Chemical constituents from Notopterygium incisum and their anti-neuroinflammatory activity.

Phytochemical research on an extract of Notopterygium incisum yielded fifteen compounds (1-15), including four previously undescribed compounds (10-13). The structures of the unreported compounds were elucidated by spectroscopic and spectrometric data analysis such as 1D and 2D NMR, IR and HR-ESI-MS. Compounds 1-5 and 10-14 were isolated from N. incisum for the first time. 7S⁎,8R⁎-Phenethyl-(7-methoxy-8-isoeugenol)-ferulate (10), 7S⁎,8R⁎-p-hydroxyphenethyl-(7-methoxy-8-isoeugenol)-ferulate (11), 7S⁎,8R⁎-benzyl-(7-methoxy-8-isoeugenol)-ferulate (12) and p-hydroxyphenethyl-(4-benzoy-3-methoxy)-cinnamate (13) are the undescribed ferulic acid derivatives. Additionly, the anti-neuroinflammatory effects of compounds were evaluated in lipopolysaccharide (LPS)-induced BV2 cells. The pharmacological results showed that 6ß,10ß-epoxy-4α-hydroxy-guaiane (6), teuclatriol (7) and 7S⁎,8R⁎-p-hydroxyphenethyl-(7-methoxy-8-isoeugenol)-ferulate (11) inhibited the production and expression of nitric oxide (NO) in the LPS-induced BV2 cells in a concentration-dependent manner. Acorusnol (4), teucladiol (9), 7S⁎,8R⁎-benzyl-(7-methoxy-8-isoeugenol)-ferulate (12) and p-hydroxyphenethyl-(4-benzoy-3-methoxy)-cinnamate (13) only inhibited the release of NO at concentration of 20 µM. Moreover, 7S⁎,8R⁎-p-hydroxyphenethyl-(7-methoxy-8-isoeugenol)-ferulate (11) reduced the level of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in LPS-stimulated BV2 cells. The results demonstrated 7S⁎,8R⁎-p-hydroxyphenethyl-(7-methoxy-8-isoeugenol)-ferulate (11) could be a potential anti-neuroinflammatory agent and is worthy of further study.

AgSbF6-catalyzed C3 aza-Friedel-Crafts alkylation of N,O-acetals with indoles for the synthesis of N-α indole substituted pyrrolidine and piperidine derivatives.

An efficient approach to access chiral N-α indole substituted pyrrolidine and piperidine skeletons has been developed through a AgSbF6-catalyzed N-α aza-Friedel-Crafts alkylation of N,O-acetals 6a, 6b, 9, and 11a-11d with indoles. As a result, a series of 2,3-trans N-α indole substituted pyrrolidines 8a-8x and piperidines 10a-10j were prepared in moderate to excellent yields and with excellent diastereoselectivities (dr up to 99 : 1). Moreover, several 2,5-cis-N-α indole substituted pyrrolidine derivatives 12a-12k were synthesized according to this strategy with moderate to good yields and diastereoselectivities (dr up to 99 : 1).

Patients with Earlobe Crease May Associate with Lower Concentration of the Age-Suppressing Hormone Klotho.

OBJECTIVE: Earlobe crease (ELC) has been considered as a skin sign of atherosclerosis, and its pathophysiological mechanism is still unclear. Our study aims to test the hypothesis that ELC patients with lower serum levels of the age-suppressing hormone Klotho, which is not only associated with premature aging but also with endothelial dysfunction, may be associated with atherosclerosis. METHODS: A total of 135 patients aged 40-68 years underwent coronary angiography. According to the presence or absence of coronary heart disease (CAD) and ELC, they were divided into three groups: CAD group and ELC group (ELC group, n = 45); no ELC group (non-ELC group, n = 45). There was no ELC or CAD in the control group (control group, n = 45). Serum Klotho concentration was obtained by enzyme-linked immunosorbent assay (ELISA). RESULTS: The Klotho level in the ELC group was 365.6 ± 38.1 pg/mL, while the Klotho level in the non-ELC group was 568.8 ± 44.9 pg/mL. It is worth noting that the Klotho level of the ELC group was significantly lower than that of the non-ELC group (P < 0.001). The serum Klotho level of the control group was higher than that of the non-ELC group (593.3±45.3 vs 568.8±44.9 pg/mL, P = 0.702), but the difference was not statistically significant. Multiple logistic regression analysis showed that the Klotho level is a parameter that affects the appearance of ELC. CONCLUSION: Serum Klotho levels were considerably lower in patients with ELC. We concluded that the perturbations of Klotho in patients might be associated with ELC and with CAD.

Zn(OTf)2-catalyzed hydroamination of ynamides with aromatic amines.

The Zn(OTf)2-catalyzed hydroamination of ynamides 2a-2l with aromatic amines 1a-1r was developed. This protocol features broad substrate scope of aromatic amines, good functional group tolerance for ynamides, and excellent regioselectivities. As a result, a variety of substituted amidine compounds 3aa-3oa, 3ab-3al and 3pa-3rk were prepared in moderate to excellent yields and with high regioselectivities.

Another Look at Pyrroloiminoquinone Alkaloids-Perspectives on Their Therapeutic Potential from Known Structures and Semisynthetic Analogues.

This study began with the goal of identifying constituents from Zyzzya fuliginosa extracts that showed selectivity in our primary cytotoxicity screen against the PANC-1 tumor cell line. During the course of this project, which focused on six Z. fuliginosa samples collected from various regions of the Indo-Pacific, known compounds were obtained consisting of nine makaluvamine and three damirone analogues. Four new acetylated derivatives were also prepared. High-accuracy electrospray ionization mass spectrometry (HAESI-MS) m/z ions produced through MS² runs were obtained and interpreted to provide a rapid way for dereplicating isomers containing a pyrrolo[4,3,2-de]quinoline core. In vitro human pancreas/duct epithelioid carcinoma (PANC-1) cell line IC50 data was obtained for 16 compounds and two therapeutic standards. These results along with data gleaned from the literature provided useful structure activity relationship conclusions. Three structural motifs proved to be important in maximizing potency against PANC-1: (i) conjugation within the core of the ABC-ring; (ii) the presence of a positive charge in the C-ring; and (iii) inclusion of a 4-ethyl phenol or 4-ethyl phenol acetate substituent off the B-ring. Two compounds, makaluvamine J (9) and 15-O-acetyl makaluvamine J (15), contained all three of these frameworks and exhibited the best potency with IC50 values of 54 nM and 81 nM, respectively. These two most potent analogs were then tested against the OVCAR-5 cell line and the presence of the acetyl group increased the potency 14-fold from that of 9 whose IC50 = 120 nM vs. that of 15 having IC50 = 8.6 nM.

[ORMDL3 polymorphisms and their relationship with OPN and TGF-ß1 levels in children with asthma in Hunan, China: an analysis of 98 cases].

OBJECTIVE: To investigate ORMDL3 polymorphisms in children with asthma in Hunan, China, and to determine the relationship between ORMDL3 polymorphisms and serum osteopontin (OPN) and transforming growth factor-ß1 (TGF-ß1) levels. METHODS: Peripheral blood samples were collected in children with asthma (n=98; astma group) or without asthma (n=30; control group) from Hunan, China. The asthma group was subdivided into atopic (n=62) and non-atopic (n=36) subgroups. Single nucleotide polymorphism (SNP) analysis was performed, and serum OPN and TGF-ß1 levels were measured. RESULTS: There were no significant differences in genotype and allele frequencies of rs7216389 of the ORMDL3 gene between the asthma and control groups. The serum level of OPN in the asthma group was significantly higher than in the control group (P<0.05). Both the atopic and non-atopic subgroups showed increased serum levels of OPN compared with the control group (P<0.05). The serum level of TGF-ß1 in the atopic subgroup was significantly higher than in the control group (P<0.05). The serum levels of OPN and TGF-ß1 showed no significant differences in asthmatic children with different genotypes. The serum levels of OPN and TGF-ß1 were in a positive linear correlation in the asthma group (r=0.620; P<0.01) and its two subgroups (r=0.734, 0.649 respectively; P<0.01). CONCLUSIONS: In children from Hunan, China, the SNP (rs7216389) of ORMDL3 is not related to asthma susceptibility. OPN and TGF-ß1 may be involved in the development of asthma, and they are in a positive linear correlation. The SNP (rs7216389) of ORMDL3 does not influence the expression of OPN and TGF-ß1, suggesting that it may not be associated with airway remodeling.

[Effect of budesonide aerosol treatment on expression of glucocorticoid receptor and nuclear factor-κB in asthmatic mice].

OBJECTIVE: To study the effect of budesonide aerosol inhalation on the expression of glucocorticoid receptor (GR) and nuclear factor (NF)-κB in asthmatic mice. METHODS: Twenty-four healthy male BALB/c mice aged 6 to 8 weeks were randomly divided into three groups (n=8 each): normal saline (control group), asthma model (asthma group) and budesonide-treated asthma (BUD group). Asthma was induced by intraperitoneal injection of ovalbumin (OVA) and aluminium hydroxide suspension and aerosol inhalation of OVA solution. Mice were sacrificed 24 hours after the last challenge. Eosinophil count in the bronchoalveolar lavage fluid (BALF) was determined. Pathological examination of the lung tissues was performed and the expression levels of GR and NF-κB were measured by immunohistochemical analysis. RESULTS: Eosinophil count in the BALF was significantly higher in the asthma and BUD groups than in the control group (P<0.05). BUD treatment decreased eosinophil count in the BALF compared with the asthma group (P<0.05). The lung tissues in the BUD group showed a less severe infiltration of eosinophils and lymphocytes compared with the asthma group. The percentage of GR-positive cells in the asthma group decreased significantly compared with the control group (P<0.05), and the percentage of GR-positive cells in the BUD group increased significantly compared with the asthma group (P<0.05). Compared with the control group, the percentage of NF-κB-positive cells increased significantly in the asthma group (P<0.05), and the percentage of NF-κB positive cells in the BUD group was significantly reduced compared with the asthma group (P<0.05). CONCLUSIONS: The action mechanism of budesonide in treating asthmatic mice may be related to the upregulation of GR expression and the inhibition of NF-κB activity.

[Extraction and purification of isocorydine from Dicranostigma leptopodum].

OBJECTIVE: To optimize the conditions of extraction and purification of isocorydine from Dicranostigma leptopodum. METHODS: Extraction conditions of isocorydine were selected on the basis of orthogonal experimental design, the static adsorption/desorption experiments were used to evaluate the optimum resin. RESULTS: The optimum extraction parameters were as follows: the ratio of raw materials to solvent 1:15 (g/mL), extraction solvent 1% vitriol, the extraction three times and 1 h each time. LX28 resin exhibited higher adsorption efficiency. CONCLUSION: Under the above optimum conditions, the extraction yield of isocorydine is 0.88%. The purity of isocorydine can reach 85.34% with a yield rate of 68.64%.

[Mycoplasma pneumoniae infection and drug resistance in children: an analysis of 1026 cases].

OBJECTIVE: To investigate the Mycoplasma pneumoniae (MP) infection and drug resistance in children with respiratory tract infection and to provide a rational basis for the clinical diagnosis and treatment of MP infection. METHODS: Throat swabs were collected from 3529 children with respiratory tract infection, who visited the pediatric outpatient department or received treatment in the pediatric ward of our hospital from September 2010 to September 2011. The swabs were cultured to detect MP. The drug sensitivity of MP to azithromycin, roxithromycin, erythromycin, acetylspiramycin and clarithromycin was evaluated. RESULTS: Of the 3529 children with respiratory tract infection, 1026 (29.07%) were MP-positive. There were cases of MP infection in all four seasons of the year but infection rates in summer and autumn were significantly higher than in spring and winter (P < 0.05). The infection rate in females was higher than in males (30.43% vs 28.32%; P > 0.05). The infection rate was negatively correlated with age in these children, and there were significant differences in the infection rate among all age groups (P < 0.05). For macrolide antibiotics suitable for children, the cultured MP developed the highest resistance to roxithromycin, followed by erythromycin, acetylspiramycin, clarithromycin, and azithromycin, with significant differences among them (P < 0.01). CONCLUSIONS: MP infection rate is very high among children with respiratory tract infection. The incidence of MP infection is relatively low among school-age children and children are more susceptible to MP infection in summer and autumn than in spring and winter. Throat swabs should be cultured and drug sensitivity tests should be performed as early as possible in children with respiratory tract infection, so that proper intervention can be undertaken in time to reduce drug-resistant strains of MP.

[Study on the chemical constituents from Clematis brevicaudata].

OBJECTIVE: To study the chemical constituents from Clematis brevicaudata. METHODS: The compounds were isolated by column chromatography and their structures were elucidated through spectroscopic analysis (NMR). RESULTS: Eight compounds were isolated and identified as: palmitic acid (1), 1-docosanol (2), pentacosanoic acid-2', 3'-dihydroxypropyl ester (3), beta-sitosterol (4), daucosterol (5), a mixture of the trans-p-coumarate of the n-alkanols (6), 3,4-dihydroxy-trans coumatate ethyl ester (7), syringaresinol-O-D-glucopyranoside (8). CONCLUSION: All these compounds are obtained from Clematis brevicaudata for the first time.

[Chemical constituents from Pyrethrum tatsienense].

OBJECTIVE: To isolate and identify the chemical constituents from the whole plant of Pyrethrum tatsienense, which has been used as traditonal herb medicine in the treatment of some diseases. METHODS: The compounds were isolated by column chromatography and their structures were elucidated through spectroscopic analysis (NMR). RESULTS: Six compounds were isolated and identified as: linoeic acid, pinoresinol, (+)-pinoresinol-4'-O-beta-D- glucopyranoside, betulabuside A, dihydrosyringin. CONCLUSION: All these compounds were obtained from Pyrethrum tatsienense for the first time.

Isolation, identification, and comparison of four isolates of avian paramyxovirus serotype 2 in China.

Four Yucaipa-like viruses of avian paramyxovirus serotype 2 (APMV-2) were isolated in China from the imported Gouldian Finch (Chloebia gouldiae) and broilers in 1998-2002, and were named F4, F6, F8, and NK, respectively. Examined under electron microscope, the isolates were found to be round in shape and varying in size. The results of the hemagglutination inhibition test and indirect enzyme-linked immunosorbent assay (using monoclonal antibodies) showed some differences between the isolates and the reference strain Yucaipa. The isolates derived from chickens had a closer relationship to Yucaipa virus than did those of finches. Sequence comparison of the fusion gene and the haemagglutinin-neuraminidase gene showed similar results, although the variations were lesser among APMV-2 viruses in nucleotide and amino acid sequence. By sequence comparison, it was also revealed that at the molecular level the four virus strains belong to APMV-2, and that two of the strains were isolated from the same group of imported Gouldian Finches.

Triterpenoids from pyrethrum tatsienense.

Two novel and eight known triterpenoids were isolated from alcoholic extract of the whole plant of Pyrethrum tatsienense. The structures of new compounds were elucidated as olean-12-en-3beta,11alpha,16beta-triol-3-O-palmitate (1), ursa-12-en-3beta,11beta,16beta-triol-3-O-palmitate (2) by spectroscopic methods including intensive 2D NMR techniques (H1-H1 COSY, gHMQC, gHMBC) and FAB-MS, and the known compounds were identified on the basis of comparing their NMR data with those of corresponding compounds in the literature.

[Studies on the alkaloids from the herb of Corydalis adunca].

OBJECTIVE: To study the alkaloid constituents of Corydalis adunca. METHOD: The constituents were isolated on silica gel column and their structures were elucidated by IR, NMR, MS data. RESULT: Eight alkaloid compounds were isolated from alcohol extracts of the herb of C. adunca, and identified as dihydrosanguinarine (I), tetrahydrocolumbamine (II), 1,2,3,4-tetrahydro-7-methoxy-1-[(4-methoxy)phenyl]methyl-8-quinolinol (III), protopine (IV) and 6-acetonyl-5,6-dihydrosanguinarine (V). CONCLUSION: Five compounds were isolated from C. adunca for the first time.