The antinociceptive and anti-alpha-glucosidase effects of glucosides from Hemiphragma heterophyllum Wall.

Hemiphragma heterophyllum Wall. is commonly used in traditional Yi herbal medicine for treating bellyache and toothache. In the current study, an unreported monoterpene glucoside, (S)-thymoquinol O-(6-O-oleuropeoyl)-ß-d-glucopyranoside (1), together with 11 known glucosides were obtained from the whole herb of H. heterophyllum. Their structures were determined based on a detailed analysis of spectroscopic data and acid hydrolysis and methanolysis reactions. Bioassay results showed that compounds 1 and 10 at 40 mg/kg exhibited significant antinociceptive activity in the acetic acid-induced writhing model, with inhibitions of 59.80% and 64.07%, respectively. Moreover, five of the isolates showed moderate anti-α-glucosidase activities with IC50 values ranging from 5.67 to 46.16 µM.

Triterpenoid saponins from Psammosilene tunicoides and their antinociceptive activities.

Herein, five undescribed oleanane-type triterpenoid saponins, namely, psammosaponins A-E, along with nine known compounds, were isolated from the roots of Psammosilene tunicoides. Moreover, part of the ethanolic extract of P. tunicoides was acid-hydrolyzed and three aglycones were isolated from the resulting hydrolysate. The structures of all compounds were established through extensive analysis involving 1D and 2D NMR experiments, HRESIMS measurements, chemical derivatization, and comparison of spectroscopic data with the values reported in the literature. In all, 10 of the isolated saponins and the three aglycones were evaluated in the acetic acid-induced writhing model for their antinociceptive activity. At a dose of 40 mg/kg, these compounds exhibited significant inhibitory effects on the mouse writhing response, with inhibitions ranging from 31.9% to 79.3%. In addition, the structure-activity relationships of the isolates were discussed. Among the isolates, quillaic acid 3-O-glucuronide and 16α-hydroxygypsogenic acid showed better antinociceptive activity with inhibitions of 79.3% and 73.7%, respectively. Both isolates also exhibited antinociceptive activities in hot plate and formalin tests on mice. Their antinociceptive mechanism was explored in lipopolysaccharide-stimulated RAW 264.7 cells. These isolates could significantly inhibit the production of nitric oxide and interleukin-6 and downregulate the expression levels of inducible NO synthase, COX-1, and COX-2.

Multiple-targeting NMR signal selection by optimal control of nuclear spin singlet.

Selectively probing specific molecules in complex mixtures with nuclear magnetic resonance promises new insights into molecular structures or molecular interaction. Such a study often can be further facilitated when two or more objects in chemical moieties of interest can be precisely targeted. Herein, we proposed a novel method to implement the multiple-targeting signal selection by optimal control of the spin singlets of two or more targeted spin systems from one or more molecules. This method can endow the conventional nuclear magnetic resonance (NMR), magnetic resonance image (MRI) and magnetic resonance spectrum (MRS) with the multiple-targeting signal selectivity to selectively probe several targeted molecules and/or chemical groups simultaneously.

[Acupuncture based on meridian diagnosis for chronic atrophic gastritis].

OBJECTIVE: To compare the efficacy between acupoint selection of meridian diagnosis and regular acupoint selection for chronic atrophic gastritis (CAG). METHODS: A total of 70 cases of CAG were randomly divided into an observation group (35 cases, 5 cases dropped off) and a control group (35 cases, 5 dropped off). In the observation group, according to the hand diagnosis of meridians and the results of 80-channels energy determinator, based on the principle of child-mother relation acupoint combination, the luo-connecting point and back-shu points were added for excess syndrome, and the yuan-primary point, front-mu points and he-sea point of foot meridians were added for deficiency syndrome; in addition, the acupoints of the eight extraordinary meridians were added based on the nature of acupoints. In the control group, Zhongwan (CV 12), Neiguan (PC 6), Zusanli (ST 36) and Gongsun (SP 4) were selected as the primary acupoints, and additional acupoints were added according to syndrome differentiation. The two groups were treated twice a week (Tuesday and Thursday, respectively), totally for 6 months. Six months after treatment, the follow-up was conducted. The clinical symptom score, gastroenteropathy patient reported outcomes (PRO) scale score before treatment, after treatment and during follow-up as well as the score of pathological changes of gastric mucosa before and after treatment were compared between the two groups. RESULTS: After treatment and during follow-up, the clinical symptom scores and gastroenteropathy PRO scale scores were decreased in the two groups (P<0.01, P<0.001); at the follow-up, the gastroenteropathy PRO scale score in the observation group was lower than that in the control group (P<0.01). After treatment, the scores of pathological changes of gastric mucosa in the two groups were decreased (P<0.01), and the score in the observation group was lower than that in the control group (P<0.05). CONCLUSION: The acupoint selection of meridian diagnosis is superior to regular acupoint selection for CAG, which has better efficacy, more significant improvement on gastric mucosa pathology, and more stable long-term effect.

IRF1 up-regulates isg15 gene expression in dsRNA stimulation or CSFV infection by targeting nucleotides -487 to -325 in the 5' flanking region.

Interferon (IFN)-stimulated gene 15 (ISG15) encodes a ubiquitin-like protein that is heavily involved in immune response elicitation. As an important member of interferon regulatory factor (IRF) family, IRF1 can activate the expression of multiple genes, including the human optineurin gene (Sudhakar et al., 2013). In this study, a sequence in the promoter region of the optineurin gene was compared to the 5' flanking region of the porcine isg15 gene. Porcine IRF1 also possesses antiviral activity against several swine viruses (Li et al., 2015), but the mechanism is not well understood. Herein, we report that porcine IRF1 and ISG15 were up-regulated in porcine kidney (PK-15) cells following stimulation with double-stranded RNA (dsRNA) or classical swine fever virus (CSFV) infection. We also found that siRNA-mediated knockdown of IRF1 expression resulted in lower ISG15 expression in response to polyinosinic:polycytidylic acid [poly(I:C)] or CSFV infection. The overexpression of IRF1 resulted in ISG15 up-regulation. IRF1 was shown to translocate to the nucleus in response to dsRNA stimulation. To further identify the functional domain of the isg15 gene that promotes IRF1 transcriptional activity, firefly luciferase and ISG15 reporter systems were constructed. The results of the firefly luciferase and ISG15 reporter assay suggested that IRF1 mediates the up-regulation of ISG15. Nucleotides -487 to -325, located in the 5' flanking region of the isg15 gene, constituted the promoter region of IRF1. ChIP assay indicated that IRF1 protein was able to interact with the DNA in the 5'fr of isg15 gene in cells. As an innate immune response protein with broad-spectrum antiviral activity, the up-regulation of ISG15 mediated by IRF1 in porcine cells is reported for the first time. These results warrant further investigation into the antiviral activity of porcine IRF1 against reported swine viruses.

[Design and implementation of a long wavelength near infrared spectrometer based on MEMS scanning mirror].

Long Wavelength Near InfraRed (LW-NIR) spectrometer has wide applications. Miniaturization and low-cost are two major goals of the development of LW-NIR spectrometer in the industrial or research community. Under the background that having a trend of spectrometer miniaturization and integration, method and main problems involved in miniaturization of LW-NIR spectrometer through MEMS scanning mirror, such as the design strategy of the light-splitting optical system, selection considerations of the MEMS scanning mirror, design method of the preamplifier circuit, etc, have been presented in detail. A prototype of miniaturized LW-NIR spectrometer, with the spectrum range of detection of 900-2,055 nm, is designed and implemented using MEMS scanning mirror, InGaAs single detector unit with high sensitivity. Littrow optical layout is used for its light-splitting optical system, and the spectral resolution is between 9.4-16 nm at 1,000-1,965 nm detection wavelength range. The prototype is successfully applied in LW-NIR spectrum measurement on pure water and ethanol aqueous solution, and a forecast analysis on ethanol aqueous solution concentration is also demonstrated. Through adopting MEMS scanning mirror into the spectrometer system, the complexity of the mechanical scanning fixtures and its controlling mechanism is greatly reduced therefore the size of the spectrometer is reduced. Furthermore, due to MEMS scanning mirror technology, LW-NIR spectrometer with single InGaAs detector is achieved, thus the cost reduction of the NIR spectrometer system is also realized because the expensive InGaAs arrays are avoided.

[Effects of garlicin on the expression of transcription factor T-bet and GATA-3 in blood lymph cells in rats with allergic rhinitis].

OBJECTIVE: To investigate the effects of garlicin on the expression of transcription factors T-bet and GATA-3 in blood lymph cells of experimental rats with allergic rhinitis. METHODS: Thirty healthy SD rats were randomly divided into 3 groups, with 10 rats for each. Ten rats (pharmacological group) were sensitized and intranasally challenged by ovalbumin (OVA), aluminium hydroxide hydrate gel and Bordetella pertussis (B. pertussis) inactive microorganism suspension adjuvants, as the allergic rhinitis models, and then injection of garlicin (0.4 ml) intraperitoneally per day for 10 days. Ten rats in the control group were immunized as the pharmacological group, and then injection of physiological saline as equal volume as garlicin. Ten rats in the negative control group were investigated using physiological saline only. Plasma and lymph cells were separated from 2 ml blood which was extracted from rat heart. Enzyme linked immunosorbent assay (ELISA) was utilized to detect the levels of plasma IL-4 and IFN-γ, and RT-PCR was utilized to detect the expression of T-bet and GATA-3. RESULTS: The levels of IL-4 (x(-) ± s) were (6.292 ± 1.734), (14.252 ± 1.971), (4.916 ± 0.600) pg/ml, respectively, and the levels of IFN-γ were (24.338 ± 2.375), (12.364 ± 1.749), (16.136 ± 2.012) pg/ml, respectively, among the pharmacological, control and negative control groups. The plasma level of IL-4 in the pharmacological group rats was lower than that of control group rats (t = 4.23, P < 0.05), while there was no significant difference between the pharmacological and negative control group rats (t = 1.01, P > 0.05). The plasma level of IFN-γ was increased significantly in the pharmacological group rats when compared with the value of control group rats (t = 4.61, P < 0.05) and with the negative control group (t = 5.79, P < 0.05), respectively. There was no significant difference (t = 1.17, P > 0.05) in plasma level of IFN-γ in the control group rats when compared with the negative control group. Relative quantization of expression of GATA-3 (median) was 0.826, 1.029 and 0.474, and those of T-bet (median) were 1.245, 0.280 and 0.544, respectively, among the pharmacological, control and negative control groups. There were significant difference among 3 groups (chi² = 6.599, P = 0.019; chi² = 9.884, P = 0.007, respectively). Relative quantization of expression of GATA-3 in the control group rats was significantly higher than that in the negative control group and pharmacological group rats (chi² value were 10.113 and 2.384, respectively, all P < 0.05), and that of GATA-3 in the pharmacological group rats was increased as compared to the negative control group rats (chi² = 3.784, P < 0.05). The level of expression of T-bet in pharmacological group rats was elevated markedly with a significant difference as compared to both control (chi² = 16.021, P < 0.05) and negative control groups (chi² = 14.103, P < 0.05). CONCLUSIONS: Garlicin may upregulate the expression of T-bet dramatically and downregulate the expression of transcription factor GATA-3 in the experimental models of allergic rhinitis.

Retroperitoneal extraskeletal osteosarcoma: imaging findings and transarterial chemoembolization.

Extraskeletal osteosarcoma (EOS) is an uncommon and usually highly aggressive mesenchymal tumor. Retroperitoneal extraskeletal osteosarma (REOS) is exceedingly rare. Due to the rare nature of the disease, both the diagnosis and the management of REOS can be challenging. We present the clinical history, CT findings, angiographic manifestations, and use of transarterial chemoembolization for treatment in a case of REOS. To our knowledge, the angiographic features of and attempt at transarterial treatment of REOS have not been reported in the literature.

Use of intra-arterial chemotherapy and embolization before limb salvage surgery for osteosarcoma of the lower extremity.

We report our experience with the use of intra-arterial chemotherapy and embolization before limb salvage surgery in patients with osteosarcoma of the lower extremity. We evaluated the effect of this procedure on the degree of tumor necrosis and on the amount of blood loss during surgery. We reviewed the medical records of all patients who received intra-arterial chemotherapy and embolization before undergoing limb salvage surgery for osteosarcoma of the lower extremity at our institution between January 2003 and April 2008. Patient demographic, tumor characteristics, treatment details, postembolization complications, and surgical and pathological findings were recorded for each patient. We evaluated the operative time, estimated blood loss (EBL), and volume of blood transfusion during surgery and in the postoperative period in all patients in the study group. The same parameters were recorded for 65 other patients with lower extremity osteosarcoma who underwent limb salvage operation at our institution without undergoing preoperative intervention. The study included 47 patients (25 males and 22 females). Angiography showed that the tumors were hypervascular. Intra-arterial chemotherapy and embolization were performed successfully, resulting in a substantial reduction or complete disappearance of tumor stain in all patients. No major complications were encountered. At the time of surgery, performed 3-7 days after embolization, a fibrous edematous band around the tumor was observed in 43 of the 47 patients, facilitating surgery. The goal of limb salvage was achieved successfully in all cases. Percentage tumor necrosis induced by treatment ranged from 70.2% to 94.2% (average, 82.9%). EBL during surgery, EBL from drains in the postoperative period, total EBL, and transfusion volumes were significantly lower in the 47 study patients compared to the 65 patients who underwent surgery without preoperative treatment with intra-arterial chemotherapy and embolization. The mean operative time was also significantly less in the intervention group compared to the nonintervention group (73.2 vs. 88.5 min; p < 0.05). In conclusion, intra-arterial chemotherapy and embolization performed 3 to 7 days before limb salvage surgery in patients with lower extremity osteosarcomas can cause substantial tumor necrosis, reduce the EBL and transfusion requirements during surgery, and induce formation of a false capsule around the tumor, thus facilitating surgical excision of the tumors.

[Effect of garlicin on the serum levels of interleukin 4 and interferon gamma in allergic rhinitis model in rats].

OBJECTIVE: To investigate the effect of garlicin on the levels of interferon gamma (INF-gamma) and interleukin 4 (IL-4) in blood of allergic rhinitis rat model. METHODS: Thirty healthy female SD rats were randomly divided into 3 groups: control group, negative control group and experimental group, 10 rats for each group. Ten rats (experimental group) were sensitized and intranasally challenged by ovalbumin, aluminium hydroxide hydrate gel and Bordetella pertussis inactive microorganism suspension adjuvants, as allergic rhinitis models, and then injection of garlicin(0.4 ml) intraperitoneally per day for 10 days. Control group rats were immunized as experimental group, and then injection of physiological saline as equal volume as garlicin. Negative control group rats were investigated using physiological saline. Blood of intrajugular vein of rat was extracted for separated plasma Enzyme liked immunosorbent assay (ELISA) was utilized to detect the serum levels of IL-4 and IFN-gamma. RESULTS: The serum levels (x +/- s) of IL4 were (22.81 +/- 8.79) pg/L, (41.43 +/- 4.93) pg/L, (9.93 +/- 2.07) pg/L, and those of IFN-gamma were (22.32 +/- 11.20) pg/L, (11.35 +/- 2.45) pg/L and (21.69 +/- 5.93) pg/L, respectively, among experimental group, control group and negative control group. The serum level of IL-4 in experimental group rats was lower than value of control group rats (t = 3.22, P < 0.05), while higher than negative control group (t = 4.17, P < 0.05). The serum level of IFN-gamma was increased significantly in experimental group rats with significant difference when compared with value of control group rats (t = 3.84, P < 0.05), while no difference was shown between experimental group and negative control group (t = 1.47, P > 0.05). CONCLUSIONS: Garlicin could increase serum level of INF-gamma and decrease serum level of IL4 significantly in allergic rhinitis rat model. It played an important role on regulating serum levels of cytokines of Thl and Th2.

[Pathologic changes of palatopharyngeal muscle in patients with obstructive sleep apnea hypopnea syndrome].

OBJECTIVE: To study the pathologic changes of the palatopharyngeal muscles in patients with obstructive sleep apnea hypopnea syndrome (OSAHS), the role of the above muscles in OSAHS pathogenesis was discussed. METHODS: Thirty OSAHS patients receiving uvulopalatopharyngoplasty selected, and ten normal subjects without snoring as the control group. The successive longitudinal sections of palatopharyngeal muscle were stained for observing Troponin-I's content. All specimens were examined with transmission electronmicroscopy (TEM) and light microscopy. RESULTS: Twenty nine of 30 specimens obtained from OSAHS patients evaluated with TEM showed pathologic changes of different degrees. While 2 among 10 specimens in control group showed mild myofibril edema or hypertrophy, no pathologic changes shown in other specimens. Immunohistochemistrial results of all specimens sections stained for observing Troponin-I antibody have shown that negative grey degree value is 146.30 +/- 10.72 in study group and 107.50 +/- 4.81 in control group respectively. There is significant difference between these two groups (P < 0.05). The negative grey degree value of study groupl and study group2 are 143.12 and 148.80 respectively , no statistical difference (P > 0.05). CONCLUSIONS: Palatopharyngeal myelofibrosis may affect pharyngeal dilator muscles function, this could be one mechanism of upper airway collapsibility.