13 research outputs found
Self-Assembled Lipid Cubic Phase and Cubosomes for the Delivery of Aspirin as a Model Drug
Three-dimensionally organized lipid cubic self-assemblies and derived oil-in-water emulsions called ācubosomesā are attractive for various biotechnological applications due to their ability to be loaded with functional molecules and their associated sustained release properties. Here, we employed both of these lipid-based systems for the delivery of a model drug, aspirin, under comparable conditions. Studies were performed by varying drug-to-lipid ratio and the type of release medium, water and phosphate buļ¬er saline (PBS). Release rates were determined using UVāvis spectroscopy, and small-angle X-ray scattering was used to conļ¬rm the type of self-assembled nanostructures formed in these lipid systems. The release from the bulk lipid cubic phase was sustained as compared to that of dispersed cubosomes, and the release in PBS was more eļ¬cient than in water. The tortuosity of the architecture, length of the diļ¬usion pathway, type of nanostructure, and physicochemical interaction with the release media evidently contribute to these observations. This work is particularly important as it is the ļ¬rst report where both of these nanostructured lipid systems have been studied together under similar conditions. This work provides important insights into understanding and therefore controlling the release behavior of lipid-based drug nanocarriers
Isolation and characterisation of endocrine disruptor nonylphenol-using bacteria from South Africa
Published ArticleEndocrine disrupting chemicals (EDCs) are synthetic chemicals that alter the function of endocrine systems in animals including humans. EDCs are considered priority pollutants and worldwide research is ongoing to develop bioremediation strategies to remove EDCs from the environment. An understanding of indigenous microorganisms is important to design efficient bioremediation strategies. However, much of the information available on EDCs has been generated from developed regions. Recent studies have revealed the presence of different EDCs in South African natural resources, but, to date, studies analysing the capabilities of microorganisms to utilise/degrade EDCs have not been reported from South Africa. Here, we report for the first time on the isolation and enrichment of six bacterial strains from six different soil samples collected from the Mpumalanga Province, which are capable of utilising EDC nonylphenol as a carbon source. Furthermore, we performed a preliminary characterisation of isolates concerning their phylogenetic identification and capabilities to degrade nonylphenol. Phylogenetic analysis using 16S rRNA gene sequencing revealed that four isolates belonged to Pseudomonas and the remaining two belonged to Enterobacteria and Stenotrophomonas. All six bacterial species showed degradation of nonylphenol in broth cultures, as HPLC analysis revealed 41ā46% degradation of nonylphenol 12 h after addition. The results of this study represent the beginning of identification of microorganisms capable of degrading nonylphenol, and pave the way for further exploration of EDC-degrading microorganisms from South Africa
In Vitro Antibacterial, Antioxidant and Anti-Inflammatory Effects of Senecio Asperulus and Gunnera Perpensa from Mohaleās Hoek, Lesotho
Original ArticleBackground: Traditional medicinal plants have been widely used to treat or manage various
ailments for centuries in Lesotho. With an increase in multi drug resistance and undesired
adverse events to current drugs challenges, there is a need for alternative drugs. Aim: In
this study we aimed at the investigation of antibacterial, antioxidant and anti-inflammatory
effects of Senecio asperulus and Gunnera perpensa roots extracted in three solvents of
different polarities. Materials and Methods: Antibacterial activity was determined using
the disc diffusion method, while antioxidant activity was determined using free radical
scavenging of 2,2-diphenyl-1-picrylhydrazyl and the ferric reducing antioxidant power assay.
The Lipopolysaccharide (LPS) stimulated RAW 264.7 mouse macrophage in vitro model was
used to evaluate the anti-inflammatory activity of both plants. Resveratrol was used as a
positive control. Results: Methanol extracts of Senecio asperulus inhibited microbial growth
even at the lowest concentration of 50 Ī¼g/ml. Senecio asperulus dichloromethane extract was
active on most bacteria with MICās between 50 Ī¼g/ml and 500 Ī¼g/ml. However, the water and
methanol extracts of Gunnera perpensa had no activity against all organisms tested. Aqueous
extracts of Senecio asperulus and Gunnera perpensa showed free radical scavenging activity
yielding EC50 values of 100 Ī¼g/ml and 25 Ī¼g/ml, respectively. The aqueous extracts of Senecio
asperulus showed moderate anti-inflammatory activity from 50 to 200 Ī¼g/ml. while the
methanol extract was at 200 Ī¼g/ml and with no cytotoxicity. No anti-inflammatory activity was
observed from all Gunnera perpensa extracts using LPS-induced macrophages, this suggests
that this species may be using other mechanisms for anti-inflammatory activity. Conclusion:
The antibacterial, antioxidant and anti-inflammatory activities observed from water extracts
of Senecio asperulus support its ethnomedicinal use for the management of inflammation
related diseases
Natural compounds isolated from African mistletoes (loranthaceae) exert anti-inflammatory and acetylcholinesterase inhibitory potentials : in vitro and in silico studies
DATA AVAILABILITY STATEMENT: All data generated or analysed during this study are included in this published article.Please read abstract in article.The Central University of Technology operational expenses and the National Research Foundation (NRF) of South Africa.https://www.mdpi.com/journal/applsciParaclinical Science
A Comprehensive Review On Zinc(Ii) Complexes As Anti-Diabetic Agents: The Advances, Scientific Gaps And Prospects
ArticleZinc has gained notable attention in the development of potent anti-diabetic agents, due to its role in insulin
storage and secretion, as well as its reported insulin mimetic properties. Consequently, zinc(II) has been complexed
with numerous organic ligands as an adjuvant to develop anti-diabetic agents with improved and/or
broader scope of pharmacological properties. This review focuses on the research advances thus far to identify
the major scientific gaps and prospects. Peer-reviewed published data on the anti-diabetic effects of zinc(II)
complexes were sourced from different scientific search engines, including, but not limited to āPubMedā,
āGoogle Scholarā, āScopusā and ScienceDirect to identify potent anti-diabetic zinc(II) complexes. The complexes
were subcategorized according to their precursor ligands. A critical analysis of the outcomes from published
studies shows promising leads, with Zn(II) complexes having a ātri-facetā mode of exerting pharmacological
effects. However, the promising leads have been flawed by some major scientific gaps. While zinc(II) complexes
of synthetic ligands with little or no anti-diabetic pharmacological history remain the most studied (about 72 %),
their toxicity profile was not reported, which raises safety concerns for clinical relevance. The zinc(II) complexes
of plant polyphenols; natural ligands, such as maltol and hinokitiol; and supplements, such as ascorbic acid (a
natural antioxidant), L-threonine and L-carnitine, showed promising insulin mimetic and glycemic control
properties but remain understudied and lack clinical validation, in spite of their minimal safety concerns and
health benefits. A paradigm shift toward probing (including clinical studies) supplements, plant polyphenol and
natural ligands as anti-diabetic zinc(II) complex is, therefore, recommended. Also, promising anti-diabetic Zn(II)
complexes of synthetic ligands should undergo critical toxicity evaluation to address possible safety concerns
In vitro antiproliferative, anti-inflammatory effects and molecular docking studies of natural compounds isolated from Sarcocephalus pobeguinii (Hua ex PobƩg)
DATA AVAILABILITY STATEMENT : The original contributions presented in the study are included in
the article/Supplementary Material, further inquiries can be directed
to the corresponding authors.BACKGROUND : Sarcocephalus pobeguinii (Hua ex PobƩg) is used in folk medicine to
treat oxidative-stress related diseases, thereby warranting the investigation of its
anticancer and anti-inflammatory properties. In our previous study, the leaf extract
of S. pobeguinii induced significant cytotoxic effect against several cancerous cells
with high selectivity indexes towards non-cancerous cells.
AIM : The current study aims to isolate natural compounds from S. pobeguinii, and
to evaluate their cytotoxicity, selectivity and anti-inflammatory effects as well as
searching for potential target proteins of bioactive compounds.
METHODS : Natural compounds were isolated from leaf, fruit and bark extracts of S.
pobeguinii and their chemical structures were elucidated using appropriate
spectroscopic methods. The antiproliferative effect of isolated compounds was
determined on four human cancerous cells (MCF-7, HepG2, Caco-2 and
A549 cells) and non-cancerous Vero cells. Additionally, the anti-inflammatory
activity of these compounds was determined by evaluating the nitric oxide (NO)
production inhibitory potential and the 15-lipoxygenase (15-LOX) inhibitory
activity. Furthermore, molecular docking studies were carried out on six
putative target proteins found in common signaling pathways of inflammation
and cancer.
RESULTS : Hederagenin (2), quinovic acid 3-O-[Ī±-D-quinovopyranoside] (6) and
quinovic acid 3-O-[Ī²-D-quinovopyranoside] (9) exhibited significant cytotoxic
effect against all cancerous cells, and they induced apoptosis in MCF-7 cells by
increasing caspase-3/-7 activity. (6) showed the highest efficacy against all
cancerous cells with poor selectivity (except for A549 cells) towards noncancerous
Vero cells; while (2) showed the highest selectivity warranting its potential safety as a chemotherapeutic agent. Moreover, (6) and (9) significantly inhibited NO production in LPS-stimulated RAW 264.7 cells which
could mainly be attributed to their high cytotoxic effect. Besides, the mixture
nauclealatifoline G and naucleofficine D (1), hederagenin (2) and chletric acid (3)
were active against 15-LOX as compared to quercetin. Docking results showed that
JAK2 and COX-2, with the highest binding scores, are the potential molecular
targets involved in the antiproliferative and anti-inflammatory effects of bioactive
compounds.
CONCLUSION : Overall, hederagenin (2), which selectively killed cancer cells with
additional anti-inflammatory effect, is the most prominent lead compound which
may be further investigated as a drug candidate to tackle cancer progression.The Central University of Technology operational expenses and the National Research Foundation (NRF), South Africa. The APC was funded by the Central University of Technology research expenses (TM).http://www.frontiersin.org/Pharmacologyam2024Paraclinical SciencesSDG-03:Good heatlh and well-bein
Characterisation and identification of phenolic compounds from Asparagus laricinus and Senecio asperulus
482-489Nature has been a good supply of medicinal agents for thousands of years, and more than 50% of modern drugs are
derived from natural sources such as plants. Asparagus laricinus and Senecio asperulus have been used in traditional
remedies to treat inflammation-related disorders and cancer. This study aimed to determine the chemical composition of
A. laricinus and S. asperulus crude extracts using Liquid chromatography-mass spectrometry (LC-MS/MS) based
untargeted analysis. The LC-MS-based untargeted analysis showed the phytochemical profile of A. laricinus cladodes
and S. asperulus roots, of which twenty-nine phytochemicals from different chemical classes were annotated,
including organic acids, phenolic acids, flavonoids, and other unknown compounds. Both these plants are used
as traditional medicines, and their pharmacological benefits are due to their phytochemical profile and high
phenolic content
Phytoconstituents of <i>Androstachys johnsonii</i> Prain Prevent Reactive Oxygen Species Production and Regulate the Expression of Inflammatory Mediators in LPS-Stimulated RAW 264.7 Macrophages
According to a survey, the medicinal use of Androstachys johnsonii Prain is kept secret by traditional healers. Considering that inflammation and oxidative stress are major risk factors for the progression of various chronic diseases and disorders, we resolved to investigate the antioxidant and anti-inflammatory potentials of A. johnsonii using in vitro and cell-based assays. The antioxidant activity of A. johnsonii hydroethanolic leaf extract (AJHLE) was evaluated using the ABTS, DPPH, and FRAP assays. Its cytotoxic effect was assessed on RAW 264.7 macrophages using an MTT assay. Then, its anti-inflammatory effect was evaluated by measuring the NO production and 15-LOX inhibitory activities. Moreover, its preventive effect on ROS production and its regulatory effect on the expression of pro-inflammatory mediators such as IL-1Ī², IL-10, TNF-Ī±, and COX-2 were determined using established methods. AJHLE strongly inhibited radicals such as ABTSā¢+, DPPHā¢, and Fe3+-TPTZ with IC50 values of 9.07 Āµg/mL, 8.53 Āµg/mL, and 79.09 Āµg/mL, respectively. Additionally, AJHLE induced a significant (p A. johnsonii is a potential source of therapeutic agents against oxidative stress and inflammatory-related diseases
Isolation and characterisation of endocrine disruptor nonylphenol-using bacteria from South Africa
Endocrine disrupting chemicals (EDCs) are synthetic chemicals that alter the function of endocrine systems in animals including humans. EDCs are considered priority pollutants and worldwide research is ongoing to develop bioremediation strategies to remove EDCs from the environment. An understanding of indigenous microorganisms is important to design efficient bioremediation strategies. However, much of the information available on EDCs has been generated from developed regions. Recent studies have revealed the presence of different EDCs in South African natural resources, but, to date, studies analysing the capabilities of microorganisms to utilise/degrade EDCs have not been reported from South Africa. Here, we report for the first time on the isolation and enrichment of six bacterial strains from six different soil samples collected from the Mpumalanga Province, which are capable of utilising EDC nonylphenol as a carbon source. Furthermore, we performed a preliminary characterisation of isolates concerning their phylogenetic identification and capabilities to degrade nonylphenol. Phylogenetic analysis using 16S rRNA gene sequencing revealed that four isolates belonged to Pseudomonas and the remaining two belonged to Enterobacteria and Stenotrophomonas. All six bacterial species showed degradation of nonylphenol in broth cultures, as HPLC analysis revealed 41ā46% degradation of nonylphenol 12 h after addition. The results of this study represent the beginning of identification of microorganisms capable of degrading nonylphenol, and pave the way for further exploration of EDC-degrading microorganisms from South Africa.
Significance:
First report of endocrine disruptor nonylphenol-using bacteria from South Africa
Six bacterial species capable of using nonylphenol as a carbon source were isolated
Results will pave the way for further exploration of endocrine disruptors degrading microbes from South Afric
Isolation and characterisation of endocrine disruptor nonylphenol-using bacteria from South Africa
Endocrine disrupting chemicals (EDCs) are synthetic chemicals that alter the function of endocrine systems in animals including humans. EDCs are considered priority pollutants and worldwide research is ongoing to develop bioremediation strategies to remove EDCs from the environment. An understanding of indigenous microorganisms is important to design efficient bioremediation strategies. However, much of the information available on EDCs has been generated from developed regions. Recent studies have revealed the presence of different EDCs in South African natural resources, but, to date, studies analysing the capabilities of microorganisms to utilise/degrade EDCs have not been reported from South Africa. Here, we report for the first time on the isolation and enrichment of six bacterial strains from six different soil samples collected from the Mpumalanga Province, which are capable of utilising EDC nonylphenol as a carbon source. Furthermore, we performed a preliminary characterisation of isolates concerning their phylogenetic identification and capabilities to degrade nonylphenol. Phylogenetic analysis using 16S rRNA gene sequencing revealed that four isolates belonged toĀ PseudomonasĀ and the remaining two belonged toĀ EnterobacteriaĀ andĀ Stenotrophomonas. All six bacterial species showed degradation of nonylphenol in broth cultures, as HPLC analysis revealed 41ā46% degradation of nonylphenol 12 h after addition. The results of this study represent the beginning of identification of microorganisms capable of degrading nonylphenol, and pave the way for further exploration of EDC-degrading microorganisms from South Africa.
Significance:Ā
ā¢ First report of endocrine disruptor nonylphenol-using bacteria from South Africa
ā¢ Six bacterial species capable of using nonylphenol as a carbon source were isolated
ā¢ Results will pave the way for further exploration of endocrine disruptors degrading microbes from South Afric