Insecticidal activities and chemical composition of the essential oil from Tarchonanthus camphoratus (L.), leaves against Sitophilus zeamais Motschulsky, and Sitophilus oryzae (L.)

The essential oil of Tarchonanthus camphoratus dry leaves growing in Kwa-Zulu Natal, South Africa was obtained by hydrodistillation and evaluated for its repellent effect, contact and fumigation toxicity against both Sitophilus zeamais and Sarocladium oryzae. Chemical composition of the essential oil was analysed by gas chromatography mass spectrometry (GC/MS). The study revealed that the essential oil of T. camphoratus had no contact and fumigation toxicity against stored insect pests, S. zeamais and S. oryzae. The oil, however, showed good repellent activity of over 50% after 24 h for all the concentrations used on both S. zeamais and S. oryzae. A total of 27 compounds accounting for 73% of the total oil composition were identified of which sesquiterpene hydrocarbons, (59.18%), were the most dominant. These results suggest that the essential oil of T. camphoratus could be considered a potential control agent of stored grain pests as a repellent

Anti-oxidant, anti-inflammatory and antiacetylcholinesterase activity of betulinic acid and 3β- acetoxybetulinic acid from Melaleuca bracteata ‘Revolution Gold’

Purpose: To evaluate the anti-oxidant, anti-inflammatory and anti-acetylcholine esterase activities of betulinic acid (BA) and 3β- acetoxybetulinic acid (BAA) from Melaleuca bracteata. ‘Revolution Gold’.Methods: Betulinic acid was isolated from the ethyl acetate extract of M. braceteata while BAA was synthesized by acetylation of BA. Structural elucidation of the compounds was achieved by spectroscopic methods. Antioxidant potential was determined using superoxide dismustase (SOD) and catalase assay kits while iron chelation activity assessed with ferrozin. Anti-inflammatory activity was determined using cotton pellet-induced granuloma rat model. Cyclooxygenase (COX) activity evaluated by COX kits; acetylcholine kit was used for anti-acetylcholinesterase (ACHE) study.Results: The compounds significantly (p < 0.05) dose-dependently inhibited ACHE and inflammatory activity. They also significantly decreased the inhibition of SOD, catalase activity but increased iron chelation activities in a dose-dependent manner. However, BAA showed higher activity than BA for all the parameters. BAA also had a greater inhibitory effect on COX-2 than on COX-1. BAA (IC50, 0.88 mg/mL) showed better iron chelation than citric acid (0.96 ± 0.04) and EDTA (1.04 ± 0.03), the positive control.Conclusion: BA and BAA possess anti-ACHE, anti-inflammatory, antioxidant and anti-COX activities. Structural modification of BAA influences its biological activities. Therefore, BAA can potentially serve as a scaffold in synthesizing potent neurodegeneration drugs.Keywords: Betulinic acid, 3β-Acetoxybetulinic acid, Antioxidant, Anti-inflammatory, Antiacetylcholinesterase, Melaleuca bracteata. ‘Revolution Gold

In silico and in vitro assessment of the anti-β-amyloid aggregation and anti-cholinesterase activities of Ptaeroxylon obliquum and Bauhinia bowkeri extracts

DATA AVAILABILITY : Data will be made available on request.BACKGROUND : Alzheimer’s disease (AD) is the most common form of dementia and dementia constitutes the fifth leading cause of mortality across the globe. Available treatment modalities and drugs have abysmally failed to curtail AD. This study evaluated the mitigation of Aβ aggregation and anti-cholinesterase activities with the crude extracts of Ptaeroxylon obliquum and Bauhinia bowkeri. Computational studies of the most abundant phytochemicals from the crude extracts of both plants with proteins were investigated. The phytochemical composition of the different crude extracts (hexane, DCM, and ethanol) of the plants were analyzed with FTIR and GC-MS. The inhibitory potential of the extracts on BACE-1 and cholinesterase activities was determined with both computational molecular docking studies and in vitro enzyme assays. Their anti-aggregation properties were confirmed with Thioflavin-T assay and TEM. RESULTS : The in silico studies revealed that though thunbergol and cyclotetradecatriene (the major constituents of the extracts) inhibited all the proteins, the latter exhibited the best inhibitory potential. The in vitro results showed that while the dichloromethane (DCM) extract of P. obliquum had the highest butyrylcholinesterase (BuChE) inhibitory activity (1.77 µg/ml), the hexane and ethanol extract of B. bowkeri exhibited the highest β-site amyloid precursor cleaving enzymes-1 (BACE-1) (30.4 µg/ml) and acetylcholinesterase (AChE) (58.11 µg/ml) inhibitory efficacy, respectively. The ethanol extract (160 μg/ml) of B. bowkeri had the most efficacious anti-aggregation activity. CONCLUSIONS : This study suggests that the plants could possess neuroprotective effects and could also be sources of anti-AD novel drugs.http://www.elsevier.com/locate/ejbthj2024BiochemistryGeneticsMicrobiology and Plant PathologySDG-03:Good heatlh and well-bein

Antithrombotic, anticoagulant and antiplatelet activity of betulinic acid and 3β-acetoxybetulinic acid from Melaleuca bracteata ‘Revolution Gold’ (Myrtaceae) Muell leaf

Purpose: To investigate the antithrombotic, anticoagulant and antiplatelet activity of betulinic acid (BA) and 3β-acetoxybetulinic acid (BAA) from Melaleuca bracteata ‘Revolution Gold’.Methods: Betulinic acid was isolated from the ethyl acetate extract of M. bracteata leaves by column chromatography, from which BAA was subsequently synthesized by acetylation. Structural elucidation of the compounds was conducted using mass spectrometry (MS), infra-red (IR) spectroscopy and nuclear magnetic resonance (NMR). The antithrombotic potential of the compounds was assessed using chromogenic substrate. Anticoagulation studies were carried using bleeding tail time assay in a rat model. Plasma-rich platelets from rats were employed for platelet aggregation studies using light microscope.Results: The compounds significantly (p < 0.05) showed antithrombotic activities in a dose-dependent manner. BAA showed significantly (p < 0.05) higher half-maximal concentration (IC50) value of 1.10 ± 0.03 mg/mL than BA (2.36 ± 0.09 mg/mL) and aspirin (2.65 ± 0.01 mg/mL) which served as positive control. The compounds exhibited anticoagulation activity with poor bleeding time, compared to aspirin. Likewise, the compounds attenuated platelets aggregation induced by thrombin.Conclusion: BAA displays better antithrombotic, antiplatelet, and anticoagulant activities than BA. Therefore, it may be a promising remedy for the management of cardiovascular events.Keywords: Betulinic acid, Thrombin, Anticoagulation, Antiplatelet, Aspirin, Platelet

In vitro and in vivo antioxidant potentials of the methanolic crude extract from Inula glomerata Oliv. & Hiern (Asteraceae) and Salacia kraussii (Harv.) Harv (Celastraceae)

Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitro as well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p<0.05) diminished the level of malondialdehyde, augmented catalase activities and elevated glutathione levels. However, SOD activities were significantly boosted in a dose-dependent manner by the crude extracts. Therefore, I. glomerata and S. kraussii possess antioxidant properties, hence, can serve as a therapeutic modality in the treatment of oxidative stress-induced erectile dysfunction.https://blacpma.ms-editions.cl/index.php/blacpmapm2021BiochemistryGeneticsMicrobiology and Plant Patholog

The triterpene, methyl-3β-hydroxylanosta-9,24-dien-21-oate (RA3), attenuates high glucose-induced oxidative damage and apoptosis by improving energy metabolism

BACKGROUND: Hyperglycemia-induced cardiovascular dysfunction has been linked to oxidative stress and accelerated apoptosis in the diabetic myocardium. While there is currently no treatment for diabetic cardiomyopathy (DCM), studies suggest that the combinational use of anti-hyperglycemic agents and triterpenes could be effective in alleviating DCM. HYPOTHESIS: To investigate the therapeutic effect of methyl-3β-hydroxylanosta-9,24-dien-21-oate (RA3), in the absence or presence of the anti-diabetic drug, metformin (MET), against hyperglycemia-induced cardiac injury using an in vitro H9c2 cell model. METHODS: To mimic a hyperglycemic state, H9c2 cells were exposed to high glucose (HG, 33 mM) for 24 h. Thereafter, the cells were treated with RA3 (1 μM), MET (1 μM) and the combination of MET (1 μM) plus RA3 (1 μM) for 24 h, to assess the treatments therapeutic effect. RESULTS: Biochemical analysis revealed that RA3, with or without MET, improves glucose uptake via insulindependent (IRS-1/PI3K/Akt signaling) and independent (AMPK) pathways whilst ameliorating the activity of antioxidant enzymes in the H9c2 cells. Mechanistically, RA3 was able to alleviate HG-stimulated oxidative stress through the inhibition of reactive oxygen species (ROS) and lipid peroxidation as well as the reduced expression of the PKC/NF-кB cascade through decreased intracellular lipid content. Subsequently, RA3 was able to mitigate HG-induced apoptosis by decreasing the activity of caspase 3/7 and DNA fragmentation in the cardiomyoblasts. CONCLUSION: RA3, in the absence or presence of MET, demonstrated potent therapeutic properties against hyperglycemia-mediated cardiac damage and could be a suitable candidate in the prevention of DCM.South African National Treasury and National Research Foundation.https://www.elsevier.com/locate/phymedpm2022BiochemistryGeneticsMicrobiology and Plant Patholog

Global, regional, and national burden of diabetes from 1990 to 2021, with projections of prevalence to 2050: a systematic analysis for the Global Burden of Disease Study 2021

This online publication has been corrected. The corrected version first appeared at thelancet.com on September 28, 2023BACKGROUND : Diabetes is one of the leading causes of death and disability worldwide, and affects people regardless of country, age group, or sex. Using the most recent evidentiary and analytical framework from the Global Burden of Diseases, Injuries, and Risk Factors Study (GBD), we produced location-specific, age-specific, and sex-specific estimates of diabetes prevalence and burden from 1990 to 2021, the proportion of type 1 and type 2 diabetes in 2021, the proportion of the type 2 diabetes burden attributable to selected risk factors, and projections of diabetes prevalence through 2050. METHODS : Estimates of diabetes prevalence and burden were computed in 204 countries and territories, across 25 age groups, for males and females separately and combined; these estimates comprised lost years of healthy life, measured in disability-adjusted life-years (DALYs; defined as the sum of years of life lost [YLLs] and years lived with disability [YLDs]). We used the Cause of Death Ensemble model (CODEm) approach to estimate deaths due to diabetes, incorporating 25 666 location-years of data from vital registration and verbal autopsy reports in separate total (including both type 1 and type 2 diabetes) and type-specific models. Other forms of diabetes, including gestational and monogenic diabetes, were not explicitly modelled. Total and type 1 diabetes prevalence was estimated by use of a Bayesian meta-regression modelling tool, DisMod-MR 2.1, to analyse 1527 location-years of data from the scientific literature, survey microdata, and insurance claims; type 2 diabetes estimates were computed by subtracting type 1 diabetes from total estimates. Mortality and prevalence estimates, along with standard life expectancy and disability weights, were used to calculate YLLs, YLDs, and DALYs. When appropriate, we extrapolated estimates to a hypothetical population with a standardised age structure to allow comparison in populations with different age structures. We used the comparative risk assessment framework to estimate the risk-attributable type 2 diabetes burden for 16 risk factors falling under risk categories including environmental and occupational factors, tobacco use, high alcohol use, high body-mass index (BMI), dietary factors, and low physical activity. Using a regression framework, we forecast type 1 and type 2 diabetes prevalence through 2050 with Socio-demographic Index (SDI) and high BMI as predictors, respectively. FINDINGS : In 2021, there were 529 million (95% uncertainty interval [UI] 500–564) people living with diabetes worldwide, and the global age-standardised total diabetes prevalence was 6·1% (5·8–6·5). At the super-region level, the highest age-standardised rates were observed in north Africa and the Middle East (9·3% [8·7–9·9]) and, at the regional level, in Oceania (12·3% [11·5–13·0]). Nationally, Qatar had the world’s highest age-specific prevalence of diabetes, at 76·1% (73·1–79·5) in individuals aged 75–79 years. Total diabetes prevalence—especially among older adults—primarily reflects type 2 diabetes, which in 2021 accounted for 96·0% (95·1–96·8) of diabetes cases and 95·4% (94·9–95·9) of diabetes DALYs worldwide. In 2021, 52·2% (25·5–71·8) of global type 2 diabetes DALYs were attributable to high BMI. The contribution of high BMI to type 2 diabetes DALYs rose by 24·3% (18·5–30·4) worldwide between 1990 and 2021. By 2050, more than 1·31 billion (1·22–1·39) people are projected to have diabetes, with expected age-standardised total diabetes prevalence rates greater than 10% in two super-regions: 16·8% (16·1–17·6) in north Africa and the Middle East and 11·3% (10·8–11·9) in Latin America and Caribbean. By 2050, 89 (43·6%) of 204 countries and territories will have an age-standardised rate greater than 10%. INTERPRETATION : Diabetes remains a substantial public health issue. Type 2 diabetes, which makes up the bulk of diabetes cases, is largely preventable and, in some cases, potentially reversible if identified and managed early in the disease course. However, all evidence indicates that diabetes prevalence is increasing worldwide, primarily due to a rise in obesity caused by multiple factors. Preventing and controlling type 2 diabetes remains an ongoing challenge. It is essential to better understand disparities in risk factor profiles and diabetes burden across populations, to inform strategies to successfully control diabetes risk factors within the context of multiple and complex drivers.Bill & Melinda Gates Foundation.http://www.thelancet.comam2024School of Health Systems and Public Health (SHSPH)SDG-03:Good heatlh and well-bein

In silico and in vitro assessment of the anti-β-amyloid aggregation and anti-cholinesterase activities of Ptaeroxylon obliquum and Bauhinia bowkeri extracts

Background: Alzheimer’s disease (AD) is the most common form of dementia and dementia constitutes the fifth leading cause of mortality across the globe. Available treatment modalities and drugs have abysmally failed to curtail AD. This study evaluated the mitigation of Aβ aggregation and anti-cholinesterase activities with the crude extracts of Ptaeroxylon obliquum and Bauhinia bowkeri. Computational studies of the most abundant phytochemicals from the crude extracts of both plants with proteins were investigated. The phytochemical composition of the different crude extracts (hexane, DCM, and ethanol) of the plants were analyzed with FTIR and GC-MS. The inhibitory potential of the extracts on BACE-1 and cholinesterase activities was determined with both computational molecular docking studies and in vitro enzyme assays. Their anti-aggregation properties were confirmed with Thioflavin-T assay and TEM. Results: The in silico studies revealed that though thunbergol and cyclotetradecatriene (the major constituents of the extracts) inhibited all the proteins, the latter exhibited the best inhibitory potential. The in vitro results showed that while the dichloromethane (DCM) extract of P. obliquum had the highest butyrylcholinesterase (BuChE) inhibitory activity (1.77 µg/ml), the hexane and ethanol extract of B. bowkeri exhibited the highest β-site amyloid precursor cleaving enzymes-1 (BACE-1) (30.4 µg/ml) and acetylcholinesterase (AChE) (58.11 µg/ml) inhibitory efficacy, respectively. The ethanol extract (160 μg/ml) of B. bowkeri had the most efficacious anti-aggregation activity. Conclusions: This study suggests that the plants could possess neuroprotective effects and could also be sources of anti-AD novel drugs.How to cite: Ojo MC, Mosa RA, Osunsanmi FO, et al. In silico and in vitro assessment of the anti-β-amyloid aggregation and anti-cholinesterase activities of Ptaeroxylon obliquum and Bauhinia bowkeri extracts. Electron J Biotechnol 2024;68. https://doi.org/10.1016/j.ejbt.2023.11.004

<em>Melaleuca bracteata</em> var. Revolution Gold (Myrtaceae) Essential Oil: Chemical Composition, Antibacterial, Membrane Damage, Antiplatelet Aggregation and Antiacetylcholinesterase Activities

Melaleuca bracteata var. Revolution Gold (a cultivar of Melaleuca bracteata) is an ornamental plant, which has been used in traditional medicine for the treatment of several diseases. Till moment, information is scanty on the biological activities of the essential oil from the plant. The water-distilled essential oil was analyzed by gas chromatography and gas chromatography-mass spectrometry. Antibacterial activity of the oil was evaluated by paper disc diffusion and micro-dilution methods. Cell membrane damage was assay using cytosolic lactate dehydrogenase released method. Platelet aggregation inhibitory activity was separately evaluated on Adenosine diphosphate, collagen, epinephrine and thrombin induced aggregation. Thirteen components representing 95.3% of the total oil were identified from the essential oil. Phenylpropanoids (82.9%) constitute the predominant class of compounds in the oil. On the whole, the oil displayed strong antibacterial action towards Staphylococcus aureus, moderate activity on Bacillus cereus and some strains of Escherichia coli. The lactate dehydrogenase released (0.78–47%) depicted the oil to exhibit low levels of membrane damage. The percentage platelet aggregation inhibition for the four platelet agonists was concentration dependent with thrombin > collagen > ADP > epi-nephrine. The acetylcholinesterase inhibitory activity (9.16%) indicated that the essential oil was not effective against the enzyme