Azelaic acid (AzA) and its derivatives have been known to be effective in the treatment of acne and various cutaneous hyperpigmentary disorders. The esterification of azelaic acid with lauryl alcohol (LA) to produce dilaurylazelate using immobilized lipase B from Candida antarctica (Novozym 435) is reported. Response surface methodology was selected to optimize the reaction conditions. A well-fitting quadratic polynomial regression model for the acid conversion was established with regards to several parameters, including reaction time and temperature, enzyme amount, and substrate molar ratios. The regression equation obtained by the central composite design of RSM predicted that the optimal reaction conditions included a reaction time of 360 min, 0.14 g of enzyme, a reaction temperature of 46 °C, and a molar ratio of substrates of 1:4.1. The results from the model were in good agreement with the experimental data and were within the experimental range (R2 of 0.9732).The inhibition zone can be seen at dilaurylazelate ester with diameter 9.0±0.1 mm activities against Staphylococcus epidermidis S273. The normal fibroblasts cell line (3T3) was used to assess the cytotoxicity activity of AzA and AzA derivative, which is dilaurylazelate ester. The comparison of the IC50 (50% inhibition of cell viability) value for AzA and AzA derivative was demonstrated. The IC50 value for AzA was 85.28 μg/mL, whereas the IC50 value for AzA derivative was more than 100 μg/mL. The 3T3 cell was still able to survive without any sign of toxicity from the AzA derivative; thus, it was proven to be non-toxic in this MTT assay when compared with AzA.
An application of artificial neural networks (ANNs) to predict the performance of a lipase-catalyzed synthesis for esterification of dilauryl azelate ester was carried out.
Artificial neural networks (ANNs) analysis was carried out to optimize the esterification of galanthamine and acetic acid in a solvent system. To predict performance parameters of the enzymatic reaction conditions, several parameters were studied which were reaction temperature (50-90 °C), enzyme amount (2-5 wt%), reaction time (6-18 h), and substrate molar ratio of galanthamine to acetic acid (2-5:1). The algoritms used in the network were batch back propagation (BBP), incremental back propagation (IBP), genetic algorithm (GA), Levenberg-Marguardt (LM) and quick propagation (QP) algorithms. The configuration of 4 inputs, one hidden layer with 7 nodes, and 1 output using the batch back propagation (BBP) was determined as the optimum algorithm. The predicted and experimental percentage yield value were 60.24% and 60.36%, respectively. These results prove the validity of ANN model.
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