Antibacterial activity of flavonoids from the stem bark of Erythrina caffra thunb.

The antibacterial activity of the stem bark of Erythrina caffra Thunb. was investigated against different bacterial strains. The antibacterial activity was determined by a micro broth dilution assay. Antibacterial compounds were isolated and identified using a Bruker Avance III LPO NMR spectrometer. Four known flavonoids, abyssione-V 4'-O-methyl ether, 6,8-diprenylgenistein, alpinumisoflavone and burttinone, were isolated. All the compounds were active against both Gram-negative and Gram-positive bacteria. The minimum inhibitory concentration values obtained (MIC) ranged from 3.9 µg/mL to 125 µg/mL. This is the first report of antibacterial activity of burttinone and the isolation of these compounds from E. caffra.

New role for crinamine as a potent, safe and selective inhibitor of human monoamine oxidase B: In vitro and in silico pharmacology and modeling.

ETHNOPHARMACOLOGICAL RELEVANCE: The development of selective inhibitors of monoamine oxidase B (MAO-B) has been essential in treating Parkinson's disease. However, the apparent hepatotoxicity and drug-drug interactions of current inhibitors accentuate the need for the development of novel pharmacotherapies. Crossyne guttata (L.) D. & U. Müll-Doblies is used frequently by Rastafarian bush doctors to treat alcoholism, a disorder which is also accentuated by MAO. OBJECTIVE: The study sought to isolate, identify and characterise the biologically active constituents of C. guttata based on their ability to inhibit the MAO enzymes. MATERIALS AND METHODS: Column chromatography was used to isolate the biologically active alkaloids of C. guttata. The ability of the alkaloids to inhibit the biotransformation of 4-aminoantipyrine by the MAO enzymes was evaluated in vitro. In silico docking was conducted using AutoDock Vina server while the pharmacokinetic properties of the compounds were evaluated using SwissADME. RESULTS: Chromatographic separation of an ethanolic fraction of C. guttata yielded the alkaloids crinamine 1 and epibuphanisine 2. 1 and 2 along with structurally related alkaloids haemanthamine 3 and haemanthidine 4 were evaluated for their ability to inhibit the action of isozymes of MAO in vitro. Alkaloids effected submicromolar IC50 values against MAO-B, the most potent of which being crinamine 1 (0.014 µM) > haemanthidine 4 (0.017 µM) > epibuphanisine 2 (0.039 µM) > haemanthamine 3 (0.112 µM). Binding energies of the alkaloids correlated well with their inhibitory potential with crinamine displaying the best binding efficacy and binding energy score with MAO-B. DISCUSSION AND CONCLUSION: Crinamine and epibuphanisine exhibited potent and selective inhibitory activity towards MAO-B. After comprehensive in silico investigations encompassing robust molecular docking analysis, the drug-like attributes and safety of the alkaloids suggest the crinamine is a potentially safe drug for human application.

Antiplasmodial diterpenoid from the leaves of Hyptis suaveolens.

Bioactivity-guided fractionation of the petroleum ether extract of the leaves of Hyptis suaveolens, widely used in Traditional Medicine, has led to the isolation of an abietane-type diterpenoid endoperoxide, 13 alpha-epi-dioxiabiet-8(14)-en-18-ol, displaying high antiplasmodial activity (IC(50) 0.1 microg/ml).

Antimicrobial, antioxidant, mutagenic and antimutagenic activities of Distephanus angulifolius and Ormocarpum trichocarpum.

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves of Distephanus angulifolius and Ormocarpum trichocarpum are used for treating stomach-related ailments in traditional medicine. AIMS OF THE STUDY: The present study evaluated the antibacterial, antioxidant, mutagenic and antimutagenic properties of extracts obtained from the leaves of Distephanus angulifolius and Ormocarpum trichocarpum. MATERIALS AND METHODS: The microtitre bioassay was used to determine the antibacterial activity against three Gram-positive and three Gram-negative bacteria. Antioxidant activity was determined using the free-radical scavenging and ß-carotene-linoleic acid model assays. The safety and possible protective properties of the extracts were investigated using Ames test. RESULTS: Dichloromethane fractions of both plants displayed a broad-spectrum antibacterial activity with minimum inhibitory concentrations ranging from 0.16 to 0.63 mg/ml. A dose-dependent antioxidant activity was recorded in both plant species. All the evaluated samples showed no mutagenic as well as weak or no antimutagenic properties in the absence of exogenous metabolic activation. CONCLUSION: The results demonstrated the antibacterial and antioxidant activities of the leaves obtained from the two plant species. Furthermore, the data provides a rationale for the use of the plant species in treating stomach-related ailments in traditional medicine.

In vitro antimicrobial, anthelmintic and cyclooxygenase-inhibitory activities and phytochemical analysis of Leucosidea sericea.

ETHNOPHARMACOLOGICAL RELEVANCE: Leucosidea sericea is used as a vermifuge and in the treatment of ophthalmia by various tribes in southern African countries. AIM OF THE STUDY: The study aimed at screening leaves and stems of Leucosidea sericea for pharmacological activity and validating the plant's traditional use. A general phytochemical screening was also carried out. MATERIALS AND METHODS: Petroleum ether (PE), dichloromethane (DCM), ethanol (EtOH) and water extracts of the plant parts were investigated for antimicrobial, anthelmintic and cyclooxygenase (COX) inhibitory activities. Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus), Gram-negative bacteria (Escherichia coli and Klebsiella pneumoniae) and Candida albicans were used for the antimicrobial evaluation. Caenorhabditis elegans was used for the anthelmintic assay using the microdilution technique. Cyclooxygenase-1 and -2 (COX-1 and -2) were used to evaluate the anti-inflammatory potential of the plant extracts. Phytochemical analysis for phenolic compounds, including gallotannins, condensed tannins and flavonoids was done using 50% methanol extracts of the leaves and stems employing spectrophotometric methods. RESULTS: The leaf extracts exhibited broad spectrum antibacterial activity ranging from 0.025 to 6.25mg/ml. The most noteworthy minimum inhibitory concentration (MIC) of 0.025 mg/ml was exhibited by PE and DCM leaf extracts against Bacillus subtilis and Staphylococcus aureus, respectively. In the anthelmintic assay, the best minimum lethal concentration (MLC) value of 0.26 mg/ml was observed for the DCM and EtOH leaf extracts. Both leaf and stem organic solvent extracts exhibited high to moderate inhibition against COX-1 and -2 at a screening concentration of 250 microg/ml. At lower concentrations, the extracts displayed a dose-dependent inhibition, with the lowest IC(50) values of 0.06 microg/ml (COX-1) and 12.66 microg/ml (COX-2) exhibited by the PE extract of the leaves. Generally, the leaf extracts exhibited better pharmacological activities and contained higher amounts of phenolic compounds than the stem extracts. Alkaloids and saponins were only detected in the leaf and stem extracts, respectively. CONCLUSION: The reported results support the local use of Leucosidea sericea against eye infections and as a vermifuge. The pharmacological activities exhibited by the leaf extracts are probably due to their higher phenolic levels.

Cytotoxic effects of five commonly abused skin toning (bleaching) creams on Allium cepa root tip mitosis.

The Allium test was used to study the cytotoxic effects of five commonly abused skin toning creams--Ikb, Tura, Top gel, Dorot and Mililo. These creams are commonly used by some black skinned people (especially the females) as skin lightening (bleaching) agents. The results showed that all the five bleaching creams were mito-depressive in action. They exhibited both chromatoclassic and mitoclassic effects. Their depressive effects were found to increase with duration of treatment. The induced abnormalities included chromosome contraction, spindle breakages, c-metaphase, star anaphase, chromosome stickiness and sticky bridges, precocious chromosome movement as well as endomitosis. It is suggested that since all eukaryotic cells are basically the same, these observed abnormalities could be similar to the effects these chemicals have on human skin when they are applied. Some of these are known to cause alteration in melanin formation as well as the biosynthesis of the enzyme tyrosinase. Furthermore, since certain points on the chromosomes called fragile sites have been implicated in oncogenesis, the observed abnormalities may be part of (or include) the switching on mechanisms of such genes, which could be responsible for the transformation of normal skin cells to malignant cells in those who abuse these creams.