| Betel nut is the dry mature seed of Areca catechu L, which belongs to the Palmaceae family, and used in traditional Chinese medicine as the antiscolic, antimalarial drugs, emictory, and agents for removing food retention and descending Qi. In particular, it is used commonly for treating of tapeworm disease, ascariasis, fasciolopsiasis, abdominalgia caused by parasitosis, diarrhea, tenesmus, beriberi edema and malaria. It’s recorded that the effects of raw and cooked betel nut are different in the past dynasties medical books. According to the traditional processing theory, the effects of raw betel nut is powerful and commonly used for the treatment of ascariasis, edema, beriberi, malaria; whereas the effects of fried yellow betel nut were weaker than raw betel nut and was used for patient whose body is weaker.Fried brown betel nut has a strong effect of relieving dyspepsia, which is used for food digestion disorder and tenesmus. Charring betel nut has the effects of relieving dyspepsia and stopping bleeding, which is used for the treatment of blood dysentery.The research has been studied on the variation of the content(such as alkaloid, tannin, amino acid, and trace elements) of crude betel nut, fried yellow betel nut and fried-brown betel nut, but the single change from the above content does not reflect the changes of the material basis in the processing of betel nut, and the study not combining with the biological effect of betel nut, so it fails to explain the theory of betel nut of processing.PurposesSo far, the principle of frying process of betel nut was still vague and the material basis of betel nut was unclear. Therefore, this work is designed to clear the principle of frying process of betel nut and provide scientific basis for formulating the quality standard and optimization process of betel nut, rich scientific connotation of traditional Chinese medicine.Methods1. Using the on-line non contact infrared temperature measurement system (NCTS) to monitor the frying process of betel nut by using automatic frying machine (AFM), and provide process parameters and to ensure the quality of fried products is uniform. 2. Using the HPLC method to determinate the content of arecoline, arecaidine, guvacine, guvacoline of betel nut product and UV for the determination of total alkaloids and tannins, in order to explore the chemical composition changes in the frying process of betel nut and reveal the material of the biological effects of betel nut.3. Using the HPLC to set up the water soluble constituents HPLC fingerprint of betel nut and its fried products, and find out the new components of fried betel nut through the comparative analysis of the above maps, which provided scientific basis for frying.4. Using silica gel column, ODS column, preparative HPLC to separate the new appeared compounds of the processing, and using the method of HPLC, LC-MS,1H-NMR for the identification of structure of new components and to evaluate its biological effect.5. Using the gastrointestinal smooth muscle experiment in vitro, gastric emptying, intestinal propulsion experiments in vivo to evaluate the promotive effects of raw betel nut, raw betel nut without alkaloids, fried-yellow betel nut, fried-dark-yellow betel nut, fried-brown betel nut, fried-brown betel nut without alkaloid, charring betel nut, arecoline, arecaidine, guvacine and new appeared compounds on gastrointestinal movements. Additionally, the correclation between biological effects and material basis was also evaluated, as well as the the acute toxicities of the raw betel nut and its processed products.6. Establishing a kinetic model to quantitative analysis of the changes of index components’contents and biological effects (toxicities) with the dynamic changes of frying degree (time), and calculate the kinetic parameters.Result1. The NCTS for betel nut frying process with AFM standardized the frying process parameters of betel nut and ensure the quality of fried products homogeneity.2. In the frying process, the contents of alkaloids were gradually decreased in the frying process, excepting the contents of arecaine were decreased first, then increased, and decreased finally, and it might be related to the decomposition of the arecoline.3. The fingerprint HPLC map of water soluble components of Betel nut and its fried products were established, and three new appeared constituents were found in the frying process of the Betel nut. What’s more, the3new appeared constituents were isolated and identified as2-hydroxyl-5-hydroxymethyl-2-furan-Formaldehyde.5-hydroxymethyl furfural, maltol. However, the results of our investigation showed that5-hydroxymethyl furfural, maltol have no effect on promoting gastrointestinal movement.4. Gastrointestinal smooth muscle test, gastric emptying, intestinal propulsion test results show that, arecoline is one of the material basis of betel nut on gastrointestinal movement, arecaidine, guvacine has no effect on promoting gastrointestinal movement.Fried-brown betel nut without alkaloid samples showed a significant effect on promoting gastric emptying and intestinal propulsion, and the effect of fried-brown betel nut is the most strong of all, it indicate that some new material had been produced which has the effect of promoting gastrointestinal movement in frying process. Therefore, the material basis of betel nut on gastrointestinal movement are arecoline and the new material which produced in the.frying process of betel nut.5. Color of betel nut was darkening with the degree of frying, and the toxicities were gradually reduced:raw betel nut> fried-yellow betel nut> fried-brown betel nut> charring betel nut; the LDso values of raw betel nut, fried-yellow betel nut and fried-brown betel nut were65.69g/kg,67.18g/kg, and71.83g/kg, respectively, what’ more, the charring betel nut unable to obtain the LDso due to no mice died in our tested doses.ConclusionOur present work systematically studied the relationship and law between the substances basis (characteristics, chemical constituents and finger print) and pharmacological activities (effects on the gastrointestinal movement in vitro and in vivo and toxicology), which will help for establishing the quality standard and processing technology. In our investigation,3constituents were found in the processing for the first time, and they were identified as5-hydroxymethyl furfural,2-hydroxyl-5-hydroxymethyl-2-furan-Formaldehyde, and maltol. Furthermore, we studied the pharmacological activities of these constituents. Arecoline is an important compound of the substances basis of betel nut on gastrointestinal movement, but is not the only constituent. The biological effect of fried-brown betel nut is much higher than that of raw betel nut and other processed products might due to the synergy of arecoline and the new appeared compounds. The LD50values of Betel nut were gradually increased with the levels of frying process, suggesting that alkaloid contents of Betel nut gradually decreased in the frying process, which also indicated that alkaloids in the Betel nut are the toxic components, and demonstrated the traditional theory that Betel nut need to fry to moderate its drug-nature.Innovations1、This paper emphasized the frying process based on "dynamic view, the whole process, the regularity of dynamic change", in other words, our work investigated substances of processed products and processing principle the based on the dynamic changes of chemical constituents in the processing, which possessed significant innovation.2、The new technology of on-line non contact infrared temperature measurement system (NCTS) was used to monitor the frying process of Betel nut; moreover, we established the kinetic model to quantitative analysis of the changes of index components’contents and biological effects (toxicities) with the dynamic changes of frying degree (time), and calculate the kinetic parameters. These methods mentioned above possessed obvious innovation compared to current technology. |
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