A new spirocyclic cycloartane triterpenoid from Souliea vaginata / 中国中药杂志

The 70% ethanol extract of the whole plant of Souliea vaginata was purified by multi-chromatographic methods including macroporous resin,silica gel,Sephadex LH-20,and C18-reversed-phase column chromatography. A new spirocyclic cycloartane triterpenoid was isolated and identified as( 16 R*,20 R*,23 S*,24 R*,25 S*)-16,23: 23,26-diepoxy-15α,24,25-trihydroxy-9,19-cycloart-3β-O-β-D-xylopyranoside( 1),and named as soulieoside S. Its planar structure and relative configuration were determined by spectroscopic techniques including 2 D NMR and HRESI-MS. As one of the main components of S. vaginata,compound 1 was evaluated for its anti-inflammatory activity by a lipopolysaccharide( LPS)-stimulated NO production model in RAW264. 7 macrophages,but it didn't show NO production inhibitory effect.

The Development of Biologically Important Spirooxindoles as New Antimicrobial Agents.

BACKGROUND: Antibiotic resistance is one of the biggest threats to global health today, leading to higher medical costs and increased mortality. Because of the emergence and rapid spread of new resistance mechanisms globally, a growing number of infections are becoming harder to treat as the antibiotics used to treat them become less effective. Therefore, the development of new effective antimicrobial agents is still urgently needed. In last decades, a large number of structurally novel spirooxindoles have been synthesized mainly based on the ylide intermediates generated in situ and further assessed for their antimicrobial activity against different types of bacteria, leading to the discovery of some potent lead compounds with antimicrobial potentials. OBJECTIVE: The aim of this review to submarize recent advances on the synthesis, structure- activity relationship studies (SARs) and antimicrobial activity of spirooxindoles. METHODS: Peer-reviewed research work on spirooxindoles with antimicrobial activity were downloaded from bibliographic databases and analyzed based on their chemoptypes. RESULTS: 50 papers were retrieved from the literature databases, of which 20 papers described the synthesis and antimicrobial activity of spirooxindoles. CONCLUSION: This review highlights the importance of spirooxindoles as potential antimicrobial agents. The antimicrobial activity of spirooxindoles against different types of bacteria is less studied, mainly centering on primary antimicrobial assessment, some of these compounds have showed interesting antimicrobial activity. However, the current study is only limited to primary antimicrobial assessment, no detailed modes of action are investigated.

[Relation of GSTM1 Polymorphism with Leukemia].

OBJECTIVE: To investigate the relation of GSTM1 polymorphism in leukemia patients with therapeutic efficacy and the main biological characteristics. METHODS: The GSTM1 genotypes were detected by nested PCR; the remission rate after 1 course of treatment and main biological characteristics at occurrence of leukemia were compared between AL patients with different GSTM1 genotypes, and their relation was analyzed. RESULTS: The remission rate and partial remission rate after 1 course of treatment in patients with GSTM1-undeleted genotype were no significantly different from those in patients with GSTM1 null genotype (χ2=0.290, P>0.05). The stratification analysis showed that GSTM1 null genotype was not related with age, sex, WBC count, Hb level, plt count at initial diagnosis and spleen enlargenent or no(P>0.05). The comparison of AML and ALL with GSTM1 null genotype by Log-rank showed that the survival rate was no statistically different between AML and ALL patients(χ2=2.043, P>0.05), while the LDH level in serum of patients with GSTM1-undeleted genotype at initial diagnosis was statistically different from that in patients with GSTM1 null genotype (P=0.001). CONCLUSION: The GSTM1 genotype does not relate with remission and partial remission rates after 1 course treatment of AL patients, but relates with LDH level. GSTM1 null genotype deletion may play a role in risk of leukemia.

Correlation between p65 and TNF-α in patients with acute myelocytic leukemia.

The correlation between the expression levels of p65 and TNF-α in patients with acute myelocytic leukemia (AML) and AML cell lines were investigated. The bone marrow samples of 30 AML patients and 10 non-leukemia controls were studied. The mRNA expression levels of p65 and TNF-α were detected by reverse transcription-quantitative polymerase chain reaction (RT-qPCR), and Pearson's Correlation test was used to demonstrate the correlation between TNF-α and p65 expression levels in AML specimens. Receiver operating characteristic (ROC) curves were plotted to determine whether TNF-α and p65 expression levels could be used to differentiate AML samples from non-leukemia samples. MG132 and anti-TNF-α antibody were used to inhibit the expression of p65 and TNF-α in the AML cell line, HL-60. The expression of p65 and TNF-α were detected by RT-qPCR and western blot analysis. The mRNA expression levels of p65 and TNF-α were significantly increased in AML patients compared with non-leukemia control bone marrow samples by RT-qPCR, and the two molecules expression pattern's exhibited sufficient predictive power to distinguish AML patients from non-leukemia control samples. Pearson's correlation analysis demonstrated that TNF-α expression was strongly correlated with p65 expression in AML bone marrow samples. In HL-60 cells, inhibition of TNF-α reduced the expression of p65; in addition, inhibition of p65 reduced the expression of TNF-α as assessed by RT-qPCR and western blot analysis. p65 and TNF-α were highly expressed in AML patients, and these 2 molecules were strongly correlated. The present study indicates that p65 and TNF-α have potential as molecular markers to distinguish AML patients from non-leukemia control samples, and that these 2 molecules may be useful prognostic factor for patients with AML.

Chemometrics-based approach to feature selection of chromatographic profiles and its application to search active fraction of herbal medicine.

In our previous report (J Pharmaceut Biomed 56 (2011) 443-447), a support vector machine (SVM)-based pharmacodynamic model was established for predicting active fractions of herbal medicines (HMs), where information contents embedded in the chromatograms of the fractions were represented with the peak areas. However, in this representation the global characteristics of the chromatograms were completely missed, which is definitely contrary to the global and holistic views in theories of HMs and undoubtedly reduce the success rate of this model. To deal with the challenge, two chemometrics methods, that is, minimum redundancy maximum relevance (mRMR) and particle swarm optimizer (PSO), were applied in this article for feature selection of the whole chromatograms, and the PSO was also used to tune the SVM parameters. As a case, a sample HM, that is, Xiangdan injection, was investigated. The predictive accuracy was fully evaluated and compared with those by other popular and reported methods. Furthermore, the confirmation on the independent predicting set exhibited that the predicted bioactivities were well consistent with the experimental values. The important potential application of the present model is to be extended to help search active fractions of other HMs.

[JAK2V617F mutation in the patients with myeloproliferative disorder and its relation with clinical characteristics].

This study was aimed to investigate the incidence of JAK2V617F mutation in BCR-ABL negative patients with myeloproliferative disorders (MPD) and its relation with clinical characteristics of MPD. The sensitive and specific test for JAK2V617F mutation was established for improving diagnosis level in Gansu province. 47 BCR/ABL negative MPD patients and 12 healthy people were enrolled in this study. Allele specific polymerase chain reaction (AS-PCR) was used to amplify the exon 12 of JAK2 gene which harbours V617F mutation. The PCR products were identified by DNA sequencing. And its relation with clinical characteristics of MPD was analyzed also. The results indicated that the incidence of JAK2V617F positive mutation in 47 patients with BCR-ABL negative MPD was 74.5 % (35/47), including 83.9 %(26/31) in patients with polycythemia vera (PV), 60 % (9/15) in patients with essential thrombocythemia (ET), only in one patient with idiopathic myelofibrosis (IMF). In PV group, the patients with JAK2V617F positive mutation had higher counts of WBC and Plt than patients with JAK2V617F negative mutation. In ET group, the patients with JAK2V617F positive mutation had higher WBC count and Hb level than those in the patients with JAK2V617F negative mutation with tendency of suffering from complications such as hepatosplenomegaly, haemorrhage and thrombosis. It is concluded that JAK2V617F mutation is more frequent in BCR-ABL negative patients with MPD, the AS-PCR method is sensitive and specific for detection of the mutation and may successfully use in clinical examination.

[Association of CD38 gene polymorphism with pathogenesis of chronic myeloid leukemia].

This study was aimed to investigate the distribution of CD38 gene 184 locus allele frequency in chronic myeloid leukemia (CML) and its relation with genetic susceptibility of CML. 100 cases of CML were enrolled in patient group; 200 cases of nonhematologic diseases and nontumor diseases were enrolled in control group. The CD38 gene 184 locus polymorphism was detected by PCR-RFLP, the difference of genotypic frequencies in patient and control groups was analyzed by χ(2) test and Fisher exact probability test, the risk of genotype induced leukemia was expressed by odds ratio (OR) and 95% confidence interval (CI). The results showed that the distribution of CD38 gene 184 locus G/G, G/C, C/C genotypes was no significantly different between patients and control groups (p = 0.072). The wild type C/C was used as reference, the distribution of variant G/C genotype frequency in CML group was different statistically from control group (p = 0.032, OR value 0.517, 95%CI 0.283 - 0.947); the C allele frequency was used as reference, the G allele frequency in CML group was higher than that in control group (p = 0.028, OR value 0.597, 95%CI 0.377 - 0.94). It is concluded that the CD38 gene 184 locus G allele may be an protective gene against CML, and reduce the risk of CML relapse.

Better synchronizability in generalized adaptive networks.

In this paper, to study the interaction between network structure and dynamical property in the context of synchronization, a previously proposed adaptive coupling method is generalized where the coupling strength of a node from its neighbors not only develops adaptively according to the local synchronization property between the node and its neighbors (dynamical part) but also is modulated by its local structure, degree of the node with the form 1/k(i)(alpha) (topological part). We can show both numerically and analytically that the input coupling strength of the network after adaptation displays a power-law dependence on the degree, k(-theta), where the exponent theta is controlled by alpha as theta=(1+alpha)/2. Compared to the original adaptive coupling method, after the addition of modulation, the distribution of the node's intensity is tunable and can be more homogenous with alpha approximately 1, which results in better synchronizability. It is also found that the synchronization time can shrink greatly. Our theoretical work in the context of synchronization provides not only a deeper understanding of the interplay between structure and dynamics in real world systems, such as opinion formation and concensus, but also potential approaches to manipulate the global collective dynamics through local adaptive control.

[Studies on the chemical constituents of Dryopteris fragrans].

OBJECTIVE: To study the chemical constituents of Dryopteris fragrans. METHODS: The constituents of CHCl3-soluble portion and ethyl acetate-soluble portion from the alcohol extract were isolated and purified by means of chromatography. All the compounds were identified by their physical characteristics and spectral features. RESULTS: Five compounds were isolated and identified as beta-sitosterol (I), rutin (II), quercetin (III), quercetin-3-O-beta-D-pyranglucoside (IV) and 5,7-dihydroxy-2-hydroxymethyl chromone (V). CONCLUSION: Compounds II - V are isolated from this plant for the first time.

[Studies on phloroglucinol derivatives of Dryopteris fragrans L].

OBJECTIVE: To study the phloroglucinol derivatives of Dryopteris fragrans. METHODS: Isolation and purification were carried out on repeated silica gel, Sephadex LH-20 column chromatography and prepare HPLC. The structures of the compounds were determined by physicochemical properties and spectral analysis. RESULTS: Four compounds were isolated and identified as aspidin PB (I), dryofragin (II), aspidinol (III), aspidin BB (IV). CONCLUSION: Compounds IV is isolated from this plant for the first time.

[Study on terpene of Dryopteris fragrans L].

OBJECTIVE: To study the terpene of Dryopteris fragrans. METHODS: Isolation and purification were carried out on repeated silica gel, Sephadex LH-20 column chromatography and prepare HPLC. The structures of the compounds were determined by physicochemical properties and spectral analysis. RESULTS: Four compounds were isolated and identified as 10-hydroxyl-15-oxo-alpha-cadinol (I), albicany acetate (II), alpha-cadinene (III), albicanol (IV). CONCLUSION: Compounds I is isolated from this plant for the first time.