Buchholzia coriacea seed induce antifertility by interfering with steroidogenic enzymes and inflammatory cytokines in rat testis.

Buchholzia coriacea has been reported to possess antifertility activities but little is known of the mechanisms responsible. This study was therefore designed to examine the mechanism responsible for the action of Buchholzia coriacea. Eighteen male Wistar rats (180-200 g) were used for this study. They were grouped into 3 (n = 6) namely, Control, Methanolic fraction of Buchholzia coriacea (MFBC) 50 mg/kg, and MFBC 100 mg/kg administered orally with respective dosage. After 6 weeks of administration, rats were euthanized, serum collected, while testes, epididymis and prostate were excised and homogenized. Testicular protein and testosterone, aromatase and 5α-reductase enzyme, 3ß hydroxysteroid dehydrogenase (HSD), 17ß-HSD, interleukin (IL) 1ß, IL-10 and Prostatic specific enzyme antigen (PSA) were assessed and data analyzed with ANOVA. There were significant increases in 3ß-HSD and 17ß-HSD levels in the MFBC 50 mg/kg with corresponding decreases in MFBC 100 mg/kg when compared to control. IL-1 was decreased in both doses while IL-10 increased in both doses compared to control. 5-α reductase enzyme was significantly decreased in the MFBC 100 mg/kg relative to the control. Testicular protein, testosterone and aromatase enzyme were not significantly different at both doses compared to control. PSA was significantly increased in the MFBC 100 mg/kg but not the 50 mg/kg relative to control. MFBC exhibits antifertility properties by interfering with testicular enzymes and inflammatory cytokines.

Prevalence and associated factors of hypertension among type 2 diabetes mellitus patients in Lautech teaching hospital, Osogbo, Nigeria.

Background: We assessed the prevalence and risk factors of hypertension among type-2 Diabetes Mellitus (DM) patients attending Ladoke Akintola University of Technology (LAUTECH) Teaching Hospital, Osogbo, Osun State Nigeria. Methods and materials: A hospital-based retrospective study was conducted among 143 type-2 DM patients in LAUTECH Teaching Hospital. Hypertension was defined as systolic BP ≥140 and or diastolic BP ≥90. Data were analysed using descriptive statistics, chi-square, and binary logistic regression. Results: The mean age of the respondents was 56.2 ±15.79 years. Hypertension was common (32.1%) among type-2 DM participants. Respondents aged 45-64 years (OR= 5.96, 95%CI= 1.60 - 19.12) had the likelihood of being hypertensive. Type-2 DM patients who were not in union (AOR=6.64, 95%CI=1.79 - 24.52) were more likely to be hypertensive. The likelihood of hypertension was lower (AOR= 0.28, 95%CI=0.11 - 0.66) among participants who engaged in moderate physical activity compared to those who engaged in low physical activity. Conclusion: This study identified the age group 45-64 years, not being in a union and engagement in low physical activity as associated factors for hypertension among Diabetes Mellitus participants. Hypertension prevention/treatment should be considered in type-2 Diabetes Mellitus routine treatment.

Effect of the COVID-19 pandemic on blood donations and transfusions in Nigeria - A multi-facility study of 34 tertiary hospitals.

Background: The coronavirus disease 2019 (COVID-19) pandemic affected blood supplies globally. Mobile blood drive campaigns halted, and voluntary blood donations reduced, challenging available blood supplies. Furthermore, fears of virus transmission led to deferrals of elective surgeries and non-urgent clinical procedures with noticeable declines in blood donations and transfusions. Aims: We aimed to assess the effect of the COVID-19 pandemic on the number of blood donations and transfusions across the country by blood product type across various hospital departments. Materials and Methods: A retrospective descriptive study was conducted to determine the impact of the COVID-19 pandemic on blood services in 34 tertiary hospitals in Nigeria, comparing January to July 2019 (pre-COVID-19) to January to July 2020 (peri-COVID-19). Data were collected from the country's web-based software District Health Information System, Version 2 (DHIS2). Results: A 17.1% decline in numbers of blood donations was observed over the study period, especially in April 2020 (44.3%), a 21.7% decline in numbers of blood transfusions, especially in April 2020 (44.3%). The largest declines in transfusion were noted in surgery department for fresh frozen plasma (80.1%) [p = 0.012] and accident and emergency department transfusion of platelets (78.3%) [p = 0.005]. The least decline of statistical significance was observed in internal medicine transfusions of whole blood (19.6%) [p = 0.011]. Conclusions: The COVID-19 pandemic significantly affected the numbers of blood donations and transfusions in Nigeria. Strengthening blood services to provide various blood components and secure safe blood supplies during public health emergencies is therefore critical.

Effect of the COVID-19 pandemic on blood donations and transfusions in Nigeria ­ A multi-facility study of 34 tertiary hospitals

Background: The coronavirus disease 2019 (COVID-19) pandemic affected blood supplies globally. Mobile blood drive campaigns halted, and voluntary blood donations reduced, challenging available blood supplies. Furthermore, fears of virus transmission led to deferrals of elective surgeries and non-urgent clinical procedures with noticeable declines in blood donations and transfusions. Aims: We aimed to assess the effect of the COVID-19 pandemic on the number of blood donations and transfusions across the country by blood product type across various hospital departments. Materials and Methods: A retrospective descriptive study was conducted to determine the impact of the COVID-19 pandemic on blood services in 34 tertiary hospitals in Nigeria, comparing January to July 2019 (pre-COVID-19) to January to July 2020 (peri-COVID-19). Data were collected from the country's web-based software District Health Information System, Version 2 (DHIS2). Results: A 17.1% decline in numbers of blood donations was observed over the study period, especially in April 2020 (44.3%), a 21.7% decline in numbers of blood transfusions, especially in April 2020 (44.3%). The largest declines in transfusion were noted in surgery department for fresh frozen plasma (80.1%) [p = 0.012] and accident and emergency department transfusion of platelets (78.3%) [p = 0.005]. The least decline of statistical significance was observed in internal medicine transfusions of whole blood (19.6%) [p = 0.011]. Conclusions: The COVID-19 pandemic significantly affected the numbers of blood donations and transfusions in Nigeria. Strengthening blood services to provide various blood components and secure safe blood supplies during public health emergencies is therefore critical.

Micropore closure time is longer following microneedle application to skin of color.

Microneedles (MNs) allow transdermal delivery of skin-impermeable drugs by creating transient epidermal micropores, and micropore lifetime directly affects drug diffusion timeframes. Healthy subjects (n = 111) completed the study, self-identifying as Asian (n = 32), Bi-/multi-racial (n = 10), Black (n = 22), White (n = 23), Latino (n = 23), and Native American/Hawaiian (n = 1). L* was measured with tristimulus colorimetry to objectively describe skin lightness/darkness. MNs were applied to the upper arm; impedance and transepidermal water loss (TEWL) were measured at baseline and post-MN to confirm micropore formation. Impedance was repeated for 4 days to determine micropore lifetime. Post-MN changes in TEWL and impedance were significant in all groups (p < 0.05), confirming micropore formation regardless of skin type. Micropore lifetime was significantly longer in Blacks (66.5 ± 19.5 h) versus Asians (44.1 ± 14.0 h), Bi-/multi-racial (48.0 ± 16.0 h), and Whites (50.2 ± 2.6 h). Latinos (61.1 ± 16.1 h) had significantly longer micropore closure time versus Asians (44.1 ± 14.0 h). When categorizing data according to L*, micropore lifetime was significantly longer in darker skin. We report for the first time that micropore lifetime differences are present in human subjects of different ethnic/racial backgrounds, with longer micropore lifetime in skin of color. These results also suggest that objectively measured skin color is a better predictor of micropore lifetime than self-identified race/ethnicity.

Phospholipids modifications in human hepatoma cell lines (HepG2) exposed to silver and iron oxide nanoparticles.

Metallic nanoparticles such as silver (Ag NPs) and iron oxide (Fe3O4 NPs) nanoparticles are high production volume materials due to their applications in various consumer products, and in nanomedicine. However, their inherent toxicities to human cells remain a challenge. The present study was aimed at combining lipidomics data with common phenotypically-based toxicological assays to gain better understanding into cellular response to Ag NPs and Fe3O4 NPs exposure. HepG2 cells were exposed to different concentrations (3.125, 6.25, 12.5, 25, 50 and 100 µg/ml) of the nanoparticles for 24 h, after which they were assayed for toxic effects using toxicological assays like cytotoxicity, mutagenicity, apoptosis and oxidative stress. The cell membrane phospholipid profile of the cells was also performed using shotgun tandem mass spectrometry. The results showed that nanoparticles exposure resulted in concentration-dependent cytotoxicity as well as reduced cytokinesis-block proliferation index (CBPI). Also, there was an increase in the production of ROS and superoxide anions in exposed cells compared to the negative control. The lipidomics data revealed that nanoparticles exposure caused a modulation of the phospholipidome of the cells. A total of 155 lipid species were identified, out of which the fold changes of 23 were significant. The high number of differentially changed phosphatidylcholine species could be an indication that inflammation is one of the major mechanisms of toxicity of the nanoparticles to the cells.

Design and Characterization of Spray-Dried Chitosan-Naltrexone Microspheres for Microneedle-Assisted Transdermal Delivery.

Naltrexone (NTX) hydrochloride is a potent opioid antagonist with significant first-pass metabolism and notable untoward effects when administered orally or intramuscularly. Microneedle (MN)-assisted transdermal delivery is an attractive alternative that can improve therapeutic delivery to deeper skin layers. In this study, chitosan-NTX microspheres were developed via spray-drying, and their potential for transdermal NTX delivery in association with MN skin treatment was assessed. A quality-by-design approach was used to evaluate the impact of key input variables (chitosan molecular weight, concentration, chitosan-NTX ratio, and feed flow rate) on microsphere physical characteristics, encapsulation efficiency, and drug-loading capacity. Formulated microspheres had high encapsulation efficiencies (70%-87%), with drug-loading capacities ranging from 10%-43%. NTX flux through MN-treated skin was 11.6 ± 2.2 µg/cm2·h from chitosan-NTX microspheres, which was significantly higher than flux across intact skin. Combining MN-assisted delivery with the chitosan microsphere formulation enabled NTX delivery across the skin barrier, while controlling the dose released to the skin.

Cytotoxicity, mutagenicity, oxidative stress and mitochondrial impairment in human hepatoma (HepG2) cells exposed to copper oxide, copper-iron oxide and carbon nanoparticles.

The increasing application of nanomaterials in various fields such as drug delivery, cosmetics, disease detection, cancer treatment, food preservation etc. has resulted in high levels of engineered nanoparticles in the environment, thus leading to higher possibility of direct or indirect interactions between these particles and biological systems. In this study, the toxic effects of three commercially available nanomaterials; copper oxide nanoparticles, copper-iron oxide nanopowders and carbon nanopowders were determined in the human hepatoma HepG2 cells using various toxicological assays which are indicative of cytotoxicity (MTT and neutral red assays), mutagenicity (cytokinesis-block micronucleus assay), oxidative stress (total reactive oxygen species and superoxide anion production) and mitochondrial impairment (cellular oxygen consumption). There was increased cytotoxicity, mutagenicity, and mitochondrial impairment in the cells treated with higher concentrations of the nanomaterials, especially the copper oxide nanoparticles. The fold production of reactive oxygen species was similar at the concentrations tested in this study but longer exposure duration resulted in production of more superoxide anions. The results of this study showed that copper oxide nanoparticles are highly toxic to the human HepG2 cells, thus implying that the liver is a target organ in human for copper oxide nanoparticles toxicity.

Prospective insulin-based ophthalmic delivery systems for the treatment of dry eye syndrome and corneal injuries.

The presence of insulin (INS) receptors on the ocular surface (OS) and lacrimal gland (LG), and the high prevalence of dry eye syndrome (DES) and corneal lesions in diabetic patients suggest that INS is relevant for OS homeostasis and wound healing. The study aims at developing delivery systems for the topical administration of INS to the OS in order to improve INS local bioavailability and evaluate the influence of the delivery systems on DES in diabetic rats (DM) (n = 05/group). Chitosan microparticles (MP), chitosan/poloxamer gel (GEL) and MP-loaded GEL (GELMP), with or without INS were developed. Formulations were instilled into the eyes of diabetic rats (DM) for 15 days and the tear fluid volume, corneal cells morphology and cornea thickness were assessed and compared with an aqueous dispersion of INS (DISP-INS). All delivery systems had pH of about 6, osmolality suitable for topical application and positive zeta potential. The MPs with or without INS had sizes close to 4 µm, spherical morphology and INS encapsulation efficiency of 77 ±â€¯6%. DISP-INS and GELMP-INS formulations produced tear secretion amounts significantly higher than those receiving formulations containing no INS and similar to healthy animals. Cornea surface impression cytology showed that treatment with INS-delivery systems and not DISP-INS almost normalized cells morphology. Treatment with GELMP-INS increased INS by 2.5 in the LG and eyeball as compared to the groups treated with GEL-INS and MP-INS, while treatment with DISP-INS left no traces of drug in the eye after treatment termination. GEL and GELMP containing INS were also able to normalize the thickness of the corneal epithelia. In conclusion, GELMP-INS normalized tear fluid volume, corneal thickness, protected corneal cells morphology and increased ocular bioavailability of INS, making it a promising treatment strategy for DES and corneal lesions.

Evaluation of distribution, redox parameters, and genotoxicity in Wistar rats co-exposed to silver and titanium dioxide nanoparticles.

The increasing production of silver nanoparticles (AgNPs) and titanium dioxide nanoparticles (TiO2NPs) has resulted in their elevated concentrations in the environment. This study was, therefore, aimed at determining the distribution, redox parameters, and genotoxic effects in male Wistar rats that were treated with either AgNP or TiO2NP individually, as well as under a co-exposure scenario. Animals were exposed via oral gavage to either sodium citrate buffer (vehicle), 0.5 mg/kg/day TiO2NP, 0.5 mg/kg/day AgNP or a mixture of TiO2NPs and AgNPs. Exposure lasted 45 days after which rats were sacrificed, and tissue biodistribution of Ag and Ti measured. The blood concentration of glutathione (GSH) and activities of glutathione peroxidase (GPx) and catalase (CAT) were determined while the genotoxicity was analyzed using the comet assay in peripheral blood and liver cells. The tissue concentrations of Ag followed the order; blood > liver > kidneys while for Ti the order was kidneys > liver > blood. There was no significant change in the measured redox parameters in animals that were exposed to TiO2NPs. However, there was a significant increase in GSH levels accompanied by a reduction in the GPx activity in AgNP-treated and co-exposed groups. The individual or co-exposure to TiO2NP and AgNP did not markedly induce genotoxicity in blood or liver cells. Data showed that TiO2NP did not produce significant oxidative stress or genotoxicity in rats at the dose used in this study while the same dose level of AgNPs resulted in oxidative stress, but no noticeable adverse genotoxic effects.

NO Exchange for a Water Molecule Favorably Changes Iontophoretic Release of Ruthenium Complexes to the Skin.

Ruthenium (Ru) complexes have been studied as promising anticancer agents. Ru nitrosyl complex (Ru-NO) is one which acts as a pro-drug for the release of nitric oxide (NO). The Ru-aqueous complex formed by the exchange of NO for a water molecule after NO release could also possess therapeutic effects. This study evaluates the influence of iontophoresis on enhancing the skin penetration of Ru-NO and Ru-aqueous and assesses its applicability as a tool in treating diverse skin diseases. Passive and iontophoretic (0.5 mA·cm-2) skin permeation of the complexes were performed for 4 h. The amount of Ru and NO in the stratum corneum (SC), viable epidermis (VE), and receptor solution was quantified while the influence of iontophoresis and irradiation on NO release from Ru-NO complex was also evaluated. Iontophoresis increased the amount of Ru-NO and Ru-aqueous recovered from the receptor solution by 15 and 400 times, respectively, as compared to passive permeation. Iontophoresis produced a higher accumulation of Ru-aqueous in the skin layers as compared to Ru-NO. At least 50% of Ru-NO penetrated the SC was stable after 4 h. The presence of Ru-NO in this skin layer suggests that further controlled release of NO can be achieved by photo-stimulation after iontophoresis.

Hydrophilic polymeric nanoparticles prepared from Delonix galactomannan with low cytotoxicity for ocular drug delivery.

Delonix is a galactomannan polysaccharide extracted from the endosperm of Delonix regia plant. This study aims at the development of Delonix nanoparticle and assesses its potential for ocular delivery by evaluating its in-vitro stability, toxicity and cellular uptake. Fluorescent nanoparticles (BODIPY-loaded nanoparticles) were prepared by a Quality-by-Design modified nanoprecipitation technique. Optimized nanoparticles had mean sizes <240nm, PdI<0.2 and zeta potential of <-30mV. Mixture of surfactants with different hydrophilic-lipophilic balance controlled nanoparticle swelling. Nanoparticles, which were stable in the presence of simulated lachrymal fluid and lysozyme also sustained the release of BODIPY. In-vitro studies suggest no toxicity of the nanoparticles in concentration range of 100-1483.3µg/mL on retinal and corneal epithelial cells. Flow cytometry and confocal microscopy techniques showed that retinal cells but not corneal cells, uptake 18% of the nanoparticles. Therefore, Delonix nanoparticles could be a safe and promising tool for ocular drug delivery.

In-vitro anti-cholinesterase activity of essential oil from four tropical medicinal plants.

The chemical inhibition of acetyl-cholinesterase (AChE) is a potent strategy for addressing signal related neuropathology and natural products are potential sources of compounds with such properties. Essential oil extracts from leaf, seed, stem and rhizome of four medicinal plants [Aframomum melegueta K. Schum, Crassocephalum crepidioides (Benth S. More), Monodora myristica (Gaertn.), and Ocimum gratissimum (Linn)] were tested for acetyl-cholinesterase inhibitory activity (AChEI) using Ellman's colorimentric method and compared to a reference acetyl-cholinesterase inhibitor (galantamine). The seed (IC50 = 6.71 mg/l) and leaf (IC50 = 6.54 mg/l) extracts from O. gratissimum showed values that matched the capacity of the reference inhibitor (IC50 = 6.62 mg/l). The least potent extract was rhizome extracts of A. melegueta (IC50 = 28.97 mg/l) about four times that of the reference inhibitor. Principal component analysis (PCA) showed that the intrinsic properties (bioactive ingredient factor) of each extract (PC1 = 29.50%) was the most important factor defining the difference or similarity in potency to the reference acetyl-cholinesterase inhibitor while 'dose response' (PC2 = 11.38%) was the second most important factor. The outstanding AChEI property of O. gratissimum extracts could largely be attributed to the high monoterpene content while the weak potency of rhizome extracts of A. melegueta may be attributed to its predominant concentrations of sesquiterpenes. Since potency could be related to interaction between bioactive components, understanding the interaction between ratios of monoterpene and sesquiterpene in extracts could be important in determining their potency for AChEI.

Some Nigerian anti-tuberculosis ethnomedicines: a preliminary efficacy assessment.

ETHNOPHARMACOLOGICAL SIGNIFICANCE: Nigerian herbalists possess indigenous ethnomedicinal recipes for the management of tuberculosis and related ailments. A collaborative preliminary modern scientific evaluation of the efficacy of some Nigerian ethnomedicines used by traditional medicine practitioners (TMPs) in the management of tuberculosis and related ailments has been carried out. MATERIALS AND METHODS: Ethnomedicinal recipes (ETMs) were collected from TMPs from locations in various ecological zones of Nigeria under a collaborative understanding. The aqueous methanolic extracts of the ETMs were screened against Mycobacterium bovis, BCG and Mycobacterium tuberculosis strain H37Rv using the broth microdilution method. RESULTS: Extracts of ETMs screened against BCG showed 69% activity against the organism. The activities varied from weak, ≤2500 µg/mL to highly active, 33 µg/mL 64% of the extracts were active against Mycobacterium tuberculosis The activities of the extracts against Mycobacterium tuberculosis varied from weak, ≤2500 µg/mL to highly active, 128 µg/mL. There was 77% agreement in results obtained using BCG or Mycobacterium tuberculosis as test organisms. CONCLUSION: The results show clear evidence for the efficacy of the majority of indigenous Nigerian herbal recipes in the ethnomedicinal management of tuberculosis and related ailments. BCG may be effectively used, to a great extent, as the organism for screening for potential anti-Mycobacterium tuberculosis agents. A set of prioritization criteria for the selection of plants for initial further studies for the purpose of antituberculosis drug discovery research is proposed.

Material and tableting properties of Azadirachta indica gum with reference to official acacia gum.

This study determined the material and tableting properties of Azadirachta indica gum (NMG) relative to acacia gum (ACA). The morphological properties were assessed with size and shape factors of aspect ratio, roundness, irregularity and equivalent-circle-diameter. The tableting properties of the gums were determined using compressional characteristics, tensile strength (TS), brittle fracture index (BFI) and crushing-strength-friability/disintegration-time ratio (CSFR/DT). The results suggest that NMG possesses larger, irregular and more elongated particles than ACA. The onset and amount of plastic deformation occurring in NMG was faster and higher, respectively, than in ACA. The result shows that, although ACA tablets were stronger, their tendency to cap/laminate was higher than in NMG tablets. The NMG tablets possess lower DT than those of ACA, while the CSFR/DT result suggests that a better balance exists between the strength and weakness of NMG tablets. The study concluded that NMG can be a useful excipient in tablet formulation.

Microarchitectural adaptations in the stomach of African tree pangolin (Manis tricuspis) / Adaptaciones microarquitecturales en el estómago del pangolin africano (Manis tricuspis)

The microarchitecture of the pangolin's stomach favouring the high chitinous diet has been less waived into, despite extensive morphological investigations. Histological analysis of the microanatomy will provide powerful tools for interpretation to yield reliable insights. We investigated this by fixing the tissues in 10 percent formol saline for histological analysis. Serial sections at 5 micron m thickness were subjected to general staining methods for light microscopic study (Haematoxylin and eosin, Van Gieson's and Verhoeff's). The results revealed basic structural arrangements in their coats, with a modification of the epithelial lining of cardia and fundus into stratified squamous keratinized epithelium. These modifications were also reflected in the distribution of collagen and elastic fibers in the various layers (coats) of the stomach. The present study has shown that there was an adaptation of the stomach of African tree pangolin to its diet as reflected in the microarchitectural configuration.

La micro arquitectura del estómago de los pangolines que favorece la alta dieta de chitinous sido poco tomada en cuenta, a pesar de las amplias investigaciones morfológicas. El análisis histológico de la microanatomía proporcionará herramientas de gran importancia para la interpretación, junto con dar una información confiable. Se investigó mediante la fijación de los tejidos en solución salina de formol al 10 por ciento para análisis histológico. Las serie de secciones fueron sometidos a métodos de tinción estándar para el estudio con microscopía de luz (hematoxilina y eosina, Van Gieson y Verhoeff s). Los resultados revelaron adaptaciones estructurales básicas en sus capas, con una modificación del revestimiento epitelial del cardias y fundus en epitelio escamoso estratificado (queratinizado). Estas modificaciones también se reflejan en la distribución de colágeno y fibras elásticas en las diversas capas del estómago. El presente estudio ha demostrado que es una adaptación del estómago a la dieta como se refleja en la configuración de la microarquitectura.

Tirucallane triterpenes from the leaf extract of Entandrophragma angolense.

From the leaves of Entandrophragma angolense, three triterpenoidal compounds were isolated and structurally elucidated by mass and NMR spectroscopy. They belong to the tirucallane group but two of them possess the rare seco-ring-A feature. The phytochemical data are discussed from a chemotaxonomic and biogenetic points of view.