Green strategies for the valorization of industrial medicinal residues of Serenoa repens small (saw palmetto) as source of bioactive compounds.

Serenoa repens is a medicinal plant well-known for its therapeutic potential in treating various urological disorders and prevention of prostatic cancer. However, the extraction process in the pharmaceutical industry leads to the generation of plant residues, typically discarded, wasting valuable resources. In this study, we aimed to explore a series of green extraction strategies to effectively valorize the residues of Serenoa repens fruits.

Valorization of the Antioxidant Effect of Mantua PGI Pear By-Product Extracts: Preparation, Analysis and Biological Investigation.

For improving the management of the production chain of PGI Mantua pears (which comprises many varieties, including Abate Fetel), applying the cardinal principles of circular economy and sustainability, the fruits with diseases or defects were recovered for producing dried rounds of pears from the Abate Fetel cultivar, a new product with high nutritional value that extends the remaining life. This process led to the production of secondary and residual by-products, which are mainly composed of the highest and lowest part of the fruits, comprising seeds, pulps, peels and petioles. Hence, this study was focused on the valorization of these secondary by-products of Abate Fetel pears through the production of pear extracts using traditional and "green" extraction methods that involve the use of supercritical CO fluid extraction.

Synthesis and Characterization of Curcumin-Loaded Nanoparticles of Poly(Glycerol Sebacate): A Novel Highly Stable Anticancer System.

The research for alternative administration methods for anticancer drugs, towards enhanced effectiveness and selectivity, represents a major challenge for the scientific community. In the last decade, polymeric nanostructured delivery systems represented a promising alternative to conventional drug administration since they ensure secure transport to the selected target, providing active compounds protection against elimination, while minimizing drug toxicity to non-target cells. In the present research, poly(glycerol sebacate), a biocompatible polymer, was synthesized and then nanostructured to allow curcumin encapsulation, a naturally occurring polyphenolic phytochemical isolated from the powdered rhizome of L.

Selective Supercritical CO Extraction and Biocatalytic Valorization of L. Industrial Residuals.

The valorization of biomass residuals constitutes a key aspect of circular economy and thus a major challenge for the scientific community. Among industrial wastes, plant residuals could represent an attractive source of bioactive compounds. In this context, a residue from the industrial extraction of L.

Stereoselective Biocatalyzed Reductions of Ginger Active Components Recovered from Industrial Wastes.

Ginger is among the most widespread and widely consumed traditional medicinal plants around the world. Its beneficial effects, which comprise e. g.

Green Extraction Strategies for Sea Urchin Waste Valorization.

Commonly known as "purple sea urchin," occurs in the Mediterranean Sea and the eastern Atlantic Ocean. This species is a highly appreciated food resource and Italy is the main consumer among the European countries. Gonads are the edible part of the animal but they represent only a small fraction (10-30%) of the entire sea urchin mass, therefore, the majority ends up as waste.

Pectin-Based Formulations for Controlled Release of an Ellagic Acid Salt with High Solubility Profile in Physiological Media.

Among bioactive phytochemicals, ellagic acid (EA) is one of the most controversial because its high antioxidant and cancer-preventing effects are strongly inhibited by low gastrointestinal absorption and rapid excretion. Strategies toward an increase of solubility in water and bioavailability, while preserving its structural integrity and warranting its controlled release at the physiological targets, are therefore largely pursued. In this work, EA lysine salt at 1:4 molar ratio (EALYS), exhibiting a more than 400 times increase of water solubility with respect to literature reports, was incorporated at 10% in low methoxylated (LM) and high methoxylated (HM) pectin films.

Sulfated Oligomers of Tyrosol: Toward a New Class of Bioinspired Nonsaccharidic Anticoagulants.

Sulfated phenolic polymers have extensively been investigated as anticoagulant agents in view of their higher bioavailability and resistance to degradation compared to heparins, allowing for increased half-lives. In this frame, we report herein the preparation of sulfated derivatives of tyrosol, one of the most representative phenolic constituents of extra virgin olive oil, by different approaches. Mild sulfation of OligoTyr, a mixture of tyrosol oligomers, that has been reported to possess antioxidant properties and osteogenic activity, afforded OligoTyrS I in good yields.

Bioactive Phenolic Compounds From Agri-Food Wastes: An Update on Green and Sustainable Extraction Methodologies.

Phenolic compounds are broadly represented in plant kingdom, and their occurrence in easily accessible low-cost sources like wastes from agri-food processing have led in the last decade to an increase of interest in their recovery and further exploitation. Indeed, most of these compounds are endowed with beneficial properties to human health (e.g.

Synthesis of Polylactic Acid Initiated through Biobased Antioxidants: Towards Intrinsically Active Food Packaging.

Polylactide (PLA)-based polymers, functionalized with biobased antioxidants, were synthesized, to develop an intrinsically active, biobased and potentially biodegradable material for food packaging applications. To achieve this result, phenolic antioxidants were exploited as initiators in the ring opening polymerization of l-lactide. The molecular weight, thermal properties and in vitro radical scavenging activity of the polymers obtained were compared with the ones of a PLA Natureworks 4043D, commonly used for flexible food packaging applications.

Antioxidant Properties of Agri-food Byproducts |and Specific Boosting Effects of Hydrolytic Treatments.

Largely produced agri-food byproducts represent a sustainable and easily available source of phenolic compounds, such as lignins and tannins, endowed with potent antioxidant properties. We report herein the characterization of the antioxidant properties of nine plant-derived byproducts. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing/antioxidant power (FRAP) assays indicated the superior activity of pomegranate peels and seeds, grape pomace and pecan nut shell.

Ellagic Acid Recovery by Solid State Fermentation of Pomegranate Wastes by and : A Comparison.

Fermentation in solid state culture (SSC) has been the focus of increasing interest because of its potential for industrial applications. In previous studies SSC of pomegranate wastes by has been extensively developed and optimized for the recovery of ellagic acid (EA), a high value bioactive. In this study we comparatively investigated the SSC of powdered pomegranate husks by and and evaluated the recovery yields of EA by an ultrasound and microwave-assisted 7:3 water/ethanol extraction.

Green Corrosion Inhibitors from Natural Sources and Biomass Wastes.

Over the past decade, green chemistry has been emphasizing the importance of protecting the environment and human health in an economically beneficial manner aiming at avoiding toxins and reducing wastes. The field of metallic materials degradation, generally faced by using toxic compounds, found a fertile research field in green chemistry. In fact, the use of inhibitors is a well-known strategy when metal corrosion needs to be prevented, controlled, or retarded.

Synthesis and antimycobacterial activity of (+)-usnic acid conjugates.

New therapeutics are urgently needed to fight tuberculosis and mycobacteria-related diseases that are a major health hazard especially in poor countries. Natural products have been the source of important antitubercular drugs in the past and still need to receive attention as a potent reservoir of chemical structures. Fifteen known and two new (+)-usnic acid (a benzofurandione formerly isolated from lichens) enamines and hydrazones are here described and tested against sensitive and multidrug-resistant strains of mycobacteria.

Fermented pomegranate wastes as sustainable source of ellagic acid: Antioxidant properties, anti-inflammatory action, and controlled release under simulated digestion conditions.

Wastes deriving from production of wines by yeast fermentation of Punica granatum (fermented pomegranate wastes, FPW) showed a marked antioxidant activity in a series of conventional chemical tests. HPLC/MS analysis of the methanol extract showed the presence of ellagic acid (EA) as the main phenolic component at levels up to 40% on a w/w basis. Experiments using murine macrophages showed that FPW extract is able to reduce the LPS-induced expression of pro-inflammatory genes IL-1β, TNF-α and iNOS.

A Malaria Transmission-Blocking (+)-Usnic Acid Derivative Prevents Plasmodium Zygote-to-Ookinete Maturation in the Mosquito Midgut.

The evolution of drug resistance is a recurrent problem that has plagued efforts to treat and control malaria. Recent emergence of artemisinin resistance in Southeast Asia underscores the need to develop novel antimalarials and identify new targetable pathways in Plasmodium parasites. Transmission-blocking approaches, which typically target gametocytes in the host bloodstream or parasite stages in the mosquito gut, are recognized collectively as a strategy that when used in combination with antimalarials that target erythrocytic stages will not only cure malaria but will also prevent subsequent transmission.

Synthesis of Resveratrol Derivatives and In Vitro Screening for Potential Cancer Chemopreventive Activities.

New resveratrol (trans-3,4',5-trihydroxystilbene) analogs were synthesized and screened for their in vitro cancer chemopreventive potential using various bioassays relevant for the prevention of carcinogenesis in humans: two assays to detect modulators of carcinogen metabolism (Cyp1A inhibition; determination of NAD(P)H/quinone reductase (QR) activity), three assays to identify radical scavenging and antioxidant properties (DPPH, ORAC, superoxide anion radicals in differentiated HL-60 cells), four assays to determine anti-inflammatory and anti-hormonal effects (iNOS, Cox-1 and aromatase inhibition, anti-estrogenic potential). 3,4',5-Tri-O-methyl resveratrol 1a was about sevenfold more active than resveratrol in inhibiting Cyp1A activity, it was a potent inducer of QR activity, and it showed pure anti-estrogenic activity (whereas resveratrol is a known mixed estrogen (ant)agonist with both estrogenic and anti-estrogenic properties). Dual estrogen ant-/agonist activity was restored in the mono-O-benzyl-substituted derivatives 4b (4'-O-benzyl resveratrol) and 5b (3-O-benzyl resveratrol).

Anticancer and Antibacterial Activity of Hyperforin and Its Derivatives.

Hyperforin is a natural phloroglucinol that has been know for the treatment of depression. Hyperforin displays also antibacterial, antiproliferant and antiangiogenic activity. Synthetic derivatives of hyperforin have also recently been reported to possess increased bioactivity.

An antioxidant bioinspired phenolic polymer for efficient stabilization of polyethylene.

The synthesis, structural characterization and properties of a new bioinspired phenolic polymer (polyCAME) produced by oxidative polymerization of caffeic acid methyl ester (CAME) with horseradish peroxidase (HRP)-H2O2 is reported as a new sustainable stabilizer toward polyethylene (PE) thermal and photo-oxidative degradation. PolyCAME exhibits high stability toward decarboxylation and oxidative degradation during the thermal processes associated with PE film preparation. Characterization of PE films by thermal methods, photo-oxidative treatments combined with chemiluminescence, and FTIR spectroscopy and mechanical tests indicate a significant effect of polyCAME on PE durability.

A small molecule glycosaminoglycan mimetic blocks Plasmodium invasion of the mosquito midgut.

Malaria transmission-blocking (T-B) interventions are essential for malaria elimination. Small molecules that inhibit the Plasmodium ookinete-to-oocyst transition in the midgut of Anopheles mosquitoes, thereby blocking sporogony, represent one approach to achieving this goal. Chondroitin sulfate glycosaminoglycans (CS-GAGs) on the Anopheles gambiae midgut surface are putative ligands for Plasmodium falciparum ookinetes.

Biological evaluation of hyperforin and its hydrogenated analogue on bacterial growth and biofilm production.

Bacterial biofilms are organized communities of microorganisms, embedded in a self-produced matrix, growing on a biotic surface and resistant to many antimicrobial agents when associated with a medical device. These biofilms require the development of new strategies for the prevention and treatment of infectious disease, including the potential use of natural products. One interesting natural product example is Hypericum, a plant genus that contains species known to have antimicrobial properties.

Two new tryptophan derivatives from the seed kernels of Entada rheedei: effects on cell viability and HIV infectivity.

Two new tryptophan derivatives, N-sulfonyl-L-tryptophan (tryptorheedei A) (1) and 3-(N-sulfonylindolyl)-D-lactic acid (tryptorheedei B) (2) together with the known 5-O-β-D-glucopyranosyl-2-hydroxyphenylacetic acid (3), 1-O-methylglucopyranoside, entadamide A, homogentisic acid and 3-O-β-D-glucopyranosyl-β-sitosterol, were isolated from the seed kernels of Entada rheedei (Mimosaceae). Their structures were established using 1D and 2D NMR spectroscopy, mass spectrometry and by comparison with spectroscopic data reported in the literature. Compounds 1 and 2 showed no toxicity to TZM and Human PBMC cells.

Synthesis of a potent antimalarial agent through natural products conjugation.

Au naturel! (+)-Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits an IC(50) value of 1.4 nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.

Synthesis and bioactivity profile of 5-s-lipoylhydroxytyrosol-based multidefense antioxidants with a sizeable (poly)sulfide chain.

Novel polyfunctionalized antioxidants, 5-S-lipoylhydroxytyrosol (1) and its disulfide 2, trisulfide 3, and tetrasulfide 4, were prepared from tyrosol and dihydrolipoic acid in the presence, when appropriate, of sulfur. Compound 1 exhibited significant activity in the ferric reducing/antioxidant power (FRAP) assay (1.60 Trolox equiv), whereas polysulfides 2-4 were more efficient in the DPPH reduction assay (88-93% reduction vs 68% by Trolox).