Natural products targeting FcεRI receptor for anti-allergic therapeutics.

Mast cells and basophils are important contributors for development of allergic reactions. The activation of these cells via cross-linking of IgE bound to FcεRI by allergen causes the generation of allergic mediators and the reaction of immediate hypersensitivity. Obviously, FcεRI is considered as a key trigger of acute allergic responses. Consequently, FcεRI is regarded as a potential target for downregulation of allergic diseases. So far, numerous synthetic agents have been reported for inhibition of FcεRI expression and FcεRI-IgE interaction. Meanwhile, natural products have received much attention due to their efficacy and safety. Recently, numerous anti-allergic agents from natural products have been revealed as promising inhibitors of allergic reactions via inhibiting the expression of FcεRI subunits as well as blocking FcεRI activation. Thus, the present contribution is mainly focused to describe natural products targeting FcεRI receptor and to emphasize their applicable potential as anti-allergic foods. PRACTICAL APPLICATIONS: Phlorotannins, epigallocatechin-3-gallate, peptides, chitooligosaccharides, and other natural products have been revealed as potential inhibitors of allergic responses. These bioactive agents target to FcεRI receptor by inhibiting expression of FcεRI and blocking interaction of FcεRI-IgE. Hence, these compounds could be applied as functional ingredients of anti-allergic foods.

The Role of Rhodomyrtus tomentosa (Aiton) Hassk. Fruits in Downregulation of Mast Cells-Mediated Allergic Responses.

Rhodomyrtus tomentosa, a flowering plant of Myrtaceae family from southern and southeastern Asia, was known to possess a rich source of structurally diverse and various biological activities. In this study, the inhibitory effect of R. tomentosa fruit extract (RFE) on allergic responses in calcium ionophore A23187-activated RBL-2H3 mast cells was investigated. The result showed that RFE was able to inhibit mast cell degranulation via decreasing ß-hexosaminidase release and intracellular Ca2+ elevation at the concentration of 400 µg/ml. Moreover, the suppressive effects of RFE on the production of interleukin-1ß (IL-1ß) and tumor necrosis factor-α (TNF-α) were evidenced. In addition, RFE effectively scavenged DPPH radical and suppressed the reactive oxygen species generation in a dose-dependent manner. Notably, the pretreatment of RFE caused the downregulation of tyrosine kinase Fyn phospholipid enzyme phospholipase Cγ (PLCγ), extracellular-signal-regulated kinase (ERK), and nuclear factor kappa B (NF-κB) phosphorylation. These results indicated that RFE could be a promising inhibitor of allergic responses and may be developed as bioactive ingredient for prevention or treatment of allergic diseases.

Investigation of Biological Activities of Wild Bitter Melon (Momordica charantia Linn. Var. Abbreviata Ser.).

Wild bitter melon (Momordica charantia L. var. Abbreviata Ser.) is a wild edible variety of M. charantia, often used in folk medicine. In this study, the biological activities of its extract and fractions were investigated in vitro. It was found that ethyl acetate (EA) fraction exhibited high 1,1-diphenyl-2-picryl-hydrazyl (DPPH) scavenging activity with a half maximal inhibitory concentration (IC50) value of 0.43 ± 0.04 mg/mL, while the chloroform (CF), EA, and n-butanol (Bu) fractions had strong 2,2-azinobis-3-ethyl benzothiazoline-6-sulfonic acid (ABTS)+ scavenging ability with IC50 values of 0.36 ± 0.04 mg/mL, 0.35 ± 0.02 mg/mL, and 0.35 ± 0.05 mg/mL, respectively. Moreover, the EA and Bu fractions exhibited the highest protective effect against H2O2-induced DNA damage in a concentration-dependent manner. Furthermore, the EA fraction was effective in the inhibition of enzyme α-amylase activity with an IC50 value of 0.27 ± 0.029 mg/mL. Finally, it was observed that the production of nitric oxide (NO), a pro-inflammatory mediator, was significantly reduced from LPS-stimulated murine macrophage RAW 264.7 cells by the ethanol extract (ET) and the EA fraction. Therefore, wild bitter melon could be considered as a promising biomaterial for the development of pharmaceutical products.

The beneficial properties of marine polysaccharides in alleviation of allergic responses.

Marine polysaccharides have been found as the principle component in cell wall structures of seaweeds or exoskeletons of crustaceans. Due to numerous pharmaceutical properties of marine polysaccharides such as antioxidant, anti-inflammatory, antiallergic, antitumor, antiobesity, antidiabetes, anticoagulant, antiviral, immunomodulatory, cardioprotective, and antihepatopathy activities, they have been applied in many fields of biomaterials, food, cosmetic, and pharmacology. Recently, several marine polysaccharides such alginate, porphyran, fucoidan, and chitin and its derivatives have been evidenced as downregulators of allergic responses due to enhancement of innate immune system, alteration of Th1/Th2 balance forward to Th1 cells, inhibition of IgE production, and suppression of mast cell degranulation. This contribution, therefore, focuses on antiallergic properties of marine polysaccharides and emphasizes their potential application as bioactive food ingredients as well as nutraceuticals for prevention of allergic disorders.

Marine fish-derived bioactive peptides as potential antihypertensive agents.

Hypertension is the most widespread risk factor for many serious cardiovascular diseases. Angiotensin-converting enzyme (ACE) plays a crucial role in cardiovascular physiological regulation by converting angiotensin I to a potent vasoconstrictor, angiotensin II. Hence, the inhibition of ACE is a key target for antihypertensive activity. Recently, potent antihypertensive peptides have been purified widely by enzymatic hydrolysis of muscle protein, skin collagen, and gelatin of many different kinds of marine fishes. Marine fish-derived bioactive peptides can be developed as antihypertensive components in functional foods or nutraceuticals. This contribution presents an overview of the ACE inhibitory peptides derived from marine fishes and discusses their future prospects to be used as potential drug candidates for preventing and treating high blood pressure.