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@#Thioredoxin-interacting protein (TXNIP), which mainly regulates glucose homeostasis in pancreatic β cells, is a novel target in the treatment of diabetes.In this study, 4-hydroxybenzopyrimidine was used as the raw material, four nitrogen-containing rings (imidazole, methylpiperazine, pyrazole, morpholine) were introduced, benzopyrimidine skeleton with nitrogen-containing rings derivatives targeting TXNIP was designed and synthesized, and the protective effect of compounds on palmitic acid-stimulated islet β cells was investigated.A total of 20 benzopyrimidine derivatives were designed and synthesized, and the structures were confirmed by 1H NMR and ESI-MS.Pharmacological studies showed that most of the compounds exhibited protective effects on islet β cells, with better axtivity for compounds C-1, C-2, C-4 and D-2 (cell survival rate > 70%) compared with PA model group (38.3%), Among the four compounds, D-2 had the highest activity of 87.2%, so it could become a potential new anti-diabetic chemical entity.
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With the enhancement of computing power and the continuous development of machine learning and deep learning algorithms, artificial intelligence (AI) has gradually become an important tool for human activities and has also given new vitality to the fields of life science and medicine. For laboratory medicine, it is both an opportunity and a challenge. The combination of inspection big data and AI algorithms has promoted the improvement of morphological inspection capabilities, the optimization of inspection processes, the discovery of new knowledge, and the development of disease diagnosis models. It has become a convenient and intelligent assistant for disease prevention, diagnosis and prognosis prediction.
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@#Ferulic acid (FA), a natural product of phenylpropanoids containing phenolic hydroxyl groups, has a wide range of pharmacological activities and some therapeutic effect on Alzheimer's disease (AD).Using FA as the raw material, the ferulic acid carbamate aniline derivatives were first synthesized by 4-step esterification reaction, splicing carbamate active functional groups, hydrolysis reaction and amide condensation.These FA derivatives were evaluated for in vitro cholinesterase inhibition activity by the Ellman method.A total of 15 novel FA derivatives were designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR and ESI-MS.Cholinesterase activity tests showed that compounds 5c, 5f, 5j, 5g, 5m possessed good acetylcholinesterase inhibition activity.Except for 5l, 5m, almost all compounds have inhibition activity on butyrylcholinesterase, which is much higher than that on acetylcholinesterase.In conclusion, compounds 5c, 5f, 5j and 5g can be used as potential anti-AD inhibitors targeting cholinesterase..
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Objective@#This study takes hydroxypropyl-β-cyclodextrin (HP-β-CD) as the inclusion materials to optimize the preparation technic of tea tree oil (TTO) and evaluate its pharmaceutical performance.@*Methods@#Take the production rate of HP-β-CD tea tree oil inclusion and entrapment rate as the evaluation index, taking the orthogonal test method to optimize the production technic of tea tree oil (HP-β-CD inclusion and using infrared (IR), differential thermal scanning (DSC) method to characterize the inclusion compound to analyze the stability of TTO-HP-β-CD.@*Results@#The best technic to produce HP-β-CD tea tree oil is as follow: the ratio of TTO and HP-β-CD should be equal to 1/10, at 40 ℃, within 1 h. The average drug loading shoud be 9.25% ± 3.25%. The IR, DSC characterization results showed that the characteristic peak of tea tree oil disappeared after the microspheres, which indicated the HP-β-CD encapsulated the tea tree oil with good compatibility. In 80 ℃ water bath, the TTO-HP-β-CD was stable with the retention rate 40% after 8 h, the retention rate was 4.32 times than that of the unwrapped tea tree oil.@*Conclusions@#The HP-β-CD tea tree oil obviously has higher rate of inclusion and stability. Therefore, it’s worth to promoting and being used in the pharmacy preparations and cosmetics field.
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Objective:This study takes hydroxypropyl-β-cyclodextrin (HP-β-CD) as the inclusion materials to optimize the preparation technic of tea tree oil (TTO) and evaluate its pharmaceutical performance.Methods:Take the production rate of HP-β-CD tea tree oil inclusion and entrapment rate as the evaluation index, taking the orthogonal test method to optimize the production technic of tea tree oil (HP-β-CD inclusion and using infrared (IR), differential thermal scanning (DSC) method to characterize the inclusion compound to analyze the stability of TTO-HP-β-CD.Results:The best technic to produce HP-β-CD tea tree oil is as follow: the ratio of TTO and HP-β-CD should be equal to 1/10, at 40 ℃, within 1 h. The average drug loading shoud be 9.25% ± 3.25%. The IR, DSC characterization results showed that the characteristic peak of tea tree oil disappeared after the microspheres, which indicated the HP-β-CD encapsulated the tea tree oil with good compatibility. In 80 ℃ water bath, the TTO-HP-β-CD was stable with the retention rate 40% after 8 h, the retention rate was 4.32 times than that of the unwrapped tea tree oil.Conclusions:The HP-β-CD tea tree oil obviously has higher rate of inclusion and stability. Therefore, it’s worth to promoting and being used in the pharmacy preparations and cosmetics field.
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Objective:To prepare ketoprofen-loaded solid lipid nanoparticles ( SLN) and evaluate the properties. Methods: The formula was optimized by orthogonal experiments with the encapsulation efficiency as the index. The optimal preparation was investiga-ted by the morphology, particle size, zeta potential and drug forms. The release property was characterized by a dialysis method and the release process was fitted. Results: The best formula was as follows: poloxamer 0. 1g, Tween-800. 2g, lecithin 0. 15g, glycerol monostearate 0. 05g and ketoprofen 50mg. The particles were spherical in shape with the encapsulation efficiency of 61. 95%, the par-ticle size was 151. 7 nm and the zeta potential was-30. 2 mV. The result of DSC indicated the drug dispersed in the lipid matrix was a-morphous and molecular state. The in-vitro release curve showed the release was rapid at the early stage and then slowed down with the accumulated amount up to (85. 11 ± 7. 62)% in 12h. The drug was released slowly from SLN with the matrix erosion. The release pro-file fitted well with a Higuchi equation. Conclusion: The solid lipid nanoparticles containing ketoprofen exhibit good quality and the preparation method is simple and feasible, therefore, it is valuable to be further studied.
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Objective:To prepare ketoprofen-loaded solid lipid nanoparticles ( SLN) and evaluate the properties. Methods: The formula was optimized by orthogonal experiments with the encapsulation efficiency as the index. The optimal preparation was investiga-ted by the morphology, particle size, zeta potential and drug forms. The release property was characterized by a dialysis method and the release process was fitted. Results: The best formula was as follows: poloxamer 0. 1g, Tween-800. 2g, lecithin 0. 15g, glycerol monostearate 0. 05g and ketoprofen 50mg. The particles were spherical in shape with the encapsulation efficiency of 61. 95%, the par-ticle size was 151. 7 nm and the zeta potential was-30. 2 mV. The result of DSC indicated the drug dispersed in the lipid matrix was a-morphous and molecular state. The in-vitro release curve showed the release was rapid at the early stage and then slowed down with the accumulated amount up to (85. 11 ± 7. 62)% in 12h. The drug was released slowly from SLN with the matrix erosion. The release pro-file fitted well with a Higuchi equation. Conclusion: The solid lipid nanoparticles containing ketoprofen exhibit good quality and the preparation method is simple and feasible, therefore, it is valuable to be further studied.
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Objective To screen endophytic fungal strains isolated from wild Huperzia serrata which can highly produce hu?perzine A. Methods The strain producing huperzine A was identified through thin layer chromatography(TLC)and high-perfor?mance liquid chromatography(HPLC)with authentic huperzine A. The fungus was identified according to its morphological character?istics and nuclear ribosomal DNA ITS sequence. Results The strain was identified as Fusarium oxysporum NSG-1 according to its morphological characteristics and nuclear ribosomal DNA ITS sequence. The amount of huperzine A produced by the fermentation li?quor of this endophytic fungus was quantified to be 1.11 mg/100 ml by HPLC,which was higher than that of previously reported endo?phytic fungi. Conclusion Endophytic fungus producing high huperzine A can be obtained from H. serrata. The production of huper?zine A based on mutagenesis and transformation of the obtained strain may adapt to the industry production.
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Objective:To study the boiling water brewing extraction of astragalus polysaccharides in order to solve the problems of long cycle , high energy consumption and poor clarity in the traditional extraction , and lay foundation for the industrial production . Methods:Using the extraction yield of astragalus polysaccharide as the evaluation index and phenol -sulfuric acid method applied to de-termine the content of astragalus polysaccharide , the boiling water brewing extraction was used for astragalus polysaccharides .The effects of brewing time , boiling water amount and brewing times on the polysaccharide content were studied by single factor experi -ments, and then an orthogonal design method was used to screen the optimum technology parameters .The traditional water decoction extraction process was employed as the control .Results:The optimum conditions of boiling water brewing were as follows:adding 9-fold amount of water and soaking 60 min for three times.The astragalus polysaccharides extraction yield (4.81) of the optimal technology was higher than that of the traditional water decoction extraction (4.06%).Conclusion:Boiling water brewing method used to extract astragalus is with high extraction yield , simple operation , short cycle and low energy consumption , the color of astragalus polysaccha-ride is light, and it is clear after dissovled in water , which is superior to the traditional water decoction extraction method , and provide a new method with broad application prospect for the preparation of astragalus related preparations .
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<p><b>OBJECTIVE</b>To prepare flexible nanoliposomes of Ginkgolid B (GB) and study the transdermal diffusion law.</p><p><b>METHOD</b>Flexible nanoliposomes of GB were prepared by film dispersion method, and the shape and particle size of nanoliposomes were analyzed. GB permeation tests in vitro through the skin of rats were performed in modified Franz diffusion cell. The accumulated permeation amounts of GB alcoholic solution, flexible nanoliposomes of GB and ordinary nanoliposomes of GB were compared.</p><p><b>RESULT</b>The average encapsulation percentage, the particle size, and the Zata potential of the flexible nanoliposomes were (89.52 +/- 1.76)%, and was (208.3 +/- 25.49) nm, and was -49.2 mV, respectively. The accumulated permeation amount of flexible nanoliposomes in 8 hours was 189.97 microg x cm(-2), and its transdermal permeability in 8 hours was 23.75 microg x cm(-2) x h(-1).</p><p><b>CONCLUSION</b>The encapsulation percentage of the flexible nanoliposomes is good,and the stability of the GB nanoliposomes is fine. Flexible nanoliposomes can significantly enhance the diffusion rate of GB through the skin of rats.</p>
Subject(s)
Animals , Female , Male , Mice , Ginkgolides , Chemistry , Pharmacokinetics , Lactones , Chemistry , Pharmacokinetics , Liposomes , Chemistry , Pharmacokinetics , Nanoparticles , Chemistry , Particle Size , Permeability , Random Allocation , Skin AbsorptionABSTRACT
Objective To study the effects on electroporation of Qingfengteng cataplasma transdermal absorption and describe the characteristics of animal pharmacokinetics of it.Methods Two-chamber diffusion cell was used and the plasma drug concentration was determined by HPLC.The application of AIC theory to analysis of the compartmentally based model of sinomenine transdermal delivery by electroporation.Results The Cmax,Ka,and AUC0→∞ of electroporation was larger than those of passive diffusion;t1/2(Ka)and tmax of electroporation were reduced compared with passive diffusion.The drug concentration-curve equation were C=2.884?(e-0.056 t-e-0.232 t)and C=2.512?(e-0.058 t-e-0.149 t)for electroporation and passive diffusion,respectively.Conclusion The change of in vivo drug concentration of Qingfengteng calaplasma transdermal absorption by electroporation could be analized in accordance with mammillary one-compartment open model.The etrectroporation technology could sharply enhance the bioavalibility compared with the passive diffusion.
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AIM: To prepare flexible nanoliposomes made from active ingredients,phillyrin and volatile oil,from forsythia suspense and study their transdermal delivery system.METHODS: Flexible nanolipsomes of phill-yrin(WN group) and phillyrin in combination with forsythia volatile oil(OWN group) were prepared by the meth-od of membrane-dispersion.Its appearance and particle sizes were measured.Transdermal experiments were carried out on the modified Franz diffusion pool through in vitro mouse skin.HPLC was applied to determining the phillyrin content to compare transdermal rate and cumulative permeation amount of various flexible nanoliposomes.RESULTS: The particle size of the WN group was(180.7 ? 13.69)nm,the Zata potential was-48.8 mV,the average encapsulation percentage was(82.53 ? 2.68)%;the particle size of the OWN group was(212.3 ? 15.31)nm,Zata potential was-51.2 mV,the average encapsulation percentage was(70.49 ? 1.06)%.The accu-mulated permeation amount of the OWN group in 8 hours was(291.92 ? 23.22) ?g/cm2,its transdermal permea-bility in 8 hours was 36.49 ?g/(cm2.h),which was 6.10 folds that of the WS group and 1.92 folds that of the WN group.This difference had statistical significance(P