scholarly journals New Pharmacophore from the Stem Bark Fractions of Acacia decurrens (Willd), an Invasive South Africa Tree

2017 ◽  
Vol 2017 ◽  
pp. 1-12
Author(s):  
Bamidele Joseph Okoli ◽  
Johannes Sekomeng Modise
Keyword(s):  
Invasive Plant ◽  
Scientific Information ◽  
Stem Bark ◽  
Radical Scavenger ◽  
Vitro Assay ◽  
Gram Positive Bacteria ◽  
Microbial Inhibition ◽  
Diffusion Assay

The tolerance of Acacia decurrens, an invasive species, was exploited pharmacologically in this study. Phytochemical screening revealed important secondary metabolites. Importantly, the assay shows that ethyl acetate and methanol fractions are sources of phytochemicals compared to the hexane and chloroform fractions. A bioassay-guided in vitro assay of the extracts led to the eventual isolation of four bioactive compounds by column chromatography, identification, and characterisation with the aid of GCMS, UV-Vis, FTIR, and NMR. The antimicrobial screening by disc diffusion assay revealed 22.2%, 44.4%, 66.7%, and 77.8% microbial inhibition by 2-methyl-octahydro-indene-4-carboxylic acid (AD1), 6-methyldecahydro-1H-phenanthren-9-one (AD2), 8-hydroxytetradecahydro-chrysene-1-carb aldehyde (AD3), and 8,9-dihydroxy-7-(2-hydroxy-ethyl)-9,9a-hexahydro-1H,3H-2-thia-5a-aza cyclopenta[b]anthracen-6-one (AD4), respectively. Compounds AD3 and AD4 are the most potent antibacterial compounds against Gram-positive bacteria with MIC 12.5–6.25 μg/ml. Antioxidant study of the compounds assayed with DPPH and ABTS•+ revealed that compound (AD4) is the most efficient DPPH radical scavenger with IC50 30.07 ± 0.31 and ABTS•+ scavenging activity of 4363.2 ± 452.4 μmol of TE/gDW. This provides scientific information on four pharmacophores with phyto-antioxidants and antimicrobial potential, despite the classification of A. decurrens as a Category 2 invasive plant by the National Water Act.

scholarly journals Short-Form Bomanins Mediate Humoral Immunity in Drosophila

2018 ◽  
Vol 10 (4) ◽  
pp. 306-314 ◽  
Author(s):  
Scott A. Lindsay ◽  
Samuel J.H. Lin ◽  
Steven A. Wasserman
Keyword(s):  
Humoral Immunity ◽  
Short Form ◽  
Family Members ◽  
Gene Encoding ◽  
Vitro Assay ◽  
Gram Positive Bacteria ◽  
Toll Receptor ◽  
Secreted Peptides

The Bomanins (Boms) are a family of a dozen secreted peptides that mediate the innate immune response governed by the Drosophila Toll receptor. We recently showed that deleting a cluster of 10 Bom genes blocks Toll-mediated defenses against a range of fungi and gram-positive bacteria. Here, we characterize the activity of individual Bom family members. We provide evidence that the Boms overlap in function and that a single Bom gene encoding a mature peptide of just 16 amino acids can act largely or entirely independent of other family members to provide phenotypic rescue in vivo. We further demonstrate that the Boms function in Drosophila humoral immunity, mediating the killing of the fungal pathogen Candida glabrata in an in vitro assay of cell-free hemolymph. In addition, we find that the level of antifungal activity both in vivo and in vitro is linked to the level of Bom gene expression. Although Toll dictates expression of the antimicrobial peptides (AMPs) drosomycin and metchnikowin, we find no evidence that Boms act by modifying the expression of the mature forms of these antifungal AMPs.

scholarly journals Machine learning prediction of UV–Vis spectra features of organic compounds related to photoreactive potential

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Rafael Mamede ◽  
Florbela Pereira ◽  
João Aires-de-Sousa
Keyword(s):  
Machine Learning ◽  
Organic Molecules ◽  
Vitro Assay ◽  
Chemical Structures ◽  
Positive Class ◽  
Global Accuracy ◽  
External Test ◽  
Experimental Absorption

AbstractMachine learning (ML) algorithms were explored for the classification of the UV–Vis absorption spectrum of organic molecules based on molecular descriptors and fingerprints generated from 2D chemical structures. Training and test data (~ 75 k molecules and associated UV–Vis data) were assembled from a database with lists of experimental absorption maxima. They were labeled with positive class (related to photoreactive potential) if an absorption maximum is reported in the range between 290 and 700 nm (UV/Vis) with molar extinction coefficient (MEC) above 1000 Lmol−1 cm−1, and as negative if no such a peak is in the list. Random forests were selected among several algorithms. The models were validated with two external test sets comprising 998 organic molecules, obtaining a global accuracy up to 0.89, sensitivity of 0.90 and specificity of 0.88. The ML output (UV–Vis spectrum class) was explored as a predictor of the 3T3 NRU phototoxicity in vitro assay for a set of 43 molecules. Comparable results were observed with the classification directly based on experimental UV–Vis data in the same format.

In vitro Antimicrobial Activity of Plants used in Cambodian Traditional Medicine

2007 ◽  
Vol 35 (05) ◽  
pp. 867-873 ◽  
Author(s):  
Aun Chea ◽  
Marie-Caroline Jonville ◽  
Sok-Siya Bun ◽  
Michèle Laget ◽  
Riad Elias ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Traditional Medicine ◽  
Bactericidal Effect ◽  
Gram Positive Bacteria ◽  
Antibacterial And Antifungal Activities ◽  
Methanolic Extracts ◽  
Disk Diffusion Assay ◽  
Antibacterial And Antifungal ◽  
Diffusion Assay

The purpose of the present study was to screen 27 plant species used in the traditional medicine of Cambodia for in vitro antibacterial and antifungal activities. Thirty-three methanolic extracts were tested against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Mycobacterium smegmatis and Candida albicans. Screened by disk diffusion assay, the extracts showed antimicrobial activity especially on Gram-positive bacteria. None of the crude methanolic extracts showed activity against P. aeruginosa. Twenty-five selected extracts were evaluated using a micro-dilution test. Harrisonia perforata (roots) and Hymenodictyon excelsum (bark) exhibited a bactericidal effect against S. aureus at a concentration of 500 μg/ml. Azadirachta indica (bark), Harrisonia perforata (roots and stem) and Shorea obtusa (roots) exhibited a bactericidal effect against M. smegmatis at 250 μg/ml.

scholarly journals New Flavan and Alkyl α,β-Lactones from the Stem Bark of Horsfieldia Superba

2013 ◽  
Vol 8 (4) ◽  
pp. 1934578X1300800
Author(s):  
Nabil Ali Al-Mekhlafi ◽  
Khozirah Shaari ◽  
Faridah Abas ◽  
Ethyl Jeyaseela Jeyaraj ◽  
Johnson Stanslas ◽  
...  
Keyword(s):  
Optical Rotation ◽  
2D Nmr ◽  
Stem Bark ◽  
Cytotoxic Activities ◽  
Dihydroxybenzoic Acid ◽  
Vitro Assay ◽  
Phytochemical Investigation ◽  
Ache Inhibitory Activity ◽  
Hct 116

In the present study phytochemical investigation of the methanol extract of the stem bark of Horsfieldia superba led to the isolation of twenty compounds (1-20), of which three (1-3) were new. However, compounds 2 and 3 were previously reported as synthetic α, β-lactones. The compounds were characterized as (-)-3,4′,7-trihydroxy-3′-methoxyflavan (1), (-)-5,6-dihydro-6-undecyl-2 H-pyran-2-one (2), and (-)-5,6-dihydro-6-tridecyl-2 H-pyran-2-one (3). Seventeen other known compounds were also isolated and identified as (-)-viridiflorol (4), hexacosanoic acid (5), β-sitosterol (6), methyl 2,4-dihydroxy-6-methylbenzoate (methylorsellinate) (7), methyl 2,4-dihydroxy-3,6-dimethylbenzoate (8), (-)-4′-hydroxy-7-methoxyflavan (9), (-)-4′,7-dihydroxyflavan (10), (-)-4′,7-dihydroxy-3′-methoxyflavan (11), (+)-3,4′,7-trihydroxyflavan (12), (-)-catechin (13), (-)-epicatechin (14), (-)-7-hydroxy-3′,4′-methylenedioxyflavan (15), 2′,3,4-trihydroxy-4′-methoxydihydrochalcone (16), 3′,4′,7-trihydroxyflavone (17), (+)-4′-hydroxy-7-methoxyflavanone (18), hexadecanoic acid (palmitic acid) (19) and 3,4-dihydroxybenzoic acid (20). The structures of the compounds were fully characterized by various physical methods (melting point, optical rotation), spectral (UV, IR, ID and 2D NMR) and mass spectrometric techniques. In vitro assay of compounds 2 and 3 demonstrated moderate cytotoxic activities against human prostate (PC-3), colon (HCT-116) and breast (MCF-7) cancer cells, while the chloroform and ethyl acetate fractions of H. superba were found to exhibit moderate AChE inhibitory activity (IC50 72 and 60 μg/mL).

scholarly journals IN VITRO ANTIMICROBIAL ACTIVITY AND MIC OF THE EXTRACELLULAR ETHYL ACETATE CRUDE EXTRACT OF ENDOPHYTIC FUNGI FUSARIUM SP. ISOLATED FROM TEPHROSIA PURPUREA ROOT

2019 ◽  
pp. 48-53
Author(s):  
DEEPENDRA THAKUR ◽  
KAMANA SAHANI
Keyword(s):  
Antimicrobial Activity ◽  
Endophytic Fungi ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Tephrosia Purpurea ◽  
Dye Reduction ◽  
Fusarium Sp ◽  
Novel Drug ◽  
Diffusion Assay

Objective: The objective of the present investigation was to find antimicrobial and MIC of endophytic fungi Fusarium sp. isolated from Tephrosia purpurea root. Methods: Well diffusion assay was performed to find out the antimicrobial activity and Resazurin dye reduction method was performed to find out MIC of the extract. Result: The extract showed the highest zone of inhibition of 22.66±0.57 mm, (Bacillus subtilis, MTCC-441) for Gram-positive bacteria and 20.66±0.57 mm, (E. coli, MTCC-443) for Gram-negative bacteria. Furthermore, the MIC of the extract was found to be (31.25 µg/ml-125 µg/ml). Conclusion: Hence, the endophytic fungi isolated from the Tephrosia purpurea root, i.e. Fusarium sp. showed good antimicrobial activity and hence can be used to find a novel drug.

scholarly journals In vitro and In vivo Antiplasmodial of Stem Bark Extract of Garcinia husor

2019 ◽  
Vol 26 (2) ◽  
pp. 81
Author(s):  
Healthy Kainama ◽  
Sri Fatmawati ◽  
Mardi Santoso ◽  
Pieter Kakisina ◽  
Taslim Ersam
Keyword(s):  
Ethyl Acetate ◽  
Ethyl Acetate Extract ◽  
Biochemical Parameter ◽  
Stem Bark ◽  
Negative Control ◽  
Antiplasmodial Activity ◽  
Bark Extract ◽  
Vitro Assay

Garcinia husor is one of the folk medicines in Maluku-Indonesia. This species has been used for the treatmet of Malaria disease. The phytochemical contents and antiplasmodial activity not reported yet. In this study we evaluated the quantitative phytochemicals, in vitro and in vivo antiplasmodial activity of stem bark ethyl acetate extract. In vitro assay was done using P. falciparum 3D7 strain sensitive of chloroquine. For in vivo analysis, four groups of M. musculus were infected by P. berghei and their parasitemia levels were for 7 days of treatment with ethyl acetate extract; hematological and biochemical parameter were analyzed at the end of experiment. The result showed ethyl acetate extract with the TPC (169.47 mg GAE/100 g ±0.61) and TPC (167.37 mg QE/100 g ±1.05) was active against P. falciparum 3D7 strain (IC50 value of 0.31±0.43 μg/ml). The animal treated with extract showed suppression of parasitemia to 87.57±1.41% compared with the P. berghei infected-mice (negative control), ED50 value of 22.30 mg/kg BW. The dose of extract in 200 mg/kg BW was reduce parasitemia of infected mice with P. berghei more potential. The ethyl acetate of the stem bark G. husor with has antiplasmodial properties and future investigation are necessary to elucidate its mechanism of action.

scholarly journals Biologically relevant surrogates of coumarins: 2-phenyl H-isophosphinoline 2-oxides with antibacterial activity

2021 ◽  
Vol 16 (2) ◽  
pp. 283-296
Author(s):  
Mina Hariri ◽  
Fatemeh Darvish ◽  
Karen-Pacelye Mengue Me Ndong ◽  
Rachida Babouri ◽  
Rachida Babouri ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Activities ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Biologically Relevant ◽  
Gram Positive Bacteria ◽  
Disk Diffusion Assay ◽  
Selective Antimicrobial Activity ◽  
Diffusion Assay

The present study aims to investigate the in vitro antibacterial activities of several isophosphinoline-2-oxides that can be perceived as combined bio isosteres of coumarins and flavonoids. More specifically, antibacterial activity was evaluated against four bacterial strains, including the Gram-negative bacteria Escherichia coli and Pseudomonas aeruginosa and the Gram-positive bacteria Staphylococcus aureus and Enterococcus faecalis by using disk diffusion assay. Notably, isophosphinoline-2-oxide compounds showed promising and highly selective antimicrobial activity against S. aureus.

Classification of sensitizing and irritative potential in a combined in-vitro assay

2010 ◽  
Vol 245 (2) ◽  
pp. 211-218 ◽  
Author(s):  
Reinhard Wanner ◽  
Anna Sonnenburg ◽  
Maria Quatchadze ◽  
Maximilian Schreiner ◽  
Matthias Peiser ◽  
...  
Keyword(s):  
In Vitro Assay ◽  
Vitro Assay

Antibacterial secotirucallane triterpenes from the stem bark of Pseudocedrela kotschyi

2018 ◽  
Vol 73 (5-6) ◽  
pp. 241-246 ◽  
Author(s):  
Christèle Sorèle Mambou ◽  
Raymond Ngansop Nono ◽  
Jean Rodolphe Chouna ◽  
Jean-de-Dieu Tamokou ◽  
Pépin Nkeng-Efouet-Alango ◽  
...  
Keyword(s):  
2D Nmr ◽  
Stem Bark ◽  
Bark Extract ◽  
Gram Negative Bacteria ◽  
2D Nmr Spectroscopy ◽  
Dioic Acid ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Stem Bark Extract

AbstractThe antibacterial-guided investigation of the stem bark extract ofPseudocedrela kotschyiled to the isolation of a new secotirucallane triterpene derivative: 4-hydroxy-3,4-secotirucalla-7,24-dien-3,21-dioic acid (1), together with the known one: 3,4-secotirucalla-4(28),7,24-trien-3,21-dioic acid (2) and 3-methyl ester 3,4-secotirucalla-4(28),7,24-trien-3,21-dioic (3). The structures of the isolated compounds were elucidated on the basis of extensive 1D- and 2D-NMR spectroscopy. Extracts, fractions and compounds (1–3) were tested in vitro for antibacterial activity against two Gram positive bacteria (Bacillus subtilisandStaphylococcus aureusATCC 25923), and two Gram negative bacteria (Escherichia coliS2(1) andPseudomonas aeruginosa). The MeOH extract and the Hex/CH2Cl2(70:30) fraction showed significant levels of activity (MIC=64– 256 μg/mL) compared with the two reference drugs [ciprofloxacin: MIC (0.5–1 μg/mL) and amoxicillin: MIC (1–128 μg/mL)]. Moreover, the compound2isolated from this Hex/CH2Cl2(70:30) fraction had the greatest potential value againstS. aureus,E. coliandP. aeruginosa, with minimum inhibitory concentrations (MIC) ranging from 4–16 μg/mL.

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