Germacrane sesquiterpenes from leaves of Eupatorium chinense inhibit protein tyrosine phosphatase.

Three new germacrane-type sesquiterpene lactones (1-3) were isolated alongside seven known related congeners (4-10) from the leaves of Eupatorium chinense L. (Compositae). The planar structures of 1-3 were elucidated by their spectroscopic data, including 1D and 2D NMR spectra. The relative and absolute configurations of 1-3 were determined using NOESY experiments and electronic circular dichroism analyses. Compounds 1, 4, 5, and 7 inhibited protein tyrosine phosphatase (PTP) 1B activity with IC50 values of 25, 11, 28, and 24 µM, respectively. Among these, compound 4 exhibited an inhibitory effect on T-cell PTP (TCPTP) with an IC50 value of 25 µM. To our knowledge, this is the first study demonstrating the PTP inhibitory activity of the germacrane sesquiterpenes. The results show that compound 4 acts as an inhibitor of both PTP1B and TCPTP.

Cytokeratin 13, Cytokeratin 17, and Ki-67 Expression in Human Acquired Cholesteatoma and Their Correlation With Its Destructive Capacity.

OBJECTIVES: Cholesteatoma is a nonneoplastic destructive lesion of the temporal bone with debated pathogenesis and bone resorptive mechanism. Both molecular and cellular events chiefly master its activity. Continued research is necessary to clarify factors related to its aggressiveness. We aimed to investigate the expression of Ki-67, cytokeratin 13 (CK13) and cytokeratin 17 (CK17) in acquired nonrecurrent human cholesteatoma and correlate them with its bone destructive capacity. METHODS: A prospective quantitative immunohistochemical study was carried out using fresh acquired cholesteatoma tissues (n=19), collected during cholesteatoma surgery. Deep meatal skin tissues from the same patients were used as control (n=8). Cholesteatoma patients were divided into 2 groups and compared (invasive and noninvasive) according to a grading score for bone resorption based upon clinical, radiologic and intraoperative findings. To our knowledge, the role of CK17 in cholesteatoma aggressiveness was first investigated in this paper. RESULTS: Both Ki-67 and CK17 were significantly overexpressed in cholesteatoma than control tissues (P<0.001 for both Ki-67 and CK17). In addition, Ki-67 and CK17 were significantly higher in the invasive group than noninvasive group of cholesteatoma (P=0.029, P=0.033, respectively). Furthermore, Ki-67 and CK17 showed a moderate positive correlation with bone erosion scores (r=0.547, P=0.015 and r=0.588, P=0.008, respectively). In terms of CK13, no significant difference was found between cholesteatoma and skin (P=0.766). CONCLUSION: Both Ki-67 and CK17 were overexpressed in cholesteatoma tissue and positively correlated with bone resorption activity. The concept that Ki-67 can be a predictor for aggressiveness of cholesteatoma was supported. In addition, this is the first study demonstrating CK17 as a favoring marker in the aggressiveness of acquired cholesteatoma.

Morphological examination of upper airway in obstructive sleep apnea.

OBJECTIVES: An aim of this study was to assess the predictive power of an otorhinolaryngological examination of the upper airway to identify risk factors of obstructive sleep apnea syndrome (OSAS) in the patients. METHODS: We examined 141 consecutive patients with OSAS. The morphological features were assessed by the designated otorhinolaryngologist while the subjects were sitting relaxedly with tidal breathing. The bilateral nasal resistance was measured using the active anterior rhinomanometry during daytime wakefulness. RESULTS: The body mass index (BMI), fauces's narrowness, neck circumference, lowest oxygen saturation, tonsil size and modified Mallampati grade (MMP) showed the statistically significant correlations with the apnea-hypopnea index (AHI) of an index of apnoeseverity, however, the age, Epworth sleepiness scale (ESS), nasal resistance and retroglossal space were not significantly associated with the AHI. CONCLUSIONS: The upper airway morphology significantly associated with AHI are fauces's narrowness, tonsil size, and MMP, but not nasal resistance and retroglossal space.

Significance of a screening device (Apnomonitor 5) for sleep apnea syndrome.

OBJECTIVES: The objective was to evaluate the significance of a portable sleep-monitoring device (Apnomonitor 5, Chest Co., Tokyo, Japan) to diagnose sleep apnea syndrome (SAS). METHODS: The Apnomonitor 5 comprised an oronasal thermistor, a pulse oximeter, chest and abdominal belts to monitor the circumferences of the chest and abdomen, a microphone to monitor tracheal sound, a position detector, and an integrative unit. This screening device was commercially available and it had been used to diagnose SAS in our country. Twenty-two consecutive adults who attended Inazawa City Hospital who were suspected for SAS were prospectively enrolled and they undertook the standard polysomnography (PSG) and Apnomonitor 5 simultaneously. The designated polysomnographers analyzed the records of the PSG and Apnomonitor 5. These sleep and respiratory parameters of the devices were compared, the results of which were double-checked by the designated sleep specialist. RESULTS: The apnea-hypopnea index (AHI), apnea index, total number of apnea, and oxygen desaturation index obtained by the PSG and Apnomonitor 5 correlated significantly, whereas the averaged sleep time, total number of hypopnea, hypopnea index, and nadir oxygen saturation differed between the devices. The sensitivity of the Apnomonitor 5 versus PSG was 95% in the SAS patients with the AHI> or =15. CONCLUSIONS: The Apnomonitor 5 can be a sensitive and useful screening device for SAS especially in patients with the AHI> or =15.