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Gamma aminobutyric acid (GABA) is produced by microorganisms such as bacteria, yeast, and fungi. Lactic acid bacteria play crucial roles in processing and preserving Vietnamese traditional fermented foods. The study aims to isolate high GABA-producing Lactobacillusstrains from traditional fermented foods. Eight bacterial strains, including BC3, BC4, BC5, BC6, BC7, K08, KC1, and KC2, were isolated from traditional fermented food sources (cabbage, pickled scallion, and kimchi). After 72 hrs of fermentation, the BC3 strain produced the highest GABA content (4.279 g/l). This strain was identified as Lactobacillus fermentum by 16S rRNA analysis. The results from the investigation of the fermentation time and concentration of monosodium glutamate (MSG) showed that the BC3 strain producing the highest GABA with the value of 6.734 g/l was after 72 hrs of fermentation and the concentration of MSG 4%.

The purpose of this study is to investigate in vitro hypoglycemic and free radical scavenging activities of some medicinal plants including Ficus glomerata (FG), Pandanus amaryllifolia (PaA), Artocarpus altilis (AA), Gomphrena celosioides (GC) and Gynostemma pentaphyllum (GP). Alpha-amylase inhibitory assay was examined by dinitrosalicylic acid reaction. Glucose uptake assay was investigated by LO-2 cell model. DPPH and ABTS+ scavenging assays were performed by spectrophotometry. Cell viability was determined by MTT method. It was found that the extracts including FG, PaA, AA, GC and GP were able to inhibit alphaamylase activity up to 38.4 ± 4.2%, 47.8 ± 4.3%, 49.3 ± 3.5%, 40.1 ± 4.4% and 38.5 ± 3.8%, respectively. Moreover, glucose adsorption and glucose uptake capacity of these extracts were evidenced. In addition, free radical scavenging activity of these extracts was indicated in a range of 30.6-54.5% for DPPH radical and 31.8-51.1% for ABTS+ radical. Especially, these extracts exhibited no cytotoxicity effect on human hepatic LO-2 cells and human gastric BGC-823 cells at the concentration of 100 μg/ml. The results indicated that A. altilis leaves were effective in inhibiting alpha-amylase activity, increasing glucose adsorption and glucose uptake and scavenging free radicals. Therefore, it could be suggested to be a promising hypoglycemic agent for managing type 2 diabetes.

Houttuynia cordata Thunb. is an edible and medicinal plant that belongs to the family of Saururaceae and widely distributes in Eastern Asia countries. H. cordata have been reported as a promising anticancer agent against various cancer cells. This study was to determine anti-proliferative effect of H. cordata extract on gastric cancer cells using an in vitro experimental model. The cytotoxicity was examined via the 2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, while cell migration was conducted by wound healing assay. The gene expression level was measured by real time PCR. The result showed that butanol extract exhibited highest anti-proliferative activity against BGC-823 cells with IC50 value of 193 µg/ml. Moreover, the wound healing assay determined the suppressive capacity of butanol extract on cell migration at concentration of 50 µg/ml. Notably, butanol extract treatment (50 µg/ml) was able to up-regulate the mRNA expression of apoptosis-mediated signaling molecules, including caspase-8, Bax, caspase-9, and caspase-3 in gastric cancer cells. These results indicate that butanol extract of H. cordata possesses inhibitory activity on tumor development and metastasis via induction of the process of programmed cell death.

Gamma-aminobutyric acid (GABA) is a potent bioactive component that widely exists in both plants and animals, has numerous health benefits. This study aimed to optimise the fermentation process conditions for the growth of Lactobacillus fermentum from rice bran extracts that have high potential to produce GABA. GABA content was assessed by thin-layer chromatography (TLC) method. In this study, fermenting conditions for medium production of GABA by L. fermentum from rice bran extracts were optimised. L. fermentum showed high potential for GABA-producing ability. Some factors influencing the GABA production such as carbon sources, nitrogen sources, mineral salt sources, substrate concentration of monosodium glutamate (MSG), pH, and the time of fermentation were investigated. When the L. fermentum is cultivated in the rice bran extracts medium supplemented with 1.5% lactose, 2% yeast extract, and 1% MSG with pH 6.0 in 48 h, this strain showed high GABA at a concentration of 736 mg/l.

In this study, the essential oil profile of Callicarpa candicans (Burm. f.) Hochr was presented. Samples were collected from Vietnam and the oils were extracted from fresh leaves and dry leaves by hydrodistillation method. GC-MS data and retention indices were used to identify the chemical composition. The essential oil performance achieved 0.263% for fresh leaves and 1.503% for dry leaves. A total of 47 components were identified from fresh leaves oil and 39 constituents from dry leaves oil. Chemical compositions of the two essential oils were similar, with the major components being α-gurjunene, δ-cadinene, ε-caryophyllene (β-caryophyllene) and α-selinene.

Two new cycloartanes, combretic acid C (1) and combretanone I (3), were isolated from the leaves of Combretum quadrangulare Kurz, together with the previously-reported combretic acids A-B (2 and 5) and combretanone A (4). An extensive set of spectroscopic methods were used to elucidate the structures of these compounds. Cytotoxicity against the K562 cancer cell line was evaluated. Compound 1 showed strong activity, with an IC50 value of 9.7 µM. The other compounds showed moderate activity. Alpha-glucosidase inhibition was also evaluated. The isolated compounds showed moderate inhibition, with IC50 values in the range 102.2-194.7 µM.

Objective: To investigate the chemical components and biological activities of avocado seed extract and fractions in order to determine the nutritional and pharmaceutical values of avocado seed. Methods: Various organic solvents were applied for extraction and fractionation of avocado seed. 1,1-diphenyl-2-picryl-hydrazyl, 2,2-azinobis-3-ethyl benzothiazoline-6-sulfonic acid, and DNA oxidation assays were applied for investigation of free radical scavenging activity. Nitric oxide production was measured by Griess reaction assay. Moreover, MTT assay was used to measure cancer cell growth inhibition. Results: The result indicated that the avocado seed contains (7.14 ± 0.40) g lipid/100 g, (1.67 ± 0.03) g protein/100 g, (54.0 ± 1.2) g carbohydrate/100 g, and (62.0 ± 2.3) mg gallic acid equivalent/g dried weight extract. Moreover, dichloromethane and ethyl acetate were revealed to be the highest free radical scavenging fractions with IC50 values of (48.0 ± 3.4) μg/mL (1,1-diphenyl-2-picryl-hydrazyl assay) and (22.0 ± 1.8) μg/mL (2,2-azinobis-3-ethyl benzothiazoline-6-sulfonic acid assay), respectively. Additionally, the avocado seed extract and fractions were able to protect against H2O2-induced DNA damage at the concentration of 100 μg/mL. On the other hand, the ethanol extract was effective in reducing nitric oxide production from lipopolysaccharide-stimulated RAW 264.7 macrophage cells without cytotoxic effect. Notably, the avocado seed significantly inhibited the proliferation of human lung A549 and human gastric BGC823 cancer cells at the concentration of 200 μg/mL, especially hexane (81 ± 3)% and dichloromethane (75 ± 2)% fractions. Conclusions: The results of the present study supported the avocado seed as potential by-product source for further development of health beneficial products.

Epidemiological studies have evidenced that natural dietary products can prevent or manage gastric cancer. Neptunia oleracea, an aquatic vegetable and edible plant, has been reported to have anti-cancer properties. In this study, N. oleracea extract’s suppression of gastric cancer cells was investigated on an in vitro experimental model. We found that ethyl acetate (EtOAc) extract inhibited cell proliferation at IC50 value of 172 µg/mL. Moreover, the treatment of EtOAc extract at a concentration of 50 µg/mL for 24 h caused suppression of cancer cell migration. Notably, a real-time PCR assay revealed that EtOAc extract induced the process of apoptosis via upregulating the mRNA expression level of caspase-8, Bax, caspase-9, and caspase-3 in cancer cells. In conclusion, N. oleracea had potential anti-cancer activity against gastric cancer cells, suggesting its role in the prevention and management of gastric cancer.

Gastric cancer is the second most common cause of cancer-related deaths in the world. In this study, a bioactive derivative of chitooligosaccharide, named gallic acid-grafted-chitooligosaccharide (G-COS), was evaluated for its capabilities against the proliferation of AGS human gastric cancer cells. It was found that G-COS treatment caused significant inhibition of gastric cancer cell growth at concentrations of 200 and 400 μg mL−1. The anti-growth effect of G-COS in AGS cells was characterized using flow cytometry, fluorescence microscopy, DNA fragmentation and evaluation of protein expression. Notably, G-COS-induced apoptosis was related to the increase in the expression of p53, p21, Bax, and caspases (-9 and -3) and the decrease in the activation of Bcl-2, p-IκB-α and NF-κB (p50 and p65). These findings indicate that G-COS has potential to be applied in the treatment of gastric cancer as a cancer chemopreventative agent.

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 &plusmn, 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 &plusmn, 0.04 mg/mL, 0.35 &plusmn, 0.02 mg/mL, and 0.35 &plusmn, 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 &alpha, amylase activity with an IC50 value of 0.27 &plusmn, 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.

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 β-hexosaminidase release and intracellular Ca2+ elevation at the concentration of 400 μg/ml. Moreover, the suppressive effects of RFE on the production of interleukin-1β (IL-1β) 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.

CBM20s are starch-binding domains found in many amylolytic enzymes, including glucoamylase, alpha-amylase, beta-amylases, and a new family of starch-active polysaccharide monooxygenases (AA13 PMOs). Previous studies of CBM20–substrate interaction only concerned relatively small or soluble amylose molecules, while amylolytic enzymes often work on extended chains of insoluble starch molecules. In this study, we utilized molecular simulation techniques to gain further insights into the interaction of CBM20 with substrates of various sizes via its two separate binding sites, termed as BdS1 and BdS2. Results show that substrate binding at BdS1 involving two conserved tryptophan residues is about 2–4 kcal mol−1 stronger than that at BdS2. CBM20 exhibits about two-fold higher affinity for helical substrates than for the amylose random coils. The affinity for amylose individual double helices does not depend on the helices' length. At least three parallel double helices are required for optimal binding. The binding affinity for a substrate containing 3 or more double helices is ∼−15 kcal mol−1, which is 2–3 kcal mol−1 larger than that for individual double helices. 100 ns molecular dynamics simulations were carried out for the binding of CBM20 to an extended substrate containing 3 layers of 9 60-unit double helices (A3L). A stable conformation of CBM20–A3L was found at BdS1. However, when CBM20 binds A3L via BdS2, it moves across the surface of the substrate and does not form a stable complex. MD simulations show that small amylose helices are quickly disrupted upon binding to CBM20. Our results provide some important molecular insights into the interactions of CBM20 with starch substrates, which will serve as the basis for further studies of CBM20-containing enzymes, including AA13 PMOs.

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 β-hexosaminidase release and intracellular Ca2+ elevation at the concentration of 400 μg/ml. Moreover, the suppressive effects of RFE on the production of interleukin-1β (IL-1β) 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.

Angiotensin- I- converting enzyme (ACE) is crucial in the control of hypertension and the development of type- 2 diabetes and other diseases associated with metabolic syndrome. The aim of this work was to utilize Pacific cod skin to purify ACE inhibitory peptides. First, gelatin was extracted from Pacific cod skin and hydrolyzed with several enzymes (pepsin, papain, α-chymotrypsin, trypsin, neutrase, and alcalase). The pepsin hydrolysate showed the strongest ACE inhibitory effect and was further fractionated into different ranges of molecular weight ( 10 kDa) using ultrafiltration (UF) membranes. The peptic hydrolysate below 1 kDa resulted in two potent ACE inhibitory peptides, GASSGMPG (662 Da) and LAYA (436 Da), with IC50 values (concentration required to decrease the ACE activity by 50%) of 6.9 and 14.5 μM, respectively. Moreover, to explore the interaction between the peptides and ACE molecule, the tertiary structure of ACE and docking simulation to the peptides were predicted using Docking Server. Pacific cod peptides can be used as functional food ingredients to prevent hypertension and its related diseases.

Houttuynia cordata Thunb (H. Cordata), an aromatic medicinal herb belonging to family Saururaceae, is a plant that grows in moist habitats, well known for its medicinal properties and widely used worldwide. H. Cordata is an aromatic medicinal herb belonging to family Saururaceae and is restricted to specialized moist habitats. Three extracts, successively obtained from the leaves of H. cordata, namely the diethyl ether leaves extract (DELE), the ethanolic leaves extract (ELE) and the aqueous leaves extract (ALE), were used to determine the polyphenol and flavonoid content in the leaves. Phytochemical screening of plant extracts showed the presence of flavonoid, saponin, alkaloid, tannin, and steroid compounds. Quantitative determination of total phenolics, total flavonoids of methanolic extract were carried out using colorimetric methods. The result of quantitative determination showed that total polyphenol content of the DELE, ELE and ALE were 32.18 ± 2.64, 97.98 ± 1.77, and 22.22 ± 2.00 mg of gallic acid equivalents per gram dry extract, respectively. Meanwhile total flavonoid content of the DELE, ELE and ALE achieved 31.65 ± 1.07, 35.72 ± 1.23, and 4.06 ± 0.54 mg of quercetin equivalents per gram dry extract, respectively.

Recently, the relationship between apoptosis and cancer has been emphasized and the induction of apoptosis is recognized as one of the key mechanisms of anti-cancer agents. Marine-derived fungi are valuable sources of structurally diverse bioactive anticancer agents. In the present study, a marine-derived fungus, Microsporum sp. was cultured and an anthraquinone derivative, physcion (11.8 mg) was isolated from the culture broth extract (1710 mg). Physcion has shown cytotoxic effect on human cervical carcinoma HeLa cells and its apoptosis induction in HeLa cells was investigated by the expressions of p53, p21, Bax, Bcl-2, caspase-9, and caspase-3 proteins. The Western blot analysis has revealed that physcion could significantly induce cell apoptosis through down-regulating of Bcl-2 expression, up-regulating of Bax expression, and activating the caspase-3 pathway. Furthermore, physcion induced the formation of reactive oxygen species (ROS) in HeLa cells. Collectively, these results suggest that physcion could be a potential candidate in the field of anticancer drug discovery against human cervical cancer.

Hibiscus sabdariffa L. (Hs, roselle; Malvaceae) is a common ingredient used in the food and pharmaceutical industries for color and health benefits. Anthocyanins along with protocatechuic acid and quercetin have been recognized as bioactive compounds in Hibiscussabdariffa L. aqueous extracts. In this work, Response Surface Methodology was implemented together with Box-Behnken experimental design to investigate the impacts of process variables on anthocyanin extraction yields from Hibiscus sabdariffa L. (Roselle) grown in Lam Dong, Vietnam. The effects of three independent variables; namely the extraction temperatures of solvent ethanol (X1); the duration of extraction (X2); solid-liquid ratios (X3) on the total anthocyanins content (Y1) were explored. The optimization model showed that with the solid liquid ratio 7.7:1, extraction time 33.29 min, and temperature 56.9°C, the highest anthocyanin concentration of 186.006 mg/L was obtained. Hibiscussabdariffa L. anthocyanin yield detailed significant correlation with high F values, low P values (

Nowadays, anthocyanins have become an interesting topic of much scientific research and act as potential sources of eco-friendly natural food dyes and their helpful effects on human health.. The purpose of the present article was to apply conventional extraction methods of pigments from Butterfly pea (Clitoria ternatea L.Flowers) in Southern Vietnam were tested to extract anthocyanins. The effects of various factors, including the solvent concentration, extraction time, temperature, and solvent/material ratio on the extraction total anthocyanins from Butterfly pea were investigated. In this study, the concentration of monomeric anthocyanins was completed by the spectrophotometry pH differential method.The highest recovered anthocyanin level was achieved with 50 % ethanol (143.49 mg/L), while the lowest one was obtained with water (90.9 mg/L). The extraction yield was significantly affected by temperature and the excellent condition was 60°C. The extraction yield raised with increasing of solvent/material ratio until equilibrium has arrived at the optimal ratio of 25:1 (mL/g). The extraction yield increased first and then decreased with an extension in time values.

Diabetes is a major metabolic disorder whose prevalence is increasing daily. Medicinal plants have played an important role in the prevention and treatment of type 2 diabetes via prophylactic and therapeutic management. In this study, Mangifera Indica leaf (MIL) extract was investigated for its promising anti-diabetic activity via an in vitro model. It was found that MIL extract possessed significant inhibition on alpha-amylase activity up to (51.4 &plusmn, 2.7)% at a concentration of 200 &micro, g/mL. Moreover, glucose adsorption capacity of MIL was identified at (2.7 &plusmn, 0.19) mM glucose/g extract. Furthermore, the extract caused a significant increase in glucose uptake up to (143 &plusmn, 9.3)% in LO-2 liver cells. Notably, MIL extract was effective in scavenging (63.3 &plusmn, 2.1)% 1,1-diphenyl-2-picryl-hydrazyl (DPPH) and (71.6 &plusmn, 4.3)% 2,2-azinobis-3-ethyl benzothiazoline-6-sulfonic acid (ABTS)+ radicals and inhibiting (66 &plusmn, 4.9)% NO production from RAW264.7 cells without any cytotoxicity effects. Accordingly, M. indica leaves are suggested as a promising material for development of hypoglycemic products.

The aminoethyl–chitooligosaccharide (AE-COS) was reported to inhibit human gastric cancer cell proliferation and human fibrosarcoma cell invasion. In this study, the role of AE-COS in down-regulation of proliferation of human lung A549 cancer cells was evaluated. It was found that AE-COS was able to reduce A549 cell proliferation to (32 ± 1.3)% at a concentration of 500 µg/mL. Moreover, AE-COS treatment caused suppression on COX-2 expression in a dose-dependent manner. Notably, the role of AE-COS in induction of cell apoptosis was observed via decreasing Bcl-2 expression and increasing caspase-3 and -9 activation. Accordingly, the antiproliferative effect of AE-COS was indicated due to suppression of cell proliferation and induction of cell apoptosis, suggesting AE-COS as a promising chemotherapy agent for treatment of lung cancer.

This paper describes the functionalization of poly(poly(ethylene glycol) methacrylate) (PPEGMA)-grafted CdTe (PPEGMA-g-CdTe) quantum dots (QDs) via surface-initiated reversible addition&ndash, fragmentation chain transfer (SI-RAFT) polymerization for immobilization of adenosine. Initially, the hydroxyl-coated CdTe QDs, synthesized using 2-mercaptoethanol (ME) as a capping agent, were coupled with a RAFT agent, S-benzyl S&prime, trimethoxysilylpropyltrithiocarbonate (BTPT), through a condensation reaction. Then, 2,2&prime, azobisisobutyronitrile (AIBN) was used to successfully initiate in situ RAFT polymerization to generate PPEGMA-g-CdTe nanocomposites. Adenosine-above-PPEGMA-grafted CdTe (Ado-i-PPEGMA-g-CdTe) hybrids were formed by the polymer shell, which had successfully undergone bioconjugation and postfunctionalization by adenosine (as a nucleoside). Fourier transform infrared (FT-IR) spectrophotometry, energy-dispersive X-ray (EDX) spectroscopy, thermogravimetric analysis (TGA), X-ray photoelectron spectroscopy (XPS), and transmission electron microscopy results indicated that a robust covalent bond was created between the organic PPEGMA part, cadmium telluride (CdTe) QDs, and the adenosine conjugate. The optical properties of the PPEGMA-g-CdTe and Ado-i-PPEGMA-g-CdTe hybrids were investigated by photoluminescence (PL) spectroscopy, and the results suggest that they have a great potential for application as optimal materials in biomedicine.

Natural bioactive peptides have been known as ingredients in nutraceuticals and pharmaceuticals. In this study, the potential anti-inflammatory peptides were purified from enzymatic hydrolysate of the edible microalgae Spirulina maxima using gastrointestinal endopeptidases (trypsin, α-chymotrypsin, and pepsin). Purification of the hydrolysate resulted in two peptides with amino acid sequences of LDAVNR (P1, 686 Da) and MMLDF (P2, 655 Da). It was found that peptides P1 and P2 exhibited significant inhibition on the release and production of histamine from antigen-stimulated RBL-2H3 mast cells. Moreover, the suppressive effect of P1 and P2 on production as well as expression of interleukin-8 in histamine-stimulated EA.hy926 endothelial cells was determined. Notably, the production of intracellular reactive oxygen species from mast cells and endothelial cells was decreased in the presence of P1 or P2. Collectively, the peptides P1 and P2 from S. maxima could be used as functional ingredients with potent anti-inflammatory benefits.

Human immunodeficiency virus (HIV) infection causes acquired immune deficiency syndrome (AIDS) and is a global public health issue. Anti-HIV therapy involving chemical drugs has improved the life quality of HIV/AIDS patients. However, emergence of HIV drug resistance, side effects and the necessity for long-term anti-HIV treatment are the main reasons for failure of anti-HIV therapy. Therefore, it is essential to isolate novel anti-HIV therapeutics from natural resources. Recently, a great deal of interest has been expressed regarding marine-derived anti-HIV agents such as phlorotannins, sulfated chitooligosaccharides, sulfated polysaccharides, lectins and bioactive peptides. This contribution presents an overview of anti-HIV therapeutics derived from marine resources and their potential application in HIV therapy.

UV light, especially UVB, is known as a trigger of allergic reaction, leading to mast cell degranulation and histamine release. In this study, phlorotannin Fucofuroeckol-A (F-A) derived from brown algal Ecklonia stolonifera Okamura was evaluated for its protective capability against UVB-induced allergic reaction in RBL-2H3 mast cells. It was revealed that F-A significantly suppress mast cell degranulation via decreasing histamine release as well as intracellular Ca2+ elevation at the concentration of 50 μM. Moreover, the inhibitory effect of F-A on IL-1β and TNF-α productions was also evidenced. Notably, the protective activity of F-A against mast cell degranulation was found due to scavenging ROS production. Accordingly, F-A from brown algal E. stolonifera was suggested to be promising candidate for its protective capability against UVB-induced allergic reaction.

Cancer targeted therapies have attracted considerable attention over the past year. Recently, 5-fluouracil (5-FU), which has high toxicity to normal cells and short half-life associated with rapid metabolism, is one of the most commonly used therapies in the treatment of cancer. In this study the folic acid-conjugated pegylated nanoliposomes were synthesized and then loaded into them with 5-FU to improve the anti-tumor efficacy. The average size of liposomes (LPs) was about 52.7 nm which was identified by TEM. In the liposome uptake studies, the level uptake of folate-conjugated liposomes has increased compared to non-conjugated LPs according to LPs concentration, incubation time and presence of concentration of free folic acid (FA). The MTT assay and apoptotic test were carried out in HCT116 and MCF-7 cells for 24 or 48 h. The results revealed that the folate-PEG modified 5-Fu loaded nanoliposomes had strong cytotoxicity to cancer cell compared to pure 5-FU or PEG modified 5-FU loaded liposomes in a concentration- and time-dependent manner, and mainly enhanced the cancer cell death through folate-mediated endocytosis. Hence, the folate-PEG modified nanoliposome is a potential targeted drug-delivery system for the treatment of FR-positive cancers.

Histamine, a potent inflammatory mediator, has been known to cause the pathogenesis of atherosclerosis. In this sense, two bioactive peptides P1 (LDAVNR; 686Da) and P2 (MMLDF; 655Da) purified from gastric enzymatic hydrolysate of Spirulina maxima were examined for their protective effects against early atherosclerotic responses induced by histamine in EA.hy926 endothelial cells. Interestingly, both P1 and P2 exhibited inhibitory activities on the production and expression of IL-6 and MCP-1. Furthermore, P1 and P2 inhibited the production of adhesion molecules including P-selectin and E-selectin, and thus reducing in vitro cell adhesion of monocyte onto endothelial cells. In addition, the production of intracellular reactive oxygen species was observed to reduce in the presence of P1 or P2. Notably, the inhibitory activities of P1 and P2 were found due to down-regulating Egr-1 expression via histamine receptor and PKCδ-dependent MAPKs activation pathway. These results suggest that peptides P1 and P2 from S. maxima are effective to suppress histamine-induced endothelial cell activation that may contribute to the prevention of early atherosclerosis.

Hydroxyapatite nanocrystals (HAP NCs) were encapsulated by poly(allyl methacrylate) (PolyAMA) employing controlled surface-initiated reversible addition-fragmentation chain transfer (SI-RAFT) polymerization of allyl methacrylate to afford HAP-PolyAMA nanohybrids. The subsequent thiol-ene coupling of nanohybrids with 2-mercaptosuccinic acid resulted HAP-Poly(AMA-COOH) possessing multicarboxyl group. The formation of the nanohybrids was confirmed by FT-IR and EDS analyses. The TGA and FE-SEM investigation were further suggested the grafting of PolyAMA onto HAP NCs. The utility of the HAP-PolyAMA nanohybrid as drug carrier was also explored. The pendant carboxyl groups on the external layers of nanohybrids were conjugated with anticancer drug cisplatin to afford HAP-Poly(AMA-COOH)/Pt complex. The formation of the complex was confirmed by FT-IR, XPS, and FE-SEM. In vitro evaluation of the synthesized complex as nanomedicine revealed its potential chemotherapeutic efficacy against cancer cell lines.

In this study, a bioactive derivative of chitooligosaccharides (3–5 kDa) was synthesized via grafting of gallic acid onto chitooligosaccharides (G-COS) to enhance anti-allergic activity. Hence, G-COS was evaluated for its capabilities against allergic reactions in RBL-2H3 mast cells sensitized with dinitrophenyl-specific immunoglobulin E antibody and stimulated by antigen dinitrophenyl-bovine serum albumin. It was revealed that G-COS exhibited significant inhibition on histamine release and production as well as intracellular Ca 2+ elevation at the concentration of 200 μg/ml. Likewise, the suppressive effects of G-COS on expression and production of interleukin (IL)-4 and tumor necrosis factor (TNF)-α were evidenced. Moreover, G-COS treatment caused a remarkable blockade on degradation of inhibitory κB-α (IκB-α) protein, translocation of nuclear factor (NF)-κB, and phosphorylation of mitogen-activated protein kinases (MAPKs). Notably, the inhibitory activities of G-COS on allergic reactions were found as a consequence of suppression of FceRI expression in antigen-stimulated cells. Accordingly, G-COS was suggested to be a promising candidate of novel inhibitors against allergic reactions.

Herpes simplex virus (HSV) is a member of the Herpesviridae family that causes general communicable infections in human populations throughout the world, the most common being genital and orolabial disease. The current treatments for HSV infections are nucleoside analogs such as acyclovir, valacyclovir and famciclovir. Despite the safety and efficacy, extensive clinical use of these drugs has led to the emergence of resistant viral strains, mainly in immunocompromised patients. To counteract these problems, alternative anti-HSV agents from natural products have been reported. Recently, a great deal of interest has been expressed regarding marine organisms such as algae, sponges, tunicates, echinoderms, mollusks, shrimp, bacteria, and fungus as promising anti-HSV agents. This contribution presents an overview of potential anti-HSV agents derived from marine organisms and their promising application in HSV therapy.