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Exposure to ethanol during critical period of development can cause severe impairments in the central nervous system (CNS). This study was conducted to assess the neurotoxic effects of chronic embryonic exposure to ethanol in the zebrafish, taking into consideration the time dependent effect. Two types of exposure regimen were applied in this study. Withdrawal exposure group received daily exposure starting from gastrulation until hatching, while continuous exposure group received daily exposure from gastrulation until behavioural assessment at 6dpf (days post fertilization). Chronic embryonic exposure to ethanol decreased spontaneous tail coiling at 24hpf (hour post fertilization), heart rate at 48hpf and increased mortality rate at 72hpf. The number of apoptotic cells in the embryos treated with ethanol was significantly increased as compared to the control. We also measured the morphological abnormalities and the most prominent effects can be observed in the treated embryos exposed to 1.50% and 2.00%. The treated embryos showed shorter body length, larger egg yolk, smaller eye diameter and heart edema as compared to the control. Larvae received 0.75% continuous ethanol exposure exhibited decreased swimming activity and increased anxiety related behavior, while withdrawal ethanol exposure showed increased swimming activity and decreased anxiety related behavior as compared to the respective control. Biochemical analysis exhibited that ethanol exposure for both exposure regimens altered proteins, lipids, carbohydrates and nucleic acids of the zebrafish larvae. Our results indicated that time dependent effect of ethanol exposure during development could target the biochemical processes thus leading to induction of apoptosis and neurobehavioral deficits in the zebrafish larvae. Thus it raised our concern about the safe limit of alcohol consumption for pregnant mother especially during critical periods of vulnerability for developing nervous system.

Sunburn, premature skin aging, skin cancers and suppression of the immune system are linked to exposure of the skin to UV light. In recent years, plant extracts are becoming a popular active ingredient in natural sunscreen formulations. In the present study, the ethyl acetate fraction of Zanthoxylum rhetsa bark (commonly called as Indian prickly Ash) was used as an active ingredient in two sunscreen cream formulations (F1 and F2). Primarily, the constituents present in the active fraction were identified using LC–MS/MS analysis. Coumaric acid, benzoic acid, p-hydroxybenzoic acid and its isomers, hesperitin, trihydroxyoctadecenoic acid and columbamine were identified in the ethyl acetate fraction of Z. rhetsa bark extract. The UV protection properties of the formulated creams were evaluated by assessment of parameters such as their SPF values (F1: 3.60 ± 0.28, F2: 6.90 ± 0.57), UVA effectiveness (moderate for both test formulations) and critical wavelengths (F1: 365.4, F2: 360.3). Moreover, the physicochemical and microbial count of the formulated creams was also assessed based on various parameters such as colour, pH, centrifugation, viscosity and microbial load over a storage period of 28 days. Both formulations showed pseudo plastic behaviour and were stable at all conditions except for samples kept at 40 °C. Altogether, these results suggested that the ethyl acetate fraction of Z. rhetsa bark has great potential to reduce exposure to harmful UVA/UVB radiations and may be utilized as an active ingredient in natural sunscreen formulation.

Ethnopharmacological relevance: Muntingia calabura L. (Muntingiaceae) is locally known as kerukup siam. Its leaves, flowers, barks and roots have been used traditionally in East Asia and South America to treat various diseases including ulcer-related diseases. The present study aimed to investigate the mechanism(s) of gastroprotective effect of methanol extract of Muntingia calabura leaves (MEMC) using the pylorus ligation induced gastric ulceration in rats. Materials and methods: Five groups of rats (n=6) were administered orally once daily for 7 days with 8% Tween 80 (negative control), 100 mg/kg ranitidine (positive control), or MEMC (100, 250 or 500 mg/kg), followed by the ulcer induction via ligation of the pyloric part of the rat’s stomach. This was followed by the macroscopic analysis of the stomach, evaluation of gastric content parameters, and quantification of mucus content. The antioxidant (measured using the superoxide anion and 2,2-diphenyl-1-picrylhydrazyl (DPPH)-radical scavenging, oxygen radical absorbance capacity (ORAC) and total phenolic content (TPC) assays), anti-inflammatory (evaluated using the in vitro lipoxygenase and xanthine oxidase assays), phytoconstituents and HPLC analysis of MEMC were also carried out. Results: The MEMC significantly (p<0.05) reduced gastric lesion in this model. Furthermore, the extract also significantly (p<0.01) reduced the volume of gastric content whereas the total acidity was significantly (p<0.05) reduced in the doses of 100 and 500 mg/kg MEMC. Moreover, the mucus content increased significantly (p<0.01) in MEMC-treated rats. The extract also showed high antioxidant and anti-inflammatory activities in all assays tested, and demonstrated the presence of high tannins and saponins followed by flavonoids. Conclusion: The MEMC exerted gastroprotective effect via several mechanisms including the anti-secretory, antioxidant and anti-inflammatory activities. These activities could be attributed to the presence of tanni

This present work was aimed at fabrication of brushite crystals using oil-in-water high internal phase emulsion as a reaction medium. The oil phase of more than 75 wt.% was dispersed in the continuous aqueous phase. Due to the high oil volume fraction, the oil droplets were no longer spherical but were squeezed to take the shape of polyhedral. The morphology of the crystals was influenced by the structure of the emulsion and precursor concentration. The crystals were subjected to cytotoxicity test to ensure their compatibility with synoviocytes, which are cells that line the knee joints of rabbits. The crystals were able to sustain the cells for 5 days, which manifest their potential as osteoconductive coatings.

A series of 16 oxadiazole and triazolothiadiazole derivatives were designed, synthesized and evaluated as mushroom tyrosinase inhibitors. Five derivatives were found to display high inhibition on the tyrosinase activity ranging from 0.87 to 1.49 lM. Compound 5 exhibited highest tyrosinase inhibitory activity with an IC50 value of 0.87 ± 0.16 lM. The in silico protein–ligand docking using AUTODOCK 4.1 was successfully performed on compound 5 with significant binding energy value of 5.58 kcal/mol. The docking results also showed that the tyrosinase inhibition might be due to the metal chelating effect by the presence of thione functionality in compounds 1–5. Further studies revealed that the presence of hydrophobic group such as cycloamine derivatives played a major role in the inhibition. Piperazine moiety in compound 5 appeared to be involved in an extensive hydrophobic contact and a 2.9 Å hydrogen bonding with residue Glu 182 in the active site.

A series of 46 curcumin related diarylpentanoidanalogues were synthesized and evaluated for their anti-inflammatory, antioxidant and anti-tyrosinaseactivities. Among these compounds 2, 13 and 33 exhibited potent NO inhibitory effect on IFN-γ/LPS-activated RAW 264.7 cells as compared to l-NAME and curcumin. However, these series of diarylpentanoidanalogues were not significantly inhibiting NO scavenging, total radical scavenging and tyrosinase enzyme activities. The results revealed that the biologicalactivity of these diarylpentanoidanalogues is most likely due to their action mainly upon inflammatory mediator, inducible nitric oxide synthase (iNOS). The present results showed that compounds 2, 13 and 33 might serve as a useful starting point for the design of improved anti-inflammatory agents.

Cardamonin, a chalcone isolated from the fruits of a local plant Alpinia rafflesiana, has demonstrated anti-inflammatory activity in cellular models of inflammation. In this report, we evaluated the ability of cardamonin to suppress both NO and PGE2 synthesis, iNOS and COX-2 expression and enzymatic activity, and key molecules in the NF-κB pathway in order to determine its molecular target. Cardamonin suppressed the production of NO and PGE2 in interferon-γ (IFN-γ)- and lipopolysaccharide (LPS)-induced RAW 264.7 cells. This inhibition was demonstrated to be caused by a dose-dependent down-regulation of both inducible enzymes, iNOS and COX-2, without direct effect upon iNOS or COX-2 enzyme activity. Subsequently we determined that the inhibition of inducible enzyme expression was due to a dose-dependent inhibition of phosphorylation and degradation of I-κBα, which resulted in a reduction of p65NF-κB nuclear translocation. We conclude that cardamonin is a potential anti-inflammatory drug lead that targets the NF-κB pathway.