Prognostic Significance of Nuclear Factor kappa B (p65) among Breast Cancer Patients in Cape Coast Teaching Hospital.

Breast cancer is the most prevalent cancer among African women, with high mortality rates in Ghana. Nuclear factor kappa B (NF-kB) has been associated with tumor progression in breast cancer. However, its clinical validation is controversial and understudied with no known published data on NF-kB (p65) among breast cancer patients in Ghana and other African countries. This study assessed the prognostic significance of NF-kB(p65) expression and its association with various clinicopathological features in breast cancer patients. 90 formalin-fixed breast cancer tissues and 15 normal breast tissues were used to determine the expression of NF-kB (p65) using immunohistochemistry. We explored the correlation between expression of NF-kB (p65) and clinicopathological features. NF-kB (p65) was expressed in 86.7% of breast cancer tissues. There was a significant relationship between NF-kB (p65) expression and tumor grade, proliferation index (Ki67), and molecular subtype. High NF-kB (p65) expression in tumor grade 3 was about 10 times that of grade 1 (54.2% versus 5.1%), and Ki67 > 20 was 79.7% compared to 20.3% for Ki67 ≤ 20. Patients with triple-negative breast cancer (TNBC) had 49.1% overexpression of NF-kB (p65) compared to 17%, 25.4% and 8.5% for luminal A, luminal B, and HER 2 cases respectively. This study demonstrates that NF-kB (p65) was highly expressed among breast cancer patients at Cape Coast Teaching Hospital, Ghana especially in TNBC. NF-kB (p65) could serve as a biomarker for cancer stage, progression, prognosis, and as a therapeutic target.

Genomic diversity and antimicrobial resistance in clinical Klebsiella pneumoniae isolates from tertiary hospitals in Southern Ghana.

OBJECTIVES: Comprehensive data on the genomic epidemiology of hospital-associated Klebsiella pneumoniae in Ghana are scarce. This study investigated the genomic diversity, antimicrobial resistance patterns, and clonal relationships of 103 clinical K. pneumoniae isolates from five tertiary hospitals in Southern Ghana-predominantly from paediatric patients aged under 5 years (67/103; 65%), with the majority collected from urine (32/103; 31%) and blood (25/103; 24%) cultures. METHODS: We generated hybrid Nanopore-Illumina assemblies and employed Pathogenwatch for genotyping via Kaptive [capsular (K) locus and lipopolysaccharide (O) antigens] and Kleborate (antimicrobial resistance and hypervirulence) and determined clonal relationships using core-genome MLST (cgMLST). RESULTS: Of 44 distinct STs detected, ST133 was the most common, comprising 23% of isolates (n = 23/103). KL116 (28/103; 27%) and O1 (66/103; 64%) were the most prevalent K-locus and O-antigen types. Single-linkage clustering highlighted the global spread of MDR clones such as ST15, ST307, ST17, ST11, ST101 and ST48, with minimal allele differences (1-5) from publicly available genomes worldwide. Conversely, 17 isolates constituted novel clonal groups and lacked close relatives among publicly available genomes, displaying unique genetic diversity within our study population. A significant proportion of isolates (88/103; 85%) carried resistance genes for ≥3 antibiotic classes, with the blaCTX-M-15 gene present in 78% (n = 80/103). Carbapenem resistance, predominantly due to blaOXA-181 and blaNDM-1 genes, was found in 10% (n = 10/103) of the isolates. CONCLUSIONS: Our findings reveal a complex genomic landscape of K. pneumoniae in Southern Ghana, underscoring the critical need for ongoing genomic surveillance to manage the substantial burden of antimicrobial resistance.

Pharmacognostic characterization, wound healing and toxicity assessment of the stem bark of Xylia evansii Hutch (Leguminosae).

Xylia evansii is widely used in traditional medicine to stop bleeding gums and treat wounds. This study was undertaken to assess the wound healing activity and toxicity profile of the stem bark methanol extract of X. evansii (XES). Wound healing activity was determined by the dermal excision model in rats. The free radical scavenging capacity, antioxidant activity, total phenolic and flavonoid contents were evaluated by the 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging, total antioxidant capacity (TAC), aluminum chloride colorimetric and Folin Ciocalteu methods respectively. Acute and sub-acute oral toxicity assessment was performed following the Organization for Economic Co-operation and Development guidelines. Significant (p < 0.05) dose-dependent wound healing effect, similar to that of 1 % silver sulphadiazine was elicit by the 10, 15 and 20 %w/w XES ointments. The highest effect was demonstrated by XES 20 %w/w which resulted in 98.3 % wound surface closure by day 9 of treatment (p < 0.0001). The total phenolic and flavonoid contents were determined to be 381.2 ± 12.57 mg/g gallic acid equivalent (GAE) and 460 ± 29.07 mg/g quercetin equivalent respectively. XES exhibited remarkable free radical scavenging effect (IC50 = 68.13 ± 1.87 µg/mL) and had a total antioxidant capacity of 279.2 ± 32.08 mg/g GAE. The LD50 of XES was estimated to be > 5000 mg/kg. In sub-acute toxicity, 28 days treatment with XES (250, 500, 1000 mg/kg body weight) did not result in any significant (p > 0.05) change in the body weight or weight of the heart, lung, spleen, liver and kidneys. The haematological and biochemical profiles of XES-treated rats were not significantly (p > 0.05) affected after 4-weeks treatment with XES, except for platelet count which increased significantly (p < 0.0001) in a non-dose-dependent manner. Histopathological examination did not reveal any toxic effect to liver cells, however at 1000 mg/kg XES, slight abnormalities were identified in the glomeruli. Microscopy of the powdered stem bark displayed calcium oxalate crystals, pitted vessels and lignified fibres. Tannins, flavonoids, coumarins, saponins, triterpenes and alkaloids were identified in the bark. This is the first report on the wound healing potential and safety profile of X. evansii, giving scientific credence to its use in traditional medicine.

Ethnobotanical Survey and Cercaricidal Activity Screening of Medicinal Plants Used for Schistosomiasis Treatment in Atwima-Nwabiagya District, Ashanti Region, Ghana.

This study focused on documenting and evaluating the cercaricidal activity of medicinal plants used for schistosomiasis treatment in an endemic area in Ghana. Through semistructured questionnaires, personal interviews with herbalists in communities surrounding the Barekese dam in the Atwima-Nwabiagya district, where the disease is endemic, were carried out. Thirty medicinal plants distributed in 19 families were reported to be used for schistosomiasis treatment in the survey. Information on the plants, including scientific names, common names, families, and the used plant part were recorded. The families Apocynaceae and Euphorbiaceae recorded the highest number of plants (14% each), followed by Asteraceae (10%), Loranthaceae (7%), and Rubiaceae (7%). In vitro cercaricidal activity of methanol extracts of nine out of the thirty plants was performed by exposing human Schistosoma mansoni cercariae obtained from Biomphalaria pfeifferi to various concentrations of extracts over a duration of 240 minutes. All the plants tested demonstrated time- and concentration-dependent cercaricidal activity. With lethality being set at <1000 µg/mL, the cercaricidal activity in order of decreasing potency was as follows: Withania somnifera (LC50 = 1.29) > Balanites aegyptiaca (LC50 = 7.1) > Xylia evansii (LC50 = 11.14) > Jathropha multifida (LC50 = 12.9) > Justicia flava (LC50 = 22.9) > Anopyxis klaineana (LC50 = 182.81) > Ximenia americana (LC50 = 194.98) > Loranthus lecardii (LC50 = 223.87) > Bridelia tenufolia (LC50 = 309.03) > Zanthoxylium zanthoxyloides (LC50 = 851.94). Phytochemicals, including alkaloids, tannins, triterpenes, saponins, phytosterols, and flavonoids were identified in the plants. The result of this study gives scientific credence to the traditional use of these plants in the treatment of schistosomiasis and proves that the rich botanical knowledge of medicinal plants provides an incredible starting point for the discovery of new anti-schistosomal drugs for the local population.

Realizing near white and warm light emission of cuprous iodide complexes by alkyl-isomerization of ligands.

Four novel all-in-one structured cuprous iodide hybrid materials are presented. Isomerization of the alkyl chain on the ligand improved material thermal stability and regulated their luminescence to warm and near-white light emission, with the internal quantum yield increasing from 5% to 83%. This provides a reasonable route for designing white light emitting cuprous iodide materials for solid-state lighting in future.

Antibacterial, Resistance Modulation, Anti-Biofilm Formation, and Efflux Pump Inhibition Properties of Loeseneriella africana (Willd.) N. Halle (Celastraceae) Stem Extract and Its Constituents.

This study investigated the antibacterial, resistance modulation, biofilm inhibition, and efflux pump inhibition potentials of Loeseneriella africana stem extract and its constituents. The antimicrobial activity was investigated by the high-throughput spot culture growth inhibition (HT-SPOTi) and broth microdilution assays. The resistance modulation activity was investigated using the anti-biofilm formation and efflux pump inhibition assays. Purification of the extract was carried out by chromatographic methods, and the isolated compounds were characterized based on nuclear magnetic resonance, Fourier transform infrared and mass spectrometry spectral data and comparison with published literature. The whole extract, methanol, ethyl acetate, and pet-ether fractions of L. africana all showed antibacterial activity against the test bacteria with MICs ranging from 62.5 to 500.0 µg/mL The whole extract demonstrated resistance modulation effect through strong biofilm inhibition and efflux pump inhibition activities against S. aureus ATCC 25923, E. coli ATCC 25922 and P. aeruginosa ATCC 27853. Chromatographic fractionation of the ethyl acetate fraction resulted in the isolation of a triterpenoid (4S,4αS,6αR,6ßS,8αS,12αS,12ßR,14αS,14ßR)-4,4α,6ß,8α,11,11,12ß,14α-Octamethyloctadecahydropicene-1,3(2H,4H)-dione) and a phytosterol (ß-sitosterol). These compounds showed antibacterial activity against susceptible bacteria at a MIC range of 31-125 µg/mL and potentiated the antibacterial activity of amoxicillin (at » MIC of compounds) against E. coli and P. aeruginosa with modulation factors of 32 and 10, respectively. These compounds also demonstrated good anti-biofilm formation effect at a concentration range of 3-100 µg/mL, and bacterial efflux pump inhibition activity at ½ MIC and » MIC against E. coli and P. aeruginosa. Loeseneriella africana stem bark extracts and constituents elicit considerable antibacterial, resistance modulation, and biofilm and efflux pump inhibition activities. The results justify the indigenous uses of L. africana for managing microbial infections.

Evaluation of the anti-inflammatory and antioxidant potential of the stem bark extract and some constituents of Aidia genipiflora (DC.) dandy (rubiaceae).

Aidia genipiflora (DC.) Dandy (Rubiaceae) is used to treat various microbial and inflammatory conditions by traditional healers in West African countries. However, there is no information on anti-inflammatory potential of A. genipiflora. This work therefore provides information on the anti-inflammatory and the antioxidant activities of the stem bark extracts and some bioactive constituents of Aidia genipiflora. Method: The anti-inflammatory activities of the extracts and compounds from A. genipiflora were investigated using the carrageenan-induced footpad oedema assay and the egg albumin denaturation assay. The antioxidant activities of the extract and compounds were investigated using the DPPH radical scavenging assay and the phosphomolybdenum total antioxidant capacity assay. The whole extract of A. genipiflora was also investigated for its acute oral toxicity using the fixed-dose procedure described by the Organization for Economic Cooperation Development guidelines. Result: The whole extract showed no acute toxicity effect and the LD50 was estimated to be greater than 3000 mg/kg body weight. The whole extract, methanol, and ethyl acetate fractions (30, 100, and 300 mg/kg) showed in vivo anti-inflammatory activity with respective percentage inhibition of oedema of 45.11 ± 3.41, 31.12 ± 3.42 and 29.28 ± 3.58 (p < 0.001) at the highest dose of 300 mg/kg. Diclofenac, used as a reference drug, gave a % inhibition of 48.94 ± 3.58. The compounds isolated from A. genipiflora demonstrated in-vitro anti-inflammatory activity at the IC50 range (16-96 µg/mL) compared to diclofenac (IC50 of 74.48 µg/mL). Oleanonic acid (AG1) and D-mannitol (AG4) further demonstrated in vivo anti-inflammatory activity (ED50 = 20.61 ± 1.29; 23.51 ± 1.26 mg/kg respectively) which was less potent compared to diclofenac (ED50 = 12.50 ± 1.41 mg/kg) in the carrageenan-induced oedema assay. The whole extract, pet. ether, ethyl acetate, and methanol fractions of A. genipiflora exhibited DPPH scavenging activities with respective IC50 of 222.2, 169.7, 121.5, and 40.7 µg/mL. The whole extract of A. genipiflora exhibited considerable total antioxidant capacity with respective values of 248.5 mg/g of ascorbic acid equivalent. All the compounds exhibited low DPPH scavenging activity with IC50 (64-86 µg/mL), compared to ascorbic acid (IC50 of 3.13 ± 1.20 µg/mL). These results highlight the anti-inflammatory and antioxidant activities of Aidia genipiflora stem bark extract and its constituents as evidence to support its traditional uses.

Antibacterial, Antibiofilm, and Efflux Pump Inhibitory Properties of the Crude Extract and Fractions from Acacia macrostachya Stem Bark.

Microbial infections remain a public health problem due to the upsurge of bacterial resistance. In this study, the antibacterial, antibiofilm, and efflux pump inhibitory activities of the stem bark of Acacia macrostachya, an indigenous African medicinal plant, were investigated. In traditional medicine, the plant is used in the treatment of microbial infections and inflammatory conditions. A crude methanol extract obtained by Soxhlet extraction was partitioned by column chromatography to obtain the petroleum ether, ethyl acetate, and methanol fractions. Antibacterial, efflux pump inhibition and antibiofilm formation activities were assessed by the high-throughput spot culture growth inhibition (HT-SPOTi), ethidium bromide accumulation, and the crystal violet retention assay, respectively. The minimum inhibitory concentrations (MICs) of the crude extract and major fractions ranged from 250 to ≥500 µg/mL. At a concentration of 3.9-250 µg/mL, all extracts demonstrated >80% inhibition of biofilm formation in S. aureus. In P. aeruginosa, the EtOAc fraction showed the highest antibiofilm activity (59-69%) while the pet-ether fraction was most active against E. coli biofilms (45-67%). Among the test samples, the crude extract, methanol, and ethyl acetate fractions showed remarkable efflux pump inhibition in S. aureus, E. coli, and P. aeruginosa. At ½ MIC, the methanol fraction demonstrated significant accumulation of EtBr in E. coli having superior efflux inhibition over the standard EPIs: chlorpromazine and verapamil. Tannins, flavonoids, triterpenoids, phytosterols, coumarins, and saponins were identified in preliminary phytochemical studies. Stigmasterol was identified in the EtOAc fraction. This study justifies the use of A. macrostachya in the treatment of infections in traditional medicine and highlights its potential as a source of bioactive compounds that could possibly interact with some resistance mechanisms in bacteria to combat antimicrobial resistance.

Amphimas pterocarpoides harms.: An Evaluation of flavonoid and phenolic contents, wound healing, anthelmintic and antioxidant activities of the leaves and stem bark.

The present study evaluated the wound healing, anthelmintic and antioxidant potentials of crude methanol extracts and fractions (petroleum ether, ethyl acetate and methanol) of the leaves and stem bark of Amphimas pterocarpoides. Wound healing activity was determined by the dermal excision model in rats; anthelmintic activity was evaluated by the adult worm motility test using the adult Indian worm, Pheretima postuma. Total flavonoid, phenolic content and antioxidant activity were assessed by the aluminum chloride colorimetric, Folin Ciocalteu, 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging and total antioxidant capacity (TAC) assays respectively. HPLC/UV fingerprints were developed for quality control. The maximum amount of phenolics and flavonoids were detected in the methanol fractions of the stem bark (225.0 ± 20.0 mg/g gallic acid equivalent (GAE) and 201.0 ± 1.41 mg/g quercetin equivalent (QCE) respectively) and leaves (84.54 ± 1.36 mg/g GAE and 130.7 ± 1.71 mg/g QCE, respectively). Both leaf and bark displayed remarkable free radical scavenging and TAC with the highest effect given by the methanol fractions. Significant (p < 0.05) wound contraction was achieved by topical application of the leaf (APL) and stem bark (APS) ointments (5-15%) with >90 % wound surface closure for 1% silver sulphadiazine, APS 15% and APL 10% treated groups by day 15. APL and APS demonstrated a concentration- and time-dependent paralysis and mortality of the P. posthuma with APL (6.25 mg/mL) causing worm paralysis at 82.60 min and death at 93 min, better than 10 mg/mL albendazole (paralysis at 76.30 min; death at 117 min). Tannins, triterpenoids, phytosterols, flavonoids, saponins and coumarins were detected in the leaves and bark. The results have proven the potential of A. pterocarpoides as a wound healing and anthelmintic agent, giving scientific credence to its use in traditional medicine.

Fruits of Vitex doniana sweet: toxicity profile, anti-inflammatory and antioxidant activities, and quantification of one of its bioactive constituents oleanolic acid.

BACKGROUND: Vitex doniana Sweet fruit, an under-utilised crop specie of Ghana, has not been validated for its ethnomedical use in managing inflammatory conditions. Therefore, the study sought to investigate its anti-inflammatory and antioxidant activities as well as isolate and quantify one of its active constituents. MATERIALS AND METHODS: In-vivo anti-inflammatory activity of the methanol fruit extract was evaluated using the carrageenan-induced oedema model in chicks. The in-vitro antioxidant property was also investigated using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. The acute and subacute toxicity studies of the fruit extract were evaluated in rodent models. RESULTS: No signs of autonomic and central nervous system stimulation/depression were recorded. The LD50 by oral route, was estimated to be beyond 3000 mg/kg. Subacute studies revealed an increase in red blood cell and lymphocyte counts. Liver enzymes, serum proteins and bilirubin levels did not significantly increase. The crude extracts at doses of 10, 30 and 100 mg/kg inhibited paw oedema considerably. The ethyl acetate fraction showed the highest antioxidant activity (IC50 = 99.35 ± 0.77 µg/mL). Oleanolic acid, isolated from the ethyl acetate extract, showed significant anti-inflammatory and antioxidant activities. A sensitive high-performance liquid chromatography method for the detection and estimation of oleanolic acid, as a biomarker compound for V. doniana fruit, was developed and validated for quality assurance purposes. CONCLUSION: The extract of V. doniana fruits possesses considerable anti-inflammatory and antioxidant properties and was non-toxic under laboratory conditions.

Investigating Ghanaian Allium Species for Anti-Infective and Resistance-Reversal Natural Product Leads to Mitigate Multidrug-Resistance in Tuberculosis.

The bulbs of Allium species are a known source of antibacterial phytochemicals. Anti-infective, efflux pump and biofilm inhibitory activities of bulb extracts of selected Ghanaian shallots Allium cepa var aggregatum were evaluated using the HT-SPOTi assay and other whole-cell phenotypic screening techniques to determine their possible mechanisms of action. Ethanol and aqueous extracts of white A. cepa inhibited the growth of Mycobacterium smegmatis mc2 155 and Escherichia coli, respectively. The majority of the Allium extracts significantly (p < 0.05) exhibited efflux pump inhibitory activity against all the acid-fast, Gram-positive and Gram-negative strains used. Hexane and chloroform extract of the pink A. cepa and the aqueous extract of the white A. cepa significantly inhibited M. smegmatis biofilm formation. For Pseudomonas aeruginosa, the inhibition was observed at 250 µg/mL for the aqueous extract (~77.34%) and 125 µg/mL for the hexane extract (~76.51%). The results suggest that Ghanaian shallots could potentially be useful when further developed to tackle antimicrobial resistance, particularly in tuberculosis (TB).

Myrianthus libericus: Possible mechanisms of hypoglycaemic action and in silico prediction of pharmacokinetics and toxicity profile of its bioactive metabolite, friedelan-3-one.

The hypoglycaemic and anti-hyperlipidaemic effects of the 70% ethanol stem bark extract of Myrianthus libericus (MLB), used traditionally in the management of diabetes in Ghana, was evaluated in this study using streptozotocin (45 mg/kg)-induced diabetic rats. In vitro hypoglycaemic activities of the extract and one of its principal compounds, friedelan-3-one were then investigated using α-amylase inhibitory and glucose uptake assay in C2C12 myotubes. In silico analysis of the pharmacokinetic and toxicity properties of the compound was also performed. MLB significantly (p < 0.001) reduced the elevated blood glucose levels and corrected considerably (p < 0.01) the altered serum lipid profiles of the diabetic rats which was comparable to glibenclamide (5 mg/kg). Together with friedelan-3-one, the extract markedly inhibited the activity of α-amylase and promoted glucose uptake in C2C12 cells. Whereas MLB significantly (p < 0.001) up-regulated PI3K and PPARγ transcripts with a corresponding increase in GLUT-4 transcripts within the muscle cells, friedelan-3-one only up-regulated PI3K and GLUT-4 transcripts to promote glucose transport. Friedelan-3-one was shown to be non-carcinogenic, non-hepatotoxic, has decent oral bioavailability and a good compound for optimisation into a drug candidate. The study has demonstrated that MLB possess hypoglycaemic and anti-hyperlipidaemic activities and could be used as a therapeutic agent in the management of diabetes mellitus.

In vitro Anti-Mycobacterium ulcerans and cytotoxic activities of some selected medicinal plants and an indoloquinoline alkaloid.

Background: Buruli ulcer (BU) is a neglected tropical disease caused by the Mycobacterium ulcerans. BU is an endemic disease in many communities in sub-Saharan Africa where population have long history of using medicinal plants for treatment. Indeed, several medicinal plants have been documented against BU and related conditions. The present study was undertaken to prove the efficacy of seven medicinal plants documented for the treatment of mycobacterial infections and related symptoms in Ghana. Method: Antimycobacterial activity of the stem bark extracts and reference control drugs were conducted using the resazurin microtiter assay (REMA) assay method in clear round bottom 96-well microtiter plates. The extracts that showed anti-mycobacterium ulcerans activity were assessed for cytotoxicity using the Alamar blue assay. Results: Overall, The Cryptolepis sanguinolenta root aqueous extract exhibited the highest antimycobacterial activity (MIC=64 µg/mL) followed by Cleistopholis patens (MIC=256 µg/mL). Based on the marked activity of the Cryptolepis sanguinolenta extracts, pure cryptolepine, its major metabolite recorded a MIC value of 32 µg/mL. These extracts with considerable antimycobacterial activity showed 50% cytotoxic concentration (CC50) ranging from 94 to 384 µg/mL. Conclusions: Thus, Cleistopholis patens and Cryptolepis sanguinolenta are primed for further studies and could afford novel drugs for the mitigation of buruli ulcer disease.

Recent Progress in Luminescent Cu(I) Halide Complexes: A Mini-Review.

Copper(I) halide complexes are well sought-after materials due to their rich structural diversities and photophysical properties. Profoundly, there is a direct relationship between each structural variation and luminescence of these complexes, for a purported use. In this review, recent publications within the last 2 years about copper(I) halide complexes, centering on their structural dimensionalities with derivatives of nitrogen, phosphorus, and sulfur ligands, have been considered alongside their effects on luminescence.

Indigenous Medicinal Plants as Biofilm Inhibitors for the Mitigation of Antimicrobial Resistance.

The majority of indigenes in the rural areas of Ghana use herbal medicines for their primary health care. In this study, an ethnobotanical survey was undertaken to document medicinal plants used by traditional healers in the Ejisu-Juaben district in the Ashanti region of Ghana to treat infections and to further investigate the antibiofilm formation properties of selected plants in resisting pathogenic bacteria. Seventy medicinal plants used by traditional practitioners for the treatment of skin infections and wounds were documented from the ethnobotanical survey. Forty out of the seventy plants were collected and their methanol extracts evaluated for antimicrobial activity by the agar diffusion assay. Extracts that showed antibacterial activity were tested for biofilm inhibitory activity, and the most active plant was subsequently purified to obtain the active constituents. Biofilm formation was significantly mitigated by petroleum ether, ethyl acetate, and methanol extracts of Holarrhena floribunda stem bark. Bioassay-guided fractionation of an alkaloidal extract prepared from the methanol fraction led to the isolation of three steroidal alkaloids, namely, holonamine, holadienine, and conessine. The isolated compounds demonstrated varying degrees of biofilm formation inhibitory properties. The current study reveals that screening of indigenous medicinal plants could unravel potential leads to salvage the declining efficacy of conventional antibiotics. Holarrhena floribunda stem bark extract has strong biofilm formation inhibition properties, which could be attributed to the presence of steroidal alkaloids.

Evaluation of the Microbial Load and Heavy Metal Content of Two Polyherbal Antimalarial Products on the Ghanaian Market.

The use of herbal products has increased and become more popularized globally; however, limited studies coupled with questions related to the quality and safety of these herbal products have been raised. Herbal products with hope of their nontoxicity may play a role of alternative to overcome the problems of multi-drug resistant pathogens. Medicinal plants used as raw materials for production may have quality and safety issues due to proximity to wastewater application of fungicides and pesticides, which may be directly deposited superficially or absorbed by the plant system. Therefore, possible contamination of some Ghanaian herbal products cannot be ignored, as it may severely affect human life in the process of treatment. Aim. To evaluate the microbial load and the presence of toxic heavy metals in Mist Amen Fevermix and Edhec Malacure, two polyherbal products used in the treatment of uncomplicated malaria in Ghana. Methods. Thermo Elemental M5 Atomic Absorption Spectrophotometer (AAS) fitted with graphite furnace and an auto sampler was used to determine the heavy metal contents of the herbal products. The herbal samples were evaluated for the microbial load by using the appropriate culture media. Results and Analysis. Mist Amen Fevermix and Edhec Malacure complied with the safety limits evaluated for all different microbial counts and contamination. The following heavy metals were present in Mist Amen Fevermix and Edhec Malacure Mixture: Fe, Ni, K, Zn, Hg, Cu, Mn, Cr, Cd, Pb, Fe, Cu, K, and Na. Ni was below detectable limit in Edhec Malacure. Conclusion. Mist Amen Fevermix and Edhec Malacure may be assured of safety. The products contained heavy metals, but all were within acceptable limit established by the FAO/WHO. The levels of microbial contamination were below the maximum acceptable limit.

In Vivo Antiplasmodial Activity of Different Solvent Extracts of Myrianthus libericus Stem Bark and Its Constituents in Plasmodium berghei-Infected Mice.

The emergence and resurgence of P. falciparum resistance to generations of antimalarial drugs have prompted the search for new, effective, and safe antimalarial agents. This study aimed at investigating the in vivo antiplasmodial activity of the 70% hydroethanolic extract and constituents of the stem bark of Myrianthus libericus based on its ethnomedicinal use as an antimalarial agent. The antiplasmodial activity was assessed in Swiss albino mice employing the 4-day suppressive and Rane's tests. MLB significantly (p < 0.0001) suppressed parasitaemia by 52.26%, 65.40%, and 77.11% at 50, 100, and 200 mg·kg-1 doses, respectively, in the 4-day suppressive test. In Rane's test, the highest parasitaemia suppression of 72.50% was recorded at a dose of 200 mg·kg-1 of the extract. Fractionation of the bioactive ethyl acetate fraction by solvent-solvent partitioning and column chromatography led to the isolation of friedelan-3-one and stigmasterol being reported for the first time from this species. The compounds demonstrated remarkable antiplasmodial activity by suppressing parasitaemia by 65-72% in the suppressive test and 61-70% in the curative test at doses of 10-30 mg·kg-1. Both the extract and the isolated compounds significantly prolonged the survival time of infected mice and averted the cardinal signs associated with P. berghei-induced malaria including weight loss, hypothermia, and haemolysis. The results obtained confirm the prospect of M. libericus as an important source of new antimalarial compounds and justifies its folkloric use as an antimalarial agent.

Antimicrobial pentacyclic triterpenes and glycosides from the stem bark of Cussonia bancoensis.

The stem bark of Cussonia bancoensis is used traditionally for the treatment of different types of infection and pain. A bioassay guided fractionation of the methanol stem bark extract led to the isolation of five pentacyclic triterpenes and glycosides identified based on spectroscopic data as 23-hydroxyursolic acid (CB1), hederagenin (CB2), 3-O-α-L-arabinopyranosyl-echinocystic acid (CB3), 3-O-α-L-arabinopyranosyl- oleanolic acid (CB4) and 3-O-α-L-arabinopyranosyl-ursolic acid (CB5). CB2 - CB5 are being reported for the first time from this species. The compounds were evaluated for antimicrobial activity against ten microorganisms using the HT-SPOTi method. CB3 demonstrated remarkable antimicrobial activity against S. aureus, S. pyogens, E. faecalis, S. typhi and C. albicans at MICs between 3.12 and 12.5 µg/mL. Among the studied compounds, it was observed that hydroxylation of position C-16 of the oleanane skeleton may enhance antimicrobial activity. This study gives insight into the anti-infective constituents of the stem bark of C. bancoensis and justifies its use in ethnomedicine.[Formula: see text].

Leishmanicidal activity of the root bark of Erythrophleum Ivorense (Fabaceae) and identification of some of its compounds by ultra-performance liquid chromatography quadrupole time of flight mass spectrometry (UPLC-QTOF-MS/MS).

ETHNOPHARMACOLOGICAL RELEVANCE: Leishmaniasis is one of the neglected tropical disease caused by a protozoan of the genus Leishmania transmitted by sandflies. High cost and lack of oral formulation of existing drugs, rapid developments of resistance by the parasite coupled with serious side effects require new treatments to augment or replace currently available therapies. The major merits of herbal medicine seem to demonstrate perceived efficacy, low incidence of serious adverse effects and low cost. Erythrophleum plants possess beneficial biological properties and, as such, characterization of the bioactive components of these plants is imperative. Previous work has shown an overwhelming presence of cassaine alkaloids in these plants. However, amongst these plants, the African based specie (Erythrophleum ivorense) is the least studied. OBJECTIVE: In the current study, the in vitro anti-leishmanial activity of the crude extract, its fractions and isolated compounds were evaluated using direct counting assay of promastigotes of Leishmania donovani using amphotericin B as positive control. MATERIALS AND METHODS: The anti-leishmanial activity of E. ivorense extract was evaluated in vitro against the promastigote forms of Leishmania Donovani using a direct counting assay based on growth inhibition. Different crude extracts from ethyl acetate, pet-ether, and methanol as well as pure isolated compounds of E. ivorense: Erythroivorensin, Eriodictyol and Betulinic acid were screened. To know the possible components of the active methanolic extract, attempt was made to elucidate the extract using ultra-performance liquid chromatography quadrupole time of flight mass spectrometry (UHPLC-QTOF-MS/MS). RESULTS: This afforded a weak pet-ether fraction, a moderately active ethyl acetate fraction and a significantly active methanol fraction (IC50 = 2.97µg/mL) compared to Amphotericin B (IC50 = 2.40±0.67µg/mL). The novel diterpene erythroivorensin, betulinic acid and the flavanone Eriodictyol, from the ethyl acetate fraction, showed weak activity. UPLC-QTOF-MS/MS was used to identify the cassaine diterpenoids from the active methanol fraction. Here, 10 compounds of this type were putatively identified from the ethanol crude extract. CONCLUSION: The fragmentation mechanism of these metabolites is also proposed and are expected to serve as reference template for identification of these and related compounds in future. The presence of these compounds is an indication that they are an inherited and evolutionary component of plants belonging to the Erythrophleum genus. Our results further present another dimension where these compounds and their relative abundances can be used as chemo-taxonomical bio-markers of the genus. The present study also successfully demonstrated/re-affirmed the use of UPLC-QTOF-MS/MS as a robust technique for the characterization of natural products.

Mosquito larvicidal activity of Cassia tora seed extract and its key anthraquinones aurantio-obtusin and obtusin.

BACKGROUND: The edible and medicinal leguminous plant Cassia tora L. (Fabaceae) is known to possess insecticidal properties against a wide range of plant-feeding insects. However, the bioactivity of extracts of this plant and their constituents against vectors of medical importance has been largely unexplored. We investigated the mosquito larvicidal activity of the seed extract and its major anthraquinones against larvae of the African malaria vector Anopheles gambiae (s.s.). METHODS: Third-fourth instar larval mortality was observed after 24, 48, 72 and 96 h of exposure to varying doses of the extracts, and two anthraquinones isolates identified using liquid chromatography- quadrupole time of flight mass spectrometry (LC-QtoF-MS). The mosquito larval mortality was evaluated relative to the natural insecticide azadirachtin. RESULTS: Fractionation of the crude extract decreased mosquito larvicidal activity, however, larvicidal activity increased with increasing dose of the treatment and exposure time. The known anthraquinones aurantio-obtusin and obtusin were identified as key larvicidal compounds. Aurantio-obtusin and obtusin, exhibited similar toxicity to larvae of A. gambiae (s.s.) with LD50 values of 10 and 10.2 ppm, respectively. However, the two anthraquinones were four- and ~ six-fold less potent than that of the crude seed extract and azadirachtin, which had comparable LD50 values of 2.5 and 1.7 ppm, respectively. CONCLUSION: Both aurantio-obtusin and obtusin showed mosquito larvicidal activity which were comparable to their respective fractions although they were less potent relative to the crude extract and azadirachtin. Further studies need to be conducted on C. tora for its exploitation as a potential eco-friendly tool in mosquito larval source reduction.