Natural organosulfur compounds (OSCs) from Allium sativum L. display antioxidant and chemo-sensitization properties, including the in vitro inhibition of tumor cell proliferation through the induction of apoptosis. Garlic water-and oil-soluble allyl sulfur compounds show distinct properties and the capability to inhibit the proliferation of tumor cells. In the present study, we optimized a new protocol for the extraction of water-soluble compounds from garlic at low temperatures and the production of glutathionyl-OSC conjugates during the extraction. Spontaneously, Cys/GSH-mixed-disulfide conjugates are produced by in vivo metabolism of OSCs and represent active molecules able to affect cellular metabolism. Water-soluble extracts, with (GSGaWS) or without (GaWS) glutathione conjugates, were here produced and tested for their ability to release hydrogen sulfide (H2S), also in the presence of reductants and of thiosulfate:cyanide sulfurtransferase (TST) enzyme. Thus, the TST catalysis of the H2S-release from garlic OSCs and their conjugates has been investigated by molecular in vitro experiments. The antiproliferative properties of these extracts on the human T-cell lymphoma cell line, HuT 78, were observed and related to histone hyperacetylation and downregulation of GAPDH expression. Altogether, the results presented here pave the way for the production of a GSGaWS as new, slowly-releasing hydrogen sulfide extract for potential therapeutic applications.
Type 2 diabetes mellitus (DM) is a socially relevant chronic disease with high prevalence worldwide. DM may lead to several vascular, macrovascular, and microvascular complications (cerebrovascular, coronary artery, and peripheral arterial diseases, retinopathy, neuropathy, and nephropathy), often accelerating the progression of atherosclerosis. Dietary therapy is generally considered to be the first step in the treatment of diabetic patients. Among the current therapeutic options, such as insulin therapy and hypoglycemic drugs, in recent years, attention has been shifting to the effects and properties—that are still not completely known—of medicinal plants as valid and inexpensive therapeutic supports with limited side effects. In this review, we report the relevant effects of medicinal plants and nutraceuticals in diabetes. In particular, we paid attention to the organosulfur compounds (OSCs) present in plant extracts that due to their antioxidant, hypoglycemic, anti-inflammatory, and immunomodulatory effects, can contribute as cardioprotective agents in type 2 DM. OSCs derived from garlic (Allium sp.), due to their properties, can represent a valuable support to the diet in type 2 DM, as outlined in this manuscript based on both in vitro and in vivo studies. Moreover, a relevant characteristic of garlic OSCs is their ability to produce the gasotransmitter H2S, and many of their effects can be explained by this property. Indeed, in recent years, several studies have demonstrated the relevant effects of endogenous and exogenous H2S in human DM, including by in vitro and in vivo experiments and clinical trials; therefore, here, we summarize the effects and the underlying molecular mechanisms of H2S and natural H2S donors.
Background: Nigella sativa seeds, commonly referred to as “black cumin”, are rich in a spectrum of biologically active substances and thus associated with a range of potential health benefits. Unlocking the activity of these phytochemicals traditionally requires solvent extraction. Previously, we have explored nanosizing as alternative to liberate biological activity of natural products, such as Solanum incanum, Pterocarpus erinaceus, Loranthus micranthus and Cynomorium coccineum. Objectives: Nanosizing natural products may increase their activity for a number of reasons ranging from an improved bioavailability to physical nano-toxicity. Because Nigella sativa is amenable to being “milled down”, this spice has been employed to explore the underlying causes of increased activity upon mechanical particle size reduction. Methods: Nigella sativa seeds were pre-milled employing a household flour mill followed by extensive grinding exploiting a planetary ball mill. The particles were characterized employing Laser Diffraction, Photon Correlation Spectroscopy and Scanning Electron Microscopy connected with Energy Dispersive X-ray Diffraction. Finally, the samples were evaluated for sterility profile, nematicidal and antioxidant activities. Results: Suspensions containing fairly uniform particles of Nigella sativa showing diameters in the range of 100-1000 nm have been obtained. These nanosuspensions are characterized by a considerably reduced microbial contamination when compared to the bulk material and reasonable antioxidant and nematicidal activity when employed in higher concentrations. This activity is comparable to the ethanolic extract of the seeds and is significantly higher when compared to aqueous extracts. A combination of “sterilization and extraction by milling”, improved liberation of soluble substances from small particles, surface activity and physical nano-activity of the particles itself is likely responsible for the activities observed. Conclusion: Nanosizing of entire natural products provides an interesting alternative to solvent extraction as it results in the liberation of active ingredients and certain additional activities. The resulting nanosuspensions can be investigated further and optimized for applications in Nutrition, Agriculture, Medicine and Cosmetics.
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