Several studies have demonstrated anti-carcinogenic and antitumor activity for many essential oils obtained from various plant species. They may be used in substitution to or in addition to conventional anti-cancer therapy. Although many studies report possible mechanisms of action for essential oils compounds, more studies are necessary in order to apply them safely and appropriately in cancer therapy.
The enzyme inhibition by natural and/ or low-cost compounds may represent a valuable adjunct to traditional serotherapy performed in cases of snakebite, mainly with a view to mitigate the local effects of envenoming. The objective of this study was to evaluate possible interactions between vitamins and enzymes that comprise Bothrops atrox and Crotalus durissus terrificus venoms, in vitro. Proteolysis inhibition assays (substrates: azocasein, collagen, gelatin and fibrinogen), hemolysis, coagulation, hemagglutination were carried out using different proportions of vitamins in face of to inhibit minimum effective dose of each venom. The vitamins were responsible for reducing 100% of breaking azocasein by C.d.t. venom, thrombolysis induced by B. atrox and fibrinogenolysis induced by both venoms. It is suggested the presence of interactions between vitamin and the active site of enzymes, for example the interactions between hydrophobic regions present in the enzymes and vitamin E, as well as the inhibitions exercised by antioxidant mechanism.
Disintegrins are non-enzymatic proteins that interfere on cell–cell interactions and signal transduction, contributing to the toxicity of snake venoms and play an essential role in envenomations. Most of their pharmacological and toxic effects are the result of the interaction of these molecules with cell surface ligands, which has been widely described and studied. These proteins may act on platelets, leading to hemorrhage, and may also induce apoptosis and cytotoxicity, which highlights a high pharmacological potential for the development of thrombolytic and antitumor agents. Additionally, these molecules interfere with the functions of integrins by altering various cellular processes such as migration, adhesion and proliferation. This review gathers information on functional characteristics of disintegrins isolated from snake venoms, emphasizing a comprehensive view of the possibility of direct use of these molecules in the development of new drugs, or even indirectly as structural models.
Dyslipidemias are associated with the incidence of cardiovascular diseases, obesity, diabetes, hypertension and hepatic steatosis, being the cause of morbidity and mortality. This study investigated the effects of lychee peel flour (PF) on serum levels of total cholesterol (TC), low-density lipoprotein (LDL-c), triacylglycerols (TAG) and various parameters related to obesity, in rats fed a hypercholesterolemic diet. Therefore, 20 male rats were used. In the first 21 days, the animals were fed a hypercholesterolemic diet, except for control group. In the following 21 days, their diets were modified, and they received a standard diet (Control); hypercholesterolemic (Hyper); hypercholesterolemic + 5% PF (PF5) and hypercholesterolemic + 10% PF (PF10). The results revealed that PF intake attenuated weight gain, reduced body mass index, glucose and the levels of TAG, TC, LDL-c, hepatic enzymes and leptin, besides the percentage of hepatic lipids, liver lipid peroxidation and frequency of severe steatosis. Histological studies of the aorta did not show the formation of the atheromatous plaque. These results reinforce its potential to reduce the risk of diseases associated with obesity.
Propolis is a complex mixture of phytochemicals, with antibacterial, antiinflammatory, and healing properties. All-trans retinoic acid is implicated in wound healing by stimulating angiogenesis, cell recruitment, extracellular matrix deposition, and reepithelization. The incorporation of both agents to a polymeric wound dressing composed of poly (vinyl alcohol) and sodium alginate may result in improved healing allied to controlled release, fluid uptake, and wound protection. In the present work, we have physically characterized this wound dressing and analyzed its release kinetics. The anti-inflammatory capacity was assayed. SEM images showed a highly porous structure with a diverse morphology. FTIR spectra displayed a highly cross-linked structure with both polymers connected by hydrogen bonds and acetal bridges. The wound dressings were able to retain great volumes of PBS. Propolis and vitamin A releasing behavior were maintained for 6 h. The concentrations of the biologically active substances were capable of promoting anti-inflammatory action in an erythrocyte membrane stabilization model. The wound dressings obtained here showed adequate physical properties. The fabrication process did not affect the anti-inflammatory capacity. Further tests are needed to ensure the biocompatibility and to assess other biological activities of the therapeutic agents.
Agro‐industrial wastes are promising sources of phytochemicals for the development of products to be used in health promotion and maintenance. In this study, extracts from acerola bagasse (AB) were characterized by HPLC, and evaluated according to its modulatory action on phospholipases A2 and proteases involved in processes such as inflammation and blood clotting. Snake venoms were used as biological tools once they have high functional and structural homology between their enzymes and human enzymes. Two types of extracts were prepared from AB: aqueous and methanolic. These extracts, evaluated at different proportions (venom:extract, w:w), significantly inhibited the phospholipase activity induced by the venoms of Bothrops moojeni, Bothrops atrox (11% to 31%), and Crotalus durissus terrificus (C. d. t.) (11% to 19%). The hemolytic activity induced by the venoms of B. moojeni and C. d. t. was better inhibited by the methanolic extract (inhibition between 23% and 48%). Thrombolysis induced by the venoms of B. moojeni and C. d. t. was inhibited by both extracts, with inhibition ranging from 13% to 63% for the aqueous extract, and from 12% to 92% for the methanolic one. Both extracts increased the time of coagulation induced by the venoms of B. moojeni and Lachesis muta muta in 26 and up to 68 s. These inhibitory actions were related to the following phenolic compounds present in the extract of AB: gallic acid, catechin, epigallocatechin gallate, epicatechin, syringic acid, p‐coumaric acid, and quercetin. Additional studies are needed to confirm their potential use for nutraceutical purposes. Practical Application Agro‐industrial wastes are promising sources of phytochemicals for the development of products that can be used by pharmaceutical, cosmetics, and food industries. Studies report the use of the acerola bagasse extract in health improvement. However, its toxic‐pharmacological characterization is still scarce. In this study, the extracts of acerola bagasse presented phenolic compounds that can modulate the activity of enzymes such as phospholipases A2 and proteases that act on the coagulant/anticoagulant and thrombotic/thrombolytic activities and the break of phospholipids, decreasing the inflammation and platelet aggregation. Although the in vivo effects of the extracts are not fully understood, this study shed light upon the possibilities of their usage.
A large number of natural compounds, such as phenolic compounds, have been scientifically evaluated in the search for enzyme inhibitors. The interactions between the phenolic compound p‐coumaric acid and the enzymes present in snake venoms (used as research tools) were evaluated in vitro and in silico. The p‐coumaric acid was able to inhibit 31% of the phospholipase activity induced by Bothrops alternatus venom, 27% of the hemolytic activity induced by B. moojeni, 62.5% of the thrombolytic activity induced by B. jararacussu, and approximately 27% of the activity thrombosis induced by Crotalus durissus terrificus. Previous incubation of p‐coumaric acid with the venoms of B. atrox and B. jararacussu increased the coagulation time by 2.18 and 2.16‐fold, respectively. The activity of serine proteases in B. atrox and B. jararacussu venoms was reduced by 60% and 66.34%, respectively. Computational chemistry analyses suggests the specific binding of p‐coumaric acid to the active site of proteases through hydrogen and hydrophobic interactions. The phenolic compound evaluated in this work has great potential in therapeutic use to both prevent and treat hemostatic alterations, because the venom proteins inhibited by the p‐coumaric acid have high homology with human proteins that have a fundamental role in several pathologies.
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