Ziziphus lotus (L.) Lam. as a source of health promoting products: metabolomic profile, antioxidant and tyrosinase inhibitory activities

The methanolic extract of the stem bark of a wild species of jujube, Ziziphus lotus (L.) Lam., growing in Sicily, was chemically and biologically investigated. The chemical profile was defined by UHPLC-HR-ESI-Orbitrap/MS analysis whereas antioxidant and tyrosinase inhibitory activities were investigated by in vitro assays. The extract showed a high total phenolic and flavonoid content (TPC = 271.65 GAE/g and TFC = 188.11 RE/g extract). Metabolomic analysis revealed a rich phytocomplex characterized by phenols, cyclopeptide alkaloids, and triterpenoid saponins, some of which here detected for the first time. The mushroom tyrosinase inhibition assay displayed that the methanolic extract efficiently inhibits the monophenolase and diphenolase activity. Furthermore, the extract showed a strong ability to scavenge DPPH, a good Fe3+ reducing antioxidant power, in addition to a Fe2+ chelating activity. Taken together, these results suggest possible novel applications of wild jujube stem bark as a source of potential skin-care agents with several uses in pharmaceutical and cosmetic industries

Antiangiogenic activity of iridoids from Lamiaceae and Plantaginaceae species

Iridoids are a group of natural compounds, occurring in a great number of plant families, usually as glycosides. The considerable interest in iridoids is due to their ecological role as plant protectant and to their wide spectrum of biological activities, including cardioprotection, neuroprotection, anti-inflammatory, and anticancer activities [1]. Interestingly, some iridoid glycosides were found to have a potent antiangiogenic activity [2-3]. Angiogenesis process may be involved in tumour development, thus its inhibition appears to be a promising approach in anti-inflammatory and anticancer therapies [4]. Within this context, the aim of the present study was the isolation and characterization of iridoid derivatives from two Lamiaceae species, Stachys ocymastrum (L.) Briq and Premna resinosa (Hochst.) Schauer leaves, and from Anarrhinum pedatum Desf. aerial parts, belonging to Plantaginaceae family, together with the evaluation of their antiangiogenic potential. The chemical study of investigated plants afforded to the isolation of one new and four known iridoid glycosides from S. ocymastrum, nine known iridoid diglycosides from P. resinosa, and ten new and five known iridoid glycosides from A. pedatum, identified by NMR and MS analyses. The antiangiogenic effects of the isolates were reported on new blood vessels formation using two in vivo models: zebrafish embryos and chick embryo chorioallantoic membrane [5]. Among the tested iridoids, -hydroxyipolamiide, ipolamiide, buddlejoside A5, and 6′-O-menthiafoloylmussaenosidic acid-11-(5-O-β-D-fructopyranosyl) ester showed a significant antiangiogenic activity in both assays, reducing the growth of blood vessels. Weaker antiangiogenic effects were also observed for some other iridoids, thus suggesting this class of compounds as promising antiangiogenic agents

Exploiting the 1-(4-fluorobenzyl)piperazine fragment for the development of novel tyrosinase inhibitors as anti-melanogenic agents: Design, synthesis, structural insights and biological profile

The development of Tyrosinase inhibitors (TYRIs) could represent an efficacious strategy for pharmacological intervention on skin pathologies related to aberrant production of melanin. Based on in silico studies we designed and tested a library of twenty-four compounds bearing the 4-(4-fluorobenzyl)piperazin-1-yl]-fragment. As result, we identified several compounds with excellent inhibit effects at low micromolar concentration against TYR from Agaricus bisporus (TyM). Among them, compound 25 (IC50 = 0.96 μM) proved to be ∼20-fold more potent than the reference compound kojic acid (IC50 = 17.76 μM) having wide applications in the cosmetics and pharmaceutical industries. The mode of interaction of active inhibitor 25 was deciphered by means of crystallography as well as molecular docking and these results were consistent with kinetic experiments. Moreover, the identified compound 25 exhibited no considerable cytotoxicity and showed anti-melanogenic effects on B16F10 melanoma cells. Therefore, a combination of computational and biochemical approaches could represent a rational guidelines for further structural modification of this class of compounds as future anti-melanogenic agents

Consensus statement from the international consensus meeting on post-traumatic cranioplasty

Abstract: Background: Due to the lack of high-quality evidence which has hindered the development of evidence-based guidelines, there is a need to provide general guidance on cranioplasty (CP) following traumatic brain injury (TBI), as well as identify areas of ongoing uncertainty via a consensus-based approach. Methods: The international consensus meeting on post-traumatic CP was held during the International Conference on Recent Advances in Neurotraumatology (ICRAN), in Naples, Italy, in June 2018. This meeting was endorsed by the Neurotrauma Committee of the World Federation of Neurosurgical Societies (WFNS), the NIHR Global Health Research Group on Neurotrauma, and several other neurotrauma organizations. Discussions and voting were organized around 5 pre-specified themes: (1) indications and technique, (2) materials, (3) timing, (4) hydrocephalus, and (5) paediatric CP. Results: The participants discussed published evidence on each topic and proposed consensus statements, which were subject to ratification using anonymous real-time voting. Statements required an agreement threshold of more than 70% for inclusion in the final recommendations. Conclusions: This document is the first set of practical consensus-based clinical recommendations on post-traumatic CP, focusing on timing, materials, complications, and surgical procedures. Future research directions are also presented

Chemical composition and antimicrobial activity of Momordica charantia seed essential oil

The essential oil obtained from the seeds of Momordica charantia was analyzed by GC/MS. Twenty-five components, representing 90.9% of the oil, were identified. The main constituents were trans-nerolidol, apiole, cis-dihydrocarveol and germacrene D. Furthermore, the oil was tested for its antibacterial and antifungal activities. Staphylococcus aureus was found to be the most sensitive microorganism with MIC values < 500 μg/ml

Phytochemical screening of Artemisia arborescens L. by means of advanced chromatographic techniques for identification of health-promoting compounds

Artemisia arborescens, also known as tree wormwood, is a typical species of the Mediterranean flora. It has been used in folk medicine for its antispasmodic, anti-pyretic, anti-inflammatory, and abortifacient properties. In the current study, the application of multidimensional comprehensive gas chromatog- raphy (GC × GC), allowed to obtain a detailed fingerprint of the essential oil from A. arborescens aerial parts, highlighting an abundant presence of chamazulene followed by camphor, beta-thujone, myrcene, and alpha-pinene. Moreover, flavonoids in the dichloromethane extract were analyzed by means of liquid chromatography with photodiode array and atmospheric pressure chemical ionization-mass spectrom- etry detections (HPLC-PDA and HPLC-APCI-MS). Six polymethoxyflavones were identified and three of them, including chrysosplenetin, eupatin, and cirsilineol, were described in this species for the first time. The anti-angiogenic activity was investigated in the dichloromethane extract by two in vivo models, chick chorioallantoic membrane (CAM) and zebrafish embryos. Results showed that this extract pro- duced a strong reduction on vessel formation, both on zebrafish (57% of inhibition, 0.1 mg/mL) and chick chorioallantoic membrane (58% of inhibition, 0.8 mg/mL). The high separation power and sensitivity of the analytical methodology applied confirmed the safety of A. arborescens essential oil for human consumption, due to the very low level of the psychotrope alpha-thujone determined. Moreover, the knowledge of the flavonoidic profile holds a great significance for the use of A. arborescens as a valuable source of anti-angiogenic compounds that might contribute to the valorization of the phytotherapeutic potential of this plant

Anti-angiogenic activity of iridoids from Galium tunetanum

The phytochemical study of Galium tunetanum Lam., Rubiaceae, leaves led to the isolation of thirteen compounds from the chloroform-methanol and the methanol extracts, including six iridoid glycosides, one non-glycoside iridoid, two p-coumaroyl iridoid glycosides, two phenolic acids, and two flavonoid glycosides. The structural determination of the isolated compounds was performed by mono- and bidimensional NMR spectroscopic data, as well as ESI-MS experiments. All compounds were isolated from this species for the first time. The anti-angiogenic effects of the isolated iridoids were also reported on new blood vessels formation using the chick embryo chorioallantoic membrane as in vivo model. Results showed that among the isolated iridoids tested at the dose of 2 μg/egg, asperuloside (1), geniposidic acid (2), and iridoid V1 (3) reduced microvessel formation of the chorioallantoic membrane on morphological observations using a stereomicroscope. The anti-angiogenic effects of the active compounds, expressed as percentages of inhibition versus control, were 67% (1), 59% (2), and 54% (3), respectively. In addition, the active compounds were able to inhibit angiogenesis in the chorioallantoic membrane assay, in a dose-dependent manner (0.5-2 μg/egg) as compared to the standard retinoic acid

Anti-ulcer, anti-inflammatory and antioxidant activities of the n-butanol fraction from Pteleopsis suberosa stem bark

Pteleopsis suberosa Engl. et Diels (Combretaceae) is a tree distributed in many African countries. The decoction from the stem bark is orally administered for the treatment of gastric ulcers in traditional medicine. Previous pharmacological studies reported the anti-ulcer activity of extracts from P. suberosa stem bark. In the present study, the anti-ulcer and anti-inflammatory effects of the n-butanol fraction (RBuOH) obtained from a methanol extract of P. suberosa bark were investigated on ethanol-induced gastric ulcers in rats and carrageenan-induced paw oedema in mice. Misoprostol (0.50 mg/kg, p.o.) and indomethacin (8.00 mg/kg, p.o.) were used as positive controls for anti-ulcer and anti-inflammatory activities, respectively. Results showed that RBuOH treatment significantly reduced the incidence of gastric lesions (50 mg/kg, P < 0.05; 100 and 200 mg/kg, P < 0.01) and restored the decreased levels of total sulfhydryl groups (T-SH) and non-protein sulfhydryl groups (NP-SH) (50, 100 mg/kg, P < 0.05; 200 mg/kg, P < 0.01) in the stomach homogenate. Moreover, RBuOH treatment attenuated MDA levels as index of lipid peroxidation in gastric mucosa. Administration of RBuOH at the same dosage (50, 100 and 200 mg/kg) reduced significantly (P < 0.01) carrageenan-induced paw oedema in dose-dependent manner (from 42.81% to 87.81% inhibition, 5 h after carrageenan injection). The anti-inflammatory effect of RBuOH at 200 mg/kg was comparable with that of indomethacin. Finally, RBuOH proved to possess elevated free radical scavenger capacity on 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay (IC50 23.48 μg/ml) which may contribute to the observed anti-ulcer and anti-inflammatory activities