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Objective:To investigate bonding ability between 4-sulfonylcalix ［6］ arene （SCA6） and 15 alkaloids （matrine， allomatrine， dauricine， daurisoline， quinidine， quinine， crotaline， vincristine， gelsemine， koumine， tetrandrine， aloperine， oxymatrine， sophocarpine and sinomenine）， and to evaluate viability<italic> in vitro</italic> of HepG2 and H9c2 cells with 12 alkaloids/SCA6 bonding systems （except allomatrine， oxymatrine， sinomenine）. Method:Fluorescence competitive titration was used to determine the binding constants of alkaloids and SCA6， the inhibitory effect of alkaloid/SCA6 complex on proliferation of HepG2 and H9c2 cells was investigated by cell counting kit-8 （CCK-8）. Result:All the 15 alkaloids had good bonding with SCA6 at the ratio of 1∶1 （the binding constants >1×10<sup>5</sup> mol·L<sup>-1</sup>， <italic>R</italic><sup>2</sup>>0.98）， the aloperine （quinolizidine alkaloids） and SCA6 had the biggest binding constant （20.55×10<sup>6</sup> mol·L<sup>-1</sup>）. In addition to gelsemine， crotaline， matrine and sophocarpine， 8 alkaloids （including aloperine， tetrandrine， dauricine， daurisoline， quinidine， quinine， vincristine and koumine） exhibited significant anti-tumor effects on HepG2 cells. Except for daurisoline， the anti-proliferation effect of the other 11 alkaloids before and after binding with SCA6 had no difference in HepG2 cells. In addition to gelsemine， crotaline， matrine and sophocarpine， the anti-proliferation effect of the other 8 alkaloids before and after binding with SCA6 had no difference in H9c2 cells. Conclusion:SCA6 shows intense binding ability with bisbenzylisoquinoline， quinolizidine and indole alkaloids. It can improve the solubility of alkaloids without affecting their anti-tumor activity， which provides a reference for subsequent related applications of SCA6 as a drug delivery carrier.
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Objective: To investigate the effect of extraction and reverse extraction conditions on the transfer of isoliquiritin. Methods: The extraction rate of isoliquiritin was used as the index to determine the best composition and concentration of complexing extractant. Taking the reverse extraction rate of isoliquiritin as the index, the species and concentration of the reverse extraction agent were investigated, and finally the technological conditions for the extraction and reverse extraction of isoliquiritin from glycyrrhizin ultrafiltration were obtained. Results: The best complexation extraction condition was: the ratio of TRPO to sulfonated kerosene was 7:93, and the extraction rate of isoliquiritin reached 97.60%. The best reverse extraction agent was 0.26% NaOH aqueous solution, and the reverse extraction rate of isoliquiritin reached 95.40%. Conclusion: Under the optimal conditions of extraction and reverse extraction obtained in this experiment, isoliquiritin can be transferred from glycyrrhizin ultrafiltration to complexing extractant and then to alkaline reverse extraction agent, and finally isoliquiritin can be obtained by extraction and reverse extraction.
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Objective: A technological route was established for preparing liquiritigenin from the licorice ultrafiltrate. Methods: U5(53) uniform design was used to optimize the ultrafiltration process with the retention rate of liquiritigenin as the index; Box-Behnken response surface method was used to optimize the complexation extraction process with the extraction rate of liquiritigenin as the index; The technological condition of back extraction of liquiritigenin was determined by the liquiritigenin stripping rate. Results: The optimal ultrafiltration conditions for liquiritigenin were inorganic ceramic membranes with a pore size of 10 nm, a pressure of 0.12 MPa, and solution temperature of 25 ℃, retention rate of liquiritigenin was 98.74%. Optimum complexation extraction conditions were as following: 1% TRPO complexing agent, extraction for 10 min in 5 mL organic phase solution, the extraction rate of liquiritigenin was 99.44%; The 12.5 mmol/L NaOH aqueous solution was the best back-extractant, and the back extraction rate was 98.88%. Conclusion: As a new Chinese medicine extraction technology, ultrafiltration-complexation extraction and back extraction technology have the advantages of high selectivity, high efficiency, and recycling of extractant, which can provide a new preparation technology for the research of liquiritigenin.
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Objective: To improve the bioactivity of PEEK by chemical methods. Methods: PEEK samples were treated by polish only (group (1)) ; concentrated sulfuric acid for 5 min (group (2)) ; concentrated sulfuric acid for 10 min (group (3)) ; concentrated sulfuric acid for 5 min, followed by treatment of hydrogen nitrate for 5 min (group (4)) and mineral chameleon and ortho-phosphoric acid (group (5)) respectively (n = 9) . Then, all samples were treated by water at 100 ℃ for 4 h. The sample surface was observed by FE-SEM, the chemical comporent of the samples was analyzed by XPS. BMSCs were cultured on the sample surface for 4 h and observed by SEM. Results: The sample sureface in group (1) was smooth, in group (2), (3) and (4) was with 3 D ethmoidal foramen structure, in group (5) with petal-like from. The sulfur content (Wt％) of the samples of group (1), (2), (3), (4) and (5) was 0, 2. 45 ± 0. 22, 3. 48 ± 0. 16 (vs (1), P= 0. 000), 1. 79 ± 0. 05 (vs (1) P = 0. 002) and 0 respectively. BMSCs cultured on the sample surface of group (2), (3), (4) and (5) were more and with more pseudopod. Conclusion: The bioactivity of PEEK can be enhanced after acid pickling. Water bath and nitric acid treatment can remove the residual acid and further enhance the bioactivity of PEEK.
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Objective:To study the effects of voriconazole sulfonated butyl ether-β-cyclodextrin inclusion compound(VCZ-SBE) eye drop on fungal keratitis (FK) in rabbits. Methods:Aspergillus fumigatus was used for the establishment of FK model in rabbits. Totally 48 healthy rabbits were divided into four groups. The 12 right eyes in group A were inoculated with Aspergillus fumigatus with-out any treatment. The 12 right eyes in group B were inoculated with Aspergillus fumigatus,and then treated with 0.5% VCZ-SBE eye drop,those in group C were inoculated with Aspergillus fumigatus,and then treated with 1.0% VCZ-SBE eye drop,and those in group D were inoculated with Aspergillus fumigatus,and then treated with 0.5% fluconazole eye drop. The cornea of normal left eyes in the four groups was used for the blank control. Ulcer grading was performed for all the eyes in 0,1,4,7 and 14 d after the successful es-tablishment of FK model. Every 3 rabbits were sacrificed in 1,4,7 and 14 d,and then the cornea was obtained to evaluate the infiltra-tion degree of inflammatory cells and the invasion depth of hyphae into cornea. Results:After the successful establishment of FK mod-el,the ulcer grading among the groups showed no significant difference(P>0.05). Respectively after the 7,4 and 14-day treatment, the ulcer grading in group B,C and D was notably lower than that in group A (P<0.05). After the 4,7 and 14-day treatment,the ulcer grading,infiltration depth and necrosis degree in group C were all lower than those in group B and D(P<0.05),and after the 7 and 14-day treatment,those in group B were lower than those in group D(P<0.05). Conclusion:Compared with fluconazole eye drop at the same concentration,VCZ-SBE inclusion compound eye drop can decrease the ulcer grading of FK and reduce the infiltration depth in a concentration-dependent manner.
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Objective: To prepare 1% voriconazole ( VCZ) sulfonated butyl ether- β-cyclodextrin ( SBE-β-CD) inclusion com-pound eye drop and study the quality. Methods: VCZ SBE-β-CD inclusion compound was prepared with the molar ratio of VCZ to SBE-β-CD of 1 :1. Sodium chloride was used as the osmotic pressure regulator and benzalkonium bromide was employed as the pre-servative in the preparation of VCZ SBE-β-CD inclusion compound eye drop. The appearance, pH value, content stability and irritation of the eye drop were studied as well. Results:The eye drop was colorless and transparent solution with the pH value of 6. 44 ± 0. 20, 6. 50 ± 0. 15,6. 48 ± 0. 22 the osmotic pressure of (320 ± 4. 62),(316 ± 2. 88),(322 ± 2. 60)MOsm and the VCZ content of 1. 02% g ·ml-1 . The results of accelerated testing and long-term testing showed no notable changes in the quality indices. The eye drop exhibi-ted no significant irritation to the rabbit eyes. Conclusion:VCZ SBE-β-CD inclusion compound eye drop shows the properties of high VCZ content, stable quality and promising safety in eye application, which is worthy of further studies.
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Objective: To prepare 1% voriconazole ( VCZ) sulfonated butyl ether- β-cyclodextrin ( SBE-β-CD) inclusion com-pound eye drop and study the quality. Methods: VCZ SBE-β-CD inclusion compound was prepared with the molar ratio of VCZ to SBE-β-CD of 1 :1. Sodium chloride was used as the osmotic pressure regulator and benzalkonium bromide was employed as the pre-servative in the preparation of VCZ SBE-β-CD inclusion compound eye drop. The appearance, pH value, content stability and irritation of the eye drop were studied as well. Results:The eye drop was colorless and transparent solution with the pH value of 6. 44 ± 0. 20, 6. 50 ± 0. 15,6. 48 ± 0. 22 the osmotic pressure of (320 ± 4. 62),(316 ± 2. 88),(322 ± 2. 60)MOsm and the VCZ content of 1. 02% g ·ml-1 . The results of accelerated testing and long-term testing showed no notable changes in the quality indices. The eye drop exhibi-ted no significant irritation to the rabbit eyes. Conclusion:VCZ SBE-β-CD inclusion compound eye drop shows the properties of high VCZ content, stable quality and promising safety in eye application, which is worthy of further studies.
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Objective: To prepare voriconazole (VCZ) sulfonated butyl ether-β-cyclodextrin (SBE-β-CD) inclusion compound and study the properties in vitro.Methods: VCZ SBE-β-CD inclusion compound was prepared respectively by a stirring method, an ultrasonic method and a grinding method, and the one with the highest inclusion rate and inclusion compound yield was chosen as the final preparation method.The formula and preparation process were optimized by an orthogonal design.The inclusion compound was identified by differential scanning calorimetry and solubility determination, and the in vitro dissolution was determined as well.Results: The stirring method had the highest inclusion rate and inclusion compound yield, and the optimal preparation and formula conditions were as follows: the inclusion temperature was 25℃, the stirring time was 4 h and the amount ratio of VCZ to SBE-β-CD was 1∶1.After the optimization, the inclusion rate was (86.14 ± 0.69)%, and the yield of inclusion compound was (97.11 ± 0.31)%.After the inclusion, the characteristic peak of VCZ disappeared and the solubility of VCZ increased significantly.Compared with those of VCZ, the dissolution rate and amount of VCZ inclusion compound both increased notably.Conclusion: VCZ SBE-β-CD inclusion compound can be prepared by the stirring method, which lays foundation for the further studies on VCZ eye drop.
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Objective: To study the solubilization of sulfonated butyl ether-β-cyclodextrin (SBE-β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) for voriconazole (VCZ) to lay basis for the preparation of inclusion compounds of VCZ.Methods: The phase-solubility method was used, and the solubilization of SBE-β-CD and HP-β-CD at different concentrations for VCZ was studied at various temperatures and the inclusion constant (K) and such inclusion parameters as ΔG, ΔH and ΔS were calculated.Results: Both SBE-β-CD and HP-β-CD could improve the solubility of VCZ in water, while the solubilization of SBE-β-CD was more significant than that of HP-β-CD at the same concentration under the same temperature.The equilibrium phase-solubility diagram of SBE-β-CD vs VCZ was AN type, and that of HP-β-CD vs VCZ was AL type.With the increase of temperature, K of both β-CD decreased.ΔG, ΔH and ΔS were all negative for the inclusion process.Conclusion: Compared with that of HP-β-CD, the solubilization of SBE-β-CD for VCZ is better.The inclusion is spontaneously formed with exothermic process, and the main acting force is Van der Waals'' force.
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Objective To observe the efficacy and safety of liver decanoic sulfonic sodium in the treatment of elderly patients with acute coronary syndrome (ACS).Methods84 ACS patients over 70 years were randomly divided into the treatment and control groups.Two groups were treated on the basis of general,treatment 40 cases of liver of dibutyl sebacate with sodium sulfonated added 2.5 mg subcutaneous injection parumbilical,day 1,course 8 d ; control group 44 cases combined with low molecular weight heparin calcium 0.4 ml,2 times/day 1 time every 12 hours,according to body weight adjusted dose,Parumbilical shot in course of 8 days,observing the clinical effect of two groups during the treatment,as well as 4 weeks and bleeding during the treatment the incidence of cardiovascular events.Results The clinical effects of treatment and control groups was no significant difference (95％ and 91％,P ＞0.05) ; None of the two sets of death,myocardial infarction and recurrent malignant ventricular arrhythmia; none of the two sets of bleeding occurs,treatment of minor bleeding rates were significantly lower than those of control groups (7.5％ and 25％,P ＜ 0.05).Conclusion The study of dibutyl sebacate with sodium heparin and low molecular weight heparin calcium in the treatment of ACS are valid,but the former which significantly reduce the incidence of minor bleeding.Liver decanoic sulfonic sodium for acute coronary syndrome ACS)anticoagulation can not only effectively reduce cardiovascular events,but also significantly reduce bleeding risk,regardless of the patient's age,gender,renal function and risk stratification,especially for bleeding in high risk elderly patients with safe and clinical promotion.