ISOLASI DAN IDENTIFIKASI KAPANG ENDOFIT ASAL AKAR TANAMAN KUNYIT (Curcuma longa) SEBAGAI ANTIMALARIA

Malaria is still the leading cause of death worldwide with nearly half the world's population at risk. Parasitic resistance to existing antimalarial drugs in the market makes the search for a source of new drugs from nature is very important. Therefore, the aims of this study are to determine in vitro antimalarial activity of endophytic fungi extract from turmeric root and to identify the selected isolate molecularly. Heme polymerization inhibition method was used as in vitro antimalarial assay. The selected isolate was thrn identified using ITS1, ITS2, and 5.8S sequences of rDNA. The result of this study obtained 16 isolates of endophytic fungi from root of turmeric plant with isolate code were of K.Cl.Sb.A1 - K.Cl.Sb.A16. All of the ethyl acetate extracts of isolated endophytic fungi have heme polymerization inhibition activity. K.Cl.Sb.A11 was the most active isolate on heme polymerization inhibition test with 94,31% at concentration of test material at 8 mg/mL and IC50 value at 1.84 mg/mL. Molecular analysis showed that K.Cl.Sb.A11 isolate was Penicillium sp. and potentially developed as an antimalarial drug.

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In vitro antimalarial activity assay of Ashitaba Leaf ethanolic extract (Angelica keiskei)

Pharmacy Education ◽

10.46542/pe.2021.212.2730 ◽

2021 ◽

pp. 27-30

Author(s):

Alvi Kusuma Wardani ◽

Abdul Rahman Wahid ◽

Miftahul Jannah

Keyword(s):

Antimalarial Activity ◽

Ethanolic Extract ◽

Inhibitory Effect ◽

Positive Control ◽

New Drugs ◽

Test Results ◽

Ic50 Value ◽

Angelica Keiskei ◽

Very High

Introduction: The incidence of malaria is still very high in number in the world. Difficulty in treating malaria is caused by the resistance of malaria parasites to conventional drugs. An alternative treatment that can be used to treat malaria is to discover new drugs from natural ingredients. Aim: This study aimed to determine the activity of the Ashitaba leaf ethanolic extract as an antimalarial drug to Plasmodium falciparum strain 3D7. Methods: This study tested the activity of Ashitaba extract on the growth of P.falciparum in five concentrations, namely concentration of 0.01 ppm, 0.1 ppm, 1 ppm, 10 ppm, and 100 ppm. Results: The test results showed that the highest inhibitory effect was found on the concentration of 100 ppm with percent inhibition of 79.47 ± 26.91%. The 50% inhibition to parasites showed the half maximal inhibitory concentration (IC50) value of 2.09 ppm, compared to the positive control of which the IC50 of chloroquine was 0.007 ppm. Conclusion: Ashitaba leaf extract can be considered to have very active anti-malarial activity, because it has an IC50 value of less than 5 ppm.

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Potential In Vitro Inhibition of Selected Plant Extracts against SARS-CoV-2 Chymotripsin-Like Protease (3CLPro) Activity

Foods ◽

10.3390/foods10071503 ◽

2021 ◽

Vol 10 (7) ◽

pp. 1503

Author(s):

Carla Guijarro-Real ◽

Mariola Plazas ◽

Adrián Rodríguez-Burruezo ◽

Jaime Prohens ◽

Ana Fita

Keyword(s):

Plant Extracts ◽

Curcuma Longa ◽

Hydrolysis Product ◽

Resonance Energy ◽

Significant Inhibition ◽

Main Role ◽

Turmeric Extract ◽

Ic50 Value

Antiviral treatments inhibiting Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication may represent a strategy complementary to vaccination to fight the ongoing Coronavirus disease 19 (COVID-19) pandemic. Molecules or extracts inhibiting the SARS-CoV-2 chymotripsin-like protease (3CLPro) could contribute to reducing or suppressing SARS-CoV-2 replication. Using a targeted approach, we identified 17 plant products that are included in current and traditional cuisines as promising inhibitors of SARS-CoV-2 3CLPro activity. Methanolic extracts were evaluated in vitro for inhibition of SARS-CoV-2 3CLPro activity using a quenched fluorescence resonance energy transfer (FRET) assay. Extracts from turmeric (Curcuma longa) rhizomes, mustard (Brassica nigra) seeds, and wall rocket (Diplotaxis erucoides subsp. erucoides) at 500 µg mL−1 displayed significant inhibition of the 3CLPro activity, resulting in residual protease activities of 0.0%, 9.4%, and 14.9%, respectively. Using different extract concentrations, an IC50 value of 15.74 µg mL−1 was calculated for turmeric extract. Commercial curcumin inhibited the 3CLPro activity, but did not fully account for the inhibitory effect of turmeric rhizomes extracts, suggesting that other components of the turmeric extract must also play a main role in inhibiting the 3CLPro activity. Sinigrin, a major glucosinolate present in mustard seeds and wall rocket, did not have relevant 3CLPro inhibitory activity; however, its hydrolysis product allyl isothiocyanate had an IC50 value of 41.43 µg mL−1. The current study identifies plant extracts and molecules that can be of interest in the search for treatments against COVID-19, acting as a basis for future chemical, in vivo, and clinical trials.

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Steroid Compounds Isolation from Carthamus tinctorius Linn as Antimalarial

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00924 ◽

2021 ◽

pp. 5297-5304

Author(s):

Rini Hamsidi ◽

Wahyuni Wahyuni ◽

Adryan Fristiohady ◽

Muhammad Hajrul Malaka ◽

Idin Sahidin ◽

...

Keyword(s):

Antimalarial Activity ◽

Carthamus Tinctorius ◽

Spectroscopic Techniques ◽

1H And 13C Nmr ◽

Marker Compound ◽

Ic50 Value ◽

Ft Ir ◽

Ir Spectroscopic

Carthamus tinctorius Linn, also known as safflower, is a plant with the potential of being used in the production of antimalarial drugs. The purpose of this study was to isolate and identify the steroid compounds in the safflower and determine its antimalarial activity in vitro. The isolation process was conducted through extraction and chromatography methods. Then, the characterization of the isolated compounds was conducted through spectroscopic techniques which include Fourier Transform Infrared Spectroscopy (FT-IR), NMR 1-D (1H and 13C-NMR), and NMR 2-D (HMQC, HMBC, and H-H COZY) as well as comparing data with the existing literatures. In addition, the tests conducted were with variations of isolate concentrations (10, 1, 0.1, 0.01, and 0.001 μg/mL) against 3D7 strain of Plasmodium falciparum. Based on the FT-IR spectroscopic data, the steroid compounds isolated from safflowers might be stigmasterols. In addition, the isolates had -OH functional group in the region of 3431 cm-1, C-O in the region of 1053 cm-1, and Csp3-H in regions of 2960, 2934, and 2865 cm-1. The NMR 1-D data showed presence of 29 carbon atoms, while the protons were 48 in number. Furthermore, the IC50 value of the compound was 34.03 μg/mL with a percentage inhibition of 43.92% against the growth of P. falciparum. Therefore, it was classified as inactive agent in inhibiting the growth of malaria parasites, however, it could be used as a marker compound in C. tinctorius Linn extract.

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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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Chenopodium album L. and Sisymbrium officinale (L.) Scop.: Phytochemical Content and In Vitro Antioxidant and Anti-Inflammatory Potential

Plants ◽

10.3390/plants8110505 ◽

2019 ◽

Vol 8 (11) ◽

pp. 505

Author(s):

Valentina Amodeo ◽

Mariangela Marrelli ◽

Veronica Pontieri ◽

Roberta Cassano ◽

Sonia Trombino ◽

...

Keyword(s):

High Performance ◽

Chenopodium Album ◽

Antioxidant Properties ◽

New Drugs ◽

Herbal Remedies ◽

Raw 264.7 Cells ◽

Phytochemical Content ◽

Ic50 Value ◽

Anti Inflammatory

Spontaneous edible plants have an old history of use in popular traditions all around the world, and the rediscovery of these species could also be useful for the search of new drugs. Chenopodium album L. (Amaranthaceae) and Sisymbrium officinale (L.) Scop. (Brassicaceae) are two annual plants traditionally used both as food and herbal remedies against inflammatory disorders. In this work, the potential anti-inflammatory and anti-arthritic activities of these plant species have been investigated, together with their antioxidant potential. The phytochemical composition was assessed as well by means of gas chromatography coupled to mass spectrometry (GC-MS) and high performance thin layer chromatography (HPTLC). The antioxidant properties were assessed using the DPPH and β-carotene bleaching test. The ability of extracts to protect against lipid peroxidation was also examined in rat-liver microsomal membranes. All the samples showed a preservation of antioxidant activity up to 60 min. A significant inhibitory activity on the production of the pro-inflammatory mediator nitric oxide was induced in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells by the dichloromethane fraction of C. album extract, with an IC50 value equal to 81.7 ± 0.9 μg/mL. The same sample showed also a concentration-dependent anti-denaturation effect on heat-treated bovine serum albumin (IC50 = 975.6 ± 5.5 μg/mL), even if the best in vitro anti-arthritic activity was observed for the dichloromethane fraction of S. officinale extract, with an IC50 value of 680.9 ± 13.2 μg/mL.

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In VitroandIn VivoAntimalarial Activity ofFicus thonningiiBlume (Moraceae) andLophira alataBanks (Ochnaceae), Identified from the Ethnomedicine of the Nigerian Middle Belt

Journal of Parasitology Research ◽

10.1155/2014/972853 ◽

2014 ◽

Vol 2014 ◽

pp. 1-6 ◽

Cited By ~ 12

Author(s):

M. O. Falade ◽

D. O. Akinboye ◽

G. O. Gbotosho ◽

E. O. Ajaiyeoba ◽

T. C. Happi ◽

...

Keyword(s):

Antimalarial Activity ◽

Human Cell Line ◽

New Drugs ◽

Leaf Extracts ◽

Potential Source ◽

Hexane Extracts ◽

Ficus Thonningii ◽

Multiresistant Strains

Drug resistance inPlasmodium falciparumrequires that new drugs must be developed. Plants are a potential source for drug discovery and development. Two plants that used to treat febrile illnesses in Nigeria were tested forin vitroandin vivoantimalarial activity and cytotoxicity in cancer cell lines. Methanol, hexane, and ethyl acetate leaf extracts ofFicus thonningiiandLophira alatawere active inin vitroassays againstP. falciparumNF54 (sensitive) and K1 (multiresistant) strains. Hexane extracts ofF. thonningiiandL. alatawere the most effective extracts inin vitroassays with IC50of2.7±1.6 μg/mL and2.5±0.3 μg/mL for NF54 and10.4±1.6 μg/mL and2.5±2.1 μg/mL for K1 strain. All extracts were nontoxic in cytotoxicity assays against KB human cell line with IC50of over 20 μg/mL, demonstrating selectivity againstP. falciparum.In vivoanalysis shows that hexane extracts of both plants reduced parasitaemia. At the maximum dose tested,L. alatahad a 74.4% reduction of parasitaemia whileF. thonningiihad a reduction of 84.5%, both extracts prolonged animal survival in mice infected withP. bergheiNK65 when compared with vehicle treated controls. The antiplasmodial activity observed justifies the use of both plants in treating febrile conditions.

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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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EVALUATION OF IN VITRO MELANOGENESIS INHIBITION ACTIVITY OF KADAMBA (ANTHOCEPHALUS CADAMBA MIQ.)

INDIAN DRUGS ◽

10.53879/id.57.04.12227 ◽

2020 ◽

Vol 57 (04) ◽

pp. 65-66

Author(s):

Siddhisha Kurve ◽

Mihir Khambete ◽

Rupa Kadam

Keyword(s):

Skin Color ◽

Skin Pigmentation ◽

Epidermal Layer ◽

Inhibition Activity ◽

Tyrosinase Inhibition ◽

Crude Drug ◽

Ic50 Value ◽

Anthocephalus Cadamba ◽

Bioactive Agent

The pigment melanin is directly responsible for imparting skin color and imbalance in its production may lead to hyper- or hypo-pigmentation. Hyperpigmentation is characterized by excessive deposition of melanin in the epidermal layer of the skin. In the growing field of bioactive cosmeceuticals, there is a constant demand for newer and more efficacious agents to counter hyperpigmentation. Kadamba is reported to regulate skin pigmentation as per Acharya Vagbhata, but remains comparatively underexplored. In the current study, Anthocephalus cadamba Miq. was screened for inhibition of melanogenesis by studying the effect on enzyme tyrosinase. The crude drug powder was examined at various concentrations ranging from 0.5mg/mL to 3 mg/mL and the IC50 value for tyrosinase inhibition was found to be 1.80 ± 0.10 mg/mL. The results indicate the potential of Anthocephalus cadamba Miq. as an effective de-pigmenting bioactive agent.

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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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SYNTHESIS, CHARACTERIZATION, AND IN VITRO ANTIMALARIAL ACTIVITY OF DIHYDROXYLATION DERIVATIVES OF TRICLOSAN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020.v12s1.ff007 ◽

2020 ◽

pp. 56-59

Author(s):

WAHYU FITRIANA ◽

ARRY YANUAR ◽

ADE ARSIANTI ◽

HIROKI TANIMOTO ◽

KIYOMI KAKIUCHI

Keyword(s):

Antimalarial Activity ◽

Enantiomeric Excess ◽

Vitro Assay ◽

Therapeutic Drugs ◽

Ofplasmodium Falciparum ◽

Ic50 Value ◽

Ic50 Values ◽

New Treatment ◽

Further Development

Objective: The emergence of malaria as a global health problem over the past few decades, accompanied by the rise of chemoresistant strains ofPlasmodium falciparum, has emphasized the need for the discovery of new therapeutic drugs against this disease. In this study, enantiomericallyenriched (enantioenriched) analogs of triclosan were synthesized and evaluated for antimalarial activity against P. falciparum cultures.Methods: Enantioselective dihydroxylation of the olefin in amide seven was performed efficiently using chiral quinine ligand (DHQ)2PHAL to yieldenantioenriched dihydroxy propionamide derivative (+)-1 in moderate yields. In a similar way, the chiral quinidine ligand (DHQD)2PHAL was used asstereoselectivity agent yielded the desired enantioenriched (−)-1. The enantioenriched products were used for further in vitro assay, and accordingly thepercent enantiomeric excess (% ee) was not determined. The structures of compounds were proven by spectral data (1H NMR, 13C NMR, and mass spectra).Results: The phenol moiety at the C1 position of triclosan was chemically substituted with a methoxy group, in conjunction with an introducedstereocenter in a 2,3-dihydroxy-propionamide group at C2’ position. Unmodified triclosan inhibited the P. falciparum cultures with an IC50 value of27.2 μM. By contrast, the triclosan analogs, compounds (+)-1 and (−)-1, inhibited the P. falciparum cultures with IC50 values of 0.034 and 0.028 μM,respectively.Conclusion: Collectively, our preliminary in vitro results suggest that these triclosan analogs have potent antimalarial activity and represent apromising new treatment strategy on further development.

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