Histone deacetylase (HDAC) is usually abnormally overexpressed, which mainly leads to the transcriptional repression of tumor suppressor genes. Histone deacetylase inhibitors (HDIs) exert anti-tumor biological effects by regulating nucleosome structure, inhibiting HDAC activity, and controlling the expression of tumor suppressor genes. There are currently 5 drugs on the market, but only for peripheral T-cell lymphoma and cutaneous T-cell lymphoma. In solid tumors, most of the HDAC inhibitors used have failed to achieve effective therapeutic effects. Phosphoinositide 3-kinase (PI3K) is the starting node of the PI3K-AKT-mTOR signaling pathway, which plays a very important role in the proliferation, migration, invasion, and differentiation of tumor cells. The abnormal activation of PI3K is closely related to the occurrence and development of tumors, and the combined use of HDAC and PI3K inhibitors and HDAC/PI3K dual-target inhibitors show synergistic anticancer activity. This article introduces the anti-tumor clinical and preclinical research progress of representative HDAC inhibitors and PI3K inhibitors, as well as HDAC/PI3K dual-target inhibitors.

Phytochemical investigation on the EtOH extract from the aerial part of Callicarpa kwangtungensis led to the isolation and characterization of 10 caffeoyl phenylethanoid glycosides, 2'-acetylacteoside (1), tubuloside E (2), acteoside (3), tubuloside B (4), isoacteoside (5), alyssonoside (6), 2'-acetylforsythoside B (7), brandioside (8), forsythoside B (9), and poliumoside (10). Compound 4 was isolated from the plants of Verbenaceae,and 6 was obtained from the Callicarpa genus, for the first time, while compounds 1, 2, 5 and 7 were firstly reported from the plant.
Caffeic Acids ; chemistry ; isolation & purification ; Catechols ; chemistry ; isolation & purification ; Chromatography, High Pressure Liquid ; Ethanol ; chemistry ; Glucosides ; chemistry ; isolation & purification ; Glycosides ; chemistry ; isolation & purification ; Phenols ; chemistry ; isolation & purification ; Verbenaceae ; chemistry

The effects of Cinnamon granules on pharmacokinetics of berberine in Rhizoma Coptidis granules in healthy male volunteers, and the compatibility mechanism of Jiao-Tai-Wan (JTW) composed of Rhizoma Coptidis granules and Cinnamon granules were investigated. The concentration of berberine in plasma of healthy male volunteers was determined directly by high performance liquid chromatography (HPLC) after an oral administration of Rhizoma Coptidis granules alone or combined with Cinnamon granules (JTW). The plasma concentration-time curves of berberine were plotted. The data were analyzed with Drug and Statistics (DAS) 2.0 pharmacokinetic program (Chinese Pharmacology Society) to obtain the main pharmacokinetic parameters. The results showed that the plasma concentration-time curve of berberine was described by a two-compartment model. The C(max), T(max), t(1/2) and CLz/F of berberine in Rhizoma Coptidis granules were 360.883 μg/L, 2.0 h, 3.882 h, 119.320 L·h(-1)·kg(-1) respectively, and those of berberine in JTW were 396.124 μg/L, 1.5 h, 4.727 h, 57.709 L·h(-1)·kg(-1) respectively. It was suggested that Rhizoma Coptidis granules combined with Cinnamon granules could increase the plasma concentration of berberine, promote berberine absorption and lengthen the detention time of berberine in healthy male volunteers.

Nine compounds were isolated from the n-butanol fraction of 95% ethanol extract of the fruit of Alpinia oxyphylla Miq. with a combination of various chromatographic approaches, including MDS resin, silica gel, reverse phase C18 and preparative HPLC. On the basis of spectroscopic data analysis, they were elucidated as (1R, 4R, 10R)-1β, 4α-dihydroxy-11, 12, 13-trinor-5, 6-eudesmen-7-one (1), 1β, 4β-dihydroxy-11, 12, 13-trinor-8, 9-eudesmen-7-one (2), oxyphyllenone A (3), oxyphyllenone B (4), rhamnocitrin (5), staphylionoside D (6), benzyl-1-O-β-D-glucopyranoside (7), 2-O-β-D-glucopyranosyl-(1S)-phenylethylene glycol (8), and (S)-1-phenylethyl-β-D-glucopyranoside (9). Among them, compound 1 is a new sesquiterpene, named as oxyphyllenone C; compounds 8 and 9 are new natural products; compounds 2 and 6 were isolated from the genus Alpinia for the first time, and compound 7 was isolated from A. oxyphylla for the first time.
1-Butanol ; Alpinia ; chemistry ; Chromatography, High Pressure Liquid ; Fruit ; chemistry ; Phytochemicals ; chemistry ; isolation & purification ; Sesquiterpenes ; chemistry ; isolation & purification

Objective:To know the effect of counseling on personality feature and self-conscious symptom of college students with internet addiction disorder (IAD).Methods:Before and after counseling,38 students with IAD in Guangdong Medical College (GDMC)were measured by Sixteen Personality Factor Questionnaire (16PF)and Symptom Check List 90 (SCL-90).Results:After counseling,these students with IAD had higher scores of 4 factors in 16PF(sociability,intelligence,perseverance,autonomy),had lowerer scores of 5 factors in 16PF (daring,suspicion,illusion,anxiety,tensity),and had lower scores of 6 factors in SCL-90 (force,interpersonal sensitivity,depression,anxiety,hostility,terror)(P＜0.05 or P＜0.01).Conclusion:To college students with IAD, counseling could enhance their positive personality features,weaken their negative personality feature and mitigate their self- conscious symptom.

Objective To analyze our clinical results of head and neck reconstruction using microsur- gical free flap transfer techniques.Methods The free flap donor sites with long vascular pedicle and large diameter of vessel were routinely chosed,and chose receipt vessels with large diameter and proper position, and perform vessel ananstomosis under surgical loups instead of microscope.The un-buried free flap with a mo- nitoring window were harvest,and do double venous anastomoses in some flaps to ensure adequate venous out- flow.Results From May 1999 to March 2005,1066 consecutive free flap transfers were used to reconstruct head and neck defects.The overall success rate of free flap was 98.3%.The vessel thrombosis rate was 3.1%,and the flap salvage rate was 45.5%.Conclusion Head and neck reconstruetion using microsurgi- cal free flap transfer technique is safe and reliable,and good clinical results can be obtained.

OBJECTIVETo introduce and evaluate the procedure and the effect of localized management of sinus floor (LMSF), bone graft and simultaneous implant placement with trephine bur in maxillary posterior region.

METHODS24 patients without enough alveolar bone height received LMSF, bone grafting and implants placement were carried out simultaneously.The autogenous bone were harvested by trephine bur in situ. Patients were followed up after 1 week, 1, 3 and 6 month.

RESULTSThere was no implant loose or lost and maxillary antritis. 6 months postoperatively, bone graft reformed to new bone seen in X-ray films, sinus floors were augmented and reached the requirements of dental implants. The implant osseointegrated tightly with new bone which was satisfactory to second-step prosthesis after implant placement of 6 months later.

CONCLUSIONSThe method enlarges the indication of dental implants and avoids operation of harvesting autogenous bone in other site. It is simple and valuable to clinical application.

Adult ; Alveolar Ridge Augmentation ; methods ; Bone Transplantation ; Dental Implantation, Endosseous ; methods ; Dental Implants ; Female ; Humans ; Male ; Maxillary Sinus ; surgery ; Middle Aged

Suspension cultures cell of Sorbus aucuparia (SASC) was used as materials, the changes of physiological and biochemical indexes of SASC after treatment with yeast extract (YE) were detected, and the synthetic mechanism of secondary metabolites in SASC treated with YE was preliminarily explored. The results were as follows: under the assay conditions, SASC was induced to synthesize five biphenyl compounds, and these compounds content changed differently with induction time prolonging; YE treatment inhibited cell growth, the culture medium pH was gradually reduced after treatment; water-soluble protein content showed a trend of slow decline, which was significantly increased in YE treatment group (YE group) compared with the control group (CK group), the maximum relative content was 147.76% in contrast with CK group; both YE group and CK group were extracellular Ca2+ flow influx, but the YE group flow was significantly slow than CK group. The results indicate that YE induced the cells in a stress state, which was not conducive to the growth of cells and forced the cells to synthesize biphenyl compounds against external stress; water-soluble protein may serve as intracellular enzymes involved in the synthesis of compounds regulation; Ca2+ may as signal molecule mediate cell signal transduction respond to YE stress.
Cell Culture Techniques ; instrumentation ; methods ; Culture Media ; chemistry ; metabolism ; Saccharomyces cerevisiae ; chemistry ; Secondary Metabolism ; Sorbus ; growth & development ; metabolism

Objective To compare the diagnostic value of myocardial perfusion imaging (MPI) and 64 multi-slice spiral CT (64-MSCT) for coronary artery disease (CAD). Methods Fifty-two patients with suspected or known CAD were included in the study. Each patient underwent both stress and rest MPI,MSCT as well as conventional coronary angiography (CAG) within 1 month. The stress and rest MPI were scored by a 5-grade criteria (0 ～ 4) based on 17 coronary artery segments. The difference between summed stress and rest scores ＞ 1 was defined as myocardial ischemia. Stenosis in one main vessel or one main branch of the main vessel ≥50% was defined as myocardial ischemia by MSCT. CAG was used as the reference for comparison. Statistical analysis was performed using SPSS 13. 0 software. Kappa value was used to test the accordance of MPI and MSCT results. X2 test was used to evaluate the difference between MPI and MSCT results. Results The patient-based sensitivity, specificity, positive and negative predictive values and accuracy of MPI and MSCT for the diagnosis of CAD were 86.7% (26/30), 77.3% ( 17/22),83.9% (26/31), 81.0% ( 17/21), 82.7% (43/52) and 83.3% ( 25/30), 86.4% ( 19/22), 89.3%( 25/28), 79.2% ( 19/24), 84.6% (44/52), respectively. The vessel-based sensitivity, specificity, positive and negative predictive values and accuracy of MPI and MSCT were 74.5% (38/51), 81.0% (85/105 ), 65.5% (38/58), 86.7% ( 85/98), 78.8% ( 123/156 ) and 90.2% (46/51 ), 88.6% ( 93/105 ),79.3 % (46/58), 94.9% (93/98), 89.1% ( 139/156), respectively. There was no statistically significant difference between MPI and MSCT for either patient or lesion-based diagnosis (X2 =0.44, 0.21, both P ＞0.05 ). 96.0% (24/25) patients with both abnormal MPI and MSCT positive were valified by CAG while 83.3% (15/18) patients with both MPI and MSCT negative were excluded by CAG. Conclusions Both MPI and MSCT are reliable diagnostic modalities for CAD. They also provide complementary diagnostic value to each other.

ObjectiveTo explore the effect of synthesized rehabilitation on detoxification addicts.Methods100 detoxification addicts were randomly divided into the rehabilitation group and control group with 50 cases in each group. Cases of the rehabilitation group were treated with "ten-step" rehabilitation treatment, but that of the control group did not. The rehabilitating treatment included cognitive psychotherapy, behavioral therapy, family treatment, social skill training and etc. The effects of two groups were evaluate with Symptom Checklist-90 (SCL-90) scale.ResultsExcept hostility, other factorial scores of the rehabilitation group including positive items, somatization, obsession, interpersonal sensitivity, depression, phobia, paranoid and psychotic factors were significantly higher than that of the control group (P<0.05～0.01).ConclusionThe synthesized rehabilitation can obviously improve the psychology of detoxification addicts.