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Halimium halimifolium (Hh) is a shrub used in Algerian folk medicine to treat gastrointestinal pain. An UHPLC-PDA-ESI/MSn method was developed to identify the metabolic profile of the traditionally used infusion (Hh-A) from the aerial parts. The structures of flavanols were confirmed by NMR analysis after the isolation procedure from a hydrohalcolic extract (Hh-B) that also allowed for the identification of phenolic acids, an aryl butanol glucoside, and different derivatives of quercetin, myricetin, and kaempferol. Tiliroside isomers were the chemical markers of Hh-A and Hh-B (54.33 and 36.00 mg/g, respectively). Hh-A showed a significant scavenging activity both against the radicals 1,1-diphenyl-2-picrylhydrazyl and 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (EC50 = 10.49 µg/mL and TEAC value = 1.98 mM Trolox/mg infusion) and the lipopolysaccharide-induced reactive oxygen species release in A375 and HeLa cells. Moreover, the antihyperglycemic properties, by inhibiting the α -amylase and α -glucosidase enzymes (IC50 = 0.82 mg/mL and 25.01 µg/mL, respectively), were demonstrated. To upgrade the therapeutic effect, a microencapsulation process is proposed as a strategy to optimize stability, handling, and delivery of bioactive components, avoiding the degradation and loss of the biological efficacy after oral intake. Hh-loaded microparticles were designed using cellulose acetate phthalate as the enteric coating material and spray drying as a production process. The results showed a satisfactory process yield (67.9%), encapsulation efficiency (96.7%), and micrometric characteristics of microparticles (laser-scattering, fluorescent, and scanning electron microscopy). In vitro dissolution studies (USPII-pH change method) showed that Hh-loaded microparticles are able to prevent the release and degradation of the bioactive components in the gastric tract, releasing them into the intestinal environment. [ABSTRACT FROM AUTHOR]

BioActive Compounds (BACs) recovered from food or food by-product matrices are useful in maintaining well being, enhancing human health, and modulating immune function to prevent or to treat chronic diseases. They are also generally seen by final consumers as safe, non-toxic and environment-friendly. Despite the complex process of production, chemical characterization, and assessment of health effects, BACs must also be manufactured in stable and bioactive ingredients to be used in pharmaceutical, food and nutraceutical industry. Generally, vegetable derivatives occur as sticky raw materials with pervasive smell and displeasing flavor. Also, they show critical water solubility and dramatic stability behavior over time, involving practical difficulties for industrial use. Therefore, the development of novel functional health products from natural sources requires the design of a suitable formulation to delivery BACs at the site of action, preserve stability during processing and storage, slow down the degradation processes, mask lousy tasting or smell, and increase the bioavailability, while maintaining the BACs functionality. The present review focuses on human health benefits, BACs composition, and innovative technologies or formulation approaches of natural ingredients from some selected foods and by-products from industrial food transformations.

Nintedanib is an orally administered intracellular tyrosine kinase inhibitor approved for idiopathic pulmonary fibrosis. Differently from oral treatment, dry powder inhalers (DPIs) can deliver a higher drug concentration at the target site, reducing doses and systemic side effects. The aim of this work was to develop dry powders of Nintedanib with properties suitable for inhalation therapy. Particles were prepared by spray drying the drug alone (3–5% w/v) or with appropriate excipients, from different hydroalcoholic solutions i.e., water/ethanol (7/3 v/v) or water/isopropyl alcohol (from 7/3 v/v to 5/5 v/v) mixtures. The powders obtained were characterized in terms of process yield, particle size distribution, morphology, density and aerodynamic properties. The results indicated that leucine improved the aerosol performance of the powders, increasing the value of the fine particle fraction (FPF) from 47.9 % in the drug only batches to 73.1 % using 5 % w/w leucine. This improvement was attributed to the ability of the amino acid to change both the surface area of the particles and the fluidity of the powder. Therefore, this study demonstrated the possibility of developing dry powder of Nintedanib for local administration in the lungs for the treatment of pulmonary fibrosis.

The phytochemical investigation of Gymnocarpos decander aerial parts extract afforded two new saponins, 3-O-β-D-glucuronopyranosyl-2β,3β,16α,23-tetrahydroxyolean-12-en-28-O-β-D-apiofuranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl ester (1), 3-O-β-D-glucuronopyranosyl-2β,3β,16α-trihydroxyolean-12-en-28-O-α-L-rhamnopyranosyl-(1→3)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl ester (2), and three new flavonol glycosides, isorhamnetin 3-O-2''''-O-acetyl-β-D-xylopyranosyl-(1→6)-[β-D-apiofuranosyl-(1→2)]-β-D-glucopyranoside (3), isorhamnetin 3-O-2'''-O-acetyl-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside (4), and quercetin 3-O-2'''-O-acetyl-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside (5), together with three known compounds. Their structures were determined by spectroscopicmethods including 1D and 2D NMR analysis and high-resolution mass spectrometry. The newisolateswere investigated for their potential cytotoxic activity on three cancer cell lines. Compounds 1 and 2 showedmoderate antiproliferative activity. [ABSTRACT FROM AUTHOR]

Pharmacological evidences have correlated a low incidence of osteoporosis, breast cancer, cardiovascular disease, and colon cancer in Asian populations, high consumers of soya, to the properties of soy isoflavones, more specifically to daidzein and genistein. However, in spite of the potent biological activity, their poor water solubility has a strong negative effect on bioavailability. In this study, an innovative technique, nano spray drying, was used to obtain nanoparticles loaded with a soybean dry extract while carboxymethyl cellulose was used as the excipient. The optimization of the process conditions allowed for the manufacturing of stable nanoparticles with a mean size of around 650 nm, a narrow size distribution, and a high encapsulation efficiency (between 78% and 89%). The presence of carboxymethyl cellulose was able to stabilize the isoflavone extract and enhance its affinity with aqueous media, strongly increasing its permeation through biological membranes up to 4.5-fold higher than pure soy isoflavone extract raw material and twice its homologous minispray-dried formulation. These results are very useful for the administration of the extract, either topically or orally, suggesting that the isoflanones extract nanoparticulate powder obtained by nano spray drying has great potential to enhance extract bioavailability and could be used as an ingredient to be enclosed in dietary supplements and nutraceutical and cosmeceutical products. [ABSTRACT FROM AUTHOR]

An investigation of a chloroform-soluble extract from the roots of Paeonia rockiissp. rockiiyielded three new noroleanane triterpenoids (1–3) together with 19 known compounds. Their structures were established by analysis of the spectroscopic data. The effects of this chloroform-soluble extract and its major constituents on cell proliferation and apoptosis of a panel of human cancer cell lines (melanoma M-14, colon cancer HT-29, breast cancer MCF-7) were evaluated by the MTT bioassay and propidium iodide staining, respectively, in comparison with normal human embryonic kidney cells (HEK-293). Two of the triterpenoids, betulinic acid (4) and oleanolic acid (5), and the crude extract were cytotoxic and induced apoptosis selectively in the M-14 melanoma cell line. This effect was reversed by the caspase-inhibitor z-VAD-fmk, suggesting that such action is mediated by caspase-3 activation.

Three new saponins (1−3) and a known saponin, together with four known polyphenolic compounds, have been isolated from the fermented and dried leaves of Fadogia ancylantha(Makoni tea). The structures of compounds 1−3were established by analysis of their spectroscopic data. Both an ethanol−water extract of F. ancylanthaand its phenolic constituents showed significant free-radical-scavenging and antimicrobial activities. No cytotoxicity, as evaluated by analysis of hypodiploid nuclei in HUVEC cells using propidium iodide staining, was observed for either the plant crude extract or its constituents.

The composition of a centrifuged product obtained from the fresh leaves and stems of Melissa officinalisand skin irritation in the reconstituted human epidermis (Episkin model) have been investigated in comparison to the EtOH−H2O (1:1) extract obtained by Soxhlet from the dried plant. Two new sulfated triterpenes (1and 2) and two ionol derivatives have been isolated for the first time from Melissa officinalistogether with caffeic and rosmarinic acids. The structures of compounds 1and 2were established by analysis of their spectroscopic data. Both the centrifuged material and its major constituents neither affected cell viability nor caused the release of pro-inflammatory mediators or the decrease of trans-epithelial electrical resistance (TEER) in the reconstituted human epidermis.

A methanol extract of the dried bark of Liriosma ovataafforded two new isoprenoid glycosides, a eudesmane sesquiterpene, 1α(β- d-glucopyranosyloxy)eudesma-3α,4β, 11-triol ( 1), and a C 13-norisoprenoid, 3α,6α-dihydroxymegastigman-7-en-9-one 3- O-β- d-apiofuranosyl-(1→6)-β- d-glucopyranoside ( 2), as well as a known constituent, isopropyl-β- d-apiofuranosyl-(1→6)-β- d-glucopyranoside ( 3). The structures of 1and 2were determined using spectroscopic methods. The methanol extract had a significant topical anti-inflammatory activity (ID 50, dose inducing 50% edema inhibition = 780 µg/cm 2) about 8 times less than that of indomethacin (ID 50, 93 µg/cm 2) assayed by the croton oil ear test in mice. In addition, the chloroform extract and compounds 1and 2showed weak antimicrobial activity against S taphylococcus aureus(MIC = 5.1, 2.1, and 4.0 mg/mL, respectively) using a broth microdilution assay.

Six new triterpenes ( 1– 6) and four known compounds have been isolated from dried stems and leaves of Melissa officinalis. The known compounds were identified as quadranoside III, salvianic acid A, rosmarinic acid, and luteolin. The structures of compounds 1– 6were established by analysis of spectroscopic data. Free radical scavenging and antimicrobial activities of the extracts and of rosmarinic acid, the major component, were evaluated.

A new phenolic compound, 6′-O-sulfonyl-salidroside (1), together with fifteen known compounds, were isolated from the all parts of Limonium pruinosum. Their structures were elucidated by 1D and 2D NMR experiments including 1D TOCSY, DQF-COSY, HSQC and HMBC spectroscopy, as well as ESIMS analysis. The antioxidant activity of the extracts and all isolated compounds was evaluated by DPPH test.

Fresh juice from bergamot (Citrus bergamiaRisso) has been studied to evaluate the polyphenolic composition by HPLC-DAD analysis and total polyphenols content by UV method. The main constituent, Naringin, has been selected as analytical and biological marker of the juice. Juice has been loaded onto maltodextrin matrix by spray-drying. The produced maltodextrin/juice powder (BMP) showed neither significant change in total polyphenols content nor decrease in antioxidant properties with respect to fresh juice. Moreover, BMP displayed high in vitrodissolution rate of the bioactive constituents in water and in simulated biological fluids. BMP appears as promising functional raw material for food, nutraceutical and pharmaceutical products. With this aim, a formulation study to develop tablets (BMT) for oral administration has been also performed. The produced solid oral dosage form preserved high polyphenols content, showed complete disaggregation in few minutes and satisfying dissolution rate of the bioactive constituents in simulated biological fluids.