scholarly journals Antimicrobial and Antiparasitic Abietane Diterpenoids from the Roots of Clerodendrum eriophyllum

2010 ◽  
Vol 5 (6) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Francis Machumi ◽  
Volodymyr Samoylenko ◽  
Abiy Yenesew ◽  
Solomon Derese ◽  
Jacob O. Midiwo ◽  
...  
Keyword(s):  
Spectroscopic Data ◽  
Antimalarial Activity ◽  
Antibacterial Activities ◽  
Cd Spectra ◽  
Normal Series ◽  
Abietane Diterpenoids ◽  
Abietane Diterpenes ◽  
First Time ◽  
Absolute Stereochemistry

Chromatographic separation of the roots of a Kenyan medicinal plant, Clerodendrum eriophyllum, led to the isolation of ten abietane diterpenoids (1-10), one of which (1) was isolated for the first time from a natural source. Using spectroscopic data, the structure of 1 was determined to be 12-hydroxy-8,12-abietadiene-3,11,14-trione. Circular dichroism (CD) spectra showed that the stereochemistry of compounds 1, 3, and 6-8 belongs to the normal series of abietane diterpenes, which confirmed the absolute stereochemistry of the isolated compounds. Compounds 1-10 were evaluated for their in vitro antiplasmodial, antileishmanial, antifungal and antibacterial activities. Compounds 3 and 7 exhibited potent antifungal activity (IC50/MIC 0.58/1.25 and 0.96/2.5 μg/mL, respectively) against C. neoformans, whereas 3, 6 and 7 showed strong antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus with IC50/MIC values between 1.33-1.75/2.5-5 and 0.96-1.56/2.5 μg/mL, respectively. In addition, compounds 3 and 9 exhibited potent antileishmanial activity (IC50 0.08 and 0.20 μg/mL, respectively) against L. donovani, while 3 and 7 displayed weak antimalarial activity against Plasmodium falciparum, but 9 was inactive.

scholarly journals Exploratory Analysis into the in vitro and in silico Activity of E. fusca Lour. (Fabaceae) Elucidates Substantial Antiplasmodial Activity of the Plant

2021 ◽  
Author(s):  
Saiful Arefeen Sazed ◽  
Ohedul Islam ◽  
Sarah L. Bliese ◽  
Muhammad Riadul Haque Hossainey ◽  
Jakaria Shawon ◽  
...  
Keyword(s):  
Antimalarial Drug ◽  
Simulation Analysis ◽  
Antimalarial Activity ◽  
Dynamics Simulation ◽  
Drug Candidate ◽  
Phytochemical Investigation ◽  
High Degree ◽  
Emergence Of Resistance ◽  
First Time

The exploration of alternative antimalarial therapeutics is a requisite for the emergence of resistance against Artemisinin. Considering the required cost and time length of classical small molecule drug discovery process, phytochemical screening of traditionally used medicinal plant which are repertoire of active compounds with antimalarial activity has become popular. To investigate the antimalarial property of traditionally used medicinal plants, a number of Erythrina spp have been reviewed systematically where less studied E. fusca has been selected for further analysis. Phytochemical investigation yielded five compounds namely; Phaseolin, Phytol, β-amyrin, Lupeol, and Stigmasterol. In-vitro antimalarial drug sensitivity HRP-II ELISA was carried out against chloroquine (CQ) sensitive 3D7 and CQ-resistant Dd2 strains. Extracts showed significant antimalarial activity against 3D7 and Dd2 strains (IC50 4.94 – 22 µg/mL) and these compounds have been reported here for the first time. Molecular docking analysis showed high binding energy (−9.0 ± 0.32 kcal/mole) indicating high degree of interaction between Phaseolin and 14 clinically important Plasmodium falciparum proteins at the active site. Stable interaction was also observed between ligand and protein from molecular dynamics simulation analysis with high free energy (−75.156 ± 11.459) that substantiates the potential of Phaseolin as an antimalarial drug candidate.

scholarly journals Sesquiterpene Lactones from Inula oculus-christi

2010 ◽  
Vol 5 (4) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Mahmoud Mosaddegh ◽  
Maryam Hamzeloo Moghadam ◽  
Saeedeh Ghafari ◽  
Farzaneh Naghibi ◽  
Seyed Nasser Ostad ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Crystal Structures ◽  
Spectroscopic Data ◽  
Sesquiterpene Lactones ◽  
X Ray ◽  
X Ray Crystallography ◽  
First Time

Inula oculus-christi L. (Compositae) extract was chromatographed and three sesquiterpene lactones ergolide, gaillardin and pulchellin C were isolated. The structures of these compounds were determined by analysis of their spectroscopic data, and their crystal structures were defined using X-ray crystallography; the isolation of ergolide and pulchellin C is reported for the first time from this species. These three compounds were evaluated for their in vitro cytotoxic activity against MDBK, MCF7 and WEHI164 cells; ergolide and gaillardin exhibited lower and significantly different IC50 values compared with pulchellin C ( p<0.001).

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.

scholarly journals Antialactone: A New γ-Lactone from Antiaris Africana, and its Absolute Configuration Determined from TDDFT CD Calculations

2008 ◽  
Vol 3 (2) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Vouffo Bertin ◽  
Hidayat Hussain ◽  
Simeon F. Kouam ◽  
Etienne Dongo ◽  
Gennaro Pescitelli ◽  
...  
Keyword(s):  
Natural Product ◽  
Absolute Configuration ◽  
Betulinic Acid ◽  
Spectroscopic Data ◽  
Nmr Spectra ◽  
2D Nmr ◽  
Stem Bark ◽  
Cd Spectra ◽  
2D Nmr Spectra ◽  
First Time

Four compounds were isolated from the stem bark of Antiaris africana. One of them, a γ-lactone named antialactone (1a), is reported for the first time as a natural product. The structures were determined by comprehensive analyses of their 1D and 2D NMR spectra and EI MS data. The absolute configuration of antialactone acetate (1b) was established by TDDFT CD calculations and comparison with measured CD spectra. The remaining three known compounds were identified, by comparing their spectroscopic data with those reported in the literature, as lichenxanthone, β-sitosterol, and betulinic acid.

scholarly journals Novel Antiplasmodial Agents from Christia vespertilionis

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Harish C. Upadhyay ◽  
Brijesh S. Sisodia ◽  
Harveer S. Cheema ◽  
Jyoti Agrawal ◽  
Anirban Pal ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Complete Suppression ◽  
The Novel ◽  
Aqueous Methanol ◽  
Isolation And Characterization ◽  
First Time ◽  
Detailed Chemical

The roots, leaves and stems of Christia vespertilionis were separately and successively extracted with methanol and aqueous-methanol (1:4, v/v) and were evaluated in vitro for their antiplasmodial potential against Plasmodium falciparum NF-54. The aqueous-methanolic stem (AS) extract was the most active (IC50 7.5 μg/mL) followed by the methanolic leaf (ML) extract (IC50 32.0 μg/mL). The in vivo antimalarial activity of the combined plant extract of C. vespertilionis was also assessed in P. berghei infected mice, which showed 87.8% suppression of parasitaemia as compared with complete suppression by chloroquine on day 8. Finally, detailed chemical investigation of C. vespertilionis resulted in the isolation and characterization of fifteen compounds (1–15), of which two (1 and 4) are being reported for the first time from nature. The novel compound 1 possesses potent antiplasmodial activity (IC50 = 9.0 μg/mL).

First-time comparison of the in vitro antimalarial activity of Artemisia annua herbal tea and artemisinin

2012 ◽  
Vol 106 (11) ◽  
pp. 696-700 ◽  
Author(s):  
Antonella De Donno ◽  
Tiziana Grassi ◽  
Adele Idolo ◽  
Marcello Guido ◽  
Paride Papadia ◽  
...  
Keyword(s):  
Artemisia Annua ◽  
Antimalarial Activity ◽  
Herbal Tea ◽  
First Time

scholarly journals Antisickling and Antibacterial Activities of Anthocleista schweinfurthii Gilg. (Gentianaceae) from Non-human Primates Pharmacopoeia in Democratic Republic of the Congo

2019 ◽  
Vol 1 (3) ◽  
pp. 14-20
Author(s):  
Samy Ngunde-te-Ngunde ◽  
Emmanuel Moke Lengbiye ◽  
Tshidibi Dipa Joseph ◽  
Kengo Velantia Franck ◽  
Ruphin D. Djolu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Ethyl Acetate ◽  
Stem Bark ◽  
Antibacterial Activities ◽  
Scientific Basis ◽  
Root Bark ◽  
Bacterial Strains ◽  
Republic Of The Congo ◽  
First Time

The aim of the present study was to evaluate the Chemical composition and bioactivity of Anthocleista schweinfurthii Gilg (Gentianaceae) fruits, leaves, root bark and stem bark extracts against Sickle cell disease (SCD) and associated bacteria. The antisickling and antibacterial activities were carried out using Emmel and micro-dilution methods respectively. The results revealed that the fruits, leaves, root bark and stem bark extracts  of A. schweinfurthii contains various secondary metabolites such as the alkaloids, saponins, total polyphenols, flavonoids, tannins, anthocyanis, leuco-anthocyanins and quinones.  The ethyl acetate and methanol extracts displayed antisickling activity. While, the antibacterial activity of different plant extracts tested was weak toward tested bacterial strains (CMI ≥125μg/mL). The antibacterial activity can be improved by bio-guided fractionation of the n-hexane, ethyl acetate or methanol soluble fraction. This study provides for the first time a scientific basis for the in vitro antisickling activity of A. schweinfurthii.

scholarly journals Novel 2-mercaptobenzimidazole derivatives: synthesis and evaluation of its antibacterial and antioxidant activities

2017 ◽  
Vol 6 (3) ◽  
pp. 77-87 ◽  
Author(s):  
Latifa El Ouasif ◽  
Abdelhakim Bouyahya ◽  
Rachid Zniber ◽  
Mostafa El Ghoul ◽  
Redouane Achour ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
Hydrocarbon Chains ◽  
Free Radical Scavenging Assay ◽  
First Time ◽  
Diffusion Assay ◽  
Antioxidant Effects

In the present study, a series of novel 2-mercapto-benzimidazolium were synthesized from 2-mercapto-benzimidazole with hydrocarbon chains. All compounds obtained are reported for the first time, and the structures of these compounds were confirmed by means of 1H-NMR, 13C-NMR and mass spectrometry. The newly synthesized compounds were subjected to in vitro biological evaluation. The antibacterial activity was evaluated will diffusion assay and density optic method. The antioxidant activity was carried out using DPPH free radical scavenging assay. The result indicated that some compounds show convincing antibacterial activities against two microorganisms: Escherichia coli and Staphylococcus aureus. While, these molecules have not shown interesting antioxidant effects.

scholarly journals In vitro Antiprotozoal Activity and Chemical Composition of Ambrosia tenuifolia and A. scabra Essential Oils

2008 ◽  
Vol 3 (4) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Valeria P. Sülsen ◽  
Silvia I. Cazorla ◽  
Fernanda M. Frank ◽  
Paola M. R. Di Leo Lira ◽  
Claudia A. Anesini ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Essential Oils ◽  
Inhibitory Concentration ◽  
Antimalarial Activity ◽  
Caryophyllene Oxide ◽  
Antiprotozoal Activity ◽  
Aerial Parts ◽  
Germacrene D ◽  
First Time

The in vitro antimalarial, trypanocidal and leishmanicidal activities and the chemical composition of Ambrosia tenuifolia and A. scabra essential oils were investigated. The oils, obtained by hydrodistillation of the aerial parts, showed significant antimalarial activity against the chloroquine sensitive (F32) and the chloroquine resistant (W2) strains of Plasmodium falciparum with 50% inhibitory concentration (IC50) values ranged from 2.8 to 7 μg/mL. Against Trypanosoma cruzi epimastigotes, only A. tenuifolia exerted slight activity (IC50 = 59.7 μg/mL). None of the essential oils showed toxicity towards Leishmania mexicana. Cytotoxicity for murine T-lymphocytes was compared with the parasiticidal activity by using the selectivity index (SI) ratio. The chemical composition of A. tenuifolia and A. scabra essential oils was analyzed by GC-FID-MS. Thirty-eight and twenty-four compounds were identified in A. tenuifolia and A. scabra, respectively. The major constituents of A. tenuifolia oil were germacrene D (22.9%) and bicyclogermacrene (14.2%), while the oil of A. scabra contained limonene (22.0%), caryophyllene oxide (13.8%) and ( E)-caryophyllene (13.5%). This is the first time that the antiprotozoal activity of both oils and the chemical composition of A. scabra essential oil have been reported.

Resorcylic Acid Lactones Produced by an Endophytic Penicillium ochrochloron Strain from Kadsura angustifolia

Planta Medica ◽  
2020 ◽  
Author(s):  
Hong Chuan Song ◽  
Dan Qin ◽  
Hai Yang Liu ◽  
Jin Yan Dong ◽  
Chuan You ◽  
...  
Keyword(s):  
Spectroscopic Analysis ◽  
Tumor Cell Line ◽  
Antibacterial Activities ◽  
Preparative Hplc ◽  
Solid Culture ◽  
Ic50 Value ◽  
Resorcylic Acid Lactones ◽  
New Compounds ◽  
First Time

AbstractFour new β-resorcylic acid lactones, including penochrochlactone A (2), 4-O-desmethyl-aigialomycin B (4), and penochrochlactones C and D (5 and 6), two compounds isolated from a natural source for the first time, 5α, 6β-acetonide-aigialomycin B (1) and penochrochlactone B (3), together with six known compounds, aigialomycin F (7), aigialomycins A, B, and D (8–10), zeaenol (11), and oxozeaenol (12), were isolated from a mycelial solid culture of the endophytic fungus Penicillium ochrochloron SWUKD4.1850 from the medicinal plant Kadsura angustifolia by sequential purification over silica gel, Sephadex LH-20 column chromatography, and preparative HPLC. Their structures were elucidated by extensive spectroscopic analysis and chemical conversions. In addition, all the new compounds were evaluated for their cytotoxic and antibacterial activities in vitro. Penochrochlactone C (5) displayed moderate cytotoxicity against the HeLa tumor cell line with an IC50 value of 9.70 µM. In the antibacterial assays, compounds 4 – 6 exhibited moderate activities against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa with MIC values between 9.7 and 32.0 µg/mL.

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