Plant-derived nanomaterials (PDNM): a review on pharmacological potentials against pathogenic microbes, antimicrobial resistance (AMR) and some metabolic diseases.

Plant-derived nanomaterials (PDNM) have gained significant attention recently due to their potential pharmacological applications against pathogenic microbes, antimicrobial resistance (AMR), and certain metabolic diseases. This review introduces the concept of PDNMs and their unique properties, including their small size, high surface area, and ability to penetrate biological barriers. Besides various methods for synthesizing PDNMs, such as green synthesis techniques that utilize plant extracts and natural compounds, the advantages of using plant-derived materials, such as their biocompatibility, biodegradability, and low toxicity, were elucidated. In addition, it examines the recent and emerging trends in nanomaterials derived from plant approaches to combat antimicrobial resistance and metabolic diseases. The sizes of nanomaterials and their surface areas are vital as they play essential roles in the interactions and relationships between these materials and the biological components or organization. We critically analyze the biomedical applications of nanoparticles which include antibacterial composites for implantable devices and nanosystems to combat antimicrobial resistance, enhance antibiotic delivery, and improve microbial diagnostic/detection systemsIn addition, plant extracts can potentially interfere with metabolic syndrome pathways; hence most nano-formulations can reduce chronic inflammation, insulin resistance, oxidative stress, lipid profile, and antimicrobial resistance. As a result, these innovative plant-based nanosystems may be a promising contender for various pharmacological applications.

FTO gene expression in diet-induced obesity is downregulated by Solanum fruit supplementation.

The Fat Mass and Obesity-associated (FTO) gene has been shown to play an important role in developing obesity, manifesting in traits such as increased body mass index, increased waist-to-hip ratio, and the distribution of adipose tissues, which increases the susceptibility to various metabolic syndromes. In this study, we evaluated the impact of fruit-based diets of Solanum melongena (SMF) and Solanum aethiopicum fruits (SAF) on the FTO gene expression levels in a high-fat diet (HFD)-induced obese animals. Our results showed that the mRNA level of the FTO gene was downregulated in the hypothalamus, and white and brown adipose tissue following three and six weeks of treatment with SMF- and SAF-based diets in the HFD-induced obese animals. Additionally, the Solanum fruit supplementation exhibited a curative effect on obesity-associated abrasions on the white adipose tissue (WAT), hypothalamus, and liver. Our findings collectively suggest the anti-obesity potential of SMF and SAF via the downregulation of the FTO gene.

Neuroprotective effect of Bryophyllum pinnatum flavonoids against aluminum chloride-induced neurotoxicity in rats.

Toxic metals such as aluminum accumulation in the brain have been associated with the pathophysiology of several neurodegenerative disorders. Bryophyllum pinnatum leaves contain a vast array of polyphenols, particularly flavonoids, that may play a role in the prevention of toxic and degenerative effects in the brain. This study assessed the neuro-restorative potential of leaves of B. pinnatum enriched flavonoid fraction (BPFRF) in aluminum-induced neurotoxicity in rats. Neurotoxicity was induced in male Wistar rats by oral administration of 150 mg/kg body weight of aluminum chloride (AlCl3) for 21 days. Rats were grouped into five (n = 6); Control (untreated), Rivastigmine group, AlCl3 group and BPFRF group (50 and 100 mg/kg b.wt.) for 21 days. Neuronal changes in the hippocampus and cortex were biochemically and histologically evaluated. Expression patterns of acetylcholinesterase (AChE) mRNA were assessed using semi-quantitative reverse-transcription-polymerase chain reaction protocols. Molecular interactions of BPFRF compounds were investigated in silico. The results revealed that oral administration of BPFRF ameliorated oxidative imbalance by augmenting antioxidant systems and decreasing lipid peroxidation caused by AlCl3. BPFRF administration also contributed to the down-regulation of AChE mRNA transcripts and improved histological features in the hippocampus and cortex. Molecular docking studies revealed strong molecular interactions between BPFRF compounds, catalase, superoxide dismutase and glutathione peroxidase Overall, these findings suggest the neuroprotective effect of Bryophyllum pinnatum against aluminum-induced neurotoxicity.

UPLC-PDA-ESI-QTOF-MS/MS fingerprint of purified flavonoid enriched fraction of Bryophyllum pinnatum; antioxidant properties, anticholinesterase activity and in silico studies.

CONTEXT: Bryophyllum pinnatum (Lam.) Oken (Crassulaceae) is used traditionally to treat many ailments. OBJECTIVES: This study characterizes the constituents of B. pinnatum flavonoid-rich fraction (BPFRF) and investigates their antioxidant and anticholinesterase activity using in vitro and in silico approaches. MATERIALS AND METHODS: Methanol extract of B. pinnatum leaves was partitioned to yield the ethyl acetate fraction. BPFRF was isolated from the ethyl acetate fraction and purified. The constituent flavonoids were structurally characterized using UPLC-PDA-MS2. Antioxidant activity (DPPH), Fe2+-induced lipid peroxidation (LP) and anticholinesterase activity (Ellman's method) of the BPFRF and standards (ascorbic acid and rivastigmine) across a concentration range of 3.125-100 µg/mL were evaluated in vitro for 4 months. Molecular docking was performed to give insight into the binding potentials of BPFRF constituents against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). RESULTS: UPLC-PDA-MS2 analysis of BPFRF identified carlinoside, quercetin (most dominant), luteolin, isorhamnetin, luteolin-7-glucoside. Carlinoside was first reported in this plant. BPFRF significantly inhibited DPPH radical (IC50 = 7.382 ± 0.79 µg/mL) and LP (IC50 = 7.182 ± 0.60 µg/mL) better than quercetin and ascorbic acid. Also, BPFRF exhibited potent inhibition against AChE and BuChE with IC50 values of 22.283 ± 0.27 µg/mL and 33.437 ± 1.46 µg/mL, respectively compared to quercetin and rivastigmine. Docking studies revealed that luteolin-7-glucoside, carlinoside and quercetin interact effectively with crucial amino acid residues of AChE and BuChE through hydrogen bonds. DISCUSSION AND CONCLUSIONS: BPFRF possesses an excellent natural source of cholinesterase inhibitor and antioxidant. The material could be further explored for the potential treatment of oxidative damage and cholinergic dysfunction in Alzheimer's disease.

Potential Enhancement of Metformin Hydrochloride in Lipid Vesicles Targeting Therapeutic Efficacy in Diabetic Treatment.

The potential enhancement of metformin hydrochloride (MH) loaded in lipid vesicles targeting therapeutic efficacy on alloxan-induced diabetic rats was investigated. This involved lipid vesicles formulated with homogenously distributed nano-sized particles by a novel integrated process of multiple emulsification by membrane and solvent evaporation. The average diameter of the water-in-oil (W1/O), W1/O/W2 emulsion droplets, and lipid vesicles was 192 nm, 52 µm, and 173 nm, respectively. The entrapment yield of metformin hydrochloride (MH) in the prepared lipid vesicles was 40.12%. The metformin hydrochloride-loaded lipid vesicles (MH-LLVs) sustained the release of the entrapped drug over a 12-h period and reduced the plasma glucose level of diabetic rats by 77.4% compared with free MH solution (2-h period and 58.2%, respectively) after one week post-diabetic treatment through oral administration of MH-LLV and the free drug. The remarkable improvement in the biochemical parameters recorded in the MH-LLV-treated animals compared with those that received free MH solutions depicted an enhanced kidney function, liver function, as well as oxidative stress status. Pancreatic histology depicted a pancreas with intralobular ducts (ID) and exocrine secretory acini that characterize an intact pancreas, which suggests the ability of the MH-LLVs to restore pancreatic cells to normal, on a continued treatment. Overall, MH-LLV appears an encouraging extended-release formulation with enhanced bioavailability, sustained release, and improved antihyperglycemic potentials.

Potentiation Effects of Ficus sycomorus Active Fraction Against Permethrin-Resistant Field-Population of Anopheles coluzzii (Diptera: Culicidae).

Insecticide resistance in mosquitoes is increasing amidst growing cases of global malaria, leading to high fatality in mostly Africa. To overcome the resistance as well as environmental effects of the synthetic insecticides, preliminary insecticidal and botanical potentiating effects of sub-lethal concentration (LC25) Ficus sycomorus active fraction (AFFS) and its synergistic potential with standard insecticide permethrin were evaluated against malarial vector Anopheles coluzzii (Coetzee & Wilkerson) populations. The glutathione-S-transferase (GST) inhibitory activity of the AFFS was also investigated compared to standard GST inhibitor, diethyl meleate (DEM). The WHO standard protocol for adult bioassay was used to expose the adult mosquitoes with sub-lethal concentration (LD25=0.49 mg/ml) of the plants' active fraction and permethrin (0.75%). The permethrin susceptibility screening result showed high level of resistance to permethrin in the field populations of A. coluzzii from Kano with 50.29 ± 2.14% average mortality after exposure to WHO diagnostic dose 0.75% permethrin. Post hoc Fisher's exact test showed that combination of sub-lethal concentration of AFFS with permethrin (mortality=73.02±12.10%; p=0.00352; RR=0.6923 and 95% CI = 0.5358-0.8946) was statistically significant, while the combination of sub-lethal concentration of AFFS with DEM showed no statistical difference (mortality=63.22±5.03; p=1; RR=0.6667 and 95% CI=0.4470-0.8438). This potentiation effect was signified to be additive effects with co-toxicity factor (CTF) of - 12.66. There was significant reduction of GST activities in the AFFS- and permethrin -exposed groups compared to unexposed populations of A. coluzzii (p < 0.05). The AFFS additively potentiate the permethrin activities by inhibiting GSTs, bio-transformational enzymes implicated in pyrethroids resistance. This study finding generally signifies the potential for bio-rational insecticide approach for malarial vector control.

Antioxidant properties and membrane stabilization effects of methanol extract of Mucuna pruriens leaves on normal and sickle erythrocytes.

This study was aimed at investigating the antioxidant properties and membrane stabilization effects of Mucuna pruriens leaves on sickle erythrocyte as a possible means of sickle cell disease management. Pulverized plant material was extracted with methanol, filtered and concentrated at reduced pressure with a rotary evaporator. Phytochemical analysis and antioxidant studies of the extract were carried out using standard methods. Blood samples of volunteer sickle cell patients and healthy individuals used in the study were collected from the University of Nigeria Medical Centre and University campus community, Nsukka respectively. The genotypes of the individuals were confirmed by cellulose acetate paper electrophoresis. Water induced haemolysis of human red blood cell was used to assess membrane stabilization of the erythrocytes. Phytochemical result of the extract showed the presence of alkaloids, flavonoids, tannins, proteins, terpenoids, saponins, cardiac glycosides and anthraquinones. Antioxidant vitamins C and E were present in concentrations of 495.36 mg/100 g and 101.03 mg/100 g respectively. The percentage (%) scavenging activity of the 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and hydroxyl radical by the extract was significant. The extract exhibited membrane stabilization on both normal and sickle erythrocytes. The percentage (%) inhibition of haemolysis by the extract in both normal and sickle erythrocytes at different concentrations of 100, 200, 400, 600 and 800 µg/ml were significant and concentration dependent. We conclude that M. pruriens leaves have antioxidant properties and erythrocyte membrane stabilizing potentials and could be recommended for use in the management of patients with sickle cell anaemia.

Membrane stabilization as a mechanism of the anti-inflammatory activity of methanol extract of garden egg (Solanum aethiopicum).

BACKGROUND: Some observations and reports show that people with high consumption of Solanum aethiopicum (African garden egg) have relief in arthritic pains and swelling. We aimed at assessing the effect of methanol extract of Solanum aethiopicum in experimentally induced inflammation using leukocyte mobilization and vascular permeability tests in rats and human red blood cell (HRBC) membrane stabilization as studies. METHODS: Twenty five (25) adult Wistar rats of either sex (120 g - 200 g) divided into five groups of five rats each were used for each of the animal models. Groups 2, 3 and 4 were administered varied doses of the extract (100, 200 and 400 mg/kg), while groups 1 (vehicle control) and 5 (treatment control) received normal saline and indomethacin (50 mg/kg) respectively. Vascular permeability was induced by the intra-peritoneal injection of 1 ml of acetic acid and monitored using 0.5 ml intravenous injection of 1% Evans blue solution. Leukocyte mobilization was induced by the intra-peritoneal injection of 0.5 ml of 3% agar suspension in normal saline. Heat and hypotonicity induced heamolysis of HRBC membrane was used to assess membrane stabilization. RESULTS: The methanol extracts of garden egg significantly and dose dependently reduced (p≤0.05) the acetic acid induced vascular permeability and agar induced leukocyte mobilization in rats. The percentage inhibitions of induced vascular permeability were 21 ± 3.39, 25 ±1.92 and 60 ± 3.81 for the 100, 200 and 400 mg/kg of the extract while the inhibitions of the agar induced leucocyte migration were 23 ± 2.17, 26 ± 1.58 and 32 ± 1.58 for the 100, 200 and 400 mg/kg of the extract respectively. The extract also, at doses of 100, 200, 400, 600 and 800 µg/ml significantly inhibited heat induced lysis of the human red cell membrane with values of 66.46 ± 2.89, 65.14 ± 4.58, 46.53 ± 2.52, 61.88 ± 4.51and 86.67 ± 3.06 respectively. CONCLUSIONS: These results show that methanol extract of Solanum aethiopicum has anti-inflammatory properties and can reduce inflammatory injury and tissue damage.

The anti-inflammatory activity of garden egg (Solanum aethiopicum) on egg albumin-induced oedema and granuloma tissue formation in rats.

OBJECTIVE: To evaluate the possible anti-inflammatory effect of garden egg [Solanum aethiopicum (S. aethiopicum)] using experimentally induced inflammatory models in rats. METHODS: Oedema was induced on the rat hind paw by the injection of 0.1 mL undiluted fresh egg albumin (philogistic agent) into the subplantar surface of the rat paw. Tissue granuloma was induced in the rats by the implantation of two autoclaved cotton pellets (30 mg) under the flank of previously shaved back of anaesthetised rats. Garden egg extract doses were administered to the rats for seven consecutive days. On day 8, the animals were killed and the pellets surrounded by granuloma tissue were dissected out and dried. RESULTS: Extracts of garden egg significantly (P<0.05) reduced the fresh egg albumin-induced rat paw oedema and also significantly (P<0.05) reduced the granuloma tissue formation in the treated groups when compared to the control. CONCLUSIONS: This study shows that the fruits of garden egg (S. aethiopicum) have anti-inflammatory activity in the models studied.

Does the African garden egg offer protection against experimentally induced ulcers?

OBJECTIVE@#To evaluate the possible antiulcer effect of the African garden egg, Solanum aethiopicum (S. aethiopicum) (a domestic vegetable) experimentally in rats.@*METHODS@#A methanol extract of the plant fruit was prepared by maceration. Twenty five overnight fasted rats for each model were divided randomly into five groups of five rats. Groups 1, 2, 3, 4 and 5 received normal saline, extract dose levels of 100, 200 and 400 mg/kg and 100 mg/kg of ranitidine respectively. All administrations were given orally. For the indomethacin and aspirin models, ulcerogenic agents (indomethacin, 50 mg/kg and aspirin 200 mg/kg) were given thirty minutes after extract treatments and animals sacrificed 8 h later. The acidified ethanol model (ethanol 60% + 0.1 mol/L HCl) was given 1 hr after extract treatment and animals sacrificed 1 h later. Ulcer index was checked and analysed with appropriate statistical tools.@*RESULTS@#Extract of S. aethiopicum showed positive effect on all the models used. It produced higher ulcer inhibition than ranitidine in the indomethacin and acid-ethanol models. All the anti-ulcer effects of the extract at different doses were dose dependent but only in indomethacin model did it produce statistically significant (P<0.05) ulcer reduction in all doses compared to control.@*CONCLUSIONS@#Garden egg, a readily cultivated crop vegetable possesses ulcer protective properties against ulcers induced experimentally making it a cheap source of natural anti-ulcer remedy.