Novel Insight into Potential Leishmanicidal Activities of Transdermal Patches of Nigella Sativa: Formulation Development, Physical Characterizations, and In vitro/In vivo Assays

Cutaneous Leishmaniasis (CL) is the most common type of Leishmaniasis, which annually affects 1.5 million people worldwide. About 90% of cases are reported from countries such as Iran, Afghanistan, Pakistan, Iraq, and Saudi Arabia. The purpose of the present study was to fabricate transdermal patches of Nigella sativa (NS), characterize, and to check its in vitro/in vivo anti-Lieshmanial activity. Hydroalcoholic extract was analyzed for preliminary phytochemicals. Five formulations of transdermal patches (NS1, NS2, NS3, NS4, and NS5) were prepared by solvent evaporation method. The optimized formulation NS5 was characterized for Fourier transform-infrared spectroscopy (FTIR), smoothness, brittleness, clarity, thickness, folding endurance, uniformity of weight, percent moisture content, in vitro drug release, release kinetics, ex vivo drug permeation, and in vitro anti-Lieshmanial activity. In vivo anti-Lieshmanial activity was assessed in 30 patients (n = 30) suffering from CL. The FTIR studies showed no incompatibility among the active extract and polymers. In vitro anti-Lieshmanial assay was 194.6% ± 1.88% as compared with standard drug (p > 0.05) and in vivo anti-Lieshmanial activity was 75%. The drug release after 24 h was 87.0% ± 0.94% in NS5, which showed non-Fickian diffusion mechanism while drug permeation across rabbit skin after 24 h was up to 80.0% ± 0.91%. The results concluded that problems related to the parenteral medications used for Lieshmanial treatment can be managed by applying extract of NS seeds in the form of transdermal patch.

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Identification and evaluation of antiviral potential of thymoquinone, a natural compound targeting Chikungunya virus capsid protein

Capsid protein (CP) of Chikungunya virus (CHIKV) is a multifunctional protein with a conserved hydrophobic pocket that plays a crucial role in the capsid assembly and virus budding process. This study demonstrates antiviral activity of thymoquinone (TQ), a natural compound targeting the hydrophobic pocket of CP. The binding of TQ to the hydrophobic pocket of CHIKV CP was analysed by structure-based molecular docking, isothermal titration calorimetry and fluorescence spectroscopy. The binding constant KD obtained for TQ was 27 μM. Additionally, cell-based antiviral studies showed that TQ diminished CHIKV replication with an EC50 value 4.478 μM. Reduction in viral RNA copy number and viral replication as assessed by the qRT-PCR and immunofluorescence assay, confirmed the antiviral potential of TQ. Our study reveals that TQ is an effective antiviral targeting the hydrophobic pocket of CHIKV CP and may serve as the basis for development of a broad-spectrum therapy against alphaviral diseases.

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Potential role of Nigella sativa supplementation with physical activity in prophylaxis and treatment of COVID-19: a contemporary review

The widespread prevalence and mortality of coronavirus diseases-2019 (COVID-19) lead many researchers to study the SARS-CoV-s2 infection to find a treatment for this disease. Discovering the mechanisms of action of COVID-19 and coping at the cellular level with this disease can have better effects. Including the target tissues of this disease are the lungs and the immune system. It is stated that COVID-19 easily infiltrates into alveoli through its receptors and then starts to proliferate. Subsequently, with the weakening of immune cells and increase inflammatory cytokines, it increases the rate of inflammation in the body. Strengthening the immune system and inhibiting COVID-19 receptors can play a preventive or even therapeutic role for this disease. Nigella sativa (N. sativa) is one of the herbal medicines to possess numerous pharmacological effects related to several organs of the body. Among the extraordinary properties of this plant is improving asthma and several lung diseases. The recent studies have shown that N. sativa at the cellular level can inhibit COVID-19 receptors. It was also stated that performing regular exercise training (especially moderate-intensity exercise training) can modulate the immune system and have an anti-inflammatory effect. Since the use of herbal supplements with exercise can have tremendous therapeutic effects at the cellular level, the hypothesis to use the Nigella sativa along with exercise training to prophylaxis and treatment COVID-19 will be highlighted in this paper.

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Nigella and Milk Thistle Seed Oils: Potential Cytoprotective Effects against 7beta-Hydroxycholesterol-Induced Toxicity on SH-SY5Y Cells

Oxysterols are assumed to be the driving force behind numerous neurodegenerative diseases. In this work, we aimed to study the ability of 7β-hydroxycholesterol (7β-OHC) to trigger oxidative stress and cell death in human neuroblastoma cells (SH-SY5Y) then the capacity of Nigella sativa and Milk thistle seed oils (NSO and MTSO, respectively) to oppose 7β-OHC-induced side effects. The impact of 7β-OHC, associated or not with NSO or MTSO, was studied on different criteria: cell viability; redox status, and apoptosis. Oxidative stress was assessed through the intracellular reactive oxygen species (ROS) production, levels of enzymatic and non-enzymatic antioxidants, lipid, and protein oxidation products. Our results indicate that 7β-OHC (40 µg/mL) exhibit pr-oxidative and pro-apoptotic activities shown by a decrease of the antioxidant enzymatic activities and an increase of ROS production, lipid, and protein oxidation end products as well as nitrotyrosine formation and caspase 3 activation. However, under the pre-treatment with NSO, and especially with MTSO (100 µg/mL), a marked attenuation of oxidative damages was observed. Our study suggests harmful effects of 7β-OHC consisting of pro-oxidative, anti-proliferative, and pro-apoptotic activities that may contribute to neurodegeneration. NSO and especially MTSO showed potential cytoprotection against the cytotoxicity of 7β-OHC.

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Dual-targeting potential of active constituents of Nigella sativa against FimH and CTX-M-15: A plausible therapeutic strategy against drug-resistant uropathogenic strains

Uropathogenic strains belonging to the Enterobacteriaceae family are considered one of factors for urinary tract infections, and type 1 pilus fimbrial adhesin (FimH) and beta lactamase CTX-M-15 play crucial roles in their pathogenesis and resistance. Thus, a promising approach is to explore dual-targeting therapeutic agents that act against both FimH and CTX-M-15. In the present study, active constituents of Nigella sativa were selected on the basis of significant activity against UTIs. Molecular docking was used to target active constituents of Nigella sativa to the active sites of FimH and CTX-M-15; these included thymoquinone, dithymoquinone, carvacrol, p-cymene, thymol, thymohydroquinone and longifolene. Dithymoquinone was found to be the most potent dual inhibitor, with binding energy of -7.01 and -5.38kcal/mol against CTX-M-15 and FimH, respectively; In addition, Dithymoquinone exhibited superior activity compared to positive controls avibactam and heptyl α-D-mannopyranoside. Further molecular dynamic simulation studies were carried out to assess the stability of dithymoquinone-target protein complexes via RMSD, Rg, SASA, hydrogen bond number, and RMSF analysis. Both protein-ligand complexes were conserved and attained equilibrium at around 2.0 to 2.5 ns during10 ns runs. These results suggest that active constituents of Nigella sativa, particularly dithymoquinone, might represent a plausible therapeutic strategy against resistant uropathogenic bacteria.

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Medicinal Plants in COVID-19: Potential and Limitations

Currently, the search to identify treatments and vaccines for novel coronavirus disease (COVID-19) are ongoing. Desperation within the community, especially among the middle-and low-income groups acutely affected by the economic impact of forced lockdowns, has driven increased interest in exploring alternative choices of medicinal plant-based therapeutics. This is evident with the rise in unsubstantiated efficacy claims of these interventions circulating on social media. Based on enquiries received, our team of researchers was given the chance to produce evidence summaries evaluating the potential of complementary interventions in COVID-19 management. Here, we present and discuss the findings of four selected medicinal plants (Nigella sativa, Vernonia amygdalina, Azadirachta indica, Eurycoma longifolia), with reported antiviral, anti-inflammatory, and immunomodulatory effects that might be interesting for further investigation. Our findings showed that only A. indica reported positive antiviral evidence specific to the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) based on preliminary in silico data while all four medicinal plants demonstrated differential anti-inflammatory or immunomodulatory effects. The definitive roles of these medicinal plants in cytokine storms and post-infection complications remains to be further investigated. Quality control and standardisation of medicinal plant-based products also needs to be emphasized. However, given the unprecedented challenges faced, ethnopharmacological research should be given a fair amount of consideration for contribution in this pandemic.

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In silico identification of compounds from Nigella sativa seed oil as potential inhibitors of SARS-CoV-2 targets

Bull Natl Res Cent. 2021;45(1):57. doi: 10.1186/s42269-021-00517-x. Epub 2021 Mar 12. ABSTRACT BACKGROUND: The growing number of cases, severity and fatality of the COVID-19 pandemic, coupled with the fact that no cure has been found has made infected individuals especially in Africa, to resort to the consumption of different natural products to alleviate their condition. […]

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Therapeutic Potential of Natural Products in Treatment of Cervical Cancer: A Review

Nutrients. 2021 Jan 5;13(1):154. doi: 10.3390/nu13010154. ABSTRACT Cervical cancer is the fourth most common cancer among women worldwide. Though several natural products have been reported regarding their efficacies against cervical cancer, there has been no review article that categorized them according to their anti-cancer mechanisms. In this study, anti-cancerous natural products against cervical cancer were […]

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