Solid Lipid Nanoparticles of Lepidium Sativum L Seed Extract: Formulation, Optimization and In vitro Cytotoxicity Studies.

The current study focused on important bioactive compounds in plants that make them pharmacologically valuable. Therefore, this study was aimed to develop Lepidium sativum (L. sativum) seed extract loaded solid lipid nanoparticles and explore its cytotoxic effect on human liver cancer cells (HepG2 cells). The ethanolic extract of L. sativam used to develop L. sativum seed extract loaded solid lipid nanoparticles (SLNs) was analyzed by gas chromatography-mass spectrometry, thin-layer chromatography (TLC) and high-performance thin-layer chromatography (HPTLC) for phytochemical profiling. The L. sativum seed extract loaded SLNs were efficaciously prepared by the nanoprecipitation method and screened on the basis of physicochemical properties. The L. sativum seed extract loaded SLN-2 was characterized using various parameters like particle size (237.1±0.104), % entrapment efficiency (80±1.15), zeta potential (42.1±0.102) and % drug release (45% at the end 8 hours and release the entire amount in 12 h). The SLN-2 formulation was optimized based on the recipient factor, and SLN-2 was used to further evaluate the in vitro cytotoxicity of HepG2 cells in a dose-dependent manner by 3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide (MTT) assay. The IC50 value of SLN2 was 52.37 ug/ml and sub IC50 26.1 ug/ml at 24 h and 48 h, respectively. Thus, we concluded that L. sativum extract loaded SLN-2 could act as an alternative therapy, possibly controlling therapeutic action by making a substantial reduction in side effects.

Molecular Docking and Dynamics Simulation Analysis of Thymoquinone and Thymol Compounds from Nigella sativa L. that Inhibit Cag A and Vac A Oncoprotein of Helicobacter pylori: Probable Treatment of H. pylori Infections.

BACKGROUND: Helicobacter pylori infection is accountable for most of the peptic ulcer and intestinal cancers. Due to the uprising resistance towards H. pylori infection through the present and common proton pump inhibitors regimens, the investigation of novel candidates is the inevitable issue. Medicinal plants have always been a source of lead compounds for drug discovery. The research of the related effective enzymes linked with this gram-negative bacterium is critical for the discovery of novel drug targets. OBJECTIVE: The aim of the study is to identify the best candidate to evaluate the inhibitory effect of thymoquinone and thymol against H. pylori oncoproteins, Cag A and Vac A in comparison to the standard drug, metronidazole by using a computational approach. MATERIALS AND METHODS: The targeted oncoproteins, Cag A and Vac A were retrieved from RCSB PDB. Lipinski's rule and ADMET toxicity profiling were carried out on the phytoconstituents of the N. sativa. The two compounds of N. sativa were further analyzed by molecular docking and MD simulation studies. The reported phytoconstituents, thymoquinone and thymol present in N. sativa were docked with H. pylori Cag A and Vac A oncoproteins. Structures of ligands were prepared using ChemDraw Ultra 10 software and then changed into their 3D PDB structures using Molinspiration followed by energy minimization by using software Discovery Studio client 2.5. RESULTS: The docking results revealed the promising inhibitory potential of thymoquinone against Cag A and Vac A with docking energy of -5.81 kcal/mole and -3.61kcal/mole, respectively. On the contrary, the inhibitory potential of thymol against Cag A and Vac A in terms of docking energy was -5.37 kcal/mole and -3.94kcal/mole as compared to the standard drug, metronidazole having docking energy of -4.87 kcal/mole and -3.20 kcal/mole, respectively. Further, molecular dynamic simulations were conducted for 5ns for optimization, flexibility prediction, and determination of folded Cag A and Vac A oncoproteins stability. The Cag A and Vac A oncoproteins-TQ complexes were found to be quite stable with the root mean square deviation value of 0.2nm. CONCLUSION: The computational approaches suggested that thymoquinone and thymol may play an effective pharmacological role to treat H. pylori infection. Hence, it could be summarized that the ligands thymoquinone and thymol bound and interacted well with the proteins Cag A and Vac A as compared to the ligand MTZ. Our study showed that all lead compounds had good interaction with Cag A and Vac A proteins and suggested them to be a useful target to inhibit H. pylori infection.

A Panoramic Review on Lepidium sativum L. Bioactives as Prospective Therapeutics.

BACKGROUND: Lepidium sativum (L. sativum), an annual herb belonging to family Brassicaceae is commonly known as Garden cress of Egyptian origin but now a day's cultivated worldwide. The plant material and its constituents are used in various traditional and folk medicines for the treatment of various liver diseases and other ailments. OBJECTIVE: This review aims to gather comprehensive information on L. sativum's bioactive constituents, and it's antioxidant, hepato-protective and anticancer activity. METHOD: Systematic exploration for research evidences were carried out using well-structured and focused review question and presented data in the tabular form for readers' convenience. RESULTS: The comprehensive literature survey was conducted, and we found that specific studies on L. Sativum and its bioactive compounds had been carried out to date. We explored the unique and selective effect of L. Sativum and its bioactive constituents to combat oxidative stress and hepatic carcinoma. CONCLUSION: The present article appraised that L. sativum extract has a potential therapeutic effect against liver toxicity and hepato-carcinoma. Graphical Abstract.

Evaluation of the anticancer activity of sprout extract-loaded nanoemulsion of N. sativa against hepatocellular carcinoma.

Nigella sativa L. belonging to Ranunculaceae family is an important medicinal spice which has been utilised to treat various chronic diseases. Lipid nanoemulsions containing oil from medicinal plants have shown to enhance drug dissolvability, diminish symptoms of different powerful medications and enhance the bioavailability of medications, in contrast with conventional formulations. In the present study, aqueous titration method was used to prepare nanoemulsion. The optimised formulation (NE11) with the mean particle size of 37.47 nm showed a minimum viscosity of 0.547 cps and maximum drug release (98.2%) in 24 h. The stability study showed considerably stable formulations at refrigerator temperature as compared to room temperature. The cancer cell line studies confirmed that 5d sprout extract of N. sativa nanoemulsion reduced the cell viability (p < .05) and increased colony formation, ROS intensity and chromatin condensation. All data such as colony formation, ROS intensity and chromatin condensation are represented as mean ± SD (p < .001) treated cells for 48 hours. Our results concluded that the development of nanoemulsion could be an efficient carrier for drug delivery.

Evaluation of Antioxidant and Antibacterial Potentials of Nigella sativa L. Suspension Cultures under Elicitation.

Nigella sativa L. (family Ranunculaceae) is an annual herb of immense medicinal properties because of its major active components (i.e., thymoquinone (TQ), thymohydroquinone (THQ), and thymol (THY)). Plant tissue culture techniques like elicitation, Agrobacterium mediated transformation, hairy root culture, and so on, are applied for substantial metabolite production. This study enumerates the antibacterial and antioxidant potentials of N. sativa epicotyl suspension cultures under biotic and abiotic elicitation along with concentration optimization of the elicitors for enhanced TQ and THY production. Cultures under different concentrations of pectin and manganese chloride (MnCl2) elicitation (i.e., 5 mg/L, 10 mg/L, and 15 mg/L) showed that the control, MnCl2 10 mg/L, and pectin 15 mg/L suspension extracts greatly inhibited the growth of E. coli, S. typhimurium, and S. aureus (MIC against E. coli, i.e., 2.35 ± 0.8, 2.4 ± 0.2, and 2.46 ± 0.5, resp.). Elicitation decreased SOD enzyme activity whereas CAT enzyme activity increased remarkably under MnCl2 elicitation. MnCl2 10 mg/L and pectin 15 mg/L elicitation enhanced the DPPH radical inhibition ability, but ferric scavenging activity was comparable to the control. TQ and THY were quantified by LC-MS/MS in the cultures with high bioactive properties revealing maximum content under MnCl2 10 mg/L elicitation. Therefore, MnCl2 elicitation can be undertaken on large scale for sustainable metabolite production.

Current approaches toward production of secondary plant metabolites.

Plants are the tremendous source for the discovery of new products with medicinal importance in drug development. Today several distinct chemicals derived from plants are important drugs, which are currently used in one or more countries in the world. Secondary metabolites are economically important as drugs, flavor and fragrances, dye and pigments, pesticides, and food additives. Many of the drugs sold today are simple synthetic modifications or copies of the naturally obtained substances. The evolving commercial importance of secondary metabolites has in recent years resulted in a great interest in secondary metabolism, particularly in the possibility of altering the production of bioactive plant metabolites by means of tissue culture technology. Plant cell and tissue culture technologies can be established routinely under sterile conditions from explants, such as plant leaves, stems, roots, and meristems for both the ways for multiplication and extraction of secondary metabolites. In vitro production of secondary metabolite in plant cell suspension cultures has been reported from various medicinal plants, and bioreactors are the key step for their commercial production. Based on this lime light, the present review is aimed to cover phytotherapeutic application and recent advancement for the production of some important plant pharmaceuticals.