Supervisor(s):Chinese Pharmaceutical Association Sponsor(s):Tianjin Institute of Pharmaceutical Research；Chinese Pharmaceutical Association ISSN:0253-2670 CN:12-1108/R
Chinese Traditional and Herbal Drugs is supervised by Chinese Pharmaceutical Association and sponsored by Tianjin Institute of Pharmaceutical Research and Chinese Pharmaceutical Association. Launched in 1970, the journal is an academic journal with a broad scope in publishing research papers, brief reports, reviews, dissertations, and special treatises on the recent achievements of basic study, production, quality control, and clinic application on traditional Chinese medicine and Chinese materia medica.
The journal is included in CA, JST and CSCD.
Objective To synthesize brain targeting lipid material [(5-cholesten-3β-yl) (D-glucopyranose-6) sebacate, CHS-SE-GLU] by lipase as catalyst in nonaqueous phase and optimize the preparation technology and formulation of CHS-SE-GLU-modified liposomes. Methods CHS-SE-GLU was synthesized from CHS-SE prepared in previous work and D-glucose using lipase Novozym 435 in acetone. The structure characterization of the products was obtained by MS and NMR. The CHS-SE-GLU-modified paclitaxel loaded brain targeting liposomes (GLU-PTX-LP) were prepared by thin film dispersion method. Single factor evaluation was applied to optimizing its preparation technology and formulation. Results CHS-SE-GLU was confirmed by MS and NMR as target products. The optimal formulation and technology of GLU-PTX-LP were as follows: HSPC as membrane material, the ratio of HSPC to PTX was 0.1, the ratio of CHS to HSPC was 0.5, the dosage of DSPG-Na was 2.5%, hydration time was 0.5 h, and hydration temperature was 50 °C. Three batches of samples were prepared by optimum preparation process and the average encapsulation efficiencies were (93.62 ±1.34)%, (93.75 ± 1.77)%, (92.04 ± 1.50)%; the average particle sizes were (89.56 ± 1.35), (92.05 ± 3.42), (104.91 ± 3.71) nm; and the average Zeta potentials were (−25.21 ± 0.27), (−26.43 ± 0.44), (−25.17 ± 0.65) mV, respectively. Conclusion The lipase-catalyzed method for preparation of brain targeting lipid material is simple and environment friendly with high yield. The entrapment efficiency, particle size, and stability of brain targeting drug-loading liposomes modified by CHS-SE-GLU all meet the requirement, which shows good application prospect.
Objective To study the preparation and separation method for anticoagulant peptide and the effect of anticoagulation and thrombolysis in vitro. Methods The casein was hydrolyzed to prepare anticoagulant peptide using the mixed four enzymes such as papain, pineapple proteinase, neutral protease, and alkali protease. The anticoagulant peptide was extracted using immobilized thrombin. The effect of haemolysis and anticoagulation in vitro was investigated through the New Zealand rabbits experiments. Results The conditions of preparation anticoagulant peptide were as follows: quality of casein was 15%, papain proteinase, pineapple proteinase, neutral protease, and alcalase dosage were 1 500, 2 400, 1 000, and 1 250 U/(g casein), respectively, temperature was 50 °C, pH value was 7.0, and hydrolysis time was 4 h. The conditions for the extraction of anticoagulant peptide were as follows: the initial concentration was 6 ATU (Anti Thrombin Unit)/mL, temperature was 30 °C, pH value was 5.0, and time was 30 min. Anti-extraction temperature was 30 °C, pH value was 7.6, and time was 40 min. The purified anticoagulant peptide was analyzed via high performance size exclusion chromatography. The molecular weight of purified anticoagulant peptide was equal to N-Hippuryl-His-Leu hydrate and the main components were three peptides. The time of anticoagulation was more than 72 h and the time of hemolysis was 24 h in vitro. Conclusion The main components of anticoagulant peptides are three peptides. The effect of hemolysis and anticoagulation in vitro is good.
Objective: To investigate the stability of aqueous solution of scutellarin at different pH values, temperature, ionic strengths, and initial concentration under the condition of dynamic characteristics of the degradation reaction according to ICH guidelines. Methods: The content of scutellarin change with time in different conditions was studied using HPLC method. Based on the chemical reaction kinetics, the parameters of degradation kinetics were calculated under different conditions. The activation energy and half-time (t1/2) were evaluted. Results: The degradation of scutellarin in different conditions followed the first-order kinetics process. The most stable enviroment was in aqueous solutions of pH 7 at 25 °C, the half-life period was 203.87 h and the reaction activation energy was 97.9 kJ/mol. But with the temperature increased, the degradation reaction rate greatly accelerated. Under any condition, the stability was higher than the monomer. The initial concentration and ionic strength of Na+ and Cl− had no influence for its degradation. Conclusion: The degradation of scutellarin in different conditions follows the first-order kinetics process and is greatly influenced by the environment of high temperature, strong acid, and weak alkaline. The injection with five kinds of commonly used infusion compatibility is unstable.
Objective To investigate the chemical constituents of Rehmannia chingii. Methods The compounds were isolated from an aqueous extract from the whole plants of R. chingii by a combination of various chromatographic techniques including column chromatography over silica gel and Sephadex LH-20 and reversed-phase HPLC. Their structures were identified by spectroscopic analysis including MS and NMR data. Results Seventeen compounds were isolated and identified as 8-methyloctahydrocyclopenta [c] pyran-1,3,6,8-tetraol (1), 3,4-dihydroxy-phenethyl alcohol (2), 3-methoxyl-4-hydroxyphenyl alcohol (3), phenylethyl-8-O-β-D-glucopyranoside (4), 3,4-dihydroxy-β-phenethyl-O-α-L-rhamnopyranosyl-(1→3)-O-β-D-glucopyranoside (5), 2-phenylethyl O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside (6), deacyl-martynoside (7), acteoside (8), isoacteoside (9), martynoside (10), isomartynoside (11), jionoside C (12), jionoside A1 (13), jionoside B1 (14), 3,4-dihydroxy-β-phenethyl-O-α-L-rhamnopyranosyl-(1→3)-O-β-D-galacopyranosyl-(1→6)-4-O-caffeoyl-β-D-glucopyranoside (15), cistanoside F (16), and isocistanoside F (17). Conclusion Among the isolated seventeen compounds, compound 1 is a new compound named rehmachinin, and compounds 16–17 are isolated from the plants of Rehmannia Libosch. ex Fisch. et Mey. for the first time. In the preliminary assays, compounds 9, 12, and 14–16 exhibit the obvious inhibition against aldose reductase.
