scholarly journals ANTIMALARIAL COMPOUNDS FROM ENDOPHYTIC FUNGI OF BROTOWALI (Tinaspora crispa L)

2011 ◽  
Vol 11 (1) ◽  
pp. 53-58 ◽  
Author(s):  
Elfita Elfita ◽  
Muharni Muharni ◽  
Munawar Munawar ◽  
Leni Legasari ◽  
Darwati Darwati
Keyword(s):  
Plasmodium Falciparum ◽  
Endophytic Fungi ◽  
Spectroscopic Data ◽  
Plant Pathogens ◽  
Antimalarial Activity ◽  
Molecular Structures ◽  
Bioactive Metabolites ◽  
Symbiotic Association ◽  
Ic50 Values ◽  
Pathogenic Effects

The term endophytic refers to a bacteria or a fungi microorganism that colonizes interior organs of plants, but does not have pathogenic effects on its host. In their symbiotic association, the host plant protects and feeds the endophytic, which ";in return"; produces bioactive metabolites to enhance the growth and compotitiveness of the host and to protect it from herbivores and plant pathogens. Plants with ethnobotanical history, for example brotowali (Tinaspora crispa L), are likely candidates to find bioactive compounds. Two alkaloids have been isolated from endophytic fungi of brotowali. The molecular structures of the isolated compounds were determined based on spectroscopic data, including UV, IR, NMR 1D and 2D spectrum. The compounds were determined as: 7- hydroxy-3,4,5-trimethyl-6-on-2,3,4,6-tetrahydroisoquinoline-8-carboxylic acid (1) and 2,5-dihydroxy-1-(hydroxymethyl)pyridin-4-on (2). The compound has antimalarial activity against Plasmodium falciparum 3D7, with IC50 values 0,129 µM and 0,127 µM.

scholarly journals Melicope moluccana Antimalarial Activity of Furoquinoline Alkaloids from the Leaves of Melicope moluccana

2020 ◽  
Vol 5 (2) ◽  
pp. 138-142
Author(s):  
Ryan Ayub Wahjoedi ◽  
Ratih Dewi Saputri ◽  
Tjitjik Srie Tjahjandarie ◽  
Mulyadi Tandjung
Keyword(s):  
Plasmodium Falciparum ◽  
Spectral Data ◽  
Spectroscopic Data ◽  
Chemical Structure ◽  
Antimalarial Activity ◽  
2D Nmr ◽  
Esi Ms ◽  
Ic50 Values

Two furoquinoline alkaloids, leptanoine C (1) and haplopine-3,3´-dimethylallyl ether (2) were isolated from the leaves of Melicope moluccana. The chemical structure of both compounds was determined based on spectroscopic data, including UV, IR, HR-ESI-MS, 1D, and 2D NMR spectral data. The antimalarial activity of compounds 1-2 against Plasmodium falciparum 3D7 showing their IC50 values are 0.18 ppm and 2.28 µg/mL, respectively.

Potential Antimalarials. XVI. 4'-Chloro-3-[7″-chloro(and trifluoromethyl)quinolin-4″-yl]amino-5-(substituted amino)methylbiphenyl-4-ols and 4'-Bromo(and 3'-trifluoromethyl)-3-(substituted amino)methyl-5-(7″-trifluoromethylquinolin-4″-yl)aminobiphenyl-2-ols

1992 ◽  
Vol 45 (11) ◽  
pp. 1845 ◽  
Author(s):  
GB Barlin ◽  
FL Tian ◽  
B Kotecka ◽  
KH Rieckmann
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Mannich Bases ◽  
In Vitro Tests ◽  
Ic50 Values

Twenty-four mono-Mannich bases of the general formulae 4'-chloro-3-[7″-chloro(and trifluoro-methyl)quinolin-4'-yl]amino-5-(substituted amino)methylbiphenyl-4-ols and 4'-bromo(and 3'- trifluoromethyl-3(substituted amino)methyl-5(7″-trifluoromethylquinolin-4″-yl) aminobiphenyl-2-ols have been prepared by condensation of the 4-chloro heterocycle with 5-amino-3-(N-substituted amino)methyl-4'-chlorobiphenyl-4-ols or 5-amino-3-(N-substituted amino)methyl- 4'-bromo(or 3'-trifluoromethyl)biphenyl-2-ols. The antimalarial activity of these products in in vitro tests against Plasmodium falciparum reveals many with IC50 values of 50-100 nM ( chloroquine 20-40 nM ). The biphenyl-2-ols were more active than comparable biphenyl-4-ols.

scholarly journals Antiplasmodial Quinones from the Rhizomes of Kniphofia Foliosa

2013 ◽  
Vol 8 (9) ◽  
pp. 1934578X1300800 ◽  
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.

Antiplasmodial Bis-Indole Alkaloids from the Bark of Flindersia pimenteliana

Planta Medica ◽  
2019 ◽  
Vol 86 (01) ◽  
pp. 19-25 ◽  
Author(s):  
Luke P. Robertson ◽  
Leonardo Lucantoni ◽  
Vicky M. Avery ◽  
Anthony R. Carroll
Keyword(s):  
Plasmodium Falciparum ◽  
Spectroscopic Data ◽  
Indole Alkaloids ◽  
2D Nmr ◽  
Antiplasmodial Activity ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Ic50 Values ◽  
Significant Attention

AbstractThree new (1–3) and 2 known (4–5) bis-indole alkaloids were identified from the bark of Flindersia pimenteliana (Rutaceae). The structures of 1–3 were elucidated on the basis of their (+)-HRESESIMS and 2D NMR spectroscopic data. Antiplasmodial activity for 1–3 against chloroquine sensitive (3D7) and chloroquine-resistant (Dd2) Plasmodium falciparum is also reported, with IC50 values ranging from 0.96 to 2.41 µg/mL. These results expand our knowledge of the structure-activity relationships of potently antiplasmodial isoborreverine-type alkaloids, the bioactivity of which have recently attracted significant attention in the literature.

scholarly journals A Novel Trimeric Triterpene From Chisocheton ceramicusMiq.

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.

scholarly journals Senyawa Antimalaria dari Jamur Endofitik Tumbuhan Sambiloto (Andographis paniculata Nees)

2012 ◽  
Vol 13 (2) ◽  
pp. 123
Author(s):  
Elfita Elfita ◽  
Muharni Muharni ◽  
Munawar Munawar ◽  
Salni Salni ◽  
Ade Oktasari
Keyword(s):  
Molecular Structure ◽  
Plasmodium Falciparum ◽  
Secondary Metabolites ◽  
Spectroscopic Data ◽  
White Crystal ◽  
Pure Compound ◽  
Potato Dextrose Broth ◽  
Ic50 Values ◽  
Isolated Compound

Plants have been the chief source of compounds of medicine for thousand of years. Plants are also the source ofmany medicines for the majority of the world’s population. The role of biotechnology is very important for multiplying,conserving the spesies, and enhancing the production of secondary metabolites. Endophytic are microbes thatinhabit plants are currently considered to be a wellspring of novel secondary metabolites offering the potensial formedical and industrial exploitation. Plants with ethnobotanical history, for example sambiloto (Andographispaniculata Nees) are likely candidates for finding bioactive compounds. Isolation begin with cultivation of Aspergillusflavus fungi in 2 liter of Potato Dextrose Broth media for four weeks. Media is extracted into the solvent n-hexaneand ethylacetate following by evaporation. Ethylacetate extracts were separated by chromatography techniquesin order to get pure compound in the form of white crystal. Phytochemical tests showed that the isolated compoundis alkaloid. The molecular structure of the isolated compound was determined based on spectroscopic data,including UV, IR, 1H-NMR, 13C-NMR, HMQC, and HMBC spectrum. The compound was determined as7-hydroxypiranopiridin-4-on with molecule formula C8H7NO2 (Mr=149). The compound has antimalarial activityagainst Plasmodium falciparum 3D7, with IC50 values 0,201 μM.

scholarly journals In vitro antimalarial activity of some organotin(IV)2-nitrobenzoate compounds against Plasmodium falciparum

2018 ◽  
Vol 37 (2) ◽  
Author(s):  
Sutopo Hadi ◽  
Noviany Noviany ◽  
Mita Rilyanti
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Drug ◽  
Antimalarial Activity ◽  
Positive Control ◽  
Intermediate Products ◽  
Nitrobenzoic Acid ◽  
The Future ◽  
Ic50 Values

Antimalarial activity study of organotin(IV) derivatives with nitrobenzoic acid derivatives used as ligands has been performed. The targeted compounds were prepared from their organotin(IV) chlorides via dibutyltin(IV) oxide, diphenyltin(IV) dihydroxide, and triphenyltin(IV) hydroxide intermediate products, followed by reacting the intermediate products with 2-nitrobenzoic acid. The antimalarial activity was performed against P. falciparum. The results showed that the IC50values of dibutyiltin(IV) di-2-nitrobenzoate, diphenyltin(IV) di-2-nitrobenzoate, and triphenyltin(IV) 2-nitrobenzoate were in 8.4 × 10‑3, 5.3 × 10–2, and 9.1 × 10–3 µg/ml, respectively. The IC50 values were slightly higher than the value for chloroquine (2 × 10–3 µg/ml) used as the positive control; however, one advantage is that all prepared organotin(IV) compounds were not resistant to Plasmodium, making the use of organotin(IV) as an antimalarial is possible. The results indicated that the derivative of triphenyltin(IV) was more potent when used as an antimalarial, as expected, and has potential to be developed as an antimalarial drug in the future.

scholarly journals Plasmodium falciparum Knockout for the GPCR-Like PfSR25 Receptor Displays Greater Susceptibility to 1,2,3-Triazole Compounds That Block Malaria Parasite Development

Biomolecules ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1197
Author(s):  
Benedito M. dos Santos ◽  
Daniel T. G. Gonzaga ◽  
Fernando C. da Silva ◽  
Vitor F. Ferreira ◽  
Celia R. S. Garcia
Keyword(s):  
Plasmodium Falciparum ◽  
Malaria Parasite ◽  
Antimalarial Activity ◽  
Parasite Development ◽  
Embryonic Cells ◽  
Hek 293 ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum ◽  
Ic50 Values ◽  
New Compounds

The search for new compounds with antimalarial activity is urgent, as resistance to ones in the classical drug, has already been described in more than one continent. Compounds derived from 1,2,3-triazoles are effective against parasites and bacteria. Here, we evaluated the potential antimalarial activity against the human malaria parasite Plasmodium falciparum in a culture of fifty-four triazole compounds derived from 1H-and 2H-1,2,3-triazole. We identified thirty-one compounds with potential antimalarial activity at concentrations in the micromolar order (µM) and IC50 values ranging from 2.80 µM (9) to 29.27 µM (21). Then, we selected some of these compounds to perform the same tests on the PfSR25- strain (knockout for P. falciparum G-protein coupled receptor-like, SR25). Our experiences with the PfSR25- strain showed that both compounds with higher antimalarial activity for the 3D7 strain and those with less activity resulted in lower IC50 values for the knockout strain. The cytotoxicity of the compounds was evaluated in human renal embryonic cells (HEK 293), using MTT assays. This demonstrated that the compounds with the highest activity (9, 13, 19, 22, 24, 29), showed no toxicity at the tested concentrations.

scholarly journals In vitro antimalarial activity of six Aspidosperma species from the state of Minas Gerais (Brazil)

2012 ◽  
Vol 84 (4) ◽  
pp. 899-910 ◽  
Author(s):  
Maria Fâni Dolabela ◽  
Salma G. Oliveira ◽  
José M. Peres ◽  
José M.S. Nascimento ◽  
Marinete M. Póvoa ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Minas Gerais ◽  
The State ◽  
Active Compounds ◽  
Human Malaria ◽  
Plant Parts ◽  
Ic50 Values

Ethnomedicinal informations point to some Aspidosperma species (Apocynaceae) as antimalarial plants in Brazil and have motivated the evaluation of six species which were collected in the state of Minas Gerais: A. cylindrocarpon Müll. Arg., A. parvifolium A. DC., A. olivaceum Müll. Arg., A. ramiflorum Müll. Arg., A. spruceanum Benth. ex Müll. Arg. and A. tomentosum Mart.. A total of 23 extracts of different plant parts in different solvents were assayed in vitro against chloroquine-resistant (W2) and chloroquine-sensitive (3D7) strains of Plasmodium falciparum. All the extracts were shown to be active with IC50 values in the range of 5.0 ± 0 2.8 µg/mL to 65.0 ± 4.2 µg/mL. TLC profile of the extracts revealed the presence of alkaloids in the six species assayed. These results seem to confirm the popular use of Aspidosperma species to treat human malaria in Brazil and seem point to alkaloids as the putative active compounds of the assayed species.

Inhibition of Protein Tyrosine Phosphatase 1B by Lutein Derivatives isolated from Mexican Oregano (Lippia graveolens)

2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Methanol Extract ◽  
Tyrosine Phosphatase ◽  
Positive Control ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Ic50 Value ◽  
Ic50 Values

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.

Sign in / Sign up

Export Citation Format

Share Document