Fatin Sofia Mohamad ◽

Nurhidanatasha Abu-Bakar

Keyword(s):

Plasmodium Falciparum ◽

Proton Pump ◽

Antimalarial Activity ◽

Fluorescein Isothiocyanate ◽

Drug Candidate ◽

Digestive Vacuole ◽

Atpase Inhibitor ◽

Trophozoite Stage ◽

Concanamycin A ◽

Ic50 Value

Pyrogallol has a capability of generating free radicals like other antimalarial drugs such as artemisinin, which is thought to inhibit the proton pump located in the membrane of the Plasmodium falciparum digestive vacuole, thus alkalinising this acidic organelle. This study aimed to determine pH changes of the malaria parasite’s digestive vacuole following treatment with pyrogallol. The antimalarial activity of this compound was evaluated by a malarial SYBR Green 1 fluorescence-based assay to determine the 50% inhibitory concentration (IC50). Based on the IC50 value, different concentrations of pyrogallol were selected to ensure changes of the digestive vacuole pH were not due to parasite death. This was measured by flow cytometry after 4-hour pyrogallol treatment on the fluorescein isothiocyanate-dextran-accumulated digestive vacuole of the mid-trophozoite stage parasites. Pyrogallol showed a moderate antimalarial activity with the IC50 of 2.84 ± 9.40 µM. The treatment of 1.42, 2.84 and 5.67 µM pyrogallol increased 2.9, 3.0 and 3.1 units of the digestive vacuole pH, respectively as compared with the untreated parasite (pH 5.6 ± 0.78). The proton pump, V-type H+-ATPase might be inhibited by pyrogallol, hence causing the digestive vacuole pH alteration, which is similar with the result shown by a standard V-type H+-ATPase inhibitor, concanamycin A. This study provides a fundamental understanding on the antimalarial activity and mechanism of action of pyrogallol that has a potential to be the antimalarial drug candidate.

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A Novel Trimeric Triterpene From Chisocheton ceramicusMiq.

Natural Product Communications ◽

10.1177/1934578x211053202 ◽

2021 ◽

Vol 16 (11) ◽

pp. 1934578X2110532

Author(s):

Alfarius Eko Nugroho ◽

Marika Okabe ◽

Yusuke Hirasawa ◽

Chin Piow Wong ◽

Toshio Kaneda ◽

...

Keyword(s):

Plasmodium Falciparum ◽

Spectroscopic Data ◽

Antimalarial Activity ◽

Falciparum Strain ◽

Chisocheton Ceramicus

A novel trimeric triterpene, bismoronic ceramicine (1), was isolated from the bark of Chisocheton ceramicus Miq. The structure was elucidated based on spectroscopic data and chemical correlations. Bismoronic ceramicine (1) showed moderate antimalarial activity against Plasmodium falciparum strain 3D7.

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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.v3i1.4088 ◽

2017 ◽

Vol 3 (1) ◽

pp. 17 ◽

Cited By ~ 1

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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