Energy-dispersive X-ray microanalysis of elements’ content and antimicrobial properties of Pereskia bleo and Goniothalamus umbrosus

This study was designed to investigate elements’ content and anti-microbial effects of two Malaysian plants, Pereskia bleo and Goniothalamus umbrosus. Elements’ analysis was carried out using Energy Dispersive X-ray Microanalysis combined with Variable Pressure Scanning Electron Microscope (EDX, VPSEM). Anti-microbial screening was performed using disc diffusion method using two gram-positive bacteria, methicillin resistant Staphylococcus aureus (MRSA) and Bacillus subtilis B29, and other two gram-negative bacteria, Pseudomonas aeruginosa 60690 and Salmonella choleraesuis. The elemental distribution revealed the presence of C, O, Mg, P, S, Cl, K, Ca, Al, Si and Fe, in these medicinal plantsand their relative weight percentages were estimated. A variable susceptibility of microbial strains of this study towards Pereskia bleo and Goniothalamus umbrosus was noticeably observed. From thisstudy, it is shown that the analysis of elements of anticancer plants can be considered as potential sources for providing information regarding the medicinal usages of plants

Thymoquinone-loaded nanostructured lipid carriers: preparation, gastroprotection, in vitro toxicity, and pharmacokinetic properties after extravascular administration

Siddig Ibrahim Abdelwahab,1 Bassem Yousef Sheikh,2 Manal Mohamed Elhassan Taha,1 Chee Wun How,3 Rasedee Abdullah,3 Umar Yagoub,1 Rashad El-Sunousi,1 Eltayeb EM Eid31Medical Research Centre, Jazan University, Jazan, Saudi Arabia; 2Department of Surgery, College of Medicine, Taibah University, Medina, Saudi Arabia; 3Laboratory of Vaccines and Immunotherapeutics, Institute of Bioscience, University Putra Malaysia, Serdang, MalaysiaBackground: Nanostructured lipid carriers (NLCs), composed of solid and liquid lipids, and surfactants are potentially good colloidal drug carriers. Thymoquinone is the main bioactive compound of Nigella sativa. In this study, the preparation, gastroprotective effects, and pharmacokinetic (PK) properties of thymoquinone (TQ)-loaded NLCs (TQNLCs) were evaluated.Method: TQNLCs were prepared using hydrogenated palm oil (Softisan® 154), olive oil, and phosphatidylcholine for the lipid phase and sorbitol, polysorbate 80, thimerosal, and double distilled water for the liquid lipid material. A morphological assessment of TQNLCs was performed using various methods. Analysis of the ulcer index, hydrogen concentration, mucus content, and biochemical and histochemical studies confirmed that the loading of TQ into the NLCs significantly improved the gastroprotective activity of this natural compound against the formation of ethanol-induced ulcers. The safety of TQNLC was tested on WRL68 liver normal cells with cisplatin as a positive control.Results: The average diameter of the TQNLCs was 75 ± 2.4 nm. The particles had negative zeta potential values of −31 ± 0.1 mV and a single melting peak of 55.85°C. Immunohistochemical methods revealed that TQNLCs inhibited the formation of ethanol-induced ulcers through the modulation of heat shock protein-70 (Hsp70). Acute hepatotoxic effects of the TQNLCs were not observed in rats or normal human liver cells (WRL-68). After validation, PK studies in rabbits showed that the PK properties of TQ were improved and indicated that the drug behaves linearly. The Tmax, Cmax, and elimination half-life of TQ were found to be 3.96 ± 0.19 hours, 4811.33 ± 55.52 ng/mL, and 4.4933 ± 0.015 hours, respectively, indicating that TQ is suitable for extravascular administration.Conclusion: NLCs could be a promising vehicle for the oral delivery of TQ and improve its gastroprotective properties.Keywords: lipid based nanoparticles, black seed oil, gastric ulce

Evidence of the gastroprotective and anti-Helicobacter pylori activities of β-mangostin isolated from Cratoxylum arborescens (vahl) blume

Heyam Mohamed Ali Sidahmed,1 Najihah Mohd Hashim,1 Syam Mohan,2 Siddig Ibrahim Abdelwahab,2 Manal Mohamed Elhassan Taha,2 Firouzeh Dehghan,3 Maizatulakmal Yahayu,4 Gwendoline Cheng Lian Ee,5 Mun Fai Loke,6 Jamuna Vadivelu6 1Department of Pharmacy, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia; 2Medical Research Center, Jazan University, Jazan, Saudi Arabia; 3Department of Exercise Science, Sports Centre, University of Malaya, Kuala Lumpur, 4Department of Bioproduct Research and Innovation, Institute of Bioproduct Development (IBD), Universiti Teknologi Malaysia (UTM), Johor Bahru, 5Department of Chemistry, Faculty of Science, Universiti Putra Malaysia (UPM), Serdang, 6Department of Medical Microbiology, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia Purpose: β-Mangostin (BM) from Cratoxylum arborescens demonstrated various pharmacological activities such as anticancer and anti-inflammatory. In this study, we aimed to investigate its antiulcer activity against ethanol ulcer model in rats. Materials and methods: BM was isolated from C. arborescens. Gastric acid output, ulcer index, gross evaluation, mucus production, histological evaluation using hematoxylin and eosin and periodic acid–Schiff staining and immunohistochemical localization for heat shock protein 70 (HSP70) and Bax proteins were investigated. Possible involvement of reduced glutathione, lipid peroxidation, prostaglandin E2, antioxidant enzymes, superoxide dismutase and catalase enzymes, radical scavenging, nonprotein sulfhydryl compounds, and anti-Helicobacter pylori were investigated. Results: BM showed antisecretory activity against the pylorus ligature model. The pretreatment with BM protect gastric mucosa from ethanol damaging effect as seen by the improved gross and histological appearance. BM significantly reduced the ulcer area formation, the submucosal edema, and the leukocytes infiltration compared to the ulcer control. The compound showed intense periodic acid–Schiff staining to the gastric mucus layer and marked amount of alcian blue binding to free gastric mucus. BM significantly increased the gastric homogenate content of prostaglandin E2 glutathione, superoxide dismutase, catalase, and nonprotein sulfhydryl compounds. The compound inhibited the lipid peroxidation revealed by the reduced gastric content of malondialdehyde. Moreover, BM upregulate HSP70 expression and downregulate Bax expression. Furthermore, the compound showed interesting anti-H. pylori activity. Conclusion: Thus, it could be concluded that BM possesses gastroprotective activity, which could be attributed to the antisecretory, mucus production, antioxidant, HSP70, antiapoptotic, and anti-H. pylori mechanisms. Keywords: gastric ulcer, reactive oxygen species, heat shock protein 7