| Selenium is an essential trace element for the human body,which participates in various physiological activities of the body and is closely related to human health.Selenium has many physiological functions such as anti-oxidation,anti-cancer,immune regulation,prevention of cardio-cerebrovascular and so on.Selenium mainly exists in the form of inorganic selenium and organic selenium.Inorganic selenium has high toxicity,is not easy to be absorbed by human body,and the utilization rate is low,while organic selenium has low toxicity,strong biological activity and higher absorption rate.Taking organic selenium through diet has become an important way to supplement selenium scientifically.Cordyceps militaris(CYM)is a valuable fungus for both medicine and food.It is an ideal substitute for CYM and has high edible and medicinal value.CYM is an excellent selenium enriched carrier,which can convert inorganic selenium into organic selenium such as selenoprotein and selenium polysaccharide.The purpose of this study was to study the content of main active components in selenium-enriched Cordyceps militaris(Se-CYM)and the distribution of selenium in Se-CYM,compare the physiological activities of CYM before and after selenium enrichment,study the bioavailability and in vitro release mechanism of main components in Se-CYM,and develop a Se-CYM tablet product with both physiological functions of Cordyceps militaris and selenium.The main conclusions of this study are as follows :1.The content of active components and selenium distribution in Se-CYM were obtained.The contents of polysaccharide,adenosine and cordycepin in Se-CYM were higher than that of CYM.The nutritional value of Se-CYM was higher than that of CYM.98.04% of selenium in Se-cym exists in the form of organic selenium.The distribution of various forms of organic selenium was protein selenium >polysaccharide selenium > nucleic acid selenium > other forms of selenium.Protein selenium was the main form of selenium in Se-CYM,accounting for 65.70% of organic selenium and 62.05% of total selenium.The distribution of selenium in protein was alkali-soluble protein > water-soluble protein > salt-soluble protein >alcohol-soluble protein.Alkali-soluble protein-bound selenium was the main form of selenoprotein,accounting for 66.98% of protein selenium.The cordycepin in Se-CYM was extracted by ultrasonic-assisted enzymatic hydrolysis,and extraction conditions had been optimized.The best process conditions were: liquid-solid ratio 1:30(g/m L),ultrasonic power 250 w,temperature 49℃,time 110 min,PH 7.9,and enzyme addition of 3.9%.Under these conditions,the cordycepin content was 2.97 mg/g.2.Se-CYM has better antioxidant capacity and immunomodulatory activity.The antioxidant capacity,immunomodulatory ability and protective effect on human gastric mucosal epithelial cells of CYM and Se-CYM extract fluid were studied and compared.The results showed that both CYM and Se-CYM extract fluid had good antioxidant capacity,and the antioxidant capacity of Se-CYM extract fluid was higher than that of CYM extract fluid.CYM and Se-CYM extract fluid could promote the proliferative activity,phagocytic ability,secretion of NO and cytokines(TNF-α,IL-6)of RAW264.7.The promoting effect of Se-CYM extract fluid was stronger than that of CYM extract fluid,and it had better immunomodulatory activity.Both CYM and Se-CYM extract fluid could promote the proliferation of human gastric mucosal epithelial cells GES-1,and the effect of Se-CYM extract fluid is significantly higher than that of CYM extract fluid.Both CYM and Se-CYM extract fluid had protective effects on ethanol-induced injury of GES-1 cells,but there was no significant difference between them.3.The in vitro simulated digestibility and simulated release kinetic mechanism of selenium,cordycepin and cordycepic acid were obtained.The digestibility of selenium,cordycepin and cordycepic acid was studied by simulating the digestion of Se-CYM in human mouth,stomach and intestine in vitro.The results showed that after simulated oral,gastric and intestinal digestion,the digestibility of selenium in Se-CYM was 4.14%,48.50% and 84.03%,cordycepic acid was 63.97%,93.68%and 96.72%,cordycepin was 0.44%,2.00% and 28.90%,respectively.The digestibility of selenium and cordycepic acid in Se-CYM is higher,while the cordycepin is lower.The release of selenium,cordycepin and cordycepin in vitro from Se-CYM was studied by forward dialysis method.The results showed that after 9h in SGF,the cumulative release rates of selenium,cordycepin and cordycepin were 62.66%,1.83% and 28.94%,respectively.After 9h in SIF,the cumulative release rates of Se,cordycepin and cordycepic acid were 51.04%,93.94% and88.92%,respectively.The fitting results of the release kinetic equation showed that the best release kinetic model of selenium and cordycepin in SGF was the logarithmic normal distribution equation,and the best release kinetic model of cordycepic acid was the first-order kinetic equation.In SIF,the optimal release kinetic models of selenium,cordycepin and cordycepic acid were first-order kinetic equation,ritger-peppas equation and logarithmic normal distribution equation,respectively.The release of selenium and cordycepin in SGF and SIF,cordycepic acid in SGF was Fickian diffusion,and cordycepic acid in SIF was released in the form of non-Fickian diffusion.4.The optimum preparation process of Se-CYM tablets was obtained.Se-CYM powder was used as the main raw material,and excellent excipients were screened.Se-CYM tablets were prepared by powder direct compression method.By evaluating the fluidity of raw and excipient powder,MCC and maltodextrin were selected as fillers and L-HPC as disintegrators.Through single factor and response surface optimization experiments,the preparation process of Se-CYM tablets was optimized,and the best formula was obtained as follows: 20% of Se-CYM,50% of MCC,trehalose of 19%,3% of L-HPC,0.8 % of magnesium stearate,and the maltodextrin was filled to 100%.The Se-CYM tablets prepared according to this formula had smooth surface,glossy appearance,complete appearance and suitable hardness.The disintegration time limit,fragmentation and tablet weight difference were in line with the relevant provisions of the 2020 edition of Chinese Pharmacopoeia.After 6 months of storage,there was no significant change in the contents of selenium,cordycepin and adenosine in the main components of Se-CYM,and the Se-CYM tablets were relatively stable. |
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