Effect of Tongxie Yaofang on Expressions of Colon SERT and Liver 5-HT2AR Proteins in Rats with Ulcerative Colitis Model of Liver Stagnation and Spleen Deficiency / 中国实验方剂学杂志

Objective:To observe the effect of Tongxie Yaofang on the expressions of colon serotonin transporter （SERT）， liver 5-hydroxytryptamine_2A receptor （5-HT_2AR） protein， serum 5-HT and inflammatory factors in ulcerative colitis （UC） model rats of liver stagnation and spleen deficiency， in order to explore the basis of syndrome of liver stagnation and spleen deficiency and the intervention mechanism of Tongxie Yaofang. Method:Fifty male SD rats were randomly divided into blank control group， model group， high， medium and low-dose Tongxie Yaofang group （10，5，2.5 g·kg^-1）， and salazosulacil group （0.3 g·kg^-1）. The ulcerative colitis model of liver depression and spleen deficiency was established by 2，4，6-trinitrobenzene sulfonic acid （TNBS）/ethanol solution enema + restraint stress + diet loss. After successful modeling， the samples were collected after 21 days of drug intervention. Htoxylin eosin （HE） staining and oil red staining were used to observe the pathological changes of colon and liver in each group. Serum interleukin-6 （IL-6）， IL-9， 5-HT and superoxide dismutase （SOD） were detected by enzyme linked immunosorbent assay （ELISA）. Protein expressions of SERT in the colons and 5-HT_2AR in liver of rats were detected by Western blot. Result:Compared with the normal group， obvious ulcers were formed in the colon and lipid droplets in the liver increased in the model group， serum levels of IL-6， IL-9 and 5-HT in the model group increased， while the level of SOD decreased （<italic>P</italic><0.05）. The protein expression of SERT in colon decreased， whereas the protein expression of 5-HT_2AR in liver increased （<italic>P</italic><0.05）. Compare with model group， the pathological damage of colon was improved， and the formation of lipid droplets in liver was reduced in high， medium-dose Tongxie Yaofang groups and sulfasalazine group. The serum levels of IL-6， IL-9 and 5-HT decreased， while the level of SOD increased in Tongxie Yaofang group and sulfasalazine group （<italic>P</italic><0.05）. The protein expression of SERT in colon increased in high，low-dose Tongxie Yaofang groups and sulfasalazine group， and the protein expression of 5-HT_2AR in liver decreased in medium， low dose Tongxie Yaofang groups and sulfasalazine group （<italic>P</italic><0.05）. Conclusion:Tongxie Yaofang may reduce the content of 5-HT， and regulate the intestinal motility and sensory system by up-regulating the expression of SERT in the colon， inhibit the expressions of IL-6，IL-9 and other inflammatory factors， and play an anti-inflammatory role， reduce the content of 5-HT and the expression of 5-HT_2AR in the liver， increase the level of SOD， regulate emotion and lipid metabolism in the liver， and then exert the intervention effect on ulcerative colitis with liver depression and spleen deficiency on the whole.

Self-fixating polypropylene/poly(lactic acid) mesh for treatment of chronic pain following tension-free repair of inguinal hernia / 中国组织工程研究

BACKGROUND:Increasing clinical studies have reported the application of self-fixating mesh in the tension-free repair of inguinal hernia,but whether the self-fixating mesh is superior to the common suture mesh is still in dispute.OBJECTIVE:To compare the effects of self-fixating polypropylene/poly(lactic acid) mesh and polypropylene mesh on chronic pain after tension-free repair of inguinal hernia.METHODS:A total of 90 male patients with primary inguinal hernia were randomly divided into two groups:self-fixating mesh and control groups (n=45 per group).All patients underwent tension-free hernioplasty followed by self-fixating polypropylene/poly(lactic acid) mesh in the self-fixating mesh group and polypropylene mesh in the control group.Operation time and length of hospital stay were recorded;complications and recurrence rate in the two groups were observed at 6 months after operation;and postoperative pain and chronic pain were assessed by the visual analog scale (VAS) at postoperative 1,10 days,1,3,6 months.RESULTS AND CONCLUSION:(1) Compared with the control group,the operation time was shorter in the self-fixating mesh group (P ＜ 0.05),but there was no significant difference in the length of hospital stay between the two groups.(2) The VAS scores showed no significant difference between the two groups at postoperative 1 day,but the VAS scores were significantly better in the self-fixating mesh group than the control group at 10 days,postoperative 1,3,6 months (P ＜ 0.05).(3) During the 6-month follow-up,there were no urinary retention,subcutaneous hematoma,wound infection and recurrence in the two groups except five patients in the control group who complained of a foreign body sensation.To conclude,compared with the traditional polypropylene mesh,the use of self-fixating polypropylene/poly(lactic acid) mesh can shorten operation time and reduce pain and discomfort of patients with unilateral inguinal hernia undergoing tension-free hemioplasty.

The secondary metabolites from a mutant 3d10-01 derived from Penicilliumchrysogenum S-3-25 by diethyl sulfate mutagenesis / 国际药学研究杂志

Objective To investigate the secondary metabolites from diethyl sulfate(DES)mutant 3d10-01 derived from Peni-cillium chrysogenum S-3-25. Methods The secondary metabolites were isolated by multiple separation techniques,such as silica gel,Sephadex LH-20 column chromatography and HPLC. The structures of the compounds were determined by ESI-MS and NMR spectroscopic data. The antitumor activity was assayed by the MTT method. HPLC-UV analysis was used to determine if compounds 1-7 were newly produced by the mutant. Results Seven secondary metabolites,including methyl 2,4-dihydroxy-3,5,6-trimethylbenzo-ate(1),6-hydroxymethyl-2,2-dimethylchromanone(2),regiolone(3),(3S,4S)-3,4-dihydro-3,4,8-trihydroxy(2H)naphthalenone (4),cerebroside C(5),cerebroside D(6)and dankasterone A(7),were isolated from the fermentation products of the mutant 3d10-01. Compounds 1,4 and 7 showed strong inhibitory effects on the five tested cell lines,but 2,3 and 6 only exhibited the proliferation of HL-60 cells to some extent. Compounds 1-4 and 7 were newly produced by the mutant 3d10-01. Conclusion Compounds 1-7 are firstly isolated from P. chrysogenum. The inhibitory effects on certain tested antitumor cell lines of compounds 1-4,6 and 7 are report-ed for the first time.

Application of several physicochemical techniques in natural products to elucidate stereochemistry / 国际药学研究杂志

The difficulty in the structure elucidation of natural products is in the elucidation of stereochemistry, especially the determination of absolute configuration, which generally involves the key techniques of structure elucidation of natural products. This paper shows some examples of our work in elucidating the stereochemistry of new chiral natural products by the application of several physicochemical techniques, such as the dimolybdenum tetraacetate [Mo2(OAc)4] induced CD (ICD, Snatzke’s method), empirical rules of classical CD, modified Mosher’s method, theoretical ECD calculation and modified Marfey’s analysis. The fundamental rules of the techniques and our experiences in the application of these techniques are also described for related researcher’s reference in relevant studies.

Galloyl glucosidic constituents of choerospondias axillaries and their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities / 国际药学研究杂志

Objective To investigate gallic acid-derived chemical constituents of Choerospondias axillaries (Roxb.) Burtt. et Hill., and evaluate their in vitro anti-tumor, anti-hypoxia and anti-bacteria activities. Methods The aimed chemical constituents were isolated by various chromatographic means, and their structures were identified by physicochemical and spectroscopic data. MTT method was employed to evaluate anti-tumor and anti-hypoxia activities. Antibacterial activities were tested by paper disc method. Results Seven compounds 1-7 were isolated from the stem barks of Choerospondias axillaries (Roxb.) Burtt. et Hill. and identified as gallic acid (1)gallic acid ethyl ether (2)l-0-galloyl-β-A-glucose (3)1, 6-di-0-galloyl-β-D-glucose (4)1, 4-di-0- galloyl-β-D-glucose (5)1,4,6-tri-0-galloyl-β-β-glucose (6), and 1, 3, 4, 6-tetra-0-galloyl-β-D-glucose (7). Compounds 1, 2 and 4-6 significantly inhibited K562 cells with the IC50 values of 2.9, 14.6, 39.1, 40.2, 41.2 mg/ml, respectively, and 3 and 7 also showed a slight inhibition of the K562 cells with the inhibition rate of 20.8% and 30.1V at 100 !g/ml respectively. Compounds 1-7 showed protective effects on anoxia-induced injury in cultured ECY304 and PC12 cells at the concentrations showing no significant cytotoxicity, and 5-7 also showed an antibacterial effect on Staphylococcus aureus ATCC6538 to a certain extent. Conclusion Compounds 2-7 were isolated from the genus Choerospondias for the first time. It was the first time to report 1-7 as anti-tumor and anti-hypoxia constituents of Choerospondias axillaries, and the anti-hypoxia activity for 1-7 was also recorded for the first time in the present study.

Screening for bioactive mutants with antitumor activity from an actinomycetic wild-type strain without antitumor activity by antibiotic-resistant mutation technique and by coupled with chemical mutagen-induced mutation / 军事医学科学院院刊

Objective To obtain antibiotic-resistant mutants producing metabolites with antitumor activity from wild-type actinomycete strains without antitumor activity. Methods An actinomycete strain L35-1 was used as an initial strain for obtaining antibiotic-resistant mutants, which is a marine-derived wild-type strain without antitumor activity with an inhibition rate of 2.8% at the 1000 μg/ml of high sample concentration on K562 cells. The antibiotic-resistant mutants both from auto-mutagenesis and chemical mutagen-induced mutagenesis were selected by single colony isolation on antibiotic-containing plates according to the method for obtaining drug-resistant mutants in ribosome engineering. The antitumor activity was assayed by the MTT method using K562 cells for the mutants with aqueous acetone extracts of the whole broth of their fermentation.Results A total of 114 neomycin-resistant (ner) and 68 streptomycin-resistant (str) mutants, all from auto-mutagenesis, was obtained on drug-containing plates. Among them, the 7 ner and 3 str mutants appeared to be bioactive with an inhibition rate above 20% at the 100 μg/ml sample concentration on K562 cells. On the other hand, 41 str and 32 ner mutants from DES-induced mutagenesis and 46 ner mutants from NTG-induced mutagenesis were obtained by mutagen-induced mutation coupled with the single colony isolation on antibiotic-containing plates, among which, one str mutant from DES-induced mutagenesis and one ner mutant from NTG-induced mutagenesis were bioactive with an inhibition rate over 20% at the 100 μg/ml sample concentration on K562 cells. Conclusions The present result has revealed that the wild-type actinomycete strains without bioactivity might become a great source initial strains to obtain bioactive mutants by drug-resistant mutation technique.