A Simple Assessment of Partition Data for Correlating Structure and Biological Activity Using Thin-Layer Chromatography

Nature ◽  
1965 ◽  
Vol 208 (5010) ◽  
pp. 537-539 ◽  
Author(s):  
C. B. C. BOYCE ◽  
B. V. MILBORROW
1978 ◽  
Vol 76 (3) ◽  
pp. 619-627 ◽  
Author(s):  
J I Clark ◽  
D Garland

The synthesis of a fluorescent colchicine derivative permits the localization of colchicine-binding receptors in cells. Fluorescein colchicine (FC) was prepared by the addition of fluorescein isothiocyanate to deacetyl colchicine. The product, FC, was separated from the reactants by thin-layer chromatography (TLC). The purity of FC was demonstrated by TLC, UV spectral analysis, and analysis of the kinetics of photodecomposition. FC inhibited [3H] colchicine binding to purified brain tubulin. The biological activity of FC was compared to the activity of unlabeled colchicine on mitosis, motility, secretion, and myogenesis. The effects of FC were identical to those of unlabeled colchicine in all biological systems tested. The results demonstrate that FC may be substituted for colchicine in biological experiments without significant loss in specificity or effectiveness.


2010 ◽  
Vol 29 (1) ◽  
pp. 30-38 ◽  
Author(s):  
J.N. Eloff

Several Leonotis species are used widely for medicinal purposes in Africa. There have been drastic changes in the taxonomic treatment of Leonotis species during the past decade. Two species, L. dysophylla and L. microphylla occurring in Pretoria have been considered as varieties of the same species and as different species by different authors. Because Leonotis species are used widely as medicinal plants inter alia against bacterial infections, we decided to compare the chemical composition and antibacterial activity of four plants from each of two populations of the species. The chemical composition of acetone extracts of finely ground leaves was determined by thin layer chromatography followed by spraying with vanillin-sulphuric acid. There were hardly any differences between plants from the same population. There were major differences between the two species in the composition of pigments separated by thin layer chromatography and for compounds visualized with the vanillin-sulphuric acid spray reagent. This supported the viewpoint that the two species should not be considered as varieties. The major differences found in chemical composition indicate that chemical parameters may play an important role in resolving taxonomic differences. Because such a small quantity of material is needed, it may be feasible to analyze one or two leaves obtained from herbarium sheets as an additional taxonomic parameter. The antibacterial activity of the acetone extracts was determined using a two-fold serial dilution microplate method with tetrazolium violet as indicator of growth. The specific strains of the four most important nosocomial bacterial pathogens suggested by the United States National Committee for Clinical Laboratory Standards were used: Staphylococcus aureus (American Type Culture Collection 29213), Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 25922) and Enterococcus faecalis (ATCC 21212). The minimum inhibitory activity of the crude extract of L. microphylla was 58, 33, 113 and 15 µg/ml against the four pathogens respectively. The MIC of the L. dysophylla extracts were 110, 95, 113 and 63 µg/ml respectively. If the total activity was calculated by dividing the quantity in mg extracted from one gram of each species with the MIC, the following values were obtained against the respective bacteria using the L. microphylla extract: 700, 1400, 381 and 2100 ml/g. The values for the L. dysophylla extract were 381, 420, 420 and 700 ml/g. This means that if one gram of dried leaves of L. microphylla were extracted with acetone it could be diluted to 2100 ml and it would still kill E. faecalis. These results not only prove the possible use of chemical and biological activity as taxonomic markers, but also the potential value of L. microphylla acetone extracts in treating infections with P. aeruginosa and E. faecalis. The activity of the crude extract against P. aeruginosa was as good as or better than the activity of ampicillin, gentamicin, nitrofurantoin, trimethroptin or sulfi soxazole. The activity against E. faecalis was as good as or better than ampicillin, gentamicin, nitrofurantoin or sulfi soxazole. If the acetone leaf extract of L. microphylla is stable and not toxic there is a good possibility of developing a commercially useful antibacterial product from it. The results indicate the taxonomic value of chemical parameters and biological activity and support the view that the two taxa should be considered as different species.


2018 ◽  
Vol 9 (2) ◽  
Author(s):  
Đeni Vaštag ◽  
Suzana Apostolov ◽  
Borko Matijević ◽  
Gorana Mrđan

Thanks to the wide range of applications, azo dyes have a special place among synthetic dyes. Also, the application of azo dyes is conditioned by their impact on humans and the environment. Lipophilicity as one of the most important molecular descriptors indicating the potential biological activity of the compound is determined experimentally for selected derivatives of azo dyes using reversed phase thin-layer chromatography (RP TLC18 F254s) in the mixtures of water and two organic modifiers. By using the relevant software packages for the studied azo dyes, the values of partition coefficient (log P) were calculated as standard measure of lipophilicity, important pharamacokinetic predictors and the values of the effective concetration (EC50) as the criteria of acute toxicity for different test organisms. The relationships between chromatographic parameters (RM 0 and m) and calculated biological activity parameters were studied by linear regression analysis.


Molekul ◽  
2010 ◽  
Vol 5 (1) ◽  
pp. 41
Author(s):  
Mochamad Chasani ◽  
Eva Vaulina ◽  
Ponco Iswanto ◽  
Yayu Rahayu

Calanone is anticancer compound that is isolated from species Calophyllum. The biological activity of calanone againts leukemia cell L1210 is relatively low showed by IC50 value at 59.4 μg/mL. A compound have a high biological activity if the value of IC50 under 10 μg/mL. This research aimed to obtained calanone hydrat compound which has a higher activity to inhibit leukemia L1210 cancer cell growth. Calanone hydrat compound is got through with two step reaction, first step was protonated double bond by acetic acid reagent and the second step is nucleophilic addition by water. Initial analysis for the synthesize product compound is done with thin layer chromatography (TLC) using n-hexane and ethyl acetate 2:1 (v/v) eluent. Coloum Chomatography and recrystallization is used to pure the synthesize product compound with n-hexane and methylen chloride 1:1 (v/v) solvent. The result analyzed by thin layer chromatography. The synthesized product give Rf at 0.4545 and rendement 4.72% (w/w), forming of brownish yellow chromatic powder and melting point at 190oC-192oC. Identification structure of synthesize product compound is done with mass spectrometer. The result of mass spectrometer identification were moleculer ion M+-18 (M+ 424) with fragments m/e=409, m/e=395, m/e=381, m/e= 331, m/e=317, m/e=303, me/=176, m/e=105, and m/e=77. Citotoxicity test againts leukemia cell L1210 yield the value IC50 equal to 45.64 μg/mL.


2015 ◽  
Vol 32 (1) ◽  
pp. 13-17 ◽  
Author(s):  
Marian Jurzysta ◽  
Edmunt Nowacki

The 24 lucerne species were investigated for their saponin content by means of the thin layer chromatography method as well as by haemolytic and fungistatic tests. Wide interspecific differences were found in the content, the chemical composition and biological activity of saponins.


Author(s):  
H. R. Bolliger ◽  
M. Brenner ◽  
H. Gänshirt ◽  
Helmut K. Mangold ◽  
H. Seiler ◽  
...  

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